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

Abstract

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::

• asthma
• chronic obstructive pulmonary disease
• Hck inhibitor
• p38 inhibitor
• Src inhibitor
• Syk inhibitor

Notes