公开(公告)号：EP0679157B1

公开(公告)日：1997-11-19

申请号：EP94906625.2

申请日：1994-01-14

申请人： G.D. SEARLE & CO. ,  THE MONSANTO COMPANY

发明人： BERTENSHAW, Stephen, R. ,  COLLINS, Paul, W. ,  PENNING, Thomas, D. ,  REITZ, David, B. ,  ROGERS, Roland, S.

IPC分类号： C07D333/18 ,  C07D333/16 ,  C07D333/28 ,  C07D333/38 ,  C07D307/38 ,  C07D409/04 ,  A61K31/38 ,  A61K31/44 ,  A61K31/34

CPC分类号： C07D409/04 ,  A61K31/341 ,  A61K31/365 ,  C07D307/38 ,  C07D307/58 ,  C07D333/16 ,  C07D333/18 ,  C07D333/28 ,  C07D333/38

摘要： A class of 3,4-diaryl substitued thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (I), wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R?2 and R3¿ are independently aryl or heteroaryl; and wherein R?2 and R3¿ are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.

公开(公告)号：EP0679157A1

公开(公告)日：1995-11-02

申请号：EP94906625.0

申请日：1994-01-14

申请人： G.D. SEARLE & CO. ,  THE MONSANTO COMPANY

发明人： BERTENSHAW, Stephen, R. ,  COLLINS, Paul, W. ,  PENNING, Thomas, D. ,  REITZ, David, B. ,  ROGERS, Roland, S.

IPC分类号： C07D333 ,  A61K31 ,  A61P19 ,  A61P29 ,  A61P43 ,  C07C311 ,  C07C317 ,  C07D207 ,  C07D213 ,  C07D307 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07D417 ,  C07D471 ,  C07D487

CPC分类号： C07D409/04 ,  A61K31/341 ,  A61K31/365 ,  C07D307/38 ,  C07D307/58 ,  C07D333/16 ,  C07D333/18 ,  C07D333/28 ,  C07D333/38

摘要： A class of 3,4-diaryl substitued thiophene, furan and pyrrole derivatives and analogs thereof, pharmaceutical compositions containing them and methods of using them to treat inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (I), wherein Y is selected from O, S and NR1; wherein R1 is selected from hydrido and lower alkyl; wherein X is one or two substituent selected from hydrido, halo, lower alkoxycarbonyl and carboxyl; wherein R?2 and R3¿ are independently aryl or heteroaryl; and wherein R?2 and R3¿ are optionally substituted at a substitutable position with one or more radicals selected from sulfamyl, alkylsulfonyl, halo, lower alkoxy and lower alkyl; or a pharmaceutically-acceptable salt thereof.

公开(公告)号：EP0731795B1

公开(公告)日：1999-12-22

申请号：EP95902444.9

申请日：1994-11-14

申请人： G.D. SEARLE & CO.

发明人： TALLEY, John, J. ,  PENNING, Thomas, D. ,  COLLINS, Paul, W. ,  ROGIER, Donald, J., Jr. ,  MALECHA, James, W. ,  MIYASHIRO, Julie M. ,  BERTENSHAW, Stephen, R. ,  KHANNA, Ish, K. ,  GRANETS, Matthew, J. ,  ROGERS, Roland, S. ,  CARTER, Jeffery, S. ,  DOCTER, Stephen, H. ,  YU, Stella, S.

IPC分类号： C07D231/12 ,  A61K31/415 ,  C07D231/14 ,  C07D231/16 ,  C07D231/18 ,  C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D495/04

CPC分类号： C07D495/04 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04

摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), whrein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R?2 and R3¿ are not both hydrido; further provided that R2 is not carboxyl or methyl when R3 is hydrido and when R4 is phenyl; further provided that R4 is not triazolyl when R2 is methyl; further provided that R4 is not aralkenyl when R2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R4 is not phenyl when R2 is methyl and R3 is carboxyl; and further provided that R4 is not unsubstituted thienyl when R2 is trifluoromethyl; or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP0977748A1

公开(公告)日：2000-02-09

申请号：EP98918305.8

申请日：1998-04-18

申请人： G.D. SEARLE & CO.

发明人： CARTER, Jeffery, S. ,  OBUKOWICZ, Mark, G. ,  DEVADAS, Balekudru ,  TALLEY, John, J. ,  BROWN, David, L. ,  GRANETO, Matthew, J. ,  BERTENSHAW, Stephen, R. ,  ROGIER, Donald, J., Jr. ,  NAGARAJAN, Srinivasan, R. ,  HANAU, Cathleen, E. ,  HARTMANN, Susan, J. ,  LUDWIG, Cindy, L. ,  METZ, Suzanne

IPC分类号： C07D311/58 ,  C07D335/06 ,  C07D215/54 ,  C07D311/92 ,  C07D493/04 ,  C07D409/04 ,  C07D491/04 ,  A61K31/35

CPC分类号： C07D335/06 ,  C07D215/54 ,  C07D311/22 ,  C07D311/58 ,  C07D311/92 ,  C07D401/12 ,  C07D405/04 ,  C07D407/04 ,  C07D407/12 ,  C07D409/04 ,  C07D471/04 ,  C07D491/04 ,  C07D493/04

摘要： A class of benzopyran derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula (I'), wherein X, A?1, A2, A3, A4¿, R, R', R?1 and R2¿ are as described in the specification.

公开(公告)号：EP0977748B1

公开(公告)日：2003-03-26

申请号：EP98918305.8

申请日：1998-04-18

申请人： G.D. SEARLE & CO.

发明人： CARTER, Jeffery, S. ,  OBUKOWICZ, Mark, G. ,  DEVADAS, Balekudru ,  TALLEY, John, J. ,  BROWN, David, L. ,  GRANETO, Matthew, J. ,  BERTENSHAW, Stephen, R. ,  ROGIER, Donald, J., Jr. ,  NAGARAJAN, Srinivasan, R. ,  HANAU, Cathleen, E. ,  HARTMANN, Susan, J. ,  LUDWIG, Cindy, L. ,  METZ, Suzanne

IPC分类号： C07D311/58 ,  C07D335/06 ,  C07D215/54 ,  C07D311/92 ,  C07D493/04 ,  C07D409/04 ,  C07D491/04 ,  A61K31/35

CPC分类号： C07D335/06 ,  C07D215/54 ,  C07D311/22 ,  C07D311/58 ,  C07D311/92 ,  C07D401/12 ,  C07D405/04 ,  C07D407/04 ,  C07D407/12 ,  C07D409/04 ,  C07D471/04 ,  C07D491/04 ,  C07D493/04

摘要： A class of benzopyran derivatives is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula (I'), wherein X, A?1, A2, A3, A4¿, R, R', R?1 and R2¿ are as described in the specification.

公开(公告)号：EP1123285A1

公开(公告)日：2001-08-16

申请号：EP99954621.1

申请日：1999-10-15

申请人： G.D. SEARLE & CO.

发明人： CARTER, Jeffery, S. ,  DEVADAS, Balekudru ,  TALLEY, John, J. ,  BROWN, David, L. ,  GRANETO, Matthew, J. ,  ROGIER, Donald, J., Jr. ,  NAGARAJAN, Srinivasan, R. ,  HANAU, Cathleen, E. ,  HARTMANN, Susan, J. ,  LUDWIG, Cindy, L. ,  METZ, Suzanne ,  KORTE, Donald, E. ,  BERTENSHAW, Stephen, R. ,  OBUKOWICZ, Mark, G.

IPC分类号： C07D311/58 ,  C07D335/06 ,  C07D215/54 ,  C07D311/92 ,  C07D493/04 ,  C07D409/04 ,  C07D491/04 ,  A61K31/35

CPC分类号： C07D215/54 ,  C07D311/22 ,  C07D311/58 ,  C07D311/92 ,  C07D335/06 ,  C07D401/12 ,  C07D405/04 ,  C07D407/04 ,  C07D407/12 ,  C07D409/04 ,  C07D471/04 ,  C07D491/04 ,  C07D493/04

摘要： A class of benzopyrans, benzothiopyrans, dihydroquinolines, dihydronaphthalenes, and analogs thereof, is described for use in treating cyclooxygenase-2 mediated disorders. Compounds of particular interest are defined by Formula (I') wherein X, A?1, A2, A3, A4¿, R, R'', R?1 and R2¿ are as described in the specification.

公开(公告)号：EP0731795A1

公开(公告)日：1996-09-18

申请号：EP95902444.0

申请日：1994-11-14

申请人： G.D. SEARLE & CO.

发明人： TALLEY, John, J. ,  PENNING, Thomas, D. ,  COLLINS, Paul, W. ,  ROGIER, Donald, J., Jr. ,  MALECHA, James, W. ,  MIYASHIRO, Julie M. ,  BERTENSHAW, Stephen, R. ,  KHANNA, Ish, K. ,  GRANETS, Matthew, J. ,  ROGERS, Roland, S. ,  CARTER, Jeffery, S. ,  DOCTER, Stephen, H. ,  YU, Stella, S.

IPC分类号： A61K31 ,  A61P5 ,  A61P9 ,  A61P19 ,  A61P25 ,  A61P29 ,  C07D231 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07D495

CPC分类号： C07D495/04 ,  C07D231/12 ,  C07D231/14 ,  C07D231/16 ,  C07D231/54 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04

摘要： A class of pyrazolyl benzenesulfonamide compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (II), whrein R2 is selected from hydrido, alkyl, haloalkyl, alkoxycarbonyl, cyano, cyanoalkyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, cycloalkylaminocarbonyl, arylaminocarbonyl, carboxyalkylaminocarbonyl, carboxyalkyl, aralkoxycarbonylalkylaminocarbonyl, aminocarbonylalkyl, alkoxycarbonylcyanoalkenyl and hydroxyalkyl; wherein R3 is selected from hydrido, alkyl, cyano, hydroxyalkyl, cycloalkyl, alkylsulfonyl and halo; and wherein R4 is selected from aralkenyl, aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R4 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfonyl, cyano, nitro, haloalkyl, alkyl, hydroxyl, alkenyl, hydroxyalkyl, carboxyl, cycloalkyl, alkylamino, dialkylamino, alkoxycarbonyl, aminocarbonyl, alkoxy, haloalkoxy, sulfamyl, heterocyclic and amino; provided R?2 and R3¿ are not both hydrido; further provided that R2 is not carboxyl or methyl when R3 is hydrido and when R4 is phenyl; further provided that R4 is not triazolyl when R2 is methyl; further provided that R4 is not aralkenyl when R2 is carboxyl, aminocarbonyl or ethoxycarbonyl; further provided that R4 is not phenyl when R2 is methyl and R3 is carboxyl; and further provided that R4 is not unsubstituted thienyl when R2 is trifluoromethyl; or a pharmaceutically acceptable salt thereof.

公开(公告)号：EP0731793A1

公开(公告)日：1996-09-18

申请号：EP95901778.0

申请日：1994-11-14

申请人： G.D. SEARLE & CO.

发明人： LEE, Len, F. ,  BERTENSHAW, Stephen, R.

IPC分类号： A61K31 ,  A61P25 ,  A61P29 ,  C07D231

CPC分类号： C07D231/12 ,  A61K31/415

摘要： A class of 1,5-diphenyl pyrazoles is described for the treatment of inflammation, including treatment of pain and disorders such as arthritis. Compounds of particular interest are of formula (I), wherein R1 is methylsulfonyl; wherein R2 is selected from -CF¿3?, -CF2Cl, -CF2H, -CF2CF3 and -CF2CF2CF3; and wherein R?3¿ is fluoro or chloro; or a pharmaceutically-acceptable salt thereof.

摘要翻译： 描述了一类1,5-二苯基吡唑类用于治疗炎症，包括治疗疼痛和失调如关节炎。 特别感兴趣的化合物具有式（I），其中R 1是甲基磺酰基; 其中R 2选自-CF 3，-CF 2 Cl，-CF 2 H，-CF 2 CF 3和-CF 2 CF 2 CF 3; 并且其中R 3是氟或氯; 或其药学上可接受的盐。