Colchinol derivatives as vascular damaging agents

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – C-o-group doai

Reexamination Certificate

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C514S646000, C568S733000

Reexamination Certificate

active

07135502

ABSTRACT:
The invention relates to the use of compounds of formula (I): wherein X is —C(O)—, —C(S)—, —C═NOH, or —CH(R7)— wherein R7is hydrogen, hydroxy, C1-7alkoxy, —OR8or —NR8R9(wherein R8is a group —Y1R10(wherein Y1is a direct bond, —C(O)—, —C(S)—, —S—, —C(O)O, —C(O)NR11—, —SO2— or —SO2NR12— (wherein R11and R12, which may be the same or different, each independently represents hydrogen, C1-3alkyl or C1-3alkoxyC2-3alkyl) and R10is as defined herein, and R9includes hydrogen; R1, R2and R3are as defined herein and are preferably methyl; R4, R5and R6are as defined herein with the proviso that R5is not hydroxy, alkoxy, substituted alkoxy, —OPO3H2, —O—C1-7alkanoyl or benzyloxy; and salts thereof in the manufacture of a medicament for use in the production of a vascular damaging effect in warm-blooded animals such as humans. The present invention further relates to compounds of the formula (I), pharmaceutical compositions containing them, processes for their preparation and to a method of treatment using the compounds to produce a vascular damaging effect in a warm-blooded animal such as a human. The compounds of formula (I) and the pharmaceutically acceptable salts thereof may be useful in the treatment of a number of disease states including cancer and rheumatoid arthritis.

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