WO2025094152 - C RADIOLABELED MCHR1 PET LIGANDS

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Publication Number WO/2025/094152
Publication Date 08.05.2025
International Application No. PCT/IB2024/060862
International Filing Date 04.11.2024
Title [English] C RADIOLABELED MCHR1 PET LIGANDS [French] C
Applicants ** RICHTER GEDEON NYRT. Gyömröi út 19-21. 1103 Budapest, HU
Inventors ** BATA, Imre Frankel Leó út 7. 1027 Budapest, HU SPRÁNITZ, Péter Hatház utca 14/III/8 H-1106 Budapest, HU TÚRÓS, György István Diófa u. 19. 2014 Csobánka, HU
Priority Data P2300374  03.11.2023  HU
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Abstract [English] The present invention provides radiolabeled 2, 3, 4, 5 -tetrahydro-1H-[1,4]diazepino[1,7-a]indol-9-yl]pyridin-2(1H)-one derivatives of general formula (I) or salts thereof and precursors of formulae (II) and (III) to said radioligands, to processes for the preparation thereof, and to intermediates of said processes. The radiolabeled compounds enable visualization and quantification of melanin concentrating hormone receptor 1 (MCHR1) receptors in various target tissues, including monitoring the MCHR1 in such target tissue. The compounds exhibit high binding affinity towards MCHR1 and can pass the blood-brain barrier, thereby facilitate the diagnosis of a range of disease states in human clinical research. [French] La présente invention concerne des dérivés de 2,3,4,5-tétrahydro-1H-[1,4] diazépino [1,7-a] indol-9-yl] pyridin -2(1H)-one radiomarqués de formule générale (I) ou des sels de ceux-ci et des précurseurs de formules (II) et (III) desdits radioligands, leurs procédés de préparation et des intermédiaires desdits processus. Les composés radiomarqués permettent la visualisation et la quantification du récepteur 1 de l'hormone de concentration de mélanine (MCHR1) dans divers tissus cibles, y compris la surveillance du MCHR1 dans un tel tissu cible. Les composés présentent une affinité de liaison élevée vis-à-vis de MCHR1 et peuvent passer la barrière hémato-encéphalique, ce qui facilite le diagnostic d'une plage d'états pathologiques dans la recherche clinique humaine. (I)