Paclitaxel and diazepinocarbazole compound combined pharmaceutical composition

A technology of diazepines and carbazoles, which is applied in the field of combined pharmaceutical compositions of paclitaxel and diazazocarbazoles, can solve problems such as the ineffectiveness of anticancer agents, and achieves reduction of clinical dosage, toxic and side effects Low, good anti-cancer effect

Inactive Publication Date: 2018-09-28
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

While regimens involving combinations of anticancer agents with different mechanisms of action may work in the context of some combinations, the same approa

Method used

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  • Paclitaxel and diazepinocarbazole compound combined pharmaceutical composition
  • Paclitaxel and diazepinocarbazole compound combined pharmaceutical composition
  • Paclitaxel and diazepinocarbazole compound combined pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] 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

[0019] Step 1 Synthesis of methyl 2-bromo-3-((3-oxocyclohex-1-en-1-yl)amino)benzoate

[0020]

[0021] 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. LC-MS m / z: [M+H]+=325.

[0022] Step 2 Synthesis of methyl 4-oxo-2,3,4,9-tetrahydro-1H-carbazole-5-carboxylate

[0023]

[0024] 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, add 15ml of water ...

Embodiment 2

[0044] 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

[0045] 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

[0046] 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 methanesulfonic acid

[0047] Weigh 2.0 g of the compound of Example 1 into a reaction flask, add 50 ml of dichloromethane to dissolve it, add 0.42 g of methanesulfonic acid, stir at room temperature for 1 h, evaporate the solvent under reduced pressure, and obtain the title compound.

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PUM

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Abstract

The invention provides a paclitaxel and diazepinocarbazole compound combined pharmaceutical composition, which comprises active ingredients and pharmaceutically acceptable excipients. The paclitaxel and diazepinocarbazole compound combined pharmaceutical composition is characterized in that the active ingredients are composed of gemcitabine and a diazepinocarbazole compound as shown in the formulaI or pharmaceutically acceptable salts thereof; and mass ratio of gemcitabine to the diazepinocarbazole compound or the pharmaceutically acceptable salts in the active ingredients is (2-8): 1. The pharmaceutical composition has good anticancer curative effect but low toxic or side effect. As the diazepinocarbazole compound is sensitive to gemcitabine, the diazepinocarbazole compound and gemcitabine are combined to produce a synergistic effect. Thereby, clinical dosage of capecitabine is reduced, toxic or side effect caused by large dosage of capecitabine is decreased, and safety index of clinic treatment is raised. The paclitaxel and diazepinocarbazole compound combined pharmaceutical composition has a good clinical application prospect.

Description

technical field [0001] The invention belongs to the field of chemical medicine, a paclitaxel and diazepine and carbazole compounds combined pharmaceutical composition. Background technique [0002] Paclitaxel, English name Paclitaxel, alias taxol, porphyrin, special element, chemical name 5β, 20-epoxy-1, 2α, 4, 7β, 10β, 13α-hexahydroxytaxane-11-en-9-one -4,10-diacetate-2-benzoate-13[(2'R,3'S)-N-benzoyl-3-phenylisoserine ester], molecular weight 853.92, molecular formula C47H51NO14. It is a new type of anti-microtubule drug, which can maintain the stability of tubulin and inhibit cell mitosis by promoting tubulin polymerization and inhibiting depolymerization. In vitro experiments have proved that paclitaxel has a significant radiosensitizing effect, which may cause cells to stop in the G2 and M phases that are sensitive to radiotherapy. , lymphoma, and brain tumors also have certain curative effects. [0003] Another problem prevalent in cancer therapy is that most anti...

Claims

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Application Information

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IPC IPC(8): A61K31/551A61K31/337A61P35/00
CPCA61K31/551A61K31/337A61K2300/00
Inventor 王小丽
Owner 南京众慧网络科技有限公司
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