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    SUBSTITUTED THIAZOLES FOR THE TREATMENT OF INFLAMMATION
    3.
    发明公开
    SUBSTITUTED THIAZOLES FOR THE TREATMENT OF INFLAMMATION 失效
    取代噻唑用于炎症的治疗

    公开(公告)号：EP0772606A1

    公开(公告)日：1997-05-14

    申请号：EP95928145.0

    申请日：1995-07-26

    申请人： G.D. SEARLE & CO.

    发明人： TALLEY, John, J. ,  CARTER, Jeffery, S. ,  COLLINS, Paul, W. ,  KRAMER, Steven, W. ,  PENNING, Thomas, D. ,  ROGIER, Donald, J., Jr. ,  ROGERS, Roland, S.

    IPC分类号： C07D277 ,  A61K31 ,  A61P3 ,  A61P29 ,  C07D417

    CPC分类号： C07D417/04 ,  C07D277/26 ,  C07D277/30 ,  C07D277/42 ,  C07D277/56 ,  C07D417/12

    摘要： A class of substituted thiazolyl compounds is described for use in treating inflammation and inflammation-related disorders. Compounds of particular interest are defined by Formula (II), wherein R4 is selected from alkyl and amino, wherein R5 is selected from aryl, cycloalkyl, cycloalkenyl and heterocyclic; wherein R5 is optionally substituted at a substitutable position with one or more radicals selected from halo, alkylthio, alkylsulfinyl, alkylsulfonyl, haloalkylsulfonyl, aminosulfonyl, alkyl, alkenyl, alkynyl, cyano, carboxyl, carboxyalkyl, alkoxycarbonyl, aminocarbonyl, acyl, N-alkylaminocarbonyl, N-arylaminocarbonyl, N,N-dialkylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, haloalkyl, hydroxyl, alkoxy, hydroxyalkyl, haloalkoxy, amino, N-alkylamino, N,N-dialkylamino, heterocyclic and nitro; and wherein R6 is selected from halo, amino, alkoxy, nitro, hydroxyl, aminocarbonyl, acyl, alkylaminocarbonyl, arylaminocarbonyl, alkenyl, alkynyl, haloalkoxy, alkylamino, arylamino, aralkylamino, alkoxycarbonylalkyl, alkylaminoalkyl, heterocycloalkyl, aralkyl, cyanoalkyl, N-alkylsulfonylamino, heteroarylsulfonylalkyl, heteroarylsulfonylhaloalkyl, aryloxyalkyl, aralkyloxyalkyl, aryl and heterocyclo, wherein the aryl and heterocyclo radicals are optionally substituted at a substitutable position with one or more radicals selected from halo, alkyl, alkoxy, alkylthio, alkylsulfinyl, haloalkyl, haloalkoxy, carboxyalkyl, alkoxycarbonyl, aminocarbonyl, amino, acyl and alkylamino; or a pharmaceutically-acceptable salt thereof.

    N-[[4-(5-METHYL-3-PHENYLISOXAZOL-4-YL]PHENYL]SULFONYLPROPYLAMIDE and its SODIUMSALT AS PRODRUGS OF COX-2 INHIBITORS
    6.
    发明授权
    N-[[4-(5-METHYL-3-PHENYLISOXAZOL-4-YL]PHENYL]SULFONYLPROPYLAMIDE and its SODIUMSALT AS PRODRUGS OF COX-2 INHIBITORS 失效
    N - [[4-（5-甲基-3-苯基恶唑-4-基]苯基]苯基]丙基]氨基]苯并咪唑盐酸盐

    公开(公告)号：EP0892791B1

    公开(公告)日：2003-03-05

    申请号：EP97921092.9

    申请日：1997-04-11

    申请人： G.D. SEARLE & CO.

    发明人： TALLEY, John, J. ,  MALECHA, James, W. ,  BERTENSHAW, Stephen ,  GRANETO, Matthew, J. ,  CARTER, Jeffery, S. ,  LI, Jinglin ,  NAGARAJAN, Srinivasan ,  BROWN, David, L. ,  ROGIER, Donald, J., Jr. ,  PENNING, Thomas, D. ,  KHANNA, Ish, K. ,  XU, Xiangdong ,  WEIER, Richard, M.

    IPC分类号： C07D261/08 ,  C07D233/54 ,  C07D401/04 ,  A61K31/42 ,  A61K31/415 ,  C07D231/12 ,  C07D495/04 ,  C07D263/32 ,  C07C311/39 ,  C07D207/32 ,  C07D307/58

    CPC分类号： C07D207/33 ,  A61K31/18 ,  A61K31/415 ,  A61K31/42 ,  A61K31/635 ,  C07C311/16 ,  C07C311/51 ,  C07C2601/10 ,  C07D231/12 ,  C07D233/64 ,  C07D261/08 ,  C07D263/32 ,  C07D307/58 ,  C07D401/04 ,  C07D417/04 ,  C07D495/04

    摘要： Prodrugs of COX-2 inhibitors of formula (I) are described as being useful in treating inflammation and inflammation-related disorders wherein A is a ring substituent selected from partially unsaturated heterocyclyl, heteroaryl, cycloalkenyl and aryl, wherein A is optionally substituted at a substitutable position with one or more radicals selected from alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, carboxyl, alkoxy, aminocarbonyl, alkoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulfonyloxy, alkoxyalkyloxyalkyl, carboxyalkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, heterocyclyloxy, alkylthio, cycloalkyl, aryl, heterocyclyl, cycloalkenyl, aralkyl, heterocyclylalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, aralkenyl, alkoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonyl, N-arylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, alkylaminocarbonylalkyl, alkylamino, N-arylamino, N-aralkylamino, N-alkyl-N-aralkylamino, N-alkyl-N-arylamino, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-aralkylaminoalkyl, N-alkyl-N-aralkylaminoalkyl, N-alkyl-N-arylaminoalkyl, aryloxy, aralkoxy, arylthio, aralkylthio, alkylsulfinyl, alkylsulfonyl, aminosulfonyl, alkylaminosulfonyl, N-arylaminosulfonyl, arylsulfonyl, and N-alkyl-N-arylaminosulfonyl; wherein R1 is selected from heterocyclyl, cycloalkyl, cycloalkenyl and aryl, wherein R1 is optionally substituted at a substitutable position with one or more radicals selected from alkyl, haloalkyl, cyano, carboxyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, alkoxyalkyl, alkylsulfinyl, halo, alkoxy and alkylthio; wherein R2 is selected from hydrido and alkoxycarbonylalkyl; and wherein R3 is selected from alkyl, carboxyalkyl, acyl, alkoxycarbonyl, heteroarylcarbonyl, alkoxycarbonylalkylcarbonyl, alkoxycarbonylcarbonyl, amino acid residue, and alkylcarbonylaminoalkylcarbonyl; provided A is not tetrazolium, or pyridinum; and further provided A is not indanone when R3 is alkyl or carboxyalkyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了式（I）的COX-2抑制剂的前药可用于治疗炎症和炎症相关疾病，其中A是选自部分不饱和杂环基，杂芳基，环烯基和芳基的环取代基，其中A任选在可取代的 位置与一个或多个选自烷基羰基，甲酰基，卤素，烷基，卤代烷基，氧代，氰基，硝基，羧基，烷氧基，氨基羰基，烷氧基羰基，羧基烷基，氰基烷基，羟基烷基，卤代烷基磺酰氧基，烷氧基烷氧基烷基，羧烷氧基烷基，环烷基烷基，烯基，炔基， 芳烷基，芳烷基羰基，芳烷基，烷氧基烷基，芳硫基烷基，芳氧基烷基，芳烷硫基烷基，芳烷氧基烷基，烷氧基羰基烷基，氨基羰基烷基，烷基氨基羰基，N-芳基氨基羰基，N-烷基-N- 芳基氨基羰基，烷基氨基羰基烷基，烷基氨基，N-芳基 不是N-芳烷基氨基，N-烷基-N-芳烷基氨基，N-烷基-N-芳基氨基，氨基烷基，烷基氨基烷基，N-芳基氨基烷基，N-芳烷基氨基烷基，N-烷基-N-芳烷基氨基烷基，N-烷基-N-芳基氨基烷基， 芳氧基，芳烷氧基，芳硫基，芳烷硫基，烷基亚磺酰基，烷基磺酰基，氨基磺酰基，烷基氨基磺酰基，N-芳基氨基磺酰基，芳基磺酰基和N-烷基-N-芳基氨基磺酰基; 其中R 1选自杂环基，环烷基，环烯基和芳基，其中R 1在可取代位置任选被一个或多个选自烷基，卤代烷基，氰基，羧基，烷氧基羰基，羟基，羟基烷基， 卤代烷氧基，氨基，烷基氨基，芳基氨基，硝基，烷氧基烷基，烷基亚磺酰基，卤素，烷氧基和烷硫基; 其中R 2选自氢化和烷氧基羰基烷基; 其中R 3选自烷基，羧基烷基，酰基，烷氧基羰基，杂芳基羰基，烷氧基羰基烷基羰基，烷氧基羰基羰基，氨基酸残基和烷基羰基氨基烷基羰基。 提供A不是四唑或吡啶; 并且当R 3是烷基或羧基烷基时，A不是茚满酮; 或其药学上可接受的盐。

    SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES AS PRODRUGS OF COX-2 INHIBITORS
    10.
    发明公开
    SUBSTITUTED BENZENESULFONAMIDE DERIVATIVES AS PRODRUGS OF COX-2 INHIBITORS 失效
    替代苯甲酰胺衍生物ALS PRODROGEN VON COX-2 INHIBITOREN

    公开(公告)号：EP0892791A1

    公开(公告)日：1999-01-27

    申请号：EP97921092.0

    申请日：1997-04-11

    申请人： G.D. SEARLE & CO.

    发明人： TALLEY, John, J. ,  MALECHA, James, W. ,  BERTENSHAW, Stephen ,  GRANETO, Matthew, J. ,  CARTER, Jeffery, S. ,  LI, Jinglin ,  NAGARAJAN, Srinivasan ,  BROWN, David, L. ,  ROGIER, Donald, J., Jr. ,  PENNING, Thomas, D. ,  KHANNA, Ish, K. ,  XU, Xiangdong ,  WEIER, Richard, M.

    IPC分类号： C07D ,  C07D233 ,  A61K31 ,  A61P1 ,  A61P3 ,  A61P5 ,  A61P7 ,  A61P9 ,  A61P11 ,  A61P13 ,  A61P15 ,  A61P17 ,  A61P19 ,  A61P21 ,  A61P25 ,  A61P27 ,  A61P29 ,  A61P31 ,  A61P35 ,  A61P37 ,  A61P43 ,  C07C311 ,  C07D207 ,  C07D231 ,  C07D261 ,  C07D263 ,  C07D307 ,  C07D401 ,  C07D417 ,  C07D495

    CPC分类号： C07D207/33 ,  A61K31/18 ,  A61K31/415 ,  A61K31/42 ,  A61K31/635 ,  C07C311/16 ,  C07C311/51 ,  C07C2601/10 ,  C07D231/12 ,  C07D233/64 ,  C07D261/08 ,  C07D263/32 ,  C07D307/58 ,  C07D401/04 ,  C07D417/04 ,  C07D495/04

    摘要： Prodrugs of COX-2 inhibitors of formula (I) are described as being useful in treating inflammation and inflammation-related disorders wherein A is a ring substituent selected from partially unsaturated heterocyclyl, heteroaryl, cycloalkenyl and aryl, wherein A is optionally substituted at a substitutable position with one or more radicals selected from alkylcarbonyl, formyl, halo, alkyl, haloalkyl, oxo, cyano, nitro, carboxyl, alkoxy, aminocarbonyl, alkoxycarbonyl, carboxyalkyl, cyanoalkyl, hydroxyalkyl, haloalkylsulfonyloxy, alkoxyalkyloxyalkyl, carboxyalkoxyalkyl, cycloalkylalkyl, alkenyl, alkynyl, heterocyclyloxy, alkylthio, cycloalkyl, aryl, heterocyclyl, cycloalkenyl, aralkyl, heterocyclylalkyl, alkylthioalkyl, arylcarbonyl, aralkylcarbonyl, aralkenyl, alkoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, alkoxycarbonylalkyl, aminocarbonylalkyl, alkylaminocarbonyl, N-arylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, alkylaminocarbonylalkyl, alkylamino, N-arylamino, N-aralkylamino, N-alkyl-N-aralkylamino, N-alkyl-N-arylamino, aminoalkyl, alkylaminoalkyl, N-arylaminoalkyl, N-aralkylaminoalkyl, N-alkyl-N-aralkylaminoalkyl, N-alkyl-N-arylaminoalkyl, aryloxy, aralkoxy, arylthio, aralkylthio, alkylsulfinyl, alkylsulfonyl, aminosulfonyl, alkylaminosulfonyl, N-arylaminosulfonyl, arylsulfonyl, and N-alkyl-N-arylaminosulfonyl; wherein R1 is selected from heterocyclyl, cycloalkyl, cycloalkenyl and aryl, wherein R1 is optionally substituted at a substitutable position with one or more radicals selected from alkyl, haloalkyl, cyano, carboxyl, alkoxycarbonyl, hydroxyl, hydroxyalkyl, haloalkoxy, amino, alkylamino, arylamino, nitro, alkoxyalkyl, alkylsulfinyl, halo, alkoxy and alkylthio; wherein R2 is selected from hydrido and alkoxycarbonylalkyl; and wherein R3 is selected from alkyl, carboxyalkyl, acyl, alkoxycarbonyl, heteroarylcarbonyl, alkoxycarbonylalkylcarbonyl, alkoxycarbonylcarbonyl, amino acid residue, and alkylcarbonylaminoalkylcarbonyl; provided A is not tetrazolium, or pyridinum; and further provided A is not indanone when R3 is alkyl or carboxyalkyl; or a pharmaceutically-acceptable salt thereof.

    摘要翻译： 描述了式（I）的COX-2抑制剂的前药可用于治疗炎症和炎症相关疾病，其中A是选自部分不饱和杂环基，杂芳基，环烯基和芳基的环取代基，其中A任选在可取代的 位置与一个或多个选自烷基羰基，甲酰基，卤素，烷基，卤代烷基，氧代，氰基，硝基，羧基，烷氧基，氨基羰基，烷氧基羰基，羧基烷基，氰基烷基，羟基烷基，卤代烷基磺酰氧基，烷氧基烷氧基烷基，羧烷氧基烷基，环烷基烷基，烯基，炔基， 芳烷基，芳烷基羰基，芳烷基，烷氧基烷基，芳硫基烷基，芳氧基烷基，芳烷硫基烷基，芳烷氧基烷基，烷氧基羰基烷基，氨基羰基烷基，烷基氨基羰基，N-芳基氨基羰基，N-烷基-N- 芳基氨基羰基，烷基氨基羰基烷基，烷基氨基，N-芳基 不是N-芳烷基氨基，N-烷基-N-芳烷基氨基，N-烷基-N-芳基氨基，氨基烷基，烷基氨基烷基，N-芳基氨基烷基，N-芳烷基氨基烷基，N-烷基-N-芳烷基氨基烷基，N-烷基-N-芳基氨基烷基， 芳氧基，芳烷氧基，芳硫基，芳烷硫基，烷基亚磺酰基，烷基磺酰基，氨基磺酰基，烷基氨基磺酰基，N-芳基氨基磺酰基，芳基磺酰基和N-烷基-N-芳基氨基磺酰基; 其中R 1选自杂环基，环烷基，环烯基和芳基，其中R 1在可取代位置任选被一个或多个选自烷基，卤代烷基，氰基，羧基，烷氧基羰基，羟基，羟基烷基， 卤代烷氧基，氨基，烷基氨基，芳基氨基，硝基，烷氧基烷基，烷基亚磺酰基，卤素，烷氧基和烷硫基; 其中R 2选自氢化和烷氧基羰基烷基; 其中R 3选自烷基，羧基烷基，酰基，烷氧基羰基，杂芳基羰基，烷氧基羰基烷基羰基，烷氧基羰基羰基，氨基酸残基和烷基羰基氨基烷基羰基。 提供A不是四唑或吡啶; 并且当R 3是烷基或羧基烷基时，A不是茚满酮; 或其药学上可接受的盐。