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Kenilworth, NJ, United States

Yang S.-W.,Merck Research Laboratory | Ho G.D.,Merck Research Laboratory | Tulshian D.,Merck Research Laboratory | Bercovici A.,Merck Research Laboratory | And 13 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized to improve the profile of the previous lead compound 1. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these analogs are described. The optimization efforts allowed the identification of 33, a quinoline amide exhibiting potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. Compound 33 displayed anti-nociceptive oral efficacy in a rat CFA inflammatory pain model at 100 mpk and in a rat spinal nerve ligation neuropathic pain model with an EC50 75 μM. © 2014 Elsevier Ltd. All rights reserved. Source


Ho G.D.,Merck Research Laboratory | Tulshian D.,Merck Research Laboratory | Bercovici A.,Merck Research Laboratory | Tan Z.,Merck Research Laboratory | And 12 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2014

A series of pyrrolo-benzo-1,4-diazine analogs have been synthesized and displayed potent Nav1.7 inhibitory activity and moderate selectivity over Nav1.5. The syntheses, structure-activity relationships, and selected pharmacokinetic data of these analogs are described. Compound 41 displayed anti-nociceptive efficacy in the rat CFA pain model at 100 mpk oral dosing. © 2014 Elsevier Ltd. All rights reserved. Source

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