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ACS Med Chem Lett. 2016 Nov 1;8(1):67-72. doi: 10.1021/acsmedchemlett.6b00375. eCollection 2017 Jan 12.

Design and Synthesis of Novel Meta-Linked Phenylglycine Macrocyclic FVIIa Inhibitors.

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1
Research & Development, Bristol-Myers Squibb , Hopewell, New Jersey 08534, United States.

Abstract

Two novel series of meta-linked phenylglycine-based macrocyclic FVIIa inhibitors have been designed to improve the rodent metabolic stability and PK observed with the precursor para-linked phenylglycine macrocycles. Through iterative structure-based design and optimization, the TF/FVIIa Ki was improved to subnanomolar levels with good clotting activity, metabolic stability, and permeability.

KEYWORDS:

FVIIa; anticoagulant; antithrombotic; factor VIIa; macrocycle; thrombosis

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