Eli Lilly and Company

Lilly Industries, Inc.

Peter Thaddeus Gallagher

William M Owton

Colin W Smith

Barry P Clark

Maria Ann Whatton

John Joseph Masters

Sandra Ann Filla

Terence Alan Hicks

Colin P Dell

John Fairhurst

Michael Brunavs

Martin Victor Miles

Serge Louis Boulet

Richard Edmund Rathmell

Anette Margareta Johansson

Brian Michael Mathes

Jeremy Gilmore

Magnus Wilhelm Walter

Kevin John Hudziak

Victor Giulio Matassa

Rushad Eruch Karanjawala

Virginia Ann Wood

Chad Nolan Wolfe

Andrew Caerwyn Williams

Manuel Javier Cases-Thomas

Anne Marie Camp

Christopher David Beadle

Graham Henry Timms

Helen Louise Haughton

Valentina O Badescu

John M Schaus

David Andrew Coates

Jai P Singh

Patrick Gianpietro Spinazze

John Richard Harris

Michael Philip Cohen

Michael Philip Mazanetz

Carlos Lamas-Peteira

Francisco Javier Agejas-Chicharro

Adam Jan Sanderson

Marta Maria Pineiro-Nunez

Sarah Lynne Hellman

Andrew James Ledgard

Hélène Catherine Eugénie Rudyk

Maria Ann Fagan

Graham W Mullier

David R Dobson

Maria Ann (nee Fagan) Whatton

John Mehnert Schaus

Barry Peter Clark

A dual H1 inverse agonist/5-HTreceptor antagonist of the formula: its uses, and methods for its preparation are described.

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A dual H1/5-HTreceptor antagonist of the formula: its uses, and methods for its preparation are described.

The present invention provides selective 5-HT7 receptor antagonist compounds of Formula I and their use in the treatment of migraine, persistent pain, and anxiety: where A and B are each independently &#x2014;C(H)&#x2550; or &#x2014;N&#x2550;, provided that at least one of A and B is &#x2014;N&#x2550;, n is 1-3, m is 0-3, and R1-4 are as defined herein.

2-[4-(pyrazol-4-ylalkyl)piperazin-1-yl]-3-phenyl pyrazines as 5-HT7 receptor antagonists

The present invention provides selective 5-HTreceptor antagonist compounds of Formula I and their use in the treatment of migraine: where A is &#x2014;C(H)&#x2550; or &#x2014;N&#x2550; and Rare as defined herein.

5-HT7 receptor antagonists

The present invention provides compounds of formula (I) and pharmaceutically acceptable salts thereof, which are useful for the inhibition of the uptake of one or more physiologically active monoamines (serotonin, norepinephrine, and dopamine).

3-Aminopyrrolidines as inhibitors of monoamine uptake

The present invention provides compounds of formula (I) wherein A is (1), (2), (3), (4), (5), (6) or (7) and wherein R1, R7, y and Arare defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system.

Aminomethyl-azacycle derivatives as inhibitors of monoamine uptake

Compounds of the general formula (I) are inhibitors of the reuptake of norepinephrine. As such, they may be useful for the treatment of disorders of the central and/or peripheral nervous system.

Morpholine derivatives as norepinephrine reuptake inhibitors

The present invention provides compounds of formula (I) where n, R1, R2, R3, R4, R5 and Heteroaryl are defined herein. The compounds are inhibitors of the uptake of one or more monoamines selected from serotonin, norepinephrine and dopamine and, as such, may be useful in the treatment of disorders of the central and/or peripheral nervous system. 

4-Amino-piperidine derivatives as monoamine uptake inhibitors

The invention relates to compounds of formula (I): 

Pyridinylmorpholine derivatives

3-aminopiperidines and 3-aminoquinuclidines as inhibitors of monoamine uptake

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

2-(phenoxymethyl)-and 2-(phenylthiomethyl)-morpholine derivatives for use as selective norepinephrine reuptake inhibitors

A compound of formula (I) (I) wherein R is H; Ar is an aromatic group selected from phenyl; X is a phenyl group; R' is H or C1-C4 alkyl; each R1 is independently H or C1-C4 alkyl; and pharmaceutically acceptable salts thereof 

Benzyl morpholine derivatives

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Basingstoke, United Kingdom

Peter Thaddeus Gallagher