Eli Lilly and Company

Brian Michael Mathes

Sandra Ann Filla

Kevin John Hudziak

John Joseph Masters

Peter Thaddeus Gallagher

Brian Morgan Watson

Serge Louis Boulet

Richard Edmund Rathmell

Anette Margareta Johansson

Victor Giulio Matassa

Rushad Eruch Karanjawala

Chad Nolan Wolfe

Leonard Larry Winneroski, Jr

Warren Jaye Porter

Yao-Chang Xu

Daniel Timothy Kohlman

Jose Eduardo Lopez

James Peter Beck

Bai-Ping Ying

Dustin James Mergott

Steven James Green

Maria Ann Whatton

Maria-Jesus Blanco-Pillado

Deyi Zhang

Zoran Rankovic

Dana Rae Benesh

Yuan Shi

John M Schaus

Michael Robert Wiley

Paul Leslie Ornstein

Vincent Patrick Rocco

Larry C Blaszczak

Qing Shi

Frantz Victor

Scott Martin Sheehan

Michael Philip Cohen

Daniel James Koch

Michael Alan Robertson

Shon Roland Pulley

DeAnna Piatt Zacherl

Maria Ann (nee Fagan) Whatton

Jr Leonard Larry Winneroski

The present invention provides compounds of Formula I: wherein A is selected from the group consisting of; Ris H or F;Ris H, &#x2014;CHOH, C1-C3 alkyl, Ris H, F, or CN;Ris H, F; or CN; andRis H, &#x2014;CH, or &#x2014;OCH;or a pharmaceutically acceptable salt thereof.

Tetrahydropyrrolothiazine compounds

The present invention provides compounds of Formula I: wherein A is selected from the group consisting of;  

The present invention is directed to compounds of formula (I) or a pharmaceutically acceptable salt thereof; wherein A is (1); X is selected from CH, CF and N; R5 is selected from H, C-Calkyl, C-Cfluoroalkyl, and &#x2014;OR12; R9 is selected from H &#x2014;NR13C(O)R14 and &#x2014;C(O)NR10R11; R12 is selected from H, C-Calkyl and C-Ccycloalkyl, for use as inhibitors of the DPP-IV enzyme in the treatment or prevention of conditions including Type II diabetes. 

Pyridine derivatives as dipeptedyl peptidase inhibitors

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. 

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There is provided a compound of formula (I) wherein A is selected from &#x2014;O&#x2014; and &#x2014;S&#x2014;; X is selected from C-Calkyl, C-Calkenyl, C-Ccycloalkyl and C-Ccycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, &#x2014;CF, &#x2014;CN and &#x2014;CONH; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, 5 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, nitro, acetyl, &#x2014;CF, &#x2014;SCFand cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C-Calkyl; Z is selected from H, ORor F, wherein Ris selected from H, C-Calkyl and phenyl C-Calkyl; Rand Rare each independently H or C-Calkyl; with the proviso that, when Z is H, then Y may not be optionally substituted phenyl or optionally substituted naphthyl. 

3-aryloxy/thio-3-substituted propanamines and their use in inhibiting serotonin and norepinephrine reuptake

There is provided a compound of formula (I) wherein A is selected from &#x2014;O&#x2014; and &#x2014;S&#x2014;; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C-Calkyl and C-Calkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C-Calkyl, and C-Calkyl, C-Calkenyl, C-Ccycloalkyl and C-Ccycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, &#x2014;CF, &#x2014;CN and &#x2014;CONH; Y is selected from phenyl, naphthyl, dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, thienopyridyl, indanyl, 1,3-benzodioxolyl, benzothienyl, indolyl and benzofuranyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, nitro, acetyl, &#x2014;CF, &#x2014;SCFand cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C-Calkyl; Z is selected from ORor F, wherein Ris selected from H, C-Calkyl and phenyl C-Calkyl; Rand Rare each independently H or C-Calkyl; and pharmaceutically acceptable salts thereof with the proviso that when Y is optionally substituted phenyl or optionally substituted 1,3-benzodioxolyl and Z is ORand X is optionally substituted phenyl then A is &#x2014;S&#x2014;. 

3-aryloxy/thio-2,3-substituted propanamines and their use in inhibiting serotonin and norepinephrine reuptake

There is provided a heretoaryloxy/thio 3-substituted propanamine compound of formula (I) wherein A is selected from &#x2014;O&#x2014; and &#x2014;S&#x2014;; X is selected from phenyl optionally substituted with up to 5 substituents each independently selected from halo, C-Calkyl and C-Calkoxy, thienyl optionally substituted with up to 3 substituents each independently selected from halo and C-Calkyl, and C-Calkyl, C-Calkenyl, C-Ccycloalkyl and C-Ccycloalkylalkyl, each of which may be optionally substituted with up to 3 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl &#x2014;S(O)&#x2014; where n is 0, 1 or 2, &#x2014;CF, &#x2014;CN and &#x2014;CONH; Y is selected from dihydrobenzothienyl, benzothiazolyl, benzoisothiazolyl, quinolyl, isoquinolyl, naphthyridyl, and thienopyridyl, each of which may be optionally substituted with up to 4 or, where possible, up to 5 substituents each independently selected from halo, C-Calkyl, C-Calkoxy, C-Calkyl-S(O)&#x2014; where n is 0, 1 or 2, nitro acetyl, &#x2014;CF, &#x2014;SCFand cyano; Z is selected from H, ORor F, wherein Ris selected from H, C-Calkyl and phenyl CCalkyl; Rand Rare each independently H or C-Calkyl; and pharmaceutically acceptable salts thereof. 

Propanamine derivatives as serotonin and norepinephrine reuptake inhibitors

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 novel compounds of Formula I or Formula II, or the pharmaceutically acceptable salts or prodrugs thereof, pharmaceutical compositions comprising an effective amount of a compound of Formula I or Formula II in combination with a suitable carrier, diluent, or excipient, and methods for treating neurological disorders and neurodegenerative diseases, particularly pain and migraine.

Excitatory amino acid receptor antagonists

5-HT1F agonists

The present invention relates to a compound of formula (I): or a pharmaceutical acid addition salt thereof; which is useful for activating 5-HT receptors and inhibiting protein extravasation in a mammal.

This invention provides 5-HT.sub.1F agonists of Formula: ##STR1## where A-B, X, and R are as defined in the specification. The invention also encompasses pharmaceutical formulations employing the compounds or the invention as well as methods of treating conditions associated with 5-HT.sub.1F activation employing these compounds or compositions.

5-HT.sub.IF -agonists effective in treating migraine

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Indianapolis, IN, United States of America

Brian Michael Mathes