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Advances in the Development of Novel Factor Xa Inhibitors: A Patent Review

Atul N Khadse1, Mayank K Sharma1, Prashant R Murumkar1

  • 1Faculty of Pharmacy, Kalabhavan Campus, The Maharaja Sayajirao University of Baroda, Vadodara, India.

Mini Reviews in Medicinal Chemistry
|April 26, 2018
PubMed

Insights

New anticoagulants, particularly direct Factor Xa (FXa) inhibitors, are crucial for treating thrombotic diseases. This review details patented FXa inhibitors, focusing on structural modifications and therapeutic advancements.

Area of Science:

  • Pharmacology
  • Medicinal Chemistry
  • Drug Discovery

Background:

  • Thrombotic diseases cause significant morbidity and mortality globally.
  • Factor Xa (FXa) is a validated target for anticoagulation therapy.
  • Oral direct FXa inhibitors offer selective and effective treatment for thromboembolic conditions.

Purpose of the Study:

  • To review industrial and academic patents on direct FXa inhibitors.
  • To cover patented compounds from December 2011 to the present.
  • To describe structural modifications, biological activity, and technological advances.

Main Methods:

  • Patent literature analysis.
  • Review of scientific publications.
  • Analysis of structural modifications and biological data.

Main Results:

  • Numerous patented direct FXa inhibitors have been developed.
  • New molecules often feature structural bioisosterism for improved efficacy and safety.
  • Advances in process and formulation technologies are reported.

Conclusions:

  • Direct FXa inhibitors represent a significant advancement in anticoagulation.
  • Ongoing research and patenting activity highlight the field's dynamism.
  • Development of antidotes for oral FXa inhibitors is anticipated to further enhance therapy.
Keywords:
AnticoagulantVTEapixabanfactor Xa inhibitorrivaroxabanthrombosis.

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