Obshchestvo S Ogranichennoy Otvetstvennostyou "Fusion Pharma"
发明人:
CHILOV, Germes Grigorievich,TITOV, Ilya Yurievich
申请号：
ES12801171
公开号：
ES2602797T3
申请日:
2012.05.29
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A protein kinase inhibitor of Formula I ** Formula ** or a tautomer, a stereoisomer or a mixture of stereoisomers, or a pharmaceutically acceptable salt, solvate or hydrate thereof, wherein: X1 is N or CRt1； X2 is N or CRt2； X3 is N or CRt3； X4 is N or CH； where X1, X2, X3 and X4 are independently selected； Rt1 is selected from -H, halo, -COOH, -CN, -CH2OH, C1-C4 alkyl, -O (C1-C3 alkyl)； Rt2 is selected from -H, halo, -CH3, -CH2CH3.-OH, -OCH3, and -NH2； Rt3 is selected from -H, halo, -S (O) rR4, -CN and C (O) YR4； ring A is aryl or a 5- or 6-membered heteroaryl ring, wherein the heteroaryl forming ring A contains 1-2 heteroatoms selected from N, S and O, and wherein ring A is optionally substituted with 1-4 Ra groups； ring B is a 5- or 6-membered phenyl or heteroaryl ring, wherein ring B heteroaryl contains 1-2 ring heteroatoms selected from N or S and where ring B is optionally substituted with 1-5 Rb groups； Ra and Rb are each independently selected from -H, halo, -CN, -R6, -OR4, -NR4R5, -C (O) YR4, -S (O) rR4, - SO2NR4R5, -NR4SO2NR4R5； alternatively, an Rb substituent on ring B may be ring C, where ring C is a 5- or 6-membered heteroaryl or heterocyclyl ring comprising carbon atoms and 1-3 heteroatoms independently selected from O, N and S (O) r , and wherein ring C is optionally substituted with 1 to Rc substituents； each Rc is independently selected from -H, halo, and -R6； alternatively, one of the Rb substituents may have a -L2-D structure, where D is a ring, L2 is (CH2) z, and z is 1, 2, 3, or 4； or L2 is (OCH2) x, where x is 0, 1, 2 or 3, and wherein ring D is a 5- or 6-membered heteroaryl or heterocyclyl ring comprising carbon atoms and 1-3 heteroatoms independently selected from O , N and S (O) r, and wherein ring D is optionally substituted with 1 to Rd substituents； each Rd is independently selected from -H, halo, R6, -OR4 or -NR4R5； L1 represents an NR3C (O) or C (O) NR3； each Y is independently selected from a chemical bond, -O-, -S-, and -NR5； each R3
