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Applications of combined CDK4/6 inhibitor and aromatase inhibitor in preparing medicines for treating breast cancer

An aromatase inhibitor and aromatase technology, which can be used in drug combination, organic chemistry, antitumor drugs, etc., and can solve the problems of no specific disclosed effect and no expected synergistic effect.

Inactive Publication Date: 2017-09-08
JIANGSU HENGRUI MEDICINE CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] However, the above-mentioned literature does not specifically disclose which compound can achieve better results when used in combination with which anti-tumor agent, and it is not expected that some specific combination methods can achieve synergistic effects.

Method used

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  • Applications of combined CDK4/6 inhibitor and aromatase inhibitor in preparing medicines for treating breast cancer
  • Applications of combined CDK4/6 inhibitor and aromatase inhibitor in preparing medicines for treating breast cancer
  • Applications of combined CDK4/6 inhibitor and aromatase inhibitor in preparing medicines for treating breast cancer

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0036] Example 1: 6-acetyl-8-cyclopentyl-5-methyl-2-((5-(piperidin-4-yl)pyridin-2-yl)amino)pyrido[2,3-d ]Pyrimidin-7(8H)-One Preparation of Isethionate

[0037] Step 1: 6-((6-(1-butoxyethenyl)-8-cyclopentyl-5-methyl-7-carbonyl-7,8-dihydropyrido[2,3-d]pyrimidine Preparation of -2-yl)amino)-5',6'-dihydro-[3,4'-bipyridine]-1'(2'H)-tert-butyl formate

[0038]

[0039] Under argon protection, (10g, 29.06mmol) 2-amino-6-(1-butoxyethenyl)-8-cyclopentyl-5-methylpyrido[2,3-d]pyrimidine-7( 8H)-ketone (prepared according to the method disclosed in WO2014183520), cesium carbonate (14.22g, 43.75mmol), Pd 2 (dba) 3 (2.12g, 2.31mmol), 4,5-bisdiphenylphosphine-9,9-dimethylxanthene (2.69g, 4.69mmol) and 125.00g of dioxane were put into a three-necked reaction flask and stirred evenly After heating to reflux, the raw material 4-(6-chloropyridin-3-yl)-5,6-dihydropyridine-1(2H)-tert-butyl carboxylate (10.34g, 35.00mmol, purchased from Yancheng City Ruikang Pharmaceutical Chemical Co., Ltd...

Embodiment 2

[0046] Example 2: Comparative study on the curative effect of compound A and PD-0332991 alone or in combination with letrozole on human breast cancer MCF-7 / ARO subcutaneously transplanted tumors in nude mice.

[0047] 1 test drug

[0048] Drug name: the isethionate of PD-0332991 is a yellow crystalline powder, prepared according to the method disclosed in CN1835951B; the isethionate of compound A is a white powder, prepared from Example 1; letrozole is White powder, provided by Jiangsu Hengrui Pharmaceutical Co., Ltd.

[0049] Preparation method: the isethionate of compound A was prepared with 50mM citric acid + 0.5% CMC + 0.5% Tween80; the isethionate of PD-0332991 was prepared with distilled water containing 0.1% Tween 80; letrozole was prepared with Prepare and dilute with 20% PEG 400 in distilled water.

[0050] 2 experimental animals

[0051] BALB / cA-nude nude mice, 6-7 weeks old, ♀, were purchased from Shanghai Lingchang Biotechnology Co., Ltd. Production license num...

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Abstract

The invention relates to applications of combined CDK4 / 6 inhibitor and aromatase inhibitor in preparing medicines for treating breast cancer. Specifically, the CDK4 / 6 inhibitor is a compound A or medicinal salt of the compound A, and the aromatase inhibitor is selected from one or more of formestane, exemestane, fadrozole, letrozole, vorozole and anastrozole.

Description

technical field [0001] The invention relates to the use of a CDK4 / 6 inhibitor combined with an aromatase inhibitor in the preparation of a medicine for treating breast cancer. Background technique [0002] Breast cancer is one of the most common malignant tumors in women. It has a high incidence rate and is quite invasive, but the course of the disease progresses slowly. On February 1, 2010, the China Population Association released the "China Breast Disease Survey Report" in Beijing. The report shows that, The mortality rate of breast cancer in my country's urban areas has increased by 38.91%. Breast cancer has become the most threatening disease to women's health. Currently, there are at least 156 breast cancer drugs under research and on the market, of which 68% are targeted therapy drugs. A large number of studies It was found that tumors are associated with abnormal cell cycle, a large number of mutations of mitotic signaling proteins in tumor cells and defects of anti-mi...

Claims

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Application Information

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IPC IPC(8): A61K31/519A61K31/4196C07D471/04A61P35/00
CPCA61K31/4196A61K31/519C07D471/04A61K2300/00
Inventor 孙飘扬曹国庆张扬马珂杨昌永张连山
Owner JIANGSU HENGRUI MEDICINE CO LTD
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