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24 条记录 (耗时 0.019 秒)

    HETEROCYCLO-SUBSTITUTED IMIDAZOLES FOR THE TREATMENT OF INFLAMMATION
    1.
    发明授权
    HETEROCYCLO-SUBSTITUTED IMIDAZOLES FOR THE TREATMENT OF INFLAMMATION 失效
    杂环取代的咪唑代替炎症的治疗

    公开(公告)号：EP0880504B1

    公开(公告)日：2003-04-02

    申请号：EP97901952.8

    申请日：1997-01-24

    申请人： G.D. SEARLE & CO.

    发明人： KHANNA, Ish, K. ,  WEIER, Richard, M. ,  COLLINS, Paul, W. ,  YU, Ui ,  XU, Xiangdong ,  PARTIS, Richard, A. ,  KOSZYK, Francis, J. ,  HUFF, Renee, M.

    IPC分类号： C07D233/54 ,  A61K31/415 ,  C07D233/32 ,  C07D233/90 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

    CPC分类号： C07D233/64 ,  C07D233/32 ,  C07D233/90 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

    摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (V), wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R?13 and R14¿ are independently selected from aryl and heterocyclo, wherein R?13 and R14¿ are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R?13 and R14¿ is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof.

    HETEROCYCLO-SUBSTITUTED IMIDAZOLES FOR THE TREATMENT OF INFLAMMATION
    2.
    发明公开
    HETEROCYCLO-SUBSTITUTED IMIDAZOLES FOR THE TREATMENT OF INFLAMMATION 失效
    杂环取代的咪唑代替炎症的治疗

    公开(公告)号：EP0880504A1

    公开(公告)日：1998-12-02

    申请号：EP97901952.0

    申请日：1997-01-24

    申请人： G.D. SEARLE & CO.

    发明人： KHANNA, Ish, K. ,  WEIER, Richard, M. ,  COLLINS, Paul, W. ,  YU, Ui ,  XU, Xiangdong ,  PARTIS, Richard, A. ,  KOSZYK, Francis, J. ,  HUFF, Renee, M.

    IPC分类号： A61K31 ,  A61P29 ,  C07D233 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D413 ,  C07D417

    CPC分类号： C07D233/64 ,  C07D233/32 ,  C07D233/90 ,  C07D401/04 ,  C07D401/12 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D413/04 ,  C07D417/04

    摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (V), wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, heteroaralkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heterocyclocarbonyl, cyanoalkyl, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, carboxyl, aminocarbonyl, alkylaminocarbonyl, alkylaminocarbonylalkyl, heteroarylalkoxyalkyl, heteroaryloxyalkyl, heteroarylthioalkyl, aralkoxy, aralkylthio, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, arylthio, aryloxy, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl; wherein R4 is a radical selected from hydrido, alkyl and halo; and wherein R?13 and R14¿ are independently selected from aryl and heterocyclo, wherein R?13 and R14¿ are optionally substituted at a substitutable position with one or more radicals independently selected from alkylsulfonyl, aminosulfonyl, halo, alkylthio, alkyl, cyano, carboxyl, alkoxycarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, alkoxyalkyl, haloalkoxy, amino, alkylamino, arylamino and nitro; provided at least one of R?13 and R14¿ is aryl substituted with alkylsulfonyl or aminosulfonyl; or a pharmaceutically-acceptable salt thereof.

    4,5-SUBSTITUTED IMIDAZOLYL COMPOUNDS FOR THE TREATMENT OF INFLAMMATION
    3.
    发明公开
    4,5-SUBSTITUTED IMIDAZOLYL COMPOUNDS FOR THE TREATMENT OF INFLAMMATION 失效
    4,5-取代的咪唑基化合物用于治疗炎症

    公开(公告)号：EP0772601A1

    公开(公告)日：1997-05-14

    申请号：EP95929327.0

    申请日：1995-07-27

    申请人： G.D. SEARLE & CO.

    发明人： WEIER, Richard, M. ,  COLLINS, Paul, W. ,  STEALEY, Michael, A. ,  BARTA, Thomas E., Apartment 3-W ,  HUFF, Renee, M.

    IPC分类号： A61P29 ,  C07D233 ,  C07D401 ,  C07D405 ,  C07D409

    CPC分类号： C07D233/64 ,  C07D233/84 ,  C07D401/04 ,  C07D401/12 ,  C07D405/04 ,  C07D409/04

    摘要： A class of compounds is described for treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by formula (I), wherein R1 is selected from lower alkyl, lower haloalkyl, lower hydroxyalkyl, lower alkoxyalkyl, lower alkenyloxyalkyl, mercapto, lower alkylcarbonyl, lower haloalkylcarbonyl, phenylcarbonyl, lower aralkylcarbonyl, lower aralkenyl, lower aryloxyalkyl, lower aralkyloxyalkyl, lower arylsulfonyl, lower aralkylsulfonyl, lower arylthioalkyl, lower heteroarylalkylthioalkyl, and heteroaryl selected from 2-thienyl, 2-furyl, 3-furyl, 2-pyridyl, 4-pyridyl and 2-benzofuryl; wherein R?2 and R3¿ are independently selected from heteroaryl, cycloalkyl and aryl, wherein the heteroaryl, cycloalkyl and aryl radicals are substituted at a substitutable position with one or more radicals selected from hydrido, halo, lower alkylthio, lower alkylsulfinyl, lower alkylsulfonyl, aminosulfonyl, lower alkyl, cyano, carboxyl, lower alkoxycarbonyl, lower haloalkyl, hydroxyl, lower alkoxy, lower hydroxyalkyl, lower alkoxyalkyl, lower haloalkoxy, amino, lower alkylamino, phenylamino and nitro; and wherein R4 is selected from hydrido, lower alkyl and acyl; or a pharmaceutically acceptable salt thereof.

    1H/3H-[4-(N,N-CYCLOALKYL AND/OR BRANCHED-ALKYLCARBOXAMIDO) -BENZYL]IMIDAZO[4,5-c]PYRIDINES AS PAF ANTAGONISTS
    4.
    发明授权
    1H/3H-[4-(N,N-CYCLOALKYL AND/OR BRANCHED-ALKYLCARBOXAMIDO) -BENZYL]IMIDAZO[4,5-c]PYRIDINES AS PAF ANTAGONISTS 失效
    1H / -3H- [4-（N，N-环烷基和/或支链的烷基甲酰胺基） - 苄基] IMDAZO [4,5-C]吡啶作为PAF拮抗剂。

    公开(公告)号：EP0404797B1

    公开(公告)日：1995-02-01

    申请号：EP89903310.4

    申请日：1989-03-15

    申请人： G.D. Searle & Co.

    发明人： WEIER, Richard, M. ,  KHANNA, Ish, K.

    IPC分类号： C07D471/04 ,  A61K31/435

    CPC分类号： C07D471/04

    摘要： Certain N-dicycloalkyl or N-branched-alkylbenzamides of imidazo[4,5-c]pyridines are useful in treatment of platelet dysfunction or hyperactivity by inhibiting PAF-induced platelet aggregation. Compounds of particular interest are those of formula (I), wherein Y is hydrido at all substitutable phenyl ring positions or is fluoro or methoxy at the 2- or 6-positions of the phenyl ring, and wherein each of R1 and R2 is independently selected from cycloalkyl and branched alkyl.

    1,2-SUBSTITUTED IMIDAZOLYL COMPOUNDS FOR THE TREATMENT OF INFLAMMATION
    7.
    发明公开
    1,2-SUBSTITUTED IMIDAZOLYL COMPOUNDS FOR THE TREATMENT OF INFLAMMATION 失效
    1,2-取代的咪唑基FOR炎症的治疗

    公开(公告)号：EP0772600A1

    公开(公告)日：1997-05-14

    申请号：EP95928164.0

    申请日：1995-07-27

    申请人： G.D. SEARLE & CO.

    发明人： KHANNA, Ish, K. ,  WEIER, Richard, M. ,  COLLINS, Paul, W. ,  YU, Yi ,  XU, Xiangdong ,  HUFF, Renee, M. ,  PARTIS, Richard, A. ,  KOSZYK, Francis, J.

    IPC分类号： C07D233 ,  A61K31 ,  A61P25 ,  A61P29 ,  A61P43 ,  C07D401 ,  C07D403 ,  C07D405 ,  C07D409 ,  C07D419

    CPC分类号： C07D233/64 ,  C07D233/32 ,  C07D233/90 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D409/04 ,  C07D419/04

    摘要： A class of imidazolyl compounds is described for use in treating inflammation. Compounds of particular interest are defined by formula (II), wherein R3 is a radical selected from hydrido, alkyl, haloalkyl, aralkyl, heterocycloalkyl, acyl, cyano, alkoxy, alkylthio, alkylthioalkyl, alkylsulfonyl, cycloalkyloxy, cycloalkyloxyalkyle, cycloalkylthio, cycloalkylthioalkyl, cycloalkylsulfonyl, cyanoalkyl, cycloalkylsulfonylalkyl, haloalkylsulfonyl, azidoalkyl, arylsulfonyl, halo, hydroxyalkyl, alkoxyalkyl, arylthio, alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, aryloxy, heterocycloalkylcarbonyl, alkylaminoalkyl, N-arylaminoalkyl, N-alkyl-N-arylaminoalkyl, carboxyalkyl, alkoxycarbonylalkyl, alkoxycarbonyl, haloalkylcarbonyl, aminocarbonyl, alkylaminocarbonylalkyl, aralkylthio, heteroarylalcoxyalkyl, heteroaryloxyalkyl, aralkoxy, heteroarylthioalkyl, heteroaralkoxy, heteroaralkylthio, heteroarylalkylthioalkyl, heteroaryloxy, heteroarylthio, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, aryl and heteroaryl, wherein the aryl and heteroaryl radicals are optionally substitued at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsufinyl, alkyl, cyano, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl and haloalkoxy; wherein R7 is a radical selected from alkyl and amino; and wherein R8 is one or more radicals selected from hydrido, halo, alkyl, haloalkyl, alkoxy, amino, haloalkoxy, cyano, carboxyl, hydroxyl, hydroxyalkyl, alkoxyalkyl, alkylamino, nitro and alkylthio.

    3(5)-HETEROARYL SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS
    10.
    发明公开
    3(5)-HETEROARYL SUBSTITUTED PYRAZOLES AS p38 KINASE INHIBITORS 失效
    4-芳基-3-（5） - 杂芳基取代的吡唑作为p38激酶抑制剂的

    公开(公告)号：EP0983260A2

    公开(公告)日：2000-03-08

    申请号：EP98924924.8

    申请日：1998-05-22

    申请人： G.D. Searle & Co.

    发明人： ANANTANARAYAN, Ashok ,  CLARE, Michael ,  GENG, Lifeng ,  HANSON, Gunnar, J. ,  PARTIS, Richard, A. ,  STEALEY, Michael, A. ,  WEIER, Richard, M.

    IPC分类号： C07D401/00

    CPC分类号： C07D401/04 ,  C07D401/14

    摘要： A class of pyrazole derivatives is described for use in treating p38 kinase mediated disorders. Compounds of particular interest are defined by Formula (I), wherein R?1 and R2¿ are as described in the specification; and Ar1 is aryl optionally substituted with one or more radicals independently selected from halo, alkyl, alkenyl, alkynyl, alkoxy, alkenoxy, alkyldioxy, alkylthio, alkylsulfinyl, alkylsulfonyl, amino, aminocarbonyl, cyano, alkoxycarbonyl, formyl, aminosulfonyl, alkylamino, nitro, arylamino, alkylcarbonylamino, halosulfonyl, aminoalkyl, and haloalkyl; and HetAr2 is pyridinyl, pyrimidinyl or quinolinyl optionally substituted with one or more radicals independently selected from alkylthio, alkylsulfonyl, alkylsulfinyl, halo, alkyl, heterocyclyl, alkoxy, aralkoxy, haloalkyl, amino, cyano, aralkyl, alkylamino, cycloalkylamino, cycloalkenylamino, arylamino, alkynylamino, and aralkylamino; or a pharmaceutically-acceptable salt or a tautomer thereof.