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Novel FFA1 and PPAR alpha/gamma/delta quadruple agonist, preparation method thereof and application of quadruple agonist as medicine

A technology for uses and drugs, applied in the field of medicine, which can solve problems such as pharmacokinetic defects

Active Publication Date: 2021-05-07
GUANGDONG PHARMA UNIV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

The inventors conducted a lot of research on this compound and found that the long-chain carboxylic acid of RLA8 is prone to β-oxidation, which makes it have obvious pharmacokinetic defects

Method used

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  • Novel FFA1 and PPAR alpha/gamma/delta quadruple agonist, preparation method thereof and application of quadruple agonist as medicine
  • Novel FFA1 and PPAR alpha/gamma/delta quadruple agonist, preparation method thereof and application of quadruple agonist as medicine
  • Novel FFA1 and PPAR alpha/gamma/delta quadruple agonist, preparation method thereof and application of quadruple agonist as medicine

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0024] (E)-2-(2-fluoro-4-((3-methoxy-5-(4-methoxystyryl)phenoxy)methyl)phenoxy)acetic acid

[0025]

[0026] Dissolve 1a (0.5g, 1.9mmol) and 1b (0.49g, 1.9mmol) in acetonitrile (20mL), add potassium carbonate (0.79g, 5.7mmol), and react at 60°C for 4h. After filtration, the mother liquor was spin-dried and the residue was purified by column chromatography (petroleum ether / ethyl acetate, 1:1, v / v) to obtain 0.71 g of a white solid with a yield of 85.2%.

[0027] 1 H NMR (400MHz, DMSO-d 6 )δ7.53(d, J=8.1Hz, 2H), 7.36-7.09(m, 3H), 7.10-6.91(m, 4H), 6.84(s, 1H), 6.75(s, 1H), 6.47(s , 1H), 5.02(s, 2H), 4.36(s, 2H), 3.77(s, 6H). 13 CNMR (75MHz, DMSO-d 6)δ170.78, 161.12,161.09,160.09,159.52,139.93,130.01,130.01,129.43,129.35,129.12,128.36,126.54,120.05,114.90, 114.68,110.45,105.39,105.38,102.53,100.73,68.99,68.00,55.69 , 55.63. ESI-MS m / z: 437.1 [M-H] - .Anal.calcd.For C 25 h 23 FO 6 : C, 68.49; H, 5.29; Found: C, 68.57; H, 5.21.

Embodiment 2

[0029] The FFA1 and PPAR agonistic activities, metabolic stability, in vivo lipid-lowering, anti-fatty liver and anti-fibrosis activities of the compounds of the present invention can be determined by using the assay system described below.

[0030] The following biological test example descriptions illustrate the invention.

[0031] The experimental method of specific conditions in the test example of the present invention is usually according to conventional conditions or according to the conditions suggested by the commodity manufacturer. Reagents whose specific sources are not indicated are commonly used reagents purchased in the market.

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Abstract

The invention relates to a novel FFA1 and PPAR-alpha / gamma / delta quadruple agonist as shown in a formula (I), a preparation method thereof and a pharmaceutical composition containing the compound. As a medicine for treating, preventing or relieving one or more diseases or dysfunction, compared with the prior art, the agonist has better metabolic stability and stronger in-vivo pharmacological effect, and can be used for preparing medicines for treating, preventing or relieving one or more diseases or dysfunction; and the agonist has a wider application prospect.

Description

technical field [0001] The invention relates to a novel FFA1 and PPARα / γ / δ quadruple agonist, a preparation method and application thereof, belonging to the technical field of medicine. The structures of the compounds involved in the present invention are novel and unique in this field. Background technique [0002] Metabolic syndrome is a common disease characterized by insulin resistance and visceral fat accumulation, accompanied by elevated low-density lipoprotein and low high-density lipoprotein cholesterol. The common symptoms are obesity, diabetes, hyperlipidemia, atherosclerosis Cirrhosis and fatty liver, etc. Among them, diabetic patients often have hyperlipidemia, cardiovascular disease, diabetic nephropathy, diabetic neuropathy and other diseases. Metabolic syndrome can be treated with dietary modification and exercise, and when these do not relieve symptoms, medication is required. In terms of drug treatment of metabolic syndrome, the hypoglycemic drugs or lipid...

Claims

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Application Information

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IPC IPC(8): C07C59/70A61K31/192A61P1/16A61P3/10A61P3/06A61P3/04A61P3/00A61P9/10A61P19/06A61P29/00A61P35/00A61P31/12
CPCC07C59/70A61P1/16A61P3/10A61P3/06A61P3/04A61P3/00A61P9/10A61P19/06A61P29/00A61P35/00A61P31/12
Inventor 李政张陆勇周宗涛
Owner GUANGDONG PHARMA UNIV
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