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Composition containing phenylaminopyrimidinyl indole derivative mixture and application of composition

A technology of anilinopyrimidinyl indole derivatives and compositions, which is applied in the field of medicine and can solve problems that need to be further improved

Inactive Publication Date: 2020-01-21
黄泳华
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] Plant extracts are rich in a variety of ingredients with antibacterial activity. For example, Yang Ruoying et al. reported (Journal of Tropical Biology, 2019, 10(03): 226-230.) The extracts of plants such as horn wind, six ear bells, rattan notoginseng, Guanzhong, golden thread grass, unipedal wind, eight hundred centimeters, and piercing stone have the effect on tobacco Ralstonia solanacearum at 100mg / L and / or 500mg / L Certain antibacterial activity, but the inventors found that the antibacterial activity of the above-mentioned plant extracts to other common pathogenic bacteria needs to be further improved

Method used

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  • Composition containing phenylaminopyrimidinyl indole derivative mixture and application of composition
  • Composition containing phenylaminopyrimidinyl indole derivative mixture and application of composition
  • Composition containing phenylaminopyrimidinyl indole derivative mixture and application of composition

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Experimental program
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Effect test

preparation example 1

[0020] The preparation of preparation example 1 plant extract

[0021] Ultrasonic extraction method is used to dry the shade-dried plant material at 40°C, crush it, pass through a 40-mesh sieve, and put it into a ziplock bag. Before the test, 50 g of plant dry powder was weighed, and different organic solvents were added for ultrasonic extraction (as shown in Table 1), and the extraction was repeated 3 times for 60 min each time. Concentrate after filtration and store in a refrigerator at 4°C until use.

[0022] Table 1 Organic solution of ultrasonic extraction of different plant extracts

[0023] plant material Extract number Organic solvents wind PE1 Chloroform Fuji Sanchi PE2 Chloroform Six ear bells PE3 Methanol Eight hundred percent PE4 n-heptane Bone style PE5 ethanol Gastrodia PE6 acetone Guan Zhong PE7 Isopropanol broken bone PE8 Chloroform Guangchamasma PE9 n-heptane go...

Embodiment 1

[0096] Example 1 Preparation of Oral Solid Formulation of Composition Containing a Mixture of Anilinopyrimidinyl Indole Derivatives

[0097] Prescription (1500 unit dose)

[0098]

[0099]

[0100] Preparation

[0101] Take the prescribed amount of MIX (X-Y-PEZ) and auxiliary materials, and pass through a 100-mesh sieve. Take MIX (X-Y-PEZ), lactose, microcrystalline cellulose, crospovidone and starch and mix thoroughly; take the prescribed amount of hypromellose, and prepare it into a product with a concentration of 10% based on hypromellose Solution, adjust the pH to 3.0-4.0 with lactic acid, add to the above-mentioned mixed material to make a soft material, granulate with a 16-mesh sieve, and dry at 80°C for 3-4 hours. Use a 16-mesh sieve to sieve the granules, add the prescribed amount of micropowder silica gel and magnesium stearate, mix well, fill the capsules, and obtain capsules;

[0102] Take the prescribed amount of MIX (X-Y-PEZ) and auxiliary materials, an...

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Abstract

The invention provides a composition of a mixture containing a first phenylaminopyrimidinyl indole derivative and phenylaminopyrimidinyl indole derivative which are different from each other. The mixture can have synergistic antibacterial effects on streptococcus parasanguis, staphylococcus cohnii, neisseria gonorrhoeae, peptostreptococcus prevotii, staphylococcus hominis, serratia liquefaciens, achromobacter xylosoxidans, mycobacterium murinum, corynebacterium macginleyi, morganella morganii, staphylococcus capitis, streptococcus sanguis, streptococcus pyogenes, peptostreptococcus anaerobius,alkali cellulase producing chryseomonas luteola, aeromonas caviae, enterobacter cloacae, micrococcus luteus, dendritic microbacterium and legionella pneumophila with extracts of plants such as broad-leaved echinops roots, stonecrop, cyrtomium rhizomes, standish's lonicera and rhizoma alocasiae macrorrhizae.

Description

technical field [0001] The invention belongs to the technical field of medicine, and specifically relates to a composition containing a mixture of anilinopyrimidinyl indole derivatives and its application. Background technique [0002] Nosocomial infection is an important issue affecting the quality of hospital care. With the continuous development and progress of modern medical technology, antibacterial drugs are widely used, and the drug-resistant strains of clinical pathogens are increasing. Therefore, improving the antibacterial activity of existing drugs will help to improve the therapeutic effect of patients with bacterial infections. [0003] CN110283052A discloses a variety of protein tyrosine kinase inhibitors with antibacterial activity, including anilinopyrimidinyl indole derivatives represented by formula I. [0004] [0005] Plant extracts are rich in a variety of ingredients with antibacterial activity. For example, Yang Ruoying et al. reported (Journal of...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/506A61K36/28A61K36/88A61K36/12A61K36/63A61K36/47A61K36/83A61K36/185A61K36/23A61P31/04
CPCA61K31/506A61K36/12A61K36/185A61K36/23A61K36/28A61K36/47A61K36/63A61K36/83A61K36/88A61P31/04A61K2300/00Y02A50/30
Inventor 向飞何沐
Owner 黄泳华
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