Genentech, Inc.;Gilead Connecticut; Inc.;Gilead Connecticut, Inc.
发明人:
BARBOSA, Antonio J. M.,BLOMGREN, Peter A.,CURRIE, Kevin S.,KRISHNAMOORTHY, Ravi,KROPF, Jeffrey E.,LEE, Seung H.,MITCHELL, Scott A.,ORTWINE, Daniel,SCHMITT, Aaron C.,WANG, Xiaojing,XU, Jianjun,YOUNG, W
申请号：
ES11731170
公开号：
ES2573716T3
申请日:
2011.05.06
申请国别(地区):
ES
年份:
2016
代理人:
摘要：
Compound selected from formula I: ** Formula ** or stereoisomers, tautomers or pharmaceutically acceptable salts thereof, wherein: R1 is H, D, F, Cl, CN, -NH2, -NHCH3, -N (CH3) 2, -OH, -OCH3, -OCH2CH3, -OCH2CH2OH, heteroaryl selected from imidazolyl and pyrazolyl, heterocyclyl selected from oxetanyl and azetidinyl, and C1-C3 alkyl； R2, R3 and R4 are independently selected from H, D, F, Cl, -NH2, -NHCH3, -N (CH3) 2, -OH, -OCH3, -OCH2CH3, -OCH2CH2OH, and C1-C3 alkyl； R5 is optionally substituted C6-C20 aryl, C3-C12 carbocyclyl, C2-C20 heterocyclyl, C1-C20 heteroaryl, - (C6-C20 aryl) - (C2-C20 heterocyclyl), - (C1 heteroaryl -C20) - (C2-C20 heterocyclyl), - (C1-C20 heteroaryl) - (C1-C6 alkyl), or - (C1-C20 heteroaryl) -C (>； = O) - (C2 heterocyclyl -C20)； R6 is H, F, -NH2, -OH, or optionally substituted C1-C3 alkyl； X is S, S (>； = O), S (>； = O) 2, N, NR6, O, or CR7； R7 is independently selected from H, D, F, Cl, -CH3, -CH2CH3, -CN, -CH2F, -CHF2, -CF3, -NH2, -OH, and -OCH3； Y1 and Y2 are independently selected from CR6 and N； Z1, Z2, Z3, and Z4 are independently selected from C, CR7, and N； Z5 is selected from -C (R3) 2-, -C (>； = O) -, -N (R6) -, -C (R3) 2C (R3) 2-, -C (R3) 2C (>； = O ) -, -CR3>； = CR3-, -CR3>； = N-, -N (R6) C (R3) 2-, -N (R6) C (R3) 2C (R3) 2-, and -OC (R3 ) 2C (R3) 2-； one of Z1 and Z2, or X and Z1, in which X is not S, S (>； = O), or S (>； = O) 2, forms an aryl, carbocyclyl, heterocyclyl or heteroaryl ring of five, six or seven members； wherein alkyl, carbocyclyl, heterocyclyl, aryl, and heteroaryl are optionally substituted with one or more groups independently selected from D, F, Cl, Br, I, -CH3, -CH2CH3, -CH2CH (CH3) 2, - CH2OH, -CH2CH2OH, -C (CH3) 2OH, -CH (OH) CH (CH3) 2, -C (CH3) 2CH2OH, -CH2CH2SO2CH3, -CH2OP (O) (OH) 2, - CN, -CH2F, -CHF2, -CF3, -CO2H, -COCH3, -CO2CH3, -CO2C (CH3) 3, -COCH (OH) CH3, -CONH2, - CONHCH3, -CON (CH3) 2, -C (CH3) 2CONH2, -NO2, - NH2, -NHCH3, -N (CH3) 2, -NHCOCH3, -N (CH3) COCH3, - NHS (O) 2CH3,
