公开(公告)号：US12071422B2

公开(公告)日：2024-08-27

申请号：US18164302

申请日：2023-02-03

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

Inventor： 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: C07D401/04 ,  B01J23/44 ,  B01J23/755

CPC classification number: C07D401/04 ,  B01J23/44 ,  B01J23/755

Abstract: 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.

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：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.