Ophthalmological preparations

• US 20040063710A1
• Filed: 10/16/2003
• Published: 04/01/2004
• Est. Priority Date: 11/22/2000
• Status: Abandoned Application

• Current Assignee: Mitsubishi Tanabe Pharma Corporation (Mitsubishi Chemical Group Corp.)
• Original Assignee: Mitsubishi Tanabe Pharma Corporation (Mitsubishi Chemical Group Corp.)
• Inventors: Inoue, Erie, Sogo, Shunji, Mano, Tomiya
• Application Number:
  US10/432,401
• Publication Number:
  US 20040063710A1
• Time in Patent Office: Days
• US Class Current: 514/247
• CPC Class Codes: A61K 31/50 Pyridazines; Hydrogenated pyridazines
• CPC Class Codes: A61P 25/02 for peripheral neuropathies
• CPC Class Codes: A61P 27/02 Ophthalmic agents
• CPC Class Codes: A61P 27/06 Antiglaucoma agents or miotics
• CPC Class Codes: A61P 3/10 for hyperglycaemia, e.g. antidiabetics
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: A61P 9/00 Drugs for disorders of the cardiovascular system
• 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

The invention relates to an ophthalmic agent comprising, as an active ingredient, a compound having a cardiotonic action including a phenyl pyridazinone derivative or salt thereof, or a hydrate thereof or solvate thereof as a typical example. Specifically, the invention relates to a preventative and/or therapeutic agent for optic nerve diseases or retinal diseases.

Claims

7. A pharmaceutical composition for an optic nerve disease or a retinal disease, which comprises a compound having a cardiotonic action as an active ingredient.

8. The pharmaceutical composition according to claim 7, wherein the compound has enhancing action on calcium sensibility.

9. The pharmaceutical composition according to claim 7 or claim 8, wherein the optic nerve disease is selected from ischemic optic neuropathy and glaucoma.

10. The pharmaceutical composition according to clam 7 or 8, wherein the retinal disease is selected from retinal vein occlusion, retinal artery occlusion, and diabetic retinopathy.

11. A preventative and/or therapeutic agent for an optic nerve disease or a retinal disease which comprises a compound having a cardiotonic action as an active ingredient.

12. The preventative and/or therapeutic agent according to claim 11, wherein the compound has enhancing action on calcium sensibility.

13. The preventative and/or therapeutic agent according to claim 11 or claim 12, wherein the optic nerve disease is selected from ischemic optic neuropathy and glaucoma.

14. The preventative and/or therapeutic agent according to claim 11 or claim 12, wherein the retinal disease is selected from retinal vein occlusion, retinal artery occlusion, and diabetic retinopathy.

15. The preventative and/or therapeutic agent according to any one of claims 11 to 14, which is selected from an orally available agent, an injection, an eye drop, an ointment, a sustained release agent for placing inside of eyelid, and an ophthalmic circulatory solution.

16. An inhibitor against retinal ganglion cell death which comprises a compound having a cardiotonic action as an active ingredient.

17. The inhibitor against retinal ganglion cell death according to claim 16, wherein the compound has enhancing action on calcium sensibility.

18. An agent for protection of retinal ganglion cell which comprises a compound having a cardiotonic action as an active ingredient.

19. The agent for protection of retinal ganglion cell according to claim 18, wherein the compound has enhancing action on calcium sensibility.

20. A method for inhibiting retinal ganglion cells death by using a compound having a cardiotonic action.

21. The method for inhibiting retinal ganglion cells death according to claim 20, wherein the compound has enhancing action on calcium sensibility.

22. A method for protecting retinal ganglion cells by using a compound having a cardiotonic action.

23. The method for protecting retinal ganglion cells according to claim 22, wherein he compound has enhancing action on calcium sensibility.

24. An agent for suppression of retinal degeneration which comprises a compound having a cardiotonic action as an active ingredient.

25. The agent for suppression of retinal degeneration according to claim 24, wherein the retinal degeneration is caused by retinal ischemia.

26-1. The method for inhibiting retinal degeneration according to claim 27 or claim 28, wherein the compound has enhancing action on calcium sensibility.

27. A method for inhibiting retinal degeneration by using a compound having a cardiotonic action.

1. An ophthalmic agent which comprises a compound having a cardiotonic action as an active ingredient.

2. The ophthalmic agent according to claim 1, wherein the compound has enhancing action on calcium sensibility.

3. The ophthalmic agent according to claim 1 or 2, wherein the compound is a phenyl pyridazinone derivative represented by the following general formula (1) or (2) or a salt thereof, or a hydrate thereof or a solvate thereof:

4. The ophthalmic agent according to any one of claims 1 to 3, wherein the compound is a phenyl pyridazinone derivative represented by the following general formula (3) or a salt thereof, or a hydrate thereof or a solvate thereof:

5. The ophthalmic agent according to any one of claims 1 to 3, wherein the compound is represented by the general formula (1) or (2) according to claim 3 wherein R₁, R₂ and R₃ independently represent hydrogen atom, methyl group, or ethyl group, and R₄ represents 2-pyridyl group, 4-pyridyl group, 2-pyrimidyl group, or 4-quinolyl group.

6. The ophthalmic agent according to any one of claims 1 to 5, wherein the compound is represented by the general formula (3) according to claim 4, wherein A is 4-pyridyl group.

26. The agent for suppression of retinal degeneration according to claim 24 or claim 25, wherein the compound has enhancing action on calcium sensibility.

28. The method for inhibiting retinal degeneration according to claim 27, wherein the retinal degeneration is caused by retinal ischemia.