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Related Experiment Videos

Factor Xa inhibitors (Berlex).

R A Lewis1

  • 1Lilly Research Centre, Erl Wood Manor, Sunninghill Road, Windelsham, Surrey, GU20 6PH, UK. Lewis_Richard@Lilly.com

Idrugs : the Investigational Drugs Journal
|August 16, 2005
PubMed
Summary
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Berlex Biosciences is developing novel Factor Xa inhibitors for treating thrombotic disorders. Research focuses on compounds like ZK-805412, showing potent inhibition, and exploring diverse chemical structures for enhanced efficacy.

Area of Science:

  • Medicinal Chemistry
  • Pharmacology
  • Biochemistry

Background:

  • Thrombotic disorders represent a significant unmet medical need.
  • Factor Xa is a key enzyme in the coagulation cascade, making it a therapeutic target.
  • Previous research has identified various chemical scaffolds with potential Factor Xa inhibitory activity.

Purpose of the Study:

  • To investigate novel series of Factor Xa inhibitors for the prevention and treatment of thrombotic disorders.
  • To identify specific compounds with high inhibitory potency against Factor Xa.

Main Methods:

  • Structure-based drug design utilizing ZK-805412 as a lead compound.
  • Synthesis and evaluation of diverse chemical series, including condensed diphenoxypyridines, indoles, benzimidazoles, and carbazoles.

Related Experiment Videos

  • In vitro assessment of inhibitory activity against Factor Xa.

    • Main Results:

    • ZK-805412, a Z,Z-2,7-bis(dibenzylidene)cycloheptanone derivative, demonstrated nanomolar potency as a Factor Xa inhibitor.
    • Specific inhibitors such as ZK-806350 and ZK-807191 were identified within the program.
    • The inhibitory activity of 2,6-diphenoxypyridines on Factor Xa was confirmed in vitro.

    Conclusions:

    • Berlex Biosciences is actively pursuing the development of potent Factor Xa inhibitors.
    • The identified compounds and explored chemical series hold promise for the therapeutic management of thrombotic conditions.
    • Collaboration with Warner-Lambert further supports the advancement of these Factor Xa inhibitors.