Fumagillol derivatives or method for preparation of...

C - Chemistry – Metallurgy – 07 – D

Patent

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C07D 407/08 (2006.01)

Patent

CA 2594951

The present invention relates to a fumagillol derivative, pharmaceutically acceptable salt thereof and a method for preparing the same. The compounds of the present invention can be prepared through acylation, hydrolysis and alkylation. And the compound of the present invention can be prepared in the form of pharmaceutically acceptable salt or inclusion compound. The present invention provides with fumagillol derivative having more excellent inhibiting effect on angiogenesis, low toxicity, excellent solubility and chemical stability as compared to conventional angiogenesis inhibitors, and the preparation method thereof. The compounds of the present invention can be used as an anti-cancer medicine, inhibitor of cancer metastasis, or the therapeutic agent for treating rheumatic arthritis, psoriasis, diabetic retinitis or obesity.

L'invention concerne un dérivé de fumagillol, un sel pharmaceutiquement acceptable de celui-ci et une méthode de préparation de celui-ci. Les composés selon l'invention peuvent être préparés par acylation, par hydrolyse et par alkylation sous la forme d'un sel pharmaceutiquement acceptable ou d'un composé d'inclusion. L'invention concerne également des dérivés de fumagillol présentant un meilleur effet d'inhibition de l'angiogenèse, une plus faible toxicité, une meilleure solubilité et une meilleure stabilité chimique comparativement avec les inhibiteurs classiques de l'angiogenèse ainsi que la méthode de préparation desdits dérivés. Les composés selon l'invention peuvent être utilisés comme médicament anticancéreux, comme inhibiteur des métastases cancéreuses ou comme agent thérapeutique permettant de traiter l'arthrite rhumatoïde, le psoriasis, la rétinopathie diabétique ou l'obésité.

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