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Compound for promoting myocardial regeneration, and preparation method, medicine and application thereof

A compound and application technology, applied in the field of compounds that promote myocardial regeneration, promoting myocardial regeneration, novel 3-aryl-2-propen-1-one series derivatives, can solve the problems of myocardial tissue recovery, side effects and the like

Active Publication Date: 2020-07-07
健裕生技股份有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0004] However, no matter in the field of clinical treatment or basic medical research, the interventional therapy or drug therapy that has been developed at present cannot promote the recovery of damaged myocardial tissue, and is more likely to generate other side effects. There is no other effective method except to wait for it to recover on its own

Method used

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  • Compound for promoting myocardial regeneration, and preparation method, medicine and application thereof
  • Compound for promoting myocardial regeneration, and preparation method, medicine and application thereof
  • Compound for promoting myocardial regeneration, and preparation method, medicine and application thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0058] Example 1: Preparation of compounds

[0059] The compound of the present invention is prepared by reacting reactant A and reactant B at a reaction temperature of 0°C to 25°C in an alkaline environment, wherein reactant A is a coumaric acid derivative and a caffeic acid derivative Or a cinnamic acid derivative; the reactant B is an acid compound, an acid anhydride compound, an acid chloride compound or an ester compound.

[0060]Compound 1

[0061] Dissolve 1 g of p-coumaric acid in 8 ml of 10% sodium hydroxide aqueous solution by weight, then cool the reaction to 5°C to 10°C, then take 0.97 g of glutaric anhydride and dissolve it in 5 ml of tetrahydrofuran, then slowly add the solution After stirring for 30 minutes, add 40 ml of water and 40 ml of ethyl acetate and adjust the pH to 5.2, take the organic layer and concentrate to dryness, add 50 ml of water to adjust the pH to 9.33, and then add 1N Aqueous hydrochloric acid solution was carried out until the pH value wa...

Embodiment 2

[0107] Example 2: Use of Compounds to Promote Cardiomyocyte Regeneration

[0108] Compounds of formula (II) can be used to promote cardiomyocyte regeneration and repair traumatized cardiomyocytes:

[0109]

[0110] In formula (II), R 1 is hydroxyl, unsubstituted C 1 -C 6 Alkyl, unsubstituted C 1 -C 6 alkoxy, substituted C 1 -C 6 alkanoic acid group, substituted C 7 -C 12 cycloalkanoate, substituted or unsubstituted C 6 -C 18 arylamino, substituted or unsubstituted C 6 -C 18 phenolic, substituted or unsubstituted C 6 -C 18 aryl, substituted or unsubstituted thienyl, substituted or unsubstituted pyrrolyl, substituted or unsubstituted pyridyl, or substituted or unsubstituted thiazolyl;

[0111] R 2 is hydrogen, hydroxyl, unsubstituted C 1 -C 6 Alkyl, amine (-NH 2 ), acetoxy (-OCOCH 3 ), or -X 2 (CO)-(Y) p -Z,R 3 is hydrogen, hydroxyl, unsubstituted C 1 -C 6 Alkyl, unsubstituted C 1 -C 6 alkoxy or -O-CO-(Y) p -Z, or, R 2 and R 3 interconnected to ...

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PUM

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Abstract

The invention provides a compound for promoting myocardial regeneration, and a preparation method, a pharmaceutical product and application thereof. Specifically, the invention relates to a novel 3-aryl-2-propylene-1-ketone series derivative and a synthesis process thereof. In addition, the invention further provides a pharmaceutical composition containing the derivative and application of the pharmaceutical composition to preparation of a medicine for promoting myocardial regeneration.

Description

technical field [0001] The present invention relates to a novel compound, its preparation method and use, in particular to a compound for promoting myocardial regeneration, its preparation method, medicinal product and use thereof, in particular to a novel 3-aryl-2-propene-1- Ketone series derivatives, their preparation method and their use for promoting myocardial regeneration. Background technique [0002] Myocardial infarction (MI) is a common clinical acute heart disease, which is caused by the sudden interruption of blood circulation in part of the myocardium and the damage caused by the lack of sufficient oxygen to the myocardium. It is generally believed that once a myocardial infarction occurs in a patient, the necrotic cardiomyocytes cannot be regenerated, and the damaged area of ​​the myocardium can only be repaired by forming fibrous scars. The fibrous scars formed after repairing are stiff scar tissue and have no contractile function. It can help the heart maint...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C69/42C07C69/44C07C69/76C07C69/65C07C67/08C07C271/22C07C269/06C07C233/54C07C233/55C07C235/64C07C231/12A61P9/10A61K31/444A61K31/196A61K31/235A61K31/192A61K31/216
CPCC07C69/42C07C69/44C07C69/76C07C69/65C07C271/22C07C233/54C07C233/55C07C235/64A61P9/10A61K31/444A61K31/196A61K31/235A61K31/192A61K31/216
Inventor 李连滋蔡蕙冰黄淑芬蔺以文黄必灿吴盈莹陈美惠许理絜
Owner 健裕生技股份有限公司