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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：US07777077B2
公开(公告)日：2010-08-17
申请号：US12012161
申请日：2008-01-31
申请人： Seok-Ki Choi , Paul R. Fatheree , Ryan Hudson , Keith Jendza , Robert M. McKinnell , Vivek Sasikumar
发明人： Seok-Ki Choi , Paul R. Fatheree , Ryan Hudson , Keith Jendza , Robert M. McKinnell , Vivek Sasikumar
IPC分类号： C07C239/00 , C07D257/00
CPC分类号： C07C237/20 , C07C243/32 , C07C319/12 , C07C323/22 , C07C323/41 , C07C323/60 , C07C2601/14 , C07D257/04
摘要： The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I 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 a process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及式I化合物：其中Ar，r，R 3，X和R 5-7如说明书中所定义，及其药学上可接受的盐。 式I的化合物具有AT1受体拮抗剂活性和去皮质激素抑制活性。 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：US20080188533A1
公开(公告)日：2008-08-07
申请号：US12012161
申请日：2008-01-31
申请人： Seok-Ki Choi , Paul R. Fatheree , Sharath Hegde , Ryan Hudson , Keith Jendza , Daniel Marquess , Robert M. McKinnel , Vivek Sasikumar
发明人： Seok-Ki Choi , Paul R. Fatheree , Sharath Hegde , Ryan Hudson , Keith Jendza , Daniel Marquess , Robert M. McKinnel , Vivek Sasikumar
IPC分类号： A61K31/41 , C07C233/51 , A61K31/165 , A61P9/12 , G01N33/566 , C07D257/04
CPC分类号： C07C237/20 , C07C243/32 , C07C319/12 , C07C323/22 , C07C323/41 , C07C323/60 , C07C2601/14 , C07D257/04
摘要： The invention is directed to compounds of formula I: wherein Ar, r, R3, X, and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. The compounds of formula I 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 a process and intermediates for preparing such compounds.
摘要翻译： 本发明涉及式I化合物：其中Ar，r，R 3，X和R 5-7如说明书中所定义，和药学上可接受的盐 其中。 式I的化合物具有AT 1受体拮抗剂活性和尿丙氨酸抑制活性。 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：US20140194426A1
公开(公告)日：2014-07-10
申请号：US14062004
申请日：2013-10-24
IPC分类号： C07D413/14 , C07D263/34 , C07D413/12 , C07D413/10
CPC分类号： C07D263/34 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5377 , C07D263/38 , C07D413/10 , C07D413/12 , C07D413/14
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中：Ar，Z，R 3，R 4和R 5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。 另一方面，本发明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：US08350027B2
公开(公告)日：2013-01-08
申请号：US13346237
申请日：2012-01-09
申请人： Brooke Blair , Paul R. Fatheree , Melissa Fleury , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Michael Wilson
发明人： Brooke Blair , Paul R. Fatheree , Melissa Fleury , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Michael Wilson
IPC分类号： C07D413/14 , C07D401/14 , C07D259/00 , C07D271/06 , C07D231/10
CPC分类号： C07D403/10 , C07D231/12 , C07D231/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/10
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中：Ar，Z，R 3，R 4和R 5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。 另一方面，本发明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：US20130245041A1
公开(公告)日：2013-09-19
申请号：US13685128
申请日：2012-11-26
申请人： Brooke Blair , Paul R. Fatheree , Melissa Fleury , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Michael Wilson
发明人： Brooke Blair , Paul R. Fatheree , Melissa Fleury , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Michael Wilson
IPC分类号： C07D403/10 , C07D403/06 , C07D401/06 , C07D231/12 , C07D401/14
CPC分类号： C07D403/10 , C07D231/12 , C07D231/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/10
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中：Ar，Z，R 3，R 4和R 5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。 另一方面，本发明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：US20110009409A1
公开(公告)日：2011-01-13
申请号：US12829667
申请日：2010-07-02
申请人： Brooke Blair , Paul R. Fatheree , Melissa Fleury , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Michael Wilson
发明人： Brooke Blair , Paul R. Fatheree , Melissa Fleury , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Michael Wilson
IPC分类号： A61K31/5377 , C07D257/04 , A61K31/41 , C07D231/20 , A61K31/415 , C07D401/12 , A61K31/4439 , C07D413/12 , A61K31/422 , C07D403/14 , A61K31/497 , A61P3/10 , A61P3/06 , A61P7/02 , A61P13/12 , A61P29/00 , A61P9/12
CPC分类号： C07D403/10 , C07D231/12 , C07D231/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/10
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中：Ar，Z，R 3，R 4和R 5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。 另一方面，本发明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：US08598170B2
公开(公告)日：2013-12-03
申请号：US13682299
申请日：2012-11-20
IPC分类号： A61K31/422 , A61K31/4439 , A61K31/5377 , A61K31/4245 , A61K31/497 , A61K31/506 , A61K31/421
CPC分类号： C07D263/34 , A61K31/421 , A61K31/422 , A61K31/4245 , A61K31/4439 , A61K31/497 , A61K31/506 , A61K31/5377 , C07D263/38 , C07D413/10 , C07D413/12 , C07D413/14
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates 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：US08119634B2
公开(公告)日：2012-02-21
申请号：US12984070
申请日：2011-01-04
申请人： Brooke Blair , Paul R. Fatheree , Melissa Fleury , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Michael Wilson
发明人： Brooke Blair , Paul R. Fatheree , Melissa Fleury , Roland Gendron , Ryan Hudson , Robert Murray McKinnell , Michael Wilson
IPC分类号： A61K31/5377 , A61K31/44 , A61K31/4155 , A61K31/41 , A61K31/415 , A61K31/4245
CPC分类号： C07D403/10 , C07D231/12 , C07D231/14 , C07D401/06 , C07D401/14 , C07D403/06 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/10
摘要： In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
摘要翻译： 一方面，本发明涉及具有下式的化合物：其中：Ar，Z，R 3，R 4和R 5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。 另一方面，本发明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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