title: Treatment of obesity and pulmonary arterial hypertension with inhibitors of the prostaglandin transporter: evaluation of patent WO2014/204895A1.
abstract: Prostaglandins display a wide array of pharmacological effects and prostaglandin analogs are already used in the treatment of pulmonary arterial hypertension (PAH). After synthesis and release from cells, prostaglandins undergo reuptake by the prostaglandin transporter (PGT). WO2014/204895 claims the use of a series of trisubstituted triazine derivatives for the treatment of obesity and PAH. Composition of matter of these triazines has been claimed in WO2011/037610 and the compounds are described as potent inhibitors of the PGT. One compound (nr 146) was shown to improve high fat diet-induced glucose tolerance in a mouse model. In addition, this compound has been explored in the rat monocrotaline model of PAH and reduced characteristic features of the pathology. This class of compounds presents a potential new treatment paradigm in the treatment of obesity-related disorders and PAH.
authors.affiliation: a 1 Actelion Pharmaceuticals Ltd, Department of Clinical Pharmacology , Gewerbestrasse 16, CH-4123 Allschwil, Switzerland +41 61 565 6463 ; +41 61 565 6200 ; jasper.dingemanse@actelion.com.
authors.forename: Jasper
authors.initials: J
authors.lastname: Dingemanse
authors.forename: Martin
authors.initials: M
authors.lastname: Bolli
authors.forename: Marc
authors.initials: M
authors.lastname: Iglarz
mesh_terms: D000818:Animals; D019440:Anti-Obesity Agents / Q000494:pharmacology; D004195:Disease Models, Animal; D015195:Drug Design; D006801:Humans; D006976:Hypertension, Pulmonary / Q000188:drug therapy* / Q000503:physiopathology; D051379:Mice; D009765:Obesity / Q000188:drug therapy*; D027361:Organic Anion Transporters / Q000037:antagonists & inhibitors*; D010330:Patents as Topic; D011453:Prostaglandins / Q000378:metabolism / Q000494:pharmacology; D011465:Prostaglandins, Synthetic / Q000494:pharmacology; D051381:Rats
chemical_list: D019440:Anti-Obesity Agents; D027361:Organic Anion Transporters; D011453:Prostaglandins; D011465:Prostaglandins, Synthetic; C503526:SLCO2A1 protein, human
keywords: obesity; prostaglandin transporter; pulmonary arterial hypertension; triazine derivatives