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Muscle relaxation accelerator and therapeutic agent for muscular tissue diseases such as muscle relaxation failure

A relaxation, muscle technique, used in the treatment or prevention of acute pulmonary edema, heart failure treatment or prevention, active compounds, angina pectoris, catecholamine-induced hypertension treatment, myocardial diastolic disorders Related diseases, drugs for the treatment of hypertension, drugs for the treatment or prevention of intramyocardial microvascular angina pectoris, drugs for the treatment or prevention of catecholamine-induced arrhythmia, can solve the problems of decreased blood drug concentration, coronary perfusion disorder, and failure to prevent sudden death, etc. , to improve blood flow

Inactive Publication Date: 2007-05-30
AETAS PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the peripheral blood vessels, smooth muscle relaxes to relax the blood vessels, relieve the sharp rise in blood pressure, and prevent the sharp drop in pressure through this regulating force. Therefore, drugs that promote muscle relaxation can be used as therapeutic drugs for catecholamine-induced hypertension, but how Promotes relaxation of vascular smooth muscle without affecting muscle contraction, which is also a problem
In addition, in ventricular tachycardia, the diastolic period of the ventricle is short, and coronary perfusion is impaired, but how to promote myocardial relaxation without affecting muscle contraction, and to treat tachycardia arrhythmias with short diastolic period, especially ventricular Treatment of tachycardia, another question
When administering antiarrhythmic drugs to express torsades de pointes, the current status quo can only wait for the blood concentration of antiarrhythmic drugs to decrease, and it is impossible to prevent sudden death during the period, which is another problem

Method used

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  • Muscle relaxation accelerator and therapeutic agent for muscular tissue diseases such as muscle relaxation failure
  • Muscle relaxation accelerator and therapeutic agent for muscular tissue diseases such as muscle relaxation failure
  • Muscle relaxation accelerator and therapeutic agent for muscular tissue diseases such as muscle relaxation failure

Examples

Experimental program
Comparison scheme
Effect test

experiment example 1

[0057] In this example, the pharmaceutically acceptable salt of the above-mentioned 1,4 benzothiazepine derivatives uses the monohydrochloride of this compound, that is, 4-[3-(4-benzylpiperidin-1-yl)propionyl ]-7-methoxy-2,3,4,5-tetrahydro-1,4-benzothiazepine monohydrochloride (hereinafter referred to as the present compound). Wistar male rats, 8 weeks old and weighing 300-330 g, were used. Anesthesia was performed by subperitoneal injection of 1000 mg / kg urethane and 80 mg / kg α-chloralose, and natural respiration was used. In this example, 100 mg of the present compound was dissolved in 1 mL of dimethyl sulfoxide (DMSO) to prepare a DMSO solution of the present compound, and the solution was stored at 4°C. The injection amount of norepinephrine is 40 μg / kg / min, and its preparation method is to dissolve 1 mg of norepinephrine in 41 μL of distilled water to make a norepinephrine solution.

[0058] First, a cannula for continuous infusion of calcium chloride aqueous solution o...

experiment example 2

[0069] The effect of this compound on blood pressure

[0070] In this experiment, 8-week-old wistar male rats weighing 310 and 330 g were used. Anesthesia was performed by subperitoneal injection of 1000 mg / kg urethane and 80 mg / kg α-chloralose, and natural respiration was used. In this experimental example, 100 mg of the present compound was dissolved in 1 mL of dimethylsulfoxide (DMSO) to prepare a DMSO solution of the present compound, and the solution was stored at 4°C. Separately, 1 mg of norepinephrine was dissolved in 41 μL of distilled water to prepare a norepinephrine solution.

[0071] This example was carried out at a room temperature of 20-25° C. as in the above-mentioned Experimental Example 1. This example is also the same as the above-mentioned Experimental Example 1. The cannula that continuously injects calcium chloride aqueous solution or norepinephrine aqueous solution containing calcium chloride is inserted into the right external jugular vein of the abov...

experiment example 3

[0083] Study on the effect of the compound on the diastolic ability of the left ventricular wall by tissue Doppler method

[0084] In this experimental example, 9-week-old Wistar male rats with body weights of 310 and 320 g were used. Anesthesia was performed by subperitoneal injection of 1000 mg / kg urethane and 80 mg / kg α-chloralose, and natural respiration was used. In this experimental example, 100 mg of the present compound was dissolved in 1 mL of dimethyl sulfoxide (DMSO) to prepare a DMSO solution of the present compound, and the solution was stored at 4°C. Separately, 1 mg of norepinephrine was dissolved in 41 μL of distilled water to prepare a norepinephrine solution.

[0085] This example was carried out at a room temperature of 20-25° C. as in the above-mentioned Experimental Example 1. This example is also the same as the above-mentioned Experimental Example 1. A cannula that continuously injects calcium chloride aqueous solution or norepinephrine aqueous solutio...

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PUM

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Abstract

A drug which can be used as a muscle relaxation accelerator, therapeutic agent for left ventricular diastolic dysfunction, therapeutic agent for angina pectoris, therapeutic agent for acute pulmonary edema, blood ameliorant for microcirculation system, therapeutic and preventive agent for hypertension, and therapeutic and preventive agent for ventricular tachycardia and Torsade de pointes. The drug is characterized by containing as an active ingredient either a 1,4-benzothiazepine derivative represented by the general formula [I]: [I] [wherein R<1> represents hydrogen or C1-3 alkoxy; R<2> represents hydrogen, C1-3 alkoxy, phenyl (provided that the phenyl may be substituted by one to three substituents selected from the group consisting of hydroxy and C1-3 alkoxys), or a group represented by the formula [II] or [III] (wherein R<3> represents C1-3 acyl); X represents -CO- or -CH2-; and n is 1 or 2] or a pharmaceutically acceptable salt of the derivative.

Description

technical field [0001] The present invention relates to the compound that has the function of promoting the relaxation of muscle tissue, i.e. cardiac muscle, smooth muscle and skeletal muscle, particularly relates to the compound that has the function of promoting myocardial tissue relaxation, more particularly relates to the compound that can be administered to patients with insufficient myocardial relaxation, i.e. myocardial relaxation failure, to promote The relaxation of myocardial tissue, the compound that eliminates the effect of myocardial tissue relaxation failure. [0002] The present invention also relates to a disease related to myocardial diastolic disorder, that is, a therapeutic or preventive drug for a disease related to myocardial relaxation disorder, which contains a compound capable of promoting relaxation of myocardial tissue. The present invention further relates to a drug for improving blood flow in the microcirculatory system, which contains a compound wi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D417/06A61K31/554A61P9/00A61P9/04A61P9/10A61P9/12A61P11/00A61P21/02A61P43/00C07D417/14
Inventor 金子升
Owner AETAS PHARMA
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