公开(公告)号：US11873305B2

公开(公告)日：2024-01-16

申请号：US17360593

申请日：2021-06-28

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

Inventor： Haiming Zhang ,  Jie Xu ,  Georg Wuitschik ,  Remy Angelaud ,  Sebastian Herold ,  Alfred Stutz ,  Tobias Bruetsch ,  Johannes Burkhard

IPC: C07D209/10 ,  C07D487/04

CPC classification number: C07D487/04

Abstract: Provided herein are processes for the preparation of indolyl intermediates using Wenker Synthesis for the total synthesis of SERD compounds useful in the treatment of cancer.

公开(公告)号：US11066389B2

公开(公告)日：2021-07-20

申请号：US16718602

申请日：2019-12-18

Applicant: Genentech, Inc.

Inventor： Jinguang Lin ,  Alexandra Chestakova ,  Wei Gu ,  Hans Iding ,  Jing Li ,  Xin Linghu ,  Patrik Meier ,  Chunbo Sha ,  Jeffrey Stults ,  Youchu Wang ,  Haiming Zhang ,  Jianqian Zhang ,  Tao Zhang

IPC: C07D401/14 ,  C07D401/04 ,  A61P35/00 ,  A61P25/00 ,  A61P29/00 ,  C12P17/16

Abstract: The present invention provides a process for the manufacture of a compound of formula VIIIa and salts forms of VIIIa where Rc is an aryl sulfonic acid

公开(公告)号：US10385058B2

公开(公告)日：2019-08-20

申请号：US15841828

申请日：2017-12-14

Applicant: Genentech, Inc.

Inventor： Danial Beaudry ,  Theresa Cravillion ,  Francis Gosselin ,  Ngiap-Kie Lim ,  Sushant Malhotra ,  Qingping Tian ,  Haiming Zhang ,  Alexander Gmehling ,  Alec Fettes ,  Stephan Bachmann

IPC: C07D487/04 ,  B01J31/24

Abstract: Methods for preparing the Bruton's Tyrosine Kinase (“BTK”) inhibitor compound 2-{3′-hydroxymethyl-1-methyl-5-[5-((S)-2-methyl-4-oxetan-3-yl-piperazin-1-yl)-pyridin-2-ylamino]-6-oxo-1,6-dihydro-[3,4′]bipyridinyl-2′-yl}-7,7-dimethyl-3,4,7,8-tetrahydro-2H,6H-cyclopenta[4,5]pyrrolo[1,2-a]pyrazin-1-one are provided. Methods for preparing tricyclic lactam compounds are also provided.

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：US09969735B2

公开(公告)日：2018-05-15

申请号：US15652776

申请日：2017-07-18

Applicant: Genentech, Inc.

Inventor： Ngiap-Kie Lim ,  Haiming Zhang ,  Chong Han

IPC: C07D471/14

CPC classification number: C07D471/14 ,  C07D471/04

Abstract: Processes are described for the preparation of tricyclic lactam compound of Formula (I), having the structure and intermediates useful for the preparation of (I).

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：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：US20220081413A1

公开(公告)日：2022-03-17

申请号：US17398345

申请日：2021-08-10

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

Inventor： Ngiap-Kie Lim ,  Jeff Shen ,  Lauren E. Sirois ,  Jacob C. Timmerman ,  Etienne Trachsel ,  Nicholas A. White ,  Jie Xu ,  Haiming Zhang ,  Stephan Bachmann ,  Raphael Bigler ,  Kyle Bradley Pascual Clagg ,  Antonio Dipasquale ,  Francis Gosselin ,  Ugo Jonathan Orcel ,  Roland Christoph Meier

IPC: C07D401/14

Abstract: Provided herein are methods of synthesizing quinazoline compounds comprising at least one atropisomeric center.

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：US20170313704A1

公开(公告)日：2017-11-02

申请号：US15652776

申请日：2017-07-18

Applicant: Genentech, Inc.

Inventor： Ngiap-Kie Lim ,  Haiming Zhang ,  Chong Han

IPC: C07D471/14

CPC classification number: C07D471/14 ,  C07D471/04

Abstract: Processes are described for the preparation of tricyclic lactam compound of Formula (I), having the structure and intermediates useful for the preparation of (I).