公开(公告)号：EP0809636A1

公开(公告)日：1997-12-03

申请号：EP96904614.0

申请日：1996-02-12

申请人： G.D. SEARLE & CO.

发明人： TALLEY, John, J. ,  BROWN, David, L. ,  NAGARAJAN, Srinivasan ,  CARTER, Jeffery, S. ,  WEIER, Richard, M. ,  STEALEY, Michael, A. ,  COLLINS, Paul, W. ,  SEIBERT, Karen ,  GRANETO, Matthew, J. ,  XU, Xiangdong ,  PARTIS, Richard

IPC分类号： A61K31 ,  A61P1 ,  A61P3 ,  A61P7 ,  A61P9 ,  A61P11 ,  A61P13 ,  A61P17 ,  A61P19 ,  A61P21 ,  A61P25 ,  A61P27 ,  A61P29 ,  A61P31 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07D261 ,  C07D413

CPC分类号： C07D261/10 ,  C07D261/08 ,  C07D261/12 ,  C07D261/18 ,  C07D413/04

摘要： A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula (III) whrein R7 is selected from hydroxyl, lower alkyl, carboxyl, halo, lower carboxyalkyl, lower alkoxycarbonylalkyl, lower alkoxyalkyl, lower carboxyalkoxyalkyl, lower haloalkyl, lower haloalkylsulfonyloxy, lower hydroxylalkyl, lower aryl (hydroxylalkyl), lower carboxyaryloxyalkyl, lower alkoxycarbonylaryloxyalkyl, lower cycloalkyl, lower cycloalkylalkyl, and lower aralkyl; and wherein R8 is one or more radicals independently selected from hydrido, lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; or a pharmaceutically-acceptable salt thereof.

公开(公告)号：EP0979077A1

公开(公告)日：2000-02-16

申请号：EP98922028.0

申请日：1998-04-16

申请人： G.D. Searle & Co.

发明人： RONIKER, Barbara ,  LaCHAPELLE, Richard, J. ,  CONNOLLY, Daniel, T. ,  SEIBERT, Karen ,  NEEDLEMAN, Philip

IPC分类号： A61K31/415 ,  A61K31/635 ,  A61K31/10 ,  A61K31/18 ,  A61K31/425 ,  A61K31/44 ,  A61K31/42 ,  A61K31/38 ,  A61K31/35 ,  A61K31/535 ,  A61K31/54 ,  A61K31/00 ,  A61K31/435

CPC分类号： A61K31/44 ,  A61K31/00 ,  A61K31/10 ,  A61K31/18 ,  A61K31/381 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/42 ,  A61K31/426 ,  A61K31/427 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/635 ,  A61K2300/00

摘要： This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing cardiovascular disorders.

公开(公告)号：EP0859642A2

公开(公告)日：1998-08-26

申请号：EP96939457.0

申请日：1996-10-16

申请人： G.D. SEARLE & CO.

发明人： ISAKSON, Peter, C. ,  SEIBERT, Karen ,  TALLEY, John, J.

IPC分类号： C07D231 ,  A61K31 ,  A61K49 ,  A61K51 ,  C07D261 ,  C07D263

CPC分类号： A61K49/06 ,  A61K51/04 ,  A61K51/0453 ,  A61K51/0455 ,  A61K2123/00

摘要： The invention relates to a method of detecting concentrations of cyclooxygenase-2 in a mammal, the method comprising: a) administering to the mammal a diagnostically effective amount of a cyclooxygenase-2 selective agent, which is capable of being detected in vivo; and b) detecting the agent so the concentration of cyclooxygenase-2 is detected.

公开(公告)号：EP0809636B1

公开(公告)日：2002-09-04

申请号：EP96904614.3

申请日：1996-02-12

申请人： G.D. SEARLE & CO.

发明人： ROGERS, Roland, S. ,  TALLEY, John, J. ,  BROWN, David, L. ,  NAGARAJAN, Srinivasan ,  CARTER, Jeffery, S. ,  WEIER, Richard, M. ,  STEALEY, Michael, A. ,  COLLINS, Paul, W. ,  SEIBERT, Karen ,  GRANETO, Matthew, J. ,  XU, Xiangdong ,  PARTIS, Richard

IPC分类号： C07D261/08 ,  C07D413/04 ,  C07D261/18 ,  C07D261/12 ,  C07D261/10 ,  A61K31/42

CPC分类号： C07D261/10 ,  C07D261/08 ,  C07D261/12 ,  C07D261/18 ,  C07D413/04

摘要： A class of substituted isoxazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula (III) whrein R7 is selected from hydroxyl, lower alkyl, carboxyl, halo, lower carboxyalkyl, lower alkoxycarbonylalkyl, lower alkoxyalkyl, lower carboxyalkoxyalkyl, lower haloalkyl, lower haloalkylsulfonyloxy, lower hydroxylalkyl, lower aryl (hydroxylalkyl), lower carboxyaryloxyalkyl, lower alkoxycarbonylaryloxyalkyl, lower cycloalkyl, lower cycloalkylalkyl, and lower aralkyl; and wherein R8 is one or more radicals independently selected from hydrido, lower alkylsulfinyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower hydroxyalkyl, lower haloalkoxy, amino, lower alkylamino, lower arylamino, lower aminoalkyl, nitro, halo, lower alkoxy, aminosulfonyl, and lower alkylthio; or a pharmaceutically-acceptable salt thereof.

公开(公告)号：EP0932402A1

公开(公告)日：1999-08-04

申请号：EP97911746.0

申请日：1997-10-14

申请人： G.D. SEARLE & CO.

发明人： SEIBERT, Karen ,  MASFERRER, Jaime ,  GORDON, Gary, B.

IPC分类号： C07D ,  C07D233 ,  A61K31 ,  A61K45 ,  A61P35 ,  A61P43 ,  C07D213 ,  C07D231 ,  C07D261 ,  C07D263 ,  C07D277 ,  C07D401 ,  C07D417

CPC分类号： A61K31/635 ,  A61K31/10 ,  A61K31/18 ,  A61K31/415 ,  A61K31/4164 ,  A61K31/4178 ,  A61K31/42 ,  A61K31/421 ,  A61K31/426 ,  A61K31/4418 ,  A61K31/4439

摘要： This invention relates to the use of cyclooxygenase-2 inhibitors or derivatives thereof in preventing and treating neoplasia. In particular, the invention describes the method of preventing and treating epithelial cell neoplasia in a subject, said method comprising treating the subject with a therapeutically-effective amount of a compound of Formula (I) wherein A, R?2 and R3¿ are as described in the specification.