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    • 20. 发明申请
    • RAF KINASE INHIBITORS
    • RAF激酶抑制剂
    • WO2005002673A1
    • 2005-01-13
    • PCT/GB2004/002877
    • 2004-07-02
    • ASTEX TECHNOLOGY LIMITEDGILL, Adrian, LiamWOODHEAD, Steven, JohnWOODHEAD, Andrew, JamesFREDERICKSON, MartynPADOVA, AlessandroAPAYA, Robert, Patrick
    • GILL, Adrian, LiamWOODHEAD, Steven, JohnWOODHEAD, Andrew, JamesFREDERICKSON, MartynPADOVA, AlessandroAPAYA, Robert, Patrick
    • A61P35/00
    • A61K31/4412A61K31/4965Y02A50/411
    • 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).
    • 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)。