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Phloridzin derivative as well as preparation method and application thereof

A technology of phlorizin and derivatives, applied in the field of phloridzin derivatives and synthesis, can solve the problems of low oral utilization rate, inability to absorb phloridzin through the intestinal tract, limited application, etc., achieve excellent blood sugar activity, improve Bioavailability, the effect of inhibiting reabsorption

Active Publication Date: 2010-02-03
CHANGZHOU HI TECH DISTRICT MULTIPLE DIMENSION IND TECH INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0003] However, phlorizin cannot be absorbed through the intestinal tract, and its oral availability is low, which limits its clinical application.

Method used

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  • Phloridzin derivative as well as preparation method and application thereof
  • Phloridzin derivative as well as preparation method and application thereof
  • Phloridzin derivative as well as preparation method and application thereof

Examples

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Effect test

Embodiment Construction

[0041] The compound of formula (I) of the present invention can be prepared by the method shown below.

[0042] Compounds in the compound formula (I) of the present invention:

[0043]

[0044] It can be prepared by reacting the initial compound (I-a) with formaldehyde (or lower alkyl aldehyde) and corresponding primary or secondary amine in a protic solvent:

[0045]

[0046] Primary and secondary amines are C 1 -C 10 Aliphatic amines, amino acids, aromatic amines, unsaturated fatty amines, cycloalkylamines, heterocycloalkylamines, unsaturated cycloalkylamines, unsaturated heterocycloalkylamines.

[0047] The solvent can be any conventional solvent that does not interfere with the reaction, such as water; alcohols (such as methanol, ethanol, propanol); esters (such as ethyl acetate); halogenated hydrocarbons (such as dichloromethane); amides (such as dimethyl formamide); ethers (such as tetrahydrofuran); nitriles (acetonitrile), etc., or mixtures thereof.

[0048] T...

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PUM

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Abstract

The invention provides a phloridzin derivative with a general structure formula (1), which has a function of inhibiting SGLT2. The preparation method of the compound is easy, and the Phloridzin derivative can be used for treating metabolic diabetes, complication thereof and the like.

Description

technical field [0001] The present invention mainly relates to a phlorizin derivative, a synthesis method, a pharmaceutical composition and an application thereof. Background technique [0002] Phlorizin belongs to dihydrochalcone compounds and was discovered in the rhizomes of Rosaceae (such as apples and pears) in the 19th century. In 1987, it was reported that the derivatives of phlorizin had the effect of treating sickle cell anemia (US Patent US4665058). In the same year, another study found that phlorizin and its derivatives were also effective in the treatment of cancer (US Patent US4684627). Phloridizin also has the effect of lowering blood pressure and lipids. Phloridizin can prevent sugar components from entering epidermal cells, inhibit excessive secretion of epidermal glands, and treat acne with exuberant secretion; phloridizin can treat psoriasis (US Patent US4853388); Phloridizin can inhibit the activity of melanocytes, and has a lightening effect on various s...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H15/26C07H15/203C07H1/00A61K31/7056A61K31/706A61K31/7034A61P43/00A61P3/10A61P25/28A61P3/00A61P9/00A61P19/00A61P17/00A61P25/00A61P13/00A61P35/00
CPCC07H15/26A61K31/7034C07H15/203A61P3/00A61P3/08A61P3/10A61P9/00A61P13/00A61P17/00A61P19/00A61P25/00A61P25/28A61P35/00A61P43/00Y02A50/30
Inventor 顾书华赵维民孙伟新
Owner CHANGZHOU HI TECH DISTRICT MULTIPLE DIMENSION IND TECH INST
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