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Taxol and CDKS kinase inhibitor anti-tumor combined pharmaceutical composition

A kinase inhibitor, paclitaxel technology, applied in the field of chemical medicine, can solve problems such as the ineffectiveness of anticancer agents, and achieve the effects of reducing clinical dosage, reducing toxic side effects, and good anticancer efficacy

Inactive Publication Date: 2018-06-08
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 approach may not work for other combinations of anticancer agents, and such combinations may not always produce a Combinations with favorable therapeutic effects

Method used

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  • Taxol and CDKS kinase inhibitor anti-tumor combined pharmaceutical composition
  • Taxol and CDKS kinase inhibitor anti-tumor combined pharmaceutical composition
  • Taxol and CDKS kinase inhibitor anti-tumor combined pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 1-phenyl-3-methyl-7-(5-(5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl)pyridin-2-ylamino ) Synthesis of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione

[0019]

[0020] Step 1 Synthesis of 2-amino-5-(5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl)pyridine

[0021]

[0022] Weigh 2.24g of 5-methyl-2,5-diazabicyclo[2.2.1]heptane into a reaction flask, add 50ml of DMF / water mixed solvent with a volume ratio of 1:1 to dissolve, add 0.52g of 2- Amino-5-chloropyridine was reacted at 100°C for 8 hours. After the reaction was completed, 20ml of water was added, extracted with ethyl acetate, the organic phase was dried over anhydrous sodium sulfate, filtered, and spin-dried to obtain the title compound.

[0023] LC-MS m / z:[M+H] + =205.

[0024] Step 2 1-phenyl-3-methyl-7-(5-(5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl)pyridin-2-ylamino) Synthesis of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione

[0025] Using the product obtained in Step 1, 2,4-dichloro-5-nitropyrimidine, and ...

Embodiment 2

[0028] Example 2 1-phenyl-3-methyl-7-(5-(5-methyl-2,5-diazabicyclo[2.2.1]hept-2-yl)pyridin-2-ylamino ) Synthesis of pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione hydrobromide

[0029]

[0030] Weigh 15g of the compound of Example 1 into a reaction flask, add 50ml of dichloromethane to dissolve, add 5.9g of hydrobromic acid, heat up to 45°C and stir for 0.5h, after cooling to room temperature, evaporate the solvent under reduced pressure to obtain the title compound.

experiment example 1

[0031] Experimental Example 1 Stability Experiment

[0032] Weighed 4 copies of 1 g of the compounds of Examples 1 to 3, and placed them under the conditions of light 4500Lx, RH70% 75°C, RH70% 60°C and RH70% room temperature for 1 month. The experimental results are shown in Table 1.

[0033] Table 1

[0034]

[0035] Experimental results show that the compounds of Examples 2 and 3 of the present invention have very high stability.

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Abstract

The invention provides a taxol and CDKS kinase inhibitor anti-tumor combined pharmaceutical composition. The pharmaceutical composition comprises active components and pharmaceutically acceptable auxiliary materials, and is characterized in that the active components comprise taxol and a CDK4 / 6 kinase inhibitor or pharmaceutically salt; and the mass ratio of the taxol to the CDK4 / 6 kinase inhibitor or pharmaceutically salt in the active components is (2-8):1. The pharmaceutical composition is high in anti-tumor efficacy and low in toxic and side effect; and as the CDK4 / 6 kinase inhibitor has sensibility for the taxol, the combination of the CDK4 / 6 kinase inhibitor and taxol has a synergistic effect, the clinical dose of xeloda is reduced, toxic and side effect caused by the use of large dose of xeloda is reduced, the clinical treatment safety index is improved, and the pharmaceutical composition has a good clinical application prospect.

Description

technical field [0001] The invention belongs to the field of chemical medicine, and in particular relates to an anti-tumor combined pharmaceutical composition of paclitaxel and CDKS kinase inhibitor. 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 ca...

Claims

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Application Information

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IPC IPC(8): A61K31/337A61K31/519A61P35/00
CPCA61K31/337A61K31/519A61K2300/00
Inventor 王小丽
Owner 南京众慧网络科技有限公司
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