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    • 1. 发明公开
    • Compositions comprising a Cyclooxygenase-2 Inhibitor and a Leukotriene B4 receptor antagonist
    • Zubereitungen enthaltend einen cyclooxygenase-2-Inhibitor and einen leukotrien-b4-Rezeptor Antagonisten
    • EP1640003A2
    • 2006-03-29
    • EP05003990.8
    • 1997-02-11
    • G.D. Searle & Co.
    • Gregory, Susan A.Isakson, Peter CAnderson, Gary
    • A61K31/4164A61K31/4178A61K38/13A61P37/06
    • A61K31/10A61K31/00A61K31/18A61K31/4164A61K31/4178A61K38/13A61K45/06A61K2300/00
    • Use of a leukotriene B 4 receptor antagonist and a cyclooxygenase-2 inhibitor,
      wherein the cyclooxygenase-2 inhibitor is selected from compounds of Formula I:
         
      wherein A is pyrazolyl;
      wherein R 1 is at least one substituent selected from heterocyclo, cycloalkyl, cycloalkenyl and aryl, wherein R 1 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 R 2 is selected from alkyl and amino; and
      wherein R 3 is a radical selected from halo, alkyl, alkenyl, alkynyl, oxo, cyano, carboxyl, cyanoalkyl, heterocyclooxy, alkyloxy, alkylthio, alkylcarbonyl, cycloalkyl, aryl, haloalkyl, heterocyclo, cycloalkenyl, aralkyl, heterocycloalkyl, acyl, alkylthioalkyl, hydroxyalkyl, alkoxycarbonyl, arylcarbonyl, aralkylcarbonyl, aralkenyl, alkoxyalkyl, arylthioalkyl, aryloxyalkyl, aralkylthioalkyl, aralkoxyalkyl, alkoxyaralkoxyalkyl, alkoxycarbonylalkyl, aminocarbonyl, aminocarbonylalkyl, alkylaminocarbonyl, N-arylaminocarbonyl, N-alkyl-N-arylaminocarbonyl, alkylaminocarbonylalkyl, carboxyalkyl, 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;
          or a pharmaceutically-acceptable salt thereof, for preparing a medicament to suppress immune, acute or delayed-type hypersensitivity response in a subject.
    • 使用白三烯B 4受体拮抗剂和环加氧酶-2抑制剂,其中所述环加氧酶-2抑制剂选自式I化合物:其中A为吡唑基; 其中R 1是选自杂环基,环烷基,环烯基和芳基中的至少一个取代基,其中R 1任选地在可取代位置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选自烷基和氨基; 并且其中R 3是选自卤素,烷基,烯基,炔基,氧代,氰基,羧基,氰基烷基,杂环氧基,烷氧基,烷硫基,烷基羰基,环烷基,芳基,卤代烷基,杂环基,环烯基,芳烷基,杂环烷基,酰基,烷硫基烷基 羟烷基,烷氧羰基,芳基羰基,芳烷基羰基,芳烯基,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,烷氧基烷氧基烷基,烷氧基羰基烷基,氨基羰基,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,羧基烷基,烷基氨基,N 芳基氨基,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; 用于制备抑制受试者中的免疫,急性或迟发型超敏反应的药物的ƒ€ƒ€或其药学上可接受的盐。