申请人:UCB, Societe Anonyme
公开号:US04443460A1
公开(公告)日:1984-04-17
New 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acids and their amides, processes for the preparation thereof and therapeutic compositions. These compounds have the formula ##STR1## wherein Y=--OH or --NR.sub.1 R.sub.2, R.sub.1 and R.sub.2 =H, alkyl or phenyl; X=H, halogen or alkoxy; m=0, 1 or 2 and n=1 or 2. The 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acids are prepared by hydrolyzing the corresponding amide or lower alkyl ester, whereas the amides are prepared either by reacting a 4-(diphenylmethylene)-piperidine with an omega-haloacetamide, or by reacting an alkali metal salt of an omega-[4-diphenylmethylene)-1-piperidinyl]-alkanol (m=1 or 2) with a 2-haloacetamide, or by reacting a nitrogen compound (HNR.sub.1 R.sub.2) with a halide or alkyl ester of a 2-[4-(diphenylmethylene)-1-piperidinyl]-acetic acid. These compounds have in particular an antiallergic, spasmolytic, antihistaminic and broncholytic activity.
新的2-[4-(二苯亚甲基)-1-哌啶基]-乙酸及其酰胺,其制备方法和治疗组合物。这些化合物的化学式为##STR1##其中Y=--OH或--NR.sub.1 R.sub.2,R.sub.1和R.sub.2=H,烷基或苯基;X=H,卤素或烷氧基;m=0,1或2,n=1或2。2-[4-(二苯亚甲基)-1-哌啶基]-乙酸是通过水解相应的酰胺或低烷基酯制备的,而酰胺则是通过将4-(二苯亚甲基)-哌啶与ω-卤代乙酰胺反应,或将ω-[4-(二苯亚甲基)-1-哌啶基]-烷醇(m=1或2)的碱金属盐与2-卤代乙酰胺反应,或将氮化合物(HNR.sub.1 R.sub.2)与2-[4-(二苯亚甲基)-1-哌啶基]-乙酸的卤化物或烷基酯反应制备的。这些化合物具有特别的抗过敏、解痉、抗组胺和支气管扩张作用。