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Stable pharmaceutical composition of fumagillol derivatives

  • US 5,422,363 A
  • Filed: 12/15/1993
  • Issued: 06/06/1995
  • Est. Priority Date: 12/16/1992
  • Status: Expired due to Term
First Claim
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1. A pharmaceutical composition comprising a fumagillol derivative represented by the formula (I):

  • ##STR2## wherein R1 is hydrogen;

    R2 is halogen, N(O)m R5 R6, N+R5 R6 R7.X-, S(O)n R5 or S+R5 R6.X-, in which R5, R6 and R7 represent each independently a substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted heterocyclic group;

    X- represents a counter anion;

    m represents 0 or 1;

    n represents an integer of 0 to 2;

    or R5 and R6 together with the adjacent nitrogen or sulfur atom may form a nitrogen- or sulfur-containing heterocyclic group which is substituted or unsubstituted and may form a condensed ring;

    or R1 and R2 together are a chemical bond;

    R3 is a substituted or unsubstituted 2-methyl-1-propenyl group or a substituted or unsubstituted isobutyl group;

    A is O or NR8, in which R8 represents hydrogen, a substituted or unsubstituted lower alkyl group or a substituted or unsubstituted aryl group; and

    R4 is hydrogen, a substituted or unsubstituted hydrocarbon group or a substituted or unsubstituted acyl group;

    or a salt thereof, and a fatty acid ester of glycerin or polyglycerin wherein the fatty acid constituting the fatty acid ester is a saturated fatty acid having 6 to 22 carbon atoms.

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