C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 271/22 (2006.01) A61K 47/48 (2006.01) A61P 35/00 (2006.01) C07K 5/103 (2006.01) C07K 7/06 (2006.01)
Patent
CA 2453245
The present invention provides compounds of formula (1) R1-HN-CH2-CF2-(CH2)l- CR3R4-CO-R2, wherein: l is 0, 1 or 2; R1 is a labile amino protecting group, R2 is hydroxy group or the residue of an activated ester or halogen atom; R3 and R4 are independently hydrogen atom or C1-C4 alkyl chain. There are also provided their preparation and the water-soluble conjugates based on these linkers, endowed with selective anticancer activity.
L'invention concerne des composés de formule (1) R¿1?-HN-CH¿2?-CF¿2?-(CH¿2?)¿l?-CR¿3?R¿4?-CO-R¿2?, dans laquelle: l vaut 0, 1 ou 2; R¿1? représente un groupe labile protégeant un groupe amino, R¿2? représente un groupe hydroxy ou le résidu d'un ester activé ou d'un atome d'halogène ; R¿3? et R¿4? représentent indépendamment l'un de l'autre un atome d'hydrogène ou une chaîne alkyle C¿1?-C¿4?. L'invention concerne également leur préparation et des conjugués hydrosolubles à base de ces séquences de liaison, présentant une activité anticancéreuse sélective.
Angelucci Francesco
Caruso Michele
Faiardi Daniela
Pesenti Enrico
Scolaro Alessandra
Pharmacia & Italia S.p.a.
Smart & Biggar
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