Patent Update: Oncologic, Endocrine & Metabolic Small molecule inhibitors of tyrosine kinase activity

Abstract

Inhibitors of tyrosine kinases may be effective in the treatment of certain cancers and chronic inflammatory conditions for which current therapy is either inadequate or lacking. As such, tyrosine kinase inhibitors are attractive targets for pharmaceutical research and may emerge as an important new class of therapeutic agents. Significant progress has been made during recent years towards the development of potent and highly selective tyrosine kinase inhibitors. In particular, recent discovery efforts at Zeneca have lead to the identification of very potent and selective inhibitors of EGF receptor tyrosine kinase. Likewise, a class of potent and selective inhibitors of PDGF receptor tyrosine kinase were described by Rhone-Poulenc Rorer and more recently by Ciba-Geigy. New inhibitors of p56^lck and pp60^src were also reported. This review focuses mainly on developments which appeared in the patent literature from 1993 to mid-1995. References to the primary literature are limited to studies which are relevant to the highlighted patents.