Eli Lilly and Company

Richard Edmund Rathmell

Peter Thaddeus Gallagher

John Joseph Masters

Sandra Ann Filla

Brian Michael Mathes

Serge Louis Boulet

Kevin John Hudziak

Victor Giulio Matassa

Anette Margareta Johansson

Rushad Eruch Karanjawala

Chad Nolan Wolfe

Andrew Caerwyn Williams

Maria Ann Whatton

Maria Angeles Martinez-Grau

Michael Philip Mazanetz

Manuel Javier Cases-Thomas

Selma Sapmaz

John Gordon Allen

Christopher Stanley Galka

Karin Briner

Natalia Pokrovskaia

Roger Ryan Rothhaar

Nicolas Jacques Francois Dreyfus

Richard C Hoying

Matthew Robert Reinhard

Anne Marie Camp

John Cunningham O'Toole

Alicia Marcos Llorente

Peter James Lindsay-Scott

Maria Ann Fagan

Maria Ann (nee Fagan) Whatton

Karen Briner

Marta Adeva Bartolome

The present invention provides a compound of Formula I: or a pharmaceutically acceptable salt thereof, and the use of compounds of Formula I for treatment of neurodegenerative diseases and disorders, such as Alzheimer's disease.

5-methyl-1,3,4-oxadiazol-2-yl compounds

The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula (I) as selective 5-HT2c receptor agonists for the treatment of 5-HT2c associated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety, where, R6 is &#x2014;NR10R11, where R10 is substituted phenylalkyl or substituted pyridylalkyl and other substituents are as defined in the specification. 

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The present invention provides 6-substituted 2,3,4,5-tetrahydro-1H-benzo[d]azepines of Formula (I) as selective 5-HTreceptor agonists for the treatment of 5-HTassociated disorders including obesity, obsessive/compulsive disorder, depression, and anxiety: where Ris &#x2014;C&#x2261;C&#x2014;R, &#x2014;CH&#x2550;CRR, or &#x2014;(C-C)alkyl-Aroptionally substituted on the alkyl moiety with 1 to 6 fluoro substituents and other substituents are as defined in the specification. 

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

There is provided a heretoaryloxy 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 selected from halo, C&#x2013;Calkyl and C&#x2013;Calkoxy, and thienyl optionally substituted with up to 3 substituents selected from halo and C&#x2013;Calkyl; Y is selected from benzothienyl, indolyl and benzofuranyl, optionally substituted with up to 5 substituents selected from halo, C&#x2013;Calkyl, C&#x2013;Calkoxy, nitro, acetyl and cyano; and when Y is indolyl it may be substituted or further substituted by an N-substituent selected from C&#x2013;Calkyl; Rand Rare each independently H or C&#x2013;Calkyl; and pharmaceutically acceptable salts thereof.

Heteroaryloxy 3-substituted propanamines as serotonin and norepinephrine reuptake inhibitors

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Basingstoke, United Kingdom

Richard Edmund Rathmell