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Phosphodiesterase 4 inhibitor capable of avoiding vomiting and preparation method thereof

A phosphodiesterase and inhibitor technology, applied in the field of phosphodiesterase 4 inhibitors that can avoid vomiting reaction and their preparation, and can solve problems such as side effects

Inactive Publication Date: 2012-10-10
徐江平
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

However, cilomilast interacts with other PDE family members at the μM level at high doses of 15 mg to produce side effects
In fact, the side effect of emesis at high doses is common for most PDE4 inhibitors, and the lack of selectivity of the inhibitors is the problem leading to emesis

Method used

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  • Phosphodiesterase 4 inhibitor capable of avoiding vomiting and preparation method thereof
  • Phosphodiesterase 4 inhibitor capable of avoiding vomiting and preparation method thereof
  • Phosphodiesterase 4 inhibitor capable of avoiding vomiting and preparation method thereof

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Embodiment Construction

[0028] Embodiments of the present invention are further described in detail below.

[0029] A phosphodiesterase 4 inhibitor capable of avoiding vomiting, wherein the phosphodiesterase 4 inhibitor is a compound or prodrug or solvate represented by DTPM; the name of DTPM is: 1-(4-difluoro Methoxy-3-(tetrahydrofuran-3-oxyl)phenyl)-3-methylbutan-1-one, the chemical formula is:

[0030] .

[0031] A method for preparing a phosphodiesterase 4 inhibitor, comprising the following steps:

[0032] Step 1: Add 4-difluoromethoxy-3-((tetrahydrofuran-3-)oxy)benzaldehyde into anhydrous tetrahydrofuran, add isobutylmagnesium bromide dropwise at -78°C, and warm to room temperature , reacted overnight, after the reaction, the reaction solution was poured into water, and the organic matter in the water was extracted with ethyl acetate. After the separated organic layer was dried over anhydrous magnesium sulfate, the magnesium sulfate was removed by filtration, and then the solvent was remov...

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Abstract

The present invention relates to a phosphodiesterase 4 inhibitor capable of avoiding vomiting. The phosphodiesterase 4 inhibitor is a compound, a prodrug or a solvate represented by DTPM; and the DTPM is named as 1-(4-difluoro methoxy-3-(tetrahydrofuran-3-oxyl) phenyl)-3-dimethyl-1-ketone, and has a chemical formula shown as below. A plurality of experiments have proved that the DTPM has better effect on improvement of learning and memory compared with an existing antidepressant PDE4 inhibitor; in a Beagle dog vomiting effect observation experiment, no obvious vomiting inducing reaction is observed; and the DTPM has an inhibitor intensity 5000 times of that of other PDE4D families. The inhibitor provided by the invention can become a drug for treating depression and Alzheimer's disease and improving the cognitive ability, and capable of effectively reducing and even avoiding adverse reactions like vomiting.

Description

technical field [0001] The present invention relates to the technical field of a compound capable of inhibiting phosphodiesterase, in particular to a phosphodiesterase 4 inhibitor capable of avoiding vomiting, which is used for the treatment of depression, Alzheimer's disease and improve cognitive abilities. Background technique [0002] Domestic and foreign studies have found that the prevalence rates of senile dementia (Alzheimer's disease) and senile depression (mostly late-onset depression) are around 1% and 2%-3%, respectively. It can be seen that these two have become common mental illnesses that seriously endanger the life and health of the elderly and cause a great burden on the social service system. When the invention of phosphodiesterase 4 (PDE4) inhibitors appeared, we were delighted to find that these senile mental diseases had the hope of being cured. Therefore, in recent decades, PDE4 inhibitors have become the focus of research by the world's pharmaceutical ...

Claims

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Application Information

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IPC IPC(8): A61K31/341C07D307/20A61P25/28A61P25/24
CPCC07D307/20A61K31/341A61P25/24A61P25/28
Inventor 徐江平周中振程玉芳张明子
Owner 徐江平
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