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1. 发明申请

WO2005002673A1 RAF KINASE INHIBITORS 审中-公开
标题翻译： RAF激酶抑制剂
公开(公告)号：WO2005002673A1
公开(公告)日：2005-01-13
申请号：PCT/GB2004/002877
申请日：2004-07-02
申请人： ASTEX TECHNOLOGY LIMITED , GILL, Adrian, Liam , WOODHEAD, Steven, John , WOODHEAD, Andrew, James , FREDERICKSON, Martyn , PADOVA, Alessandro , APAYA, Robert, Patrick
发明人： GILL, Adrian, Liam , WOODHEAD, Steven, John , WOODHEAD, Andrew, James , FREDERICKSON, Martyn , PADOVA, Alessandro , APAYA, Robert, Patrick
IPC分类号： A61P35/00
CPC分类号： A61K31/4412 , A61K31/4965 , Y02A50/411
摘要： The use of a compound of the formula I or a pharmaceutically acceptable salt or solvate thereof, for the manufacture of a medicament for use in the treatment of a condition ameliorated by the inhibition of raf kinase, wherein: -X=Y- is selected from -CR 2 =CR 3 - and -CR 2 =N-; R 1 is selected from H, halo, NRR', NHC (=O)R, NHC (=O)NRR', NH 2 SO 2 R, and C (=O)NRR', where R and R' are independently selected from H and C 1-4 alkyl, and are optionally substituted by OH, NH 2 , SO 2 -NH 2 , C 5-20 carboaryl, C 5-20 heteroaryl and C 3-20 heterocyclyl, or may together form, with the nitrogen atom to which they are attached, an optionally substituted nitrogen containing C 5-7 heterocyclyl group; R 2 and R 3 (where present) are independently selected from H, optionally substituted C 1-7 alkyl, optionally substituted C 5-20 aryl, optionally substituted C 3-20 heterocyclyl, halo, amino, amido, hydroxy, ether, thio, thioether, acylamido, ureido and sulfonamino; R 4 an optionally substituted C 5-20 carboaryl or C 5-20 heteroaryl group; and R 5 is selected from R 5 ', halo, NHR 5' , C(=O)NHR 5' , OR 5 ', SR 5' , NHC (=O)R 5' , NHC (=O)NHR 5' , NHS (=O) 2 R 5' , wherein R 5' is H or C 1-3 alkyl (optionally substituted by halo, NH 2 , OH, SH).
摘要翻译：使用式I化合物或其药学上可接受的盐或溶剂合物，用于制备用于治疗通过抑制raf激酶改善的病症的药物，其中：-X = Y-选自 -CR 2 = CR 3 - 和-CR 2 = N-; R 1选自H，卤素，NRR'，NHC（= O）R，NHC（= O）NRR'，NH2SO2R和C（= O）NRR'，其中R和R'独立地选自H 和C 1-4烷基，并且任选地被OH，NH 2，SO 2 -NH 2，C 5-20碳酰基，C 5-20杂芳基和C 3-20杂环基取代，或者可以与它们所连接的氮原子一起形成一个任选取代的含有C 5-7杂环基的氮; R 2和R 3（如果存在）独立地选自H，任选取代的C 1-7烷基，任选取代的C 5-20芳基，任选取代的C 3-20杂环基，卤素，氨基，酰胺基，羟基，醚，硫代，硫醚，酰氨基，脲基和磺氨基; R 4是任选取代的C 5-20碳芳基或C 5-20杂芳基; R 5选自R 5，卤素，NHR 5，C（= O）NHR 5，OR 5，SR 5，NHC（= O） R 5，NHC（= O）NHR 5，NHS（= O）2 R 5，其中R 5'是H或C 1-3烷基（任选地被卤素，NH 2，OH ，SH）。

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