公开(公告)号：US07772252B2

公开(公告)日：2010-08-10

申请号：US12425731

申请日：2009-04-17

申请人： James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M Shutske ,  Joseph T Strupczewski ,  Kenneth J Bordeau ,  John G Jurcak ,  Thaddeus Nieduzak ,  Sharon A. Jackson ,  Paul Angell ,  James P Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

发明人： James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M Shutske ,  Joseph T Strupczewski ,  Kenneth J Bordeau ,  John G Jurcak ,  Thaddeus Nieduzak ,  Sharon A. Jackson ,  Paul Angell ,  James P Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

IPC分类号： A61K31/4535 ,  C07D409/04 ,  C07D409/14 ,  C07D495/04

CPC分类号： A61K31/496 ,  C07D209/08 ,  C07D213/74 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D239/42 ,  C07D241/04 ,  C07D241/20 ,  C07D249/08 ,  C07D261/20 ,  C07D295/14 ,  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 ,  C07D498/04

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 D3 receptors.

摘要翻译： 本发明涉及显示与多巴胺D3受体的选择性结合的杂环取代的羰基衍生物。 另一方面，本发明涉及一种治疗需要这种治疗的患者中与多巴胺D3受体活性相关的中枢神经系统障碍的方法，其包括向受试者施用治疗有效量的所述化合物以减轻这种病症。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏综合征和亨廷顿疾病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及本文所述化合物的制备方法以及制备和使用化合物作为多巴胺D3受体的显像剂的方法。

公开(公告)号：US07521445B2

公开(公告)日：2009-04-21

申请号：US11714047

申请日：2007-03-05

申请人： James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M Shutske ,  Joseph T Strupczewski ,  Kenneth J Bordeau ,  John G Jurcak ,  Thaddeus Nieduzak ,  Sharon A. Jackson ,  Paul Angell ,  James P Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

发明人： James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M Shutske ,  Joseph T Strupczewski ,  Kenneth J Bordeau ,  John G Jurcak ,  Thaddeus Nieduzak ,  Sharon A. Jackson ,  Paul Angell ,  James P Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

IPC分类号： A61K31/5377 ,  A61K31/454 ,  A61K31/4535 ,  A61K31/4525 ,  C07D498/04 ,  C07D413/04 ,  C07D409/04

CPC分类号： A61K31/496 ,  C07D209/08 ,  C07D213/74 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D239/42 ,  C07D241/04 ,  C07D241/20 ,  C07D249/08 ,  C07D261/20 ,  C07D295/14 ,  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 ,  C07D498/04

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 D3 receptors.

摘要翻译： 本发明涉及显示与多巴胺D3受体的选择性结合的杂环取代的羰基衍生物。 另一方面，本发明涉及一种治疗需要这种治疗的患者中与多巴胺D3受体活性相关的中枢神经系统障碍的方法，其包括向受试者施用治疗有效量的所述化合物以减轻这种病症。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏综合征和亨廷顿疾病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及本文所述化合物的制备方法以及制备和使用化合物作为多巴胺D3受体的显像剂的方法。

公开(公告)号：US20090247509A1

公开(公告)日：2009-10-01

申请号：US12425731

申请日：2009-04-17

申请人： James A. Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M. Shutske ,  Joseph T. Strupczewski ,  Kenneth J. Bordeau ,  John G. Jurcak ,  Thaddeus R. Nieduzak ,  Sharon A. Jackson ,  Paul Angell ,  James P. Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

发明人： James A. Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M. Shutske ,  Joseph T. Strupczewski ,  Kenneth J. Bordeau ,  John G. Jurcak ,  Thaddeus R. Nieduzak ,  Sharon A. Jackson ,  Paul Angell ,  James P. Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

IPC分类号： A61K31/496 ,  C07D409/04 ,  C07D403/04 ,  C07D401/04 ,  C07D295/10 ,  C07D498/04 ,  C07D413/14 ,  C07D401/14 ,  A61K31/497 ,  A61K31/4965 ,  A61K31/454 ,  A61K31/551 ,  A61K31/4545 ,  A61K31/453

CPC分类号： A61K31/496 ,  C07D209/08 ,  C07D213/74 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D239/42 ,  C07D241/04 ,  C07D241/20 ,  C07D249/08 ,  C07D261/20 ,  C07D295/14 ,  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 ,  C07D498/04

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 D3 receptors.

摘要翻译： 本发明涉及显示与多巴胺D3受体的选择性结合的杂环取代的羰基衍生物。 另一方面，本发明涉及一种治疗需要这种治疗的患者中与多巴胺D3受体活性相关的中枢神经系统障碍的方法，其包括向受试者施用治疗有效量的所述化合物以减轻这种病症。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏综合征和亨廷顿疾病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及本文所述化合物的制备方法以及制备和使用化合物作为多巴胺D3受体的显像剂的方法。

公开(公告)号：US07186724B2

公开(公告)日：2007-03-06

申请号：US10819037

申请日：2004-04-06

申请人： James A Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M Shutske ,  Jospeh T Strupczewski ,  Kenneth J Bordeau ,  John G Jurcak ,  Thaddeus Nieduzak ,  Sharon A Jackson ,  Paul Angell ,  James P Carey ,  George Lee ,  David Fink ,  Jean-Fancois Sabuco ,  Yulin Chiang ,  Nicola Collar

发明人： James A Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory M Shutske ,  Jospeh T Strupczewski ,  Kenneth J Bordeau ,  John G Jurcak ,  Thaddeus Nieduzak ,  Sharon A Jackson ,  Paul Angell ,  James P Carey ,  George Lee ,  David Fink ,  Jean-Fancois Sabuco ,  Yulin Chiang ,  Nicola Collar

IPC分类号： A61K31/496 ,  C07D409/04 ,  C07D409/14 ,  A61K31/4535 ,  A61K31/454 ,  C07D403/04

CPC分类号： A61K31/496 ,  C07D209/08 ,  C07D213/74 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D239/42 ,  C07D241/04 ,  C07D241/20 ,  C07D249/08 ,  C07D261/20 ,  C07D295/14 ,  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 ,  C07D498/04

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 D3 receptors.

摘要翻译： 本发明涉及显示与多巴胺D 3受体的选择性结合的杂环取代的羰基衍生物。 另一方面，本发明涉及在需要这种治疗的患者中治疗与多巴胺D 3 N 3受体活性相关的中枢神经系统障碍的方法，包括向所述受试者施用治疗有效量的所述 用于缓解这种病症的化合物。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏综合征和亨廷顿疾病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及制备本文所述化合物的方法以及制备和使用化合物作为多巴胺D 3受体的显像剂的方法。

公开(公告)号：US20070161641A1

公开(公告)日：2007-07-12

申请号：US11714047

申请日：2007-03-05

申请人： James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory Shutske ,  Joseph Strupczewski ,  Kenneth Bordeau ,  John Jurcak ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Paul Angell ,  James Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

发明人： James Hendrix ,  Horst Hemmerle ,  Matthias Urmann ,  Gregory Shutske ,  Joseph Strupczewski ,  Kenneth Bordeau ,  John Jurcak ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Paul Angell ,  James Carey ,  George Lee ,  David Fink ,  Jean-Francois Sabuco ,  Yulin Chiang ,  Nicola Collar

IPC分类号： A61K31/498 ,  A61K31/497 ,  A61K31/496

CPC分类号： A61K31/496 ,  C07D209/08 ,  C07D213/74 ,  C07D215/40 ,  C07D231/12 ,  C07D233/56 ,  C07D239/42 ,  C07D241/04 ,  C07D241/20 ,  C07D249/08 ,  C07D261/20 ,  C07D295/14 ,  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 ,  C07D498/04

摘要： The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates is 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.

摘要翻译： 本发明涉及显示与多巴胺D 3受体的选择性结合的杂环取代的羰基衍生物。 另一方面，本发明涉及在需要这种治疗的患者中治疗与多巴胺D 3 N 3受体活性相关的中枢神经系统障碍的方法，包括向受试者施用治疗有效量的 所述化合物用于缓解这种病症。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏杜勒氏综合征和亨廷顿病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及制备本文所述化合物的方法以及制备和使用化合物作为多巴胺D 3受体的显像剂的方法。

公开(公告)号：US07550469B2

公开(公告)日：2009-06-23

申请号：US11643594

申请日：2006-12-21

申请人： James A Hendrix ,  Joseph T Strupczewski ,  Kenneth Bordeau ,  Matthias Urmann ,  Gregory Shutske ,  Horst Hemmerle ,  John G Jurcak ,  Harpal Gill ,  Franz J Weiberth ,  Thaddeus Nieduzak ,  Sharon Anne Jackson ,  Xu-Yang Zhao ,  Paul Justin Mueller

发明人： James A Hendrix ,  Joseph T Strupczewski ,  Kenneth Bordeau ,  Matthias Urmann ,  Gregory Shutske ,  Horst Hemmerle ,  John G Jurcak ,  Harpal Gill ,  Franz J Weiberth ,  Thaddeus Nieduzak ,  Sharon Anne Jackson ,  Xu-Yang Zhao ,  Paul Justin Mueller

IPC分类号： A61K31/496 ,  C07D495/04 ,  C07D498/04 ,  A61K31/4525 ,  A61K31/4535 ,  A61K31/551 ,  C07D333/66 ,  C07D409/12 ,  C07D409/14 ,  C07D413/041

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 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.

摘要翻译： 本发明涉及显示与多巴胺D3受体的选择性结合的杂环取代的酰胺衍生物。 另一方面，本发明涉及一种治疗需要这种治疗的患者中与多巴胺D3受体活性相关的中枢神经系统障碍的方法，其包括向受试者施用治疗有效量的所述化合物以减轻这种病症。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏综合征和亨廷顿疾病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及本文所述化合物的制备方法以及制备和使用化合物作为多巴胺D3受体的显像剂的方法。

公开(公告)号：US20050107389A1

公开(公告)日：2005-05-19

申请号：US10960399

申请日：2004-10-07

申请人： James Hendrix ,  Joseph Strupczeski ,  Kenneth Bordeau ,  Matthias Urmann ,  Gregory Shutske ,  Horst Hemmerle ,  John Jurcak ,  Harpal Gill ,  Franz Weiberth ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Xu-Yang Zhao ,  Paul Mueller

发明人： James Hendrix ,  Joseph Strupczeski ,  Kenneth Bordeau ,  Matthias Urmann ,  Gregory Shutske ,  Horst Hemmerle ,  John Jurcak ,  Harpal Gill ,  Franz Weiberth ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Xu-Yang Zhao ,  Paul Mueller

IPC分类号： A61K31/33 ,  C07D333/58 ,  C07D333/66 ,  C07D333/68 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D495/04 ,  C07D498/04 ,  C07D521/00 ,  C07D471/02 ,  A61K31/4745 ,  A61K31/503 ,  C07D487/04

CPC分类号： A61K31/33 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08 ,  C07D333/58 ,  C07D333/66 ,  C07D333/68 ,  C07D409/04 ,  C07D409/12 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D451/02 ,  C07D471/04 ,  C07D495/04

摘要： The invention relates to heterocyclic substituted amide 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 D3 receptors.

摘要翻译： 本发明涉及显示与多巴胺D 3受体的选择性结合的杂环取代的酰胺衍生物。 另一方面，本发明涉及在需要这种治疗的患者中治疗与多巴胺D 3 N 3受体活性相关的中枢神经系统障碍的方法，包括向所述受试者施用治疗有效量的所述 用于缓解这种病症的化合物。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏综合征和亨廷顿疾病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及制备本文所述化合物的方法以及制备和使用化合物作为多巴胺D 3受体的显像剂的方法。

公开(公告)号：US20070142351A1

公开(公告)日：2007-06-21

申请号：US11643594

申请日：2006-12-21

申请人： James Hendrix ,  Joseph Strupczewski ,  Kenneth Bordeau ,  Matthias Urmann ,  Gregory Shutske ,  Horst Hemmerte ,  John Jurcak ,  Harpal Gill ,  Franz Weiberth ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Xu-Yang Zhao ,  Paul Mueller

发明人： James Hendrix ,  Joseph Strupczewski ,  Kenneth Bordeau ,  Matthias Urmann ,  Gregory Shutske ,  Horst Hemmerte ,  John Jurcak ,  Harpal Gill ,  Franz Weiberth ,  Thaddeus Nieduzak ,  Sharon Jackson ,  Xu-Yang Zhao ,  Paul Mueller

IPC分类号： A61K31/498 ,  A61K31/46 ,  C07D451/02 ,  C07D487/04

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 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.

摘要翻译： 本发明涉及显示与多巴胺D 3受体的选择性结合的杂环取代的酰胺衍生物。 另一方面，本发明涉及在需要这种治疗的患者中治疗与多巴胺D 3 N 3受体活性相关的中枢神经系统障碍的方法，包括向所述受试者施用治疗有效量的所述 用于缓解这种病症的化合物。 可能用这些化合物治疗的中枢神经系统疾病包括心理障碍，物质依赖性，物质滥用，运动障碍（例如帕金森病，帕金森综合征，神经灵敏诱导的迟发性运动障碍，杜氏综合征和亨廷顿疾病），痴呆，焦虑 疾病，睡眠障碍，昼夜节律紊乱和情绪障碍。 本发明还涉及制备本文所述化合物的方法以及制备和使用化合物作为多巴胺D 3受体的显像剂的方法。

公开(公告)号：US08946212B2

公开(公告)日：2015-02-03

申请号：US12996692

申请日：2009-05-22

申请人： Stefanie Keil ,  Matthias Urmann ,  Maike Glien ,  Hans Matter ,  Eugen Falk ,  Ulrike Wendler

发明人： Stefanie Keil ,  Matthias Urmann ,  Wolfgang Wendler ,  Maike Glien ,  Hans Matter ,  Eugen Falk

IPC分类号： A61K31/538 ,  C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

CPC分类号： C07D413/10 ,  C07D413/12 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D498/04

摘要： Annelated N-heterocyclic sulfonamides with oxadiazolone headgroup, processes for their preparation and their use as pharmaceuticals The invention relates to annelated N-heterocyclic sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula I, in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.

摘要翻译： 具有恶二唑酮头基的神经化N-杂环磺酰胺，其制备方法及其作为药物的用途本发明涉及具有恶二唑酮头基的环状N-杂环磺酰胺及其生理学上可接受的盐和生理功能衍生物，其显示PPARδ或PPARα和PPARα激动剂活性。 所描述的是式I化合物，其中自由基如所定义，以及它们的生理上可接受的盐及其制备方法。 该化合物适用于治疗和/或预防脂肪酸代谢紊乱和葡萄糖利用障碍以及其中涉及胰岛素抵抗和中枢神经和周围神经系统的脱髓鞘和其它神经变性疾病的疾病。

公开(公告)号：US08748483B2

公开(公告)日：2014-06-10

申请号：US12504198

申请日：2009-07-16

申请人： Harm Brummerhop ,  Siegfried Stengelin ,  Hubert Heuer ,  Susanne Kilp ,  Andreas Herling ,  Thomas Klabunde ,  Dieter Kadereit ,  Matthias Urmann

发明人： Harm Brummerhop ,  Siegfried Stengelin ,  Hubert Heuer ,  Susanne Kilp ,  Andreas Herling ,  Thomas Klabunde ,  Dieter Kadereit ,  Matthias Urmann

IPC分类号： A01N43/16 ,  A61K31/35 ,  C09B3/00 ,  C07D209/80 ,  C09B7/00

CPC分类号： A61K31/351

摘要： The invention relates to the use of substituted pyranone acid derivatives and of their physiologically acceptable salts for producing medicaments for treating the metabolic syndrome.

摘要翻译： 本发明涉及取代的吡喃酮酸衍生物及其生理学上可接受的盐用于制备用于治疗代谢综合征的药物的用途。