公开(公告)号：US20150182537A1

公开(公告)日：2015-07-02

申请号：US14559786

申请日：2014-12-03

Applicant: GENENTECH, INC.

Inventor： Aleksandr Kolesnikov ,  Steven Do

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

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.

Abstract translation: 具有式I的化合物，其中如本文定义的R1，X1，X2，X3和X4是ERK激酶的抑制剂。 还公开了用于治疗过度增殖性疾病的组合物和方法。

公开(公告)号：US20150094347A1

公开(公告)日：2015-04-02

申请号：US14565669

申请日：2014-12-10

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Steven Do ,  Danette Dudley ,  Adrian Folkes ,  Richard Goldsmith ,  Robert Heald ,  Timothy Heffron ,  Aleksandr Kolesnikov ,  Chudi Ndubaku ,  Alan G. Olivero ,  Stephen Price ,  Steven Staben ,  BinQing Wei

IPC: C07D495/04

CPC classification number: C07D495/04 ,  A61K31/381 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D249/14 ,  C07D495/14 ,  C07D513/04 ,  C07D513/14

Abstract: Benzoxepin compounds of Formula I, and 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 where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, 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的苯并氧杂环己烯化合物，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; 并且其中（i）X1为N且X2为S，（ii）X1为S且X2为N，（iii）X1为CR7，X2为S，（iv）X1为S且X2为CR7; （ⅴ）X1为NR8，X2为N，（vi）X1为N，X2为NR8，i X1为CR7，X2为O，（ii）X1为O，X2为CR7，ix为CR7 X2为C（R7）2，（x）X1为C（R7）2，X2为CR7; （xi）X1是N，X2是O，或（xii）X1是O，X2是N，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：US20140135308A1

公开(公告)日：2014-05-15

申请号：US14162520

申请日：2014-01-23

Applicant: Genentech, Inc.

Inventor： Nicole Blaquiere ,  Steven Do ,  Danette Dudley ,  Adrian Folkes ,  Richard Goldsmith ,  Robert Heald ,  Timothy Heffron ,  Aleksandr Kolesnikov ,  Chudi Ndubaku ,  Alan G. Olivero ,  Stephen Price ,  Steven Staben ,  BinQing Wei

IPC: C07D495/04 ,  C07D495/14 ,  A61K45/06 ,  A61K31/429 ,  A61K31/541 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/4545 ,  A61K31/4439 ,  A61K31/4365 ,  A61K31/4196 ,  A61K31/506 ,  A61K31/4985 ,  A61K31/551 ,  C07D513/04

CPC classification number: C07D495/04 ,  A61K31/381 ,  A61K31/41 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/429 ,  A61K31/4365 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/551 ,  A61K45/06 ,  C07D249/14 ,  C07D495/14 ,  C07D513/04 ,  C07D513/14

Abstract: Benzoxepin compounds of Formula I, and 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 where (i) X1 is N and X2 is S, (ii) X1 is S and X2 is N, (iii) X1 is CR7 and X2 is S, (iv) X1 is S and X2 is CR7; (v) X1 is NR8 and X2 is N, (vi) X1 is N and X2 is NR8, (vii) X1 is CR7 and X2 is O, (viii) X1 is O and X2 is CR7, (ix) X1 is CR7 and X2 is C(R7)2, (x) X1 is C(R7)2 and X2 is CR7; (xi) X1 is N and X2 is O, or (xii) X1 is O and X2 is N, 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的苯并氧杂环己烯化合物，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; 并且其中（i）X1为N且X2为S，（ii）X1为S且X2为N，（iii）X1为CR7，X2为S，（iv）X1为S且X2为CR7; （ⅴ）X1为NR8，X2为N，（vi）X1为N，X2为NR8，i X1为CR7，X2为O，（ii）X1为O，X2为CR7，ix为CR7 X2为C（R7）2，（x）X1为C（R7）2，X2为CR7; （xi）X1是N，X2是O，或（xii）X1是O，X2是N，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：US20250059163A1

公开(公告)日：2025-02-20

申请号：US18747054

申请日：2024-06-18

Applicant: Genentech, Inc.

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

IPC: C07D401/14 ,  A61K9/00 ,  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：US20240368186A1

公开(公告)日：2024-11-07

申请号：US18676200

申请日：2024-05-28

Applicant: Genentech, Inc.

Inventor： Matthew Leo Landry ,  Christian Nilewski ,  Michael Siu ,  Elisia Villemure ,  Yong Wang ,  BinQing Wei ,  Melissa Ann Ashley ,  Steven Do ,  Lewis John Gazzard ,  Samantha Alyson Green

IPC: C07D498/22 ,  A61K31/553 ,  A61K45/06 ,  A61P35/00 ,  C07D519/00

Abstract: Provided herein are aza-tetracyclic oxazepinyl compounds useful in the treatment of cancers.

公开(公告)号：US11236068B2

公开(公告)日：2022-02-01

申请号：US16679104

申请日：2019-11-08

Applicant: Genentech, Inc.

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

IPC: A61K31/517 ,  A61K31/519 ,  A61P35/00 ,  C07D401/14 ,  C07D403/14 ,  C07D407/14 ,  C07D471/04 ,  A61K9/00 ,  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：US20210106593A1

公开(公告)日：2021-04-15

申请号：US17075380

申请日：2020-10-20

Applicant: GENENTECH, INC.

Inventor： Aleksandr Kolesnikov ,  Steven Do

IPC: A61K31/553 ,  C07D471/16 ,  C07D498/16 ,  A61K31/519 ,  A61K31/53 ,  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：US20200078371A1

公开(公告)日：2020-03-12

申请号：US16680221

申请日：2019-11-11

Applicant: GENENTECH, INC.

Inventor： Aleksandr Kolesnikov ,  Steven Do

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

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：US10278975B2

公开(公告)日：2019-05-07

申请号：US15705104

申请日：2017-09-14

Applicant: GENENTECH, INC.

Inventor： Aleksandr Kolesnikov ,  Steven Do

IPC: A61K31/551 ,  C07D471/16 ,  A61K31/553 ,  C07D498/16 ,  A61K31/519 ,  A61K31/53 ,  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：US20170081341A1

公开(公告)日：2017-03-23

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.