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：US20160235754A1

公开(公告)日：2016-08-18

申请号：US15140874

申请日：2016-04-28

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: A61K31/517

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 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: 本发明提供包括拆分的对映异构体，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，其包含式还提供使用本发明化合物作为AKT蛋白激酶抑制剂和治疗过度增殖性疾病如癌症的方法。

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.

公开(公告)号：US20160152606A9

公开(公告)日：2016-06-02

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: C07D413/12 ,  C07D401/12 ,  C07D409/14 ,  C07D407/12 ,  C07D409/12 ,  C07D239/70 ,  C07D403/12

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。

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。