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公开(公告)号：US08518874B2
公开(公告)日：2013-08-27
申请号：US12605271
申请日：2009-10-23
CPC分类号： A61K38/05 , C07K5/06034
摘要： The present invention is directed to compounds that are antiviral agents. Specifically the compounds of the present invention inhibit replication of HCV and are therefore useful in treating hepatitis C infections. The present invention is also directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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公开(公告)号：US08450373B2
公开(公告)日：2013-05-28
申请号：US13192403
申请日：2011-07-27
申请人： Michael Graupe , John O. Link , Michael G. Roepel
发明人： Michael Graupe , John O. Link , Michael G. Roepel
IPC分类号： A61K31/65
CPC分类号： C07C317/48 , C07C2601/02 , C07D213/32
摘要： The present invention is directed to compounds that are inhibitors of cysteine proteases, in particular, cathepsins B, K, L, F, and S and are therefore useful in treating diseases mediated by these proteases. The present invention is directed to pharmaceutical compositions comprising these compounds and processes for preparing them.
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公开(公告)号：US20120301426A1
公开(公告)日：2012-11-29
申请号：US13563068
申请日：2012-07-31
IPC分类号： A61K45/00
CPC分类号： C07C271/22 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/475 , A61K31/496 , A61K31/513 , A61K31/519 , A61K31/52 , A61K31/5375 , A61K31/5377 , A61K31/573 , A61K31/655 , A61K31/661 , A61K31/704 , A61K31/7068 , C07D207/27 , C07D211/76 , C07D295/108 , C07D295/125 , C07D333/46
摘要： The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
摘要翻译： 本发明提供具有组蛋白脱乙酰酶（HDAC）抑制活性的通式（I）的化合物，包含该化合物的药物组合物和可用于使用该化合物治疗疾病的方法。
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公开(公告)号：US20120289493A1
公开(公告)日：2012-11-15
申请号：US13466995
申请日：2012-05-08
申请人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Gregory Notte , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
发明人： Britton Kenneth Corkey , Elfatih Elzein , Robert H. Jiang , Rao V. Kalla , Tetsuya Kobayashi , Dmitry Koltun , Xiaofen Li , Ruben Martinez , Gregory Notte , Eric Q. Parkhill , Thao Perry , Jeff Zablocki , Chandrasekar Venkataramani , Michael Graupe , Juan Guerrero
IPC分类号： A61K31/53 , C07D401/10 , C07D403/10 , C07D413/06 , C07D413/14 , A61K31/5377 , C07D401/14 , A61K31/501 , A61K31/506 , C07D265/22 , A61K31/536 , C07D498/10 , A61K31/4725 , C07D417/06 , A61K31/5415 , A61P9/00 , A61P9/10 , A61P9/12 , A61P3/10 , A61P25/08 , A61P25/00 , C07D253/08
CPC分类号： C07D498/10 , C07D217/26 , C07D237/32 , C07D239/88 , C07D239/90 , C07D253/08 , C07D263/58 , C07D265/22 , C07D279/08 , C07D401/04 , C07D401/06 , C07D401/12 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/08 , C07D403/12 , C07D403/14 , C07D405/12 , C07D413/06 , C07D413/12 , C07D413/14 , C07D417/06 , C07D417/12 , C07D417/14 , C07D498/04
摘要： The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein Q, R1, X1, X2, Y and R2 are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
摘要翻译： 本公开涉及作为钠通道抑制剂的化合物及其用于治疗各种疾病状态（包括心血管疾病和糖尿病）的用途。 在具体实施方案中，化合物的结构由式I给出：其中Q，R 1，X 1，X 2，Y和R 2如本文所述，用于制备和使用该化合物的方法以及含有该化合物的药物组合物。
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公开(公告)号：US20120244121A1
公开(公告)日：2012-09-27
申请号：US13490696
申请日：2012-06-07
申请人： Michael Graupe , Randall L. Halcomb
发明人： Michael Graupe , Randall L. Halcomb
IPC分类号： A61K31/52 , A61K31/7056 , C12N5/07 , A61P31/14 , A61K31/55 , A61K31/5377 , A61P31/12 , A61K39/395 , A61K38/21 , A61K31/551
CPC分类号： C07D473/18 , A61K31/522 , A61K31/5377 , A61K31/55 , A61K31/551 , A61K45/06
摘要： The present invention includes therapeutic methods that include the administration of a compound of Formula I or II: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, to a subject in need of such, and therapeutic methods that include the administration of such compounds with at least one additional active agent.
摘要翻译： 本发明包括治疗方法，其包括向需要这种治疗方法的受试者施用式I或II化合物或其药学上可接受的盐，溶剂合物和/或酯，包括施用 化合物与至少一种另外的活性剂。
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公开(公告)号：US08258316B2
公开(公告)日：2012-09-04
申请号：US12795554
申请日：2010-06-07
IPC分类号： C07D207/08 , A61K31/4025
CPC分类号： C07C271/22 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/475 , A61K31/496 , A61K31/513 , A61K31/519 , A61K31/52 , A61K31/5375 , A61K31/5377 , A61K31/573 , A61K31/655 , A61K31/661 , A61K31/704 , A61K31/7068 , C07D207/27 , C07D211/76 , C07D295/108 , C07D295/125 , C07D333/46
摘要： The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
摘要翻译： 本发明提供具有组蛋白脱乙酰酶（HDAC）抑制活性的通式（I）的化合物，包含该化合物的药物组合物和可用于使用该化合物治疗疾病的方法。
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公开(公告)号：US20120045412A1
公开(公告)日：2012-02-23
申请号：US13284559
申请日：2011-10-28
IPC分类号： A61K31/437 , C07D513/04 , C07D417/14 , A61K31/496 , A61K31/5377 , A61K31/664 , A61K33/24 , A61K31/519 , A61K31/52 , A61K31/513 , A61K31/7068 , A61K31/475 , A61K31/704 , A61K31/7064 , A61K31/573 , A61K38/50 , A61K39/395 , A61K31/506 , A61K38/19 , A61K31/661 , A61K31/454 , A61K31/4745 , A61P35/00 , C07D471/04
CPC分类号： C07D471/04 , C07D213/56 , C07D277/24 , C07D277/30 , C07D277/56 , C07D277/60 , C07D405/04 , C07D405/14 , C07D409/14 , C07D417/04 , C07D417/12 , C07D417/14 , C07D513/04
摘要： The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
摘要翻译： 本发明提供具有组蛋白脱乙酰酶（HDAC）抑制活性的通式（I）的化合物，包含该化合物的药物组合物和可用于使用该化合物治疗疾病的方法。
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公开(公告)号：US20110009410A1
公开(公告)日：2011-01-13
申请号：US12834673
申请日：2010-07-12
IPC分类号： A61K31/444 , C07D401/14 , C07D401/12 , C07D471/04 , C07D413/14 , A61K31/4439 , A61K31/496 , A61K31/506 , A61K31/4725 , A61K31/437 , A61K31/5377 , A61P37/00 , A61P25/28 , A61P9/00 , A61P29/00
CPC分类号： A61K31/444 , A61K31/4439 , A61K31/4709 , A61K31/496 , A61K31/497 , A61K31/506 , A61K31/5377 , A61K31/585 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/14 , C07D413/12 , C07D413/14 , C07D417/14 , C07D471/04 , C07D491/048
摘要： The present invention relates to compounds of Formula (I): where in X1, X2, X3, X4, X5, X6, X7, X8, R1, R2, R3 are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases and neurodegenerative diseases. The invention also relates to pharmaceutical compositions comprising one or more of the compounds of Formula (I), and to methods of preparing the compounds of Formula (I).
摘要翻译： 本发明涉及式（I）化合物：其中X 1，X 2，X 3，X 4，X 5，X 6，X 7，X 8，R 1，R 2，R 3如上所定义。 该化合物具有凋亡信号调节激酶（“ASK1”）抑制活性，因此可用于治疗ASK1介导的病症，包括自身免疫性疾病，炎性疾病，心血管疾病和神经变性疾病。 本发明还涉及包含一种或多种式（I）化合物的药物组合物和制备式（I）化合物的方法。
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公开(公告)号：US20100310512A1
公开(公告)日：2010-12-09
申请号：US12779023
申请日：2010-05-12
申请人： Hongyan Guo , Darryl Kato , Thorsten A. Kirschberg , Hongtao Liu , John O. Link , Michael L. Mitchell , Jay P. Parrish , Jianyu Sun , James Taylor , Elizabeth M. Bacon , Eda Canales , Aesop Cho , Choung U. Kim , Jeromy J. Cottell , Manoj C. Desai , Randall L. Halcomb , Michael Graupe , Evan S. Krygowski , Scott E. Lazerwith , Qi Liu , Richard L. Mackman , Hyung-Jun Pyun , Joseph H. Saugier , James D. Trenkle , Winston C. Tse , Randall W. Vivian , Scott D. Schroeder , William J. Watkins , Lianhong Xu
发明人： Hongyan Guo , Darryl Kato , Thorsten A. Kirschberg , Hongtao Liu , John O. Link , Michael L. Mitchell , Jay P. Parrish , Jianyu Sun , James Taylor , Elizabeth M. Bacon , Eda Canales , Aesop Cho , Choung U. Kim , Jeromy J. Cottell , Manoj C. Desai , Randall L. Halcomb , Michael Graupe , Evan S. Krygowski , Scott E. Lazerwith , Qi Liu , Richard L. Mackman , Hyung-Jun Pyun , Joseph H. Saugier , James D. Trenkle , Winston C. Tse , Randall W. Vivian , Scott D. Schroeder , William J. Watkins , Lianhong Xu
IPC分类号： A61K31/4178 , C07D403/14 , C07D401/14 , C07D417/14 , A61K31/435 , A61K31/55 , A61K31/438 , A61K31/496 , A61K31/5415 , A61K38/21 , A61K31/708 , A61K31/7052 , A61P31/14
CPC分类号： C07D403/14 , A61K31/4025 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/435 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/519 , A61K31/5377 , A61K31/5415 , A61K31/55 , A61K45/06 , A61P31/12 , C07D207/16 , C07D401/14 , C07D403/04 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D471/04 , C07D471/08 , C07D471/10 , C07D487/04 , C07D491/113 , C07D495/04 , C07F5/025
摘要： The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明涉及抗病毒化合物，含有这些化合物的组合物和包括施用这些化合物的治疗方法以及可用于制备这些化合物的方法和中间体。
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公开(公告)号：US20100310500A1
公开(公告)日：2010-12-09
申请号：US12795554
申请日：2010-06-07
IPC分类号： A61K38/19 , C07D207/06 , A61K31/40 , A61P35/00 , A61P3/10 , A61P25/28 , A61P35/04 , A61P11/00 , A61P13/12 , A61K31/4025 , C07D409/12 , C07D207/263 , A61K31/4015 , C07D295/145 , A61K31/5375 , C07D413/12 , A61K31/5377 , C07D401/04 , A61K31/496 , A61K31/661 , A61K31/655 , A61K33/24 , A61K31/519 , A61K31/52 , A61K31/513 , A61K31/7068 , A61K31/475 , A61K31/704 , A61K31/573 , A61K38/50 , A61K39/395
CPC分类号： C07C271/22 , A61K31/40 , A61K31/4015 , A61K31/4025 , A61K31/475 , A61K31/496 , A61K31/513 , A61K31/519 , A61K31/52 , A61K31/5375 , A61K31/5377 , A61K31/573 , A61K31/655 , A61K31/661 , A61K31/704 , A61K31/7068 , C07D207/27 , C07D211/76 , C07D295/108 , C07D295/125 , C07D333/46
摘要： The present invention provides a compound of general Formula (I) having histone deacetylase (HDAC) inhibitory activity, a pharmaceutical composition comprising the compound, and a method useful to treat diseases using the compound.
摘要翻译： 本发明提供具有组蛋白脱乙酰酶（HDAC）抑制活性的通式（I）的化合物，包含该化合物的药物组合物和可用于使用该化合物治疗疾病的方法。
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