Substituted phenypropionic acid derivatives as agonists to human peroxisome proliferator-activated receptor α(PPAR)
AssigneeAstraZeneca AB
InventorsEva-lotte Alstermark Lindstedt, Anna Christina Olsson, Lanna Li
Life of this patent
Estimating the term…
Abstract
The present invention provides the S enantiomer of a compound of formula (I); wherein R1 represents 2,4-difluorophenyl or cyclohexyl as well as pharmaceutically acceptable salts, solvates, crystalline forms and prodrugs thereof, to processes for preparing such compounds, to their the utility in treating clinical conditions including lipid disorders (dyslipidemias) whether or not associated with insulin resistance, to methods for their therapeutic use and to pharmaceutical compositions containing them.
Claims22
The S enantiomer of a compound of formula I
- wherein R1 represents 2,4-difluorophenyl or cyclohexyl and pharmaceutically acceptable salts, and prodrugs thereof.
A compound selected from:
- (2S)-3-(4-{2-[(Cyclohexylmethyl)(heptyl)amino]-2-oxoethoxy}phenyl)-2-ethoxypropanoic acid;
- and
- (2S)-3-(4-{2-[(2,4-Difluorobenzyl)(heptyl)amino]-2-oxoethoxy}phenyl)-2-ethoxypropanoic acid and pharmaceutically acceptable salts thereof.
2S)-3-(4-{2-[(Cyclohexylmethyl)(heptyl)amino]-2-oxoethoxy}phenyl)-2-ethoxypropanoic acid and pharmaceutically acceptable salts, thereof.
(2S)-3-(4-{2-[(2,4-Difluorobenzyl)(heptyl)amino]-2-oxoethoxy}phenyl)-2-ethoxypropanoic acid and pharmaceutically acceptable salts, thereof.
A process for the preparation of a compound of formula I comprising reacting a compound of formula II
- in which R1 is 2,4-difluorophenyl or cyclohexyl, and R2 is C7H15, and n is 1 and R3 represents a protecting group for carboxylic hydroxy group with a de-protecting agent.
A compound of formula II
- in which R1 is 2,4-difluorophenyl or cyclohexyl, and R2 is C7H15, and n is 1 and R3 represents a protecting group for carboxylic hydroxy group.
A compound of formula III
- in which R2 is a protecting group for carboxylic hydroxy group.
The S enantiomer of a compound of formula I
- wherein R1 represents 2,4-difluorophenyl or cyclohexyl and pharmaceutically acceptable salts, and C1-6 alkoxymethyl esters, C1-6 alkanoyloxymethyl esters, phthalidyl esters, C3-8 cycloalkoxycarbonyloxy C1-6 alkyl esters, 1,3-dioxolen-2-onylmethyl esters, and C1-6 alkoxycarbonyloxyethyl esters thereof.
Dependencies are inferred from the claim text.