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J Med Chem. 2014 Feb 13;57(3):955-69. doi: 10.1021/jm401670x. Epub 2014 Jan 17.

Tetrahydroquinoline derivatives as potent and selective factor XIa inhibitors.

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1
Discovery Chemistry and Cardiovascular Biology, Research and Development, Bristol-Myers Squibb Company , 311 Pennington-Rocky Hill Road, Pennington, New Jersey 08543, United States.

Abstract

Antithrombotic agents that are inhibitors of factor XIa (FXIa) have the potential to demonstrate robust efficacy with a low bleeding risk profile. Herein, we describe a series of tetrahydroquinoline (THQ) derivatives as FXIa inhibitors. Compound 1 was identified as a potent and selective tool compound for proof of concept studies. It exhibited excellent antithrombotic efficacy in rabbit thrombosis models and did not prolong bleeding times. This demonstrates proof of concept for the FXIa mechanism in animal models with a reversible, small molecule inhibitor.

PMID:
24405333
DOI:
10.1021/jm401670x
[Indexed for MEDLINE]

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