abstract |
"COMPOUND, PHARMACEUTICAL COMPOSITION, METHODS TO ACTIVATE 5-HT ~ 1F ~ RECEIVERS IN A MAMMER, TO INHIBIT NEURONAL PROTEIN EXTRAVASION AND TO TREAT OR PREVENT HAZARD IN A MAMMETER," AND, USE. The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein; X is C (R¬3c¬ = or N =; R¬1¬ is C1 -C2 alkyl, substituted C1 -C6 alkyl, C3 -C7 cycloalkyl -, substituted C 3 -C 7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle R 2 is hydrogen, C 1 -C 3 n-alkyl, C 3 cycloalkyl -C ~ 6 -C 1-1 -C 1-6 alkyl, or a group of formula II provided that when R 1 'is C 2-6 alkyl or C 2-6 alkyl 6 ~ substituted R¬ 2¬ is hydrogen or methyl; R¬ 3a¬, R¬ 3b¬, and when X is C (R¬ 3c¬) =, R¬ 3c¬ are each independently hydrogen, fluorine, or methyl, provided that no more than one of R¬ 3a¬, R¬ 3b¬, and R¬ 3c¬ may be other than hydrogen; R¬ 4¬ is hydrogen or C ~ 1 -CC ~ 3 ~ alkyl. R¬ 5¬ is hydrogen, C ~ 1 1C alqu 3 ~ alkyl, or C ~ 3 ~ ~ ciclo ciclo ciclo cycloalkylcarbonyl, provided that when R¬¬a is other than hydrogen, R¬5¬ is hydrogen R 6 is hydrogen or C 1 -C 6 alkyl and n is an integer from 1 to 6 inclusive. The compounds of the present invention are useful for activating 5-HT-1F-receptors, inhibiting neuronal protein leakage, and for treating or preventing migraine in a mammal. |