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SGLT2 (Sodium-glucose co-transporter 2) inhibitor and use thereof

A technology of inhibitors and uses, applied in the field of type 2 Na+-glucose co-transporter inhibitors, can solve the problems of diarrhea, gene mutation, serious problems, etc.

Inactive Publication Date: 2013-12-18
CHINA PHARM UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, clinical studies have found that genetic mutations in SGLT1 can lead to severe or even fatal diarrhea

Method used

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  • SGLT2 (Sodium-glucose co-transporter 2) inhibitor and use thereof
  • SGLT2 (Sodium-glucose co-transporter 2) inhibitor and use thereof
  • SGLT2 (Sodium-glucose co-transporter 2) inhibitor and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Experimental Study on Inhibitory Activity of Compounds 1 to 25 on SGLT2 and SGLT1

[0017] 1. Experimental materials: 96-well plate, Fetal bovine serum (FBS), Ham's F12 medium, Dimethyl sulfoxide (DMSO), Sodium assay buffer (140mM NaCl, 2mM KCl, 1mM CaCl 2 , 1mM MgCl 2 , 10mMN-2-hydroxyethylpiperazine-N'-2-ethanesulfonic acid [HEPES], 5mM tris-HCl, pH7.4), Choline assay buffer, 14 C-AMG, Nonlabeled AMG, Sodium dodecyl sulphate (SDS), MicroScint MS-40 (Packard Instrument Co., Meriden, Ct, USA), Top Count Microplate Scintillation Counter (Packard Instrument Co., Meriden, CT, USA).

[0018] 2. Experimental steps:

[0019] · Transfection of full-length cDNA clones expressing human SGLT1 and SGLT2 into Chinese Hamster Ovary (CHO) cells.

[0020] The transfected cells were cultured in Ham's F12 medium (3*10 per well) containing 10% fetal bovine serum (FBS). 4 cells) at 37°C, 5% CO 2 Incubate for 24 hours under conditions.

[0021] • Dimethyl sulfoxide (DMSO) dissolves c...

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Abstract

The invention relates to the field of medicinal chemistry, and particularly relates to compounds (1-25) and a medicinal use of a medicinal composition containing the compounds, in particular a use as an SGLT2 (Sodium-glucose co-transporter 2) inhibitor.

Description

technical field [0001] The present invention relates to the field of medicinal chemistry, in particular to 25 compounds and containing these compounds, pharmaceutical compositions and their medical uses, especially as type 2 Na + - Use of glucose cooperating transporter (SGLT2) inhibitors. Background technique [0002] The incidence of diabetes is increasing year by year. At present, there are about 285 million diabetic patients in the world, accounting for 6.4% of the world's population. It is expected that by 2030, this number will reach 438 million. Diabetes mellitus is a metabolic disease characterized by elevated blood sugar caused by insulin resistance and secretion defects in the human body. It is mainly divided into type I (T1DM) and type II (T2DM). The former is due to the inability of pancreatic β-cells to produce enough insulin (absolute insulin deficiency), which mostly occurs in adolescents; the latter is due to insufficient insulin secretion or insulin resista...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/7048A61K31/704A61K31/7034A61K31/7032A61K31/34A61K31/343A61K31/404A61K31/443A61P3/10
Inventor 徐金星陆涛
Owner CHINA PHARM UNIV
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