Use of arylpiperazine derivatives in preparing medicament for treating ache

A technology of use and medicine, which is applied in the field of use of arylpiperazine derivatives in the preparation of medicines for treating pain, and can solve problems such as renal dysfunction, easy addiction, respiratory depression, etc.

Active Publication Date: 2009-08-05
NHWA PHARMA CORPORATION
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Such drugs have no advantages such as addiction, dependence, or drug resistance. The disadvantages are severe gastrointestinal reactions, gastrointestinal bleeding, and renal dysfunction.
Opioid analgesics mainly include full agonists of opioid receptors (such as morphine) and partial agonists of opioid receptors (pentazocine), which are effective for most pains except neuropathic pain Analgesic effect, especially for moderate to severe central pain that other analgesics are ineffective. It is mainly used for acute pain, cancer pain, etc. Its disadvantages are easy addiction, depression, respiratory depression, nausea, Constipation, etc.

Method used

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  • Use of arylpiperazine derivatives in preparing medicament for treating ache
  • Use of arylpiperazine derivatives in preparing medicament for treating ache
  • Use of arylpiperazine derivatives in preparing medicament for treating ache

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0063] Preparation of 2-[4-(2-methoxyphenyl)-1-piperazinyl]-1-phenylethanone

[0064] 4-(2-methoxyphenyl)-1-piperazine hydrochloride (46.7g, 0.20mol), α-chloroacetophenone (37.2g, 0.24mol), ethanol (480ml), sodium carbonate (50.4g, 0.5mol), was added into a 1000ml four-neck flask, and refluxed for 4 hours. TLC was followed until the reaction was complete. Cool and filter. The filter cake was dissolved in dichloromethane, the inorganic salts were filtered off, the filtrate was evaporated to dryness, recrystallized from ethanol, and vacuum-dried at 50°C to obtain 52.5 g of off-white solid with a yield of 84.7%. See Table 1 for the spectrogram data to confirm the structure.

Embodiment 2

[0066] Preparation of 2-[4-(3-methoxyphenyl)-1-piperazinyl]-1-phenylethanone

[0067] 4-(3-methoxyphenyl)-1-piperazine hydrochloride (46.7g, 0.20mol), the feeding amount and operation of α-chloroacetophenone, ethanol, sodium carbonate are the same as in Example 1, to obtain The off-white solid was 50.5 g, and the yield was 84%. See Table 1 for the spectrogram data for confirming the structure.

Embodiment 3

[0069] Preparation of 2-[4-(4-methoxyphenyl)-1-piperazinyl]-1-phenylethanone

[0070] 4-(4-methoxyphenyl)-1-piperazine hydrochloride (46.7g, 0.20mol), the feeding amount and operation of α-chloroacetophenone, ethanol, sodium carbonate are the same as in Example 1, to obtain The off-white solid was 53.5 g, and the yield was 85%. See Table 1 for the spectrogram data for confirming the structure.

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PUM

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Abstract

The invention discloses application of an aryl piperazine compound shown in a formula (I) in preparing medicines for treating acute pain, nerve pain and nociceptive pain of mammals including human beings. The medicines are particularly suitable for treating complex pain caused by various reasons.

Description

technical field [0001] The invention relates to the use of arylpiperazine derivatives and pharmaceutically acceptable salts in the preparation of medicines for treating acute pain, neural pain and nociceptive pain in mammals including humans. Background technique [0002] Severe acute and chronic pain, including inflammatory pain, cancer pain, postoperative pain, neuropathic pain, and various recurrent acute and chronic pains, plagues tens of millions of patients. The mechanism of pain is complex, and several pain mechanisms intertwined often appear clinically. At present, the commonly used analgesic drugs in clinical practice are mainly divided into three categories: 1) non-steroidal anti-inflammatory analgesics; 2) opioid analgesics including opioid receptor agonists and opioid receptor partial agonists; 3) auxiliary analgesia The main indications of such drugs are often not analgesic, but they have a unique therapeutic effect on chronic pathological pain. Non-steroidal ...

Claims

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Application Information

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IPC IPC(8): A61K31/495A61K31/496A61P29/00A61P25/04
CPCA61K31/495A61K31/506A61K31/496A61P25/04A61P29/00A61P43/00
Inventor 张桂森郭琳杨相平徐祥清李建其王冠马彦琴胡书明刘世成周世暇
Owner NHWA PHARMA CORPORATION
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