Eli Lilly and Company

Lilly Industries, Inc.

John Richard Harris

Barry P Clark

Peter Thaddeus Gallagher

Stephen Richard Baker

Maria Ann Whatton

Jeremy Gilmore

John Goldsworthy

Ann Elizabeth Kingston

Mark A Finch

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

 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

A compound having pharmaceutical activity, of the formula ##STR1## in which A is hydrogen or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x is 0 or 1 to 4, R.sup.1 and R.sup.2 are each hydrogen or C.sub.1-4 alkyl and R.sup.3 is --CN, --COOH, tetrazolyl or --CONHSO.sub.2 R.sup.4 where R.sup.4 is optionally substituted phenyl, and ##STR2## where R.sup.5 and R.sup.6 are each hydrogen, C.sub.1-4 alkyl or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x, R.sup.1, R.sup.2 and R.sup.3 are as defined above, and R.sup.7 is hydrogen, C.sub.1-4 alkyl or --(CR.sup.1 R.sup.2).sub.x R.sup.3 where x is 1 to 4, and R.sup.1, R.sup.2 and R.sup.3 are as defined above;

Pharmaceutical compounds

Compounds are described of the following formula ##STR1## in which R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-12 alkyl or C.sub.2-12 alkenyl, at least one of R.sup.1 and R.sup.2 being C.sub.1-12 alkyl or C.sub.2-12 alkenyl; X.sup.1 and X.sup.2 are each hydrogen or a protecting group; and Y is

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Guildford, United Kingdom

John Richard Harris