Neurogen Corporation

Stanislaw Rachwal

George D Maynard

Alan J Hutchison

Jun Yuan

Kevin J Hodgetts

Andrew Y Thurkauf

Linghong Xie

Daniel L Rosewater

Xiaoyan Zhang

Pamela Ann Albaugh

Kenneth Shaw

Robert W DeSimone

Linda M Gustavson

Xiao-shu He

Disclosed are compounds of the formula and the pharmaceutically acceptable salts thereof wherein R, Ar, A, n, Rand Rare defined herein. These compounds are highly selective agonists, antagonists or inverse agonists for GABAbrain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAbrain receptors and are therefore useful in the diagnosis and treatment of anxiety, depression, Down Syndrome, sleep and seizure disorders, overdose with benzodiazepine drugs and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are also disclosed.

Substituted fused pyrroleoximes and fused pyrazoleoximes

Heterocyclic compounds such as 3,4,5,6-tetrahydro-2,3,10-triaza-benzo[e]azulene-1-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinoline-9-carboxylic acid arylamides, 5,7-Dihydro-6H-pyrazolo[3,4-h]quinazoline-9-carboxylic acid arylamides, 2,4,5,6-Tetrahydro-1,2,6,7-tetraaza-as-indacene-8-carboxylic acid arylamides and related compounds are disclosed. These compounds are highly selective agonists, antagonists or inverse agonists for GABAbrain receptors or prodrugs of agonists, antagonists or inverse agonists for GABAbrain receptors and are therefore useful in the treatment of anxiety, depression, sleep and seizure disorders, overdose with benzodiazepine drugs, Alzheimer's dementia, and for enhancement of memory. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Intermediates useful for the synthesis of pyrazolecarboxylic acid arylamides are also provided. Compounds of the invention are also useful as probes for the localization of GABAreceptors in tissue samples.

Substituted fused pyrazolecarboxylic acid arylamides and related compounds

Substituted fused pyrroleimines and pyrazoleimines

Aryl substituted tetrahydroindazoles

4-Substituted quinoline derivatives

Substituted imidazoles as selective modulators of Bradykinin B2 receptors

4-substituted quinoline derivatives

Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABA receptors in tissue samples.

1-azatricyclic-4-benzylpiperazines

Disclosed are 1-Azatricyclic-4-benzylpiperazine compounds which are useful for the treatment and/or prevention of neuropsychological disorders including, but not limited to, schizophrenia, mania, dementia, depression, anxiety, compulsive behavior, substance abuse, Parkinson-like motor disorders and motion disorders related to the use of neuroleptic agents. Pharmaceutical compositions, including packaged pharmaceutical compositions, are further provided. Compounds of the invention are also useful as probes for the localization of GABA,receptors in tissue samples.

Growing community of inventors

Branford, CT, United States of America

Stanislaw Rachwal