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：US20240409539A1

公开(公告)日：2024-12-12

申请号：US18747301

申请日：2024-06-18

Applicant: GENENTECH, INC.

Inventor： Karthik Nagapudi ,  Yuan Liu ,  Shuai Wang ,  Wei Zhang

IPC: C07D471/04 ,  A61J3/10 ,  A61K9/00 ,  A61K9/16 ,  A61K9/20 ,  C07C317/14

Abstract: Novel salts, hydrates, and solvates of Compound I, and methods of making and using the same, and related dosage forms thereof, are disclosed.

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：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：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.