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Pyrazolo [1,5-a] pyrimidine compounds substituted as inhibitors of TRK kinase
专利权人:
INC.;ARRAY BIOPHARMA;ARRAY BIOPHARMA INC
发明人:
HAAS, JULIA,ANDREWS, STEVEN W.,JIANG, YUTONG,ZHANG, GAN,HAAS JULIA,ANDREWS STEVEN W,JIANG YUTONG,ZHANG GAN
申请号:
ES09740245
公开号:
ES2456346T3
申请日:
2009.10.21
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
Compound having the general formula I: ** Formula ** or a pharmaceutically acceptable salt thereof, wherein: R1 is H or alkyl (1-6C); R2 is NRbRc, alkyl (1-4C), fluoroalkyl (1-4C), CF3, hydroxyalkyl (1-4C), -alkyl (1-4C) hetAr1, -alkyl (1-4C) NH2, -alkyl (1- 4C) NH-alkyl (1-4C), -alkyl (1-4C) N-alkyl (1-4C) 2, hetAr2, hetCic1, hetCic2, phenyl which is optionally substituted by NHSO2alkyl (1-4C), or cycloalkyl ( 3-6C) which is optionally substituted by (1-4C) alkyl, CN, OH, OMe, NH2, NHMe, N (CH3) 2, F, CF3, CO2-alkyl (C1-4), CO2H, C (>; = O) NReRf or C (>; = O) ORg; Rb is H or alkyl (1-6C); Rc is H, alkyl (1-4C), hydroxyalkyl (1-4C), hetAr3, or phenyl, wherein said phenyl is optionally substituted by one or more substituents independently selected from halogen, CN, CF3 and -O-alkyl (1-4C), or NRbRc forms a 4-link heterocyclic ring having a nitrogen atom in the ring, wherein said heterocyclic ring is optionally substituted by one or more substituents independently selected from halogen, OH, alkyl (1 -4C), alkoxy (1-4C), -OC (>; = O) -alkyl (1-4C), NH2, - NHC (>; = O) Oalkyl (1-4C) and hydroxyalkyl (1-4C), or NRbRc forms a 5-6 link heterocyclic ring that has a ring heteroatom that is nitrogen and optionally has a second ring heteroatom or a group selected from N, O and SO2, in which the heterocyclic ring is optionally substituted by one or more substituents independently selected from OH, halogen, CF3, alkyl (1-4C), CO2-alkyl l (1-4C), CO2H, NH2, NHC (>; = O) O-30 alkyl (1-4C) and oxo, or NRbRc forms a 7-8 bridge link heterocyclic ring that has a nitrogen atom in the ring and optionally presenting a second heteroatom in the ring selected from N and O, wherein said ring is optionally substituted by CO2-alkyl (1-4C); hetAr1 is a 5-link heteroaryl ring that has 1-3 nitrogen atoms in the ring; hetAr2 is a 5-6 link heteroaryl ring that has at least one nitrogen atom in the ring and optionally has a second heteroatom in the ring independently selected from N and S
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