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Pharmaceutical composition combining substituted butene amide and mTOR inhibitor as well as application of pharmaceutical composition

A technology of crotene amide and composition, which is applied in the direction of drug combination, antineoplastic drugs, and pharmaceutical formulations, and can solve problems such as lack of effective means

Active Publication Date: 2020-09-04
JIANGSU SUZHONG PHARM GRP CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] EGFR-targeted drugs often have skin toxicity clinically, and there is still a lack of effective means in terms of improving drug efficacy and reducing toxic and side effects. Therefore, it is necessary to develop a synergistic anti-tumor drug composition

Method used

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  • Pharmaceutical composition combining substituted butene amide and mTOR inhibitor as well as application of pharmaceutical composition
  • Pharmaceutical composition combining substituted butene amide and mTOR inhibitor as well as application of pharmaceutical composition
  • Pharmaceutical composition combining substituted butene amide and mTOR inhibitor as well as application of pharmaceutical composition

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0113] Example 1 The pharmacodynamic effect of compound SZMD4-mal administered alone and in combination with rapamycin on EGFR-L858R, EGFR-T790M mutated human lung cancer cell NCL-H1975 subcutaneous tumorigenic model nude mice

[0114] The SZMD4-mal involved in this example is (E)-N-(3-cyano-7-ethoxy-4-(3-ethynylphenylamino)quinolin-6-yl)-4-(di Methylamino)but-2-enamide maleate monohydrate.

[0115] 1. Experimental animals

[0116] Mice, BALB / c-nu / nu nude mice, female, 4-6 weeks old, 17-22g. Breeding environment: SPF grade.

[0117] 2. Test drug

[0118] Drug name: SZMD4-mal; rapamycin (Repamycin).

[0119] Preparation method: SZMD4-mal, under sterile conditions, add sterile deionized water to grind and mix, then add deionized water to the required volume, shake well, prepare once a week and store in a 4°C refrigerator, take it out before use to room temperature, fully vortexed before administration; rapamycin, aseptically ground in an agate mortar with saline containing ...

Embodiment 2

[0149] Example 2 The pharmacodynamic effect of compound SZMD4-mal administered alone and in combination with rapamycin on EGFR and HER2 positive and K-ras mutated human lung cancer cell A549 subcutaneous tumorigenic model nude mice

[0150] The SZMD4-mal involved in this example is (E)N-(3-cyano-7-ethoxy-4-(3-ethynylphenylamino)quinolin-6-yl)-4-(dimethyl (amino)but-2-enamide maleate monohydrate.

[0151] 1. Experimental animals

[0152] Mice, BALB / c-nu / nu nude mice, female, 4-6 weeks old, 17-22g. Breeding environment: SPF grade.

[0153] 2. Test drug

[0154] Drug name: SZMD4-mal; rapamycin (Repamycin).

[0155] Preparation method: SZMD4-mal, under sterile conditions, add sterile deionized water to grind and mix, then add deionized water to the required volume, shake well, prepare once a week and store in a 4°C refrigerator, take it out before use To room temperature, fully vortex and mix before administration; rapamycin, prepared as a solution with physiological saline u...

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PUM

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Abstract

The invention discloses a pharmaceutical composition combining substituted butene amide and a mTOR inhibitor as well as application of the pharmaceutical composition, and particularly relates to a composition or kit containing at least one substituted butene amide or a pharmaceutically acceptable salt or solvate thereof and at least one mTOR inhibitor as well as application of at least one substituted butene amide or a pharmaceutically acceptable salt or solvate and at least one mTOR inhibitor in preparation of a cancer treating medicine or kit. Compared with the prior art, the pharmaceuticalcomposition has the following advantages: the substituted butene amide or the medicinal salt thereof and the mTOR inhibitor have proliferation inhibition effects on multiple cancers, and have significant synergistic effects through combined use.

Description

technical field [0001] The invention belongs to the field of biomedicine, and in particular relates to a pharmaceutical composition of a substituted crotenamide combined with an mTOR inhibitor and its use in preparing a medicine or a kit for treating cancer. Background technique [0002] Malignant tumor is a major disease that endangers people's life and health. In recent years, with the rapid development of tumor biology and related disciplines, specific anti-tumor drugs targeting abnormal signaling system targets in tumor cells have become the focus of new drug research and development. At the same time, the combination of multiple anti-tumor drugs for the treatment of tumor diseases is also a hot spot of scientific research. [0003] Molecular targeted therapy targeting human epidermal growth factor receptor (EGFR) has become the most important way to treat NSCLC. EGFR is the expression product of the proto-oncogene C-erbB-1. The gene is located on chromosome 7 and belo...

Claims

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Application Information

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IPC IPC(8): A61K31/4706C07D215/54A61P35/00A61K31/436A61K31/675
CPCA61K31/436A61K31/4706A61K31/675A61P35/00C07D215/54A61K2300/00
Inventor 唐海涛种法政葛海涛王正俊曹苏闵马继梅
Owner JIANGSU SUZHONG PHARM GRP CO LTD
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