公开(公告)号：US08431694B1

公开(公告)日：2013-04-30

申请号：US13712114

申请日：2012-12-12

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Zhigang Cheng ,  Mark E. Reynolds ,  Scott J. Savage ,  Qingping Tian ,  Herbert Yajima

IPC: C07D413/14

CPC classification number: C07D513/04 ,  C07D405/04 ,  C07D495/04 ,  C07F5/025

Abstract: The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds.

Abstract translation: 本发明提供制备，分离和纯化PI3K抑制剂，式I和II化合物的方法，以及制备式I和II化合物的新型中间体。

公开(公告)号：US20130109852A1

公开(公告)日：2013-05-02

申请号：US13712114

申请日：2012-12-12

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Zhigang Cheng ,  Mark E. Reynolds ,  Scott J. Savage ,  Qingping Tian ,  Herbert Yajima

IPC: C07D513/04

CPC classification number: C07D513/04 ,  C07D405/04 ,  C07D495/04 ,  C07F5/025

Abstract: The invention provides processes of preparing, separating, and purifying PI3K inhibitor, Formula I and II compounds, and novel intermediates for preparing Formula I and II compounds.

Abstract translation: 本发明提供制备，分离和纯化PI3K抑制剂，式I和II化合物的方法，以及制备式I和II化合物的新型中间体。

公开(公告)号：US11414412B2

公开(公告)日：2022-08-16

申请号：US17016900

申请日：2020-09-10

Applicant: Genentech, Inc.

Inventor： Francis Gosselin ,  Andrew McClory ,  Zhigang Cheng

IPC: C07D417/14

Abstract: A process for the manufacture N-(5-((5R,6S)-5-amino-6-fluorooxepan-2-yl)-1-methyl-1H-pyrazol-4-yl)-2-(2,6-difluorophenyl)thiazole-4-carboxamide (I) wherein the vicinal amino fluoro substituents are introduced by treating 5 with sodium chloro((4-nitrophenyl)sulfonyl)amide and N-bromosucinimide and unraveling the resulting substituted aziridine (6) with trimethylamine trihydrofluoride to afford 7 which is further processed to afford 1.

公开(公告)号：US08895729B2

公开(公告)日：2014-11-25

申请号：US14049477

申请日：2013-10-09

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Zhigang Cheng ,  Francis Gosselin ,  Pirmin Hidber ,  Ursula Hoffmann ,  Theresa Humphries ,  Reinhard Reents ,  Qingping Tian ,  Herbert Yajima

IPC: C07D495/04 ,  C07D295/185 ,  C07D491/00

CPC classification number: C07D495/04 ,  C07D295/185

Abstract: Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure: and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.

Abstract translation: 制备双重mTOR / PI3K抑制剂GDC-0980的方法，命名为（S）-1-（4 - （（2-（2-氨基嘧啶-5-基）-7-甲基-4-吗啉代噻吩并[3,2 d]嘧啶-6-基）甲基）哌嗪-1-基）-2-羟基丙-1-酮，其具有以下结构：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。

公开(公告)号：US20140100366A1

公开(公告)日：2014-04-10

申请号：US14049477

申请日：2013-10-09

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Zhigang Cheng ,  Francis Gosselin ,  Pirmin Hidber ,  Ursula Hoffmann ,  Theresa Humphries ,  Reinhard Reents ,  Qingping Tian ,  Herbert Yajima

IPC: C07D495/04 ,  C07D295/185

CPC classification number: C07D495/04 ,  C07D295/185

Abstract: Process methods for making the dual mTOR/PI3K inhibitor GDC-0980, named as (S)-1-(4-((2-(2-aminopyrimidin-5-yl)-7-methyl-4-morpholinothieno[3,2-d]pyrimidin-6-yl)methyl)piperazin-1-yl)-2-hydroxypropan-1-one, having the structure: and stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof.

Abstract translation: 制备双重mTOR / PI3K抑制剂GDC-0980的方法，命名为（S）-1-（4 - （（2-（2-氨基嘧啶-5-基）-7-甲基-4-吗啉代噻吩并[3,2 d]嘧啶-6-基）甲基）哌嗪-1-基）-2-羟基丙-1-酮，其具有以下结构：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。