公开(公告)号：US11878977B2

公开(公告)日：2024-01-23

申请号：US17885475

申请日：2022-08-10

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Paul R. Fatheree ,  Gary E. L. Brandt ,  Cameron Smith ,  Steven D. E. Sullivan ,  Lori Jean Van Orden ,  Melanie A. Kleinschek ,  Glenn D. Crater

IPC: C07D471/04 ,  C07D519/00 ,  A61P11/06 ,  A61P11/00 ,  A61K31/437

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61P11/00 ,  A61P11/06 ,  C07D519/00

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




which contain a 4-membered heterocyclic amide, where 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：US20230322774A1

公开(公告)日：2023-10-12

申请号：US18181138

申请日：2023-03-09

Applicant: Theravance Biopharma R&D IP, LLC

Inventor： Daniel D. Long ,  Cameron Smith ,  Corbin Thompson

IPC: C07D471/04

CPC classification number: C07D471/04

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




where 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 and methods of using such compounds to treat respiratory diseases.

公开(公告)号：US10550118B2

公开(公告)日：2020-02-04

申请号：US16511410

申请日：2019-07-15

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Paul R. Fatheree ,  Gary E. L. Brandt ,  Cameron Smith ,  Steven D. E. Sullivan ,  Lori Jean Van Orden ,  Melanie A. Kleinschek ,  Glenn D. Crater

IPC: A61P11/00 ,  A61P11/06 ,  C07D471/04 ,  C07D519/00

Abstract: The invention provides compounds of formula (I): which contain a 4-membered heterocyclic amide, where 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：US10208040B2

公开(公告)日：2019-02-19

申请号：US15915434

申请日：2018-03-08

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Paul R. Fatheree ,  Gary E. L. Brandt ,  Cameron Smith ,  Steven D. E. Sullivan ,  Lori Jean Van Orden ,  Melanie A. Kleinschek ,  Glenn D. Crater

IPC: C07D471/04 ,  C07D519/00 ,  A61P11/06 ,  A61P11/00

Abstract: The invention provides compounds of formula (I): where 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：US09725448B2

公开(公告)日：2017-08-08

申请号：US15270187

申请日：2016-09-20

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

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

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/42 ,  C07D239/34 ,  A61K31/505 ,  C07D231/14 ,  A61K31/415 ,  C07D231/20 ,  C07D249/04 ,  A61K31/4192 ,  C07D249/10 ,  A61K31/4196 ,  C07D249/18 ,  A61K31/437 ,  C07D261/18 ,  C07D239/36 ,  C07D257/04 ,  C07D261/12 ,  C07D403/04 ,  C07C271/22 ,  C07C243/28 ,  C07D487/04

CPC classification number: 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

Abstract: 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.

公开(公告)号：US20170217959A1

公开(公告)日：2017-08-03

申请号：US15379188

申请日：2016-12-14

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Cameron Smith ,  Ryan Hudson ,  Adam D. Hughes

IPC: C07D471/04 ,  A61K31/415 ,  A61K31/4155 ,  C07D401/06 ,  A61K31/454 ,  A61K31/5377 ,  C07D261/12 ,  A61K31/42 ,  C07D249/10 ,  A61K31/4196 ,  C07D249/04 ,  A61K31/4192 ,  A61K31/437 ,  C07D249/18 ,  C07D257/04 ,  A61K31/41 ,  C07D401/04 ,  A61K31/4439 ,  C07D403/04 ,  A61K31/497 ,  C07D263/32 ,  A61K31/421 ,  C07D239/34 ,  A61K31/505 ,  C07D277/34 ,  A61K31/426 ,  C07D237/14 ,  A61K31/50 ,  C07D231/14

CPC classification number: 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

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：US20170066764A1

公开(公告)日：2017-03-09

申请号：US15270187

申请日：2016-09-20

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

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

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/42 ,  C07D239/34 ,  A61K31/505 ,  C07D231/14 ,  A61K31/415 ,  C07D231/20 ,  C07D249/04 ,  A61K31/4192 ,  C07D249/10 ,  A61K31/4196 ,  C07D249/18 ,  A61K31/437 ,  C07D261/18

CPC classification number: 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

Abstract: 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.

Abstract translation: 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。

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：US11713315B2

公开(公告)日：2023-08-01

申请号：US16949067

申请日：2020-10-13

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Daniel D. Long ,  Cameron Smith ,  Corbin Thompson

IPC: C07D471/04 ,  A61K9/00 ,  A61P11/06 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K9/0073 ,  A61P11/06 ,  C07D519/00

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




where 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 and methods of using such compounds to treat respiratory diseases.

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.