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
CN102716110AInactive Publication Date: 2012-10-10徐江平
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
徐江平
Publication Date
2012-10-10
Estimated Expiration
Not applicable · inactive patent

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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.
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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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