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公开(公告)号：US20230227441A1
公开(公告)日：2023-07-20
申请号：US18009306
申请日：2021-06-14
申请人： Ashok ARASAPPAN , Ian M. BELL , Christopher James BUNGARD , Christopher S. BURGEY , Jason M. COX , Deodial Guy GUIADEEN , Michael J. KELLY , Mark E. LAYTON , Hong LIU , Jian LIU , James T. OLSEN , James J. PERKINS , Jeffrey W. SCHUBERT , Akshay A. SHAH , Michael D. VANHEYST , Zhe WU , Shawn J. STACHEL , MERCK SHARP & DOHME CORP.
发明人： Ashok Arasappan , Ian M. Bell , Christopher James Bungard , Christopher S. Burgey , Jason Michael Cox , Deodial Guy Guiadeen, III , Michael J. Kelly, III , Mark E. Layton , Hong Liu , Jian Liu , James T. Olsen , James J. Perkins , Jeffrey W. Schubert , Akshay A. Shah , Shawn J. Stachel , Michael David VanHeyst , Zhe Wu
IPC分类号： C07D413/12 , C07D263/24 , C07D417/12
CPC分类号： C07D413/12 , C07D263/24 , C07D417/12
摘要： Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
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2.发明申请5'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES 有权5'-取代的核苷衍生物及其用于治疗病毒性疾病的方法公开(公告)号：US20140235567A1
公开(公告)日：2014-08-21
申请号：US14232540
申请日：2012-07-10
申请人： Vishal A. Verma , Ashok Arasappan , F. George Njoroge , Vinay Girijavallabhan , Stephane L. Bogen , Qun Dang , David B. Olsen
发明人： Vishal A. Verma , Ashok Arasappan , F. George Njoroge , Vinay Girijavallabhan , Stephane L. Bogen , Qun Dang , David B. Olsen
IPC分类号： C07H19/14 , A61K45/06 , A61K31/7056 , A61K31/7064
CPC分类号： C07H19/14 , A61K31/7056 , A61K31/7064 , A61K45/06
摘要： The present invention relates to 5′-Substituted Nucleoside Derivatives of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein B, X, Y, Z, R1, R2, R3 and R3′ are as defined herein. The present invention also relates to compositions comprising at least one 5′-Substituted Nucleoside Derivative, and methods of using the 5′-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
摘要翻译： 本发明涉及式（I）的5'-取代的核苷衍生物：（I）及其药学上可接受的盐，其中B，X，Y，Z，R 1，R 2，R 3和R 3'如本文所定义。 本发明还涉及包含至少一种5'-取代的核苷衍生物的组合物，以及使用5'-取代的核苷衍生物治疗或预防患者HCV感染的方法。
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公开(公告)号：US07592316B2
公开(公告)日：2009-09-22
申请号：US11714457
申请日：2007-03-06
申请人： F. George Njoroge , Ashok Arasappan , Srikanth Venkatraman , Stephane L. Bogen , Kevin X. Chen , Frank Bennett
发明人： F. George Njoroge , Ashok Arasappan , Srikanth Venkatraman , Stephane L. Bogen , Kevin X. Chen , Frank Bennett
IPC分类号： A61K38/06
CPC分类号： C07K5/0804 , A61K38/00 , C07K5/0202 , C07K5/0812 , C07K5/0827 , C07K7/02
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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公开(公告)号：US20070142301A1
公开(公告)日：2007-06-21
申请号：US11645181
申请日：2006-12-21
申请人： Stephane Bogen , Weidong Pan , Sumei Ruan , Kevin Chen , Ashok Arasappan , Srikanth Venkatraman , Latha Nair , Mousumi Sannigrahi , Frank Bennett , Anil Saksena , F. Njoroge , Viyyoor Girijavallabhan
发明人： Stephane Bogen , Weidong Pan , Sumei Ruan , Kevin Chen , Ashok Arasappan , Srikanth Venkatraman , Latha Nair , Mousumi Sannigrahi , Frank Bennett , Anil Saksena , F. Njoroge , Viyyoor Girijavallabhan
CPC分类号： C07D209/52 , A61K38/00 , C07D209/02 , C07D401/12 , C07D403/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12 , C07K5/0205 , C07K5/0808 , C07K5/0812 , C07K5/0827
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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5.发明申请公开(公告)号：US20070032433A1
公开(公告)日：2007-02-08
申请号：US10052386
申请日：2002-01-18
申请人： Anil Saksena , Viyyoor Girijavallabhan , Raymond Lovey , Edwin Jao , Frank Bennett , Jinping Mc Cormick , Haiyan Wang , Russell Pike , Stephane Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. Njoroge , Ashok Arasappan , Tejal Parekh , Ashit Ganguly , Kevin Chen , Srikanth Venkatraman , Henry Vaccaro , Patrick Pinto , Bama Santhanam , Scott Kemp , Odile Levy , Marguerita Lim-wilby , Susan Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang , Jesse Wong , Latha Nair
发明人： Anil Saksena , Viyyoor Girijavallabhan , Raymond Lovey , Edwin Jao , Frank Bennett , Jinping Mc Cormick , Haiyan Wang , Russell Pike , Stephane Bogen , Tin-Yau Chan , Yi-Tsung Liu , Zhaoning Zhu , F. Njoroge , Ashok Arasappan , Tejal Parekh , Ashit Ganguly , Kevin Chen , Srikanth Venkatraman , Henry Vaccaro , Patrick Pinto , Bama Santhanam , Scott Kemp , Odile Levy , Marguerita Lim-wilby , Susan Tamura , Wanli Wu , Siska Hendrata , Yuhua Huang , Jesse Wong , Latha Nair
CPC分类号： C07K5/0804 , A61K38/00 , C07K5/0202 , C07K5/0812 , C07K5/0827 , C07K7/02
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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6.发明申请3,4-(cyclopentyl)-fused proline compounds as inhibitors of hepatitis C virus NS3 serine protease 失效3,4-（环戊基） - 脯氨酸化合物作为丙型肝炎病毒NS3丝氨酸蛋白酶的抑制剂公开(公告)号：US20050197301A1
公开(公告)日：2005-09-08
申请号：US11064757
申请日：2005-02-24
申请人： F. Njoroge , Srikanth Venkatraman , Ashok Arasappan , Francisco Velazquez , Viyyoor Girijavallabhan
发明人： F. Njoroge , Srikanth Venkatraman , Ashok Arasappan , Francisco Velazquez , Viyyoor Girijavallabhan
IPC分类号： A61K38/04 , C07D209/52 , C07K5/02 , C07K5/04 , C07K5/08
CPC分类号： C07K5/0202
摘要： The present invention discloses novel compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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7.发明申请公开(公告)号：US20050176648A1
公开(公告)日：2005-08-11
申请号：US11089192
申请日：2005-03-24
申请人： Anil Saksena , Viyyoor Girijavallabhan , Stephane Bogen , Raymond Lovey , Edwin Jao , Frank Bennett , Jinping McCormick , Haiyan Wang , Russell Pike , Yi-Tsung Liu , Tin-Yau Chan , Zhaoning Zhu , Ashok Arasappan , Kevin Chen , Srikanth Venkatraman , Tejal Parekh , Patrick Pinto , Bama Santhanam , F. Njoroge , Ashit Ganguly , Henry Vaccaro , Scott Kemp , Odile Levy , Marguerita Lim-Wilby , Susan Tamura
发明人： Anil Saksena , Viyyoor Girijavallabhan , Stephane Bogen , Raymond Lovey , Edwin Jao , Frank Bennett , Jinping McCormick , Haiyan Wang , Russell Pike , Yi-Tsung Liu , Tin-Yau Chan , Zhaoning Zhu , Ashok Arasappan , Kevin Chen , Srikanth Venkatraman , Tejal Parekh , Patrick Pinto , Bama Santhanam , F. Njoroge , Ashit Ganguly , Henry Vaccaro , Scott Kemp , Odile Levy , Marguerita Lim-Wilby , Susan Tamura
IPC分类号： C12N9/99 , A61K31/16 , A61K31/195 , A61K31/27 , A61K31/357 , A61K31/385 , A61K31/403 , A61K31/4164 , A61K31/445 , A61K31/7052 , A61K38/00 , A61K38/05 , A61K38/21 , A61K38/55 , A61K45/00 , A61P1/16 , A61P31/12 , A61P31/14 , A61P43/00 , C07C205/51 , C07C229/00 , C07D209/02 , C07K5/02 , C07K5/103 , C07K7/02 , C07K7/04 , C07K7/06 , A61K38/06 , A61K31/165 , A61K38/08
CPC分类号： C07K7/06 , A61K31/16 , A61K31/195 , A61K31/27 , A61K31/357 , A61K31/385 , A61K31/403 , A61K31/4164 , A61K31/445 , A61K38/05 , C07C205/51 , C07K5/101 , C07K7/02 , A61K2300/00
摘要： The present invention discloses novel peptide compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such compounds as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型肽化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这些化合物的药物组合物以及使用它们来治疗与HCV蛋白酶相关的病症的方法。
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8.发明授权Macrocyclic NS-3 serine protease inhibitors of hepatitis C virus comprising alkyl and aryl alanine P2 moieties 失效丙型肝炎病毒的大环NS-3丝氨酸蛋白酶抑制剂包含烷基和芳基丙氨酸P2部分公开(公告)号：US06914122B2
公开(公告)日：2005-07-05
申请号：US09836636
申请日：2001-04-17
申请人： Srikanth Venkatraman , Kevin X. Chen , Ashok Arasappan , F. George Njoroge , Viyyoor Moopil Girijavallabhan , Ashit K. Ganguly , Tin-Yau Chan , Brian Alexander Mc Kittrick , Nanhua Hugh Yao , Andrew Joseph Prongay , Vincent Stewart Madison
发明人： Srikanth Venkatraman , Kevin X. Chen , Ashok Arasappan , F. George Njoroge , Viyyoor Moopil Girijavallabhan , Ashit K. Ganguly , Tin-Yau Chan , Brian Alexander Mc Kittrick , Nanhua Hugh Yao , Andrew Joseph Prongay , Vincent Stewart Madison
IPC分类号： A61K45/00 , A61K31/7052 , A61K38/00 , A61K38/21 , A61P31/12 , A61P31/14 , A61P43/00 , C07D273/00 , C07K5/02 , C07K7/02 , C07K7/64 , C07K7/50
CPC分类号： C07K5/0202 , A61K38/00 , C07K7/02
摘要： The present invention discloses novel macrocyclic compounds which have HCV protease inhibitory activity as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising such macrocycles as well as methods of using them to treat disorders associated with the HCV protease.
摘要翻译： 本发明公开了具有HCV蛋白酶抑制活性的新型大环化合物及其制备方法。 在另一个实施方案中，本发明公开了包含这种大环化合物的药物组合物以及使用它们治疗与HCV蛋白酶相关的病症的方法。
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公开(公告)号：US20160002224A1
公开(公告)日：2016-01-07
申请号：US14769159
申请日：2014-03-10
申请人： John J. ACTON, III , Rajan ANAND , Ashok ARASAPPAN , Qun DANG , Iyassu SEBHAT , Zhifa PU , Takao SUZUKI , MERCK SHARP & DOHME CORP.
发明人： John J. Acton, III , Rajan Anand , Ashok Arasappan , Qun Dang , Iyassu Sebhat , Zhifa Pu , Takao Suzuki
IPC分类号： C07D471/04 , A61K31/404 , A61K31/437 , A61K31/4985 , A61K31/4439 , A61K31/366 , A61K31/397 , C07D209/08 , C07D401/10
CPC分类号： C07D471/04 , A61K31/366 , A61K31/397 , A61K31/404 , A61K31/437 , A61K31/4439 , A61K31/4545 , A61K31/496 , A61K31/4985 , A61K31/5377 , A61K31/541 , C07D209/08 , C07D209/12 , C07D209/18 , C07D209/30 , C07D401/04 , C07D401/06 , C07D401/10 , C07D403/04 , C07D405/04 , C07D405/06 , C07D405/10 , C07D413/04 , C07D413/10 , C07D493/04 , C07D519/00 , A61K2300/00
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK-activated protein kinase. The compounds of the present invention may be 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，预防和抑制由AMPK激活的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，肥胖症，高胆固醇血症和高血压。
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![NOVEL AZABENZIMIDAZOLE HEXAHYDROFURO[E,2-B]FURAN DERIVATIVES](/abs-image/US/2015/10/08/US20150284411A1/abs.jpg.150x150.jpg)
公开(公告)号：US20150284411A1
公开(公告)日：2015-10-08
申请号：US14419774
申请日：2013-08-19
申请人： James M. APGAR , Ashok ARASAPPAN , Tesfaye BIFTU , Ping CHEN , Danqing FENG , Erin GUIDRY , Jacqueline HICKS , Ahmet KEKEC , Kenneth LEAVITT , Bing LI , Troy MCCRACKEN , Iyassu SEBHAT , Xiaoxia QIAN , Lan WEI , Robert WILKENING , Zhicai WU , Merck Sharp & Dohme Corp.
发明人： James M. Apgar , Ashok Arasappan , Tesfaye Biftu , Ping Chen , Danqing Feng , Erin Guidry , Jacqueline D. Hicks , Ahmet Kekec , Kenneth J. Leavitt , Bing Li , Troy McCracken , Iyassu Sebhat , Xiaoxia Qian , Lan Wei , Robert R. Wilkening , Zhicai Wu
IPC分类号： C07D519/00 , A61K31/438 , A61K45/06 , A61K31/501 , A61K31/5377 , A61K31/541 , A61K31/437 , A61K31/506
CPC分类号： C07D519/00 , A61K31/366 , A61K31/397 , A61K31/437 , A61K31/438 , A61K31/4985 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K45/06 , A61K2300/00
摘要： Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be 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，肥胖症，高胆固醇血症和高血压。
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