ECSP993010A

ECSP993010A - FORMULA COMPOUNDS (1) AND ITS PHARMACEUTICALLY ACCEPTABLE SALTS AND SOLVATES

Info

Publication number: ECSP993010A
Authority: EC
Inventors: Mervyn Thompson; John David Harling; Frank Peter Harrington
Priority date: 1999-06-10
Filing date: 1999-06-10
Publication date: 1999-09-09

Abstract

Se describen compuestos de fórmula (I) y sus sales y solvatos farmacéuticamente aceptables: (gráfico), en la que: R1 es hidrógeno, alquilo C1-C6 (opcionalmente sustituido con hidroxi o alcoxi C1-C4), fenil-alquilo C1-C4, alquenilo C1-C6, o alquinilo C1-C6; R2 es hidrógeno o hasta tres sustituyentes seleccionados entre halógeno, NO2, CN, N3, CF3O-, CF3S, CF3SO2-, CF3CO-, alquilo C1-C6, alquenilo C1-C6, alquinilo C1-C6, perfluoro-alquilo C1-C6, cicloalquilo C3-C6, cicloalquil C3-C6-alquilo C1-C4, alquil C1-C6 -O-, alquil C1-C6 -CO, cicloalquil C3-C6 -O-, cicloalquil C3-C6 -CO-, cicloalquil C3-C6-alquil C1-C4-O-, cicloalquil C3-C6-alquil C1-C4 -CO-, fenilo, fenoxi, benciloxi, benzoflo, fenil-alquilo C1-C4-, alquil C1-C6 -S-, alquil C1-C6 -SO2-, (alquil C1-C4)2 NSO2-, (alquil C1-C4)-NHSO2-, (alquil C1-C4)2NCO-, (alquil C1-C4) NHCO- o CONH2; o -NR5R6, donde R5 es hidrógeno o alquilo C1-C4; y R6 es hidrógeno, alquilo C1-C4, formilo, -CO2-alquilo C1-C4 o -CO-alquilo C1-C4; o dos grupos R2 juntos forman un anillo carbocíclico que es saturado o insaturado, opcionalmente interrumpido con O ó NH; los grupos R3 y R4 son independientemente en cada caso hidrógeno o alquilo C1-C6 y/o los dos grupos R3 y/o los dos grupos R4 juntos forman un grupo espiroalquilo, siempre que al menos un grupo R3 o R4 no sea hidrógeno; y X se selecciona entre hidrógeno, halógeno, ciano, alquilo y alcoxi, que son útiles en el tratamiento y la profilaxis de epilepsia, migraña y otros trastornos.Compounds of formula (I) and their pharmaceutically acceptable salts and solvates are described: (graph), wherein: R1 is hydrogen, C1-C6 alkyl (optionally substituted with hydroxy or C1-C4 alkoxy), phenyl-C1-C4 alkyl , C1-C6 alkenyl, or C1-C6 alkynyl; R2 is hydrogen or up to three substituents selected from halogen, NO2, CN, N3, CF3O-, CF3S, CF3SO2-, CF3CO-, C1-C6 alkyl, C1-C6 alkenyl, C1-C6 alkynyl, perfluoro-C1-C6 alkyl, C3-C6 cycloalkyl, C3-C6 cycloalkyl-C1-C4 alkyl, C1-C6 alkyl-O-, C1-C6 alkyl -CO, C3-C6 cycloalkyl-O-, C3-C6 cycloalkyl -C1-C4-alkyl-O-, C3-C6-cycloalkyl-C1-C4-alkyl-, phenyl, phenoxy, benzyloxy, benzoflo, phenyl-C1-C4-alkyl-, C1-C6-alkyl, C1-C6-alkyl -SO2-, (C1-C4 alkyl) 2 NSO2-, (C1-C4 alkyl) -NHSO2-, (C1-C4 alkyl) 2NCO-, (C1-C4 alkyl) NHCO- or CONH2; or -NR5R6, where R5 is hydrogen or C1-C4 alkyl; and R6 is hydrogen, C1-C4 alkyl, formyl, -CO2-C1-C4 alkyl or -CO-C1-C4 alkyl; or two R2 groups together form a carbocyclic ring that is saturated or unsaturated, optionally interrupted with O or NH; the groups R3 and R4 are independently in each case hydrogen or C1-C6 alkyl and / or the two groups R3 and / or the two groups R4 together form a spiroalkyl group, provided that at least one group R3 or R4 is not hydrogen; and X is selected from hydrogen, halogen, cyano, alkyl, and alkoxy, which are useful in the treatment and prophylaxis of epilepsy, migraine, and other disorders.