Aventis Pharmaceuticals Inc.

Nicola Collar

Yulin Chiang

David Fink

Kenneth J Bordeau

John G Jurcak

Matthias Urmann

Horst Hemmerle

James Hendrix

George Lee

Gregory Shutske

Thaddeus Nieduzak

Sharon Anne Jackson

James P Carey

Paul Angell

Joseph T Strupczewski

Jean-Francois Sabuco

Tahir Nadeem Majid

Brian L Pedgrift

Jean Merrill

Jean-Fancois Sabuco

Friederike Wirtz-Brugger

Corey Hopkins

Jospeh T Strupczewski

George E Lee

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 present invention comprises methods for the treatment of central nervous system diseases and disorders including mood disorders and sleep disorders through the administration of compounds of formula (I) and formula (II) which are useful as inhibitors of human casein kinase I&#x3b5;. Pharmaceutical compositions comprising compounds of formula (I) or formula (II) as well as methods for their preparation are also disclosed and claimed.

Substituted thienopyrrole carboxylic acid amides, pyrrolothiazole carboxylic acid amides, and related analogs as inhibitors of casein kinase I

The present invention discloses and claims compounds of formula (I) and formula (II), as inhibitors of human casein kinase I&#x3b5; and methods for using said compounds for treating central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) or formula (II) and a method for the preparation of compounds of formula (I) or formula (II) are also disclosed and claimed.

Compounds of the formula I are suitable for producing pharmaceuticals for the prophylaxis and therapy of diseases whose course involves an increased activity of NIK.

Pyrazoloisoquinoline derivative as kinase inhibitors for the treatment of various disorders

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Hoboken, NJ, United States of America

Nicola Collar