1769-85-3Relevant articles and documents
GUANIDINE DERIVATIVES AS TRPC MODULATORS
-
Page/Page column 43; 49, (2014/02/16)
The present invention is directed to guanidine derivatives as inhibitors of transient receptor potential canonical channels (TRPC channels), in particular TRPC3 and/or TRPC6 and/or TRPC7 activity, more particularly TRPC6 activity. Also provided herein are processes for preparing compounds described herein, intermediates used in their synthesis, pharmaceutical compositions thereof, and methods for treating or preventing diseases, conditions and/or disorders mediated by TRPC channels (Formula (I))
Inhibitors of acyl CoA:cholesterol acyltransferase
Vaccaro, Wayne,Amore, Cindy,Berger, Joel,Burrier, Robert,Clader, John,Davis, Harry,Domalski, Martin,Fevig, Tom,Salisbury, Brian,Sher, Rosy
, p. 1704 - 1719 (2007/10/03)
Conformational restriction of previously disclosed acyclic diphenylethyl)diphenylacetamides led to the discovery of several potent inhibitors of acyl CoA:cholesterol acyltransferase (ACAT). cis-[2-(4- Hydroxyphenyl)-1-indanyl]diphenylacetamide (4a) was the most potent ACAT inhibitor identified (IC50 = 0.04 μM in an in vitro rat hepatic microsomal ACAT assay, ED50 = 0.72 mg/kg/day in cholesterol-fed hamsters).