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    • 23. 发明申请
    • 3-PYRAZOLECARBOXAMIDE DERIVATIVES HAVING CANNABINOID RECEPTOR AFFINITY
    • 具有CANNABINOID受体亲和力的3-吡咯烷酰胺衍生物
    • WO1997021682A1
    • 1997-06-19
    • PCT/FR1996001953
    • 1996-12-06
    • SANOFIBARTH, FrancisCASELLAS, PierreMILLAN, JosephOUSTRIC, DidierRINALDI, MurielleSARRAN, Martine
    • SANOFI
    • C07D231/14
    • C07D231/14
    • Compounds of formula (I), wherein X1 is a -NR1R2 or -OR2 group; each of g2, g3, g4, g5, g6, w2, w3, w4, w5 and w6, which are the same or different, is hydrogen, a halogen atom, (C1-4) alkyl, (C1-4) alkoxy, trifluoromethyl, nitro or (C1-4) alkylthio, with the proviso that at least one of substituents g2, g3, g4, g5, g6 and at least one of substituents w2, w3, w4, w5 and w6 is other than hydrogen; R1 is hydrogen or (C1-4) alkyl; R2 is a non-aromatic (C3-15) carbocyclic radical optionally substituted one or more times by a substituent selected from a halogen atom, (C1-4) alkyl or (C1-4) alkoxy; R3 is hydrogen or a -CH2-R6 group; each of R4 and R5 is independently hydrogen, (C1-4) alkyl or trifluoromethyl; or R4 is hydrogen and R5 and w6 together form an ethylene or trimethylene radical; R6 is hydrogen or, when substituents g2, g3, g4, g5 and/or g6 are not (C1-4) alkyl, R6 is hydrogen, (C1-4) alkyl, fluorine, hydroxy, (C1-5) alkoxy, (C1-5) alkylthio, hydroxy (C1-5) alkoxy, cyano, (C1-5) alkylsulphinyl or (C1-5) alkylsulphonyl; and salts thereof; a method for preparing same and pharmaceutical compositions containing said compounds, are disclosed. Said compounds have excellent CB2 receptor affinity.
    • 式(I)的化合物,其中X 1是-NR 1 R 2或-OR 2基团; g2,g3,g4,g5,g6,w2,w3,w4,w5和w6各自相同或不同,为氢,卤素原子,(C1-4)烷基,(C1-4)烷氧基, 三氟甲基,硝基或(C 1-4)烷硫基,条件是取代基g2,g3,g4,g5,g6和至少一个取代基w2,w3,w4,w5和w6中的至少一个不是氢; R1是氢或(C1-4)烷基; R2是选自卤素原子,(C1-4)烷基或(C1-4)烷氧基的取代基任意取代一次或多次的非芳香族(C 3-15)碳环基; R3是氢或-CH2-R6基团; R 4和R 5各自独立地为氢,(C 1-4)烷基或三氟甲基; 或R4是氢,R5和w6一起形成乙烯或三亚甲基; 当取代基g2,g3,g4,g5和/或g6不为(C1-4)烷基时,R6为氢,(C1-4)烷基,氟,羟基,(C1-5)烷氧基,( C 1-5)烷硫基,羟基(C 1-5)烷氧基,氰基,(C 1-5)烷基亚磺酰基或(C 1-5)烷基磺酰基; 及其盐; 公开了其制备方法和含有所述化合物的药物组合物。 所述化合物具有优异的CB2受体亲和力。