Method for preparing linaclotide

A technology of linaclotide and crude peptide, which is applied in the field of preparation of linaclotide, can solve the problems of inability to form three pairs of disulfide bonds with complete selectivity, unable to obtain target products, unsatisfactory results, etc., and achieves considerable economy. The effect of practical value, easy post-processing and low cost
CN103626849AInactive Publication Date: 2014-03-12HYBIO PHARMA
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
HYBIO PHARMA
Publication Date
2014-03-12
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention belongs to the technical field of medicine synthesis, and discloses a method for synthesizing linaclotide by three pairs of total selectively formed disulfide bonds. By using the process, formation of three pairs of disulfide bonds in linaclotide can be sequentially completed in the same solution system, so that the operation method of the process is simple, the yield of final fine peptide of linaclotide can be greatly increased, and large-scale production can be realized.
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Description

technical field

[0001] The invention relates to the technical field of drug synthesis, in particular to a preparation method of linaclotide. Background technique

[0002] Linaclotide, the English name is Linaclotide; the trade name is Linzess; the Chinese common name is Linaclotide. It is a GC-C (intestinal cell uridine cyclase C) receptor agonist, approved by the US FDA in August 2012 for the treatment of adults with chronic idiopathic constipation and constipation-predominant irritable bowel syndrome (IBS) -C). The drug was developed by Ironwood Pharmaceuticals. The compound structure is a polypeptide composed of 14 amino acids containing three pairs of disulfide bonds (the three pairs of disulfide bonds are: 1-6; 2-10 and 5-13), which can be expressed by cells and chemical synthesis, the specific peptide sequence is shown in the following formula:

[0003]

[0004] At present, there is no relatively efficient preparation method for linaclotide, and there are no rele...

Claims

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