Pim kinase inhibitors: a survey of the patent literature.
BACKGROUND
Pim kinases have recently emerged as targets of interest in oncology and immune regulation. Ongoing studies have identified a role for these proteins in cell survival and proliferation, both functionally and mechanistically, and overexpression has been observed in a number of human cancers and inflammatory states.


METHODS
This report reviews the patent literature for Pim kinase inhibitors identified from a search of the Thomson patent databases from 1970 through July 2009. Full analyses are provided for publications reporting Pim kinases as primary targets, and a cursory description is given for those disclosing Pim as one of a limited number of secondary targets.


RESULTS
Readers will gain an overview of the various inhibitor series including coverage, potency, selectivity, protein binding features and therapeutic focus, and an appreciation for which scaffolds and structural features have been most highly exploited.


CONCLUSIONS
A greater understanding of pathological mechanisms for Pim kinases has stimulated the recent development of a variety of inhibitor classes with one compound advancing into the clinic earlier this year. Ongoing studies will help define applications for these inhibitors in the treatment of Pim-associated human diseases.
Morwick
Tina
T
Boehringer Ingelheim Pharmaceuticals, Department of Medicinal Chemistry, Inc., 900 Ridgebury Rd. Ridgefield, CT 06801-0368, USA. tmorwick@rdg.boehringer-ingelheim.com
D000970:Antineoplastic Agents / Q000494:pharmacology / Q000627:therapeutic use; D015195:Drug Design; D006801:Humans; D009369:Neoplasms / Q000188:drug therapy / Q000201:enzymology; D010330:Patents as Topic; D011487:Protein Conformation; D047428:Protein Kinase Inhibitors / Q000494:pharmacology* / Q000627:therapeutic use; D051573:Proto-Oncogene Proteins c-pim-1 / Q000037:antagonists & inhibitors* / Q000737:chemistry / Q000502:physiology
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D051573:Proto-Oncogene Proteins c-pim-1; C406031:proto-oncogene proteins pim