Novel serine protease inhibitors.

Area of Science:

• Medicinal Chemistry
• Drug Discovery
• Organic Chemistry

Background:

• Serine protease inhibitors are actively researched for anticoagulant and anti-hepatitis C virus (HCV) applications.
• Approved HCV drugs like telaprevir and boceprevir underscore the pharmaceutical industry's interest in this drug class.

Purpose of the Study:

• To review patent literature on serine protease inhibitors published between 2009 and 2010.
• To identify emerging trends and key chemical scaffolds in serine protease inhibitor development.

Main Methods:

• Comprehensive search of patent databases for serine protease inhibitors.
• Analysis of chemical structures and therapeutic targets reported in patents.
• Categorization of inhibitors based on chemical class and target (e.g., HCV protease, Factor XIa).

Main Results:

• Identified various compound classes, including macrocyclic peptides, linear peptides, phenylglycinamide derivatives, biaryls, and others, as potent inhibitors.
• Highlighted specific applications for HCV protease inhibition and Factor XIa inhibition.
• Documented the significant patent activity in the field during the review period.

Conclusions:

• The development of serine protease inhibitors remains a high-priority area in pharmaceutical research.
• Diverse chemical scaffolds show promise for both antiviral and anticoagulant therapies.
• Patent literature reflects ongoing innovation and a robust pipeline for serine protease inhibitor drugs.