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Claims for Patent: 5,510,383

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Claims 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): Bishop; John E. (Arlington, TX), DeSantis, Jr.; Louis (Fort Worth, TX), Sallee; Verney L. (Burleson, TX)
Assignee: Alcon Laboratories, Inc. (Fort Worth, TX)
Application Number:08/101,598
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: R.sup.1 =hydrogen, a cationic salt moiety, a pharmaceutically acceptable amine moiety or C.sub.1 -C.sub.12 alkyl, cycloalkyl or aryl; and R.sup.2 =Cl or CF.sub.3.

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

3. The method of claim 1, wherein R.sup.1 is selected from the group consisting of Na.sup.+ and CH.sub.3 N.sup.+ (CH.sub.2 OH).sub.3.

4. The method of claim 1, wherein R.sup.2 is Cl.

5. The method of claim 1, wherein R.sup.2 is CF.sub.3.

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

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

8. The method of claim 6, wherein between about 0,05 and about 10 .mu.g/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: R.sup.1 =hydrogen, a cationic salt moiety, a pharmaceutically acceptable amine moiety or C.sub.1 -C.sub.12 alkyl, cycloalky or aryl; and R.sup.2 =Cl or CF.sub.3.

10. The composition of claim 9, wherein R.sup.1 is selected from the group consisting of H, CH.sub.3, CH(CH.sub.3).sub.2 and C(CH.sub.3).sub.3.

11. The composition of claim 9, wherein R.sup.1 is selected from the group consisting of Na.sup.+ and CH.sub.3 N.sup.+ (CH.sub.2 OH).sub.3.

12. The composition of claim 9, wherein R.sup.2 is Cl.

13. The composition of claim 9, wherein R.sup.2 is CF.sub.3.

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

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

16. The composition of claim 15, wherein between about 0.05 and about 10 .mu.g/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: R.sup.1 =a pharmaceutically acceptable ester moiety; and R.sup.2 =Cl or CF.sub.3.

18. The method of claim 17, wherein R.sup.2 is Cl.

19. The method of claim 17, wherein R.sup.2 is CF.sub.3.

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