John Wyeth Brother, Limited

American Home Products Corporation

Howard L Mansell

Ian A Cliffe

Alan C White

Terence J Ward

Richard S Todd

James Albert Nelson

Uresh Shantilal Shah

Christopher Ian Brightwell

Anderson D Ifill

Mira A Kanzelberger

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 A is C.sub.2-4 alkylene chain optionally substituted by lower alkyl, Z is oxygen or sulphur, R is hydrogen or lower alkyl, R.sup.1 is a mono or bicyclic aryl or heteroaryl radical, R.sup.2 is a mono or bicyclic heteroaryl radical and R.sup.3 is hydrogen or a specified radical such as lower alkyl, cycloalkyl, aryl, heteroaryl or optionally substituted amino.

N-((phenyl, benzodioxinyl or

Piperazine derivatives

Bicyclic carboxamides of formula I ##STR1## and the 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

Bicyclic carboxamides

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.

Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2; R is hydrogen, hydroxy, lower alkyl, lower alkoxy, halogen, trifluoromethyl, nitro, amino, (lower)alkylamino or di(lower)alkylamino; R.sup.1 is hydrogen or lower alkyl; R.sup.2 is --(CH.sub.2).sub.n --R.sup.3 or --CH.sub.2 --CH.dbd.CH--(CH.sub.2).sub.m --R.sup.3 or --CH.sub.2.C.tbd.C.(CH.sub.2).sub.m --R.sup.3 where n is 1 to 6, and m is 0 to 3; and R.sup.3 is a ring of formula ##STR2## The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are used for the treatment of CNS disorders, e.g. anxiety, as antihypertensives and in treating anorexia.

N-(2,3-dihydro-1,4-benzodioxinyl)-N-substituted aminopyrido-fused

Pyridine derivatives of formula ##STR1## their heteroaromatic N-oxides and their pharmaceutically acceptable acid addition salts are disclosed. In the formula z is 0, 1 and 2 and R, R.sup.1, R.sup.2 and R.sup.2 have specified meanings. The compounds exhibit activity as 5-HT.sub.1A agonists, antagonists or partial agonists and are useful for the treatment of CNS disorders e.g. anxiety, as antihypertensives and in treating anorexia.

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Burnham, United Kingdom

Howard L Mansell