Aventis Pharma Deutschland, Gmbh

Aventis Pharmaceuticals Inc.

Sanofi-a Ventis Deutschland Gmbh

Horst Hemmerle

Heinz-Werner Kleemann

Joachim Brendel

Stefan Peukert

Kenneth J Bordeau

John G Jurcak

Matthias Urmann

James Hendrix

Gregory Shutske

Thaddeus Nieduzak

Sharon Anne Jackson

Yulin Chiang

Joseph T Strupczewski

David Fink

George Lee

Nicola Collar

Paul Angell

James P Carey

Hans-Ludwig Schaefer

Reinhard Kirsch

Eugen Falk

Jean-Francois Sabuco

Paul Justin Mueller

Xu-Yang Zhao

Bernard Pirard

Franz J Weiberth

Jean-Fancois Sabuco

Jospeh T Strupczewski

Harpal Gill

George E Lee

Bernard Dr Pirard

James A Hendrix

Jackson Sharon Anne Anne

Kenneth K Bordeau

Joseph T c/o Sanofi-Aventis US Inc Strupczewski

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 present invention is related to a process for preparing anthranilamides of formula I, in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).

Anthranilamides and methods of their use

The present invention is related to anthranilamides of formula I,in which R(1) to R(7) have the meanings indicated herein, a process for their preparation, their use as medicaments, and pharmaceutical preparations containing them. The compounds act on the Kv1.5 potassium channel and inhibit a potassium current which is referred to as the ultra-rapidly activating delayed rectifier in the atrium of the human heart. The compounds are therefore suitable for use as novel antiarrhythmic agents for the treatment and prophylaxis of atrial arrhythmias (e.g., atrial fibrillation (AF) or atrial flutter).

Compounds of the formulae IA and Ib.in which X, R(1), R(2), R(3), R(4), R(5), R(6), R(7), R(30) and R(31) have the meanings indicated in the claims, are very particularly suitable as novel antiarrhythmic active compounds, in particular for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters.

Arylated furan- and thiophenecarboxamides, processes for their preparation, their use as medicaments, and pharmaceutical preparations comprising them

Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters. Compounds of the invention include compounds of the formula I

Ortho, meta-substituted bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations comprising them

Ortho, ortho-substituted nitrogen-containing bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparations including their use as antiarrhythmic active compounds, for example, for the treatment and prophylaxis of atrial arrhythmias, e.g. atrial fibrillation (AF) or atrial flutters. Compounds of the invention include compounds of the formula I

Ortho, ortho-substituted nitrogen-containing bisaryl compounds, processes for their preparation, their use as medicaments, and pharmaceutical preparation comprising them

Sulfonylcarboxamide derivatives, process for their preparation and their use as pharmaceuticals

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Indianapolis, IN, United States of America

Horst Hemmerle