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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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公开(公告)号：US20230227405A1
公开(公告)日：2023-07-20
申请号：US18009310
申请日：2021-06-14
申请人： Ashok ARASAPPAN , Ian M. BELL , Jason M. COX , Michael J. KELLY, III , Mark E. LAYTON , Hong LIU , Jian LIU , Akshay A. SHAH , Michael D. VANHEYST , MERCK SHARP & DOHME CORP.
发明人： Ashok Arasappan , Ian M. Bell , Jason Michael Cox , Michael J. Kelly, III , Mark E. Layton , Hong Liu , Jian Liu , Akshay A. Shah , Michael David VanHeyst
IPC分类号： C07D207/277 , C07D401/12 , C07D417/12
CPC分类号： C07D207/277 , C07D401/12 , 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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公开(公告)号：US10519147B2
公开(公告)日：2019-12-31
申请号：US16061815
申请日：2016-12-15
申请人： Merck Sharp & Dohme Corp. , Thomas J. Greshock , James Mulhearn , Liangqin Guo , Ting Zhang , Deping Wang , Ronald M. Kim , Mark E. Layton , Michael J. Kelly, III , Rajan Anand , Philippe Nantermet , Tianying Jian , Anthony J. Roecker , Walter Won , Gang Zhou
发明人： Thomas J. Greshock , James Mulhearn , Liangqin Guo , Ting Zhang , Deping Wang , Ronald M. Kim , Mark E. Layton , Michael J. Kelly, III , Rajan Anand , Philippe Nantermet , Tianying Jian , Anthony J. Roecker , Walter Won , Gang Zhou
IPC分类号： C07D417/12 , A61K45/06 , C07D277/52 , C07D285/135 , A61P25/02 , A61P25/04 , A61P11/14 , A61P17/04
摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting 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 pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.
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4.发明申请公开(公告)号：US20180362518A1
公开(公告)日：2018-12-20
申请号：US16061815
申请日：2016-12-15
申请人： Thomas J. GRESHOCK , James MULHEARN , Liangqin GUO , Ting ZHANG , Deping WANG , Ronald M. KIM , Mark E. LAYTON , Michael J. KELLY, III , Rajan ANAND , Tianying JIAN , Philippe NANTERMET , Anthony J. ROECKER , Walter WON , Gang ZHOU , Merck Sharp & Dohme Corp.
发明人： Thomas J. Greshock , James Mulhearn , Liangqin Guo , Ting Zhang , Deping Wang , Ronald M. Kim , Mark E. Layton , Michael J. Kelly, III , Rajan Anand , Philippe Nantermet , Tianying Jian , Anthony J. Roecker , Walter Won , Gang Zhou
IPC分类号： C07D417/12 , C07D285/135 , C07D277/52 , A61P11/14 , A61P17/04 , A61P25/04 , A61P25/02
CPC分类号： C07D417/12 , A61K45/06 , A61P11/14 , A61P17/04 , A61P25/02 , A61P25/04 , C07D277/52 , C07D285/135
摘要： Disclosed are compounds of Formula A, or a salt thereof, where Q, X, R1 and R2 are as defined herein, which compounds have properties for inhibiting Na 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 pain (acute, post-operative, neuropathic), or cough or itch disorders using the same.
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公开(公告)号：US20110288090A1
公开(公告)日：2011-11-24
申请号：US13147392
申请日：2010-01-25
申请人： Donna J. Armstrong , Yasuhiro Goto , Takashi Hashihayata , Tetsuya Kato , Michael J. Kelly, III , Mark E. Layton , Craig W. Lindsley , Yoshio Ogino , Yu Onozaki , Kenvin J. Rodzinak , Michael A. Rossi , Philip E. Sanderson , Jiabing Wang , Melissa M. Yaroschak
发明人： Donna J. Armstrong , Yasuhiro Goto , Takashi Hashihayata , Tetsuya Kato , Michael J. Kelly, III , Mark E. Layton , Craig W. Lindsley , Yoshio Ogino , Yu Onozaki , Kenvin J. Rodzinak , Michael A. Rossi , Philip E. Sanderson , Jiabing Wang , Melissa M. Yaroschak
IPC分类号： A61K31/5377 , A61K31/4985 , A61K31/496 , A61K31/506 , A61K31/498 , A61K31/438 , A61K31/4375 , C07D475/04 , C07D471/04 , C07D401/12 , A61P35/00 , A61K31/519
CPC分类号： C07D471/04 , C07D217/24 , C07D241/42 , C07D401/04 , C07D401/12 , C07D403/04 , C07D475/02 , C07D475/04 , C07D487/04 , C07D519/00
摘要： The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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公开(公告)号：US08008317B2
公开(公告)日：2011-08-30
申请号：US11921352
申请日：2006-06-07
申请人： Donna J. Armstrong , Essa H. Hu , Michael J. Kelly, III , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Michael J. Rossi , Philip E. Sanderson , Jiabing Wang
发明人： Donna J. Armstrong , Essa H. Hu , Michael J. Kelly, III , Mark E. Layton , Yiwei Li , Jun Liang , Kevin J. Rodzinak , Michael J. Rossi , Philip E. Sanderson , Jiabing Wang
IPC分类号： A61K31/437 , A61K31/4375 , C07D471/14 , C07D471/16
CPC分类号： C07D471/14 , C07D487/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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公开(公告)号：US20120252806A1
公开(公告)日：2012-10-04
申请号：US13515326
申请日：2010-12-09
IPC分类号： A61K31/4375 , C07D241/36 , A61K31/517 , A61K31/5377 , A61P35/00 , A61K31/497 , A61K31/506 , C07D487/04 , A61K31/519 , C07D471/04 , C07D413/06
CPC分类号： C07D471/04 , C07D513/04 , C07D519/00
摘要： The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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公开(公告)号：US07576209B2
公开(公告)日：2009-08-18
申请号：US11999234
申请日：2007-12-04
IPC分类号： C07D471/14 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D411/14 , C07D413/14 , C07D419/14 , C07D35/00
CPC分类号： C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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公开(公告)号：US08288407B2
公开(公告)日：2012-10-16
申请号：US13046322
申请日：2011-03-11
IPC分类号： C07D471/14 , A61K31/437 , A61P35/00
CPC分类号： C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. Compounds disclosed herein have the following chemical structure:
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。 本文公开的化合物具有以下化学结构：
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公开(公告)号：US20110160183A1
公开(公告)日：2011-06-30
申请号：US13046322
申请日：2011-03-11
IPC分类号： A61K31/397 , C07D471/14 , A61K31/4985 , A61K31/4375 , A61K31/506 , A61K31/501 , C07D413/14 , A61K31/5377 , C07D487/04 , A61K31/519 , A61P35/00
CPC分类号： C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D407/04 , C07D409/04 , C07D413/04 , C07D417/04 , C07D471/14
摘要： The instant invention provides for substituted naphthyridine compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer.
摘要翻译： 本发明提供抑制Akt活性的取代的萘啶化合物。 特别地，所公开的化合物选择性地抑制一种或两种Akt同种型。 本发明还提供了包含这种抑制化合物的组合物和通过将该化合物给予需要治疗癌症的患者来抑制Akt活性的方法。
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