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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：US20120022022A1
公开(公告)日：2012-01-26
申请号：US13245208
申请日：2011-09-26
申请人： Michael J. Hawkins , Michael N. Greco , Eugene Powell , Lawrence de Garavilla , Bruce E. Maryanoff
发明人： Michael J. Hawkins , Michael N. Greco , Eugene Powell , Lawrence de Garavilla , Bruce E. Maryanoff
CPC分类号： A61K31/381 , A61K31/445 , A61K31/4535 , A61K31/662
摘要： The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.
摘要翻译： 本发明涉及式（I）化合物，这些化合物的制备方法，组合物，中间体及其衍生物，以及治疗炎性和丝氨酸蛋白酶介导的病症的方法。
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公开(公告)号：US07915260B2
公开(公告)日：2011-03-29
申请号：US11651848
申请日：2007-01-10
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： A61K31/501 , A61K31/496 , C07D209/48 , C07D401/06 , C07D401/12 , C07D403/06 , C07D403/12 , C07D407/06 , C07D407/12 , C07D409/06 , C07D409/12 , C07D413/14 , C07D417/12 , A61K31/439 , A61K31/4439 , A61K31/454 , A61K31/4035 , A61K31/551 , C07D451/02 , C07D487/08
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：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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75.发明授权公开(公告)号：US07759331B2
公开(公告)日：2010-07-20
申请号：US11716185
申请日：2007-03-09
申请人： Han-Cheng Zhang , Llorente Vincente R. Bonaga , Claudia K. Derian , Bruce E. Maryanoff , Hong Ye
发明人： Han-Cheng Zhang , Llorente Vincente R. Bonaga , Claudia K. Derian , Bruce E. Maryanoff , Hong Ye
IPC分类号： A01N43/00 , A61K31/33 , C07D225/00 , C07D295/00
CPC分类号： C07D471/22
摘要： This invention is directed to pyridine-containing macroheterocyclic compounds useful as kinase inhibitors, methods for producing such compounds and methods for treating or preventing a kinase mediated disorder.
摘要翻译： 本发明涉及可用作激酶抑制剂的含吡啶的大杂环化合物，用于制备这些化合物的方法以及用于治疗或预防激酶介导的病症的方法。
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公开(公告)号：US20090124804A1
公开(公告)日：2009-05-14
申请号：US12290438
申请日：2008-10-30
IPC分类号： C07D401/14 , C07D401/02
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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77.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：US06890939B2
公开(公告)日：2005-05-10
申请号：US10439884
申请日：2003-05-16
IPC分类号： A61P11/00 , A61P43/00 , C07D207/14 , C07D207/48 , A61K31/40 , C07D207/02
CPC分类号： C07D207/14 , C07D207/48
摘要： The present invention is directed to compounds useful as selective serine protease or dual-serine protease inhibitors, compositions thereof and methods for treating serine protease or dual-serine protease mediated disorders.
摘要翻译： 本发明涉及可用作选择性丝氨酸蛋白酶或双丝氨酸蛋白酶抑制剂的化合物，其组合物和治疗丝氨酸蛋白酶或双丝氨酸蛋白酶介导的病症的方法。
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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：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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