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Pyrimidine acetamides and their application as inhibitors of phosphodiesterase pde2 activity

A technology of pyrimidine acetamide, compounds, applied in the field of medicine

Active Publication Date: 2022-01-25
CHANGZHOU UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Existing PDE2 inhibitors mainly include EHNA, BAY60-7750, and dipyridamole, etc., but no drugs have been marketed yet

Method used

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  • Pyrimidine acetamides and their application as inhibitors of phosphodiesterase pde2 activity
  • Pyrimidine acetamides and their application as inhibitors of phosphodiesterase pde2 activity
  • Pyrimidine acetamides and their application as inhibitors of phosphodiesterase pde2 activity

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0066] Using 4-{2-[5-(2-hydroxy-ethyl)-4-methyl-6-oxo-1,6-dihydro-pyrimidin-2-ylsulfanyl]-acetylamino}-benzene Isopropyl formate (SPECS library number: AS-871 / 43478043) was tested by AMP kit detects its enzymatic level IC 50 The value is 57.75±6.91μmol / L (such as figure 1 shown), and by PDE-Glo TM Phosphodiesterase Assay detects its enzymatic level IC 50 The value is 16.29±0.35μmol / L (such as figure 2 Shown), has good PDE2 enzyme inhibitory effect;

Embodiment 2

[0068] Using N-(3-ethynyl-5,6-dihydro-4H-cyclopenta[b]thiophen-2-yl)-2-[5-(2-hydroxy-ethyl)-4-methyl-6 -Oxo-1,6-dihydropyrimidin-2-ylsulfanyl]-acetamide (SPECS library number: AS-871 / 43478035) by PDE-Glo TM Phosphodiesterase Assay to detect its enzymatic level IC 50 The value is 1.652±0.352μmol / L (such as image 3 ), has a good PDE2 enzyme inhibitory effect.

Embodiment 3

[0070] N-(4-fluorophenyl)-2-((5-(2-hydroxyethyl)-4-methyl-6-oxo-1,6-dihydropyrimidin-2-yl)thio)ethyl Amide AMP kit detects its enzymatic level IC 50 The value is 16.905±2.155μmol / L (such as Figure 4 shown), and by PDE-Glo TM Phosphodiesterase Assay to detect its enzymatic level IC 50 The value is 6.068±0.872μmol / L (such as Figure 5 Shown), has a good PDE2 enzyme inhibitory effect.

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PUM

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Abstract

The invention belongs to the technical field of medicines, and specifically discloses pyrimidine acetamide compounds and their application as phosphodiesterase PDE2 activity inhibitors. Using at least one of pyrimidineacetamide compounds or their hydrates, pharmaceutically acceptable salts, tautomers, stereoisomers, and precursor compounds as active ingredients for the preparation of drugs for preventing or treating PDE2 disorders . The pyrimidine acetamide compound of the present invention can effectively inhibit PDE2 enzymatic activity, through kit and PDE-Glo TM Phosphodiesterase Assay to detect its enzymatic level IC 50 Value, has a good PDE2 enzyme inhibitory effect. As an effective inhibitor of PDE2, the compound of the invention is expected to be used as an active ingredient in the preparation of medicines for treating PDE2 disorders, and has medicinal prospects.

Description

technical field [0001] The invention belongs to the technical field of medicines, and specifically discloses pyrimidine acetamide compounds and their application as phosphodiesterase PDE2 activity inhibitors. Background technique [0002] In 1958, Rall and Sutherland et al. first discovered cyclic adenosine monophosphate (Cyclic adenosine 3', 5'-monophosphate, cAMP); in 1963, Ashman et al. discovered cyclic guanosine monophosphate (cGMP) . Since then, the research on cyclic adenosine monophosphate and cyclic guanosine monophosphate has received more and more attention. [0003] Cyclic adenosine monophosphate (cAMP) and cyclic guanosine monophosphate (cGMP) regulate gene expression by controlling ion channels in cells, are important second messengers in cells, and are related to the realization of many physiological functions, such as learning and memory , cell cycle regulation, cell differentiation, proliferation, inflammatory processes, smooth muscle contraction and relax...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D239/56C07D409/12C07D417/12A61K31/513A61P25/00A61P25/30A61P25/04A61P25/18A61P25/22A61P25/14
CPCC07D239/56C07D409/12C07D417/12A61P25/00A61P25/30A61P25/04A61P25/18A61P25/22A61P25/14
Inventor 冯筱晴唐龙黄险峰孔韧宋国强高英夏颜谈颖
Owner CHANGZHOU UNIV