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：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.

公开(公告)号：US11780834B2

公开(公告)日：2023-10-10

申请号：US17110607

申请日：2020-12-03

Applicant: Hoffmann-La Roche Inc. ,  GENENTECH, INC.

Inventor： Cheol Keun Chung ,  Jie Xu ,  Hans Iding ,  Kyle Clagg ,  Michael Dalziel ,  Alec Fettes ,  Francis Gosselin ,  Ngiap-Kie Lim ,  Andrew McClory ,  Haiming Zhang ,  Paroma Chakravarty ,  Karthik Nagapudi ,  Sarah Robinson

IPC: C07D471/04 ,  C07D403/14

CPC classification number: C07D471/04 ,  C07D403/14 ,  C07B2200/13

Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

公开(公告)号：US10954234B2

公开(公告)日：2021-03-23

申请号：US16443515

申请日：2019-06-17

Applicant: Genentech, Inc. ,  Hoffman-La Roche, Inc.

Inventor： Cheol Keun Chung ,  Jie Xu ,  Hans Iding ,  Kyle Clagg ,  Michael Dalziel ,  Alec Fettes ,  Francis Gosselin ,  Ngiap-Kie Lim ,  Andrew McClory ,  Haiming Zhang ,  Paroma Chakravarty ,  Karthik Nagapudi ,  Sarah Robinson

IPC: C07D471/04 ,  C07D403/14 ,  A61P35/00 ,  A61P35/04

Abstract: Provided herein are solid forms, salts, and formulations of 3-((1R,3R)-1-(2,6-difluoro-4-((1-(3-fluoropropyl)azetidin-3-yl)amino)phenyl)-3-methyl-1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indol-2-yl)-2,2-difluoropropan-1-ol, processes and synthesis thereof, and methods of their use in the treatment of cancer.

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：US11066389B2

公开(公告)日：2021-07-20

申请号：US16718602

申请日：2019-12-18

Applicant: Genentech, Inc.

Inventor： Jinguang Lin ,  Alexandra Chestakova ,  Wei Gu ,  Hans Iding ,  Jing Li ,  Xin Linghu ,  Patrik Meier ,  Chunbo Sha ,  Jeffrey Stults ,  Youchu Wang ,  Haiming Zhang ,  Jianqian Zhang ,  Tao Zhang

IPC: C07D401/14 ,  C07D401/04 ,  A61P35/00 ,  A61P25/00 ,  A61P29/00 ,  C12P17/16

Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid

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.