Hoechst Roussel Pharmaceuticals

Hoechst Marion Roussel

Aventis Pharmaceuticals Inc.

Sanofi-a Ventis Deutschland Gmbh

Other

Hoescht Marion Roussel, Inc.

Hoechst Marion Rosueel, Inc.

Aventis Holdings, Inc.

Yulin Chiang

Hmr Pharma Inc.

Grover Cleveland Helsley

Joseph Thomas Strupczewski

Kenneth J. Bordeau

Kenneth J Bordeau

Joseph T Strupczewski

Edward J Glamkowski

Peter A Nemoto

John J Tegeler

Grover C Helsley

John G Jurcak

Gregory Shutske

Matthias Urmann

Horst Hemmerle

James Hendrix

Thaddeus Nieduzak

Sharon Anne Jackson

David Fink

George Lee

Nicola Collar

Joseph T Klein

James P Carey

Paul Angell

Siegfried Stengelin

Matthias Gossel

Thomas Klabunde

Gregory H Merriman

Brian K Whiteley

Martin Smrcina

Pavel Safar

Jean-Francois Sabuco

Carolina Lanter

James Spoonamore

Zhaoxia Yang

Nicholas J Hrib

Michael R Angelastro

Stefanie Flohr

Petra Lennig

Petra Stahl

Stanly John

Keith John Harris

Paul Justin Mueller

Jinqi Lu

Franz J Weiberth

Xu-Yang Zhao

Jean-Fancois Sabuco

Jospeh T Strupczewski

Harpal Gill

Catherine Bomont

Joseph T Strupczewksi

Shelley L Pavlek

Joseph T Stupczewski

John J Tegler

Keith J Harris

The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives substituted with amino acids, and to the physiologically tolerated salts thereof, processes for their preparation and their use as medicaments.

Hexahydro-pyrazino[1,2-A]pyrimidine-4,7-dione derivatives substituted with amino acids

The present invention provides compounds of formula I: a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R, R, R, R, X and n are defined as defined herein. Additionally, a method for treating dopamine-related neurological disorders selected form the group consisting of neurological, psychological, cardiovascular, cognitive or attention disorders, substance abuse and addictive behavior, or a combination thereof, comprising administering to a patient in need of such treatment a therapeutically effective amount of compounds of formula I.

3-piperidinylisochroman-5-ols as dopamine agonists

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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Nitrogen-substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives, processes for the preparation and their use as medicaments The invention relates to substituted hexahydropyrazino[1,2-a]pyrimidine-4,7-dione derivatives and to the physiologically tolerated salts and physiologically functional derivatives thereof. Compounds of the formula I in which the radicals have the stated meanings, and the physiologically tolerated salts thereof and processes for preparing them are described. The compounds are suitable for example as anorectic agents.

Nitrogen-substituted hexahydropyrazino[1,2-A]pyrimidine-4,7-dione derivatives, processes for their preparation and their use as medicaments

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

Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Heteroarylpiperidines, and their use as antipsychotics and analgetics

Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amounts of one of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Heteroarylpiperidines, pyrrolidines and piperazines and their use as antipsychotics and analgesics

Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

Heteroarylpiperidines and their use as antipsychotics

Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents, the compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

1-(arylthioalkyl, arylaminoalkyl, or arylmethylenealkyl)-4-(heteroaryl)piperazines and related compounds useful as antipsychotics and analgesics

Heteroarylpiperidines, pyrrolidines, and piperazines are useful as antipsychotic and analgesic agents. The compounds are especially useful for treating psychoses by administering to a mammal a psychoses-treating effective amount of one of the compounds. Depot derivatives of the compounds are useful for providing long acting effects of the compounds. The compounds are also useful as analgesics by administering a pain-relieving effective amount of one of the compounds to a mammal.

1-(aryloxyalkyl)-4-(heteroaryl) piperazines and related compounds useful as antipsychotics and analgesics

Heteroarylpiperidines and their use as antipsychotics and analgesics

N-&lsqb;(3-heteroaryl-1-pyrrolidinyl)-alkyl&rsqb;phthalimides and related compounds and their therapeutic utility

1-(aryloxyalkyl)-4-(heteroaryl)piperidines and related compounds useful

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Kintnersville, PA, United States of America

Kenneth J Bordeau