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公开(公告)号：US20130040978A1
公开(公告)日：2013-02-14
申请号：US13641767
申请日：2011-05-13
申请人： Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Paul E. Finke , Yi Zang , Michael A. Plotkin , F. Anthony Romero , Remond Moningka , Zahid Hussain
发明人： Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Paul E. Finke , Yi Zang , Michael A. Plotkin , F. Anthony Romero , Remond Moningka , Zahid Hussain
IPC分类号： C07D498/10 , C07D519/00 , A61P25/22 , A61P3/04 , A61P3/00 , A61P25/24 , A61K31/438 , A61P3/10
CPC分类号： C07D498/10 , C07D519/00
摘要： Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
摘要翻译： 结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍 ，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。
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公开(公告)号：US20090069284A1
公开(公告)日：2009-03-12
申请号：US12288518
申请日：2008-10-21
IPC分类号： A61K31/397 , C07D205/04 , C07D401/06 , A61K31/4427 , A61K31/4178 , A61K31/4196 , C07D205/06 , C07D403/06
CPC分类号： C07D205/04 , C07D205/06 , C07D401/06 , C07D403/06 , C07D403/10 , C07D405/06 , C07D409/06
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
摘要翻译： 结构式（I）的新型化合物是大麻素-1（CB1）受体的拮抗剂和/或反向激动剂，可用于治疗，预防和抑制由CB1受体介导的疾病。 本发明的化合物可用作治疗精神病，记忆缺陷，认知障碍，偏头痛，神经病，包括多发性硬化和神经 - 巴利综合征的神经炎症性疾病以及病毒性脑炎的炎症性后遗症，脑血管 事故和头部创伤，焦虑症，压力，癫痫，帕金森病，运动障碍和精神分裂症。 这些化合物还可用于治疗药物滥用障碍，治疗肥胖或进食障碍，以及治疗哮喘，便秘，慢性肠假性梗阻和肝硬化。
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23.发明授权(Halo-benzo carbonyl)heterocyclo fused phenyl p38 kinase inhibiting agents 失效（卤 - 苯并羰基）杂环稠合苯基p38激酶抑制剂公开(公告)号：US06809199B2
公开(公告)日：2004-10-26
申请号：US10023231
申请日：2001-12-17
申请人： James B. Doherty , John E. Stelmach , Meng-Hsin Chen , Luping Liu , Julianne A. Hunt , Rowena D. Ruzck , Joung L. Goulet , David D. Wisnoski , Swaminathan Ravi Natarajan , Kathleen M. Rupprecht , Jianming Bao , Shouwu Miao , Xingfang Hong , Peter J. Sinclair , Florida Kallashi
发明人： James B. Doherty , John E. Stelmach , Meng-Hsin Chen , Luping Liu , Julianne A. Hunt , Rowena D. Ruzck , Joung L. Goulet , David D. Wisnoski , Swaminathan Ravi Natarajan , Kathleen M. Rupprecht , Jianming Bao , Shouwu Miao , Xingfang Hong , Peter J. Sinclair , Florida Kallashi
IPC分类号： C07D23972
CPC分类号： C07D215/227 , C07D221/06 , C07D231/12 , C07D233/56 , C07D239/80 , C07D249/08 , C07D401/04 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/12 , C07D403/14 , C07D405/04 , C07D409/14 , C07D417/12 , C07D451/02 , C07D471/04 , C07D487/08
摘要： Compounds described by the chemical formula (I) or a pharmaceutically acceptable salt thereof: are inhibitors of p38 useful in the treatment of inflammatory diseases such as arthritis.
摘要翻译： 由化学式（I）表示的化合物或其药学上可接受的盐是可用于治疗炎性疾病如关节炎的p38的抑制剂。
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公开(公告)号：US06303637B1
公开(公告)日：2001-10-16
申请号：US09422500
申请日：1999-10-21
申请人： Jianming Bao , Andrew Kotliar , Frank Kayser , William H. Parsons , Kathleen M. Rupprecht , Christopher F. Claiborne , David A. Claremon , Nigel Liverton , Wayne J. Thompson
发明人： Jianming Bao , Andrew Kotliar , Frank Kayser , William H. Parsons , Kathleen M. Rupprecht , Christopher F. Claiborne , David A. Claremon , Nigel Liverton , Wayne J. Thompson
IPC分类号： A61K31445
CPC分类号： C07D211/96 , A61K31/445 , A61K31/47 , A61K31/52 , A61K31/535 , A61K31/70 , A61K38/13 , A61K45/06 , C07D211/26 , A61K31/365 , A61K31/16 , A61K2300/00
摘要： The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.
摘要翻译： 本发明涉及可用作治疗自身免疫性疾病，心律失常等的钾通道抑制剂的一类式I的杂环化合物。
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公开(公告)号：US06194458B1
公开(公告)日：2001-02-27
申请号：US09422499
申请日：1999-10-21
申请人： Robert K. Baker , Jianming Bao , Frank Kayser , Andrew Kotliar , William H. Parsons , Kathleen M. Rupprecht , Christopher F. Claiborne , David A. Claremon , Nigel Liverton , Wayne J. Thompson
发明人： Robert K. Baker , Jianming Bao , Frank Kayser , Andrew Kotliar , William H. Parsons , Kathleen M. Rupprecht , Christopher F. Claiborne , David A. Claremon , Nigel Liverton , Wayne J. Thompson
IPC分类号： A61K3122
CPC分类号： C07D307/79 , A61K45/06 , C07C235/60 , C07C271/20
摘要： This invention relates to benzamide potassium channel inhibitors of general structural Formula I. The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and related afflictions, diseases and illnesses, and cardiac arrhythmias. Also within the scope of this invention are pharmaceutical formulations comprising a compound of Formula I and a pharmaceutical carrier, as well as pharmaceutical formulations comprising a compound of Formula I, one or more immunosuppressive compounds and a pharmaceutical carrier.
摘要翻译： 本发明涉及一般结构式I的苯甲酰胺钾通道抑制剂。本发明的化合物可用于治疗自身免疫性疾病，预防外来器官移植排斥和相关疾病，疾病和疾病以及心律失常。 也包括本发明范围的药物制剂，其包含式I化合物和药物载体，以及包含式I化合物，一种或多种免疫抑制化合物和药物载体的药物制剂。
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公开(公告)号：US5763478A
公开(公告)日：1998-06-09
申请号：US733040
申请日：1996-10-16
IPC分类号： C07D313/06 , C07D493/04 , A61K31/365 , C07D493/02
CPC分类号： C07D493/04 , C07D313/06
摘要： The compounds of Formula I ##STR1## are useful as immunosuppressive agents.
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27.发明授权公开(公告)号：US11149036B2
公开(公告)日：2021-10-19
申请号：US16621959
申请日：2018-06-22
申请人： John J. Acton, III , Merck Sharp & Dohme Corp. , MSD R&D (China) Co., Ltd. , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
发明人： John J. Acton, III , Jianming Bao , Qiaolin Deng , Melissa Egbertson , Ronald Ferguson, II , Xiaolei Gao , Scott Timothy Harrison , Sandra L. Knowles , Chunsing Li , Michael Man-Chu Lo , Robert D. Mazzola, Jr. , Zhaoyang Meng , Meng Na , Michael T. Rudd , Oleg Selyutin , David M. Tellers , Ling Tong , Fengqi Zhang
IPC分类号： C07D471/04 , C07D401/04 , C07D401/14 , C07D405/14 , C07D413/14 , C07D491/048 , C07D498/04
摘要： The present invention is directed to pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
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公开(公告)号：US08742110B2
公开(公告)日：2014-06-03
申请号：US13810946
申请日：2011-08-12
申请人： Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Aaron Zwicker , Edward C. Sherer , Michael A. Plotkin , Remond Moningka , Zahid Hussain , Harold B. Wood , Feroze Ujjainwalla , F. Anthony Romero , Paul E. Finke , Yi Zang , Weiguo Liu
发明人： Joseph L. Duffy , Jianming Bao , Debra L. Ondeyka , Sriram Tyagarajan , Patrick Shao , Feng Ye , Revathi Katipally , Aaron Zwicker , Edward C. Sherer , Michael A. Plotkin , Remond Moningka , Zahid Hussain , Harold B. Wood , Feroze Ujjainwalla , F. Anthony Romero , Paul E. Finke , Yi Zang , Weiguo Liu
IPC分类号： C07D215/00 , C07D229/00 , A61K31/44 , A61K31/397
CPC分类号： C07D498/10 , C07D519/00
摘要： Substituted spirocyclic amines of structural formula (I) are selective antagonists of the somatostatin subtype receptor 5 (SSTR5) and are useful for the treatment, control or prevention of disorders responsive to antagonism of SSTR5, such as Type 2 diabetes, insulin resistance, lipid disorders, obesity, atherosclerosis, Metabolic Syndrome, depression, and anxiety.
摘要翻译： 结构式（I）的取代的螺环胺是生长抑素亚型受体5（SSTR5）的选择性拮抗剂，可用于治疗，控制或预防对SSTR5的拮抗作用有响应的病症，例如2型糖尿病，胰岛素抵抗，脂质障碍 ，肥胖症，动脉粥样硬化，代谢综合征，抑郁症和焦虑症。
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29.发明申请公开(公告)号：US20110263533A1
公开(公告)日：2011-10-27
申请号：US13124898
申请日：2009-10-12
申请人： Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka , Brett C. Bookser
发明人： Qun Dang , Tony S. Gibson , Hongjian Jiang , De Michael Chung , Jianming Bao , Jinlong Jiang , Andy Kassick , Ahmet Kekec , Ping Lan , Huagang Lu , Gergely M. Makara , F. Anthony Romero , Iyassu Sebhat , David Wilson , Dariusz Wodka , Brett C. Bookser
IPC分类号： A61K31/675 , C07F9/40 , C07F9/6574 , A61P35/00 , A61P3/04 , A61P3/06 , A61P9/12 , C07F9/6506 , A61P3/10
CPC分类号： C07F9/65068 , C07F9/65583 , C07F9/657181
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and are useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention are useful in the treatment of Type 2 diabetes, hyperglycemia, Metabolic Syndrome, obesity, hypercholesterolemia, and hypertension.
摘要翻译： 结构式（I）的新型化合物是AMP-蛋白激酶的活化剂，可用于治疗，预防和抑制AMPK活化蛋白激酶介导的疾病。 本发明的化合物可用于治疗2型糖尿病，高血糖症，代谢综合征，肥胖，高胆固醇血症和高血压。
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公开(公告)号：US07485732B2
公开(公告)日：2009-02-03
申请号：US10557246
申请日：2004-06-09
IPC分类号： C07D205/04
CPC分类号： C07D205/04 , C07D205/06 , C07D401/06 , C07D403/06 , C07D403/10 , C07D405/06 , C07D409/06
摘要： Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.
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