O6-substituted guanine derivatives, a process for their...

C - Chemistry – Metallurgy – 07 – D

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C07D 473/18 (2006.01) A61K 31/52 (2006.01) A61K 31/70 (2006.01) C07H 19/16 (2006.01)

Patent

CA 2164847

O6-hetarylalkyl- or naphthylalkylguanine derivatives of formula (I) wherein Y is H, ribosyl, deoxyribosyl, or R"XCHR''', wherein X is O or S, R" and R''' are alkyl, or substituted derivatives thereof; R' is H, or alkyl or hydroxyalkyl; R is (i) a cyclic group having at least one 5- or 6-membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, the or each heterocyclic ring having at least one hereto atom chosen from O, N or S, or a substituted derivative thereof; or (ii) naphthyl or a substituted derivative thereof; and pharmaceutically acceptable salts thereof, exhibit the ability to deplete O6- alkylguanine-DNA alkyltransferase (ATase) activity. A process for preparation of the compounds is described. The compounds have utility in combination with alkylating agents in the chemotherapeutic treatment of tumour cells.

Dérivés de naphtylalkylguanine ou hétarylalkylguanine substituée en position O &cir& _<6>, répondant à la formule (I), dans laquelle Y représente H, ribosyle, désoxyribosyle ou R"XCHR"', où X représente O ou S, R" et R"' représentent alkyle, ou leurs dérivés substitués; R' représente H, alkyle ou hydroxyalkyle; R représente (i) un groupe cyclique possédant au moins un hétérocycle pentagonal ou hexagonal éventuellement condensé avec un carbocycle ou hétérocycle, le ou chaque hétérocycle possédant au moins un hétéroatome choisi parmi O, N et S, ou son dérivé substitué; ou (ii) naphtyle ou son dérivé substitué; et leurs sels pharmaceutiquement acceptables; pouvant diminuer l'activité de l'O &cir& _<6>-alkylguanine-ADN alkyltransférase (Atase). On décrit un procédé de préparation de ces composés. Lesdits composés sont utilisables en association avec des agents d'alkylation dans le traitement chimiothérapeutique des cellules tumorales.

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