Substituted piperazines as cb1 antagonists

Abstract

Compounds of Formula (I): or pharmaceutically acceptable salts, solvates, or esters thereof, are useful in treating diseases or conditions mediated by CB1 receptors, such as metabolic syndrome and obesity, neuroinflammatory disorders, cognitive disorders and psychosis, addiction (e.g., smoking cessation), gastrointestinal disorders, and cardiovascular conditions.

Description

[0001] prior application [0002] This application claims the benefit of priority to Application No. 60 / 946,896, filed June 28, 2007, which is incorporated by reference in its entirety. Background of the invention [0003] CB 1 The receptor is one of the most abundant neuromodulatory receptors in the brain and is expressed at high levels in the hippocampus, cortex, cerebellum, and basal ganglia (eg, Wilson et al., Science, 2002, Vol. 296, 678-682). Selective CB 1 Receptor antagonists, e.g. pyrazole derivatives such as rimonabant (e.g. US6,432,984) are useful in the treatment of various conditions such as obesity and metabolic syndrome (e.g. Bensaid et al., Molecular Pharmacology, 2003 Vol. 63, No. 4, pp. 908-914; Trillou et al., Am. J. Physiol. Regul. Integr. Comp. Physiol. 2002 Vol. 284, R345-R353; Kirkham, Am. J. Physiol. Regul .Integr.Comp.Physiol.2002 Vol. 284, R343-R344), neuroinflammatory diseases (eg Adam et al., Expert Opin. Ther. Patents, 2002, Vol. 12, No. 10, 14...

AI Technical Summary

Problems solved by technology

However, none of the disclosed compounds have substituted aryl and / or heteroaryl substituents at both the 1 and 2 positions of the piperazine ring

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