Fumagillol derivatives and processes for preparing the same

Details Fumagillol derivatives and processes for preparing the same Fumagillol derivatives and processes for preparing the same

C - Chemistry, Metallurgy

07

D

C07D 303/22 (2006.01) A61K 31/336 (2006.01) A61P 9/10 (2006.01) C07D 407/14 (2006.01)

Patent

CA 2331873

The present invention relates to a fumagillol derivative represented by chemical formula (1) Image wherein, X represents hydroxy group and Y represents a halogen, or X and Y may form an oxirane ring; B represents O or H2; and R1, R2, R3, R4 and R5 independently represent hydrogen, hydroxy, acetoxy, substituted or unsubstituted amino, substituted or unsubstituted alkyl, substituted or unsubstituted aminoalkoxy, C1 - C6 alkoxy, halogen, cyano, trifluoromethyl, nitro, alkylenedioxy, formyl, acetamido or methylenoxycarboxyl, provided that R1, R2, R3, R4 and R5 do not represent hydrogen at the same time, or pharmaceutically acceptable salt thereof, a process for preparing the same and to a pharmaceutical composition comprising the same as an active ingredient. The compounds of chemical formula (1) and salts thereof can be used as an excellent angiogenesis inhibiting agent.

La présente invention concerne un dérivé de fumagillol représenté par la formule générale (1) ou l'un de ses sels pharmaceutiquement admis. L'invention concerne plus précisément, d'une part un procédé permettant l'élaboration de ce dérivé, et d'autre part une composition pharmaceutique où ce dérivé sert de un principe actif. Les composés représentés par la formule générale (1) et leurs sels conviennent particulièrement comme inhibiteurs de l'angiogenèse.

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