发明名称 Thiazole And Isothiazole Derivatives That Modulate The Activity Of CDK, GSK And Aurora Kinases
摘要 The invention provides a compound of the formula (I): or a salt, N-oxide, tautomer or solvate thereof, wherein X is CR5 or N; each of Q1 and Q2 is a carbon atom; Q3 is selected from S and CH; Q4 is selected from CR2 and S; provided that one of Q3 and Q4 is S and the other of Q3 and Q4 is not S; wherein when Q3 is S, there is a double bond between Q1 and Q4 and a double bond between Q2 and the adjacent ring nitrogen atom N; and when Q4 is S, there is a double bond between Q1 and Q2, and a double bond between Q3 and the adjacent ring nitrogen atom N; A is a bond or -(CH2)m-(B)n-; B is C-O, NR8(C-O) or O(C-O) wherein R1 is hydrogen or C1_4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; m is 0, 1 or 2; n is 0 or 1; Ro is hydrogen or, together with NRg when present, forms a group -(CH2)p- wherein p is 2 to 4; R1 is hydrogen, a carbocyclic or heterocyclic group having from 3 to 12 ring members, or an optionally substituted C1-8 hydrocarbyl group; R2 is hydrogen, halogen, methoxy, or a C1-4 hydrocarbyl group optionally substituted by halogen, hydroxyl or methoxy; R3 and R4 together with the carbon atoms to which they are attached form an optionally substituted fused carbocyclic or heterocyclic ring having from 5 to 7 ring members of which up to 3 can be heteroatoms selected from N, O and S; and R5 is hydrogen, a group R2 or a group R10 wherein R10 is as defined in the claims. The compounds have activity as inhibitors of cyclin dependent kinases, glycogen synthase kinases and Aurora kinases.
申请公布号 US2008312223(A1) 申请公布日期 2008.12.18
申请号 US20050813173 申请日期 2005.12.30
申请人 ASTEX THERAPEUTICS LIMITED 发明人 BERDINI VALERIO;O'BRIEN MICHAEL ALISTAIR;PHILLIPS THERESA RACHEL;WYATT PAUL GRAHAM
分类号 A61K31/5377;A61K31/426;A61P35/00;A61P35/02;C07D277/38;C07D417/14 主分类号 A61K31/5377
代理机构 代理人
主权项
地址