公开(公告)号：US11780852B2

公开(公告)日：2023-10-10

申请号：US17248832

申请日：2021-02-10

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Jennifer Kozak ,  Dante D. Podesto ,  Xiaojun Huang ,  Venkat R. Thalladi

IPC: A61K31/4375 ,  C07D471/04 ,  C07D519/00 ,  A61K31/46 ,  A61K45/06

CPC classification number: C07D519/00 ,  A61K31/46 ,  A61K45/06 ,  C07B2200/13

Abstract: Disclosed are methods for treating Crohn's disease using a compound of the formula:




or a pharmaceutically-acceptable salt thereof.

公开(公告)号：US20220112219A1

公开(公告)日：2022-04-14

申请号：US17450199

申请日：2021-10-07

Applicant: Janssen Biotech, Inc. ,  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 ,  B01J31/22 ,  B01J31/18

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：US20210179637A1

公开(公告)日：2021-06-17

申请号：US17248832

申请日：2021-02-10

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Jennifer Kozak ,  Dante D. Podesto ,  Xiaojun Huang ,  Venkat R. Thalladi

IPC: C07D519/00 ,  A61K31/46 ,  A61K45/06

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 inflammatory bowel diseases, and processes and intermediates useful for preparing such compounds.

公开(公告)号：US20200046709A1

公开(公告)日：2020-02-13

申请号：US16656927

申请日：2019-10-18

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

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

IPC: A61K31/519 ,  C07D487/04 ,  C07D211/06 ,  C07D211/00 ,  C07D451/14 ,  C07D451/04

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.

公开(公告)号：US20180303836A1

公开(公告)日：2018-10-25

申请号：US16014233

申请日：2018-06-21

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Xiaojun Huang

IPC: A61K31/519 ,  C07D211/00 ,  C07D487/04 ,  C07D451/04 ,  C07D451/14 ,  C07D211/06

CPC classification number: A61K31/519 ,  C07D211/00 ,  C07D211/06 ,  C07D451/04 ,  C07D451/14 ,  C07D487/04

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.

公开(公告)号：US20160347772A1

公开(公告)日：2016-12-01

申请号：US15165126

申请日：2016-05-26

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Jennifer Kozak ,  Paul R. Fatheree ,  Dante D. Podesto ,  Gary E.L. Brandt ,  Melissa Fleury ,  Anne-Marie Beausoleil ,  Xiaojun Huang ,  Venkat R. Thalladi

IPC: C07D519/00

CPC classification number: C07D519/00 ,  A61K31/46 ,  A61K45/06 ,  C07B2200/13

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 inflammatory bowel diseases, and processes and intermediates useful for preparing such compounds.

Abstract translation: 其中所述变量在说明书中或其可药用盐作为JAK激酶抑制剂定义。 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炎症性肠病的方法，以及可用于制备这些化合物的方法和中间体。

公开(公告)号：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：US11110095B2

公开(公告)日：2021-09-07

申请号：US16656927

申请日：2019-10-18

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

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

IPC: A61K31/519 ,  C07D451/04 ,  C07D451/14 ,  C07D211/00 ,  C07D211/06 ,  C07D487/04

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.

公开(公告)号：US20200040010A1

公开(公告)日：2020-02-06

申请号：US16599434

申请日：2019-10-11

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Ryan Hudson ,  Jennifer Kozak ,  Dante D. Podesto ,  Xiaojun Huang ,  Venkat R. Thalladi

IPC: C07D519/00 ,  A61K45/06 ,  A61K31/46

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 inflammatory bowel diseases, and processes and intermediates useful for preparing such compounds.

公开(公告)号：US10072026B2

公开(公告)日：2018-09-11

申请号：US15631220

申请日：2017-06-23

Applicant: THERAVANCE BIOPHARMA R&D IP, LLC

Inventor： Xiaojun Huang ,  Venkat R. Thalladi

IPC: A61K31/4375 ,  C07D471/04 ,  C07D519/00 ,  A61K31/46 ,  A61K45/06

CPC classification number: C07D519/00 ,  A61K31/46 ,  A61K45/06 ,  C07B2200/13

Abstract: The invention provides a crystalline form of the compound of formula: that is an inhibitor of JAK kinases. The invention also provides pharmaceutical compositions comprising such crystalline form and methods of using such crystalline form in mammals suffering from inflammatory bowel diseases.