WO2025172252 - PROTRACTED CCR5 ANTAGONISTS AND USES THEREOF

National phase entry is expected:
Publication Number WO/2025/172252
Publication Date 21.08.2025
International Application No. PCT/EP2025/053504
International Filing Date 11.02.2025
Title **
[English] PROTRACTED CCR5 ANTAGONISTS AND USES THEREOF
[French] ANTAGONISTES DE CCR5 À ACTION PROLONGÉE ET LEURS UTILISATIONS
Applicants **
NOVO NORDISK A/S
Inventors
PREMDJEE, Bhavesh
TORNØE, Christian, Wenzel
BUCHARDT , Jens
HAXVIG, Christina, Sophie
WANG, Zhou
HELGSTRAND, Charlotte, Marie
HØIBERG-NIELSEN, Rasmus
Priority Data
24157786.5   15.02.2024   EP
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Quotation for National Phase entry

Country StagesTotal
China Filing, Examination, Granting3584
EPO Filing, Examination, Granting14275
Japan Filing, Examination, Granting2153
South Korea Filing, Examination, Granting2071
USA Filing, Examination, Granting7890
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Total: 29,973
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Abstract[English] A CCR5 antagonist comprising a polypeptide comprising a Glutamic acid or an Aspartic Acid at position 45 and 46, and a Cysteine or a Lysine at position 68, optionally comprising a protraction moiety attached to the polypeptide at position 68 comprising a fatty acid and a linker with at least one negative charge. The CCR5 antagonist providing increased potency, stability, and/or pharmacokinetic properties. A formulation comprising the CCR5 antagonist may be suitable for parenteral administration. The compound and pharmaceutical formulation comprising such a compound may be used for medical treatment of patients with non-alcoholic steatohepatitis (NASH), more specifically F3 and/or F4 NASH.[French] L'invention concerne un antagoniste de CCR5 comprenant un polypeptide comprenant un acide glutamique ou un acide aspartique en position 45 et 46, et une cystéine ou une lysine en position 68, comprenant éventuellement une fraction de prolongation fixée au polypeptide en position 68 comprenant un acide gras et un lieur ayant au moins une charge négative. L'antagoniste de CCR5 présente une activité accrue, une stabilité améliorée et/ou des propriétés pharmacocinétiques optimisées. Une formulation comprenant l'antagoniste de CCR5 peut être appropriée pour une administration parentérale. Le composé et la formulation pharmaceutique comprenant un tel composé peuvent être utilisés pour le traitement médical de patients atteints de stéatohépatite non alcoolique (NASH), plus particulièrement NASH F3 et/ou F4.

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