Tetrahydrocarboline antiviral agents
    22.
    发明授权
    Tetrahydrocarboline antiviral agents 有权
    四氢咔啉抗病毒剂

    公开(公告)号:US07449476B2

    公开(公告)日:2008-11-11

    申请号:US11133614

    申请日:2005-05-20

    IPC分类号: C07D471/04 A61K31/437

    CPC分类号: C07D519/00

    摘要: The invention encompasses a series of tetrahydrocarboline compounds of Formula I which inhibit HIV entry by attaching to the exterior viral envelop protein gp120 and interrupting the viral entry process, possibly by interfering with the cellular receptor CD4. This action makes the compounds useful for treating HIV infection and AIDS. The invention also encompasses pharmaceutical compositions and methods for treating those infected with HIV.

    摘要翻译: 本发明包括一系列式I的四氢咔啉化合物,其可能通过干扰细胞受体CD4而阻止HIV外部病毒包膜蛋白gp120并中断病毒进入过程来抑制HIV进入。 这种作用使这些化合物可用于治疗艾滋病毒和艾滋病。 本发明还包括用于治疗感染HIV的那些的药物组合物和方法。

    INDOLE, AZAINDOLE AND RELATED HETEROCYCLIC N-SUBSTITUTED PIPERAZINE DERIVATIVES
    26.
    发明申请
    INDOLE, AZAINDOLE AND RELATED HETEROCYCLIC N-SUBSTITUTED PIPERAZINE DERIVATIVES 有权
    吲哚,氮杂和相关杂环N-取代的哌嗪衍生物

    公开(公告)号:US20080132516A1

    公开(公告)日:2008-06-05

    申请号:US12028189

    申请日:2008-02-08

    摘要: This invention provides compounds of Formula I, including pharmaceutically acceptable salts thereof, having drug and bio-affecting properties, their pharmaceutical compositions and method of use. 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 have the formula wherein: Z is Q is selected from the group consisting of m is 2; A is selected from the group consisting of cinnolinyl, napthyridinyl, quinoxalinyl, pyridinyl, pyrimidinyl, quinolinyl, isoquinolinyl, quinazolinyl, azabenzofuryl, and phthalazinyl each of which may be optionally substituted with one or two groups independently selected from methyl, methoxy, hydroxy, amino and halogen; and —W— is

    摘要翻译: 本发明提供具有药物和生物影响性质的式I化合物,包括其药学上可接受的盐,其药物组合物和使用方法。 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他抗病毒药,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的化合物具有下式:其中:Z为Q选自m为2; A选自噌啉基,萘啶基,喹喔啉基,吡啶基,嘧啶基,喹啉基,异喹啉基,喹唑啉基,氮杂苯并呋喃基和酞嗪基,其各自可以任选被一个或两个独立地选自甲基,甲氧基,羟基,氨基 和卤素; 和-W-是

    Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
    27.
    发明授权
    Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives 有权
    取代的氮杂脱氧乙酸哌嗪衍生物的组成和抗病毒活性

    公开(公告)号:US07354924B2

    公开(公告)日:2008-04-08

    申请号:US10969675

    申请日:2004-10-20

    摘要: This invention provides Compounds I having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. 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. Compound I is wherein: Q is selected from the group consisting of: m is 1 or 2; —W— is A is selected from the group consisting of C1-6alkoxy, aryl and heteroaryl; in which said aryl is phenyl or napthyl; said heteroaryl is selected from the group consisting of pyridinyl, pyrimidinyl, pyrazinyl, triazinyl, furanyl, thienyl, pyrrolyl, imidazolyl, thiazolyl, isothiazolyl, oxazolyl, isoxazolyl, quinolinyl, isoquinolinyl, benzofuranyl, benzothienyl, benzoimidazolyl and benzothiazolyl; and said aryl or heteroaryl is optionally substituted with one or two of the same or different members selected from the group consisting of amino, nitro, cyano, hydroxy, C1-6alkoxy, —C(O)NH2; and C1-6alkyl, —NHC(O)CH3, halogen and trifluoromethyl.

    摘要翻译: 本发明提供具有药物和生物影响性质的化合物I,其药物组合物和使用方法。 特别地,本发明涉及氮杂吲哚乙酰基哌嗪衍生物。 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他抗病毒药,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。 化合物I是其中:Q选自:m是1或2; -W-是A选自C 1-6烷氧基,芳基和杂芳基; 其中所述芳基是苯基或萘基; 吡啶基,吡嗪基,咪唑基,噻唑基,异噻唑基,恶唑基,异恶唑基,喹啉基,异喹啉基,苯并呋喃基,苯并噻吩基,苯并咪唑基和苯并噻唑基; 并且所述芳基或杂芳基任选被一个或两个相同或不同的选自氨基,硝基,氰基,羟基,C 1-6烷氧基,-C(O) NH 2; 和C 1-6烷基,-NHC(O)CH 3,卤素和三氟甲基。

    Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives
    30.
    发明授权
    Indole, azaindole and related heterocyclic sulfonylureido piperazine derivatives 有权
    吲哚,氮杂吲哚和相关的杂环磺酰脲基哌嗪衍生物

    公开(公告)号:US06900206B2

    公开(公告)日:2005-05-31

    申请号:US10457620

    申请日:2003-06-09

    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 sulfonylureido 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. wherein: Z is Q is selected from the group consisting of: —W— is — represents a carbon-carbon bond or does not exist; and A is NR13R14.

    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的磺酰脲基哌嗪衍生物。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。 其中:Z为Q选自:-W-表示碳 - 碳键或不存在; A是NR 13 R 14。