Benzosuberonylpiperdine compounds as analgesics

US7115633B2 · kind B2 · utility

Assignee

• GLAXOSMITHKLINE SA · IT

Inventors

• Daniela Barlocco · Milano, IT
• Giorgio Cignarella · Milano, IT
• Giuseppe Giardina · Milano, IT
• Mario Grugni · Milano, IT
• Silvano Ronzoni · Milano, IT

Key dates

• Filing date: May 1, 2001
• Grant date: Oct 3, 2006
• Expiry date: Jun 13, 2022

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D211/22
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

Compounds of formula (I) or a derivative thereof, wherein; R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 is hydrogen or C1-6alkyl; R4 and R5 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; with the proviso that, when R3 is hydrogen, then R4 and R5 are not both hydrogen; and wherein any alkyl group or the alkyl moiety of any group containing such a moiety may be substituted one or more times by halo; are ligands of the ORL-1 receptor and are useful in therapy.