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Hybrid mu opioid receptor and neuropeptide ff receptor binding molecules, their methods of preparation and applications in therapeutic treatment

A molecular, alkyl-based technology applied in the field of hybrid μ-opioid receptor and neuropeptide FF receptor-binding molecules, their preparation and use in therapy, capable of solving little-studied problems

Pending Publication Date: 2021-01-08
CENT NAT DE LA RECHERCHE SCI +2
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

However, little research has been done on the consequences of long-term administration of this class of compounds

Method used

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  • Hybrid mu opioid receptor and neuropeptide ff receptor binding molecules, their methods of preparation and applications in therapeutic treatment
  • Hybrid mu opioid receptor and neuropeptide ff receptor binding molecules, their methods of preparation and applications in therapeutic treatment
  • Hybrid mu opioid receptor and neuropeptide ff receptor binding molecules, their methods of preparation and applications in therapeutic treatment

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0376]1. Materials and methods

[0377]1.1. Chemical synthesis

[0378]1.1.1. Peptide KGFF01-KGFF07

[0379]The peptides KGFF01-KGFF07 were manually synthesized by standard Fmoc-SPPS on Rink amide AM resin. Standard coupling was carried out for 1.5 h by using 3 equivalents (equiv.) of Fmoc protected amino acids and 3 equivalents of coupling reagent (HCTU) in 0.4NMM DMF. Fmoc-Aba-β-Ala-OH was only coupled with a 1.5 equivalent excess of Fmoc-dipeptide and the coupling agent for 3 hours. Boc-Dmt-OH was coupled by using 1.5 equivalents of amino acids in DMF and 1.5 equivalents of HOBt / DIC for 2h without adding alkali to avoid coupling with unprotected phenolic groups. For Fmoc-deprotection, the resin was treated with 20% 4-methylpiperidine in DMF for 5 and 15 minutes, or with DBU / piperidine / DMF 2 / 2 / 96 for 3×30s and 7 minutes. After each coupling and after the deprotection step, use DMF (3×), iPrOH or MeOH (3×) and CH2Cl2(3×) Wash the resin. Use the cutting mixture (TFA / TES / H2O 95:2.5:2.5, TES c...

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Abstract

The present invention relates to molecules binding the mu opioid receptor (MOR) and the neuropeptide FF receptor (NPFFR) and in particular molecules having a MOR agonist and NPFFR modulatory activity.The present invention relates to pharmaceutical compositions, and in particular useful in the treatment of pain and / or hyperalgesia.

Description

Technical field[0001]The present invention relates to molecules that bind to the mu opioid receptor (MOR) and neuropeptide FF receptor (NPFFR), as well as compositions containing the molecules and their use in therapy.Background technique[0002]Opioid analgesics (such as morphine and fentanyl) are still the cornerstone drugs for the treatment of moderate to severe pain. Although opioids have undeniable benefits in the treatment of acute severe pain, there is still a lack of evidence of long-term therapeutic effects. Indeed, repeated administration of morphine exacerbates its adverse reactions, such as pain hypersensitivity, which in turn impairs the efficacy (tolerability) of analgesics and triggers a downward spiral in dose escalation. In addition to pain hypersensitivity, the risk of respiratory depression, addiction, and severe constipation also leads to a decrease in the patient's quality of life. In pursuit of safer analgesics, two main strategies have recently emerged: G protei...

Claims

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Application Information

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IPC IPC(8): A61K38/04C07K7/06
CPCC07K7/06A61K38/04C07D223/14
Inventor 弗雷德里克·西莫南阿尔芒·德里厄·拉罗谢勒弗雷德里克·比赫尔史蒂文·巴莱
Owner CENT NAT DE LA RECHERCHE SCI
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