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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:US20100222321A1
公开(公告)日:2010-09-02
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 A. 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 A. Rossi , Philip E. Sanderson , Jiabing Wang
IPC分类号: A61K31/4375 , C07D471/14 , A61K31/496 , A61K31/519 , A61K31/506 , C07D513/04 , A61K31/501 , A61K31/5377 , A61K31/517 , A61K31/4709 , A61P35/00
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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13.
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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公开(公告)号:US20090253734A1
公开(公告)日:2009-10-08
申请号:US12482095
申请日:2009-06-10
IPC分类号: A61K31/4375 , C07D471/14
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:US09315518B2
公开(公告)日:2016-04-19
申请号:US14125813
申请日:2012-06-14
申请人: Hannah D. Fiji , Michael J. Kelly, III , Jeffrey C. Kern , Mark E. Layton , Joseph E. Pero , Alexander J. Reif , Michael A. Rossi
发明人: Hannah D. Fiji , Michael J. Kelly, III , Jeffrey C. Kern , Mark E. Layton , Joseph E. Pero , Alexander J. Reif , Michael A. Rossi
IPC分类号: C07D513/04 , C07D471/04 , C07D519/00
CPC分类号: C07D513/04 , C07D471/04 , C07D519/00
摘要: The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译: 本发明涉及作为代谢型谷氨酸受体,特别是mGluR2受体的增强剂的咪唑并吡啶-2-酮衍生物,其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神病学障碍以及代谢型谷氨酸受体 涉及。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。
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公开(公告)号:US20140350002A1
公开(公告)日:2014-11-27
申请号:US14125813
申请日:2012-06-14
申请人: Hannah D. Fiji , Michael J. Kelly, III , Jeffrey C. Kern , Mark E. Layton , Joseph E. Pero , Alexander J. Reif , Michael A. Rossi
发明人: Hannah D. Fiji , Michael J. Kelly, III , Jeffrey C. Kern , Mark E. Layton , Joseph E. Pero , Alexander J. Reif , Michael A. Rossi
IPC分类号: C07D513/04 , C07D471/04
CPC分类号: C07D513/04 , C07D471/04 , C07D519/00
摘要: The present invention is directed to imidazopyridin-2-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.
摘要翻译: 本发明涉及作为代谢型谷氨酸受体,特别是mGluR2受体的增强剂的咪唑并吡啶-2-酮衍生物,其可用于治疗或预防与谷氨酸功能障碍相关的神经和精神病学障碍以及代谢型谷氨酸受体 涉及。 本发明还涉及包含这些化合物的药物组合物以及这些化合物和组合物在预防或治疗涉及代谢型谷氨酸受体的疾病中的用途。
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公开(公告)号:US20210387966A1
公开(公告)日:2021-12-16
申请号:US17289123
申请日:2019-10-31
发明人: Ashok Arasappan , Ian M. Bell , Michael J. Breslin , Christopher James Bungard , Christopher S. Burgey , Harry R. Chobanian , Jason M. Cox , Anthony T. Ginnetti , Deodial Guy Guiadeen , Kristen L. G. Jones , Mark E. Layton , Hong Liu , Jian Liu , James J. Perkins , Shawn J. Stachel , Linda M. Suen-Lai , Zhe Wu
IPC分类号: C07D401/14 , C07D471/04 , C07D413/14 , C07D471/08 , C07D495/04 , C07D401/12 , C07D487/04 , C07D491/048
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:US09624208B2
公开(公告)日:2017-04-18
申请号:US14437315
申请日:2013-10-23
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.
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公开(公告)号:US20220119363A1
公开(公告)日:2022-04-21
申请号:US17289152
申请日:2019-10-28
发明人: Michael J. Breslin , Christopher James Bungard , Harry R. Chobanian , Kristen L. G. Jones , Mark E. Layton , Jian Liu , James J. Perkins , Jeffrey William Schubert , Shawn J. Stachel , Linda M. Suen-Lai , Zhe Wu
IPC分类号: C07D401/04 , C07D213/82 , C07D401/14 , C07D487/18 , C07D498/08 , C07D513/04 , C07D413/04 , C07D417/04 , C07D487/08 , C07D491/107 , C07D498/04 , C07D491/048 , C07D417/14 , C07D409/14 , C07D405/14 , C07D403/04 , C07D451/02
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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