公开(公告)号：US20180000833A1

公开(公告)日：2018-01-04

申请号：US15705104

申请日：2017-09-14

Applicant: GENENTECH, INC.

Inventor： Aleksandr Kolesnikov ,  Steven Do

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

CPC classification number: A61K31/553 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5365 ,  A61K31/542 ,  A61K31/55 ,  A61K45/06 ,  C07D471/16 ,  C07D498/16 ,  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：US09850239B2

公开(公告)日：2017-12-26

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 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4995 ,  A61K31/506 ,  A61K31/55 ,  A61K31/551 ,  A61K45/06 ,  C07D519/00 ,  C07D231/00

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.

公开(公告)号：US09309265B2

公开(公告)日：2016-04-12

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: A01N37/00 ,  C07D333/00 ,  C07F5/02 ,  C07D495/04 ,  C07D495/14 ,  C07D513/14 ,  A61K31/381 ,  A61K31/4155 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/4436 ,  A61K31/496 ,  A61K31/53

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：US20160052933A1

公开(公告)日：2016-02-25

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 ,  C07D519/00 ,  C07D498/14

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：US08846762B2

公开(公告)日：2014-09-30

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 Folkes ,  Neil Pegg

IPC: A01N37/00 ,  C07D333/00 ,  A61K31/4365 ,  A61K31/4196 ,  A61K31/53 ,  C07D495/04 ,  A61K31/496 ,  A61K31/427 ,  A61K31/429 ,  A61K31/4155 ,  C07D495/14 ,  A61K31/4245 ,  A61K31/4436 ,  C07D513/14 ,  A61K31/381

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。

公开(公告)号：US08785626B2

公开(公告)日：2014-07-22

申请号：US14047206

申请日：2013-10-07

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.

Abstract translation: 式I的苯并氧氮杂化合物，包括立体异构体，几何异构体，互变异构体，溶剂合物，代谢物及其药学上可接受的盐，其中：Z1是CR1或N; Z2为CR2或N; Z3为CR3或N; Z4是CR4或N; B是与苯并氧杂环环稠合的吡唑基，咪唑基或三唑基环，可用于抑制脂质激酶，包括p110α和PI3K的其他同种型，并用于治疗由脂质激酶介导的癌症等疾病。 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：US11760744B2

公开(公告)日：2023-09-19

申请号：US16642824

申请日：2019-08-15

Applicant: Genentech, Inc.

Inventor： Aijun Lu ,  Sushant Malhotra ,  Alan G. Olivero ,  Cheng Shao ,  Yamin Zhang ,  Steven Do

IPC: C07D401/04 ,  C07D239/94 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D413/12 ,  C07D471/04

CPC classification number: C07D401/04 ,  C07D239/94 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/04 ,  C07D413/12 ,  C07D471/04

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

公开(公告)号：US11376260B2

公开(公告)日：2022-07-05

申请号：US17075380

申请日：2020-10-20

Applicant: GENENTECH, INC.

Inventor： Aleksandr Kolesnikov ,  Steven Do

IPC: A61K31/53 ,  A61P35/00 ,  A61P35/02 ,  A61P43/00 ,  C07D471/16 ,  A61K31/553 ,  C07D498/16 ,  A61K31/519 ,  A61K31/5365 ,  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：US09867833B2

公开(公告)日：2018-01-16

申请号：US14559786

申请日：2014-12-03

Applicant: GENENTECH, INC.

Inventor： Aleksandr Kolesnikov ,  Steven Do

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

CPC classification number: A61K31/553 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5365 ,  A61K31/542 ,  A61K31/55 ,  A61K45/06 ,  C07D471/16 ,  C07D498/16 ,  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：US09359340B2

公开(公告)日：2016-06-07

申请号：US14458062

申请日：2014-08-12

Applicant: Array BioPharma Inc. ,  Genentech, Inc.

Inventor： Ian S. Mitchell ,  James F. Blake ,  Rui Xu ,  Nicholas C. Kallan ,  Dengming Xiao ,  Keith Lee Spencer ,  Josef R. Bencsik ,  Eli M. Wallace ,  Stephen T. Schlachter ,  Anna L. Leivers ,  Jun Liang ,  Brian Safina ,  Birong Zhang ,  Christine Chabot ,  Steven Do

IPC: C07D239/70 ,  C07D403/04 ,  C07D413/12 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D407/12 ,  A61P29/00 ,  A61P35/00 ,  A61P9/00 ,  A61P25/28 ,  A61P15/00 ,  A61P17/00 ,  A61K31/517 ,  A61K31/496

CPC classification number: A61K31/517 ,  C07D239/70 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D407/12 ,  C07D409/12 ,  C07D409/14 ,  C07D413/12

Abstract: The present invention provides compounds, including resolved enantiomers, resolved diastereomers, solvates and pharmaceutically acceptable salts thereof, comprising the Formula I: Also provided are methods of using the compounds of this invention as AKT protein kinase inhibitors and for the treatment of hyperproliferative diseases such as cancer.

Abstract translation: 本发明提供了包含分解的对映异构体，分解的非对映异构体，溶剂合物和其药学上可接受的盐的化合物，其包含式I：还提供了使用本发明化合物作为AKT蛋白激酶抑制剂和用于治疗过度增殖性疾病 癌症。