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公开(公告)号：US06916819B2
公开(公告)日：2005-07-12
申请号：US10038069
申请日：2001-12-21
申请人： Guiying Li , John M. Peterson , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , Vinod Singh , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu
发明人： Guiying Li , John M. Peterson , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , Vinod Singh , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu
IPC分类号： A61K31/415 , A61K31/4184 , A61K31/4196 , A61K31/422 , A61K31/4245 , A61K31/435 , A61K31/437 , A61K31/438 , A61K31/4439 , A61K31/454 , A61K31/506 , A61K31/5377 , A61K31/541 , A61K31/55 , A61P25/00 , A61P25/18 , A61P25/20 , A61P25/22 , A61P25/24 , A61P25/28 , C07D233/20 , C07D233/54 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/04 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10 , C07D491/113 , C07D403/12
CPC分类号： C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed.This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译： 本发明涉及苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物，所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A的苯并二氮杂部位的化合物， / SUB>受体。 本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统（CNS）疾病中的用途。 公开了制备式I化合物的新方法。 本发明还涉及式I的苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。 此外，本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。
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22.发明授权Two-step pretargeting methods using improved bidtin-active agent conjugates 失效使用改进的bidtin活性剂缀合物的两步预靶向方法公开(公告)号：US06287536B1
公开(公告)日：2001-09-11
申请号：US08788339
申请日：1997-01-27
IPC分类号： A61K5100
CPC分类号： B82Y5/00 , A61K47/557 , A61K47/665 , A61K47/68 , A61K47/6887 , A61K47/6893 , A61K47/6898 , A61K51/0497 , A61K51/1268 , A61K2121/00 , A61K2123/00 , Y10S530/825
摘要： Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin and for improved radiohalogenation of biotin, as well as related compounds, are described. Also, clearing agents, anti-ligand-targeting moiety conjugates, target cell retention enhancing moieties and additional methods are discussed.
摘要翻译： 公开了与诊断和治疗剂的预靶向递送相关的方法，化合物，组合物和试剂盒。 特别地，描述了用于生物素的放射性金属标记和改善生物素的放射性卤化的方法以及相关化合物。 此外，讨论了清除剂，抗配体靶向部分缀合物，靶细胞保留增强部分和另外的方法。
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公开(公告)号：US5608060A
公开(公告)日：1997-03-04
申请号：US351469
申请日：1995-02-21
IPC分类号： A61K39/395 , A61K47/48 , A61K51/00 , A61K51/04 , A61K51/12 , A61P43/00 , C07D495/04 , C07D257/02 , A61K31/415 , C07H17/04
CPC分类号： C07D495/04 , A61K47/48023 , A61K47/48146 , A61K47/48353 , A61K47/48369 , A61K47/48707 , A61K47/4873 , A61K47/48753 , A61K51/0497 , A61K51/1268 , B82Y5/00 , A61K2121/00 , A61K2123/00
摘要： Biotinidase-resistant biotin-DOTA conjugates, and methods of use thereof in diagnostic and therapeutic pretargeting methods are provided. These conjugates are useful in diagnosis and treatment of cancer.
摘要翻译： PCT No.PCT / US93 / 05406 Sec。 371日期1995年2月21日 102（e）日期1995年2月21日PCT提交1993年6月7日PCT公布。 公开号WO93 / 25240 日期：1993年12月23日提供了用于诊断和治疗预靶向方法中的抗生物素 - 生物素 - DOTA缀合物及其使用方法。 这些缀合物可用于诊断和治疗癌症。
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公开(公告)号：US07642267B2
公开(公告)日：2010-01-05
申请号：US11942480
申请日：2007-11-19
申请人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
发明人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I. The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed. This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译： 本发明涉及苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物，所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A受体的苯并二氮杂位点的化合物。 本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统（CNS）疾病中的用途。 公开了制备式I化合物的新方法。 本发明还涉及式I的苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。 此外，本发明涉及使用这些化合物作为组织切片中GABA A受体定位的探针。
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公开(公告)号：US07300945B2
公开(公告)日：2007-11-27
申请号：US11179458
申请日：2005-07-12
申请人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
发明人： Guiying Li , Pamela Albaugh , Kevin S. Currie , Guolin Cai , Linda M. Gustavson , Kyungae Lee , Alan Hutchison , George D. Maynard , Jun Yuan , Ling Hong Xie , Manuka Ghosh , Nian Liu , George P. Luke , Scott Mitchell , Martin Patrick Allen , Spiros Liras
IPC分类号： C07D471/04 , A61K31/437
CPC分类号： C07D401/04 , C07D233/20 , C07D401/14 , C07D403/04 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/06 , C07D413/14 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D473/00 , C07D491/08 , C07D491/10
摘要： This invention relates to benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds, all of which may be described by of Formula I The invention is particularly related to such compounds that bind with high selectivity and high affinity to the benzodiazepine site of GABAA receptors. This invention also relates to pharmaceutical compositions comprising such compounds and to the use of such compounds in treatment of certain central nervous system (CNS) diseases. Novel processes for preparing compounds of Formula I are disclosed.This invention also relates to the use of benzimidazoles, pyridylimidazoles and related bicyclic heteroaryl compounds of Formula I in combination with one or more other CNS agents to potentiate the effects of the other CNS agents. Additionally this invention relates to the use such compounds as probes for the localization of GABAA receptors in tissue sections.
摘要翻译： 本发明涉及苯并咪唑，吡啶基咪唑和相关双环杂芳基化合物，所有这些可以由式I描述。本发明特别涉及以高选择性和高亲和力结合GABA A的苯并二氮杂部位的化合物， / SUB>受体。 本发明还涉及包含这些化合物的药物组合物以及这些化合物在治疗某些中枢神经系统（CNS）疾病中的用途。 公开了制备式I化合物的新方法。 本发明还涉及式I的苯并咪唑，吡啶基咪唑和相关的双环杂芳基化合物与一种或多种其它CNS剂的组合用于增强其它CNS剂的作用。 此外，本发明涉及使用这些化合物作为组织切片中GABA A A受体定位的探针。
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公开(公告)号：US07253168B2
公开(公告)日：2007-08-07
申请号：US11100355
申请日：2005-04-06
申请人： Alan J. Hutchison , Bertrand L. Chenard , James G. Tarrant , Guiying Li , Manuka Ghosh , George P. Luke , John M. Peterson , Wallace C. Pringle , Mary-Margaret E. O'Donnell , Kyungae Lee , Linda M. Gustavson , Dario Doller
发明人： Alan J. Hutchison , Bertrand L. Chenard , James G. Tarrant , Guiying Li , Manuka Ghosh , George P. Luke , John M. Peterson , Wallace C. Pringle , Mary-Margaret E. O'Donnell , Kyungae Lee , Linda M. Gustavson , Dario Doller
IPC分类号： A07D241/36 , A61K31/498 , A61P3/04 , A61P3/10 , C07D239/70 , C07D487/08 , C07D471/14 , A61K31/517 , A61K31/407
CPC分类号： C07D213/74 , C07D213/82 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Compounds of Formula I are provided, in which variables are as described herein: Such compounds may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要翻译： 提供了式I化合物，其中变量如本文所述：这样的化合物可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗各种代谢，进食和性障碍 在人类，驯养的伴侣动物和家畜中。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。
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27.发明授权Melanin concentrating hormone receptor ligands: substituted 1-benzyl-4-aryl piperazine analogues 失效黑色素浓缩激素受体配体：取代的1-苄基-4-芳基哌嗪类似物公开(公告)号：US07241765B2
公开(公告)日：2007-07-10
申请号：US11436099
申请日：2006-05-17
申请人： Alan J. Hutchison , Linda M. Gustavson , John M. Peterson , Dario Doller , Timothy M. Caldwell , Taeyoung Yoon , Wallace C. Pringle , Rajagopal Bakthavatchalam , Yiping Shen , Cheryl K. Steenstra , Helen Yin , Robert W. DeSimone , Xiao-shu He
发明人： Alan J. Hutchison , Linda M. Gustavson , John M. Peterson , Dario Doller , Timothy M. Caldwell , Taeyoung Yoon , Wallace C. Pringle , Rajagopal Bakthavatchalam , Yiping Shen , Cheryl K. Steenstra , Helen Yin , Robert W. DeSimone , Xiao-shu He
IPC分类号： A61K31/495 , C07D295/096 , A61K31/451
CPC分类号： C07D513/04 , C07D209/86 , C07D211/52 , C07D213/64 , C07D213/74 , C07D215/12 , C07D215/20 , C07D243/08 , C07D295/096 , C07D295/108 , C07D311/18 , C07D317/58 , C07D401/12 , C07D471/04 , C07D487/04 , C07D487/08
摘要： Melanin concentrating hormone receptor ligands (especially 1-benzyl-4-aryl-piperazines, 1-benzyl-4-aryl-piperidines and related compounds), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).
摘要翻译： 提供能够调节MCH受体活性的黑色素浓缩激素受体配体（特别是1-苄基-4-芳基哌嗪，1-苄基-4-芳基哌啶和相关化合物）。 这样的配体可用于在体内或体外调节MCH与MCH受体的结合，并且特别可用于治疗人，驯养的伴侣动物和家畜中的各种代谢，喂养和性障碍。 还提供了用于治疗这种病症的药物组合物和方法，以及使用这些配体检测MCH受体的方法（例如受体定位研究）。
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公开(公告)号：US06358490B2
公开(公告)日：2002-03-19
申请号：US09316452
申请日：1999-05-21
IPC分类号： A61K5110
CPC分类号： B82Y5/00 , A61K47/557 , A61K47/665 , A61K47/68 , A61K47/6887 , A61K47/6893 , A61K47/6897 , A61K47/6898 , A61K51/0497 , A61K51/1268 , A61K2121/00 , A61K2123/00
摘要： Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, three-step pretargeting methods are described.
摘要翻译： 公开了与诊断和治疗剂的预靶向递送相关的方法，化合物，组合物和试剂盒。 特别地，描述了三步预定靶方法。
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公开(公告)号：US5955605A
公开(公告)日：1999-09-21
申请号：US695940
申请日：1996-08-12
IPC分类号： A61K51/04 , C07D495/04 , C07H7/033 , C07D257/02 , A61K31/415 , C07H17/04
CPC分类号： C07D495/04 , A61K51/0497 , C07H7/033
摘要： Biotinidase-resistant biotin-DOTA conjugates, and methods of use thereof in diagnostic and therapeutic pretargeting methods are provided. These conjugates are useful in diagnosis and treatment of cancer.
摘要翻译： 提供了生物素抗性生物素-DTOTA缀合物及其在诊断和治疗预靶向方法中的应用方法。 这些缀合物可用于诊断和治疗癌症。
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公开(公告)号：US5578287A
公开(公告)日：1996-11-26
申请号：US156614
申请日：1993-11-23
IPC分类号： C07H13/06 , A61K31/70 , A61K31/7024 , A61K38/00 , A61K39/395 , A61K45/00 , A61K47/48 , A61K48/00 , A61K51/00 , A61K51/04 , A61K51/12 , A61P35/00 , A61K51/10 , A61K31/415 , C07D257/02 , C07K16/30
CPC分类号： B82Y5/00 , A61K47/48023 , A61K47/48146 , A61K47/48353 , A61K47/48707 , A61K47/4873 , A61K47/48746 , A61K47/48753 , A61K51/0497 , A61K51/1268 , A61K2121/00 , A61K2123/00
摘要： Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, three-step pretargeting methods are described.
摘要翻译： 公开了与诊断和治疗剂的预靶向递送相关的方法，化合物，组合物和试剂盒。 特别地，描述了三步预定靶方法。
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