US Pat. No. 10,336,957

ACID-FREE QUATERNIZED NITROGEN COMPOUNDS AND USE THEREOF AS ADDITIVES IN FUELS AND LUBRICANTS

BASF SE, Ludwigshafen (D...

1. A process for preparing a quaternized nitrogen compound, comprising:a) reacting a compound comprising at least one oxygen- or nitrogen-containing group reactive with an anhydride and at least one quaternizable amino group with a polycarboxylic anhydride compound to obtain an amide compound having at least one quaternizable amino group, and
b) quaternizing the at least one quaternizable amino group of the amide compound by reaction with a hydrocarbyl epoxide of formula (II) to obtain the quaternized nitrogen compound:

wherein the Ra radicals are each independently H or a hydrocarbyl radical having 1 to 10 carbon atoms;
wherein the plycarboxylic anhydride compound is a di-, tri- or tetracarboxylic anhydride comprising a hydrophobic hydrocarbyl radical having a number-average molecular weight (Mn) of 85 to 20,000,
and
wherein at least the quaternizing is performed in the absence of a protic solvent and a protic acid.

US Pat. No. 10,336,956

NATURAL-GAS PURIFICATION APPARATUS

MITSUBISHI HEAVY INDUSTRI...

1. A natural-gas purification apparatus for purifying natural gas by separating carbon dioxide from the natural gas, comprising:a natural-gas-liquid separator that liquefies and separates a part of natural-gas liquid by cooling the natural gas having an adjusted pressure;
a heater that heats the natural gas after the separation of the part of the natural-gas liquid by the natural-gas-liquid separator;
a plurality of carbon-dioxide separators that are arranged in series and separate carbon dioxide from the natural gas heated by the heater through carbon-dioxide separation membranes; and
a thermostatic chamber in which at least the carbon-dioxide separator disposed at a most downstream side among the plurality of carbon-dioxide separators is disposed and which adjusts a temperature of the carbon-dioxide separator disposed in the thermostatic chamber to a temperature not higher than a withstand temperature of the carbon-dioxide separation membrane but higher than a dew point of a remaining component of the natural-gas liquid inside the carbon-dioxide separator, wherein
the thermostatic chamber adjusts the temperature of the carbon-dioxide separator to the temperature higher than the dew point according to a composition of the natural gas figured out using analysis equipment.

US Pat. No. 10,336,955

FIXED BED GASIFIER AND METHOD OF GASIFICATION OF BIOMASS USING THE SAME

1. A gasifier comprising:a) a vertically disposed furnace body, the furnace body comprising a housing having a material and fuel inlet, a syngas outlet, a first oxygen/vapor nozzle, and a slag outlet; and a chamber having a clearance zone and a fixed bed zone;
b) a monitoring unit; and
c) a first microwave plasma generating device and a second microwave plasma generating device;wherein:the slag outlet is disposed at a bottom of the furnace body;
the monitoring unit is disposed close to the syngas outlet;
the chamber is defined by the housing;
the material and fuel inlet is disposed between the clearance zone and the fixed bed zone, and is configured for introducing biomass to the chamber;
the fixed bed zone contains the biomass and is configured for gasifying the biomass to yield a syngas;
the clearance zone is disposed above the material and fuel inlet and the fixed bed zone, and is devoid of the biomass;
the clearance zone is configured for receiving the syngas;
the first microwave plasma generating device is disposed around the fixed bed zone, and is adapted to supply a first microwave plasma to the fixed bed zone; and
the second microwave plasma generating device is disposed around the clearance zone, and is adapted to supply a second microwave plasma to the clearance zone.

US Pat. No. 10,336,954

COMPOSITIONS AND METHODS FOR INHIBITING FOULING IN HYDROCARBONS OR PETROCHEMICALS

BL TECHNOLOGIES, INC., M...

1. An antifoulant composition for inhibiting fouling on structural parts of a system exposed to a fluid hydrocarbon or petrochemical stream, said antifoulant composition comprising (1) at least one polyalkylene anhydride ester (“PAAE”) dispersant, wherein said dispersant is a polyisobutenyl succinic anhydride derived ester (“PASAE”) with a molecular weight, Mw, of about 1,000 to about 25,000, wherein said polyisobutenyl succinic anhydride ester (“PASAE”) includes a polyol moiety, wherein said polyol moiety is represented by the formulawherein R is a polyisobutenyl moiety, said dispersant providing a stable dispersion when mixed with said fluid hydrocarbon or petrochemical stream, wherein said fluid hydrocarbon or petrochemical stream comprises heavy crudes or crude blends,wherein said at least one structural part is selected from the group consisting of hydrocarbon or petroleum storage units, heat exchangers, piping, pumps, flow meters, valves, desalters, preheat furnaces, furnaces, coker preheaters, cokers, distillation columns, fractionation columns, atmospheric columns, pipe stills, debutanizers, reactors, fluid catalytic cracking units, fluid catalytic cracking slurry settlers, hydrocracking units, steam cracking units, thermal cracking units, visbreakers, reflux units, condensers, and scrubbers.

US Pat. No. 10,336,953

OPTIMIZATION OF A DEASPHALTING PROCESS WITH THE AIM OF PRODUCING A FEED FOR A CARBON BLACK UNIT

IFP Energies nouvelles, ...

1. A process for the production of a composition suitable for use as a feed for the production of carbon black, comprising vacuum distilling an atmospheric residue in order to produce at least one vacuum distillate fraction and at least one vacuum residue fraction, subjecting said vacuum distillate fraction to at least the following two steps in succession:1) fluid catalytic cracking, producing a FCC residue,
2) filtration of fine solid particles contained in said FCC residue obtained from cracking 1), resulting in a filtrate containing less than 300 ppm of particles below 10 microns;
deasphalting said vacuum residue fraction without hydrotreatment, resulting in a deasphalted vacuum residue fraction, at least a portion thereof being mixed with at least a portion of said filtrate obtained in the filtration 2) in order to form said composition.

US Pat. No. 10,336,952

MIXING DEVICE FOR A DOWN-FLOW HYDROPROCESSING REACTOR

Chevron U.S.A. Inc., San...

1. A mixing device for a multi-bed down-flow catalytic reactor, the mixing device comprising:a. a top plate having an inner surface and a periphery;
b. a base plate extending parallel to the top plate, the base plate having an inner surface, a periphery, and a base plate aperture, wherein the top and base plates are separated by a distance to define an interior region of the mixing device;
c. a plurality of inwardly-directed vanes contained within the interior region of the mixing device extending perpendicular to and interposed between the inner surfaces of the top and base plates, wherein the vanes are inwardly-directed from the periphery of the top and base plates toward the base plate aperture and are spaced around the area extending from the base plate aperture to the periphery of the top and base plates; and
d. a mixing region;
wherein, the mixing device does not include a weir ring extending from the inner surface of the base plate or a bubble cap extending from the inner surface of the top plate.

US Pat. No. 10,336,951

DESALTER EMULSION SEPARATION BY HYDROCARBON HEATING MEDIUM DIRECT VAPORIZATION

ExxonMobil Research and E...

1. A petroleum desalting process which comprises:mixing a crude oil to be desalted with desalting water and passing the mixture of oil and water to a desalter vessel to form (i) a settled water layer containing salts dissolved from the oil in the lower portion of the vessel, (ii) a settled supernatant, desalted oil layer in the upper portion of the vessel and (iii) an emulsion layer formed from the oil and the water and comprising emulsified oil and water, between the settled water layer and the settled oil layer,
removing a stream of the emulsion from the emulsion layer,
contacting the removed emulsion stream with a hydrocarbon heating medium to transfer heat from the heating medium to the emulsion to break the emulsion and vaporize water from the emulsion.

US Pat. No. 10,336,950

ANTIFOULING AND HYDROGEN SULFIDE SCAVENGING COMPOSITIONS AND METHODS

ECOLAB USA INC., St. Pau...

1. A composition, comprising:a Michael acceptor selected from the group consisting of acrylic acid, acrylamide, methacrylate, dimethyl maleate, crotonaldehyde, 3-butene-2-one, and any combination thereof; and
one or more compounds of formula (I),

wherein
R1, R2, and R3 are each independently selected from the group consisting of hydrogen, alkylenyl, alkenylenyl, alkynylenyl, alkyl, alkenyl, and alkynyl, wherein said alkylenyl, alkenylenyl, alkynylenyl, alkyl, alkenyl, and alkynyl are each independently, at each occurrence, substituted or unsubstituted with one or more suitable substituents;
k, l, and m are each independently an integer selected from the group consisting of 0 to 25, wherein k+l+m is >0; and
x, y, and z are each independently an integer selected from the group consisting of 0 and 1, wherein x+y+z is 1, 2, or 3;
provided that:
when x is 0, R1 is hydrogen, alkyl, alkenyl, or alkynyl; and when x is 1, R1 is alkylenyl, alkenylenyl, or alkynylenyl;
when y is 0, R2 is hydrogen, alkyl, alkenyl, or alkynyl; and when y is 1, R2 is alkylenyl, alkenylenyl, or alkynylenyl;
when z is 0, R3 is hydrogen, alkyl, alkenyl, or alkynyl; and when z is 1, R3 is alkylenyl, alkenylenyl, or alkynylenyl; and
when x is 1, y is 1, z is 1, k is 1, l is 1, and m is 1, then R1, R2, and R3 are not simultaneously unsubstituted C2-alkylenyl.

US Pat. No. 10,336,949

OXIDATION PROCESS

MERICHEM COMPANY, Housto...

1. A method for regenerating a caustic solution comprising:providing a rich caustic liquid containing mercaptans;
mixing the rich caustic liquid with a liquid catalyst to form a liquid caustic catalyst admixture;
directing the liquid caustic catalyst admixture into a bottom section of a vertical column configured to cause the liquid caustic catalyst admixture to flow upward inside the column;
injecting an oxygen containing gas into the liquid caustic catalyst admixture to form a gas liquid mix that flows upward inside the column entering a first reaction zone;
oxidizing the mercaptans to disulfide oil in the first reaction zone forming an oxidized gas liquid mix;
directing the oxidized gas liquid mix into a conduit positioned between a top tray and a bottom tray such that a liquid mix of disulfide oil and caustic exits the conduit onto an upper surface of the top tray that is fixedly attached to an upper section of the column;
directing the liquid mix of disulfide oil and caustic into a shroud connected to a lower surface of the top tray where the liquid mix of disulfide oil and caustic contacts a bundle of vertical hanging fibers such that the liquid mix of disulfide oil and caustic flows down individual fibers in the bundle and into a second reaction zone;
maintaining the second reaction zone as a gas continuous phase comprising from about 20% to about 100% by volume vapor;
oxidizing mercaptans in the liquid mix of disulfide oil and caustic while the liquid mix of disulfide oil and caustic flows down the fibers in the second reaction zone to form a regenerated caustic and disulfide oil admixture;
collecting the regenerated caustic and disulfide oil admixture on the bottom tray to allow separation of the disulfide oil from the regenerated caustic;
removing an off gas stream from the upper section; and
separately removing from the column a continuous stream of disulfide oil and a stream of regenerated caustic.

US Pat. No. 10,336,948

CATALYTIC CRACKING PROCESS ALLOWING IMPROVED UPCYCLING OF THE CALORIES FROM THE COMBUSTION FUMES

IFP ENERGIES NOUVELLES, ...

1. Process comprising:catalytic cracking of heavy hydrocarbon cuts wherein said heavy hydrocarbon cuts are VGO or atmospheric residue, using a fluidized bed catalytic cracking unit comprising:
a reaction section with an upward flow or with a downward flow, and
a catalyst regeneration section wherein said catalyst regeneration section consists of combustion of a coke deposited on a catalyst in the reaction section by combustion air, wherein said catalyst regeneration section produces flue gas that exchange calories inside a waste heat boiler, the flue gas from the waste heat boiler is introduced in an electric precipitator (ESP), then in an economizer (ECO) that allows for the production of low pressure superheated steam (LPSH) from low pressure water (LPBFW), and for the production of high pressure superheated water (HPBFW) from high pressure water,
a cat cooler wherein said cat cooler is a fluidized bed exchanger suitable for generating high-pressure steam (HPS) from calories directly contained on a hot catalyst in a process of regeneration,
wherein said combustion air in said process is preheated to a temperature of between 200 and 350° C. by a heat exchange using regeneration fumes collected downstream of a waste heat boiler and upstream of an economizer,
wherein said regeneration fumes at this location are at a temperature of between 300° C. and 650° C., and
wherein the excess calories supplied by the combustion air are converted to high-pressure steam of between 45 and 100 bar at a level of an external exchanger on hot catalyst collected at said cat cooler.

US Pat. No. 10,336,946

CATALYTIC PYROLYSIS METHOD AND APPARATUS

1. A process comprising:passing to a feed mixture through a line reactor, the mixture comprising 100 parts by weight heavy oil (API<22.3), from about 5 to 100 parts by weight water, and from about 1 to 20 parts by weight solid catalyst particulates comprising a mineral support and an oxide or acid addition salt of a Group 3-16 metal;
heating the feed mixture in the reactor at a temperature, pressure, and for a period of time sufficient to produce a pyrolyzate vapor phase at an exit from the reactor condensable to form an oil phase lighter than the heavy oil, wherein the mixture comprises an emulsion of the oil, water, and catalyst particulates.

US Pat. No. 10,336,945

PROCESS AND APPARATUS FOR DECOKING A HYDROCARBON STEAM CRACKING FURNACE

ExxonMobil Chemical Paten...

1. A decoking process for removing coke formed during steam cracking of a liquid hydrocarbon feed in a furnace having a firebox, radiant coils, a transfer line exchanger, and an oil quench connection wherein liquid quench oil is injected to directly cool the steam-cracked hydrocarbon, the process comprising the steps of:(a) stopping the flow of hydrocarbon feed comprising liquids to the furnace;
(b) stopping the flow of quench oil to the oil quench connection;
(c) supplying a decoking feed comprising steam and air to the furnace under conditions sufficient to at least partially combust coke accumulated on the interior of the radiant coils, the transfer line exchanger, and the oil quench connection; and
(d) supplying a first portion of quench steam via the oil quench connection into the decoking process effluent, and supplying a second portion of quench steam to the decoking process effluent via a steam quench connection at a point downstream from the oil quench connection at sufficient flow to cool the decoking process effluent to a temperature less than 450° C.

US Pat. No. 10,336,944

DIRECT SYNTHESIS OF HYDROCARBONS FROM CO-ELECTROLYSIS SOLID OXIDE CELL

University of South Carol...

1. A hydrocarbon generation system comprising:a plurality of microtubular reactors in an array, each microtubular reactor including
a first region including a cathode and an anode in electrical communication with one another and an oxygen ion conducting electrolyte between the cathode and the anode,
a second region including a Fischer-Tropsch reaction catalyst in fluid communication and downstream of the cathode; and
a temperature control unit configured to provide the first region at a first temperature that is greater than a second temperature of the second region, wherein each microtubular reactor defines a continuous space, such that the first region and second region are in contact producing a temperature gradient along each microtubular reactor.

US Pat. No. 10,336,943

METHOD FOR COKE OVEN REPAIR

PAUL WURTH DO BRASIL TECN...

1. Method for the repair of coke ovens arranged side by side in a battery which are each delimited by two hollow sidewalls, each formed by side bricks, superimposed in two opposed and spaced rows and spaced together by transverse bricks and defining, between them, heating chambers, wherein the method comprises the following steps:selecting a group of adjacent sidewalls and having a middle wall portion to be kept throughout the repair and two end wall portions to be replaced by new end wall portions;
cutting each sidewall to be repaired in accordance with a cross-sectional vertical cutting plane in order to define a respective flat end face in the middle wall portion, said cutting plane being coincident with a face of a transverse row of bricks facing the adjacent end wall portion being removed;
providing, in the region of each flat end face of the middle wall portion, a pair of side and opposing cutouts and extending over the entire height of the sidewall;
producing, at a basic transverse face of each cutout, a middle longitudinal channel defining a groove for a corresponding tongue of the new bricks, the larger side and standard side of the new end wall portion;
fitting, in each cutout of a flat end face, the corresponding portion of a vertical row of side bricks of a new adjacent portion of the end wall, and the said side bricks comprise, alternately along the vertical row, a new standard side brick of a length equal to the side bricks of the middle wall portion, and a new larger side brick; and
completing the formation of the new end wall portion using new transverse bricks.

US Pat. No. 10,336,942

COKE OVEN CORBEL STRUCTURES AND METHODS OF FORMING THE SAME

FOSBEL, INC., Brook Park...

1. A corbel structure for a coke oven comprising:an assembly of multiple stacked tiers of refractory blocks defining a plurality of substantially vertically oriented central flues and a plurality of diagonally oriented flues positioned laterally of the central flues, wherein
at least one tier of refractory blocks in the assembly includes a plurality of tongue-and-groove interconnected refractory blocks, and wherein
the plurality of interconnected refractory blocks of the at least one tier comprise mutually substantially orthogonal faces defining an edge and respectively including an elongate tongue protruding outwardly therefrom and an elongate groove recessed therein, and wherein
the elongate tongue and groove include respective adjacent ends which co-terminate with one another at the edge defined by the mutually orthogonal faces of the refractory blocks, wherein
the at least one tier includes a plurality of transverse spanner flue blocks, wherein each transverse spanner flue block defines a respective vertical flue section of a vertically oriented central flue and a diagonal flue section of a respective diagonally oriented flue located laterally of the respective vertical flue section, and wherein the transverse spanner flue blocks of the at least one tier are comprised of:
(i) a base section; and
(ii) a central platform section upwardly extending from the base section so as to define (a) opposed L-shaped lateral step regions, the central platform section defining the respective vertically oriented flue, and (b) upper and lower portions of each respective diagonally oriented flue, wherein
(iii) the central platform section includes opposed laterally directed U-shaped ends defining the upper portion of each respective diagonally oriented flue; and wherein
the at least one tier further comprises lateral spacer blocks positioned laterally of the at least one tier, wherein at least some of the lateral spacer blocks are positioned on the L-shaped lateral step regions in abutment with the U-shaped ends of the central platform.

US Pat. No. 10,336,940

DEVICE FOR REGULATING THE ENTRY OF LIGHT

MERCK PATENT GMBH, Darms...

1. A window containing a device for regulating the transmission of light into a room, comprising a switchable layer S comprising a liquid-crystalline medium which comprises at least two different dichroic compounds,where the following applies to the thickness d of layer S and the optical anisotropy ?n of the liquid-crystalline medium of layer S:
d<2 ?m/?n
wherein the molecules of the liquid-crystalline medium of switchable layer S are in a twisted nematic state in a switching state of the device and the switchable layer S is switchable between two different transmission levels, wherein the transmission level is determined by whether an electrical voltage is being applied or not being applied,
wherein the liquid crystalline medium has a clearing point in the temperature range from 70° C. to 170° C., and
wherein the device is colourless when looked through in all its switching states.

US Pat. No. 10,336,939

STABILIZER COMPOUND, LIQUID CRYSTAL COMPOSITION, AND DISPLAY DEVICE

DIC CORPORATION, Tokyo (...

1. A compound represented by the formula (I-b)wherein in the formula, RH3, RH4, and RH5 are each independently a hydrogen atom, and nH1 and nH2 each independently represent an integer of 1 to 4.

US Pat. No. 10,336,937

MONOLITHIC RARE EARTH OXIDE AEROGELS

Lawrence Livermore Nation...

1. A method for making a monolithic rare earth oxide (REO) aerogel, comprising:preparing a reaction mixture consisting essentially of at least one rare earth metal nitrate, at least one epoxide, at least one base catalyst, and at least one organic solvent, wherein the reaction mixture is substantially free of chloride;
curing the mixture to produce a wet gel;
drying the wet gel to produce a dry gel; and
thermally annealing the dry gel to produce the monolithic REO aerogel.

US Pat. No. 10,336,936

PHOSPHOR AND LIGHT EMITTING DEVICE HAVING THE SAME

LG INNOTEK CO., LTD., Se...

1. A phosphor comprising:a phosphor composition of a M4D1-xOyF:Ax structure containing a divalent metal (M), an elements (A) of the active agent, a fluorine or fluor (F) and an oxygen (O), and,
wherein the x satisfies a range of 0.001?x?0.1, and the y satisfies a range of 1?y?5,
wherein the M is at least one of Mg, Ca, Sr, Ba and Zn,
wherein the D is at least one of Si, Ge, Sn, Ti, Zr and Hf,
wherein the F is fluorine,
wherein the A comprises at least one of Mn, Ce, Pr, Nd, Sm, Eu, Tb, Dy, Ho, Er, Tm, and Yb,
wherein the phosphor composition emits red light by a peak wavelength of 400 nm to 470 nm as an excitation wavelength, and
wherein the red light has a peak wavelength of 655 nm to 670 nm and has a FWHM of less than 20 nm.

US Pat. No. 10,336,935

LOW TEMPERATURE STABILIZED FOAM-FORMING COMPOSITION FOR ENHANCED OIL RECOVERY

Dow Global Technologies L...

1. A method of recovering hydrocarbons from a reservoir during gas injection into the reservoir for enhanced oil recovery, the method comprising:(a) at least periodically injecting a gas and a foam-forming composition into a reservoir, the foam-forming composition including an aqueous anionic surfactant foaming solution comprising:
(i) one or more alpha-olefin sulfonate (AOS),
(ii) a solvent having the chemical formula C8H18O3, C8H16O3, or mixtures thereof, the solvent being present in an amount from 30 weight percent to 60 weight percent, based on a total weight of the aqueous anionic surfactant foaming solution, and
(iii) water; and
(b) contacting hydrocarbons in the reservoir with the gas and foam formed using the foam-forming composition to assist in recovering the hydrocarbons from the reservoir.

US Pat. No. 10,336,933

VULCANIZED OIL AND WATER SWELLABLE PARTICULATE COMPOSITE COMPOSITIONS

Halliburton Energy Servic...

1. A vulcanized oil and water swellable particulate composite comprising:an elastomer, a crosslinked water swellable superabsorbent polymer, and a hydrophobically modified water-soluble polymer,
wherein the elastomer comprises a non-polar monomer, a polar monomer, and an ionizable polar monomer, and
wherein the vulcanized oil and water swellable particulate composite is capable of swelling in the presence of a non-aqueous fluid and an aqueous fluid.

US Pat. No. 10,336,931

USE OF DUAL-CATION FLUOROCARBON SURFACTANT AS AMPHIPHOBIC WETTABILITY REVERSAL AGENT IN DRILLING FLUID

CHINA UNIVERSITY OF PETRO...

1. A wettability reversal agent for use in a drilling fluid, the wettability reversal agent comprising a dual-cation fluorocarbon surfactant, of which the cation part is represented by formula (1):
wherein, each R1 is independently selected from C1-C6 alkyl, each R2 is independently selected from H and C1-C6 alkyl, each R3 is independently selected from C1-C10 alkylene, each n is independently 5-15, and m is 1-10.

US Pat. No. 10,336,930

DATE TREE WASTE-BASED BINARY FIBROUS MIX FOR MODERATE TO SEVERE LOSS CONTROL

Saudi Arabian Oil Company...

1. A method to control lost circulation in a lost circulation zone in a wellbore, comprising:introducing an altered drilling fluid into the wellbore such that the altered drilling fluid contacts the lost circulation zone and reduces a rate of lost circulation into the lost circulation zone, where the altered drilling fluid comprises a drilling fluid and a lost circulation material (LCM), wherein the LCM consists of:
a first plurality of fibers produced from date tree trunks, wherein each of the first plurality of fibers has a diameter in the range of 0.4 millimeters (mm) to about 0.8 mm; and
a second plurality of fibers produced from at least one of date tree leaves and date tree leaf stems, wherein each of the second plurality of fibers has a diameter in the range of 0.5 millimeters (mm) to about 1 mm;
wherein the first plurality of fibers comprise 30% by weight of the LCM and the second plurality of fibers comprise 70% by weight of the LCM.

US Pat. No. 10,336,927

BIO-DERIVED COMPOSITION FOR DUST CONTROL

NDSU RESEARCH FOUNDATION,...

1. A composition comprising a biomaterial comprising a mixture of bio-derived glycerides, wherein the composition is formulated for use as a dust control agent.

US Pat. No. 10,336,923

PHOTORESPONSIVE POLYMERS FOR ADHESIVE APPLICATIONS

The University of Akron, ...

1. A photoresponsive adhesive polymer comprising adhesive polymers crosslinked with a crosslinker that includes a photoresponsive group not pendantly attached to the crosslinker, where the photoresponsive adhesive polymer is prepared by polymerizing a vinyl monomer and photoresponsive crosslinker defined by the formula:
where P is an alkoxyphenacyl photoresponsive group, where the adhesive polymers are polysiloxanes, and wherein the alkoxyphenacyl photoresponsive group has the following formula:

where each R is individually an organic group.

US Pat. No. 10,336,921

ADHESIVE COMPOSITIONS FOR NONWOVEN APPLICATIONS

ExxonMobil Chemical Paten...

1. An adhesive composition comprising:(a) a polymer blend comprising
a first propylene-based polymer, wherein the first propylene-based polymer is a homopolymer of propylene or a copolymer of propylene and ethylene or a C4 to C10 alpha-olefin; and
a second propylene-based polymer, wherein the second propylene-based polymer is a homopolymer of propylene or a copolymer of propylene and ethylene or a C4 to C10 alpha-olefin, wherein the second propylene-based polymer is different than the first propylene-based polymer,
wherein the polymer blend has a melt viscosity, measured at 190° C. of about 3,000 cP to about 12,000 cP; and
(b) one or more tackifiers;
wherein the one or more tackifiers has a softening point as determined by ASTM E-28 of about 80° C. to about 145° C., an aromaticity of about 3 mol % to about 11 mol % aromatic protons, and a Cloud Point of about ?10 ° C. to about 15 ° C.,
wherein the polymer blend is present in the amount of about 50 wt % to about 90 wt % of the adhesive composition.

US Pat. No. 10,336,919

ADHESIVE COMPOSITION

LG Chem, Ltd., Seoul (KR...

1. An adhesive composition for encapsulating an organic electronic element, comprising:an olefin-based resin having a water vapor transmission rate (WVTR) of 50 g/m2·day or less;
a heat-curable resin; and
a photocurable compound,
wherein the olefin-based resin has a weight average molecular weight of less than 100,000,
wherein the olefin-based resin, the heat-curable resin and the photocurable compound are comprises at 40 to 90 parts by weight, 5 to 50 parts by weight and 1 to 40 parts by weight, respectively, and
wherein the adhesive composition is a solventless liquid at 25° C.

US Pat. No. 10,336,917

PRESSURE-SENSITIVE ADHESIVE FILM AND METHOD OF MANUFACTURING ORGANIC ELECTRONIC DEVICE USING THE SAME

LG Chem, Ltd., Seoul (KR...

1. A pressure-sensitive adhesive film satisfying Equation 1, comprising:a pressure-sensitive adhesive having a water vapor transmission rate of 50 g/m2·day or less in a thickness direction, wherein the water vapor transmission rate is measured according to a specification of ASTM F1249:
?X?0.3 mm  [Equation 1]
wherein ?X is a change in a creeping distance of a pressure-sensitive adhesive layer between 50 to 200 seconds when a base film, in which the pressure-sensitive adhesive layer comprising a crosslinked product of the pressure-sensitive adhesive is formed to have a thickness of 50 ?m on one surface thereof, is adhered to a glass plate having an adhesive area of 1 cm2, and aged for 24 hours, and then an 1 kg load is applied thereto at 80° C. for 1000 seconds, and
wherein the pressure-sensitive adhesive comprises a pressure-sensitive adhesive composition comprising: an encapsulating resin which is a polyolefin-based resin or elastomer; and a multifunctional active energy ray-polymerizable compound,
wherein the pressure-sensitive adhesive film has a loss factor (tan ?) of 0.05 to 0.25 at 80° C. and a frequency of 1 Hz, and
wherein the active energy ray-polymerizable compound satisfies Formula 1:

wherein R1 is hydrogen or an alkyl group having 1 to 4 carbon atoms, n is an integer of 2 or more, and X is a residue derived from a cyclic alkyl group having 3 to 30 carbon atoms.

US Pat. No. 10,336,916

THERMALLY CONDUCTIVE FLEXIBLE ADHESIVE FOR AEROSPACE APPLICATIONS

The Boeing Company, Chic...

1. A method of preparing a thermally conductive flexible adhesive material, the method comprising:pretreating boron nitride particles in a water-vapor containing environment, thereby attaching hydroxyl groups to surfaces of the boron nitride particles;
exposing the boron nitride particles comprising the hydroxyl groups to the surfaces of the boron nitride particles to a silane-containing solution, thereby converting the hydroxyl groups to silane-containing organofunctional groups, covalently bound to the surfaces of the boron nitride particles;
combining a urethane modified epoxy with the boron nitride particles, comprising the silane-containing organofunctional groups, covalently bound to the surfaces of the boron nitride particles, thereby forming a combined material,
mixing the combined material to form the thermally conductive flexible adhesive material.

US Pat. No. 10,336,914

HEXAHYDROTRIAZINE HYBRID COATINGS FOR SULFUR CAPTURE

International Business Ma...

1. An electronic article, comprising:a substrate comprising electronic components; and
a coating disposed over and upon the substrate, wherein the coating contains polyhexahydrotriazine bonded to silicon containing groups or hexahydrotriazine bonded to silicon containing groups, wherein the silicon containing groups are selected from the group consisting of organosilicon groups, silane groups, alkoxy silane groups, and polysiloxane groups.

US Pat. No. 10,336,911

AMPHIPHILIC GRAFT COPOLYMER FOR WATERBORNE SHAPE MEMORY COATINGS

Syracuse University, Syr...

1. A fiber having a graft copolymer coating thereon, the coating comprising a covalently cross-linked graft copolymer produced by reacting, at room temperature:a graft copolymer comprising a backbone of deacetylized chitosan having a plurality of reactive amino groups and a side chain comprising oligomeric poly (?-caprolactone) grafted onto said backbone, and
a diepoxide linker selected from the group consisting of neopentyl glycol diglycidyl ether (NGDE) and 1,4-butanediol diglycidyl ether (BDGE).

US Pat. No. 10,336,910

SACRIFICIAL COATING FOR INTERMEDIATE TRANSFER MEMBER OF AN INDIRECT PRINTING APPARATUS

XEROX CORPORATION, Norwa...

1. An indirect printing process comprising:providing an ink composition to an inkjet printing apparatus comprising an intermediate transfer member;
forming a sacrificial coating onto the intermediate transfer member, the sacrificial coating made from ingredients comprising:
a latex comprising polymer particles dispersed in a continuous liquid phase;
at least one hygroscopic material;
at least one oil-in-water emulsion; and
at least one surfactant;
ejecting droplets of ink in an imagewise pattern onto the sacrificial coating;
at least partially drying the ink to form a substantially dry ink pattern on the intermediate transfer member; and
transferring both the substantially dry ink pattern and the sacrificial coating from the intermediate transfer member to a final substrate.

US Pat. No. 10,336,908

THREE-DIMENSION FORMING SUPPORT MATERIAL, THREE-DIMENSION FORMING SUPPORT MATERIAL CARTRIDGE, AND THREE-DIMENSION FORMING COMPOSITION SET

FUJI XEROX CO., LTD., To...

1. A three-dimension forming support material for ink jet, comprising:a warm water-soluble radiation curable compound that exhibits solubility in warm water of at least 40° C. to 90° C. after the compound is cured; and
at least one polyglycerin compound selected from the group consisting of fatty acid esters of polyglycerin, ethylene oxide adducts of polyglycerin, and propylene oxide adducts of polyglycerin,
wherein a content of the polyglycerin compound is from 10 to 35 wt % with respect to a total amount of the three-dimension forming support material.

US Pat. No. 10,336,906

USE OF AN ESTER ADDITIVE AND PAVING GRADE ASPHALT IN BUILT UP ROOFING ASPHALT COMPOSITION MANUFACTURE

Owens Corning Intellectua...

1. Thermally stable built-up roofing asphalt (“BURA”) composition comprising:a paving grade asphalt, wherein said paving grade asphalt has been over-blown to a first softening point that is at least 225° F.; and
an additive comprising at least one ester,
wherein said BURA composition has a second softening point that is between 210 and 225° F., a viscosity between 250 cps and 450 cps at 400° F., and is thermally stable at processing temperatures of at least 450° F.

US Pat. No. 10,336,900

COMPOSITE MATERIALS COMPRISING A THERMOPLASTIC MATRIX POLYMER AND WOOD PARTICLES

ONBONE OY, Helsinki (FI)...

1. A composite material, comprisinga first component including polycaprolactone having a melt flow index of less than 7 g/10 min, and
a second component including a woody material in the form of platy wood particles, the platy wood particles having a thickness, a width and a length such that a ratio of the thickness of the platy wood particles to the smaller of the width or the length of the platy wood particles is between 1:2 and 1:500, wherein
the composite material has a density of 0.74 g/mL to 0.92 g/mL, and a specific modulus of 800 MPa/(g/mL) to 1080 MPa/(g/mL).

US Pat. No. 10,336,896

ONE-POT SYNTHESIS OF HIGHLY MECHANICAL AND RECOVERABLE DOUBLE-NETWORK HYDROGELS

The University of Akron, ...

1. A method of forming a hybrid physically and chemically cross-linked double-network hydrogel with highly recoverable and mechanical properties in a single-pot synthesis comprising the steps of:combining the hydrogel precursor reactants including:
a. water,
b. a polysaccharide,
c. an acrylate monomer,
d. an ultraviolet initiator, and
e. a chemical crosslinker to form a single pot mixture;
heating the hydrogel precursor reactants to a temperature higher than the melting point of the polysaccharide and retaining this temperature until the polysaccharide is in a sol state;
cooling the single-pot to a temperature lower than the gelation point of the polysaccharide and retaining this temperature to form a first network; and
thereafter photo-initiating polymerization of the acrylate monomer via the ultraviolet initiator to form the second network, wherein the double-network hydrogel has a polysaccharide concentration of 20 mg/mL, an acrylate monomer concentration of 3.4 mol/L, a ultraviolet initiator concentration of 1 mol % of acrylate monomer, and a chemical crosslinker concentration of 0.03 mol % of acrylate monomer.

US Pat. No. 10,336,893

PROCESS FOR PREPARING A MODIFIED ETHYLENE-BASED POLYMER USING A HYDROCARBON INITIATOR

Dow Global Technologies L...

1. A process to form a second composition comprising a modified ethylene-based polymer the process comprising reacting at a temperature lower than 280° C. a first composition comprising a first ethylene-based polymer with at least the following:(A) at least one carbon-carbon (C—C) free radical initiator of Structure I:

wherein R1, R2, R3, R4, R5 and R6 are each, independently, hydrogen or a hydrocarbyl group; and
wherein, optionally, two or more R groups (R1, R2, R3, R4, R5 and R6) form a ring structure; and
with the provisos that (i) at least one of R2 and R5 is a hydrocarbyl group of at least two carbon atoms, and (ii) at least one of R3 and R6 is a hydrocarbyl group of at least two carbon atoms; and
(B) at least one free radical initiator other than the carbon-carbon (C—C) free radical initiator of Structure I (a non-C—C free radical initiator); and
(C) less than 10 ppm of a hindered phenol antioxidant, based on the weight of the first composition.

US Pat. No. 10,336,891

METHODS AND COMPOSITIONS RELATED TO RECYCLING POLYMER WASTE

ImerTech SAS, Paris (FR)...

1. A functional filler comprising:an inorganic particulate material, wherein the inorganic particulate material has a d50 of less than about 10 ?m; and
a coating comprising a first compound including a terminating propanoic group or ethylenic group with one or two adjacent carbonyl groups,
wherein the first compound has the following formula:
A-(X—Y—CO)m(O—B—CO)nOH
wherein:
A is a moiety containing a terminating ethylenic bond with one or two adjacent carbonyl groups;
X is O and m is 1 to 4 or X is N and m is 1;
Y is C1-18-alkylene or C2-18-alkenylene;
B is C2-6-alkylene;
n is 0 to 5;
provided that when A contains two carbonyl groups adjacent to the ethylenic group, X is N.

US Pat. No. 10,336,889

PNEUMATIC TIRE

1. A pneumatic tire having a tread comprising a vulcanizable rubber composition comprising, based on 100 parts by weight of elastomer (phr),100 phr of a diene based elastomer having a glass transition temperature less than ?50° C., wherein the diene based elastomer is selected form the group consisting of natural rubber, polybutadiene, synthetic polyisoprene, solution polymerized styrene-butadiene rubber with bound styrene content ranging from 9 to 15 percent by weight, and emulsion polymerized styrene-butadiene rubber with bound styrene content ranging from 5 to 23.5 percent by weight;
from 40 to 55 phr of a fatty acid monoester of formula 1
where R1 is selected from C1 to C8 linear or branched alkyl, and C1 to C8 linear or branched alkenyl; R2 is C11 to C21 alkyl or C11 to C21 alkenyl;less than 10 phr of a processing oil;
from 50 to 130 phr of silica; and
optionally, from about 5 to 50 phr carbon black.

US Pat. No. 10,336,887

PRESSURE-SENSITIVE ADHESIVES INCLUDING EXPANDABLE GRAPHITE

Firestone Building Produc...

1. A method of preparing a composite, the method comprising the steps of:i. providing a polymeric sheet;
ii. applying a pressure-sensitive adhesive having a first and second planar surfaces to the polymeric sheet; and
iii. applying expandable graphite to the second planar surface of the pressure-sensitive adhesive to form a concentrated region of expandable graphite.

US Pat. No. 10,336,882

METHOD OF RECOVERING LACTIDE

TOYO SEIKAN CO., LTD., T...

1. A method of recovering lactide comprising introducing a molten resin composition that contains a polylactic acid, a depolymerization catalyst and a carrier resin into a vent chamber that is maintained under a reduced pressure by using a first screw conveyer passage that is extending in the vent chamber, gasifying the lactide contained in said molten resin composition, and recovering a gaseous lactide from said vent chamber, wherein a second screw conveyer passage is provided under said first screw conveyer passage in said vent chamber to recover the carrier resin.

US Pat. No. 10,336,877

MOLDED POLYURETHANE BODIES WITH EXCELLENT FLEXIBILITY AT LOW TEMPERATURE

BASF SE, Ludwigshafen am...

1. A process for producing polyurethane moldings, whereina) organic polyisocyanates are mixed with
b) one or more compounds having at least two hydrogen atoms which are reactive toward isocyanate, comprising polyester polyol,
c) blowing agent,
d) catalyst, and
e) propylene carbonate and at least one compound selected from the group consisting of compounds of the general formula (I),

where R is a hydrocarbon radical which has from 3 to 9 carbon atoms and is bound to the oxygen via a secondary or tertiary carbon atom,
and a compound of the formula (II),

to give a reaction mixture, introduced into a mold and allowed to react to give a polyurethane molding.

US Pat. No. 10,336,875

HALOGEN-FREE RESIN COMPOSITION AND PREPREG AND LAMINATE PREPARED THEREFROM

SHENGYI TECHNOLOGY CO., L...

18. A laminate comprising the prepreg of claim 16.

US Pat. No. 10,336,874

CO-EXTRUDED ULTRA THIN FILMS

National Research Council...

1. An ion exchange resin membrane or an ion exchange precursor resin membrane having a thickness of 25 microns or less and having an orientation ratio of 1.5 or less.

US Pat. No. 10,336,873

FUNCTIONAL POLYMER MEMBRANE, MANUFACTURING METHOD THEREFOR, ION EXCHANGE MEMBRANE AND PROTON CONDUCTIVE MEMBRANE EQUIPPED WITH FUNCTIONAL POLYMER MEMBRANE, AND ION EXCHANGE DEVICE

FUJIFILM Corporation, To...

1. A functional polymer membrane comprising a polymer containing at least a structure represented by the following Formula (I):
wherein in Formula (I), R1 and R2 each independently represent a hydrogen atom or an alkyl group; R3, R4, R5 and R6 each independently represent a substituent, and k1, k2, k3 and k4 each independently represent an integer from 0 to 4; in the case where R3, R4, R5 and R6 are plural, R3, R4, R5 and R6 may be respectively identical to or different from each other, or may be bonded to each other and form a ring; A1, A2, A3 and A4 each independently represent a single bond or a divalent linking group; M1 represents a hydrogen ion, an organic base ion, or a metal ion; in the case where M1 is plural, M1 may be identical to or different from each other; n1 and n2 each independently represent an integer from 1 to 4, and m1 and m2 each independently represent 0 or 1; J1 represents a single bond, —O—, —S—, —CO—, —CR8R9—, or an alkenylene group, and R8 and R9 each independently represent a hydrogen atom, an alkyl group, or a halogen atom;
and p represents an integer of 1 or larger, and q represents an integer from 1 to 4.

US Pat. No. 10,336,872

RESIN COMPOSITION AND FILM

KURARAY CO., LTD., Kuras...

1. A resin composition, comprising a modified polyvinyl alcohol comprising a monomer unit represented by formula (I), and an amine compound represented by formula (II):
wherein in the formula (I):
R1 represents a hydrogen atom, or a linear or branched alkyl group having 1 to 8 carbon atoms,
R2 represents —R3—SO3?X+, —R3—N+(R4)3Cl?, or a hydrogen atom,
R3 representing a linear or branched alkanediyl group having 1 to 10 carbon atoms,
X+ representing a hydrogen atom, a metal atom, or an ammonium group, and
R4 representing a linear or branched alkyl group having 1 to 5 carbon atoms, wherein a plurality of R4s are identical or different; and
H2N—R5  (II),
wherein in the formula (II):
R5 represents —R3?—SO3?X+?, —R3?—N+(R4?)3Cl?, or a hydrogen atom,
R3? representing a linear or branched alkanediyl group having 1 to 10 carbon atoms,
X+? representing a hydrogen atom, a metal atom, or an ammonium group, and
R4? representing a linear or branched alkyl group having 1 to 5 carbon atoms, wherein a plurality of R4?s are identical or different,
wherein the content of the amine compound with respect to 100 parts by mass of the modified polyvinyl alcohol is from 0.01 parts by mass to 1 part by mass.

US Pat. No. 10,336,871

HEAT-SHRINKABLE POLYESTER FILM AND PACKAGE

TOYOBO CO., LTD., Osaka ...

1. A heat-shrinkable polyester film, having an ethylene terephthalate unit, and containing a constituent unit derived from butanediol in a content of 1 to 25% by mole, a constituent unit derived from ?-caprolactone in a content of 1 to 25% by mole, and a constituent unit derived from one or more monomers capable of forming an amorphous component other than the constituent units derived from butanediol and ?-caprolactone in a content not less than 18% by mole in 100% by mole of the whole polyester resin component, the heat-shrinkable polyester film satisfying the following requirements (1) to (3):(1) the film has a ratio A1/A2 (absorbancy ratio) of an absorbancy A1 at 1340 cm?1 to an absorbancy A2 at 1410 cm?1 measured by a polarized ATR-FTIR method of not less than 0.45 and not more than 0.75 in either of the width direction and longitudinal direction of the film;
(2) the film has a ratio (shrinkage stress in the width direction after 30 seconds/maximum shrinkage stress in the width direction) of a shrinkage stress in the width direction after 30 seconds when the film is heat shrunk in hot air of 90° C. for 30 seconds (shrinkage stress in the width direction after 30 seconds) to the maximum shrinkage stress in the width direction of not less than 75% and not more than 100%; and
(3) the film has a hot-water heat shrinkage in the width direction of not less than 30% and not more than 55% when the film is aged for 672 hours in an atmosphere of 30° C. and 85% RH, and then the aged film is dipped in hot water of 70° C. for 10 seconds.

US Pat. No. 10,336,868

POLYCARBOXYLATED COMPOUNDS AND COMPOSITIONS CONTAINING SAME

WISCONSIN ALUMNI RESEARCH...

1. A polycarboxylated compound comprising phenylpropanoid units, wherein:each phenylpropanoid unit comprises an ?-carbon and a ?-carbon;
the phenylpropanoid units are linked to each other via linkages selected from the group consisting of a ?-O-4 linkage, a ?-1 linkage, a ?-5 linkage, a 4-O-5 linkage, a 5-5 linkage, and a ?-? linkage;
the phenylpropanoid units comprise ?-O-4 phenylpropanoid units;
each of the ?-O-4 phenylpropanoid units is a single one of the phenylpropanoid units and is linked via its ?-carbon with a ?-O-4 linkage;
each ?-O-4 phenylpropanoid unit in at least a portion of the ?-O-4 phenylpropanoid units comprises a secondary hydroxyl moiety on the ?-carbon of the ?-O-4 phenylpropanoid unit and a carboxylic acid or carboxylate moiety on the ?-carbon of the ?-O-4 phenylpropanoid unit; and
the polycarboxylated compound further comprises a phenylpropanoid unit linked via a ?-1 linkage, a phenylpropanoid unit linked via a 4-O-5 linkage, or a phenylpropanoid unit linked via a ?-1 linkage and a phenylpropanoid unit linked via a 4-O-5 linkage.

US Pat. No. 10,336,867

CATIONIC POLYPHOSPHAZENE COMPOUND, POLYPHOSPHAZENES-DRUG CONJUGATE COMPOUND AND METHOD FOR PREPARING SAME

CNPHARM CO., LTD, Seoul ...

1. Linear Polyphosphazene-drug conjugate compounds represented by the following chemical formula 2:
wherein, in chemical formula 2, n is an integer from 3 to 300;
MPEG represents methoxy poly(ethylene glycol);
S is a spacer group selected from the group consisting of lysine, arginine, glutamine, asparagine, tyrosine, lysine-containing oligopeptide, arginine-containing oligopeptide, glutamine-containing oligopeptide, asparagine-containing oligopeptide, tyrosinecontaining oligopeptide, amino-ethanol, amino-propanol, amino-butanol, amino-pentanol, and amino-hexanol;
L is a linker to connect the spacer group and drug molecule D, wherein drug molecule D is an hydrophobic anticancer drug having at least one functional group of hydroxyl or amine;
x and y are independently in the range of 0-0.5;
z is in the range of 0-1; and
x+y+z=1.

US Pat. No. 10,336,865

LIQUID CRYSTAL ALIGNING AGENT, LIQUID CRYSTAL ALIGNMENT FILM AND LIQUID CRYSTAL DISPLAY DEVICE

Nissan Chemical Industrie...

1. A liquid crystal aligning agent comprising at least one polymer selected from the group consisting of a polyimide precursor having both of structural units represented by the following formula (1) and structural units represented by the following formula (2) and an imidized polymer thereof:
wherein each of X1 and X2 is a tetravalent organic group represented by the formula (XA-1), Y1 is a bivalent organic group represented by the following formula (Y1-1), Y2 is a bivalent organic group represented by the following formula (Y2-1) or (Y2-2), and each of R1 and R2 which are independent of each other, is a hydrogen atom or a C1-5 alkyl group:

wherein each of R3, R4, R5 and R6 which are independent of one another, is a hydrogen atom, a halogen atom, a C1-6 alkyl group, a C2-6 alkenyl group, a C2-6 alkynyl group or a phenyl group;

wherein each of A1 and A5 which are independent of each other, is a single bond or a C1-5 alkylene group, each of A2 and A4 which are independent of each other, is a C1-5 alkylene group, A3 is a C1-6 alkylene group or a cycloalkylene group, each of B1 and B2 which are independent of each other, is a single bond, —O—, —NH—, —NMe-, —C(?O)—, —C(?O)O—, —C(?O)NH—, —C(?O)NMe-, —OC(?O)—, —NHC(?O)— or —N(Me)C(?O)—, D1 is a group to be replaced with a hydrogen atom by heat, and a is 0 or 1;

US Pat. No. 10,336,864

PRODUCTION METHOD FOR POLY(AMINO ACID)

TAKEDA PHARMACEUTICAL COM...

1. An ionized graft copolymer represented by Formula (II):
suitable for production of nanoparticles, wherein M is alkali metal, A is a hydrophobic moiety, and n is an integer from 10 to 100,000; diagonal lines intervening three monomer units represent that the monomer units are arranged in irregular order, and x is a mole fraction of the monomer unit represented by Formula (III):

y is a mole fraction of the monomer unit represented by Formula (IV):

z is a mole fraction of the monomer unit represented by Formula (V):
andx, y, and z satisfy the following equations:
0?x<1;
0 0 x+y+z=1.

US Pat. No. 10,336,863

CURABLE COMPOSITION HAVING A SPECIAL CATALYST/SOFTNER SYSTEM

1. A curable composition consisting ofA) at least one polymer having at least one terminal group of the general formula (I)
-An-R—SiXYZ  (I),
in which
A is a divalent bonding group containing at least one heteroatom,
R is a divalent hydrocarbon residue having 1 to 12 carbon atoms, and
X, Y, Z are substituents on the Si atom and, mutually independently, are C1 to C8 alkyl, C1 to C8 alkoxy, or C1 to C8 acyloxy groups, where at least one of the residues X, Y, Z is a C1 to C8 alkoxy or C1 to C8 acyloxy group, and
n is 0 or 1;
B) at least one cyclic compound that contains at least one structural motif of formula (II)

as a constituent of the ring structure;
C) at least one cyclohexanedicarboxylic acid dialkyl ester in which the alkyl residues of the ester groups each, mutually independently, contain 1 to 20carbon atoms;
D) optionally one or more fillers;
E) optionally one or more plasticizers selected from the group consisting of a fatty acid ester, a dicarboxylic acid ester except for cyclohexanedicarboxylic acid dialkyl esters, an ester of OH-group-carrying or epoxidized fatty acids, a fat, a glycolic acid ester, a benzoic acid ester, a sulfonic acid ester, a trimellitic acid ester, an epoxidized plasticizer, a polyether plasticizer, a polystyrene, a hydrocarbon plasticizer, a chlorinated paraffin and mixtures thereof; and
F) optionally one or more adjuvants selected from the group consisting of reactive diluent, solvent, adhesion promoter, tackifier, antioxidant, drying agent, UV stabilizer, aging protection agent, rheological adjuvant, color pigment or color paste, fungicide and flame retardant.

US Pat. No. 10,336,862

BIODEGRADABLE POLYMERS WITH PENDANT FUNCTIONAL GROUPS ATTACHED THROUGH AMIDE BONDS

THE UNIVERSITY OF AKRON, ...

1. A functionalized amide polymer comprising:a polyester backbone;
an amide group with a pendant functional group, where the nitrogen atom of the amide group is part of the polymer backbone, where the functionalized amide polymer is formed by a process that comprises a reaction of a dicarboxylic acid and a diol that includes an amide group, or a reaction of a diol and a dicarboxylic acid that includes an amide group, and where the pendant functional group is selected from the group consisting of azides, carboxylic acids, hydroxyls, amines, nitriles, furans, aldehydes, ketones, maleimides, propargyls, halogens, imaging labels, peptides, amino acids,
wherein HAL is halogen, wherein x is from 0 to 6, and wherein TBS is tertbutyl dimethylsilyl.

US Pat. No. 10,336,860

POLYMER COMPOUND AND LIGHT EMITTING DEVICE USING THE SAME

Sumitomo Chemical Company...

1. A polymer compound comprising:at least one terminal constitutional unit represented by the following formula (1) and
a constitutional unit represented by the following formula (2):
whereinmT represents an integer of 0 to 5, nT represents an integer of 1 to 4, and cT represents 1, and when there are a plurality of mT, they can be the same or different,
QT represents a crosslinkable group represented by the following formula (XL-1), (XL-7), (XL-16) or (XL-17), and when there are a plurality of QT, they can be the same or different,
KT represents an alkylene group, a cycloalkylene group, an arylene group, a divalent heterocyclic group, a group represented by —NR?—, an oxygen atom or a sulfur atom, the foregoing groups each optionally having a substituent, wherein R? represents a hydrogen atom, an alkyl group, a cycloalkyl group, an aryl group or a monovalent heterocyclic group, the foregoing groups each optionally having a substituent, and when there are a plurality of KT, they can be the same or different, and
ArT represents a group obtained by removing from a benzene ring optionally having a substituent, a fluorene ring optionally having a substituent, a naphthalene ring optionally having a substituent, a phenanthrene ring optionally having a substituent or a dihydrophenanthrene ring optionally having a substituent (nT+1) hydrogen atoms attached directly to carbon atoms constituting the ring;
whereinmA represents an integer of 0 to 5, and n represents 1 or 2, and when there are a plurality of mA, they can be the same or different,
Ar1 represents an aromatic hydrocarbon group optionally having a substituent,
KA represents an alkylene group, a cycloalkylene group, an arylene group, an oxygen atom or a sulfur atom, the foregoing groups each optionally having a substituent, and when there are a plurality of KA, they can be the same or different, and
Q1 represents a crosslinkable group selected from Group A of crosslinkable groups, and when there are a plurality of Q1, they can be the same or different;wherein Group A is a crosslinkable group selected from the group consisting of:wherein RX L represents a methylene group, an oxygen atom or a sulfur atom, and nX L represents an integer of 0 to 5, and when there are a plurality of RX L, they can be the same or different, and when there are a plurality of nX L, they can be the same or different, and * represents a binding site, the foregoing crosslinkable groups each optionally having a substituent.

US Pat. No. 10,336,858

PREPARATION OF BROMINE-CONTAINING POLYMERS USEFUL AS FLAME RETARDANTS

Bromine Compounds Ltd., ...

1. A process for preparing bromine-containing polymer, comprising a Friedel-Crafts alkylation reaction of tetrabromoxylylene dihalide, or tetrabromoxylylene dihalide in combination with pentabromobenzyl halide, with a reactant having one or more six-membered aromatic rings of Formula (II):
where R is a linear or branched aliphatic chain; k is an integer from 0 to 3; m is 0 or 1; and Z is selected from the group consisting of null, O, S and a linear or branched alkylene, wherein the reaction takes place in a solvent in the presence of a Friedel-Crafts catalyst, and isolating from the reaction mixture the bromine-containing polymer of Formula (I):

wherein R, k, m, and Z are as defined above; each of a1 and a2 is independently an integer from 1 to 3; and each of b1 and b2 is independently an integer from 1 to 3, such that a1+b1?3 and a2+b2?3.

US Pat. No. 10,336,857

PROCESS FOR THE PREPARATION OF SILYLATED POLYMERS EMPLOYING A BACKMIXING STEP

Momentive Performance Mat...

1. A silylated polyurethane having the general formula (10)X1g—(R1)[-A1C(?O)A2R4Si(CH3)b(OR5)3-b]a-g  (10)
wherein
each occurrence of X1 is a functional group selected from the group consisting of

 wherein each occurrence of R15 is a monovalent hydrocarbon radical containing from about 1 to about 30 carbon atoms and optionally may contain a heteroatom, each occurrence of R16 is hydrogen, an alkyl group of from 1 to 6 carbon atoms or phenyl, each occurrence of R17 is hydrogen, an alkyl group of from 1 to about 6 carbon atoms or phenyl and the subscript his an integer of from 1 to about 6;
each occurrence of A1 is a functional group selected from the group consisting of —O—, —S— and —NH—;
each occurrence of A2 is a functional group selected from the group consisting of —S—, —NR6, where R6 is selected from the group consisting of hydrogen, an alkyl group containing 1 to about 10 carbon atoms, cycloalkyl group containing from about 5 to about 10 carbon atoms, an aralkyl group containing from about 7 to about 10 carbon atoms, phenyl and —CH[(C?O)OR7]CHR8C(?O)OR7, where R7 is an alkyl group of from 1 to about 10 carbon atoms, a cycloalkyl group of from about 5 to about 10 carbon atoms, an aryl group of from about 6 to about 10 carbon atoms, and aralkyl group of from about 7 to about 10 carbon atoms and R8 is an alkyl group of from 1 to about 10 carbon atoms, a cycloalkyl group of from about 5 to about 10 carbon atoms, an aryl group of from about 6 to about 10 carbon atoms, and aralkyl group of from about 7 to about 10 carbon atoms;
R1 is an organic group containing from about 50 to about 4,000 carbon atoms and at least one functional group selected from group consisting of —O—, —S—, —OC(?O)NH—, —R2NC(?O)NH—, —C(?O)O—, —OC(?O)O—, —OCHR2O—, —C(?O)NR2— and —NR2—, wherein each occurrence of R2 is independently hydrogen, an alkyl group containing from 1 to about 6 carbon atoms or phenyl;
R4 is a divalent alkylene group containing from 1 to about 10 carbon atoms, a cycloalkylene group containing from about 5 to about 10 carbon atoms and an arylene group containing from about 6 to about 10 carbon atoms;
each occurrence of R5 is an alkyl group of from 1 to about 18 carbon atoms or a —R9(OR10)cOR11, wherein R9 is an alkyl group of from 1 to about 18 carbon atoms, R10 is a divalent alkylene group of from about 2 to about 4 carbon atoms, and R11 is an alkyl group of from 1 to about 10 carbon atoms or —C(?O)R12, where R12 is hydrogen, or an alkyl group of from 1 to about 6 carbon atoms, and
the subscripts a, b, c and h are integers wherein a is 1 to about 5, b is 0 to about 2, c is 0 to about 5 and g is 1, with the provisos that (i) a-g is greater than or equal to 1, and (ii) when A1 is —O— or —S—, then A2 is —NH—.

US Pat. No. 10,336,852

AMPHIPHILIC GRAFT COPOLYMERS

Becton, Dickinson and Com...

1. An amphiphilic copolymer of the formula (I):
wherein R is hydrogen, alkyl, substituted alkyl, vinylic substituted alkyl, hydrocarbyl, substituted hydrocarbyl, or vinylic substituted hydrocarbyl group; the molar value of m is in the range from 2 to 40 mole percent; the molar value of n is in the range from 60 to 98 mole percent; and p is in the range from 30 to 500 ethylene oxide units.

US Pat. No. 10,336,851

COPOLYMER FOR SEMICONDUCTOR LITHOGRAPHY, RESIST COMPOSITION, AND METHOD FOR MANUFACTURING SUBSTRATE

Mitsubishi Chemical Corpo...

1. A copolymer for lithography having a turbidity Th(80) of 1.0 NTU or more and 4.6 NTU or less and a turbidity Tm(80) of 1.0 NTU or more and 3.8 NTU or less, whereinthe turbidity Th(80) is a turbidity of a PGMEA solution when n-heptane in an amount to be 80% of (X)h is added to the PGMEA solution where (X)h denotes an amount of n-heptane added to have a turbidity of 10 NTU when n-heptane is added to the PGMEA solution containing the copolymer for lithography at 20 wt % with respect to a total mass of the PGMEA solution; and
the turbidity Tm(80) is a turbidity of a PGMEA solution when methanol in an amount to be 80% of (X)m is added to the PGMEA solution where (X)m denotes an amount of methanol added to have a turbidity of 5.0 NTU when methanol is added to the PGMEA solution containing the copolymer for lithography at 20 wt % with respect to a total mass of the PGMEA solution.

US Pat. No. 10,336,850

METHODS OF USE FOR CROSSLINKED POLYMER COMPOSITIONS IN SUBTERRANEAN FORMATION OPERATIONS

Hallibunon Energy Service...

1. A method comprising:introducing a treatment fluid into a subterranean formation, wherein the treatment fluid comprises a base fluid and a crosslinked polymer, the crosslinked polymer comprising:
reactants of a first repeating unit, a second repeating unit, and a crosslinker that react to form the crosslinked polymer,
wherein the first repeating unit is a sulfonic acid-containing monomer present from 50% to 99% by weight of the reactants,
wherein the second repeating unit selected from the group consisting of an N-vinyl amide-containing monomer, a terminal double bond-containing monomer, and any combination thereof, and is present from 1% to 50% by weight of the reactants, and
wherein the crosslinker comprises at least two olefinic bonds.

US Pat. No. 10,336,848

SURFACTANT-COMPATIBLE STAR MACROMOLECULES

Pilot Polymer Technologie...

1. A surfactant-system thickening macromolecule is represented by Formula B:
wherein:
Core represents a crosslinked polymeric segment;
P1 independently represents the hydrophilic polymeric segment of the at least first polymeric arm comprised of monomeric residues of polymerized hydrophilic monomers;
P2 independently represents the further segment of the at least second polymeric arm comprised of at least one monomeric residue of a polymerized surfactant-system thickening monomer comprising a C6 or greater alkyl acrylate; C6 or greater alkenyl acrylate; C6 or greater alkyl alkyl acrylate; C6 or greater alkenyl alkyl acrylate; C6 or greater alkyl acrylamide; C6 or greater alkenyl acrylamide; C6 or greater alkyl alkyl acrylamide; C6 or greater alkenyl alkyl acrylamide; C2 or greater alkyl vinyl ether; C2 or greater alkenyl vinyl ether; C1 or greater alkyl allyl ether; or C1 or greater alkenyl allyl ether;
P3 independently represents the hydrophilic polymeric segment of the at least second polymeric arm comprised of monomeric residues of polymerized hydrophilic monomers;
P4 independently represents the hydrophobic polymeric segment of the at least third polymeric arm comprised of monomeric residues of polymerized hydrophobic monomers;
P5 independently represents the hydrophilic polymeric segment of the at least third polymeric arm comprised of monomeric residues of polymerized hydrophilic monomers;
q1 independently represents the number of monomeric residues in P1 and has a value in the range of between 5 to 2000;
q2 independently represents the number of monomeric residues in P2 and has a value in the range of between 1 to 500;
q3 independently represents the number of monomeric residues in P3 and has a value in the range of between 10 to 5000;
q4 independently represents the number of monomeric residues in P4 and has a value in the range of between 1 to 500;
q5 independently represents the number of monomeric residues in P5 and has a value in the range of between 10 to 5000;
r independently represents the number of the at least first polymeric arms covalently attached to the Core and has a value in the range of between 1 to 1000;
s independently represents the number of the at least second polymeric arms covalently attached to the Core and has a value in the range of between 1 to 1000; and
t independently represents the number of the at least third polymeric arms covalently attached to the Core and has a value in the range of between 1 to 1000.

US Pat. No. 10,336,846

PROCESS TO FORM ETHYLENE/?-OLEFIN INTERPOLYMERS

Dow Global Technologies L...

1. A process to form an ethylene/?-olefin interpolymer, said process comprising at least the following steps A) through C):A) polymerizing, in at least one reactor, at least one reaction mixture comprising ethylene and the ?-olefin, in a solution polymerization, and, in the presence of at least the following components I), II) and III), to form a final polymer solution;
I) at least one compound of Structure 1 below:

wherein for Structure 1:
M is titanium, zirconium, or hafnium, each independently being in a formal oxidation state of +2, +3, or +4; n is an integer of from 0 to 3, wherein when n is 0, X is absent;
each X independently is a monodentate ligand that is neutral, monoanionic, or dianionic; or two X are taken together to form a bidentate ligand that is neutral, monoanionic, or dianionic; and wherein X and n are chosen in such a way that the metal-ligand complex of Structure 1 is, overall, neutral;
each Z independently is O or S;
L is hydrocarbylene or heterohydrocarbylene, wherein the hydrocarbylene has a portion that comprises a 1-carbon atom to 6-carbon atom linker backbone, linking the Z atoms in Structure 1, and the heterohydrocarbylene has a portion that comprises a 1-atom to 6-atom linker backbone, linking the Z atoms in Structure 1, wherein each atom of the 1-atom to 6-atom linker backbone of the heterohydrocarbylene independently is a carbon atom or a moiety comprising a heteroatom, wherein each moiety comprising a heteroatom independently is O, S, S(O), S(O)2, Si(Rc)2, Ge(Rc)2, P(RP), or N(RN), wherein independently each Rc is unsubstituted (C1-C18)hydrocarbyl or the two Rc are taken together to form a (C2-C19)alkylene, each RP is unsubstituted (C1-C18)hydrocarbyl; and each RN is unsubstituted (C1-C18)hydrocarbyl, a hydrogen atom or absent;
R1a, R2a, R3a, R4a, R1b, R2b, R3b, R4b, R5c, R6c, R7c, R8e, R9e, R10e, R11e, R12e, R13e, R14e, R15e, R5d, R6d, R7d, R8f, R9f, R10f, R11f, R12f, R13f, R14f and R15f are each, independently, a hydrogen atom, an unsubstituted hydrocarbyl, a substituted hydrocarbyl an unsubstituted heterohydrocarbyl, a substituted heterohydrocabyl, or a halogen atom; and
wherein two or more of R1a, R2a, R3a, R4a, R1b, R2b, R3b, R4b, R5c, R6c, R7c, R8e, R9e, R10e, R11e, R12e, R13e, R14e, R15e, R5d, R6d, R7d, R8f, R9f, R10f, R11f, R12f, R13f, R14f and R15f may, optionally, form one or more ring structures;
II) at least one co-catalyst selected from the following:
i) a borane compound,
ii) a borate compound,
iii) an alkyl aluminum compound,
iv) a combination of two or more from i) through iii);
III) at least one compound of Structure 2 below:

wherein, for Structure 2, R1, R2 and R3 are each, independently, hydrogen, an unsubstituted hydrocarbon, a substituted hydrocarbon, and/or two or more of R1, R2 and R3 may, optionally, form one or more ring structures; and wherein if R1 is hydrogen, then R2 and R3 are each not hydrogen; and if R2 is hydrogen, then R1 and R3 are each not hydrogen; and if R3 is hydrogen, then R1 and R2 are each not hydrogen; and
wherein R4, R5 and R6 are each, independently, hydrogen, an unsubstituted hydrocarbon, or a substituted hydrocarbon;
B) separating the final polymer solution into at least a polymer-rich solution and a polymer-free solution; and wherein, optionally, at least a portion of the polymer-free solution is recycled back to the reactor;
C) maintaining the level of the at least one compound of Structure 2 in the at least one reactor, from 100 ppm to 10,000 ppm, based on the total content weight of the reactor; and
wherein for step C), the level of the at least one compound of Structure 2 is maintained using one or more of the following features:
a) adding water to the final polymer solution, after this solution exits the at least one reactor, at a level from 0.1 to 1000 ppm, based on the total content weight of the reactor, and wherein, after the addition of the water, at least a portion of the polymer-free solution is recycled back to the reactor;
b) increasing or decreasing the level of the at least one co-catalyst of component II), and wherein, after the final polymer solution exits the at least one reactor, and at least a portion of the polymer-free solution is recycled back to the reactor;
c) adding at least one base compound to the final polymer solution, after this solution exits the at least one reactor, and wherein, after the addition of the base compound, at least a portion of the polymer-free solution is recycled back to the reactor;
d) adding at least one oil to the final polymer solution, and after this solution exits the at least one reactor, and wherein, after the addition of the oil, at least a portion of the polymer-free solution is recycled back to the reactor;
e) continuously adding the compound of Structure 2 to the reactor, to maintain the level of this compound, in the reactor, from 100 ppm to 10,000 ppm, based on the total content weight of the reactor;
f) any combination of two or more from a) through e).

US Pat. No. 10,336,844

METHOD OF PREPARING POWDERY DIACETAL CLARIFYING AGENT

SUNKO INK CO., LTD., Tai...

1. A method of preparing a powdery diacetal clarifying agent, comprising steps of:(a) mixing an aromatic aldehyde, a polyol, and an acid catalyst in an organic polar solvent to obtain a first reaction mixture, wherein an equivalence ratio of the aromatic aldehyde to the polyol is from 2:1 to 2:2;
(b) adding a hydrogenating agent and an inorganic silicon-containing agent into the first reaction mixture to obtain a second reaction mixture, wherein an equivalence ratio of the hydrogenating agent to the aromatic aldehyde is more than 0.01:1, a pH value of the inorganic silicon-containing agent is from pH 6 to pH 12, and an amount of the inorganic silicon-containing agent ranges from 0.02 wt % to 3.5 wt % based on an amount of the aromatic aldehyde; and
(c) filtering and drying the second reaction mixture to obtain the powdery diacetal clarifying agent;
wherein the inorganic silicon-containing agent is a sodium aluminosilicate containing trisulfur radical anion.

US Pat. No. 10,336,842

TRANSITION METAL COMPOUND AND CATALYST COMPOSITION INCLUDING THE SAME

LG CHEM, LTD., Seoul (KR...

1. A transition metal compound of the following Chemical Formula 1:
wherein,
M is a group 4 transition metal;
R is selected from the group consisting of an alkyl group having 1 to 20 carbon atoms, a cycloalkyl group having 3 to 20 carbon atoms, an aryl group having 6 to 20 carbon atoms, an arylalkyl group having 7 to 20 carbon atoms, and an alkylaryl group having 7 to 20 carbon atoms;
R1 and R2 are each independently selected from the group consisting of a hydrogen atom, an alkyl group having 1 to 20 carbon atoms, an alkenyl group having 2 to 20 carbon atoms, a haloalkyl group having 1 to 20 carbon atoms, a cycloalkyl group having 3 to 20 carbon atoms, an aryl group having 6 to 20 carbon atoms, an arylalkyl group having 7 to 20 carbon atoms, an alkylaryl group having 7 to 20 carbon atoms, and combinations thereof, or R1 and R2 are linked to each other to form an aliphatic ring having 3 to 20 carbon atoms or an aromatic ring having 6 to 20 carbon atoms;
R3 to R8 are each independently selected from the group consisting of a hydrogen atom, a halogen group, an alkyl group having 1 to 20 carbon atoms, an alkenyl group having 2 to 20 carbon atoms, a cycloalkyl group having 3 to 20 carbon atoms, an aryl group having 6 to 20 carbon atoms, an arylalkyl group having 7 to 20 carbon atoms, an alkylaryl group having 7 to 20 carbon atoms, an alkoxy group having 1 to 20 carbon atoms, an aryloxy group having 6 to 20 carbon atoms, a silyl group, and combinations thereof, or adjacent two or more functional groups among R3 to R8 are linked to each other to form an aliphatic ring having 3 to 20 carbon atoms or an aromatic ring having 6 to 20 carbon atoms;
R9 is selected from the group consisting of an alkyl group having 1 to 20 carbon atoms, an alkenyl group having 2 to 20 carbon atoms, a cycloalkyl group having 3 to 20 carbon atoms, an aryl group having 6 to 20 carbon atoms, an arylalkyl group having 7 to 20 carbon atoms, an alkylaryl group having 7 to 20 carbon atoms, a silyl group, and a metalloid radical of a group 14 metal substituted with a hydrocarbyl group having 1 to 20 carbon atoms;
X1 and X2 are each independently selected from the group consisting of a halogen group, an alkyl group having 1 to 20 carbon atoms, an alkenyl group having 2 to 20 carbon atoms, an aryl group having 6 to 20 carbon atoms, an alkylaryl group having 7 to 20 carbon atoms, an arylalkyl group having 7 to 20 carbon atoms, an alkylamino group having 1 to 20 carbon atoms, an arylamino group having 6 to 20 carbon atoms, and an alkylidene group having 1 to 20 carbon atoms;
R, R1 to R9, X1 and X2 are each independently unsubstituted or substituted with one or more substituents selected from the group consisting of a halogen group, an alkyl group having 1 to 20 carbon atoms, a haloalkyl group having 1 to 20 carbon atoms, an alkenyl group having 2 to 20 carbon atoms, an alkoxy group having 1 to 20 carbon atoms, a cycloalkyl group having 3 to 20 carbon atoms, an aryl group having 6 to 20 carbon atoms, an arylalkyl group having 7 to 20 carbon atoms, an alkylaryl group having 7 to 20 carbon atoms, and an aryloxy group having 6 to 20 carbon atoms; and
n is an integer of 1 or 2, and when n is an integer of 2, two R9s are the same as or different from each other.

US Pat. No. 10,336,841

SELF SUPPORTED PHOSPHINIMINE CATALYST

NOVA Chemicals (Internati...

1. A spherical self supported single site catalyst having a diameter from 5 to 200 ?m comprising a catalyst of the formula
wherein M is a transition metal selected from Ti, Hf and Zr; PI is a phosphinimine ligands of the formula:

wherein each R21 is independently selected from a hydrogen atom; a halogen atom; C1-20, hydrocarbyl radicals which are unsubstituted by or further substituted by a halogen atom; a C1-8 alkoxy radical; a C6-10 aryl or aryloxy radical; an amido radical; a silyl radical of the formula:
—Si—(R22)3
wherein each R22 is independently selected from hydrogen, a Ci-8 alkyl or alkoxy radical, and C6-10 aryl or aryloxy radicals; and a germanyl radical of the formula:
—Ge—(R22)3
wherein R22 is as defined above;
L is a monoanionic ligand selected from a cyclopentadienyl ligand which is substituted by up to three C1-6 linear, branched, cyclic or aromatic hydrocarbons which are unsubstituted or up to fully substituted by fluorine atoms; and
Y is independently selected from a halogen atom, C1-4 alkyl radicals, C6-20 aryl radicals, C7-12 arylalkyl radicals, C6-10 phenoxy radicals, amido radicals which is optionally substituted by up to two C1-4 alkyl radicals and C1-4 alkoxy radicals; m is 1 or 2; n is 0 or 1; p is an integer and the sum of m+n+p equals the valence state of M;
supported on an activator of the formula:
R122AlO(R12AlO)qAlR122
wherein each R12 is independently selected from C1-20 hydrocarbyl radicals and q is from 3 to 50 to provide a molar ratio of A1 from the activator to M from the catalyst from 5:1 to 90:1.

US Pat. No. 10,336,840

PROPYLENE ETHYLENE RANDOM COPOLYMER SUITABLE FOR PIPE

1. A composition suitable for pipe applications comprising a propylene ethylene random copolymer, the copolymer having the following properties:(A) a melt flow rate (MFR) less than 1 g/10 min as determined according to ASTM D1238, at 230° C. and 2.16 kg;
(B) an ethylene content of from 3 to 5 percent by weight of the random copolymer;
(C) a xylene insoluble fraction of the random copolymer which is obtained by the wet method, wherein said fraction exhibits a [(Koenig B value)*(% mm)]?92; and
(D) a xylene solubles content measured by the wet method of ?7.0% by weight.

US Pat. No. 10,336,838

PROCESS FOR PRODUCING OLEFIN POLYMER AND OLEFIN POLYMER

MITSUI CHEMICALS, INC., ...

1. A 4-methyl-1-pentene polymer fulfilling the following requirements (a) to (c):(a) the amount of constituent units derived from 4-methyl-1-pentene is 100 to 80 mol %, and the amount of constituent units derived from at least one selected from olefins having 2 to 30 carbon atoms (except 4-methyl-1-pentene) is 0 to 20 mol %;
(b) the meso diad fraction (m) as measured by 13C-NMR is 98.5% to 100%; and
(c) the heat of fusion ?Hm (unit: J/g) and the melting point Tm (unit: ° C.) as measured by Differential Scanning calorimetry (DSC) fulfill the following relation (1):
?Hm?0.5×Tm?76.  Relation (1):

US Pat. No. 10,336,836

PHOTOCURABLE RESIN COMPOSITION, INK, AND COATING

Osaka Soda Co., Ltd., Os...

1. A photocurable resin composition, comprising:an allylic polymer (A) produced by polymerization of an allylic compound represented by the formula (I) below; and
a tackifier resin (B),
wherein R1 and R2 each represent H or CH3; X represents an a-valent group having an unsubstituted saturated or partially unsaturated four- to eight-membered cyclic structure;and a represents 2 or 3.

US Pat. No. 10,336,829

INTRACELLULAR DELIVERY COMPOUNDS

Sorrento Therapeutics, In...

1. A compound having the Formula I:wherein,each Ba is independently selected from adenine (A), guanine (G), cytosine (C), and thymine (T);
X is O or S;
each R1 is independently selected from hydrogen and (C1-C6)alkyl substituted with a fluorophore;
q is an integer from 12 to 35;
r is an integer from 1 to 10;
t is an integer from 1 to 10;
L is —CH2—R2—*;
R2 is —(C1-C6)alkyl substituted with 1 or 2 groups selected from —C(?O)NRa, —NRaC(?O)Rb, —NRaC(?O)Rd, ?NORe, —NRa, —NRaRb, —ORb, —S(O)kRb, —NRaS(O)2Rb, —S(O)2NRaRb, —S(O)2NRa, —C(?O)ORb, —OC(?O)ORb, —OC(?O)Rb, —C(?O)NRaRb, —NRaC(?O)Rb, —NRaC(?O)ORb, —OC(?O)NRaRb, phenyl, —OC(?O)NRa, —NRaC(?O)NRaRb, —NRaC(?O)NRa, —NRa(C?S)NRaRb, —NRa(C?S)NRa, and —C(?O)Rb;
k is 0, 1, or 2;
each Ra is independently hydrogen or (C1-C6)alkyl optionally substituted with Rf;
each Rb is independently (C1-C6)alkyl optionally substituted with Rf or —C(?O)Rf;
Rd is —[(C1-C6)alkyl-O—(C1-C6)alkyl]vC(?O)NH;
Re is —[(C1-C6)alkyl-O—(C1-C6)alkyl]pC(?O);
each Rf is independently
wherein the wavy bond indicates the point of attachment to the (C1-C6)alkyl defined by Ra, or the (C1-C6)alkyl or carbonyl each defined by Rb;Rg is (C1-C6)alkyl or —[(C1-C6)alkyl-O—(C1-C6)alkyl]wC(?O)NH;
ring A is
wherein the dashed bonds indicate the points of attachment to the triazolyl of Rf, and the wavy bond indicates the point of attachment to the (C1-C6)alkyl defined by Ra, or the (C1-C6)alkyl or carbonyl each defined by Rb;p is an integer from 1 to 10;
v is an integer from 1 to 10;
w is an integer from 2 to 12;
* indicates the point of attachment to AT; and
AT is an antibody.

US Pat. No. 10,336,815

PHAGE-DISPLAYED ANTIBODY LIBRARIES AND USES THEREOF

Academia Sinica, Taipei ...

1. A phage-displayed single-chain variable fragment (scFv) library comprising a plurality of scFvs that are expressed by a phage and exhibit binding affinity and specificity to an H1 hemagglutinin of influenza virus, wherein the plurality of scFvs respectively comprises the amino acid sequences of SEQ ID NOs: 24-26, 34-37 and 44-46.

US Pat. No. 10,336,792

ANTIMICROBIAL PEPTIDE DENDRIMERS

UNIVERSITAT BERN, Bern (...

1. A method of antibacterial treatment, comprising administering to a subject in need thereof, a peptide dendrimer described by a general formulaX—(B2-[Y2]s-D1)2-B1Z, wherein
X is
(D2)4, or
(D3)8-(B3-[Y3]r-D2)4,and whereineach Y (Y2 and Y3) independently from any other Y is a linkage moiety di- or tripetide H-Cys or CH-Cys linked to the N-terminus of the C-terminally neighboring amino acid in D through a thioether moiety exemplified by the formula

wherein the sulfur atom belongs to the cysteine and the amino group constitutes the N-terminus of the neighboring amino acid in D, wherein the C-terminus of cysteine is a carboxamide,
r and s is 0 or 1;
Z is a central moiety;
each B (B1, B2, and B3) independently from any other B denotes a diaminoalkylcarboxylic acid moiety described by the general formula: CnH2n-1(NH2)2CO— wherein n is a number between 2 and 10,
each D (D1, D2, and D3) independently from any other D is
i) a dipeptide CH, HC, CC or HH, or
ii) a tripeptide HCH, HHC, CHH, CCH, CHC, HCC, HHH or CCC wherein
H is any amino acid comprising a hydrophobic side chain, and
C is any amino acid comprising a cationic side chain,
thereby providing antibacterial treatment to the subject.

US Pat. No. 10,336,787

PROGESTERONE ANALOGS AND USES RELATED THERETO

Emory University, Atlant...

1. A method of treating stroke or traumatic brain injury comprising administering an effective amount of a pharmaceutical composition comprising a compound of Formula II
or salts thereof to a subject in need thereof, wherein
R is selected from H, Me, Et,

US Pat. No. 10,336,785

METHODS FOR SYNTHESIZING NUCLEOTIDE ANALOGUES WITH DISULFIDE LINKERS

Qiagen Sciences, LLC, Ge...

1. A compound wherein the structure is:

US Pat. No. 10,336,784

METHODS FOR MODULAR SYNTHESIS OF N-GLYCANS AND ARRAYS THEREOF

ACADEMIA SINICA, Taipei ...

1. A method of preparation of a compound having the general formula:
wherein, each of R2, R3, R4, R1?, R2?, and R3? is independently selected from —H, benzyl (Bn), acetyl (Ac), benzoyl (Bz), or independently selected from a sugar moiety selected from:

wherein at least one of R2, R3, R4, R1?, R2?, and R3? is one of said sugar moieties,
wherein, each of R5, R6, R7, R8, R9 R10, and R12 is independently selected from —H, benzyl (Bn), acetyl (Ac), or benzoyl (Bz);
R11 is selected from —H, Me (methyl) or Et (ethyl);
R13 is selected from —H, benzyl (Bn), acetyl (Ac), benzoyl (Bz), or:

X is —OR14 or an anomeric leaving group;
wherein, R14 is selected from H, alkyl, alkenyl, alkynyl, aryl, unsubstituted aryl, substituted aryl; benzyl (Bn), para-methoxy benzyl ether (PMB), methoxy phenyl ether (PMP), or allyl ether (allyl);
Y is —NHR16; and R16 is acetyl (Ac),
wherein the method comprises the stepwise enzymatic extension on a hydroxyl group of a compound having the structure of formula (III):

wherein,
each of R1? and R2? is independently selected from —H, acetyl (Ac), or benzoyl (Bz);
X? is —OR3? and R3? is selected from —H, benzyl (Bn), para-methoxy benzyl ether (PMB), methoxy phenyl ether (PMP), or allyl ether (allyl);
wherein the enzymes to enzymatically extend the compounds of formula (III) are independently selected from the group consisting of ? (1?2) Fucosyltransferase, ? (1?3) N-acetyl glucosamine transferase, and ? (2?3) sialyltransferase.

US Pat. No. 10,336,782

SUBSTITUTED CYCLOPENTADIENYL COBALT COMPLEX AND METHOD FOR PRODUCTION THEREOF, AND COBALT-CONTAINING THIN FILM AND METHOD FOR PRODUCTION THEREOF

SAGAMI CHEMICAL RESEARCH ...

5. A method for producing a cobalt-containing thin film using, as a raw material in a vapor phase deposition method based on a chemical reaction, a cobalt complex represented by Formula (1)
[where R1 is a silyloxy group represented by Formula (2)

where R6, R7 and R8 each independently represent an alkyl group having from 1 to 6 carbon atoms; R2 is a hydrogen atom, an alkyl group having from 1 to 6 carbon atoms, or a silyloxy group represented by Formula (2); R3, R4 and R5 each independently represent a hydrogen atom or an alkyl group having from 1 to 6 carbon atoms; and L is a diene having from 4 to 10 carbon atoms].

US Pat. No. 10,336,781

RECYCLABLE METATHESIS CATALYSTS

THE TRUSTEES OF BOSTON CO...

1. A composition comprising a transition metal catalyst having the following structure:wherein:M is a transition metal;
R is an alkyl, alkenyl, alkynyl, aryl, alkoxy carbonyl, alkylsulfonyl, or alkylsulfinyl;
each optionally substituted with an alkyl, alkoxy, aryl or heteroaryl moiety;
R1 and R2 each is or together are, an electron withdrawing anionic ligand;
a, b, c, and d each are H, a halogen atom or an alkyl, alkenyl, alkynyl, aryl, alkoxy, alkenyloxy, alkynyloxy, aryloxy, alkoxycarbonyl, alkylamino, alkylthio, alkylsulfonyl, or alkylsulfinyl; each optionally substituted with an alkyl, halogen, aryl or heteroaryl moiety;
X is oxygen, sulfur, nitrogen or phosphorus; and
Y is an electron-donating heterocyclic carbene ligand.

US Pat. No. 10,336,780

DIOXOLANE ANALOGUES OF URIDINE FOR THE TREATMENT OF CANCER

MEDIVIR AB, Stockholm (S...

1. A compound represented by formula Ia:
wherein:
R1 is NH2;
R2 is H;
R13 is phenyl or naphthyl any of which is optionally substituted with 1, 2 or 3 R22;
R15 is methyl;
R16 is C3-C7cycloalkyl;
each R22 is independently selected from halo, C1-C6alkyl, C2-C6alkenyl, C1-C6haloalkyl, C1-C6alkoxy, C1-C6haloalkoxy, phenyl, hydroxyC1-C6alkyl, C3-C6cycloalkyl, C1-C6alkylcarbonyl, C3-C6cycloalkylcarbonyl, carboxyC1-C6alkyl, hydroxy, amino CN, and NO2, or any two R22 groups attached to adjacent ring carbon atoms can combine to form —O—(CR23R23?)1-6—O—;
R23 and R23? are independently H or C1-C3alkyl;
or a pharmaceutically acceptable salt and/or solvate thereof.

US Pat. No. 10,336,779

GOLD(I) COMPLEXES, PHARMACEUTICAL COMPOSITIONS THEREOF, AND METHODS OF TREATING CANCER

King Fahd University of P...

1. A gold(I) complex of formula (I):or a salt thereof, a tautomer thereof, a stereoisomer thereof, or a mixture thereof;wherein R1, R2, R3, and R4 are independently selected from the group consisting of a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted alkoxy, an optionally substituted aryl, an optionally substituted arylalkyl, an optionally substituted alkanoyl, an optionally substituted aroyl, a halogen, a cyano, and a nitro;
R5, R6, R7, R8, R9, R10, R11, and R12 are independently selected from the group consisting of a hydrogen, an optionally substituted alkyl, an optionally substituted cycloalkyl, an optionally substituted aryl, and an optionally substituted arylalkyl; and
X is an anion.

US Pat. No. 10,336,778

PRODRUGS OF GLUTAMINE ANALOGS

The Johns Hopkins Univers...

1. A compound selected from the group consisting of:

US Pat. No. 10,336,777

CYSTEINE-MODIFYING SUBSTRATE ANALOGUE INHIBITORS OF RIBOSE 5-PHOSPHATE ISOMERASE FOR PARASITIC DISEASES, ALONG WITH METHODS OF THEIR FORMATION AND USE

University of South Carol...

1. A compound having the formula:where:X1 is P and both R1 are OH or X1 is S, one R1 is OH and the other R1 is O;
X3 is CH2;
n is an integer from 0 to 5; and
X6 is a halogen.

US Pat. No. 10,336,776

INVERT EMULSIONS MADE WITH NON-PEG CONTAINING SILICONE BASED POLYHYDRIC EMULSIFIERS

SILTECH CORP, Toronto, O...

1. A silicone emulsifier having the following structure:
wherein;
x is an integer ranging from 1 to 100;
y is an integer ranging from 1 to 50;
z is an integer ranging from 1 to 50;
o is an integer ranging from 1 to 21;
G is selected from the group consisting of CH3; OH and mixtures thereof.

US Pat. No. 10,336,775

GLYCOSIDASE INHIBITORS

Asceneuron SA, Lausanne ...

1. A compound, N-(5-(4-(1-(Benzo[d][1,3]dioxol-5-yl)ethyl)piperazin-1-yl)-1,3,4-thiadiazol-2-yl)acetamide, which is:or any of its tautomers, enantiomers or mixtures thereof.

US Pat. No. 10,336,774

N-AZASPIROCYCLOALKANE SUBSTITUTED N-HETEROARYL COMPOUNDS AND COMPOSITIONS FOR INHIBITING THE ACTIVITY OF SHP2

Novartis AG, Basel (CH)

1. A method of treatment of lung cancer comprising administering a compound of formula I, or a pharmaceutically acceptable salt thereof, to a person in need of such treatment in an effective amount for the therapeutic treatment of lung cancer:
in which:
p is selected from 0 and 1;
q is selected from 0 and 1;
Y1 is N;
Y2 is CR6;
R1 is ?XR1a; wherein R1a is selected from C6-10aryl, C3-8cycloalkyl, C3-8cycloalkenyl and a 5-9 member heteroaryl group containing from 1 to 4 heteroatoms or groups independently selected from N, C(O), O and S; wherein said aryl or heteroaryl of R1a is substituted with 1 to 5 R9 groups independently selected from halo, amino, hydroxy, N3, C1-4alkyl, C1-4alkoxy, dimethyl-amino, hydroxy-substituted-C1-4alkyl, halo-substituted-C1-4alkyl, amino-substituted-C1-4alkyl, —C(O)OR10, —C(O)NH2 and —NHC(O)R10, wherein R10 is selected from hydrogen, phenyl and naphthyl; wherein said phenyl of R10 is unsubstituted or substituted with methoxy; and X is selected from a bond, S(O)m, O, C(O), CR10aR10b, NR11; wherein m is selected from 0, 1 and 2; each R10a and R10b is independently selected from halo and C1-4alkyl; and R11 is selected from hydrogen and C1-4alkyl;
R2a and R2b are independently selected from hydrogen, C1-4alkyl, C1-4alkoxy, amino, hydroxy, C3-8cycloalkyl and C1-4alkyl-amino;
R3a and R3b are independently selected from hydrogen, halo, C1-4alkyl, C1-4alkoxy, amino, hydroxy, C3-8cycloalkyl and C1-4alkyl-amino;
R4a and R4b are independently selected from hydrogen, halo, C1-4alkyl, C1-4alkoxy, amino, hydroxy, C3-8cycloalkyl and C1-4alkyl-amino;
R5a and R5b are independently selected from hydrogen, C1-4alkyl, C1-4alkoxy, amino, hydroxy, C3-8cycloalkyl and C1-4alkyl-amino;
R6 is selected from hydrogen, halo, cyano, C1-4alkyl, C1-4alkoxy, amino-carbonyl, halo-substituted C1-4alkyl, halo-substituted C1-4alkoxy, hydroxy-substituted C1-4alkyl, amino-substituted C1-4alkyl, —S(O)1-2R6a, —C(S)R6a, —C(O)NR6aR6b, —C(NH)NR6aR6b and —NR6aC(O)R6b; wherein R6a and R6b are independently selected from hydrogen and C1-4alkyl;
R7 and R8 together with the carbon atom to which they are both attached form a 3 to 7 member saturated or partially unsaturated ring that can optionally contain 1 to 3 heteroatoms or groups independently selected from N, C(O), O and S(O)m; wherein m is selected from 0, 1 and 2; wherein said saturated ring formed by R7 and R8 can be unsubstituted or substituted with 1 to 3 groups independently selected from amino, hydroxy, methoxy, halo, methyl, amino-methyl, methyl-amino and
isobutyryloxy.

US Pat. No. 10,336,772

BICARBAZOLE COMPOUND, MATERIAL FOR ORGANIC LIGHT-EMITTING DEVICE INCLUDING BICARBAZOLE COMPOUND, AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING BICARBAZOLE COMPOUND

SAMSUNG ELECTRONICS CO., ...

1. A bicarbazole compound represented by Formula 1:[Ar1]n1-(L1)a1-[Ar2]n2  Formula 1
wherein, in Formula 1,
Ar1 is represented by one of Formulae 1-1, 1-2, and 1-4 to 1-21:

wherein, in Formulae 1-1, 1-2, and 1-4 to 1-21,
at least one hydrogen is substituted with a group serving as a binding site to L1, Ar2 is represented by Formula 1B:

wherein, in Formula 1B,
X1 to X16 are each independently selected from a nitrogen atom and CR21,
R21 is selected from a binding site to L1, a binding site to L2, hydrogen, a deuterium atom, a substituted or unsubstituted C1-C10 alkyl group, a substituted or unsubstituted aryl group comprising 6 to 30 ring-forming atoms, and a substituted or unsubstituted heteroaryl group comprising 5 to 30 ring-forming atoms,
R21 is optionally bound to adjacent R21 to form a condensed ring,
two substituents of X1 to X16 each comprises a C-(L2-binding site) structure,
R22 and R23 are each independently selected from a binding site to L1, a substituted or unsubstituted aryl group comprising 6 to 30 ring-forming atoms, and a substituted or unsubstituted heteroaryl group comprising 5 to 30 ring-forming atoms,
at least one selected from R21 to R23 is a binding site to L1,
n1 and n2 are each independently an integer from 1 to 20,
L1 and L2 are each independently selected from a single bond and a substituted or unsubstituted arylene group comprising 6 to 30 ring-forming atoms, and
a1 and a2 are each independently an integer from 0 to 3.

US Pat. No. 10,336,771

COMPOUNDS TARGETING PROTEINS, COMPOSITIONS, METHODS, AND USES THEREOF

BioTheryX, Inc., Chappaq...

1. A compound of Formula (IId):
or a pharmaceutically acceptable salt thereof, wherein:
R1 and R2 are each independently H, deuterium, hydroxyl, halogen, cyano, nitro, optionally substituted amino, optionally substituted C1-C6 alkoxy, optionally substituted C1-C6 alkyl, optionally substituted C2-C6 alkenyl, optionally substituted C2-C6 alkynyl, optionally substituted C3-C8 cycloalkyl, optionally substituted C6-C10 aryl, optionally substituted 3 to 10-membered heterocyclyl, or optionally substituted 5 to 10-membered heteroaryl.

US Pat. No. 10,336,770

PHOSPHOINOSITIDE 3-KINASE INHIBITORS WITH A ZINC BINDING MOIETY

Curis, Inc., Lexington, ...

1. A compound represented by formula (II);or a pharmaceutically acceptable salt thereof,wherein represents a single or double bond;
X and Y are independently CR1, N(R8), S or O , wherein when one of X and Y is CR1, the other is N(R8), S or O;
R1 is selected from hydrogen, hydroxy, amino, halogen, alkoxy, alkylamino, dialkylamino, CF3, CN, NO2, sulfonyl, acyl, aliphatic, substituted aliphatic, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, and substituted heterocyclic;
G1 is O;
G2 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or, substituted or unsubstituted heterocyclic;
each R8 is independently hydrogen, acyl, aliphatic or substituted aliphatic;
B is a linker; and
C is

 wherein R33 is hydrogen.

US Pat. No. 10,336,769

GONADOTROPIN-RELEASING HORMONE RECEPTOR ANTAGONISTS AND METHODS RELATING THERETO

Neurocrine Biosciences, I...

1. A compound chosen fromor a pharmaceutically acceptable salt thereof.

US Pat. No. 10,336,768

PYRIMIDINE COMPOUNDS AND METHODS USING THE SAME

Yuma Therapeutics, Inc., ...

1. A compound according to formula (I):or a pharmaceutically acceptable salt thereof,wherein
Z1 is —OR7 or —SR7;
Z2 is —C(R3)? or —N?;
each R1 and R2 is, independently, H, optionally substituted C1-3 acyl, or optionally substituted C1-3 alkyl;
R3 and R4 combine to form —X1—X2—X3—; or R3 is H, halogen, cyano, optionally substituted C1-6 alkyl, optionally substituted C1-3 alkoxy, or optionally substituted amino, and R4 is halogen, cyano, optionally substituted C1-6 alkyl, optionally substituted C1-3 alkoxy, optionally substituted amino, or optionally substituted C1-6 thioalkoxy;
wherein
X1 is —S—, —O—, —(CR14R15)—, —C(R16)?, —N(R9)—, or —N?;
X2 is —(CR17R18)n—, —S—, —O—, —N(R9)—, —C(R19)?, ?C(R20)—, or ?C(R21)—C(R22)?;
X3 is —(CR14R15)—, —S—, —O—, —N(R9)—, ?N—, ?C(R23)—;
each R14 and R15 is, independently, H or optionally substituted C1-3 alkyl, or R14 and R15 combine to form ?O or ?S;
each R17 and R18 is, independently, H or optionally substituted C1-3 alkyl, or R17 and R18 combine to form ?O or ?S;
each R16, R19, R20, R21, R22, and R23 is, independently, H or optionally substituted C1-3 alkyl; and
n is 1 or 2;
R5 is halogen, H, optionally substituted C1-3 alkyl, optionally substituted C1-3 alkoxy, or CN;
R6 is halogen, H, optionally substituted C1-3 alkyl, optionally substituted C1-3 alkoxy, or CN;
R7 and R8, together with the atoms to which each is attached, join to form an optionally substituted five membered ring comprising one or two heteroatoms selected from the group consisting of oxygen and sulfur;
R9 is H, optionally substituted C1-3 alkyl, optionally substituted C3-8 cycloalkyl, optionally substituted C6-10 aryl, optionally substituted C2-9 heteroaryl, optionally substituted C2-9 heterocyclyl, optionally substituted C1-3 alkcycloalkyl, optionally substituted C1-3 alkheterocyclyl, or optionally substituted C1-3 alkaryl; and
Rm is H, halogen, cyano, optionally substituted C1-4 acyl, optionally substituted C1-4 alkyl, or optionally substituted C1-3 alkoxy;
wherein
when each R5 and R6 is chloro, Z is —OR7, R7 and R8 combine to form —CH2—CH2—, Z2 is CR3, and R3 and R4 combine to form a group according to formula (IIa),

wherein R9 is H or —C(O)—N(H)-(linear C1-3 alkyl).

US Pat. No. 10,336,767

CRYSTALLINE FORMS OF THERAPEUTIC COMPOUNDS AND USES THEREOF

Kala Pharmaceuticals, Inc...

4. A pharmaceutical composition comprising the crystalline form of claim 1 and a pharmaceutically acceptable carrier.

US Pat. No. 10,336,766

ANTICANCER DRUG CANDIDATES

The Scripps Research Inst...

1. An enediyne compound comprising a structure represented by formula (I):
or a pharmaceutically acceptable salt thereof, wherein:
R1, R2, R3, R4, are each independently: H, OH, F, Cl, Br, R?, OR?, CH3, NH2, NHR?, NR?2, SH, SR?, C(O)R, RCO2R?, halogen, or alkyl;
R5 and R6 are each independently OH, F, Cl, Br, OR?, NH2, NHR?, NR?2, SH, SR?, C(O)R, RCO2R?;
R7 is H or alkyl;
R? and R are independently: H, C1-C10 alkyl, or aryl;
X is N.

US Pat. No. 10,336,765

DIHYDROPYRANOPYRIMIDINONE DERIVATIVES, AND USE THEREOF

ST. PHARM CO., LTD., (KR...

1. A compound represented by Chemical Formula 1, a tautomer thereof, a stereoisomer thereof and their mixture, or a pharmaceutically acceptable salt thereof:wherein,X is CHR4 or C?O;
Y is N or C;
1 is 0, 1, or 2;
R1 is hydrogen, hydroxyl, cyano or C1-6 alkyl {herein, if Y is N, R1 is null};
R2 is

 heteroaryl or heterocyclyl;
R4 is hydrogen, hydroxyl, C1-6 alkyl or amino;
m is 0, 1, 2 or 3;
n is 0, 1, 2, 3, 4 or 5;
each of R5 is independently —Z—(CH2)p—R6, halo, cyano, nitro, carboxy, C1-6 alkyl, C1-6 alkyloxo, C2-6 alkenyl, C1-6 alkoxy, C1-6 alkoxycarbonyl, C1-6 hydroxyalkyl, C1-6 dihydroxyalkyl, C1-6 haloalkyl unsubstituted or optionally substituted with hydroxyl or C3-7 cycloalkyl;
Z is —O—, —S(O)q—,—NR7—, —CONR7—, —CHR7—, or null;
p is 0, 1, 2, 3, 4, 5 or 6;
q is 0, 1 or 2;
R6 is hydrogen, hydroxyl, —OR8, —O—(C?O)—R8, —S(O)r—R8, cyano, —(C?O)—R8,—(C?O)OR8, —(C?O)NR9R10, —NR9R10, azido, C1-6 alkyl, C1-6 dihydroxyalkyl, C1-6 haloalkyl unsubstituted or optionally substituted with hydroxyl, C3-7 cycloalkyl, heterocyclyl, C5-10 aryl or heteroaryl;
r is 0, 1 or 2;
R7 is hydrogen, C1-6 alkyl, C1-6 alkoxy, C3-7 cycloalkyl or C1-3 alkyl-C3-7 cycloalkyl;
R8 is hydrogen, C1-6 alkyl, C1-6 alkyloxo, C1-6 alkoxy, amino, C1-6 alkylamino, C1-6 aminoalkyl, C3-7 cycloalkyl, C1-3 alkyl —C3-7 cycloalkyl or heterocyclyl;
each of R9 and R10 is independently hydrogen, C1-6 alkyl, C1-6 alkoxy, C3-6 cycloalkyl, C1-3 alkyl—C3-6 cycloalkyl, or —(SO2)—C1-3 alkyl;
each of the heteroaryls is a 5- to 10-membered single or fused ring containing one or more heteroatoms selected from the group consisting of N, O, S and a combination thereof, and
each of the heterocyclyls is a 3- to 10-membered single or fused ring containing one or more heteroatoms selected from the group consisting of N, O, S and a combination thereof;
one or more than one hydrogen of each of the cycloalkyls and heterocyclyls may be unsubstituted or substituted with hydroxyl, oxo, halo, cyano, nitro, C1-6 alkyl, C1-6 hydroxyalkyl, C1-6 haloalkyl, C1-6 alkoxy, formyl, C1-6 alkylformyl, carboxy, C1-6 alkylcarboxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, carbamoyl, C1-6 alkylcarbamoyl or di(C1-6 alkyl)carbamoyl; and
one or more than one hydrogen of each of the aryls and heteroaryls may be unsubstituted or substituted with hydroxyl, oxo, halo, cyano, nitro, C1-6 alkyl, C1-6 alkoxy, C1-6 hydroxyalkyl, C1-6 haloalkyl, pyrazinyl, formyl, C1-6 alkylformyl, carboxy, C1-6 alkylcarboxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, carbamoyl, C1-6 alkylcarbamoyl, di(C1-6 alkyl)carbamoyl or C1-6 alkylsulfonyl.

US Pat. No. 10,336,764

FULLERENE DERIVATIVE AND LUBRICANT

SHOWA DENKO K.K., Tokyo ...

1. A fullerene derivative comprising, in a molecule:a fullerene backbone; and
n pyrrolidine rings each being condensed to the fullerene backbone,
each of the pyrrolidine rings including one aryl group including m substituents each including a perfluoropolyether chain, “m” being an integer from 2 to 5 and “n” being an integer from 1 to 5.

US Pat. No. 10,336,762

PYRROLO[1,2-B]PYRIDAZINE DERIVATIVES

Gilead Sciences, Inc., F...

1. A compound of Formula (I)
wherein:
R1 and R2 are each independently selected from:
a) C1-10 alkyl optionally substituted with Z1;
b) C3-10 cycloalkyl optionally substituted with Z1;
c) 5-10 membered heteroaryl optionally substituted with Z1;
d) C6-10 aryl optionally substituted with Z1;
e) 4-7 membered monocyclic heterocyclyl optionally substituted with Z1;
f) 6-12 membered bicyclic heterocyclyl optionally substituted with Z1; or
g) —N(R12)(R12), —S(O)2R12, —S(O)2N(R12)(R12), or —H;
R3 and R4 are each independently selected from:
a) H, halo, —NO2, —CN, —O—R12, —C(O)—R12, —C(O)—N(R12)(R12), —N(R12)(R12), —N(R12)C(O)—R12, —N(R12)C(O)O—R12, —N(R12)S(O)2(R12), —N(R12)C(O)—N(R12)(R12), —S(O)2R12 or —S(O)2N(R12)(R12);
b) C1-9 alkyl optionally substituted with Z1;
c) C2-9 alkynyl optionally substituted with Z1;
d) C2-9 alkenyl optionally substituted with Z1;
e) 5-10 membered heteroaryl optionally substituted with Z1;
f) C6-10 aryl optionally substituted with Z1;
g) 4-12 membered heterocyclyl optionally substituted with Z1; or
h) C3-10 cycloalkyl optionally substituted with Z1;
R5, R6 and R7 are each independently selected from:
a) H, halo, —NO2, —CN, —O—R12, —C(O)—R12, —C(O)—N(R12)(R12), —N(R12)(R12), —N(R12)C(O)—R12, —N(R12)C(O)O—R12, or —N(R12)S(O)2(R12;
b) C1-5 alkyl optionally substituted with Z1; or
c) Cyclopropyl, oxetanyl or azetidinyl optionally substituted with Z1;
Z1 is independently oxo, halo, —NO2, —N3, —CN, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, C1-8 haloalkyl, aryl, heteroaryl, heterocyclyl, —O—R12, —C(O)—R12, —C(O)O—R12, —C(O)—N(R12)(R12), —N(R12)(R12), —N(R12)2(R12)+, —N(R12)C(O)—R12, —N(R12)C(O)O—R12, —N(R12)C(O)N(R12)(R12), —N(R12)S(O)2(R12), —NR12S(O)2N(R12)(R12), —NR12S(O)2O(R12), —OC(O)R12, —OC(O)OR12, —OC(O)—N(R12)(R12), —Si(R12)3, —S—R12, —S(O)R12, —S(O)(NH)R12, —S(O)2R12 or —S(O)2N(R12)(R12);
wherein any alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with Z1a;
each Z1a is independently oxo, halo, —NO2, —CN, —N3, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, C1-8 haloalkyl, aryl, heteroaryl, heterocyclyl, —O—R12, —C(O)R12, —C(O)O—R12, —C(O)N(R12)(R12), —N(R12)(R12), —N(R12)2(R12)+, —N(R12)—C(O)R12, —N(R12)C(O)O(R12), —N(R12)C(O)N(R12)(R12), —N(R12)S(O)2(R12), —N(R12)S(O)2—N(R12)(R12), —N(R12)S(O)2O(R12), —OC(O)R12, —OC(O)OR12, —OC(O)—N(R12)(R12), —Si(R12)3, —S—R12, —S(O)R12, —S(O)(NH)R12, —S(O)2R12 or —S(O)2N(R12)(R12);
wherein any alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with Z1b;
each R12 is independently H, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, aryl, heteroaryl or heterocyclyl;
wherein any alkyl, alkenyl, alkynyl, cycloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with Z1a;
each Z1b is independently oxo, hydroxy, halo, —NO2, —N3, —CN, C1-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, C1-8 haloalkyl, aryl, heteroaryl, heterocyclyl, —O(C1-9 alkyl), —O(C2-6 alkenyl), —O(C2-6 alkynyl), —O(C3-15 cycloalkyl), —O(C1-8 haloalkyl), —O(aryl), —O(heteroaryl), —O(heterocyclyl), —NH2, —NH(C1-9 alkyl), —NH(C2-6 alkenyl), —NH(C2-6 alkynyl), —NH(C3-15 cycloalkyl), —NH(C1-8 haloalkyl), —NH(aryl), —NH(heteroaryl), —NH(heterocyclyl), —N(C1-9 alkyl)2, —N(C3-15 cycloalkyl)2, —N(C2-6 alkenyl)2, —N(C2-6 alkynyl)2, —N(C3-15 cycloalkyl)2, —N(C1-8 haloalkyl)2, —N(aryl)2, —N(heteroaryl)2, —N(heterocyclyl)2, —N(C1-9 alkyl)(C3-15 cycloalkyl), —N(C1-9 alkyl)(C2-6 alkenyl), —N(C1-9 alkyl)(C2-6 alkynyl), —N(C1-9 alkyl)(C3-15 cycloalkyl), —N(C1-9 alkyl)(C1-8 haloalkyl), —N(C1-9 alkyl)(aryl), —N(C1-9 alkyl)(heteroaryl), —N(C1-9 alkyl)(heterocyclyl), —C(O)(C1-9 alkyl), —C(O)(C2-6 alkenyl), —C(O)(C2-6 alkynyl), —C(O)(C3-15 cycloalkyl), —C(O)(C1-8 haloalkyl), —C(O)(aryl), —C(O)(heteroaryl), —C(O)(heterocyclyl), —C(O)O(C1-9 alkyl), —C(O)O(C2-6 alkenyl), —C(O)O(C2-6 alkynyl), —C(O)O(C3-15 cycloalkyl), —C(O)O(C1-8 haloalkyl), —C(O)O(aryl), —C(O)O(heteroaryl), —C(O)O(heterocyclyl), —C(O)NH2, —C(O)NH(C1-9 alkyl), —C(O)NH(C2-6 alkenyl), —C(O)NH(C2-6 alkynyl), —C(O)NH(C3-15 cycloalkyl), —C(O)NH(C1-8 haloalkyl), —C(O)NH(aryl), —C(O)NH(heteroaryl), —C(O)NH(heterocyclyl), —C(O)N(C1-9 alkyl)2, —C(O)N(C3-15 cycloalkyl)2, —C(O)N(C2-6 alkenyl)2, —C(O)N(C2-6 alkynyl)2, —C(O)N(C3-15 cycloalkyl)2, —C(O)N(C1-8 haloalkyl)2, —C(O)N(aryl)2, —C(O)N(heteroaryl)2, —C(O)N(heterocyclyl)2, —NHC(O)(C1-9 alkyl), —NHC(O)(C2-6 alkenyl), —NHC(O)(C2-6 alkynyl), —NHC(O)(C3-15 cycloalkyl), —NHC(O)(C1-8 haloalkyl), —NHC(O)(aryl), —NHC(O)(heteroaryl), —NHC(O)(heterocyclyl), —NHC(O)O(C1-9 alkyl), —NHC(O)O(C2-6 alkenyl), —NHC(O)O(C2-6 alkynyl), —NHC(O)O(C3-15 cycloalkyl), —NHC(O)O(C1-8 haloalkyl), —NHC(O)O(aryl), —NHC(O)O(heteroaryl), —NHC(O)O(heterocyclyl), —NHC(O)NH(C1-9 alkyl), —NHC(O)NH(C2-6 alkenyl), —NHC(O)NH(C2-6 alkynyl), —NHC(O)NH(C3-15 cycloalkyl), —NHC(O)NH(C1-8 haloalkyl), —NHC(O)NH(aryl), —NHC(O)NH(heteroaryl), —NHC(O)NH(heterocyclyl), —SH, —S(C1-9 alkyl), —S(C2-6 alkenyl), —S(C2-6 alkynyl), —S(C3-15 cycloalkyl), —S(C1-8 haloalkyl), —S(aryl), —S(heteroaryl), —S(heterocyclyl), —NHS(O)(C1-9 alkyl), —N(C1-9 alkyl)(S(O)(C1-9 alkyl), —S(O)N(C1-9 alkyl)2, —S(O)(C1-9 alkyl), —S(O)(NH)(C1-9 alkyl), —S(O)(C2-6 alkenyl), —S(O)(C2-6 alkynyl), —S(O)(C3-15 cycloalkyl), —S(O)(C1-8 haloalkyl), —S(O)(aryl), —S(O)(heteroaryl), —S(O)(heterocyclyl), —S(O)2(C1-9 alkyl), —S(O)2(C2-6 alkenyl), —S(O)2(C2-6 alkynyl), —S(O)2(C3-15 cycloalkyl), —S(O)2(C1-8 haloalkyl), —S(O)2(aryl), —S(O)2(heteroaryl), —S(O)2(heterocyclyl), —S(O)2NH(C1-9 alkyl), or —S(O)2N(C1-9 alkyl)2;
wherein any alkyl, cycloalkyl, aryl, heteroaryl, or heterocyclyl is optionally substituted with one or more halo, C1-9 alkyl, C1-8 haloalkyl, —OH, —NH2, —NH(C1-9 alkyl), —NH(C3-15 cycloalkyl), —NH(C1-8 haloalkyl), —NH(aryl), —NH(heteroaryl), —NH(heterocyclyl), —N(C1-9 alkyl)2, —N(C3-15 cycloalkyl)2, —NHC(O)(C3-15 cycloalkyl), —NHC(O)(C1-8 haloalkyl), —NHC(O)(aryl), —NHC(O)(heteroaryl), —NHC(O)(heterocyclyl), —NHC(O)O(C1-9 alkyl), —NHC(O)O(C2-6 alkynyl), —NHC(O)O(C3-15 cycloalkyl), —NHC(O)O(C1-8 haloalkyl), —NHC(O)O(aryl), —NHC(O)O(heteroaryl), —NHC(O)O(heterocyclyl), —NHC(O)NH(C1-9 alkyl), —S(O)(NH)(C1-9 alkyl), S(O)2(C1-9 alkyl), —S(O)2(C3-15 cycloalkyl), —S(O)2(C1-8 haloalkyl), —S(O)2(aryl), —S(O)2(heteroaryl), —S(O)2(heterocyclyl), —S(O)2NH(C1-9 alkyl), —S(O)2N(C1-9 alkyl)2, —O(C3-15 cycloalkyl), —O(C1-8 haloalkyl), —O(aryl), —O(heteroaryl), —O(heterocyclyl), or —O(C1-9 alkyl); and
with the proviso that when R1 is C3 alkyl, R2 is C5 alkyl substituted with F and hydroxyl, R3, R5, R6, R7 are H, and R4 is CN, then R1 is substituted with oxo, halo, —NO2, —N3, —CN, C2-9 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-15 cycloalkyl, C1-8 haloalkyl, aryl, heteroaryl, heterocyclyl, —O—R12, —C(O)—R12, —C(O)O—R12, —C(O)—N(R12)(R12), —N(R12)(R12), —N(R12)2(R12)+, —N(R12)C(O)—R12, —N(R12)C(O)O—R12, —N(R12)C(O)N(R12)(R12), —N(R12)S(O)2(R12), —NR12S(O)2N(R12)(R12), —NR12S(O)2O(R12), —OC(O)R12, —OC(O)OR12, —OC(O)—N(R12)(R12), —Si(R12)3, —S—R12, —S(O)R12, —S(O)(NH)R12, —S(O)2R12 or —S(O)2N(R12)(R12);
wherein any alkyl, alkenyl, alkynyl, cycloalkyl, haloalkyl, aryl, heteroaryl or heterocyclyl is optionally substituted with Z1a;
or a pharmaceutically acceptable salt, stereoisomer, mixture of stereoisomers, or deuterated analog thereof.

US Pat. No. 10,336,760

INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)

SYROS PHARMACEUTICALS, IN...

1. A compound having the structural formula (IIIc):or a pharmaceutically acceptable salt thereof, wherein:R2 is —C(O)—;
Q is
wherein “1” represents a point of attachment to R2;R3 is a bond, optionally substituted —CH2—, optionally substituted —NH—, —C(O), —N(CH3)—, or optionally substituted —CH(CH3)—;
Z is a monocyclic or bicyclic aryl, carbocyclyl, heterocyclyl, or heteroaryl, wherein Z is optionally substituted;
R4 is
wherein L3 is a bond, an optionally substituted C1-C7 alkylene, or an optionally substituted C2-C7 alkenylene or alkynylene, wherein one or more methylene units of the alkylene, alkenylene or alkynylene are optionally and independently replaced with —O—, —S—, —S(O)—, —S(O)2, —N— or —N(R6)—;Y is O, S, or N(R6);
each R6 is independently selected from hydrogen and optionally substituted —C1-C6 alkyl; and
each of RE1, RE2 and RE3 is independently selected from hydrogen, halogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, optionally substituted heteroaryl, —CH2OR9, —CH2N(R9)2, —CH2SR9, —CN, —OR9, —N(R9)2, and —SR9, wherein each occurrence of R9 is independently selected from hydrogen, optionally substituted alkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted carbocyclyl, optionally substituted heterocyclyl, optionally substituted aryl, and optionally substituted heteroaryl, or
RE1 and RE3, or RE2 and RE3, or RE1 and RE2 are joined to form an optionally substituted carbocyclic or optionally substituted heterocyclic ring.

US Pat. No. 10,336,757

TREATMENT OF NEURODEGENERATIVE DISEASES THROUGH INHIBITION OF HSP90

Sloan-Kettering Institute...

1. A method for treatment of neurodegenerative disease, comprising administering to an individual in need of such treatment a therapeutically effective amount of a compound having structure:wherein R is hydrogen, or a C1 to C10 alkyl, C2 to C10 alkynyl, or C2 to C10 alkoxyalkyl group, optionally including heteroatoms;Y1 and Y2 are independently C or N;
X4 is hydrogen or halogen;
X3 is CH2, CF2, S, SO, SO2, O, NH, or NR2, wherein R2 is alkyl; and
X2 is halogen, alkyl, halogenated alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido, dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2-alkyl, COO-alkylm NH2, OH, or CN; and
X1 has the formula —X—Y—Z— wherein, X, Y and Z are independently C, N, S or O, connected by single or double bonds and with apporpriate hydrogen substitution to satisfy valence, or Y may be (CH2)2,wherein one of X and Z is bonded at the 5?-position to the aryl ring and the other is bonded to the 4?position, and wherein the compound is optionally in the form of an acid addition salt;wherein the neurodegenerative disease is selected from the group consisting of complete androgen insensitivity syndrome (CAIS), spinal and bulbar muscular atrophy (SBMA or Kennedy's disease), Alzheimer's Disease (AD), sporadic frontotemporal dementia with parkinsonism (FTDP), familial FTDP-17 syndromes, Parkinson's disease, and Huntington disease.

US Pat. No. 10,336,756

(S)-2-(1-AMINOPROPYL)-5-FLUORO-3-PHENYLQUINAZOLIN-4(3H)-ONE PRECURSOR OF A QUINAZOLINONE AS INHIBITOR OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA

ICOS CORPORATION, Foster...

2. A composition, comprising a compound having a structure

US Pat. No. 10,336,755

FUSED PYRAZOLE DERIVATIVES, PREPARATION METHOD THEREOF, AND USE THEREOF IN TREATMENT OF CANCERS, INFLAMMATION AND IMMUNE DISEASES

Beijing Innocare Pharma T...

1. A compound represented by formula (I),or its tautomers, mesomers, racemates, enantiomers, diastereoisomers, mixtures thereof, or a pharmaceutically acceptable salt thereof:wherein:
A1, A2 and A3 are each independently selected from the group consisting of CR1 and N;
B1 is independently selected from the group consisting of C3-8 cyclic group, 3- to 8-membered heterocyclic group, aryl, and heteroaryl, wherein the cyclic group, heterocyclic group, aryl or heteroaryl is optionally substituted with one or more G1;
B2 is independently selected from the group consisting of H, C3-8 cyclic group, 3- to 8-membered heterocyclic group, aryl and heteroaryl, wherein the cyclic group, heterocyclic group, aryl or heteroaryl is optionally substituted with one or more G2;
L1 is independently selected from the group consisting of —C0-2 alkyl-, —CR5R6—, —C1-2 alkyl (R5)(OH)—, —C(O)—, —CR5R6O—, —OCR5R6—, —SCR5R6—, —CR5R6S—, —NR5—, —NR5C(O)—, —C(O)NR5—, —NR5CONR6—, —CF2—, —O—, —S—, —S(O)m—, —NR5S(O)2— and —S(O)2NR5—;
L2 is independently selected from the group consisting of —C0-4 alkyl-, —C(O)—, —O—, —NR7—, —NR7C(O)— and —NR7S(O)2—;
X is independently selected from the group consisting of C0-4 alkyl, C3-8 cyclic group, 3- to 8-membered heterocyclic group, aryl and heteroaryl, wherein the alkyl, cyclic group, heterocyclic group, aryl or heteroaryl is optionally substituted with one or more G3;
Y is independently selected from the group consisting of —C(O)—, —NR8C(O)—, —S(O)m— and —NR8S(O)m—;
R1 is independently selected from the group consisting of H, D, C0-4 alkyl, halogen and cyano;
bond is a double bond or a triple bond;
when bond is a double bond, R2, R3 and R4 are each independently selected from the group consisting of H, D, cyano, halogen, alkyl, cyclic group, heterocyclic group, aryl, and heteroaryl, wherein the alkyl, cyclic group, heterocyclic group, aryl or heteroaryl is optionally substituted with one or more G4; and when bond is a triple bond, R3 and R4 are absent, and R2 is independently selected from the group consisting of H, D, cyano, halogen, alkyl, cyclic group, heterocyclic group, aryl and heteroaryl, wherein the alkyl, cyclic group, heterocyclic group, aryl or heteroaryl is optionally substituted with one or more G4; wherein R3 and R2 , together with the carbon atom attached thereto, can form a ring which contains optionally a heteroatom;
R5, R6, R7 and R8 are each independently selected from the group consisting of H, D, C0-8 alkyl, C3-8 cyclic group, 3- to 8-membered heterocyclic group, aryl, and heteroaryl, wherein the alkyl, cyclic group, heterocyclic group, aryl or heteroaryl is optionally substituted with one or more G5;
G1, G2, G3, G4 and G5 are each independently selected from the group consisting of H, D, halogen, cyano, alkyl, alkenyl, alkynyl, cyclic group, heterocyclic group, aryl, heteroaryl, —OR9, —OC(O)NR9R10, —C(O)OR10, —C(O)NR9R10, —C(O)R9, —NR9R10, —NR9C(O)R10, —NR9C(O)NR10R11, —S(O)mR10 and —NR9S(O)mR10, wherein the alkyl, alkenyl, alkynyl, cyclic group, heterocyclic group, aryl or heteroaryl is optionally substituted with one or more substituents selected from the group consisting of D, halogen, cyano, C1-8 alkyl, C3-8 cycloalkyl, 3- to 8-membered heterocyclic group, —OR12, —OC(O)NR12R13, —C(O)OR12, —C(O)NR12R13, —C(O)R12, —NR12R13, —NR12C(O)R13, —NR12C(O)NR13R14, —S(O)mR12, and —NR12S(O)mR13;
R9, R10, R11, R12, R13 and R14 are each independently selected from the group consisting of H, C1-6 alkyl, C1-C6 heteroalkyl, C3-8 cycloalkyl, 3- to 8-membered monocyclic heterocyclic group, monocyclic heteroaryl and monocyclic aryl; and
m is 1 or 2.

US Pat. No. 10,336,754

PYRIMIDINONES AS FACTOR XIA INHIBITORS

Bristol-Myers Squibb Comp...

1. A method for the treatment or prophylaxis of a venous cardiovascular thromboembolic disorder comprising administering to a patient in need thereof a therapeutically effective amount of a compound of Formula (VII):
or a pharmaceutically acceptable salt thereof, wherein:
ring A is independently selected from

ring B is independently selected from

R1 is independently selected from H and C1-4 alkyl;
R10 is independently selected from H, F, Cl, CF3, CHF2, and COOH;
R3c is independently selected from H, CHF2, CD3, CH3, and

R8b is independently selected from H and F; and
R8c is independently selected from H, F, Cl, CH3, and OCH3.

US Pat. No. 10,336,753

PROCESS FOR THE PREPARATION OF APIXABAN AND INTERMEDIATES THEREOF

Unichem Laboratories Limi...

1. A process for preparation of lactam compound of formula (18) comprising steps of;a. reacting amino-morpholine compound of formula (17) with compound of formula (22) in presence of inorganic base or aqueous solution of inorganic base or absence of any base optionally in presence of phase transfer catalyst to obtain amide-compound of formula (23), wherein X is leaving group;
b. optionally isolating the amide-compound of formula (23); and
c. cyclizing amide-compound of formula (23) in presence of inorganic base or aqueous solution of inorganic base optionally in presence of phase transfer catalyst to obtain a lactam compound of formula (18).

US Pat. No. 10,336,752

TYK2 INHIBITORS, USES, AND METHODS FOR PRODUCTION THEREOF

Nimbus Lakshmi, Inc., Ca...

3. The mesylate salt of the compound of claim 2.

US Pat. No. 10,336,751

TRICYCLIC 4-PYRIDONE-3-CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION

Hoffmann-La Roche Inc., ...

1. A compound of formula (I),
wherein:
R1, R2, R3 and R4 are independently selected from C1-6alkyl, haloC1-6alkyl, hydrogen, halogen, amino, cyano, pyrrolidinyl and OR8;
R5, R6, R7 are independently selected from hydrogen, C1-6alkyl or haloC1-6alkyl;
R8 is hydrogen; C1-6alkyl; haloC1-6alkyl; C3-7cycloalkylC1-6alkyl; phenylC1-6alkyl; hydroxyC1-6alkyl; C1-6alkoxyC1-6alkyl; C1-6alkylsulfanylC1-6alkyl; C1-6alkylsulfonylC1-6alkyl; cyanoC1-6alkyl; aminoC1-6alkyl; C1-6alkylaminoC1-6alkyl; diC1-6alkylaminoC1-6alkyl; C1-6alkylcarbonylaminoC1-6alkyl; C1-6alkylsulfonylaminoC1-6alkyl; C1-6alkoxycarbonylaminoC1-6alkyl; pyrazolylC1-6alkyl or triazolylC1-6alkyl;
or a pharmaceutically acceptable salt, or an enantiomer, or diastereomer thereof.

US Pat. No. 10,336,750

COMPOSITION AND METHODS FOR THE TREATMENT OF CAMKK2-MEDIATED DISORDERS

Duke University, Durham,...

1. A method of modulating CaMKK2 in a subject comprising administering to the subject an effective amount of a compound comprising the Formula (I):
or a pharmaceutically acceptable salt, solvate, hydrate, or derivative thereof,
wherein R1 and R2 are Hydrogen (H), and R3 is selected from the group consisting of

US Pat. No. 10,336,749

METHOD FOR THE PREPARATION OF (4S)-4-(4-CYANO-2-METHOXYPHENYL)-5-ETHOXY-2,8-DIMETHYL-1,4-DIHYDRO-1-6-NAPHTHYRIDINE-3-CARBOXAMIDE AND THE PURIFICATION THEREOF FOR USE AS AN ACTIVE PHARMACEUTICAL INGREDIENT

BAYER PHARMA AKTIENGESELL...

1. A process for preparing a compound of the formula (I)
comprising separating a racemic compound of the formula (XIII) into its enantiomers, wherein the compound of the formula (XIII)

is prepared by reacting a compound of the formula (XVIII)

with an orthoester (XX)

where R may be H or methyl, wherein
the compound of the formula (XVIII)

is prepared by reacting compounds of the formula (XVI a,b)

with a compound of the formula (IX)

and wherein
the compound of the formula (XVI a,b) is prepared by reacting a compound of the formula (VI)

with a compound of the formula (XVII)

US Pat. No. 10,336,748

METHYOXY-SUBSTITUTED PYRROLOPYRIDINE MODULATORS OF RORC2 AND METHODS OF USE THEREOF

Pfizer Inc., New York, N...

1. A compound of Formula I:or a pharmaceutically acceptable salt thereof, wherein,X is phenyl optionally substituted with one, two, three, four or five substituents independently selected from the group consisting of —CH3, —CH2CH3, —CH2OH, —OH, —OCH3, —SCH3, —OCH2CH3, —OCH2CH2OH, —OCH2CH2OCH3, —F, —Cl, —Br and —CN;
R1 is —CH3 or —CH2CH3;
W is

 optionally substituted with one, two, three, four or five —CH3; and
R2 is (C1-C6)alkyl, (C3-C10)cycloalkyl, phenyl, tetrahydrothiophenyl, thietanyl or indanyl, optionally substituted with one, two, three, four or five substituents independently selected for each occurrence from the group consisting of —F, —Cl, —Br, —OH, (C1-C3)alkyl, (C1-C3)haloalkyl and (C3-C10)cycloalkyl.

US Pat. No. 10,336,747

PYRIMIDO[4,5-B]INDOLE DERIVATIVES AND USE THEREOF IN THE EXPANSION OF HEMATOPOIETIC STEM CELLS

1. A compound of general formula I or IIor a salt thereof,wherein:Z is
1) —P(O) (OR1) (OR1),
2) —C(O)OR1,
3) —C(O)NHR1,
4) —C(O)N(R1)R1,
5) —C(O)R1,
6) —SR1,
7) —S(O)2NH2,
8) —S(O)2NHR1,
9) —S(O)2N(R1)R1,
10) —S(O)R1,
11) —S(O)2R1,
12) -L,
13) -benzyl optionally substituted with 1, 2 or 3 RA or R1 substituents,
14) -L-heteroaryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and the heteroaryl groups,
15) -L-heterocyclyl optionally substituted with one or more RA or R1 substituents attached on either one or both the L and the heterocyclyl groups,
16) -L-aryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and the heteroaryl groups,
17) -heteroaryl optionally substituted with one or more RA or R1 substituents, or
18) -aryl optionally substituted with one or more RA or R1 substituents, and wherein each substituent is optionally attached to the L group if it is not already present, and wherein, when (R1) and R1 are attached to a nitrogen atom, optionally they join together with the nitrogen atom to form a 3 to 7-membered ring which optionally includes one or more other heteroatom selected from N, O and S, optionally the is substituted with one or more R1 or RA;
W is
1) —OR1,
2) -L-OH,
3) -L-OR1,
4) —SR1,
5) —CN,
6) —P(O)(OR1)(OR1),
7) —NHR1,
8) —N(R1)R1,
9) -L-NH2,
10) -L-NHR1,
11) -L-N(R1)R1,
12) -L-SR1,
13) -L-S(O)R1,
14) -L-S(O)2R1,
15) -L-P(O)(OR1)(OR1),
16) —C(O)OR1,
17) —C(O)NH2,
18) —C(O)NHR1,
19) —C(O)N(R1)R1,
20) —NHC(O)R1,
21) —NR1C(O)R1,
22) —NHC(O)OR1,
23) —NR1C(O)OR1,
24) —OC(O)NH2,
25) —OC(O)NHR1,
26) —OC(O)N(R1)R1,
27) —OC(O)R1,
28) —C(O)R1,
29) —NHC(O)NH2,
30) —NHC(O)NHR1,
31) —NHC(O)N(R1)R1,
32) —NR1C(O)NHR2,
33) —NR1C(O)NHR1,
34) —NR1C(O)N(R1)R1,
35) —NHS(O)2R1,
36) —NR1S(O)2R1,
37) —S(O)2NH2,
38) —S(O)2NHR1,
39) —S(O)2N(R1)R1,
40) —S(O)R1,
41) —S(O)2R1,
42) —OS(O)2R1,
43) —S(O)2OR1,
44) -benzyl optionally substituted with 1, 2 or 3 RA or R1 substituents,
45) -L-heteroaryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and the heteroaryl groups,
46) -L-heterocyclyl optionally substituted with one or more RA or R1 substituents attached on either or both the L and the heterocyclyl goups,
47) -L-aryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and aryl groups,
48) -L-NR1(R1),
49) -L-(N(R1)-L)n—N(R1)R1,
50) -L-(N(R1)-L)n-heteroaryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and heteroaryl groups,
51) -L-(N(R1)-L)n-heterocyclyl optionally substituted with one or more RA or R1 substituents attached on either or both the L and heterocyclyl groups,
52) -L-(N(R1)-L)n-aryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and aryl groups,
53) —O-L-N(R1)R1,
54) —O-L- heteroaryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and heteroaryl groups,
55) —O-L- heterocyclyl optionally substituted with one or more RA or R1 substituents attached on either or both the L and heterocyclyl groups,
56) —O-L- aryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and aryl groups,
57) —O-L)2—NR1,
58) —O-L-(N(R1)-L)n—N(R1)R1,
59) —O-L-(N(R1)-L)n-heteroaryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and heteroaryl groups,
60) —O-L-(N(R1)-L)n-heterocyclyl optionally substituted with one or more RA or R1 substituents attached on either or both the L and heterocyclyl groups,
61) —O-L-(N(R1)-L)n-aryl optionally substituted with one or more RA or R1 substituents,
62) —S-L-heteroaryl optionally substituted with one or more RA or R1 substituents,
63) —S-L-heterocyclyl optionally substituted with one or more RA or R1 substituents,
64) —S-L-aryl optionally substituted with one or more RA or R1 substituents attached on either or both the L and aryl groups,
65) —S-L)2NR1,
66) —S-L-(N(R1)-L)n-N(R1)R1,
67) —S-L-(N(R1)-L)n-heteroaryl optionally substituted with one or more RA substituents,
68) —S-L-(N(R1)-L)n-heterocyclyl optionally substituted with one or more RA substituents,
69) —S-L-(N(R1)-L)n-aryl optionally substituted with one or more RA substituents,
70) —NR1(R1),
71) —(N(R1)-L)n-N(R1)R1,
72) —N(R1)L)2 —NR1,
73) —(N(R1)-L)n-N(R1)RA,
74) —(N(R1)-L)n-heteroaryl optionally substituted with one or more RA or R1 substituents,
75) —(N(R1)-L)n-heterocyclyl optionally substituted with one or more RA or R1 substituents,
76) —(N(R1)-L)n-aryl optionally substituted with one or more RA or R1 substituents,
77) -heteroaryl optionally substituted with one or more RA substituents, or
78) -aryl optionally substituted with one or more RA substituents,
and wherein each substituent is optionally attached to the L group if it is not already present, and wherein when two R1 substituents are present on the same nitrogen atom, then each R1 substituent is independently selected from the list of R1 values described thereafter, and wherein n is an integer equal to either 0, 1, 2, 3, 4, or 5,
and wherein, when (R1) and R1 are attached to a nitrogen atom, optionally they join together with the nitrogen atom to form a 3 to 7-membered ring which optionally includes one or more other heteroatom selected from N, O and S, optionally the ring is substituted with one or more R1 or RA;
L is
1) —C1-6alkyl,
2) —C2-6alkenyl,
3) —C2-6alkynyl,
4) —C3-7cycloalkyl,
5) —C3-7cycloalkenyl,
6) heterocyclyl,
7) —C1-6alkyl-C3-7cycloalkyl,
8) —C1-6alkyl-heterocyclyl,
9) aryl, or
10) heteroaryl,
and wherein the alkyl, the alkenyl, the alkynyl, the cycloalkyl, the cycloalkenyl, the heterocyclyl, the aryl and the heteroaryl groups are each independently optionally substituted with one or two RA substituent;
R1 is
1) —H,
2) —C1-6alkyl,
3) —C2-6alkenyl,
4) —C2-6aIkynyl,
5) —C3-7cycloalkyl,
6) —C3-7cycloalkenyl,
7) —C1-5perfluorinated,
8) -heterocyclyl,
9) -aryl,
10) -heteroaryl,
11) -benzyl, or
12) 5-[(3aS,4S,6aR)-2-oxohexahydro-1H-thieno[3,4-d]imidazol-4-yl]pentanoyl, and wherein the alkyl, the alkenyl, the alkynyl, the cycloalkenyl, the perfluorinated alkyl, the heterocyclyl, the aryl, the heteroaryl and the benzyl groups are each independently optionally substituted with 1,2 or 3 RA or R1 substituents;
R2 is
1) —H,
2) —C1-6alkyl,
3) —SR1,
4) —C(O)R1,
5) —S(O)R1,
6) —S(O)2R1,
7) -benzyl optionally substituted with 1, 2 or 3 RA or R1 substituents,
8) -L-heteroaryl optionally substituted with one or more RA or R1 substituents attached on either one or both the L and the heteroaryl groups,
9) -L-heterocyclyl optionally substituted with one or more RA or R1 substituents attached on either one or both the L and the heterocyclyl groups,
10) -L-aryl optionally substituted with one or more RA or R1 substituents attached on either one or both the L and the aryl groups,
11) -heteroaryl optionally substituted with one or more RA or R1 substituents, or
12) -aryl optionally substituted with one or more RA or R1 substituents, and wherein each substituent is optionally attached to the L group if it is not already present;
RA is
1) -halogen,
2) —CF3,
3) —OH,
4) —OR1,
5) -L-OH,
6) -L-OR1,
7) —OCF3,
8) —SH,
9) —SR1,
10) —CN,
11) —NO2,
12) —NH2,
13) —NHR1,
14) —NR1R1,
15) -L-NH2,
16) -L-NHR1,
17) -L-NR4R1,
18) -L-SR1,
19) -L-S(O)R1,
20) -L-S(O)2R1,
21) —C(O)OH,
22) —C(O)OR1,
23) —C(O)NH2,
24) —C(O)NHR1,
25) —C(O)N(R1)R1,
26) —NHC(O)R1,
27) —NR1C(O)R1,
28) —NHC(O)OR1,
29) —NR1C(O)OR1,
30) —OC(O)NH2,
31) —OC(O)NHR1,
32) —OC(O)N(R1)R1,
33) —OC(O)R1,
34) —C(O)R1,
35) —NHC(O)NH2,
36) —NHC(O)NHR1,
37) —NHC(O)N(R1)R1,
38) —NR1C(O)NH2,
39) —NR1C(O)NHR1,
40) —NR1C(O)N(R1)R1,
41) —NHS(O)2R1,
42) —NR1S(O)2R1,
43) —S(O)2NH2,
44) —S(O)2NHR1,
45) —S(O)2N(R1)R1,
46) —S(O)R1,
47) —S(O)2R1,
48) —OS(O)2R1,
49) —S(O)2OR1,
50) -benzyl,
51) —N3, or
52) —C(—N?N—)(CF3),
and wherein the benzyl group is optionally substituted with 1, 2 or 3 RA or R1 substituents.

US Pat. No. 10,336,746

RAD51 INHIBITORS

Cyteir Therapeutics, Inc....

1. A compound of the following structure:
or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,336,745

PIPERAZINE-CONTAINING TWO-PHOTON ABSORBING COMPOUNDS

The United States of Amer...

1. A two-photo active compound having a formula:
where Rl and R2 are independently selected from the group consisting of linear or branched alkyl chains having a general formula CnH2n+1, n ranges from about 6 to about 20, and ethoxylated alkyls having a general formula R3(OCH2CH2)mOCH2CH2—, where R3 is a C1 to C4 alkyl group and m ranges from 0 to about 5; and
Y is selected from the group consisting of H, OH, and alkoxyl groups.

US Pat. No. 10,336,743

AMINOPYRIMIDINE KINASE INHIBITORS

Jasco Pharmaceuticals, LL...

1. A compound selected from the group consisting of:or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,336,742

PROCESS FOR PREPARING THIAZOLE DERIVATIVES

Bayer CropScience Aktieng...

1. A process for preparing a compound of formula (I),wherein:R3 is hydrogen;
each R6 is independently halogen or C1-C4-alkylsulfonyloxy; and
n is 0, 1, 2, or 3;
comprising reacting a compound of formula (II) or a salt thereof,
wherein:R3 is as defined for the compound of formula (I);
with a compound of formula (III),
wherein:R6 and n are as defined for the compound of formula (I); and
X is halogen;
in the presence of an acid to form the compound of formula (I).

US Pat. No. 10,336,741

SUBSTITUTED PYRROLIDINES AS FACTOR XIA INHIBITORS FOR THE TREATMENT THROMBOEMBOLIC DISEASES

ONO PHARMACEUTICAL CO., L...

1. A compound represented by formula (I):
wherein Cyc A represents cyclohexyl, phenyl, piperidinyl, piperazinyl, or indole;
Cyc B represents phenyl;
Cyc C represents pyrrolidinyl, piperidinyl, piperazinyl, or morpholinyl;
each R1 may be the same or different and represents (1) —C(?NH)NH2, (2) 5- to 10-membered heteroaryl, (3) C6-C10 aryl or 5- to 10-membered heteroaryl substituted with 1 to 5 groups selected from halogen, C1-4 alkyl, C1-4 alkoxy, —C1-4 alkylene-C1-4 alkoxy, CN, —COOH, —COO—C1-4 alkyl, —CO—NH2, —OCONH2, —OCONH-C1-4 alkyl, —CONH-C1-4 alkyl, —NHCOO—C1-4 alkyl and —NHCO—C1-4 alkyl, (4) C6-C10 aryl, (5) —NH—C(?NH)NH2, (6) C1-4 alkyl, (7) C2-4 alkenyl, (8) C2-4 alkynyl, (9) —C1-4 alkylene-NH2, (10) C1-4 alkoxy, (11) CN, (12) —CO—C1-4 alkyl, (13) halogen or (14) —R10—C(?NR11)NR12R13;
wherein R10 represents (1) a bond or (2) NH;
R11, R12 and R13 each independently represents (1) hydrogen, (2) OH, (3) C1-4 alkyl, (4) C2-4 alkenyl, (5) C2-4 alkynyl, (6) C1-4 alkoxy, (7) —C1-4 alkylene-C1-4 alkoxy, (8) —CO—C1-4 alkyl, (9) —COO—C1-4 alkyl, (10) —OCO—C1-4 alkyl, (11) —CO—R14, (12) —COO—R15 or (13) —OCO—R16, with the proviso that R11, R12 and R13 do not all simultaneously represent hydrogen;
wherein R14, R15 and R16 each independently represents C1-4 alkyl, C2-4 alkenyl or C2-4 alkynyl, which are substituted with 1 to 5 groups selected from C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, halogen, trifluoromethyl, OH, —COO—C1-4 alkyl, COOH, oxo, C1-4 alkoxy, C6-C10 aryl, 5- to 10-membered heteroaryl and NR17R18;
wherein R17 and R18 each independently represents (1) hydrogen, (2) C1-4 alkyl, (3) C2-4 alkenyl or (4) C2-4 alkynyl;
t represents an integer of 0 to 6;
each R2 may be the same or different and represents (1) —COOH, (2) —COO—C1-4 alkyl, (3) —COO—C1-4 alkylene-C1-4 alkoxy, (4) —NH2, (5) —NH—C1-4 alkyl, (6) —NH—C1-4 alkylene-C1-4 alkoxy, (7) —NHCO—C1-4 alkyl, (8) —NHCO—C1-4 alkylene-C1-4 alkoxy, (9) —NHCOO—C1-4 alkyl, (10) —NHCOO—C1-4 alkylene-C1-4 alkoxy, (11) —CONH2, (12) —CONH—C1-4 alkyl, (13) —CONH—C2-4 alkylene-C1-4 alkoxy, (14) halogen, (15) —SO2—C1-4 alkyl, (16) oxo, (17) C1-4 alkoxy, (18) —CO—C1-4 alkyl, (19) —CO—C1-4 alkylene-C1-4 alkoxy or (20) —COO— C1-4 alkyl substituted with 1 to 5 groups selected from C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, halogen, trifluoromethyl, OH, —COO—C1-4 alkyl, COOH, oxo, C1-4 alkoxy, C6-C10 aryl, 5- to 10-membered heteroaryl and NR19R20;
wherein R19 and R20 each independently represents (1) hydrogen, (2) C1-4 alkyl, (3) C2-4 alkenyl or (4) C2-4 alkynyl;
m represents an integer of 0 to 6;
each R3 may be the same or different and represents (1) —SO2—R6-R7, (2) oxo, (3) —CO—C1-4 alkyl, (4) —CO—NH2, (5) —SO2—NH2 or (6) —COO—C1-4 alkyl;
n represents an integer of 0 to 6;
R6 represents (1) a bond or (2) NH;
R7 represents (1) C1-4 alkyl, (2) Cyc D or (3) C1-4 alkyl or Cyc D substituted with 1 to 5 R8;
wherein Cyc D represents C3-C8 cycloalkyl, 5- to 10-membered heterocycloalkyl, C6-C10 aryl or 5- to 10-membered heteroaryl;
each R8 may be the same or different and represents (1) —COOH, (2) —COO—C1-4 alkyl, (3) —COO—C1-4 alkylene-C1-4 alkoxy, (4) —NH2, (5) —NH—C1-4 alkyl, (6) —NHCO—C1-4 alkyl, (8) —CONH2, (12) —CONH—C1-4 alkyl (13) OH or (14) halogen;
R4 represents (1) a bond, (2) C1-4 alkylene, (3) C2-4 alkenylene or (4) C2-4 alkynylene;
R5 represents (1) —CONH—, (2) Cyc E or (3) Cyc E substituted with 1 to 5 R9;
wherein Cyc E represents C3-C8 cycloalkyl, 5- to 10-membered heterocycloalkyl, C6-C10 aryl or 5- to 10-membered heteroaryl; and
each R9 may be the same or different and represents C1-4 alkyl or halogen;
a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof.

US Pat. No. 10,336,740

NITROCATECHOL DERIVATIVES AS COMT INHIBITORS

1. A process for the preparation of compounds according to formula I,whereinR1 and R2 independently from each other represent hydrogen, optionally substituted lower alkanoyl or optionally substituted lower aroyl;
R3 represents a pyridine N-oxide group according to the formula A, B or C, which is connected as indicated by the unmarked bond:

comprising steps wherein a compound of formula IIA, IIB or IIC,
wherein R4, R5, R6 and R7 independently from each other represent hydrogen, C1-C6-alkyl, C1-C6-thioalkyl, C1-C6-alkoxy, C6-C12-aryloxy, a C6-C12-thioaryl group, C1-C6-alkanoyl, a C7-C13-aroyl group, amino, C1-C6-alkylamino, C1-C6-dialkylamino, C3-C12-cycloalkylamino, C3-C12-heterocycloalkylamino, C1-C6-alkylsulphonyl, C6-C12-arylsulphonyl, halogen, C1-C6-haloalkyl, trifluoromethyl, cyano, nitro or a heteroaryl group; or where two or more of residues R4, R5, R6 and R7 taken together represent aliphatic or heteroaliphatic rings or aromatic or heteroaromatic rings,is subjected to cyclisation with a compound of formula III,
wherein R8 and R9 independently from each other represent hydrogen or suitable protective groups for aromatic hydroxyl groups, under conditions suitable to produce oxadiazole derivatives of formula IVA, IVB or IVC,optionally followed by removal of the protecting groups R8 and or R9.

US Pat. No. 10,336,739

4-HYDROXY-3-(HETEROARYL)PYRIDINE-2-ONE APJ AGONISTS

Bristol-Myers Squibb Comp...

1. A compound having the structure:
or a stereoisomer, a tautomer, or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,336,738

COMPOUNDS THAT MODULATE INTRACELLULAR CALCIUM

CALCIMEDICA, INC., La Jo...

1. A compound having the structure of Formula (I):
wherein:
R1 is

X is S, O, or NRS;
Y is independently selected from CR10 or N;
R2 is aryl, heteroaryl, fused aryl or fused heteroaryl; wherein aryl, heteroaryl, fused aryl or fused heteroaryl is optionally substituted with at least one R3;
R3 is independently selected from the group consisting of H, F, D, Cl, Br, I, —CN, —NO2, —OH, —CF3, —OCF3, —OR5, optionally substituted C1-C6alkyl, optionally substituted C3-C8cycloalkyl, optionally substituted C1-C6heteroalkyl, C1-C6haloalkyl, optionally substituted C2-C8heterocycloalkyl, optionally substituted aryl, optionally substituted O-aryl, and optionally substituted heteroaryl;
R5 is selected from the group consisting of H, C1-C6alkyl, C1-C6haloalkyl, C3-C8cycloalkyl, phenyl, and benzyl; and
R9 and R10 are each independently selected from H, D, optionally substituted C1-C6alkyl, halogen, C1-C6 alkylcarbonyl, or CF3;
or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or pharmaceutically acceptable prodrug thereof.

US Pat. No. 10,336,737

METAL CATALYZED DEAROMATIVE 1,2-CARBOAMINATION

The Board of Trustees of ...

1. An urazole compound of Formula I:or the enantiomer thereof;wherein
R1 is alkyl, alkenyl, aryl, or heteroaryl;
R2, R3 and R6 are each independently H, D, halo, alkyl, cycloalkyl, ORA, N(RA)2, aryl, heteroaryl, or R2 and R3 taken together form a ring wherein the ring is unsaturated or aromatic;
R4 is H, alkyl, or cycloalkyl;
R5 is H, alkyl, cycloalkyl, or aryl;
each RA is independently H, alkyl, cycloalkyl, C(?O)RB, aryl, or heteroaryl; and
each RB is independently H, OH, halo, alkyl, aryl, heteroaryl, or N(RA)2, wherein N(RA)2 is not recursive with C(?O)RB;
wherein each alkyl, cycloalkyl, alkenyl, aryl, and heteroaryl is optionally substituted with one or more substituents.

US Pat. No. 10,336,736

MODULATORS OF CHEMOKINE RECEPTORS

ChemoCentryx, Inc., Moun...

1. A method of treating a CXCR2- and/or CCR6-mediated disease or condition in a subject in need thereof, said method comprising administering an effective amount of a compound of formula (A1) to said subject,
wherein
R1a is selected from CH3 and Cl;
R1b is H or is CH3;
R3 is H or D;
R4 is H, C1-8 alkyl, OH, —NRaRb, —C1-4 alkoxy, and Y; wherein the C1-8 alkyl is optionally substituted with halogen, —CN, —CO2Ra, —CONRaRb, —C(O)Ra, OC(O)NRaRb, —NRaC(O)Rb, —NRaC(O)2Rc, —NRaC(O)NRaRb, —NRaRb, —ORa, —S(O)2NRaRb, —NRaS(O)2Rb and Y, wherein Y is a 4 to 8 membered cycloheteroalkyl group or a 3 to 8 membered cycloalkyl group or a 5- or 6-membered aryl or heteroaryl group any of which is optionally substituted with from 1 to four substituents selected from halogen, oxo, —CN, —C1-6 alkyl, —C1-6 alkoxy, —C1-6 hydroxyalkyl, —C1-6 haloalkyl, O— C1-6 haloalkyl, —C1-4alkyl-O—C1-4 alkyl, —C1-6 alkyl-NRaRb, —C1-6 alkyl-CO2H, —C1-6 alkyl-CO2Ra, —C1-6 alkyl-CONRaRb, —C1-6 alkyl-C(O)Ra, —C1-6 alkyl-OC(O)NRaRb, —C1-6 alkyl-NRaC(O)Rb, —C1-6 alkyl-NRaC(O)2Rc, —C1-6 alkyl-NRaC(O)NRaRb, —C1-6 alkyl-ORa, —C1-6 alkyl-S(O)2NRaRb, —C1-6 alkyl-NRaS(O)2Rb, —CO2Ra, —CONRaRb, —C(O)Ra, —OC(O)NRaRb, —NRaC(O)Rb, —NRaC(O)2Rc, —NRaC(O)NRaRb, —NRaRb, —ORa, —S(O)2NRaRb, —NRaS(O)2Rb, —CH2CO2Ra; each Ra and Rb is independently selected from hydrogen, C1-4 alkyl, C1-4 hydroxyalkyl and C1-4 haloalkyl, and Rc is selected from C1-4 alkyl, C1-4 hydroxyalkyl and C1-4 haloalkyl; and wherein the 4 to 8 membered cycloheteroalkyl group and the 3 to 8 membered cycloalkyl group may additionally be optionally substituted with oxo;
R5a and R5b are each independently selected from H, F, Cl, Br and CH3;
R6a and R6b are each members independently selected from the group consisting of H, C1-4 alkyl, C1-4 hydroxyalkyl and C1-4 haloalkyl; or optionally R6a and R6b are taken together to form oxo (?O) or a 4 to 6 membered cycloheteroalkyl group or a 3 to 6 membered cycloalkyl group; and
R7 is methyl or ethyl; or a pharmaceutically acceptable salt, solvate or hydrate thereof.

US Pat. No. 10,336,735

SMALL MOLECULE INHIBITORS OF FIBROSIS

THE SCRIPPS RESEARCH INST...

1. A compound of Formula (I) or Formula (Ia):
wherein:
R1 is —CH(CH3)CH2CH2CH3 or —CH(CH2CH3)2;
R5 is H, —CN, halogen, haloalkyl, alkyl, —NR13R14, -alkylene(NR13R14), and —SO2R13;
each R8 is independently selected from halogen, —OH, —NO2, —N3, —CN, alkyl, alkoxy, haloalkoxy, haloalkyl, hydroxyalkyl, alkoxyalkyl, -alkylene(NR13R14), -alkylene(cycloalkyl), -alkylene(heterocyclyl), cycloalkyl, heterocyclyl, aryl, heteroaryl, —SR13, —SOR13, —SO2R13, —SO2NR13R14, —NR13R14, —NR13SO2R14, —NR13C(O)R14, —NR13C(O)OR14, —NR13C(O)NR13R14, —C(O)R14, —C(O)OR14, and —C(O)NR13R14; or two adjacent R8 form a heterocyclyl ring;
each R13 and each R14 is each independently selected from H, alkyl, cycloalkyl, heterocyclylalkyl, haloalkyl, hydroxyalkyl, alkoxyalkyl, arylalkyl, heteroarylalkyl, aryl, and heteroaryl; or R13 and R14 taken together form a heterocycle with the atoms to which they are attached; and
n is selected from 0, 1, 2, 3, and 4;
or a pharmaceutically acceptable salt, pharmaceutically acceptable solvate, or pharmaceutically acceptable prodrug thereof.

US Pat. No. 10,336,733

ARYL ACYLSULFONAMIDES AS BLT1 ANTAGONISTS

1. A compound of structural formula I:
or a pharmaceutically acceptable salt thereof; wherein
A is heteroaryl, wherein heteroaryl is unsubstituted or substituted with 1-3 substituents independently selected from C1-6alkyl and halogen;
B is selected from the group consisting of:
(1) aryl, and
(2) heteroaryl,
wherein aryl and heteroaryl are unsubstituted or substituted with 1-4 substituents independently selected from C1-6alkyl and halogen;
X is selected from the group consisting of:
(1) —C(O)NHSO2CF3,
(2) —C(O)NHSO2CH2CF3,
(3) —C(O)NHSO2CHF2,
(4) —C(O)NHSO2C1-6alkyl,
(5) —C(O)NHSO2CH2C3-6cycloalkyl, and
(6) —C(O)NHSO2C3-6cycloalkyl,
wherein alkyl and cycloalkyl are unsubstituted or substituted with 1-3 substituents independently selected from C1-6alkyl;
Z is selected from the group consisting of:
(1) hydrogen,
(2) —C1-6alkyl, and
(3) phenyl,
wherein alkyl and phenyl are unsubstituted or substituted with 1-4 substituents independently selected from C1-6alkyl;
Ra is selected from the group consisting of:
(1) hydrogen,
(2) halogen, and
(3) C1-6alkyl; and
Rb is selected from the group consisting of:
(1) hydrogen,
(2) halogen, and
(3) C1-6alkyl.

US Pat. No. 10,336,732

1-HETEROCYCLYL ISOCHROMANYL COMPOUNDS AND ANALOGS FOR TREATING CNS DISORDERS

Sunovion Pharmaceuticals ...

1. A method for treating a neurological or psychiatric disorder in a patient, wherein the disorder is major depression, schizophrenia, bipolar disorder, obsessive compulsive disorder (OCD), panic disorder, posttraumatic stress disorder (PTSD), mania, or psychosis, comprising administering to said patient an effective amount of a compound of formula:
or a pharmaceutically acceptable salt thereof, wherein:
m is 0, 1, or 2;
R is —H or C1-C3 alkyl;
Ra is —H or C1-C3 alkyl;
R1, R2, R3, and R4 are independently —H, halo, —OH, —NH2, C1-C3 alkyl, —OR7, —NHR7, —N(R7)R7, —CN, phenyl, or 5- or 6-membered heteroaryl, wherein:
each instance of R7 independently is unsubstituted C1-C2 alkyl or C1-C2 alkyl substituted with 1-3 halo,
each instance of C1-C3 alkyl independently is unsubstituted or substituted with 1-3 halo, and
the phenyl or heteroaryl is unsubstituted or substituted with 1 or 2 groups independently selected from halo, —OH, —OCH3, —OCF3, —NH2, —NH(CH3), —N(CH3)2, —CH3, ethyl, —CF3, and —CN,
optionally wherein
two adjacent instances of R1, R2, R3, and R4 together form —O—CH2—O—, —O—CH(CH3)—O—, —O—C(CH3)2—O—, —O—CH2—CH2—O—, or —O—C(CH3)2—C(CH3)2—O—;
each instance of R5 independently is halo, —CH3, or ethyl;
each instance of R6 independently is halo, —CH3, ethyl or —OH;
w is 0, 1, or 2; and
provided that the compound is not:

US Pat. No. 10,336,731

SUBSTITUTED 1H-INDOLE-2-CARBOXAMIDE COMPOUNDS AS INDOLEAMINE-2,3-DIOXYGENASE INHIBITORS

Iomet Pharma Ltd., (GB)

1. A compound of formula (I), or a pharmaceutically acceptable salt thereof:
wherein R2 is selected from Cl, —Br and —CN;
R1 and R4 are independently selected from —H and —F;
R631, R632, R641 and R642 are independently selected from —H, —F and C1-C3 alkyl;
R651 and R652 are independently selected from —H, and C1-C3 alkyl; and
wherein at least one of R631, R632, R641, and R642 is not —H.

US Pat. No. 10,336,730

SUBSTITUTED GLYCINE DERIVED FXIA INHIBITORS

Bristol-Myers Squibb Comp...

8. A pharmaceutical composition comprising one or more compounds according to claim 1 and a pharmaceutically acceptable carrier or diluent.

US Pat. No. 10,336,729

4-CYANO-BENZYL CARBAMIMIDOYLCARBAMATE DERIVATIVES AND THEIR USE AS AOC3 INHIBITORS

Boehringer Ingelheim Inte...

1. A compound of formula (I)
wherein
R1 is H or halogen;
R2 is H or halogen;
R3 is H or halogen;
with the proviso that not more than one of R1, R2 and R3 is halogen;
A is selected from the group consisting of:

R4 is selected from the group consisting of: pyrrolidinyl, piperidinyl, piperazinyl, tetrahydropyranyl, oxazolidinyl, C3-8-cycloalkyl, phenyl, pyridinyl, pyrazinyl, pyridazinyl, pyrimidinyl, [1,3,5]triazinyl, triazolyl, thiazolyl, imidazo[1,2-a]pyridin-2-yl, oxazolyl and oxadiazolyl,
wherein each R4 is optionally substituted with one or more groups independently of each other selected from the group consisting of halogen, OH, CO2H, CN, CF3, C1-3-alkyl, C1-3-alkyl-O—, (RN)2N—, C1-3-alkyl-C(?O)—, C1-4-alkyl-O—C(?O)—, (RN)2N—C(?O)—, (RN)2N—C1-3-alkyl-, C3-6-cycloalkyl-C1-3-alkyl-O—, C1-3-alkyl-SO2—, (RN)2N—SO2— and C1-3-alkyl-C(?O)—(RN)N—C1-3-alkyl-; and
wherein a —CH2— group of the pyrrolidinyl, oxazolidinyl, piperidinyl or piperazinyl group of R4 is optionally replaced with a —C(?O)— group;
RN is H or C1-4-alkyl;
R5 is CN or OH;
or, R4 and R5 groups together with the carbon atom, to which they are attached, may form the following group:
wherein each of the above-mentioned alkyl and —O-alkyl groups may be linear or branched and are optionally substituted by one or more F;or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,336,728

SALTS OF A PIM KINASE INHIBITOR

Incyte Corporation, Wilm...

1. A solid form of a compound having the formula:wherein the solid form is crystalline having Form I.

US Pat. No. 10,336,727

HISTONE DEMETHYLASE INHIBITORS

CELGENE QUANTICEL RESEARC...

1. A compound of Formula (IV), or a pharmaceutically acceptable salt thereof,wherein,R1 is hydrogen or alkyl; and
R2 is heteroaryl;with the provision that R2 is not selected from the group consisting of:

US Pat. No. 10,336,726

3-METHYL-PYRROLIDINE-2,5-DIONE DERIVATIVES USEFUL AS CGRP RECEPTOR ANTAGONISTS

Eli Lilly and Company, I...

14. A pharmaceutical composition, comprising a compound or salt, or hydrate thereof, according to claim 1 with one or more pharmaceutically acceptable carriers, diluents, or excipients.

US Pat. No. 10,336,725

CHEMICAL COMPOUNDS

AstraZeneca AB, Sodertal...

1. A method of treating an epithelial sodium channel (ENaC) mediated disease state in a mammal suffering from, or at risk of, said disease, which comprises administering to the mammal in need of such treatment a therapeutically effective amount of a compound which is 3,5-diamino-6-chloro-N—((R)-3-((4-((2-(hexyl((2S,3R,4R)-2,3,4,5-tetrahydroxypentyl)amino)ethyl) carbamoyl)benzyl)amino)-2-(2-methylbenzyl)propyl)pyrazine-2-carboxamide having the below formula:
or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,336,724

D-AMINO ACID OXIDASE INHIBITORS AND THERAPEUTIC USES THEREOF

SyneuRx International (Ta...

1. A compound of Formula (I):
or a pharmaceutically acceptable salt thereof, wherein:
the moiety

the moiety

 is bonded to E;
X is aryl;
Y is a five-membered heteroaryl with 1-2 ring heteroatoms selected from the group consisting of nitrogen and oxygen;
Z is aryl;
L1 is CH2 or C2-10 alkyl;
L2 is CH2, C2-10 alkyl, —CH2S—, or absent;
provided that when L2 is present, L2 is bonded to B or C, and when L2 is absent, Z is aryl fused with BC.

US Pat. No. 10,336,723

INHIBITORS OF TRKA KINASE

GVK BIOSCIENCES PRIVATE L...

1. A compound of Formula I:
or stereoisomers, tautomers, or pharmaceutically acceptable salts, isotopologues, solvates, or prodrugs thereof, wherein:
Ra and Rb are each independently selected from H, alkyl, alkenyl, alkynyl, haloalkyl, halogen, hydroxy, hydroxyalkyl, alkoxy, haloalkoxy, optionally substituted phenyl, optionally substituted 5-6 membered aromatic ring having 1-3 heteroatoms selected from O, N, and S or Ra and Rb together forms carbonyl group, optionally substituted phenyl which is further optionally substituted with a halogen;
Rc and Rd is H, alkyl, alkenyl, alkynyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, optionally substituted phenyl, optionally substituted 5-6 membered aromatic ring having 1-3 heteroatoms selected from O, N, or S or Rc and Rd together form a ring (4-6 membered) with or without a hetero atom;
R1 is alkenyl, alkynyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, (1-3C alkoxy)(1-3C)alkyl, (1-4C alkoxycarbonyl) (1-6Calkyl), mono, di, tri halo(1-4C alkyl), alkoxy (1-3C) carbonyl, (1-3C alkyl)aminocarbonyl, cyano(1-3C alkyl), (1-3C haloalkoxy)(1-3C)alkyl, 3-6 membered heterocyclic ring with one or more heteroatom selected from O, N or S and optionally substituted with one or more substituents independently selected from H, alkyl, alkenyl, alkynyl, haloalkyl, halogen, hydroxy, alkoxy, haloalkoxy, nitro or amino, a 9-10 membered bicyclic heteroaryl having 1-3 ring nitrogen atoms;
R2 and R3 are independently selected from H, alkyl, alkenyl, alkynyl, isopropyl, tert butyl, haloalkyl, halogen, hydroxy, alkoxy, haloalkoxy, optionally substituted phenyl, or optionally substituted 5-6 membered aromatic ring having 1-3 heteroatoms selected from O, N, or S with the provision that R2 and R3 cannot be hydrogen atoms at the same time;
L is a NR?C(O)N(R?) wherein each R? is independently selected from H or alkyl;Het-Ar ring is selected from the group consisting of H1A-H1G;
R4 and R5 are each independently selected from the group consisting of H, alkyl, alkenyl, alkynyl, isopropyl, tert-butyl, haloalkyl, halogen, mono, di, tri halo(1-4C alkyl)hydroxy, alkoxy, haloalkoxy, cyano, cycloalkyl(3-7 carbon), optionally substituted phenyl, optionally substituted 5-6 membered heterocyclic ring having 1-3 heteroatoms selected from O, N, or S or 3-6 membered carbocyclic ring having one or more heteroatom selected from O, N or S, —NH2, —N(H)(alkyl), —N(alkyl)2, —N(H)C(O)alkyl, —N(alkyl)C(O)alkyl, —N(H)C(O)O alkyl, —N(alkyl)C(O)Oalkyl, —N(H)SO2(alkyl), —N(alkyl)SO2(alkyl), —C(O)alkyl, —C(O)OH, —(O)Oalkyl, —C(O)NH2, —C(O)N(H)(alkyl), —C(O)N(alkyl)2, —S(alkyl), —S(O)alkyl, —S(O)2alkyl, —S(O)2N(H)2, —S(O)2N(H)(alkyl) and —S(O)2N(alkyl)2.

US Pat. No. 10,336,722

TETRAHYDROQUINOLINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS

FORMA Therapeutics, Inc.,...

1. A composition comprising a compound in an enantiomeric excess (e.e. %) of at least 94% as determined by chiral HPLC analysis, wherein the compound is:

US Pat. No. 10,336,721

BIARYLTRIAZOLE INHIBITORS OF MACROPHAGE MIGRATION INHIBITORY FACTOR

Yale University, New Hav...

1. A compound of Formula (I):or a pharmaceutically acceptable salt thereof, wherein:X3 is CR3 or N;
X8 is CR8 or N;
R3 is selected from the group consisting of H, halogen, C1-6 alkyl, and C1-6 haloalkyl;
R4 is selected from the group consisting of H, halogen C1-6 alkyl, and C1-6 haloalkyl;
R5, R6, R7 and R8 are each independently selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, 4-10 membered heterocycloalkyl-C1-4 alkylene, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(?NRe1)NRc1Rd1, NRc1C(?NRe1)NRc1Rd1, S(O)Rb1, S(O)2Rb1, NRc1S(O)2Rb1 and S(O)2NRc1Rd1;
wherein each of said C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl forming R5, R6, R7 or R8 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of halogen, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(?NRe2)NRc2Rd2, NRc2C(?NRe2)NRc2Rd2, S(O)Rb2, S(O)2Rb2, NRc2S(O)2Rb2, and S(O)2NRc2Rd2 and
wherein each of said C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene and 4-10 membered heterocycloalkyl-C1-4 alkylene forming R5, R6, R7 or R8 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of C1-6 alkyl, halogen, C1-6 haloalkyl, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(?NRe2)NRc2Rd2, NRc2C(?NRe2)NRc2Rd2, S(O)Rb2, S(O)2Rb2, NRc2S(O)2Rb2, and S(O)2NRc2Rd2;
or any one of R5, R6, R7, and R8 may represent a group of formula ArS;
or R6 and R7 in combination with the atoms to which they are attached may form a 5-7 membered carbocyclic or heterocyclic ring that is unsubstituted or substituted by 1, 2 or 3 substituents each independently selected from R9;
or at least one of R5, R6, R7, or R8 may be each independently a water solubilizing group;
each R9 is independently selected from the group consisting of halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, 4-10 membered heterocycloalkyl-C1-4 alkylene, CN, NO2, ORa1, SRa1, C(O)Rb1, C(O)NRc1Rd1, C(O)ORa1, OC(O)Rb1, OC(O)NRc1Rd1, NRc1Rd1, NRc1C(O)Rb1, NRc1C(O)NRc1Rd1, NRc1C(O)ORa1, C(?NRe1)NRc1Rd1, NRc1C(?NRe1)NRc1Rd1, S(O)Rb1, S(O)2Rb1, NRc1S(O)2Rb1, and S(O)2NRc1Rd1;
wherein each of said C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl forming R9 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of halogen, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(?NRe2)NRc2Rd2, NRc2C(?NRe2)NRc2Rd2, S(O)Rb2, S(O)2Rb2, NRc2S(O)2Rb2, and S(O)2NRc2Rd2; and
wherein each of said C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene and 4-10 membered heterocycloalkyl-C1-4 alkylene forming R9 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of C1-6 alkyl, halogen, C1-6 haloalkyl, CN, NO2, ORa2, SRa2, C(O)Rb2, C(O)NRc2Rd2, C(O)ORa2, OC(O)Rb2, OC(O)NRc2Rd2, NRc2Rd2, NRc2C(O)Rb2, NRc2C(O)NRc2Rd2, NRc2C(O)ORa2, C(?NRe2)NRc2Rd2, NRc2C(?NRe2)NRc2Rd2, S(O)Rb2, S(O)2Rb2, NRc2S(O)2Rb2, S(O)2NRc2Rd2, and water solubilizing groups;
Y1, Y2, Y3, Y4, and Y5 are each independently selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, 4-10 membered heterocycloalkyl-C1-4 alkylene, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, C(?NRe3)NRc3Rd3, NRc3C(?NRe3)NRc3Rd3, S(O)Rb3, S(O)2Rb3, NRc3S(O)2Rb3, and S(O)2NRc2Rd2;
wherein each of said C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl forming Y1, Y2, Y3, Y4 or Y5 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of halogen, CN, NO2, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(?NRe4)NRc4Rd4, NRc4C(?NRe4)NRc4Rd4, S(O)Rb4, S(O)2Rb4, NRc4S(O)2Rb4, and S(O)2NRc4Rd4; and
wherein each of said C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene and 4-10 membered heterocycloalkyl-C1-4 alkylene forming Y1, Y2, Y3, Y4 or Y5 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of C1-6 alkyl, halogen, C1-6 haloalkyl, CN, NO2, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(?NRe4)NRc4Rd4, NRc4C(?NRe4)NRc4Rd4, S(O)Rb4, S(O)2Rb4, NRc4S(O)2Rb4 and S(O)2NRc4Rd4;
or Y3 is NH, and Y2 and Y3 or Y3 and Y4, in combination with the carbon atoms to which they are attached, form a 5-membered fused heteroaromatic ring that is unsubstituted or substituted by 1 or 2 substituents independently selected from Y6;
each Y6 is independently selected from the group consisting of halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, 4-10 membered heterocycloalkyl-C1-4 alkylene, CN, NO2, ORa3, SRa3, C(O)Rb3, C(O)NRc3Rd3, C(O)ORa3, OC(O)Rb3, OC(O)NRc3Rd3, NRc3Rd3, NRc3C(O)Rb3, NRc3C(O)NRc3Rd3, NRc3C(O)ORa3, (?NRe3)NRc3Rd3, NRc3C(?NRe3)NRc3Rd3, S(O)Rb3, S(O)2Rb3, NRc3S(O)2Rb3, and S(O)2NRc1Rd1;
wherein each of said C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl forming Y6 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of halogen, CN, NO2, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(?NRe4)NRc4Rd4, NRc4C(?NRe4)NRc4Rd4, S(O)Rb4, S(O)2Rb4, NRc4S(O)2Rb4, and S(O)2NRc4Rd4; and
wherein each of said C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene and 4-10 membered heterocycloalkyl-C1-4 alkylene forming Y6 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of C1-6 alkyl, halogen, C1-6 haloalkyl, CN, NO2, ORa4, SRa4, C(O)Rb4, C(O)NRc4Rd4, C(O)ORa4, OC(O)Rb4, OC(O)NRc4Rd4, NRc4Rd4, NRc4C(O)Rb4, NRc4C(O)NRc4Rd4, NRc4C(O)ORa4, C(?NRe4)NRc4Rd4, NRc4C(?NRe4)NRc4Rd4, S(O)Rb4, S(O)2Rb4, NRc4S(O)2Rb4, and S(O)2NRc4Rd4;
each ArS is:

A1 is N or CZ1;
A2 is N or CZ2;
A3 is N or CZ3;
A4 is N or CZ4;
A5 is N or CZ5;
provided that 0, 1 or 2 of Z1, Z2, Z3, Z4, and Z5 are nitrogen;
Z1, Z2, Z3, Z4, and Z5 are each independently selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, 4-10 membered heterocycloalkyl-C1-4 alkylene, CN, NO2, ORa5, SRa5, C(O)Rb5, C(O)NRc5Rd5, C(O)ORa5, OC(O)Rb5, OC(O)NRc5Rd5, NRc5Rd5, NRc5C(O)Rb5, NRc5C(O)NRc5Rd5, NRc5C(O)ORa5, C(?NRe5)NRc5Rd5, NRc5C(?NRe5)NRc5Rd5, S(O)Rb5, S(O)2Rb5, NRc5S(O)2Rb5, and S(O)2NRc5Rd5;
wherein each of said C1-6 alkyl, C2-6 alkenyl, and C2-6 alkynyl forming Z1, Z2, Z3, Z4, or Z5 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of halogen, CN, NO2, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(?NRe6)NRc6Rd6, NRc6C(?NRe6)NRc6Rd6, S(O)Rb6, S(O)2Rb6, NRc6S(O)2Rb6, and S(O)2NRc6Rd6; and
wherein each of said C3-7 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, 4-10 membered heterocycloalkyl, C3-7 cycloalkyl-C1-4 alkylene, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene and 4-10 membered heterocycloalkyl-C1-4 alkylene forming Z1, Z2, Z3, Z4, or Z5 is independently unsubstituted or substituted with 1, 2, 3, 4 or 5 substituents independently selected from the group consisting of C1-6 alkyl, halogen, C1-6 haloalkyl, CN, NO2, ORa6, SRa6, C(O)Rb6, C(O)NRc6Rd6, C(O)ORa6, OC(O)Rb6, OC(O)NRc6Rd6, NRc6Rd6, NRc6C(O)Rb6, NRc6C(O)NRc6Rd6, NRc6C(O)ORa6, C(?NRe6)NRc6Rd6, NRc6C(?NRe6)NRc6Rd6, S(O)Rb6, S(O)2Rb6, NRc6S(O)2Rb6, and S(O)2NRc6Rd6;
or wherein any one or two of Z1, Z2, Z3, Z4, and Z5 is independently selected from water solubilizing groups;
provided that at least one of R5, R6, R7, R8, Z1, and Z2 is a water solubilizing group;
LS is a bond, O, NRc6, C1-4 alkylene, C(O), NRc6C(O), or C(O)NRc6;
Ra1, Rb1, Ra2, Rb2, Ra3, Rb3, Ra4, Rb4, Ra5, Rb5, Ra6 and Rb6 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C6-10 aryl, 5-10 membered heteroaryl, C3-7 cycloalkyl, 5-10 membered heterocycloalkyl, C6-10 aryl-C1-4 alkylene, C3-7 cycloalkyl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, 5-10 membered heterocycloalkyl-C1-4 alkylene, and C1-4 alkoxy-C1-4 alkylene,
wherein each of said C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, and C1-4 alkoxy-C1-4 alkylene forming Ra1, Rb1, Ra2, Rb2, Ra3, Rb3, Ra4, Rb4, Ra5, Rb5, Ra6 or Rb6 is independently unsubstituted or substituted by 1, 2, 3, 4 or 5 groups independently selected from the group consisting of halogen, CN, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(?NRe7)NRc7Rd7, NRc7C(?NRe7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, and S(O)2NRc7Rd7 and
wherein said C6-10 aryl, 5-10 membered heteroaryl, C3-7 cycloalkyl, 5-10 membered heterocycloalkyl, C6-10 aryl-C1-4 alkylene, C3-7 cycloalkyl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, and 5-10 membered heterocycloalkyl-C1-4 alkylene, forming Ra1, Rb1, Ra2, Rb2, Ra3, Rb3, Ra4 or Rb4 is independently unsubstituted or substituted by 1, 2, 3, 4 or 5 groups independently selected from the group consisting of C1-6 alkyl, halogen, CN, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(?NRe7)NRc7Rd7, NRc7C(?NRe7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, and S(O)2NRc7Rd7;
Rc1, Rd1, Rc2, Rd2, Rc3, Rd3, Rc4, Rd4, Rc5, Rd5, Rc6, and Rd6 are each independently selected from the group consisting of hydrogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, C6-10 aryl, 5-10 membered heteroaryl, C3-7 cycloalkyl, 5-10 membered heterocycloalkyl, C6-10 aryl-C1-4 alkylene, C3-7 cycloalkyl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, 5-10 membered heterocycloalkyl-C1-4 alkylene, and C1-4 alkoxy-C1-4 alkylene,
wherein each of said C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, and C1-4 alkoxy-C1-4 alkylene forming Rc1, Rd1, Rc2, Rd2, Rc3, Rd3, Rc4, Rd4, Rc5, Rd5, Rc6, or Rd6 is independently unsubstituted or substituted by 1, 2, 3, 4 or 5 groups independently selected from the group consisting of halo, CN, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(?NRe7)NRc7Rd7, NRc7C(?NRc7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, and S(O)2NRc7Rd7 and
wherein each of said C6-10 aryl, 5-10 membered heteroaryl, C3-7 cycloalkyl, 5-10 membered heterocycloalkyl, C6-10 alkylene, C3-7 cycloalkyl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, and 5-10 membered heterocycloalkyl-C1-4 alkylene, forming Rc1, Rd1, Rc2, Rd2, Rc3, Rd3, Rc4, Rd4, Rc5, Rd5, Rc6, or Rd6 is independently unsubstituted or substituted by 1, 2, 3, 4 or 5 groups independently selected from the group consisting of C1-6 alkyl, halo, CN, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(?NRe7)NRc7Rd7, NRc7C(?NRe7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, and S(O)2NRc7Rd7;
or Rc1 and Rd1, Rc2 and Rd2, Rc3 and Rd3, Rc4 and Rd4, Rc5 and Rd5, or Rc6 and Rd6, attached to the same N atom, together with the N atom to which they are both attached, form a 4-, 5-, 6- or 7-membered heterocycloalkyl group or 5-membered heteroaryl group, each optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of C1-6 alkyl, halo, CN, ORa7, SRa7, C(O)Rb7, C(O)NRc7Rd7, C(O)ORa7, OC(O)Rb7, OC(O)NRc7Rd7, NRc7Rd7, NRc7C(O)Rb7, NRc7C(O)NRc7Rd7, NRc7C(O)ORa7, C(?NRe7)NRc7Rd7, NRc7C(?NRe7)NRc7Rd7, S(O)Rb7, S(O)NRc7Rd7, S(O)2Rb7, NRc7S(O)2Rb7, and S(O)2NRc7Rd7;
Ra7, Rb7, Rc7 and Rd7 are each independently selected from the group consisting of H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, 5-10 membered heteroaryl, C3-7 cycloalkyl, 4-10 membered heterocycloalkyl, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, C3-7 cycloalkyl-C1-4 alkylene, and 4-10 membered heterocycloalkyl-C1-3 alkylene,
wherein said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, C6-10 aryl, 5-10 membered heteroaryl, C3-7 cycloalkyl, 4-10 membered heterocycloalkyl, C6-10 aryl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, C3-7 cycloalkyl-C1-4 alkylene, and 4-10 membered heterocycloalkyl-C1-3 alkylene forming Ra7, Rb7, Rc7 and Rd7 are each optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of OH, CN, amino, NH(C1-6 alkyl), N(C1-6 alkyl)2, halo, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl, and C1-6 haloalkoxy;
or Rc7 and Rd7 attached to the same N atom, together with the N atom to which they are both attached, form a 4-, 5-, 6- or 7-membered heterocycloalkyl group or 5-membered heteroaryl group, each optionally substituted with 1, 2 or 3 substituents independently selected from the group consisting of OH, CN, amino, NH(C1-6 alkyl), N(C1-6 alkyl)2, halo, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl and C1-6 haloalkoxy; and
Re1, Re2, Re3, Re4, Re5, Re6 and Re7 are each independently selected from the group consisting of H, C1-4 alkyl, OH, and C1-4 alkoxy;
each water solubilizing group is independently selected from the group consisting of -LW-ORaW, -LW-C(O)RbW, -LW-C(O)NRcWRdW, -LW-C(O)ORaW, -LW-OC(O)RbW, -LW-OC(O)NRcWRdW, -LW-NRcWRdW, -LW-NRcWC(O)RbW, -LW-NRcWC(O)NRcWRdW, -LW-NRcWC(O)ORaW, -LW-C(?NReW)NRcWRdW, -LW-NRcWC(?NReW)NRcWRdW, -LW-S(O)2ORaW, -LW-NRcWS(O)2RbW, S(O)2NRcWRdW, —P(?O)(ORaW)2, -OP(?O)(ORaW)2, —OP(?O)(ORaW)—OP(?O)(ORaW)2, —OP(?O)(ORaW)—OP(?O)(ORaW)—OP(?O)(ORaW)2, and -LW-CyW; Wherein:
each CyW is unsubstituted 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl, or 5-10 membered heteroaryl or 4-10 membered heterocycloalkyl substituted with one or more (e.g., 1, 2, 3, 4 or 5) substituents each independently selected from C1-6 alkyl, halogen, C1-6 haloalkyl, CN, NO2, ORaW, SRaW, C(O)RbW, C(O)NRcWRdW, C(O)ORaW, OC(O)RbW, OC(O)NRcWRdW, NRcWRdW, NRcWC(O)RbW, NRcWC(O)NRcWRdW, NRcWC(O)ORaW, C(?NReW)NRcWRdW, NRcWC(?NReW)NRcWRdW, S(O)RbW, S(O)2RbW, NRcWS(O)2RbW and S(O)2NleWRdW;
each -LW- is a bond or a linking group selected from groups of the formula -LW1-LW2-;
the group -Lwi- is attached to the core molecule and is selected from a bond and groups of the formula —O—, —S—, —S(O)—, —S(O)2—, —C(O)—, —NH—, —NRcW, —NRcWC(O)—, —C(O)NRcW—, —O(CO)—, —C(O)O—, —O(CO)NRcW—, —NRcWC(O)O—, —O(CO)O—, and —NRcWC(O)NRcW—;
the group -LW2- is selected from a bond, unsubstituted-C1-10 alkylene-, unsubstituted-C1-10 heteroalkylene, and —C1-10 alkylene and —C1-10 heteroalkylene substituted with one or more (e.g., 1, 2, 3, 4 or 5 substituents) independently selected from the group consisting of H, halogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, CN, NO2, ORaW, SRaW, C(O)RbW, C(O)NRcWRdW, C(O)ORaW, OC(O)RbW, OC(O)NRcWRdW, NRcWRdW, NRcWC(O)RbW, NRcWC(O)NRcWRdW, NRcWC(O)ORaW, C(?NReW)NRcWRdW, NRcWC(?NReW)NRcWRdW, S(O)RbW, S(O)2RbW, NRcWS(O)2RbW, S(O)2NRcWRdW, —P(?O)(ORaW)2, —OP(?O)(ORaW)2, —OP(?O)(ORaW)—OP(?O)(ORaW)2, —OP(?O)(ORaW)—OP(?O)(ORaW)—OP(?O)(ORaW)2, oxo and sulfido;
RaW, RbW, RcW, and RdW are each independently selected from the group consisting of hydrogen, C1-4 alkyl, C2-4 alkenyl, C2-4 alkenyl, C6-10 aryl, 5-10 membered heteroaryl, C3-7 cycloalkyl, 5-10 membered heterocycloalkyl, C6-10 aryl-C14 alkylene, C3-7 cycloalkyl-C1-4 alkylene, 5-10 membered heteroaryl-C14 alkylene, 5-10 membered heterocycloalkyl-C1-4 alkylene, and C1-4 alkoxy-C1-4 alkylene, wherein said C1-4 alkyl, C2-4 alkenyl, C2-4 alkynyl, and C1-4 alkoxy-C1-4 alkylene forming RaW, RbW, RaW, or RdW are each optionally substituted by 1, 2, 3, 4 or 5 groups independently selected from halo, CN, ORaW*, SRaW*, C(O)RbW*, C(O)NRcW*RdW*, C(O)ORaW*, OC(O)RbW*, OC(O)NRcW*RdW*, NRcW*RdW*, NRcW*C(O)RbW*, NRcW*C(O)NRcW*RdW*, NRcW*C(O)ORaW*, C(?NReW*)NRcW*RdW*, NRcW*C(?NReW*)NRcW*RdW*, S(O)RbW*, S(O)NRcW*RdW*, S(O)2RbW*, NRcW*S(O)2RbW* and S(O)2NRcW*RdW* and Wherein said C6-10 aryl, 5-10 membered heteroaryl, C3-7 cycloalkyl, 5-10 membered heterocycloalkyl, C6-10 aryl-C14 alkylene, C3-7 cycloalkyl-C1-4 alkylene, 5-10 membered heteroaryl-C1-4 alkylene, and 5-10 membered heterocycloalkyl-C1-4 alkylene, forming RaW, RbW, RaW, or RdW are each optionally substituted by 1, 2, 3, 4 or 5 groups independently selected from C1-6 alkyl, halo, CN, ORaW*, SRaW*, C(O)RbW*, C(O)NRcW*RdW*, C(O)ORaW*, OC(O)RbW*, OC(O)NRcW*RdW*, NRcW*RdW*, NRcW*C(O)RbW*, NRcW*C(O)NRcW*RdW*, NRcW*C(O)ORaW*, C(?NReW*)NRcW*RdW*, NRcW*C(?NReW*)NRcW*RdW*, S(O)RbW*, S(O)NRcW*RdW*, S(O)2RbW*, NRcW*S(O)2RbW* and S(O)2NRcW*RdW*;
or RcW and RdW, attached to the same N atom, together with the N atom to which they are both attached, form a 4-, 5-, 6- or 7-membered heterocycloalkyl group or 5-membered heteroaryl group, each optionally substituted with 1, 2 or 3 substituents independently selected from C1-6 alkyl, halo, CN, ORaW*, SRaW*, C(O)RbW*, C(O)NRcW*RdW*, C(O) ORa*, OC(O)Rb*, OC(O)NRcW*RdW*, NRcW*RdW*, NRcW*C(O)RbW*, NRcW*C(O)NRcW*RdW*, NRcW*C(O)ORaW*, C(?NReW*)NRcW*RdW*, NRcW*C(?NReW*)NRcW*RdW*, S(O)RbW*, S(O)NRcW*RdW*, S(O)2RbW*, NRcW*S(O)2RbW* and S(O)2NRcW*RdW*;
RaW*, RbW*, RcW* and RdW* are each independently selected from H, C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl, aryl, C6-10 aryl-C1-3 alkyl, 5-10 membered heteroaryl-C1-3 alkyl, C3-7 cycloalkyl-C1-3 alkyl and 4-10 membered heterocycloalkyl-C1-3 alkyl, wherein said C1-6 alkyl, C1-6 haloalkyl, C2-6 alkenyl, C2-6 alkynyl C6-10 aryl-C1-3 alkyl, 5-10 membered heteroaryl-C1-3 alkyl, C3-7 cycloalkyl-C1-3 alkyl and 4-10 membered heterocycloalkyl-C1-3 alkyl forming RaW* RbW*, ReW* and RdW* are each optionally substituted with 1, 2 or 3 substituents independently selected from OH, CN, amino, NH(C1-6 alkyl), N(C1-6 alkyl)2, halo, C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl and C1-6 haloalkoxy,
or RcW* and RdW* attached to the same N atom, together with the N atom to which they are both attached, form a 4-, 5-, 6- or 7-membered heterocycloalkyl group or 5-membered heteroaryl group, each optionally substituted with 1, 2 or 3 substituents independently selected from OH, CN, amino, NH(C1-6 alkyl), N(C1-6 alkyl)2 halo C1-6 alkyl, C1-6 alkoxy, C1-6 haloalkyl and C1-6 haloalkoxy;
ReW and ReW* are each independently selected from H, C1-4 alkyl, OH, and C1-4 alkoxy;with the proviso that when Y1, Y2, Y4, Y5, and R4 are each H, Y3 is F, and X3 is H or C1-6 alkyl, then at least one of R5, R6, and R7 is not H.

US Pat. No. 10,336,720

CYCLIC CARBONATE MONOMER CONTAINING DOUBLE IODINE, BIODEGRADABLE POLYMER PREPARED THEREBY AND USE

SOOCHOW UNIVERSITY, Suzh...

1. A biodegradable polymer containing a functional group of double iodine in the side chain, which includes cyclic carbonate monomer containing double iodine, wherein the biodegradable polymer containing a functional group of double iodine is polymerized of cyclic carbonate monomer containing double iodine by one of the following steps:(1) homopolymerize by cyclic carbonate monomer containing double iodine; or
(2) cyclic carbonate monomer containing double iodine has copolymerization with cyclic carbonate containing double sulfur or trimethylene cyclic carbonate;
said cyclic carbonate monomer containing double iodine is

the molecular weight of said biodegradable polymer containing a functional group of double iodine in the side chain is 3-500 kDa;
said biodegradable polymer containing a functional group of double iodine in the side chain has a polydispersity index (PDI) of 1.30 to 1.53; and
said biodegradable polymer containing a functional group of double iodine in the side chain forms nano-vesicles after dialysis.

US Pat. No. 10,336,719

1-(CYCLOPENT-2-EN-1-YL)-3-(2-HYDROXY-3-(ARYLSULFONYL)PHENYL)UREA DERIVATIVES AS CXCR2 INHIBITORS

GlaxoSmithKline Intellect...

1. A method of treating a disease or condition selected from the group consisting of: cancer, autoimmune or inflammatory diseases, neurodegenerative diseases, chronic obstructive pulmonary disease (COPD), chemotherapy induced peripheral neuropathy (CIPN), traumatic brain injury and spinal chord injury in a human in need thereof, the method comprising administering to the human a compound of formula (I) or a pharmaceutically acceptable salt thereof,whereinR1 is H, C1-3alkyl, C1-3haloalkyl or halo;
R2 is H, C1-3alkyl, C1-3haloalkyl or halo;
R3 is fluoro, chloro or cyano; and
R4 is selected from the group consisting of:
a) C1-6alkyl optionally substituted by one or more substituents independently selected from the group consisting of: fluoro, C1-3alkoxy, C1-3fluoroalkyl, C1-3fluoroalkoxy and hydroxy;
b) —(CH2)n—(R4a)(R4b); wherein
n is 0, 1 or 2;
the —(CH2)n— linker is optionally substituted by one or more groups independently selected from fluoro and methyl optionally substituted by one or more deuterium; and
wherein R4aand R4b are independently C1-3alkyl, or R4a and R4b may, together with the nitrogen to which they are attached, form a 4, 5 or 6-membered ring, which ring
i) optionally contains one additional ring-heteroatom selected from nitrogen and oxygen;
ii) may be saturated, or when the ring is a 5 or 6-membered, be unsaturated or aromatic;
iii) is optionally substituted by one or more substituents independently selected from C1-3alkyl optionally substituted by one or more substituents independently selected from the group consisting of deuterium, fluoro, C1-3fluoroalkyl, hydroxy, C1-3alkoxy, C1-3alkoxyC1-3alkyl and C1-3fluoroalkoxy; or
iv) is ortho-fused to a further 5 or 6-membered ring which further ring is saturated, unsaturated or aromatic; which further ring optionally contains one additional ring-heteroatom selected from nitrogen and oxygen; and which further ring is optionally independently substituted by one or more fluoro or methyl substituents;
c) —(CH2)p-heteroaryl; wherein
p is 1 or 2;
the —(CH2)p— linker is optionally substituted by one or more groups independently selected from fluoro and methyl optionally substituted by one or more deuterium;
the heteroaryl is 5 or 6-membered and is attached to the —(CH2)p— via a ring carbon atom; and
wherein the heteroaryl is optionally substituted by one or more substituents independently selected from the group consisting of C1-3alkyl, fluoro, C1-3fluoroalkyl; C1-3alkoxy, C1-3alkoxyC1-3alkyl and C1-3fluoroalkoxy; or wherein two substituents on adjacent ring-atoms, together with the interconnecting atoms form a further 5 or 6-membered ring ortho-fused to the heteroaryl group; which further ring is saturated, unsaturated or aromatic; and which further ring optionally contains one additional heteroatom selected from nitrogen and oxygen; and which further ring is optionally independently substituted by one or more fluoro or methyl substituents;
d) —(CH2)q-heterocyclyl; wherein
q is 0, 1 or 2;
the —(CH2)q— linker is optionally substituted by one or more groups independently selected from fluoro and methyl optionally substituted by one or more deuterium;
the heterocyclyl group is 3, 4, 5 or 6-membered and is attached to the —(CH2)q— via a ring carbon atom;
the heterocyclyl is saturated or unsaturated; and
wherein the heterocyclyl group is optionally substituted by one or more substituents independently selected from the group consisting of deuterium, C1-3alkyl optionally substituted by one or more deuterium, fluoro, C1-3fluoroalkyl, hydroxy, C1-3alkoxy, C1-3alkoxyC1-3alkyl, C1-3fluoroalkoxy, C3-6cycloalkyl and —(CH2)sNR4cR4d; or two substituents on the heterocyclyl group together with the interconnecting atom(s), form a further 5 or 6-membered ring which further ring is saturated, unsaturated or aromatic when the further ring is ortho-fused; and which further ring optionally contains one additional heteroatom selected from nitrogen and oxygen; and which further ring is optionally independently substituted by one or more fluoro or methyl substituents; wherein s is 0 or 1, and wherein R4c and R4dare independently C1-3alkyl, or R4c and R4d, together with the nitrogen to which they are attached, form a 4, 5 or 6-membered saturated ring which ring is optionally substituted by one or more fluoro substituent; and
e) —(CH2)r —C3-6cycloalkyl; wherein
r is 0, 1 or 2;
the —(CH2)r — linker is optionally substituted by one or more groups independently selected from fluoro and methyl optionally substituted by one or more deuterium; and
wherein the C3-6cycloalkyl group is optionally substituted by one or more substituents independently selected from the group consisting of C1-3alkyl optionally substituted by one or more deuterium, fluoro, C1-3fluoroalkyl, hydroxy, C1-3alkoxy, C1-3alkoxyC1-3alkyl, C1-3fluoroalkoxy and —(CH2)tNR4eR4f; or wherein two substituents on the cycloalkyl group together with the interconnecting atom(s) form a further 5 or 6-membered ring which further ring is saturated, unsaturated or aromatic when the further ring is ortho-fused; and which further ring optionally contains one heteroatom selected from nitrogen and oxygen; and which further ring is optionally independently substituted by one or more fluoro or methyl substituents; wherein t is 0 or 1, and wherein R4e and R4f are independently C1-3alkyl, or R4e and R4f, together with the nitrogen to which they are attached, form a 4, 5 or 6-membered saturated ring which ring is optionally substituted by one or more fluoro substituent.

US Pat. No. 10,336,718

METHOD FOR INDUSTRIAL PRODUCTION OF OPTICALLY ACTIVE FLUOROALKYL ETHYLENE OXIDE

Central Glass Company, Li...

1. A method for producing an optically active fluoroalkyl chloromethyl alcohol represented by formula [2]:
wherein, * represents an asymmetric atom, and Rf is defined as in formula [1],
the method comprising the step of treating a fluoroalkyl chloromethyl ketone represented by formula [1]:

wherein, Rf represents a C1-6 straight-chain or branched-chain fluoroalkyl group having at least one fluorine atom,
with a microorganism having an activity for asymmetrically reducing the ketone or an enzyme having the activity.

US Pat. No. 10,336,717

INHIBITORS OF BETA-SECRETASE

Vitae Pharmaceuticals, LL...

1. A compound represented by the following Structural Formula:
or a pharmaceutically acceptable salt thereof, wherein:
ring Het is a 5 membered monocyclic heterocycle;
X is —C(R3R4)—;
each R0 is independent selected from —H, ?O, ?S, ?NR15, (C1-C6)alkyl, halo(C1-C6)alkyl, —CN, —NO2,
halogen, —OR5, —NR6R7, —S(O)iR5, —S(O)iNR12R13, —NR11S(O)iR5, —C(?O)OR5, —OC(?O)O R5, —C(?S)OR5, —O(C?S)R5, —C(?O)NR12R13, —NR11C(?O)R5, —C(?S)NR12R13, —NR11C(?S)R5, —NR1(C?O)OR5, —O(C?O)NR12R13, —NR11(C?S)OR5, —O(C?S)NR12R13, —NR11(C?O)NR12R13, —NR11(C?S)NR12R13, —C(?S)R5, —C(?O)R5, (C3-C8)cycloalkyl, (C3-C8)cycloalkyl(C1-C3)alkyl, (C3-C9)heterocycloalkyl, (C3-C9)heterocycloalkyl(C1-C3)alkyl, aryl, aryl(C1-C6)alkyl, heteroaryl or heteroaryl(C1-C6)alkyl, each of the (C1-C6)alkyl, halo(C1-C6)alkyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkyl(C1-C3)alkyl, (C3-C9)heterocycloalkyl, (C3-C9)heterocycloalkyl(C1-C3)alkyl, aryl, aryl(C1-C6)alkyl, heteroaryl or heteroaryl(C1-C6)alkyl group represented by R0 is optionally substituted with 1 to 5 substituents independently selected from the group consisting of -halogen, —CN, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C3)alkoxy, halo(C1-C3)alkoxy, (C1-C3)alkoxy(C1-C3)alkyl, (C3-C8)cycloalkyl, (C3-C9)heterocycloalkyl, aryl,
heteroaryl, —NR6R7, —NR11S(O)iR5, —C(?O)NR12R13, —NR11C(?O)R5, —S(O)iR5, —S(O)iNR12R13, —OR5, —C(?O)R5, —C(?S)NR12R13, —NR11C(?S)R5, —C(O)OR5, —OC(?O)OR5, —C(?S) OR5, —O(C?S)R5, —O(C?O)NR12R13, —NR11(C?O)OR5, —NR11(C?S)OR5, —O(C?S)NR12R13 , —NR11(C?O)NR12R13, —NR11(C?S)NR12R13 and —C(?S)R5, wherein the cycloalkyl, heterocycloalkyl, aryl and heteroaryl groups in the substituents on the groups represented by R0 are each optionally substituted with 1 to 3 substituents independently selected from halogen, —CN, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C3)alkoxy, halo(C1-C3)alkoxy and (C1-C3)alkoxy(C1-C6)alkyl;
R1 is —H or —C(?O)(C1-C3)alkyl;
R2 is —H, halogen, —CN, —OR5, —C(?O)NR12R13, —C(?O)OR5, —C(O)R5, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C3-C6)cycloalkyl, (C3-C6)cycloalkyl(C1-C3)alkyl, (C4-C6)cycloalkenyl, phenyl, phenyl(C1-C3)alkyl, heteroaryl, heteroaryl(C1-C3)alkyl, (C5-C6)heterocycloalkyl, (C5-C6)heterocycloalky(C1-C3)alkyl, wherein the heteroaryl is selected from pyridyl, pyridazinyl, pyridinonyl, pyridazinonyl, thiazolyl, oxazolyl, oxadiazolyl, pyrazinyl, pyrimidyl, indolyl, quinolyl, quinoxalinyl, triazole and thiophenyl, the heterocycloalkyl is selected from oxetanyl, tretrahydrafuran, tetrapyran, piperidine, pyrrolidinyl and pyrrolidinonyl, and each of (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C3-C6)cycloalkyl, (C3-C6)cycloalkyl(C1-C3)alkyl, (C4-C6)cycloalkenyl, phenyl, phenyl(C1-C3)alkyl, heteroaryl, heteroaryl(C1-C3)alkyl, (C5-C6)heterocycloalkyl and (C5-C6)heterocycloalky(C1-C3)alkyl groups represented by R2 is optionally substituted with 1 to 5 substituents independently selected from halogen, —CN, (C1-C3)alkyl, halo(C1-C3)alkyl, (C2-C6)alkynyl, —NR6R7, —S(O)iR5, —C(O)R5, —OH, (C3-C6)cycloalkyl, (C1-C3)alkoxy and halo(C1-C3)alkoxy;
R3 and R4 are each
independently —H, -halogen, —CN, —NO2, —OR5, —NR6R7, —S(O)iR5, —NR11S(O)iR5, —S(O)iN R12R13, —C(?O)OR5, —OC(?O)OR5, —C(?S)OR5, —O(C?S)R5, —C(?O)NR12R13, —NR11C(?O)R5, —C(?S)NR12R13, —NR11C(?S)R5, —NR11(C?O)OR5, —O(C?O)NR12R13, —NR11(C?S)O R5, —O(C?S)NR12R13, —NR11(C?O)NR12R13, —NR11(C?S)NR12R13, —C(?S)R5, —C(?O)R5, (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkyl(C1-C6)alkyl, (C3-C8)cycloalkyl(C2-C6)alkynyl, (C3-C9)heterocycloalkyl, (C3-C9)heterocycloalkyl(C1-C6)alkyl, (C3-C9)heterocycloalkyl(C2-C6)alkynyl, aryl, aryl(C1-C6)alkyl, aryl(C2-C6)alkynyl, heteroaryl, heteroaryl(C1-C6)alkyl or heteroaryl(C1-C6)alkynyl, wherein each (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, (C3-C8)cycloalkyl, (C3-C8)cycloalkyl(C1-C6)alkyl, (C3-C8)cycloalkyl(C2-C6)alkynyl, (C3-C9)heterocycloalkyl, (C3-C9)heterocycloalkyl(C1-C6)alkyl, (C3-C9)heterocycloalkyl(C2-C6)alkynyl, aryl, aryl(C1-C6)alkyl, aryl(C2-C6)alkynyl, heteroaryl, heteroaryl(C1-C6)alkyl or heteroaryl(C1-C6)alkynyl represented by R3 and R4 is optionally substituted with 1 to 5 substituents independently selected from the group consisting of
halogen, —OR5, —NR6R7, —S(O)iR5, —NR11S(O)iR5, —S(O)iNR12R13, —C(?O)OR5, —OC(?O)O R5, —C(?S)OR5, —O(C?S)R5, —C(?O)NR12R13, —NR11C(?O)R5, —C(?S)NR12R13, —NR11C(?S)R5, —NR11(C?O)OR5, —O(C?O)NR12R13, —NR11(C?S)OR5, —O(C?S)NR12R13, —NR11(C?O)NR12R13, —NR11(C?S)NR12R13, —C(?S)R5, —C(?O)R5, (C1-C6)alkyl, (C2-C6)alkenyl, halo(C1-C6)alkyl, (C1-C3)alkylsulfonylaminoalkyl, hydroxy(C1-C6)alkyl, cyano(C1-C6)alkyl, (C1-C3)alkylcarbonylamino(C1-C6)alkyl, (C1-C3)alkoxy, halo(C1-C3)alkoxy, (C1-C6)alkoxy(C1-C3)alkyl, (C3-C5)cycloalkyl, (C3-C9)heterocycloalkyl, aryl and heteroaryl, wherein the cycloalkyl, heterocycloalkyl, aryl and heteroaryl groups in the substituents on the groups represented by R3 and R4 are each optionally substituted with 1 to 3 substituents independently selected from halogen, —CN, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C3)alkoxy, halo(C1-C3)alkoxy and (C1-C3)alkoxy(C1-C6)alkyl;
R5 is selected from the group consisting of —H, (C1-C3)alkyl, halo(C1-C3)alkyl, (C1-C3)alkoxy(C1-C3)alkyl, (C3-C6)cycloalkyl, (C3-C6)cycloalkyl(C1-C3)alkyl, phenyl and phenyl(C1-C3)alkyl, wherein the phenyl group in the groups represented by R5 is optionally substituted with 1 to 3 substituents independently selected from ——F, —Cl, —Br, —CN, ?O, —NR6R7, (C1-C3)alkyl, halo(C1-C3)alkyl and (C1-C3)alkoxy(C1-C3)alkyl;
R6 is —H or (C1-C3)alkyl;
R7 is —H, (C1-C3)alkyl, halo(C1-C3)alkyl, (C3-C6)cycloalkyl, (C3-C6)cycloalkyl(C1-C3)alkyl or (C1-C3)alkoxy(C1-C3)alkyl;
R8 and R9 together with the carbon to which they are attached, form

R11 is —H or (C1-C3)alkyl;
R12 is —H or (C1-C3)alkyl; and
R13 is —H, (C1-C3)alkyl, halo(C1-C3)alkyl, (C3-C6)cycloalkyl(C1-C3)alkyl or (C1-C3)alkoxy(C1-C3)alkyl, or R12 and R13 together with the nitrogen atom to which they are attached forms a pyrrolidine or piperidine ring;
R14 is —H, —OR5, —NR6R7, (C1-C6)alkyl, (C3-C6)cycloalkyl, (C3-C6)cycloalkyl(C1-C3)alkyl, (C3-C5)heterocycloalkyl, (C3-C5)heterocycloalkyl(C1-C3)alkyl, heteroaryl, phenyl, phenyl(C1-C3)alkyl and heteroaryl(C1-C3)alkyl, wherein the heteroaryl is selected from pyridyl, pyridazinyl, pyridinonyl, pyridazinonyl, thiazolyl, oxazolyl, oxadiazolyl, pyrazinyl, pyrimidyl, indolyl, quinolyl, quinoxalinyl and thiophenyl and triazolyl, the (C3-C5)heterocycloalkyl is selected from oxetanyl, tetrahydrofuran, tetrahydropyran, piperidinyl and pyrrolidinyl, and each of the (C1-C6)alkyl, (C3-C6)cycloalkyl, (C3-C6)cycloalkyl(C1-C3)alkyl, (C3-C5)heterocycloalkyl, (C3-C5)heterocycloalkyl(C1-C3)alkyl, heteroaryl, phenyl, phenyl(C1-C3)alkyl and heteroaryl(C1-C3)alkyl groups represented by R14 is optionally substituted with 1 to 3 substituents independently selected from halogen, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C3)alkoxy, —NR6R7, —S(O)iR5, —NR11SO2R5, —OH, —COOR5, —C(?O)R5, —C(?O)NR12R13 and thiazolyl;
R15 is —H or (C1-C6)alkyl optionally substituted with 1 to 5 —F;
R19 and R20 are each independently selected from —H,
halogen, —CN, —OR5, —NR6R7, —S(O)iR5, —NR11S(?O)iR5, —C(?O)OR5, —C(?O)NR12R13, —NR11C(?O)R5, —C(?S)NR12R13, —C(?O)R5, (C1-C6)alkyl, (C2-C6)alkenyl, aryl, aryl(C1-C6)alkyl, heteroaryl and heteroaryl(C1-C6)alkyl, wherein each of the (C1-C6)alkyl, (C2-C6)alkenyl, aryl, aryl(C1-C6)alkyl, heteroaryl and heteroaryl(C1-C6)alkyl groups represented by R19 and R20 is optionally substituted with 1 to 5 substituents independently selected from the group consisting of halogen, —CN, —OH, —NR11SO2(C1-C3)alkyl, —NR11C(?O)—(C1-C3)alkyl, (C1-C6)alkyl, halo(C1-C6)alkyl, (C1-C3)alkoxy, halo(C1-C3)alkoxy and (C1-C3)alkoxy(C1-C6)alkyl;
i is 0, 1 or 2;
p is 1, 2 3 or 4; and
q is 1, 2 or 3.

US Pat. No. 10,336,713

TRIAZOLE-BASED READER MOLECULES AND METHODS FOR SYNTHESIZING AND USE THEREOF

Arizona Board of Regents,...

1. A universal reader molecule for functionalization onto electrodes of a recognition tunneling molecule identification system comprising a triazole carboxamide compound of 5-(2-mercaptoethyl)-4H-1,2,4-triazole-3-carboxamide and its tautomers.

US Pat. No. 10,336,712

COMPOUND FOR ENHANCING THE COUPLING DEGREE OF COMPLEX TRPV4-KCA2.3 AND ANTI-HYPERTENSION APPLICATIONS THEREOF

JIANGNAN UNIVERSITY, Wux...

1. A preparation method of a compound for enhancing the space coupling degree of an endothelial cell ion channel complex TRPV4-KCa2.3, wherein structural domains of interacting sites of the endothelial cell ion channel complex TRPV4-KCa2.3 are structural domain AR2 of protein TRPV4 and structural domain 17C of protein KCa2.3 and the compound is represented by structure formula (1):
the method comprising:
providing propane diamine with t-butyloxycarboryl to protect a single amino first:

an exposed amino reacting with diphenylacetyl chloride to generate an amide:

removing a t-butyloxycarboryl protection from the amide under an acidic condition:

a compound obtained after removing the t-butyloxycarboryl protection performing an amino-ester exchange with 4-quinazolone-2-carboxylic acid ethyl ester to obtain a target compound:

US Pat. No. 10,336,710

BENZIMIDAZOLE DERIVATIVES, PREPARATION METHOD THEREFOR, AND APPLICATIONS THEREOF

1. A benzimidazole derivative having the structure of Formula (I):
or a pharmaceutically acceptable salt or prodrug thereof, wherein:
R1 and R2 are selected from the group consisting of alkyl;
R3 is selected from the group consisting of hydrogen, halogen, cyano, linear or branched C1-6 alkyl and linear or branched C1-6 alkoxy;
R4 is selected from the group consisting of phenyl, substituted phenyl, naphthyl and substituted naphthyl, wherein the substituent in said substituted phenyl and substituted naphthyl is selected from the group consisting of halogen, cyano, alkyl, alkoxy, ester, N-acyl derivatives, N-acyloxy derivatives and amino acid conjugates; and
M is selected from the group consisting of hydrogen, alkyl, and pharmaceutically acceptable cations.

US Pat. No. 10,336,709

LP-PLA2 INHIBITORS

ABIDE THERAPEUTICS, INC, ...

1. A compound having the structure of Formula (I), or a pharmaceutically acceptable salt or solvate thereof:wherein:R1 is selected from the group consisting of —N(R10)R11, —OH, C1-C6alkyl, and C1-C6alkoxy;
R2 is selected from the group consisting of hydrogen, halogen, —N(R12)R13, —CF3, C1-C6alkyl, and C1-C6alkoxy;
R3 is hydrogen or C1-C3alkyl;
R4 and R5 are each independently selected from the group consisting of hydrogen, C1-C6alkyl optionally substituted by one, two, or three groups independently selected from halogen, cyano, and hydroxyl, and —(C1-C6alkylene)-(phenyl) optionally substituted by one, two, or three groups independently selected from halogen, cyano, —CF3, —OH, C1-C6alkyl, and C1-C6alkoxy;
each R6 is independently selected from the group consisting of halogen, —N(R12)R13, —CF3, C1-C6alkyl, and C1-C6alkoxy;
R10 and R11 are each independently selected from the group consisting of hydrogen, and C1-C3alkyl; or R10 and R11 together with the nitrogen atom to which they are attached, form a 4-6 membered heterocyclic ring optionally substituted by C1-C6alkyl or —CO2H;
each R12 and R13 are each independently selected from the group consisting of hydrogen, and C1-C3alkyl;
n is 1 or 2; and
p is 0, 1, or 2.

US Pat. No. 10,336,708

IMIDAZOLE COMPOUND, METAL SURFACE TREATMENT LIQUID, METAL SURFACE TREATMENT METHOD, AND LAMINATE PRODUCTION METHOD

TOKYO OHKA KOGYO CO., LTD...

1. An imidazole compound represented by the following formula (1-1-1):wherein R1 represents a hydrogen atom or an alkyl group, R4 represents a halogen atom, a hydroxyl group, a mercapto group, a sulfide group, a silyl group, a silanol group, a nitro group, a nitroso group, a sulfonate group, a phosphino group, a phosphinyl group, a phosphonato group, or an organic group,at least one of R11, R12, R13, R14, and R15 is a group represented by —O—R10 wherein R10 is an alkyl group, and each remaining member of R11, R12, R13, R14, and R15 is a hydrogen atom, and
n represents an integer of 0 to 3.

US Pat. No. 10,336,707

HETEROCYCLIC DERIVATIVES MODULATING ACTIVITY OF CERTAIN PROTEIN KINASES

EUDENDRON S.R.L., Varese...

1. Compounds of general formula (I):
in which:
X is —NH— or —O—;
R1 is hydrogen or —COR6;
R2 and R5 are independently selected from hydrogen, halogen and C1-C6 alkyl;
R3 is —Y—Ar where Y is a divalent group selected from —CH2—, —NH—, —O—, —S—, —S(O)—, and —S(O)2—;
Ar is an aryl, or a 5-10 membered heteroaryl, where said aryl or heteroaryl is optionally substituted by one to three groups independently selected from halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 hydroxyalkyl, C1-C6 haloalkoxy, C1-C6 halothioalkoxy, cyano, hydroxyl, mercapto, amino, C1-C6 alkoxy, C1-C6 thioalkoxy, C1-C6 mono alkylamino, C1-C6 bis alkylamino, carbamoyl, N—(C1-C6 alkyl)carbamoyl, N,N-bis (C1-C6 alkyl)carbamoyl, C1-C6 acylamino, N—(C1-C6 alkyl)-N—(C1-C6 acyl)amino, N—(C1-C6 alkyl)sulfonylamino and N,N-bis (C1-C6 alkyl)sulfonylamino;
R4 is selected from the group consisting of:
aryl optionally substituted by one to three substituents independently selected from hydroxyl, amino, —OC(O)NHRe, —ORe, —NHC(O)NHRe, halogen, cyano, carbamoyl, C1-C6 alkyl, C1-C6 hydroxyalkyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, C1-C3 alkoxy, —OCH2CH2Re, —OCH2C(O)NHRe, —OCH2CH2ORe, —OCH2CH2NHRe, —CH2C(O)NHRe, N—(C1-C6 alkyl)carbamoyl, N—(C3-C6 cycloalkyl)carbamoyl, C1-C6 acylamino, C1-C6 alkylsulfonylamino, aminosulfonyl, N—(C1-C6 alkyl)aminosulfonyl, and C1-C6 alkylsulfonyl being Re an aryl optionally substituted by one or two substituents independently selected from C1-C6 haloalkyl and CH2-A, where A is an heterocyclyl selected among pyrrolidinyl, piperidinyl, piperazinyl and morpholinyl, and said heterocyclyl being optionally substituted by a C1-C3-alkyl group;
5-10 membered heteroaryl optionally substituted on the carbon atoms with one or two groups independently selected from amino, C1-C6 acylamino, oxo, hydroxyl, halogen, C1-C6 alkylsulfonyl, C1-C6 alkylsulfonylamino, aminosulfonyl, N—(C1-C6 alkyl)aminosulfonyl, cyano, C1-C6 alkyl, C1-C6 haloalkyl, C1-C3 alkoxy, C1-C6 hydroxyalkyl, carbamoyl, N—(C1-C6 alkyl)carbamoyl and N—(C3-C6 cycloalkyl)carbamoyl;
R6 is aryl substituted by R7 and R8;
R7 is selected from the group consisting of hydrogen, —ORf and —NRfRg, where Rf and Rg are independently selected from hydrogen, C1-C6 alkyl, C2-C6 alkyl optionally substituted by amino, C1-C3 mono alkylamino, C1-C3 bis alkylamino, hydroxy or C1-C3 alkoxy, C3-C7 cycloalkyl and heterocyclyl groups from 4 to 7 atoms containing up to 2 heteroatoms selected from oxygen, sulfur and nitrogen, in which those C3-C7 cycloalkyl and heterocyclyl are optionally substituted by one or two substituents independently selected from halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, halothioalkoxy, nitro, cyano, hydroxy, C1-C6 alkoxy, mercapto, amino, C1-C6 alkylthio, C1-C6 mono alkylamino, C1-C6 bis alkylamino, C1-C6 acylamino, N—(C1-C6 alkyl)-N—(C1-C6 acyl)amino, C1-C6 alkyl sulfonylamino, N—(C1-C6 alkyl)-N—(C1-C6 alkyl)sulfonylamino, N—(C1-C6 alkyl)carbamoyl; N—(C3-C7 cycloalkyl)carbamoyl and heterocyclyl groups from 4 to 7 atoms containing up to 2 heteroatoms selected from oxygen, sulfur and nitrogen;
R8 is selected from the group consisting of hydrogen, —ORc, —NRcRd and 5-10 membered heteroaryl or heterocyclyl groups from 4 to 7 atoms containing up to 2 heteroatoms selected from oxygen, sulfur and nitrogen and optionally substituted by a substituent selected from halogen, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 haloalkoxy, C1-C6 halothioalkoxy, nitro, cyano, hydroxy, C1-C6 alkoxy, mercapto, C1-C6 alkylthio, amino, C1-C6 mono alkylamino, C1-C6 bis alkylamino, C1-C6 acylamino, N—(C1-C6 alkyl)-N—(C1-C6 acyl)amino, C1-C6 alkylsulfonylamino, N—(C1-C6 alkyl)-N—(C1-C6 alkyl)sulfonylamino, (N,N-bis(C1-C6 alkyl)carbamoyl)C1-C6 alkyl and heterocyclyl groups from 4 to 7 atoms containing up to two heteroatoms selected from oxygen, sulfur and nitrogen;
Rc and Rd are independently selected from hydrogen, C1-C6 alkyl, C2-C6 alkyl optionally substituted by amino, C1-C3 mono alkylamino, C1-C3 bis alkylamino, hydroxyl, and C1-C3 alkoxy;
n is 0;
their N-oxides, pharmaceutically acceptable salts, enantiomers, stereoisomers, atropisomers, rotamers, tautomers, diastereomers, or racemates.

US Pat. No. 10,336,705

ELECTRICALLY CONDUCTING OLIGO(PYRAZOLES)

The United States of Amer...

1. An electrically conducting organic oligomer comprising 4-nitro-1H-pyrazole-3-yl-amine, 4-trifluoromethyl-1H-pyrazol-3-yl-amine, 4-trichloromethyl-1H-pyrazol-3-yl-amine, 4-tribromomethyl-1H-pyrazol-3-yl-amine, 4-ammonium-1H-pyrazol-3-yl-amine, 4-trimethylammonium-1H-pyrazol-3-yl-amine, 4-triethylammonium-1H-pyrazol-3-yl-amine, or 4-tripropylammonium-1H-pyrazol-3-yl-amine.

US Pat. No. 10,336,704

METHOD FOR PREPARING INDENOISOQUINOLINE DERIVATIVES

NATIONAL TAIWAN NORMAL UN...

1. A method for preparing indenoisoquinoline derivatives represented by one of the following formulas (1) to (31), (34) to (39) and (41) to (46), comprising the following steps:
(A) providing a first reactant represented by the following formula (II) and a second reactant represented by the following formula (III):

wherein A is —OH or —NHR2;
X is —CO;
Y ring is a phenyl ring;
Z is F, Cl, Br or I;
n is an integral of 1 to 4;
each R1 independently is H, nitro, Br, Cl or methoxy; or when n is 2, two adjacent R1 and carbon atoms attached thereto together form a dioxolane; and
R2 is H, methyl, ethyl, propyl, pentyl, allyl, phenyl, benzyl, morpholinoethyl, morpholinopropyl, imidazolpropyl, methoxyethyl, methoxypropyl, phenylbutyl, 4-fluorophenyl, 4-chlorophenyl,
wherein * is a bonding position,
wherein m is an integral of 1 to 4; and
each R3 independently is H, Br, nitro or methoxy; or when m is 2, two adjacent R3 and carbon atoms attached thereto together form a dioxolane; and
(B) reacting the first reactant represented by the formula (II) and the second reactant represented by the formula (III) in a solvent with a catalyst and adding R2NH2 therein in the case where A is —OH, to obtain the indenoisoquinoline derivatives represented by one of the formulas (1) to (31), (34) to (39) and (41) to (46), wherein the catalyst comprises Cu+ or Cu2+.

US Pat. No. 10,336,703

PROCESS FOR THE SYNTHESIS OF IVACAFTOR AND RELATED COMPOUNDS

Council of Scientific and...

1. A one pot process for the preparation of compounds of formula (I) and formula (II);wherein, Ar1 is a 5-6 membered aromatic/hetero aromatic ring, which could be further substituted by alkyl, aryl, hetero aryl and having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, wherein said ring is optionally fused to a 5-12 membered monocyclic or bicyclic, aromatic, partially unsaturated, or saturated ring, wherein each ring contains 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur, wherein Ar1 has m substituents, each selected independently from —WRW; W is a bond or is an optionally substituted C1-C6 alkylidene chain wherein up to two methylene units of W are optionally and independently replaced by —CO—, —CS—, —COCO—, —CONR?—, —CONR?NR?—, —CO2—, —OCO—, —NR?CO2—, —O—, —NR?CONR?—, OCONR?, —NRTSIR?, —NR?NR?CO—, —NR?CO—, —S—, —SO, —SO2—, —NR?—, —SO2NR?—, NR?SO2—, or —NR?SO2NR?—; RW is independently R?, halo, NO2, CN, CF3, or OCF3; m is 0-5; each of R1, R2, R3, R4, and R5 is hydrogen, —X—RX; X is a bond or is an optionally substituted C1-C6 alkylidene chain wherein up to two methylene units of X are optionally and independently replaced by —CO—, —CS—, —COCO—, —CONR?—, —CONR?NR?—, —CO2—, —OCO—, —NR?CO2—, —O—, —NR?CONR?—, —OCONR?—, —NRTSIR?, —NR?NR?CO—, —NR?CO—, —S—, —SO, —SO2—, —NR?—, —SO2NR?—, NR?SO2—, or —NR?SO2NR?—; RX is independently R?, halo, NO2, CN, CF3, or OCF3; R6 is hydrogen, CF3, —OR?, —SR?, or an optionally substituted C1-6 aliphatic group; R7, R8 is hydrogen or a C1-6 aliphatic group optionally substituted with —X—RX; R? is independently selected from hydrogen or an optionally substituted group selected from a C1-C8 aliphatic group, a 3-8-membered saturated, partially unsaturated, or fully unsaturated monocyclic ring having 0-3 heteroatoms independently selected from nitrogen, oxygen, or sulfur, or an 8-12 membered saturated, partially unsaturated, or fully unsaturated bicyclic ring system having 0-5 heteroatoms independently selected from nitrogen, oxygen, or sulfur; or two occurrences of R? are taken together with the atom(s) to which they are bound to form an optionally substituted 3-12 membered saturated, partially unsaturated, or fully unsaturated monocyclic or bicyclic ring having 0-4 heteroatoms independently selected from nitrogen, oxygen, or sulfur; its tautomers or pharmaceutically acceptable salts thereof comprising the steps of;a) coupling indole acetic acid with corresponding amines using suitable coupling agent to obtain indole amides;
b) oxidizing indole amides of step (a) using suitable oxidizing agent followed by treatment with base to obtain desired quinolone carboxamides with 40 to 65% yield, wherein the base is an organic base selected from pyridine, 2,6-lutidine, DMAP (4-dimethylaminopyridine), Et3N (triethylamine), DIPEA (N,N-diisopropyl ethyl amine), N,N-dimethylaniline, DBN (1,5-diazabicyclo(4.3.0)non-5-ene), DABCO (1,4-diazabicyclo[2.2.2]octane) and DBU (1,8-diazabicycloundec-7-ene) or mixture thereof.

US Pat. No. 10,336,702

PHARMACEUTICALLY ACTIVE COMPOUNDS

BerGenBio ASA, Bergen (N...

1. A compound of formula (I):
wherein
one of Q1 and Q2 represents a nitrogen atom and the other represents CH, or both Q1 and Q2 represent nitrogen atoms, and Q3 represents CH;
A represents an optionally substituted five- or six-membered aromatic ring;
R1 represents an aliphatic carbocyclic or heterocyclic ring, optionally substituted by —(C?O)xNRaRb, —ORc, —SO2Rg or optionally substituted alkyl, in which
x is 0 or 1;
Ra and Rb independently represent (a) H, (b) optionally substituted alkyl, (c) optionally substituted cycloalkyl, (d) optionally substituted heterocycloalkyl, (e) —(C?O)Rd, or (f) —SO2Re, wherein Rd and Re independently represent (i) optionally substituted alkyl, (ii) optionally substituted alkoxy, or (iii) optionally substituted cycloalkyl; or Ra and Rb together with the nitrogen atom to which they are attached form an optionally substituted aromatic or aliphatic heterocyclic ring;
Rc represents optionally substituted alkyl;
and
Rg represents optionally substituted cycloalkyl;
R2 represents H, optionally substituted alkyl or halo;
R3 represents an optionally substituted aryl or heteroaryl ring;
R5 and R6 independently represent H or optionally substituted alkyl; or R5 and R6 together with the carbon atom to which they are attached form an optionally substituted cycloalkyl ring, optionally containing a heteroatom;
and the corresponding N-oxides; and pharmaceutically acceptable salts and solvates of such compounds and their N-oxides and prodrugs.

US Pat. No. 10,336,701

PYRIDIN-2-ONE DERIVATIVES OF FORMULA (II) USEFUL AS EP3 RECEPTOR ANTAGONISTS

Janssen Pharmaceutica NV,...

1. A compound of formula (II)
wherein
is selected from the group consisting of naphth-2-yl, indol-5-yl, indazol-5-yl, indazol-6-yl, benzimidazol-5-yl, benzimidazol-6-yl, benzothiazol-5-yl, benzothiazol-6-yl, benzoisothiazol-6-yl, chroman-7-yl, chromen-7-yl, benzo[d][1,3]dioxol-5-yl, 3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl, 3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl and 2,3-dihydro-benzo[b][1,4]dioxin-6-yl;wherein the naphth-2-yl, indol-5-yl, indazol-5-yl, indazol-6-yl, benzimidazol-5-yl, benzimidazol-6-yl, benzothiazol-5-yl, benzothiazol-6-yl, benzoisothiazol-6-yl, chroman-7-yl, chromen-7-yl, benzo[d][1,3]dioxol-5-yl, 3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl, 3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl or 2,3-dihydro-benzo[b][1,4]dioxin-6-yl; is optionally substituted on the phenyl portion of the
bicycle with one to two substituents independently selected from the group consisting of halogen, oxo, cyano, C1-3alkyl, fluorinated C1-2alkyl, C1-3alkoxy, fluorinated C1-2alkoxy and C3-6cycloalkyl;and wherein the naphth-2-yl, indol-5-yl, indazol-5-yl, indazol-6-yl, benzimidazol-5-yl, benzimidazol-6-yl, benzothiazol-5-yl, benzothiazol-6-yl, benzoisothiazol-6-yl, chroman-7-yl, chromen-7-yl, benzo[d][1,3]dioxol-5-yl, 3,4-dihydro-2H-benzo[b][1,4]oxazin-6-yl, 3,4-dihydro-2H-benzo[b][1,4]oxazin-7-yl or 2,3-dihydro-benzo[b][1,4]dioxin-6-yl; is further optionally substituted on the
portion of thebicycle with one to two substituents independently selected from the group consisting of halogen, oxo, cyano, C1-3alkyl, fluorinated C1-2alkyl, C1-3alkoxy, fluorinated C1-2alkoxy and C3-6cycloalkyl;R3 is selected from the group consisting of hydrogen, halogen and C1-4alkyl;
R4 is selected from the group consisting of hydrogen, halogen and C1-4alkyl;
R5 is selected from the group consisting of hydrogen, fluoro, hydroxy, C1-4alkyl, C3-6cycloalkyl and —C(O)NRURV; wherein RU and RV are each independently selected from the group consisting of hydrogen and C1-2alkyl;
is a ring structure selected from the group consisting of cyclopentyl, cyclohexyl, azetidin-3-yl, pyrrolidin-3-yl, piperidin-3-yl, piperidin-4-yl, morpholin-2-yl, thiomorpholin-4-yl, tetrahydropyran-4-yl, 4,5,6,7-tetrahydro-2H-indazol-5-yl, 1,5-dihydro-imidazol-5-yl, 3,5-dihydro-imidazol-5-yl, 4,5-dihydro-imidazol-4-yl, 4,5-dihydro-imidazol-5-yl, imidazolidin-4-yl, imidazolidin-5-yl, 4,5-dihydro-pyrrol-3-yl, 4,5-dihydro-pyrazol-5-yl, 1,2,5-thiadiazolidin-3-yl, 4,5,6,7-tetrahydro-benzo[d]isoxazol-5-yl, imidazo[1,2-a]imdazol-3-yl, imidazo[2,1-c][1,2,4]triazol-5-yl, 6,7-dihydro-5H-imidazo[2,1-c][1,2,4]triazol-6-yl, tetrahydro-1H,3H-pyrrolo[1,2-c]oxazol-6-yl, 6-oxabicyclo[3.2.1]octan-5-yl, 8-azabicyclo[3.2.1]octan-3-yl, 6-azabicyclo[3.2.1]octan-4-yl, 1-oxa-3-azaspiro[4.5]decan-7-yl, 2-azaspiro[4.5]decan-8-yl, 1?2,3-diazaspiro[4.5]decan-7-yl, 2-azaspiro[5.5]undecan-9-yl, 3-azaspiro[5.5]undecan-9-yl, 1,3-diazaspiro[4.5]decan-8-yl and octahydro-cyclopenta[c]pyrrol-5-yl;wherein the
ring structure is optionally substituted with one or more substituents independently selected from the group consisting of C1-4alkyl, hydroxy, oxo, thioxo, cyano, —NRFRG, —NH(CN), ?NH, ?N(CN), ?N(OH), ?N(O—C1-2alkyl), —CH2—NRFRG—C(O)—NRFRG, —C(O)—NRFRG, —C(O)—CH2OH, —SO2—(C1-4alkyl), —NRF—SO2—(C1-4alkyl) and —C(NRFRG)(?N—CN);wherein RF and RG are each independently selected from the group consisting of hydrogen and C1-4alkyl;
provided that when R3 is hydrogen, R4 is hydrogen, R5 is selected from the group consisting of hydrogen, C1-4alkyl and C3-6cycloalkyl, and
is selected from the group consisting of pyrrolidin-3-yl-2-one and piperidin-3-yl-2-one, thenis other than indol-5-yl, indazol-5-yl, indazol-6-yl, benzimidazol-5-yl or benzimidazol-6-yl; wherein the indol-5-yl, indazol-5-yl, indazol-6-yl, benzimidazol-5-yl or benzimidazol-6-yl is optionally substituted with one or more substituents independently selected from the group consisting of halogen, C1-3alkyl and C3-6cycloalkyl;provided further that when
is selected from the group consisting of indol-5-yl, indazol-6-yl and benzimidazol-6-yl; wherein the indol-5-yl, indazol-6-yl or benzimidazol-6-yl is optionally substituted with one to two substituents independently selected from the group consisting of halogen and C1-3alkyl, R3 is hydrogen, R4 is hydrogen and R5 is methyl, thenis other than pyrrolidin-3-yl-2-one or piperidin-3-yl-2-one;provided further than when
is selected from the group consisting of naphth-2-yl and 8-fluoro-naphth-2-yl, R3 is selected from the group consisting of hydrogen, halogen and C1-3alkyl, R4 is hydrogen and R5 is selected from the group consisting of hydrogen, C1-4alkyl and C3-6cycloalkyl, thenis other than imidazolidin-4-yl-2-one;or a tautomer or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,336,700

COMPOUNDS FOR MODULATING MITOCHONDRIAL FUNCTION

Mayo Foundation for Medic...

1. A compound of Formula (I):
or a pharmaceutically acceptable salt thereof,
wherein:
X is absent or selected from the group consisting of CH2 and C(O);
R1 is selected from the group consisting of H, OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, and di(C1-3 alkyl)amino;
R2 is selected from the group consisting of H and C1-6 alkyl;
R3 is selected from the group consisting of H, C1-6 alkyl, —C(O)(C1-3 alkyl), and —C(O)O(C1-3 alkyl);
R4 is selected from the group consisting of C3-10 cycloalkyl, C6-10 aryl, 5-10 membered heteroaryl, and 5-10 membered heterocycloalkyl, each optionally substituted by 1, 2, 3, or 4 independently selected R5 groups; and
R5 is selected from the group consisting of OH, CN, NO2, halo, C1-3 alkyl, C1-3 haloalkyl, C1-3 alkoxy, C1-3 haloalkoxy, C3-7 cycloalkyl, amino, C1-3 alkylamino, and di(C1-3 alkyl)amino.

US Pat. No. 10,336,699

METHOD FOR SYNTHESIZING N,N'-BIS(2,2,6,6-TETRAMETHYL-4-PIPERIDYL)-1,3-BENZENEDICARBOXAMIDE

SUNSHOW (YANTAI) SPECIALT...

1. A method for synthesizing N,N?-bis(2,2,6,6-tetramethyl-4-piperidyl)-1,3-benzenedicarboxamide as shown in the following formula (III),
comprising the following specific steps that a compound of the following formula (I) and a compound of the following formula (II) react under stirring in an organic solvent in the presence of a solid supported catalyst, and after the completion of the reaction, a compound of the formula (III) is obtained by post-treatment,

wherein R1 and R2 are each the same or differently selected from C1-6 alkyl; and
wherein, the solid supported catalyst is prepared by a method comprising the following steps:
S1: treating a KIT-1 molecular sieve with 120° C. to 130° C. water vapor for 20 to 30 minutes, then naturally cooling to room temperature and thoroughly drying in vacuum to obtain a heat-treated molecular sieve;
S2: immersing the heat-treated molecular sieve in a nitric acid aqueous solution with a molar concentration of 0.5 to 0.7 mol/L for 2 to 3 hours and then thoroughly washing with deionized water and completely drying to obtain an acid-treated molecular sieve;
S3: preparing a nickel chloride aqueous solution with a molar concentration of 1.0 mol/L and a lanthanum trifluoromethanesulfonate aqueous solution with a molar concentration of 0.4 mol/L respectively;
S4: impregnating the acid-treated molecular sieve with the nickel chloride aqueous solution, enabling the mass ratio of adsorbed nickel ions to the heat-treated molecular sieve of Step 1 to be (0.05 to 0.08) to 1, and then completely drying to obtain a nickel ion supported molecular sieve; and
S5: impregnating the nickel ion supported molecular sieve with the lanthanum trifluoromethanesulfonate aqueous solution until the molar ratio of the adsorbed lanthanum ions to the adsorbed nickel ions in step S4 is (1.5 to 2.5) to 1, and then completely drying again to obtain the solid supported catalyst.

US Pat. No. 10,336,698

PROCESS FOR THE PRODUCTION OF 2-[4-(CYCLOPROPANECARBONYL)PHENYL]-2-METHYL-PROPANENITRILE

SANOFI-AVENTIS DEUTSCHLAN...

1. A process for preparing a compound of formula I
comprising reacting a compound of formula XX

wherein R1 is fluoro or chloro,
with isobutyronitrile of formula XXI

in the presence of a base, wherein the base is potassium hexamethyldisilazane (KHMDS), sodium hexamethyldisilazane (NaHMDS) or sodium amide.

US Pat. No. 10,336,697

SPIRO[CYCLOBUTANE-1,3?-INDOLIN]-2?-ONE DERIVATIVES AS BROMODOMAIN INHIBITORS

ORION CORPORATION, (FI)

1. A compound of formula (I)
wherein
Cy is a 4-12 membered monocyclic or bicyclic ring containing 0-4 heteroatoms independently selected form N, O, or S;
L is a linker selected from —N(R3a)S(O)2—, —S(O)2N(R3b)—, —C(R3c)(OR3d)—, —NS(O)(CH3)—, —N(R3e)C(O)—, —N(R3f)C(O)N(R3g)—, —N(R3h)C(O)CH(R3i)—, —N(R3j)C(O)CH(R3k)CH(R3l)—, or —N(R3m)C(O)CHCH—;
R3a, R3b, R3c, R3d, R3e, R3f, R3g, R3h, R3i, R3j, R3k, R3l, and R3m are selected, independently, from hydrogen or C1-7 alkyl;
R2 is halogen, C1-7 alkoxy, amino, cyano, oxo, —C(O)O—C1-7 alkyl, optionally substituted aryl, or optionally substituted heterocyclyl; wherein the optional substitution at each occurrence is, independently, selected from 1, 2, or 3 substituents selected from halogen or C1-7 alkoxy;
R4 is hydrogen or halogen;
in cases wherein L is —S(O)2N(R3b)—, —C(R3c)(OR3d)—, —NS(O)(CH3)—, —N(R3e)C(O)—, —N(R3f)C(O)N(R3g)—, —N(R3h)C(O)CH(R3i)—, —N(R3j)C(O)CH(R3k)CH(R3l)—, or —N(R3i)C(O)CHCH—;
then R1 is hydrogen, C1-7 alkyl, halogen, nitro, hydroxy C1-7 alkyl, C3-10 cycloalkyl, optionally substituted aryl, optionally substituted heterocyclyl, optionally substituted heterocyclyl C1-7 alkyl, optionally substituted heterocyclyl C2-7 alkenyl, optionally substituted aryl C1-7 alkyl, optionally substituted aryl C2-7 alkenyl, —NRaRb, —C(O)NRcRd, —C(O)ORe, —C(O)Rf, —C(ORg)-aryl, —C(ORh)(Ri)-aryl, —ORj, or —OC(O)Rk;
wherein the optional substitution at each occurrence is, independently, selected from 1, 2, or 3 substituents selected from halogen, hydroxy, C1-7 alkyl, or C1-7 alkoxy; except that R1 is not hydrogen when L is —S(O)2NH— or —CH(OH)—, and R1 is not hydrogen or halogen when L is —NHC(O)CH(CH3)—;
in cases wherein L is —N(R3a)S(O)2—;
then R1 is —NRaRb, —C(O)NRcRd, —C(O)ORe, —C(O)Rf, —C(ORg)-aryl, —B(OH)2, —C(ORh)(Ri)-aryl, —ORn or —OC(O)Rk, —CH(CH3)—aryl, hydroxy C1-7 alkyl, aryl halo C1-7 alkyl, optionally substituted heterocyclyl C1-7 alkyl, optionally substituted heterocyclyl C2-7 alkenyl, optionally substituted aryl, optionally substituted aryl C2-7 alkenyl, optionally substituted 9-12 membered heterocyclic ring having 1-3 heteroatoms selected from N or O, pyridinyl having 1-2 substituents selected from halogen, hydroxy or C1-7 alkoxy, 2-oxopiperidinyl, fluorophenyl C1-7 alkyl, 1-methylpiperidinyl (when at least one of R2 is halogen), piperidinyl (when at least two of R2 is C1-7 alkoxy), or phenyl C1-7 alkyl (when at least one of R2 is halogen and at least one another of R2 is C1-7 alkoxy); wherein the optional substitution at each occurrence is, independently, selected from 1, 2, or 3 substituents selected from halogen, hydroxy, oxo, C1-7 alkyl, or C1-7 alkoxy;
Ra, Rb, Rc, and Rd are, independently, selected from hydrogen, C1-7 alkyl, C2-7 alkenyl, —C(O)—C1-7 alkyl, optionally substituted heterocyclyl, optionally substituted C3-10 cycloalkyl, optionally substituted heterocyclyl C1-7 alkyl, optionally substituted aryl, optionally substituted aryl C1-7 alkyl, optionally substituted C3-10 cycloalkyl C1-7 alkyl, or optionally substituted —C(O)heterocyclyl; wherein the optional substitution at each occurrence is, independently, selected from 1, 2, or 3 substituents selected from C1-7 alkyl,
—C(O)—C1-7 alkyl, —C(O)O—C1-7 alkyl, halogen, aryl C1-7 alkyl, C1-7 alkoxy, oxo, or hydroxy C1-7 alkyl;
Re, Rf, Rg, Rh, Ri, and Rj are, independently, selected from hydrogen, C1-7 alkyl, halo C1-7 alkyl, optionally substituted aryl, optionally substituted heterocyclyl, optionally substituted heterocyclyl C1-7 alkyl, or optionally substituted heterocyclyl C3-7 cycloalkyl;
wherein the optional substitution at each occurrence is, independently, selected from 1, 2, or 3 substituents selected from C1-7 alkyl or hydroxy C1-7 alkyl;
Rk is selected from optionally substituted aryl, optionally substituted heterocyclyl, optionally substituted heterocyclyl C1-7 alkyl; wherein the optional substitution at each occurrence is, independently, selected from 1, 2, or 3 substituents selected from C1-7 alkyl or hydroxy C1-7 alkyl;
Rn is selected from optionally substituted aryl, halo C1-7 alkyl, C3-7 cycloalkyl substituted by 1-2 substituents selected from halogen, hydroxy or oxo, optionally substituted heterocyclyl, optionally substituted heterocyclyl C1-7 alkyl, optionally substituted heterocyclyl C3-7 cycloalkyl, or —Z—NRa1Rb1; wherein the optional substitution at each occurrence is, independently, selected from 1, 2, or 3 substituents selected from hydroxy, C1-7 alkyl, C3-7 cycloalkyl, hydroxy C1-7 alkyl, methylsulfonyl, halogen, amino, acetyl, or oxo;
Ra1 and Rb1 are, independently, hydrogen, C1-7 alkyl, or C3-7 cycloalkyl;
Z is C1-7 alkyl, C3-7 cycloalkyl or C3-7 cycloalkyl C1-7 alkyl;
m is selected from 0, 1, 2, or 3;
wherein heterocyclyl, at each occurrence is, independently, a non-aromatic, saturated or partially saturated, monocyclic or polycyclic ring with 3 to 10 ring atoms of which at least one is a heteroatom selected from the group consisting of O, N, and S; or a monocyclic, bicyclic, or polycyclic aromatic rings of 6-14 ring atoms containing at least one heteroatom selected from the group consisting of N, O, and S;
or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,336,696

BICARBAZOLE COMPOUND, PHOTO-CURABLE COMPOSITION, CURED PRODUCT THEREOF, CURABLE COMPOSITION FOR PLASTIC LENS, AND PLASTIC LENS

DIC Corporation, Tokyo (...

1. A bicarbazole compound represented by structural formula (1):
(wherein X1 and X2 are each independently a photopolyrnerizable functional group, a structural site having a photopolymerizable functional group, or a hydrogen atom, at least one of X1 and X2 is a photopolymerizable functional group or a structural site having a photopolymerizable functional group, R1 and R2 are each independently a hydrogen atom, an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms, a bromine atom, or a chlorine atom, and at least one of R1 and R2 is a hydrogen atom).

US Pat. No. 10,336,692

METHOD OF FORMING PARACYCLOPHANE CONTAINING FUNCTIONAL GROUP WITH DISULFIDE BOND

MAY-HWA ENTERPRISE CORPOR...

1. A method of forming a paracyclophane containing a disulfide functional group, comprising:adding 3,3?-dithiodipropionic acid and N-ethyl-N?-(3-(dimethylamino)propyl)carbodiimide into 4-aminomethyl [2,2] paracyclophane, thereby obtaining the paracyclophane comprising the disulfide functional group.

US Pat. No. 10,336,691

PESTICIDALLY ACTIVE OXIME AND HYDRAZONE DERIVATIVES

Syngenta Participations A...

1. A compound of formula (I)
wherein
Ar1 is phenyl which is unsubstituted or substituted by one to three substituents independently selected from C1-C6alkyl, C3-C6cycloalkyl, C1-C6haloalkyl, C3-C6halocycloalkyl, C1-C3haloalkyl-C3-C6cycloalkyl, C3-C6cycloalkoxy, halogen, C1-C6alkoxy and C1-C6haloalkoxy;
Ar2 is phenyl which is unsubstituted or substituted by one to three substituents independently selected from C1-C6alkyl, C2-C6alkenyl, C2-C6alkynyl, C3-C6cycloalkyl, C1-C6haloalkyl, C3-C6halocycloalkyl, C1-C3haloalkyl-C3-C6cycloalkyl, C3-C6cycloalkoxy, halogen, cyano, C1-C6alkoxy, C1-C6haloalkoxy and —S—C1-C6alkyl;
X1 is O or NR6;
X2 is a bond, —CH2— or —CH2CH2—;
W is O or NR2;
Y is oxygen or sulfur;
R1 is hydrogen or C1-C6alkyl;
R2 is selected from hydrogen, C1-C6alkyl and C1-C6haloalkyl;
R3 is selected from hydrogen, C1-C6alkyl and C1-C6haloalkyl;
R6 is hydrogen or C1-C6alkyl;
J is a group selected from J1?, J2?, J3?, J9 and J11:

wherein n is 0, 1 or 2, and R20 is independently selected from hydrogen, C3-C6halocycloalkyl and C1-C6haloalkoxy;
RY is C1-C6alkyl; or
J and RY together with the carbon atom to which they are attached form a bicyclic ring of formula

q is 1 or 2;
R16 and R17 are independently selected from hydrogen, C3-C6halocycloalkyl and C1-C6haloalkoxy;
or an agrochemically acceptable salt, stereoisomer, tautomer, N-oxide thereof.

US Pat. No. 10,336,689

GOSSYPOL EFLORNITHINE SCHIFF BASE COMPOUND WITH ANTITUMOR ACTIVITIES AND A METHOD OF PREPARING THE SAME

1. A gossypol eflornithine Schiff base compound having the following Formula I:

US Pat. No. 10,336,688

CARBOCYCLIC COMPOUNDS AS ROR GAMMA MODULATORS

GLENMARK PHARMACEUTICALS ...

1. A process for preparing a compound of formula (Ia)or a pharmaceutically acceptable salt thereof, the process comprising:(i) reacting a compound of formula (1) with a compound of formula (2) to afford the compound of formula (Ia)
whereinR1 is selected from hydroxyl, C1-8alkyl and C1-8alkoxy;
R2 is selected from C1-8alkyl, haloC1-8alkyl, hydroxyC1-8alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-8alkyl;
R3 is selected from hydrogen, C1-8alkyl, haloC1-8alkyl and hydroxyC1-8alkyl;
R4 is selected from C1-8alkyl, C1-8alkoxy, haloC1-8alkyl, hydroxyC1-8alkyl, C3-6cycloalkyl and C3-6cycloalkylC1-8alkyl;
each occurrence of R5 is independently selected from halogen, hydroxyl, cyano, C1-8alkyl, C1-8alkoxy, haloC1-8alkyl, haloC1-8alkoxy, hydroxyC1-8alkyl, C3-6cycloalkyl and optionally substituted C6-14aryl, wherein the substitution on C6-14aryl is halogen;
each occurrence of R6 is independently selected from halogen, cyano, hydroxyl, C1-8alkyl and C3-6cycloalkyl;
‘n’ is 1, 2, 3 or 4;
‘m’ is 0, 1 or 2; and
‘p’ is 0 or 1.

US Pat. No. 10,336,687

SELECTED AMIDE OF Y-HYDROXYBUTYRIC ACID AND USES THEREOF IN THE TREATMENT OF ALCOHOL MISUSE

LABORATORIO FARMACEUTICO ...

1. A compound of Formula (I):
or a pharmaceutically acceptable salt thereof.

US Pat. No. 10,336,686

FLUORINE ATOM-CONTAINING COMPOUND AND USE THEREOF

NISSAN CHEMICAL INDUSTRIE...

1. A fluorine atom-containing compound of formula (1) belowwherein Z is a group of any of formulas (2) to (7) beloweach R1 is independently a hydrogen atom or an alkyl group of 1 to 20 carbon atoms;each Ar is independently a group of any of formulas (8) to (11) below
R2 in formula (8) is a hydrogen atom, an alkyl group of 1 to 20 carbon atoms, an aryl group of 6 to 20 carbon atoms which may be substituted with a cyano group, a nitro group, a halogen atom, an alkyl group of 1 to 20 carbon atoms or a haloalkyl group of 1 to 20 carbon atoms, or a group of any of formulas (12) to (14) belowwherein D is a diarylamino group in which the aryl groups are each independently an aryl group of 6 to 20 carbon atoms; and R3 to R77 in formulas (8) to (14) are each independently a hydrogen atom, a cyano group, a nitro group, a halogen atom, an alkyl group of 1 to 20 carbon atoms or a haloalkyl group of 1 to 20 carbon atoms; andeach ArF is independently a fluoroaryl group of 6 to 20 carbon atoms which may be substituted with a cyano group, a chlorine atom, a bromine atom, an iodine atom, a nitro group, an alkyl group of 1 to 20 carbon atoms, a fluoroalkyl group of 1 to 20 carbon atoms or a fluoroalkoxy group of 1 to 20 carbon atoms; an aryl group of 6 to 20 carbon atoms which, along with being substituted with a fluoroalkyl group of 1 to 20 carbon atoms, a fluorocycloalkyl group of 3 to 20 carbon atoms, a fluorobicycloalkyl group of 4 to 20 carbon atoms, a fluoroalkenyl group of 2 to 20 carbon atoms or a fluoroalkynyl group of 2 to 20 carbon atoms, may also be substituted with a cyano group, a halogen atom or a fluoroalkoxy group of 1 to 20 carbon atoms; a phenyl group substituted with 1 to 3 trifluoromethyl groups; or a 4-ethoxy-3-(trifluoromethyl)phenyl group.

US Pat. No. 10,336,684

PHENYL-(AZA)CYCLOALKYL CARBOXYLIC ACID GPR120 MODULATORS

1. A compound of Formula (II):or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein:L1 is independently selected from: (CH2)3-4, (CH2)2-3OCH2,


W is independently selected from: CH and N;
R2, at each occurrence, is independently selected from: halogen, C1-4 alkyl, and C1-4 alkoxy;
R3 is independently selected from: C1-4 haloalkoxy, Bn, and —(O)0-1—R5;
R4, at each occurrence, is independently selected from: halogen, and C1-4 alkyl;
R5 is independently selected from: phenyl, tetrahydropyranyl, oxadiazolyl, thiazolyl, pyridyl, and pyridazinyl; wherein each moiety is substituted with 0-2 Rc;
Rc, at each occurrence, is independently selected from: halogen, C1-4 alkyl, C1-4 alkoxy, C1-4 alkylthio, C1-4 haloalkyl, C1-4 haloalkoxy, CO2(C1-4 alkyl), and COPh; and
m is independently 0, 1, or 2.

US Pat. No. 10,336,683

PROCESS FOR THE PREPARATION OF AN ANTIBODY-RIFAMYCIN CONJUGATE

Genentech, Inc., South S...

1. A semi-continuous loop process for the preparation of F-benzoxazinorifamycin I,
comprising:
(i) reacting rifamycin S II, and 2-amino-5-fluorobenzene-1,3-diol III in a batch reactor vessel to form I

wherein RIFA SV is formed as a by-product and delivered to a flow-reactor

(ii) one or more oxidants oxidizes the RIFA SV to form II in the flow-reactor, wherein the one or more oxidants are selected from 2,2,6,6-tetramethyl-1-piperidinyloxy (TEMPO), oxygen gas comprising about 5% to about 100% of the reaction gas phase, and benzoquinone; and
(iii) the II formed in the flow-reactor is delivered to the batch reactor vessel,
wherein the one or more oxidants and 2-amino-5-fluorobenzene-1,3-diol III are kept separate.

US Pat. No. 10,336,682

HYDROXYTYROSOL SHIKIMIC ACID ESTER FOR TREATING CARDIOVASCULAR DECEASES AND A METHOD OF PREPARING THE SAME

1. A compound having the following formula I:

US Pat. No. 10,336,678

COMPOSITIONS AND METHODS FOR PREPARING ?,?-UNSATURATED ACIDS

California Institute of T...

1. A method for preparing a compound of formula (I):
or a salt thereof,
comprising
treating a compound of formula (II):

or a salt thereof,
with a masked acyl cyanide (MAC) nucleophile and an iridium catalyst under alkylation conditions, to provide a compound of formula (Ia):

and
treating the compound of Formula (Ia) with an amine, an alcohol, or an acid in the presence of water, to provide the compound of Formula (I);
wherein, as valence and stability permit,
A1 is —OH or any protecting group;
X is OH, OR4, or NRaRb;
R1 and R2 are each independently substituted or unsubstituted alkyl, haloalkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, aryl, heteroaralkyl, heteroaryl, (cycloalkyl)alkyl, cycloalkyl, (heterocycloalkyl)alkyl, or heterocycloalkyl;
R3 is substituted or unsubstituted alkyl;
R4 is substituted or unsubstituted alkyl, alkenyl, haloalkyl, (cycloalkyl)alkyl, or cycloalkyl; and
Ra and Rb are each independently hydrogen or substituted or unsubstituted alkyl, alkenyl, alkynyl, aralkyl, cycloalkyl, aryl, heteroaralkyl, heteroaryl, (cycloalkyl)alkyl, cycloalkyl, (heterocycloalkyl)alkyl, or heterocycloalkyl; or
Ra and Rb, together with the nitrogen atom to which they are attached, form a 5- or 6-membered heterocycloalkyl.

US Pat. No. 10,336,676

ORGANOLEPTIC (ALKOXYMETHYLENE)OCTAHYDRO-1H-4,7-METHANOINDENE COMPOUNDS

1. A compound of formula:
wherein an alkoxymethylene group, ?CHOR, is present at position 1, 2 or 3; and
wherein R represents a C1-3 alkyl group.

US Pat. No. 10,336,675

BIAROMATIC VITAMIN D ANALOGS

DSM IP ASSETS B.V., Heer...

1. A compound according to formula (I):
wherein
X and Y, are either both —CH2—, or one of X and Y is —CH2— and the other is —O—;
R1 is a methyl group or an ethyl group;
A is either a carbon atom, CH group, CH2 group or an oxygen atom;
one of Z1 and Z2 represents a hydroxyl group and the other one is a hydrogen atom;
R2 and R3, independently of each other, represent a hydrogen atom, a methyl group, an ethyl group, or a CF3 group or R2 and R3, together with the carbon they are bound to, form a cyclopropyl group;
the dotted/solid lines () represent either a single carbon-carbon bond or a double carbon-carbon bond, with the proviso that, if two of said bonds are double bonds, the double bonds are conjugated;
one of R6 and R7 represents a hydrogen atom and the other one represents a radical R8, wherein
wherein R4 represents a hydrogen atom, a methyl group, an ethyl group, a propyl group, a (CH2)nOR9 group where n is 1, 2, 3 or 4; and R5 represents a hydrogen atom, a methyl group, an ethyl group, a propyl group, or a (CH2)nOR10 group where n is 1, 2 or 3, and whereinR9 and R10, independently of each other, represent a hydrogen atom, a methyl group, or an ethyl group.

US Pat. No. 10,336,674

PROCESS AND SYSTEM FOR CHEMICAL SYNTHESIS

SIEMENS AKTIENGESELLSCHAF...

1. A method for chemical synthesis, the method comprising:compressing gaseous starting materials to an operating pressure of at least 200 bar;
supplying the starting materials to a synthesis reactor;
removing a product mixture from the synthesis reactor in a liquid state;
at least partially converting the product mixture into a gaseous phase;
withdrawing mechanical energy from the at least partially gaseous product mixture by reducing a pressure of the product mixture; and
using the mechanical energy to compress the gaseous starting materials.

US Pat. No. 10,336,671

PROCESS FOR RECOVERING A METALLIC COMPONENT

SHELL OIL COMPANY, Houst...

1. A process for preparing glycols from a saccharide-containing feedstock comprising steps of:(i) providing a saccharide-containing feedstock, water and hydrogen to a reactor, wherein the reactor contains at least two active catalytic components, said active catalyst components comprising, as a first active catalyst component, one or more materials selected from transition metals from groups 8, 9 or 10 or compounds thereof, with catalytic hydrogenation capabilities; and, as a second active catalyst component, one or more homogeneous catalysts selected from tungsten, molybdenum, lanthanum, tin or compounds or complexes thereof;
(ii) withdrawing a reactor product stream from the reactor;
(iii) separating the reactor product stream into at least a glycol product stream and a hydrocarbon heavies stream, wherein the hydrocarbon heavies stream is at least partially recycled back to the reactor;
(iv) bleeding a hydrocarbon product stream from the hydrocarbon heavies stream as it is recycled to the reactor;
(v) subjecting the hydrocarbon product stream to a thermal oxidation at a temperature of from 300 to 750° C., thereby providing a solid residue; and
(vi) collecting the solid residue.

US Pat. No. 10,336,668

METHOD FOR PRODUCING CIS- AND TRANS-ENRICHED MDACH

BASF SE, Ludwigshafen (D...

1. A process for preparing trans-enriched MDACH, the process comprising:distilling an MDACH starting mixture in the presence of an auxiliary, wherein trans-enriched MDACH is distilled off,
and wherein
the auxiliary is an organic compound having
a molar mass of 62 to 500 g/mol,
a boiling point at least 5° C. above the boiling point of cis,cis-2,6-diamino-1-methylcyclohexane, where the boiling points are each based on a pressure of 50 mbar, and
2 to 4 functional groups selected independently from the group consisting of an alcohol group, a primary amino group, a secondary amino group and a tertiary amino group,
wherein the MDACH starting mixture comprises a total amount of MDACH, wherein the total amount of MDACH in the MDACH starting mixture comprises 0% to 100% by weight of 2,4-diamino-1-methylcyclohexane (2,4-MDACH) and 0% to 100% by weight of 2,6-diamino-1-methylcyclohexane (2,6-MDACH), and wherein the MDACH starting mixture comprises both trans and cis isomers, and
wherein trans-enriched MDACH is a mixture comprising a total amount of MDACH, wherein the total amount of MDACH in the mixture of trans-enriched MDACH comprises 0% to 100% by weight of 2,4-MDACH and 0% to 100% by weight of 2,6-MDACH, where the proportion of trans isomers in the total amount of MDACH in the mixture of trans-enriched MDACH is higher than the proportion of trans isomers in the total amount of MDACH in the MDACH starting mixture.

US Pat. No. 10,336,667

CATALYST FOR DEHYDROGENATING HYDROCARBONS

BASF SE, (DE)

1. A dehydrogenation catalyst comprisingat least one iron compound,
at least one potassium compound and
from 15 to 20% by weight, based on the total catalyst, of at least one cerium compound, calculated as CeO2,
wherein the at least one iron compound and the at least one potassium compound are at least partly present in the form of one or more K/Fe mixed oxide phases of the general formula
KxFeyOz,
where x is from 1 to 17; y is from 1 to 22 and z is from 2 to 34, where the catalyst comprises from 65 to 85% by weight, based on the total catalyst, of the one or more K/Fe mixed oxide phases.

US Pat. No. 10,336,666

PROCESSES FOR PRODUCING OLEFINS FROM PARAFFINS

UOP LLC, des plaines, IL...

1. A process for dehydrogenation of a hydrocarbon-containing feed stream comprising:a) passing a first portion of the hydrocarbon-containing feedstream through at a first catalytic dehydrogenation reactor to provide a first effluent stream, the hydrocarbon-containing feedstream comprising propane, butane, or a combination thereof;
b) measuring a first internal differential pressure across a first screen or a second screen in the first catalytic dehydrogenation reactor and bypassing a second portion of the hydrocarbon-containing feed stream around the first catalytic dehydrogenation reactor when the first internal differential pressure is above a first predetermined limit;
c) passing a first portion of first effluent stream and at least a portion of the bypassed second portion of the hydrocarbon-containing feed stream to a second catalytic dehydrogenation reactor to provide a second effluent stream;
d) measuring a second internal differential pressure across a first screen or a second screen in the second catalytic dehydrogenation reactor and bypassing a second portion of the first effluent stream around the second catalytic dehydrogenation reactor when the second internal differential pressure is above a second predetermined limit;
e) passing a first portion of the second effluent stream and at least one of, at least a portion of the bypassed section portion of the hydrocarbon-containing feed stream and at least a portion of the bypassed second portion of the first effluent stream, to a third catalytic dehydrogenation reactor to provide a third effluent stream;
f) measuring a third internal differential pressure across a first screen or a second screen in the third catalytic dehydrogenation reactor and bypassing a second portion of the second effluent stream around the third catalytic dehydrogenation reactor when the third internal differential pressure is above a third predetermined limit;
g) passing a first portion of the third effluent stream and at least one of, at least a portion of the bypassed section portion of the hydrocarbon-containing feed stream, at least a portion of the bypassed second portion of the first effluent stream and at least a portion of the bypassed second portion of the second effluent stream, to a fourth catalytic dehydrogenation reactor to provide a fourth effluent stream; and
h) measuring a fourth internal differential pressure across a first screen or a second screen in the fourth catalytic dehydrogenation reactor and bypassing a second portion of the third effluent stream around the fourth catalytic dehydrogenation reactor when the fourth internal differential pressure is above a fourth pre-determined limit
wherein the first, second, third, and fourth catalytic dehydrogenation reactors are moving bed reactors and are arranged in series.

US Pat. No. 10,336,664

METHOD OF MAKING VANADIUM CATALYST

King Fahd University of P...

1. A method for producing a cerium-modified vanadium catalyst, comprisinga support material comprising alumina modified by cerium, and
a catalytic material comprising one or more selected from the group consisting of V2O5, VO2, and V2O3 disposed on the support material,
wherein the catalyst comprises 1-15% of the one or more V2O5, VO2, and V2O3 and 0.05-1.0% of cerium by weight relative to the total weight of the catalyst,
wherein the method comprises:
mixing an aluminum salt or hydrate with a cerium salt or hydrate in a solvent to form an alumina precursor solution;
adding a base to and hydrolyzing the alumina precursor solution to form the support material comprising alumina modified by cerium;
mixing the support material with a solution comprising a vanadyl coordination complex or salt in toluene to form loaded catalyst precursors;
reducing the loaded catalyst precursors with H2 gas to form reduced catalyst precursors; and
oxidizing the reduced catalyst precursors with oxygen to form the catalyst.

US Pat. No. 10,336,662

AMMONIUM NITRATE PRILL HAVING A NON-HYGROSCOPIC SHELL

The United States of Amer...

1. An in-situ process for converting a prilled ammonium nitrate to a quantity of sealed prills, where the quantity of sealed prills are non-hygroscopic, comprising:drying the prilled ammonium nitrate under a vacuum and at an elevated temperature, over an extended time period, therein producing a quantity of dried prills;
selecting a desired shell weight percent, where the desired shell weight percent is a weight percentage of the quantity of dried prills;
preparing a first solution having a total first volume comprising a first reactant having a moiety with an affinity for ammonium nitrate and at least two epoxy groups, and a first dilution solvent having a partial first volume accounting for most of the total first volume, wherein the first dilution solvent is miscible with a nonpolar reaction diluent;
preparing a second solution having a total second volume comprising a second reactant having at least two nucleophilic groups, wherein each of said at least two nucleophilic group reacts with at least one epoxy group, and a second dilution solvent having a partial second volume that accounts for most of the total second volume, and wherein the second dilution solvent is miscible with the nonpolar reaction diluent;
adding to a reaction vessel a desired weight of the quantity of dried prills, a volume of the reaction diluent sufficient for covering the dried prills, and an inflow of a purge gas, which is a dry inert gas;
clearing the reaction vessel of any residual air, which contains moisture, by several repetitions of purging the vessel and vacuuming out the purge gas;
heating and gently moving the dried prills and the reaction diluent in the reaction vessel;
adding dropwise the first solution to the reaction vessel, wherein the first solution contains a weight quantity of the first reactant that is about a first half of a needed equivalents to form shells on the dried prills added to the reaction vessel, and wherein when added the first reactant migrates through the nonpolar reaction diluent to the dried prills;
adding dropwise the second solution to the reaction vessel, wherein the second solution contains a weight quantity of the second reactant that is about a second half of a needed equivalents to form shells on the dried prills added to the reaction vessel, wherein when added the second reactant reacts with the first reactant that has collected on the dried prills, therein beginning an in-situ formation of shells having a shape that is specific to an individual prill;
heating and gently mixing the reaction vessel at about 80° C. for multiple hours, maintaining a positive inert gas pressure, therein reacting in-situ the first reagent with the second reagent forming a plurality of highly crosslinked polymeric shells for individually encapsulating and sealing all of the dried prills, wherein the formed plurality of highly crosslinked polymeric shells have a cumulative weight based on the desired shell weight percent; and
using vacuum filtration for isolating the quantity of sealed dried prills, wherein the AN is not hygroscopic.

US Pat. No. 10,336,661

HIERARCHICAL SELF-ASSEMBLED ENERGETIC MATERIALS AND FORMATION METHODS

The Curators of the Unive...

1. An energetic nanocomposite comprising Al fuel nanoparticles and oxidizer nanoparticles covalently bonded to functionalized graphene sheets.

US Pat. No. 10,336,660

STABILIZED DCD AND/OR ALKYL THIOPHOSPHORIC TRIAMIDE SOLVENT SYSTEMS AND USE IN AGRICULTURAL APPLICATIONS

RHODIA OPERATIONS, Paris...

16. A stable liquid agricultural composition consisting ofbetween 45 and 55 wt. % N-(n-butyl)-thiophosphoric triamide (NBPT) as a urease inhibitor;
dimethyl sulfoxide, wherein at least 38 wt. % of the composition is dimethyl sulfoxide;
an amine stabilizer selected from the group consisting of 2-amino-2-methyl-1-propanol, 2-amino-1-butanol and mixtures thereof, wherein the amine stabilizer is present in an amount of from 4 wt % to 10 wt %, by weight of composition;
optionally, at least one nitrification inhibitor;
optionally, at least one co-solvent selected from the group consisting of:
(a) at least one dioxolane compound of formula (II.b):

wherein R6 and R7 individually comprises a hydrogen, an alkyl group, an alkenyl group, or a phenyl group, wherein n is an integer of from 1 to 10;
b) at least one compound of formula (III):
R3OOC-A-CONR4R5  (III),
wherein R3 comprises a C1-C36 alkyl group; wherein R4 and R5 individually comprise a C1-C36 alkyl group, wherein R4 and R5 can optionally together form a ring; and wherein A is a linear or a branched divalent C2-C12 alkyl group; and
c) a glycol, or glycol derivative, or combinations thereof; and
optionally, at least one dye;
optionally, an odor masking agent comprising at least one member selected from the group consisting of terpineol, 4-allylanisole, limonene4-(2,6,6-Trimethyl-2-cyclohexenyl)-3-buten-2-one, isoamyl butyrate, benzaldehyde, diethyl malonate, cyclohexyl acetate, anisole, mint, oil Japanese cherry, and ?-Ionone.

US Pat. No. 10,336,656

CERAMIC ARTICLE WITH REDUCED SURFACE DEFECT DENSITY

APPLIED MATERIALS, INC., ...

1. A heat-treated ceramic article prepared by a process comprising:heating a machined ceramic article to a temperature range between about 1000° C. and about 1800° C., wherein the machined ceramic article comprises an uncoated bulk sintered ceramic comprising a rare earth oxide, the machined ceramic article has a surface with an initial surface defect density and an initial surface roughness, the initial surface defect density is based on a plurality of surface defects, the plurality of surface defects comprises a plurality of broken bonds having surface particles bound thereto, and the surface particles comprise the rare earth oxide and are formed by breaking of bonds of the machined ceramic article to form the plurality of broken bonds;
heat treating the machined ceramic article at one or more temperatures within the temperature range for a duration of up to about 24 hours, the heat treating comprising:
melting a layer of the machined ceramic article at the surface, wherein at least a fraction of the surface particles are melted to produce melted surface particles;
diffusing the melted surface particles comprising the rare earth oxide into the plurality of surface defects at the melted layer to form unbroken bonds with the layer at the plurality of surface defects; and
re-growing the melted surface particles comprising the rare earth oxide on grains of the machined ceramic article; and
cooling the machined ceramic article, wherein the heating and cooling are each performed at a ramping rate of less than about 5° C. per minute to avoid cracking of the machined ceramic article, and wherein the heat-treated ceramic article has a reduced surface defect density that is lower than the initial surface defect density, a reduced amount of surface particles comprising the rare earth oxide that are trapped by broken bonds, and a reduced surface roughness, caused by the heat treating that comprises an average roughness of about 26.26 ?-inch or less and a maximum peak to valley height of about 198.65 ?-inch or less, wherein the reduced surface roughness is lower than the initial surface roughness.

US Pat. No. 10,336,654

CEMENTED CARBIDE WITH COBALT-MOLYBDENUM ALLOY BINDER

KENNAMETAL INC., Latrobe...

1. A sintered cemented carbide composition comprising:a hard particle phase including tungsten carbide; and
a cobalt-based metallic binder comprising a cubic cobalt-molybdenum solid solution phase.

US Pat. No. 10,336,653

CHROMIUM OXIDE REFRACTORY OBJECT AND METHODS OF FORMING THEREOF

1. A refractory object comprising:a Cr2O3 content of at least about 80 wt. % of a total weight of the refractory object;
an Al2O3 content of at least about 0.7 wt. % and not greater than about 10.0 wt. % of the total weight of the refractory object;
a SiO2 content of at least about 0.3 wt. % and not greater than about 5.0 wt. % of the total weight of the refractory object;
a TiO2 content of at least about 1.8 wt. % and not greater than about 5.6 wt. % TiO2 of the total weight of the refractory object;
a ZrO2 content of not greater than about 7.5 wt. % of the total weight of the refractory object;
a ratio ROCAl2O3/ROCSiO2 of at least 1 and not greater than 6.5, wherein ROCAl2O3 represents a content of Al2O3 in wt. % of the total weight of the refractory object and ROCSiO2 represents a content of SiO2 in wt. % of the total weight of the refractory object; and
an MOR of at least about 47 MPa as measured at 1200° C.

US Pat. No. 10,336,651

COATED ARTICLE WITH IR REFLECTING LAYER(S) AND SILICON ZIRCONIUM OXYNITRIDE LAYER(S) AND METHOD OF MAKING SAME

GUARDIAN GLASS, LLC, Aub...

1. A coated article including a coating supported by a glass substrate, the coating comprising moving away from the glass substrate:a dielectric layer comprising zirconium silicon oxynitride;
a first layer comprising zinc stannate;
a first layer comprising zinc oxide located over and directly contacting the layer comprising zinc stannate;
a first infrared (IR) reflecting layer comprising silver located on the substrate over and directly contacting the first layer comprising zinc oxide; and
a contact layer comprising metal oxide located over and directly contacting the first IR reflecting layer comprising silver;
a second layer comprising zinc stannate on the glass substrate over at least the first IR reflecting layer and the contact layer;
a second layer comprising zinc oxide located over at least the second layer comprising zinc stannate;
a second IR reflecting layer comprising silver located over at least the first IR reflecting layer, the first and second layers comprising zinc stannate, and the first and second layers comprising zinc oxide;
another dielectric layer over at least the second IR reflecting layer comprising silver;
wherein the coating contains two silver based IR reflecting layers;
wherein the second IR reflecting layer comprising silver is at least 10 angstroms (?) thicker than the first IR reflecting layer comprising silver;
wherein the dielectric layer comprising zirconium silicon oxynitride is at least 10 angstroms (?) thicker than the first layer comprising zinc stannate; and
wherein the second layer comprising zinc stannate is at least 20 angstroms (?) thicker than the dielectric layer comprising zirconium silicon oxynitride.

US Pat. No. 10,336,650

ANTI-SOILING COMPOSITIONS FOR DRY AND WET SOIL

3M Innovative Properties ...

1. A coated article comprising a dried coating comprising:a first set of silica nanoparticles having an average diameter of less than 20 nm;
a second set of silica nanoparticles having an average diameter of 20 nm to 120 nm; and
a silane comprising at least one organic group bound to the silicon atom of the silane via a carbon atom,
wherein the organic group is substituted with both at least one (a) anionic group or the conjugate acid thereof, and at least one (b) cationic group or the conjugate base thereof,
wherein the dried coating has essentially no binders,
wherein the dried coating is hydrophilic, and
wherein the average surface roughness of the dried coating is from 5 nm to 100 nm over a 5 micron by 5 micron area.

US Pat. No. 10,336,645

RARE EARTH METAL-DOPED QUARTZ GLASS AND METHOD FOR PRODUCING THE SAME

1. Method for producing rare earth metal-doped quartz glass, the method comprising the steps of:(a) providing a blank of the rare earth metal-doped quartz glass; and
(b) homogenizing the blank by softening the blank zone by zone in a heating zone and by twisting the softened zone along a rotation axis,
wherein during homogenization according to method step (b), the blank is softened under the action of an oxidizingly acting or neutral plasma.