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Pharmaceutical composition containing diazepine and carbazole compound and application thereof

A composition and compound technology, applied in the application field of preparing antitumor drugs, can solve the problems of looseness, low bioavailability, moisture absorption and the like

Inactive Publication Date: 2018-05-15
南京众慧网络科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, when studying the oral pharmaceutical preparation of this compound, it was found that its bioavailability was not high, and after the prepared oral preparation tablet was stored for 3 months, the moisture absorption was serious, and spots and loose phenomena appeared on the tablet. Therefore, it is necessary to develop Oral preparations with stable and high bioavailability of the compound of formula I,

Method used

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  • Pharmaceutical composition containing diazepine and carbazole compound and application thereof
  • Pharmaceutical composition containing diazepine and carbazole compound and application thereof
  • Pharmaceutical composition containing diazepine and carbazole compound and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] Example 1 1-(2,3,5,10-tetrahydro-[1,2]diazepine And[3,4,5,6-def]carbazol-6(1H)-one-10-yl)-3-(4-ethoxycarbonyl)phenylurea

[0029] Step 1 Synthesis of methyl 2-bromo-3-((3-oxocyclohex-1-en-1-yl)amino)benzoate

[0030]

[0031] Weigh 3.58g of methyl 3-amino-2-bromobenzoate and 1.68g of cyclohexane-1,3-dione into a reaction flask, add 20ml of acetic acid to dissolve, and react at 80°C for 8h. After the reaction, evaporate under reduced pressure Remove the solvent and purify by column chromatography to obtain the title compound.

[0032] LC-MS m / z: [M+H]+=325.

[0033] Step 2 Synthesis of 4-oxo-2,3,4,9-tetrahydro-1H-carbazole-5-carboxylic acid methyl ester

[0034]

[0035] Weigh 1.62g of the product obtained in step 1, 0.23g of palladium acetate, 1.22g of tris(o-tolyl)phosphine and 0.63g of triethylamine in a sealed tube, add 15ml of acetonitrile, and seal the reaction at 100°C for 20 hours under a nitrogen atmosphere, and the reaction is complete After cooling,...

Embodiment 2

[0056] Example 2 1-(2,3,5,10-tetrahydro-[1,2]diazepine Synthesis of [3,4,5,6-def]carbazol-6(1H)-on-10-yl)-3-(4-ethoxycarbonyl)phenylurea citrate

[0057] Weigh 1.0 g of the compound of Example 1 into a reaction flask, add 20 ml of chloroform to dissolve it, add 0.42 g of citric acid, stir at room temperature for 3 h, and evaporate the solvent under reduced pressure to obtain the title compound.

Embodiment 3

[0058] Example 3 1-(2,3,5,10-tetrahydro-[1,2]diazepine Synthesis of [3,4,5,6-def]carbazol-6(1H)-on-10-yl)-3-(4-ethoxycarbonyl)phenylurea citrate

[0059] Weigh 1.0 g of the compound of Example 1 into a reaction flask, add 20 ml of chloroform to dissolve it, add 0.21 g of citric acid, stir at room temperature for 3 h, and evaporate the solvent under reduced pressure to obtain the title compound.

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PUM

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Abstract

The invention belongs to the field of medicinal preparations and particularly relates to a pharmaceutical composition containing a diazepine and carbazole compound and application thereof to preparation of an anti-tumor drug. The pharmaceutical composition comprises 10-20 percent by weight of compound shown as a formula (I), 5-20 percent of copovidone, 25-50 percent of hydroxypropyl-beta-cyclodextrin, 10-55 percent of a filling agent, 10-35 percent of a disintegrating agent and 0.5-1.5 percent of a lubricating agent and has high bioavailability and good stability.

Description

technical field [0001] The invention belongs to the field of pharmaceutical preparations, in particular to a diazepine-containing The pharmaceutical composition of the carbazole compound, and the application of the pharmaceutical composition containing the compound in the preparation of antitumor drugs. Background technique [0002] Indoleamine 2,3-dioxygenase (IDO) is the only rate-limiting enzyme that catalyzes the metabolism of tryptophan along the kynurenine pathway outside the liver, and has been shown to be associated with tumors, Alzheimer's disease, depression, and aging Cataract and other major human diseases are closely related, and the abnormal increase of IDO expression or activity is an important factor leading to the above diseases. Therefore, screening efficient IDO inhibitors can provide effective therapeutic drugs for these diseases. [0003] In recent years, studies have confirmed that the expression of IDO in various solid tumors such as lung cancer, liv...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K47/32A61K47/40A61K31/551A61P35/00
CPCA61K47/32A61K31/551A61K47/40
Inventor 许乐
Owner 南京众慧网络科技有限公司