Azacycloalkane derivatives as inhibitors of delta-9 stearoyl-coenzyme A desaturase.
BACKGROUND
Extensive target validation has supported a controlling role for delta-9 stearoyl-CoA desaturase in the regulation of lipid biosynthesis and energy expenditure.


OBJECTIVE
A group of structurally related azacycloalkane derivatives are disclosed in the latest of a series of patent applications from Merck Frosst, some of which are claimed to inhibit delta-9 desaturase activity in HepG2 cells.


CONCLUSIONS
These compounds have potential utility in the treatment of disorders associated with abnormal lipid synthesis and metabolism, in particular for obesity, diabetes, metabolic syndrome, insulin resistance, and hepatic steatosis, when administered either alone or in combination with other agents, for example, peroxisome proliferator-activated receptor gamma (PPAR-gamma) agonists.
Liu
Gang
G
Ambit Biosciences, 4215 Sorrento Valley Blvd, San Diego, CA 92121, USA. gliu@ambitbio.com
D000473:Alkanes / Q000737:chemistry / Q000494:pharmacology*; D000818:Animals; D001372:Aza Compounds / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D004791:Enzyme Inhibitors / Q000494:pharmacology; D006801:Humans; D050356:Lipid Metabolism / Q000187:drug effects; D010330:Patents as Topic; D013230:Stearoyl-CoA Desaturase / Q000037:antagonists & inhibitors*
D000473:Alkanes; D001372:Aza Compounds; D004791:Enzyme Inhibitors; D013230:Stearoyl-CoA Desaturase