2-[4-(Diphenylmethylene)-1-piperidinyl]-acetic acids and their amides

US4443460A · kind A · utility

Assignee

• UCB, Inc. · BE

Inventors

• Ludovic Rodriguez · Brussels, BE
• Eugene Baltes · Sint-Genesius-Rode, BE

Key dates

• Filing date: Sep 17, 1981
• Grant date: Apr 17, 1984
• Expiry date: Sep 17, 2001

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P43/00
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

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.