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公开(公告)号：US06765004B1
公开(公告)日：2004-07-20
申请号：US09592520
申请日：2000-06-12
申请人： William J. Hoekstra , Michael N. Greco , Leonard R. Hecker , Bruce E. Maryanoff , Jay M. Matthews
发明人： William J. Hoekstra , Michael N. Greco , Leonard R. Hecker , Bruce E. Maryanoff , Jay M. Matthews
IPC分类号： A61K3155
CPC分类号： C07D487/06
摘要： The invention is directed to tricyclic indoloazepine compounds useful as vasopressin receptor antagonists, pharmaceutical compositions comprising the compounds of the present invention and methods of treating conditions involving increased vascular resistance and cardiac insufficiency which include hypertension, congestive heart failure, cardiac insufficiency, coronary vasospasm, cardiac ischemia, liver cirrhosis, renal vasospasm, renal failure, cerebral edema and ischemia, stroke, thrombosis or water retention in a subject in need thereof.
摘要翻译： 本发明涉及可用作加压素受体拮抗剂的三环吲哚吖啶化合物，包含本发明化合物的药物组合物和治疗包括高血压，充血性心力衰竭，心功能不全，冠状动脉血管痉挛，心脏不良 缺血，肝硬化，肾血管痉挛，肾衰竭，脑水肿和缺血，中风，血栓形成或需要的受试者的潴留。
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12.发明授权Substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators 有权用作凝血酶受体调节剂的取代的杂环酰基三肽公开(公告)号：US06747127B1
公开(公告)日：2004-06-08
申请号：US09565715
申请日：2000-05-05
IPC分类号： C07K508
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0812 , C07K5/1024
摘要： The invention is directed to substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators, their use in wound healing and preventing platelet aggregation. Pharmaceutical compositions comprising the substituted heterocyclic acyl-tripeptides of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
摘要翻译： 本发明涉及用作凝血酶受体调节剂的取代杂环酰基三肽，其用于伤口愈合和预防血小板聚集。 还公开了包含本发明的取代的杂环酰基三肽和治疗由凝血酶受体介导的病症的方法的药物组合物。
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13.发明授权Substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators 有权用作凝血酶受体调节剂的取代的杂环酰基三肽公开(公告)号：US07312306B2
公开(公告)日：2007-12-25
申请号：US10606422
申请日：2003-06-26
IPC分类号： C07K5/08
CPC分类号： C07K5/0202 , A61K38/00 , C07K5/0812 , C07K5/1024
摘要： The invention is directed to substituted heterocyclic acyl-tripeptides useful as thrombin receptor modulators, their use in wound healing and preventing platelet aggregation. Pharmaceutical compositions comprising the substituted heterocyclic acyl-tripeptides of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
摘要翻译： 本发明涉及用作凝血酶受体调节剂的取代杂环酰基三肽，其用于伤口愈合和预防血小板聚集。 还公开了包含本发明的取代的杂环酰基三肽和治疗由凝血酶受体介导的病症的方法的药物组合物。
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公开(公告)号：US07872044B2
公开(公告)日：2011-01-18
申请号：US11975235
申请日：2007-10-18
IPC分类号： A61K31/343 , C07D307/87 , C07F9/28
CPC分类号： C07F9/65517
摘要： The present invention is directed to a compound of Formula (I): or an enantiomer, diastereomer, polymorph or pharmaceutically acceptable salt thereof and methods for preparing said compounds and compositions, intermediates and derivatives thereof, and methods for treating inflammatory or serine protease mediated disorders.
摘要翻译： 本发明涉及式（I）的化合物或其对映体，非对映异构体，多晶型物或其药学上可接受的盐以及制备所述化合物及其组合物，中间体及其衍生物的方法，以及用于治疗炎性或丝氨酸蛋白酶介导的病症的方法 。
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公开(公告)号：US09079896B2
公开(公告)日：2015-07-14
申请号：US12533257
申请日：2009-07-31
IPC分类号： C07D487/12 , C07D471/04 , C07D487/04
CPC分类号： C07D471/04 , C07D487/04
摘要： The present invention is directed to compounds of formula (I) and pharmaceutically acceptable salts, esters and prodrugs thereof, pharmaceutical compositions containing compounds of formula (I) and the use of said compounds and compositions as urotensin II receptor antagonists.
摘要翻译： 本发明涉及式（I）化合物及其药学上可接受的盐，酯和前药，含有式（I）化合物的药物组合物以及所述化合物和组合物作为尿素转运蛋白II受体拮抗剂的用途。
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公开(公告)号：US08680278B2
公开(公告)日：2014-03-25
申请号：US12290438
申请日：2008-10-30
申请人： William A. Kinney , Christopher A. Teleha , Shyamali Ghosh , Bruce E. Maryanoff , Gabriela Grasa , Antonio Zanotti-Gerosa , Jonathan Alan Medlock
发明人： William A. Kinney , Christopher A. Teleha , Shyamali Ghosh , Bruce E. Maryanoff , Gabriela Grasa , Antonio Zanotti-Gerosa , Jonathan Alan Medlock
IPC分类号： C07D215/00 , C07D417/02 , C07D401/00
CPC分类号： C07D401/06 , B01J31/2213 , B01J31/2409 , B01J31/2495 , B01J2231/645 , B01J2531/0263 , B01J2531/0266 , B01J2531/821 , B01J2531/822 , B01J2531/827 , C07D405/14 , C07D471/04
摘要： The present invention is directed to a process for enantioselectively preparing substituted piperidine alkanoic acid integrin antagonist compounds.
摘要翻译： 本发明涉及对映选择性制备取代的哌啶链烷酸整联蛋白拮抗剂化合物的方法。
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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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18.发明授权Sulfamate and sulfamide derivatives useful for the treatment of epilepsy and related disorders 有权用于治疗癫痫和相关疾病的氨磺酸盐和磺酰胺衍生物公开(公告)号：US08084490B2
公开(公告)日：2011-12-27
申请号：US11154443
申请日：2005-06-16
IPC分类号： A61K31/357 , C07D319/20
CPC分类号： C07D319/20 , C07D311/58 , C07D317/58 , C07D321/10
摘要： The present invention is directed to novel sulfamide and sulfamate derivatives, pharmaceutical compositions containing them and their use in the treatment of epilepsy and related disorders.
摘要翻译： 本发明涉及新型磺酰胺和氨基磺酸酯衍生物，含有它们的药物组合物及其在治疗癫痫和相关疾病中的用途。
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公开(公告)号：US20110136824A1
公开(公告)日：2011-06-09
申请号：US13026549
申请日：2011-02-14
申请人： Bruce E. Maryanoff , William A. Kinney , Edward C. Lawson , Diane K. Luci , Nikolay Marchenko , Sergey Sviridov , Shyamali Ghosh
发明人： Bruce E. Maryanoff , William A. Kinney , Edward C. Lawson , Diane K. Luci , Nikolay Marchenko , Sergey Sviridov , Shyamali Ghosh
IPC分类号： A61K31/496 , C07D403/10 , C07D209/48 , A61K31/4035 , C07D403/14 , A61P9/00 , A61P13/12 , A61P1/18 , A61P25/28
CPC分类号： C07D209/48 , C07D401/06 , C07D401/12 , C07D403/04 , C07D403/06 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/12 , C07D413/14 , C07D417/12 , C07D451/14 , C07D487/08 , C07D513/04
摘要： The invention is directed to Urotensin II antagonists. More specifically, the present invention relates to certain novel compounds, methods for preparing compounds, compositions, intermediates and derivatives thereof and methods for treating Urotensin-II mediated disorders. Pharmaceutical and veterinary compositions and methods of treating cardiovascular disorders and various other disease states or conditions using compounds of the invention are also described.
摘要翻译： 本发明涉及尿激素II拮抗剂。 更具体地，本发明涉及某些新化合物，其制备方法，组合物，中间体及其衍生物以及用于治疗促肾上腺素II介导的病症的方法。 还描述了使用本发明化合物治疗心血管疾病和各种其它疾病状态或病症的药物和兽医组合物和方法。
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公开(公告)号：US07759380B2
公开(公告)日：2010-07-20
申请号：US11800878
申请日：2007-05-08
申请人： Han-Cheng Zhang , Bruce E. Maryanoff , David F. McComsey , Kimberly White , Hong Ye , Leonard R. Hecker
发明人： Han-Cheng Zhang , Bruce E. Maryanoff , David F. McComsey , Kimberly White , Hong Ye , Leonard R. Hecker
IPC分类号： A61K31/40 , C07D231/56
CPC分类号： C07D409/14 , C07D401/14 , C07D403/04 , C07D403/14 , C07D405/14 , C07D417/14
摘要： The present invention is directed to novel substituted pyrroline compounds useful as kinase or dual-kinase inhibitors, methods for producing such compounds and methods for treating or ameliorating a kinase or dual-kinase mediated disorder.
摘要翻译： 本发明涉及用作激酶或双重激酶抑制剂的新型取代的吡咯啉化合物，用于制备这些化合物的方法以及用于治疗或改善激酶或双重激酶介导的病症的方法。
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