Takeda Chemical Industries, Inc.

Katsuichi Sudo

Hiroaki Okada

Shoji Kishimoto

Yohko Akiyama

Naoki Nagahara

Tsuneo Kanamaru

Shigeru Kamei

Koichi Kondo

Yukimasa Nozaki

Shigeo Yanai

Kaori Wakamatsu

The present invention relates to a pharmaceutical composition for oral administration in which a fumagillol derivative is stabilized and exhibits remarkable antiangiogenesis activity in oral administration.

Oral composition of fumagillol derivative

A complex of a fumagillin derivative represented by the general formula: ##STR1## wherein R.sup.1 is hydrogen; R.sup.2 is halogen, N(O)mR.sup.5 R.sup.6, N.sup.+ R.sup.5 R.sup.6 R.sup.7.X.sup.-, S(O)nR.sup.5 or S.sup.+ R.sup.5 R.sup.6.X.sup.- (wherein R.sup.5, R.sup.6 and R.sup.7 are independently an optionally substituted hydrocarbon or heterocyclic group; X.sup.- is a counter anion; m is an integer of 0 or 1; n is an integer from 0 to 2; and R.sup.5 and R.sup.6 together with the adjacent nitrogen or sulfur atom may form a nitrogen- or sulfur-containing heterocyclic group which may be substituted and form a condensed ring); or R.sup.1 and R.sup.2 together represent a bond; R.sup.3 is 2-methyl-1-propenyl group or isobutyl group; A is O or NR.sup.8 (wherein R.sup.8 is hydrogen or an optionally substituted lower alkyl or aryl group); R.sup.4 is hydrogen, an optionally substituted hydrocarbon group or an optionally substituted acyl group); or a salt thereof, with an optionally etherified cyclodextrin is disclosed. The present invention also provides an antineoplastic agent containing the complex.

Cyclodextrin complex of fumagillin derivative

Dextran sulfate, .beta.-1,3-glucan sulfate, and the salts thereof are angiostatic and useful for treatment and prevention of various diseases caused by abnormally accelerated angiogenesis. Combination of such a compound with a steroidal or non-steroidal substance increases the angiostatic activity of each compound to induce the combined effect.

Angiostatic agents

The present invention relates to a composition with enhanced angiogenic activity which contains a compound of the formula:

Angiogenesis enhancer

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Takatsuki, Japan

Katsuichi Sudo