Indole, azaindole and related heterocyclic ureido and thioureido piperazine derivatives
    5.
    发明申请
    Indole, azaindole and related heterocyclic ureido and thioureido piperazine derivatives 审中-公开
    吲哚,氮杂吲哚和相关杂环脲基和硫脲基哌嗪衍生物

    公开(公告)号:US20060094717A1

    公开(公告)日:2006-05-04

    申请号:US11304183

    申请日:2005-12-15

    摘要: This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with ureido and thioureido piperazine derivatives of Formula I. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS. The compounds of Formula I are wherein: Y is O or S; Q is selected from the group consisting of m is 2; A is NR13R14; and —W— is

    摘要翻译: 本发明提供具有药物和生物影响性质的化合物,其药物组合物和使用方法。 特别地,本发明涉及式I的脲基和硫脲基哌嗪衍生物。这些化合物具有独特的抗病毒活性,无论是单独使用还是与其它抗病毒剂,抗感染剂,免疫调节剂或HIV进入抑制剂组合使用。 更具体地说,本发明涉及艾滋病毒和艾滋病的治疗。 式I的化合物是其中:Y是O或S; Q选自m为2; A是NR 13 R 14; 和-W-是

    Amino heteroaryl compounds as beta-secretase modulators and methods of use
    9.
    发明授权
    Amino heteroaryl compounds as beta-secretase modulators and methods of use 有权
    氨基杂芳基化合物作为β-分泌酶调节剂和使用方法

    公开(公告)号:US08822485B2

    公开(公告)日:2014-09-02

    申请号:US13511360

    申请日:2010-11-19

    IPC分类号: A61K31/505

    摘要: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I, wherein ring A, B1, B2, B3, L, R1, R4, ring Z, m and p of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease (AD), cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.

    摘要翻译: 本发明包括可用于调节β-分泌酶酶活性和用于治疗β-分泌酶介导的疾病(包括阿尔茨海默病(AD))和相关病症的新一类化合物。 在一个实施方案中,化合物具有通式I,其中式I的环A,B 1,B 2,B 3,L,R 1,R 4,环Z,m和p如本文所定义。 本发明还包括在药物组合物中用于治疗,预防或治疗与β-分泌酶蛋白活性相关的病症和病症的用途。 这些疾病包括例如阿尔茨海默氏病(AD),认知缺陷,认知障碍,精神分裂症和与脑上形成和/或沉积斑块相关和/或引起的其他中枢神经系统病症。 本发明还包括式I的其它实施方案,可用于制备式I化合物的中间体和方法。