US 2014/0235633 A1 · 4-Aminoquinazoline Derivatives and Uses Thereof

Abstract

The present invention provides a 4-aminoquinazoline derivative having the chemical structure of the following formula, and the use thereof. It is demonstrated by the pharmacological experiment that, the compound or a salt thereof according to the present invention not only has distinct inhibitory effect on histone deacetylases, but also has stronger differentiation induction and anti-proliferative activities for certain tumor cells. It can be used in the treatment of cancers and diseases related to cell differentiation and proliferation. Excellent efficacy is observed especially for leukemia and a solid tumor. As demonstrated by the animal test, the compound or a salt thereof according to the present invention is less toxic.

Claims17

Dependent claims

A 4-aminoquinazoline derivative, characterized in that, it is a compound having the chemical structure of the following formula or a salt thereof:

wherein
R1, R2, R3 and R4 each independently represent hydrogen, halogen, amino, nitro, hydroxyamino, carboxyl, C1-C4 alkoxycarbonyl, C1-C4 aminoalkyl, C1-C4 aminoalkyl, C1-C4 alkylamino, C1-C4 alkyl, C1-C4 amido, (E)-4-(dimethylamino)-2-butenamido, alkoxy, guanidyl, carbamido, trifluoromethyl, C1-C4 sulfonyl, aryl sulfonyl, substituted phenyl, phenyl, heterocyclyl or substituted heterocyclyl;
Y is N or C;
X1 is hydrogen, halogen, substituted phenyl, phenyl, heterocyclyl or substituted heterocyclyl;
m=0 or 1;
when R3, R4 and R5 are all hydrogen, then Y is C, and m=1;
when X1 is hydrogen or F, Y is C, and m=1, then R1 and R2 are not both methoxy.

4 more elements

Dependencies are inferred from the claim text.

4-Aminoquinazoline Derivatives and Uses Thereof

Life of this patent

4-Aminoquinazoline Derivatives and Uses Thereof

Life of this patent

Abstract

Claims17