Inclusion Compounds of Fumagillol Derivative or its Salt, and Pharmaceutical Compositions Comprising the Same

摘要

The present invention relates to an inclusion compound of fumagillol derivative or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrin, and pharmaceutical compositions comprising the same. The inclusion compound according to the present invention has superior water solubility and stability while exhibiting low toxicity, rendering it valuable as an anticancer agent or inhibitor of tumor metastasis.

主权项

1. An inclusion compound of fumagillol derivative of the following Formula 1 or its salt with hydroxypropyl-β-cyclodextrin or sulfobutylether-7-β-cyclodextrinWherein,
X is hydroxy, Y is halogen, or X and Y together forms oxirane ring; B is O or H2; and R1, R2, R3, R4 and R5 independently represent hydrogen, hydroxy, acetoxy, C1-C6 alkyl, C1-C6 alkoxy, amino, alkylamino, dialkylamino, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, aminoalkoxy, alkylaminoalkoxy, dialkylaminoalkoxy, halogen, cyano, trifluoromethyl, nitro, formyl, acetamido, methyleneoxycarboxy, methylenedioxy or ethylenedioxy group, provided that R1, R2, R3, R4 and R5 cannot be hydrogen at the same time.