Glaxo Laboratories Limited

Smithkline Beecham Corporation

Glaxo Group Limited

Richard J Coles

Alan D Borthwick

Gerard Martin Paul Giblin

Mark James Bamford

Peter C Cherry

Nicholas Maughan Clayton

Steven Michael Foord

John Kitchin

Adrian J Pipe

Susanne Denise Collins

Derek Burn

Jennifer M Doughty

The present invention relates to the use of an EP4 receptor ligand in the manufacture of a medicament for use in the treatment of neuropathic pain, colon cancer, migraine, and for increasing the latency of HIV infection.

Use of EP4 receptor ligands in the treatment of neuropathic pain and colon cancer

Compounds of the general formula (I) ##STR1## (wherein R is H, alkyl, alkenyl, alkynyl, cycloalkyl, aralkyl or CHO; and R.sup.1 and R.sup.2 each represents H, fluorine or chlorine); and their salts have selective .alpha..sub.2 -adrenoreceptor antagonist action. The compounds may be prepared by amination of compounds of the general formula (II): ##STR2## (wherein X is a leaving group).

Heterocyclic amino compounds

Compounds of the general formula: ##STR1## in which A is a benzene ring or a carbocyclic aromatic group consisting of two or three fused benzene rings, the group A being linked to the nitrogen containing ring at two adjacent carbon atoms and the benzene ring or each benzene ring optionally carrying one or more substituents which may be the same or different, and may be alkyl, aryl, halo, hydroxy, acyloxy or alkoxy, or two adjacent positions in a ring may be substituted so as to form a methylene dioxy group (--O--CH.sub.2 --O--);

N-Cyclopropylisoindolines

Compounds of the general formula: ##STR1## wherein the groups CHR.sup.1 NR.sup.2 R.sup.3 and CHR.sup.4 NR.sup.5 R.sup.6 may be the same or different and where the group CHR.sup.4 NR.sup.5 R.sup.6 is in either the 1 or the 3 position and R.sup.1 and R.sup.4 independently represent a hydrogen atom or an aryl group; R.sup.2, r.sup.3, r.sup.5 and R.sup.6 which may be the same or different are each a hydrogen atom or an alkyl group or an aryl group both of which may in turn be substituted by one or more hydroxy, alkoxy, acyloxy, dialkylamino or aryl groups or the groups --NR.sup.2 R.sup.3 and/or NR.sup.5 R.sup.6 represent a heterocyclic ring containing one or more hetero atoms and which ring may optionally be substituted by an alkyl, aryl or aralkyl group and in which either aromatic ring of the naphthalene nucleus may be further substituted; with the proviso that when R.sup.1, R.sup.4, R.sup.2 and R.sup.5 are hydrogen, then R.sup.3 and R.sup.6 cannot both be benzyl, when the second substituent is in the 1 position; and when R.sup.1 and R.sup.4 are hydrogen, then R.sup.2, R.sup.3, R.sup.5 and R.sup.6 cannot all be methyl when the second substituent is in the 1 position; and when R.sup.1 and R.sup.4 are hydrogen, then R.sup.2 and R.sup.3 and R.sup.5 and R.sup.6 together with the nitrogen atom cannot both be piperidino when the second substituent is in the 3 position and the naphthalene nucleus is further substituted by hydroxy in the 1 and 4 positions; and pharmaceutically acceptable salts of such compounds; and hydrates of such compounds and such salts. The compounds have activity on the central nervous system in particular as analgesics.

Analgesic basic naphthalene derivatives

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Uxbridge, United Kingdom

Richard J Coles