Treatment of microsporidial and acanthamoeba keratoconjunctivitis with topical fumagillin
AssigneeEmory University
InventorLouis A. Wilson
Life of this patent
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Abstract
Methods for the treatment of Microsporidia keratoconjunctivitis and Acanthamoeba keratitis are disclosed that include the topical administration of an effective amount of fumagillin or a derivative or pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier or diluent.
Claims24
A method for the treatment of microsporidial keratoconjunctivitis that includes the topical administration of an effective amount of a compound of the formula:
- ##STR3## wherein R is hydrogen;
- alkyl;
- phenyl or benzyl, optionally substituted with halogen, C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy, or a mixture thereof;
- and
- R' is hydrogen;
- alkyl;
- phenyl or benzyl, optionally substituted with halogen, C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy, or a mixture thereof;
- or C(O)R" wherein R" is straight, branched, or cyclic C.sub.1 to C.sub.10 alkyl, alkoxyalkyl, aralkyl including benzyl, aryloxyalkyl;
- phenyl or benzyl, optionally substituted with halogen, C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy, or a mixture thereof;
- sulfonate ester, the mono, di or triphosphate ester, trityl or monomethoxytrityl;
- trialkylsilyl, or diphenylmethylsilyl.
A method for the treatment of Acanthamoeba keratoconjunctivitis that includes the topical administration of an effective amount of a compound of the formula:
- ##STR4## wherein R is hydrogen;
- alkyl;
- phenyl or benzyl optionally substituted with halogen, C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy, or a mixture thereof;
- and
- R' is hydrogen;
- alkyl;
- phenyl or benzyl, optionally substituted with halogen, C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy, or a mixture thereof;
- or C(O)R" wherein R" is straight, branched, or cyclic C.sub.1 to C.sub.10 alkyl, alkoxyalkyl, aralkyl including benzyl, aryloxyalkyl;
- phenyl or benzyl, optionally substituted with halogen, C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy, or a mixture thereof;
- sulfonate ester, the mono, di or triphosphate ester, trityl or monomethoxytrityl;
- trialkylsilyl, or diphenylmethylsilyl.
A topical composition for the treatment of Microsporidial Keratoconjunctivitis or Acanthamoeba Keratitis that includes an effective amount of a compound of the formula:
- ##STR5## wherein R is hydrogen;
- alkyl;
- phenyl or benzyl optionally substituted with halogen, C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy, or a mixture thereof;
- and
- R' is hydrogen;
- alkyl;
- phenyl or benzyl, optionally substituted with halogen, C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy, or a mixture thereof;
- or C(O)R" wherein R" is straight, branched, or cyclic C.sub.1 to C.sub.10 alkyl, alkoxyalkyl, aralkyl including benzyl, aryloxyalkyl;
- phenyl or benzyl, optionally substituted with halogen, C.sub.1 to C.sub.4 alkyl or C.sub.1 to C.sub.4 alkoxy, or a mixture thereof;
- sulfonate ester, the mono, di or triphosphate ester, trityl or monomethoxytrityl;
- trialkylsilyl, or diphenylmethylsilyl;
- or its pharmaceutically acceptable salt, in a pharmaceutically acceptable carrier or diluent.
Dependencies are inferred from the claim text.