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AssigneeNone recorded
InventorsYoshiharu Hayashi, Nobuharu Goto
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The present invention relates to an agent for the prophylaxis and treatment of diabetic complications comprising, as an active ingredient, 4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid, an optically active compound thereof or a pharmaceutically acceptable salt thereof. The present invention further relates to a method for the prophylaxis and treatment of diabetic complications comprising administering an effective amount of this compound. The medicament of the present invention is useful for the prophylaxis and treatment of diabetic complications, namely, diabetic neuropathy, nephropathy, ophthalmopathy, arteriosclerosis and the like. The action of the drug is long-lasting for very small doses and a single administration a day is sufficient.
A method for the prophylaxis and treatment of diabetic ophthalmopathy, comprising administering an effective amount of 4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid, an optically active compound thereof or a pharmaceutically acceptable salt thereof.
A method for the prophylaxis and treatment of diabetic ophthalmopathy, comprising administering an effective amount of sodium 4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoate dihydrate.
A method for the prophylaxis and treatment of diabetic ophthalmopathy, comprising administering an effective amount of (S)-(−)-4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid or a pharmaceutically acceptable salt thereof.
A method for the prophylaxis and treatment of diabetic ophthalmopathy, comprising administering an effective amount of sodium (S)-(−)-4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoate ⅔ hydrate.
A method for the prophylaxis and treatment of diabetic arteriosclerosis, comprising administering an effective amount of 4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid, an optically active compound thereof or a pharmaceutically acceptable salt thereof.
A method for the prophylaxis and treatment of diabetic arteriosclerosis, comprising administering an effective amount of sodium 4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoate dihydrate.
A method for the prophylaxis and treatment of diabetic arteriosclerosis, comprising administering an effective amount of (S)-(−)-4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid or a pharmaceutically acceptable salt thereof.
A method for the prophylaxis and treatment of diabetic arteriosclerosis, comprising administering an effective amount of sodium (S)-(−)-4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoate {fraction (2/3)} hydrate.
Dependencies are inferred from the claim text.
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Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings: having two double bonds between…
Having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole: 1,3-Diazoles
Drugs for disorders of the metabolism
For glucose homeostasis: for hyperglycaemia, e.g. antidiabetics
Term end not estimated
The present invention relates to an agent for the prophylaxes and treatment of diabetic complications, namely, to an agent for the prophylaxis and treatment of diabetic neuropathy, nephropathy, ophthalmopathy and arteriosclerosis. More particularly, the present invention relates to an agent for the prophylaxis and treatment of diabetic complications comprising, as an active ingredient, 4-[α-hydroxy-2-methyl-5-(1-imidazolyl)benzyl]-3,5-dimethylbenzoic acid, an optically active compound thereof or a pharmaceutically acceptable salt thereof. The present invention further relates to a method for the prophylaxis and treatment of diabetic complications.
The discovery of insulin and its clinical application resulted in drastic progress in the treatment of diabetes. Life sustention of the patients with diabetes—which had been a deadly disease until then—was strikingly improved. However, the therapy of chronic complications of diabetes has become a new problem.
The therapy of diabetes aims at prevention of such chronic complications, and practically consists of a further control of blood glucose and a direct therapy of complications. The major chronic complications of diabetes are known to be neuropathy, nephropathy, ophthalmopathy, arteriosclerosis and the like (David M. et al., N. Engl. J. Med., 328, p.1676-1685(1993)).
The action as the agent for the prophylaxis and treatment of diabetic complications of the present invention, namely, the action as the agent for the prophylaxis and treatment of neuropathy, nephropathy, ophthalmopathy and arteriosclerosis, can be confirmed through rat tail nerve conduction velocity, sciatic nerve conduction velocity, degree of glomerular disorder, amount of urinary albumin excretion, degree of cataract examining funduscopy, degree of hypertrophy and the like.
Of the diabetic complications in the present invention, neuropathy means symmetric polyneuropathy of sensory, motor and autonomic nerves, and local or polydomous neuropathy of cerebral nerve; and ophthalmopathy means cataract, glaucoma, retinopathy, iritis and the like.
The compounds of the present invention can be synthesized by the methods described in Japanese Patent Examined Publication No. 41143/1993 and Japanese Patent Unexamined Publication No. 215771/1990.