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1. 发明授权

US09586968B2 Bicycloamine-substituted-N-benzenesulfonamide compounds with selective activity in voltage-gated sodium channels 有权
标题翻译：在电压门控钠通道中具有选择性活性的双环胺取代的N-苯磺酰胺化合物
公开(公告)号：US09586968B2
公开(公告)日：2017-03-07
申请号：US15038805
申请日：2014-11-24
申请人： Merck Sharp & Dohme Corp. , Dansu Li , Mark E. Layton , Anthony J. Roecker , Melissa Egbertson , Kristen L. G. Jones , Xiu Wang , Xuanjia Peng
发明人： Mark E. Layton , Anthony J. Roecker , Melissa Egbertson , Kristen L. G. Jones , Dansu Li , Xiu Wang , Xuanjia Peng
IPC分类号： C07D487/04 , A61K31/407 , C07D471/04 , A61K31/4353 , C07D491/20 , C07D487/10 , C07D277/52 , C07D213/76 , C07D239/42 , C07D237/20 , C07D285/135
CPC分类号： C07D487/04 , C07D213/76 , C07D237/20 , C07D239/42 , C07D277/52 , C07D285/135 , C07D471/04 , C07D487/10 , C07D491/20
摘要： Disclosed are compounds of Formula A-a, or a salt thereof: Where “B1” and “R1” through “R5” are as defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-a or their salts, and methods of treating neuropathic pain disorders using the same.
摘要翻译：公开了式A-a或其盐的化合物：其中“B1”和“R1”至“R5”如本文所定义，这些化合物具有阻断外周和交感神经元中的Nav 1.7离子通道的性质。还描述了包含式A-a化合物或其盐的药物制剂，以及使用其制备神经性疼痛病症的方法。

2. 发明申请

US20170002008A1 BICYCLOAMINE-SUBSTITUTED-N-BENZENESULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS 有权
标题翻译：具有选择性活性的双环胺取代的N-苯并呋喃胺化合物在电压筛选的钠通道中
公开(公告)号：US20170002008A1
公开(公告)日：2017-01-05
申请号：US15038805
申请日：2014-11-24
申请人： Dansu LI , Mark E. LAYTON , Anthony J. ROECKER , Melissa EGBERTSON , Kristen L. G. JONES , Xiu WANG , Xuanjia PENG , MERCK SHARP & DOHME CORP.
发明人： Mark E. Layton , Anthony J. Roecker , Melissa Egbertson , Kristen L. G. Jones , Dansu Li , Xiu Wang , Xuanjia Peng
IPC分类号： C07D487/04 , C07D487/10 , C07D471/04 , C07D285/135 , C07D213/76 , C07D239/42 , C07D237/20 , C07D491/20 , C07D277/52
CPC分类号： C07D487/04 , C07D213/76 , C07D237/20 , C07D239/42 , C07D277/52 , C07D285/135 , C07D471/04 , C07D487/10 , C07D491/20
摘要： Disclosed are compounds of Formula A-a, or a salt thereof: Where “B1” and “R1” through “R5” are as defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A-a or their salts, and methods of treating neuropathic pain disorders using the same.
摘要翻译：公开了式A-a或其盐的化合物：其中“B1”和“R1”至“R5”如本文所定义，这些化合物具有阻断外周和交感神经元中的Nav 1.7离子通道的性质。还描述了包含式A-a化合物或其盐的药物制剂，以及使用其制备神经性疼痛病症的方法。

3. 发明授权

US09273040B2 Benzoxazolinone compounds with selective activity in voltage-gated sodium channels 有权
标题翻译：在电压门控钠通道中具有选择性活性的苯并恶唑啉酮化合物
公开(公告)号：US09273040B2
公开(公告)日：2016-03-01
申请号：US14353488
申请日：2012-10-26
申请人： Mark E. Layton , Joseph E. Pero , Hannah Fiji , Michael J. Kelly, III , Pablo de Leon , Michael A. Rossi , Kevin F. Gilbert , Anthony J. Roecker , Zhijian Zhao , Swati I P. Mercer , Scott Wolkenberg , James Mulhearn , Lianyun Zhao , Dansu Li
发明人： Mark E. Layton , Joseph E. Pero , Hannah Fiji , Michael J. Kelly, III , Pablo de Leon , Michael A. Rossi , Kevin F. Gilbert , Anthony J. Roecker , Zhijian Zhao , Swati I P. Mercer , Scott Wolkenberg , James Mulhearn , Lianyun Zhao , Dansu Li
IPC分类号： A61K31/00 , C07D417/12 , C07D417/14 , C07D451/02 , C07D471/04 , C07D491/107 , C07D493/10
CPC分类号： C07D417/12 , C07D417/14 , C07D451/02 , C07D471/04 , C07D491/107 , C07D493/10
摘要： Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.
摘要翻译：公开了式（A）的化合物或其盐，其中“Het”，Ra和Rb在本文中定义，其具有用于阻断在外周和交感神经元中发现的Nav 1.7离子通道的性质。还描述了包含式（A）化合物或其盐的药物制剂，以及使用其制备神经性疼痛障碍的方法。

4. 发明授权

US09242995B2 Isoxazolopyridine orexin receptor antagonists 有权
标题翻译：异氮杂吡啶食欲素受体拮抗剂
公开(公告)号：US09242995B2
公开(公告)日：2016-01-26
申请号：US14354392
申请日：2012-10-19
申请人： Dansu Li , Anthony J. Roecker
发明人： Dansu Li , Anthony J. Roecker
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： The present invention is directed to isoxazolopyndine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the isoxazolopyndine compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲肽受体拮抗剂的异恶唑嘌呤类化合物。本发明还涉及本文所述的异恶唑嘌呤类化合物在治疗或预防涉及食欲素受体的神经和精神疾病和疾病中的用途。本发明还涉及包含这些化合物的药物组合物。本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

5. 发明授权

US09624208B2 Benzoxazolinone compounds with selective activity in voltage-gated sodium channels 有权
公开(公告)号：US09624208B2
公开(公告)日：2017-04-18
申请号：US14437315
申请日：2013-10-23
申请人： Merck Sharp & Dohme Corp.
发明人： Joseph E. Pero , Hannah D. G. F. Lehman , Michael J. Kelly, III , Lianyun Zhao , Michael A. Rossi , Dansu Li , Kevin F. Gilbert , Scott Wolkenberg , James Mulhearn , Mark E. Layton , Pablo de Leon
IPC分类号： C07D413/12 , C07D413/14 , C07D263/58 , A61K31/44
CPC分类号： C07D413/14 , A61K31/44 , C07D263/58 , C07D413/12
摘要： Disclosed are compounds of Formula A: Formula A, or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating neuropathic pain disorders using the same.

6. 发明申请

US20150038502A1 ISOXAZOLOPYRIDINE OREXIN RECEPTOR ANTAGONISTS 有权
标题翻译： ISOXAZOLOPYRIDINE OREXIN受体拮抗剂
公开(公告)号：US20150038502A1
公开(公告)日：2015-02-05
申请号：US14354392
申请日：2012-10-19
申请人： MERCK SHARP & DOHME CORP.
发明人： Dansu Li , Anthony J. Roecker
IPC分类号： C07D498/04
CPC分类号： C07D498/04
摘要： The present invention is directed to isoxazolopyndine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the isoxazolopyndine compounds described herein in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
摘要翻译：本发明涉及作为食欲肽受体拮抗剂的异恶唑嘌呤类化合物。本发明还涉及本文所述的异恶唑嘌呤化合物在治疗或预防涉及食欲肽受体的神经和精神疾病和疾病中的用途。本发明还涉及包含这些化合物的药物组合物。本发明还涉及这些药物组合物在预防或治疗涉及食欲素受体的疾病中的用途。

7. 发明申请

US20150252034A1 BENZOXAZOLINONE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS 有权
标题翻译：在电压筛选的通道中具有选择性活性的苯并咪唑啉酮化合物
公开(公告)号：US20150252034A1
公开(公告)日：2015-09-10
申请号：US14437315
申请日：2013-10-23
申请人： Merck Sharp & Dohme Corp.
发明人： Joseph E. Pero , Hannah D.G.F. Lehman , Michael J. Kelly, III , Lianyun Zhao , Michael A. Rossi , Dansu Li , Kevin F. Gilbert , Scott Wolkenberg , James Mulhearn , Mark E. Layton , Pablo de Leon
IPC分类号： C07D413/14 , C07D413/12
CPC分类号： C07D413/14 , A61K31/44 , C07D263/58 , C07D413/12
摘要： Disclosed are compounds of Formula A: Formula A, or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating neuropathic pain disorders using the same.
摘要翻译：公开了式A的化合物：式A或其盐，其中“Het”，Ra和Rb在本文中定义，其具有用于阻断在外周和交感神经元中发现的Nav 1.7离子通道的性质。还描述了包含式A或其盐的化合物的药物制剂，以及使用其制备治疗神经性疼痛障碍的方法。

8. 发明申请

US20140303143A1 BENZOXAZOLINONE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS 有权
标题翻译：在电压筛选的通道中具有选择性活性的苯并咪唑啉酮化合物
公开(公告)号：US20140303143A1
公开(公告)日：2014-10-09
申请号：US14353488
申请日：2012-10-26
申请人： MERCK SHARP & DOHME CORP.
发明人： Mark E. Layton , Joseph E. Pero , Hannah Fiji , Michael J. Kelly, III , Pablo de Leon , Michael A. Rossi , Kevin F. Gilbert , Anthony J. Roecker , Zhijian Zhao , Swati I P. Mercer , Scott Wolkenberg , James Mulhearn , Lianyun Zhao , Dansu Li
IPC分类号： C07D417/12 , C07D491/107 , C07D471/04 , C07D493/10 , C07D417/14 , C07D451/02
CPC分类号： C07D417/12 , C07D417/14 , C07D451/02 , C07D471/04 , C07D491/107 , C07D493/10
摘要： Disclosed are compounds of Formula (A) or a salt thereof, wherein “Het”, Ra, and Rb are defined herein, which have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula (A) or their salts, and methods of treating neuropathic pain disorders using the same.
摘要翻译：公开了式（A）的化合物或其盐，其中“Het”，Ra和Rb在本文中定义，其具有用于阻断在外周和交感神经元中发现的Nav 1.7离子通道的性质。还描述了包含式（A）化合物或其盐的药物制剂，以及使用其制备神经性疼痛障碍的方法。

9. 发明授权

US08569336B2 Compounds for the treatment of inflammatory disorders 失效
标题翻译：用于治疗炎性疾病的化合物
公开(公告)号：US08569336B2
公开(公告)日：2013-10-29
申请号：US13127953
申请日：2009-11-09
申请人： Ling Tong , Brian J. Lavey , Bandarpalle B. Shankar , Seong Heon Kim , Wensheng Yu , Joseph A. Kozlowski , Michael K. C. Wong , Lei Chen , Guowei Zhou , Razia K. Rizvi , Robert Feltz , Aneta Maria Kosinski , De-Yi Yang , Chaoyang Dai , Luke Fire , Vinay Girijavallabhan , Dansu Li , Janeta Popovici-Muller , Judson E. Richard , Kristin E. Rosner , M. Arshad Siddiqui , Liping Yang
发明人： Ling Tong , Brian J. Lavey , Bandarpalle B. Shankar , Seong Heon Kim , Wensheng Yu , Joseph A. Kozlowski , Michael K. C. Wong , Lei Chen , Guowei Zhou , Razia K. Rizvi , Robert Feltz , Aneta Maria Kosinski , De-Yi Yang , Chaoyang Dai , Luke Fire , Vinay Girijavallabhan , Dansu Li , Janeta Popovici-Muller , Judson E. Richard , Kristin E. Rosner , M. Arshad Siddiqui , Liping Yang
IPC分类号： A61K31/4166 , A61K31/4178 , A61K31/4439 , A61K31/454 , A61K31/506 , C07D233/76 , C07D213/24
CPC分类号： C07D498/04 , C07D513/00 , C07D519/00
摘要： This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.
摘要翻译：本发明涉及式（I）的化合物：（化学式应该插在这里，它以纸的形式出现）（I）或其药学上可接受的盐，其可用于治疗疾病或病症介导通过MMP，ADAM，TACE，聚蛋白聚糖蛋白聚糖酶，TNF-或其组合。

10. 发明授权

US07652020B2 Compounds for the treatment of inflammatory disorders 失效
标题翻译：用于治疗炎性疾病的化合物
公开(公告)号：US07652020B2
公开(公告)日：2010-01-26
申请号：US11142601
申请日：2005-06-01
申请人： Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, Jr. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
发明人： Zhuyan Guo , Peter Orth , Zhaoning Zhu , Robert D. Mazzola , Tin-Yau Chan , Henry A. Vaccaro , Brian McKittrick , Joseph A. Kozlowski , Brian J. Lavey , Guowei Zhou , Sunil Paliwal , Shing-Chun Wong , Neng-Yang Shih , Pauline C. Ting , Kristin E. Rosner , Gerald W. Shipps, Jr. , M. Arshad Siddiqui , David B. Belanger , Chaoyang Dai , Dansu Li , Vinay M. Girijavallabhan , Janeta Popovici-Muller , Wensheng Yu , Lianyun Zhao
IPC分类号： A61K31/519 , A61K31/506 , A61K31/4709 , A61K31/43 , A61K31/4245 , C07D413/00 , C07D241/36 , C07D471/00 , C07D295/00 , C07D471/02 , C07D401/00 , C07D513/00 , C07D277/22 , C07D277/62 , C07D263/30 , C07D261/06 , C07D235/00 , C07D209/04 , C07D207/00 , C07D205/00 , C07D409/00 , C07D307/00
CPC分类号： C07D409/14 , C07C235/06 , C07C235/08 , C07C235/10 , C07C2601/08 , C07D207/20 , C07D207/26 , C07D209/44 , C07D215/14 , C07D217/06 , C07D263/32 , C07D295/185 , C07D307/52 , C07D333/20 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D471/10 , C07D487/04 , C07D513/04
摘要： This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, TNF-α or combinations thereof.
摘要翻译：本发明涉及式（I）化合物或其药学上可接受的盐，溶剂合物或异构体，其可用于治疗由MMP，ADAM，TACE，TNF-α或其组合介导的疾病或病症。

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