Use of cloprostenol and fluprostenol analogues to treat glaucoma and ocular hypertension
AssigneeAlcon Manufacturing, Ltd.
InventorsPeter G. Klimko, John E. Bishop, Verney L. Sallee, Paul W. Zinke
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Abstract
Disclosed is the use of cloprostenol and fluprostenol analogues in combination with carbonic anhydrase inhibitors for the treatment of glaucoma and ocular hypertension and ophthalmic compositions therefor.
Claims15
A method of treating glaucoma and ocular hypertension which comprises topically administering to the affected eye a composition comprising a therapeutically effective amount of a compound having the absolute stereochemical structure of the following formula (IV):
- wherein:
- R1=H;
- C1-C12 straight-chain or branched alkyl;
- C1-C12 straight-chain or branched acyl;
- C3-C8 cycloalkyl;
- or a cationic salt moiety;
- R2, R3=H, or C1-C5 straight-chain or branched alkyl;
- or R2 and R3 taken together may represent O;
- X=O, S, or CH2;
- represents any combination of a single bond, or a cis or trans double bond for the alpha (upper) chain;
- and a single bond or trans double bond for the omega (lower) chain;
- R9=H, C1-C10 straight-chain or branched alkyl, or C1-C10 straight-chain or branched acyl;
- R11=H, C1-C10 straight-chain or branched alkyl, or C1-C10 straight-chain or branched acyl;
- Y=O;
- and Z=Cl or CF3;
- with the proviso that when R2 and R3 taken together represent O, then R1≠C1-C12 straight-chain or branched acyl;
- and when R2=R3=H, then R1≠ a cationic salt moiety.
topical ophthalmic composition for the treatment of glaucoma and ocular hypertension comprising an ophthalmically acceptable carrier and a therapeutically effective amount of a compound having the absolute stereochemical structure of the following formula (IV) and being substantially free of the enantiomer of said compound:
- wherein:
- R1=H;
- C1-C12 straight-chain or branched alkyl;
- C1-C12 straight-chain or branched acyl;
- C3-C8 cycloalkyl;
- or a cationic salt moiety;
- R2, R3 =H, or C1-C5 straight-chain or branched alkyl;
- or R2 and R3 taken together may represent O;
- X=O, S, or CH2;
- represents any combination of a single bond, or a cis or trans double bond for the alpha (upper) chain;
- and a single bond or trans double bond for the omega (lower) chain;
- R9=H, C1-C10 straight-chain or branched alkyl, or C1-C10 straight-chain or branched acyl;
- R11=H, C1-C10 straight-chain or branched alkyl, or C1-C10 straight-chain or branched acyl;
- Y=O;
- and
- Z=Cl or CF3;
- with the proviso that when R2 and R3 taken together represent O, then R1≠C1-C12 straight-chain or branched acyl;
- and when R2=R3=H, then R1≠ a cationic salt moiety.
Dependencies are inferred from the claim text.