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公开(公告)号：US08304434B2
公开(公告)日：2012-11-06
申请号：US12678454
申请日：2008-09-30
申请人： Prasun K. Chakravarty , Yanbing Ding , Joseph L. Duffy , Hassan Pajouhesh , Pengcheng Patrick Shao , Sriram Tyagarajan , Feng Ye
发明人： Prasun K. Chakravarty , Yanbing Ding , Joseph L. Duffy , Hassan Pajouhesh , Pengcheng Patrick Shao , Sriram Tyagarajan , Feng Ye
IPC分类号： A61K31/445 , C07D401/12
CPC分类号： C07D211/24 , C07D205/04 , C07D207/08 , C07D211/98 , C07D401/06 , C07D401/08 , C07D401/10 , C07D401/12 , C07D401/14 , C07D413/04 , C07D413/06 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/04 , C07D487/04
摘要： A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
摘要翻译： 一系列由式I表示的取代的芳基砜衍生物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钙通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，糖尿病性神经病，肠易激综合征 综合征，抑郁症，焦虑症，多发性硬化症，睡眠障碍，双相性精神障碍和中风，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。
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公开(公告)号：US20110172223A1
公开(公告)日：2011-07-14
申请号：US13119529
申请日：2009-09-21
IPC分类号： A61K31/5375 , A61P25/08 , A61P25/00 , C07D263/06 , C07D265/32 , C07D413/04 , A61K31/421 , A61K31/4439
CPC分类号： C07D263/20 , C07D265/32
摘要： A series of substituted aryl sulfone derivatives represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, calcium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, diabetic neuropathy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, sleep disorder, bipolar disorder and stroke, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
摘要翻译： 一系列由式I表示的取代的芳基砜衍生物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钙通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，糖尿病性神经病，肠易激综合征 综合征，抑郁症，焦虑症，多发性硬化症，睡眠障碍，双相性精神障碍和中风，包括单独施用有效量的本发明化合物或与一种或多种其它治疗活性化合物组合施用。
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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：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：US20090048227A1
公开(公告)日：2009-02-19
申请号：US12086740
申请日：2006-12-18
IPC分类号： A61K31/397 , C07D401/02 , C07D471/04 , C07D211/58 , A61K31/497 , A61K31/4545 , A61K31/4535 , A61K31/4525 , A61P29/00 , A61K31/453 , A61K31/454 , A61K31/4468 , C07D405/02 , C07D413/02 , C07D409/02
CPC分类号： C07D211/58 , C07D401/06 , C07D401/10 , C07D401/12 , C07D405/06 , C07D405/12 , C07D413/04 , C07D413/06 , C07D413/10 , C07D471/04 , C07D513/04
摘要： Substituted piperidine compounds represented by Formula I, or pharmaceutically acceptable salts thereof. Pharmaceutical compositions comprise an effective amount of the instant compounds, either alone, or in combination with one or more other therapeutically active compounds, and a pharmaceutically acceptable carrier. Methods of treating conditions associated with, or caused by, sodium channel activity, including, for example, acute pain, chronic pain, visceral pain, inflammatory pain, neuropathic pain, urinary incontinence, itchiness, allergic dermatitis, epilepsy, irritable bowel syndrome, depression, anxiety, multiple sclerosis, and bipolar disorder, comprise administering an effective amount of the present compounds, either alone, or in combination with one or more other therapeutically active compounds.
摘要翻译： 由式I表示的取代的哌啶化合物或其药学上可接受的盐。 药物组合物包含单独的或与一种或多种其它治疗活性化合物组合的有效量的本发明化合物和药学上可接受的载体。 治疗与钠通道活性相关或由其引起的疾病的方法，包括例如急性疼痛，慢性疼痛，内脏痛，炎性疼痛，神经性疼痛，尿失禁，瘙痒，过敏性皮炎，癫痫，肠易激综合征，抑郁症 ，焦虑，多发性硬化和双相性精神障碍，包括单独或与一种或多种其它治疗活性化合物组合施用有效量的本发明化合物。
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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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7.发明申请C6-SPIRO IMINOTHIADIAZINE DIOXIDES AS BACE INHIBITORS, COMPOSITIONS, AND THEIR USE 有权C6-SPIRO三嗪二氧化物作为BACE抑制剂，组合物及其使用公开(公告)号：US20160264538A1
公开(公告)日：2016-09-15
申请号：US14653671
申请日：2013-12-16
申请人： Jared N. CUMMING , Jack D. SCOTT , Andrew W. STAMFORD , Ulrich ISERLOH , Santhosh Francis NEELAMKAVIL , Pengcheng Patrick SHAO , Jonathan E. WILSON , MERCK SHARP & DOHME CORP.
发明人： Jared N. Cumming , Jack D. Scott, JR. , Andrew W. Stamford , Ulrich Iserloh , Santhosh Francis Neelamkavil , Pengcheng Patrick Shao , Jonathan E. Wilson
IPC分类号： C07D285/24 , C07D471/04 , C07D417/12 , C07D513/10 , C07D519/00
CPC分类号： C07D285/24 , C07D285/20 , C07D417/12 , C07D471/04 , C07D513/10 , C07D519/00
摘要： In its many embodiments, the present invention provides certain C5-spiro iminothiadiazine dioxide compounds, including compounds Formula (I): (structurally represented) or tautomers thereof, and pharmaceutically acceptable salts of said compounds, wherein R1, R2, R3, X, Y, s, ring A, RA, m, -L1-, and RL are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed:
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