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Claims for Patent: 4,454,151

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Claims for Patent: 4,454,151

Title: Use of pyrrolo pyrroles in treatment of ophthalmic diseases
Abstract:Certain known pyrroles have been found to be useful in the topical treatment of various ophthalmic diseases in mammals; especially those originating from or associated with inflammation such as, for example, cystoid macular edema, glaucoma, conjunctivitis, uveitis, diabetic retinopathy and eye surgery or trauma.
Inventor(s): Waterbury; L. David (San Mateo, CA)
Assignee: Syntex (U.S.A.) Inc. (Palo Alto, CA)
Application Number:06/360,754
Patent Claims: 1. A method for treating inflammation of the eye in mammals which method comprises topical application to the eye of a mammal in need thereof a therapeutically effective amount of a pharmaceutical ophthalmic composition containing 0.005-1% wt/vol of a compound chosen from those represented by the formulas: ##STR8## and the individual (l-) and (d-)acid isomers thereof and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein

R.sub.1 represents hydrogen; lower alkyl group having from one to four carbon atoms; chloro or bromo;

R.sub.2 represents hydrogen, a lower alkyl group having from one to four carbon atoms, a lower alkoxy group having from one to four carbon atoms, chloro, bromo, fluoro; or R.sub.4 S(O)n wherein

R.sub.4 is lower alkyl and

n is the integer 0, 1 or 2;

X represents oxygen or sulphur; and

R.sub.5 represents hydrogen or lower alkyl group having from one to four carbon atoms.

2. A method for treating corneal neovascularization, uveitis and cystoid macular edema in mammals which method comprises topical application to the eye of a mammal in need thereof a therapeutically effective amount of a pharmaceutical ophthalmic composition containing 0.005-1% wt/vol of a compound chosen from those represented by the formulas: ##STR9## and the individual (l-) and (d)acid isomers thereof and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein

R.sub.1 represents hydrogen; lower alkyl group having from one to four carbon atoms; chloro or bromo;

R.sub.2 represents hydrogen, a lower alkyl group having from one to four carbon atoms, a lower alkoxy group having from one to four carbon atoms, chloro, bromo, fluoro; or R.sub.4 S(O)n wherein

R.sub.4 is lower alkyl and

n is the integer 0, 1 or 2;

X represents oxygen or sulphur; and

R.sub.5 represents hydrogen or lower alkyl group having from one to four carbon atoms.

3. The method of claim 2 for treating corneal neovascularization.

4. The method of claim 2 for treating uveitis.

5. The method of claim 2 for treating cystoid macular edema.

6. The method of claim 2 wherein compounds are represented by those of Formula (A).

7. The method of claim 6 wherein R.sub.1 is hydrogen.

8. The method of claim 6 wherein R.sub.2 is hydrogen, namely 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid.

9. The method of claim 6 wherein R.sub.2 is R.sub.4 S where R.sub.4 is methyl and the R.sub.2 substituent is at the para-position of the phenyl ring, namely 5-(p-methylthio)benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid.

10. The method of claim 6 wherein R.sub.2 is methoxy at the para-position, namely 5-(p-methoxy)-benzoyl-1,2-dihydro-3H-pyrrolo-[1,2-a]pyrrole-1-carboxylic acid.

11. The method of claim 6 wherein R.sub.1 is methyl.

12. A topical ophthalmic pharmaceutical composition for the treatment of inflammation of the eye comprising an 99% to 99.995% wt/vol of ophthalmologically acceptable excipient in admixture with 0.005-1% wt/vol of a compound chosen from those represented by the formulas: ##STR10## and the individual (l-) and (d-)acid isomers thereof and the pharmaceutically acceptable non-toxic esters and salts thereof, wherein

R.sub.1 represents hydrogen; lower alkyl group having from one to four carbon atoms; chloro or bromo;

R.sub.2 represents hydrogen, a lower alkyl group having from one to four carbon atoms, a lower alkoxy group having from one to four carbon atoms, chloro, bromo, fluoro; or R.sub.4 S(O)n wherein

R.sub.4 is lower alkyl and

n is the integer 0, 1 or 2;

X represents oxygen or sulphur; and

R.sub.5 represents hydrogen or lower alkyl group having from one to four carbon atoms.

13. The topical pharmaceutical ophthalmic composition of claim 11 wherein the compound is represented by formula (A).

14. The topical pharmaceutical ophthalmic composition of claim 13 wherein R.sub.1 is hydrogen.

15. The topical pharmaceutical ophthalmic composition of claim 14 wherein R.sub.2 is hydrogen; namely, 5-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid.

16. The topical pharmaceutical ophthalmic composition of claim 14 wherein R.sub.2 is R.sub.4 S where R.sub.4 is methyl and the R.sub.2 substituent is at the para-position of the phenyl ring; namely, 5-(p-methylthio)benzoyl-1,2-dihydro-3H-pyrrolo-[1,2-a]-pyrrole-1-carboxyli c acid.

17. The topical pharmaceutical ophthalmic composition of claim 14 wherein R.sub.4 is methoxy at the para-position; namely, 5-(p-methoxy)-benzoyl-1,2-dihydro-3H-pyrrolo[1,2-a]pyrrole-1-carboxylic acid.

18. The topical pharmaceutical ophthalmic composition of claim 12 wherein the compound is chosen from those represented by formula (A) wherein R.sub.1 is methyl.
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