公开(公告)号：US5635477A

公开(公告)日：1997-06-03

申请号：US461611

申请日：1995-06-05

申请人： William F. Degrado ,  Sharon A. Jackson ,  Shaker A. Mousa ,  Anju Parthasarathy ,  Michael Sworin ,  Maria Rafalski

发明人： William F. Degrado ,  Sharon A. Jackson ,  Shaker A. Mousa ,  Anju Parthasarathy ,  Michael Sworin ,  Maria Rafalski

IPC分类号： A61K38/00 ,  C07K7/56 ,  C07K14/75 ,  A61K38/12

CPC分类号： C07K14/75 ,  C07K7/56 ,  A61K38/00

摘要： This invention relates to novel cyclic compounds containing carbocyclic ring systems useful as antagonists of the platelet glycoprotein IIb/IIIa complex, to pharmaceutical compositions containing such cyclic compounds, with or without other therapeutic agents, and to methods of using these compounds, with or without other therapeutic agents, for the inhibition of platelet aggregation, as thrombolytics, and/or for the treatment of other thromboembolic disorders. This invention also relates to methods of using the cyclic compounds of the invention in combination with anti-coagulants such as warfarin or heparin, or additional anti-platelet agents such as aspirin, piroxicam or ticlopidine, or thrombin inhibitors such as boropeptides, hirudin or argatroban, or thrombolytic agents such as tissue plasminogen activator, anistreplase, urokinase or streptokinase, or combinations thereof, for the treatment of thromboembolic disorders. A representative compound of the invention is cyclo(D-Val-(.sup..alpha. N-methyl Arg)-Gly-Asp-(3-aminomethylbenzoic acid).

摘要翻译： 本发明涉及含有可用作血小板糖蛋白IIb / IIIa复合物的拮抗剂的碳环系的新型环状化合物，含有或不含其它治疗剂的含有环状化合物的药物组合物，以及使用或不使用其它治疗剂的方法 治疗剂，用于抑制血小板聚集，作为血栓溶解剂，和/或用于治疗其他血栓栓塞障碍。 本发明还涉及使用本发明的环状化合物与抗凝血剂如华法林或肝素或另外的抗血小板药如阿司匹林，吡罗昔康或噻氯匹定或凝血酶抑制剂如硼多肽，水蛭素或阿加曲班联合使用的方法 ，或血栓溶解剂如组织纤溶酶原激活剂，anistreplase，尿激酶或链激酶或其组合，用于治疗血栓栓塞性疾病。 本发明的代表性化合物是环（D-Val-（αN-甲基Arg）-Gly-Asp-（3-氨基甲基苯甲酸）。

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：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：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。