Tumour targeting prodrugs activated by metallo...

Details Tumour targeting prodrugs activated by metallo... Tumour targeting prodrugs activated by metallo...

C - Chemistry, Metallurgy

07

K

C07K 7/06 (2006.01) A61K 31/122 (2006.01) A61K 31/407 (2006.01) A61K 31/56 (2006.01) A61K 47/42 (2006.01) A61K 47/48 (2006.01) C07K 5/00 (2006.01) C07K 14/00 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2440208

A compound is of general formula (I) wherein (A) is a moiety comprising one of more of a heterocylcic ring, a carbocyclic ring and a fused ring system, the ring or ring system being essential for a biological activity of the compound by action at a nucleic acid or protein target (B) is a bivalent spacer molecule attached directly to the ring system n is an integer 0 or 1 and (X) is a monovalent moiety containing a amide bond that is cleavable by the action of a matrix metalloproteinase enzyme such as to produce a compound of formula (II) wherein the efficacy of the biological activity of the compound of formula (II) is increased over that of the compound of formula (I).

L'invention concerne un composé de formule générale (I) dans lequel (A) représente un fragment renfermant un ou plusieurs hétérocycliques, un carbocyclique et un système de cycles accolés, le cycle ou le système de cycle étant essentiel à l'activité biologique du composé s'exprimant au niveau d'un acide nucléique ou d'une protéine cibles, (B) représente une molécule de séparateur bivalent fixé directement au système de cycle, n prend la valeur d'un nombre entier 0 ou 1 et (X) représente un fragment monovalent contenant une liaison amide pouvant être clivé par l'action d'une enzyme de métalloprotéinase de matrice de sorte à produire un composé de formule (II), l'efficacité de l'activité biologique du composé de formule (II) est augmentée sur celle du composé de formule (I).

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