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Piperazine derivatives, methods for preparing same, and uses thereof in the treatment of insulin resistance

A compound and halogen atom technology, applied in piperazine derivatives and its preparation and application in the treatment of insulin resistance, can solve the problems of no effect, failure to obtain blood sugar threshold, etc.

Inactive Publication Date: 2014-04-16
马特波利公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] Currently, in about 40% of cases, the treatment used is ineffective and does not achieve the fasting blood glucose threshold of 1.26 g / liter of blood

Method used

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  • Piperazine derivatives, methods for preparing same, and uses thereof in the treatment of insulin resistance
  • Piperazine derivatives, methods for preparing same, and uses thereof in the treatment of insulin resistance
  • Piperazine derivatives, methods for preparing same, and uses thereof in the treatment of insulin resistance

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0219] General Synthetic Routes for the Preparation of Compounds According to the Invention .

[0220]

[0221] Step 1 is an esterification reaction, steps 2 and 3 are nucleophilic substitution reactions and step 4 is a hydrolysis reaction.

[0222] step 1: Esterification

[0223]

[0224] Apparatus: Equipped with a 500mL three-necked flask with magnetic stirring and a refrigerated oil bath under nitrogen purging.

[0225] 5-(4-Hydroxyphenyl)-pentanoic acid 1 (25g) was added to methanol (375mL), then slowly added to sulfuric acid solution (25mL). The resulting solution was heated at 65 °C overnight.

[0226] The progress of the reaction was monitored by TLC (eluent: heptane / ethyl acetate: 1:1). After stirring overnight under these conditions, the starting acid 1 Disappeared and replaced by less polar products.

[0227] The reaction medium is dried and concentrated under reduced pressure. The residue was removed with dichloromethane (300 mL) and the heterogeneou...

Embodiment 2

[0267] Study of antidiabetic activity in db / db mice.

[0268] The antidiabetic activity of the compound represented by formula (I) was tested by oral administration to the animal model of type 2 diabetes, ie, db / db mice.

[0269] Eight-week-old diabetic mice with severe hyperglycemia were used. After receiving and before carrying out the experiment, the animals used were given fixed light (7a.m.-7p.m.) and dark (7p.m.-7a.m.) at the prescribed temperature 21-22°C. Stable in the animal room for at least one week and until the day of the experiment. Their diet consists of a maintenance regime; water and food are available ad libitum.

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Abstract

The invention relates to a compound of formula (I), where R1, R2, R3, m, n, and L1 are as defined in claim 1, to the methods for preparing same, to the pharmaceutical compositions containing same, and to the uses thereof in the treatment of diseases associated with insulin resistance syndrome.

Description

technical field [0001] The present invention relates to a new compound specially used for the treatment of conditions related to insulin resistance syndrome (or syndrome X), especially for the treatment of type 2 diabetes. Background technique [0002] According to surveys, the number of cases of diabetes in the world has increased significantly in recent years. At present, there are nearly 250 million diabetic patients in the world, and it is estimated that there will be more than 400 million diabetic patients in 2030. Type 1 diabetes (destruction of the cells that produce insulin) is mainly treated with insulin injections, and the more common type 2 diabetes (90% of diabetes cases) is characterized by insulin resistance in the body's tissues and requires specific treatment. [0003] A large number of compounds have been proposed for the treatment of diabetes, especially type 2 diabetes. In particular the piperazine derivatives mentioned in EP2781797, and the phenylated d...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D295/088C07D295/096C07D213/74C07D241/20A61K31/495A61P3/10
CPCC07D295/088C07D295/096A61K31/495A61K31/496C07D241/20C07D213/74A61K31/497A61K45/06A61P3/10
Inventor G·莫伊内特G·巴弗瑞尔R·纳萨雷特B·费里尔
Owner 马特波利公司
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