公开(公告)号：US09862689B2

公开(公告)日：2018-01-09

申请号：US15036741

申请日：2014-11-13

Applicant: GENENTECH, INC.

Inventor： Hans Iding ,  Reinhard Reents ,  Michelangelo Scalone ,  Francis Gosselin

IPC: C07D239/70 ,  C07C269/06 ,  C07C271/22 ,  C12P17/16

CPC classification number: C07D239/70 ,  C07B2200/07 ,  C07C269/06 ,  C07C271/22 ,  C12P17/165

Abstract: The present invention relates to a process for the preparation of a compound of formula (I), wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

公开(公告)号：US20200062717A1

公开(公告)日：2020-02-27

申请号：US16555842

申请日：2019-08-29

Applicant: GENENTECH, INC.

Inventor： Hans Iding ,  Reinhard Reents ,  Michelangelo Scalone ,  Francis Gosselin

IPC: C07D239/70 ,  C12P17/16 ,  C07C271/22 ,  C07C269/06

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

公开(公告)号：US20200010428A1

公开(公告)日：2020-01-09

申请号：US16574933

申请日：2019-09-18

Applicant: F. HOFFMANN-LA ROCHE AG ,  GENENTECH INC.

Inventor： Francis Gosselin ,  Chong Han ,  Hans Iding ,  Reinhard Reents ,  Scott Savage ,  Beat Wirz

IPC: C07D239/70 ,  C07B57/00 ,  C07D239/42 ,  C07D239/54 ,  C12N9/78 ,  C12P41/00 ,  C07C253/30 ,  C07C253/34 ,  C07C255/22

Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (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). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

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：US20250009749A1

公开(公告)日：2025-01-09

申请号：US18605258

申请日：2024-03-14

Applicant: Genentech, Inc.

Inventor： Reinhard Reents ,  Pirmin Hidber ,  Andre Hell ,  Peter Steidle ,  Martin Wunderlich ,  Marie Pepelnjak ,  Francis Gosselin ,  Edward Yost

IPC: A61K31/517 ,  A61K9/20 ,  A61K9/28

Abstract: The present invention relates to pharmaceutical compositions comprising Akt protein kinase inhibitors with therapeutic activity against diseases such as cancer as well as processes for their preparation and their use as medicament.

公开(公告)号：US20180086722A1

公开(公告)日：2018-03-29

申请号：US15827985

申请日：2017-11-30

Applicant: GENENTECH, INC.

Inventor： Hans Iding ,  Reinhard Reents ,  Michelangelo Scalone ,  Francis Gosselin

IPC: C07D239/70 ,  C12P17/16 ,  C07C271/22 ,  C07C269/06

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

公开(公告)号：US10858324B2

公开(公告)日：2020-12-08

申请号：US16555842

申请日：2019-08-29

Applicant: GENENTECH, INC.

Inventor： Hans Iding ,  Reinhard Reents ,  Michelangelo Scalone ,  Francis Gosselin

IPC: A61K31/517 ,  C07D239/70 ,  C07C269/06 ,  C07C271/22 ,  C12P17/16

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

公开(公告)号：US10457648B2

公开(公告)日：2019-10-29

申请号：US15514188

申请日：2015-09-25

Applicant: F. HOFFMANN-LA ROCHE AG ,  GENENTECH, INC.

Inventor： Francis Gosselin ,  Chong Han ,  Hans Iding ,  Reinhard Reents ,  Scott Savage ,  Beat Wirz

IPC: C07D239/70 ,  C07D239/54 ,  C07D239/42 ,  C07C253/30 ,  C07C255/22 ,  C07B57/00 ,  C12P41/00 ,  C07C253/34 ,  C12N9/78

Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (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). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.

公开(公告)号：US10435378B2

公开(公告)日：2019-10-08

申请号：US15827985

申请日：2017-11-30

Applicant: GENENTECH, INC.

Inventor： Hans Iding ,  Reinhard Reents ,  Michelangelo Scalone ,  Francis Gosselin

IPC: C12P9/00 ,  C07D239/70 ,  C07C269/06 ,  C07C271/22 ,  C12P17/16

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.