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Pharmaceutical composition prepared by combining paclitaxel with CDKS kinase inhibitor for use

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

Inactive Publication Date: 2018-04-20
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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  • Pharmaceutical composition prepared by combining paclitaxel with CDKS kinase inhibitor for use
  • Pharmaceutical composition prepared by combining paclitaxel with CDKS kinase inhibitor for use
  • Pharmaceutical composition prepared by combining paclitaxel with CDKS kinase inhibitor for use

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 in the reaction flask, add 30m dichloromethane to dissolve, slowly add dropwise to dissolve 4g (BOC) at 0℃ 2 Dichloromethane solution of O, after dropping, react at room temperature for 2h, 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 with sodium sulfate, filter, Spin to dryness to obtain 2.98 g of oil. Add 50ml of DMF / water mixed solvent with a volume ratio of 1:1 to dissolve the obtained oil, add 0.41g of 2-amino-5-chloropyridine, and react at 100°C for 8 hours. After the reaction is over, add 20ml of water, extract with ethyl acetate, and anhydrous sulfuric acid The organi...

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 in 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 to 45°C and stir for 0.5h, cool to room temperature, and cool in the refrigerator overnight , Filter, wash with methanol water with a volume ratio of 2:1, and dry 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 in a reaction flask, add 50ml of dichloromethane to dissolve, add 5.9g of hydrobromic acid, heat to 45°C and stir for 0.5h, after cooling to room temperature, the solvent is evaporated under reduced pressure to obtain the title compound.

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Abstract

The present invention provides a combined pharmaceutical composition of paclitaxel and CDKS kinase inhibitors, comprising active ingredients and pharmaceutically acceptable excipients, characterized in that: the active ingredients are composed of paclitaxel and CDK4 / 6 kinase represented by formula I Inhibitors or pharmaceutically acceptable salts thereof, the mass ratio of paclitaxel and CDK4 / 6 kinase inhibitors or pharmaceutically acceptable salts thereof in the active ingredient is (2‑8):1. The pharmaceutical composition has good anticancer curative effect and low toxic and side effects; due to the sensitivity of CDK4 / 6 kinase inhibitors to paclitaxel, the combination of the two produces a synergistic effect, thereby reducing the clinical dosage of capecitabine and reducing the large dosage Toxic and side effects produced by using capecitabine can improve the safety index of clinical treatment and have good clinical application prospects.

Description

Technical field [0001] The invention belongs to the field of chemical medicine, and is a combined pharmaceutical composition of paclitaxel and CDKS kinase inhibitor. Background technique [0002] Paclitaxel, English name Paclitaxel, alias taxol, purpurin, 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 that promotes tubulin polymerization to inhibit depolymerization, keep tubulin stable, and inhibit cell mitosis. In vitro experiments have shown that paclitaxel has a significant radiosensitization effect, which may stop cells in G2 and M phases that are sensitive to radiotherapy. It is clinically suitable for ovarian cancer and breast cancer, and for lung cancer, colorectal cancer, melanoma, and head and neck cancer. , Lymphoma and brain tumors also have certain cura...

Claims

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Application Information

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Patent Type & Authority Applications(China)
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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