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1.发明授权Carboxamide derivatives of piperidine for the treatment of thrombosis disorders 失效哌啶羧酰胺衍生物用于治疗血栓形成障碍
公开(公告)号：US6069254A
公开(公告)日：2000-05-30
申请号：US841016
申请日：1997-04-29
IPC分类号： C12P17/12 , A61K31/00 , A61K31/44 , A61K31/4406 , A61K31/4427 , A61K31/443 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4545 , A61K31/47 , A61K31/472 , A61K31/4725 , A61K31/495 , A61K31/55 , A61P7/00 , A61P7/02 , C07D211/00 , C07D211/60 , C07D213/00 , C07D213/55 , C07D215/00 , C07D241/00 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07F7/08 , C07D403/14
CPC分类号： C07F7/0812 , C07D211/60 , C07D213/55 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14
摘要： Carboxamide derivatives of pyrrolidine, piperidine, and hexahydroazepine of formula (I): ##STR1## are disclosed as useful in treating platelet-mediated thrombotic disorders.
摘要翻译： 公开了式（I）的吡咯烷，哌啶和六氢氮杂的羧酰胺衍生物：用于治疗血小板介导的血栓形成障碍。
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公开(公告)号：US08158792B2
公开(公告)日：2012-04-17
申请号：US12313289
申请日：2008-11-19
IPC分类号： C07D491/107 , A61K31/438
CPC分类号： C07D491/10 , C07D405/06 , C07D471/10 , C07D495/10
摘要： The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.
摘要翻译： 本发明涉及式（I）化合物或其形式，其中X 1，X 2，X 3，X 4，R 1，R 2和R 3如本文所定义，可用作类胰蛋白酶抑制剂。
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公开(公告)号：US5827860A
公开(公告)日：1998-10-27
申请号：US481934
申请日：1995-06-07
IPC分类号： A61K38/00 , C07D263/22 , C07D277/56 , C07D277/68 , C07D417/06 , C07K5/06 , C07K5/065 , A61K31/425 , A01N43/78
CPC分类号： C07D277/68 , C07D263/22 , C07D277/56 , C07D417/06 , C07K5/06078 , C07K5/06191 , A61K38/00
摘要： Compounds of the Formula I: ##STR1## useful in the treatment of thrombin and trypsin related disorders.
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公开(公告)号：US20120165327A1
公开(公告)日：2012-06-28
申请号：US13409559
申请日：2012-03-01
IPC分类号： A61K31/438 , C07D405/06 , C07D471/10 , C07D495/10 , A61K31/506 , A61K31/5377 , A61K31/444 , A61P29/00 , A61P9/00 , A61P17/00 , A61P11/06 , A61P11/02 , A61P37/08 , A61P19/02 , A61P37/00 , A61P1/04 , A61P27/02 , A61P1/00 , A61P11/00 , A61P17/02 , A61P17/06 , A61P17/04 , A61P1/16 , A61P13/12 , A61P9/10 , A61P9/08 , C07D495/04 , C07D491/107
CPC分类号： C07D491/10 , C07D405/06 , C07D471/10 , C07D495/10
摘要： The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.
摘要翻译： 本发明涉及式（I）化合物或其形式，其中X 1，X 2，X 3，X 4，R 1，R 2和R 3如本文所定义，可用作类胰蛋白酶抑制剂。
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公开(公告)号：US08536189B2
公开(公告)日：2013-09-17
申请号：US13409559
申请日：2012-03-01
IPC分类号： C07D407/02 , A61K31/438
CPC分类号： C07D491/10 , C07D405/06 , C07D471/10 , C07D495/10
摘要： The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.
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公开(公告)号：US06469036B1
公开(公告)日：2002-10-22
申请号：US09482802
申请日：2000-01-13
IPC分类号： A61K3140
CPC分类号： C07K5/06139 , C07D277/64 , C07D417/12 , C07K5/06026
摘要： The present invention relates to a series of peptidyl heterocyclic ketones which are inflammatory cell serine protease inhibitors and their compositions and methods for the prevention and treatment of a variety of immunomediated inflammatory disorders. More particularly, these compounds are potent and selective inhibitors of tryptase and are therefore effective for the prevention and treatment of inflammatory diseases associated with the respiratory tract, such as asthma and allergic rhinitis.
摘要翻译： 本发明涉及一系列作为炎性细胞丝氨酸蛋白酶抑制剂的肽基杂环酮及其组合物和预防和治疗各种免疫缺陷性炎症性疾病的方法。 更具体地，这些化合物是类胰蛋白酶的有效和选择性抑制剂，因此对于预防和治疗与呼吸道相关的炎性疾病如哮喘和过敏性鼻炎是有效的。
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公开(公告)号：US5384327A
公开(公告)日：1995-01-24
申请号：US994735
申请日：1992-12-22
IPC分类号： A61K31/70 , A61K31/7048 , A61K31/76 , A61P1/06 , A61P13/06 , A61P25/08 , C07D493/04 , C07D493/14 , C07H9/04 , C07H11/00 , C07H13/00 , C07H13/06 , A61K31/35 , C07D311/94
摘要： Sulfamate derivatives having the following formula (I): ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are as herein defined, have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, the present invention encompasses pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and novel intermediates are disclosed.
摘要翻译： 具有下式（I）的氨基磺酸衍生物：其中R 1，R 2，R 3，R 4，R 5和R 6如本文所定义的其中R 1，R 2，R 3，R 4，R 5和R 6具有抗惊厥活性，因此可用于治疗条件 如癫痫。 此外，本发明包括含有式（I）化合物的药物组合物及其用途及新型中间体。
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公开(公告)号：US07718673B2
公开(公告)日：2010-05-18
申请号：US10345808
申请日：2003-01-16
IPC分类号： A61P9/00 , A61P19/10 , A61K31/445 , C07D211/00 , C07D401/00 , C07D405/00 , C07D409/00
CPC分类号： C07D401/04 , C07D211/62 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/12
摘要： The invention is directed to novel isonipecotamide derivatives of Formula (I): which are useful in treating integrin-mediated disorders.
摘要翻译： 本发明涉及式（I）的新型异哌耳酰胺衍生物：其可用于治疗整联蛋白介导的病症。
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公开(公告)号：US20090163527A1
公开(公告)日：2009-06-25
申请号：US12313289
申请日：2008-11-19
IPC分类号： A61K31/438 , C07D491/107
CPC分类号： C07D491/10 , C07D405/06 , C07D471/10 , C07D495/10
摘要： The present invention is directed to a compound of Formula (I): or a form thereof, wherein X1, X2, X3, X4, R1, R2 and R3 are as defined herein, useful as tryptase inhibitors.
摘要翻译： 本发明涉及式（I）化合物或其形式，其中X 1，X 2，X 3，X 4，R 1，R 2和R 3如本文所定义，可用作类胰蛋白酶抑制剂。
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10.发明授权Tricyclic monosaccharide derivatives useful in treating acute ischemia-induced neurodegeneration 失效用于治疗急性缺血诱导的神经变性的三环单糖衍生物公开(公告)号：US06495523B1
公开(公告)日：2002-12-17
申请号：US09620510
申请日：2000-07-20
IPC分类号： A01N6100
CPC分类号： C07H11/00 , A61K31/357 , A61K31/7048 , C07H9/04
摘要： Anticonvulsant compounds of the general formula I: where X, R1, R2, R3, R4, R5, and R6 are as herein defined; are useful in treating acute ischemia-induced neurodegeneration, such as occurs during and after stroke, head trauma, spinal injury, non-fatal cardiac arrest, or major surgical procedures. Furthermore, pharmaceutical compositions containing a compound of formula I as well as methods for their use are disclosed.
摘要翻译： 通式I的抗惊厥化合物：其中X，R 1，R 2，R 3，R 4，R 5和R 6如本文所定义; 可用于治疗急性缺血诱发的神经退行性疾病，例如卒中发作，头部外伤，脊柱损伤，非致命性心脏骤停或主要外科手术。 此外，公开了含有式I化合物的药物组合物及其使用方法。
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