The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Jul. 16, 1996
Filed:
Jan. 29, 1993
Takeda Chemical Industries, Ltd., Osaka, JP;
Abstract
The present invention provides 1) a method of producing a complex of a fumagillol derivative of the formula: ##STR1## wherein R.sup.1 is hydrogen; R.sup.2 is halogen, N(O)mR.sup.5 R.sup.6, N+R.sup.5 R.sup.6 R.sup.7.X-- or S(O)nR.sup.5, wherein R.sup.5, R.sup.6 and R.sup.7 are independently an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; X-- is a counter anion; m is 0 or 1; n is an integer of 0 to 2; and R.sup.5 and R.sup.6 together with the adjacent nitrogen or sulfur atom may form an optionally substituted nitrogen- or sulfur-containing heterocyclic group which may form a condensed ring; or R.sup.1 and R.sup.2 are combined to represent a chemical bond; R.sup.3 is 2-methyl-1-propenyl group or isobutyl group; A is oxygen or NR.sup.8, wherein R.sup.8 is hydrogen or an optionally substituted lower alkyl or aryl group; and R.sup.4 is hydrogen, an optionally substituted hydrocarbon group or an optionally substituted acyl group; or a physiologically acceptable salt thereof, with a highly water-soluble cyclodextrin derivative, which comprises mixing the fumagillol derivative or a physiologically acceptable salt thereof with the highly water-soluble cyclodextrin derivative into an aqueous solution, the concentration of the highly water-soluble cyclodextrin derivative being at about 100 mg/ml or more, and 2) the complex of the fumaggillol derivative (I) or physiologically acceptable salt thereof with the highly water-soluble cyclodextrin derivative obtained by the production method 1). The complex of the fumagillol derivative (I) or physiologically acceptable salt thereof with the highly water-soluble cyclodextrin derivative is highly soluble in water, highly stable in storage and can be used as a preparation for injection.