C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 475/04 (2006.01) A61K 31/519 (2006.01) A61P 35/00 (2006.01)
Patent
CA 2552826
Disclosed are pteridine derivatives of formula (I): (I), wherein, for example, R1 and R2 are hydrogen, C1-C6 alkyl, carboxyl, formyl, C1-C6 hydroxyalkyl, C1- C6 carboxyalkyl, C1-C6 formyl alkyl, C1-C6 alkoxy, acyloxy, acyloxyalkyl wherein the alkyl is C1-C6, halogen, or hydroxy, or a group of formula II: (II); and R3 is (a) phenyl or (b) a cyclic group having at least one 5 or 6- membered heterocyclic ring, optionally with a carbocyclic or heterocyclic ring fused thereto, wherein each heterocyclic ring has at least one hetero atom chosen from O, N, or S; or (c) a phenyl group or a cyclic group, the cyclic group optionally with a carbocyclic or heterocyclic ring fused thereto, which is substituted with 1 to 5 substituents. Disclosed also are pharmaceutical compositions, a method of enhancing the chemotherapeutic effectiveness of cancer treatment agents, a method of deactivating the O6-alkylguanine-DNA alkyltransferase enzyme, and a method of inhibiting the reaction of O6- alkylguanine-DNA alkyltransferase enzyme with an alkylated DNA.
Des dérivés de ptéridine de formule (I), dans laquelle, R¿1? et R¿2? désignent, par exemple, hydrogène, alkyle C¿1?-C¿6?, carboxyle, formyle, hydroxyalkyle C¿1?-C¿6?, carboxylalkyle C¿1?-C¿6?, formylalkyle C¿1?-C¿6?, alcoxy C¿1?-C¿6?, acyloxy, acyloxyalkyle, l'alkyle désignant C¿1?-C¿6?, halogène ou hydroxy, ou un groupe de formule II, et R¿3? désigne (a) phényle ou (b) un groupe cyclique ayant au moins un cycle hétérocyclique à 5 ou 6 membres, éventuellement avec un cycle carbocyclique ou hétérocyclique fusionné, chaque cycle hétérocyclique présentant au moins un hétéroatome sélectionné dans O, N, ou S; ou (c) un groupe phényle ou un groupe cyclique, le groupe cyclique contenant éventuellement un cycle carbocyclique ou hétérocyclique fusionné substitué avec 1 à 5 substituants. Des compositions pharmaceutiques, un procédé d'amélioration de l'efficacité chimiothérapeutique des agents de traitement du cancer, un procédé de désactivation de O?6¿-alkylguanine-ADN alkyltransférase et un procédé d'inhibition de la réaction de l'enzyme O?6¿-alkylguanine-ADN alkyltransférase avec un ADN alkylé.
Loktionova Natalia A.
Moschel Robert C.
Nelson Michael E.
Pegg Anthony E.
Department Of Health And Human Services Government Of The United States Of America Represented By The Se
Ridout & Maybee Llp
The Penn State Research Foundation
LandOfFree
2-amino-o4-substituted pteridines and their use as... does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with 2-amino-o4-substituted pteridines and their use as..., we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and 2-amino-o4-substituted pteridines and their use as... will most certainly appreciate the feedback.
Profile ID: LFCA-PAI-O-1624642