公开(公告)号：US20240034739A1

公开(公告)日：2024-02-01

申请号：US18479596

申请日：2023-10-02

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

Inventor： Allen Yu HONG ,  Nicholas WONG ,  Sean M. KELLY ,  Lauren Elizabeth SIROIS ,  Sara SCHWEGLER ,  Xin LINGHU ,  Francis GOSSELIN ,  Katarzyna Aleksandra PIECHOWICZ ,  Carmela MOLINARO ,  Dennis WETZL

IPC: C07D487/04 ,  C12P7/62 ,  C07D207/273

CPC classification number: C07D487/04 ,  C12P7/62 ,  C07D207/273

Abstract: Processes are provided herein for the preparation of a bicyclic ketone compound of formula (I), or a stereoisomer thereof:






or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3 and n are as defined herein; and compounds prepared by these processes.

公开(公告)号：US20190292201A1

公开(公告)日：2019-09-26

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：US20170368039A1

公开(公告)日：2017-12-28

申请号：US15352184

申请日：2016-11-15

Applicant: Forma TM, LLC ,  Genentech, Inc.

Inventor： BAIR W. Kenneth ,  Timm R. BAUMEISTER ,  Alexandre J. BUCKMELTER ,  Karl H. CLODFELTER ,  Peter DRAGOVICH ,  Francis GOSSELIN ,  Bingsong HAN ,  Jian LIN ,  Dominic J. REYNOLDS ,  Bruce ROTH ,  Chase C. SMITH ,  Zhongguo WANG ,  Po-Wai YUEN ,  Xiaozhang ZHENG

IPC: A61K31/4355 ,  C07D491/048 ,  C07D491/04 ,  C07D487/04 ,  C07D471/04 ,  A61K31/55 ,  A61K31/4365 ,  A61K31/5377 ,  A61K31/519 ,  A61K31/497 ,  A61K31/496 ,  A61K31/437 ,  C07D495/04 ,  A61K45/06

CPC classification number: A61K31/4355 ,  A61K31/4365 ,  A61K31/437 ,  A61K31/496 ,  A61K31/497 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  A61K45/06 ,  C07D471/04 ,  C07D487/04 ,  C07D491/04 ,  C07D491/048 ,  C07D495/04

Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes. An illustrative compound of the invention is shown below:

公开(公告)号：US20250059147A1

公开(公告)日：2025-02-20

申请号：US18816550

申请日：2024-08-27

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

Inventor： Allen Yu HONG ,  Jacob C. TIMMERMAN ,  Francis GOSSELIN ,  Katarzyna Aleksandra PIECHOWICZ ,  Filip PETRONIJEVIC ,  Kurt PUENTENER ,  Anna-Lena GLASS ,  Etienne TRACHSEL

IPC: C07D307/24 ,  B01J31/20 ,  B01J31/22 ,  B01J31/24 ,  C07D307/12 ,  C07D307/14 ,  C07D307/16

Abstract: Provided are phenyltetrahydrofuran compounds that are useful as intermediates in the preparation of pharmaceutical compounds and further provided are processes for the preparation of phenyltetrahydrofuran compounds.

公开(公告)号：US20200255476A1

公开(公告)日：2020-08-13

申请号：US16581116

申请日：2019-09-24

Applicant: Genentech, Inc.

Inventor： Filip PETRONIJEVIC ,  Ngiap-Kie LIM ,  Nicholas WONG ,  Allen HONG ,  Haiyun HOU ,  Xin LINGHU ,  Francis GOSSELIN

IPC: C07K7/64 ,  C07K1/06

Abstract: Methods for making an arylomycin ring of formula t or salts or solvates thereof, wherein R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R5, R10 and Pg1 are as defined herein.

公开(公告)号：US20160297773A1

公开(公告)日：2016-10-13

申请号：US15036741

申请日：2014-11-13

Applicant: F. HOFFMANN-LA ROCHE AG ,  GENENTECH, INC.

Inventor： Hans IDING ,  Reinhard REENTS ,  Michelangelo SCALONE ,  Francis GOSSELIN

IPC: C07D239/70 ,  C12P17/16 ,  C07C271/22

CPC classification number: C07D239/70 ,  C07B2200/07 ,  C07C269/06 ,  C07C271/22 ,  C12P17/165

Abstract: The present invention relates to a process for the preparation of a compound of formula (I), wherein R1 is as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.

公开(公告)号：US20250059155A1

公开(公告)日：2025-02-20

申请号：US18776585

申请日：2024-07-18

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

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：US20220056078A1

公开(公告)日：2022-02-24

申请号：US17517103

申请日：2021-11-02

Applicant: Genentech, Inc.

Inventor： Filip PETRONIJEVIC ,  Ngiap-Kie LIM ,  Nicholas WONG ,  Allen HONG ,  Haiyun HOU ,  Xin LINGHU ,  Francis GOSSELIN

IPC: C07K7/64 ,  C07K1/06

Abstract: Methods for making an arylomycin ring of formula t or salts or solvates thereof, wherein R, R1, R2, R3, R4, R5, R6, R7, R8, R9, R5, R10 and Pg1 are as defined herein.

公开(公告)号：US20240409535A1

公开(公告)日：2024-12-12

申请号：US18652953

申请日：2024-05-02

Applicant: Genentech, Inc. ,  Hoffmann-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

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：US20230250103A1

公开(公告)日：2023-08-10

申请号：US18299622

申请日：2023-04-12

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

CPC classification number: C07D487/04 ,  B01J31/2409 ,  B01J31/2414 ,  B01J2231/40 ,  B01J2531/824 ,  C07B2200/09

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.