Optimization of drug-like properties of nonsteroidal glucocorticoid mimetics and identification of a clinical candidate.

ACS Med Chem Lett

Department of Medicinal Chemistry and Department of Immunology and Inflammation, Boehringer Ingelheim Pharmaceuticals, Inc. , 900 Ridgebury Road, Ridgefield, Connecticut 06877, United States.

Published: December 2014

A series of nonsteroidal "dissociated" glucocorticoid receptor agonists was optimized for drug-like properties such as cytochrome P450 inhibition, metabolic stability, aqueous solubility, and hERG ion channel inhibition. This effort culminated in the identification of the clinical candidate compound ( R )-39.

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Source
http://www.ncbi.nlm.nih.gov/pmc/articles/PMC4265816PMC
http://dx.doi.org/10.1021/ml500387yDOI Listing

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