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TNIK inhibitor as well as preparation method and application thereof

A technology selected from heteroatoms, applied in the field of medicine, to achieve the effect of good application prospect, low cost and good inhibitory activity

Active Publication Date: 2021-12-10
SICHUAN UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Meanwhile, pharmacological inhibition of TNIK is expected to block this signaling pathway even in the presence of APC gene mutations in colorectal cancer cells

Method used

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  • TNIK inhibitor as well as preparation method and application thereof
  • TNIK inhibitor as well as preparation method and application thereof
  • TNIK inhibitor as well as preparation method and application thereof

Examples

Experimental program
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Effect test

Embodiment 14

[0093] Example 1 4-(3-methoxybenzyl)-8-(1H-pyrrolo[2,3-b]pyridin-5-yl)-3,4-dihydro-1,4-benzooxy Preparation of azepine-5(2H)-one (compound 38)

[0094] Intermediate 1: Preparation of 8-bromo-3,4-dihydro-1,4-benzoxazepine-5(2H)-one.

[0095]

[0096] Put raw material 1 (7-bromo-4-dihydrochromanone 1.0g, 4.40mmol), sodium azide (858.97mg, 13.21mmol) and dichloromethane (80mL) in a round-bottomed flask and stir at room temperature, add dropwise Methanesulfonic acid (9 mL), after reacting for 24 hours, extracted with water and saturated sodium chloride respectively, dried the organic phase with magnesium sulfate, suction filtered, and column chromatographed to obtain a white solid. Yield 85%.

[0097] 1H NMR (400MHz, DMSO-d 6 )δ8.41(d, J=6.0Hz, 1H), 7.73(d, J=8.5Hz, 1H), 7.31(dd, J=8.4, 2.0Hz, 1H), 7.24(d, J=1.9Hz, 1H), 4.36–4.28(m, 2H), 3.33(q, J=5.1Hz, 2H).

[0098] Intermediate 2: Preparation of 8-bromo-4-(3-methoxybenzyl)-3,4-dihydro-1,4-benzoxazepine-5(2H)-one.

[...

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Abstract

The invention relates to a TNIK inhibitor as well as a preparation method and application thereof, and belongs to the field of medicines. The invention provides a compound shown in a formula I or a pharmaceutically acceptable salt thereof. The series of compounds provided by the invention have good inhibitory activity on Traf2 and Nck interaction serine kinase (TNIK) in vitro, and meanwhile, the series of compounds provided by the invention have a remarkable effect on treatment of colorectal cancer, so that the series of compounds provided by the invention provide a new choice for development of TNIK inhibitors and development of anti-tumor and anti-inflammatory-disease drugs in the field, and has a good application prospect.

Description

technical field [0001] The invention relates to a TNIK inhibitor, a preparation method and application thereof, and belongs to the field of medicine. Background technique [0002] Traf2 interacts with Nck Serine kinase (TNIK) is a member of the germinal central kinase family (GCKs), involved in the formation of the cytoskeleton and the extension of neurites. The NF-κB system exists in almost all cells, and it is involved in the regulation of many important cell functions, such as cell survival, growth and immune response. TNIK is necessary for both canonical NF-κB signaling pathway and JNK signaling pathway. Therefore, TNIK has been widely studied as an anti-tumor target. According to literature reports, TNIK kinase is overexpressed in various cancer cell lines and tissues and is closely related to poor prognosis. [0003] Colorectal cancer is an important cause of death among cancer patients, and approximately 700,000 people die from the disease every year worldwide. Mo...

Claims

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Application Information

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IPC IPC(8): C07D471/04C07D413/04C07D487/04C07D417/04A61K31/553A61K31/437A61K31/536A61K31/506A61K31/4985A61K31/519A61K31/53A61K31/4439A61K31/498A61K31/4375A61K31/538A61P35/00
CPCC07D471/04C07D413/04C07D487/04C07D417/04A61P35/00
Inventor 杨胜勇李琳丽
Owner SICHUAN UNIV
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