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Details for Patent: 5,578,618

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Details for Patent: 5,578,618

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. (Upsala, SE), Resul; Bahram (Upsala, SE)
Assignee: Pharmacia Aktiebolag (Upsala, SE)
Filing Date:Feb 16, 1995
Application Number:08/390,394
Claims:1. 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 double bonds, allene 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 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

R.sub.2 is an aromatic heterocyclic group having 5-6 ring atoms.

2. A composition according to claim 1 in which, in the omega chain, R.sub.2 is thiazol.

3. A composition according to claim 1 in which, in the omega chain, R.sub.2 is imidazole.

4. A composition according to claim 1 in which, in the omega chain, R.sub.2 is pyrrolidine.

5. A composition according to claim 1 in which, in the omega chain, R.sub.2 is thiophene.

6. A composition according to claim 1 in which, in the omega chain, R.sub.2 is oxazole.

7. 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 double bonds, allene 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 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

R.sub.2 is a cycloalkane or a cycloalkene with 3-7 carbon atoms in the ring, which is

(e) unsubstituted or

(f) has at least one substituent selected from the group consisting of lower alkyl groups with 1-5 carbon atoms.

8. 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 as 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 oxygen, sulfur, and nitrogen, 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

R.sub.2 is an aromatic heterocyclic group having 5-6 ring atoms.

9. A composition according to claim 8 in which, in the omega chain, R.sub.2 is thiazol.

10. A composition according to claim 8 in which, in the omega chain, R.sub.2 is imidazole.

11. A composition according to claim 8 in which, in the omega chain, R.sub.2 is pyrrolidine.

12. A composition according to claim 8 in which, in the omega chain, R.sub.2 is thiophene.

13. A therapeutic composition for in which, in the omega chain, R.sub.2 is oxazole.

14. 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 oxygen, sulfur, and nitrogen, 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

R.sub.2, is a cycloalkane or a cycloalkene with 3-7 carbon atoms in the ring, which is

(e) unsubstituted or

(f) has at least one substituent selected from the group consisting of lower alkyl groups with 1-5 carbon atoms.

15. A composition according to claim 1 in which the prostaglandin is a PGF.sub.2.alpha. and, in the omega chain of the prostaglandin, the D subchain contains 2-5 carbon atoms.

16. A composition according to claim 14 in which the prostaglandin is a PGF.sub.2.alpha. and, in the omega chain of the prostaglandin, the D subchain contains 2-5 carbon atoms.

17. A therapeutic composition for topical treatment of ocular hypertension or glaucoma containing a prostaglandin PGD 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 is a chain of 6 to 10 carbon atoms, which is either

(a) saturated or

(b) unsaturated having one or more double bonds, allene 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 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

R.sub.2 is an aromatic heterocyclic group having 5-6 ring atoms.

18. A composition according to claim 17 in which, in the omega chain of the prostaglandin the group R.sub.2 is thiazol.

19. A composition according to claim 17 in which, in the omega chain of the prostaglandin the group R.sub.2 is imidazole.

20. A composition according to claim 17 in which, in the omega chain of the prostaglandin the group R.sub.2 is pyrrolidine.

21. A composition according to claim 17 in which, in the omega chain of the prostaglandin the group R.sub.2 is thiophene.
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