公开(公告)号：US09034866B2

公开(公告)日：2015-05-19

申请号：US13768873

申请日：2013-02-15

Applicant: Genentech, Inc.

Inventor： Steven Staben ,  Georgette Castanedo ,  Christian A. G. N. Montalbetti ,  Jianwen Feng

IPC: C07D498/04 ,  C07D498/14 ,  C07D519/00 ,  C07D513/04 ,  C07D498/00 ,  C07D498/12

CPC classification number: C07D498/04 ,  C07D487/04 ,  C07D498/00 ,  C07D498/12 ,  C07D513/04 ,  C07D519/00

Abstract: The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

Abstract translation: 本发明涉及式I的新化合物：其中A1，A2，A3，A4，A5，A6，R2，R4，R5，R6，R7，R8和下标m和n各自具有本文所述的含义。 式I化合物及其药物组合物可用于治疗观察到NF-kB信号传导的不期望或过度活化的疾病和病症。

公开(公告)号：US20180298015A1

公开(公告)日：2018-10-18

申请号：US16014231

申请日：2018-06-21

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 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02

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：US20150166569A1

公开(公告)日：2015-06-18

申请号：US14622446

申请日：2015-02-13

Applicant: Genentech, Inc.

Inventor： Steven Staben ,  Georgette Castanedo ,  Christian A.G.N. Montalbetti ,  Jianwen Feng

IPC: C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C07D487/04

CPC classification number: C07D498/04 ,  C07D487/04 ,  C07D498/00 ,  C07D498/12 ,  C07D513/04 ,  C07D519/00

Abstract: The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

Abstract translation: 本发明涉及式I的新化合物：其中A1，A2，A3，A4，A5，A6，R2，R4，R5，R6，R7，R8和下标m和n各自具有本文所述的含义。 式I化合物及其药物组合物可用于治疗观察到NF-kB信号传导的不期望或过度活化的疾病和病症。

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：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：US20150038460A1

公开(公告)日：2015-02-05

申请号：US14515742

申请日：2014-10-16

Applicant: Genentech, Inc.

Inventor： Steven Staben ,  Jianwen Feng ,  Pui Leng Loke ,  Christian A.G.N. Montalbetti

IPC: C07F7/08 ,  C07D491/107 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/04 ,  C07D487/04 ,  C07D491/08 ,  C07D401/14 ,  C07D417/14

CPC classification number: C07F7/0805 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D487/04 ,  C07D491/08 ,  C07D491/10 ,  C07D491/107

Abstract: The invention relates to novel compounds of Formula I: wherein A, Y, R1, R2 and the subscript b each has the meaning as described herein and compounds of Formula I, and stereoisomers, geometric isomers, tautomers, solvates, metabolites, isotopes, pharmaceutically acceptable salts, or prodrugs thereof. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.

Abstract translation: 本发明涉及式I的新化合物：其中A，Y，R 1，R 2和下标b各自具有本文所述的含义，式I化合物和立体异构体，几何异构体，互变异构体，溶剂合物，代谢物，同位素，药学上 其可接受的盐或前药。 式I化合物及其药物组合物可用于治疗观察到NF-kB信号传导的不期望或过度活化的疾病和病症。

公开(公告)号：US20130345215A1

公开(公告)日：2013-12-26

申请号：US13911585

申请日：2013-06-06

Applicant: Genentech, Inc.

Inventor： Jianwen Feng ,  Nancy-Ellen Haynes ,  Johannes Cornelius Hermann ,  Kyungjin Kim ,  Jin-Jun Liu ,  Nathan Robert Scott ,  Lin Yi ,  Mark Edward Zak ,  Guiling Zhao

IPC: C07D487/04 ,  C07D471/04

CPC classification number: C07D487/04 ,  C07D471/04

Abstract: There are provided compounds of the formula or a pharmaceutically acceptable salt thereof, wherein Q, R1 and R2 are as defined herein.The compounds of formula I are useful in the treatment of cancer.

Abstract translation: 提供下式的化合物或其药学上可接受的盐，其中Q，R 1和R 2如本文所定义。 式I化合物可用于治疗癌症。

公开(公告)号：US20130217666A1

公开(公告)日：2013-08-22

申请号：US13768873

申请日：2013-02-15

Applicant: Genentech, Inc.

Inventor： Steven Staben ,  Georgette Castanedo ,  Christian A.G.N. Montalbetti ,  Jianwen Feng

IPC: C07D513/04 ,  C07D498/04

CPC classification number: C07D498/04 ,  C07D487/04 ,  C07D498/00 ,  C07D498/12 ,  C07D513/04 ,  C07D519/00

Abstract: The invention relates to novel compounds of Formula I: wherein A1, A2, A3, A4, A5, A6, R2, R4, R5, R6, R7, R8 and subscripts m and n each has the meaning as described herein. Compounds of Formula I and pharmaceutical compositions thereof are useful in the treatment of disease and disorders in which undesired or over-activation of NF-kB signaling is observed.