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Compounds useful as modulators of protein kinases and their use

A technology of compounds, uses, applied in the field of medicine

Active Publication Date: 2021-08-17
TETRANOV PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Although TPX-0005 has achieved relatively good results in clinical Ⅰ / Ⅱ trials, in order to meet the urgent clinical needs of anti-drug resistance and benefit the majority of patients, it is necessary to develop new drugs with high activity and / or better pharmacodynamics. Compounds with pharmacokinetic properties have become an urgent problem to be solved in the development of new anti-tumor drugs

Method used

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  • Compounds useful as modulators of protein kinases and their use
  • Compounds useful as modulators of protein kinases and their use
  • Compounds useful as modulators of protein kinases and their use

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0099] Target compound:

[0100]

[0101] The synthetic route is:

[0102]

[0103] specific synthesis process

[0104] Synthesis of compound 2

[0105]Under nitrogen atmosphere, under stirring at room temperature, tetraethyl titanate (24g, 84mmol) was added dropwise to compound 1 (5.0g, 32.4mmol) and R-tert-butylsulfinamide (3.9g, 32.4mmol) in dichloromethane (150mL) solution, stirred overnight at room temperature after the dropwise addition, added water (100mL) to quench the reaction, filtered with diatomaceous earth, and washed the filter cake with dichloromethane (300mL), separated, and extracted the aqueous phase with dichloromethane, combined The organic phase was dried over anhydrous magnesium sulfate and subjected to silica gel column chromatography (PE:EA=1:1) to obtain 2.8 g of a yellow solid.

[0106] Characterization data: 1 H NMR (400MHz, CDCl 3 ): δ12.78(s, 1H), 7.32(dd, J=3.2, 9.6Hz, 1H), 7.26(m, 1H), 6.93(dd, J=3.2, 9.6Hz, 1H), 2.79(s, 3H), 1.34(...

Embodiment 2

[0132] Target compound:

[0133]

[0134] The synthesis of the target compound in Example 2, with reference to Example 1, the difference is that the compound (R)-1-(BOC-amino)-2-propanol in the compound 9 synthesis step is replaced by:

[0135] Example 2 target compound: MS m / z (ESI): 383.1 [M+H] + .

Embodiment 3

[0137] Target compound:

[0138]

[0139] The synthesis of the target compound in Example 3, with reference to Example 1, the difference is that the compound (R)-1-(BOC-amino)-2-propanol in the compound 9 synthesis step is replaced by:

[0140] Example 3 target compound: MS m / z (ESI): 369.2[M+H] + .

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PUM

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Abstract

The present invention discloses a compound represented by formula I, wherein each symbol is as defined in the claims. The compound represented by formula I of the present invention has good inhibitory activity on ALK, ROS1 and / or TRK kinases, and can be used to prepare drugs for inhibiting ALK, ROS1 and / or TRK kinases, and to treat cancer, pain, neurological diseases, autoimmunity disease or inflammation.

Description

technical field [0001] The invention relates to the field of medical technology, in particular to a compound used as a protein kinase regulator, a pharmaceutical composition containing the compound, and also to its application in the preparation of drugs for regulating protein kinase activity or treating protein kinase-related diseases . Background technique [0002] Malignant tumors are one of the main killers of human health. The latest edition of the "World Cancer Report" predicts that global cancer cases will show a rapid growth trend, from 14 million in 2012 to 19 million in 2025, and by 2035 will reach 24 million people. The report also shows that developing countries in Africa, Asia, and Central and South America have the most severe cancer incidence. In 2012, there were 14 million new cancer cases and 8.2 million deaths worldwide. Among them, China added 3.07 million cancer patients and caused about 2.2 million deaths, accounting for 21.9% and 26.8% of the global ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D498/18C07D498/22C07D498/20C07D513/18A61K31/529A61P35/00A61P29/00A61P25/00A61P37/02A61P35/02A61P31/12A61P3/00A61P37/06
CPCA61P3/00A61P25/00A61P29/00A61P31/12A61P35/00A61P35/02A61P37/02A61P37/06C07D498/18C07D498/20C07D498/22C07D513/18
Inventor 吴豫生职五斌李敬亚王新吴世勇梁阿朋郭瑞云
Owner TETRANOV PHARMA CO LTD
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