公开(公告)号：EP1362039A1

公开(公告)日：2003-11-19

申请号：EP02718999.2

申请日：2002-02-15

申请人： Aventis Pharmaceuticals, Inc.

发明人： HENDRIX, James A. ,  HEMMERLE, Horst ,  URMANN, Matthias ,  SHUTSKE, Gregory ,  STRUPCZEWSKI, Joseph T. ,  BORDEAU, Kenneth J. ,  JURCAK, John G. ,  NIEDUZAK, Thaddeus ,  JACKSON, Sharon Anne ,  ANGELL, Paul ,  FINK, David M. ,  SABUCO, Jean-Francois ,  CHIANG, Yulin ,  COLLAR, Nicola ,  CAREY, James P. ,  LEE, George E.

IPC分类号： C07D241/04 ,  C07D409/04 ,  C07D401/04 ,  C07D403/04 ,  C07D498/04 ,  C07D405/04 ,  C07D409/14 ,  C07D495/04 ,  A61K31/495 ,  A61P25/18

CPC分类号： C07D239/42 ,  A61K31/496 ,  C07D209/08 ,  C07D213/74 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D241/04 ,  C07D241/20 ,  C07D249/08 ,  C07D261/20 ,  C07D295/155 ,  C07D307/66 ,  C07D307/68 ,  C07D317/58 ,  C07D333/58 ,  C07D333/66 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/06 ,  C07D495/04

摘要： The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor 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 D¿3 receptors.

公开(公告)号：EP1749001B1

公开(公告)日：2010-03-03

申请号：EP05740005.3

申请日：2005-04-27

申请人： Aventis Pharmaceuticals Inc.

发明人： SHUTSKE, Gregory ,  HARRIS, Keith, J. ,  BORDEAU, Kenneth, J. ,  ANGELASTRO, Michael, R. ,  JOHN, Stanly ,  KLEIN, Joseph, T. ,  LU, Jinqi ,  BOMONT, Catherine

IPC分类号： C07D405/04 ,  A61K31/352 ,  A61P25/00

CPC分类号： C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides compounds of formula (I): a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, 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).

摘要翻译： 本发明提供式（I）的化合物：其立体异构体或其药学上可接受的盐，其中变量R 1，R 2，R 3，R 4，X和n如本文所定义。 此外，用于治疗选自由神经学，心理学，心血管，认知或注意力障碍，药物滥用和成瘾行为或其组合组成的组的多巴胺相关神经障碍的方法，包括向需要这种治疗的患者施用 治疗有效量的式（I）化合物。

公开(公告)号：EP1362039B1

公开(公告)日：2005-12-21

申请号：EP02718999.2

申请日：2002-02-15

申请人： AVENTIS PHARMACEUTICALS INC.

发明人： HENDRIX, James A. ,  HEMMERLE, Horst ,  URMANN, Matthias ,  SHUTSKE, Gregory ,  STRUPCZEWSKI, Joseph T. ,  BORDEAU, Kenneth J. ,  JURCAK, John G. ,  NIEDUZAK, Thaddeus ,  JACKSON, Sharon Anne ,  ANGELL, Paul ,  FINK, David M. ,  SABUCO, Jean-Francois ,  CHIANG, Yulin ,  COLLAR, Nicola ,  CAREY, James P. ,  LEE, George E.

IPC分类号： C07D241/04 ,  C07D409/04 ,  C07D401/04 ,  C07D403/04 ,  C07D498/04 ,  C07D405/04 ,  C07D409/14 ,  C07D495/04 ,  A61K31/495 ,  A61P25/18

CPC分类号： C07D239/42 ,  A61K31/496 ,  C07D209/08 ,  C07D213/74 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D241/04 ,  C07D241/20 ,  C07D249/08 ,  C07D261/20 ,  C07D295/155 ,  C07D307/66 ,  C07D307/68 ,  C07D317/58 ,  C07D333/58 ,  C07D333/66 ,  C07D401/04 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D471/06 ,  C07D495/04

公开(公告)号：EP1749001A1

公开(公告)日：2007-02-07

申请号：EP05740005.3

申请日：2005-04-27

申请人： Aventis Pharmaceuticals Inc.

发明人： SHUTSKE, Gregory ,  HARRIS, Keith, J. ,  BORDEAU, Kenneth, J. ,  ANGELASTRO, Michael, R. ,  JOHN, Stanly ,  KLEIN, Joseph, T. ,  LU, Jinqi ,  BOMONT, Catherine

IPC分类号： C07D405/04 ,  A61K31/352 ,  A61P25/00

CPC分类号： C07D405/04 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14

摘要： The present invention provides compounds of formula (I): a stereoisomer or a pharmaceutically acceptable salt thereof, wherein the variables R1, R2, R3, R4, 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).

公开(公告)号：EP1361875A2

公开(公告)日：2003-11-19

申请号：EP02721057.4

申请日：2002-02-15

申请人： Aventis Pharmaceuticals Inc.

发明人： HENDRIX, James, A. ,  STRUPCZEWSKI, Joseph, T. ,  BORDEAU, Kenneth, J. ,  URMANN, Matthias ,  SHUTSKE, Gregory ,  HEMMERLE, Horst ,  JURCAK, John, G. ,  GILL, Harpal ,  WEIBERTH, Franz, Jr. ,  NIEDUZAK, Thaddeus ,  JACKSON, Sharon, A. ,  ZHAO, Xu-Yang ,  MUELLER, Paul J.

IPC分类号： A61K31/33

CPC分类号： C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D333/58 ,  C07D333/66 ,  C07D333/68 ,  C07D333/70 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D495/04

摘要： The invention relates to heterocyclic substituted amide derivatives of formula (I) that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor 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 D3 receptors.