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Up-regulator for expression of ATP (adenosine triphosphate)-binding cassette transporter A1 and application thereof

A technology of transporters and uses, applied in the field of medicine, can solve problems such as ineffectiveness

Active Publication Date: 2014-08-06
KUNMING BAKER NORTON PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Lowering plasma low-density lipoprotein (low-density lipoprotein, LDL) is currently the most commonly used method for clinical treatment of atherosclerosis. The mechanism of action of drugs that inhibit endogenous cholesterol production popular in the European and American markets is the key to inhibiting human cholesterol synthesis The enzyme HMG-CoA reductase has little or no effect on the treatment of atherosclerosis caused by exogenous cholesterol increase

Method used

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  • Up-regulator for expression of ATP (adenosine triphosphate)-binding cassette transporter A1 and application thereof
  • Up-regulator for expression of ATP (adenosine triphosphate)-binding cassette transporter A1 and application thereof
  • Up-regulator for expression of ATP (adenosine triphosphate)-binding cassette transporter A1 and application thereof

Examples

Experimental program
Comparison scheme
Effect test

preparation example 1

[0072] Preparation Example 1: Preparation of Compound Ia

[0073]

[0074] Take 1.22g (0.01mol) of p-hydroxybenzaldehyde, 15mL of dioxane, 5mL of water, and 0.44g (0.011mol) of sodium hydroxide in a 50mL round bottom flask. The reaction is exothermic. After stirring for 0.5h, let it cool to At room temperature, add chloroethanol (3 mL, excess), reflux for 3 h, cool to room temperature, extract with ether, wash twice with water, dry with anhydrous sodium sulfate, evaporate the solvent under reduced pressure, and obtain a light yellow solid Ia by column chromatography , Yield 1.35g, yield 81%. IR(KBr,cm -1 )ν: 3370, 1684, 1600, 1509, 1309, 1164, 1112, 1034, 839; 1 H NMR (CDCl 3 ,300MHz)δ:9.89(s,1H,CHO),7.79(d,J=8.3Hz,2H,ArH),7.32(d,J=8.4Hz,2H,ArH),4.75(t,2H,CH 2 ),4.42(t,2H,CH 2 ).

preparation example 2

[0075] Preparation Example 2: Preparation of Compound Ib

[0076]

[0077] Step (1): Take 6g (0.05mol) of ethylene glycol monobutyl ether, 4g of sodium hydroxide, and 10mL of water in a 50mL round-bottomed flask, stir in an ice bath for half an hour, control the temperature at 0°C, and use a constant pressure dropping funnel to Slowly add 20 mL of a THF solution in which 20.96 g (0.11 mol) of TsCl was dissolved. Continue to react for 5h. Then add 2M NaOH 20mL and heat up to 60°C to react for half an hour to remove excess TsCl, extract with chloroform, dry over anhydrous magnesium sulfate, and evaporate to dryness to obtain a colorless transparent viscous liquid, namely ethylene glycol monobutyl ether sulfonate, yield 11.88g, yield The rate is 92%. 1 H NMR (CDCl 3 ,300MHz)δ:7.79(d,J=8.3Hz,2H,ArH),7.32(d,J=8.4Hz,2H,ArH),4.60(t,2H,CH 2 ),4.15(t,2H,CH 2 ),3.40(t,2H,CH 2 ),2.44(s,3H,CH 3 ),1.50-1.43(m,2H,CH 2 ),1.34-1.26(m,2H,CH 2 ),0.89(t,3H,CH 3 ).

[0078] Step (...

preparation example 3

[0079] Preparation Example 3: Preparation of Compound Ic

[0080]

[0081] The title compound was prepared with reference to the method of Preparation Example 2, using diethylene glycol monomethyl ether instead of ethylene glycol monobutyl ether, and condensed with p-hydroxybenzaldehyde to obtain 4-(2-(2-methoxyl) shown in formula Ic Ethoxy)ethoxy)benzaldehyde: pale yellow low-melting solid, yield 1.62g, yield 73%, mp.44-45°C. IR(KBr,cm -1 )ν: 2891, 1689, 1601, 1509, 1129, 1104, 1034, 836; 1 H NMR (CDCl 3 ,300MHz)δ:9.89(s,1H,CHO),7.81(d,J=8.7Hz,2H,ArH),7.02(d,J=8.6Hz,2H,ArH),4.23(t,J=5.0Hz ,2H,CH 2 ),3.90(t,J=4.7Hz,2H,CH 2 ),3.73(dd,J=2.0Hz,4.8Hz,2H,CH 2 ),3.59(dd,2H,J=2.0Hz,4.8Hz,CH 2 ),3.34(s,3H,CH 3 );ESI-MS: m / z223(M+1,82).

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Abstract

The invention relates to an up-regulator for expression of an ATP (adenosine triphosphate)-binding cassette transporter A1 and an application thereof. The up-regulator for expression of the ATP-binding cassette transporter A1 is a compound shown in a formula I, or pharmaceutically acceptable salts, ester isomers and solvates thereof, wherein all substituent groups are described in description. The up-regulator for expression of the ATP-binding cassette transporter A1, disclosed by the invention, can be used for treating or preventing cardiovascular diseases, such as atherosclerosis.

Description

technical field [0001] The invention belongs to the technical field of medicine, and relates to an agent for up-regulating the expression of transporter A1 with an ATP binding cassette and its application. Background technique [0002] At present, sudden death caused by cardiovascular and cerebrovascular diseases ranks first among all diseases. Among the lethal causes of cardiovascular and cerebrovascular diseases, atherosclerosis (Atherosclerosis, AS) is the most important pathological basis (Murray C J, Lopez A D. Global mortality, disability, and the contribution of risk factors: Global burden of disease study. Lancet1997 , 349(9063):1436-1442). Lowering plasma low-density lipoprotein (low-density lipoprotein, LDL) is currently the most commonly used method for clinical treatment of atherosclerosis. The mechanism of action of drugs that inhibit endogenous cholesterol production popular in the European and American markets is the key to inhibiting human cholesterol synthe...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C47/575C07C45/64A61K31/11A61P9/00A61P9/10
Inventor 戴晓畅王子厚许艳妮闻环阳彦张利生韩武建司书毅段玲燕
Owner KUNMING BAKER NORTON PHARMA