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Compound with pyrazine and thiazolone structure and application thereof in preparing medicament for treating diabetes mellitus

The technology of a diabetes drug and compound is applied to a compound containing pyrazine and a thiazolone structure and its use in the preparation of a drug for treating diabetes, which can solve the problems of uncertain effects and the like, and achieve the effect of reducing side effects

Inactive Publication Date: 2011-10-19
宁波尖锋紫星生物科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Epalrestat is especially suitable for diabetic patients with high glycosylated hemoglobin value due to diet therapy, exercise therapy, oral hypoglycemic drugs or insulin therapy, but not for patients with diabetic peripheral nerve disorders accompanied by irreversible organic changes. affirm its effect

Method used

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  • Compound with pyrazine and thiazolone structure and application thereof in preparing medicament for treating diabetes mellitus
  • Compound with pyrazine and thiazolone structure and application thereof in preparing medicament for treating diabetes mellitus
  • Compound with pyrazine and thiazolone structure and application thereof in preparing medicament for treating diabetes mellitus

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0013] In a 150 ml round bottom flask was added 4.07 g (10 mmol) of 7-[(3R)-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8 - Tetrahydro-3-(1-trifluoromethyl)-1,2,4-oxazole-[4,3,-a]formylpyrazine (sitagliptin) (2) and 3.51 g (11 mmol )(Z,Z)-5-(2-methyl-3-phenyl-2-propenyl)-4-oxo-2-thiooxy-3-thiazolineacetic acid (epalrestat) (1) Dissolve in 50 ml of absolute ethanol, reflux under stirring for 24 hours, filter after completion of the reaction, and dry the filter residue to obtain 6.53 g (9 mmol) of the product (compound of the present invention), melting range: 188.0~189.5° C., yield: 90%.

[0014] The two raw materials used above (7-[(3R)-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3 -(1-Trifluoromethyl)-1,2,4-oxazole-[4,3,-a]formylpyrazine and (Z,Z)-5-(2-methyl-3-phenyl) -2-propenyl)-4-oxo-2-thiooxy-3-thiazoline acetic acid) were purchased from Acros.

[0015] Characterize the target final product obtained in Example 1 of the present invention:

[0...

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PUM

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Abstract

The invention discloses a compound with a pyrazine and thiazolone structure, comprising the following structural formula: a pharmacokinetics test shows that the pharmacokinetics action of the compound in a rat has no obvious difference from the pharmacokinetics action of the monomer obtained after decomposition so that the compound has good absorption, and the absorption of the compound and the monomer obtained after decomposition has no obvious mutual inhibition or promotion function. Because two monomer compounds are medicaments in the markets and have synergism in treating the diabetes mellitus, the compound synthesized by the two monomers has good application prospect in treating the diabetes mellitus.

Description

technical field [0001] The present invention relates to a compound containing pyrazine and thiazolone structures and its use in preparing medicine for treating diabetes. Background technique [0002] Epalrestat is an aldose reductase inhibitor that acts by reversibly inhibiting the aldose reductase enzyme that converts glucose to sorbitol in polyol metabolism associated with the pathogenesis of diabetic complications. Sorbitol is known to affect nerve cell function, and its accumulation in neurons can cause symptoms of diabetic peripheral sensory-motor peripheral neuropathy, such as peripheral nerve disorders (numbness, pain), paresthesias of vibration, and abnormal heartbeats (indicating glycated hemoglobin values). Epalrestat can be used to prevent, improve and treat these peripheral neuropathy symptoms. Epalrestat is clinically especially suitable for diabetic patients with high glycated hemoglobin value due to diet therapy, exercise therapy, oral hypoglycemic drugs or i...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D487/04C07D277/36A61K31/4985A61K31/426A61P3/10
Inventor 徐亚萍余露山余魏峰陈金虎张华星杨志杰骆成才
Owner 宁波尖锋紫星生物科技有限公司
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