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PYRIDAZINE DERIVATIVES USEFUL IN THERAPY
专利权人:
INHIBITAXIN LIMITED
发明人:
Karl Richard Gibson,Dafydd Rhys Owen
申请号:
US14353434
公开号:
US20140275100A1
申请日:
2012.10.26
申请国别(地区):
US
年份:
2014
代理人:
摘要:
The invention provides compounds of formula I, (I) wherein: R represents a cyclic group selected from phenyl, heteroaryl, heterocyclyl and C 3-6 cycloalkyl; 10 wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C -6 alkyl optionally substituted with 1-3 halogen atoms, phenyl, C -6 alkoxy optionally substituted with 1-3 halogen atoms, cyano, heteroaryl 1a and heterocyclyl 1a; and wherein each cyclic group is optionally fused to a benzene ring or a 5- or 16-membered heteroaromatic or heterocyclic ring each containing from 1 to 3 heteroatoms (selected from N, O and S); and when the group is substituted the substitution may occur anywhere on the optionally fused ring system as a whole; and wherein heterocyclyl and heterocyclyl 1a may additionally be substituted with ═O; 20 X represents a bond or C -6 alkylene (which may be straight or branched); R 2 represents H or C -6 alkyl; R 3 represents H or C -6 alkyl; Y represents a bond or C -6 alkylene (which may be straight or branched, and optionally substituted with OH or CF 3); 2 R 4 represents a cyclic group selected from phenyl, heteroaryl 4, heterocyclyl 4 and C 3-6 cycloalkyl; wherein each cyclic group is optionally substituted with from 1 to 3 substituents selected from halo, C -6 alkyl optionally substituted with 1-3 halogen atoms, TET01063WO 4 phenyl, C -6 alkyl substituted with phenyl, C -6 alkoxy optionally substituted with -3 halogen atoms, cyano, heteroaryl 4a and heterocyclyl 4a; and wherein each cyclic group is optionally fused to benzene ring or a 5- or 6-membered heteroaromatic or heterocyclic ring each containing from 1 to 3 heteroatoms (selected from N, O and S); and when the group is substituted the substitution may occur anywhere on the optionally fused ring system as a whole; and wherein heterocyclyl 4 and heterocyclyl 4a may additionally be substituted with ═O; heteroaryl, heteroaryl 1a, heteroaryl 4 and heteroaryl 4a independently represent a 5- or 6-m
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