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公开(公告)号：US11866428B2
公开(公告)日：2024-01-09
申请号：US17034926
申请日：2020-09-28
发明人： Alison Jo-Anne Woolford , Steven Howard , Ildiko Maria Buck , Gianni Chessari , Christopher Norbert Johnson , Emiliano Tamanini , James Edward Harvey Day , Elisabetta Chiarparin , Thomas Daniel Heightman , Martyn Frederickson , Charlotte Mary Griffiths-Jones
IPC分类号： C07D471/04 , C07D401/06 , C07D471/10 , C07D403/06 , C07D487/10 , C07D403/14 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , C07D413/14 , C07D487/04 , C07D519/00
CPC分类号： C07D471/04 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5025 , A61K31/5377 , C07D401/06 , C07D403/06 , C07D403/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/10 , C07D519/00
摘要： The invention relates to bicyclic heterocycle compounds of formula (I):
or tautomeric or stereochemically isomeric forms, N-oxides, pharmaceutically acceptable salts or the solvates thereof; wherein R1, R2a, R2b, R3a, R3b, R5, R6, R7, R8, R9, p and E are as defined herein; to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.-
公开(公告)号：US20230278989A1
公开(公告)日：2023-09-07
申请号：US18159452
申请日：2023-01-25
发明人： Steven HOWARD , Benjamin David CONS , Jeffrey David ST. DENIS , Charlotte Mary GRIFFITHS-JONES , Steven Douglas HISCOCK , Rhian Sara HOLVEY , Alan Richard BURNS , David COUSIN , Hannah Louise DEXTER , Guillaume François PARRA , John Paul WATTS , Robert JEWELL , Jennifer Ann STOCKWELL , Kim Louise HIRST , Isabelle Anne LEMASSON , David John NASH , James Daniel OSBORNE , Jonas Calleja PRIEDE , Nicholas Paul RICHARDS , Aaron Michael DUMAS , Brian Christopher BISHOP , David PARRY-JONES , Jeremy Peter SCOTT , Meenakshi Sundaram SHANMUGHAM , Peter Richard MULLENS , David Charles LATHBURY , Darren James DIXON , Matthew James GAUNT
IPC分类号： C07D405/06
CPC分类号： C07D405/06 , C07B2200/13
摘要： The invention relates to processes for preparing isoindolin-1-one derivatives, and in particular processes for preparing (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid. The invention also relates to crystalline forms of the compound (2S,3S)-3-(4-chlorophenyl)-3-[(1R)-1-(4-chlorophenyl)-7-fluoro-5-[(1S)-1-hydroxy-1-(oxan-4-yl)propyl]-1-methoxy-3-oxo-2,3-dihydro-1H-isoindol-2-yl]-2-methylpropanoic acid and its salts.
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公开(公告)号：US20230047296A1
公开(公告)日：2023-02-16
申请号：US17495115
申请日：2021-10-06
发明人： Jeffrey K. KERNS , James Callahan , Hongxing Yan , Thomas Daniel Heightman , Charlotte Mary Griffiths-Jones , Alison Jo-Anne Woolford , Tindy Li , Ami Lakdawala Shah , Roderick S. Davis , David Norton , Jeffrey Charles Boehm , Paris L. Hamilton , Nicole Cathleen Goodwin , Yun Jin
IPC分类号： C07D403/10 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/10 , C07D403/14 , C07D413/10 , C07D471/04 , C07D487/04 , C07D498/04 , C07D267/14 , C07D249/18 , C07D233/60 , C07D487/08 , C07D451/02 , A61P9/00 , A61P25/00 , A61P11/00 , A61P27/00 , A61P35/00 , A61P37/00 , C07D233/64 , C07D255/04 , C07D273/01 , C07D405/10
摘要： The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.
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公开(公告)号：US11236047B2
公开(公告)日：2022-02-01
申请号：US16497135
申请日：2018-03-28
IPC分类号： C07D209/48 , C07H21/04 , C07D403/12 , C07D405/12 , C07D405/14 , C07D401/10 , A61P35/00 , C07D403/06 , A61K45/06
摘要： The invention provides a combination comprising: (i) a compound of formula (Io): or a tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims; and (ii) a compound which is SGI-110 or a tautomer or a solvate or a pharmaceutically acceptable salt thereof. Also provided are pharmaceutical compositions containing the combinations and medical uses of the combinations.
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公开(公告)号：US10604509B2
公开(公告)日：2020-03-31
申请号：US15736075
申请日：2016-06-15
发明人： Jeffrey K. Kerns , James Callahan , Thomas Daniel Heightman , Alison Jo-Anne Woolford , Ami Lakdawala Shah , Roderick S. Davis , David Norton , Jeffrey Charles Boehm , Nicole Cathleen Goodwin
IPC分类号： C07D417/10 , C07D403/10 , C07D249/04 , C07D249/18 , C07D401/14 , C07D405/14 , C07D413/14 , C07D401/10 , C07D403/14 , C07D413/10 , C07D471/04 , C07D487/04 , C07D498/04 , C07D267/14 , C07D233/60 , C07D487/08 , C07D451/02 , A61P9/00 , A61P25/00 , A61P11/00 , A61P27/00 , A61P35/00 , A61P37/00 , C07D233/64 , C07D255/04 , C07D273/01 , C07D405/10
摘要： Provided are aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.
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公开(公告)号：US20200079761A1
公开(公告)日：2020-03-12
申请号：US16535931
申请日：2019-08-08
发明人： Gianni CHESSARI , Steven HOWARD , lldiko Maria BUCK , Benjamin David CONS , Christopher Norbert JOHNSON , Rhian Sara HOLVEY , David Charles REES , Jeffrey David ST. DENIS , Emiliano TAMANINI , Bernard Thomas GOLDING , Ian Robert HARDCASTLE , Celine Florence CANO , Duncan Charles MILLER , Martin Edward Mantyla NOBLE , Roger John GRIFFIN , James Daniel OSBORNE , Joanne PEACH , Arwel LEWIS , Kim Louise HIRST , Benjamin Paul WHITTAKER , David Wyn WATSON , Dale Robert MITCHELL
IPC分类号： C07D405/14 , C07D403/06 , C07D405/12 , C07D413/12 , C07D209/48 , A61P35/00 , C07D413/06 , C07D403/12 , C07F9/572
摘要： The invention provides a compound of formula (I): or tautomer or a solvate or a pharmaceutically acceptable salt thereof, wherein the various substituents are as defined in the claims.Also provided are pharmaceutical compositions containing the compounds of formula (I), processes for making the compounds and the medical uses of the compounds.
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公开(公告)号：US10364256B2
公开(公告)日：2019-07-30
申请号：US15765354
申请日：2016-10-06
发明人： James Callahan , Jeffrey K. Kerns , Peng Li , Tindy Li , Brent W. McCleland , Hong Nie , Joseph E. Pero , Thomas Glanmor Davies , Maria Grazia Carr , Charlotte Mary Griffiths-Jones , Thomas Daniel Heightman , David Norton , Marinus Leendert Verdonk , Alison Jo-Anne Woolford , Hendrika Maria Gerarda Willems
IPC分类号： C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D403/14 , C07D405/14 , C07D413/08 , C07D413/14 , C07D417/14 , A61K31/41 , A61K31/4196 , A61K31/445 , A61P11/00 , C07D515/14 , A61K9/00
摘要： The present invention relates to biaryl pyrazole compounds of Formula (I) methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators.
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公开(公告)号：US10272095B2
公开(公告)日：2019-04-30
申请号：US15735977
申请日：2016-06-15
发明人： Jeffrey K. Kerns , James Francis Callahan , Hongxing Yan , Thomas Daniel Heightman , Jeffrey Charles Boehm , Alison Jo-Anne Woolford
IPC分类号： A61K31/5513 , A61K31/421 , A61K31/403 , A61P11/00 , C07D403/06 , C07D413/06 , C07D413/10 , C07D267/14 , C07D498/04 , C07D519/00
摘要： The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.
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公开(公告)号：US20170029419A1
公开(公告)日：2017-02-02
申请号：US15105360
申请日：2014-12-19
发明人： Gianni CHESSARI , Christopher Norbert JOHNSON , Steven HOWARD , James Edward Harvey DAY , Ildiko Maria BUCK , Charlotte Mary GRIFFITHS-JONES , Gordon SAXTY , Emiliano TAMANINI , Nicola Elisabeth WILSHER
IPC分类号： C07D471/04 , A61K31/5377
CPC分类号： C07D471/04 , A61K31/5377
摘要： The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
摘要翻译： 本发明涉及新的双环杂环化合物，包含所述化合物的药物组合物和所述化合物在治疗疾病中的用途。 癌症。
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公开(公告)号：US09493426B2
公开(公告)日：2016-11-15
申请号：US14787089
申请日：2014-04-25
发明人： Patrick René Angibaud , Olivier Alexis Georges Querolle , Isabelle Noëlle Constance Pilatte , Lieven Meerpoel , Virginie Sophie Poncelet
IPC分类号： C07D239/91 , A61K45/06 , A61K31/517 , C07D403/12 , C07D401/14 , C07D405/04 , C07D401/04 , C07D403/04 , C07D403/14 , C07D405/14
CPC分类号： C07D239/91 , A61K31/517 , A61K45/06 , C07D401/04 , C07D401/14 , C07D403/04 , C07D403/12 , C07D403/14 , C07D405/04 , C07D405/14
摘要： The invention relates to new quinazolinone derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer.
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