Protective agent for retinal neuronal cell containing prostaglandin f2alpha derivative as active ingredient

• US 20090234005A1
• Filed: 03/31/2006
• Published: 09/17/2009
• Est. Priority Date: 03/31/2005
• Status: Abandoned Application

• Current Assignee: Asahi Glass Company, Limited (AGC, Inc.), Santen Pharmaceutical Company Limited
• Original Assignee: Asahi Glass Company, Limited (AGC, Inc.), Santen Pharmaceutical Company Limited
• Inventors: Ishida, Naruhiro, Shimazaki, Atsushi
• Application Number:
  US11/887,037
• Publication Number:
  US 20090234005A1
• Time in Patent Office: Days
• US Class Current: 514/559
• CPC Class Codes: A61K 31/5575 having a cyclopentane, e.g. prostaglandin E2, prostaglandin F2-alpha
• CPC Class Codes: A61P 25/00 Drugs for disorders of the nervous system
• CPC Class Codes: A61P 27/00 Drugs for disorders of the senses
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 9/10 for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis

Abstract

An object of the present invention is to find a new pharmaceutical application of a prostaglandin F2α derivative. It was found that the prostaglandin F2α derivative inhibits glutamate-induced retinal neuronal cell death in a concentration-dependent manner in rat fetal retinal neuronal cells, in other words, the prostaglandin F2α derivative acts directly on the retinal neuronal cells and exhibits a protective effect. Accordingly, the prostaglandin F2α derivative is useful for the prevention or treatment of an eye disease associated with retinal neuronal cell damage.

Claims

1. A protective agent for a retinal neuronal cell comprising a prostaglandin F2α

derivative as an active ingredient.

2. The protective agent for a retinal neuronal cell according to claim 1, wherein the prostaglandin F2α

derivative is a fluorine-containing prostaglandin F2α

derivative.

3. The protective agent for a retinal neuronal cell according to claim 2, wherein the fluorine-containing prostaglandin F2α

derivative is a 15,15-difluoroprostaglandin F2α

derivative.

4. The protective agent for a retinal neuronal cell according to claim 3, wherein the 15,15-difluoroprostaglandin F2α

derivative is a compound represented by the following general formula (I) or a salt thereof;

wherein R represents a hydroxyalkyl group, a formyl group, a carboxy group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aminocarbonyl group, an alkylaminocarbonyl group or an arylaminocarbonyl group, and when R is an aryloxycarbonyl group or an arylaminocarbonyl group, the aryl moiety thereof may have a substituent.

5. The protective agent for a retinal neuronal cell according to claim 4, wherein in the general formula (I), R represents a carboxy group or a salt group thereof or an alkoxycarbonyl group.

6. The protective agent for a retinal neuronal cell according to claim 2, wherein the fluorine-containing prostaglandin F2α

derivative is a 15-monofluoroprostaglandin F2α

derivative.

7. The protective agent for a retinal neuronal cell according to claim 1, wherein the retinal neuronal cell is a photoreceptor cell, a bipolar cell, an optic ganglion cell, a horizontal cell or an amacrine cell.

8. The protective agent for a retinal neuronal cell according to claim 1, which is used for the prevention or treatment of an eye disease.

9. A method of protecting a retinal neuronal cell comprising administering an effective amount of a prostaglandin F2α

derivative to a patient.

10. The protection method according to claim 9, wherein the prostaglandin F2α

derivative is a fluorine-containing prostaglandin F2α

derivative.

11. The protection method according to claim 10, wherein the fluorine-containing prostaglandin F2α

derivative is a 15,15-difluoroprostaglandin F2α

derivative.

12. The protection method according to claim 11, wherein the 15,15-difluoroprostaglandin F2α

derivative is a compound represented by the following general formula (I) or a salt thereof;

wherein R represents a hydroxyalkyl group, a formyl group, a carboxy group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aminocarbonyl group, an alkylaminocarbonyl group or an arylaminocarbonyl group, and when R is an aryloxycarbonyl group or an arylaminocarbonyl group, the aryl moiety thereof may have a substituent.

13. The protection method according to claim 12, wherein in the general formula (I), R represents a carboxy group or a salt group thereof or an alkoxycarbonyl group.

14. The protection method according to claim 10, wherein the fluorine-containing prostaglandin F2α

derivative is a 15-monofluoroprostaglandin F2α

derivative.

15. The protection method according to claim 13, wherein the retinal neuronal cell is a photoreceptor cell, a bipolar cell, an optic ganglion cell, a horizontal cell or an amacrine cell.

16. A method of preventing or treating an eye disease associated with retinal neuronal cell damage comprising administering a therapeutically effective amount of a prostaglandin F2α

derivative to a patient.

17. The prevention or treatment method according to claim 16, wherein the prostaglandin F2α

derivative is a fluorine-containing prostaglandin F2α

derivative.

18. The prevention or treatment method according to claim 17, wherein the fluorine-containing prostaglandin F2α

derivative is a 15,15-difluoroprostaglandin F2α

derivative.

19. The prevention or treatment method according to claim 18, wherein the 15,15-difluoroprostaglandin F2α

derivative is a compound represented by the following general formula (I) or a salt thereof;

wherein R represents a hydroxyalkyl group, a formyl group, a carboxy group, an alkoxycarbonyl group, an aryloxycarbonyl group, an aminocarbonyl group, an alkylaminocarbonyl group or an arylaminocarbonyl group, and when R is an aryloxycarbonyl group or an arylaminocarbonyl group, the aryl moiety thereof may have a substituent.

20. The prevention or treatment method according to claim 19, wherein in the general formula (I), R represents a carboxy group or a salt group thereof or an alkoxycarbonyl group.

21. The prevention or treatment method according to claim 17, wherein the fluorine-containing prostaglandin F2α

derivative is a 15-monofluoroprostaglandin F2α

derivative.

22. The prevention or treatment method according to claim 16, wherein the retinal neuronal cell is a photoreceptor cell, a bipolar cell, an optic ganglion cell, a horizontal cell or an amacrine cell.

23-30. -30. (canceled)