Wyeth

American Home Products Corporation

Other

Annmarie Louise Sabb

Robert Lewis Vogel

Gregory Scott Welmaker

James Albert Nelson

Sharon J Rosenzweig-Lipson

Reinhardt P Stein

Joan E Sabalski

Gary Paul Stack

Wayne Everett Childers

Michael Byron Webb

Magid A Abou-Gharbia

Amedeo A Failli

Michael G Kelly

William Alvin Kinney

Panolil C Raveendranath

Reinhardt Bernhard Baudy

Yvette L Palmer

Gervais Dionne

Sreenivasulu Megati

Robert L Vogel

Madelene M Antane

Magda Asselin

Anita Wai-Yin Chan

George Theodore Grosu

Jianxin Ren

Deborah Ann Evrard

Lalitha Krishnan

Hong Gao

Yanfang Li

Lisa Marie Havran

Zhongqi Shen

Charles Guinosso

Michael D Smith

Antonia Nikitenko

Jean Yi-ching Sze

James Jacob Bicksler

Dan Chaekoo Chong

Charles John Stanton, Iii

The present invention relates to novel piperazine-piperidine compounds. The compounds are useful as 5-HT1A binding agents, particularly as 5-HT1A receptor antagonists and agonists. These compounds are useful in treating central nervous system disorders, such as cognition disorders, anxiety disorders, depression and sexual dysfunction. The invention relates to compounds and pharmaceutically acceptable salts of formula (I'): wherein R-R, R, R, and n are set forth in the specification. The invention also relates to pharmaceutical compositions comprising compounds and pharmaceutically acceptable salts of formula (I&#x2032;).

[object Object]

Compounds of formula 1 or pharmaceutically acceptable salts thereof are provided: which are agonists or partial agonists of the 2C subtype of brain serotonin receptors. The compounds, and compositions containing the compounds, can be used to treat a variety of central nervous system disorders such as schizophrenia.

Substituted indolizines and derivatives as CNS agents

The present invention provides cycloalkylfused indole, benzothiophene, benzofuran, and indene derivatives, and methods for using them to, for example, treat, prevent and/or ameliorate central nervous system diseases by antagonizing 5-HTreceptors and modulating serotonin levels.

Cycloalkyfused indole, benzothiophene, benzofuran and idene derivatives

This invention provides compounds of the formula: wherein Rand Rare each, independently, H, alkyl, cycloalkyl, &#x2014;CH-cycloalkyl, alkoxy, halogen, fluorinated alkyl, &#x2014;CN, &#x2014;NH&#x2014;SO-alkyl, &#x2014;SO&#x2014;NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or phenoyl or thiophenoyl; Rand Rare each, independently, H, alkyl or cycloalkyl; Ris H or alkyl; Ris H or; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions and methods utilizing these compounds for the treatment or prevention of disorders including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

Cyclohepta[b][1,4]diazepino[6,7,1,-hi]indoles and derivatives

This invention provides compounds of formula I having the structure wherein: Rand Rare H, alkyl, cycloalkyl, alkoxy, halogen, fluorinated alkyl, &#x2014;CN, &#x2014;NH&#x2014;SO-alkyl, &#x2014;SO&#x2014;NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated, acyl, or aroyl; R, Rare H, alkyl, cycloalkyl or &#x2014;CH-cycloalkyl; Ris H or alkyl; Ris H or alkyl; and wherein the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, as well as methods for using these compounds to treat central nervous system disorders, including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

Cycloocta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives

This invention provides compounds of the formulae: wherein:

Cyclopenta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives

This invention provides compounds of formula I, wherein

2,3,4,4a-tetrahydro-1H-pyrazino(1,2-a) quinoxalin-5(6H)one derivatives

Compounds of formula (I) or pharmaceutically acceptable salts thereof are provided:where Rthrough Rare defined herein. The compounds of formula (I) are 5HT2c agonists or partial agonists, and are useful for treating a variety of disorders.

[1,4]Diazocino[7,8,1-hi]indole derivatives as antipsychotic and antiobesity agents

This invention provides compounds of the formula:wherein Rand Rare each, independently, H, alkyl, cycloalkyl, &#x2014;CH-cycloalkyl, alkoxy, halogen, fluorinated alkyl, &#x2014;CN, &#x2014;NH&#x2014;SO-alkyl, &#x2014;SO&#x2014;NH-alkyl, alkyl amide, amino, alkylamino, dialkylamino, fluorinated alkoxy, acyl, or phenoyl or thiophenoyl; Rand Rare each, independently, H, alkyl or cycloalkyl; Ris H or alkyl; Ris H or; and the dashed line indicates an optional double bond; or a pharmaceutically acceptable salt thereof, and pharmaceutical compositions and methods utilizing these compounds for the treatment or prevention of disorders including obsessive-compulsive disorder, depression, anxiety, generalized anxiety disorder, schizophrenia, migraine, sleep disorders, eating disorders, obesity, epilepsy, and spinal cord injury.

Cyclohepta[b][1,4]diazepino[6,7,1-hi]indoles and derivatives

Processes for preparation of cyclopenta&lsqb;b&rsqb;&lsqb;1,4&rsqb;diazepino&lsqb;6,7,1-hi&rsqb;indoles and derivatives

Cyclopenta&lsqb;b&rsqb;&lsqb;1,4&rsqb;diazepino&lsqb;6,7,1-hi&rsqb;indoles and derivatives

Cycloocta&lsqb;b&rsqb;&lsqb;1,4&rsqb;diazepino&lsqb;6,7,1-hi&rsqb;indoles and derivatives

2,3,4,4a-tetrahydro-1H-pyrazino&lsqb;1,2-a&rsqb;quinoxalin-5(6H)one derivatives

&lsqb;1,4&rsqb;diazepino &lsqb;6,7,1-jk &rsqb;carbazoles and derivatives

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Pennington, NJ, United States of America

Annmarie Louise Sabb