FLUORO-ALKYL-CYCLOPEPTIDE DERIVATIVES HAVING ANTI-INTEGRIN ACTIVITY

摘要

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 alphavbeta3 and alphavbeta5 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.