US 2003/0149003 A1 · Functionalized stilbene derivatives as improved vascular targeting agents

Abstract

Novel stilbenoid compounds and their prodrug forms are disclosed, which serve as potent vascular targeting agents useful for the treatment of solid tumor cancers and other diseases associated with unwanted neovascularization. The novel stilbenoid compounds are tubulin-binding stilbenoid analogs structurally related to combretastatin A-1 and combretastatin A-4. The prodrug forms serve as potent vascular targeting agents (VTAs) useful for the treatment of solid tumor cancers and diseases associated with retinal neovascularization.

Claims33

Dependent claims

A compound of the formula:

59
wherein:
R1, R4 and R5 is independently H, OH, lower alkoxy, NH2, NO2, N3, NH-R6, halogen, a phosphate ester salt moiety of the general formula (—O—P(O)(O−M+)2, wherein M is a metal cation or salt such as Na, K and Li, or —OPO3R7R8;
R2 is H, OH, lower alkoxy, NH2, NO2, NH-R6, or phosphate ester salt moiety of the general formula (—O—P(O)(O−M+)2, wherein M is a metal cation or salt such as Na, K and Li;
or —OPO3R7R8, wherein NH2 or OH may cyclize with R1;
R3 is H, lower alkoxy, or phosphate ester salt moiety of the general formula (—O—P(O)(O−M+)2, wherein M is a metal cation or salt such as Na, K and Li or —OPO3R7R8;
R6 is an amino acid acylamino group;
and
R7 and R8 is independently lower alkyl, cycloalkyl, aryl or an ammonium salt (NH4+).

6 more elements

Dependencies are inferred from the claim text.

Functionalized stilbene derivatives as improved vascular targeting agents

Life of this patent

Functionalized stilbene derivatives as improved vascular targeting agents

Life of this patent

Abstract

Claims33