Agonists specific for the peripheral cannabinoid receptor

US6864291B1 · kind B1 · utility

Assignee

• YISSUM RESEARCH DEVELOPMENT COMPANY OF THE HEBREW UNIVERSITY OF JERUSALEM LTD. · IL

Inventors

• Ester Fride · Jerusalem, IL
• Aviva Breuer · Jerusalem, IL
• Lumir Hanus · Jerusalem, IL
• Susanna Tchilibon · Jerusalem, IL
• Michal Horowitz · Jerusalem, IL
• Raphael Mechoulam · Jerusalem, IL
• Aaron Garzon · Segrate, IT

Key dates

• Filing date: Oct 30, 2000
• Grant date: Mar 8, 2005
• Expiry date: Jul 28, 2021

Classification

• Technology area (CPC A): Human Necessities
• CPC primary: A61P37/06
• WIPO field: Pharmaceuticals
• WIPO sector: Chemistry

Abstract

The invention provides novel pharmaceutical compositions comprising as the active ingredient 4-phenyl pinene derivatives which are specific for the peripheral cannabinoid receptors. In particular, the compounds of the invention binds efficiently to CB2 but do not bind to CB1. The compounds show no activity in behavioral tests in mice which together have been shown to be specific for tetrahydrocannabinol (THC)-type activity in the central nervous system mediated by CB1 but reduce blood pressure, block intestinal motility, and elicit anti-inflammatory and peripheral analgetic activity. The invention also relates to methods of treating, preventing, or managing hypertension, inflammation, pain, gastrointestinal diseases, autoimmune diseases, and tumors with the compounds of the invention.