公开(公告)号：US09975856B2

公开(公告)日：2018-05-22

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 ,  C07D405/04 ,  C07C309/73 ,  C07C69/73 ,  C07F5/04 ,  C07C69/612 ,  C07F5/02

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：US20230242550A1

公开(公告)日：2023-08-03

申请号：US18189623

申请日：2023-03-24

Applicant: Genentech, Inc.

Inventor： Andreas Stumpf ,  Remy Angelaud ,  Andrew McClory ,  Herbert Yajima ,  Chudi Ndubaku ,  Alan Olivero

IPC: C07D498/14 ,  C07D487/04 ,  C07D498/22 ,  A61P35/00 ,  A61K9/00 ,  A61K31/495 ,  A61K31/5383 ,  A61K39/395 ,  A61K45/06

CPC classification number: C07D498/14 ,  C07D487/04 ,  C07D498/22 ,  A61P35/00 ,  A61K9/0053 ,  A61K31/495 ,  A61K31/5383 ,  A61K39/3955 ,  A61K45/06

Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.

公开(公告)号：US20180354970A1

公开(公告)日：2018-12-13

申请号：US15780328

申请日：2016-12-16

Applicant: GENENTECH, INC.

Inventor： Andreas Stumpf ,  Remy Angelaud ,  Andrew McClory ,  Herbert Yajima ,  Chudi Ndubaku ,  Alan Olivero

IPC: C07D498/14 ,  A61P35/00 ,  A61K9/00 ,  A61K45/06 ,  A61K39/395 ,  A61K31/495 ,  A61K31/5383

CPC classification number: C07D498/14 ,  A61K9/0053 ,  A61K31/495 ,  A61K31/5383 ,  A61K39/3955 ,  A61K45/06 ,  A61P35/00 ,  C07D487/04 ,  C07D498/22

Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.

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：US11643421B2

公开(公告)日：2023-05-09

申请号：US17115095

申请日：2020-12-08

Applicant: Genentech, Inc.

Inventor： Andreas Stumpf ,  Remy Angelaud ,  Andrew McClory ,  Herbert Yajima ,  Chudi Ndubaku ,  Alan Olivero

IPC: C07D498/14 ,  C07D487/04 ,  C07D498/22 ,  A61P35/00 ,  A61K9/00 ,  A61K31/495 ,  A61K31/5383 ,  A61K39/395 ,  A61K45/06

CPC classification number: C07D498/14 ,  A61K9/0053 ,  A61K31/495 ,  A61K31/5383 ,  A61K39/3955 ,  A61K45/06 ,  A61P35/00 ,  C07D487/04 ,  C07D498/22

Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.

公开(公告)号：US11414412B2

公开(公告)日：2022-08-16

申请号：US17016900

申请日：2020-09-10

Applicant: Genentech, Inc.

Inventor： Francis Gosselin ,  Andrew McClory ,  Zhigang Cheng

IPC: C07D417/14

Abstract: A process for the manufacture N-(5-((5R,6S)-5-amino-6-fluorooxepan-2-yl)-1-methyl-1H-pyrazol-4-yl)-2-(2,6-difluorophenyl)thiazole-4-carboxamide (I) wherein the vicinal amino fluoro substituents are introduced by treating 5 with sodium chloro((4-nitrophenyl)sulfonyl)amide and N-bromosucinimide and unraveling the resulting substituted aziridine (6) with trimethylamine trihydrofluoride to afford 7 which is further processed to afford 1.

公开(公告)号：US20210253599A1

公开(公告)日：2021-08-19

申请号：US17115095

申请日：2020-12-08

Applicant: Genentech, Inc.

Inventor： Andreas Stumpf ,  Remy Angelaud ,  Andrew McClory ,  Herbert Yajima ,  Chudi Ndubaku ,  Alan Olivero

IPC: C07D498/14 ,  C07D487/04 ,  C07D498/22 ,  A61P35/00 ,  A61K9/00 ,  A61K31/495 ,  A61K31/5383 ,  A61K39/395 ,  A61K45/06

Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.

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：US10906918B2

公开(公告)日：2021-02-02

申请号：US15780328

申请日：2016-12-16

Applicant: GENENTECH, INC.

Inventor： Andreas Stumpf ,  Remy Angelaud ,  Andrew McClory ,  Herbert Yajima ,  Chudi Ndubaku ,  Alan Olivero

IPC: C07D498/14 ,  C07D487/04 ,  C07D498/22 ,  A61P35/00 ,  A61K9/00 ,  A61K31/495 ,  A61K31/5383 ,  A61K39/395 ,  A61K45/06

Abstract: The present disclosure provides for methods for preparing tricyclic PI3K inhibitor compounds in high yield and purity in aqueous solvent systems.

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.