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公开(公告)号：EP1265863A1
公开(公告)日：2002-12-18
申请号：EP01918833.3
申请日：2001-03-20
发明人： PIKUL, Stanislaw , OHLER, Norman, Eugene , ALMSTEAD, Neil, Gregory , LAUGHLIN, Steven, Karl , NATCHUS, Michael, George , DE, Biswanath
IPC分类号： C07D211/34 , C07D401/06 , C07D405/06 , C07D409/06 , C07D417/06 , C07D413/06 , C07D211/66 , C07D335/02 , C07D309/06 , A61K31/4545 , A61P29/00
CPC分类号： C07D401/06 , C07D211/34 , C07D211/66 , C07D309/06 , C07D335/02 , C07D405/06 , C07D409/06 , C07D413/06 , C07D417/06
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to the following Formula (I) where R1, R2, n, A, E, X, G and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
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2.发明公开HETEROCYCLIC SIDE CHAIN CONTAINING, N-SUBSTITUTED METALLOPROTEASE INHIBITORS 审中-公开杂环侧链ENHALTENDE，N-取代的金属蛋白酶
公开(公告)号：EP1265864A1
公开(公告)日：2002-12-18
申请号：EP01918867.1
申请日：2001-03-02
发明人： PIKUL, Stanislaw , OHLER, Norman, Eugene , ALMSTEAD, Neil, Gregory , LAUGHLIN, Steven, Karl , NATCHUS, Michael, George , DE, Biswanath
IPC分类号： C07D211/34 , C07D211/96 , C07D211/66 , C07D309/14 , C07D309/08 , C07D309/06 , C07D407/12 , C07D401/12 , A61K31/445 , A61K31/535 , A61K31/35
CPC分类号： C07D401/12 , C07D211/34 , C07D211/66 , C07D211/96 , C07D309/06 , C07D309/08 , C07D309/14 , C07D407/12
摘要： Disclosed are compounds which are inhibitors of metalloproteases and which are effective in treating conditions characterized by excess activity of these enzymes. In particular, the compounds have a structure according to Formula (I): where R?1, R2, R3¿, n, A, E, X, G, G', M and Z have the meanings described in the specification and the claims, as well as optical isomers, diastereomers and enantiomers of Formula I, and pharmaceutically-acceptable salts, biohydrolyzable amides, esters, and imides thereof. Also described are pharmaceutical compositions comprising these compounds, and methods of treating metalloprotease-related maladies using the compounds or the pharmaceutical compositions.
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公开(公告)号：EP1682551A2
公开(公告)日：2006-07-26
申请号：EP04810572.0
申请日：2004-11-09
发明人： CLARK, Michael, Philip , LAUGHLIN, Steven, Karl , GOLEBIOWSKI, Adam , BRUGEL, Todd, Andrew , SABAT, Mark
IPC分类号： C07D487/00 , A61K31/4162 , A61P29/00
CPC分类号： C07D487/04
摘要： The present invention relates to 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones which inhibit the extracellular release of inflammatory cytokines, said cytokines responsible for one or more human or higher mammalian disease states. The present invention further relates to compositions comprising said 6,7-dihydro-5H-pyrazolo[1,2a]pyrazol-1-ones and methods for preventing, abating, or otherwise controlling enzymes which are understood to be the active components responsible for the herein described disease states.
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4.发明公开ISOXAZOLONE COMPOUNDS USEFUL IN TREATING DISEASES ASSOCIATED WITH UNWANTED CYTOKINE ACTIVITY 审中-公开异恶唑链接对于不需要的细胞因子活性相关疾病的治疗
公开(公告)号：EP1392299A1
公开(公告)日：2004-03-03
申请号：EP02734439.9
申请日：2002-05-15
发明人： CLARK, Michael, Philip , DJUNG, Jane, Far-Jine , LAUGHLIN, Steven, Karl , TULLIS, Joshua, Spector , NATCHUS, Michael, George , DE, Biswanath
IPC分类号： A61K31/44 , A61K31/445 , A61K31/495 , A61K31/535 , A61P19/02 , A61P29/00 , C07D413/04 , C07D413/14
CPC分类号： C07D413/04 , A61K31/44 , A61K31/505 , A61K31/506 , A61K31/53 , C07D413/14
摘要： Isoxazolone compounds having the generic structure: are used to treat disease associated with unwanted cytokine activity, including rheumatoid arthritis, osteoarthritis, diabetes, HIV/AIDS, inflammatory bowel disease, Crohn's disease, ulcerative colitis, congestive heart, hypertension, chronic obstructive pulmonary disease, septic shock syndrome, tuberculosis, adult respiratory distress, asthma, atherosclerosis, muscle degeneration, periodontal disease, cachexia, Reiter's syndrome, gout, acute synovitis, anorexia and bulimia nervosa fever, malaise, myalgia and headaches.
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