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Fused ring pyridone compound, preparation method and application

A technology of condensed ring pyridone and compound, applied in the field of medicinal chemistry, can solve the problems such as the failure to successfully develop targeted drugs and the small effect

Active Publication Date: 2021-02-02
RUDONG RINGENE PHARMA CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, more than 30 years have passed since the Kras oncogene was first discovered, and several generations of targeted drugs for common proto-oncogenes such as EGFR and BCL have gone through, but the targeted drug for Kras has never been successfully developed
For a long time, targeted drugs for KRas pathway mutant tumors have mainly focused on farnesyl transferase inhibitors and Raf-MEK pathway inhibitors, but with little success

Method used

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  • Fused ring pyridone compound, preparation method and application
  • Fused ring pyridone compound, preparation method and application
  • Fused ring pyridone compound, preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0110] Embodiment General preparation method two

[0111]

[0112] Step 1: Dissolve the fused ring pyridone intermediate (1eq.) in anhydrous tetrahydrofuran, add DIPEA (1.6eq.) and piperazine intermediate (1.5eq.) in sequence, and heat to reflux for 18 hours under nitrogen protection . The reaction was complete as monitored by TLC, cooled to room temperature, and concentrated under reduced pressure. The residue was separated by adding water and dichloromethane. The aqueous phase was extracted three times with dichloromethane. The extract was dried over anhydrous sodium sulfate and concentrated under reduced pressure. The target product was obtained by chromatography separation and purification, and its structure was confirmed by NMR and mass spectrometry.

[0113] The second step: dissolve the above-mentioned first step product (1eq.) in anhydrous glacial acetic acid, slowly add reduced iron powder (3eq.), and heat to 80 degrees under nitrogen protection and stir for 0.5 h...

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Abstract

The invention discloses a fused ring pyridone compound, a preparation method and application. Specifically, the invention relates to a fused ring pyridone compound shown as a general formula I, or pharmaceutically acceptable salts thereof, or an enantiomer, a diastereoisomer, a tautomer, a solvate, a polymorphic substance or a prodrug thereof, and a preparation method and application thereof in pharmacy, and the definition of each group is shown in the specification.

Description

technical field [0001] The invention belongs to the field of medicinal chemistry, and in particular relates to a class of fused-ring pyridone compounds, a compound capable of inhibiting the activity of Ras mutant protein, a preparation method and an application. Background technique [0002] RAS was the first oncogene identified in a human tumor and was first identified in two murine sarcoma viruses. The RAS gene family has three members, namely Hras, ​​Kras, and Nras. In human tumors, Kras mutations are the most common, accounting for about 85%. Previous studies have shown that the Kras mutation can cause cancer because of a missense mutation at codon 12, which changes the structure of the Kras protein and keeps it active. The role of Ras in the transmission of signal pathways is mainly to activate kinases that control gene transcription, thereby regulating cell differentiation and proliferation, and are closely related to the survival, proliferation, migration, metastasi...

Claims

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Application Information

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IPC IPC(8): C07D498/14C07D498/22C07D487/14C07D471/22A61K31/5383A61K31/4985A61P35/00A61P35/02
CPCC07D498/14C07D498/22C07D487/14C07D471/22A61P35/00A61P35/02
Inventor 万惠新查传涛马金贵潘建峰
Owner RUDONG RINGENE PHARMA CO LTD
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