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![(2R,4R)-5-(5'-CHLORO-2'-FLUOROBIPHENYL-4-YL)-2-HYDROXY-4-[(5-METHYLOXAZOLE-2-CARBONYL)AMINO]PENTANOIC ACID](/abs-image/US/2021/12/30/US20210401808A1/abs.jpg.150x150.jpg)
公开(公告)号：US20210401808A1
公开(公告)日：2021-12-30
申请号：US17302877
申请日：2021-05-14
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Melissa Fleury , Adam D. Hughes , Anne-Marie Beausoleil , Erik Fenster , Venkat R. Thalladi , Miroslav Rapta
IPC: A61K31/421 , A61K9/48 , A61K47/12 , C07D263/34 , C30B7/14 , C30B29/54 , A61K45/06
Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
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公开(公告)号：US10123984B2
公开(公告)日：2018-11-13
申请号：US15593833
申请日：2017-05-12
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Adam D. Hughes , Erik Fenster , Melissa Fleury , Roland Gendron , Edmund J. Moran
IPC: 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
Abstract: 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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3.发明申请公开(公告)号：US20170355665A1
公开(公告)日：2017-12-14
申请号：US15581347
申请日：2017-04-28
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Adam D. Hughes , Erik Fenster , Melissa Fleury , Anne-Marie Beausoleil , Venkat R. Thalladi , Jerry Nzerem , Miroslav Rapta
IPC: C07C235/74
CPC classification number: C07C235/74 , A61K9/0019 , A61K9/0075 , A61K9/0078 , A61K9/008 , A61K9/0095 , A61K9/10 , A61K9/19 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K9/4866 , A61K31/216 , A61K45/06 , C07B2200/13 , C07C233/56 , A61K2300/00
Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
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4.发明申请公开(公告)号：US20170088508A1
公开(公告)日：2017-03-30
申请号：US15229398
申请日：2016-08-05
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Adam D. Hughes , Erik Fenster , Melissa Fleury , Anne-Marie Beausoleil , Venkat R. Thalladi , Jerry Nzerem , Miroslav Rapta
IPC: C07C235/74
CPC classification number: C07C235/74 , A61K9/0019 , A61K9/0075 , A61K9/0078 , A61K9/008 , A61K9/0095 , A61K9/10 , A61K9/19 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K9/4866 , A61K31/216 , A61K45/06 , C07B2200/13 , C07C233/56 , A61K2300/00
Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
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5.发明授权(2S,4R)-5-(5′-chloro-2′-fluorobiphenyl-4-yl)-4-(ethoxyoxalylamino)-2-hydroxymethyl-2-methylpentanoic acid 有权（2S，4R）-5-（5'-氯-2'-氟联苯-4-基）-4-（乙氧基草酰氨基）-2-羟甲基-2-甲基戊酸公开(公告)号：US09433598B2
公开(公告)日：2016-09-06
申请号：US15040481
申请日：2016-02-10
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Adam D. Hughes , Erik Fenster , Melissa Fleury , Anne-Marie Beausoleil , Venkat R. Thalladi , Jerry Nzerem , Miroslav Rapta
IPC: A61K31/216 , A61K9/08 , C07C231/24 , C07C231/12 , A61K45/06 , A61K9/00 , C07C235/74 , C07C231/14
CPC classification number: C07C235/74 , A61K9/0019 , A61K9/0075 , A61K9/0078 , A61K9/008 , A61K9/0095 , A61K9/10 , A61K9/19 , A61K9/2054 , A61K9/2059 , A61K9/4858 , A61K9/4866 , A61K31/216 , A61K45/06 , C07B2200/13 , C07C233/56 , A61K2300/00
Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
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Patent Agency Ranking
![(2R,4R)-5-(5′-chloro-2′-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid](/abs-image/US/2023/05/09/US11642332B2/abs.jpg.150x150.jpg)
公开(公告)号：US11642332B2
公开(公告)日：2023-05-09
申请号：US17302877
申请日：2021-05-14
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Melissa Fleury , Adam D. Hughes , Anne-Marie Beausoleil , Erik Fenster , Venkat R. Thalladi , Miroslav Rapta
IPC: A61K31/421 , A61K9/48 , A61K47/12 , C07D263/34 , C30B7/14 , C30B29/54 , A61K45/06
CPC classification number: A61K31/421 , A61K9/4816 , A61K9/4825 , A61K45/06 , A61K47/12 , C07D263/34 , C30B7/14 , C30B29/54 , C07B2200/13
Abstract: In one aspect, the invention relates to a compound of the structure:
or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.-
![(2R,4R)-5-(5′-chloro-2′-fluorobiphenyl-4-yl)-2-hydroxy-4-[(5-methyloxazole-2-carbonyl)amino]pentanoic acid](/abs-image/US/2021/06/15/US11033533B2/abs.jpg.150x150.jpg)
公开(公告)号：US11033533B2
公开(公告)日：2021-06-15
申请号：US16715722
申请日：2019-12-16
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Melissa Fleury , Adam D. Hughes , Anne-Marie Beausoleil , Erik Fenster , Venkat R. Thalladi , Miroslav Rapta
IPC: A61K31/421 , C07D263/34 , C30B7/14 , C30B29/54 , A61K9/48 , A61K47/12 , A61K45/06
Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
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公开(公告)号：US20210059966A1
公开(公告)日：2021-03-04
申请号：US16923396
申请日：2020-07-08
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Adam D. Hughes , Erik Fenster , Melissa Fleury , Roland Gendron , Edmund J. Moran
IPC: A61K31/197 , C07C243/26 , C07C271/22 , C07D317/40 , C07C231/02 , C07D319/06 , C07D207/263 , C07C233/56 , C07C243/30 , A61K31/24 , A61K31/27 , A61K31/365 , A61K45/06 , C07C243/28
Abstract: 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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![(2R,4R)-5-(5'-CHLORO-2'-FLUOROBIPHENYL-4-YL)-2-HYDROXY-4-[(5-METHYLOXAZOLE-2-CARBONYL)AMINO]PENTANOIC ACID](/abs-image/US/2019/09/05/US20190269659A1/abs.jpg.150x150.jpg)
9.发明申请公开(公告)号：US20190269659A1
公开(公告)日：2019-09-05
申请号：US16207501
申请日：2018-12-03
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Melissa Fleury , Adam D. Hughes , Anne-Marie Beausoleil , Erik Fenster , Venkat R. Thalladi , Miroslav Rapta
IPC: A61K31/421 , C30B29/54 , A61K9/48 , A61K47/12 , C07D263/34 , C30B7/14 , A61K45/06
Abstract: In one aspect, the invention relates to a compound of the structure: or a pharmaceutically acceptable salt thereof, and a crystalline form of this compound, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this compound; methods of using this compound; and processes for preparing this compound.
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公开(公告)号：US10392368B2
公开(公告)日：2019-08-27
申请号：US16050227
申请日：2018-07-31
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Erik Fenster , Tom M. Lam , Mandy Loo , Robert Murray McKinnell , Anthony Francesco Palermo , Diana Jin Wang , Breena Fraga , Jerry Nzerem , Marta Dabros , Venkat R. Thalladi , Miroslav Rapta
IPC: A61P1/00 , A61P17/00 , A61P29/00 , A61P35/00 , C07D401/12 , C07D403/12 , C07D413/12 , C07D471/04 , C07D487/04
Abstract: The invention provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.
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