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Pharmaceutical compositions for the treatment of chronic heart failure comprising pyrazolopyrimidinone derivative compound

A technology for chronic heart failure and pyrazolopyrimidone, which is applied in the field of pharmaceutical compositions for the treatment of chronic heart failure, can solve problems such as sudden swelling, and achieve the effects of reducing administration frequency, reducing inherent side effects, and increasing plasma levels

Inactive Publication Date: 2010-03-24
DONG A PHARMA
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In addition, other side effects include dizziness due to low blood pressure, rash and sudden swelling of the lips and cheeks

Method used

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  • Pharmaceutical compositions for the treatment of chronic heart failure comprising pyrazolopyrimidinone derivative compound
  • Pharmaceutical compositions for the treatment of chronic heart failure comprising pyrazolopyrimidinone derivative compound
  • Pharmaceutical compositions for the treatment of chronic heart failure comprising pyrazolopyrimidinone derivative compound

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0047] Example: Evaluation of the therapeutic effect of pyrazolopyrimidinone derivatives in animal models of heart failure

[0048] The pyrazolopyrimidinone derivative of Chemical Formula 1 according to the present invention was evaluated as follows to determine whether it has a therapeutic effect on heart failure.

[0049] Male Sprague-Dawley rats weighing 220-240 g were randomly divided into three groups: normal control group (normal), heart failure control group (CHF) and treatment group (CHF plus cpd.1), each consisting of seven large rat composition. The pyrazolopyrimidinone derivative was orally administered at a dose of 30 mg / kg to animals in the treatment group that had developed heart failure.

[0050] Normal control animals were sham-operated. Heart failure control and treatment animals underwent surgical abdominal incision to create an abdominal aorto-inferior vena cava fistula to artificially increase blood flow from the inferior vena cava to the right atrium. E...

preparation Embodiment

[0062] Formulation Example: Preparation of Pharmaceutical Formulations for Oral Administration

[0063] 1. Preparation of powder

[0064] Compound of formula 1 2 g

[0065] Lactose 1g

[0066] The above ingredients are mixed and placed in an airtight package to produce a powder.

[0067] 2. Preparation of tablets

[0068] Compound of formula 1 100mg

[0069] Corn starch 100mg

[0070] Lactose 100mg

[0071] Magnesium Stearate 2mg

[0072] The above ingredients are mixed and compressed according to conventional tablet manufacturing methods to produce tablets.

[0073] 3. Preparation of Capsules

[0074] Compound of formula 1 100mg

[0075] Corn starch 100mg

[0076] Lactose 100mg

[0077] Magnesium Stearate 2mg

[0078] The above-mentioned ingredients are mixed and loaded into gelatin capsules according to a conventional capsule manufacturing method to prepare capsules.

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Abstract

Disclosed herein is a therapeutic agent for chronic heart failure comprising, as an effective ingredient, 5- [2-propyloxy- 5- (l-methyl-2-pyrrolidinyleneamidosulfonyl) phenyl] - 1 -methyl - propyl-l,6-dihydro-7H-pyrazolo(4,3-d)pyrimidine-7-one. The compound inhibits phosphodiesterase-5 (PDE-5), which catalyzes the intracellular degradation of cyclic guanosine monophosphatase (cGMP), thereby mitigating several signs of chronic heart failure, that is, thereby preventing left ventricular dilatation, decreasing ventricular wall thinning, lowering elevated cardiac and circulating levels of atrial natriuretic peptide (ANP), and inhibiting ventricular fibrosis. Also, the compound has advantages in that it reaches the maximal plasma level in a short time, has an in vivo half-life longer than conventional PDE-5 inhibitors, allowing decreased administration frequency, and has fewer side effects, thus ensuring safety. Thus, the compound is useful as a therapeutic agent for chronic heart failure.

Description

【Technical field】 [0001] The present invention relates to a pharmaceutical composition for the treatment of chronic heart failure (CHF) comprising 5-[2-propoxy-5-(1-methyl-2-pyrrolidinyleneamidosulfonyl)phenyl ]-1-methyl-propyl-1,6-dihydro-7H-pyrazolo(4,3-d)pyrimidin-7-one as an active ingredient. 【Background technique】 [0002] The heart consists of four chambers, two atria (superior) and two ventricles (inferior), and four major valves. When the heart beats, the right atrium receives venous blood from the body. Blood then passes through the tricuspid valve into the right ventricle. At the same time, blood oxygenated in the lungs flows into the left atrium and then through the mitral valve into the left ventricle. Contraction of the right ventricle pushes blood collected in the right atrium into the lungs, where venous blood is combined with oxygen. Oxygenated blood returns to the left atrium and flows down into the left ventricle. The left ventricle contracts to pump ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/519
CPCA61K9/4866A61K31/519A61K9/2059A61P43/00A61P9/00A61P9/04
Inventor 申芝贤安国俊姜庆求安秉玉刘武姬
Owner DONG A PHARMA
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