申请人:Rhone-Poulenc Sante
公开号:US04720500A1
公开(公告)日:1988-01-19
Amides of formula ##STR1## in which either R is 2-quinolyl, substituted phenyl (substituted by Br, 3-Cl, CF.sub.3, alkyloxycarbonyl, 4-dialkylamino), dichlorophenyl, trialkyloxyphenyl, benzyl, styryl, benzoyl or anilino and R' is halogen, phenyl or anilino or R' is phenoxy or 4-chlorophenoxy when R is 2-quinolyl, substituted phenyl, trialkyloxyphenyl, benzyl or styryl or R' is 4-fluoro(or alkyloxy)phenyl when R is 4-trifluoromethyl (or dialkylamino)phenyl, or R' is 3-bromophenyl when R is anilino, or R is phenyl or alkyloxyphenyl and R' is phenyl, 4-chlorophenoxy, anilino or 1-pyrrolidinyl or R' is 2-(or 4-)chlorophenyl, 3-(or 4-)bromophenyl, 4-alkyloxyphenyl or 3,4-dichloro(or dibromo)phenyl when R is phenyl or R is 3-halophenyl and R' is 3-(or 4-)fluorophenyl, 3-(or 4-)bromophenyl, 4-chlorophenyl, 2-(or 3-)-alkyloxyphenyl, 3-alkylphenyl or 3,4-difluoro(dichloro or dibromo)phenyl, the straight-chain or branched alkyl radical containing 1 to 4 carbon atoms each, are useful as immunostimulant agents. The invention also provides processes for their preparation and pharmaceutical compositions containing them.
式为## STR1 ##的酰胺,其中R为2-喹啉基,取代苯基(取代基为Br,3-Cl,CF.sub.3,烷氧羰基,4-二烷基氨基),二氯苯基,三烷氧基苯基,苄基,苯乙烯基,苯甲酰基或苯胺基,R'为卤素,苯基或苯胺基,或当R为2-喹啉基,取代苯基,三烷氧基苯基,苄基或苯乙烯基时,R'为苯氧基或4-氯苯氧基,或当R为4-三氟甲基(或二烷基氨基)苯基时,R'为4-氟(或烷氧基)苯基,或当R为苯胺基时,R'为3-溴苯基,或当R为苯基或烷氧基苯基时,R'为苯基,4-氯苯氧基,苯胺基或1-吡咯烷基,或当R'为2-(或4-)氯苯基,3-(或4-)溴苯基,4-烷氧基苯基或3,4-二氯(或二溴)苯基时,R为苯基,或R为3-卤代苯基且R'为3-(或4-)氟苯基,3-(或4-)溴苯基,4-氯苯基,2-(或3-)烷氧基苯基,3-烷基苯基或3,4-二氟(二氯或二溴)苯基,含有1至4个碳原子的直链或支链烷基,可用作免疫刺激剂。本发明还提供了它们的制备方法和含有它们的制药组合物。