GABA (Gamma-Aminobutyric Acid) conjugates and using method thereof

A compound and composition technology, applied in the field of GABA conjugates, can solve problems such as the inability to successfully apply sustained-release methods

Inactive Publication Date: 2010-12-01
徐锋
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Sustained-release approaches cannot be successfully applied due to the rapid passage of these GABA analogs through the upper GI tract
[0007] Because of these deficiencies, it is clear that in the process of treating pain, there will be many benefits to patients if there are improved therapeutic effects (i.e., reduced pain severity and / or frequency) while reducing side effects.

Method used

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  • GABA (Gamma-Aminobutyric Acid) conjugates and using method thereof
  • GABA (Gamma-Aminobutyric Acid) conjugates and using method thereof
  • GABA (Gamma-Aminobutyric Acid) conjugates and using method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0152] Embodiment 1: the synthesis of pregabalin-naproxen conjugate

[0153] The present invention provides a method for synthesizing GABA-agent conjugates. The examples below generally describe the synthesis of GABA analog-NSAID conjugates, and more specifically, pregabalin-naproxen conjugates.

[0154]

Embodiment 2

[0155] Embodiment 2: the synthesis of gabapentin-GHB conjugate

[0156] This example generally provides a method for the synthesis of GABA analogue-gamma-hydroxybutyric acid (GHB) conjugates, more specifically gabapentin-GHB conjugates.

[0157]

Embodiment 3

[0158] Example 3: GABA B Synthesis of Agonist-Morphine Conjugates

[0159] This example provides a method for the synthesis of GABA receptor agonist-opiate analgesic conjugates, more specifically GABA B Agonist-morphine conjugates.

[0160]

[0161] The examples provided above should be considered illustrative rather than restrictive, and the invention should not be limited to the various details given herein, changes can be made within the scope of the invention and equivalents of the invention things.

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Abstract

On the one hand, the invention provides a composite of covalent conjugates of GABA (Gamma-Aminobutyric Acid) analogues and medicaments, and on the other hand, the invention provides a method for treating pain and neurological disorder by adopting the conjugates of the GABA analogues.

Description

technical field [0001] The present invention relates to GABA conjugates and methods of use thereof. Background technique [0002] Currently, single-agent treatments are recommended for the relief of many pain conditions, including neuralgia. Narcotic analgesics, gamma-aminobutyric acid (GABA) analogues such as gabapentin, pregabalin and baclofen, antidepressants and non-steroidal anti-inflammatory drugs (NSAIDs) administered alone, in clinical and different animal models Both exhibit pain-relieving properties. [0003] Despite the advantages of currently used single-agent pain relief regimens, these regimens also suffer from a number of drawbacks. One area of ​​concern is that many existing pain treatment options lead to undesired side effects. Narcotic analgesics such as morphine are rarely used to treat chronic pain because of their well-known addictive effects and central nervous system (CNS) side effects, as well as gastrointestinal side effects due to their sole admi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07C271/22C07F9/6561A61K31/27A61K31/675A61P25/00A61P25/04A61P25/22A61P25/24A61P25/28A61P25/18A61P25/16A61P25/08A61P25/14A61P25/20A61P25/30
Inventor 徐锋
Owner 徐锋
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