Enhanced anti-angiogenic activity of permanently charged...

A - Human Necessities – 61 – K

Patent

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A61K 31/14 (2006.01)

Patent

CA 2280181

The present invention discloses the use of permanently charged steroid agonists or antagonists as potent anti-angiogenic compositions comprising as an active ingredient a compound of general formulae (I), (II) or (III), wherein DRUG is any steroid agonist or antagonist, a mixed agonist-antagonist, or a partial agonist and the substituents are as defined in the specification. The effects of estradiol, tamoxifen, TMI or a placebo on the growth or MCF-7 tumors implanted in the vnetral fat pad of nude mice (see the figure). The left panel gives data for tamoxifen, TMI and the placebo, while the right panel adds the group treated with estradiol.

L'invention concerne l'utilisation d'agonistes ou d'antagonistes constamment chargés de stéroïdes comme compositions puissamment anti-angiogéniques, qui renferment comme principe actif un composé de formules générales I (médicament), II (anti-oestrogènes) ou III, dans lesquelles "médicament" est un agoniste ou un antagoniste des stéroïdes, un mélange agoniste-antagoniste ou un agoniste partiel, et les substituants sont tels que définis dans la spécification.

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