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公开(公告)号：US07405209B2
公开(公告)日：2008-07-29
申请号：US11152745
申请日：2005-06-14
申请人： Robert Wells Marquis, Jr. , Yu Ru , Daniel Frank Veber , Maxwell David Cummings , Scott Kevin Thompson , Dennis Shinji Yamashita
发明人： Robert Wells Marquis, Jr. , Yu Ru , Daniel Frank Veber , Maxwell David Cummings , Scott Kevin Thompson , Dennis Shinji Yamashita
IPC分类号： A61P19/00 , A61K31/55 , A61K31/00 , C07D223/08 , C07D403/00 , C07D405/00 , C07D409/00
CPC分类号： C07D405/14 , A61K38/00 , C07D223/12 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/12 , C07D405/12 , C07D409/12 , C07D409/14 , C07D413/14 , C07D417/12 , C07D417/14 , C07D471/04 , C07D491/04 , C07D495/04 , C07K5/06139
摘要： The present invention provides 4-amino-azepan-3-one protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, novel intermediates of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
摘要翻译： 本发明提供了抑制蛋白酶的4-氨基 - 氮杂-3-酮蛋白酶抑制剂及其药学上可接受的盐，水合物和溶剂化物，包括组织蛋白酶K，这些化合物的药物组合物，这些化合物的新中间体，以及治疗疾病的方法 骨质疏松过多或软骨或基质降解，包括骨质疏松症; 牙龈疾病包括牙龈炎和牙周炎; 关节炎，更具体地，骨关节炎和类风湿性关节炎; 佩吉特病 恶性高钙血症; 和代谢性骨病，其包括通过向有需要的患者施用本发明的化合物来抑制所述骨丢失或过度软骨或基质降解。
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公开(公告)号：US06232342B1
公开(公告)日：2001-05-15
申请号：US09330451
申请日：1999-06-11
申请人： Thomas Joseph Carr , Renee Louise Desjarlais , Timothy Francis Gallagher , Stacie Marie Halbert , Hye-Ja Oh , Scott Kevin Thompson , Daniel Frank Veber , Dennis Shinji Yamashita , Jack Hwekwo Yen
发明人： Thomas Joseph Carr , Renee Louise Desjarlais , Timothy Francis Gallagher , Stacie Marie Halbert , Hye-Ja Oh , Scott Kevin Thompson , Daniel Frank Veber , Dennis Shinji Yamashita , Jack Hwekwo Yen
IPC分类号： A61K31277
CPC分类号： C07D213/30 , C07C243/34 , C07C311/16 , C07C311/29 , C07D215/36 , C07D241/24 , C07D249/10 , C07D271/10 , C07D277/56 , C07D285/12 , C07D285/125 , C07D295/155 , C07D295/215 , C07D307/91 , C07D333/34 , C07D333/76 , C07D401/12 , C07D405/12 , C07D417/12 , C12N9/6472 , C12Q1/37 , G01N33/573
摘要： The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease, hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting and bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
摘要翻译： 本发明提供了抑制蛋白酶的化合物，包括组织蛋白酶K，这些化合物的药物组合物，以及用于治疗过度骨丢失或软骨或基质降解（包括骨质疏松症）的疾病的方法。 牙龈疾病包括牙龈炎和牙周炎; 关节炎，更具体地，骨关节炎和类风湿性关节炎; 佩吉特氏病，恶性高钙血症; 和代谢性骨病，其包括通过向有需要的患者施用本发明的化合物来抑制和骨丢失或过度的软骨或基质降解。
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公开(公告)号：US06331542B1
公开(公告)日：2001-12-18
申请号：US09551968
申请日：2000-04-19
申请人： Thomas Joseph Carr , Renee Louise Desjarlais , Timothy Francis Gallagher , Stacie Marie Halbert , Hye-Ja Oh , Scott Kevin Thompson , Daniel Frank Veber , Dennis Shinji Yamashita , Jack Hwekwo Yen
发明人： Thomas Joseph Carr , Renee Louise Desjarlais , Timothy Francis Gallagher , Stacie Marie Halbert , Hye-Ja Oh , Scott Kevin Thompson , Daniel Frank Veber , Dennis Shinji Yamashita , Jack Hwekwo Yen
IPC分类号： A61K315375
CPC分类号： C07D213/30 , C07C243/34 , C07C311/16 , C07C311/29 , C07D215/36 , C07D241/24 , C07D249/10 , C07D271/10 , C07D277/56 , C07D285/12 , C07D285/125 , C07D295/155 , C07D295/215 , C07D307/91 , C07D333/34 , C07D333/76 , C07D401/12 , C07D405/12 , C07D417/12 , C12N9/6472 , C12Q1/37 , G01N33/573
摘要： The present invention provides compounds which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
摘要翻译： 本发明提供了抑制蛋白酶的化合物，包括组织蛋白酶K，这些化合物的药物组合物，以及用于治疗过度骨丢失或软骨或基质降解（包括骨质疏松症）的疾病的方法。 牙龈疾病包括牙龈炎和牙周炎; 关节炎，更具体地，骨关节炎和类风湿性关节炎; 佩吉特病 恶性高钙血症; 和代谢性骨病，其包括通过向有需要的患者施用本发明的化合物来抑制所述骨丢失或过度软骨或基质降解。
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公开(公告)号：US06583137B1
公开(公告)日：2003-06-24
申请号：US10129674
申请日：2002-05-06
IPC分类号： A61K3155
CPC分类号： C07D401/14 , A61K31/55 , Y02A50/411 , Y02A50/423
摘要： This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvent thereof, which is an inhibitor of cysteine proteases, particularly cathespin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，水合物或溶剂，其是半胱氨酸蛋白酶，特别是cathespin K的抑制剂，并且可用于治疗其中抑制骨丢失或 软骨退化是一个因素
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公开(公告)号：US06518267B1
公开(公告)日：2003-02-11
申请号：US09700828
申请日：2000-11-21
申请人： William Edward Bondinell , Renee Louise DesJarlais , Daniel Frank Veber , Dennis Shinji Yamashita
发明人： William Edward Bondinell , Renee Louise DesJarlais , Daniel Frank Veber , Dennis Shinji Yamashita
IPC分类号： A61K31535
CPC分类号： C07D213/89 , A61K38/00 , C07C271/22 , C07C311/16 , C07D213/56 , C07D215/48 , C07D215/54 , C07D295/155 , C07D307/85 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D413/14 , C07D417/12 , C07D417/14 , C07D487/04 , C07D495/04 , C07K5/06026 , C07K5/06139
摘要： The present invention provides bis-aminomethyl carbonyl protease inhibitors and pharmaceutically acceptable salts, hydrates and solvates thereof which inhibit proteases, including cathepsin K, pharmaceutical compositions of such compounds, and methods for treating diseases of excessive bone loss or cartilage or matrix degradation, including osteoporosis; gingival disease including gingivitis and periodontitis; arthritis, more specifically, osteoarthritis and rheumatoid arthritis; Paget's disease; hypercalcemia of malignancy; and metabolic bone disease, comprising inhibiting said bone loss or excessive cartilage or matrix degradation by administering to a patient in need thereof a compound of the present invention.
摘要翻译： 本发明提供了二氨基甲基羰基蛋白酶抑制剂及其药学上可接受的盐，水合物和溶剂合物，其抑制蛋白酶，包括组织蛋白酶K，这些化合物的药物组合物，以及用于治疗过度骨丢失或软骨或基质降解的疾病的方法，包括骨质疏松症 ; 牙龈疾病包括牙龈炎和牙周炎; 关节炎，更具体地，骨关节炎和类风湿性关节炎; 佩吉特病 恶性高钙血症; 和代谢性骨病，其包括通过向有需要的患者施用本发明的化合物来抑制所述骨丢失或过度软骨或基质降解。
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公开(公告)号：US5998470A
公开(公告)日：1999-12-07
申请号：US290958
申请日：1999-04-13
IPC分类号： A61K31/00 , A61K31/16 , A61K31/18 , A61K31/34 , A61K31/343 , A61K31/38 , A61K31/381 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4245 , A61K31/425 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/4439 , A61K31/445 , A61K31/4465 , A61K31/4523 , A61K31/4525 , A61K31/47 , A61K31/4709 , A61K31/495 , A61K31/496 , A61K31/4965 , A61K31/497 , A61K31/535 , A61K31/5375 , A61K31/5377 , A61K31/54 , A61K38/00 , A61P1/00 , A61P1/02 , A61P19/00 , A61P19/10 , A61P29/00 , A61P43/00 , C07C235/50 , C07C243/34 , C07C271/22 , C07C281/06 , C07C311/16 , C07C311/29 , C07D211/62 , C07D213/30 , C07D213/71 , C07D213/81 , C07D215/36 , C07D231/18 , C07D233/56 , C07D241/24 , C07D249/10 , C07D271/06 , C07D271/10 , C07D277/20 , C07D277/36 , C07D277/40 , C07D277/56 , C07D285/06 , C07D285/12 , C07D285/125 , C07D285/135 , C07D295/155 , C07D295/20 , C07D295/215 , C07D307/91 , C07D333/34 , C07D333/76 , C07D401/12 , C07D405/12 , C07D417/12 , C07D417/14 , C07K5/062 , C07K5/083 , C12N9/64 , C12Q1/37 , G01N33/573 , A61K31/27 , C07D275/00 , C07D271/20
CPC分类号： C07D213/30 , C07C243/34 , C07C311/16 , C07C311/29 , C07D215/36 , C07D241/24 , C07D249/10 , C07D271/10 , C07D277/56 , C07D285/12 , C07D285/125 , C07D295/155 , C07D295/215 , C07D307/91 , C07D333/34 , C07D333/76 , C07D401/12 , C07D405/12 , C07D417/12 , C12N9/6472 , C12Q1/37 , G01N33/573
摘要： Disclosed herein is a compound of the formula ##STR1## known as 2-[N-(N-benzyloxycarbonyl-L-leucinyl)]-2'-[N'-[4-(N,N-dimethylaminomethyl)benzyloxy]carbonyl-L-leucinyl]carbohydrazide; and pharmaceutically acceptable salts, hydrates and solvates thereof.
摘要翻译： 本文公开了一种称为2- [N-（N-苄氧基羰基-L-亮氨酰））-2' - [N' - [4-（N，N-二甲基氨基甲基）苄氧基]羰基-L-亮氨酰基 ]碳酰肼; 及其药学上可接受的盐，水合物和溶剂化物。
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公开(公告)号：US06534498B1
公开(公告)日：2003-03-18
申请号：US10129681
申请日：2002-05-06
IPC分类号： A61K3155
CPC分类号： C07D401/14 , A61K31/55 , Y02A50/411
摘要： This invention relates to the compound of Formula (I) or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，水合物或溶剂合物，其是半胱氨酸蛋白酶，特别是组织蛋白酶K的抑制剂，并且可用于治疗其中抑制骨丢失或 软骨退化是一个因素。
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公开(公告)号：US06262113B1
公开(公告)日：2001-07-17
申请号：US09125279
申请日：1998-08-14
申请人： Katherine Louisa Widdowson , Daniel Frank Veber , Anthony Joseph Jurewicz , Robert Philip Hertzberg , Melvin Clarence Rutledge, Jr.
发明人： Katherine Louisa Widdowson , Daniel Frank Veber , Anthony Joseph Jurewicz , Robert Philip Hertzberg , Melvin Clarence Rutledge, Jr.
IPC分类号： A61K31275
CPC分类号： A61K31/18 , A61K31/17 , A61K31/223 , A61K31/275 , A61K31/277 , A61K31/36 , A61K31/381 , A61K31/426 , A61K31/47 , C07C275/34 , C07C275/38 , C07C275/40 , C07C275/42 , C07C307/10 , C07C309/15 , C07C311/10 , C07C311/13 , C07C311/21 , C07C311/29 , C07C311/46 , C07C317/42 , C07C323/44 , C07C335/18 , C07C2602/08 , C07C2603/18 , C07D213/30 , C07D213/71 , C07D215/36 , C07D217/02 , C07D277/36 , C07D277/46 , C07D317/66 , C07D333/28 , C07D333/34 , C07D333/36 , C07D409/04 , Y02A50/411
摘要： The present invention relates to novel compounds and a novel use of phenyl ureas in the treatment of disease states mediated by the chemokine Interleukin-8 (IL-8).
摘要翻译： 本发明涉及新化合物和苯尿脲在治疗由趋化因子白细胞介素-8（IL-8）介导的疾病状态中的新用途。
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9.发明授权1,2,4-triazole derivatives, compositions, process of making and methods of use 失效1,2,4-三唑衍生物，组合物，制备方法和使用方法公开(公告)号：US07304082B2
公开(公告)日：2007-12-04
申请号：US11186519
申请日：2005-07-21
IPC分类号： A61K31/4196 , C07D249/14
CPC分类号： C07D405/12 , A61K31/4196 , A61K31/422 , A61K31/4439 , C07D249/14 , C07D409/12
摘要： Compounds of this invention are non-peptide, reversible inhibitors of type 2 methionine aminopeptidase, useful in treating conditions mediated by angiogenesis, such as cancer, haemangioma, proliferative retinopathy, rheumatoid arthritis, atherosclerotic neovascularization, psoriasis, ocular neovascularization and obesity.
摘要翻译： 本发明化合物是可用于治疗由血管发生介导的病症，例如癌症，血管瘤，增殖性视网膜病变，类风湿性关节炎，动脉粥样硬化新生血管形成，牛皮癣，眼新生血管形成和肥胖的2型甲硫氨酸氨基肽酶的非肽可逆抑制剂。
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公开(公告)号：US06596715B1
公开(公告)日：2003-07-22
申请号：US10129671
申请日：2002-05-06
IPC分类号： C07D41300
CPC分类号： C07D401/14 , C07B2200/05
摘要： This invention relates to the compound of Formula (I): or a pharmaceutically acceptable salt, hydrate or solvate thereof, which is an inhibitor of cysteine proteases, particularly cathepsin K, and is useful in the treatment of diseases in which inhibition of bone loss or of cartilage degradation is a factor.
摘要翻译： 本发明涉及式（I）化合物或其药学上可接受的盐，水合物或溶剂化物，其是半胱氨酸蛋白酶，特别是组织蛋白酶K的抑制剂，并且可用于治疗其中抑制骨丢失或 的软骨退化是一个因素。
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