LAM, Patrick Y.S.,CLARK, Charles G.,CORTE, James R.,EWING, William R.,GILLIGAN, Paul J.,JEON, Yoon,YANG, Wu,SMITH, Leon M.,WANG, Yufeng
申请号：
ES12766737
公开号：
ES2563445T3
申请日:
2012.08.06
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
A compound of Formula (Ia): ** Formula ** or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a solvate thereof, in which: G1 is selected from the group consisting of a 6-membered aryl and a 5-6 membered heteroaryl, wherein said aryl and heteroaryl are substituted with 1-5 R8； Ring A is selected from the group consisting of a 6-membered aryl and a 5-6 membered heterocycle, wherein said aryl and heterocycle are substituted with 1-3 R13； X is selected from the group consisting of C4-8 alkylene and C4-8 alkenylene, wherein said alkylene and alkenylene are substituted with R1, R2 and R6； alternatively, one or more of the carbon atoms of said alkylene and alkenylene may be replaced by O, C>； = O, S (O) p, NH and N (C1-4 alkyl)； X2 is selected from the group consisting of CHR11, C>； = O, O, NH and N (C1-4 alkyl)； X3 is CR12 or N； provided that X3 is CR12 when X2 is O, NH or N (C1-4 alkyl)； R1 and R2 are independently selected from the group consisting of H, halogen, C1-6 alkyl, OH, NH2, -CH2NH2, C1-4 haloalkyl, -OCH2F, -OCHF2, -OCF3, NH (C1-4 alkyl), N (C1-4 alkyl) 2, C1-4 alkoxy, -CH2OH and -CH2O (C1-4 alkyl)； alternatively, R1 and R2 are taken together with the carbon atoms to which they are attached to form a carbocycle； R3 is selected from the group consisting of H, haloalkyl, -C (>； = O) OH, -C (>； = O) O-C1-4alkyl and -C (>； = O) NR9R10； R4 is selected from the group consisting of H and C1-6 alkyl； alternatively, R3 and R4 are, together,>； = O； R5 is independently selected from the group consisting of H, halogen, C1-4 alkyl, OH, CN, NR9R10, NO2, C1-4 alkoxy, -C (>； = O) OH, -C (>； = O) O (alkyl C1-4), -C (>； = O) NH2, C (>； = O) NR9 (C1-4 alkyl), -C (>； = O) NR9-C1-4 alkylene- (C1-4 alkyl), -NR9C (>； = O) C1-4alkyl, -NR9C (>； = O) C1-4alkyl, -NR9C (>； = O) C1-4alkyl (C1-4alkyl), - NR9C (>； = O ) C1-4-Oalkylene (C1-4 alkyl), -NR9C (>； = O) NH (C1-4 alkyl), R15, -C (>； = O) OR15, -C (>； = O) NR9R15, - NR9R15, - NR9C (
