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：US11028100B2

公开(公告)日：2021-06-08

申请号：US16875537

申请日：2020-05-15

Applicant: Genentech, Inc.

Inventor： Paroma Chakravarty ,  Chong Han ,  Sean M. Kelly ,  Karthik Nagapudi ,  Scott Savage

IPC: C07D498/04 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61K9/20

Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.

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：US20170101380A1

公开(公告)日：2017-04-13

申请号：US15287023

申请日：2016-10-06

Applicant: Genentech, Inc.

Inventor： Stephan Bachmann ,  Serena Maria Fantasia ,  Francis Gosselin ,  Chong Han ,  Stefan Hildbrand ,  Theresa Humphries ,  Christian Jenny ,  Ngiap-Kie Lim ,  Andrew McClory ,  Christian Moessner ,  Pankaj Rege ,  Scott Savage ,  Haiming Zhang

IPC: C07D231/56 ,  C07C309/73 ,  C07C69/73 ,  C07F5/04 ,  C07D405/04

CPC classification number: C07D231/56 ,  C07C69/612 ,  C07C69/73 ,  C07C69/738 ,  C07C309/73 ,  C07D405/04 ,  C07F5/025 ,  C07F5/04

Abstract: Processes are described for the preparation of estrogen receptor modulating compound, (E)-3-(4-((E)-2-(2-chloro-4-fluorophenyl)-1-(1H-indazol-5-yl)but-1-en-1-yl)phenyl)acrylic acid I: and salts thereof, and intermediates useful for the preparation of I.

公开(公告)号：US20170247338A1

公开(公告)日：2017-08-31

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

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：US20230167128A1

公开(公告)日：2023-06-01

申请号：US18101951

申请日：2023-01-26

Applicant: Genentech, Inc.

Inventor： Paroma Chakravarty ,  Chong Han ,  Sean M. Kelly ,  Karthik Nagapudi ,  Scott Savage

IPC: C07D498/04 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04

CPC classification number: C07D498/04 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61K9/20

Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[ƒ]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I:





or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.

公开(公告)号：US11591345B2

公开(公告)日：2023-02-28

申请号：US16875545

申请日：2020-05-15

Applicant: Genentech, Inc.

Inventor： Paroma Chakravarty ,  Chong Han ,  Sean M. Kelly ,  Karthik Nagapudi ,  Scott Savage

IPC: C07D498/04 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04 ,  A61K9/20

Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.

公开(公告)号：US20210094970A1

公开(公告)日：2021-04-01

申请号：US16875545

申请日：2020-05-15

Applicant: Genentech, Inc.

Inventor： Paroma Chakravarty ,  Chong Han ,  Sean M. Kelly ,  Karthik Nagapudi ,  Scott Savage

IPC: C07D498/04 ,  A61P35/00 ,  A61P35/02 ,  A61P35/04

Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.

公开(公告)号：US10781219B2

公开(公告)日：2020-09-22

申请号：US16441765

申请日：2019-06-14

Applicant: Genentech, Inc.

Inventor： Francis Gosselin ,  Chong Han ,  Theresa Cravillion ,  Sean M. Kelly ,  Scott Savage

IPC: C07D498/04

Abstract: Methods of making benzoxazepin oxazolidinone compounds as well as synthetic intermediates are described, including compound 18, having the structure:

公开(公告)号：US20180339997A1

公开(公告)日：2018-11-29

申请号：US15963876

申请日：2018-04-26

Applicant: Genentech, Inc.

Inventor： Paroma Chakravarty ,  Chong Han ,  Sean M. Kelly ,  Karthik Nagapudi ,  Scott Savage

IPC: C07D498/04 ,  A61P35/02 ,  A61P35/04

Abstract: The present invention relates to crystalline polymorph forms of (S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide (GDC-0077), having the structure, Formula I: or stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, and processes of preparing the polymorph forms.