申请人:JANSSEN PHARMACEUTICA N.V.
公开号:EP0219898A1
公开(公告)日:1987-04-29
Novel α,α-diaryl-4-aryl-4-hydroxy-1-piperidinebutanamide, N-oxides of formula
wherein
R is hydrogen or methyl;
Ar¹ and Ar² are, each independently, phenyl or halophenyl;
Alk is -CH₂-CH₂- or -CH₂-CH(CH₃)-;
R¹ and R² are, each independently, hydrogen, C1-6alkyl, phenylmethyl or 2-propenyl or R¹ and R² combined with the nitrogen atom bearing said R¹ and R² may form a pyrrolidinyl, piperidinyl, C1-6alkylpipridinyl, 4-morpholinyl or 2,6-di(C1-6alkyl)-4-morpholinyl radical;
Ar³ is phenyl being optionally substituted with up to 3 substituents selected from the group consisting of C1-6alkyl, C1-6alkyloxy, halo and trifluoromethyl;
the pharmaceutically acceptable acid addition salts and possible stereochemically isomeric forms thereof, which compounds are anti-diarrheal agents; pharmaceutical compositions containing such compounds as an active ingredient and methods of preparing said compounds and pharmaceutical compositions.
新颖的 α,α-二芳基-4-羟基-1-哌啶丁酰胺,式中的 N-氧化物
其中
R 是氢或甲基;
Ar¹ 和 Ar² 各自独立地为苯基或卤代苯基;
烷基是-CH₂-CH₂-或-CH₂-CH(CH₃)-;
R¹ 和 R² 各自独立地为氢、C1-6 烷基、苯基甲基或 2-丙烯基,或者 R¹ 和 R² 与带有所述 R¹ 和 R² 的氮原子结合可形成吡咯烷基、哌啶基、C1-6 烷基哌啶基、4-吗啉基或 2,6-二(C1-6烷基)-4-吗啉基;
Ar³ 是苯基,最多可任选被 3 个取代基取代,这 3 个取代基可从 C1-6 烷基、C1-6 烷氧基、卤代和三氟甲基组成的组中选出;
药学上可接受的酸加成盐及其可能的立体化学异构形式,这些化合物是止泻剂;含有这些化合物作为活性成分的药物组合物,以及制备所述化合物和药物组合物的方法。