Novel non-hydrolysable analogue of endogenous cannabinoids, which are found to be more potent therapeutic agents as they are more stable, for example, to hydrolytic cleavage in the gastrointestinal tract. Such compositions may be used as anti-inflammatory, anti-asthmatic, analgetic, hypotensive, antiemetic or anti-spasmodic compositions, and for treating and/or preventing glaucoma or migraine, or for relieving symptoms of multiple sclerosis and mood stimulating compositions. HU310, HU313 etc can be used for : antiinflammatory, antiasthamtic, analgetic, hypotensive, antiemetic or anti-spasmodic effect, useful e.g. for treating glaucoma or migraine.

A novel group of related synthetic derivatives of 2-archidonoyl glycerol which are stable to hydrolysis

Highlights

• Endogenous cannabinoid constituents discovered until now have therapeutic effects but are prone to easy and rapid enzymatic hydrolysis causing them to undergo changes in the gastrointestinal tract.
• Therapeutic effects of these new compounds include reduced intraocular pressure in rabbits (a model for glaucoma), reduced pain and vomiting, lowered blood pressure, anti-inflammatory properties, anti-spasticity effects, useful in the treatment of multiple sclerosis

Our Innovation

• A novel group of related synthetic derivatives of 2-archidonoyl glycerol which are stable to hydrolysis. These are ethers derived from long chain fatty alcohols (in particular archidonyl alcohol). The compounds bind to the CB.sub.1 and CB.sub.2 cannabinoid receptors and exhibit in vivo effects similar to those of anandamide and 2-Ara-Gl, the two types of endogenous cannabinoid constituents discovered so far. Since there are no etherases in the body, these compounds will be much more stable.

Key Features

• More potent therapeutic agents
• More stable, for example, to hydrolytic cleavage in the gastrointestinal tract.
• The novel compounds show prolonged effects, a distinct advantage for some diseases

Development Milestones

• Seeking pharmaceutical companies for ongoing development

The Opportunity

• Cannabinoids have the potential to be blockbuster drugs;
• 5 EU and US neuropathic pain markets, forecast to reach over $4 million in 2007
• Neuroprotection market value will rise to $11.5 billion by the year 2010 when it will constitute a major and important component of the CNS market

project-id 12-2006-1448

Patent granted in U.S., Europe, Spain, Germany, and Israel;
PCT publication number: WO 99/51560