摘要:
The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein X is C(R3c)═ or N═; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b and, when X is —C(R3c)═, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要:
The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R3c═ or N═; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II (II) provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b, and, when X is C(R3c)═, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要:
The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.
摘要:
The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl; R4 is hydrogen, halo, or C1-C3 alkyl; R5 is hydrogen or C1-C3 alkyl; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.
摘要:
The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, wherein X is C(R3c)═ or N═; R1 is C2-C6 alkyl, substituted C2-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1-C3 n-alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II provided that when R1 is C2-C6 alkyl or substituted C2-C6 alkyl, R2 is hydrogen or methyl; R3a, R3b and, when X is —C(R3c)═, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1-C3 alkyl; R5 is hydrogen, C1-C3 alkyl, or C3-C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1-C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要:
The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R3c═ or N═; R1 is C2–C6 alkyl, substituted C2–C6 alkyl, C3–C7 cycloalkyl, substituted C3–C7 cycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R2 is hydrogen, C1–C3 n-alkyl, C3–C6 cycloalkyl-C1–C3 alkyl, or a group of formula II (II) provided that when R1 is C2–C6 alkyl or substituted C2–C6 alkyl, R2 is hydrogen or methyl; R3a, R3b, and, when X is C(R3c)═, R3c, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R3a, R3b, and R3c may be other than hydrogen; R4 is hydrogen or C1–C3 alkyl; R5 is hydrogen, C1–C3 alkyl, or C3–C6 cycloalkylcarbonyl, provided that when R3a is other than hydrogen, R5 is hydrogen; R6 is hydrogen or C1–C6 alkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要:
The present invention relates to compounds of formula 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans.
摘要:
The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, where; X is —C(R4)═ or —N═; Ar is phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R1 and R2 are independently hydrogen or C1-C3 alkyl; R3 is hydrogen, fluoro, or methyl; when X is —C(R4)═, R4 is hydrogen, fluoro, or methyl, provided that no more than one of R3 and R4 may be other than hydrogen; and R5 is hydrogen, methyl, or ethyl. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting dural protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要翻译:本发明涉及式I化合物或其药学上可接受的酸加成盐,其中: X是-C(R 4) - 或-N-; Ar是苯基,取代的苯基,杂环或取代的杂环; R 1和R 2独立地是氢或C 1 -C 3烷基; R 3是氢,氟或甲基; 当X是-C(R 4) - )时,R 4是氢,氟或甲基,条件是R 3不超过一个 >和R 4可以不同于氢; R 5是氢,甲基或乙基。 本发明的化合物可用于活化5-HT 1F受体,抑制硬脑膜蛋白质外渗,以及治疗或预防哺乳动物偏头痛。
摘要:
The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; R1 is C1-C6 alkyl, substituted C1-C6 alkyl, C3-C7 cycloalkyl, substituted C3-C7 cycloalkyl, C3-C7 cycloalkyl-C1-C3 alkyl, substituted C3-C7 cycloalkyl-C1-C3 alkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle;R2 is hydrogen, C1-C3 alkyl, C3-C6 cycloalkyl-C1-C3 alkyl, or a group of formula II R3 is hydrogen or C1-C3 alkyl;R4 is hydrogen, halo, or C1-C3 alkyl;R5 is hydrogen or C1-C3 alkyl;R6 is hydrogen or C1-C6 alkyl; andn is an integer from 1 to 6 inclusively.The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. The present invention also relates to a process for the synthesis of intermediates in the synthesis of compounds of Formula I.
摘要:
The present invention relates to compounds of formula I: or a pharmaceutically acceptable acid addition salt thereof, where; X is —C(R4)═ or —N═; Ar is phenyl, substituted phenyl, heterocycle, or substituted heterocycle; R1 and R2 are independently hydrogen or C1-C3 alkyl; R3 is hydrogen, fluoro, or methyl; when X is —C(R4)═,R4 is hydrogen, fluoro, or methyl, provided that no more than one of R3and R4 may be other than hydrogen; and R5 is hydrogen, methyl, or ethyl. The compounds of the present invention are useful for activating 5-HT1F receptors, inhibiting dural protein extravasation, and for the treatment or prevention of migraine in a mammal.
摘要翻译:本发明涉及式I化合物或其药学上可接受的酸加成盐,其中: X是-C(R 4) - 或-N-; Ar是苯基,取代的苯基,杂环或取代的杂环; R 1和R 2独立地是氢或C 1 -C 3烷基; R 3是氢,氟或甲基; 当X是-C(R 4) - )时,R 4是氢,氟或甲基,条件是R 3不超过一个 >和R 4可以不同于氢; R 5是氢,甲基或乙基。 本发明的化合物可用于活化5-HT 1F受体,抑制硬脑膜蛋白质外渗,以及治疗或预防哺乳动物偏头痛。