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A compound for the treatment of erectile dysfunction in men

A technology of erectile dysfunction and compounds, applied in the field of medicine, can solve problems such as low incidence of back pain and audio-visual impairment

Active Publication Date: 2021-06-04
北京精华耀邦医药科技有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Moreover, the high selectivity of avanafil results in fewer side effects than other similar products, and a lower incidence of back pain and hearing impairment
However, avanafil can still cause adverse reactions such as back pain, dizziness, headache, palpitations, vision or hearing loss, etc.

Method used

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  • A compound for the treatment of erectile dysfunction in men
  • A compound for the treatment of erectile dysfunction in men
  • A compound for the treatment of erectile dysfunction in men

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0016] Randomly select 20 volunteers who suffer from male erectile dysfunction disease, and are divided into two groups on average, with 10 people in each group. The first group of volunteers takes the medicine 100 mg for treating male erectile dysfunction of the present invention, and the second group of volunteers After taking 100 mg of avanafil tablets, the onset time and duration of drug effects of the two drugs were counted, and the physical symptoms of the two groups of volunteers were observed.

[0017] The first group of statistical results shows that the onset time of the medicine of the present invention is 40-120 minutes, and the maintenance time of the drug effect morning erection is about 5-10 days. Adverse reactions;

[0018] The second set of statistics shows that the onset time of avanafil tablets is 20-40 minutes, and the duration of drug effect is 4-6 hours. Adverse reactions such as headache, dizziness, and palpitations may occur, and in severe cases, sudde...

Embodiment 2

[0021] Randomly select 20 volunteers suffering from male erectile dysfunction disease, and divide them into two groups on average, with 10 people in each group. The volunteers in the first group take 100 mg of avanafil tablets first, and take 100 mg of the medicine of the present invention after the efficacy of the drug fails. The second group of volunteers first took 100 mg of the drug of the present invention, and then took 100 mg of avanafil tablets after the efficacy of the drug failed, and then observed the symptoms of the two groups of volunteers in terms of physical fitness.

[0022] Observation results found that after the first group of volunteers took avanafil tablets, adverse reactions such as backache and back pain occurred, and after the efficacy of the drug failed, the above adverse reactions disappeared gradually; the second group of volunteers took the medicine of the present invention Afterwards, no adverse reactions occurred, and after taking avanafil tablets ...

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Abstract

The invention discloses a compound for treating male erectile dysfunction, the chemical formula is (S)-4-(3-chloro-4-methoxybenzylamino)-2-(2-(propoxymethyl )pyrrolidin-1-yl)-N-(pyrimidin-2-ylmethyl-1)pyrimidine-5-carboxamide hydrochloride, obtained by hydroxyalkylation of avanafil. After the compound is taken, it can inhibit the metabolism of cyclic guanosine monophosphate in the body, thereby enhancing the relaxation effect of smooth muscle, increasing the blood flow of the penis, and then helping erection. Indeed, after using the compound of the present invention, the morning erection effect is obvious within a certain period of time, and the male penis erects unconsciously and naturally at 4-7 o'clock in the morning without any side effects; and the compound can also be used for the treatment of climacteric syndrome, depression, Back pain caused by fatigue, relieve side effects such as heart palpitations, flushed face, dizziness, listlessness and other side effects caused by nafil drugs, and is beneficial to expel dampness, moisten intestines, laxative, diuresis, etc.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a compound for treating male erectile dysfunction. Background technique [0002] Avanafil (avanafil) is a drug developed by American Vivus Company authorized by Tanabe Mitsubishi Pharmaceutical Co., Ltd. for the treatment of male erectile dysfunction (ED). It was approved by the US FDA on April 27, 2012. The trade name is Stendra, which is an oral, fast-acting, highly selective phosphodiesterase-5 (PDE-5) inhibitor. The chemical formula of avanafil is 4-[(3-chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidine Chloromethyl)-5-pyrimidinecarboxamide, English name: 4-[(3-Chloro-4-methoxybenzyl)amino]-2-[2-(hydroxymethyl)-1-pyrrolidinyl]-N-(2-pyrimidinylmethyl) -5-pyrimidinecarboxamid, the molecular formula is C 23 h 26 ClN 7 o 3 , the molecular weight is 483.9506, and the density is 1.373g / cm 3 , the structural formula is [0003] [0004] Th...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D403/14A61P15/10A61P15/12A61P25/24A61P27/02A61P27/16A61P9/06A61P1/08
CPCA61P1/08A61P9/06A61P15/10A61P15/12A61P25/24A61P27/02A61P27/16C07D403/14
Inventor 卫永刚陈宁王正濂
Owner 北京精华耀邦医药科技有限公司