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    Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
    10.
    发明授权
    Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors 失效
    双环杂芳族化合物作为蛋白酪氨酸激酶抑制剂

    公开(公告)号：US06169091A

    公开(公告)日：2001-01-02

    申请号：US09051324

    申请日：1998-08-26

    申请人： George Stuart Cockerill ,  Stephen Barry Guntrip ,  Stephen Carl McKeown ,  Martin John Page ,  Kathryn Jane Smith ,  Sadie Vile ,  Alan Thomas Hudson ,  Paul Barraclough ,  Karl Witold Franzmann

    发明人： George Stuart Cockerill ,  Stephen Barry Guntrip ,  Stephen Carl McKeown ,  Martin John Page ,  Kathryn Jane Smith ,  Sadie Vile ,  Alan Thomas Hudson ,  Paul Barraclough ,  Karl Witold Franzmann

    IPC分类号： C07D48704

    CPC分类号： C07D471/04 ,  C07D495/04

    摘要： Substituted heteroaromatic compounds of formula (A) wherein X is N or CH; in which (a) represents a fused 5, 6 or 7-membered heterocyclic ring and R3 is a group ZR4 wherein Z is joined to R4 through a (CH2)p group in which p is 0, 1, or 2 and Z represents a group V(CH2), V(CF2), (CH2)V, (CF2)V, V(CRR′), V(CHR) or V where R and R′ are each C1-4 alkyl and in which V is a hydrocarbyl group containing 0, 1 or 2 carbon atoms, carbonyl, dicarbonyl, CH(OH), CH(CN), sulphonamide, amide, O, S(O)m or NRb where Rb is hydrogen or Rb is C1-4 alkyl; and R4 is an optionally substituted C3-6 cycloalkyl or an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety; or R3 is a group ZR4 in which Z is NRb, and NRb and R4 together form an optionally substituted 5, 6, 7, 8, 9 or 10-membered carbocyclic or heterocyclic moiety, 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 psoriasis, fibrosis, atherosclerosis, restenosis, auto-immune disease, allergy, asthma, transplantation rejection, inflammation, thrombosis, nervous system diseases, and cancer.

    摘要翻译： 取代的式（A）的杂芳族化合物，其中X是N或CH; 其中（a）表示稠合的5,6或7-元杂环，R3是基团ZR4，其中Z通过其中p为0,1或2的（CH 2）p基团连接到R 4，Z表示 组V（CH 2），V（CF 2），（CH 2）V，（CF 2）V，V（CRR'），V（CHR）或V其中R和R'各自是C 1-4烷基，其中V是 羰基，二羰基，CH（OH），CH（CN），磺酰胺，酰胺，O，S（O）m或NR b，其中R b是氢或R b是C 1-4烷基; 并且R 4是任选取代的C 3-6环烷基或任选取代的5,6,7,8,9或10元碳环或杂环部分; 或R3是Z Z4，其中Z是NRb，NRb和R4一起形成任选取代的5,6,7,8,9或10元碳环或杂环部分是蛋白质酪氨酸激酶抑制剂。 描述了这些化合物，以及其制备方法，包括这些化合物的药物组合物及其在医学中的用途，例如治疗牛皮癣，纤维化，动脉粥样硬化，再狭窄，自身免疫疾病，变态反应，哮喘，移植排斥，炎症 ，血栓形成，神经系统疾病和癌症。