申请人:Dainippon Pharmaceutical Co., Ltd.
公开号:EP1403235A1
公开(公告)日:2004-03-31
N-Arylphenylacetamide derivatives represented by the following formula [I]:
(wherein R1 is C1-6 alkoxy, etc.; R2 is hydrogen, -(CH2)m-N(R6)(R7) (m is an integer of from 1 to 4; R6 is hydrogen, C1-4 alkyl, etc., R7 is hydrogen, etc.), etc.; R3 is hydrogen, halogen, etc.; R4 is C6-10 alkyl, -Y-R8 (Y is a single bond, C1-6 alkylene, C2-6 alkenylene, C2-6 alkynylene, etc., R8 is aryl, C3-8 cycloalkyl, C6-15 polycycloalkyl, etc.), etc.; R5 is hydrogen, etc.; and X1 is hydrogen), or pharmaceutically acceptable salts thereof or hydrates or solvates of the same, and a pharmaceutical composition containing the same. These compounds are useful as preventives and/or remedies giving no pain at the early stage of administration, which are efficacious in oral administration and have potent analgesic and antiinflammatory effects.
下式[I]代表的 N-芳基苯乙酰胺衍生物:
(其中 R1 是 C1-6 烷氧基等;R2 是氢、-(CH2)m-N(R6)(R7)(m 是 1 至 4 的整数;R6 是氢、C1-4 烷基等,R7 是氢等)等;R3 是氢、卤素等;R4 是 C6-10 烷基、-Y-R8(Y 是单键、C1-6 烯基、C2-6 烯基、C2-6 烯炔基等、R8为芳基、C3-8环烷基、C6-15多环烷基等)等;R5为氢等;X1为氢),或其药学上可接受的盐或其水合物或溶液,以及含有这些化合物的药物组合物。这些化合物可作为预防药物和/或治疗药物,用药初期无疼痛感,口服有效,并具有强效镇痛和抗炎作用。