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Application of an acridinedione compound in the preparation of antidiabetic drugs

An acridione, anti-diabetic technology, applied in the field of biomedicine, can solve the problems of increasing hypoglycemia in patients, achieve the effects of promoting insulin secretion, improving insulin resistance, and increasing glucose consumption

Active Publication Date: 2021-06-29
FOURTH MILITARY MEDICAL UNIVERSITY
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  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The hypoglycemic effect of traditional anti-type 2 diabetes drugs is mainly by stimulating the secretion of insulin from pancreatic β cells and improving insulin sensitivity. These effects are not related to peripheral blood sugar. Therefore, the use of these drugs to lower blood sugar will increase the risk of hypoglycemia in patients

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  • Application of an acridinedione compound in the preparation of antidiabetic drugs
  • Application of an acridinedione compound in the preparation of antidiabetic drugs
  • Application of an acridinedione compound in the preparation of antidiabetic drugs

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Embodiment Construction

[0044] The invention will be further described in detail below in conjunction with specific embodiments, which are explanations of the invention rather than limitations.

[0045] An application of an acridione compound or a pharmaceutically acceptable salt or a pharmaceutically acceptable ester thereof in the preparation of an antidiabetic drug, wherein the structure of the acridione compound is as follows.

[0046]

[0047] each R 1 and R 2 independently for hydrogen, C 1-3 Alkyl, COOH, CH 2 Ph, CH 2 CH(CH 3 ) 2 , Ph, or (X = O, N, S);

[0048] each R 3 independently for hydrogen, halogen, CF 3 、C 1-4 Alkyl or alkoxy, NO 2 or OH;

[0049] each R 4 independently for hydrogen, halogen, CF 3 、C 1-4 Alkyl or alkoxy, NO 2 or OH;

[0050] R 5 is carboxyl, potassium carboxylate, sodium carboxylate or calcium carboxylate, methyl carboxylate or ethyl carboxylate;

[0051] n is 0, 1 or 2

[0052] Preferably, the antidiabetic drug is a GPR40 agonist.

[0053] Pr...

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Abstract

The invention provides an application of an acridine diketone compound in the preparation of antidiabetic drugs, which belongs to the technical field of biomedicine. The present invention confirms for the first time that acridinediones can activate and up-regulate GPR40 protein expression, participate in the GPR40-PPARγ-PI3K / Akt-GLUT4 signaling pathway, promote insulin secretion, increase glucose consumption in liver and muscle tissue, and improve insulin resistance. The target of acridinediones is the GPR40 receptor, and its insulin secretion-stimulating effect is glucose-dependent. When the peripheral blood sugar is lower than a certain level, its hypoglycemic effect will disappear. The preparation of acridinediones into antidiabetic drugs will provide new options and strategies for the treatment of diabetes.

Description

technical field [0001] The invention belongs to the technical field of biomedicine, and particularly relates to the application of acridinediones in the preparation of antidiabetic drugs. Background technique [0002] At present, about 463 million adults aged 20 to 79 worldwide suffer from diabetes, among which type 2 diabetes (T2DM) accounts for more than 90% of the total number of diabetic patients. According to statistics, in 2019, the number of deaths caused by diabetes and its complications was as high as 4.2 million. Diabetic patients in China have reached 116 million, accounting for about a quarter of the total number of diabetic patients in the world. In 2019, the number of deaths caused by diabetes and its complications in my country was about 823,000. Type 2 diabetes has become an important problem affecting human health. The hypoglycemic effect of traditional anti-type 2 diabetes drugs is mainly through stimulating the secretion of insulin by pancreatic β cells ...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D219/06C07D405/14C07D409/14A61P3/10
CPCC07D219/06C07D405/14C07D409/14A61P3/10A61K31/473
Inventor 刘雪英沈歆刘吉元张生勇王庆伟张杰魏朝张东旭梁佳龙张鑫磊
Owner FOURTH MILITARY MEDICAL UNIVERSITY
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