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Preventive or remedy for diseases caused by hyperglycemia

A technology for hyperglycemia and postprandial hyperglycemia, applied to metabolic diseases, medical preparations containing active ingredients, organic active ingredients, etc.

Inactive Publication Date: 2006-03-08
KISSEI PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, oral administration of phlorizin does not have this effect because of the degradation effect of β-glucosidase present in the gastrointestinal tract (for example, see the following literatures 21-22)

Method used

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  • Preventive or remedy for diseases caused by hyperglycemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0114] 5-Hydroxy-3-methyl-2-(4-[3-(3-pyridylmethyl)ureido]benzyl}-phenyl β-D-galactopyranoside

[0115] To the 2-(4-aminobenzyl)-5-methoxycarbonyloxy-3-methylphenyl 2,3,4,6-tetra-O-acetyl-β-D-galactopyran To a solution of glycoside (0.25g) and pyridine (0.043ml) in dichloromethane (10ml) was added 4-nitrophenylchloroformate (90mg), and the mixture was stirred at room temperature for 12 hours. Then, 3-aminomethylpyridine (0.045ml) and triethylamine (0.11ml) were added to the reaction mixture, and the mixture was stirred at room temperature for 5 hours. The reaction mixture was concentrated under reduced pressure, and the residue was dissolved in methanol (8 ml). To this solution was added sodium methoxide (28% in methanol, 0.39 ml), and the mixture was stirred at room temperature for 2 hours. The reaction mixture was concentrated under reduced pressure, and the residue was washed successively in ODS (washing solvent: distilled water, eluent: methanol) and VARIAN BOND ELUT  ...

Embodiment 2

[0149] 3-(β-D-glucopyranoseoxy)-4-{[4-(2-guanidinoethoxy)-2-methylphenyl]methyl}-5-isopropyl-1H-pyridine azole

[0150] To 3-(2,3,4,6-tetra-O-acetyl-β-D-glucopyranoseoxy)-4-{[4-(2-aminoethoxy)-2-methylbenzene Base] methyl}-5-isopropyl-1H-pyrazole (0.6 grams) in tetrahydrofuran (5ml)-N, N-dimethylformamide (1ml) solution, add N-(benzyloxycarbonyl) - 1H-pyrazole-1-carboxamidine (N-(benzyloxycarbonyl)-1H-pyrazole-1-carboxamidine) (1.89 g), and the mixture was stirred at 60°C for 20 hours. The reaction mixture was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (eluent: n-hexane / ethyl acetate=1 / 1-ethyl acetate-ethyl acetate / ethanol=10 / 1) to obtain 3-(2 , 3,4,6-tetra-O-acetyl-β-D-glucopyranosyloxy)-4-({4-[2-(N′-benzyloxycarbonyl-guanidino)ethoxy] -2-Methylphenyl}methyl)-5-isopropyl-1H-pyrazole (0.31 g). This material was dissolved in methanol (6ml). To the methanol solution was added sodium methoxide (28% methanol solution,...

Embodiment 3

[0154] Testing for inhibition of SGLT1 activity in rats

[0155] 1) Cloning and construction of vector expressing rat SGLT1

[0156] Rat kidney cDNA library (QUICK-Cline TM cDNA; Clontech) was used as a template to amplify a DNA fragment of 111-2203bp encoding rat SGLT1 (accession number: M16101, reported by Kasahara et al.) by PCR method, and inserted into the SrfI site of pCMV-Script (Stratagene). The inserted DNA sequence exactly matches the previously reported sequence at the amino acid level.

[0157] 2) Establish a cell line stably expressing rat SGLT1

[0158] The expression vector of rat SGLT1 was digested with MluI to form linear DNA. This linear DNA was transferred into CHO-K1 cells by lipofection (Superfect transfection reagent: QIAGEN). Neomycin-resistant cell lines were selected by culturing in a medium containing G418 (1 mg / mL, LIFE TECHNOLOGIES), and then the activity of antagonizing methyl-α-D-glucopyranose uptake was measured by the following method. The...

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PUM

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Abstract

It is intended to provide a medicinal composition containing as the active ingredient a selective SGLT1 inhibitor (for example, an SGLT1 inhibitor substantially showing no GLUT2 and / or GLUT5 inhibitory effect) which exerts a sugar absorption inhibitory effect over a wide range, also has a hypoglycemic effect caused by fructose intake in usual diet and thus can show an outstanding hypoglycemic effect and which is appropriate as a preventive or a remedy for diseases caused by hyperglycemia (for example, diabetes, impaired glucose tolerance, diabetic complications or obesity).

Description

technical field [0001] The present invention relates to preparations for preventing or treating hyperglycemia-related diseases, which contain a selective Na-dependent glucose transporter (hereinafter referred to as SGLT) 1 inhibitor as an active ingredient. [0002] More specifically, the present invention relates to a preparation for preventing or treating hyperglycemia-related diseases, which comprises, as an active ingredient, an SGLT1 inhibitor which does not substantially inhibit the absorption of fructose through the small intestine, for example, does not substantially promote Effects of glucose transporter (hereinafter referred to as GLUT) 2 and / or SGLT1 inhibitors without GLUT5 inhibition. Background technique [0003] In recent years, with the rapid increase of diabetic patients and the need for strict control of blood sugar levels as confirmed by large-scale clinical trials (see the following documents 1-3), various preparations for treating diabetes are being deve...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K45/00A61K31/7056A61K31/706A61P3/04A61P43/00
CPCA61K31/706A61K31/7056A61P3/10A61P3/04A61P43/00A61K45/00
Inventor 伊东史显柴崎利英戸前昌樹伏见信彦伊佐治正幸
Owner KISSEI PHARMA
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