A - Human Necessities – 61 – K
Patent
A - Human Necessities
61
K
A61K 47/48 (2006.01) A61P 31/12 (2006.01) A61P 33/00 (2006.01) A61P 35/00 (2006.01) A61P 35/04 (2006.01)
Patent
CA 2562569
Compounds of Formula (I) are described; in which the R1 group is as defined in the specification and includes the condensation of 7-t- butoxyiminomethylcamptothecin in position 20 with a cyclopeptide containing the RGD sequence. Said compounds are endowed both with high affinity for integrin receptors .alpha.v.beta.3 and .alpha.v.beta.5 and with selective cytotoxic activity on human tumour cell lines at micromolar concentrations.
L'invention concerne des composés représentés par la formule (I), dans laquelle le groupe R¿1? est tel que défini dans la description et comprend la condensation de 7-t-butoxyiminométhylcamptothécine en position 20 avec un cyclopeptide contenant la séquence RGD. Ces composés sont tous deux d'une affinité élevée pour des récepteurs d'intégrine .alpha.¿v?.beta.¿3? et .alpha.¿v?.beta.¿5? et d'une activité cytotoxique sélective sur des lignes cellulaires tumorales humaines à des concentrations micromolaires.
Alloatti Domenico
Dal Pozzo Alma
Dallavalle Sabrina
Giannini Giuseppe
Merlini Lucio
Fetherstonhaugh & Co.
Istituto Nazionale Per Lo Studio E. La Cura Dei Tumori
Sigma-Tau Industrie Farmaceutiche Riunite S.p.a.
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