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    Bicyclic heteroaromatic compounds as protein tyrosine kinase inhibitors
    1.
    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。

    USE OF MTKI 1 FOR TREATING OR PREVENTING BRAIN CANCER
    2.
    发明申请
    USE OF MTKI 1 FOR TREATING OR PREVENTING BRAIN CANCER 审中-公开
    使用MTKI 1治疗或预防脑癌

    公开(公告)号：US20080153853A1

    公开(公告)日：2008-06-26

    申请号：US11875350

    申请日：2007-10-19

    申请人： Eddy Jean Edgard FREYNE ,  Michel Marie Francois Janicot ,  Martin John Page ,  Timothy Pietro Suren Perera

    发明人： Eddy Jean Edgard FREYNE ,  Michel Marie Francois Janicot ,  Martin John Page ,  Timothy Pietro Suren Perera

    IPC分类号： A61K31/519 ,  A61P35/00

    CPC分类号： A61K31/519 ,  A61K31/4188 ,  A61K2300/00

    摘要： The present invention is concerned with the finding that some the macrocyclic quinazoline derivative 4,6-ethanediylidenepyrimido[4,5-b][6,1,12]benzoxadiazacyclo-pentadecine, 17-bromo-8,9,10,11,12,13,14,19-octahydro-20-methoxy-13-methyl-, described as compound 22 in PCT publication W02004/105765, is useful in the manufacture of a medicament for the treatment or prevention of a primary brain cancer or brain metastasis. It accordingly provides methods for treating, preventing, delaying or mitigating brain cancer, or for preventing or slowing proliferation of cells of brain origin.

    摘要翻译： 本发明涉及一些大环喹唑啉衍生物4,6-乙二亚甲基嘧啶并[4,5-b] [6,1,12]苯并二氮杂环十五碳烯，17-溴-8,9,10,11,12 在PCT公开WO2004 / 105765中描述为化合物22的13,14,19-八氢-20-甲氧基-13-甲基，可用于制备用于治疗或预防原发性脑癌或脑转移的药物 。 因此，它提供了治疗，预防，延迟或减轻脑癌或预防或减缓脑源性细胞增殖的方法。