US Patent No. 10,035,792

RESORCINOL DERIVATIVE AS HSP90 INHIBITOR


Patent No. 10,035,792
Issue Date July 31, 2018
Title Resorcinol Derivative As Hsp90 Inhibitor
Inventorship Shuhui Chen, Shanghai (CN)
Charles Z. Ding, Shanghai (CN)
Xiaobing Yan, Shanghai (CN)
Wei Huang, Shanghai (CN)
Guoping Hu, Shanghai (CN)
Jian Li, Shanghai (CN)
Xiquan Zhang, Lianyungang (CN)
Ling Yang, Lianyungang (CN)
Hongjiang Xu, Lianyungang (CN)
Assignee CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD., Lianyungang (CN)

Claim of US Patent No. 10,035,792

1. A compound represented by formula (I), or a pharmaceutically acceptable salt thereof,
wherein:
X and Y are each independently selected from N, O or S;
X1, X2, Y1, Y2 and the carbon atom linking X1 and X2 together form a 5- to 7-membered aromatic ring, aliphatic saturated ring or aliphatic unsaturated ring;
X1 and X2 are each independently selected from C, O, S, N, —C?C—, —C?N—;
C in X1 or X2 may be unsubstituted, or may be substituted with R01 or R02;
R01 and R02 are each independently selected from halogen, CN, OH, SH, NH2,CHO, COOH, C1-10 alkyl, N—C1-10 alkylamino, N,N-di(C1-10 alkyl)amino, C1-10 alkoxy, C1-10 alkanoyl, C1-10 alkoxycarbonyl, C1-10 alkylsulfonyl, C1-10 alkylsulfinyl, C3-10 cycloalkyl, C3-10 cycloalkylamino, C3-10 cycloalkoxy, C3-10 cycloalkyl acyl, C3-10 cycloalkoxycarbonyl, C3-10 cycloalkylsulfonyl, C3-10 cycloalkylsulfinyl, C1-10 alkyl substituted with C3-10 cycloalkyl;
Y1 and Y2 are each independently selected from C or N;
two substituents on Y1 and Y2 are linked together to form a five-, six- or seven-membered nitrogen-containing saturated ring or aromatic ring having substituents R1, R2 and R3;
R1, R2 and R3 are each independently selected from hydrogen, C1-10 alkyl, hydroxyl C1-10 alkyl, C1-6 alkoxy-C1-6 alkyl, halo C1-10 alkyl, C1-6 alkylsulfonyl-C1-6 alkyl, C1-6 alkylamido-C1-6 alkyl, N,N-di(C1-6 alkyl)aminoacyl-C1-6 alkyl, N,N-di(C1-6 alkyl)amino-C1-6 alkanoyl, morpholinyl-C1-6 alkanoyl, N-C1-10 alkylamino, N,N-di(C1-10 alkyl)amino, C1-10 alkoxy, C1-10 alkanoyl, C1-10 alkoxycarbonyl, C1-10 alkylsulfonyl, C1-10 alkylsulfinyl, C3-10 cycloalkyl, C3-10 cycloalkylamino, C3-10 cycloalkyloxy, C3-10 cycloalkyl acyl, C3-10 cycloalkoxycarbonyl, C3-10 cycloalkylsulfonyl, C3-10 cycloalkylsulfinyl, C3-10 cycloalkyl-C1-5 alkyl;
or substituents of R2 and R3 are linked with each other by a covalent bond to form a five-, six- or seven-membered saturated ring with a substituent R03 or without substituents;
R03 is selected from C1-6 alkyl or halogen;
R4 is selected from H, halogen, C1-6 alkyl, C3-10 cycloalkoxy, phenyl substituted C1-6 alkyl, phenyl substituted C2-6 alkenyl, phenyl, C1-6 alkyl substituted phenyl, C3-6 cycloalkyl;
R5 is selected from H, cyano, carboxyl, C1-6 alkoxyacyl, C1-7 alkylaminocarbonyl, halo C1-6 alkylaminocarbonyl, C1-6 alkoxy-C1-6 alkylaminocarbonyl, N,N-di(C1-6 alkyl)amino-C1-6 alkylaminocarbonyl, aminocarbonyl, hydroxy C1-6 alkylaminocarbonyl, hydroxyl-substituted halo C1-6 alkyl, nitrile group-substituted amidino, or selected from C3-10 cycloalkyl, C3-10 cycloalkenyl, or a 5- to 10-membered aromatic ring optionally substituted with one or more R05;
R05 is selected from C1-6 alkyl, C3-10 cycloalkyl.