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公开(公告)号：US20170210715A1
公开(公告)日：2017-07-27
申请号：US15329284
申请日：2015-07-24
申请人： Pengcheng Patrick Shao , Feng Ye , Petr Vachal , Jayanth Thiruveliore Thatal , Merck Sharp & Dohme Corp.
IPC分类号： C07D261/04 , A61K31/397 , A61K31/42 , A61K31/444 , A61K31/4245 , A61K31/4439 , C07D413/14 , A61K45/06 , C07D413/10
CPC分类号： C07D261/04 , A61K31/397 , A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D413/10 , C07D413/14 , A61K2300/00
摘要： Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein D1, D2 and D3 are each N, CH, or substituted CH, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
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公开(公告)号：US20130109649A1
公开(公告)日：2013-05-02
申请号：US13660010
申请日：2012-10-25
申请人： Pengcheng Patrick Shao , Wanying Sun , Revathi Reddy Katipally , Petr Vachal , Feng Ye , Jian Liu , Deyou Sha
发明人： Pengcheng Patrick Shao , Wanying Sun , Revathi Reddy Katipally , Petr Vachal , Feng Ye , Jian Liu , Deyou Sha
IPC分类号： A61K31/424 , A61K31/4439 , A61K31/506 , A61K31/454 , A61K31/5355 , A61K31/519 , A61P9/10 , A61P3/06 , A61K31/437 , A61K31/444 , A61K31/455 , A61K31/714 , C07D498/04 , A61K31/4245
CPC分类号： C07D498/04 , A61K31/424 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06
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.
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。
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公开(公告)号：US20150274755A1
公开(公告)日：2015-10-01
申请号：US14431134
申请日：2013-09-20
申请人： Shane W. KRSKA , Petr VACHAL , Christopher J. WELCH , Graham F. SMITH , MERCK SHARP & DOHME CORP.
IPC分类号： C07F5/02 , C07D311/56
CPC分类号： C07C17/10 , C07C17/013 , C07D311/56 , C07F5/025 , C40B40/04 , C40B50/08
摘要： The present invention relates to methods for generating limited chemical diversity for biologically relevant lead molecules by late state functionalization, separation, and post-functionalization modification. The methods optionally include one or more screening steps. Traditional drug development has relied on the synthesis of individual compounds or the generation of large chemical libraries, but these methods have generally been fairly inefficient in obtaining drug products.
摘要翻译： 本发明涉及通过后期官能化，分离和后官能化修饰产生生物相关铅分子的有限化学多样性的方法。 方法可选地包括一个或多个筛选步骤。 传统药物开发依赖于单个化合物的合成或大量化学文库的产生，但这些方法在获得药物产品方面通常相当低效。
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公开(公告)号：US09981970B2
公开(公告)日：2018-05-29
申请号：US14908180
申请日：2014-07-28
IPC分类号： C07D487/04 , A61K45/06 , A61K31/519 , A61K31/714 , A61K31/4439 , C07D513/04 , A61K31/4188
CPC分类号： C07D487/04 , A61K31/4188 , A61K31/4439 , A61K31/519 , A61K31/714 , A61K45/06 , C07D513/04 , A61K2300/00
摘要： Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein X is —C(═O) or —S(O)2—, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
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公开(公告)号：US10011572B2
公开(公告)日：2018-07-03
申请号：US15329284
申请日：2015-07-24
IPC分类号： C07D261/04 , A61K31/397 , A61K31/42 , A61K31/444 , A61K31/4245 , A61K31/4439 , C07D413/14 , A61K45/06 , C07D413/10
CPC分类号： C07D261/04 , A61K31/397 , A61K31/42 , A61K31/4245 , A61K31/4439 , A61K31/444 , A61K45/06 , C07D413/10 , C07D413/14 , A61K2300/00
摘要： Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein D1, D2 and D3 are each N, CH, or substituted CH, are CETP inhibitors and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
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公开(公告)号：US09717714B2
公开(公告)日：2017-08-01
申请号：US14653445
申请日：2013-12-17
发明人： Debra Ondeyka , Xiaoxia Qian , Petr Vachal , Sriram Tyagarajan , Cameron J. Smith , Hong Li , Jianming Bao
IPC分类号： A61K31/4439 , A61K31/423 , A61K31/444 , A61K31/506 , A61K31/5377 , C07D413/14 , C07D413/06 , C07D263/52 , A61K45/06
CPC分类号： A61K31/423 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D263/52 , C07D413/06 , C07D413/14
摘要： Compounds having the structure of Formula (I), including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis. The chemical compounds that are disclosed cholesterol ester transfer protein (CETP) and are expected to have utility in raising HDL-C, lowering LDL-C, and in the treatment and prevention of atherosclerosis.
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公开(公告)号：US09688630B2
公开(公告)日：2017-06-27
申请号：US15028306
申请日：2014-10-06
IPC分类号： C07D491/107 , C07D417/06 , C07D413/10 , C07D405/12 , C07D403/10 , C07D401/04 , C07D401/06 , C07D401/10 , A61K31/5377 , A61K31/4439 , A61K31/454 , A61K31/427 , A61K31/404 , C07D209/12 , A61K45/06 , C07D209/10 , C07D209/24 , C07D209/14 , C07D209/18
CPC分类号： C07D209/12 , A61K31/404 , A61K31/427 , A61K31/4439 , A61K31/454 , A61K31/5377 , A61K45/06 , C07D209/10 , C07D209/14 , C07D209/18 , C07D209/24 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/10 , C07D405/12 , C07D413/10 , C07D417/06 , C07D491/107
摘要： 3,3′-Disubstituted indoline compounds, 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.
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公开(公告)号：US20180065999A1
公开(公告)日：2018-03-08
申请号：US15714786
申请日：2017-09-25
发明人： Petr Vachal , Izzat Raheem , Zhiqiang Guo , Timothy John Hartingh
IPC分类号： C07F9/6561 , A61K31/675 , A61K45/06 , C07F9/16
CPC分类号： C07F9/65616 , A61K31/675 , A61K45/06 , C07F9/16
摘要： Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
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公开(公告)号：US09346825B2
公开(公告)日：2016-05-24
申请号：US14480202
申请日：2014-09-08
发明人： Pengcheng Patrick Shao , Wanying Sun , Revathi Reddy Katipally , Petr Vachal , Feng Ye , Jian Liu , Deyou Sha
IPC分类号： C07D498/04 , A61K31/437 , A61K31/4439 , A61K45/06 , A61K31/424 , A61K31/444 , A61K31/506
CPC分类号： C07D498/04 , A61K31/424 , A61K31/437 , A61K31/4439 , A61K31/444 , A61K31/506 , A61K45/06
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.
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。
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公开(公告)号：US20180230166A1
公开(公告)日：2018-08-16
申请号：US15743424
申请日：2016-07-08
发明人： Pengcheng Patrick Shao , Revathi Reddy Katipally , Petr Vachal , Jayanth Thiruvellore Thatai , Sujit Kumar Sarkar
IPC分类号： C07D513/04 , A61K31/429 , C07D487/04 , A61K31/407 , A61K31/4439 , A61K31/444
CPC分类号： C07D513/04 , A61K31/407 , A61K31/429 , A61K31/4439 , A61K31/444 , A61K31/455 , A61K31/519 , A61K31/714 , A61K45/06 , C07D487/04 , C07D498/04 , A61K2300/00
摘要： The invention provides compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, wherein D1, D2, D3, X, Y, A1, A2, R1, R5 and the subscript a are as described herein. The compounds are CETP inhibitors and are useful for raising FIDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis:
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