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Pyrrolo [2,3-d] pyrimidine derivatives as inhibitors of tropomyosin-related kinases
专利权人:
Pfizer Limited
发明人:
ANDREWS, Mark David,BAGAL, Sharanjeet Kaur,GIBSON, Karl Richard,OMOTO, Kiyoyuki,RYCKMANS, Thomas,SKERRATT, Sarah Elizabeth,STUPPLE, Paul Anthony
申请号:
ES12713362
公开号:
ES2581848T3
申请日:
2012.03.22
申请国别(地区):
ES
年份:
2016
代理人:
摘要:
A compound of Formula I: ** Formula ** or a pharmaceutically acceptable salt thereof, wherein R1 is H, or C1-5 alkyl optionally substituted with up to 3 substituents independently selected from OH, CON (R5Re), SO2R7, SR7 , OR7, CH2OH, CO2R5, SONR7R7, NR7SO2R5, CN, NO2 and R8, or a ring system selected from C3-5 cycloalkyl, propelanyl, or a 4-6 membered saturated heterocyclyl ring, a ring system having up to 3 ring heteroatoms selected from N, O and S, and whose ring system is optionally substituted with up to 3 substituents independently selected from methyl, OH, CON (R5Re), SO2R7, OR7, CH2OH, CO2R5, SONR7R7, NR7SO2R5, CN, NO2 and R8; R2 is H or methyl; R3 is H, NH2 or NH (C1-3 alkyl optionally substituted with up to 3 substituents independently selected from OH and O (C1-3 alkyl)); R101 is H, OH, methyl, cyclopropyl, methoxy, ethyl, ethoxy or CN, X is a bond, O, (CH-R4) n, NR104, OCH2 or CH2O; R4 is independently H, CH3, CH2OH, CH2OCH3, OH, NH2, NHCH3, N (CH3) 2, CH2NH2, CH2NHCH3, or CH2N (CH3) 2; R104 is H, C1-3 alkyl or a C4-6 saturated carbocycle, each of which is optionally substituted with up to 3 substituents independently selected from C1-3 alkyl, CH2OH and NH2; n is 1 or 2; R102 is a ring system that is a 3-7 membered monocyclic carbocyclic or heterocyclic system, or an 8-14 member bicyclic system, a ring system that can be saturated or partially or totally unsaturated, in which the ring system heterocyclic may have up to 5 ring heteroatoms selected from N, S and O, in which the bicyclic ring system may be 2 rings (carbocyclic-carbocyclic, carbocyclic-heterocyclic, heterocyclic-carbocyclic or heterocyclic-heterocyclic) fused or linked by a single bond, ring system that is optionally substituted with up to 3 substituents independently selected from, where possible -halo, CN, NR5R6, SO2R7, SR7, C1-4 alkyl optionally substituted with up to 3 OH groups and / or C1-3 alkoxy , C3-6 cycloalkyl optionally substituted with up to 3 OH groups and / or C1-3 alkoxy, C1-
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