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公开(公告)号：US06303625B1
公开(公告)日：2001-10-16
申请号：US09354032
申请日：1999-07-15
IPC分类号： A61K31437
CPC分类号： C07D471/04 , C07D211/34
摘要： The invention is directed to novel triazolopyridine derivatives which are useful as antagonists of GPIIb/IIIa. Pharmaceutical compositions comprising the triazolopyridine derivatives of the present invention, methods of treating conditions mediated by GPIIb/IIIa (e.g., methods for treating platelet-mediated thrombotic disorders) along with processes for making the compounds and novel intermediates are also disclosed.
摘要翻译： 本发明涉及可用作GPIIb / IIIa的拮抗剂的新型三唑并吡啶衍生物。 还公开了包含本发明的三唑并吡啶衍生物的药物组合物，治疗由GPIIb / IIIa介导的病症的方法（例如，用于治疗血小板介导的血栓形成障碍的方法）以及制备该化合物和新型中间体的方法。
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公开(公告)号：US07618945B2
公开(公告)日：2009-11-17
申请号：US11227504
申请日：2005-09-15
CPC分类号： C07K5/06191 , C07K5/06095
摘要： The invention is directed to novel heteroaryl peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, angiogenesis and related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted heteroaryl peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
摘要翻译： 本发明涉及可用作凝血酶受体拮抗剂用于治疗与血栓形成，再狭窄，高血压，心力衰竭，心律失常，炎症，心绞痛，中风，动脉粥样硬化，缺血性疾病，血管生成和相关疾病相关的疾病的新型杂肽体模拟化合物， 癌症和神经变性疾病。 还公开了包含本发明的取代的杂芳基肽模拟物的药物组合物和治疗由凝血酶受体介导的病症的方法。
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公开(公告)号：US07183252B2
公开(公告)日：2007-02-27
申请号：US10403542
申请日：2003-03-31
IPC分类号： A61K38/00
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06139
摘要： The invention is directed to novel indole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indole peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
摘要翻译： 本发明涉及可用作治疗与血栓形成，再狭窄，高血压，心力衰竭，心律失常，炎症，心绞痛，中风，动脉粥样硬化，缺血性疾病，血管发生相关疾病，癌症相关的疾病的凝血酶受体拮抗剂的新型吲哚拟肽化合物 ，和神经变性疾病。 还公开了包含本发明的取代的吲哚肽模拟物的药物组合物和治疗由凝血酶受体介导的病症的方法。
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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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公开(公告)号：US07629319B2
公开(公告)日：2009-12-08
申请号：US10732701
申请日：2003-12-10
CPC分类号： C07K5/06191 , C07K5/06095
摘要： The invention is directed to novel heteroaryl peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, angiogenesis and related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted heteroaryl peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
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公开(公告)号：US06858577B1
公开(公告)日：2005-02-22
申请号：US09603231
申请日：2000-06-26
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/06139
摘要： The invention is directed to novel indole peptidomimetic compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indole peptidomimetics of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
摘要翻译： 本发明涉及可用作治疗与血栓形成，再狭窄，高血压，心力衰竭，心律失常，炎症，心绞痛，中风，动脉粥样硬化，缺血性疾病，血管发生相关疾病，癌症相关的疾病的凝血酶受体拮抗剂的新型吲哚拟肽化合物 ，和神经变性疾病。 还公开了包含本发明的取代的吲哚肽模拟物的药物组合物和治疗由凝血酶受体介导的病症的方法。
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7.发明授权公开(公告)号：US06365617B1
公开(公告)日：2002-04-02
申请号：US09603229
申请日：2000-06-26
IPC分类号： A61K31416
CPC分类号： C07D209/14 , C07D231/56
摘要： The invention is directed to novel indole and indazole urea-peptoid compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indole and indazole urea-peptoid compounds of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.
摘要翻译： 本发明涉及可用作治疗与血栓形成，再狭窄，高血压，心力衰竭，心律失常，炎症，心绞痛，中风，动脉粥样硬化，缺血性疾病，血管生成相关的疾病的凝血酶受体拮抗剂的新型吲哚和吲唑脲 - 拟肽化合物 相关疾病，癌症和神经变性疾病。 还公开了包含本发明的取代的吲哚和吲唑脲 - 拟肽化合物的药物组合物和治疗由凝血酶受体介导的病症的方法。
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8.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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9.发明授权公开(公告)号：US06960597B2
公开(公告)日：2005-11-01
申请号：US09891602
申请日：2001-06-26
IPC分类号： A61K38/00 , A61P1/04 , A61P9/10 , A61P11/06 , A61P17/06 , A61P19/02 , A61P25/00 , A61P29/00 , A61P35/00 , A61P37/02 , A61P37/06 , A61P43/00 , C07D209/52 , C07D453/06 , C07K5/06 , A61K31/46 , C07D221/22 , C07D401/12
CPC分类号： C07D453/06 , C07D209/52
摘要： The invention is directed to aza-bridged-bicyclic compounds having Formula (I): and pharmaceutically acceptable salts thereof. The compounds are useful (α4 integrin receptor antagonists and, in particular, α4β1 and α4β7 integrin receptor antagonists. The invention is further directed to methods for use of the instant compounds for treating integrin mediated disorders including, but not limited to, inflammatory disorders, autoimmune disorders and cell-proliferative disorders, methods for preparing the compounds and methods for preparing the intermediates, derivatives and pharmaceutical compositions thereof.
摘要翻译： 本发明涉及具有式（I）的氮杂桥联双环化合物及其药学上可接受的盐。 该化合物是有用的（α4整联蛋白受体拮抗剂，特别是α4β1和α4β7整联蛋白受体拮抗剂。本发明还涉及本发明化合物用于治疗整联蛋白介导的病症的方法，包括但不限于炎症性疾病，自身免疫性 疾病和细胞增殖性疾病，制备化合物的方法和制备中间体的方法，其衍生物和药物组合物。
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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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