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31.发明授权公开(公告)号：US08377964B2
公开(公告)日：2013-02-19
申请号：US12796902
申请日：2010-06-09
申请人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess
发明人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess
IPC分类号： A61K31/4545
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , G01N33/5058
摘要： The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
摘要翻译： 本发明涉及式（I）的苯并咪唑 - 甲酰胺5-HT 4受体激动剂化合物，其中R 1和X如说明书中所定义，或其药学上可接受的盐或溶剂合物或立体异构体。 本发明还涉及包含这些化合物的药物组合物，使用这些化合物治疗与5-HT 4受体活性有关的疾病的方法，以及可用于制备这些化合物的方法和中间体。
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公开(公告)号：US08158659B2
公开(公告)日：2012-04-17
申请号：US12974210
申请日：2010-12-21
申请人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
发明人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
IPC分类号： A61K31/4164 , A61K31/44 , A61K31/415 , C07D233/54 , G01N33/53 , G01N33/566
CPC分类号： C07D233/70 , A61K31/415 , A61K31/4164 , A61K31/417 , A61K31/4188 , A61K31/4196 , A61K31/4412 , A61K45/00 , A61K45/06 , C07D207/36 , C07D207/46 , C07D213/64 , C07D213/89 , C07D231/14 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D255/02 , C07D401/12 , C07D403/10 , C07D513/04 , C07D513/14
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及具有下式的化合物：其中：Ar，r，R2-3，X和R5-7如说明书中所定义，及其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US08013005B2
公开(公告)日：2011-09-06
申请号：US12148872
申请日：2008-04-23
申请人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
发明人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
IPC分类号： A01N43/64 , C07D249/08
CPC分类号： C07D233/70 , A61K31/415 , A61K31/4164 , A61K31/417 , A61K31/4188 , A61K31/4196 , A61K31/4412 , A61K45/00 , A61K45/06 , C07D207/36 , C07D207/46 , C07D213/64 , C07D213/89 , C07D231/14 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D255/02 , C07D401/12 , C07D403/10 , C07D513/04 , C07D513/14
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, Y, Z, Q, W, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及具有下式的化合物：其中：Ar，r，Y，Z，Q，W，X和R5-7如说明书中所定义，及其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US07879896B2
公开(公告)日：2011-02-01
申请号：US12148842
申请日：2008-04-23
申请人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
发明人： Paul Allegretti , Seok-Ki Choi , Roland Gendron , Paul R. Fatheree , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
IPC分类号： A61K31/4164 , C07D233/54
CPC分类号： C07D233/70 , A61K31/415 , A61K31/4164 , A61K31/417 , A61K31/4188 , A61K31/4196 , A61K31/4412 , A61K45/00 , A61K45/06 , C07D207/36 , C07D207/46 , C07D213/64 , C07D213/89 , C07D231/14 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D255/02 , C07D401/12 , C07D403/10 , C07D513/04 , C07D513/14
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及具有下式的化合物：其中：Ar，r，R2-3，X和R5-7如说明书中所定义，及其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US20080318951A1
公开(公告)日：2008-12-25
申请号：US12156695
申请日：2008-06-04
申请人： Paul Allegretti , Seok-Ki Choi , Paul R. Fatheree , Roland Gendron , Ryan Hudson , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
发明人： Paul Allegretti , Seok-Ki Choi , Paul R. Fatheree , Roland Gendron , Ryan Hudson , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
IPC分类号： A61K31/5377 , C07D235/04 , A61K31/4184 , C07D257/04 , A61K31/41 , A61K31/496 , A61K31/454 , A61P9/00 , C07D295/00 , C07D403/02 , C07D401/02 , A61K31/4439 , C07D413/02
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D235/08 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及具有下式的化合物：其中：Ar，r，n，X，R2-3和R5-7如说明书中所定义，及其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US09273008B2
公开(公告)日：2016-03-01
申请号：US14662722
申请日：2015-03-19
IPC分类号： A61K31/4164 , C07D233/54 , C07D233/70 , C07D213/64 , C07D231/14 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D401/12 , C07D403/10 , C07D513/04 , C07D513/14 , A61K31/415 , A61K31/417 , A61K31/4188 , A61K31/4196 , A61K31/4412 , A61K45/00 , C07D207/46 , C07D213/89 , C07D255/02 , A61K45/06 , C07D207/36
CPC分类号： C07D233/70 , A61K31/415 , A61K31/4164 , A61K31/417 , A61K31/4188 , A61K31/4196 , A61K31/4412 , A61K45/00 , A61K45/06 , C07D207/36 , C07D207/46 , C07D213/64 , C07D213/89 , C07D231/14 , C07D233/64 , C07D233/68 , C07D233/90 , C07D249/08 , C07D255/02 , C07D401/12 , C07D403/10 , C07D513/04 , C07D513/14
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, R2-3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
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公开(公告)号：US09198899B2
公开(公告)日：2015-12-01
申请号：US14132391
申请日：2013-12-18
申请人： Paul Allegretti , Seok-Ki Choi , Paul R. Fatheree , Roland Gendron , Ryan Hudson , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
发明人： Paul Allegretti , Seok-Ki Choi , Paul R. Fatheree , Roland Gendron , Ryan Hudson , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
IPC分类号： C07D235/08 , A61K31/4184 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/12 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D405/10
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D235/08 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及具有下式的化合物：其中：Ar，r，n，X，R2-3和R5-7如说明书中所定义，及其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US08637676B2
公开(公告)日：2014-01-28
申请号：US12156695
申请日：2008-06-04
申请人： Paul Allegretti , Seok-Ki Choi , Paul R. Fatheree , Roland Gendron , Ryan Hudson , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
发明人： Paul Allegretti , Seok-Ki Choi , Paul R. Fatheree , Roland Gendron , Ryan Hudson , Keith Jendza , Robert Murray McKinnell , Darren McMurtrie , Brooke Olson
IPC分类号： A61K31/4184 , C07D235/08
CPC分类号： A61K31/4184 , A61K31/4439 , A61K31/5377 , A61K45/06 , C07D235/08 , C07D401/12 , C07D403/10 , C07D403/12 , C07D405/10 , C07D405/12
摘要： The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及具有下式的化合物：其中：Ar，r，n，X，R2-3和R5-7如说明书中所定义，及其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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公开(公告)号：US20130273568A1
公开(公告)日：2013-10-17
申请号：US13742783
申请日：2013-01-16
申请人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-Ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess
发明人： Robert Murray McKinnell , Roland Gendron , Lan Jiang , Seok-Ki Choi , Daniel D. Long , Paul R. Fatheree , Daniel Marquess
IPC分类号： G01N33/50
CPC分类号： C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , G01N33/5058
摘要： The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
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公开(公告)号：US08236839B2
公开(公告)日：2012-08-07
申请号：US13330372
申请日：2011-12-19
申请人： Seok-Ki Choi , Paul R. Fatheree , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Vivek Sasikumar
发明人： Seok-Ki Choi , Paul R. Fatheree , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Vivek Sasikumar
IPC分类号： A61K31/41 , C07D257/04
CPC分类号： C07C323/60 , C07C259/06 , C07D207/16 , C07D257/04 , C07D403/12
摘要： The invention relates to compounds having the formula: wherein: Ar, r, R3, Z, X, and R5-7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention also relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及具有下式的化合物：其中：Ar，r，R3，Z，X和R5-7如说明书中所定义，或其药学上可接受的盐。 这些化合物具有AT1受体拮抗剂活性和neprilysin抑制活性。 本发明还涉及包含这些化合物的药物组合物; 使用这些化合物的方法; 以及制备这些化合物的方法和中间体。
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