Heteropyrrole analogs acting on cannabinoid receptors

Details Heteropyrrole analogs acting on cannabinoid receptors Heteropyrrole analogs acting on cannabinoid receptors

2006-01-10

2011-12-27

Chung, Susannah (Department: 1626)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C514S310000, C514S381000, C514S406000, C548S253000, C548S312400, C548S365700

Reexamination Certificate

active

08084451

ABSTRACT:
Disclosed are biologically active hetero pyrrole analogs such as imidazoles, thiazoles, oxazoles and pyrazoles capable of interacting with the CB1 and/or the CB2 cannabinoid receptors. One aspect discloses hetero pyrrole analogs acting as antagonists for the CB1 and/or the CB2 receptors. Another aspect discloses hetero pyrrole analogs having selectivity for the CB1 or CB2 cannabinoid receptor. Also disclosed are pharmaceutical preparations employing the disclosed analogs and methods of administering therapeutically effective amounts of the disclosed analogs to provide a physiological effect.

REFERENCES:
patent: 5462960 (1995-10-01), Barth et al.
patent: 7119108 (2006-10-01), Makriyannis et al.
patent: 7393842 (2008-07-01), Makriyannis et al.
patent: 7745440 (2010-06-01), Makriyannis et al.
patent: WO 2005/000820 (2005-01-01), None
Patani et al., Chem Rev, 1996, vol. 96 (8), especially p. 3147.
Jarbe T. U.; Lemay B. J.; Vemuri V. K.; Vadivel S. K.; Zvonok A.; Makriyannis A. Central mediation and differential blockade by cannabinergics of the discriminative stimulus effects of the cannabinoid CB(1) receptor antagonist rimonabant in rats.Psychopharmacology(Berl). 2011 DOI 10.1007/s00213-011-2226-3).
Cluny N. L.; Chambers A. P.; Vemuri V. K.; Wood J. T.; Eller L. K.; Freni C.; Reimer R. A.; Makriyannis A.; Sharkey K. A. The neutral cannabinoid CB receptor antagonist AM4113 regulates body weight through changes in energy intake in the rat.Pharmacol Biochem Behav. 2011, 97, (3), 537-43.
Randall P. A.; Vemuri V. K.; Segovia K. N.; Torres E. F.; Hosmer S.; Nunes E. J.; Santerre J. L.; Makriyannis A.; Salamone J. D. The novel cannabinoid CB1 antagonist AM6545 suppresses food intake and food-reinforced behavior.Pharmacol Biochem Behav. 2010, 97, (1), 179-84.
Jarbe T. U.; LeMay B. J.; Olszewska T.; Vemuri V. K.; Wood J. T.; Makriyannis A. Intrinsic effects of AM4113, a putative neutral CB1 receptor selective antagonist, on open-field behaviors in rats.Pharmacol Biochem Behav. 2008, 91, (1), 84-90.
Hodge J.; Bow J. P.; Plyler K. S.; Vemuri V. K.; Wisniecki A.; Salamone J. D.; Makriyannis A.; McLaughlin P. J. The cannabinoid CB1 receptor inverse agonist AM 251 and antagonist AM 4113 produce similar effects on the behavioral satiety sequence in rats.Behav Brain Res. 2008, 193, (2), 298-305.
Bergman J.; Delatte M. S.; Paronis C. A.; Vemuri K.; Thakur G. A.; Makriyannis A. Some effects of CB1 antagonists with inverse agonist and neutral biochemical properties.Physiol Behav. 2008, 93, (4-5), 666-70.
Sink K. S.; Vemuri V. K.; Wood J.; Makriyannis A.; Salamone J. D. Oral bioavailability of the novel cannabinoid CB1 antagonist AM6527: effects on food-reinforced behavior and comparisons with AM4113.Pharmacol Biochem Behav. 2009, 91, (3), 303-6.
Cluny N. L.; Vemuri V. K.; Chambers A. P.; Limebeer C. L.; Bedard H.; Wood J. T.; Lutz B.; Zimmer A.; Parker L. A.; Makriyannis A.; Sharkey K. A. A novel peripherally restricted cannabinoid receptor antagonist, AM6545, reduces food intake and body weight, but does not cause malaise, in rodents.Br J Pharmacol. 2010, 161, (3), 629-42.
Limebeer C. L.; Vemuri V. K.; Bedard H.; Lang S. T.; Ossenkopp K. P.; Makriyannis A.; Parker L. A. Inverse agonism of cannabinoid CB1 receptors potentiates LiCl-induced nausea in the conditioned gaping model in rats.Br J Pharmacol. 2010, 161, (2), 336-49.
Tam J.; Vemuri V. K.; Liu J.; Batkai S.; Mukhopadhyay B.; Godlewski G.; Osei-Hyiaman D.; Ohnuma S.; Ambudkar S. V.; Pickel J.; Makriyannis A.; Kunos G. Peripheral CB1 cannabinoid receptor blockade improves cardiometabolic risk in mouse models of obesity.J Clin Invest. 2010, 120, (8), 2953-66.
Sink K. S.; Segovia K. N.; Collins L. E.; Markus E. J.; Vemuri V. K.; Makriyannis A.; Salamone J. D. The CB1 inverse agonist AM251, but not the CB1 antagonist AM4113, enhances retention of contextual fear conditioning in rats.Pharmacol Biochem Behav. 2010, 95, (4), 479-84.
Sink K. S.; Segovia K. N.; Sink J.; Randall P. A.; Collins L. E.; Correa M.; Markus E. J.; Vemuri V. K.; Makriyannis A.; Salamone J. D. Potential anxiogenic effects of cannabinoid CB1 receptor antagonists/inverse agonists in rats: comparisons between AM4113, AM251, and the benzodiazepine inverse agonist FG-7142.Eur Neuropsychopharmacol. 2010, 20, (2), 112-22.
Storr M. A.; Bashashati M.; Hirota C.; Vemuri V. K.; Keenan C. M.; Duncan M.; Lutz B.; Mackie K.; Makriyannis A.; Macnaughton W. K.; Sharkey K. A. Differential effects of CB(1) neutral antagonists and inverse agonists on gastrointestinal motility in mice.Neurogastroenterol Motil. 2010, 22, (7), 787-96, e223.
Chambers A. P.; Vemuri V. K.; Peng Y.; Wood J. T.; Olszewska T.; Pittman Q. J.; Makriyannis A.; Sharkey K. A. A neutral CB1 receptor antagonist reduces weight gain in rat.Am J Physiol Regul Integr Comp Physiol. 2007, 293, (6), R2185-93.
Sink K. S.; McLaughlin P. J.; Wood J. A.; Brown C.; Fan P.; Vemuri V. K.; Peng Y.; Olszewska T.; Thankur G. A.; Makriyannis A.; Parker L. A.; Salamone J. D. The novel cannabinoid CB1 receptor neutral antagonist AM4113 suppresses food intake and food-reinforced behavior but does not induce signs of nausea in rats.Neuropsychopharmacology. 2008, 33, (4), 946-55.

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