WO2023012709 - AN IMPROVED PROCESS FOR FMOC SYNTHESIS OF SEMAGLUTIDE
National phase entry is expected:
Publication Number
WO/2023/012709
Publication Date
09.02.2023
International Application No.
PCT/IB2022/057235
International Filing Date
04.08.2022
Title **
[English]
AN IMPROVED PROCESS FOR FMOC SYNTHESIS OF SEMAGLUTIDE
[French]
PROCÉDÉ AMÉLIORÉ POUR LA SYNTHÈSE FMOC DE SÉMAGLUTIDE
Applicants **
USV PRIVATE LIMITED
Arvind Vithal Gandhi Chowk, B.S.D. Marg, Govandi
Mumbai 400 088, IN
Inventors
LOBO, Lester John
USV PRIVATE LIMITED
Arvind Vithal Gandhi Chowk, B.S.D. Marg, Govandi
Mumbai 400 088, IN
CHANDRAKESAN, Muralidharan
USV PRIVATE LIMITED
Arvind Vithal Gandhi Chowk, B.S.D. Marg, Govandi
Mumbai 400 088, IN
DOSHI, Chetan
USV PRIVATE LIMITED
Arvind Vithal Gandhi Chowk, B.S.D. Marg, Govandi
Mumbai 400 088, IN
CHANADAK, Shailesh Lalchand
USV PRIVATE LIMITED
Arvind Vithal Gandhi Chowk, B.S.D. Marg, Govandi
Mumbai 400 088, IN
YADAV, Nandlal Gopal
USV PRIVATE LIMITED
Arvind Vithal Gandhi Chowk, B.S.D. Marg, Govandi
Mumbai 400 088, IN
MOHE, Nikhil Umesh
USV PRIVATE LIMITED
Arvind Vithal Gandhi Chowk, B.S.D. Marg, Govandi
Mumbai 400 088, IN
VISHWANATHAN, Kodandaraman
USV PRIVATE LIMITED
Arvind Vithal Gandhi Chowk, B.S.D. Marg, Govandi
Mumbai 400 088, IN
Priority Data
202121035240
05.08.2021
IN
Application details
| Total Number of Claims/PCT | * |
| Number of Independent Claims | * |
| Number of Priorities | * |
| Number of Multi-Dependent Claims | * |
| Number of Drawings | * |
| Pages for Publication | * |
| Number of Pages with Drawings | * |
| Pages of Specification | * |
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International Searching Authority |
EPO
* |
| Applicant's Legal Status |
Legal Entity
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| * | |
| * | |
| * | |
| * | |
| Entry into National Phase under |
Chapter I
* |
| Translation |
|
Recalculate
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Quotation for National Phase entry
| Country | Stages | Total | |
|---|---|---|---|
| China | Filing | 981 | |
| EPO | Filing, Examination | 4588 | |
| Japan | Filing | 590 | |
| South Korea | Filing | 574 | |
| USA | Filing, Examination | 2710 |
Total: 9443 USD
The term for entry into the National Phase has expired. This quotation is for informational purposes only
Abstract[English]
The present invention relates to an improved process for the synthesis of glucagon-like-peptide-1 (GLP-1) and its analogs by using combination of solid and solution phase synthesis of Fmoc protected amino acids in a sequential manner, optionally incorporating Boc protected dipeptide for unnatural amino acid in the Sequence of GLP-1, cleaving GLP-1 sequence from the resin followed by purification; attaching side-chain to the desired amino acid in the solution phase to synthesize desired GLP-1 analog, purifying it to Semaglutide. Temperature gradient is applied during initial coupling of amino acids to facilitate completion of difficult coupling reactions.[French]
La présente invention concerne un procédé amélioré pour la synthèse du peptide-1 de type glucagon (GLP-1) et ses analogues à l'aide d'une combinaison de synthèse en phase solide et en solution d'acides aminés protégés par Fmoc de manière séquentielle, l'incorporation éventuelle d'un dipeptide protégé par Boc pour un acide aminé non naturel dans la séquence de GLP-1, le clivage de la séquence de GLP-1 à partir de la résine suivie d'une purification ; la fixation d'une chaîne latérale à l'acide aminé souhaité dans la phase de solution pour synthétiser un analogue de GLP-1 souhaité, la purification de celui-ci en sémaglutide. Un gradient de température est appliqué pendant le couplage initial d'acides aminés afin de faciliter l'achèvement de réactions de couplage difficiles.