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Therapeutic for gout or hyperuricemia

A technology for hyperuricemia and gout, which can be used in drug combination, drug delivery, pharmaceutical formulation and other directions, and can solve problems such as the use of colchicine

Pending Publication Date: 2022-01-11
NIPPON CHEMIPHAR CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, colchicine has limitations and is contraindicated in patients with hepatic or renal impairment

Method used

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  • Therapeutic for gout or hyperuricemia
  • Therapeutic for gout or hyperuricemia
  • Therapeutic for gout or hyperuricemia

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0255] Hereinafter, the present invention will be described in more detail with examples, reference examples, comparative reference examples, test examples, etc., but the present invention is not limited to these contents.

[0256]

[0257] Dissolve 9 g of compound 14 (2-(3-cyano-4-phenoxyphenyl)-7-hydroxythiazolo[5,4-d]pyrimidine) in tetrahydrofuran (sometimes abbreviated as THF), ethanol and water After 1936g of mixed solvent (weight ratio: THF / ethanol / water=1600.5 / 254.5 / 81) (slightly heated and dissolved), it is pumped into the spray drier via a peristaltic pump at a speed of about 5mL / min, and is injected from a 2-fluid nozzle (diameter 508μm) with an inlet temperature of 80°C, an outlet temperature of about 60°C, and a dry air volume of 0.30m 3 / min and nozzle spray air pressure 1.0kgf / cm 2 conditions for spray drying and granulation. The obtained dried product was left overnight at room temperature to obtain 100% amorphous compound 14.

[0258] For the volume averag...

reference example 1

[0271] The HPMCAS used in Reference Example 1b is MF type (that is, the substitution ratio per 1 monomer unit is methoxy: 21.0-25.0%, hydroxypropoxy: 5.0-9.0%, acetyl: 7.0-11.0%, amber Acyl: 10.0-14.0%, viscosity: 2.4-3.6mPa·s).

[0272] [Form 2B]

[0273]

reference example 2

[0279]

[0280] Compound 14 was dissolved in tetrahydrofuran to prepare 2.5 mg / mL. Each polymer shown in Table 4B was dissolved in a mixed solvent (methanol / dichloromethane=3 / 4) to prepare about 45 mg / mL. The compound 14 solution was added to the above polymer solution while stirring so that the weight ratio of the compound 14 to the polymer became 1:25. In addition, a sample in which no polymer was added was also prepared. Immediately, the mixture was transferred to an eggplant-shaped flask, and the organic solvent was distilled off with a rotary evaporator (N-1100, Tokyo Rikagaku Co., Ltd.). The eggplant-shaped flask was moved to a desiccator, and dried under reduced pressure using a vacuum pump for about 16 hours to obtain a solid dispersion of compound 14. After the solid dispersion was dried, it was pulverized with an agate mortar or a portable high-speed pulverizer (LM-PLUS, Osaka Chemical Co., Ltd.), and then sieved (mesh: 150 μm).

[0281] [Form 4B]

[0282] ...

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Abstract

The present invention provides a pharmaceutical composition for treating or preventing gout or hyperuricemia that contains a compound represented by general formula (I) (in the formula, R1 represents a substituted or unsubstituted phenyl group, R2 represents a cyano group or a nitro group, R3 represents a hydrogen atom or a hydroxyl group, X represents an oxygen atom or -S(O)n-, n represents an integer of 0-2, and Y represents an oxygen atom or a sulfur atom) or a pharmaceutically acceptable salt thereof.

Description

technical field [0001] The present invention relates to a pharmaceutical composition for treatment or prevention of gout or hyperuricemia. [0002] This application claims priority based on Japanese Patent Application No. 2019-104534 for which it applied in Japan on June 4, 2019, and uses the content for this specification. Background technique [0003] Hyperuricemia causes gout, renal failure, etc., and is considered a risk factor for coronary artery disease. In addition, it is pointed out that it is also closely related to the onset and progression of lifestyle-related diseases represented by hypertension. Therefore, the treatment of hyperuricemia is not only related to the treatment of gout, but also related to the prevention of various lifestyle-related diseases accompanying aging. [0004] At present, xanthine oxidase inhibitors such as allopurinol and febuxostat are mainly used in the treatment of hyperuricemia. [0005] These agents are very excellent agents from t...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61P19/06
CPCA61K31/519A61P19/06C07D513/04A61K9/1652A61K9/146A61K47/38A61K9/48A61K9/0053A61K9/10
Inventor 小林四郎宫山绘里平野益治太田隆
Owner NIPPON CHEMIPHAR CO LTD
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