Substituted piperazines as cb1 antagonists
A kind of piperazine, C3-C10 technology, applied in the field of substituted piperazine as CB1 antagonist
Inactive Publication Date: 2010-07-28
INTERVET INT BV
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However, none of the disclosed compounds have substituted aryl and / or heteroaryl substituents at both the 1 and 2 positions of the piperazine ring
Method used
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[0974] The compounds of formula (I) shown in the table below were prepared following one or more of the methods reported above.
[0975]
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[0978]
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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...
Claims
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IPC IPC(8): C07D241/04C07D401/06A61K31/495A61P3/00
CPCC07D401/06C07D241/04A61P1/00A61P1/08A61P1/12A61P1/16A61P3/00A61P3/04A61P3/10A61P9/00A61P9/10A61P13/02A61P15/08A61P25/06A61P25/08A61P25/14A61P25/16A61P25/18A61P25/22A61P25/24A61P25/28A61P25/32A61P25/34A61P25/36A61P29/00A61P31/00A61P35/00A61P43/00
Inventor E·J·吉尔伯特W·J·格林李S·W·李M·W·米勒J·D·斯科特A·斯坦福德C·S·西利
Owner INTERVET INT BV
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