公开(公告)号：US09951064B2

公开(公告)日：2018-04-24

申请号：US15152947

申请日：2016-05-12

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Bryan Chan ,  Francois Diederich ,  Jennafer Dotson ,  Emily Hanan ,  Timothy Heffron ,  Michael Lainchbury ,  Robert Heald ,  Eileen M. Seward

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/517 ,  A61K31/5386 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/541

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K45/06 ,  C07D519/00

Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.

公开(公告)号：US20220332718A1

公开(公告)日：2022-10-20

申请号：US17172766

申请日：2021-02-10

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Alberto Gobbi ,  James Richard Kiefer, Jr. ,  Aleksandr Kolesnikov ,  Alan G. Olivero ,  Joy Drobnick ,  Jun Liang ,  Naomi Rajapaksa ,  Chudi Ndubaku ,  Jianwen Feng

IPC: C07D487/04 ,  A61P37/02 ,  A61P35/00 ,  C07D519/00 ,  A61P29/00

Abstract: A method for treating an inflammatory or autoimmune disease with compounds of Formula 0, Formula I, and Formula II and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.

公开(公告)号：US11034698B2

公开(公告)日：2021-06-15

申请号：US16715933

申请日：2019-12-16

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Steven Do ,  Joy Drobnick ,  Alberto Gobbi ,  Tamiko Katsumoto ,  James Richard Kiefer, Jr. ,  Jun Liang ,  Naomi S. Rajapaksa ,  Yongsheng Chen ,  Liqiang Fu ,  Kwong Wah Lai ,  Zhiguo Liu ,  John Wai ,  Fei Wang

IPC: C07D487/04 ,  C07D519/00

Abstract: Compounds of Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, Formula VIII, and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) 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.

公开(公告)号：US10988478B1

公开(公告)日：2021-04-27

申请号：US16775650

申请日：2020-01-29

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Alberto Gobbi ,  James Richard Kiefer, Jr. ,  Aleksandr Kolesnikov ,  Alan G. Olivero ,  Joy Drobnick ,  Jun Liang ,  Naomi Rajapaksa ,  Chudi Ndubaku ,  Jianwen Feng

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00 ,  A61P37/02 ,  A61P29/00

Abstract: Compounds of Formula 0, Formula I, and Formula II and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.

公开(公告)号：US11434250B2

公开(公告)日：2022-09-06

申请号：US16863741

申请日：2020-04-30

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Joy Drobnick ,  James Richard Kiefer, Jr. ,  Aleksandr Kolesnikov ,  Naomi S. Rajapaksa

IPC: C07D519/00 ,  A61P1/04 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/06 ,  A61P25/00 ,  A61P25/04 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00

Abstract: Compounds of Formula I and methods of use as Interleukin-1 Receptor Associated Kinase 4 (IRAK4) inhibitors are described herein.

公开(公告)号：US20160257682A1

公开(公告)日：2016-09-08

申请号：US15152947

申请日：2016-05-12

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Bryan Chan ,  Francois Diederich ,  Jennafer Dotson ,  Emily Hanan ,  Timothy Heffron ,  Michael Lainchbury

IPC: C07D471/04 ,  A61K31/517 ,  A61K31/5386 ,  C07D519/00 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/541

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K45/06 ,  C07D519/00

Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.

Abstract translation: 本发明涉及作为含有EGFR突变体的T790M抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中用于预防或治疗癌症的新化合物。

公开(公告)号：US20230167123A1

公开(公告)日：2023-06-01

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: C07D487/04 ,  A61P37/06

CPC classification number: C07D487/04 ,  A61P37/06

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.