PMID- 22017411 OWN - NLM STAT- MEDLINE DCOM- 20120215 LR - 20131106 IS - 1744-7674 (Electronic) IS - 1354-3776 (Linking) VI - 21 IP - 11 DP - 2011 Nov TI - Recent patents of dipeptidyl peptidase IV inhibitors. PG - 1693-741 LID - 10.1517/13543776.2011.627325 [doi] AB - INTRODUCTION: The serine exopeptidase DPP IV is a dual protein able to work as an enzyme and an interacting protein. The incretin molecules glucagon-like peptide 1 (GLP-1) and glucose-dependent insulinotropic peptide (GIP) are hydrolyzed by DPP IV into inactive forms, which are unable to promote insulin secretion. Therefore, DPP IV is a validated target for the treatment of type 2 diabetes mellitus (T2DM), and a number of inhibitors have been reported in the literature as antidiabetic drugs. AREAS COVERED: DPP IV inhibitor patents from 2006 are included in this review. Documents are classified into chemical groups depending on the main claim. Groups are: i) pyrrolidines and thiazolidines; ii) cyclohexanes, piperidines, piperazines, pyridines and pyrimidines; iii) fused 5-carbon cycles; iv) pyridine, pyrimidine and pyrazine-based bicyclic structures; v) indoles, condensed-imidazoles and xanthines; vi) pyrido-pyrimidines, quinolones, isoquinolines, quinozalines, quinoxalines, naphthyridines, quinolones and quinazolinones; vii) benzoquinolizines, fused aminopiperidines and fused triazoles; viii) other heterocyclic structures and ix) peptidomimetics. EXPERT OPINION: Research in finding new DPP IV inhibitors is intense, despite the number of reported molecules. This is mainly because marketed compounds have been approved in the last 5 years and long-term side effects have not been detected. The perfect inhibitor for the T2DM treatment would therefore be a molecule that inhibits GLP-1 and GIP degradation by DPP IV, but does not affect the activity of the protease in other substrates, nor disturbs the communication of DPP IV with other proteins. FAU - Mendieta, Laura AU - Mendieta L AD - Institute for Research in Biomedicine, Barcelona - Chemistry and Molecular Pharmacology, Spain. FAU - Tarrago, Teresa AU - Tarrago T FAU - Giralt, Ernest AU - Giralt E LA - eng PT - Journal Article PT - Research Support, Non-U.S. Gov't PT - Review PL - England TA - Expert Opin Ther Pat JT - Expert opinion on therapeutic patents JID - 9516419 RN - 0 (Dipeptidyl-Peptidase IV Inhibitors) RN - 0 (Hypoglycemic Agents) RN - EC 3.4.14.5 (DPP4 protein, human) RN - EC 3.4.14.5 (Dipeptidyl Peptidase 4) SB - IM MH - Animals MH - Diabetes Mellitus, Type 2/*drug therapy/physiopathology MH - Dipeptidyl Peptidase 4/drug effects/metabolism MH - Dipeptidyl-Peptidase IV Inhibitors/adverse effects/*pharmacology/therapeutic use MH - Drug Delivery Systems MH - Drug Design MH - Humans MH - Hypoglycemic Agents/adverse effects/*pharmacology/therapeutic use MH - Patents as Topic EDAT- 2011/10/25 06:00 MHDA- 2012/02/16 06:00 CRDT- 2011/10/25 06:00 PHST- 2011/10/25 06:00 [entrez] PHST- 2011/10/25 06:00 [pubmed] PHST- 2012/02/16 06:00 [medline] AID - 10.1517/13543776.2011.627325 [doi] PST - ppublish SO - Expert Opin Ther Pat. 2011 Nov;21(11):1693-741. doi: 10.1517/13543776.2011.627325.