C - Chemistry – Metallurgy – 07 – H
Patent
C - Chemistry, Metallurgy
07
H
C07H 19/04 (2006.01) C07D 235/04 (2006.01) C07D 401/00 (2006.01) C07D 403/02 (2006.01)
Patent
CA 2531869
The present invention is directed to the means by which to alter the binding affinity and/or specificity of a compound with a sequence of DNA in the minor groove of a double-strand thereof. More particularly, the present invention is directed to a synthetic and/or non-naturally occurring compound (e.g., an analog of a polyamide oligomer or polymer) which contains at least one hydrogen bond donor moiety and at least one hydrogen bond acceptor moiety, wherein the latter moiety or "building block" has a fused, bicyclic structure which is heteroaromatic, said structure having a heteroatom therein which acts as a hydrogen bond acceptor to bind guanine in the minor groove of the dsDNA sequence, and which is incapable of forming a tautomer. In one particular embodiment of the synthetic and/or non-naturally occurring compound, the fused, bicyclic structure occupies an initial or first terminal position within the compound.
L'invention concerne des moyens permettant de modifier l'affinité et/ou la spécificité de liaison d'un composé avec une séquence d'ADN dans le petit sillon d'un double brin d'ADN. Elle concerne plus particulièrement un composé synthétique et/ou d'origine non naturelle (p. ex. analogue d'un oligomère ou d'un polymère de polyamide) qui contient au moins une fraction donneur de liaison d'hydrogène et au moins une fraction accepteur de liaison d'hydrogène ; cette dernière fraction ou <= élément structural >= présente une structure bicyclique fusionnée qui est hétéroaromatique. Ladite structure contient un hétéroatome agissant comme accepteur de liaison d'hydrogène, qui se lie à la guanine du petit sillon de la séquence d'ADN double brin et est incapable de former un tautomère. Dans une forme de réalisation particulière du composé synthétique et/ou d'origine non naturelle, la structure bicyclique fusionnée occupe dans le composé une position initiale ou une première position terminale.
Bashkin James K.
Phillion Dennis P.
Pharmacia Corporation
Sim & Mcburney
LandOfFree
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