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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：US08481044B2
公开(公告)日：2013-07-09
申请号：US13398015
申请日：2012-02-16
申请人： Melissa Fleury , Roland Gendron , Adam D. Hughes
发明人： Melissa Fleury , Roland Gendron , Adam D. Hughes
IPC分类号： A61K9/00 , A61K31/33 , A61K33/36 , A61P35/00 , C07C229/02 , C07C271/10
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：US08449890B2
公开(公告)日：2013-05-28
申请号：US13398027
申请日：2012-02-16
申请人： Melissa Fleury , Roland Gendron , Adam D. Hughes , Cameron Smith
发明人： Melissa Fleury , Roland Gendron , Adam D. Hughes , Cameron Smith
IPC分类号： A61K9/00 , A61K31/33 , A61K33/36 , A61P35/00 , C07C229/02 , C07C271/10
CPC分类号： C07D471/04 , A61K31/415 , A61K31/4192 , A61K31/4196 , A61K31/42 , A61K31/437 , A61K31/505 , A61K45/06 , C07C243/28 , C07C271/22 , C07C2601/02 , C07D231/14 , C07D231/20 , C07D239/34 , C07D239/36 , C07D249/04 , C07D249/10 , C07D249/18 , C07D257/04 , C07D261/12 , C07D261/18 , C07D403/04 , C07D487/04
摘要： In one aspect, the invention relates to compounds having the formula: where R1, R2a, R2b, R3-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R1，R2a，R2b，R3-R6，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：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：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：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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