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Last Updated: April 2, 2025

Claims for Patent: 6,429,226

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Summary for Patent: 6,429,226

Title:	Prostaglandin derivatives for the treatment of glaucoma or ocular hypertension
Abstract:	The invention relates to ophthalmological compositions for topical treatment of glaucoma or ocular hypertension comprising an effective intraocular pressure reducing amount of a prostaglandin derivative of PGA, PGB, PGD, PGE or PGF, in which the omega chain contains a ring structure, in an ophthalmologically compatible carrier. The invention further relates to the preparation of said compositions and their use for treatment of glaucoma or ocular hypertension.
Inventor(s):	Stjernschantz; Johan Wilhelm (Uppsala, SE), Resul; Bahram (Uppsala, SE)
Assignee:	Pharmacia Aktiebolag (Stolkholm, SE)
Application Number:	09/562,447
Patent Claims:	1. A therapeutic composition for topical treatment of glaucoma or ocular hypertension in humans containing a prostaglandin PGA, PGB, PGE or PGF in an amount sufficient to reduce intraocular pressure without causing substantial ocular irritation and an ophthalmologically compatible vehicle, wherein the omega chain of the prostaglandin has the formula C.sub.13 --B--C.sub.14 --D--R.sub.2 wherein C is a carbon atom (the number according to standard prostaglandin nomenclature being indicated by the subscript); B is a single bond or double bond; D is a subchain of 3 carbon atoms, having a hydroxyl group substituent; and R.sub.2 is 17-phenyl which is urnsubstituted or has at least one substituent selected from the group consisting of C.sub.1 -C.sub.5 alkyl groups, C.sub.1 -C.sub.4 alkoxy groups, trifluoromethyl groups, C.sub.1 -C.sub.3 aliphatic acylamino groups, nitro groups, and a phenyl group. 2. A method of treating glaucoma or ocular hypertension in humans by topical application of a therapeutic composition according to claim 1. 3. The therapeutic composition of claim 1, wherein B is a single bond. 4. The therapeutic composition of claim 1, wherein B is a double bond. 5. The therapeutic composition of claim 1, wherein R.sub.2 is an unsubstituted 17-phenyl group. 6. The therapeutic composition of claim 1, wherein R.sub.2 is a 17-phenyl group having at least one substituent selected from the group consisting of C.sub.1 -C.sub.5 alkyl groups, C.sub.1 -C.sub.4 alkoxy groups, trifluoromethyl groups, C.sub.1 -C.sub.3 aliphatic acylamino groups, nitro groups, and a phenyl group. 7. The therapeutic composition of claim 1, wherein the prostaglandin is a PGF prostaglandin. 8. The therapeutic composition of claim 1, wherein said hydroxyl group substituent is on the C.sub.15 atom of the D subchain. 9. The therapeutic composition of claim 8, wherein R.sub.2 is an unsubstituted 17-phenyl group. 10. The therapeutic composition of claim 8, wherein the prostaglandin is a PGF prostaglandin, the hydroxyl group substituent on the C.sub.15 atom of the D subchain is a 15-(R) hydroxy substituent, and R.sub.2 is an unsubstituted 17-phenyl group. 11. The therapeutic composition of claim 1, wherein said prostaglandin is 17-phenyl-18,19,20-trinor-PGF.sub.2.alpha. -isopropylester. 12. The therapeutic composition of claim 1, wherein said prostaglandin is 15-(R)-17-phenyl-18,19,20-trinor-PGF.sub.2.alpha. -isopropylester. 13. The therapeutic composition of claim 1, wherein said prostaglandin is 13,14-dihydro-17-phenyl-18,19,20-trinor-PGF.sub.2.alpha. -isopropylester. 14. The therapeutic composition of claim 1, wherein said prostaglandin is 15-(R,S)-17-phenyl-18,19,20-trinor-PGF.sub.2.alpha.. 15. A therapeutic composition for topical treatment of glaucoma or ocular hypertension in humans containing a prostaglandin PGA, PGB, PGE or PGF in an amount sufficient to reduce intraocular pressure without causing substantial ocular irritation and an ophthalmologically compatible vehicle, wherein the omega chain of the prostaglandin has the formula C.sub.13 --B--C.sub.14 --D--R.sub.2 wherein C is a carbon atom (the number according to standard prostaglandin nomenclature being indicated by the subscript); B is a single bond or double bond; D is a subchain of 2-5 carbon atoms, with a substituent at C.sub.15 selected from the group consisting of hydroxyl and oxo; and R.sub.2 is a terminal phenyl group which is unsubstituted or has at least one substituent selected from the group consisting of C.sub.1 -C.sub.5 alkyl groups, C.sub.1 -C.sub.4 alkoxy groups, trifluoromethyl groups, C.sub.1 -C.sub.3 aliphatic acylamino groups, nitro groups, and a phenyl group. 16. A method of treating glaucoma or ocular hypertension in humans by topical application of a therapeutic composition according to claim 15. 17. The therapeutic composition of claim 15, wherein B is a single bond. 18. The therapeutic composition of claim 15, wherein B is a double bond. 19. The therapeutic composition of claim 15, wherein D is a subchain of 3 carbon atoms and R.sub.2 is an unsubstituted 17-phenyl group. 20. The therapeutic composition of claim 15 wherein the substituent at C.sub.15 is hydroxyl. 21. The therapeutic composition of claim 15 wherein the substituent at C.sub.15 is oxo. 22. The therapeutic composition of claim 19 wherein the substituent at C.sub.15 is hydroxyl. 23. The therapeutic composition of claim 19 wherein the substituent at C.sub.15 is oxo. 24. The therapeutic composition of claim 15, wherein D is a subchain of 3 carbon atoms and R.sub.2 is a phenyl group having at least one substituent selected from the group consisting of C.sub.1 -C.sub.5 alkyl groups, C.sub.1 -C.sub.4 alkoxy groups, trifluoromethyl groups, C.sub.1 -C.sub.3 aliphatic acylamino groups, nitro groups, and a phenyl group. 25. The therapeutic composition of claim 15, wherein the prostaglandin is a PGF prostaglandin. 26. The therapeutic composition of claim 1, wherein said prostaglandin is 15-(R)-13,14-dihydro-17-phenyl-18,19,20-trinor-PGF.sub.2.alpha. -isopropyl ester. 27. The therapeutic composition of claim 8, wherein the prostaglandin is a PGF prostaglandin, the hydroxyl group substituent on the C.sub.15 atom of the D subchain is a 15-(S) hydroxy substituent, and R.sub.2 is an unsubstituted 17-phenyl group. 28. The therapeutic composition of claim 9, wherein the prostaglandin is a PGF.sub.60 prostaglandin and B is a double bond. 29. A therapeutic composition for topical treatment of glaucoma or ocular hypertension in humans containing a PGF.sub.2.alpha. prostaglandin in an amount sufficient to reduce intraocular pressure without causing substantial ocular irritation and an ophthalmologically compatible vehicle, wherein the omega chain of the prostaglandin has the formula C.sub.13 --B--C.sub.14 --D--R.sub.2 wherein C is a carbon atom (the number according to standard prostaglandin nomenclature being indicated by the subscript); B is a double bond; D is a subchain of 3 carbon atoms, having a hydroxyl group substituent on the C.sub.15 atom of the D subchain; and R.sub.2 is an unsubstituted 17-phenyl group.

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