WO2026118062 - LIQUID PHASE PREPARATION METHOD FOR SEMAGLUTIDE
National phase entry is expected:
Publication Number
WO/2026/118062
Publication Date
11.06.2026
International Application No.
PCT/CN2024/137454
International Filing Date
06.12.2024
Title **
[English]
LIQUID PHASE PREPARATION METHOD FOR SEMAGLUTIDE
[French]
PROCÉDÉ DE PRÉPARATION EN PHASE LIQUIDE DE SÉMAGLUTIDE
[Chinese]
一种司美格鲁肽的液相制备方法
Applicants **
SHENZHEN JYMED TECHNOLOGY CO., LTD
Inventors
LIU, Zicheng
LI, Xinyu
YAO, Zhiyong
FU, Yuqing
ZHANG, Lixiang
Application details
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International Searching Authority |
CNIPA
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| Recordal of a Change of the Applicant's Name/Address |
Change of Applicant's Name and Address
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| Type of Assignment |
The Standard Agent's Assignment
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| Applicant's Legal Status |
Legal Entity
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| Entry into National Phase under |
Chapter I
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| Patent Delivery |
Send the Letters Patent by Courier
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| Translation |
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1676 | |
| EPO | Filing, Examination, Granting | 12068 | |
| Japan | Filing, Examination, Granting | 2183 | |
| South Korea | Filing, Examination, Granting | 2110 | |
| USA | Filing, Examination, Granting | 4740 |
Total:
22,777
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Abstract[English]
Provided is a liquid phase preparation method for semaglutide, which method mainly comprises: deprotecting compound C2 to obtain semaglutide C3, wherein R1 is H or Fmoc, and the remaining amino acids each carry or do not carry a protecting group; and a deprotection reagent is selected from one or more of piperazine and piperazine derivatives. The method for removing Fmoc by using the piperazine or piperazine derivatives results in few impurities. In particular, the Asp/Asn-related impurities, namely [iso-Asp9]-semaglutide and [D-Asp9]-semaglutide, are both present at low levels. Moreover, the method allows for direct purification without precipitation, such that the impurities can be substantially removed by means of simple purification, which is greatly conducive to industrial production.[French]
L'invention concerne un procédé de préparation en phase liquide de sémaglutide, lequel procédé comprend principalement : la déprotection d'un composé C2 pour obtenir du sémaglutide C3, R1 étant H ou Fmoc, et les acides aminés restants portant ou ne portant pas de groupe protecteur ; et un réactif de déprotection étant choisi parmi un ou plusieurs de la pipérazine et de ses dérivés. Le procédé d'élimination de Fmoc à l'aide de pipérazine ou des dérivés de pipérazine conduit à peu d'impuretés. En particulier, les impuretés liées à Asp/Asn, à savoir [iso-Asp9]-sémaglutide et [D-Asp9]-sémaglutide, sont toutes deux présentes à de faibles niveaux. De plus, le procédé permet une purification directe sans précipitation, de telle sorte que les impuretés peuvent être sensiblement éliminées au moyen d'une purification simple, ce qui est considérablement favorable à la production industrielle.[Chinese]
提供一种司美格鲁肽的液相制备方法，主要包括将化合物C2脱保护得到司美格鲁肽C3：其中，R1为H或Fmoc，其余氨基酸各自带或不带保护基团；脱保护试剂选自哌嗪、哌嗪衍生物中的一种或多种。采用哌嗪或哌嗪衍生物脱除Fmoc的方法，产生的杂质少，尤其是Asp/Asn相关的杂质[iso-Asp9]-司美格鲁肽、[D-Asp9]-司美格鲁肽均较小，并且无需沉降，直接进行纯化，经过简单的纯化杂质即可基本去除，大大有利于工业化生产。