公开(公告)号：US11919888B2

公开(公告)日：2024-03-05

申请号：US18173573

申请日：2023-02-23

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Melissa Fleury ,  Adam D. Hughes

IPC: C07D231/14 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/421 ,  A61K45/06 ,  C07D231/20 ,  C07D249/04 ,  C07D261/18 ,  C07D263/38 ,  C07D405/12

CPC classification number: C07D405/12 ,  A61K31/415 ,  A61K31/4192 ,  A61K31/42 ,  A61K31/421 ,  A61K45/06 ,  C07D231/14 ,  C07D231/20 ,  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.

公开(公告)号：US20240025897A1

公开(公告)日：2024-01-25

申请号：US18326732

申请日：2023-05-31

Applicant: Theravance Biopharma R&D IP, LLC

Inventor： Gene Timothy Fass

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

CPC classification number: C07D471/04 ,  A61P11/06 ,  A61K9/0053 ,  C07B2200/13

Abstract: Provided herein is a crystalline hydrate of the compound of formula 1:




Also provides herein are pharmaceutical compositions comprising such crystalline hydrate, methods of using such crystalline hydrate to treat respiratory diseases, and processes useful for preparing such crystalline hydrate.

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：US11739103B2

公开(公告)日：2023-08-29

申请号：US17450199

申请日：2021-10-07

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Norbert Kraut ,  Matteo Conza ,  Anja Huste ,  Vit Lellek ,  Bjorn Gielen ,  Christian Pater ,  Dimitar Filipov ,  Xiaojun Huang ,  Stephen Roseblade

IPC: C07D519/00 ,  B01J31/18 ,  B01J31/22

CPC classification number: C07D519/00 ,  B01J31/1805 ,  B01J31/1845 ,  B01J31/2226 ,  B01J31/2252 ,  B01J31/2295 ,  B01J2531/824

Abstract: The present disclosure provides processes for preparing a crystalline form of 3-((1R,3s,5S)-3-((7-((5-methyl-1H-pyrazol-3-yl)amino)-1,6-naphthyridin-5-yl)amino)-8-azabicyclo[3.2.1]octan-8-yl)propanenitrile and related intermediate compounds.

公开(公告)号：US11730720B2

公开(公告)日：2023-08-22

申请号：US17247225

申请日：2020-12-04

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Svitlana Kulyk ,  Christina Owens ,  Steven D. E. Sullivan ,  Jennifer Kozak ,  Adam D. Hughes

IPC: A61K31/4375 ,  A61K9/00 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/551 ,  A61K45/06 ,  C07D401/14 ,  C07D471/04 ,  C07D519/00

CPC classification number: A61K31/4375 ,  A61K9/0073 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/551 ,  A61K45/06 ,  C07D401/14 ,  C07D471/04 ,  C07D519/00

Abstract: The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.

公开(公告)号：US11718591B2

公开(公告)日：2023-08-08

申请号：US17550564

申请日：2021-12-14

Applicant: Theravance Biopharma R&D IP, LLC

Inventor： Adam D. Hughes ,  Melissa Fleury ,  Miroslav Rapta ,  Venkat R. Thalladi ,  Gene Timothy Fass ,  Michael Simeone ,  R. Michael Baldwin ,  David L. Bourdet

IPC: C07D261/18 ,  A61K9/00 ,  A61K9/48 ,  A61K31/415 ,  A61K45/06

CPC classification number: C07D261/18 ,  A61K9/0053 ,  A61K9/4816 ,  A61K31/415 ,  A61K45/06 ,  C07B2200/13

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：US20230201181A1

公开(公告)日：2023-06-29

申请号：US18115436

申请日：2023-02-28

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Lori Jean Patterson ,  Robert S. Chao ,  Miroslav Rapta

IPC: A61K31/4465 ,  C07D211/22 ,  C07D211/32

CPC classification number: A61K31/4465 ,  C07D211/22 ,  C07D211/32

Abstract: The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.

公开(公告)号：US11673879B2

公开(公告)日：2023-06-13

申请号：US17301242

申请日：2021-03-30

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Mandy Loo ,  Svitlana Kulyk ,  Christopher Bailey ,  Jennifer Kozak ,  Matthew B. Soellner ,  Adam D. Hughes

IPC: C07D401/14 ,  A61K31/506 ,  A61K9/12 ,  A61P1/16 ,  A61P9/00 ,  A61P11/00 ,  A61P35/00 ,  A61K9/00 ,  A61K45/06

CPC classification number: C07D401/14 ,  A61K9/008 ,  A61K9/0075 ,  A61K9/0078 ,  A61K45/06 ,  A61P1/16 ,  A61P9/00 ,  A61P11/00 ,  A61P35/00 ,  A61K31/506

Abstract: The present disclosure provides inhibitors of activin receptor-like kinase 5 (ALK5). Also disclosed are methods to modulate the activity of ALK5 and methods of treatment of disorders mediated by ALK5.

公开(公告)号：US11649209B2

公开(公告)日：2023-05-16

申请号：US17841567

申请日：2022-06-15

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Grahame Woollam

IPC: C07D211/62 ,  C07D401/12 ,  A61K31/4545 ,  A61K9/12 ,  A61K9/16 ,  A61K45/06

CPC classification number: C07D211/62 ,  A61K9/124 ,  A61K9/1623 ,  A61K31/4545 ,  A61K45/06 ,  C07D401/12 ,  C07B2200/13

Abstract: The invention provides two crystalline freebase forms of biphenyl-2-ylcarbamic acid 1-(2-{[4-(4-carbamoylpiperidin-1-ylmethyl)benzoyl]methylamino}ethyl)piperidin-4-yl ester. The invention also provides pharmaceutical compositions comprising the crystalline freebase or prepared using the crystalline freebases; processes and intermediates for preparing the crystalline freebases; and methods of using the crystalline freebases to treat a pulmonary disorder.