DK2862860T3 - 1,3-oxazolidin- eller 1,3-oxazinanforbindelser som orexinreceptorantagonister - Google Patents

1,3-oxazolidin- eller 1,3-oxazinanforbindelser som orexinreceptorantagonister Download PDF

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DK2862860T3
DK2862860T3 DK13804876.4T DK13804876T DK2862860T3 DK 2862860 T3 DK2862860 T3 DK 2862860T3 DK 13804876 T DK13804876 T DK 13804876T DK 2862860 T3 DK2862860 T3 DK 2862860T3
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methyl
methanone
pyrazol
phenyl
triazol
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Aya Futamura
Yuko Araki
Masahito Abe
Hiroshi Ohta
Ryo Suzuki
Dai Nozawa
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Taisho Pharmaceutical Co Ltd
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Claims (9)

1. Forbindelse gengivet ved formlen (IA):
hvor, X1 og X2 er ens eller forskellige og står for et nitrogenatom eller formlen CH; Y står for en hvilken som helst af strukturerne i følgende formelgruppe (a):
n står for 1 eller 2; R1 står for et hydrogenatom, et halogenatom eller en Ci-6-alkylgruppe; R2 står for en triazolylgruppe, en pyridylgruppe eller en pyrimidinylgruppe; R3 står for et hydrogenatom, et halogenatom eller en Ci-6-alkylgruppe, hvor Ci-6-alkylgruppen eventuelt kan være substitueret med 1 til 3 halogenatomer; og R4 står for et hydrogenatom eller en Ci-6-alkylgruppe; eller et farmaceutisk acceptabelt salt deraf.
2. Forbindelse eller et farmaceutisk acceptabelt salt deraf ifølge krav 1, hvor det i ovenanførte formel (IA) gælder, at R2 er en triazolylgruppe eller en pyrimidinylgruppe; og R3 er et halogenatom.
3. Forbindelse eller et farmaceutisk acceptabelt salt deraf ifølge krav 1 eller 2, hvor n i den ovenanførte formel (IA) er 2.
4. Forbindelse eller et farmaceutisk acceptabelt salt deraf ifølge krav 1 gengivet ved formlen (I):
hvor, X1 og X2 er ens eller forskellige og står for et nitrogenatom eller formlen CH; den ene af Y1 og Y2 står for et nitrogenatom, og den anden står for CH; n står for 1 eller 2; R1 står for et hydrogenatom, et halogenatom eller en Ci-e-alkylgruppe; R2 står for en triazolylgruppe, en pyridylgruppe eller en pyrimidinylgruppe; R3 står for et hydrogenatom, et halogenatom eller en Ci-6-alkylgruppe, hvor Ci-6-alkylgruppen eventuelt kan være substitueret med 1 til 3 halogenatomer; og R4 står for et hydrogenatom eller en Ci-6-alkylgruppe; eller et farmaceutisk acceptabelt salt deraf.
5. Forbindelse eller et farmaceutisk acceptabelt salt deraf ifølge krav 4, hvor det i den ovenanførte formel (I) gælder, at R2 er en triazolylgruppe eller en pyrimidinylgruppe; og R3 er et halogenatom.
6. Forbindelse eller et farmaceutisk acceptabelt salt deraf ifølge krav 4 eller 5, hvor n i den ovenanførte formel (I) er 2.
7. Forbindelse eller et farmaceutisk acceptabelt salt deraf ifølge krav 1, som er en specie eller en blanding af to eller flere specier udvalgt blandt: (-)-(2-{[3-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-l,3-oxazolidin-3-yl)[5-methyl-2- (2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-(2-{[4-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-l,3-oxazolidin-3-yl)[5-methyl-2- (2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-(2-{[3-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-l,3-oxazinan-3-yl)[5-methyl-2- (2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-(2-{[4-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl>-l,3-oxazinan-3-yl)[5-methyl-2- (2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-[(2S,5S)-2-{[4-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-5-methyl-l,3-oxazolidin- 3-yl][5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-[(2S,5R)-2-{[4-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-5-methyl-l,3-oxazolidin- 3-yl][5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, [(2S,4R)-2-{[3-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-4-methyl-l,3-oxazolidin-3- yl][5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-[(2S,4S)-2-{[3-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-4-methyl-l,3-oxazolidin- 3-yl][5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, (±)-2-{[3-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl] methyl }-l,3-oxazolidin-3-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanon, (±)-(2-{[3-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-l,3-oxazolidin-3-yl)[5-fluor-2- (pyrimidin-2-yl)phenyl]methanon, (±)-(2-{[3-(4-fluorphenyl)-lH-pyrazol-l-yl] methyl}-!,3-oxazolidin-3-yl)[5-methyl-2-(2H- 1.2.3- triazol-2-yl)phenyl]methanon, (±)-(2-{[4-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl}-l,3-oxazolidin-3-yl)[5-methyl-2-(2H- 1.2.3- triazol-2-yl)phenyl]methanon, (±)-(2-{[4-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl}-l,3-oxazolidin-3-yl)[5-methyl-2- (pyrimidin-2-yl)phenyl]methanon, (-)-(2-{{[3-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl>-l,3-oxazolidin-3-yl)[6-methyl-3-(2H- 1.2) 3-triazol-2-yl)pyridin-2-yl]methanon, (-)-(2-{[3-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl}-l,3-oxazinan-3-yl)[6-methyl-3-(2H- 1.2) 3-triazol-2-yl)pyridin-2-yl]methanon, (-)-(2-{[3-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl}-l,3-oxazinan-3-yl)[6-methyl-3- (pyrimidin-2-yl)pyridin-2-yl]methanon, (-)-(2-{[3-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-l,3-oxazinan-3-yl)[5-fluor-2-(2H- l,2(3-triazol-2-yl)phenyl]methanon, (^-^-{^-(S-fluorpyridin^-yO-lH-pyrazol-l-ylJmethylJ-l^-oxazinan-S-yOCS-methyl^- (pyrimidin-2-yl)phenyl]methanon, (-)-(2-{[4-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl}-l,3-oxazinan-3-yl)[6-methyl-3-(2H- 1.2.3- triazol-2-yl)pyridin-2-yl]methanon, (-)-(2-{[4-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl}-l,3-oxazinan-3-yl)[6-methyl-3- (pyrimidin-2-yl)pyridin-2-yl]methanon, (-)'[2-{[3-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl>-l,3-oxazinan-3-yl][5-fluor-2- (pyrimidin-2-yl)phenyl]methanon, (-)-[2-{[4-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl>-l,3-oxazinan-3-yl][5-methyl-2-(2H- l,2(3-triazol-2-yl)phenyl]methanon, (-)-[2-{[5-(5-fluorpyridin-2-yl)-l,2,4-oxadiazol-3-yl]methyl>-l,3-oxazinan-3-yl][5- methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, ()-[2-{ [5-(4-fluorphenyl)-1,2,4-oxadiazol-3-yl] methyl}-l,3-oxazinan-3-yl] [5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-[2-{[5-(4-fluorphenyl)-l,2,4-oxadiazol-3-yl]methyl>-l,3-oxazinan-3-yl][6-methyl-3- (2H-l,2,3-triazol-2-yl)pyridin-2-yl]methanon, [(2S,4S)-2-{[4-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-4-methyl-l,3-oxazinan-3- yl[5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-[(2S*,5S*)-2-{[4-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-5-methyl-l,3- oxazinan-3-yl][5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-[2-{[3-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl)-l,3-oxazinan-3-yl][5-methyl-2- (pyrimidin-2-yl)phenyl]methanon, (±)-[2-{[l-(5-fluorpyridin-2-yl)-lH-pyrazol-4-yl] methyl }-l,3-oxazinan-3-yl][5-methyl-2-(pyrimidin-2-yl)phenyl]methanon, ()'[2-{[4-(4-fluorphenyl)-lH-pyrazol-l-yl]methyl>-l,3-oxazlnan-3-yl][5-methyl-2- (pyrimidin-2-yl)phenyl]methanon, (-)-[2-< [ l-(5-fluorpyridin-2-yl)-1 H-pyrazol-4-yl] methyl}-l,3-oxazinan-3-yl][5-fluor-2-(pyrimidin-2-yl)phenyl]methanon, (-)-[2-[l-(5-fluorpyridin-2-yl)-lH-pyrazol-3-yl]methyl}-l,3-oxazolidin-3-yl][5-methyl-2- (2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-[2-{[l-(5-fluorpyridin-2-yl)-lH-pyrazol-4-yl] methyl}-l,3-oxazolidin-3-yl][5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-[2-{[l-(5-fluorpyridin-2-yl)-lH-pyrazol-4-yl] methyl}-l,3-oxazinan-3-yl][5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon, (-)-[(2S*,5R*)-2-{[4-(5-fluorpyridin-2-yl)-lH-pyrazol-l-yl]methyl}-5-methyl-l,3- oxazinan-3-yl][5-methyl-2-(2H-l,2,3-triazol-2-yl)phenyl]methanon.
8. Farmaceutisk sammensætning indeholdende forbindelsen eller et acceptabelt salt deraf ifølge et hvilket som helst af kravene 1 til 7 som virksom bestanddel.
9. Lægemiddel indeholdende forbindelsen eller et farmaceutisk acceptabelt salt deraf ifølge et hvilket som helst af kravene 1 til 7 som virksom bestanddel til anvendelse i behandling eller forebyggelse af en sygdom såsom søvnforstyrrelse, depression, angstlidelse, panisk forstyrrelse, skizofreni, stofafhængighed, Alzheimers sygdom, Parkinsons sygdom, Huntingtons sygdom, spiseforstyrrelse, hovedpine, migræne, smerte, mave-tarm-sygdom, epilepsi, inflammation, immunologisk sygdom, endokrin sygdom eller forhøjet blodtryk.
DK13804876.4T 2012-06-15 2013-06-13 1,3-oxazolidin- eller 1,3-oxazinanforbindelser som orexinreceptorantagonister DK2862860T3 (da)

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US (1) US9266870B2 (da)
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CN110967321A (zh) * 2018-09-29 2020-04-07 泰州医药城国科化物生物医药科技有限公司 一种用于均一体系细胞荧光检测钙流方法
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