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Glucagon-like peptide-1 receptor regulator, its preparation method and uses

A receptor regulator, glucagon technology, applied in pharmaceutical formulations, medical preparations containing active ingredients, metabolic diseases, etc.

Inactive Publication Date: 2006-12-27
SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, apart from GLP-1 and its analogues, no studies have been reported on non-peptide GLP-1R modulators

Method used

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  • Glucagon-like peptide-1 receptor regulator, its preparation method and uses
  • Glucagon-like peptide-1 receptor regulator, its preparation method and uses
  • Glucagon-like peptide-1 receptor regulator, its preparation method and uses

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0230] NMR calibration: δH / C 7.26 / 77.0ppm (CDCl3); δH / C 2.50 / 39.51ppm (DMSO-d6).

[0231]

[0232] Compound 1 (1g) was dissolved in an appropriate amount of DMSO, placed under a 150W high-pressure mercury lamp for 3 days of irradiation, 1ml of water was added, and the irradiation was continued for 7-10 days, during which the reaction was detected and tracked by HPLC. After the reaction is completed, the solvent is removed by lyophilization, and the residue is separated by column chromatography [the chromatographic column is ZORBAX SB-C18 (2.1 × 150mm, 3.5 μm), the mobile phase is acetonitrile / water=65: 35, and the flow rate is 0.2ml / min, The detection wavelength is 254nm]. Compound 2 was obtained as light yellow powder solid.

[0233] 1 HNMR (300MHz, DMSO-d6) 10.053 (2H, br.s), 8.630 (2H, br.s), 8.029 (2H, dd, J 1 = 3.6Hz,J 2 = 1.2Hz), 8.090 (2H, dd, J 1 = 4.8Hz,J 2 =1.2Hz), 7.605(4H, d, J=8.4Hz), 7.395(4H, d, J=8.1Hz), 7.31(2H, m), 7.280(2H, br.s), 7.260(2H, m ), 7....

Embodiment 2

[0236]

[0237] Compound 1 (10g) was dissolved in an appropriate amount of DMSO, placed at room temperature under natural light for 30-90 days, lyophilized to remove the solvent, and the residue was separated by HPLC [the chromatographic column was ZORBAX SB-C18 (2.1×150mm, 3.5μm) , the mobile phase is acetonitrile / water=65:35, the flow rate is 0.2ml / min, and the detection wavelength is 254nm], a small amount of light yellow powdery solid compound 2 can be obtained.

Embodiment 3

[0239]

[0240] Compound 1 (20 mg) was dissolved in an appropriate amount of DMSO, 25 mg of benzophenone was added, and placed under a 150w high-pressure mercury lamp for irradiation for 1 day, the solvent was removed by lyophilization, and the residue was separated by column chromatography [the chromatographic column was ZORBAX SB-C18 ( 2.1×150 mm, 3.5 μm), the mobile phase is acetonitrile / water=65:35, the flow rate is 0.2 ml / min, and the detection wavelength is 254 nm] to obtain light yellow powdery solid compound 2.

[0241]In the above reaction example, according to the reaction conditions, the reaction solution is dichloromethane, dichloroethane, water, DMSO or a mixed solvent of DMSO and water, dioxochlorocycline or a mixed solvent of the above solvents. Natural light, light or high-pressure mercury lamps are used to irradiate, the light temperature is 0° to room temperature, and the light time is 1 to 90 days. During the reaction, a catalytic amount of benzophenone is...

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Abstract

The invention provides substituted cyclic compound presented with general formula Iand II, method for preparing the same and application of preventing or treating metabolic disorder disease (including diabetes, insuline resistance and adiposis, and etc.) As modifier for glucagons-1 acceptor.

Description

technical field [0001] The present invention relates to the structure and preparation method of a class of substituted cyclic compounds and their use as glucagon-like peptide-1 receptor (Glucagon like peptide-1 receptor, GLP-1R) modulators in the prevention or treatment of metabolic disorders (including but not limited to medical use in diabetes, insulin resistance and obesity, etc.). Background technique [0002] Diabetes mellitus is a group of clinical syndromes caused by the interaction of genetic and environmental factors. It is mainly divided into type 1 and type 2. The basic pathophysiology of type 1 diabetes is absolute insulin deficiency, and the clinical treatment is mainly based on insulin supplementation. Therefore, it is also called insulin-dependent diabetes. Type 2 diabetes accounts for more than 95% of the affected population. Clinical studies have found that most patients with type 2 diabetes can synthesize normal or even excess insulin, but the sensitivity ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D333/38C07C69/003A61K31/381A61P3/10A61P3/04A61P3/00
CPCC07D333/38A61P3/00A61P3/10A61P3/04A61P43/00A61P5/50C07C233/06C07C233/07C07C229/28
Inventor 王明伟李娜王光星廖嘉渝谢欣刘青周彩红南发俊
Owner SHANGHAI INST OF MATERIA MEDICA CHINESE ACAD OF SCI
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