Antifungal agents with enhanced activity in acidic pH
AssigneeScynexis, Inc.
InventorDavid A. Angulo Gonzalez
Life of this patent
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Abstract
Enfumafungin derivative triterpenoid antifungal compounds are used to treat or prevent fungal infections occurring in or under acidic conditions where the pH is lower than about 7, due to their unexpected, enhanced efficacy under such conditions. The enfumafungin derivative triterpenoids (or pharmaceutically acceptable salts or hydrates thereof) are inhibitors of (1,3)-β-D-glucan synthesis and are useful in the treatment or prevention of yeast or mold infections that occur in anatomic areas having a low pH, such as the vaginal cavity, or under acidic local environment conditions such of those seen in fungal abscesses, empyema, or upper gastrointestinal tract infections.
Claims15
A method of treating vulvovaginal candidiasis (VVC) infection in a subject, the method comprising administering to the subject a compound of Formula (IIa):
- which is (1S,4aR,6aS,7R,8R,10aR,10bR,12aR,14R,15R)-15-[[(2R)-2-amino-2,3,3-trimethylbutyl]oxy]-8-[(1R)-1,2-dimethylpropyl]-14-[5-(4-pyridinyl)-1H-1,2,4-triazol-1-yl]-1,6,6a,7,8,9,10,10a,10b,11,12,12a-dodecahydro-1,6a,8,10a-tetramethyl-4H-1,4a-propano-2H-phenanthro[1,2-c]pyran-7-carboxylic acid,
- or a pharmaceutically acceptable salt or hydrate thereof,
- wherein the compound or the pharmaceutically acceptable salt thereof is administered at a total daily dose of 150 to 600 mg of the compound, and
- wherein the VVC infection occurs in a condition or an anatomic area in which the pH is lower than about 5.
A method of preventing vulvovaginal candidiasis (VVC) infection in a subject, the method comprising administering to the subject a compound of Formula (IIa):
- which is (1S,4aR,6aS,7R,8R,10aR,10bR,12aR,14R,15R)-15-[[(2R)-2-amino-2,3,3-trimethylbutyl]oxy]-8-[(1R)-1,2-dimethylpropyl]-14-[5-(4-pyridinyl)-1H-1,2,4-triazol-1-yl]-1,6,6a,7,8,9,10,10a,10b,11,12,12a-dodecahydro-1,6a,8,10a-tetramethyl-4H-1,4a-propano-2H-phenanthro[1,2-c]pyran-7-carboxylic acid,
- or a pharmaceutically acceptable salt or hydrate thereof,
- wherein the compound or the pharmaceutically acceptable salt thereof is administered at a total daily dose of 150 to 600 mg of the compound, and
- wherein the VVC infection occurs in a condition or an anatomic area in which the pH is lower than about 5.
A method of treating vulvovaginal candidiasis (VVC) infection in a subject, the method comprising orally administering to the subject a citrate salt of a compound of Formula (IIa):
- which is (1S,4aR,6aS,7R,8R,10aR,10bR,12aR,14R,15R)-15-[[(2R)-2-amino-2,3,3-trimethylbutyl]oxy]-8-[(1R)-1,2-dimethylpropyl]-14-[5-(4-pyridinyl)-1H-1,2,4-triazol-1-yl]-1,6,6a,7,8,9,10,10a,10b,11,12,12a-dodecahydro-1,6a,8,10a-tetramethyl-4H-1,4a-propano-2H-phenanthro[1,2-c]pyran-7-carboxylic acid,
- wherein the citrate salt of the compound is administered at a total daily dose of 150 to 600 mg of the compound.
Dependencies are inferred from the claim text.