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    Quinolizinone compound and use thereof as HIV integrase inhibitor
    3.
    发明授权
    Quinolizinone compound and use thereof as HIV integrase inhibitor 有权
    喹诺酮酮化合物及其作为HIV整合酶抑制剂的用途

    公开(公告)号：US07745459B2

    公开(公告)日：2010-06-29

    申请号：US11230330

    申请日：2005-09-20

    申请人： Motohide Satoh ,  Hisateru Aramaki ,  Hiroshi Nakamura ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Kazunobu Yamataka

    发明人： Motohide Satoh ,  Hisateru Aramaki ,  Hiroshi Nakamura ,  Masafumi Inoue ,  Hiroshi Kawakami ,  Hisashi Shinkai ,  Yuji Matsuzaki ,  Kazunobu Yamataka

    IPC分类号： A01N43/90 ,  A61K31/44 ,  C07D455/02

    CPC分类号： C07D471/04 ,  A61K31/4745 ,  A61K31/519 ,  C07D455/02

    摘要： A pharmaceutical agent having an anti-HIV action, particularly, a pharmaceutical agent having an integrase inhibitory action, is provided.The present invention relates to a quinolizinone compound represented by the following formula [I] wherein each symbol is as defined in the specification, a pharmaceutically acceptable salt thereof, and an anti-HIV agent containing same as an active ingredient. The compound of the present invention has an HIV integrase inhibitory action and is useful as an anti-HIV agent for the prophylaxis or therapy of AIDS. Moreover, by a combined use with other anti-HIV agents such as protease inhibitors, reverse transcriptase inhibitors and the like, the compounds can become a more effective anti-HIV agent. Since the compound has a high inhibitory activity specific for integrases, the compound can provide a safe pharmaceutical agent for human with a fewer side effects.

    摘要翻译： 提供具有抗HIV作用的药剂，特别是具有整合酶抑制作用的药剂。 本发明涉及由下式[I]表示的喹嗪酮化合物，其中各符号如说明书中所定义，其药学上可接受的盐和含有作为活性成分的抗HIV剂。 本发明的化合物具有HIV整合酶抑制作用，可用作预防或治疗AIDS的抗HIV剂。 此外，通过与其它抗HIV剂如蛋白酶抑制剂，逆转录酶抑制剂等的组合使用，化合物可以成为更有效的抗HIV剂。 由于化合物对整合酶具有高的抑制活性，所以化合物可以为人体提供安全的药剂，副作用较少。

    CETP activity inhibitor
    7.
    发明授权
    CETP activity inhibitor 有权
    CETP活性抑制剂

    公开(公告)号：US06753346B2

    公开(公告)日：2004-06-22

    申请号：US10151813

    申请日：2002-05-22

    申请人： Hisashi Shinkai ,  Kimiya Maeda ,  Hiroshi Okamoto

    发明人： Hisashi Shinkai ,  Kimiya Maeda ,  Hiroshi Okamoto

    IPC分类号： A61K31255

    CPC分类号： C07D307/10 ,  A61K31/164 ,  A61K31/18 ,  A61K31/33 ,  A61K31/341 ,  A61K31/381 ,  A61K31/40 ,  A61K31/435 ,  A61K31/44 ,  C07C311/14 ,  C07C311/15 ,  C07C311/21 ,  C07C323/40 ,  C07C323/41 ,  C07C323/42 ,  C07C327/30 ,  C07C329/10 ,  C07C329/20 ,  C07C333/04 ,  C07C333/08 ,  C07C333/10 ,  C07C2601/02 ,  C07C2601/04 ,  C07C2601/08 ,  C07C2601/14 ,  C07C2601/18 ,  C07C2602/08 ,  C07C2602/22 ,  C07C2602/28 ,  C07C2603/74 ,  C07D211/34 ,  C07D213/80 ,  C07D213/81 ,  C07D307/68 ,  C07D333/38 ,  Y02P20/55

    摘要： The present invention provides a CETP activity inhibitor comprising as an active ingredient a compound represented by the formula (I): wherein R represents a straight chain or branched alkyl group; a straight chain or branched alkenyl group; a lower haloalkyl group; a substituted or unsubstituted cycloalkyl group; a substituted or unsubstituted cycloalkenyl group; a substituted or unsubstituted cycloalkylalkyl group; a substituted or unsubstituted aryl group, or a substituted or unsubstituted heterocyclic group, X1, X2, X3, and X4 may be the same or different and each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower haloalkyl group; a lower alkoxy group; a cyano group; a nitro group; an acyl group; or an aryl group, Y represents —CO— or —SO2—, and Z represents a hydrogen atom or a mercapto-protecting group, or a prodrug compound, a pharmaceutically acceptable salt, or hydrate or solvate thereof. The compounds represented by the formula (I) can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity and, therefore, is expected to be useful as a new type of a preventive or therapeutic agent for atherosclerosis or hyperlipidemia.

    摘要翻译： 本发明提供一种CETP活性抑制剂，其包含由式（I）表示的化合物作为活性成分：其中R表示直链或支链烷基; 直链或支链烯基; 低级卤代烷基; 取代或未取代的环烷基; 取代或未取代的环烯基; 取代或未取代的环烷基烷基; 取代或未取代的芳基或取代或未取代的杂环基，X 1，X 2，X 3和X 4可以相同或不同，各自表示氢原子，卤素原子，低级烷基，低级卤代烷基。 低级烷氧基; 氰基; 硝基; 酰基; 或芳基，Y表示-CO-或-SO 2 - ，Z表示氢原子或巯基保护基，或前药化合物，其药学上可接受的盐或水合物或溶剂化物。 由式（I）表示的化合物可以增加HDL，同时通过选择性抑制CETP活性降低LDL，因此预期可用作动脉粥样硬化或高脂血症的新型预防或治疗剂。