Agonists specific for the peripheral cannabinoid receptor

Details Agonists specific for the peripheral cannabinoid receptor Agonists specific for the peripheral cannabinoid receptor

2005-03-08

2005-03-08

Barts, Samuel (Department: 1621)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ether doai

C514S619000, C568S632000, C568S633000

Reexamination Certificate

active

06864291

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.

REFERENCES:
patent: 4282248 (1981-08-01), Mechoulam et al.
patent: 5434295 (1995-07-01), Mechoulam et al.
patent: 6013648 (2000-01-01), Rinaldi et al.
Gareau, Y. et al., “Structure Activity Relationships Of Tetrahydrocannabinol Analogues on Human Cannabinoid Receptors,”Bioorganic&Medicinal Chemistry Letters, vol. 6, No. 2, pp. 189-194 (1996).
Levin, S. et al., “Structural Features Affecting Chiral Resolution of Cannabinmimetic Enantiomers by Amylose 3,5-Dimethylphenylcarbamate Chiral Stationary Phase,”Chirality, vol. 7, pp. 140-146 (1995).

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