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：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：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：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：US09346817B2

公开(公告)日：2016-05-24

申请号：US14013256

申请日：2013-08-29

Applicant: Genentech, Inc.

Inventor： Robert Andrew Heald ,  Neville James McLean

IPC: C07D491/056 ,  A61K31/5377 ,  C07D491/04 ,  C07D498/04 ,  A61K39/395 ,  A61K45/06

CPC classification number: C07D491/056 ,  A61K31/5377 ,  A61K39/3955 ,  A61K45/06 ,  C07D491/04 ,  C07D498/04

Abstract: Dioxino- and oxazin-[2,3-d]pyrimidine 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.

Abstract translation: 描述了具有抗癌活性，抗炎活性或免疫调节性质的更具体地具有PI3激酶调节或抑制活性的式I的二氧杂环丁烷酮和恶嗪 - [2,3-d]嘧啶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。

公开(公告)号：US20140065136A1

公开(公告)日：2014-03-06

申请号：US14013256

申请日：2013-08-29

Applicant: Genentech, Inc.

Inventor： Robert Andrew Heald ,  Neville James McLean

IPC: C07D491/056 ,  A61K39/395 ,  A61K45/06 ,  A61K31/5377

CPC classification number: C07D491/056 ,  A61K31/5377 ,  A61K39/3955 ,  A61K45/06 ,  C07D491/04 ,  C07D498/04

Abstract: Dioxino- and oxazin-[2,3-d]pyrimidine 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.

Abstract translation: 描述了具有抗癌活性，抗炎活性或免疫调节性质的更具体地具有PI3激酶调节或抑制活性的式I的二氧杂环丁烷酮和恶嗪 - [2,3-d]嘧啶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。