Substituted alkanoic acids

Details Substituted alkanoic acids Substituted alkanoic acids

C - Chemistry, Metallurgy

07

C

C07C 275/42 (2006.01) A61K 31/17 (2006.01) A61K 31/423 (2006.01) A61P 35/00 (2006.01) C07D 263/58 (2006.01) C07D 413/12 (2006.01)

Patent

CA 2427750

The invention is directed to physiologically active compounds of general formula (1): wherein:- A1 represents (i) a saturated 3 to 6 membered carbocycle, optionally substituted by one or more alkyl groups, (ii) indanyl or (iii) a saturated 4 to 6 membered heterocyclic ring; R1 represents R3 Z1- Het-or R4N(R5)-C(=0)-NH-Ar1-; L1 represents an R6-R7-linkage; R2 represents hydrogen, halogen, lower alkyl or lower alkoxy; L2 represents an alkylene linkage; Y is carboxy or an acid bioisostere; and their corresponding N-oxides or prodrugs, and pharmaceutically acceptable salts and solvates of such compounds and their corresponding N-oxides or prodrugs. Such compounds have valuable pharmaceutical properties, in particular the ability to regulate the interaction of VCAM-1 and fibronectin with the integrin VLA-4 (.alpha.4.beta.1).

L'invention porte sur des composés .physiologiquement actifs de formule générale (I) dans laquelle: - A1 représente (i) un carbocycle saturé à 3 à 6 éléments facultativement substitué par un ou plusieurs groupes alkyle, (ii) indanyle ou (iii) un anneau hétérocyclique saturé à 4 à 6 éléments; R?1¿ représente R?3 ¿Z?1¿-Het-ou R4N(R?5¿)-C(=0)-NH-Ar?1¿-; L?1¿ représente une liaison R?6¿-R?7¿-; R?2¿ représente hydrogène, halogène, alkyle inférieur ou alkoxy inférieur; L?2¿ représente une liaison alkylène; Y est carboxy ou un bioisostère acide; et sur leurs N-oxides et prodrogues correspondants, et sur leurs sels et solvates pharmacocompatibles et les N-oxides et prodrogues correspondants. Lesdits composés présentent des propriétés intéressantes, dont la capacité de réguler l'interaction de la VCAM-1 et de la fibronectine avec l'intégrine VLA-4 (.alpha.4.beta.1).

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