Pim kinase inhibitors: a survey of the patent literature. 2010

Tina Morwick
Boehringer Ingelheim Pharmaceuticals, Department of Medicinal Chemistry, Inc., 900 Ridgebury Rd. Ridgefield, CT 06801-0368, USA. tmorwick@rdg.boehringer-ingelheim.com

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.

UI MeSH Term Description Entries
D009369 Neoplasms New abnormal growth of tissue. Malignant neoplasms show a greater degree of anaplasia and have the properties of invasion and metastasis, compared to benign neoplasms. Benign Neoplasm,Cancer,Malignant Neoplasm,Tumor,Tumors,Benign Neoplasms,Malignancy,Malignant Neoplasms,Neoplasia,Neoplasm,Neoplasms, Benign,Cancers,Malignancies,Neoplasias,Neoplasm, Benign,Neoplasm, Malignant,Neoplasms, Malignant
D010330 Patents as Topic Works about exclusive legal rights or privileges applied to inventions, plants, etc. Trademarks,Patents as Topics,Trademark
D011487 Protein Conformation The characteristic 3-dimensional shape of a protein, including the secondary, supersecondary (motifs), tertiary (domains) and quaternary structure of the peptide chain. PROTEIN STRUCTURE, QUATERNARY describes the conformation assumed by multimeric proteins (aggregates of more than one polypeptide chain). Conformation, Protein,Conformations, Protein,Protein Conformations
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000970 Antineoplastic Agents Substances that inhibit or prevent the proliferation of NEOPLASMS. Anticancer Agent,Antineoplastic,Antineoplastic Agent,Antineoplastic Drug,Antitumor Agent,Antitumor Drug,Cancer Chemotherapy Agent,Cancer Chemotherapy Drug,Anticancer Agents,Antineoplastic Drugs,Antineoplastics,Antitumor Agents,Antitumor Drugs,Cancer Chemotherapy Agents,Cancer Chemotherapy Drugs,Chemotherapeutic Anticancer Agents,Chemotherapeutic Anticancer Drug,Agent, Anticancer,Agent, Antineoplastic,Agent, Antitumor,Agent, Cancer Chemotherapy,Agents, Anticancer,Agents, Antineoplastic,Agents, Antitumor,Agents, Cancer Chemotherapy,Agents, Chemotherapeutic Anticancer,Chemotherapy Agent, Cancer,Chemotherapy Agents, Cancer,Chemotherapy Drug, Cancer,Chemotherapy Drugs, Cancer,Drug, Antineoplastic,Drug, Antitumor,Drug, Cancer Chemotherapy,Drug, Chemotherapeutic Anticancer,Drugs, Antineoplastic,Drugs, Antitumor,Drugs, Cancer Chemotherapy
D015195 Drug Design The molecular designing of drugs for specific purposes (such as DNA-binding, enzyme inhibition, anti-cancer efficacy, etc.) based on knowledge of molecular properties such as activity of functional groups, molecular geometry, and electronic structure, and also on information cataloged on analogous molecules. Drug design is generally computer-assisted molecular modeling and does not include PHARMACOKINETICS, dosage analysis, or drug administration analysis. Computer-Aided Drug Design,Computerized Drug Design,Drug Modeling,Pharmaceutical Design,Computer Aided Drug Design,Computer-Aided Drug Designs,Computerized Drug Designs,Design, Pharmaceutical,Drug Design, Computer-Aided,Drug Design, Computerized,Drug Designs,Drug Modelings,Pharmaceutical Designs
D047428 Protein Kinase Inhibitors Agents that inhibit PROTEIN KINASES. Protein Kinase Inhibitor,Inhibitor, Protein Kinase,Inhibitors, Protein Kinase,Kinase Inhibitor, Protein,Kinase Inhibitors, Protein
D051573 Proto-Oncogene Proteins c-pim-1 Serine-threonine protein kinases that relay signals from CYTOKINE RECEPTORS and are involved in control of CELL GROWTH PROCESSES; CELL DIFFERENTIATION; and APOPTOSIS. c-pim-1 Protein,pim-1 Proto-Oncogene Protein,Pim-1 Kinase,Proto-Oncogene Protein c-pim-1,Proto-Oncogene Protein pim-1,Kinase, Pim-1,Pim 1 Kinase,Proto Oncogene Protein c pim 1,Proto Oncogene Protein pim 1,Proto Oncogene Proteins c pim 1,c pim 1 Protein,c-pim-1, Proto-Oncogene Protein,c-pim-1, Proto-Oncogene Proteins,pim 1 Proto Oncogene Protein,pim-1, Proto-Oncogene Protein

Related Publications

Tina Morwick
March 2010, Expert opinion on therapeutic patents,
Tina Morwick
June 2024, Expert opinion on therapeutic patents,
Tina Morwick
January 2023, Expert opinion on therapeutic patents,
Tina Morwick
February 2009, Expert opinion on therapeutic patents,
Tina Morwick
November 2010, Expert opinion on therapeutic patents,
Tina Morwick
December 2016, Expert opinion on therapeutic patents,
Tina Morwick
September 2014, Expert opinion on therapeutic patents,
Tina Morwick
May 2014, Expert opinion on therapeutic patents,
Tina Morwick
January 2016, Recent patents on anti-cancer drug discovery,
Copied contents to your clipboard!