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Anaplastic lymphoma kinase inhibitor, preparation method and uses thereof

A compound and the selected technology are applied in the direction of antineoplastic drugs, pharmaceutical formulations, organic active ingredients, etc., and can solve problems such as drug resistance

Active Publication Date: 2018-04-20
CENTAURUS BIOPHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] Although people have studied a large number of compounds with inhibitory activity on protein kinases, and some protein kinase inhibitors have been marketed for anti-tumor treatment, drug resistance will occur

Method used

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  • Anaplastic lymphoma kinase inhibitor, preparation method and uses thereof
  • Anaplastic lymphoma kinase inhibitor, preparation method and uses thereof
  • Anaplastic lymphoma kinase inhibitor, preparation method and uses thereof

Examples

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specific Embodiment approach

[0057] The compounds of the present invention and their preparation methods and uses are illustrated below in conjunction with the examples. Process 1.:

[0058]

[0059] The compounds shown in the present invention can be prepared according to the route described in Scheme 1. The product obtained from the reaction in scheme 1 can be obtained by conventional separation techniques, such traditional techniques include but not limited to filtration, distillation, crystallization, chromatographic separation and the like. Starting materials can be synthesized in-house or purchased from commercial establishments such as, but not limited to, Adrich or Sigma. These starting materials can be characterized using conventional means, such as physical constants and spectral data. The compounds described in this invention may be obtained using synthetic methods as single isomers or as mixtures of isomers.

[0060]In scheme 1, raw material 1 reacts with PMBC1 under basic conditions to ...

Embodiment 1

[0081]

[0082] Step A: 2,4-Dichloro-7-(4-methoxybenzyl)-7H-pyrrolo[2,3-d]pyrimidine

[0083]

[0084] Add 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine (18.8g, 0.1mol), potassium carbonate (20.7g, 0.15mol) to a DMF (188mL) solution under stirring at room temperature (30°C) 4-methoxybenzyl chloride (18.8 g, 0.12 mol) was added dropwise to the solution. After the addition was complete, it was heated to 50-55° C. and stirred at this temperature for 17 h. Cool to room temperature, filter, and add water (564 mL) and ethyl acetate (188 mL) to the filtrate. The aqueous phase was separated, extracted once with ethyl acetate (100 mL), the extract was combined with the organic phase, washed with saturated brine (400 mL X 2), dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated under reduced pressure to obtain a dark oil. The oil was slurried with ethyl acetate (30mL), filtered, and the filter cake was rinsed with ethyl acetate (20mL) and petroleum ether (1...

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Abstract

The present invention relates to a compound represented by a formula (I), a pharmaceutical composition and a preparation method thereof, wherein the compound can be used as an ALK inhibitor to treat ALK-mediated diseases. The invention further relates to the preparation method of the compound represented by the formula (I), and applications of the compound represented by the formula (I) and the pharmaceutical composition thereof in preparation f drugs for treatment of ALK-mediated diseases. The formula (I) is defined in the specification.

Description

technical field [0001] The present invention relates to novel pyrrolopyrimidine derivatives with protein kinase inhibitory activity, their preparation method, pharmaceutical composition, and the use of such compounds and their pharmaceutical compositions in treating diseases related to protein kinases. Background technique [0002] ALK (alternative lymphokinase) is a receptor-type protein tyrosine phosphokinase that belongs to the insulin receptor superfamily. It has been reported that as a result of gene abnormality (translocation, point gene mutation or gene amplification) of ALK, abnormal kinases fused with other genes are produced and involved in carcinogenesis. [0003] For example, in lung cancer, ALK combines with the intracellular skeleton protein EML4 through chromosomal translocation to produce EML4-ALK with activated tyrosine kinase activity, and acquires the ability to become cancerous (Proc.Natl.Acad.Sci.USA, 2004 , 101, 13306-13311). [0004] In addition, abn...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04A61K31/63A61P35/00
CPCC07D487/04
Inventor 杨利民张传玉孔凡胜孙德广冀冲张晓军孙莹张慧彭勇罗鸿
Owner CENTAURUS BIOPHARMA
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