Spiroindenes and spiroindanes as antagonists of CC chemokine receptor 2: WO 2009023754.
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.
Carter
Percy H
PH
Bristol-Myers Squibb Company, Research & Development, Rt. 206 & Province Line Road, Princeton, NJ 08543, USA. percy.carter@bms.com
D000818:Animals; D015195:Drug Design; D004353:Drug Evaluation, Preclinical; D006801:Humans; D007189:Indans / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D007192:Indenes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D010330:Patents as Topic; D054390:Receptors, CCR2 / Q000037:antagonists & inhibitors*; D013141:Spiro Compounds / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology
D007189:Indans; D007192:Indenes; D054390:Receptors, CCR2; D013141:Spiro Compounds