公开(公告)号：US12084429B2

公开(公告)日：2024-09-10

申请号：US17644993

申请日：2021-12-17

Applicant: Genentech, Inc.

Inventor： Sushant Malhotra ,  Jianfeng Xin ,  Steven Do ,  Jack Terrett

IPC: C07D401/04 ,  A61K9/00 ,  A61K31/517 ,  A61P35/00 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D471/14

CPC classification number: C07D401/14 ,  A61K9/0019 ,  A61K9/0053 ,  A61P35/00 ,  C07D405/14

Abstract: This invention pertains to fused ring compounds of Formula (I), as further detailed herein, which are used for the inhibition of Ras proteins, as well as compositions comprising these compounds and methods of treatment by their administration.

公开(公告)号：US11236046B2

公开(公告)日：2022-02-01

申请号：US16657102

申请日：2019-10-18

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Yanyan Chu ,  Steven Do ,  Anthony Estrada ,  Baihua Hu ,  Aleksandr Kolesnikov ,  Xingyu Lin ,  Joseph P. Lyssikatos ,  Daniel Shore ,  Vishal Verma ,  Lan Wang ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D207/48 ,  C07D403/12 ,  C07D401/14 ,  C07D401/12 ,  C07D403/14 ,  C07D417/12 ,  C07D451/02 ,  C07D491/048 ,  C07D405/14

Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

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：US10517878B2

公开(公告)日：2019-12-31

申请号：US16286955

申请日：2019-02-27

Applicant: GENENTECH, INC.

Inventor： Aleksandr Kolesnikov ,  Steven Do

IPC: A61K31/5365 ,  C07D498/16 ,  A61K31/553 ,  C07D471/16 ,  A61K31/519 ,  A61K31/53 ,  A61K31/542 ,  A61K31/55 ,  A61K45/06 ,  C07D513/16

Abstract: Compounds having the formula I wherein R1, X1, X2, X3 and X4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

公开(公告)号：US20190192534A1

公开(公告)日：2019-06-27

申请号：US16286955

申请日：2019-02-27

Applicant: GENENTECH, INC.

Inventor： Aleksandr Kolesnikov ,  Steven Do

IPC: A61K31/553 ,  C07D498/16 ,  C07D471/16 ,  C07D513/16 ,  A61K45/06 ,  A61K31/55 ,  A61K31/53 ,  A61K31/5365 ,  A61K31/542 ,  A61K31/519

Abstract: Compounds having the formula I wherein R1, X1, X2, X3 and X4 as defined herein are inhibitors of ERK kinase. Also disclosed are compositions and methods for treating hyperproliferative disorders.

公开(公告)号：US20180118680A1

公开(公告)日：2018-05-03

申请号：US15851322

申请日：2017-12-21

Applicant: Genentech, Inc.

Inventor： Huifen Chen ,  Yanyan Chu ,  Steven Do ,  Anthony Estrada ,  Baihua Hu ,  Aleksandr Kolesnikov ,  Xingyu Lin ,  Joseph P. Lyssikatos ,  Daniel Shore ,  Vishal Verma ,  Lan Wang ,  Guosheng Wu ,  Po-wai Yuen

IPC: C07D207/48 ,  C07D403/14 ,  C07D417/12 ,  C07D403/12 ,  C07D451/02 ,  C07D405/14 ,  C07D401/14 ,  C07D491/048 ,  C07D401/12

Abstract: The invention is concerned with the compounds of formula I or II: and salts thereof. In addition, the present invention relates to methods of manufacturing and methods of using the compounds of formula I or II as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

公开(公告)号：US09670228B2

公开(公告)日：2017-06-06

申请号：US15368937

申请日：2016-12-05

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Steven Do ,  Danette Dudley ,  Adrian Folkes ,  Robert Heald ,  Timothy Heffron ,  Mark Jones ,  Aleksandr Kolesnikov ,  Chudi Ndubaku ,  Alan G. Olivero ,  Stephen Price ,  Steven Staben ,  Lan Wang

IPC: C07D498/04

CPC classification number: C07D498/04 ,  A61K31/553 ,  A61K45/06 ,  C07D491/044 ,  C07D498/14 ,  C07D519/00

Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US09546178B2

公开(公告)日：2017-01-17

申请号：US14930929

申请日：2015-11-03

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Steven Do ,  Danette Dudley ,  Adrian Folkes ,  Robert Heald ,  Timothy Heffron ,  Mark Jones ,  Aleksandr Kolesnikov ,  Chudi Ndubaku ,  Alan G. Olivero ,  Stephen Price ,  Steven Staben ,  Lan Wang

IPC: C07D491/044 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00 ,  A61K31/553 ,  A61K45/06

CPC classification number: C07D498/04 ,  A61K31/553 ,  A61K45/06 ,  C07D491/044 ,  C07D498/14 ,  C07D519/00

Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

Abstract translation: 本发明涉及式I的苯并氧氮杂化合物，其包括立体异构体，几何异构体，互变异构体或其药学上可接受的盐，其中：Z 1为CR 1或N; Z 2为CR 2或N; Z 3为CR 3或N; Z 4为CR 4或N; 并且B是吡唑基，咪唑基或三唑基环，该化合物具有抗癌活性，更具体地，抑制PI3激酶活性。

公开(公告)号：US09434725B2

公开(公告)日：2016-09-06

申请号：US13927278

申请日：2013-06-26

Applicant: Genentech, Inc.

Inventor： Steven Do ,  Huiyong Hu ,  Aleksandr Kolesnikov ,  Vickie H. Tsui ,  Xiaojing Wang

IPC: C07D471/04 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052 ,  A61K31/496 ,  A61K31/551 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/513 ,  A61K31/444 ,  A61K31/55 ,  A61K45/06 ,  A61K31/501

CPC classification number: C07D471/04 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/513 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D471/10 ,  C07D487/10 ,  C07D491/052

Abstract: 5-Azaindazole compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US20160159797A1

公开(公告)日：2016-06-09

申请号：US15044231

申请日：2016-02-16

Applicant: Genentech, Inc.

Inventor： Steven Do ,  Huiyong Hu ,  Aleksandr Kolesnikov ,  Wendy Lee ,  Vickie Hsiao-Wei Tsui ,  Xiaojing Wang ,  Zhaoyang Wen

IPC: C07D471/04 ,  A61K31/497 ,  A61K31/506 ,  A61K45/06 ,  A61K31/55 ,  A61K31/551 ,  C07D519/00 ,  A61K31/4995 ,  A61K31/437 ,  A61K31/496

CPC classification number: C07D471/04 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D231/00 ,  C07D519/00

Abstract: Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R1 and R2 are as defined herein, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.