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[摘要]：Background. CC chemokine receptor 2 (CCR2) is a GPCR involved in the migration and activation of inflammatory monocytes. A number of studies have highlighted a role for CCR2 in preclinical animal models of atherosclerosis, restenosis, multiple sclerosis, rheumatoid arthritis and insulin resistance. Accordingly, pharmaceutical scientists have been investigating the antagonism of CCR2 as a potential therapy. Objective: This patent evaluation examines the report of a new chemical subseries of CCR2 antagonists. Methods: The compounds of the title invention are compared to the related earlier work in the area of CCR2 antagonism. Conclusions: The compounds disclosed in PCT application WO 2009023754 extend previous work in a dipiperidine series of CCR2 antagonists through the introduction of both a 1,2-disubstituted ethanol spacer and a 1'H-spiro [indene-1,4'-piperin]-1'-yl group. These compounds may represent a means of treating diseases driven by CCR2-bearing leukocytes. |
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