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GPR119 hydrazide agonist, preparation method and use thereof

A technology of hydrazine hydrate, C1-C3, applied in the field of GPR119 agonist containing hydrazide structure, which can solve the problems of decreased insulin secretion, unclear exact reasons, and decreased GIP activity

Inactive Publication Date: 2015-04-29
FOSHAN SAIWEISI MEDICINE SCI & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, in patients with type 2 diabetes it has been shown that the insulinotropic effect of GIP is decreased, although the insulinotropic effect of GLP-1 is maintained
What is puzzling is that patients with type 2 diabetes still have a good response to a large injection of GIP, but lose sensitivity to continuous small injections (Meier et al., Diabetes, 2004, 53, S220-S224), The exact reason for this decrease in GIP activity is therefore unclear

Method used

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  • GPR119 hydrazide agonist, preparation method and use thereof
  • GPR119 hydrazide agonist, preparation method and use thereof
  • GPR119 hydrazide agonist, preparation method and use thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0028] The synthesis of embodiment 1 compound I-1

[0029]

[0030] A. Synthesis of Compound IV-1

[0031] Compound II-1 (0.68g, 10mmol) and compound III (1.95g, 10mmol) were dissolved in 20mL dry DMF, stirred at room temperature, solid potassium carbonate (4.15g, 30mmol) and 0.5g KI were added, and then heated at 80°C Stirring was continued until the reaction was complete (about 5 hours). The reaction mixture was poured into 150 mL ice water with 50 mL × 3 CH 2 Cl 2 After extraction, the extract phases were combined, washed with brine, and dried over anhydrous sodium sulfate. The desiccant was removed by suction filtration, the filtrate was evaporated to dryness on a rotary evaporator, and the obtained residue was purified by column chromatography to obtain compound IV-1, a white solid, ESI-MS, m / z=183 ([M+H] + ).

[0032] B. Synthesis of Compound V-1

[0033] Compound IV-1 (1.28g, 7mmol) was dissolved in 15mL of absolute ethanol, stirred at room temperature, 1mL of...

Embodiment 2

[0036] The synthesis of embodiment 2 compound 1-2

[0037]

[0038] A. Synthesis of Compound IV-1

[0039] Compound II-1 (0.68g, 10mmol) and compound III (1.95g, 10mmol) were dissolved in 20mL dry DMF, stirred at room temperature, solid potassium carbonate (4.15g, 30mmol) and 0.5g KI were added, and then heated at 80°C Stirring was continued until the reaction was complete (about 5 hours). The reaction mixture was poured into 150 mL ice water with 50 mL × 3 CH 2 Cl 2 After extraction, the extract phases were combined, washed with brine, and dried over anhydrous sodium sulfate. The desiccant was removed by suction filtration, the filtrate was evaporated to dryness on a rotary evaporator, and the obtained residue was purified by column chromatography to obtain compound IV-1, a white solid, ESI-MS, m / z=183 ([M+H] + ).

[0040] B. Synthesis of Compound V-1

[0041] Compound IV-1 (1.28g, 7mmol) was dissolved in 15mL of absolute ethanol, stirred at room temperature, 1mL o...

Embodiment 3-8

[0045] Referring to the operation steps of Example 1, the compounds listed in the following table were synthesized.

[0046]

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PUM

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Abstract

The invention relates to the field of medicines related to type 2 diabetes, and in particular relates to a GPR119 agonist containing a hydrazide structure, and a preparation method and application thereof in preparation of a medicine for treating type 2 diabetes. The GPR119 agonist disclosed by the invention is represented by the formula shown in the specification, wherein R is selected from a group including H, C1-C3 alkyl and C3-C6 cycloalkyl.

Description

technical field [0001] The present invention relates to the pharmaceutical field for the treatment of type II diabetes. More specifically, the present invention relates to a kind of GPR119 agonist containing a hydrazide structure, which has a therapeutic effect on type II diabetes, its preparation method and its application in pharmacy. Background technique [0002] Diabetes is increasingly threatening human health. In the United States today, approximately 16 million people are suffering from diabetes. Type 1 diabetes, also known as insulin-dependent diabetes, is an autoimmune disease. It is caused by the destruction of the pancreatic islet β cells that can produce insulin by the autoimmune system. There is currently no cure for this disease in the world, so patients must receive insulin injections. Without insulin injections, cells cannot absorb glucose for energy. Symptoms associated with type 1 diabetes usually appear in childhood and adolescence. Because the course...

Claims

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Application Information

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IPC IPC(8): C07D233/56A61P3/10
CPCC07D233/56
Inventor 蔡子洋
Owner FOSHAN SAIWEISI MEDICINE SCI & TECH
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