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1.发明授权公开(公告)号：US07786122B2
公开(公告)日：2010-08-31
申请号：US11870595
申请日：2007-10-11
申请人： Michael F. Parker , Katharine E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
发明人： Michael F. Parker , Katharine E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
IPC分类号： A01N43/58 , A61K3/495 , C07D403/00
CPC分类号： C07D207/325 , C07C311/19 , C07C317/32 , C07C323/49 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07D211/28 , C07D211/60 , C07D213/42 , C07D213/74 , C07D215/06 , C07D217/04 , C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D285/01 , C07D295/13 , C07D295/135 , C07D307/68 , C07D333/20
摘要： There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
摘要翻译： 提供了一系列新颖的式（I）的α-（N-亚磺酰氨基）乙酰胺化合物，其中R，R 1，R 2和R 3在本文中定义，其为β-淀粉状蛋白肽（＆bgr; -AP）生产的抑制剂 并且可用于治疗阿尔茨海默氏病和其他受抗淀粉样蛋白活性影响的病症。
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2.发明授权公开(公告)号：US08513253B2
公开(公告)日：2013-08-20
申请号：US12840612
申请日：2010-07-21
申请人： Michael F. Parker , Katharine E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
发明人： Michael F. Parker , Katharine E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
IPC分类号： A01N43/58 , A61K31/495 , C07D403/00
CPC分类号： C07D207/325 , C07C311/19 , C07C317/32 , C07C323/49 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07D211/28 , C07D211/60 , C07D213/42 , C07D213/74 , C07D215/06 , C07D217/04 , C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D285/01 , C07D295/13 , C07D295/135 , C07D307/68 , C07D333/20
摘要： There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
摘要翻译： 提供了一系列式（I）的新型α-（N-亚磺酰氨基）乙酰胺化合物，其中R，R 1，R 2和R 3在本文中定义，其是β-淀粉样蛋白肽（β-AP）产生的抑制剂，并且是 可用于治疗阿尔茨海默病和其他受抗淀粉样蛋白活性影响的病症。
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3.发明申请Alpha-(N-Sulfonamido)Acetamide Derivatives as Beta-Amyloid Inhibitors 有权α-（N-磺酰氨基）乙酰胺衍生物作为β-淀粉样蛋白抑制剂公开(公告)号：US20110105485A1
公开(公告)日：2011-05-05
申请号：US12840612
申请日：2010-07-21
申请人： Michael F. Parker , Katharine E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
发明人： Michael F. Parker , Katharine E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
IPC分类号： A61K31/541 , A61K31/18 , C07C311/46 , A61K31/277 , C07D233/61 , A61K31/4164 , C07D295/14 , A61K31/5375 , C07D211/34 , A61K31/4453 , A61K31/54 , C07D217/04 , A61K31/472 , A61K31/216 , A61K31/495 , C07D211/16 , C07D417/06 , A61P25/28 , A61P25/00
CPC分类号： C07D207/325 , C07C311/19 , C07C317/32 , C07C323/49 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07D211/28 , C07D211/60 , C07D213/42 , C07D213/74 , C07D215/06 , C07D217/04 , C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D285/01 , C07D295/13 , C07D295/135 , C07D307/68 , C07D333/20
摘要： There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
摘要翻译： 提供了一系列新颖的式（I）的α-（N-亚磺酰氨基）乙酰胺化合物，其中R，R 1，R 2和R 3在本文中定义，其为β-淀粉状蛋白肽（＆bgr; -AP）生产的抑制剂 并且可用于治疗阿尔茨海默氏病和其他受抗淀粉样蛋白活性影响的病症。
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4.发明授权公开(公告)号：US07300936B2
公开(公告)日：2007-11-27
申请号：US10326365
申请日：2002-12-20
申请人： Michael F. Parker , Katharin E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
发明人： Michael F. Parker , Katharin E. McElhone , Robert A. Mate , Joanne J. Bronson , Yonghua Gai , Carl P. Bergstrom , Lawrence R. Marcin , John E. Macor
IPC分类号： A01N43/58 , A61K31/495 , C07D403/00 , C07D241/04 , C07D295/00
CPC分类号： C07D207/325 , C07C311/19 , C07C317/32 , C07C323/49 , C07C323/60 , C07C2601/02 , C07C2601/14 , C07D211/28 , C07D211/60 , C07D213/42 , C07D213/74 , C07D215/06 , C07D217/04 , C07D231/12 , C07D233/56 , C07D235/14 , C07D249/08 , C07D257/04 , C07D261/08 , C07D271/06 , C07D271/10 , C07D277/28 , C07D285/01 , C07D295/13 , C07D295/135 , C07D307/68 , C07D333/20
摘要： There is provided a series of novel α-(N-sulfonamido)acetamide compounds of the Formula (I) wherein R, R1, R2 and R3 are defined herein, which are inhibitors of β-amyloid peptide (β-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by anti-amyloid activity.
摘要翻译： 提供了一系列新的式（I）的α-（N-亚磺酰氨基）乙酰胺化合物，其中R 1，R 1，R 2和R 3 本文定义为β-淀粉样蛋白肽（β-AP）产生的抑制剂，并且可用于治疗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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5.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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6.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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7.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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![Azabicyclo[2.2.1]Heptane Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands](/abs-image/US/2011/10/27/US20110263605A1/abs.jpg.150x150.jpg)
8.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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![Azabicyclo[2.2.1]heptane compounds as alpha-7 nicotinic acetylcholine receptor ligands](/abs-image/US/2012/10/02/US08278320B2/abs.jpg.150x150.jpg)
9.发明授权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：US08278320B2
公开(公告)日：2012-10-02
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： A61K31/438 , A61K31/439 , C07D471/08
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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10.发明申请Azabicyclic Compounds as Alpha-7 Nicotinic Acetylcholine Receptor Ligands 有权Azabicyclic化合物作为α-7烟碱乙酰胆碱受体配体公开(公告)号：US20110269787A1
公开(公告)日：2011-11-03
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： A61K31/438 , A61P25/18 , A61P3/10 , A61P19/02 , A61P1/02 , C07D498/20 , 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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