Indolone derivatives having vascular damaging activity

摘要

This invention relates to the use of compounds of Formula (I) as vascular damaging agents: wherein X is selected from: -O-, -S-, -S(O)-, -S(O₂)-, -N(R₅)-, -C(O)-, -C(O)N(R₅)-, -N(R₅)C(O)-, -S(O2)N(R₅)-, or -N(R₅)S(O₂)-; R₁ is independently selected from: amino, halo, hydroxy, -OPO₃H₂, C_1-4alkyl, or C_1-4alkoxy, wherein the amino group is optionally substituted by an amino acid residue and the hydroxy group is optionally esterified; R₂ is selected from: hydrogen or C_1-4alkyl; R₃ is selected from: hydrogen, halo, hydroxy, hydroxyC_1-4alkyl, cyano, cyanoC_1-4alkyl, carboxy, carboxyC_1-4alkyl, C_1-4alkanoyl, C_1-4alkanoylC_1-4alkyl, carbamoyl, carbamoylC_1-4alkyl, C_1-4alkoxy, C_1-4alkoxycarbonyl, C_1-4alkoxycarbonylC_1-4alkyl, C_1-4alkoxycarbonylamino, amino, N-C_1-4alkylamino, NN-diC_1-4alkylamino, aminoC_1-4alkyl, N-C_1-4alkylaminoC_1-4alkyl, NN-diC_1-4alkylaminoC_1-4alkyl, ureido, or C_1-4alkylureyleno; R₄ is independently selected from: C_1-4alkyl, C_1-4alkoxy or halo; R₅ is selected from: hydrogen or C_1-4alkyl; n is 0 or 1; p is 0, 1, 2 or 3; and q is 0, 1 or 2; or a salt, pro-drug or solvate thereof. The invention also relates to novel compounds of Formula (I) and to processes for the preparation of compounds of Formula (I).