(Benzimidazolyl- and imidazopyridinyl) containing 1-(1,2-disubstituted piperidinyl) derivatives

US6110939A · kind A · utility

Assignee

• Janssen Pharmaceutica NA · BE

Inventors

• Frans Eduard Janssens · Bonheiden, BE
• François Maria Sommen · Wortel, BE
• Dominique Louis Nestor Ghislain Surleraux · Braine-le-Comte, BE
• Joseph Elisabeth Leenaerts · Rijkevorsel, BE

Key dates

• Filing date: Jun 19, 1998
• Grant date: Aug 29, 2000
• Expiry date: Jun 19, 2018

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D471/04
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

This invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein n is 0, 1 or 2; m is 1 or 2, provided that if m is 2, then n is 1; X is a covalent bond or a bivalent radical of formula --O--, --S--, --NR.sup.3 --; .dbd.Q is .dbd.O or .dbd.NR.sup.3 ; R.sup.1 is Ar.sup.1, Ar.sup.1 C.sub.1-6 alkyl or di(Ar.sup.1)C.sub.1-6 alkyl wherein the C.sub.1-6 alkyl group is optionally substituted; R.sup.2 is Ar.sup.2, Ar.sup.2 C.sub.1-6 alkyl, Het or HetC.sub.1-6 alkyl; L is a benzimidazole or imidazopyridine derivative of formula (A) or (B) Ar.sup.1 is optionally substituted phenyl Ar.sup.2 is naphtalenyl or optionally substituted phenyl; and Het is an optionally substituted monocyclic or bicyclic heterocycle; as substance P antagonists; their preparation, compositions containing them and their use as a medicine.