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Application of Thrazolopyrimidine Compounds in the Preparation of Medicines for Treating Lung Cancer

A technology of azolopyrimidines and compounds, which is applied in the field of application of thalazopyrimidines in the preparation of drugs for the treatment of lung cancer, can solve the problems of toxic and side effects, serious side effects, erosion of normal cells and internal organs, etc., to reduce drug resistance, The effect of huge economic benefits

Inactive Publication Date: 2011-12-07
广州市第十二人民医院
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  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0003] Existing drugs often have many shortcomings: A. Traditional chemotherapy drugs: Although chemotherapy can kill cancer cells, it is also eroding the normal cells and internal organs of the human body, and the side effects are quite serious; at the same time, it is often ineffective for patients with metastatic lung cancer At present, the 5-year survival rate of lung cancer in the world is only 15%, and the toxic and side effects of chemotherapy drugs and tumor metastasis are the main causes of death
However, there is no report about the application of thalazozolopyrimidine compounds in the preparation of drugs for the treatment of lung cancer.

Method used

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  • Application of Thrazolopyrimidine Compounds in the Preparation of Medicines for Treating Lung Cancer
  • Application of Thrazolopyrimidine Compounds in the Preparation of Medicines for Treating Lung Cancer
  • Application of Thrazolopyrimidine Compounds in the Preparation of Medicines for Treating Lung Cancer

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Embodiment

[0027] (1) Design idea: Aiming at the two most important signaling pathways in the pathogenesis of lung cancer, look for their intersection points as possible targets. Small molecule drugs are used to inhibit this target to achieve the purpose of treating lung cancer.

[0028] (2) Select the key signaling pathways for entry: two signaling pathways, mitogen-activated protein kinase (MAPK) and target of rapamycin (mTOR), are selected as entry points for the following reasons:

[0029] ① The genes of these two signaling pathways have the highest mutation rate in lung cancer: the Tumor Sequencing Project (TSP) funded by the National Human Genome Research Institute (NHGRI) under the National Institutes of Health (NIH) found that in 188 lung cancer tissues, more than At least one MAPK pathway gene mutation will appear in 70% of lung cancer tissues; and at least 30% of lung cancer tissues will have more than one MAPK pathway gene mutation.

[0030] ②The MAPK signaling pathway is a s...

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Abstract

The invention relates to the application of thalazozolopyrimidine compounds in the preparation of drugs for treating lung cancer. The invention also provides the application of the thalazozolopyrimidine compound in the preparation of medicines for treating malignant melanoma and human ovarian cancer. The advantage of the present invention is that: as a MNK1 inhibitor, the thalazozolopyrimidine compound of the present invention is a new target for the treatment of lung cancer and inhibits two mechanism pathways of lung cancer pathogenesis, MAPK and mTOR signaling pathways, rather than targeting a single mechanism, so as to avoid and reduce drug resistance; in view of the current poor therapeutic effect and low survival rate of lung cancer and malignant melanoma, it can greatly improve the therapeutic effect of these two diseases, which has great positive significance to the society; the present invention has huge economic benefits .

Description

technical field [0001] The present invention relates to the application of a class of compounds, in particular, the application of thalazopyrimidine compounds in the preparation of drugs for treating lung cancer. Background technique [0002] Lung cancer is the most common primary malignant tumor of the lung. The vast majority of lung cancers originate from the bronchial mucosal epithelium, so it is also called bronchial lung cancer. Over the past 50 years, the morbidity and mortality of lung cancer have risen rapidly in countries all over the world, especially in industrialized countries, and lung cancer has ranked first among male patients who died of cancer. In the prior art, there are mainly three kinds of drugs for the treatment of lung cancer: A. Traditional chemotherapy drugs: common chemotherapy drugs for SCLC include cyclophosphamide (CTX), ifosfamide (IFO), doxorubicin (ADM), vincristine ( VCR), vinblastine (VBL), etoposide (VP16), Vumon (Vumon), carboplatin (CBP)...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519A61P35/00
Inventor 刘斌
Owner 广州市第十二人民医院
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