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A kind of analgesic medicine and its preparation method and application

A compound and crude product technology, applied in the field of analgesic drugs and their preparation, can solve the problems of lack of long-acting analgesic effect, easy to produce drug dependence, short duration of action, etc., so as to achieve improved drug application experience and long-acting analgesia. effect, the effect of reducing side effects

Active Publication Date: 2022-04-15
GUANGDONG JIABO PHARM CO LTD
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, this type of powerful analgesic also shows three common shortcomings: first, it is easy to produce drug dependence; second, it will cause severe respiratory depression in patients with poor respiratory function; third, these powerful analgesics Analgesics have a relatively short duration of action (typically 3 to 5 hours) and do not last longer than 24 hours even when given as a neuraxial injection
However, BU08028 also does not have long-lasting analgesic effect

Method used

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  • A kind of analgesic medicine and its preparation method and application

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0029] Embodiment 1: Preparation of BU08028 propionate

[0030] Add 75 ml of dichloromethane and 0.01 mole of BU08028 base into a 250 ml round bottom flask under ice-cooling conditions. Mix well, and slowly add 20 mL of a dichloromethane solution containing 0.03 M triethylamine. Under the condition of rapid stirring, 20 ml of dichloromethane solution containing 0.011 mol of propionyl chloride was added dropwise. Afterwards, the mixture was stirred and reacted at room temperature for 1 hour; in the reacted mixture, 20 ml of 10% by mass sodium carbonate solution was added to neutralize the residual acid, and after the organic layer was separated, it was dehydrated using sodium sulfate, After filtration and concentration, the crude product of BU08028 propionate derivatives was obtained; the crude product of BU08028 propionate derivatives was subjected to silica gel column chromatography, and gradient elution was carried out with dichloromethane and methanol, and the volume perce...

Embodiment 2

[0032] Embodiment 2: Preparation of BU08028 valerate

[0033] Add 75 ml of dichloromethane and 0.01 mole of BU08028 base into a 250 ml round bottom flask under ice-cooling conditions. Mix well, and slowly add 20 mL of a dichloromethane solution containing 0.03 M triethylamine. Under the condition of rapid stirring, 20 ml of dichloromethane solution containing 0.011 mol of valeryl chloride was added dropwise. Afterwards, the mixture was stirred and reacted at room temperature for 1 hour; in the reacted mixture, 20 ml of 10% by mass sodium carbonate solution was added to neutralize the residual acid, and after the organic layer was separated, it was dehydrated using sodium sulfate, After filtration and concentration, the crude product of BU08028 valerate was obtained; the crude product of BU08028 valerate was subjected to silica gel column chromatography, and gradient elution was carried out with dichloromethane and methanol, and the volume percentage of methanol was from 1% to...

Embodiment 3

[0035] Embodiment 3: the preparation of BU08028 adipate

[0036]The preparation of BU08028 adipate can be prepared according to the method described in Example 1, except that 0.006 mol of adipate chloride is used instead of propionyl chloride. BU08028 adipate was tested by NMR, the results are as follows:

[0037] 1H-NMR (400MHz, CDCl 3 ): 6.64(d, 2H, J=8.0Hz), 6.55(d, 2H, J=8.0Hz), 4.32(s, 2H), 3.24(s, 6H), 2.91-2.71(m, 6H), 2.32 -2.25 (m, 12H), 1.80-1.53 ​​(m, 12H), 1.35-0.20 (m, 52H).

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Abstract

The present invention provides an analgesic drug whose structural formula is shown in Formula I wherein R is selected from alkyl groups with 1-40 carbon atoms. The invention belongs to the technical field of pharmacy, and the analgesic drug provided by the invention realizes long-acting analgesic effect while having significant analgesic activity.

Description

technical field [0001] The invention belongs to the technical field of pharmacy, and in particular relates to an analgesic drug and its preparation method and application. Background technique [0002] Patients with moderate to severe pain, such as postoperative pain and cancer pain, require longer-term analgesic management. Currently, local anesthetics, weak analgesics, and strong analgesics are used in such patients, requiring more frequent administration. [0003] Local anesthetics, such as bupivacaine, can relieve some forms of pain, but they are only applied topically. Furthermore, local anesthetics are short-acting, and even when introduced by intraspinal injection, they usually do not have a duration of action of more than 6 hours. Consequently, local anesthetics are insufficient for acute and severe pain caused by cardiac, pulmonary, abdominal, orthopedic and obstetric surgery, as well as severe burn injuries and terminal cancer. Weak analgesics, such as acetamino...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07D489/12C07D519/06A61K31/485A61P25/04
CPCC07D489/12C07D519/06A61K31/485A61P25/04
Inventor 蔡廷威黄佩雯陈三妹童伟国
Owner GUANGDONG JIABO PHARM CO LTD