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Details for Patent: 6,417,230

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Details for Patent: 6,417,230

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 (Stockholm, SE)
Filing Date:Feb 12, 2001
Application Number:09/781,896
Claims:1. A therapeutic composition for topical treatment of ocular hypertension or glaucoma in humans containing a prostaglandin PGF in an amount sufficient to reduce intraocular pressure without causing substantial ocular irritation, and an ophthalmologically compatible vehicle, in which the alpha chain of the prostaglandin comprises a chain having the structure

and in which the omega chain of the prostaglandin has the formula

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 and 1-2 heteroatoms selected from the group consisting of O, N and S, with substituents on each carbon atom selected from the group consisting of a hydrogen atom, an alkyl group, an oxo group and a hydroxyl group; and

R.sub.2 is a phenyl group substituted with a trifluoromethyl group.

2. The therapeutic composition according to claim 1 wherein the prostaglandin is a PGF.sub.2.alpha..

3. The therapeutic composition of claim 2 wherein the substituents on C.sub.15 are a hydrogen atom and a hydroxyl group.

4. The therapeutic composition according to claim 2 wherein D is a subchain of tow carbon atoms and one heteroatom.

5. The therapeutic composition according to claim 4, wherein the substituents on C.sub.15 are a hydrogen atom and a hydroxyl group.

6. A method of treating ocular hypertension or glaucoma in humans by topical application of a therapeutic composition according to claim 1.

7. A method of treating ocular hypertension or glaucoma in humans by topical application of a therapeutic composition according to claim 5.

8. A therapeutic composition for the topical treatment of ocular hypertension or glaucoma in humans containing a prostaglandin in an amount sufficient to reduce intraocular pressure without causing substantial ocular irritation and an ophthalmologically compatible vehicle wherein said prostaglandin is 16-phenoxy-17,18,19,20-tetranorprostaglandin F.sub.2.varies..

9. A method for treating ocular hypertension or glaucoma in humans comprising topical administration of a therapeutically effective dose of the therapeutic composition of claim 8.
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