公开(公告)号：US20230047209A1

公开(公告)日：2023-02-16

申请号：US17366923

申请日：2021-07-02

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Georgette Castanedo ,  Paul Gibbons ,  Joachim Rudolph ,  William Vernier ,  Ramsay Beveridge ,  Yao Wu ,  Guosheng Wu

IPC: C07D471/04 ,  C07D475/00

Abstract: Described herein are pyrido-pyrimidinone and pteridinone compounds or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods treating cancer, alone and in combination with other therapeutic agents.

公开(公告)号：US20220389020A1

公开(公告)日：2022-12-08

申请号：US17648045

申请日：2022-01-14

Applicant: Genentech, Inc.

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu ,  Christopher Hurley

IPC: C07D487/04 ,  A61P17/06 ,  A61P35/02 ,  A61K31/519 ,  A61P29/00

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

公开(公告)号：US20220249487A1

公开(公告)日：2022-08-11

申请号：US17643623

申请日：2021-12-10

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Georgette Castanedo ,  Paul Gibbons ,  Joachim Rudolph ,  Yao Wu ,  Guosheng Wu

IPC: A61K31/517 ,  C07D401/12 ,  C07D239/84 ,  C07D401/04 ,  C07D401/14 ,  A61K31/573 ,  A61K38/07 ,  A61K31/69 ,  A61K31/454 ,  A61K39/395 ,  C07D405/14

Abstract: Provided herein are compounds and pharmaceutically acceptable salts thereof useful in the treatment of IRE1-related diseases and disorders described herein.

公开(公告)号：US20180297997A1

公开(公告)日：2018-10-18

申请号：US16009596

申请日：2018-06-15

Applicant: Genentech, Inc.

Inventor： Yun-Xing Cheng ,  Rongbao Hua ,  Terry Kellar ,  Wei Li ,  Paul Gibbons ,  Mark Edward Zak

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

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

Abstract: Compounds of Formula (I) and methods of use as Janus kinase inhibitors are described herein.

公开(公告)号：US11795170B2

公开(公告)日：2023-10-24

申请号：US17027352

申请日：2020-09-21

Applicant: Genentech, Inc.

Inventor： Mark Zak ,  Terry Kellar ,  Paul Gibbons

IPC: C07D487/04 ,  A61P11/06

CPC classification number: C07D487/04 ,  A61P11/06

Abstract: Compounds of Formula (I):




salts thereof and methods of making and use as Janus kinase inhibitors are described herein.

公开(公告)号：US20230057166A1

公开(公告)日：2023-02-23

申请号：US17275606

申请日：2019-09-12

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Cuong Q. Ly ,  Georgette Castanedo ,  Paul Gibbons ,  Wendy Lee ,  Joachim Rudolph ,  Nicole Alice Blaquiere ,  Jacob Bradley Schwarz ,  Ramsay Beveridge ,  Jean-Philippe Leclerc ,  Alexandre Lemire ,  Leo Fu

IPC: C07D401/14 ,  C07D401/04 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08 ,  A61K45/06

Abstract: Described herein are phenoxy-pyridyl-pyrimidine compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula I structure or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US20200165260A1

公开(公告)日：2020-05-28

申请号：US16777049

申请日：2020-01-30

Applicant: Genentech, Inc.

Inventor： Yun-Xing Cheng ,  Paul Gibbons ,  Terry Kellar ,  Wei Li ,  Rohan Mendonca ,  Po-wai Yuen ,  Mark Edward Zak ,  Lei Zhang

IPC: C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and salts thereof, wherein R1, R2 R3, R4 and n are defined herein, are useful as inhibitors of one or more Janus kinases. Also provided are pharmaceutical compositions that include a compound of Formula (00A) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.

公开(公告)号：US20170283424A1

公开(公告)日：2017-10-05

申请号：US15627847

申请日：2017-06-20

Applicant: Genentech, Inc.

Inventor： Paul Gibbons ,  Emily Hanan ,  Wendy Liu ,  Joseph P. Lyssikatos ,  Steven R. Magnuson ,  Rohan Mendonca ,  Richard Pastor ,  Thomas E. Rawson ,  Michael Siu ,  Mark E. Zak ,  Aihe Zhou ,  Bing-Yan Zhu ,  Christopher Hurley

IPC: C07D487/04

CPC classification number: C07D487/04 ,  A61K31/519 ,  A61P17/06 ,  A61P29/00 ,  A61P35/02

Abstract: A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2 and R3 are defined herein, are useful as inhibitors of one or more Janus kinases. A pharmaceutical composition that includes a compound of Formula I and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient are disclosed.

公开(公告)号：US12071425B2

公开(公告)日：2024-08-27

申请号：US17275606

申请日：2019-09-12

Applicant: Genentech, Inc.

Inventor： Marie-Gabrielle Braun ,  Cuong Q. Ly ,  Georgette Castanedo ,  Paul Gibbons ,  Wendy Lee ,  Joachim Rudolph ,  Nicole Alice Blaquiere ,  Jacob Bradley Schwarz ,  Ramsay Beveridge ,  Jean-Philippe Leclerc ,  Alexandre Lemire ,  Leo Fu

IPC: C07D401/14 ,  A61K45/06 ,  C07D401/04 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08

CPC classification number: C07D401/14 ,  A61K45/06 ,  C07D401/04 ,  C07D413/14 ,  C07D471/04 ,  C07D471/08

Abstract: Described herein are phenoxy-pyridyl-pyrimidine compounds with inositol requiring enzyme 1 (IRE1) modulation activity or function having the Formula I structure or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, and with the substituents and structural features described herein. Also described are pharmaceutical compositions and medicaments that include the Formula I compounds, as well as methods of using such IRE1 modulators, alone and in combination with other therapeutic agents, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.

公开(公告)号：US20220204517A1

公开(公告)日：2022-06-30

申请号：US17654131

申请日：2022-03-09

Applicant: Genentech, Inc.

Inventor： Yun-Xing Cheng ,  Paul Gibbons ,  Terry Kellar ,  Wei Li ,  Rohan Mendonca ,  Po-wai Yuen ,  Mark Edward Zak ,  Lei Zhang

IPC: C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and salts thereof, wherein R1, R2 R3, R4 and n are defined herein, are useful as inhibitors of one or more Janus kinases. Also provided are pharmaceutical compositions that include a compound of Formula (00A) and a pharmaceutically acceptable carrier, adjuvant or vehicle, and methods of treating or lessening the severity of a disease or condition responsive to the inhibition of a Janus kinase activity in a patient.