WO2026113275 - SOLID-PHASE PREPARATION METHOD FOR TIRZEPATIDE
National phase entry is expected:
Publication Number
WO/2026/113275
Publication Date
04.06.2026
International Application No.
PCT/CN2025/095319
International Filing Date
16.05.2025
Title **
[English]
SOLID-PHASE PREPARATION METHOD FOR TIRZEPATIDE
[French]
PROCÉDÉ DE PRÉPARATION EN PHASE SOLIDE DE TIRZÉPATIDE
[Chinese]
一种替尔泊肽的固相制备方法
Applicants **
FUJIAN GENOHOPE BIOTECH LTD.
Inventors
HE, Zhiquan
HOU, Zhidong
CHEN, Chengyun
XU, Jinxing
FAN, Linlin
WU, Yongfan
Priority Data
202411746036.4
29.11.2024
CN
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International Searching Authority |
CNIPA
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The Standard Agent's Assignment
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Legal Entity
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| Entry into National Phase under |
Chapter I
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Send the Letters Patent by Courier
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing, Examination, Granting | 1576 | |
| EPO | Filing, Examination, Granting | 11558 | |
| Japan | Filing, Examination, Granting | 1998 | |
| South Korea | Filing, Examination, Granting | 1804 | |
| USA | Filing, Examination, Granting | 4740 |
Total:
21,676
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Abstract[English]
The present invention relates to the technical field of polypeptide drug preparation methods. Provided is a solid-phase preparation method for high-yield and high-purity tirzepatide. An amino resin is used as a starting resin; amino acids and small-fragment peptides are sequentially coupled according to the amino acid sequence of tirzepatide using a solid-phase synthesis method to synthesize a tirzepatide resin; and the tirzepatide resin is cleaved and purified to obtain a pure tirzepatide product. The small-fragment peptides include a 1-4 tetrapeptide fragment Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH, a 5-6 dipeptide fragment Fmoc-Thr(tBu)-Phe-OH, a 7-8 dipeptide fragment Fmoc-Thr(tBu)-Ser(tBu)-OH, a 10-11 dipeptide fragment Fmoc-Tyr(tBu)-Ser(tBu)-OH, a 12-13 dipeptide fragment Fmoc-Ile-Aib-OH, a 17-18 dipeptide fragment Fmoc-Ile-Ala-OH, a 20-side-chain peptide Fmoc-Lys(AEEA-AEEA-γ-Glu(α-OtBu)-Eicosanedioic acid(mon-tBu))-OH, a 28-30 tripeptide fragment Fmoc-Ala-Gly-Gly-OH, a 32-34 tripeptide fragment Fmoc-Ser(tBu)-Ser(tBu)-Gly-OH, and a 36-38 tripeptide fragment Fmoc-Pro-Pro-Pro-OH. A coupling agent for coupling the amino acid and the small-fragment peptide is selected from Oxyma and DIC, TPTU and TMP, or COMU and DIEA.[French]
La présente invention relève du domaine technique des procédés de préparation de médicament polypeptidique. L'invention concerne un procédé de préparation en phase solide de tirzépatide à haut rendement et à pureté élevée. Une résine amino est utilisée en tant que résine de départ ; des acides aminés et des peptides à petits fragments sont couplés de manière séquentielle selon la séquence d'acides aminés de tirzépatide à l'aide d'un procédé de synthèse en phase solide pour synthétiser une résine tirzépatide ; et la résine tirzépatide est clivée et purifiée pour obtenir un produit tirzépatide pur. Les peptides à petits fragments comprennent un fragment tétrapeptidique 1-4 Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH, un fragment dipeptidique 5-6 Fmoc-Thr(tBu)-Phe-OH, un fragment dipeptidique 7-8 Fmoc-Thr (tBu)-Ser (tBu)-OH, un fragment dipeptidique 10-11 Fmoc-Tyr(tBu)-Ser(tBu)-OH, un fragment dipeptidique 12-13 Fmoc-Ile-Aib-OH, un fragment dipeptidique 17-18 Fmoc-Ile-Ala-OH, un peptide de chaîne latérale 20 Fmoc-Lys(AEEA-AEEA-γ-Glu(α-OtBu)-acide eicosanedioïque (mon-tBu))-OH, un fragment tripeptidique 28-30 Fmoc-Ala-Gly-Gly-OH, un fragment tripeptidique 32-34 Fmoc-Ser(tBu)-Ser(tBu)-Gly-OH, et un fragment tripeptidique 36-38 Fmoc-Pro-OH. Un agent de couplage pour coupler l'acide aminé et le peptide à petits fragments est choisi parmi Oxyma et DIC, TPTU et TMP ou COMU et DIEA.[Chinese]
涉及多肽药物制备方法技术领域，提供了一种收率高、纯度高的替尔泊肽的固相制备方法，以氨基树脂为起始树脂，用固相合成法按照替尔泊肽的氨基酸序列依次偶联氨基酸和小片段肽合成替尔泊肽树脂，替尔泊肽树脂经裂解、纯化得到替尔泊肽纯品。其中，小片段肽为1～4四肽片段Boc-Tyr(tBu)-Aib-Glu(OtBu)-Gly-OH、5～6二肽片段Fmoc-Thr(tBu)-Phe-OH、7～8二肽片段Fmoc-Thr(tBu)-Ser(tBu)-OH、10～11二肽片段Fmoc-Tyr(tBu)-Ser(tBu)-OH、12～13二肽片段Fmoc-Ile-Aib-OH、17～18二肽片段Fmoc-Ile-Ala-OH、20侧链肽Fmoc-Lys(AEEA-AEEA-γ-Glu(α-OtBu)-Eicosanedioic acid(mon-tBu))-OH、28～30三肽片段Fmoc-Ala-Gly-Gly-OH、32～34三肽片段Fmoc-Ser(tBu)-Ser(tBu)-Gly-OH和36～38三肽片段Fmoc-Pro-Pro-Pro-OH；偶联氨基酸和小片段肽的偶联剂选自Oxyma和DIC、TPTU和TMP或COMU和DIEA。