WO2025233464 - PROCESS AND INTERMEDIATES FOR THE PREPARATION OF A PHOSPHOGLICERATE DEHYDROGENASE INHIBITOR

National phase entry is expected:
Publication Number WO/2025/233464
Publication Date 13.11.2025
International Application No. PCT/EP2025/062641
International Filing Date 08.05.2025
Title **
[English] PROCESS AND INTERMEDIATES FOR THE PREPARATION OF A PHOSPHOGLICERATE DEHYDROGENASE INHIBITOR
[French] PROCÉDÉ ET INTERMÉDIAIRES POUR PRÉPARER UN INHIBITEUR DE PHOSPHOGLYCÉRATE DÉSHYDROGÉNASE
Applicants **
CHIESI FARMACEUTICI S.P.A.
Inventors
PIVETTI, Fausto
RONCHI, Paolo
BRUNO, Paolo
MONDINI, Simonetta
MALYSA, Piotr Jan
Priority Data
24175140.3   10.05.2024   EP
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Quotation for National Phase entry

Country StagesTotal
China Filing, Examination, Granting2214
EPO Filing, Examination, Granting8885
Japan Filing, Examination, Granting2171
South Korea Filing, Examination, Granting2057
USA Filing, Examination, Granting5940
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Total: 21,267
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Abstract[English] The present invention relates to a process for the preparation of a PHGDH inhibitor, i.e. a stereoisomer of 2-(4-(1-(4-chloro-1,6-dimethyl-1H-indole-2-carboxamido)-2- hydroxyethyl)phenyl) propanoic acid, or a pharmaceutically acceptable salt thereof. The present invention also relates to intermediate compounds which are useful in such process and their preparation thereof. The synthesized PHGDH inhibitor is suitable for use in pharmaceutical applications, for instance in the treatment of fibrosis.[French] La présente invention concerne un procédé de préparation d'un inhibiteur de PHGDH, c'est-à-dire un stéréoisomère de l'acide 2-(4-(1-(4-chloro-1,6-diméthyl-1H-indole-2-carboxamido)-2-hydroxyéthyl)phényl)propanoïque, ou un sel pharmaceutiquement acceptable de celui-ci. La présente invention concerne également des composés intermédiaires qui sont utiles dans un tel procédé et leur préparation. L'inhibiteur de PHGDH synthétisé est approprié pour être utilisé dans des applications pharmaceutiques, par exemple dans le traitement de la fibrose.

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