公开(公告)号：US10988478B1

公开(公告)日：2021-04-27

申请号：US16775650

申请日：2020-01-29

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Alberto Gobbi ,  James Richard Kiefer, Jr. ,  Aleksandr Kolesnikov ,  Alan G. Olivero ,  Joy Drobnick ,  Jun Liang ,  Naomi Rajapaksa ,  Chudi Ndubaku ,  Jianwen Feng

IPC: C07D487/04 ,  C07D519/00 ,  A61P35/00 ,  A61P37/02 ,  A61P29/00

Abstract: Compounds of Formula 0, Formula I, and Formula II and methods of use as Interleukin-1 Receptor Associated Kinase (IRAK4) inhibitors are described herein.

公开(公告)号：US20190119274A1

公开(公告)日：2019-04-25

申请号：US16221274

申请日：2018-12-14

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Aleksandr Kolesnikov ,  Jianwen A. Feng

IPC: C07D471/04 ,  C07D417/10

Abstract: The invention relates to compounds of formula (I): wherein Q, A1, A2, A3, A5, A6, A7, A8, R4a, R4b and R5 are as described herein. Compounds of formula (I) 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：US20140288047A1

公开(公告)日：2014-09-25

申请号：US14297142

申请日：2014-06-05

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: C07D498/14 ,  A61K31/553 ,  A61K45/06 ,  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：US20140005168A1

公开(公告)日：2014-01-02

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 ,  A61K31/551 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/513 ,  C07D491/052 ,  A61K31/55 ,  C07D471/10 ,  C07D487/10 ,  A61K45/06 ,  A61K31/501 ,  A61K31/496 ,  A61K31/444

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.

Abstract translation: 式I的5-氮杂吲唑化合物，包括立体异构体，几何异构体，互变异构体及其药学上可接受的盐，可用于抑制Pim激酶和用于治疗由Pim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：US08586574B2

公开(公告)日：2013-11-19

申请号：US13681763

申请日：2012-11-20

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: A61K31/553 ,  C07D498/04 ,  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：US11434250B2

公开(公告)日：2022-09-06

申请号：US16863741

申请日：2020-04-30

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Joy Drobnick ,  James Richard Kiefer, Jr. ,  Aleksandr Kolesnikov ,  Naomi S. Rajapaksa

IPC: C07D519/00 ,  A61P1/04 ,  A61P11/00 ,  A61P11/06 ,  A61P13/12 ,  A61P17/00 ,  A61P17/06 ,  A61P19/02 ,  A61P19/06 ,  A61P25/00 ,  A61P25/04 ,  A61P29/00 ,  A61P35/00 ,  A61P37/02 ,  A61P37/06 ,  A61P43/00

Abstract: Compounds of Formula I and methods of use as Interleukin-1 Receptor Associated Kinase 4 (IRAK4) inhibitors are described herein.

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：US10550117B2

公开(公告)日：2020-02-04

申请号：US16221274

申请日：2018-12-14

Applicant: Genentech, Inc.

Inventor： James John Crawford ,  Aleksandr Kolesnikov ,  Jianwen A. Feng

IPC: C07D471/04 ,  C07D417/10 ,  A61P27/14 ,  A61P37/06 ,  A61P17/00 ,  A61P19/02 ,  A61P1/00 ,  A61P11/00

Abstract: The invention relates to compounds of formula (I): wherein Q, A1, A2, A3, A5, A6, A7, A8, R4a, R4b and R5 are as described herein. Compounds of formula (I) 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：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：US09198918B2

公开(公告)日：2015-12-01

申请号：US14297142

申请日：2014-06-05

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: A61K31/553 ,  C07D498/04 ,  C07D498/14 ,  C07D519/00 ,  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: 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。