DPP-4 inhibitors: a patent review (2012 – 2014). (February 2015)

• Record Type: Journal Article
• Authors: Costante, Roberto; Stefanucci, Azzurra; Carradori, Simone; Novellino, Ettore; Mollica, Adriano
• Is Part Of: Expert opinion on therapeutic patents. Volume 25:Number 2(2015:Feb.)
• Page Start: 209
• Page End: 236
• Publication Date: 2015-02
• Subjects: Drugs -- Patents -- Periodicals; 615.10272
• DOI: 10.1517/13543776.2014.991309
• Languages: English
• ISSNs: 1354-3776

Abstract

<abstract> <title> <x xml:space="preserve">Abstract</x> </title> <p> <bold> <italic>Introduction</italic>:</bold> 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 <italic>N</italic>-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.</p> <p> <bold> <italic>Areas covered</italic>:</bold> 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.</p> <p> <bold> <italic>Expert opinion</italic>:</bold> 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.</p> </abstract>