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Hydrochloride of fused-heterocycle compound

A compound and drug technology, applied in the field of hydrochloride of fused heterocyclic compounds, can solve the problems of no specific record of physical properties, no record of biological test data, etc.

Inactive Publication Date: 2004-07-07
SANKYO CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, the hydrochloride as the compound of the present invention not only has no biological test data described in the above-mentioned documents, but also has no specific description of physical properties.

Method used

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  • Hydrochloride of fused-heterocycle compound
  • Hydrochloride of fused-heterocycle compound

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0057] Preparation Example 1. Powder

[0058] 4 g of Compound A, 10 g of polyvinylpyrrolidone, and 0.5 g of hydroxypropylmethylcellulose (trade name: TC-5E, manufactured by Shin-Etsu Chemical Co., Ltd.), which is the compound of the present invention, were mixed and pulverized for 30 minutes using a vibrating mill. Get powder.

preparation example 2

[0059] Preparation example 2. Capsules

[0060] Dissolve 20 g of Compound A and 20 g of polyvinylpyrrolidone in a mixed solvent of 100 g of acetone and 100 g of ethanol, and spray the mixed solution into 200 g of croscarmellose sodium using a fluidized bed granulator to obtain granules. 0.1 g of hydroxypropylmethylcellulose (trade name: TC-5E, manufactured by Shin-Etsu Chemical Co., Ltd.) and 1.9 g of lactose were mixed with 10 g of the granules. Next, 0.24 g of the mixture was filled into gelatin capsules to obtain capsules. The capsules contained 0.1 g of compound A per capsule.

preparation example 3

[0061] Preparation Example 3. Tablet

[0062] 1 g of the compound and 1 g of polyvinylpyrrolidone were dissolved in a mixed solvent of 5 g of acetone and 5 g of ethanol, and then the organic solvent was distilled off under reduced pressure using a rotary evaporator. The solid matter thus obtained was pulverized to obtain fine particles. 0.25 g of crystalline cellulose, 0.25 g of low-substituted hydroxypropyl cellulose, 0.05 g of hydroxypropyl methylcellulose (trade name: TC-5E, manufactured by Shin-Etsu Chemical Co., Ltd.) were mixed with 1 g of the fine particles. After 0.18 g of lactose and 0.2 g of magnesium stearate, tableting was performed with a tablet machine to obtain tablets.

[0063] Compound 5-[4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)benzyl]thiazolidine-2,4-dione hydrochloride Salt shows excellent insulin resistance improving effect, hypoglycemic effect, anti-inflammatory effect, immunomodulatory effect, aldose reductase inhibitory effect, 5-lipoxygenase...

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Abstract

The present invention concerns the hydrochloride of the compound (5-Ä4-(6-methoxy-1-methyl-1H-benzimidazol-2-ylmethoxy)benzylÜthiazolid in-2,4-dione) of the following structure (I) which exhibits an excellent hypoglycemic activity and the like. <CHEM>

Description

technical field [0001] The present invention relates to improving hyperglycemia, impaired glucose tolerance (Impaired Glucose Tolerance: IGT) state, diabetic complications (such as retinopathy, nephropathy, neuropathy, cataract, coronary artery disease, etc.), hyperlipidemia and gestational diabetes mellitus (GestationalDiabetes Mellitus: GDM), Hydrochloride of a fused heterocyclic compound with excellent oral absorbability for diseases caused by insulin resistance such as polycystic ovary syndrome. [0002] Furthermore, the present invention also relates to diabetes mellitus, hyperglycemia, impaired glucose tolerance, diabetic complications (such as retinopathy, nephropathy, neuropathy, cataract, coronary artery disease), hyperlipidemia, which contain hydrochloride of a fused heterocyclic compound as an active ingredient. , obesity, hypertension, fatty liver, arteriosclerosis, diseases caused by insulin resistance, gestational diabetes, polycystic ovary syndrome, cardiovascul...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/427A61P3/04A61P3/06A61P3/10A61P9/10A61P19/06C07D235/00C07D277/00C07D417/12
CPCA61K31/427C07D417/12A61P19/06A61P3/10A61P3/04A61P3/06A61P9/10
Inventor 藤田岳藤原俊彦泉高司
Owner SANKYO CO LTD