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Compounds for targeted degradation of focal adhesion kinase and application of the compounds in medicine

A compound, hydrate technology, applied in the field of biomedicine and drug synthesis

Inactive Publication Date: 2020-06-16
SHENYANG PHARMA UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, with the development of new technology of protein degradation targeting chimera (PROTAC) in recent years, drugs that can effectively degrade FAK protein have yet to be developed.

Method used

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  • Compounds for targeted degradation of focal adhesion kinase and application of the compounds in medicine
  • Compounds for targeted degradation of focal adhesion kinase and application of the compounds in medicine
  • Compounds for targeted degradation of focal adhesion kinase and application of the compounds in medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0138]

[0139] 1 H NMR (600MHz, CDCl 3 )δ10.98(s, 1H), 8.67(d, J=8.4Hz, 1H), 8.07(t, J=4.3 Hz, 2H), 7.55(dd, J=8.1, 7.6Hz, 1H), 7.48( dd,J=7.8,1.2Hz,1H),7.44(t,J=7.8Hz,1H),7.25–7.23(m,2H),7.06(t,J=7.6Hz,1H),6.82(d,J =8.5Hz,1H),6.65(d,J=5.8Hz,1H),6.55(d,J=2.3Hz,1H),6.49(dd,J=8.8,2.3Hz,1H),6.41(t,J =5.6Hz,1H),6.26(d,J=4.6Hz,1H),4.93(dd,J=12.5,5.4Hz,1H),3.95(d,J=6.0Hz,2H),3.86(s,3H ),3.20–3.15(m,4H),3.09(dd,J=14.7,7.3Hz,2H),3.02(d,J=4.8Hz,3H),2.85–2.73(m,3H),2.66(s, 4H),2.44–2.39(m,2H),2.15–2.12 (m,1H),1.49–1.42(m,12H).ESI-MS m / z:908.3[M+H] + .

Embodiment 2

[0141]

[0142] 1 H NMR (600MHz, CDCl 3 )δ11.00(s,1H),9.85(s,1H),8.61(d,J=8.4Hz,1H), 8.05(d,J=8.4Hz,2H),7.49–7.46(m,2H), 7.41(t, J=7.8Hz, 1H), 7.32(s, 1H), 7.06(d, J=7.1Hz, 1H), 7.03(t, J=7.9Hz, 1H), 6.95(d, J=8.6 Hz,2H),6.56(d,J=3.9Hz,1H),6.50(d,J=2.3Hz,1H),6.45–6.40(m,2H),4.88(dd,J=12.2,5.5Hz,1H ),3.82(s,3H),3.65(t,J=5.7Hz,2H),3.52–3.42(m,6H),3.20(s,4H),2.99(d,J=4.8Hz,3H),2.85 –2.63(m,9H),2.46(t,J=5.4Hz,2H),2.09(dd,J=12.8,4.9Hz,1H),1.87–1.82(m,2H).ESI-MS m / z: 896.4[M+H] + .

Embodiment 3

[0144]

[0145] 1 H NMR (600MHz, CDCl 3 )δ10.97(s,1H),10.16(s,1H),8.63(d,J=8.4Hz,1H), 8.06(s,1H),8.05(d,J=8.8Hz,1H),7.46( t,J=7.8Hz,2H),7.42(t,J=7.8Hz,1H), 7.27(s,1H),7.08(d,J=7.1Hz,1H),7.04(t,J=7.5Hz, 1H), 6.87(d, J=8.5Hz, 1H), 6.51(t, J=5.0Hz, 2H), 6.46(dd, J=8.8, 2.3Hz, 1H), 6.39(d, J=4.3Hz, 1H), 4.87(dd, J=12.3, 5.4Hz, 1H), 3.83(s, 3H), 3.73–3.63(m, 12H), 3.45–3.41(m, 2H), 3.19(s, 4H), 3.00 (d,J=4.8Hz,3H),2.84–2.64(m,9H),2.12–2.07(m,1H). ESI-MS m / z:899.5[M+H] + .

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Abstract

The invention relates to the field of biomedicine and drug synthesis, in particular to compounds for targeted degradation of focal adhesion kinase (FAK) protein, pharmaceutically acceptable salts, hydrates, solvates or prodrugs of the compounds, preparation methods of the compounds and the pharmaceutically acceptable salts, hydrates, solvates or prodrugs, and application of the compounds as therapeutic agents, especially as FAK degradation agents. The structures of the compounds, and the geometric isomers or pharmaceutically acceptable salts, hydrates, solvates or prodrugs thereof are shown inthe specification. The compounds provided by the invention have a good degradation effect on FAK kinase, and can be used for preventing, treating or adjunctively treating various diseases related tothe expression or activity of FAK kinase.

Description

technical field [0001] The present invention relates to the field of biomedicine and drug synthesis, and relates to a class of compounds targeting the degradation of focal adhesion kinase (FAK) proteins, as well as pharmaceutically acceptable salts, hydrates, solvates or prodrugs of the compounds, and their preparation methods and its use as a therapeutic agent, especially as a FAK degradation agent. Background technique [0002] Focal adhesion kinase (FAK) is a kind of intracellular non-receptor tyrosine kinase, which belongs to the protein tyrosine kinase family. Since 1992, Schaller et al. have identified FAK as a substrate of the Src oncogene, and it is a highly phosphorylated protein located at focal adhesions. A large number of studies have found that in human breast cancer, ovarian cancer, liver cancer, lung cancer, pancreatic cancer and other tumor cells, FAK mRNA is highly expressed to varying degrees, and the increase in the expression and activity of FAK is an im...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D401/14A61K31/506A61P35/00
CPCA61P35/00C07D401/14
Inventor 赵冬梅王瑞峰程卯生陈以轩赵相欣于思佳吴天啸
Owner SHENYANG PHARMA UNIVERSITY
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