Cyclopeptide derivatives with anti-integrin activity

Details Cyclopeptide derivatives with anti-integrin activity Cyclopeptide derivatives with anti-integrin activity

C - Chemistry, Metallurgy

07

K

C07K 7/64 (2006.01) A61K 38/12 (2006.01)

Patent

CA 2562576

Formula (I) compounds are described c(R1-Arg- Gly-Asp-R2) where the meanings of the various groups are as described here below, which are integrin inhibitors, and particularly inhibitors of integrins of the .alpha.v.beta.3 and .alpha.v.beta.5 family, and therefore are useful as medicaments, particularly for the treatment of the diseases underlying abnormal angiogenesis, such as retinopathy, acute renal failure, osteoporosis and metastases. The compounds described herein, when suitably labelled, are also useful as diagnostic agents, especially for the detection of small tumor masses and arterial occlusion events, and as targeted drug vectors.

L'invention concerne des composés de formule (I), soit c(R1-Arg-Gly-Asp-R2), les significations des divers groupes étant définies dans la description. Ces composés sont des inhibiteurs d'intégrines, et plus particulièrement des inhibiteurs d'intégrines de la famille ?v?3 et ?v?5, et sont donc utiles comme médicaments, notamment pour le traitement de maladies sous-jacentes à une angiogenèse anormale, telles que la rétinopathie, l'insuffisance rénale aiguë, l'ostéoporose et les métastases. Les composés susmentionnés, lorsqu'ils sont marqués de façon appropriée, sont également utiles comme agents de diagnostic, notamment pour la détection de masses tumorales de petite taille et d'événements d'occlusion artérielle, et comme vecteurs de médicaments à cible définie.

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