公开(公告)号：US10961267B2

公开(公告)日：2021-03-30

申请号：US16555222

申请日：2019-08-29

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Daniel D. Long ,  Donna A. A. Wilton ,  Mandy Loo ,  Patrick J. Brassil

IPC: C07H15/26 ,  A61P1/00 ,  C07D487/04 ,  C07H1/00 ,  C12P17/16

Abstract: The invention provides compounds which are prodrugs of a JAK inhibitor agent for the targeted delivery of the JAK inhibitor to the gastrointestinal tract of a mammal. The invention also provides pharmaceutical compositions comprising the compounds, methods of using the compounds to treat gastrointestinal inflammatory diseases, and processes and intermediates useful for preparing the compounds.

公开(公告)号：US09669027B2

公开(公告)日：2017-06-06

申请号：US14883856

申请日：2015-10-15

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Daniel D. Long ,  Robert Murray McKinnell ,  Lan Jiang ,  Mandy Loo ,  Kassandra Lepack ,  Lori Jean Van Orden ,  Gavin Ogawa

IPC: C07D405/14 ,  A61K31/496 ,  C07D401/14 ,  C07D413/14 ,  C07D409/14 ,  C07D491/113 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06

CPC classification number: A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K45/06 ,  C07D401/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D491/113

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 replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.

公开(公告)号：US20210179655A1

公开(公告)日：2021-06-17

申请号：US17249126

申请日：2021-02-22

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Daniel D. Long ,  Donna A.A. Wilton ,  Mandy Loo ,  Patrick J. Brassil

IPC: C07H15/26 ,  C07D487/04 ,  C07H1/00 ,  A61P1/00 ,  C12P17/16

Abstract: The invention provides compounds which are prodrugs of a JAK inhibitor agent for the targeted delivery of the JAK inhibitor to the gastrointestinal tract of a mammal. The invention also provides pharmaceutical compositions comprising the compounds, methods of using the compounds to treat gastrointestinal inflammatory diseases, and processes and intermediates useful for preparing the compounds.

公开(公告)号：US20210154179A1

公开(公告)日：2021-05-27

申请号：US16949915

申请日：2020-11-20

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Christina Owens ,  Svitlana Kulyk ,  Steven D.E. Sullivan ,  Paul Allegretti ,  Mandy Loo ,  Jennifer Kozak ,  Erik Fenster ,  Adam D. Hughes

IPC: A61K31/444 ,  A61K9/00 ,  A61K45/06 ,  C07D471/04 ,  C07D519/00 ,  C07D401/14 ,  C07D405/14 ,  C07D487/04 ,  C07D487/08 ,  C07D513/04 ,  C07D417/14 ,  C07D409/14 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/496 ,  A61K31/519 ,  A61K31/4709 ,  A61K31/4995 ,  A61P19/04 ,  A61P11/00 ,  A61P35/00

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：US11608354B2

公开(公告)日：2023-03-21

申请号：US17249126

申请日：2021-02-22

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Daniel D. Long ,  Donna A. A. Wilton ,  Mandy Loo ,  Patrick J. Brassil

IPC: C07H15/26 ,  C07H1/00 ,  C07D487/04 ,  A61P1/00 ,  C12P17/16

Abstract: The invention provides compounds which are prodrugs of a JAK inhibitor agent for the targeted delivery of the JAK inhibitor to the gastrointestinal tract of a mammal. The invention also provides pharmaceutical compositions comprising the compounds, methods of using the compounds to treat gastrointestinal inflammatory diseases, and processes and intermediates useful for preparing the compounds.

公开(公告)号：US10435428B2

公开(公告)日：2019-10-08

申请号：US15358462

申请日：2016-11-22

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Daniel D. Long ,  Donna A. A. Wilton ,  Mandy Loo ,  Patrick J. Brassil

IPC: C07H15/26 ,  C12P17/16 ,  C07D487/04 ,  C07H1/00

Abstract: The invention provides compounds which are prodrugs of a JAK inhibitor agent for the targeted delivery of the JAK inhibitor to the gastrointestinal tract of a mammal. The invention also provides pharmaceutical compositions comprising the compounds, methods of using the compounds to treat gastrointestinal inflammatory diseases, and processes and intermediates useful for preparing the compounds.

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.

公开(公告)号：US09260414B2

公开(公告)日：2016-02-16

申请号：US14539039

申请日：2014-11-12

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Robert Murray McKinnell ,  Daniel D. Long ,  Lori Jean Van Orden ,  Lan Jiang ,  Mandy Loo ,  Daisuke Roland Saito ,  Sheila Zipfel ,  Eric L. Stangeland ,  Kassandra Lepack ,  Gavin Ogawa

IPC: A61K31/496 ,  C07D401/14 ,  C07D403/14 ,  A61K45/06

CPC classification number: C07D401/14 ,  A61K31/496 ,  A61K45/06 ,  C07D403/14

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 replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.

Abstract translation: 本发明提供式（I）化合物：其中变量在说明书中定义，或其药学上可接受的盐，其是丙型肝炎病毒的复制抑制剂。 本发明还提供包含这些化合物的药物组合物，使用这些化合物治疗丙型肝炎病毒感染的方法，以及可用于制备这些化合物的方法和中间体。

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：US20220372015A1

公开(公告)日：2022-11-24

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 ,  A61P1/16 ,  A61K45/06 ,  A61P35/00 ,  A61P11/00 ,  A61P9/00 ,  A61K9/00

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.