C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 7/54 (2006.01) A61K 38/12 (2006.01) C07K 7/64 (2006.01) G01N 33/68 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2486795
Compounds of formula (I) cyclo ~NX1-R1-CO-NX2-R2-CO-NX3-R3-CO-NX4-CO-NX5-R5- CO~, wherein at least one x-fluoroalkylated amino acid is present, are inhibitors of integrins, particularly those belonging to the .alpha.v.beta.3 and .alpha.v.beta.5 family, and thus are useful as medicaments, particularly for the treatment of the underlying diseases responsible for abnormal angiogenesis, such as retinopathy, acute kidney failure, osteoporosis and metastases. The compounds described herein are also useful as diagnostic agents, when appropriately labelled, especially for the detection and location of small tumour masses and arterial occlusion events.
La présente invention concerne des composés représentés par la formule (I) cyclo ÝNX¿1?-R¿1?-CO-NX¿2?-R¿2?-CO-NX¿3?-R¿3?-CO-NX¿4?-CO-NX¿5?-R¿5?-CO¨. La signification des divers groupes est telle que décrite ci-après. Ces composés sont des inhibiteurs des intégrines, notamment de celles appartenant à la famille ?¿v??¿3? et ?¿v??¿5 ?et sont par conséquent utiles en tant que médicaments, plus particulièrement pour le traitement des affections sous-jacentes responsables de l'angiogenèse anormale, telle que la rétinopathie, l-insuffisance rénale aiguë, l'ostéoporose et les métastases. Les composés selon l'invention sont égalemnt utiles en tant qu'agents de diagnostic, avec des marqueurs appropriés, notamment pour détecter et localiser les petites masses tumorales et les accidents (complications) .d'occlusion artérielle.
Dal Pozzo Alma
Giannini Giuseppe
Pisano Claudio
Fetherstonhaugh & Co.
Sigma-Tau Industrie Farmaceutiche Riunite S.p.a.
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