Prodrugs of proton pump inhibitors

US6559167B1 · kind B1 · utility

Assignees

• The Regents of the University of California · US
• The United States of America as represented by the Department of Veteran Affairs · US
• Winston Pharmaceuticals, Inc. · US

Inventors

• Michael E. Garst · Newport Beach, US
• George Sachs · Calabasas, US
• Jai Shin · Brentwood, US

Key dates

• Filing date: Feb 14, 2001
• Grant date: May 6, 2003
• Expiry date: Feb 14, 2021

Classification

• Technology area (CPC C): Chemistry; Metallurgy
• CPC primary: C07F9/65583
• WIPO field: Organic fine chemistry
• WIPO sector: Chemistry

Abstract

Prodrugs of the pyridyl methyl sulfinyl benzimidazole type proton pump inhibitor drugs have a hydrolyzable arylsulfonyl or heteroarylsulfonyl group attached to the benzimidazole nitrogen. The prodrugs of the invention hydrolyze under physiological conditions to provide the proton pump inhibitors with a half life measurable in hours, and are capable of providing sustained plasma concentrations of the proton pump inhibitor drugs for longer time than presently used drugs. The generation of the proton pump inhibitor drugs from the prodrugs of the invention under physiological conditions allows for more effective treatment of several diseases and conditions caused by gastric acid secretion.