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Details for Patent: 6,723,748

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Details for Patent: 6,723,748

Title: Use of cloprostenol and fluprostenol analogues to treat glaucoma and ocular hypertension
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.
Inventor(s): Klimko; Peter G. (Fort Worth, TX), Bishop; John E. (Groton, MA), Sallee; Verney L. (Burleson, TX), Zinke; Paul W. (Fort Worth, TX)
Assignee: Alcon Manufacturing, Ltd. (Fort-Worth, TX)
Filing Date:Feb 05, 2002
Application Number:10/068,027
Claims:1. 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): ##STR18##

wherein: R.sub.1 =H; C.sub.1 -C.sub.12 straight-chain or branched alkyl; C.sub.1 -C.sub.12 straight-chain or branched acyl; C.sub.3 -C.sub.8 cycloalkyl; or a cationic salt moiety; R.sub.2, R.sub.3 =H, or C.sub.1 -C.sub.5 straight-chain or branched alkyl; or R.sub.2 and R.sub.3 taken together may represent O; X=O, S, or CH.sub.2 ; {character pullout}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; R.sub.9 =H, C.sub.1 -C.sub.10 straight-chain or branched alkyl, or C.sub.1 -C.sub.10 straight-chain or branched acyl; R.sub.11 =H, C.sub.1 -C.sub.10 straight-chain or branched alkyl, or C.sub.1 -C.sub.10 straight-chain or branched acyl; Y=O; and Z=Cl or CF.sub.3 ;

with the proviso that when R.sub.2 and R.sub.3 taken together represent O, then R.sub.1.noteq.C.sub.1 -C.sub.12 straight-chain or branched acyl; and when R.sub.2 =R.sub.3 =H, then R.sub.1.noteq. a cationic salt moiety.

2. The method of claim 1, wherein for the compound (IV): R.sub.2, R.sub.3 taken together represent O; X=CH.sub.2 ; {character pullout}represents a cis double bond for the alpha (upper) chain and a trans double or a single bond for the omega (lower) chain; and R.sub.9 and R.sub.11 =H.

3. The method of claim 2, wherein for the compound (IV): Z=CF.sub.3.

4. The method of claim 1, wherein: R.sub.2 =R.sub.3 =H, or R.sub.2 and R.sub.3 taken together represent O; X=O or CH.sub.2 ; and R.sub.9 = R.sub.11 =H.

5. The method of claim 4, wherein: R.sub.1 =H, C.sub.1 -C.sub.12 straight chain or branched alkyl or cationic salt moiety; and R.sub.2 and R.sub.3 taken together represent O.

6. The method of claim 5, wherein the compound of formula (IV) is selected from the group consisting of the 15-keto analogues of: cloprostenol, fluprostenol, 3-oxacloprostenol, 13,14-dihydrofluprostenol, and their pharmaceutically acceptable esters and salts.

7. The method of claim 6, wherein the compound of formula (IV) is the 15-keto analogue of fluprostenol isopropyl ester.

8. The method of claim 1, wherein between about 0.01 and about 1000 .mu.g/eye of the compounds of formula (IV) is administered.

9. The method of claim 8, wherein between about 0.1 and about 100 .mu.g/eye of the compound of formula (IV) is administered.

10. The method of claim 9, wherein between about 0.1 and about 10 .mu.g/eye of the compound of formula (IV) is administered.

11. 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: ##STR19##

wherein: R.sub.1 =H; C.sub.1 -C.sub.12 straight-chain or branched alkyl; C.sub.1 -C.sub.12 straight-chain or branched acyl; C.sub.3 -C.sub.8 cycloalkyl; or a cationic salt moiety; R.sub.2, R.sub.3 = H, or C.sub.1 -C.sub.5 straight-chain or branched alkyl; or R.sub.2 and R.sub.3 taken together may represent O; X=O, S, or CH.sub.2 ; {character pullout}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; R.sub.9 =H, C.sub.1 -C.sub.10 straight-chain or branched alkyl, or C.sub.1 -C.sub.10 straight-chain or branched acyl; R.sub.11 =H, C.sub.1 -C.sub.10 straight-chain or branched alkyl, or C.sub.1 -C.sub.10 straight-chain or branched acyl; Y=O; and Z=Cl or CF.sub.3 ; with the proviso that when R.sub.2 and R.sub.3 taken together represent O, then R.sub.1.noteq.C.sub.1 -C.sub.12 straight-chain or branched acyl; and when R.sub.2 =R.sub.3 =H, then R.sub.1.noteq. a cationic salt moiety.

12. The composition of claim 11, wherein for the compound (IV): R.sub.2, R.sub.3 taken together represent O; X CH.sub.2 ; {character pullout}represents a cis double bond for the alpha (upper) chain and a trans double or a single bond for the omega (lower) chain; and R.sub.9 and R.sub.11 =H.

13. The composition of claim 12, wherein for the compound (IV): Z=CF.sub.3.

14. The composition of claim 13, wherein the compound of formula (IV) is the 15-keto analogue of 13,14-dihydrofluprostenol isopropyl ester.

15. The method of claim 6, wherein the compound of formula (IV) is the 15-keto analogue of 13,14-dihydrofluprostenol isopropyl ester.
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