Eli Lilly and Company

Lilly Industries, Inc.

John Fairhurst

Peter Thaddeus Gallagher

David Edward Tupper

Martin Victor Miles

Colin W Smith

William M Owton

David T Wong

Terrence M Hotten

Barry P Clark

Serge Louis Boulet

Maria Ann Whatton

Anette Margareta Johansson

Virginia Ann Wood

Barry Peter Clark

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

A pharmaceutical compound of the formula (I) in which Rand Rare each hydrogen or Calkyl, Ris &#x2014;SR, &#x2014;SOR, &#x2014;SOR, &#x2014;COR, &#x2014;CHOH or &#x2014;CONHR, where Ris Calkyl and Ris hydrogen or Calkyl, R, R, Rand Rare each hydrogen or Calkyl, provided that at least one of R, R, Rand Ris Calkyl, Rand Rare each hydrogen, halo, Calkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein Rand Rare each hydrogen, Calkyl, cyclopropyl or cyclopropyl-Calkyl; and salts thereof.

Piperidyindoles as serotonin receptor ligands

Pharmaceutical compounds

Pharmaceutical compounds of the formula: ##STR1## in which n is 1 to 6, m is 1 or 2 and p is 1 or 2, R.sup.1 and R.sup.2 are each hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, HO--C.sub.1-4 alkyl, C.sub.1-4 alkoxy-C.sub.1-4 alkyl, C.sub.1-4 alkylthio, halo, optionally substituted phenyl, optionally substituted phenyl-C.sub.1-4 alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form a C.sub.3-6 cycloalkyl group, &gt;C.dbd.O, C.dbd.NOR' where R' is hydrogen or C.sub.1-4 alkyl, R.sup.3, R.sup.4 and R.sup.5 are each hydrogen, halo, nitro, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkyl-CO--, where m is 0, 1 or 2, R'R'N--SO.sub.2 --, --COOR', --CONR'R', --NR'R', --N(OR')COOR', --COR', --NHSO.sub.2 R', where R' and R' are each hydrogen or C.sub.1-4 alkyl, R.sup.6 and R.sup.7 are each hydrogen or C.sub.1-4 alkyl, X is oxygen or sulphur, the dotted line represents an optional double bond, and the fluorine atom is attached at the 6- or 7-position; and salts thereof.

Indole compounds

Pharmaceutical compounds of the formula ##STR1## in which R.sup.1 is hydrogen or halo, and R.sup.2 is C.sub.1-10 alkyl, C.sub.2-10 alkenyl, C.sub.2-10 alkynyl, C.sub.3-6 cycloalkyl optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, C.sub.3-6 cycloalkyl-C.sub.1-4 alkyl in which the cycloalkyl group is optionally substituted by 1 to 3 C.sub.1-4 alkyl groups, or optionally substituted phenyl-C.sub.1-4 alkyl; or a salt thereof. Such compounds are useful for treating a disorder of the central nervous system which is associated with the modulation of a 5-HT.sub.3 receptor.

Thienobenzodiazepine compounds

A pharmaceutical compound having the formula: ##STR1## in which n is 1 or 2, m is 1 or 2, p is 1 to 6, q is 0 or 1 to 3,

1H-2,1,3-benzothiadiazine-2,2-dioxide compounds or derivatives thereof

Pharmaceutical compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkylthio, halogen, nitro or --NR'R' where R' and R' are each hydrogen or C.sub.1-4 alkyl, R.sup.4 and R.sup.5 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.6 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1-4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof.

Naphthalene carboxamides

Compounds of the formula: ##STR1## in which each R.sup.1 is hydrogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, halogen or nitro, and n is 0, 1, 2 or 3, R.sup.2 is hydrogen, C.sub.1-4 alkyl or C.sub.2-4 alkenyl, R.sup.3 and R.sup.4 are each hydrogen, C.sub.1-4 alkyl, optionally substituted phenyl or C.sub.6-9 cycloalkyl optionally substituted by 1 to 4 C.sub.1-4 alkyl groups, R.sup.5 is optionally substituted phenyl, tetrahydronaphthyl, phthalimido, saccharinyl, glutaramido, C.sub.6-10 cycloalkyl optionally substituted with 1 to 4 C.sub.1-4 alkyl groups or a phenyl group, or C.sub.4-9 heterosubstituted cycloalkyl optionally substituted with 1 to 4 alkyl groups, x is 1, 2 or 3, y is 0 or 1 and z is 0, 1, 2 or 3; and salts thereof. The compounds are indicated for use in the treatment of disorders of the central nervous system.

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Basingstoke, United Kingdom

John Fairhurst