John Wyeth Brother, Limited

Anderson D Ifill

Ian A Cliffe

Alan C White

Terence J Ward

Howard L Mansell

Amide derivatives as 5-HT.sub.1A ligands

4-amino-2-(hetero)aryl-butanamides useful as 5-HT.sub.1A -antagonists

Piperazine derivatives of formula I ##STR1## and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents, particularly 5-HT.sub.1A antagonists and may be used, for example, as anxiolytics. In the formula R is hydrogen or one or two lower alkyl groups, R.sup.1 is a mono of bicyclic aryl or heteroaryl radical, R.sup.2 is aryl and A is a C.sub.2-5 alkylene chain optionally substituted by lower alkyl.

Piperazine derivatives

##STR1## where A is an alkylene chain of 1 or 2 carbon atoms optionally substituted by one or more lower alkyl groups, R is hydrogen or lower alkyl, R.sup.1 is a mono or bicyclic aryl or a heteroaryl radical, R.sup.2 is an aryl radical, a heteroaryl radical, or an aryl-or heteroaryl-lower alkyl radical, R.sup.3 is hydrogen, lower alkyl or aryl and R.sup.4 is hydrogen, lower alkyl, cycloalkyl, cycloalkyl(lower)alkyl, aryl, or aryl(lower)alkyl or R.sup.3 and R.sup.4 together with the nitrogen atom to which they are both attached represent a saturated heterocyclic ring which may contain a further hetero atom and the dotted line represents a single or double bond, the hydrogen atoms shown in brackets being present when the dotted line represents a single bond and their pharmaceutically acceptable acid addition salts are 5-HT.sub.1A binding agents which may be used, for example, for the treatment of CNS disorders such as anxiety.

Growing community of inventors

Didcot, United Kingdom

Anderson D Ifill