Method for preparing ziconotide

A technology of ziconotide and solid-phase synthesis, which is applied in the field of peptide synthesis, can solve the problems of unfavorable high purity, increased impurities, unfavorable and other problems, achieve wide application prospects, improve reaction efficiency, and avoid the effect of impact
CN101709082BInactive Publication Date: 2012-04-18HYBIO PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
HYBIO PHARMA
Publication Date
2012-04-18
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a method for preparing ziconotide. The technical scheme of the invention comprises the following steps: (1) obtaining an Fmoc-Cys(Acm)-amino resin from Fmoc-Cys(Acm)-OH and an amino resin; (2) obtaining a linear-ziconotide-amino resin of which a Cys side chain comprises Acm by performing the solid phase synthesis on the Fmoc-Cys(Acm)-amino resin and an amino acid adopting Fmoc group protection; (3) obtaining a linear crude peptide of which the Cys side chain comprises the Acm by performing cracking on the linear-ziconotide-amino resin of which the Cys side chain comprises the Acm, and obtaining linear ziconotide by removing the Acm, purifying and freeze-drying; (4) and obtaining the ziconotide by performing cyclization, purifying and freeze-drying on the linear ziconotide. The method for preparing ziconotide has the characteristics of simple reaction operation, easy subsequent treatment, low raw material investment, low cost, high yield and the like, and has considerable economic and practical value, and also has wide application prospect in the field of design synthesis of polypeptide drugs.
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Description

technical field

[0001] The invention relates to a synthesis method of polypeptide, especially a solid-phase synthesis method of ziconotide. Background technique

[0002] Ziconotide (Ziconotide) is an N-type calcium channel (N-type calcium channel (NCC)) blocker, which is extracted from a toxin secreted by a fish-eating cone snail (Conus magus) in the South Pacific, containing 25 Amino Acids, Peptide Toxoid Synthesis of Three Pairs of Disulfide Bonds.

[0003] Currently used painkillers mainly include the following two mechanisms: non-steroidal anti-inflammatory drugs (such as ibuprofen) and COX-2 inhibitors (such as Vioxx and Celebrex) work by blocking the pain-causing, COX enzymes in periarticular inflammation; narcotics (such as morphine, cocaine, and oxycodone) block pain-sensing opioid receptors in the brain for more severe pain.

[0004] Opioid painkillers are currently the most effective painkillers, which can relieve any type of pain, but their use is greatly limite...

Claims

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