Keywords: Cd26, Dipeptidyl Peptidase 4 Inhibitors, Incretin System, Type 2 Diabetes Mellitus, Anticancer Drugs, Ca Ix, Ca Xii, Carbonic Anhydrase, Coumarin, Hypoxia, Sulfamate, Sulfamide, Sulfonamide, Thiocoumarin, Carbonate Dehydratase Inhibitor, Carbonate Dehydratase Ix Inhibitor, Unclassified Drug, Antineoplastic Activity, Cancer Inhibition, Drug Potency, Drug Selectivity, Enzyme Inhibition, Human, Review, Structure Activity Relation, Animals, Antigens, Antineoplastic Agents, Carbonic Anhydrase Inhibitors, Disease Progression, Drug Design, Patents As Topic,
Affiliations: *** IBB - CNR ***
Universita di Chieti-Pescara "G. d'Annunzio", Dipartimento di Farmacia , Via dei Vestini 31, 66100, Chieti , Italy +08713554476
Istituto di Biostrutture e Bioimmagini-CNR, via Mezzocannone 16, 80134 Naples, Italy
Università Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
Universit Degli Studi di Firenze, Laboratorio di Chimica Bioinorganica, Via della Lastruccia 3, I-50019 Sesto Fiorentino (Firenze), Italy
References: Not available.
DPP-4 inhibitors: a patent review (2012 - 2014)
INTRODUCTION: Dipeptidyl peptidase 4 (DPP-4) is a serine protease, which catalyzes the hydrolytic process of the amide bond X-Ala or X-Pro at the N-terminus of peptides. This enzyme is involved in the degradation of two incretin hormones glucagon-like peptide-1 and glucose-dependent-insulinotropic polypeptide, which increase the production and release of insulin. Therefore, DPP-4 inhibitors are considered as one of the well-established therapies available for type 2 diabetes mellitus. AREAS COVERED: In this review, the authors report all the patents related to DPP-4 inhibitors from 2012 to 2014. The chemical-related patents have been divided in three general families: i) peptidomimetics; ii) peptides; and iii) non-peptidomimetics compounds. The third group is the most consistent; thus the patents have been further divided on the basis of the chemical structure. In the last section, we briefly discuss the patents containing the formulations or associations of DPP-4 inhibitors with other drugs. EXPERT OPINION: In the last few years, the research on DPP-4 inhibitors has significantly grown leading to the development of heterocyclic scaffolds and non-peptidomimetic structures. Unfortunately, these compounds are not immune from side effects associated with the inhibition of other substrates, indicating that DPP-4 inhibitors are likely multi-target drugs. Therefore, their potential multi-target effects require more attention in clinical practice, even if at this moment, all the patents are focused only on diabetes.