Oxazolyl-arylpropionic acid derivatives and their use as...

C - Chemistry – Metallurgy – 07 – D

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C07D 263/32 (2006.01) A61K 31/421 (2006.01) A61K 31/422 (2006.01) A61K 31/4439 (2006.01) A61K 31/4709 (2006.01) A61P 3/10 (2006.01) C07D 413/04 (2006.01) C07D 413/06 (2006.01) C07D 413/10 (2006.01) C07D 413/12 (2006.01) C07D 413/14 (2006.01)

Patent

CA 2418104

Compounds represented by the following structural formula (I), and pharmaceutically acceptable salts, solvates and hydrates thereof, wherein: n is 2, 3, or 4 and W is CH2, CH(OH), C(O) or O; R1 is an unsubstituted or substituted aryl, heteroaryl, cycloalkyl, heterocycloalkyl, aryl-alkyl, heteroaryl-alkyl, cycloalkyl-alkyl, or t-butyl; R2 is H, alkyl, haloalkyl or phenyl; Y is an unsubstituted or substituted thiophen-2,5-diyl or phenylene; R3 is alkyl or haloalkyl; R4 is a substituted or unsubstituted phenyl, naphthyl, 1,2,3,4-tetrahydronaphthyl, quinolyl, pyridyl or benzo[1,3]dioxol-5- yl group; and R5 is H, alkyl, or aminoalkyl; are useful for modulating a peroxisome proliferator activated receptor, particularly in the treatment of diabetes mellitus.

La présente invention concerne des composés représentés par la formule structurelle (I) et certains de leurs sels, solvates et hydrates pharmaceutiquement admis. Ces composés, sels, solvates et hydrates conviennent particulièrement pour la modulation des récepteurs PPAR (Peroxisome Proliferator Activated Receptor), et plus particulièrement pour le traitement du diabète sucré. Dans cette formule, n vaut 2, 3, ou 4. W est CH¿2?, CH(OH), C(O) ou O. R1 est aryle, hétéroaryle, cycloalkyle, hétérocycloalkyle, aryl-alkyle, hétéroaryl-alkyle, cycloalkyl-alkyle, ou t-butyle substitués ou non substitués. R2 est H, alkyle, haloalkyle ou phényle. Y est thiophène-2,5-diyle ou phénylène substitués ou non substitués. R3 est alkyle ou haloalkyle. R4 est phényle, naphtyle, 1,2,3,4-tétrahydronaphtyle, quinolyle, pyridyle ou benzo[1,3]dioxol-5-yle substitués ou non substitués. Enfin, R5 est H, alkyle, ou aminoalkyle.

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