Agonists specific for the peripheral cannabinoid receptor

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

2007-05-08

2007-05-08

Barts, Samuel (Department: 1621)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Ether doai

C514S729000

Reexamination Certificate

active

11043089

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.
patent: 6903137 (2005-06-01), Fride et al.
Calignano, A. et al., “Control of pain initiation by endogenous cannabinoids”, Nature 394: 277-81, 1998.
Devane, W.A. et al., “Isolation and structure of a brain constituent that binds to the cannabinoid receptor”, Science 258: 1946-9, 1992.
Devane, W.A. et al., “A novel probe for the cannabinoid receptor”, J. Med. Chem. 35: 2065-9, 1992.
Fride, E. et al., “Pharmacological activity of the cannabinoid receptor agonist, anandamide, a brain constituent”, Eur. J. Pharmacol. 231: 313-4, 1993.
Galve-Roperh, I. et al., “Anti-tumoral action of cannabinoids: involvement of sustained ceramide accumulation and extracellular signal-regulated kinase activation”, Nature Medicine 6: 313-9, 2000.
Griffin, G. et al., “Evidence for the presence of CB2-like cannabinoid receptors on peripheral nerve terminals”, Eur. J. Pharmacol. 339: 53-61, 1997.
Hanus, L. et al., “HU-308: a specific agonist for CB2, a peripheral cannabinoid receptor”, Proc. Nat. Acad. Sci. USA 96: 14228-33, 1999.
Jaggar, S.I. et al., “The anti-hyperalgesic actions of the cannabinoid anandamide and the putative CB2 receptor agonist palmitoylethanolamide in visceral and somatic inflammatory pain”, Pain 76: 189-99, 1998.
Martin, B.R. et al., “Behavioral, biochemical, and molecular modeling evaluations of cannabinoid analogs”, Pharmacol. Biochem. Behavior 40: 471-8, 1991.
Mechoulam, R. et al., “Synthesis of the individual, pharmacologically distinct, enantiomers of a tetrahydrocannabinol derivative”, Tetrahedron Asymmetry 1(5): 315-8, 1990.
Mechoulam, R. et al., “Identification of an endogenous 2-monoglyceride, present in canine gut, that binds to cannabinoid receptors”, Biochem. Pharmacol. 50: 83-90, 1995.
Murthy, S.N.S. et al., “Treatment of dextran sulfate sodium-induced murine colitis by intracolonic cyclosporin”, Dig. Dis. Sci. 38: 1722-34, 1993.
Tjølsen, A. et al., “The formalin test: an evaluation of the method”, Pain 51: 5-17, 1992.
Young, J.M. et al., “The mouse ear inflammatory response to topical arachidonic acid”, J. Invest. Dermatol. 82: 367-71, 1984.
Gareau 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 et al., “Structural features affecting chiral resolution of cannabimimetic enantiomers by amylose 3,5-dimethylphenylcarbamate chiral stationary phase,” Chirality, vol. 7, No. 3, pp. 140-146 (1995).

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