公开(公告)号：US20180298033A1

公开(公告)日：2018-10-18

申请号：US15842642

申请日：2017-12-14

Applicant: Genentech, Inc.

Inventor： Nicholas C. Ray ,  Yun-Xing Cheng ,  Christine Edwards ,  Simon C. Goodacre ,  Wei Li ,  Snahel Patel ,  Matthew W. Cartwright ,  Mohammed Sajad ,  Po-wai Yuen ,  Mark E. Zak

IPC: C07D519/00 ,  C07D471/04

Abstract: Compounds of Formula 0, Formula I and Formula II and methods of use as Janus kinase inhibitors are described herein.

公开(公告)号：US20180086757A1

公开(公告)日：2018-03-29

申请号：US15692907

申请日：2017-08-31

Applicant: Genentech, Inc.

Inventor： Simon Charles Goodacre ,  Nicholas Charles Ray ,  Mark Edward Zak ,  Yun-Xing Cheng ,  Wei Li

IPC: C07D471/04 ,  C07D471/10

CPC classification number: C07D471/04 ,  C07D471/10

Abstract: Provided are triazolopyridine compounds that are inhibitors of JAK kinase, such as JAK1, compositions containing these compounds and methods for treating diseases mediated by a JAK kinase. In particular, provided are compounds of formula (I), stereoisomers, tautomers, solvates, prodrugs or pharmaceutically acceptable salts thereof, where R1a, R1b, R1c, R2, R3, R4 and R5 are defined herein, pharmaceutical compositions comprising the compound and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, for example, for treating a disease or condition mediated by a JAK kinase in a patient.

公开(公告)号：US20150336962A1

公开(公告)日：2015-11-26

申请号：US14720323

申请日：2015-05-22

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Nicholas Charles Ray ,  Simon Charles Goodacre ,  Rohan Mendonca ,  Terry Kellar ,  Yun-Xing Cheng ,  Wei Li ,  Po-Wai Yuen

IPC: C07D487/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula (00A) and methods of use as Janus kinase inhibitors are described herein.

Abstract translation: 本文描述了式（00A）的化合物和用作Janus激酶抑制剂的方法。

公开(公告)号：US20250042919A1

公开(公告)日：2025-02-06

申请号：US18882588

申请日：2024-09-11

Applicant: Genentech, Inc.

Inventor： Lewis J. Gazzard ,  Samantha Alyson Green ,  Matthew Leo Landry ,  Sushant Malhotra ,  Michael Siu ,  Steven Do ,  Yun-Xing Cheng ,  Limin Cheng ,  Jianfeng Xin ,  Mingtao He

IPC: C07D498/22 ,  A61K31/553 ,  A61K45/06 ,  A61P35/00 ,  C07D519/00

Abstract: Provided herein are tetracyclic oxazepinyl compounds useful in the treatment on cancers.

公开(公告)号：US20180327402A1

公开(公告)日：2018-11-15

申请号：US15975462

申请日：2018-05-09

Applicant: Genentech, Inc.

Inventor： Simon Charles Goodacre ,  Nicholas Charles Ray ,  Mark Edward Zak ,  Yun-Xing Cheng ,  Wei Li

IPC: C07D471/04 ,  C07D471/10

CPC classification number: C07D471/04 ,  C07D471/10

Abstract: Provided are triazolopyridine compounds that are inhibitors of JAK kinase, such as JAK1, compositions containing these compounds and methods for treating diseases mediated by a JAK kinase. In particular, provided are compounds of formula (I), stereoisomers, tautomers, solvates, prodrugs or pharmaceutically acceptable salts thereof, where R1a, R1b, R1c, R2, R3, R4 and R5 are defined herein, pharmaceutical compositions comprising the compound and a pharmaceutically acceptable carrier, adjuvant or vehicle, methods of using the compound or composition in therapy, for example, for treating a disease or condition mediated by a JAK kinase in a patient.

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：US20170226132A1

公开(公告)日：2017-08-10

申请号：US15499662

申请日：2017-04-27

Applicant: Genentech, Inc.

Inventor： Nicholas C. Ray ,  Yun-Xing Cheng ,  Christine Edwards ,  Simon C. Goodacre ,  Wei Li ,  Snahel Patel ,  Matthew W. Cartwright ,  Mohammed Sajad ,  Po-wai Yuen ,  Mark E. Zak

IPC: C07D519/00 ,  C07D471/04

CPC classification number: C07D519/00 ,  C07D471/04

Abstract: Compounds of Formula 0, Formula I and Formula II and methods of use as Janus kinase inhibitors are described herein.

公开(公告)号：US12247032B2

公开(公告)日：2025-03-11

申请号：US18063575

申请日：2022-12-08

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Naomi S. Rajapaksa ,  Yun-Xing Cheng ,  Jessica Grandner ,  Daniel G. M. Shore ,  F. Anthony Romero ,  Marian C. Bryan

IPC: A61P37/06 ,  C07D487/04

Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined herein, and salts thereof, that are useful as JAK kinase inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor 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：US20230016791A1

公开(公告)日：2023-01-19

申请号：US17821851

申请日：2022-08-24

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Naomi S. Rajapaksa ,  Yun-Xing Cheng ,  Jessica Marie Grandner ,  Daniel G.M. Shore ,  Marian C. Bryan

IPC: C07D487/04 ,  A61P11/06 ,  A61K9/00 ,  A61K9/19

Abstract: wherein R1, R2, R3, R4, R5 and R6 are as defined herein, and salts thereof that are useful as JAK kinse inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor 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：US11453671B2

公开(公告)日：2022-09-27

申请号：US16902499

申请日：2020-06-16

Applicant: Genentech, Inc.

Inventor： Mark Edward Zak ,  Naomi S. Rajapaksa ,  Yun-Xing Cheng ,  Jessica Grandner ,  Daniel G. M. Shore ,  Marian C. Bryan

IPC: A61K31/519 ,  C07D487/04 ,  A61P11/06 ,  A61K9/00 ,  A61K9/19

Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5 and R6 are as defined herein, and salts thereof that are useful as JAK kinse inhibitors are described herein. Also provided are pharmaceutical compositions that include such a JAK inhibitor 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.