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    3-pyrazolecarboxamide derivatives having cannabinoid receptor affinity
    3.
    发明授权
    3-pyrazolecarboxamide derivatives having cannabinoid receptor affinity 失效
    具有大麻素受体亲和力的3-吡唑酰胺衍生物

    公开(公告)号：US5925768A

    公开(公告)日：1999-07-20

    申请号：US77767

    申请日：1998-06-03

    申请人： Francis Barth ,  Pierre Casellas ,  Joseph Millan ,  Didier Oustric ,  Murielle Rinaldi ,  Martine Sarran

    发明人： Francis Barth ,  Pierre Casellas ,  Joseph Millan ,  Didier Oustric ,  Murielle Rinaldi ,  Martine Sarran

    IPC分类号： A61K31/00 ,  A61K31/415 ,  A61P37/00 ,  A61P37/02 ,  A61P43/00 ,  C07D231/14

    CPC分类号： C07D231/14

    摘要： The present invention relates to compounds of the formula ##STR1## in which: X.sub.1 is a group --NR.sub.1 R.sub.2 or a group --OR.sub.2 ;g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are identical or different and are each independently hydrogen, a halogen atom, a (C.sub.1 -C.sub.4)alkyl, a (C.sub.1 -C.sub.4)alkoxy, a trifluoromethyl, a nitro or a (C.sub.1 -C.sub.4)alkylthio, with the proviso that at least one of the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5, g.sub.6 and at least one of the substituents w.sub.2, w.sub.3, w.sub.4, w.sub.5, w.sub.6 are other than hydrogen;R.sub.1 is hydrogen or a (C.sub.1 -C.sub.4)alkyl;R.sub.2 is a non-aromatic (C.sub.3 -C.sub.15)carbocyclic radical which is unsubstituted or monosubstituted or polysubstituted by a substituent selected from a halogen atom, a (C.sub.1 -C.sub.4)alkyl and a (C.sub.1 -C.sub.4)alkoxy;R.sub.3 is hydrogen or a group --CH.sub.2 R.sub.6 ; andR.sub.4 and R.sub.5 are each independently a hydrogen, a (C.sub.1 -C.sub.4)alkyl or a trifluoromethyl;or else R.sub.4 is hydrogen and R.sub.5 and w.sub.6 together constitute an ethylene or trimethylene radical; andR.sub.6 is hydrogen, a (C.sub.1 -C.sub.4)alkyl, a fluorine, a hydroxyl, a (C.sub.1 -C.sub.5)alkoxy, a (C.sub.1 -C.sub.5)alkylthio, a hydroxy(C.sub.1 -C.sub.5)alkoxy, a cyano, a (C.sub.1 -C.sub.5)alkylsulfinyl or a (C.sub.1 -C.sub.5)alkylsulfonyl with the proviso that when the substituents g.sub.2, g.sub.3, g.sub.4, g.sub.5 and/or g.sub.6 are a (C.sub.1 -C.sub.4)alkyl R.sub.6 is only hydrogen;to a process for their preparation and to the pharmaceutical compositions in which they are present.These compounds have a good affinity for the peripheral cannabinoid receptors.

    摘要翻译： PCT No.PCT / FR96 / 01953 Sec。 371日期1998年6月3日第 102（e）1998年6月3日PCT PCT 1996年12月6日PCT公布。 公开号WO97 / 21682 日期：1997年6月19日本发明涉及下式的化合物，其中：X 1为基团-NR 1 R 2或基团-OR 2; g2，g3，g4，g5，g6和w2，w3，w4，w5，w6相同或不同，各自独立地为氢，卤素原子，（C1-C4）烷基，（C1-C4）烷氧基， 三氟甲基，硝基或（C 1 -C 4）烷硫基，条件是至少一个取代基g2，g3，g4，g5，g6和至少一个取代基w2，w3，w4，w5，w6是其他 比氢; R1是氢或（C1-C4）烷基; R 2是未被取代或被选自卤素原子，（C 1 -C 4）烷基和（C 1 -C 4）烷氧基的取代基单取代或多取代的非芳族（C 3 -C 15）碳环基团; R3是氢或基团-CH2R6; 和R 4和R 5各自独立地为氢，（C 1 -C 4）烷基或三氟甲基; 或者R4是氢，R5和w6一起构成乙烯或三亚甲基; （C 1 -C 5）烷氧基，（C 1 -C 5）烷硫基，羟基（C 1 -C 5）烷氧基，氰基，（C 1 -C 5）烷氧基， -C 5）烷基亚磺酰基或（C 1 -C 5）烷基磺酰基，条件是当取代基g2，g3，g4，g5和/或g6为（C1-C4）烷基时，R6仅为氢; 涉及其制备方法及其存在的药物组合物。 这些化合物对外周大麻素受体具有良好的亲和力。