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公开(公告)号:US20100197736A1
公开(公告)日:2010-08-05
申请号:US12502012
申请日:2009-07-13
申请人: Hisashi SHINKAI , Kimiya Maeda , Hiroshi Okamoto
发明人: Hisashi SHINKAI , Kimiya Maeda , Hiroshi Okamoto
IPC分类号: A61K31/445 , C07C237/04 , A61K31/167 , C07D409/12 , A61K31/381 , C07D401/12 , A61K31/444 , C07D211/32 , A61P9/10 , A61P3/06
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。
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公开(公告)号:US20080027109A1
公开(公告)日:2008-01-31
申请号:US11833859
申请日:2007-08-03
申请人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
发明人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
IPC分类号: A61K31/435 , A61K31/164 , A61K31/18 , A61K31/341 , A61P9/00 , C07C233/00 , C07D207/00 , C07D221/00 , C07D333/02 , C07D307/02 , C07D213/00 , C07C311/00 , A61P9/10 , A61K31/44 , A61K31/381 , A61K31/40
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。
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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。
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公开(公告)号:US07579379B2
公开(公告)日:2009-08-25
申请号:US11833859
申请日:2007-08-03
申请人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
发明人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
IPC分类号: A61K31/167 , C07C53/44 , C07C231/02 , C07C237/40 , C07C321/26
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。
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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。
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公开(公告)号:US09000045B2
公开(公告)日:2015-04-07
申请号:US13426246
申请日:2012-03-21
申请人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
发明人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
IPC分类号: A61K31/18 , A61K31/33 , A61P3/06 , A61P9/00 , C07C311/14 , C07C311/15 , C07C311/21 , C07D307/10 , A61K31/164 , A61K31/341 , A61K31/381 , A61K31/40 , A61K31/435 , A61K31/44 , C07C323/40 , C07C323/41 , C07C323/42 , C07C327/30 , C07C329/10 , C07C329/20 , C07C333/04 , C07C333/08 , C07C333/10 , C07D211/34 , C07D213/80 , C07D213/81 , C07D307/68 , C07D333/38
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 invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity. the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.
摘要翻译: 本发明提供了作为CETP活性抑制剂的化合物。 该化合物可以增加HDL,同时通过选择性抑制CETP活性降低LDL。 本发明还提供了该化合物用于预防或治疗动脉粥样硬化或高脂血症的用途。
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公开(公告)号:US20130053417A1
公开(公告)日:2013-02-28
申请号:US13426246
申请日:2012-03-21
申请人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
发明人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
IPC分类号: C07C323/40 , C07C323/42 , C07D307/68 , C07D213/82 , C07C323/49 , C07D211/62 , A61K31/167 , A61K31/381 , C07D333/38 , A61K31/341 , A61K31/444 , A61K31/18 , A61K31/445 , A61P3/06 , A61P9/10 , C07C323/41
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 invention provides a compound that is a CETP activity inhibitor. The compound can increase HDL and at the same time decrease LDL through selective inhibition of CETP activity, the invention also provides for the use of the compound to prevent or treat atherosclerosis or hyperlipidemia.
摘要翻译: 本发明提供了作为CETP活性抑制剂的化合物。 该化合物可以增加HDL,同时通过选择性抑制CETP活性降低LDL,本发明还提供了该化合物用于预防或治疗动脉粥样硬化或高脂血症的用途。
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公开(公告)号:US06426365B1
公开(公告)日:2002-07-30
申请号:US09367299
申请日:1999-12-23
申请人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
发明人: Hisashi Shinkai , Kimiya Maeda , Hiroshi Okamoto
IPC分类号: A61K31165
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。
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公开(公告)号:US20080146620A1
公开(公告)日:2008-06-19
申请号:US11939359
申请日:2007-11-13
申请人: Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
发明人: Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
IPC分类号: A61K31/4406 , C07C211/27 , A61K31/136 , C07D257/06 , A61K31/41 , A61P3/06 , A61P3/04 , A61P3/10 , A61P9/10 , A61K31/4184 , C07D277/38 , A61K31/426 , C07D211/56
CPC分类号: C07D213/74 , C07C229/46 , C07C255/58 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D231/38 , C07D239/42 , C07D249/14 , C07D257/06 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/10 , C07D275/02
摘要: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 allyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7)(R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 allyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.
摘要翻译: 由式(1)表示的二苄胺化合物,其中R 1和R 2各自为任选被卤素取代的C 1-6 - 烯丙基 原子等; R 3,R 4和R 5各自为氢原子,卤素原子等,或R 3, SUP>和R 4可以与其键合的碳原子一起形成任选具有取代基的杂环或杂环; A是-N(R 7)(R 8)等; 环B是芳基或杂环残基; R 6是氢原子,卤素原子,硝基,C 1-6烯丙基等; n为1〜3的整数,其前药及其药学上可接受的盐具有选择性且有效的CETP抑制活性,因此可作为高脂血症或动脉硬化等的治疗剂或预防剂使用。
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公开(公告)号:US20050059810A1
公开(公告)日:2005-03-17
申请号:US10503185
申请日:2003-08-29
申请人: Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
发明人: Kimiya Maeda , Hironobu Nagamori , Hiroshi Nakamura , Hisashi Shinkai , Yasunori Suzuki , Daisuke Takahashi , Toshio Taniguchi
IPC分类号: A61P3/04 , A61P3/06 , A61P9/10 , A61P43/00 , C07C229/46 , C07C255/58 , C07D213/74 , C07D231/38 , C07D239/42 , C07D249/14 , C07D257/06 , C07D261/14 , C07D263/48 , C07D271/06 , C07D271/07 , C07D271/10 , C07D275/02 , C07D277/42 , C07F5/00 , C07C211/30 , C07C255/50
CPC分类号: C07D213/74 , C07C229/46 , C07C255/58 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D231/38 , C07D239/42 , C07D249/14 , C07D257/06 , C07D261/14 , C07D263/48 , C07D271/07 , C07D271/10 , C07D275/02
摘要: A dibenzylamine compound represented by the formula (1) wherein R1 and R2 are each a C1-6 alkyl group optionally substituted by halogen atoms and the like; R3, R4 and R5 are each a hydrogen atom, a halogen atom and the like, or R3 and R4 may form, together with carbon atoms bonded thereto, a homocyclic or heterocyclic ring optionally having substituent(s); A is —N(R7) (R8) and the like; ring B is an aryl group or a heterocyclic residue; R6 is a hydrogen atom, a halogen atom, a nitro group, a C1-6 alkyl group and the like; n is an integer of 1 to 3, a prodrug thereof and a pharmaceutically acceptable salt thereof show selective and potent CETP inhibitory activity, and therefore, they can be provided as therapeutic or prophylactic agents for hyperlipidemia or arteriosclerosis and the like.
摘要翻译: 由式(1)表示的二苄胺化合物,其中R 1和R 2各自为任选被卤素原子等取代的C 1-6烷基; R 3,R 4和R 5各自为氢原子,卤素原子等,或者R 3和R 4可以与其键合的碳原子一起形成稠环或 任选具有取代基的杂环; A是-N(R 7)(R 8)等; 环B是芳基或杂环残基; R 6是氢原子,卤原子,硝基,C 1-6烷基等; n为1〜3的整数,其前药及其药学上可接受的盐具有选择性且有效的CETP抑制活性,因此可作为高脂血症或动脉硬化等的治疗剂或预防剂使用。
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