公开(公告)号：US11851443B2

公开(公告)日：2023-12-26

申请号：US17579457

申请日：2022-01-19

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Roland Gendron ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07D498/08 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/24 ,  C07D239/34 ,  C07D241/24 ,  C07D249/04 ,  C07D249/10 ,  C07D249/18 ,  C07D257/04 ,  C07D261/20 ,  C07D263/34 ,  C07D271/06 ,  C07D277/56 ,  C07D307/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D471/04 ,  C07D498/04 ,  C07D261/18 ,  C07D207/34 ,  C07D239/36 ,  C07D413/06 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D413/12 ,  C07D213/79 ,  C07D213/80 ,  C07D237/04 ,  C07D249/08 ,  C07D249/12 ,  C07D261/12 ,  C07D263/56 ,  C07D277/46 ,  C07D333/40

CPC classification number: 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

Abstract: 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.

公开(公告)号：US11718616B2

公开(公告)日：2023-08-08

申请号：US17688001

申请日：2022-03-07

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Paul R. Fatheree ,  John R. Jacobsen ,  Anne-Marie Beausoleil ,  Gary E. L. Brandt ,  Melissa Fleury ,  Lan Jiang ,  Cameron Smith ,  Steven D. E. Sullivan ,  Lori Jean Van Orden ,  Pierre-Jean Colson ,  Gene Timothy Fass ,  Miroslav Rapta ,  Noah Benjamin ,  Marta Dabros ,  Venkat R. Thalladi

IPC: A61K31/437 ,  A61K31/416 ,  A61P43/00 ,  A61P11/06 ,  A61P11/00 ,  C07D471/04

CPC classification number: C07D471/04 ,  A61K31/416 ,  A61K31/437 ,  A61P11/00 ,  A61P11/06 ,  A61P43/00

Abstract: The invention provides compounds of formula (I):




wherein X is





and the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.

公开(公告)号：US11547687B2

公开(公告)日：2023-01-10

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: A61K39/00 ,  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 ,  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.

公开(公告)号：US20210079017A1

公开(公告)日：2021-03-18

申请号：US16947214

申请日：2020-07-23

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Roland Gendron ,  Melissa Fleury ,  Adam D. Hughes

IPC: C07D498/08 ,  C07D213/81 ,  C07D231/14 ,  C07D233/26 ,  C07D233/90 ,  C07D237/24 ,  C07D239/34 ,  C07D241/24 ,  C07D249/04 ,  C07D249/10 ,  C07D249/18 ,  C07D257/04 ,  C07D261/20 ,  C07D263/34 ,  C07D271/06 ,  C07D277/56 ,  C07D307/68 ,  C07D333/70 ,  C07D401/04 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/12 ,  C07D409/06 ,  C07D471/04 ,  C07D498/04 ,  C07D261/18 ,  C07D207/34 ,  C07D239/36 ,  C07D413/06 ,  A61K31/42 ,  A61K31/422 ,  A61K31/5377 ,  A61K45/06 ,  C07D413/04 ,  C07D413/12 ,  C07D213/79 ,  C07D213/80 ,  C07D237/04 ,  C07D249/08 ,  C07D249/12 ,  C07D261/12 ,  C07D263/56 ,  C07D277/46 ,  C07D333/40

Abstract: 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.

公开(公告)号：US10829438B2

公开(公告)日：2020-11-10

申请号：US16392920

申请日：2019-04-24

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 ,  C07D257/04 ,  C07D249/04 ,  C07D249/12 ,  A61K31/41 ,  A61K31/675 ,  C07F9/6503 ,  C07D231/18 ,  C07D253/08 ,  C07C271/22 ,  C07D207/26 ,  C07D263/38 ,  A61K31/42 ,  A61K31/4196

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.

公开(公告)号：US20200281900A1

公开(公告)日：2020-09-10

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 ,  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.

公开(公告)号：US10752599B2

公开(公告)日：2020-08-25

申请号：US16582051

申请日：2019-09-25

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 ,  A61K31/415 ,  A61K45/06 ,  A61K9/48 ,  A61K9/00

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.

公开(公告)号：US10100049B2

公开(公告)日：2018-10-16

申请号：US15341226

申请日：2016-11-02

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Paul R. Fatheree ,  John R. Jacobsen ,  Anne-Marie Beausoleil ,  Gary E. Brandt ,  Melissa Fleury ,  Lan Jiang ,  Cameron Smith ,  Steven D. E. Sullivan ,  Lori Jean Van Orden

IPC: C07D471/04

Abstract: The invention provides compounds of formula (I): wherein X is and the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.

公开(公告)号：US20180228774A1

公开(公告)日：2018-08-16

申请号：US15841799

申请日：2017-12-14

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 ,  A61K45/06

CPC classification number: A61K31/421 ,  A61K9/4816 ,  A61K9/4825 ,  A61K45/06 ,  A61K47/12 ,  C07B2200/13 ,  C07D263/34 ,  C30B7/14 ,  C30B29/54

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：US10028960B2

公开(公告)日：2018-07-24

申请号：US15498803

申请日：2017-04-27

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Jennifer Kozak ,  Melissa Fleury ,  Paul R. Fatheree ,  Anne-Marie Beausoleil ,  Dante D. Podesto

IPC: A61K31/519 ,  C07D487/04 ,  C07D211/06 ,  C07D211/00

Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of JAK kinases. The invention also provides 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.