Benzothiazoloquinolines as protease-activated receptor 4 (PAR4) antagonists with excellent rat pharmacokinetic properties

  • Bioorg Med Chem Lett. 2026 Oct 10:143:130795. doi: 10.1016/j.bmcl.2026.130795.
Jeremy M Richter  1 ,  J Alex Bates  2 ,  Xiaojun Zhang  2 ,  Wen Jiang  2 ,  Samuel K Reznik  2 ,  O Scott Halpern  2 ,  Qinghong Fu  2 ,  Shana L Posy  2 ,  Chi Sum  2 ,  Ji Hua  2 ,  Jing Yang  2 ,  Victor R Guarino  2 ,  David A Gordon  2 ,  Ruth R Wexler  2 ,  E Scott Priestley  2
Affiliations
  • 1. Bristol-Myers Squibb, Route 206 & Province Line Road, Lawrenceville, NJ, 08543, USA. Electronic address: [email protected].
  • 2. Bristol-Myers Squibb, Route 206 & Province Line Road, Lawrenceville, NJ, 08543, USA.
PMID: 42858890 DOI: 10.1016/j.bmcl.2026.130795
Abstract

A novel series of quinoline-based PAR4 antagonists with single digit nanomolar potency has been discovered through iterative structure-activity relationship optimization. This series of quinoline antagonists demonstrates excellent rat pharmacokinetic properties with favorable oral exposure and Cmax.

Keywords
Anticoagulant; Antithrombotic; PAR4; Protease-activated receptor 4; Thrombosis.
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