Intermediates useful for the preparation of antihistaminic piperidine derivatives

US6777555B2 · kind B2 · utility

Assignee

• Merrell Pharmaceuticals, Inc. · US

Inventors

• Richard C. Krauss · Midland, US
• Robert M. Strom · Midland, US
• Carey L. Scortichini · Midland, US
• William J. Kruper, Jr. · Sanford, US
• Richard A. Wolf · Midland, US
• Weishi Wu · Landenberg, US
• Albert A. Carr · Cincinnati, US
• David A. Hay · Indianapolis, US
• Duane E. Rudisill · Sharonville, US
• Gianbattista Panzone · Cornaredo, IT

Key dates

• Filing date: Feb 12, 2003
• Grant date: Aug 17, 2004
• Expiry date: Feb 12, 2023

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07D401/10
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

The present invention is related to a novel intermediates and processes which are useful in the preparation of certain antihistaminic piperidine derivatives of the formula whereinW represents —C(═O)— or —CH(OH)—;R1 represents hydrogen or hydroxy;R2 represents hydrogen;R1 and R2 taken together form a second bond between the carbon atoms bearing R1 and R2;n is an integer of from 1 to 5;m is an integer 0 or 1;R3 is —COOH or —COOalkyl wherein the alkyl moiety has from 1 to 6 carbon atoms and is straight or branched each of A is hydrogen or hydroxy; andpharmaceutically acceptable salts and individual optical isomers thereof,with the proviso that where R1 and R2 are taken together to form a second bond between the carbon atoms bearing R1 and R2 or where R1 represented hydroxy, n is an integer 0.