Eli Lilly and Company

Lilly Industries, Inc.

Barry P Clark

Peter Thaddeus Gallagher

John Richard Harris

Maria Ann Whatton

William J Ross

Alec Todd

David Edward Tupper

Magnus Wilhelm Walter

Christopher David Beadle

Virginia Ann Wood

John Joseph Masters

Stephen Richard Baker

Jeremy Gilmore

Manuel Javier Cases-Thomas

Graham H Timms

Graham Henry Timms

Helen Louise Haughton

John M Schaus

James Allen Monn

Sandra Ann Filla

Patrick Gianpietro Spinazze

Serge Louis Boulet

Michael Philip Cohen

John Fairhurst

Michael Philip Mazanetz

John Goldsworthy

Anette Margareta Johansson

Lourdes Prieto

Marta Maria Pineiro-Nunez

Anne Marie Camp

Hélène Catherine Eugénie Rudyk

Sarah Lynne Hellman

Valentina O Badescu

Ann Elizabeth Kingston

The present invention provides novel mGlu2/3 agonists of the formula wherein R, R, and Rare as defined herein, for use in the treatment of neurological or psychiatric disorders.

MGlu 2/3 agonists

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 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

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

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

 Use of a compound of formula (I) in which, R , R and R are independently hydrogen, (C -C )alkyl, (C -C )alkenyl, C -C )cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted aryl(C -C )alkyl, unsubstituted or substituted aryl(C -C )alkenyl, halo, carboxy, (C -C )alkoxycarbonyl or &mdash;(CH ) &mdash;OH wherein m is 1, 2 or 3; - - - indicates a single or a double bond; X and each independently hydrogen, or X and Y together represent a bridge of the formula &mdash;CH ) &mdash;, where n is 1 or 2; A and A are each independently an unsubstituted or substituted aryl; Z is &mdash;CO&mdash;, &mdash;SO &mdash; or &mdash;CH ; provided that, when Z is &mdash;CO&mdash;, A is not 3,4,5-trimethoxyphenyl; or a pharmaceutically-acceptable salt or ester thereof, for the manufacture of a medicament for the treatment of a condition indicating the administration of a selective mGluR1 antagonist.

Use of n-substituted (3,6-dihydro)-2h-1,2-oxazine derivatives as selective mglur1 antagonists

Compounds of the formula ##STR1## in which R.sup.1 is Y or Y--C.sub.1-6 alkyl, where Y is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or optionally substituted phenyl-C.sub.1-6 alkyl,

2-amino-2-(3-substituted cyclobutyl) acetic acid derivatives

A pharmaceutical compound of the formula: ##STR1## in which A is carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OPO(OH)OR'

Pharmaceutical xanthene compounds

A pharmaceutical compound of the formula: ##STR1## in which R.sup.1 is hydrogen, hydroxy or C.sub.1-6 alkoxy, R.sup.2 is hydrogen, carboxy, tetrazolyl, --SO.sub.2 H, --SO.sub.3 H, --OSO.sub.3 H, --CONHOH, or --P(OH)OR', --PO(OH)OR', --OP(OH)OR' or --OPO(OH)OR' where R' is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or aryl C.sub.1-6 alkyl,

Phenylglycine derivatives useful for treating disorders of the central

A compound of the formula: ##STR1## in which each R.sup.1 to R.sup.4 group is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxy-carbonyl, halo, hydroxy, nitro, cyano, trihalomethyl or optionally substituted phenyl, each R.sup.5 to R.sup.16 group is hydrogen or C.sub.1-4 alkyl, each Z', Z', Z'' and Z'' group is an alkylene radical, and X and Y are each --(CH.sub.2).sub.n -- or --(CH.sub.2).sub.m --A--(CH.sub.2).sub.p -- where A is --CH.dbd.CH--, optionally substituted phenylene or optionally substituted naphthalenyl, n is 2 to 10, and m and p are each 1 or 2, salts thereof, and intermediates for the production thereof.

Macrocyclic compounds

Compounds

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Lower Froyle, United Kingdom

Barry P Clark