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公开(公告)号：EP0998572A2
公开(公告)日：2000-05-10
申请号：EP98936003.7
申请日：1998-07-24
发明人： ARNER, Elizabeth, C. , BURN, Timothy, C. , COPELAND, Robert, A. , DECICCO, Carl, P. , LIU, Ruiqin , MAGOLDA, Ronald , PRATTA, Michael , SOLOMON, Kimberly, A. , TORTORELLA, Micky, D. , TRZASKOS, James, M. , YANG, Fude
IPC分类号： C12N15/57 , C12N9/64 , C07K16/40 , C12N1/19 , C12N5/10 , C12Q1/68 , C12Q1/37 , A61K38/55 , A61K39/395 , G01N33/573 , G01N33/68
CPC分类号： C12N9/6489 , A61K38/00 , C07K16/40 , C12Q1/37 , G01N33/6887 , G01N2333/96486 , G01N2500/00 , G01N2800/102
摘要： The invention is directed to the family of aggrecan degrading metallo proteases (ADMPs) that exhibit the ability to cleave the aggrecan core protein between amino acid residues Glu?373-Ala374¿. The invention encompasses the nucleic acids encoding such enzymes, processes for production of recombinant ADMPs, compositions containing such enzymes, and the use of these enzymes in various assays and for the development of novel inhibitors for use as therapies for diseases involving aggrecanase-mediated degradation of cartilage or other aggrecanase-associated diseases.
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公开(公告)号：EP1054877A1
公开(公告)日：2000-11-29
申请号：EP99905898.5
申请日：1999-02-10
IPC分类号： C07D285/36 , C07D279/02 , C07D417/12 , C07D417/06 , A61K31/55 , A61K31/54
CPC分类号： C07D417/06 , C07D279/02 , C07D285/36 , C07D417/12
摘要： The present application describes novel lactams and derivatives thereof of formula (I) or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered cyclic sulfonamide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
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3.发明公开NOVEL INHIBITORS OF AGGRECANASE AND MATRIX METALLOPROTEINASES FOR THE TREATMENT OF ARTHRITIS 审中-公开抑制剂VON AGGRECANASE UND MATRIXMETALLPROTEINASEN ZUR BEHANDLUNG VON ARTHRITIS
公开(公告)号：EP1005448A2
公开(公告)日：2000-06-07
申请号：EP98942083.1
申请日：1998-08-18
发明人： YAO, Wenqing , DECICCO, Carl, P.
IPC分类号： C07C259/06
CPC分类号： C07D257/04 , C07C259/06 , C07C271/22 , C07C311/06 , C07C311/08 , C07C311/16 , C07C311/21 , C07C2601/02 , C07C2601/04 , C07C2601/08 , C07C2601/14 , C07C2602/08 , C07D295/155 , C07D295/205 , C07D307/79 , C07D317/60 , C07D413/04
摘要： This invention relates to molecules which inhibit metalloproteinases such as formulas (I, IV) including aggrecanase, and the production of tumor necrosis factor (TNF). In particular, the compounds are inhibitors of metalloproteinases involved in tissue degradation and inhibitors of the release of tumor necrosis factor. The present invention also relates to pharmaceutical compositions comprising such compounds and to methods of using these compounds for the treatment of inflammatory diseases.
摘要翻译： 本发明涉及抑制金属蛋白酶（包括聚蛋白聚糖蛋白聚糖酶）和肿瘤坏死因子（TNF）的产生的分子。 特别地，化合物是参与组织降解的金属蛋白酶抑制剂和肿瘤坏死因子释放抑制剂。 本发明还涉及包含这些化合物的药物组合物和使用这些化合物治疗炎性疾病的方法。
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4.发明公开CYCLIC HYDROXAMIC ACIDS AS METALLOPROTEINASE INHIBITORS 审中-公开CYCLISCHEHYDROXAMSÄURENALS METROOPROTEINASE-INHIBITOREN
公开(公告)号：EP1087937A1
公开(公告)日：2001-04-04
申请号：EP99930371.2
申请日：1999-06-17
发明人： XUE, Chu-Baio , DECICCO, Carl, P. , HE, Xiaohua
IPC分类号： C07C259/08 , C07D211/16 , A61K31/47 , C07D211/22 , C07D213/30 , C07D215/22 , C07D213/40 , C07D215/20 , C07D401/12 , C07D211/60 , C07D405/14 , C07D417/14 , C07D401/14 , C07D409/14 , A61K31/445
CPC分类号： C07D213/30 , C07C259/08 , C07C2601/08 , C07C2601/14 , C07D211/16 , C07D211/22 , C07D211/60 , C07D213/40 , C07D215/20 , C07D215/233 , C07D401/12 , C07D401/14 , C07D405/14 , C07D409/14 , C07D417/14
摘要： The present application describes novel cyclic hydroxamic acids of formula (I): or pharmaceutically acceptable salt forms thereof, wherein ring B is a 5-7 membered cyclic system containing from 0-2 heteroatoms selected from O, N, NRa and S(O)¿p?, and 0-1 carbonyl groups and the other variables are defined in the present specification, which are useful as metalloprotease inhibitors.
摘要翻译： 本申请描述了式I的新型环状异羟肟酸或其药学上可接受的盐形式，其中环B为5-7元环系，其含有0-2个选自O，N，NR a和S（ O）p和0-1个羰基，其它变量在本说明书中定义，其可用作金属蛋白酶抑制剂。
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5.发明公开NOVEL SUBSTITUTED ARYL HYDROXAMIC ACIDS AS METALLOPROTEINASE INHIBITORS 审中-公开取代的芳基异羟肟酸衍生物作为金属蛋白酶抑制剂
公开(公告)号：EP1077978A1
公开(公告)日：2001-02-28
申请号：EP99922940.4
申请日：1999-05-12
IPC分类号： C07D417/12 , C07D401/12 , C07D279/12 , C07D207/16 , A61K31/54 , A61K31/40
CPC分类号： C07D401/12 , C07D207/16 , C07D279/12 , C07D417/12
摘要： The present application describes novel substituted aryl hydroxamic acids of formula (I) or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-1 additional heteroatoms selected from N, O, and S, which are useful as metalloproteinase inhibitors and inhibitors of TNF.
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公开(公告)号：EP1077974A1
公开(公告)日：2001-02-28
申请号：EP99924184.7
申请日：1999-05-12
IPC分类号： C07D405/12 , C07D401/12 , A61K31/445 , A61K31/44 , A61K31/35
CPC分类号： C07D401/12 , C07D405/12
摘要： The present application describes novel substituted aryl hydroxamic acids of formula (I) or pharmaceutically acceptable salt forms thereof, wherein ring A is a 5-8 membered ring containing from 0-2 heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
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公开(公告)号：EP1027332A1
公开(公告)日：2000-08-16
申请号：EP98950954.2
申请日：1998-10-02
IPC分类号： C07D207/27 , A61K31/40 , C07D401/12 , C07D417/12
CPC分类号： C07D207/26 , C07D205/08 , C07D209/96 , C07D211/76 , C07D233/32 , C07D233/78 , C07D401/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/12 , C07D417/12 , C07D417/14 , C07D471/04 , C07D487/10
摘要： The present application describes novel lactams and derivatives thereof of formula (I), or pharmaceutically acceptable salt forms thereof, wherein ring B is a 4-8 membered cyclic amide containing from 0-3 additional heteroatoms selected from N, O, and S, which are useful as metalloprotease inhibitors.
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