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3-(2-carboxylbenzoyl)-oleanolic acid, pharmaceutical composition of same and application of same in treating diabetes and/or obesity

A technology of benzoyl and oleanolic acid, applied in the field of 3-(2-carboxybenzoyl)-oleanolic acid, its pharmaceutical composition and its application for treating diabetes and/or obesity, It can solve the problems that drugs are difficult to achieve therapeutic effect and have many targets, and achieve the effect of abundant synthetic raw materials, easy preparation and simple synthesis

Inactive Publication Date: 2009-09-09
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, drugs with a single target often prompt the body to produce a compensation mechanism to avoid the attack of the drug and thus develop drug resistance. In addition,

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  • 3-(2-carboxylbenzoyl)-oleanolic acid, pharmaceutical composition of same and application of same in treating diabetes and/or obesity
  • 3-(2-carboxylbenzoyl)-oleanolic acid, pharmaceutical composition of same and application of same in treating diabetes and/or obesity
  • 3-(2-carboxylbenzoyl)-oleanolic acid, pharmaceutical composition of same and application of same in treating diabetes and/or obesity

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Abstract

The invention discloses 3-(2-carboxylbenzoyl)-oleanolic acid or physiologically acceptable salt of the same, application of the same and a pharmaceutical composition containing the compound. The compound has inhibition effect on protein tyrosine phosphatase 1B (PTP1B) and 11beta-hydroxysteriod dehydrogenase 1 (11beta-HSD1), has antagonism effect on a glucocorticoid receptor (GR), has agonistic effect on nuclear receptor LXRa: RXRa heterodimer, and can also strengthen the expression of glucose transporter 4 (Glut4) at the same time. A whole animal experiment shows that the compound has hypoglycemic activity. Therefore, the 3-(2-carboxylbenzoyl)-oleanolic acid or the physiologically acceptable salt of the same can be used for treating diabetes, obesity and complicating diseases thereof caused by insulin resistance.

Description

technical field [0001] The present invention relates to the fields of medicinal chemistry and pharmacotherapeutics, in particular to 3-(2-carboxybenzoyl)-oleanolic acid or its physiologically acceptable salt, its pharmaceutical composition, and its ability to be used as protein tyrosine Phosphatase 1B (PTP1B) inhibitors, 11β-hydroxysteroid dehydrogenase 1 (11β-HSD1) inhibitors, glucocorticoid receptor (GR) antagonists, and nuclear receptor LXRα:RXRα heterodimer agonists Medicinal use for the treatment of diabetes and / or obesity. Background technique [0002] Diabetes mellitus (diabetes mellitus) is a group of clinical syndromes caused by the interaction of genetic and environmental factors. Due to the absolute or relative insufficiency of insulin secretion and the decreased sensitivity of target tissue cells to insulin, sugar, protein, fat, water and electrolytes are caused. A range of metabolic disorders. Severe complications such as coronary heart disease, iron deficienc...

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Application Information

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IPC IPC(8): C07J63/00A61K31/56A61P3/10A61P3/04
Inventor 陈静胡立宏沈旭蒋华良林忠辉
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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