Minor structural modifications convert a selective PPARα agonist into a potent, highly selective PPARδ agonist
摘要:
We report the solid-phase synthesis and pharmacological evaluation of a new series of small-molecule agonists of the human peroxisome proliferator-activated receptor delta (PPAR delta) based on a lead structure from our PPAR alpha program. Compound 33 showed good pharmacokinetics. (c) 2005 Elsevier Ltd. All rights reserved.
[DE] ESSIGSÄUREDERIVATE<br/>[EN] ACETIC ACID DERIVATIVES<br/>[FR] DERIVES DE L'ACIDE ACETIQUE
申请人:BAYER AG
公开号:WO2003035603A1
公开(公告)日:2003-05-01
Die vorliegende Anmeldung betrifft neue substituierte Essigsäurederivate, Verfahren zu ihrer Herstellung sowie ihre Verwendung in Arzneimitteln, insbesondere als potente PPAR-delta aktivierende Verbindungen zur Prophylaxe und/oder Behand-lung kardiovaskulärer Erkrankungen, insbesondere von Dyslipidämien und koronaren Herzkrankheiten.
The present invention relates to novel substituted acetic acid derivatives, to processes for their preparation and to their use in medicaments, in particular as potent PPAR-delta-activating compounds for the prophylaxis and/or treatment of cardiovascular disorders, in particular dyslipidaemias and coronary heart diseases.
The present invention provides a method for producing an unsaturated ether compound represented by general formula (2) below, the method comprising reacting an acetal represented by general formula (1) below in the presence of an aliphatic or aromatic sulfonic acid and an organic base having a total carbon number of 3 to 7. (In the formulae, R1, R2, and R3 may be the same or different and each represent substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted aralkyl, or R1 and R2 form cycloalkyl together with the adjacent carbon atom.)