Evaluation of WO2012003387, Gilead's ASK1 inhibitors

Expert Opin Ther Pat. 2012 Apr;22(4):455-9. doi: 10.1517/13543776.2012.674515. Epub 2012 Mar 23.

Abstract

A small number of novel N-(triazolylthiazol-2-yl) and N-(triazolylthienyl) benzamide and picolinamide derivatives are claimed. The compounds are ASK1 kinase inhibitors among which some have nanomolar potency and are potentially useful in the treatment of a diverse range of conditions. The claimed compounds define a pharmacophore, distinct from that described in the limited number of patent filings claiming ASK1 inhibitors.

MeSH terms

  • Animals
  • Drug Design
  • Humans
  • MAP Kinase Kinase Kinase 5 / antagonists & inhibitors*
  • MAP Kinase Kinase Kinase 5 / metabolism
  • Molecular Structure
  • Patents as Topic
  • Protein Kinase Inhibitors / chemistry
  • Protein Kinase Inhibitors / pharmacology*
  • Structure-Activity Relationship

Substances

  • Protein Kinase Inhibitors
  • MAP Kinase Kinase Kinase 5