US Patent No. 9,403,846

CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-D][1,3]THIAZIN-2-AMINE COMPOUNDS


Patent No. 9,403,846
Issue Date August 02, 2016
Title Carbocyclic- And Heterocyclic-substituted Hexahydropyrano[3,4-d][1,3]thiazin-2-amine Compounds
Inventorship Michael Aaron Brodney, Newton, MA (US)
Christopher Ryan Butler, Canton, MA (US)
Erik Alphie LaChapelle, Johnston, RI (US)
Assignee Pfizer Inc., New York, NY (US)

Claim of US Patent No. 9,403,846

1. A compound of formula (I)
or a tautomer thereof or a pharmaceutically acceptable salt of said compound or tautomer, wherein:
R1 is selected from hydrogen, —CH3, —CH2F, —CHF2, —CF3, or —CH2OCH3;

R2 is —(C(R3a)(R3b))m—(C3-C6)cycloalkyl or —(C(R3a)(R3b))m-(4- to 10-membered) heterocycloalkyl having one to three heteroatoms independently selected from N, O or S, wherein said
N is optionally substituted with R4; and wherein each available carbon position of said (C3-C6)cycloalkyl moiety or said (4- to 10-membered)heterocycloalkyl moiety is optionally substituted with one to two R6;

R3a and R3b are each independently hydrogen, fluoro, or (C1-C6)alkyl; wherein said (C1-C6)alkyl is optionally substituted with one to three fluoro;

R4 is selected from (C1-C6)alkyl, (C1-C6)alkylcarbonyl, (C3-C6)cycloalkylcarbonyl or (C1-C6)alkylcarbonyl(C1-C6)alkyl; wherein said (C1-C6)alkyl moiety, said (C1-C6)alkylcarbonyl moiety and said (C1-C6)alkylcarbonyl(C1-C6)alkyl moiety are optionally substituted with one to three fluoro;

R5 at each occurrence is independently halogen, (C1-C3)alkyl, and (C1-C3)alkoxy, wherein said (C1-C3)alkyl moiety and said (C1-C3)alkoxy are optionally substituted with one to three fluoro;

R6 at each occurrence is independently halogen, —OH, —CN, (C1-C6)alkyl, and (C1-C6)alkoxy, wherein said (C1-C6)alkyl or (C1-C6)alkoxy is optionally substituted with one to three fluoro;

m is 0, 1, or 2; and
b is 0, 1, 2, 3, 4, or 5.