Antitumor drug composition

A technology of anti-tumor drugs and compositions, applied in the field of chemical medicine, can solve the problems of ineffective anti-cancer drugs, achieve the effects of reducing clinical dosage, reducing toxic and side effects, and improving clinical application prospects

Inactive Publication Date: 2018-06-29
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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Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0018] Example 1 1-phenyl-3-methyl-7-(5-piperazinylpyridin-2-ylamino)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Synthesis

[0019]

[0020] Step 1 Synthesis of 1-tert-butoxycarbonyl-4-(2-aminopyridin-5-yl)piperazine

[0021]

[0022] Weigh 3.15g of anhydrous piperazine into a reaction flask, add 30m of dichloromethane to dissolve, slowly add dropwise at 0°C to dissolve 4g of (BOC) 2 O in dichloromethane solution, dropwise, react at room temperature for 2 hours, filter, evaporate the solvent, add 10ml of water, filter, add sodium carbonate to the aqueous solution to saturation, extract with dichloromethane 3 times, collect the organic phase, dry over sodium sulfate, filter, Spin dry to obtain 2.98g oil. Add 50ml of DMF / water mixed solvent with a volume ratio of 1:1 to the obtained oil to dissolve, add 0.41g of 2-amino-5-chloropyridine, and react at 100°C for 8h. After the reaction is completed, add 20ml of water, extract with ethyl acetate, and then The organic phase w...

Embodiment 2

[0048] Example 2 1-phenyl-3-methyl-7-(5-piperazinylpyridin-2-ylamino)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Synthesis of maleate

[0049]

[0050] Weigh 10.78g of the compound of Example 1 into a reaction flask, add 50ml of methanol aqueous solution with a volume ratio of 2:1 to dissolve, add 2.9g of maleic acid, heat up to 45°C and stir for 0.5h, after cooling to room temperature, cool in the refrigerator overnight , filtered, washed with methanol water at a volume ratio of 2:1, and dried to obtain the title compound.

Embodiment 3

[0051] Example 3 1-phenyl-3-methyl-7-(5-piperazinylpyridin-2-ylamino)pyrimido[4,5-d]pyrimidine-2,4(1H,3H)-dione Synthesis of hydrobromide

[0052]

[0053] 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.

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Abstract

The invention provides an antitumor drug composition, which is prepared from an active ingredient and a pharmacologically acceptable ingredient. The antitumor drug composition is characterized in thatthe active ingredient is prepared from gemcitabine and a CDK4 / 6 kinase inhibitor as shown in a formula I or pharmacologically acceptable salt thereof; the mass ratio of the gemcitabine and the CDK4 / 6kinase inhibitor or the pharmacologically acceptable salt thereof is (2 to 8):1. The drug composition is good in anticancer effect and low in toxic and side effects; due to the sensitivity of the CDK4 / 6 kinase inhibitor on the gemcitabine, the CDK4 / 6 kinase inhibitor and the gemcitabine are combined to produce a synergistic effect, so that the clinic dosage of capecitabine is reduced, the toxic and side effects produced by using a great amount of capecitabine are reduced, a clinic treatment safety index is improved, and a better clinic application prospect is realized.

Description

technical field [0001] The invention belongs to the field of chemical medicine and relates to an antitumor drug composition. Background technique [0002] Cyclin-dependent kinase (CDK) is a kind of serine / threonine kinase, as an important signal transduction molecule in the cell, and the CDK-cyclin complex formed by cyclin (cyclin), participates in the Growth, proliferation, dormancy, or apoptosis. The CDK family includes 1-13, among which, CDK4 and CDK6 link the cyclin D family (cyclin D1, D2, D3) to form a CDK4 / 6-Cyclin D complex, including the retinoblastoma protein (Retinoblastoma protein, Rb) After phosphorylation of a series of substrates, the proteins bound to and inhibited by it are released, such as the transcription factor E2F. E2F further activates and transcribes some genes necessary for entering the S phase, and realizes the promotion and transformation of different phases of the cell cycle. . Existing studies have shown that the specific activation of CDK4 / 6...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7068A61K31/519A61P35/00
CPCA61K31/7068A61K31/519A61K2300/00
Inventor 许乐
Owner 南京众慧网络科技有限公司
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