John Wyeth Brother, Limited

American Home Products Corporation

Wyeth

John Wyeth & Bro., Limited

Magid A. Abou-gharbia

John P. Yardley

Ian A. Cliffe

Ian A Cliffe

Alan C White

Howard L Mansell

Richard S Todd

Terence J Ward

Anderson D Ifill

Magid A Abou-Gharbia

Gary Paul Stack

Richard Eric Mewshaw

Graham John Warrellow

John P Yardley

George E M Husbands

Allan Fletcher

Roger Crossley

James Albert Nelson

Uresh Shantilal Shah

Wayne E Childers, Jr

Christopher Ian Brightwell

Mark A Ashwell

Mira A Kanzelberger

Chapman White Alan

Bernhard Baudy Reinhardt

Antony Ashwell Mark

Compounds of the formulauseful for the treatment of depression and other conditions such as obsessive compulsive disorder, panic attacks, generalized anxiety disorder, sexual dysfunction, eating disorders, addictive disorders caused by ethanol or cocaine abuse and related illnesses.

Antidepressant azaheterocyclylmethyl derivatives of 2,3-dihydro-1, 4-benzodiozan

Antidepressant azaheterocyclymethyl derivatives of 2,3-dihydro-1,4-benzodioxan

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

Selective 5-HT.sub.1A antagonists radiolabelled with .sup.3 H or .sup.11 C are radiolabelled ligands useful, for example, in pharmacological screening procedures and in positron emission tomography (PET) studies.

5-HT.sub.1A ligands

Treatment of cognitive disorders with piperazine derivatives

N-(piperidinyl-1-alkyl)-substituted cyclohexane carboxylic acid amides

This invention concerns compounds of formula (I) ##STR1## where A is a C.sub.1 or C.sub.2 alkylene chain optionally substituted by lower alkyl; Z is a bicyclic oxygen-containing aryl radical (e.g. 2,3-dihydro-1,4-benzodioxin-5-yl); R is hydrogen or lower alkyl; R.sup.1 is aryl or aryl(lower)alkyl; R.sup.2 is hydrogen or lower alkyl; and R.sup.3 is hydrogen, an alkyl group of 1 to 10 carbon atoms, cycloalkyl of 3 to 12 carbon atoms; cycloalkyl(lower)alkyl, aryl or aryl(lower)alkyl or R.sup.2 and R.sup.3 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 pharmaceutically acceptable acid addition salts thereof. The compounds are 5-HT.sub.1A -antagonists which may be used, for example, in treating anxiety.

Piperazine derivatives as 5-ht antagonists

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

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

Piperazine derivatives

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

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

Amide derivatives

Piperazine derivatives of formula: ##STR1## and their pharmaceutically acceptable acid addition salts are disclosed. In the formula, n is 1 or 2; R and R.sup.5 are hydrogen or lower alkyl, R.sup.1 is substituted or unsubstituted aryl or a heteroaromatic radical; R.sup.3 is substituted or unsubstituted aryl or substituted or unsubstituted arylalkyl; R.sup.9 is hydrogen, alkyl, cycloalkyl, cycloalkylalkyl or substituted or unsubstituted arylalkyl with the proviso that when R.sup.9 is hydrogen, alkyl, or arylalkyl, R.sup.5 is other than a tertiary alkyl group. The compounds of this invention are useful 5-HT.sub.1A antagonists for the treatment of CNS disorders such as anxiety.

Piperazine Derivatives

##STR1## This invention concerns compounds of formula (I) where A is an alkylene chain of 2 to 5 carbon atoms optionally substituted by one or more lower alkyl groups, R represents hydrogen or one or two same or different lower alkyl groups, R.sup.1 is a monocyclic aryl or heteroaryl radical, R.sup.2 is a mono or bicyclic aryl radical and R.sup.3 is cycloalkyl. The compounds of the invention are useful as antidepressant, antianxiety, or hypotensive agents; or for regulating the sleep/wake cycle, feeding behavior and/or sexual function; and for treating cognition disorders.

Piperazine derivatives as 5-HT receptors antagonists

Growing community of inventors

Slough, United Kingdom

Ian A Cliffe