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Imidazo [1,2-b] pyridacin derivatives and their use as PDE10 inhibitors
专利权人:
Janssen Pharmaceutica; N.V.
发明人:
PASTOR-FERNANDEZ, Joaquin,BARTOLOME-NEBREDA, José,MACDONALD, Gregor,CONDE-CEIDE, Susana,DELGADO-GONZALEZ, Oscar,VANHOOF, Greta,VAN GOOL, Michiel,MARTIN-MARTIN, María,ALONSO-DE DIEGO, Sergio-Alvar,SWIN
申请号:
ES10768978
公开号:
ES2651296T3
申请日:
2010.10.27
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound of Formula (I) ** Formula ** or a stereoisomeric form thereof, wherein R1 is selected from pyridinyl, morpholinyl and pyrrolidinyl; R2 is selected from hydrogen, methyl, ethyl, cyclopropyl, isopropyl, methoxy and trifluoromethyl; R3 is selected from hydrogen, chlorine, methyl, trifluoromethyl and cyclopropyl; Het is selected from pyridinyl and pyrazolyl; R4 is selected from hydrogen; methyl; ethyl; isopropyl; isobutyl; trifluoromethyl; 2,2,2-trifluoroethyl; 2-hydroxy-2-methylpropyl; (2,2-difluorocyclopropyl) methyl; 2,2-difluoro-2-cyclopropylethyl; cyclopropyl; 2-methoxyethyl; 2-methoxypropyl; (2S) -2-methoxypropyl; 2-isopropoxyethyl; 2-ethoxyethyl; ethoxymethyl; 1-methoxy-1-methylethyl; 1-methoxy-1-methylethyl; 2-methoxy-1,1-dimethylethyl; 3-methoxy-3-methylbutyl; 3-methoxypropyl; 2-methoxy-2-methyl-propyl; isopropoxy; 2,2,2-trifluoroethoxy; cyclopropylmethoxy; 2-methoxyethoxy; 2-methoxy-2-methylpropoxy; tetrahydro-2H-pyran-4-yl; (pyridin-3-yl) methyl; 2- (pyrrolidin-1- yl) ethyl; isopropylamino; morpholin-4-yl; pyrrolidin-1-yl; piperazin-1-yl; (3R) -3-methoxypyrrolidin-1-yl; and (3S) -3-methoxypyrrolidin-1-yl; and R5 is hydrogen or methyl or a pharmaceutically acceptable salt or a solvate thereof.Un compuesto de Fórmula (I) **Fórmula** o una forma estereoisómera del mismos, en donde R1 se selecciona de piridinilo, morfolinilo y pirrolidinilo; R2 se selecciona de hidrógeno, metilo, etilo, ciclopropilo, isopropilo, metoxi y trifluorometilo; R3 se selecciona de hidrógeno, cloro, metilo, trifluorometilo y ciclopropilo; Het se selecciona de piridinilo y pirazolilo; R4 se selecciona de hidrógeno; metilo; etilo; isopropilo; isobutilo; trifluorometilo; 2,2,2-trifluoroetilo; 2-hidroxi-2- metilpropilo; (2,2-difluorociclopropil)metilo; 2,2-difluoro-2-ciclopropiletilo; ciclopropilo; 2-metoxietilo; 2-metoxipropilo; (2S)-2-metoxipropilo; 2-isopropoxietilo; 2-etoxietilo; etoximetilo; 1-metoxi-1-metiletilo; 1-metoxi-1-metiletilo; 2-metoxi- 1,1-dimetiletilo; 3-metoxi-3-
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