WO2023242809 - CRYSTALLINE FORMS OF 4-[(5-CHLOROPYRIDIN-2-YL)METHOXY]-1-[3-(PROPAN-2-YL)-1H,2H,3H,4H,5H-[1,4]DIAZEPINO[1,7-A]INDOL-9-YL]-1,2-DIHYDROPYRIDIN-2-ONE AND SALTS THEREOF, METHOD OF PREPARATION, AND USES THEREOF

National phase entry:
Publication Number WO/2023/242809
Publication Date 21.12.2023
International Application No. PCT/IB2023/056244
International Filing Date 16.06.2023
Title **
[English] CRYSTALLINE FORMS OF 4-[(5-CHLOROPYRIDIN-2-YL)METHOXY]-1-[3-(PROPAN-2-YL)-1H,2H,3H,4H,5H-[1,4]DIAZEPINO[1,7-A]INDOL-9-YL]-1,2-DIHYDROPYRIDIN-2-ONE AND SALTS THEREOF, METHOD OF PREPARATION, AND USES THEREOF
[French] FORMES CRISTALLINES DE 4-[(5-CHLOROPYRIDIN-2-YL)MÉTHOXY]-1-[3-(PROPAN-2-YL)-1H,2H,3H,4H,5H-[1,4]DIAZÉPINO[1,7-A]INDOL-9-YL]-1,2-DIHYDROPYRIDIN-2-ONE ET LEURS SELS, LEUR PROCÉDÉ DE PRÉPARATION ET LEURS UTILISATIONS
Applicants **
RICHTER GEDEON NYRT.
Inventors
JANKE, Dénes
HOFFMANNÉ SZALAY, Zsófia
DEMETER, Ádám
BEKE, Gyula
Priority Data
P2200221   17.06.2022   HU
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Quotation for National Phase entry

Country StagesTotal
China Filing, Examination, Granting3199
EPO Filing, Examination, Granting21851
Japan Filing, Examination, Granting2862
South Korea Filing, Examination, Granting3516
USA Filing, Examination, Granting15390
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Total: 46,818

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Abstract[English] The present disclosure relates to hydrochloride salts of 4-[(5-chloropyridin-2-yl)methoxy]-1-[3-(propan-2-yl)-1H,2H,3H,4H,5H-[1,4]diazepino[1,7-a]indol-9-yl]-1,2- dihydropyridin-2-one (Compound 1), a potent, and orally active selective melanin-concentrating hormone receptor 1 (MCHR1) antagonist useful in the treatment and/or prevention of obesity, obesity related comorbid conditions and complications, diabetes, metabolic disorders, coronary artery disease, cerebrovascular disease, peripheral artery disease, hypertension, endocrine disorders, psychiatric conditions, personality disorders, eating disorders, sleep-wake cycle disorders, substance abuse and addictive disorders, chronic liver and kidney diseases, gastrointestinal disorders, chronic conditions of the musculo- skeletal system, osteoporosis, cancer, and also in Prader-Willi Syndrome (PWS) or in one or more symptoms of PWS. The present disclosure also relates to crystalline forms of 4-[(5- chloropyridin-2-yl)methoxy]-1-[3-(propan-2-yl)-1H,2H,3H,4H,5H-[1,4]diazepino[1,7-a]indol-9-yl]-1,2-dihydropyridin-2-one in free base form, different crystalline forms of the hydrochloride salt thereof, methods of producing the same, pharmaceutical compositions thereof, and therapeutic applications thereof as well.[French] La présente divulgation concerne des sels de chlorhydrate de 4-[(5-chloropyridin-2-yl)méthoxy]-1-[3-(propan-2-yl)-1H,2H,3H,4H,5H-[1,4]diazépino[1,7-a]indol-9-yl]-1,2-dihydropyridin-2-one (Composé 1), un puissant antagoniste sélectif du récepteur 1 de l'hormone de concentration de mélanine (MCHR1) actif par voie orale utile dans le traitement et/ou la prévention de l'obésité, de troubles et de complications liés à l'obésité comorbides, du diabète, de troubles métaboliques, de maladies coronariennes, de maladies cérébrovasculaires, de maladies artérielles périphériques, de l'hypertension, de troubles endocriniens, de troubles psychiatriques, de troubles de la personnalité, de troubles alimentaires, de troubles du cycle de sommeil-éveil, de l'abus de substances et de troubles addictifs, de maladies hépatiques et rénales, de troubles gastro-intestinaux, de troubles chroniques du système musculo-squelettique, de l'ostéoporose, du cancer, et également dans le syndrome de Prader-Willi (PWS) ou dans un ou plusieurs symptômes de PWS. La présente divulgation concerne également des formes cristallines de 4-[(5-chloropyridin-2-yl)méthoxy]-1-[3-(propan-2-yl)-1H,2H,3H,4H,5H-[1,4]diazépino[1,7-a]indol-9-yl]-1,2-dihydropyridin-2-one sous forme de base libre, différentes formes cristallines du sel de chlorhydrate de celle-ci, leurs procédés de production, leurs compositions pharmaceutiques et leurs applications thérapeutiques.