Diaminoquinazoline esters for use as dihydrofolate reductade...

C - Chemistry – Metallurgy – 07 – D

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C07D 239/95 (2006.01) A61K 31/505 (2006.01) A61P 35/00 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01)

Patent

CA 2439463

Compounds of the formula (I) wherein R1, R2, R1' and R2' are independently hydrogen or a group releasing the free aminein vivo, R6 is a substituted phenyl or an optionally substituted, bicyclic or tricyclic aryl ring system or an optionally substituted mono, bi- or tricyclic heteroaryl ring system having utility as dihydrofolate reductase (DHFR) inhibitors with favourable pharmacokinetic properties.

Cette invention concerne des composés représentés par la formule (I) dans laquelle R¿1?, R¿2?, R¿1?' et R¿2?' sont indépendamment hydrogène ou un groupe libérant l'amine libre <i>in vivo</i>, R¿6? est un phényle substitué ou un système à noyau aryle bicyclique ou tricyclique éventuellement substitué ou bien un groupe à noyau hétéroaryle mono, bi- ou tricyclique éventuellement substitué. Ces composés sont utiles en tant qu'inhibiteurs de la dihydrofolate reductase (DHFR) et possèdent des propriétés pharmacocinétiques favorables.

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