Small molecule inhibitors of PIM1 kinase: July 2009 to February 2013 patent update

Abstract

Introduction: The proviral insertion in murine (PIM) lymphoma proteins for which three isoforms, PIM1, PIM2 and PIM3 have been identified, belonging to the family of serine/threonine kinases has emerged recently as an important therapeutic target for the development of selective inhibitors as the new drugs for treating hematological malignancies and solid tumors. The small molecules developed by academia and the pharmaceutical industry have steadily increased in the last few years. Several drug discovery groups focus on treating disorders, such as cancer mediated by PIM kinase, have provided preclinical evidence suggesting that PIM inhibitor provides anti-apoptotic activity, inhibit cell survival and cell proliferation.

Areas covered: This article discloses recent reviews on research and advances published in the patent literature and scientific publications from July 2009 to February 2013, highlighting discoveries on PIM1 kinase.

Expert opinion: Several PIM1 kinase small molecule inhibitors are now at the pre-clinical research stage, development and testing. Though nearly 40 patents emerged in the last 3 years, greater efforts towards additional designs and medicinal chemistry continues for developing clinically efficacious PIM1 inhibitors, due to the significance of the target for cancer and the potential for novel and diverse inhibitors as drug candidates.