US 2021/0230122 A1 · 5-FLUOROURACIL DERIVATIVES, PREPARATION METHODS AND USES THEREOF

Abstract

Disclosed is a 5-fluorouracil derivative having the molecular structure shown in general formula VI, in which Ra and Rb groups are an alkoxy group or a fluorine-substituted alkoxy group having 1, 2, 3, or 4 carbon atoms, and are mono-, bis-, tri-, tetra- or penta-substituted on a phenyl group; a linking group L1 is an alkyl or alkenyl group having 1, 2, 3, or 4 carbon atoms, a linking group L2 is oxygen, or an alkyl or alkoxy group having 1, 2, 3, or 4 carbon atoms, or an amino acid, or an alkyl group having 1, 2, 3, or 4 carbon atoms containing an amino moiety, or a furyl group, and an X group is O or —NH—. Further disclosed is a method for preparing such a derivative and a use of the same in the treatment of cancer, tumor diseases, and diseases caused by abnormal neovascularization in a human or non-human mammal, and a medicament or a composition containing the 5-fluorouracil derivative.

Claims11

Dependent claims

A 5-fluorouracil derivatives, characterized in that the structure is shown in formula VI:

wherein:
1) Ra is a mono-substituted, di-substituted, tri-substituted, tetra-substituted or penta-substituted group in which the substituent group is independently (C1-C4) alkoxy, or fluorine-substituted (C1-C4) alkoxy;
2) Rb is mono-substituted, di-substituted, tri-substituted, or tetra-substituted group in which the substituent group is independently (C1-C4) alkoxy, or fluorine-substituted (C1-C4) alkoxy;
3) the linking group L1 is independently —CnH2n— (n=1, 2, 3, 4), or —CH═CHCnH2n— (n=0, 1, 2);
4) the linking group L2 is independently selected from the group of a bond, —O—, —CnH2n— (n=1, 2, 3, 4), —OCH2n— (n=1, 2, 3, 4), amino acid, (C1-C4) alkyl with amino, or furanyl;
5) the group X is independently selected from the group of a bond, 0, —NH—.

3 more elements

Dependencies are inferred from the claim text.

5-fluorouracil derivatives, preparation methods and uses thereof

Life of this patent

5-fluorouracil derivatives, preparation methods and uses thereof

Life of this patent

Abstract

Claims11