申请人:Eli Lilly and Company
公开号:US07423050B2
公开(公告)日:2008-09-09
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.
本发明涉及以下式子的化合物:或其药学上可接受的酸盐,其中;R1是C1-C6烷基,取代的C1-C6烷基,C3-C7环烷基,取代的C3-C7环烷基,C3-C7环烷基-C1-C3烷基,取代的C3-C7环烷基-C1-C3烷基,苯基,取代的苯基,杂环或取代的杂环;R2是氢,C1-C3烷基,C3-C6环烷基-C1-C3烷基或式子II的基团;R3是氢或C1-C3烷基;R4是氢,卤素或C1-C3烷基;R5是氢或C1-C3烷基;R6是氢或C1-C6烷基;n是1到6的整数。本发明的化合物对于激活5-HT1F受体,抑制神经元蛋白外渗以及治疗或预防哺乳动物偏头痛有用。本发明还涉及一种合成式I化合物中间体的合成方法。