American Cyanamid Company

Wyeth Holdings Corporation

Dov Pharmaceutical, Inc.

Neurovance, Inc.

Otsuka America Pharmaceutical, Inc.

Dor Pharmaceutical, Inc.

Dov Pharmaceuticals Inc.

Euthymics Bioscience, Inc.

Joseph William Epstein

William J Fanshawe

Shin S Tseng

Gary H Birnberg

Arnold Stan Lippa

Semiramis Ayral-Kaloustian

Herbert J Brabander

Jeremy Ian Levin

Zhengming Chen

Lantz S Crawley

Phil Skolnick

Anthony Basile

Sidney Robert Safir

Minu D Dutia

Corris M Hofmann

Thomas C McKenzie

Edward James Salaski

John P Dusza

Thomas H Claus

Jonathan D Bloom

Elwood Eugene Largis

Gary Harold Birnberg

Gloria Jean Macewan

Katherine Cheung

Gary E Walker

Andrew S Tomcufcik

Adam Matthew Gilbert

James J Gibbons, Jr

James D Warren

Leon Goldman

James S Dixon

Arnold Curtis Osterberg

Jannie S Baker

Bernard Beer

Judy Lucas

Feng L Qing

Feng Ling Qing

The invention provides novel, multiply-substituted 1-aryl-3-azabicyclo[3.1.0]hexanes, and related processes and intermediates for preparing these compounds, as well as compositions and methods employing these compounds for the treatment and/or prevention of central nervous system (CNS) disorders, including depression and anxiety.

1-aryl-3-azabicyclo[3.1.0]hexanes: preparation and use to treat neuropsychiatric disorders

The present invention relates to (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating of or preventing relapse of depression, anxiety disorders, eating disorders, or urinary incontinence in a patient comprising administering (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof. The (+)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or pharmaceutically acceptable salt thereof is preferably substantially free of its corresponding (&#x2212;)-enantiomer.

(+)-1-(3,4-Dichlorophenyl)-3-azabicyclo[3.1.0]hexane, compositions and uses thereof

The present invention relates to (&#x2212;)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane and pharmaceutically acceptable salts thereof, compositions comprising (&#x2212;)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing a disorder alleviated by inhibiting dopamine reuptake. In one embodiment, the disorder is attention-deficit disorder, depression, obesity, Parkinson's disease, a tic disorder, or an addictive disorder. The (&#x2212;)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane or pharmaceutically acceptable salt thereof is preferably substantially free of its corresponding (+)-enantiomer.

(-)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, compositions thereof, and uses as a dopamine-reuptake inhibitor

(&#x2212;)-1-(3,4-dichlorophenyl)-3-azabicyclo[3.1.0]hexane, compositions thereof, and uses as a dopamine-reuptake inhibitor

The invention relates to compounds of Formula (I), to processes for their preparation and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.

3-substituted-3-(substitutedsulfonyl or sulfanyl) pyrrolidine-2,5-diones useful for inhibition of farnesyl-protein transferase

The invention relates to compounds of Formula (I), to processes for their preparation and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid

3-Substituted-3-(substitutedsulfonyl or sulfanyl)pyrrolidine-2,5-diones useful for inhibition of farnesyl-protein transferase

This invention relates to a method of using novel 5-(arylsulfonyl)-,5-(arylsulfinyl), and 5-(arylsulfanyl)-thiazolidine-2,4-diones of Formula (I), wherein Ar, Ar&prime;, R , m and n are as defined in the specification as inhibitors of Ras FPTase, and may be used as an alternative to, or in conjunction with, traditional cancer therapy for treating ras-oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.

5-(arylsulfonyl)-,5-(arylsulfinyl), and 5-(arylsulfanyl)-thiazolidine-2,4-diones useful for inhibition of farnesyl-protein transferase

3-substituted-3-(substitutedsulfonyl or sulfanyl)pyrrolidine-2,5-diones useful for inhibition of farnesyl-protein transferase

The present invention relates to (&minus;)-1-(3,4-dichlorophenyl)-3-azabicyclo&lsqb;3.1.0&rsqb;hexane and pharmaceutically acceptable salts thereof, compositions comprising (&minus;)-1-(3,4-dichlorophenyl)-3-azabicyclo&lsqb;3.1.0&rsqb;hexane or a pharmaceutically acceptable salt thereof, and methods for treating or preventing a disorder alleviated by inhibiting dopamine reuptake. In one embodiment, the disorder is attention-deficit disorder, depression, obesity, Parkinson's disease, a tic disorder, or an addictive disorder. The (&minus;)-1-(3,4-dichlorophenyl)-3-azabicyclo&lsqb;3.1.0&rsqb;hexane or pharmaceutically acceptable salt thereof is preferably substantially free of its corresponding (&plus;)-enantiomer.

(-)-1-(3,4-Dichlorophenyl)-3-azabicyclo&lsqb;3.1.0&rsqb;hexane, compositions thereof, and uses as a dopamine-reuptake inhibitor

The invention relates to compounds of Formula (I) wherein R , (R ) , R and n are defined in the specification and pharmaceutical compositions thereof, that inhibit the Ras farnesyl-protein transferase enzyme (FPTase), and may be used as an alternative to, or in conjunction with, traditional cancer therapy for the treatment of ras oncogene-dependent tumors, such as cancers of the pancreas, colon, bladder, and thyroid.

5-(Substituted)-5-(substitutedsulfonyl or sulfanyl) thiazolidine-2,4-diones useful for inhibition of farnesyl-protein transferase

Growing community of inventors

Monroe, NY, United States of America

Joseph William Epstein