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2,4,6,7-tetrasubstituted quinoline compounds as inhibitors of DNA methyltransferases

A compound and substituent technology, applied in the field of 2,4,6,7-quaternary substituted quinoline compounds, can solve problems such as inactivity and achieve effective therapeutic effects

Inactive Publication Date: 2018-09-28
FUNDACION PARA LA INVESTIGACION MEDICA APLICADA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

Compounds 41 and 42 were found to be inactive against DNA methyltransferases, according to the authors

Method used

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  • 2,4,6,7-tetrasubstituted quinoline compounds as inhibitors of DNA methyltransferases
  • 2,4,6,7-tetrasubstituted quinoline compounds as inhibitors of DNA methyltransferases
  • 2,4,6,7-tetrasubstituted quinoline compounds as inhibitors of DNA methyltransferases

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Experimental program
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Embodiment

[0326] The general procedure of the preparative HPLC purification method:

[0327] HPLC measurements were performed using a Gilson 281 from a 233 pump (binary), autosampler and UV detector. Fractions were detected by LC-MS. The MS detector was configured with an electrospray ionization source. The source temperature was maintained at 300-350°C.

[0328] HPLC method (purification method):

[0329] General conditions for methods 1~2, 5~14, 17~42: Reverse phase HPLC was performed on a Luna C18 (100 x 30 mm; 5 μm). Solvent A: water containing 0.1% trifluoroacetic acid; solvent B: acetonitrile. UV detector.

[0330] General conditions for methods 3 and 15: Reverse phase HPLC was performed on a Luna C18 (100 x 30 mm; 4 μm). Solvent A: water containing 0.075% trifluoroacetic acid; solvent B: acetonitrile containing 0.075% trifluoroacetic acid. UV detector.

[0331] General conditions for Method 4: Reverse phase HPLC was performed on a Waters Xbridge (150 x 25 mm; 5 μm)...

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Abstract

The invention relates to the compounds of formula (I), or their pharmaceutically or veterinary acceptable salts, or their stereoisomers or mixtures of stereoisomers, wherein R is a radical selected from the group consisting of formula (A), formula (B), formula (C), formula (D), and formula (E), and R1, R2, and R3 are as defined herein, which are inhibitors of one or more DNMTs selected from the group consisting of DNMT1, DNMT3A and DNMT3B. It also relates to pharmaceutical or veterinary compositions containing them, and to their use in medicine, in particular in the treatment and / or preventionof cancer, fibrosis and / or immunomodulation.

Description

[0001] This application claims the benefit of European Patent Application EP15382620.1 filed on December 14, 2015. [0002] The present invention relates to 2,4,6,7-quaternary substituted quinoline compounds which are inhibitors of DNA methyltransferases. The present invention also relates to pharmaceutical or veterinary pharmaceutical compositions containing them, and their use in medicine, especially as anticancer agents, antifibrotic agents and immunomodulators. Background technique [0003] In recent years, it has been shown that cancer is a genetic and epigenetic disease in which epigenetic and genetic alterations interact to promote cancer development. However, unlike genetic mutations, epigenetic alterations are reversible, and therefore, drugs that restore epigenetic balance represent exciting potential cancer therapeutic targets. Epigenetics refers to heritable changes in gene expression patterns that occur independently of changes in the original DNA sequence. The ...

Claims

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Application Information

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IPC IPC(8): C07D401/14C07D405/14C07D405/04A61K31/4709A61P35/00
CPCA61P35/00C07D401/14C07D405/04C07D405/14
Inventor X·阿吉雷·埃娜J·奥亚扎巴尔·圣玛丽娜F·普罗斯佩尔·卡多索M·O·拉巴尔·格雷西亚E·圣·乔斯·埃内里斯J·A·桑切斯·阿里亚斯
Owner FUNDACION PARA LA INVESTIGACION MEDICA APLICADA
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