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Phenylimorpholins and analogues thereof
专利权人:
United States of America, as represented by The Secretary, Department of Health and Human Services;Research Triangle Institute
发明人:
BLOUGH, Bruce E.,ROTHMAN, Richard,LANDAVAZO, Antonio,PAGE, Kevin M.,DECKER, Ann Marie
申请号:
ES11723158
公开号:
ES2687095T3
申请日:
2011.05.20
申请国别(地区):
ES
年份:
2018
代理人:
摘要:
A compound according to the formula: ** Formula ** wherein: R1 is optionally substituted aryl; wherein the substituents are selected from the group consisting of OH, C1-4 alkyl, C1-4 alkoxy, C2-4 alkenyl, C2-4 alkynyl, Cl, F, acylamido, CN, CF3, N3, CONH2, CO2R12, CH2OH, CH2OR12, NHCOR12, NHCO2R12, CONR12R13, C1-3 alkylthio, R12SO, R12SO2, CF3S and CF3SO2, wherein R12 and R13 are each independently selected from H or optionally substituted C1-10 alkyl; R2 is H or C1-3 alkyl; R3 is H; R4 is C1-3 alkyl; and R5 is H or OH; R 6 is H or C1-3 alkyl; with the proviso that, when R2 is CH3 and R1 is phenyl, then the phenyl ring of R1 is substituted with one or more substituents and R1 is trans with respect to R2, wherein the compound comprises an enantiomeric excess of at least 95% of the enantiomer (2S-5S), or a pharmaceutically acceptable ester, amide, salt or solvate thereof.Un compuesto según la fórmula:**Fórmula** en donde: R1 es arilo opcionalmente sustituido; en donde los sustituyentes se seleccionan del grupo consistente en OH, alquilo C1-4, alcoxi C1-4, alquenilo C2-4, alquinilo C2-4, Cl, F, acilamido, CN, CF3, N3, CONH2, CO2R12, CH2OH, CH2OR12, NHCOR12, NHCO2R12, CONR12R13, alquiltio C1-3, R12SO, R12SO2, CF3S and CF3SO2, en donde R12 y R13 están cada uno seleccionado, de manera independiente, de H o alquilo C1-10 opcionalmente sustituido; R2 es H o alquilo C1-3; R3 es H; R4 es alquilo C1-3; y R5 es H u OH; R 6 es H o alquilo C1-3; con la salvedad de que, cuando R2 es CH3 y R1 es fenilo, entonces el anillo fenílico de R1 está sustituido con uno o varios sustituyentes y R1 es trans con respecto a R2, en donde el compuesto comprende un exceso enantiomérico de al menos 95% del enantiómero (2S-5S), o un éster, amida, sal o solvato farmacéuticamente aceptable del mismo.
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