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。

公开(公告)号：US20150099880A1

公开(公告)日：2015-04-09

申请号：US14401089

申请日：2013-05-17

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Francis Gosselin ,  Yingqing Ran ,  Travis Remarchuk ,  Scott J. Savage ,  Jeffrey Stults ,  Herbert Yajima

IPC: C07D239/70 ,  C12P17/16

CPC classification number: C07D239/70 ,  C07D403/04 ,  C12P17/165

Abstract: The invention provides new processes for making and purifying salts of hydroxylated cyclopentapyrimidine compounds, which are useful as AKT inhibitors used in the treatment of diseases such as cancer, including the monohydrochloride salt of (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.

Abstract translation: 本发明提供了用于制备和纯化羟基化环戊并嘧啶化合物的盐的新方法，其可用作用于治疗诸如癌症的疾病的AKT抑制剂，包括（S）-2-（4-氯苯基）-1- （4 - （（5R，7R）-7-羟基-5-甲基-6,7-二氢-5H-环戊二烯并[d]嘧啶-4-基）哌嗪-1-基）-3-（异丙基氨基） 1-one。

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：US09315471B2

公开(公告)日：2016-04-19

申请号：US14401089

申请日：2013-05-17

Applicant: Genentech, Inc.

Inventor： Srinivasan Babu ,  Francis Gosselin ,  Yingqing Ran ,  Travis Remarchuk ,  Scott J. Savage ,  Jeffrey Stults ,  Herbert Yajima

IPC: C07D239/70 ,  C07D403/04 ,  C12P17/16

CPC classification number: C07D239/70 ,  C07D403/04 ,  C12P17/165

Abstract: The invention provides new processes for making and purifying salts of hydroxylated cyclopentapyrimidine compounds, which are useful as AKT inhibitors used in the treatment of diseases such as cancer, including the monohydrochloride salt of (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one.

Abstract translation: 本发明提供了用于制备和纯化羟基化环戊并嘧啶化合物的盐的新方法，其可用作用于治疗诸如癌症的疾病的AKT抑制剂，包括（S）-2-（4-氯苯基）-1- （4 - （（5R，7R）-7-羟基-5-甲基-6,7-二氢-5H-环戊二烯并[d]嘧啶-4-基）哌嗪-1-基）-3-（异丙基氨基） 1-one。

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。