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Generated: August 21, 2017

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Title: Control of post-surgical intraocular pressure using clonidine derivatives
Abstract:A method of controlling intraocular pressure by nonchronic, topical administration of a clonidine derivative immediately prior and post trauma to the affected eye.
Inventor(s): House; Betty R. (Euless, TX), DeFaller; Joseph M. (Bedford, TX), York; Billie M. (Fort Worth, TX)
Assignee: Alcon Laboratories, Inc. (Fort Worth, TX)
Application Number:07/918,874
Patent Claims: 1. A method of controlling or preventing an acute post-operative intraocular pressure rise associated with an ophthalmic laser surgical procedure, which comprises topically applying to the involved eye prior and subsequent to the procedure an amount of an imidazoline compound effective to control such an acute post-operative intraocular pressure rise, said imidazoline compound having the formula: ##STR4## wherein: R.sub.1 and R.sub.2 are selected from the group consisting of H, OH, and NHR', wherein R' is selected from the group consisting of H and C.sub.1 -C.sub.4 alkyl, provided that one of R.sub.1 and R.sub.2 is always hydrogen; and X and Y are selected from the group consisting of Br, Cl, CH.sub.3 and CH.sub.2 CH.sub.3, or a pharmaceutically acceptable free base or acid salt thereof.

2. The method of claim 1 wherein R.sub.1 is NHCH.sub.3, R.sub.2 is H, X is CH.sub.3 and Y is CH.sub.3.

3. The method of claim 1 wherein R.sub.1 is NHCH.sub.3, R.sub.2 is H, X is CH.sub.2 CH.sub.3 and Y is CH.sub.2 CH.sub.3.

4. The method of claim 1 wherein R.sub.1 is NH.sub.2 CH.sub.3, R.sub.2 is H, X is Cl and Y is Cl.

5. The method of claim 1 wherein R.sub.1 is NH.sub.2, R.sub.2 is H, X is Br and Y is Br.

6. The method of claim 1 wherein R.sub.1 and R.sub.2 are selected from H and NH.sub.2 and X and Y are selected from Cl, CH.sub.3 and CH.sub.2 CH.sub.3.

7. The method of claim 6 wherein R.sub.1 is H, R.sub.2 is NH.sub.2, X is CH.sub.3 and Y is CH.sub.3.

8. The method of claim 6 wherein R.sub.1 is NH.sub.2, R.sub.2 is H, X is CH.sub.2 CH.sub.3 and Y is CH.sub.2 CH.sub.3.

9. The method of claim 6 wherein R.sub.1 is H, R.sub.2 is NH.sub.2, X is Cl and Y is Cl.

10. The method of claim 6 wherein R.sub.1 is NH.sub.2, R.sub.2 is H, X is CH.sub.2 CH.sub.3 and Y is Cl.

11. The method of claim 6 wherein R.sub.1 is NH.sub.2, R.sub.2 is H, X is CH.sub.3 and Y is Cl.

12. The method of claim 6 wherein R.sub.1 is NH.sub.2, R.sub.2 is H, X is CH.sub.2 CH.sub.3 and Y is CH.sub.3.

13. The method of claim 6 wherein R.sub.1 is NH.sub.2, R.sub.2 is H, X is CH.sub.3 and Y is CH.sub.3.

14. The method of claim 6 wherein R.sub.1 is H, R.sub.2 is NH.sub.2, X is CH.sub.2 CH.sub.3 and Y is CH.sub.2 CH.sub.3.

15. The method of claim 6 wherein R.sub.1 is NH.sub.2, R.sub.2 is H, X is Cl and Y is Cl.

16. The method of claim 1 wherein the 2-(trisubstituted phenylimino)-imidazoline compound is applied to the eye in a concentration of from about 0.05% to 5% by weight.

17. A method of controlling or preventing an acute post-operative intraocular pressure rise associated with an ophthalmic laser surgical procedure, which comprises topically applying to the involved eye prior and subsequent to the procedure an amount of an imidazoline compound effective to control such an acute post-operative intraocular pressure rise, said imidazoline compound having the formula: ##STR5## wherein: X and Y are selected from the group consisting of Br, Cl, CH.sub.3 and CH.sub.2 CH.sub.3, with the provision that at least one of X and Y is alkyl, or a pharmaceutically acceptable free base salt thereof.

18. The method of claim 17 wherein both X and Y are CH.sub.2 CH.sub.3.

19. The method of claim 17 wherein X is CH.sub.2 CH.sub.3 and Y is CH.sub.3.

20. The method of claim 17 wherein X is C1 and Y is CH.sub.2 CH.sub.3.

21. The method of claim 17 wherein the compound of formula (II) is applied to the eye in a concentration of from about 0.05% to 5% by weight.

22. A method of controlling or preventing an acute post-operative intraocular pressure rise associated with an ophthalmic laser surgical procedure which comprises topically applying to the involved eye prior and subsequent to the procedure an amount of a substituted phenylimino-imidazoline effective to control such an acute post-operative intraocular pressure rise.
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