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: Jasper Dingemanse, Martin Bolli, Marc Iglarz
• Journal: Expert opinion on therapeutic patents (Expert Opin Ther Pat) Vol. 25 Issue 9 Pg. 1069-77 ( 2015) ISSN: 1744-7674 [Electronic] England
• PMID: 26099857 (Publication Type: Journal Article)

Chemical References

• Anti-Obesity Agents
• Organic Anion Transporters
• Prostaglandins
• Prostaglandins, Synthetic
• SLCO2A1 protein, human

Topics

• Animals
• Anti-Obesity Agents (pharmacology)
• Disease Models, Animal
• Drug Design
• Humans
• Hypertension, Pulmonary (drug therapy, physiopathology)
• Mice
• Obesity (drug therapy)
• Organic Anion Transporters (antagonists & inhibitors)
• Patents as Topic
• Prostaglandins (metabolism, pharmacology)
• Prostaglandins, Synthetic (pharmacology)
• Rats