公开(公告)号：US20230212153A1

公开(公告)日：2023-07-06

申请号：US18052851

申请日：2022-11-04

Applicant: Genentech, Inc.

Inventor： Malcolm HUESTIS ,  Michael John LAMBRECHT ,  Jun LIANG ,  Man Un UNG ,  Xiaojing WANG ,  Jason Robert ZBIEG ,  Bing-Yan Zhu ,  Lisa Marie BARTON ,  Fabio BROCCATELLI ,  Georgette Marie CASTANEDO ,  Araz JAKALIAN ,  Robin LAROUCHE-GAUTHIER ,  Arun YADAV

IPC: C07D403/12 ,  A61P35/00 ,  C07D493/08 ,  C07D405/14 ,  C07D403/14 ,  C07D409/14 ,  C07D401/14

CPC classification number: C07D403/12 ,  A61P35/00 ,  C07D493/08 ,  C07D405/14 ,  C07D403/14 ,  C07D409/14 ,  C07D401/14

Abstract: A compound, of formula (I):




suitable for treating a cancer wherein the cancer is susceptible to inhibition of Cbl-B.

公开(公告)号：US20230202984A1

公开(公告)日：2023-06-29

申请号：US18057738

申请日：2022-11-21

Applicant: Genentech, Inc.

Inventor： Jason Robert Zbieg ,  Russell Tyler Smith ,  Paul Powell Beroza ,  Vishal Anil Verma ,  Bing-Yan Zhu ,  Ramsay Beveridge ,  Lisa Marie Barton ,  Bryan Ka lp Chan ,  Curtis Colwell ,  Samir Bouayad-Gervais ,  Anwesha Dey ,  Marie Anne Evangelista

IPC: C07D231/56 ,  C07D471/04 ,  C07F9/09

CPC classification number: C07D231/56 ,  C07D471/04 ,  C07F9/095

Abstract: This disclosure relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.

公开(公告)号：US09943519B2

公开(公告)日：2018-04-17

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: C07D413/14 ,  A61K31/535 ,  A61K31/5377 ,  C07D491/04 ,  C07D495/04 ,  A61K31/551 ,  A61K45/06 ,  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.

公开(公告)号：US08993563B2

公开(公告)日：2015-03-31

申请号：US13738829

申请日：2013-01-10

Applicant: Genentech, Inc. ,  F. Hoffmann-la Roche AG

Inventor： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

IPC: A61K31/519 ,  C07D495/04 ,  C07D413/14 ,  A61K31/5377 ,  C07D491/04

CPC classification number: A61K31/5377 ,  A61K31/519 ,  C07D413/14 ,  C07D491/04 ,  C07D495/04

Abstract: Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d 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-d的化合物，其中X是S或O，mor是吗啉基团，R3是单环杂芳基，并且包括立体异构体，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调节 脂质激酶（包括PI3K）的活性，以及​​用于治疗脂质激酶介导的疾病如癌症。 公开了使用式Ia-d的化合物在体外，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：US20140336154A1

公开(公告)日：2014-11-13

申请号：US14446154

申请日：2014-07-29

Applicant: Genentech, Inc. ,  F. HOFFMANN - LA ROCHE AG

Inventor： Steven Do ,  Richard Goldsmith ,  Tim Heffron ,  Aleksandr Kolesnikov ,  Steven Staben ,  Alan G. Olivero ,  Michael Siu ,  Daniel P. Sutherlin ,  Bing-Yan Zhu ,  Paul Goldsmith ,  Tracy Bayliss ,  Adrian Folkes ,  Neil Pegg

IPC: C07F5/02 ,  C07D495/14

CPC classification number: C07F5/02 ,  A61K31/381 ,  A61K31/4155 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/4436 ,  A61K31/496 ,  A61K31/53 ,  C07D495/04 ,  C07D495/14 ,  C07D513/14

Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, 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 Formulas I and II 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和II的苯并吡喃和苯并辛菌素化合物，包括立体异构体，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p110α和PI3K的其他同种型，并用于治疗疾病如癌症 由脂质激酶介导。 公开了使用式I和II的化合物在体外，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：US20130129820A1

公开(公告)日：2013-05-23

申请号：US13738829

申请日：2013-01-10

Applicant: Genentech, Inc.

Inventor： Tracy Bayliss ,  Irina Chuckowree ,  Adrian Folkes ,  Sally Oxenford ,  Nan Chi Wan ,  Georgette Castanedo ,  Richard Goldsmith ,  Janet Gunzner ,  Tim Heffron ,  Simon Mathieu ,  Alan Olivero ,  Steven Staben ,  Daniel P. Sutherlin ,  Bing-Yan Zhu

IPC: A61K31/5377

CPC classification number: A61K31/5377 ,  A61K31/519 ,  C07D413/14 ,  C07D491/04 ,  C07D495/04

Abstract: Compounds of Formulas Ia-d where X is S or O, mor is a morpholine group, and R3 is a monocyclic heteroaryl group, and including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, are useful for modulating the activity of lipid kinases including PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula Ia-d 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-d的化合物，其中X是S或O，mor是吗啉基团，R3是单环杂芳基，并且包括立体异构体，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调节 脂质激酶（包括PI3K）的活性，以及​​用于治疗脂质激酶介导的疾病如癌症。 公开了使用式Ia-d的化合物在体外，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：US20130123263A1

公开(公告)日：2013-05-16

申请号：US13738846

申请日：2013-01-10

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

Inventor： Steven Do ,  Richard Goldsmith ,  Tim Heffron ,  Aleksandr Kolesnikov ,  Steven Staben ,  Alan G. Olivero ,  Michael Siu ,  Daniel P. Sutherlin ,  Bing-Yan Zhu ,  Paul Goldsmith ,  Tracy Bayliss ,  Adrian Follkes ,  Neil Pegg

IPC: A61K31/53 ,  A61K31/4365 ,  A61K31/4436 ,  A61K31/381 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4196 ,  A61K31/4155 ,  A61K31/496 ,  A61K31/4245

CPC classification number: C07F5/02 ,  A61K31/381 ,  A61K31/4155 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/4436 ,  A61K31/496 ,  A61K31/53 ,  C07D495/04 ,  C07D495/14 ,  C07D513/14

Abstract: Benzopyran and benzoxepin compounds of Formulas I and II, and including stereoisomers, geometric isomers, tautomer solvates, metabolites and pharmaceutically acceptable salts thereof, 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 Formulas I and II 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和II的苯并吡喃和苯并氧杂环己酮化合物，包括立体异构体，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p110α和PI3K的其他同种型，并用于治疗疾病如癌症介导 通过脂质激酶。 公开了使用式I和II的化合物在体外，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。