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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.
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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.
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公开(公告)号：US20230250074A1
公开(公告)日：2023-08-10
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.
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Patent Agency Ranking
![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](/abs-image/US/2023/01/26/US20230028651A1/abs.jpg.150x150.jpg)
公开(公告)号：US20230028651A1
公开(公告)日：2023-01-26
申请号：US17852227
申请日：2022-06-28
Applicant: Genentech, Inc. , Hoffmann-La Roche Inc.
Inventor： 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: C07D495/04
Abstract: 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 PtN/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.
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![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](/abs-image/US/2025/02/13/US20250051351A1/abs.jpg.150x150.jpg)
公开(公告)号：US20250051351A1
公开(公告)日：2025-02-13
申请号：US18680689
申请日：2024-05-31
Applicant: Genentech, Inc. , Hoffmann-La Roche Inc.
Inventor： 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: C07D495/04
Abstract: 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 2and 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.
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公开(公告)号：US20210079004A1
公开(公告)日：2021-03-18
申请号：US17102086
申请日：2020-11-23
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.
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公开(公告)号：US20200062762A1
公开(公告)日：2020-02-27
申请号：US16460889
申请日：2019-07-02
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.
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公开(公告)号：US20180230155A1
公开(公告)日：2018-08-16
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
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.
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