公开(公告)号：US20170233407A1

公开(公告)日：2017-08-17

申请号：US15374867

申请日：2016-12-09

Applicant: Genentech, Inc.

Inventor： Jennafer Dotson ,  Robert Andrew Heald ,  Timothy Heffron ,  Graham Elgin Jones ,  Sussie Lerche Krintel ,  Neville James McLean ,  Chudi Ndubaku ,  Alan G. Olivero ,  Laurent Salphati ,  Lan Wang ,  BinQing Wei

IPC: C07D498/22 ,  A61K31/5377 ,  C07K16/22 ,  A61K39/395 ,  C07D495/14 ,  A61K31/5383 ,  C07D471/14 ,  C07D487/14 ,  A61K31/5386 ,  C07D491/147 ,  C07D498/14

Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

公开(公告)号：US20160257682A1

公开(公告)日：2016-09-08

申请号：US15152947

申请日：2016-05-12

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Bryan Chan ,  Francois Diederich ,  Jennafer Dotson ,  Emily Hanan ,  Timothy Heffron ,  Michael Lainchbury

IPC: C07D471/04 ,  A61K31/517 ,  A61K31/5386 ,  C07D519/00 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/541

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K45/06 ,  C07D519/00

Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.

Abstract translation: 本发明涉及作为含有EGFR突变体的T790M抑制剂的新化合物，含有它们的药物组合物，其制备方法及其在治疗中用于预防或治疗癌症的新化合物。

公开(公告)号：US20220348593A1

公开(公告)日：2022-11-03

申请号：US17535124

申请日：2021-11-24

Applicant: Genentech, Inc.

Inventor： Jennafer Dotson ,  Robert Andrew Heald ,  Timothy Heffron ,  Graham Elgin Jones ,  Sussie Lerche Krintel ,  Neville James McLean ,  Chudi Ndubaku ,  Alan G. Olivero ,  Laurent Salphati ,  Lan Wang ,  BinQing Wei

IPC: C07D498/22 ,  C07D471/14 ,  C07D491/14 ,  C07D495/14 ,  C07D487/14 ,  C07D498/14 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K39/395 ,  C07D491/147 ,  C07D498/20 ,  C07K16/22

Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

公开(公告)号：US09212186B2

公开(公告)日：2015-12-15

申请号：US14531349

申请日：2014-11-03

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Bryan K. Chan ,  Jennafer Dotson ,  Anthony Estrada ,  Timothy Heffron ,  Joseph Lyssikatos ,  Zachary Sweeney

IPC: A61K31/506 ,  C07D487/04 ,  C07D471/04 ,  C07D498/04 ,  C07D498/20 ,  C07D491/04 ,  C07D403/12 ,  C07D491/048

CPC classification number: C07D487/04 ,  A61K31/506 ,  C07D403/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D498/04 ,  C07D498/20

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I化合物或其药学上可接受的盐，其中X，R 1，R 2，R 3和A如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。

公开(公告)号：US09546182B2

公开(公告)日：2017-01-17

申请号：US14524204

申请日：2014-10-27

Applicant: Genentech, Inc.

Inventor： Jennafer Dotson ,  Robert Andrew Heald ,  Timothy Heffron ,  Graham Elgin Jones ,  Sussie Lerche Krintel ,  Neville James McLean ,  Chudi Ndubaku ,  Alan G. Olivero ,  Laurent Salphati ,  Lan Wang ,  BinQuing Wei

IPC: C07D471/14 ,  C07D471/22 ,  C07D487/14 ,  C07D498/14 ,  C07D491/14 ,  C07D495/14 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K39/395 ,  C07D491/147 ,  C07D498/20 ,  A61K39/00

CPC classification number: C07D498/22 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K39/3955 ,  A61K2039/505 ,  C07D471/14 ,  C07D471/22 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07D495/14 ,  C07D498/14 ,  C07D498/20 ,  C07K16/22 ,  C07K2317/24

Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Abstract translation: 式I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。 虚线表示可选的双键，至少一条虚线是双键。 取代基如所述。

公开(公告)号：US20150079081A1

公开(公告)日：2015-03-19

申请号：US14524204

申请日：2014-10-27

Applicant: Genentech, Inc.

Inventor： Jennafer Dotson ,  Robert Andrew Heald ,  Timothy Heffron ,  Graham Elgin Jones ,  Sussie Lerche Krintel ,  Neville James McLean ,  Chudi Ndubaku ,  Alan G. Olivero ,  Laurent Salphati ,  Lan Wang ,  BinQuing Wei

IPC: C07D498/14 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/5383 ,  C07D498/20 ,  C07D491/147 ,  A61K39/395

CPC classification number: C07D498/22 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K39/3955 ,  A61K2039/505 ,  C07D471/14 ,  C07D471/22 ,  C07D487/14 ,  C07D491/14 ,  C07D491/147 ,  C07D495/14 ,  C07D498/14 ,  C07D498/20 ,  C07K16/22 ,  C07K2317/24

Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

Abstract translation: 描述了具有抗癌活性，抗炎活性或免疫调节特性，更具体地与PI3激酶调节或抑制活性的式I的三环PI3k抑制剂化合物。 描述了使用式I的三环PI3K抑制剂化合物用于体外，原位和体内诊断或治疗哺乳动物细胞，生物体或相关病理条件的方法。 式I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。 虚线表示可选的双键，至少一条虚线是双键。 取代基如所述。

公开(公告)号：US20150051201A1

公开(公告)日：2015-02-19

申请号：US14531349

申请日：2014-11-03

Applicant: Genentech, Inc.

Inventor： Charles Baker-Glenn ,  Bryan K. Chan ,  Jennafer Dotson ,  Anthony Estrada ,  Timothy Heffron ,  Joseph Lyssikatos ,  Zachary Sweeney

IPC: C07D487/04 ,  C07D498/04 ,  C07D498/20 ,  C07D471/04

CPC classification number: C07D487/04 ,  A61K31/506 ,  C07D403/12 ,  C07D471/04 ,  C07D491/04 ,  C07D491/048 ,  C07D498/04 ,  C07D498/20

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein X, R1, R2, R3 and A are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with LRRK2 receptor, such as Parkinson's disease.

Abstract translation: 式I化合物或其药学上可接受的盐，其中X，R 1，R 2，R 3和A如本文所定义。 还公开了制备化合物和使用该化合物治疗与LRRK2受体（例如帕金森病）相关的疾病的方法。

公开(公告)号：US20190330235A1

公开(公告)日：2019-10-31

申请号：US16507523

申请日：2019-07-10

Applicant: Genentech, Inc.

Inventor： Jennafer Dotson ,  Robert Andrew Heald ,  Timothy Heffron ,  Graham Elgin Jones ,  Sussie Lerche Krintel ,  Neville James McLean ,  Chudi Ndubaku ,  Alan G. Olivero ,  Laurent Salphati ,  Lan Wang ,  BinQing Wei

IPC: C07D498/22 ,  C07D498/20 ,  A61K31/5377 ,  C07D471/14 ,  C07D498/14 ,  A61K31/5383 ,  A61K31/5386 ,  A61K39/395 ,  C07D491/147 ,  C07D495/14 ,  C07D491/14 ,  C07D487/14 ,  C07K16/22

Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.

公开(公告)号：US09951064B2

公开(公告)日：2018-04-24

申请号：US15152947

申请日：2016-05-12

Applicant: Genentech, Inc.

Inventor： Marian C. Bryan ,  Bryan Chan ,  Francois Diederich ,  Jennafer Dotson ,  Emily Hanan ,  Timothy Heffron ,  Michael Lainchbury ,  Robert Heald ,  Eileen M. Seward

IPC: C07D471/04 ,  C07D519/00 ,  A61K31/517 ,  A61K31/5386 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61K31/541

CPC classification number: C07D471/04 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/541 ,  A61K45/06 ,  C07D519/00

Abstract: This invention relates to novel compounds which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.