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Medical use of optical isomer of amine compound in treating pain

A technology of amine compounds and compounds, applied in the field of medical application of optical isomers of amine compounds to treat pain, can solve the problems of central sedation adverse reactions, cardiotoxicity, dependence and addiction, and achieve excellent analgesia Effect, little toxicity effect

Pending Publication Date: 2019-05-17
CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Opioid analgesics have strong analgesic effects, but long-term use can easily lead to tolerance, dependence, and addiction, and have adverse reactions such as respiratory depression and central sedation. They are currently used for acute sharp pain and severe cancer pain.
Non-steroidal anti-inflammatory drugs only exert a moderate degree of analgesic effect and are suitable for mild and moderate chronic dull pain, but are ineffective for sharp pain caused by direct stimulation of sensory extremities. In addition, they also have adverse reactions such as gastrointestinal bleeding and cardiotoxicity

Method used

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  • Medical use of optical isomer of amine compound in treating pain
  • Medical use of optical isomer of amine compound in treating pain
  • Medical use of optical isomer of amine compound in treating pain

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0052] Embodiment 1. Mouse acetic acid writhing method evaluates the analgesic effect of amoxetine

[0053] 1. Experimental animals:

[0054] KM mouse, male, SPF grade, 22-25g,

[0055] The animals were purchased from the Experimental Animal Center of the Academy of Military Medical Sciences and bred in the Experimental Animal Center of the Academy of Military Medical Sciences.

[0056] 2. Test sample:

[0057] Amoxetine, the structural formula is According to the method of embodiment 5 in the patent CN102850335A, it is prepared;

[0058] Duloxetine hydrochloride (Zhejiang Haixiang Pharmaceutical Co., Ltd.).

[0059] 3. Experimental method:

[0060] 30 minutes after the mice were orally administered the test drug amoxetine or the positive drug duloxetine, each mouse was intraperitoneally injected with 2% acetic acid aqueous solution 0.1ml / 10g, and the writhing of each mouse was observed and recorded within 5-20 minutes The number of times, that is, the body twisting or...

Embodiment 2

[0066] Embodiment 2. Mouse formalin method evaluates the analgesic effect of amoxetine

[0067] 1. Experimental animals:

[0068] KM mouse, male, SPF grade, 22-25g,

[0069] The animals were purchased from the Experimental Animal Center of the Academy of Military Medical Sciences and bred in the Experimental Animal Center of the Academy of Military Medical Sciences.

[0070] 2. Test sample:

[0071] Amoxetine, prepared according to the method of Example 5 in the patent CN102850335A;

[0072] Duloxetine hydrochloride (Zhejiang Haixiang Pharmaceutical Co., Ltd.).

[0073] 3. Experimental method:

[0074] 30 minutes after the mice were orally administered the test drug amoxetine or the positive drug duloxetine, each mouse was subcutaneously injected with 5% formalin aqueous solution 0.02ml on the right paw of each mouse, and observed and recorded for 0-5 minutes respectively (acute phase) The times of licking the feet of each mouse in the two time periods of 10-25 minutes ...

Embodiment 3

[0080] Embodiment 3. Rat sciatic nerve branch selective injury (SNI) model evaluates the analgesic effect of amoxetine

[0081] 1. Experimental animals:

[0082] SD rat, male, SPF grade, 180-220g,

[0083] The animals were purchased from the Experimental Animal Center of the Academy of Military Medical Sciences and bred in the Experimental Animal Center of the Academy of Military Medical Sciences.

[0084] 2. Test sample:

[0085] Amoxetine, prepared according to the method of Example 5 in the patent CN102850335A;

[0086] Duloxetine hydrochloride (Zhejiang Haixiang Pharmaceutical Co., Ltd.).

[0087] 3. Experimental method:

[0088] Rats were anesthetized by intraperitoneal injection of pentobarbital sodium (50mg / kg), and the rats were fixed on the operating table in a lateral position. After disinfection with iodine, the skin on the upper edge of the mouse's right hind limb was cut, the muscles were separated, and the trunk of the sciatic nerve was exposed. and three ...

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Abstract

The invention relates to medical use of an optical isomer of an amine compound, in particular to use of an amine compound represented by a formula I or a pharmaceutically acceptable salt thereof for preventing and / or treating pain. It is proved by experiments that the amine compound represented by the formula I or the pharmaceutically acceptable salt thereof has an excellent abirritation effect, and a novel and effective medicine is provided for preventing and / or treating pain. The formula I is in the description below.

Description

[0001] This application is a divisional application of the invention patent application with the application number 201410495094.4 entitled "The Medical Application of Optical Isomers of Amine Compounds in Treating Pain" filed on September 25, 2014. technical field [0002] The present invention relates to the medical use of amine compounds, in particular to the use of optical isomers of amine compounds for preparing medicines for preventing and / or treating pain. Background technique [0003] Pain is a painful sensation resulting from actual or potential tissue damage, often accompanied by unpleasant emotions or cardiovascular and respiratory changes. It is not only a protective response of the body, but also a common symptom of many clinical diseases. [0004] Depending on the duration, pain can be divided into acute pain and chronic pain. Acute pain is mostly nociceptive pain caused by tissue trauma, while chronic pain is mainly neuropathic pain. Pain has a high clinical...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): A61K31/381A61P29/00A61P25/04A61P21/00
Inventor 仲伯华张有志薛瑞董华进张亭亭何新华樊士勇李云峰黄世杰袁莉
Owner CSPC ZHONGQI PHARM TECH (SHIJIAZHUANG) CO LTD
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