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. 2017 Dec 14;60(23):9769-9789.
doi: 10.1021/acs.jmedchem.7b01236. Epub 2017 Nov 20.

Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies

Olivier Bezençon  1 , Bibia Heidmann  1 , Romain Siegrist  1 , Simon Stamm  1 , Sylvia Richard  1 , Davide Pozzi  1 , Olivier Corminboeuf  1 , Catherine Roch  1 , Melanie Kessler  1 , Eric A Ertel  1 , Isabelle Reymond  1 , Thomas Pfeifer  1 , Ruben de Kanter  1 , Michael Toeroek-Schafroth  1 , Luca G Moccia  1 , Jacques Mawet  1 , Richard Moon  1 , Markus Rey  1 , Bruno Capeleto  1 , Elvire Fournier  1
Affiliations

Discovery of a Potent, Selective T-type Calcium Channel Blocker as a Drug Candidate for the Treatment of Generalized Epilepsies

Olivier Bezençon et al. J Med Chem. .

Abstract

We report here the discovery and pharmacological characterization of N-(1-benzyl-1H-pyrazol-3-yl)-2-phenylacetamide derivatives as potent, selective, brain-penetrating T-type calcium channel blockers. Optimization focused mainly on solubility, brain penetration, and the search for an aminopyrazole metabolite that would be negative in an Ames test. This resulted in the preparation and complete characterization of compound 66b (ACT-709478), which has been selected as a clinical candidate.

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