Last Updated: May 11, 2026

Claims for Patent: 5,510,383


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Summary for Patent: 5,510,383
Title:Use of cloprostenol, fluprostenol and their salts and esters to treat glaucoma and ocular hypertension
Abstract:Disclosed is the use of cloprostenol, fluprostenol, and their pharmaceutically acceptable salts and esters for the treatment of glaucoma and ocular hypertension. Also disclosed are ophthalmic compositions comprising said compounds.
Inventor(s):John E. Bishop, Louis DeSantis, Jr., Verney L. Sallee
Assignee: Alcon Research LLC
Application Number:US08/101,598
Patent Claims: 1. A method of treating glaucoma and ocular hypertension which comprises topically administering to the affected eye a therapeutically effective amount of a compound of formula: ##STR9## wherein: R1 =hydrogen, a cationic salt moiety, a pharmaceutically acceptable amine moiety or C1 -C12 alkyl, cycloalkyl or aryl; and R2 =Cl or CF3.

2. The method of claim 1, wherein R1 is selected from the group consisting of H, CH3, CH(CH3)2 and C(CH3)3.

3. The method of claim 1, wherein R1 is selected from the group consisting of Na+ and CH3 N+ (CH2 OH)3.

4. The method of claim 1, wherein R2 is Cl.

5. The method of claim 1, wherein R2 is CF3.

6. The method of claim 1, wherein between about 0.001 and about 1000 μg/eye of a compound of formula (I) is administered.

7. The method of claim 6, wherein between about 0.01 and about 100 μg/eye of a compound of formula (I) is administered.

8. The method of claim 6, wherein between about 0,05 and about 10 μg/eye of a compound of formula (I) is administered.

9. A topical ophthalmic composition for the treatment of glaucoma and ocular hypertension in primates, comprising a therapeutically effective amount of a compound of formula: ##STR10## wherein: R1 =hydrogen, a cationic salt moiety, a pharmaceutically acceptable amine moiety or C1 -C12 alkyl, cycloalky or aryl; and R2 =Cl or CF3.

10. The composition of claim 9, wherein R1 is selected from the group consisting of H, CH3, CH(CH3)2 and C(CH3)3.

11. The composition of claim 9, wherein R1 is selected from the group consisting of Na+ and CH3 N+ (CH2 OH)3.

12. The composition of claim 9, wherein R2 is Cl.

13. The composition of claim 9, wherein R2 is CF3.

14. The composition of claim 9, wherein between about 0.001 and about 100 μg/eye of a compound of formula (I) is administered.

15. The composition of claim 14, wherein between about 0.01 and about 100 μg/eye of a compound of formula (I) is administered.

16. The composition of claim 15, wherein between about 0.05 and about 10 μg/eye of a compound of formula (I) is administered.

17. A method of treating glaucoma and ocular hypertension, which comprises topically administering to the affected eye a therapeutically effective amount of a compound of formula: ##STR11## wherein: R1 =a pharmaceutically acceptable ester moiety; and R2 =Cl or CF3.

18. The method of claim 17, wherein R2 is Cl.

19. The method of claim 17, wherein R2 is CF3.

20. The method of claim 17, wherein between about 0.001 and about 1000 μg\eye of a compound of formula (I) is administered.

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