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公开(公告)号：US09682052B2
公开(公告)日：2017-06-20
申请号：US14838842
申请日：2015-08-28
IPC分类号： A01N37/00 , A61K31/21 , A61K31/197 , C07C271/22 , C07D317/40 , C07C231/02 , C07C233/56 , C07C243/30 , C07D319/06 , C07D207/263 , A61K31/24 , A61K31/27 , A61K31/365 , A61K45/06 , C07C243/28 , C07C243/26 , A61K31/167 , A61K31/165 , A61K31/16 , A61K31/166 , A61K31/164
CPC分类号： A61K31/197 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/24 , A61K31/27 , A61K31/365 , A61K45/06 , C07C231/02 , C07C233/56 , C07C243/26 , C07C243/28 , C07C243/30 , C07C271/22 , C07D207/263 , C07D317/40 , C07D319/06
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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公开(公告)号：US09499487B2
公开(公告)日：2016-11-22
申请号：US13475076
申请日：2012-05-18
申请人： Melissa Fleury , Roland Gendron , Adam D. Hughes , Jane Schmidt
发明人： Melissa Fleury , Roland Gendron , Adam D. Hughes , Jane Schmidt
IPC分类号： A61K31/565 , A61K31/4418 , C07D261/18 , A61K31/42 , C07D213/81 , C07D237/04 , C07D237/24 , C07D239/28 , C07D241/24 , C07D249/04 , C07D249/10 , C07D249/18 , C07D263/34 , C07D307/68 , C07D333/38 , C07D401/06 , C07D471/04 , C07D487/04 , C07D498/04
CPC分类号： C07D261/18 , A01N47/16 , A61K31/4196 , A61K31/42 , A61K31/4355 , A61K31/437 , A61K45/06 , A61K47/55 , A61K47/6895 , C07D213/81 , C07D237/04 , C07D237/24 , C07D239/28 , C07D241/24 , C07D249/04 , C07D249/10 , C07D249/18 , C07D263/34 , C07D307/68 , C07D333/38 , C07D401/06 , C07D471/04 , C07D487/04 , C07D498/04 , C09K15/30
摘要： In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have 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：US09120758B2
公开(公告)日：2015-09-01
申请号：US14024974
申请日：2013-09-12
申请人： Cameron Smith , Melissa Fleury , Roland Gendron , Ryan Hudson , Adam D. Hughes
发明人： Cameron Smith , Melissa Fleury , Roland Gendron , Ryan Hudson , Adam D. Hughes
IPC分类号： C07D231/14 , C07D401/06 , C07D261/18 , C07D249/10 , C07D471/04 , C07D257/04 , C07D263/34 , C07C281/02 , C07D231/20 , C07D231/22 , C07D231/40 , C07D237/24 , C07D239/36 , C07D239/54 , C07D249/04 , C07D249/12 , C07D249/18 , C07D263/38 , C07D277/56 , C07D401/04 , C07D403/04 , C07D403/06 , C07D413/04 , C07D239/28 , C07D239/34 , C07D239/52
CPC分类号： C07D471/04 , A61K31/41 , A61K31/415 , A61K31/4155 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/421 , A61K31/422 , A61K31/426 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/497 , A61K31/50 , A61K31/505 , A61K31/5377 , C07C281/02 , C07D231/14 , C07D231/20 , C07D231/22 , C07D231/40 , C07D237/14 , C07D237/24 , C07D239/28 , C07D239/34 , C07D239/36 , C07D239/52 , C07D239/54 , C07D249/04 , C07D249/10 , C07D249/12 , C07D249/18 , C07D257/04 , C07D261/12 , C07D261/18 , C07D263/32 , C07D263/34 , C07D263/38 , C07D277/34 , C07D277/56 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D413/04 , Y02P20/55
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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公开(公告)号：US20150191435A1
公开(公告)日：2015-07-09
申请号：US14662722
申请日：2015-03-19
IPC分类号： C07D233/70 , A61K45/06 , A61K31/417
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：US08853427B2
公开(公告)日：2014-10-07
申请号：US13908619
申请日：2013-06-03
申请人： Melissa Fleury , Roland Gendron , Adam D. Hughes
发明人： Melissa Fleury , Roland Gendron , Adam D. Hughes
IPC分类号： C07C229/34 , C07C271/22 , C07D231/14 , C07D231/18 , C07D233/70 , C07D235/08 , C07D237/14 , C07D239/34 , C07D249/04 , C07D249/10 , C07D249/12 , C07D249/18 , C07D261/12 , C07D263/18 , C07D309/40 , C07D401/04 , C07D405/12 , C07D471/04 , C07D319/06
CPC分类号： A61K31/675 , A61K31/351 , A61K31/415 , A61K31/4155 , A61K31/4164 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/437 , A61K31/4439 , A61K31/454 , A61K31/50 , A61K31/505 , A61K31/5377 , A61K45/06 , C07B2200/07 , C07C229/34 , C07C271/22 , C07D231/14 , C07D231/18 , C07D231/20 , C07D233/70 , C07D233/90 , C07D235/08 , C07D237/14 , C07D239/34 , C07D239/36 , C07D249/04 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/18 , C07D261/12 , C07D263/18 , C07D295/10 , C07D309/32 , C07D309/40 , C07D319/06 , C07D401/04 , C07D401/06 , C07D403/06 , C07D403/12 , C07D405/12 , C07D405/14 , C07D471/04 , C07F9/6518
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, Z, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes 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R 1 -R 6，a，b，Z和X如说明书中所定义，或其药学上可接受的盐。 这些化合物具有去血清抑制活性。 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：US20140107120A1
公开(公告)日：2014-04-17
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： A61K31/4184 , A61K45/06 , A61K31/4439 , C07D405/10 , A61K31/5377 , C07D401/12 , C07D235/08 , C07D403/10
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：US08691868B2
公开(公告)日：2014-04-08
申请号：US13666538
申请日：2012-11-01
CPC分类号： A61K31/197 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/166 , A61K31/167 , A61K31/24 , A61K31/27 , A61K31/365 , A61K45/06 , C07C231/02 , C07C233/56 , C07C243/26 , C07C243/28 , C07C243/30 , C07C271/22 , C07D207/263 , C07D317/40 , C07D319/06
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and Z are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes 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R 1 -R 6，a，b和Z如说明书中所定义，或其药学上可接受的盐。 这些化合物具有去血清抑制活性。 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：US08686184B2
公开(公告)日：2014-04-01
申请号：US13475017
申请日：2012-05-18
申请人： Melissa Fleury , Roland Gendron , Adam D. Hughes , Jane Schmidt
发明人： Melissa Fleury , Roland Gendron , Adam D. Hughes , Jane Schmidt
IPC分类号： C07C229/34 , A61K31/185 , A61K31/195
CPC分类号： C07D231/26 , C07C231/02 , C07C233/87 , C07D207/327 , C07D207/333 , C07D213/56 , C07D213/79 , C07D213/80 , C07D213/81 , C07D213/82 , C07D231/22 , C07D233/61 , C07D257/04 , C07D295/155 , C07D333/38 , C07D495/02
摘要： In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, a, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have 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R1，R2，R3，a，R4，R5和R6如说明书中所定义，或其药学上可接受的盐。 这些化合物具有去血清抑制活性。 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：US08586536B2
公开(公告)日：2013-11-19
申请号：US13325425
申请日：2011-12-14
申请人： Roland Gendron , Melissa Fleury , Adam D. Hughes
发明人： Roland Gendron , Melissa Fleury , Adam D. Hughes
IPC分类号： C07D213/81 , C07D231/14 , C07D233/26 , C07D233/90 , C07D237/24 , C07D239/34 , C07D241/24 , C07D249/04 , C07D257/04 , C07D261/20 , C07D263/34 , C07D498/08
CPC分类号： C07D498/08 , A61K31/42 , A61K31/422 , A61K31/5377 , A61K45/06 , C07D207/34 , C07D213/79 , C07D213/80 , C07D213/81 , C07D231/14 , C07D233/26 , C07D233/90 , C07D237/04 , C07D237/24 , C07D239/34 , C07D239/36 , C07D241/24 , C07D249/04 , C07D249/08 , C07D249/10 , C07D249/12 , C07D249/18 , C07D257/04 , C07D261/12 , C07D261/18 , C07D261/20 , C07D263/34 , C07D263/56 , C07D271/06 , C07D277/46 , C07D277/56 , C07D307/68 , C07D333/40 , C07D333/70 , C07D401/04 , C07D401/06 , C07D403/04 , C07D403/06 , C07D405/12 , C07D409/06 , C07D413/04 , C07D413/06 , C07D413/12 , C07D471/04 , C07D498/04
摘要： In one aspect, the invention relates to compounds having the formula: where R1-R6, a, b, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.
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10.发明授权Dual-acting benzyl triazole antihypertensive agents having angiotensin II type receptor antagonist activity and neprilysin-inhibition activity 有权具有血管紧张素II型受体拮抗剂活性和去甲肾上腺素抑制活性的双作用苄基三唑抗高血压药公开(公告)号：US08569351B2
公开(公告)日：2013-10-29
申请号：US13692538
申请日：2012-12-03
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： A61K31/41 , 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, X, R3, 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，X，R 3和R 5-7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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