Respivert's multikinase inhibitors, an evaluation of WO2014033446 to WO2014033449

Expert Opin Ther Pat. 2014 Dec;24(12):1397-407. doi: 10.1517/13543776.2014.967213.


These four patent applications all claim that N-aryl-N'-pyrazol-5-yl urea derivatives , related to RV-568, which are inhibitors of p38, Syk and Src kinases. All four applications claim their use in the treatment of inflammatory diseases, notably asthma and chronic obstructive pulmonary disease. The four applications are primarily differentiated by the claimed substitution of the pyrazole ring. This is accompanied by differential kinase specificity profiles. Many of the exemplified compounds show reduced potency as p38 inhibitors but high potency as inhibitors of Syk and/or Src kinases.

Keywords: Hck inhibitor; Src inhibitor; Syk inhibitor; asthma; chronic obstructive pulmonary disease; p38 inhibitor.

MeSH terms

  • Animals
  • Humans
  • Intracellular Signaling Peptides and Proteins / antagonists & inhibitors
  • Patents as Topic*
  • Protein Kinase Inhibitors / therapeutic use*
  • Protein-Tyrosine Kinases / antagonists & inhibitors
  • Pulmonary Disease, Chronic Obstructive / drug therapy
  • Syk Kinase
  • p38 Mitogen-Activated Protein Kinases / antagonists & inhibitors*
  • src-Family Kinases / antagonists & inhibitors


  • Intracellular Signaling Peptides and Proteins
  • Protein Kinase Inhibitors
  • Protein-Tyrosine Kinases
  • SYK protein, human
  • Syk Kinase
  • src-Family Kinases
  • p38 Mitogen-Activated Protein Kinases