Eli Lilly and Company

DeAnna Piatt Zacherl

Yao-Chang Xu

Daniel Timothy Kohlman

Frantz Victor

Bai-Ping Ying

Michael Philip Cohen

Deyi Zhang

Sidney Xi Liang

Sandra Ann Filla

Brian Michael Mathes

Maria-Jesus Blanco-Pillado

Vincent Mancuso

Kevin John Hudziak

Dana Rae Benesh

The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where;  The compounds of the present invention are useful for activating 5-HTreceptors, 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.

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The present invention relates to compounds of formula I: or pharmaceutically acceptable acid addition salts thereof, where; Ris C-Calkyl, substituted C-Calkyl, C-Ccycloalkyl, substituted C-Ccycloalkyl, C-Ccycloalkyl-C-Calkyl, substituted C-Ccycloalkyl-C-Calkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; Ris hydrogen, C-Calkyl, C-Ccycloalkyl-C-Calkyl, or a group of formula II  Ris hydrogen or C-Calkyl; Ris hydrogen, halo, or C-Calkyl; Ris hydrogen or C-Calkyl; Ris hydrogen or C-Calkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HTreceptors, 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.

The present invention relates to compounds of formula I: (I) or a pharmaceutically acceptable acid addition salt thereof, where; X is C(R&#x2550; or N&#x2550;; Ris C&#x2013;Calkyl, substituted C&#x2013;Calkyl, C&#x2013;Ccycloalkyl, substituted C&#x2013;Ccycloalkyl, phenyl, substituted phenyl, heterocycle, or substituted heterocycle; Ris hydrogen, C&#x2013;Cn-alkyl, C&#x2013;Ccycloalkyl-C&#x2013;Calkyl, or a group of formula II (II) provided that when Ris C&#x2013;Calkyl or substituted C&#x2013;Calkyl, Ris hydrogen or methyl; R, R, and, when X is C(R)&#x2550;, R, are each independently hydrogen, fluoro, or methyl, provided that no more than one of R, R, and Rmay be other than hydrogen; Ris hydrogen or C&#x2013;Calkyl; Ris hydrogen, C&#x2013;Calkyl, or C&#x2013;Ccycloalkylcarbonyl, provided that when Ris other than hydrogen, Ris hydrogen; Ris hydrogen or C&#x2013;Calkyl; and n is an integer from 1 to 6 inclusively. The compounds of the present invention are useful for activating 5-HTreceptors, inhibiting neuronal protein extravasation, and for the treatment or prevention of migraine in a mammal. 

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Noblesville, IN, United States of America

DeAnna Piatt Zacherl