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：US20160185797A1

公开(公告)日：2016-06-30

申请号：US15060325

申请日：2016-03-03

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Georgette Castanedo ,  Jianwen A. Feng ,  Baihua Hu ,  Steven Staben ,  Po-wai Yuen ,  Guosheng Wu ,  Xingyu Lin ,  Jason Burch

IPC: C07D495/04 ,  C07D403/10 ,  C07D403/14 ,  C07D491/107 ,  C07D409/14 ,  C07D417/14 ,  C07D487/04 ,  C07D401/14 ,  C07D471/04 ,  C07D413/10 ,  C07D405/10 ,  C07D401/10 ,  C07D405/14

CPC classification number: C07D401/10 ,  A61K31/395 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/107 ,  C07D495/04 ,  C07D495/06

Abstract: The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

公开(公告)号：US20130225557A1

公开(公告)日：2013-08-29

申请号：US13854635

申请日：2013-04-01

Applicant: Genentech, Inc.

Inventor： Georgette Castanedo ,  Bryan Chan ,  Matthew C. Lucas ,  Brian Safina ,  Daniel P. Sutherlin ,  Zachary Sweeney

IPC: C07D471/04 ,  C07D491/107

CPC classification number: C07D471/04 ,  C07D491/107

Abstract: Formula I compounds, including stereoisomers, geometric isomers, tautomers, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting the delta isoform of PI3K, and for treating disorders mediated by lipid kinases such as inflammation, immunological disorders, and cancer. 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: 式I化合物，包括立体异构体，几何异构体，互变异构体，代谢物及其药学上可接受的盐，可用于抑制PI3K的δ同种型，以及用于治疗由脂质激酶如炎症，免疫学障碍和癌症介导的病症。 公开了使用式I化合物在体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理状况中的这种病症的方法。

公开(公告)号：US09605005B2

公开(公告)日：2017-03-28

申请号：US15074100

申请日：2016-03-18

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Georgette Castanedo ,  Jianwen A. Feng ,  Baihua Hu ,  Steven Staben ,  Po-wai Yuen ,  Guosheng Wu ,  Jason Burch

IPC: C07D401/00 ,  C07D513/04 ,  C07D401/14 ,  C07D413/14 ,  C07D401/10 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04

CPC classification number: C07D513/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04

Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

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：US20150057260A1

公开(公告)日：2015-02-26

申请号：US14466176

申请日：2014-08-22

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Georgette Castanedo ,  Jianwen A. Feng ,  Baihua Hu ,  Steven Staben ,  Po-wai Yuen ,  Guosheng Wu ,  Xingyu Lin ,  Jason Burch

IPC: C07D495/04 ,  C07D403/10 ,  C07D405/14 ,  C07D409/14 ,  C07D491/107 ,  C07D403/14 ,  C07D401/10

CPC classification number: C07D401/10 ,  A61K31/395 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/107 ,  C07D495/04 ,  C07D495/06

Abstract: The invention relates to compounds of Formula (0): wherein A1-A8, R4 and R5 each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

Abstract translation: 本发明涉及式（O）的化合物：其中A1-A8，R4和R5各自具有如本文所述的含义。 式（0）的化合物及其药物组合物可用于治疗其中观察到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：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：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：US20160200739A1

公开(公告)日：2016-07-14

申请号：US15074100

申请日：2016-03-18

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Georgette Castanedo ,  Jianwen A. Feng ,  Baihua Hu ,  Steven Staben ,  Po-wai Yuen ,  Guosheng Wu ,  Jason Burch

IPC: C07D513/04 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D413/10 ,  C07D401/10 ,  C07D403/10 ,  C07D491/052

CPC classification number: C07D513/04 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D413/10 ,  C07D413/14 ,  C07D417/10 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04

Abstract: The invention relates to compounds of Formula (0): wherein Q, A1-A8, R4 and R5 and each has the meaning as described herein. Compounds of Formula (0) and pharmaceutical compositions thereof are useful in the treatment of diseases and disorders in which undesired or over-activation of NF-kB signaling is observed.

公开(公告)号：US20160152632A9

公开(公告)日：2016-06-02

申请号：US14316166

申请日：2014-06-26

Applicant: F.HOFFMANN-LA ROCHE AG ,  GENENTECH, INC.

Inventor： Adrian Folkes ,  Stephen Shuttleworth ,  Irina Chuckowree ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzer-Toste ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

IPC: C07D495/04 ,  A61K45/06 ,  A61K31/551 ,  A61K31/5377 ,  C07D491/048

CPC classification number: A61K31/5377 ,  A61K31/551 ,  A61K45/06 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

Abstract: Compounds of Formulae Ia, and stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for inhibiting lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia 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: 式Ia化合物和立体异构体，几何异构体，互变异构体，溶剂合物，代谢物和药学上可接受的盐可用于抑制脂质激酶（包括PI3K）和用于治疗由脂质激酶介导的癌症等疾病。 公开了将式Ia化合物用于体外，原位和体内诊断，预防或治疗哺乳动物细胞或相关病理条件中的这种病症的方法。