Compounds for the inhibition of integrins and use thereof

Details Compounds for the inhibition of integrins and use thereof Compounds for the inhibition of integrins and use thereof

C - Chemistry, Metallurgy

07

D

C07D 401/12 (2006.01) A61K 31/4545 (2006.01) A61P 35/00 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2635403

The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring., Ar is either absent or phenylene; .PSI. is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.

L'invention concerne un composé représenté par la formule (I), G - Z - A - Ar - Y - .psi. (I), dans laquelle A représente un noyau hétérocyclique non aromatique, Ar est soit absent soit représente un phénylène, .psi.représente un radical de formule (II), R2 représente une fraction hydrophobe et G représente un radical contenant une ou plusieurs fractions choisies dans le groupe comprenant NH, OH et une fraction de base. Ces composés sont des inhibiteurs d'intégrines, plus spécifiquement des antagonistes du récepteur de fibronectine alpha5beta1, utiles en tant qu'agents anti-angiogéniques.

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