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Application of compound as JAK-STAT3 signal passage inhibitor

A technology of JAK-STAT3 and signaling pathways, which is applied in the direction of drug combinations, medical preparations containing active ingredients, organic active ingredients, etc., can solve the problems that have not yet been clinically treated for cancer, and achieve the effect of improving prognosis and improving curative effect

Inactive Publication Date: 2009-09-23
GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0015] At present, there is no literature report about the drug or its derivatives or its analogs and its salts being used in the clinical treatment of cancer

Method used

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  • Application of compound as JAK-STAT3 signal passage inhibitor
  • Application of compound as JAK-STAT3 signal passage inhibitor
  • Application of compound as JAK-STAT3 signal passage inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0150] 5-Chloro-N-(4-fluorophenyl)-2-hydroxybenzamide

[0151] (5-chloro-N-(4-fluorophenyl)-2-hydroxybenzamide)

[0152]

[0153] resolve resolution:

[0154] Mix 1 mmol of 5-chloro-2-methoxybenzoic acid and 2 ml of thionyl chloride and heat to reflux for one hour. Thionyl chloride was distilled off, then diluted with 2 ml of anhydrous tetrahydrofuran, and then used.

[0155] 2 mmol of 4-fluoroaniline compounds were dissolved in 2 ml of anhydrous tetrahydrofuran, and then added dropwise to the previously prepared 5-chloro-2-methoxybenzoyl chloride solution at room temperature, and stirred overnight at room temperature. After the reaction was detected by thin layer chromatography, at room temperature, an appropriate amount of water and dichloromethane were added, the mixture was transferred to a separatory funnel, and the organic layer was taken. The organic layer solution was washed successively with appropriate amount of dilute sodium hydroxide solution (once), saturate...

Embodiment 2

[0160] 5-Chloro-N-(3,4-difluorophenyl)-2-hydroxybenzamide

[0161] (5-chloro-N-(3,4-difluorophenyl)-2-hydroxybenzamide)

[0162]

[0163] The synthesis method is as in Example 1.

[0164] 1 HNMR (400MHz, DMSO-d 6 ), δ11.60(s, 1H), 10.52(s, 1H), 7.86~7.91(m, 2H), 7.43~7.48(m, 3H), 7.46~7.49(m, 1H), 7.02(d, J = 1.6Hz, 1H)

[0165] MS(ES+APCI), m / z: 284.1(M+H) + , 282.0(M-H) -

Embodiment 3

[0167] 5-Chloro-N-(4-(4-morpholinyl)phenyl)-2-hydroxybenzamide

[0168]

[0169] The synthesis method is as in Example 1.

[0170] 1 HNMR (400MHz, DMSO-d 6 ), δ10.41(s, 1H), 7.99(d, J=2.0Hz, 1H), 7.54(d, J=8.8Hz, 2H), 7.43~7.46(m, 1H), 6.94~6.99(m, 3H),

[0171] MS(ES+APCI), m / z: 333.0(M+H) + , 331.2(M-H) -

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Abstract

The invention discloses an application of a compound as a JAK-STAT3 signal passage inhibitor, and particularly relates to an application of a compound with a formula I or pharmaceutically acceptable salt of the compound in the process of preparing an anti-tumor medicament. The application provides a novel treating candidate medicament for a tumor patient, thereby probably further improving the treatment effect on the patient and improving the prognosis of the patient. The compound with the formula I or the pharmaceutically acceptable salt of the compound has the effect on various tumor cells, which indicates that the compound can be used for treating various cancers including cerebral tumor, genitourinary system tumor, lymphatic system tumor, stomach cancer, laryngeal cancer, nasopharyngeal cancer, skin cancer, bone cancer, blood cancer, leukemia, breast cancer and histiocytic lymphoma, non-small cell lung cancer, small-cell lung cancer, lung adenocarcinoma, lung squamous cell cancer, pancreatic cancer, prostatic cancer, liver cancer, epithelial cell cancer and the like. The definition of genes in the formula refers to description for details.

Description

technical field [0001] The present invention relates to the application of a class of compounds as JAK-STAT3 signaling pathway inhibitors. technical background [0002] Tumor is currently the number one killer of human health and life, and its incidence rate is second only to cardiovascular diseases. And with the impact of environmental pollution and other factors, the incidence of malignant tumors is rising rapidly. According to the data released by the World Health Organization in 2003, there were 10 million malignant tumor patients in the world in 2000, and 6.2 million deaths due to malignant tumors, accounting for 12% to 25% of the total deaths. It is expected that by 2020, there will be 15 million new cases worldwide each year. In recent years, although some novel tyrosine protein inhibitors and other targeted new drugs have been developed and marketed, they are still far from meeting the growing needs of clinical cancer patients. The research and development of anti...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/167A61K31/4196A61K31/5375A61P35/00
Inventor 丁克裴端卿李正伟任小梅段磊何蔷张章
Owner GUANGZHOU INST OF BIOMEDICINE & HEALTH CHINESE ACAD OF SCI
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