Preventive and/or therapeutic drugs for inflammatory intestinal diseases
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An inflammatory bowel disease and drug technology, applied in the field of myeloperoxidase activity inhibitors, can solve the problem of no research on whether edaravone is effective for inflammatory bowel disease
Inactive Publication Date: 2005-10-12
MITSUBISHI TANABE PHARMA CORP
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As noted above, although superoxide anion, free radicals such as hydroxyl radicals, or hydrogen peroxide from macrophages and leukocytes have been shown to be associated with the development of ulcerative colitis, edara has not been studied Report on whether Bong is effective for inflammatory bowel disease
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[0116] Below, illustrate the present invention more specifically by embodiment, the present invention is not limited to following
[0117] Example.
Synthetic example
[0118] Synthesis example: Synthesis of 3-methyl-1-phenyl-2-pyrazolin-5-one (hereinafter referred to as edaravone)
[0119] 13.0 g of ethyl acetoacetate and 10.8 g of phenylhydrazine were added to 50 ml of ethanol, and the mixture was stirred under reflux for 3 hours. After the reaction solution was left to cool, the precipitated crystals were filtered and recrystallized from ethanol to obtain 1.3 g of the title compound as colorless crystals.
[0120] Yield 67%
[0121] Melting point 127.5~128.5℃
Embodiment 1
[0123] (1) Experimental method
[0124] 1 material
[0125] The edaravone synthesized as above was dissolved in a small amount of 1N sodium hydroxide solution, and the pH was adjusted to be near neutral.
[0126] 2 Methods of glycosyl esters (DSS) inducing colitis
[0127] Using 6-week-old Sprague-Dawley male rats (Japan CLEA Co., Ltd., according to the existing method (Araki, Y., et al., Scand J Gastroentero, 35, 1060-1067, 2000), the following induced in rats Colitis. That is, add 4% (w / w) sugar anhydroester (DSS: molecular weight 5000, Wako Pure Chemical Industry Co., Ltd., Osaka) in powdered food MF (Oriental Yeast Industry Co., Ltd.), with 30g / The amount of day / only was fed to the rats. Since the beginning of DSS administration, the Edaravone administration group was injected with 1mg / kg / day, 5mg / kg / day, and 20mg / kg / day of Edaravone in the morning and evening respectively. Subcutaneously in the back. The control group also injected saline subcutaneously in the back. ...
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Abstract
The object of the present invention is to provide a medicament useful for preventing and / or treating inflammatory bowel disease. The present invention provides a medicament for preventing and / or treating inflammatory bowel disease which comprises as an active ingredient a pyrazolone derivative represented by the following formula (I) or a physiologically acceptable salt thereof, or a hydrate thereof or a solvate thereof: wherein R<1> represents a hydrogen atom, an aryl group, an alkyl group, or an alkoxycarbonylalkyl group; R<2> represents a hydrogen atom, an aryloxy group, an arylmercapto group, an alkyl group or a hydroxyalkyl group; or R<1> and R<2> are combined with each other to represent an alkylene group; and R<3> represents a hydrogen atom, an alkyl group, a cycloalkyl group, a hydroxyalkyl group, a benzyl group, a naphthyl group, a phenyl group, or a phenyl group substituted with 1 to 3 substituents selected from the group consisting of an alkyl group, an alkoxy group, a hydroxyalkyl group, an alkoxycarbonyl group, an alkylmercapto group, an alkylamino group, a dialkylamino group, a halogen atom, a trifluoromethyl group, a carboxyl group, a cyano group, a hydroxyl group, a nitro group, an amino group and an acetamide group.
Description
technical field [0001] The present invention relates to a drug for preventing and / or treating inflammatory bowel disease, an intestinal mucosal protective agent, and neutrophils containing pyrazolone derivatives or physiologically acceptable salts thereof, or hydrates or solvates thereof as active ingredients Activation inhibitors, and myeloperoxidase activity inhibitors. Background technique [0002] Inflammatory Bowel Disease (IBD) such as ulcerative colitis (UC) and Crohn's disease (CD) have various causes, such as bacterial infection theory, autoimmune abnormality theory, etc. , but the reason for this is still unclear. However, since its incidence is increasing as civilization advances, it has been shown to be associated with environmental factors such as mental stress. For its treatment, oral, adrenal corticosteroid (prednisolone) containing sulfasalazine (Sakazosulfapyridine) or aminosalicylic acid (for example, 5-aminosalicylic acid) as active ingredients are mainl...
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