A group of 2-amido-3-alkoxy substituted pyridine compounds and their new applications

A compound and composition technology, applied in 2-amido-3-alkoxypyridine compounds, the preparation of the compound, the field of the pharmaceutical composition of the compound, to achieve good anti-atherosclerosis effect, broad The effect of the application foreground

Active Publication Date: 2018-09-25
MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
View PDF2 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

2-amido-3-alkoxy substituted pyridine compounds have no literature reports on the anti-atherosclerosis effect, which is the first discovery of this patent application

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • A group of 2-amido-3-alkoxy substituted pyridine compounds and their new applications
  • A group of 2-amido-3-alkoxy substituted pyridine compounds and their new applications
  • A group of 2-amido-3-alkoxy substituted pyridine compounds and their new applications

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0045] The preparation of embodiment 1N-(3-hydroxyl-2-pyridyl)-4-(1,3-dithio-2-cyclopentyl)benzamide (LX-1)

[0046] According to the operating method of Example 1, with 0.23g (0.001mol) 4-(1,3-dithio-2-cyclopentyl) benzoic acid and 0.11g (0.001mol) 2-amino-3-pyridinol Feed, to obtain LX-1 pure product 0.31g white solid, yield 97%. MS (ESI, m / z): 319[M]+, 1H NMR (500MHz, d6-DMSO) δ (ppm): 10.568 (s, 1H, NH-CO), 9.856 (s, 1H, -OH), 7.977(m, 2H, Ph-H), 7.655(m, 2H, Ph-H), 7.341(dd, 1H, J=8.0Hz, 1.5Hz, Py-6H), 7.224(dd, 1H, J=8.0 Hz, 5.0Hz, Py-4H), 5.843(s, 1H, SCHS), 5.337(t, 1H, J=5.0Hz, Py-5H), 3.57(m, 2H, CH2), 3.396(m, 2H, CH2)

Embodiment 2

[0047] The preparation of embodiment 2N-(3-hydroxyl-2-pyridyl)-4-trifluoromethoxybenzamide (LX-3)

[0048] According to the operating method of Example 1, 0.21g (0.001mol) 4-trifluoromethoxybenzoic acid and 0.11g (0.001mol) 2-amino-3-pyridinol were fed to obtain 0.25g of LX-3 pure product yellow Solid, 84% yield. MS (ESI, m / z): 299[M]+, 1H NMR (500MHz, d6-DMSO) δ (ppm): 8.151 (m, 1H, Ph-H), 7.960 (d, 1H, J=5.0Hz , Py-6H), 7.530(m, 1H, Ph-H), 7.326(d, 1H, J=7.5Hz, Py-4H), 7.203(m, 1H, NH-CO), 6.654(s, 1H, -OH), 5.337(t, 1H, J=5.0Hz, Py-5H),

Embodiment 3

[0049] The preparation of embodiment 3N-(3-hydroxyl-2-pyridyl)-4-iodobenzamide (LX-5)

[0050] According to the operation method of Example 1, feed intake with 0.25g (0.001mol) 4-iodobenzoic acid and 0.11g (0.001mol) 2-amino-3-pyridinol, obtain LX-5 pure product 0.36g white solid, the yield 90%. MS (ESI, m / z): 341[M]+, 1H NMR (500MHz, d6-DMSO) δ (ppm): 7.957 (s, 1H, NH), 7.924 (m, 2H, Ph-2H), 7.650 (s, 1H, Py-6), 7.323 (m, 2H, Ph-2H), 7.199 (s, 1H, OH), 5.337 (m, 2H, Py-4, 5H),

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention discloses 2-acylamino-3-alkoxyl substituted pyridine compounds and an application of the compounds in treatment and / or prevention of atherosclerosis-induced cardiovascular diseases. Experiments verify that the compounds or pharmaceutical compositions have the function of up-regulating or stabilizing ABCA1 and SR-BI / CLA-1 and can be used for inhibiting bubblization of macrophage or enhancing cholesterol efflux of macrophage. Experiments show that the compounds have the effects of reducing blood fat and cholesterol and have an application prospect of becoming a medicine for reducing blood fat, treating atherosclerosis, cardiovascular diseases and the like.

Description

technical field [0001] The present invention relates to a class of 2-amido-3-alkoxypyridine compounds, which are used in the treatment and / or prevention of atherosclerotic cardiovascular diseases and belong to the field of pharmacy; , SR-BI / CLA-1, the application of lipid-lowering and cholesterol-lowering drugs; the present invention also relates to the preparation method of the compound; the present invention also relates to the pharmaceutical composition of the compound. Background technique [0002] Cardiovascular disease is the main killer of human health in developed countries and most developing countries. In recent years, with the improvement of people's material living standards, the incidence of cardiovascular and cerebrovascular diseases has shown an obvious upward trend, and the death rate of cardiovascular and cerebrovascular diseases accounts for the The composition of population death has reached 1 / 3. Atherosclerosis is the pathological basis of many serious c...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Patents(China)
IPC IPC(8): A61K31/4439A61K31/4412A61K31/443A61K31/496A61K31/4545C07D409/12C07D213/75C07D403/12C07D405/12C07D417/14A61P9/00A61P3/06A61P9/10
Inventor 司书毅洪斌许艳妮贾晓健李永臻刘畅王丽刘祺
Owner MEDICINE & BIOENG INST OF CHINESE ACAD OF MEDICAL SCI
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap