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    • 7. 发明申请
    • FUSED HETEROCYCLIC COMPOUNDS AS PROTEIN TYROSINE KINASE INHIBITORS
    • 熔化的杂环化合物作为蛋白酪氨酸激酶抑制剂
    • WO1998002434A1
    • 1998-01-22
    • PCT/EP1997003672
    • 1997-07-11
    • GLAXO GROUP LIMITEDCOCKERILL, George, StuartCARTER, Malcolm, CliveGUNTRIP, Stephen, BarrySMITH, Kathryn, Jane
    • GLAXO GROUP LIMITED
    • C07D405/04
    • C07D401/04C07D403/04C07D403/14C07D405/04C07D405/14C07D409/04C07D413/04C07D413/14
    • Substituted heteroaromatic compounds of formula (I) and in particular substituted quinolines and quinazolines, are protein tyrosine kinase inhibitors. The compounds are described as are methods for their preparation, pharmaceutical compositions including such compounds and their use in medicine, for example in the treatment of cancer and psoriasis, or a salt or solvate thereof; wherein X is N or CH; Y is a group W(CH2), (CH2)W, or W, in which W is O, S(O)m wherein m is 0, 1 or 2, or NR wherein R is hydrogen or a C1-8 alkyl group; R represents a phenyl group or a 5- or 6-membered heterocyclic ring containing 1 to 4 heteroatoms selected from N, O or S(O)m, wherein m is as defined above, with the provisos that the ring does not contain two adjacent O or S(O)m atoms and that where the ring contains only N as heteroatom(s) the ring is C-linked to the quinazoline or quinoline ring, R being optionally substituted by one or more R groups; P = 0 to 3; U, R , R are as defined in the application.
    • 取代的式(I)的杂芳族化合物,特别是取代的喹啉和喹唑啉是蛋白质酪氨酸激酶抑制剂。 这些化合物被描述为它们的制备方法,包括这些化合物的药物组合物及其在药物中的用途,例如治疗癌症和牛皮癣,或其盐或溶剂合物; 其中X是N或CH; Y是基团W(CH 2),(CH 2)W或W,其中W是O,S(O)m,其中m是0,1或2,或NR a,其中R a是氢或 C 1-8烷基; R 1表示苯基或含有1至4个选自N,O或S(O)m的杂原子的5或6元杂环,其中m如上所定义,条件是该环不是 含有两个相邻的O或S(O)m原子,并且当环仅含有N作为杂原子时,该环与喹唑啉或喹啉环C-连接,R 1任选地被一个或多个R' 3>组 P = 0〜3; U,R 2,R 3如本申请中所定义。