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Details for Patent: 5,627,208

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Details for Patent: 5,627,208

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 W. (Uppsala, SE), Resul; Bahram (Uppsala, SE)
Assignee: Pharmacia Aktiebolag (Uppsala, SE)
Filing Date:Jun 06, 1995
Application Number:08/470,607
Claims:1. In a therapeutic composition for topical treatment of ocular hypertension or glaucoma 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, the improvement comprising the omega chain of the prostaglandin having 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, a double bond, or a triple bond;

D represents a sub-chain of 1-10 carbon atoms with 1-2 heteroatoms selected from the group that consisists of N, and S, with substituents on each carbon atom that are selected from the group consisting of a hydrogen atom, an alkyl group, an oxo group and a hydroxyl group, and

an cycloalkyl or cycloalkenyl ring structure, with 3-7-carbon atoms in the ring, which is

(1) unsubstituted or

(2) substituted with at least one lower alkyl group containing 1-5 carbon atoms.

2. A composition according to claim 1 in which, in the omega chain of the prostaglandin, R.sub.2 is a cyclohexyl group.

3. A Method of treating glaucoma or ocular hypertension by topical application of the therapeutic composition of claim 1.

4. A method of treating glaucoma or ocular hypertension by topical application of the therapeutic composition of claim 2.

5. A therapeutic composition for topical treatment of ocular hypertension or glaucoma, 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, in which the alpha chain of the prostaglandin comprises a chain of 6 to 10 carbon atoms, which is either

(a) saturated or

(b) unsaturated having one or more non-cummulated double bonds, or a triple bond,

the alpha chain being

c) unsubstituted or

d) substituted with one or more substituents selected from the group of alkyl groups, alicyclic rings, aromatic rings or heteroaromatic rings,

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, a double bond, or a triple bond;

D represents a sub-chain of 1-10 carbon atoms and 1-2 heteroatoms selected from the group that consists of O, N, and S, with substituents on each sub-chain atom that are 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 cycloalkyl or cycloalkyenyl ring of 3 to 7 carbon atoms, which is unsubstituted or substituted with at least one lower alkyl substituent of 1-5 carbon atoms.

6. A composition according to claim 5 in which, in the omega chain of the prostaglandin, R.sub.2 is a cyclohexyl group.

7. A method of treating ocular hypertension or glaucoma by topical application of the therapeutic composition of claim 5.

8. A method of treating ocular hypertension or glaucoma by topical application of the therapeutic composition of claim 6.
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