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New compound for gout and preparation method thereof, and application and pharmaceutical preparation of new compound

A compound and chemical technology, applied in the field of medicine, can solve the problem of inability to quickly oxidize and eliminate uric acid, and achieve the effect of simple preparation method and lower blood uric acid concentration

Inactive Publication Date: 2015-06-17
ANHUI YIXINMING PHARMA TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Due to the lack of urate oxidase in the human body, it cannot oxidize and eliminate uric acid as quickly as mammals

Method used

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  • New compound for gout and preparation method thereof, and application and pharmaceutical preparation of new compound
  • New compound for gout and preparation method thereof, and application and pharmaceutical preparation of new compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0034] Example 1: Preparation of 2-[5-bromo-4-(4-cyclopropyl-1-naphthyl)-4H-1,2,4-triazole-3-sulfanyl]-N-hydroxyacetamide

[0035] The technical route is as follows:

[0036]

[0037] 1) Preparation of 1-cyclopropylnaphthalene

[0038] To a dry 5 L round bottom flask, add 1-bromonaphthalene (414.0 g, 2 mol), [1,3-bis(diphenylphosphino)propane]nickel chloride (165 g, 0.4 mol) and 1500 mL of dry 3000 mL of THF solution of 1.0 mol / L cyclopropylmagnesium bromide was slowly added dropwise to the system with a constant pressure dropping funnel. After the dropwise addition, the reaction compound was stirred at room temperature for 8 h under nitrogen protection, then heated to reflux, and reacted for 36 h. After the reaction was complete, the reaction mixture was cooled to room temperature, then carefully poured into 10 L of stirred ice water, stirred, and adjusted to pH 2 with concentrated hydrochloric acid, CH 2 Cl 2 (4000 mL×3) extraction. Combine the organic phases, wash...

Embodiment 2

[0057] Example 2: Preparation of formula 1 compound tablet

[0058] prescription:

[0059]

[0060] Preparation Process:

[0061] ①. Pretreatment: The compound of formula 1, lactose monohydrate, microcrystalline cellulose, croscarmellose, low-substituted hydroxypropyl cellulose and magnesium stearate were respectively pulverized through a 100-mesh sieve.

[0062] ②. Total mixing: mix the compound of formula 1 and lactose monohydrate, then add magnesium stearate to increase fluidity, and mix well

[0063] Add other ingredients and mix well.

[0064] ③, tableting: direct tableting, the temperature between tableting is 20-25℃, and the relative humidity is controlled at 35-45%.

Embodiment 3

[0065] Example 3: Bioactivity assay

[0066] 1. Effect of formula I compound on mouse hyperuricemia

[0067] Experimental animals: healthy Kunming mice, weighing 15-20 g, provided by the Experimental Animal Center of Kunming Medical College. Breeding conditions: Room temperature is 25±2°C, relative humidity is 45-75%.

[0068] Grouping, modeling and administration: 40 Kunming mice were randomly divided into 4 groups, 10 in each group, half male and half male: normal control group, hyperuricemia model group, compound group of formula I, lesinurad group. The mice in the normal control group were injected intraperitoneally with 0.5% CMC-Na solution, and the mice in the other groups were injected intraperitoneally with oxonic acid potassium salt 500 mg / kg. After 1 hour, the mice in the normal control group and hyperuricemia model group were injected intraperitoneally. Volume 0.5% CMC-Na solution, and the mice in other groups were intraperitoneally injected with the test drug. ...

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Abstract

The invention relates to a new compound lesinurad hydroxamate disclosed as Formula I and a preparation method thereof, a pharmaceutical composition and preparation containing the new compound, and application of the new compound in drug preparation. The preparation method is implemented by reacting lesinurad methyl ester under the action of hydroxylamine hydrochloride. The method has the advantages of accessible raw materials, mild reaction conditions, high product yield and high product purity, and is simple to operate. The new compound has specific therapeutic actions on hyperuricemia, gout, arthritis and gouty arthritis, has the characteristics of high efficiency, low toxicity and high metabolism stability, and has wide application prospects.

Description

technical field [0001] The present invention relates to the field of medicine, in particular to a new compound hydroxamic acid lesinurad shown in formula I, a preparation method thereof, a pharmaceutical composition containing the new compound, and its use as a therapeutic agent, especially for hyperuricemia and gout Uses in medicine. Background technique [0002] Gout is a metabolic disease caused by the increase of blood uric acid level caused by purine metabolism disorder and (or) decreased uric acid excretion, and the deposition of monosodium urate crystals in joints, cartilage and kidneys. Its main manifestations are recurrent joint redness, swelling, heat, pain and dysfunction, and even joint deformity, nephrolithiasis and uric acid nephropathy. Hyperuricemia caused by decreased uric acid excretion or increased production is the main cause of gout. [0003] In recent years, the prevalence of gout and hyperuricemia has increased year by year. Epidemiological studies ...

Claims

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Application Information

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IPC IPC(8): C07D249/12A61K31/4196A61P19/06
CPCC07D249/12
Inventor 徐奎刘经星曽飞
Owner ANHUI YIXINMING PHARMA TECH
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