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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/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.-
公开(公告)号：US11634413B2
公开(公告)日：2023-04-25
申请号：US17445096
申请日：2021-08-16
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Melissa Fleury , Adam D. Hughes
IPC: C07D405/12 , A61K31/415 , A61K31/4192 , A61K31/42 , A61K31/421 , C07D231/14 , C07D231/20 , C07D249/04 , C07D261/18 , C07D263/38 , A61K45/06
Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these 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/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：US20210155576A1
公开(公告)日：2021-05-27
申请号：US16948872
申请日：2020-10-05
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Melissa Fleury , Adam D. Hughes
IPC: C07C229/22 , C07D249/18 , A61K31/4192 , A61K45/06 , C07D231/20 , A61K31/415 , C07D405/12 , A61K31/4155 , A61K31/4439 , C07D401/04 , C07D405/14 , C07D231/14 , C07D261/18 , A61K31/42 , C07D249/04 , C07D249/12 , A61K31/4196 , C07D257/04 , A61K31/41 , A61K31/675 , C07F9/6503 , C07D231/18 , C07D253/08 , C07C271/22 , C07D207/26 , C07D263/38
Abstract: In one aspect, the invention relates to compounds having the formula XII: where Ra, Rb, R2, R7, and X are as defined in the specification, or a pharmaceutically acceptable salt thereof. The compounds described herein are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
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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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Patent Agency Ranking
公开(公告)号：US10570120B2
公开(公告)日：2020-02-25
申请号：US16209112
申请日：2018-12-04
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Melissa Fleury , Adam D. Hughes
IPC: C07D405/12 , C07D231/14 , C07D249/04 , C07D261/18 , C07D263/38 , A61K31/415 , A61K31/42 , A61K45/06 , C07D231/20 , A61K31/4192 , A61K31/421
Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
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![Crystalline(2S,4R)-5-(5′-chloro-2′-fluoro-[1,1′-bipheny]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof](/abs-image/US/2019/11/12/US10472335B2/abs.jpg.150x150.jpg)
公开(公告)号：US10472335B2
公开(公告)日：2019-11-12
申请号：US16125991
申请日：2018-09-10
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Adam D. Hughes , Melissa Fleury , Miroslav Rapta , Venkat R. Thalladi , R. Michael Baldwin , David L. Bourdet
IPC: C07D261/18 , A61K9/00 , A61K31/415 , A61K9/48 , A61K45/06
Abstract: In one aspect, the invention relates to a crystalline form of the structure: or a pharmaceutically acceptable salt thereof, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this crystalline form; methods of using this crystalline form and its soluble form (I); and processes for preparing soluble (I) and crystalline (I′) forms.
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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)
8.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：US10189823B2
公开(公告)日：2019-01-29
申请号：US15841749
申请日：2017-12-14
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Melissa Fleury , Adam D. Hughes
IPC: C07D405/12 , C07D231/20 , A61K31/4192 , A61K31/421 , A61K31/42 , A61K45/06 , A61K31/415 , C07D231/14 , C07D249/04 , C07D261/18 , C07D263/38
Abstract: In one aspect, the invention relates to compounds having the formula: where X, Ra, Rb, R2, and R7 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are prodrugs of compounds having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.
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![Crystalline(2S,4R)-5-(5′-chloro-2′-fluoro-[1,1′-biphenyl]-4-yl)-2-(ethoxymethyl)-4-(3-hydroxyisoxazole-5-carboxamido)-2-methylpentanoic acid and uses thereof](/abs-image/US/2018/10/16/US10100021B2/abs.jpg.150x150.jpg)
公开(公告)号：US10100021B2
公开(公告)日：2018-10-16
申请号：US15452333
申请日：2017-03-07
Applicant: THERAVANCE BIOPHARMA R&D IP, LLC
Inventor： Adam D. Hughes , Melissa Fleury , Miroslav Rapta , Venkat R. Thalladi , Gene Timothy Fass , Michael Simeone
IPC: C07D261/18 , A61K9/48 , A61K9/00 , A61K31/415 , A61K45/06
Abstract: In one aspect, the invention relates to a crystalline form of the structure: or a pharmaceutically acceptable salt thereof, having neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising this crystalline form; methods of using this crystalline form and its soluble form (I); and processes for preparing soluble (I) and crystalline (I′) forms.
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