Aventis Pharmaceuticals Inc.

Aventis Hoklings Inc.

David Fink

Yulin Chiang

George Lee

Nicola Collar

Kenneth J Bordeau

John G Jurcak

Matthias Urmann

Horst Hemmerle

James Hendrix

Gregory Shutske

Sharon Anne Jackson

Thaddeus Nieduzak

Paul Angell

James P Carey

Joseph T Strupczewski

Raymond W Kosley, Jr

Nicholas J Hrib

Brian S Freed

Frank Halley

Gregory H Merriman

Barbara S Rauckman

Gilles Dutruc-Rosset

Yong Mi Choi-Sledeski

Gilles Doerflinger

Gregory Bernard Poli

Jean-Francois Sabuco

William Joseph Hurst

William Arthur Metz, Jr

Bao-Guo Huang

Joseph T Tsay

Fernando Camacho

Ann Marie Gelormini

Andrew Giovanni

Joachim E Roehr

Stephen Wayne Harnish

Hazel Joan Hunt

Paul Robert Eastwood

Juan Antonio Gamboa

Juan Anotonio Gamboa

Helen Katherine Smith

Richard Simon Todd

Jospeh T Strupczewski

Jean-Fancois Sabuco

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) wherein M is N, and K and L are each C with the remaining substituents further defined herein. These compounds are effective as inhibitors of human casein kinase I&#x3b5;, and as such are useful in the treatment of central nervous system diseases and disorders including mood disorders and sleep disorders. Pharmaceutical compositions comprising compounds of formula (I) and methods for the preparation of compounds of formula (I) are also disclosed and claimed.

Substituted 1H-pyrrolo[2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase I&#x3b5;

The present invention relates to a series of substituted bis aryl and heteroaryl compounds of formula (I): Wherein X, Y, Z, A, B, D, Ar, Rand Rare as defined herein. The compounds of this invention are selective 5HTantagonists, and are therefore, useful in treating a variety of diseases including but not limited to a wide variety of sleep disorders as disclosed and claimed herein.

The compounds are of the class thienoisoxazolyl- and thienylpyrrazolyl-phenoxy substituted propyl 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.

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

Substituted 1H-pyrrolo[3,2-b, 3,2-c, and 2,3-c]pyridine-2-carboxamides and related analogs as inhibitors of casein kinase lepsilon

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.

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Lebanon, NJ, United States of America

David Fink