发明名称 Thiazole and oxazole kinase inhibitors
摘要 The present invention is concerned with substituted azole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant proteine kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, allergic, and degenerative disorders. In particular, several of these compounds are potent and selective Flt-3 inhibitors or/and syk inhibitors.
申请公布号 US8962665(B2) 申请公布日期 2015.02.24
申请号 US201113521676 申请日期 2011.01.12
申请人 AB Science 发明人 Moussy Alain;Benjahad Abdellah;Martin Jason;Chevenier Emmanuel;Pez Didier;Sandrinelli Franck;Picoul Willy
分类号 A61K31/42;C07D413/00;C07D413/14;C07D413/12;C07D417/14 主分类号 A61K31/42
代理机构 Hamre, Schumann, Mueller & Larson, P.C. 代理人 Hamre, Schumann, Mueller & Larson, P.C.
主权项 1. A compound of formula I: wherein substituents A, Q, X, R1, R2, R3, V and W in Formula I are defined as follows: A is one of the following: i) N(R4)(CH2)n where n is 0<n<3 ii) O(CH2)n where n is 0<n<3 iii) S(CH2)n where n is 0<n<3 iv) (CH2)n where n is 0≦n<4 v) C(O)(CH2)n where n is 0<n<3 vi) C(R4)=C(R5) vii) C≡C R4 and R5 each independently are hydrogen, C1-4alkyl, C2-6alkenyl, C2-6alkynyl, C3-7cycloalkyl, C1-4haloalkyl, C1-4 alkoxy, C1-4hydroxyalkyl, C1-4 alkylamino; X is CH or N; V is O; Q is selected from: i) an alkyl1 group, or ii) an aryl1 group, or iii) an heteroaryl1 group; an alkyl1 group is defined as a linear, branched or cycloalkyl group containing from 1 to 10 carbon atoms and optionally substituted with one or more hetereoatoms selected from halogen, oxygen, and nitrogen; trifluoromethyl, carboxyl, cyano, nitro, formyl; CO—R, COO—R, CONR—R′, SO2-R, and SO2NR—R′ wherein R and R′ are a linear or branched alkyl group containing 1 to 10 carbon atoms and optionally substituted with at least one heteroatom selected from a halogen, oxygen, and nitrogen; and a cycloalkyl group; an aryl1 group is defined as phenyl or a substituted variant thereof bearing any combination, at any one ring position, of one or more substituents selected from halogen;an alkyl1 group;an aryl or heteroaryl group;trifluoromethyl, O-alkyl, carboxyl, cyano, nitro, formyl, hydroxy, NH-alkyl, N(alkyl)(alkyl), and amino group;NRCO—R′ or NRCOO—R′ or NRCONR′—R″ or NRSO2-R′ or NRSO2NR′—R″ or CO—R or COO—R or CONR—R′ or SO2-R or or SO2NRR′ wherein R, R′ and R″ each independently are selected from hydrogen, alkyl, aryl or heteroaryl group; an heteroaryl1 group is defined as a pyridyl, pyrimidinyl, pyrazinyl, pyridazinyl, thienyl, thiazolyl, imidazolyl, pyrazolyl, pyrrolyl, furanyl, oxazolyl, isoxazolyl, triazolyl, tetrazolyl, indolyl, benzimidazole, benzoxazole, benzothiazole, quinolinyl group, which may additionally bear any combination, at any one ring position, of one or more substituents selected from halogen;an alkyl1 group;an aryl or heteroaryl group,trifluoromethyl, O-alkyl, carboxyl, cyano, nitro, formyl, hydroxy, NH-alkyl, N(alkyl)(alkyl), and amino group;NRCO—R′ or NRCOO—R′ or NRCONR′—R″ or NRSO2-R′ or NRSO2NR′—R″ or CO—R or COO—R or CONR—R′ or SO2-R or SO2NRR′ wherein R, R′ and R″ each independently are selected from hydrogen, alkyl, aryl or heteroaryl group; R1, R2 and R3 each independently are selected from hydrogen, halogen, a linear or branched alkyl group containing from 1 to 10 carbon atoms and optionally substituted with one or more hetereoatoms selected from halogen, oxygen, and nitrogen; trifluoromethyl, C1-6alkyloxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, carboxyl, cyano, nitro, formyl, hydroxy, and CO—R, COO—R, CONR—R′, SO2-R, and SO2NR—R′ wherein R and R′ corresponds to hydrogen, alkyl, aryl or heteroaryl group; W is aryl1 or heteroaryl1.
地址 Paris FR