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    CETP activity inhibitors
    14.
    发明授权
    CETP activity inhibitors 有权
    CETP活性抑制剂

    公开(公告)号：US07271196B2

    公开(公告)日：2007-09-18

    申请号：US10825531

    申请日：2004-04-15

    申请人： Hisashi Shinkai ,  Kimiya Maeda ,  Hiroshi Okamoto

    发明人： Hisashi Shinkai ,  Kimiya Maeda ,  Hiroshi Okamoto

    IPC分类号： A61K31/167 ,  C07C327/22

    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 3， 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，药学上可接受的盐或水合物或溶剂合物 其中。 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。

    Isoxazolidinedione derivatives and use thereof
    15.
    发明授权
    Isoxazolidinedione derivatives and use thereof 失效

    公开(公告)号：US6037359A

    公开(公告)日：2000-03-14

    申请号：US291203

    申请日：1999-04-14

    申请人： Hisashi Shinkai

    发明人： Hisashi Shinkai

    IPC分类号： A61K31/42 ,  C07D263/32 ,  C07D413/12 ,  C07D413/14

    CPC分类号： C07D413/12 ,  C07D413/14

    摘要： Novel isoxazolidinedione derivatives of the formula (I) ##STR1## wherein R is an optionally substituted aromatic hydrocarbon, an optionally substituted alicyclic hydrocarbon, an optionally substituted heterocyclic group, an optionally substituted condensed heterocyclic group or a group of the formula ##STR2## R.sub.4 is a hydrogen atom, a lower alkyl or a hydroxy; R.sub.5 is a lower alkyl optionally substituted by hydroxy; and P and Q are each a hydrogen atom or P and Q together form a bond, and pharmaceutically acceptable salts thereof. Said novel isoxazolidinedione derivatives and pharmaceutically acceptable salts thereof have superior hypoglycemic and hypolipidemic actions and are useful for the treatment of diabetes and the complications thereof, as well as therapeutic agents for related diseases such as hyperlipidemia.