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    Pyrimidin-4-yl-3, 4-thione compounds and their use in therapy
    8.
    发明授权
    Pyrimidin-4-yl-3, 4-thione compounds and their use in therapy 有权
    嘧啶-4-基-3,4-硫酮化合物及其在治疗中的应用

    公开(公告)号：US07902361B2

    公开(公告)日：2011-03-08

    申请号：US11408463

    申请日：2006-04-21

    申请人： Shudong Wang ,  Gavin Wood ,  Kenneth Duncan ,  Christopher Meades ,  Darren Gibson ,  Janice McLachlan ,  Alex Perry ,  David Blake ,  Daniella I. Zheleva ,  Peter Martin Fischer

    发明人： Shudong Wang ,  Gavin Wood ,  Kenneth Duncan ,  Christopher Meades ,  Darren Gibson ,  Janice McLachlan ,  Alex Perry ,  David Blake ,  Daniella I. Zheleva ,  Peter Martin Fischer

    IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D417/04 ,  C07D417/14 ,  A61K31/506 ,  A61P3/10 ,  A61P19/02 ,  A61P35/02

    CPC分类号： C07D417/04 ,  C07D417/14

    摘要： The present invention relates to compounds of formula I, or pharmaceutically acceptable salts thereof, wherein R1 and R5 are each independently H, C(ORj′) or a hydrocarbyl group optionally substituted by one or more R6 groups; R2, R3, and R4 are each independently H, alkyl or alkenyl, each of which may be optionally substituted with one or more R7 groups; R6 and R7 are each independently halogen, NO2, CN, (CH2)mORa, O(CH2)nORb, (CH2)pNRcRd, CF3, COORe, CONRfRg, CORh, SO3H, SO2Ri, SO2NRjRk, (CH2)qNRa′CORg′, Rf′, (CH2)rNRb′SO2Rh′, SO2NRd′Ri′, SO2NRe′(CH2)sORc′, heterocycloalkyl or heteroaryl, wherein said heterocycloalkyl and heteroaryl may be optionally substituted by one or more substituents selected from aralkyl, sulfonyl, Rm and CORn; Rg′, Rh′, Ri′ and Rj′ are each independently selected from alkyl, aryl, aralkyl and heteroaryl, each of which may be optionally substituted with one or more substituents selected from halogen, OH, NO2, NH2 CF3 and COOH; m, p, q and r are each independently 0, 1, 2 or 3; n and s are each independently 1, 2, or 3; and Ra-n and Ra′-f′ are each independently H or alkyl. Further aspects of the invention relate to pharmaceutical compositions comprising such compounds, and their use in the preparation of a medicament for treating one or more of the following: a proliferative disorder, a viral disorder, a CNS disorder, a stroke, alopecia and diabetes.

    摘要翻译： 本发明涉及式I化合物或其药学上可接受的盐，其中R 1和R 5各自独立地为H，C（OR j'）或任选被一个或多个R 6基团取代的烃基; R 2，R 3和R 4各自独立地为H，烷基或烯基，其各自可以任选被一个或多个R 7基团取代; R6和R7各自独立地为卤素，NO2，CN，（CH2）mORa，O（CH2）nORb，（CH2）pNRcRd，CF3，COORe，CONRfRg，CORh，SO3H，SO2Ri，SO2NRjRk，（CH2）qNRa'CORg' Rf'，（CH2）rNRb'SO2Rh'，SO2NRd'Ri'，SO2NRe'（CH2）sORc'，杂环烷基或杂芳基，其中所述杂环烷基和杂芳基可以任选地被一个或多个选自芳烷基，磺酰基，R m和 玉米; R''，R''，R''和R“'各自独立地选自烷基，芳基，芳烷基和杂芳基，它们各自可以被一个或多个选自卤素，OH，NO 2，NH 2 CF 3和COOH的取代基取代; m，p，q和r各自独立地为0,1,2或3; n和s各自独立地为1,2或3; 和Ra-n和Ra'-f'各自独立地为H或烷基。 本发明的其它方面涉及包含这些化合物的药物组合物及其在制备用于治疗以下一种或多种的药物中的用途：增殖性病症，病毒病症，CNS病症，中风，脱发和糖尿病。