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1.发明授权Aza-bicyclic amine N-oxide compounds as alpha-7 nicotinic acetylcholine receptor ligand pro-drugs 有权氮杂双环胺N-氧化物作为α-7烟碱乙酰胆碱受体配体原药公开(公告)号：US08481555B2
公开(公告)日：2013-07-09
申请号：US13097153
申请日：2011-04-29
申请人： Kimberley A. Lentz , Rex Denton , James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Robert A. Mate , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor , Matthew D. Hill , Haiquan Fang
发明人： Kimberley A. Lentz , Rex Denton , James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Robert A. Mate , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor , Matthew D. Hill , Haiquan Fang
IPC分类号： A01N43/42 , A61K31/44 , C07D491/10 , C07D491/20
CPC分类号： C07D498/10
摘要： The disclosure generally relates to compounds of the following formula, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开一般涉及下式的化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是配体，激动剂和烟碱型α7受体的部分激动剂的前药，并且可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。
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2.发明申请Aza-Bicyclic Amine N-Oxide Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligand Pro-Drugs 有权氮杂双环胺氧化物作为α-7烟碱乙酰胆碱受体配体药物公开(公告)号：US20120108596A1
公开(公告)日：2012-05-03
申请号：US13097153
申请日：2011-04-29
申请人： Kimberley A. Lentz , Rex Denton , James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Robert A. Mate , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor , Matthew D. Hill , Haiquan Fang
发明人： Kimberley A. Lentz , Rex Denton , James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Robert A. Mate , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor , Matthew D. Hill , Haiquan Fang
IPC分类号： A61K31/4725 , A61P25/18 , A61P25/28 , A61K31/439 , A61K31/498 , A61K31/506 , A61K31/444 , A61K31/497 , C07D498/20 , C07D519/00
CPC分类号： C07D498/10
摘要： The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are prodrugs for ligands, agonists, and partial agonists for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开内容通常涉及式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是用于烟碱型α7受体的配体，激动剂和部分激动剂的前药，并且可用于治疗中枢神经系统的各种疾病，特别是情感和神经变性疾病。
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3.发明申请公开(公告)号：US20100099684A1
公开(公告)日：2010-04-22
申请号：US12607354
申请日：2009-10-28
申请人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
发明人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
IPC分类号： A61K31/499 , C07D239/12 , C07D241/36 , C07D401/14 , A61K31/498 , A61K31/444 , A61P25/28
CPC分类号： A61K31/506 , A61K31/439 , C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。
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4.发明授权公开(公告)号：US08507516B2
公开(公告)日：2013-08-13
申请号：US12911882
申请日：2010-10-26
申请人： Ivar M. McDonald , Robert A. Mate , James H. Cook, II , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
发明人： Ivar M. McDonald , Robert A. Mate , James H. Cook, II , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
IPC分类号： C07D401/04 , A61K31/438 , A61K31/439
CPC分类号： C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。
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公开(公告)号：US20120035189A1
公开(公告)日：2012-02-09
申请号：US13271028
申请日：2011-10-11
申请人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
发明人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
IPC分类号： A61K31/506 , A61P25/28 , A61P3/00 , A61P19/02 , A61P1/00 , C07D413/14 , A61P25/18
CPC分类号： A61K31/506 , A61K31/439 , C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
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6.发明申请Quinuclidine Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands 审中-公开奎宁环化合物作为α-7烟碱乙酰胆碱受体配体公开(公告)号：US20120035178A1
公开(公告)日：2012-02-09
申请号：US13270121
申请日：2011-10-10
申请人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
发明人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
CPC分类号： A61K31/506 , A61K31/439 , C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经变性疾病。
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7.发明申请QUINUCLIDINE COMPOUNDS AS ALPHA-7 NICOTINIC ACETYLCHOLINE RECEPTOR LIGANDS 有权喹啉化合物作为ALPHA-7非丁醇乙酰胆碱受体配体公开(公告)号：US20090270405A1
公开(公告)日：2009-10-29
申请号：US12423299
申请日：2009-04-14
申请人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
发明人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
IPC分类号： A61K31/498 , C07D498/10 , A61K31/439 , A61P25/28
CPC分类号： C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。
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8.发明申请DIAMINOPROPANE DERIVED MACROCYCLES AS INHIBITORS OF BETA AMYLOID PRODUCTION 有权作为淀粉酶生产的抑制剂的二亚胺衍生的大环化合物公开(公告)号：US20080194535A1
公开(公告)日：2008-08-14
申请号：US12019986
申请日：2008-01-25
申请人： Lawrence R. Marcin , Andrew C. Good , Yong-Jin Wu , Dmitry S. Zuev , Richard E. Olson , Nenghui Wang
发明人： Lawrence R. Marcin , Andrew C. Good , Yong-Jin Wu , Dmitry S. Zuev , Richard E. Olson , Nenghui Wang
IPC分类号： A61K31/395 , C07D273/02 , A61P25/00
CPC分类号： C07D273/02 , C07D413/04 , C07D487/04
摘要： There is provided a series of macrocyclic diaminopropanes of Formula (I) or a stereoisomer; or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, m, n, W, X, Y, Z and L as defined herein, their pharmaceutical compositions and methods of use. These novel compounds inhibit the processing of amyloid precursor protein (APP) by β-secretase and, more specifically, inhibit the production of Aβ-peptide. The present disclosure is directed to compounds useful in the treatment of neurological disorders related to β-amyloid production, such as Alzheimer's disease and other conditions affected by anti-amyloid activity.
摘要翻译： 提供一系列式（I）的大环二氨基丙烷或立体异构体; 或其药学上可接受的盐，其中R 1，R 2，R 3，m，n，W，X，Y，Z和 L，其药物组合物和使用方法。 这些新型化合物通过β-分泌酶抑制淀粉样前体蛋白（APP）的加工，更具体地，抑制Aβ-肽的产生。 本公开涉及可用于治疗与β-淀粉样蛋白产生相关的神经系统疾病的化合物，例如阿尔茨海默病和受抗淀粉样蛋白活性影响的其它病症。
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9.发明授权公开(公告)号：US08309577B2
公开(公告)日：2012-11-13
申请号：US12607354
申请日：2009-10-28
申请人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
发明人： James H. Cook, II , Ivar M. McDonald , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , John E. Macor
IPC分类号： A01N43/40 , A61K31/445 , C07D413/00
CPC分类号： A61K31/506 , A61K31/439 , C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开提供式I化合物，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。
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![Azabicyclo[2.2.1]Heptane Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands](/abs-image/US/2011/10/27/US20110263605A1/abs.jpg.150x150.jpg)
10.发明申请Azabicyclo[2.2.1]Heptane Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands 有权氮杂双环[2.2.1]庚烷化合物作为α-7烟碱乙酰胆碱受体配体公开(公告)号：US20110263605A1
公开(公告)日：2011-10-27
申请号：US12907122
申请日：2010-10-19
申请人： Ivar M. McDonald , Robert A. Mate , James H. Cook, II , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , Matthew D. Hill , Haiquan Fang , John E. Macor
发明人： Ivar M. McDonald , Robert A. Mate , James H. Cook, II , Dalton King , Richard E. Olson , Nenghui Wang , Christiana I. Iwuagwu , F. Christopher Zusi , Matthew D. Hill , Haiquan Fang , John E. Macor
IPC分类号： A61K31/439 , C07D487/00 , A61K31/506 , A61K31/497 , A61K31/53 , A61P1/00 , A61P25/28 , A61P25/18 , A61P19/02 , A61P1/04 , A61P3/10 , C07D498/20 , A61K31/519
CPC分类号： C07D498/20 , C07D519/00
摘要： The disclosure provides compounds of formula I, including Ia, Ib, Ic, or Id, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands for the nicotinic α7 receptor and may be useful for the treatment of various disorders of the central nervous system, especially affective and neurodegenerative disorders.
摘要翻译： 本公开提供式I化合物，包括Ia，Ib，Ic或Id，包括其盐，以及使用该化合物的组合物和方法。 这些化合物是烟碱型α7受体的配体，可用于治疗中枢神经系统的各种疾病，特别是情感和神经退行性疾病。
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