Aventis Pharmaceuticals Inc.

Oligomerix, Inc.

James Hendrix

John G Jurcak

Gregory Shutske

Kenneth J Bordeau

Matthias Urmann

Horst Hemmerle

Sharon Anne Jackson

Thaddeus Nieduzak

Allen B Reitz

Yulin Chiang

Joseph T Strupczewski

Charles Gluchowski

Mark E McDonnell

Haiyan Bian

David Fink

James G Moe

Eliot J Davidowitz

George Lee

H Marie Loughran

Nicola Collar

James P Carey

Paul Angell

Albert S Yehaskel

Jean-Francois Sabuco

Nicholas J Hrib

Brian S Freed

John D Tomer, Iv

Reda Hanna

Franz J Weiberth

Paul Justin Mueller

Xu-Yang Zhao

Harpal Gill

Jospeh T Strupczewski

Jean-Fancois Sabuco

Marie H Loughran

Novel benzofurans, benzothiophenes and indoles useful as inhibitors of tau oligomer formation, useful for the treatment of neurodegenerative diseases and related conditions are disclosed. The invention also relates to the pharmaceutically acceptable salts of said compounds, processes for the preparation of said compounds, intermediates used in the preparation of said compounds, and pharmaceutical compositions containing said compounds. The invention further relates to methods of use of said compounds, salts of said compounds, and said compositions in treating neurodegenerative diseases and related conditions.

Benzofuran, benzothiophene, and indole analogs that inhibit the formation of tau oligomers and their method of use

Novel quinazolinones useful as inhibitors of tau oligomer formation, useful for the treatment of neurodegenerative diseases and related conditions are disclosed. The invention also relates to the pharmaceutically acceptable salts of said compounds, processes for the preparation of said compounds, intermediates used in the preparation of said compounds, and pharmaceutical compositions containing said compounds. The invention further relates to methods of use of said compounds, salts of said compounds, and said compositions in treating neurodegenerative diseases and related conditions.

Quinazolinones that inhibit the formation of tau oligomers and their method of use

The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine Dreceptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine Dreceptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine Dreceptors.

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The invention relates to heterocyclic substituted amide derivatives that display selective binding to dopamine Dreceptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine Dreceptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders. The subject invention is also directed towards processes for the preparation of the compounds described herein as well as methods for making and using the compounds as imaging agents for dopamine Dreceptors.

Heterocyclic amide derivatives and their use as dopamine D3 receptor ligands

The compounds are of the class of benzisoxazolyl-, pyridoisoxazolyl- and benzthienyl-phenoxy derivatives, useful as Dantagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of Dreceptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.

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Hillsborough, NJ, United States of America

James Hendrix