专利检索 ap:("Genentech, Inc.") AND inv:"Stephan Bachmann" 第 1 页

1.

发明授权
Synthesis of a bis-mesylate salt of 4-amino-N-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto 有权

公开(公告)号：US11999749B2

公开(公告)日：2024-06-04

申请号：US17852227

申请日：2022-06-28

申请人： Genentech, Inc. , Hoffmann-La Roche Inc.

发明人： Francis Gosselin , Stefan G. Koenig , Eduardo V. Mercado-Marin , Andreas Stumpf , Daniel Zell , Haiming Zhang , Stephan Bachmann , Diane E. Carrera , Michael E. Dalziel , Yonghui Ge , Jie Zhang , Raphael Bigler , Laure Elizabeth Simone Finet , Regis Jean Georges Mondiere , Yuki Nakagawa

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N′,N′-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.

2.

发明授权
Process for preparing BTK inhibitors 有权

公开(公告)号：US10882864B2

公开(公告)日：2021-01-05

申请号：US16460889

申请日：2019-07-02

申请人： Genentech, Inc.

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

IPC分类号： C07D487/04 , B01J31/24

摘要： 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.

3.

发明授权
Process for synthesis of quinazoline compounds 有权

公开(公告)号：US12071422B2

公开(公告)日：2024-08-27

申请号：US18164302

申请日：2023-02-03

申请人： Genentech, Inc. , Hoffmann-La Roche Inc.

发明人： 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分类号： C07D401/04 , B01J23/44 , B01J23/755

CPC分类号： C07D401/04 , B01J23/44 , B01J23/755

摘要： 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.

4.

发明申请
SYNTHESIS OF QUINAZOLINE COMPOUNDS 有权

公开(公告)号：US20220081413A1

公开(公告)日：2022-03-17

申请号：US17398345

申请日：2021-08-10

申请人： Genentech, Inc. , Hoffmann-La Roche Inc.

发明人： 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分类号： C07D401/14

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

5.

发明申请
PROCESS FOR THE PREPARATION OF (E)-3-(4-((E)-2-(2-CHLORO-4-FLUOROPHENYL)-1-(1H-INDAZOL-5-YL)BUT-1-EN-1-YL)PHENYL)ACRYLIC ACID 审中-公开

公开(公告)号：US20170101380A1

公开(公告)日：2017-04-13

申请号：US15287023

申请日：2016-10-06

申请人： Genentech, Inc.

发明人： 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分类号： C07D231/56 , C07C309/73 , C07C69/73 , C07F5/04 , C07D405/04

CPC分类号： C07D231/56 , C07C69/612 , C07C69/73 , C07C69/738 , C07C309/73 , C07D405/04 , C07F5/025 , C07F5/04

摘要： 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.

6.

发明授权
Process for preparing BTK inhibitors 有权

公开(公告)号：US10385058B2

公开(公告)日：2019-08-20

申请号：US15841828

申请日：2017-12-14

申请人： Genentech, Inc.

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

IPC分类号： C07D487/04 , B01J31/24

摘要： 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.