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公开(公告)号：US20090075979A1
公开(公告)日：2009-03-19
申请号：US12087184
申请日：2006-12-29
申请人： Amjad Ali , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Cameron J. Smith , Adrian A. Dowst , Yi-Heng Chen
发明人： Amjad Ali , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Cameron J. Smith , Adrian A. Dowst , Yi-Heng Chen
IPC分类号： A61K31/55 , C07D263/22 , A61K31/421 , C07D401/02 , A61K31/454 , A61K31/4439 , A61P9/10 , C07D413/02 , A61K31/5377 , C07D417/02 , A61K31/541 , A61K31/496
CPC分类号： C07D263/20 , C07D413/06 , C07D413/10 , C07D413/12
摘要： Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R2 is also a cyclic group.
摘要翻译： 具有式（I）结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于提高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式（I）的化合物中，B或R 2是具有进一步取代的邻位或氨基甲基取代基的苯基，B或R2中的另一个也是环状基团。
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公开(公告)号：US09221834B2
公开(公告)日：2015-12-29
申请号：US13881896
申请日：2011-10-25
申请人： Zhijian Lu , Yi-Heng Chen , Cameron Smith , Hong Li , Christopher F. Thompson , Julianne Hunt , Florida Kallashi , Ramzi Sweis , Peter Sinclair , Samantha E. Adamson , Guizhen Dong , Debra L. Ondeyka , Xiaoxia Qian , Wanying Sun , Petr Vachal , Kake Zhao
发明人： Zhijian Lu , Yi-Heng Chen , Cameron Smith , Hong Li , Christopher F. Thompson , Julianne Hunt , Florida Kallashi , Ramzi Sweis , Peter Sinclair , Samantha E. Adamson , Guizhen Dong , Debra L. Ondeyka , Xiaoxia Qian , Wanying Sun , Petr Vachal , Kake Zhao
IPC分类号： A61K31/4439 , A61K31/506 , A61K31/5377 , A61K31/4545 , A61K31/497 , A61K31/444 , C07D491/08 , C07D417/14 , C07D413/14 , A61K31/42 , A61K45/06 , C07D413/06
CPC分类号： C07D491/08 , A61K31/42 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/06 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, A3 is a substituted phenyl group or indanyl group. Formula (I).
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式I的化合物中，A3是取代的苯基或茚满基。 式（I）。
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公开(公告)号：US08735435B2
公开(公告)日：2014-05-27
申请号：US12625783
申请日：2009-11-25
申请人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Hallett , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith
发明人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Hallett , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith
IPC分类号： C07D263/04 , A61K31/421
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接到环上或连接到环上的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH2-。
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公开(公告)号：US20130331372A1
公开(公告)日：2013-12-12
申请号：US13881896
申请日：2011-10-25
申请人： Zhijian Lu , Yi-Heng Chen , Cameron Smith , Hong Li , Christopher F. Thompson , Julianne Hunt , Florida Kallashi , Ramzi Sweis , Peter Sinclair , Samantha E. Adamson , Guizhen Dong , Debra L. Ondeyka , Xiaoxia Qian , Wanying Sun , Petr Vachal , Kake Zhao
发明人： Zhijian Lu , Yi-Heng Chen , Cameron Smith , Hong Li , Christopher F. Thompson , Julianne Hunt , Florida Kallashi , Ramzi Sweis , Peter Sinclair , Samantha E. Adamson , Guizhen Dong , Debra L. Ondeyka , Xiaoxia Qian , Wanying Sun , Petr Vachal , Kake Zhao
IPC分类号： C07D491/08 , A61K31/5377 , A61K31/4545 , A61K31/444 , A61K31/497 , C07D417/14 , C07D413/14 , A61K45/06 , A61K31/4439 , A61K31/506
CPC分类号： C07D491/08 , A61K31/42 , A61K31/4439 , A61K31/444 , A61K31/4545 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/06 , C07D413/14 , C07D417/14 , A61K2300/00
摘要： Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compound of Formula I, A3 is a substituted phenyl group or indanyl group. Formula (I).
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式I的化合物中，A3是取代的苯基或茚满基。 式（I）。
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公开(公告)号：US08334290B2
公开(公告)日：2012-12-18
申请号：US12083324
申请日：2006-10-30
申请人： Amjad Ali , Julianne A. Hunt , Florida Kallashi , Jennifer Kowalchick , Dooseop Kim , Cameron J. Smith , Peter J. Sinclair , Ramzi F. Sweis , Gayle E. Taylor , Christopher F. Thompson , Liya Chen , Nazia Quraishi
发明人： Amjad Ali , Julianne A. Hunt , Florida Kallashi , Jennifer Kowalchick , Dooseop Kim , Cameron J. Smith , Peter J. Sinclair , Ramzi F. Sweis , Gayle E. Taylor , Christopher F. Thompson , Liya Chen , Nazia Quraishi
IPC分类号： A61K31/496 , A61K31/497 , A61K31/443 , A61K31/421 , C07D239/42 , C07D413/14 , C07D211/32 , C07D213/26 , C07D263/57
CPC分类号： C07D263/57 , C07D235/18 , C07D239/74 , C07D277/64 , C07D277/66 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D495/10 , C07D498/04
摘要： Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
摘要翻译： 式I化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及治疗或预防动脉粥样硬化。
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公开(公告)号：US07652049B2
公开(公告)日：2010-01-26
申请号：US11173295
申请日：2005-07-01
申请人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
发明人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
IPC分类号： C07D263/20 , A61K31/4015
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接到环上或连接到环上的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH2-。
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公开(公告)号：US20090264405A1
公开(公告)日：2009-10-22
申请号：US12083324
申请日：2006-10-30
申请人： Amjad Ali , Julianne A. Hunt , Florida Kallashi , Jennifer Kowalchick , Dooseop Kim , Cameron J. Smith , Peter J. Sinclair , Ramzi F. Sweis , Gayle E. Taylor , Christopher F. Thompson , Liya Chen , Nazia Quraishi
发明人： Amjad Ali , Julianne A. Hunt , Florida Kallashi , Jennifer Kowalchick , Dooseop Kim , Cameron J. Smith , Peter J. Sinclair , Ramzi F. Sweis , Gayle E. Taylor , Christopher F. Thompson , Liya Chen , Nazia Quraishi
IPC分类号： A61K31/428 , C07D263/56 , C07D413/12 , C07D498/04 , C07D239/74 , C07D277/64 , C07D413/14 , C07D487/04 , C07D471/10 , A61K31/423 , A61K31/454 , A61K31/4439 , A61K31/437 , A61K31/496 , A61K31/5377 , A61K31/506 , A61K31/4709 , A61K31/55 , A61K31/4985
CPC分类号： C07D263/57 , C07D235/18 , C07D239/74 , C07D277/64 , C07D277/66 , C07D413/04 , C07D413/10 , C07D413/12 , C07D413/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D495/10 , C07D498/04
摘要： Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
摘要翻译： 式I化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及治疗或预防动脉粥样硬化。
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公开(公告)号：US20080119476A1
公开(公告)日：2008-05-22
申请号：US11631821
申请日：2005-07-01
申请人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
发明人： Amjad Ali , Joann M. Napolitano , Qiaolin Deng , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Nazia Quraishi , Cameron J. Smith , Julianne A. Hunt , Adrian A. Dowst , Yi-Heng Chen , Hong Li
IPC分类号： A61K31/422 , A61K31/40 , A61K31/4166 , A61K31/427 , A61K31/4439 , A61K31/501 , A61P9/10 , C07D233/32 , C07D263/20 , C07D417/10 , C07D417/04 , C07D413/10 , C07D413/04 , C07D401/04 , C07D285/10 , C07D233/44 , C07D207/24 , A61K31/506 , A61K31/497 , A61K31/433 , A61K31/4168 , A61K31/421
CPC分类号： C07F7/10 , A61K31/4015 , A61K31/4166 , A61K31/4168 , A61K31/421 , A61K31/422 , A61K31/427 , A61K31/433 , A61K31/4439 , A61K31/497 , A61K31/501 , A61K31/506 , A61K45/06 , C07D207/26 , C07D207/27 , C07D233/32 , C07D233/38 , C07D233/50 , C07D233/52 , C07D263/04 , C07D263/20 , C07D263/22 , C07D263/24 , C07D263/26 , C07D285/06 , C07D285/10 , C07D401/04 , C07D413/04 , C07D413/06 , C07D413/10 , C07D417/04 , C07D417/10
摘要： Compounds having the structures of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis: In the compounds of Formula I, B or R2 is a phenyl group which has an ortho aryl, heterocyclic, benzoheterocyclic or benzocycloalkyl substituent, and one other position on the 5-membered ring has an aromatic, heterocyclic, cycloalkyl, benzoheterocyclic or benzocycloalkyl substituent connected directly to the ring or attached to the ring through a —CH2—.
摘要翻译： 具有式I结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于升高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。在式I化合物中，B或 R 2是具有邻芳基，杂环，苯并杂环或苯并环烷基取代基的苯基，并且在5元环上的另一个位置具有直接连接的芳族，杂环，环烷基，苯并杂环或苯并环烷基取代基 通过-CH 2 - 2连接到环上或连接到环上。
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公开(公告)号：US07910592B2
公开(公告)日：2011-03-22
申请号：US12087185
申请日：2006-12-29
申请人： Amjad Ali , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li , Christopher F. Thompson
发明人： Amjad Ali , Zhijian Lu , Peter J. Sinclair , Yi-Heng Chen , Cameron J. Smith , Hong Li , Christopher F. Thompson
IPC分类号： A61K31/497 , A61K31/427 , A61K31/422 , A61K31/506 , C07D239/02 , C07D241/02 , C07D401/02 , C07D277/02 , C07D263/02
CPC分类号： C07D413/06 , C07D263/24
摘要： Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B is a cyclic group other than phenyl, and B has a cyclic substituent at a position that is ortho to the position at which B is connected to the remainder of the structure of Formula (I). The 5-membered ring of Formula (I) has a second cyclic substituent in addition to B.
摘要翻译： 具有式（I）结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于培养HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式（I）的化合物中，B是苯基以外的环状基团，B在与B与式（I）的结构的其余部分连接的位置的邻位的位置具有环状取代基。 式（I）的5元环除了B之外还具有第二个环状取代基。
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公开(公告)号：US07781426B2
公开(公告)日：2010-08-24
申请号：US12087184
申请日：2006-12-29
申请人： Amjad Ali , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Cameron J. Smith , Adrian A. Dowst , Yi-Heng Chen
发明人： Amjad Ali , Zhijian Lu , Peter J. Sinclair , Gayle E. Taylor , Christopher F. Thompson , Cameron J. Smith , Adrian A. Dowst , Yi-Heng Chen
IPC分类号： A61K31/422 , A61K31/5377 , A61K31/541 , A61K31/496 , A61K31/443 , A61K31/4525 , A61K31/55 , C07D403/02 , C07D413/02 , C07D417/02 , C07D401/02
CPC分类号： C07D263/20 , C07D413/06 , C07D413/10 , C07D413/12
摘要： Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. In the compounds of Formula (I), B or R2 is a phenyl group which has an ortho amine or aminomethyl substituent which is further substituted, and the other of B or R2 is also a cyclic group.
摘要翻译： 具有式（I）结构的化合物，包括化合物的药学上可接受的盐，是CETP抑制剂，可用于提高HDL-胆固醇，降低LDL-胆固醇，以及用于治疗或预防动脉粥样硬化。 在式（I）的化合物中，B或R 2是具有进一步取代的邻位或氨基甲基取代基的苯基，B或R2中的另一个也是环状基团。
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