公开(公告)号：US20170247338A1

公开(公告)日：2017-08-31

申请号：US15514188

申请日：2015-09-25

申请人： F. HOFFMANN-LA ROCHE AG ,  GENENTECH, INC.

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

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

摘要： 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：US10457648B2

公开(公告)日：2019-10-29

申请号：US15514188

申请日：2015-09-25

申请人： F. HOFFMANN-LA ROCHE AG ,  GENENTECH, INC.

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

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

摘要： 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：US20200010428A1

公开(公告)日：2020-01-09

申请号：US16574933

申请日：2019-09-18

申请人： F. HOFFMANN-LA ROCHE AG ,  GENENTECH INC.

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

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

摘要： 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

申请人： Genentech, Inc.

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

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

摘要： 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：US09790190B2

公开(公告)日：2017-10-17

申请号：US15593064

申请日：2017-05-11

申请人： Array BioPharma Inc. ,  Genentech, Inc.

发明人： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC分类号： C07D403/00 ,  C07D239/42 ,  C07D403/04

CPC分类号： C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

摘要： The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

公开(公告)号：US20180258054A1

公开(公告)日：2018-09-13

申请号：US15782620

申请日：2017-10-12

申请人： Array BioPharma Inc. ,  Genentech, Inc.

发明人： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC分类号： C07D239/42 ,  C07D403/04

CPC分类号： C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

摘要： The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

公开(公告)号：US09676730B2

公开(公告)日：2017-06-13

申请号：US15204715

申请日：2016-07-07

申请人： Array BioPharma Inc. ,  Genentech, Inc.

发明人： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC分类号： C07D239/70 ,  C07D239/42 ,  C07D239/30 ,  C07D403/04

CPC分类号： C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

摘要： The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

公开(公告)号：US20160318877A1

公开(公告)日：2016-11-03

申请号：US15204715

申请日：2016-07-07

申请人： Array BioPharma Inc. ,  Genentech, Inc.

发明人： David Askin ,  Chong Han ,  Jonathan W. Lane ,  Travis Remarchuk ,  Sagar Shakya ,  C. Gregory Sowell ,  Keith L. Spencer ,  Peter J. Stengel

IPC分类号： C07D239/42

CPC分类号： C07D239/42 ,  C07D239/30 ,  C07D239/70 ,  C07D403/04

摘要： The invention provides processes for preparing a compound of formula I and salts thereof, wherein R1 is defined herein, and compounds and intermediates of said formula.

摘要翻译： 和其盐，其中R1如本文所定义，以及所述式的化合物和中间体。

公开(公告)号：US09221813B2

公开(公告)日：2015-12-29

申请号：US14396346

申请日：2013-04-22

申请人： Genentech, Inc.

发明人： Chong Han

IPC分类号： C07D401/10 ,  C07D471/04

CPC分类号： C07D471/04

摘要： The invention provides intermediates and processes of preparation thereof useful in the preparation of compounds that can be used as CHK1 inhibitors.

摘要翻译： 本发明提供了可用于制备可用作CHK1抑制剂的化合物的中间体及其制备方法。

公开(公告)号：US12071422B2

公开(公告)日：2024-08-27

申请号：US18164302

申请日：2023-02-03

申请人： Genentech, Inc. ,  Hoffmann-La Roche Inc.

发明人： Rene Lebl ,  Ngiap Kie Lim ,  Roland Christoph Meier ,  Ugo Jonathan Orcel ,  Joerg Sedelmeier ,  Jeff Shen ,  Lauren Elizabeth Sirois ,  Jacob C. Timmerman ,  Etienne Trachsel ,  Nicholas Andrew White ,  Jie Xu ,  Haiming Zhang ,  Stephan Bachmann ,  Thomas Michael Bass ,  Raphael Bigler ,  Johannes Adrian Burkhard ,  Kyle Bradley Pascual Clagg ,  Francis Gosselin ,  Chong Han ,  Dainis Kaldre ,  Sean M. Kelly ,  Sebastian Herold ,  Christian Leitner

IPC分类号： C07D401/04 ,  B01J23/44 ,  B01J23/755

CPC分类号： C07D401/04 ,  B01J23/44 ,  B01J23/755

摘要： Provided herein are methods to synthesize compounds useful in the treatment of cancer where such compounds comprise a quinazolinyl core moiety and at least one stereoisomeric or atropisomeric moiety.