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1. 发明公开

EP1232155A1 PROTEASE INHIBITORS 审中-公开
标题翻译：蛋白酶抑制剂
公开(公告)号：EP1232155A1
公开(公告)日：2002-08-21
申请号：EP00978423.2
申请日：2000-11-08
申请人： SmithKline Beecham Corporation
发明人： MARQUIS, Robert, W., Jr. , VEBER, Daniel, Frank
IPC分类号： C07D413/00 , A61K31/55
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.

2. 发明公开

EP1229911A1 PROTEASE INHIBITORS 审中-公开
标题翻译：蛋白酶抑制剂
公开(公告)号：EP1229911A1
公开(公告)日：2002-08-14
申请号：EP00975607.3
申请日：2000-11-08
申请人： SmithKline Beecham Corporation
发明人： MARQUIS, Robert, Wells, Jr. , VEBER, Daniel, Frank
IPC分类号： A61K31/55 , C07D409/14 , A61P19/08 , A61P19/10
CPC分类号： C07D495/04 , A61K31/55 , Y02A50/411 , Y02A50/414 , Y02A50/423
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，并且可用于治疗抑制骨丢失或软骨退化是一个因素。

3. 发明公开

EP1153022A1 PROTHEASE INHIBITORS 审中-公开
标题翻译： PROTHEASE抑制剂
公开(公告)号：EP1153022A1
公开(公告)日：2001-11-14
申请号：EP00910222.9
申请日：2000-02-17
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： MARQUIS, Robert, Wells, Jr. , VEBER, Daniel, Frank
IPC分类号： C07D313/04 , C07D333/70 , C07D241/36 , C07D209/42 , A61K31/336 , A61K31/381 , A61K31/498 , A61K31/404
CPC分类号： C07D405/12 , C07D313/18 , C07D407/12 , C07D409/12
摘要： The present invention provides 7-14 membered ring ether 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7-14元环醚蛋白酶抑制剂及其抑制蛋白酶（包括组织蛋白酶K）的药学上可接受的盐，水合物和溶剂化物，所述化合物的药物组合物，所述化合物的新型中间体以及治疗过度骨丢失疾病的方法或软骨或基质降解，包括骨质疏松症; 牙龈疾病，包括牙龈炎和牙周炎; 关节炎，更具体地说，骨关节炎和类风湿性关节炎; 佩吉特氏病; 恶性肿瘤高钙血症; 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。

4. 发明公开

EP0809492A1 IL-8 RECEPTOR ANTAGONISTS 失效
标题翻译： IL-8受体拮抗剂
公开(公告)号：EP0809492A1
公开(公告)日：1997-12-03
申请号：EP96906547.0
申请日：1996-02-16
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： WIDDOWSON, Katherine, Louisa , VEBER, Daniel, Frank , JUREWICZ, Anthony, Joseph , RUTLEDGE, Melvin, Clarence, Jr. , HERTZBERG, Robert, Philip
IPC分类号： A61K31 , A61P29 , A61P37 , C07C253 , C07C255 , C07C275 , C07C307 , C07C309 , C07C311 , C07C317 , C07C323 , C07C335 , C07D213 , C07D215 , C07D217 , C07D277 , C07D317 , C07D333 , C07D409
CPC分类号： C07D213/30 , A61K31/17 , A61K31/18 , 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 , C07D213/71 , C07D215/36 , C07D217/02 , C07D277/36 , C07D277/46 , C07D317/66 , C07D333/28 , C07D333/34 , C07D333/36 , C07D409/04 , Y02A50/411
摘要： This invention relates to the novel use of phenyl ureas in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).

5. 发明公开

EP1229914A1 PROTEASE INHIBITORS 审中-公开
公开(公告)号：EP1229914A1
公开(公告)日：2002-08-14
申请号：EP00977057.9
申请日：2000-11-08
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： MARQUIS, Robert, W., Jr. , RU, Yu , VEBER, Daniel, Frank
IPC分类号： A61K31/55 , C07D401/14 , A61P19/08 , A61P19/10
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.

6. 发明公开

EP1223932A1 COMPOUNDS AND METHODS 审中-公开
标题翻译：化合物和方法
公开(公告)号：EP1223932A1
公开(公告)日：2002-07-24
申请号：EP00970527.8
申请日：2000-09-29
申请人： SmithKline Beecham Corporation
发明人： MARINO, Joseph, P., Jr. , THOMPSON, Scott, K. , VEBER, Daniel, Frank
IPC分类号： A61K31/422 , A61K31/4196 , A61K31/4439 , C07D261/02 , C07D249/12 , C07D249/14 , C07D401/02 , C07D413/02
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.

7. 发明公开

EP1140897A1 PROTEASE INHIBITORS 审中-公开
标题翻译：蛋白酶抑制剂
公开(公告)号：EP1140897A1
公开(公告)日：2001-10-10
申请号：EP99968936.7
申请日：1999-12-21
申请人： SmithKline Beecham Corporation
发明人： MARQUIS, Robert, Wells, Jr. , VEBER, Daniel, Frank
IPC分类号： C07D401/02 , C07D401/14 , C07D225/02 , A61K31/33 , A61K31/44 , A61K31/47 , A61P19/02 , A61P19/10
CPC分类号： C07D401/12 , C07D225/02
摘要： The present invention provides compounds of formula (I) 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 of 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 or 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：本发明提供了式（I）化合物及其药学上可接受的盐，水合物和溶剂化物，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，这类化合物的新中间体，以及治疗过量骨丢失或软骨疾病的方法或基质降解，包括骨质疏松症，包括牙龈炎和牙周炎的牙龈疾病; 关节炎，更具体地说是骨关节炎和类风湿性关节炎; 佩吉特氏病; 高钙血症或恶性肿瘤以及代谢性骨病，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。

8. 发明公开

EP1067894A2 PROTEASE INHIBITORS 审中-公开
标题翻译：蛋白酶抑制剂
公开(公告)号：EP1067894A2
公开(公告)日：2001-01-17
申请号：EP99924421.3
申请日：1999-05-20
申请人： SmithKline Beecham Corporation
发明人： BONDINELL, William, Edward , DESJARLAIS, Renee, Louise , VEBER, Daniel, Frank , YAMASHITA, Dennis, Shinji
IPC分类号： A61K6/00
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：本发明提供了双氨甲基羰基蛋白酶抑制剂及其抑制蛋白酶（包括组织蛋白酶K）的药学上可接受的盐，水合物和溶剂合物，这类化合物的药物组合物，以及治疗过度骨丢失或软骨或基质降解疾病，包括骨质疏松症 ; 牙龈疾病，包括牙龈炎和牙周炎; 关节炎，更具体地说，骨关节炎和类风湿性关节炎; 佩吉特氏病; 恶性肿瘤高钙血症; 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。

9. 发明公开

EP1229912A1 PROTEASE INHIBITORS 审中-公开
标题翻译：蛋白酶抑制剂
公开(公告)号：EP1229912A1
公开(公告)日：2002-08-14
申请号：EP00975609.9
申请日：2000-11-08
申请人： SMITHKLINE BEECHAM CORPORATION
发明人： MARQUIS, Robert, W., Jr. , RU, Yu , VEBER, Daniel, Frank
IPC分类号： A61K31/55 , C07D409/14 , A61P19/08 , A61P19/10
CPC分类号： C07D495/04 , A61K31/55 , Y02A50/411
摘要： The 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，并且可用于治疗抑制骨丢失或软骨退化是一个因素。

10. 发明公开

EP1158986A1 PROTEASE INHIBITORS 审中-公开
标题翻译：蛋白酶抑制剂
公开(公告)号：EP1158986A1
公开(公告)日：2001-12-05
申请号：EP99963112.0
申请日：1999-12-21
申请人： SmithKline Beecham Corporation
发明人： MARQUIS, Robert, Wells, Jr. , RU, Yu , VEBER, Daniel, Frank , CUMMINGS, Maxwell, David , THOMPSON, Scott, Kevin , YAMASHITA, Dennis
IPC分类号： A61K31/55 , C07D223/08 , C07D401/02 , C07D403/02 , C07D405/02 , C07D409/02 , C07D411/02 , C07D413/02 , C07D417/02 , C07D419/02
CPC分类号： C07D405/14 , 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
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.

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