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Medicine composition, and preparation and application thereof

A technology of pharmaceutical preparations and compositions, applied in the field of pharmaceutical compositions containing indane amide compounds, which can solve the problems of inability to specifically act on cancer cells, hair loss, etc.

Inactive Publication Date: 2013-04-03
北京美迪康信医药科技有限公司 +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Classical cancer drugs are cytotoxic chemotherapeutics, such as cisplatin, carboplatin, paclitaxel, pemetrexed, gemcitabine, etc. These drugs cannot be specific In addition to killing cancer cells, it can also kill normal cells, causing hair loss, red blood cell reduction, vomiting and weight loss and other toxic side effects
For this reason, these drugs can only be given in doses and for as long as the body can tolerate

Method used

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  • Medicine composition, and preparation and application thereof
  • Medicine composition, and preparation and application thereof
  • Medicine composition, and preparation and application thereof

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0065] The effect on prostate cancer PC-3 cells

[0066] 1. Cells and culture conditions: Human prostate cancer PC-3 cells were cultured in RPMI1640 medium containing 10% calf serum, supplemented with 100 U / ml penicillin and 100 mg / L streptomycin. Routine cultivation was carried out at 37°C and 50 ml / L CO2. About 5×106 / ml cells in the exponential growth phase were subcultured and inoculated in 24-well plates, and then cultured for 12 h before use.

[0067] 2. Experimental drugs

[0068] Experimental drug group 1: docetaxel 6.7×10-5g / L;

[0069] Experimental drug group 2: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino ]Phenyl)-2,3-indane-5-amide sesquisulfate 6.7×10-5g / L;

[0070] Experimental drug group 3: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino ]phenyl)-2,3-indane-5-position amide sesquisulfate 6.7×10-5g / L; docetaxel 6.7×10-5g / L;

[0071] Experimental drug group 4: (1S)-1-(4-methylpiperazin-1...

experiment example 2

[0079] Study on antitumor effect in human chronic myeloid leukemia K562 tumor model

[0080] 1. Experimental animals: NOD / SCID mice, female, 6-8 weeks old, weighing 18-22 g.

[0081] 2. Experimental drugs:

[0082] Experimental drug group 1: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino ]Phenyl)-2,3-indane-5-amide sesquisulfate 90mg / kg.

[0083] Experimental drug group 2: docetaxel 10 mg / kg.

[0084] Experimental drug group 3: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino ]Phenyl)-2,3-indane-5-amide sesquisulfate 90mg / kg, docetaxel 10mg / kg.

[0085] Experimental drug group 4: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino ]Phenyl)-2,3-indane-5-amide sesquisulfate 40mg / kg, docetaxel 10mg / kg.

[0086] Experimental drug group 5: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino ]Phenyl)-2,3-indane-5-amide sesquisulfate 25mg / kg, doce...

experiment example 3

[0097] Effects on lung cancer in mice

[0098] 1. Experimental animals: C57BL / 6 pure line mice, female, 6-8 weeks old, weighing 18-22 g.

[0099] 2. Tumor strain: Lewis lung cancer cell line (3LL), preserved in C57BL / 6 mice, passaged once every 2 weeks.

[0100] 3. Experimental drugs:

[0101] Experimental drug group 1: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino ]Phenyl)-2,3-indane-5-amide sesquisulfate 20mg / kg.

[0102] Experimental drug group 2: cephalomannine 20 mg / kg.

[0103] Experimental drug group 3: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino ]Phenyl)-2,3-indane-5-amide sesquisulfate 18mg / kg, cephalomannine 2mg / kg.

[0104] Experimental drug group 4: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-ylpyrimidin-2-yl)amino ]Phenyl)-2,3-indane-5-amide sesquisulfate 15mg / kg, cephalomannine 5mg / kg.

[0105] Experimental drug group 5: (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[...

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Abstract

The invention belongs to the technical field of medicines, and discloses a medicine composition composed of (1S)-1-(4-methylpiperazin-1-yl)-N-(4-methyl-3-[(4-pyridin-3-pyrimidine-2-yl)amino]phenyl)-2,3-dihydroindene-5-amide sesquisulfate and a taxanes microtubule inhibitor. The medicine composition is determined through scientific experiments. As a result of experiments, the taxanes microtubule inhibitor has no influence on the stability of the compound. As a result of pharmacological test, the two components provide a synergetic effect.

Description

technical field [0001] The invention belongs to the technical field of medicine, and in particular relates to a pharmaceutical composition containing an indane amide compound and its preparation and use. Background technique [0002] Cancer, also known as malignant neoplasm in medical terms, is a disease caused by abnormalities in the mechanism of controlling cell growth and proliferation. Cancer is the enemy of human health. According to statistics, in China, since 2007, cancer has surpassed cardiovascular disease to become the number one killer of human beings. Classical cancer drugs are cytotoxic chemotherapeutics, such as cisplatin, carboplatin, paclitaxel, pemetrexed, gemcitabine, etc. These drugs cannot be specific In addition to killing cancer cells, it can also kill normal cells, causing hair loss, red blood cell reduction, vomiting and weight loss and other toxic side effects. For this reason, these drugs are only given in doses and for as long as the body can to...

Claims

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Application Information

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IPC IPC(8): A61K31/506A61K31/337A61P35/00A61P35/02
Inventor 朱吉满曹捷解菁雅杨艳朱希卓郭永起孙德杰
Owner 北京美迪康信医药科技有限公司
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