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公开(公告)号:US20130040983A1
公开(公告)日:2013-02-14
申请号:US13520548
申请日:2011-01-07
申请人: Jean-Michel Vernier , Patrick O'Connor , William Ripka , David Matthews , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
发明人: Jean-Michel Vernier , Patrick O'Connor , William Ripka , David Matthews , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
IPC分类号: C07D401/04 , C12N9/99 , A61P35/00 , C07D471/04 , A61K31/437 , A61K31/4439 , C07D401/14
CPC分类号: C07D401/04 , C07D471/04
摘要: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinae mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.
摘要翻译: 本文描述了用于抑制RAF基因介导的信号传导的化合物,药物组合物和方法。 所述化合物,药物组合物和方法可用于治疗人类疾病和病症。
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公开(公告)号:US20130012513A1
公开(公告)日:2013-01-10
申请号:US13520150
申请日:2011-01-06
申请人: Jean-Michel Vernier , John May , Patrick O'Connor , William Ripka , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
发明人: Jean-Michel Vernier , John May , Patrick O'Connor , William Ripka , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
IPC分类号: C07D277/30 , C12N5/07 , C07D413/12 , A61P35/00 , C07D263/32 , A61K31/421 , C07D417/12 , A61K31/496 , A61K31/426 , A61K31/5377
CPC分类号: C07D277/28 , C07D263/32 , C07D277/24 , C07D277/30
摘要: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary disease and disorders.
摘要翻译: 本文描述了用于抑制Hedgehog信号传导的化合物,药物组合物和方法。 所述化合物,药物组合物和方法可用于治疗人和兽医疾病和病症。
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公开(公告)号:US09174949B2
公开(公告)日:2015-11-03
申请号:US13520150
申请日:2011-01-06
申请人: Jean-Michel Vernier , John May , Patrick O'Connor , William Ripka , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
发明人: Jean-Michel Vernier , John May , Patrick O'Connor , William Ripka , Anthony Pinkerton , Pierre-Yves Bounaud , Stephanie Hopkins
IPC分类号: A61K31/496 , A61K31/5377 , A61K31/427 , C07D417/12 , C07D277/22 , C07D277/28 , C07D263/32 , C07D277/24 , C07D277/30
CPC分类号: C07D277/28 , C07D263/32 , C07D277/24 , C07D277/30
摘要: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary disease and disorders.
摘要翻译: 本文描述了用于抑制Hedgehog信号传导的化合物,药物组合物和方法。 所述化合物,药物组合物和方法可用于治疗人和兽医疾病和病症。
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公开(公告)号:US20140221374A1
公开(公告)日:2014-08-07
申请号:US14005720
申请日:2012-03-16
申请人: Jean-Michel Vernier , Stephanie Hopkins , Pierre-Yves Bounaud , Patrick O'Connor , David Matthews , Steve Bender
发明人: Jean-Michel Vernier , Stephanie Hopkins , Pierre-Yves Bounaud , Patrick O'Connor , David Matthews , Steve Bender
IPC分类号: C07D417/14 , C07D403/14 , C07D401/14 , C07D401/04 , C07D403/04 , C07D417/04
CPC分类号: C07D417/14 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/04 , C07D471/04
摘要: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of RAF kinase mediated signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human disease and disorders.
摘要翻译: 本文描述了用于抑制RAF激酶介导的信号传导的化合物,药物组合物和方法。 所述化合物,药物组合物和方法可用于治疗人类疾病和病症。
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公开(公告)号:US08486936B2
公开(公告)日:2013-07-16
申请号:US12773656
申请日:2010-05-04
申请人: Alexander Khvat , Sergey Tkachenko , Ilya Okun , Borys Rogovoy , Nikolay Savchuk , John May , Patrick O'Connor , William Ripka , Jean-Michel Vernier , David Matthews
发明人: Alexander Khvat , Sergey Tkachenko , Ilya Okun , Borys Rogovoy , Nikolay Savchuk , John May , Patrick O'Connor , William Ripka , Jean-Michel Vernier , David Matthews
IPC分类号: A61K31/5377 , A61K31/497 , A61K31/437 , C12N5/02 , C07D471/04 , A61P35/00
CPC分类号: C07D471/04
摘要: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary diseases and disorders.
摘要翻译: 本文描述了用于抑制Hedgehog信号传导的化合物,药物组合物和方法。 所述化合物,药物组合物和方法可用于治疗人和兽医疾病和病症。
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6.
公开(公告)号:US20080096935A1
公开(公告)日:2008-04-24
申请号:US11666072
申请日:2005-10-21
IPC分类号: A61K31/4412 , A61K31/4196 , A61K31/4152
CPC分类号: C07D213/30 , C07D207/32 , C07D213/65 , C07D213/70 , C07D231/12 , C07D235/18 , C07D249/08
摘要: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including 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的增强剂(包括mGluR2受体)的化合物,其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。 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:US20050288346A1
公开(公告)日:2005-12-29
申请号:US10524704
申请日:2003-08-22
IPC分类号: A61K31/41 , A61P25/00 , C07D257/02 , C07D257/04
CPC分类号: C07D257/04
摘要: The present invention is directed to compounds which are potentiators of metabotropic glutamate receptors, including 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的增强剂(包括mGluR2受体)的化合物,其可用于治疗或预防与谷氨酸能力障碍相关的神经和精神病学障碍以及其中涉及代谢型谷氨酸受体的疾病。 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:US20130150381A1
公开(公告)日:2013-06-13
申请号:US13703891
申请日:2011-06-15
申请人: Samedy Ouk , Jean-Michel Vernier , Esmir Gunic
发明人: Samedy Ouk , Jean-Michel Vernier , Esmir Gunic
IPC分类号: C07C323/52 , C07C323/53 , A61K45/06 , A61K31/195 , C07D213/32 , A61K31/4418 , A61K31/277 , A61K31/192
CPC分类号: C07C323/52 , A61K31/192 , A61K31/195 , A61K31/277 , A61K31/4418 , A61K45/06 , C07C323/53 , C07C323/61 , C07C323/62 , C07C2601/02 , C07C2601/04 , C07D213/32 , C07D213/55
摘要: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of using them. In some embodiments, the compounds described herein are used in the treatment or prevention of dis orders related to aberrant levels of uric acid.
摘要翻译: 本文描述了可用于调节血液尿酸水平的化合物,含有它们的制剂和使用它们的方法。 在一些实施方案中,本文所述的化合物用于治疗或预防与尿酸异常水平相关的疾病顺序。
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公开(公告)号:US08372852B2
公开(公告)日:2013-02-12
申请号:US13470122
申请日:2012-05-11
IPC分类号: C07D473/28 , C07D473/34 , A61K31/52 , A61P31/18 , C07D487/04 , A61K31/519
CPC分类号: C07D487/04 , C07D473/18
摘要: Described herein are novel enzyme inhibitors. In some embodiments, the enzyme inhibitors are reverse transcriptase inhibitors, particularly HIV reverse transcriptase inhibitors. Also described herein are compositions containing them and methods of using them. Thus, the compounds and compositions described herein are useful for the in vitro and in vivo inhibition of HIV reverse transcriptase as a method of treating or preventing HIV, AIDS or related disorders. In some embodiments, the enzyme inhibitors are compounds of formula (I) or a pharmaceutically acceptable salt or tautomer thereof:
摘要翻译: 本文描述的是新的酶抑制剂。 在一些实施方案中,酶抑制剂是逆转录酶抑制剂,特别是HIV逆转录酶抑制剂。 本文还描述了含有它们的组合物和使用它们的方法。 因此,本文所述的化合物和组合物可用于体外和体内抑制HIV逆转录酶,作为治疗或预防HIV,AIDS或相关病症的方法。 在一些实施方案中,酶抑制剂是式(I)的化合物或其药学上可接受的盐或互变异构体:
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10.
公开(公告)号:US20120289696A1
公开(公告)日:2012-11-15
申请号:US13558537
申请日:2012-07-26
申请人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
发明人: Nicholas D. Cosford , Thomas J. Seiders , Joseph E. Payne , Jeffrey R. Roppe , Dehua Huang , Nicholas D. Smith , Steve F. Poon , Chris King , Brian W. Eastman , Bowei Wang , Jeannie M. Arruda , Jean-Michel Vernier , Xiumin Zhao
IPC分类号: C07D417/06 , C07D417/14 , C07D471/04
CPC分类号: C07D417/06 , C07D417/14 , C07D471/04
摘要: The identification of a unique series of compounds which possesses special advantages in terms of drug-like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.
摘要翻译: 由于在效力和/或药代动力学和/或选择性和/或体内受体占有性方面具有有利的性质,鉴定了具有药物性质特征的独特系列化合物。 具体地说,通过亚乙炔基连接到吡啶环的3位或嘧啶环的5位上的1,3-噻唑-2-基环成员的选择,其中环被选定的取代基取代,得到 具有优异药物性质的化合物。 本发明包括这些杂环化合物的药学上可接受的盐形式,特别是氯化物盐和三氟乙酸盐。
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