Eli Lilly and Company

Avera Pharmaceuticals, Inc.

Daniel Timothy Kohlman

Yao-Chang Xu

Bai-Ping Ying

Sidney Xi Liang

Deyi Zhang

Frantz Victor

Tony Yantao Zhang

Alexander Glenn Godfrey

Michael Philip Cohen

John Cunningham O'Toole

DeAnna Piatt Zacherl

Sandra Ann Filla

Brian Michael Mathes

Maria-Jesus Blanco-Pillado

Kevin John Hudziak

Dana Rae Benesh

Matthew Joseph Fisher

Timothy Paul Burkholder

David T Wong

Joseph P Burkhart

Yanping Xu

Larry W Hertel

Shawn Christopher Miller

Karin Briner

Jeffrey Thomas Mullaney

Vincent Mancuso

William Harlan Gritton

Jeffrey Forrester McKelvy

Deanna Piatt Zacherl

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 1: and pharmaceutically acceptable acid addition sails thereof. The compounds of the present invention are useful for activating 5-HTreceptors, inhibiting neuronal protein extravasation, and for the treatment or preverition of migraine in mammals, particularly humans. 

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: or a pharmaceutically acceptable acid addition salt thereof, where;

A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

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. 

The present invention provides serotonergic aminoalkylbenzofurans of Formula (I): where R, R, R, R, R, R', R, R&#x2032;, and Rare as described in the specification. 

Aminoalkylbenzofurans as serotonin (5-HT(2c)) agonists

Arylpiperazines having activity at the serotonin 1A receptor

The present invention provides compounds of formula (I) and a method of inhibiting the reuptake of serotonin and antagonizing the serotonin receptor which comprises administering to a subject in need of such treatment an effective amount of a compound of formula (I).

Piperidine derivatives as reuptake inhibitors

Piperidine derivatives having effects on serotonin related systems

A series of aryl piperazine compounds are effective pharmaceuticals for the treatment of conditions related to or affected by the serotonin 1 receptor; the compounds are particularly effective antagonists at that receptor, and are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal.

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Camby, IN, United States of America

Daniel Timothy Kohlman