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A tyrosine kinase inhibitor

A pharmacy and compound technology, applied in the field of tyrosine kinase inhibitors, can solve problems such as single structure

Active Publication Date: 2020-12-29
SUZHOU SINOVENT PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The technical problem to be solved by the present invention is that the structure of the existing RET kinase inhibitors is relatively single. Therefore, the present invention provides a compound with a new structure, its use and a pharmaceutical composition containing it

Method used

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  • A tyrosine kinase inhibitor
  • A tyrosine kinase inhibitor
  • A tyrosine kinase inhibitor

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0031] Example 1 SZ-013026

[0032]

[0033] step 1:

[0034] 1-(tert-butyl)4-methyl 4-((((9H-fluoren-9-yl)methoxy)carbonyl)amino)piperidine-1,4-dicarboxylate

[0035] Add 9307A1 (4.6g, 10mmol) and DMF (20ml) into the reaction flask, stir, then add MeOH (3.2g, 100mmol), DIPEA (3.8g, 30mmol), and finally add HATU (4.3g, 11mmol), and react at 20°C 12 hours. Add water (100ml) to the reaction solution, extract with EA (50ml*3), combine the organic phases, dry over anhydrous sodium sulfate, filter, and concentrate the filtrate under reduced pressure to obtain a crude product, which is purified by flash silica gel column chromatography (EA / PE0-50%) Obtained 013026A1 (4.0 g, 82%, white solid).

[0036] Step 2:

[0037] 1-(tert-butyl) 4-methyl 4-aminopiperidine-1,4-dicarboxylate

[0038] Compound 013026A1 (4.0g, 8.2mmol) and methanol (5ml) were stirred, then ethylenediamine (10ml) was added, and reacted at 20°C for 2 hours. The reaction solution was concentrated under reduced...

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Abstract

The invention discloses a compound and application thereof and a pharmaceutical composition containing the compound. The structure of the compound is shown as a formula I, and the compound has a goodinhibition effect on RET kinase.

Description

technical field [0001] The present invention relates to a tyrosine kinase inhibitor, its application and its pharmaceutical composition. Background technique [0002] The RET gene was transformed into mouse NTH3T3 cells by Takahashi et al. Discovered and named RET gene. The RET gene is a proto-oncogene (10q11.2) located on the long arm of chromosome 10. The encoded RET protein is a tyrosine kinase receptor composed of a cysteine-rich cadherin-like extracellular domain, The transmembrane region and the intracellular domain with tyrosine kinase activity are composed of three parts, and have 37% amino acid identity with the ALK kinase domain. The RET protein stimulates the dimerization of the receptor through the binding of the ligand to the receptor, autophosphorylation of the intracellular region and phosphorylation of the intracellular substrate, thereby activating the downstream signal and playing an important role in the process of cell proliferation, migration and diffe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D519/00A61K31/444A61P35/00A61P35/02
CPCA61P35/00A61P35/02C07D519/00
Inventor 吴冬冬卢亮张秀春胡永韩
Owner SUZHOU SINOVENT PHARMA CO LTD