Colchinol derivatives as vascular damaging agents

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United States of America Patent

SERIAL NO

11256018

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Abstract

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The invention relates to the use of compounds of formula (I): wherein X is --C(O)--, --C(S)--, --C.dbd.NOH, or --CH(R.sup.7)-- wherein R.sup.7 is hydrogen, hydroxy, C.sub.1-7alkoxy, --OR.sup.8 or --NR.sup.8R.sup.9 (wherein R.sup.8 is a group --Y.sup.1R.sup.10 (wherein Y.sup.1 is a direct bond, --C(O)--, --C(S)--, --S--, --C(O)O--, --C(O)NR.sup.11--, --SO.sub.2-- or --SO.sub.2NR.sup.12-- (wherein R.sup.11 and R.sup.12, which may be the same or different, each independently represents hydrogen; C.sub.1-3alkyl or C.sub.1-3alkoxyC.sub.2-3alkyl) and R.sup.10 is as defined herein, R.sup.9 includes hydrogen; R.sup.11, R.sup.12 and R.sup.13 are as defined herein and are preferably methyl; R.sup.4, R.sup.5 and R.sup.6 are as defined herein with the proviso that R.sup.5 is not hydroxy, alkoxy, substituted alkoxy, --OPO.sub.3H.sub.2, --O--C.sub.1-7alkanoyl 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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Patent Owner(s)

Patent OwnerAddress
ANGIOGENE PHARMACEUTICALS LTDMAGDALEN CENTRETHE OXFORD SCIENCE PARKOXFORD OX4 4GAUNITED KINGDOM

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Arnould, Jean-Claude Reims, FR 20 129
Boyle, Francis T Cheshire, GB 18 121
Davis, Peter D Oxfordshire, GB 8 287

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