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Discovery of 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine as a Potent I Kur Inhibitor. 2016
Heather J Finlay, and
James A Johnson, and
John L Lloyd, and
Ji Jiang, and
James Neels, and
Prashantha Gunaga, and
Abhisek Banerjee, and
Naveen Dhondi, and
Anjaneya Chimalakonda, and
Sandhya Mandlekar, and
Mary Lee Conder, and
Harinath Sale, and
Dezhi Xing, and
Paul Levesque, and
Ruth R Wexler
Departments of Discovery Chemistry, Biology, and Preclinical Candidate Optimization, Bristol-Myers Squibb, Research and Development , P.O. Box 5400, Princeton, New Jersey 08543-5400, United States.
A new series of phenylquinazoline inhibitors of Kv 1.5 is disclosed. The series was optimized for Kv 1.5 potency, selectivity versus hERG, pharmacokinetic exposure, and pharmacodynamic potency. 5-Phenyl-N-(pyridin-2-ylmethyl)-2-(pyrimidin-5-yl)quinazolin-4-amine (13k) was identified as a potent and ion channel selective inhibitor with robust efficacy in the preclinical rat ventricular effective refractory period (VERP) model and the rabbit atrial effective refractory period (AERP) model.
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