Cyclodextrin complex of fumagillin derivative

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Carbohydrate doai

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514778, 536103, 549356, A61K 31335, A61K 4740

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active

051964066

ABSTRACT:
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.

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D. Duchene et al., Pharmaceutical Technology, pp. 26, 28, 32 and 34 (1990).

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