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公开(公告)号:US11603367B2
公开(公告)日:2023-03-14
申请号:US16498207
申请日:2018-03-28
Inventor: Steven Howard , Jeffrey David St. Denis , Charlotte Mary Griffiths-Jones , Steven Douglas Hiscock , Alan Richard Burns , David Cousin , Kim Louise Hirst , James Daniel Osborne , Jonas Calleja Priede , Aaron Michael Dumas , Brian Christopher Bishop , David Parry-Jones , Jeremy Peter Scott , Meenakshi Sundaram Shanmugham , Peter Richard Mullens , Darren James Dixon , Matthew James Gaunt
IPC: C07D405/06
Abstract: 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:US20220204503A1
公开(公告)日:2022-06-30
申请号:US17643083
申请日:2021-12-07
Applicant: ASTEX THERAPEUTICS LIMITED
Inventor: Gianni CHESSARI , Christopher Norbert JOHNSON , Steven HOWARD , James Edward Harvey DAY , Ildiko Maria BUCK , Charlotte Mary GRIFFITHS-JONES , Gordon SAXTY , Emiliano TAMANINI , Nicola Elizabeth WILSHER
IPC: C07D471/04 , A61K31/5377
Abstract: 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.
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公开(公告)号:US20220135544A1
公开(公告)日:2022-05-05
申请号:US17451601
申请日:2021-10-20
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Gordon SAXTY , Christopher William Murray , Valerio Berdini , Gilbert Ebai Besong , Christopher Charles Frederick Hamlett , Christopher Norbert Johnson , Steven John Woodhead , Michael Reader , David Charles Rees , Laurence Anne Mevellec , Patrick René Angibaud , Eddy Jean Edgard Freyne , Tom Cornelis Hortense Govaerts , Johan Erwin Edmond Weerts , Timothy Pietro Suren Perera , Ronaldus Arnodus Hendrika Joseph Gilissen , Berthold Wroblowski , Jean Fernand Armand Lacrampe , Alexandra Papanikos , Olivier Alexis Georges Querolle , Elisabeth Thérèse Jeanne Pasquier , Isabelle Noëlle Constance Pilatte , Pascal Ghislain André Bonnet , Werner Constant Johan Embrechts , Rhalid Akkari , Lieven Meerpoel
IPC: C07D403/04 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D487/08 , A61K31/498 , A61K31/5377 , A61K45/06 , C07D491/113 , C07D401/14 , C07F9/6524
Abstract: The invention relates to new quinoxaline 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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公开(公告)号:US10981898B2
公开(公告)日:2021-04-20
申请号:US16535931
申请日:2019-08-08
Inventor: Gianni Chessari , Steven Howard , Ildiko 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 Mäntylä Noble , Roger John Griffin , James Daniel Osborne , Joanne Peach , Arwel Lewis , Kim Louise Hirst , Benjamin Paul Whittaker , David Wyn Watson , Dale Robert Mitchell
IPC: C07D405/14 , C07D403/06 , C07D405/12 , C07D413/12 , C07D209/48 , C07D413/06 , C07D403/12 , C07F9/572 , A61P35/00
Abstract: 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:US20200325134A1
公开(公告)日:2020-10-15
申请号:US16795117
申请日:2020-02-19
Applicant: ASTEX THERAPEUTICS LIMITED
Inventor: Gianni CHESSARI , Christopher Norbert JOHNSON , Steven HOWARD , James Edward Harvey DAY , Ildiko Maria BUCK , Charlotte Mary GRIFFITHS-JONES , Gordon SAXTY , Emiliano TAMANINI , Nicola Elizabeth WILSHER
IPC: C07D471/04 , A61K31/5377
Abstract: 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.
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公开(公告)号:US20200071310A1
公开(公告)日:2020-03-05
申请号:US16467148
申请日:2017-12-11
Inventor: Brian W. BUDZIK , Peng LI , Joseph E. PERO , Charlotte Mary GRIFFITHS-JONES , Thomas Daniel HEIGHTMAN , David NORTON , Hendrika Maria Gerarda WILLEMS , Alison Jo-Anne WOOLFORD
IPC: C07D413/08 , C07D413/14 , C07D403/08 , C07D401/14 , C07D417/14 , C07D419/14 , A61P11/00
Abstract: The present invention relates to N-aryl pyrazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 regulators. In particular, the compounds of this invention include a compound of Formula (I):
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公开(公告)号:US10421747B2
公开(公告)日:2019-09-24
申请号:US15856998
申请日:2017-12-28
Applicant: ASTEX THERAPEUTICS LTD
Inventor: Wim Vermeulen , Steven Anna Hostyn , Filip Albert Celine Cuyckens , Russell Mark Jones , Diego Fernando Domenico Broggini
IPC: C07D403/14 , A61K31/5513 , A61K31/4985 , A61P35/00
Abstract: The invention relates to new quinoxaline 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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公开(公告)号:US20190224212A1
公开(公告)日:2019-07-25
申请号:US16375047
申请日:2019-04-04
Inventor: Jeffrey K. Kerns , James Francis Callahan , Hongxing Yan , Thomas Daniel Heightman , Jeffrey Charles Boehm , Alison Jo-Anne Woolford
IPC: A61K31/5513 , A61K31/421 , A61K31/403 , A61P11/00 , C07D519/00 , C07D403/06 , C07D267/14 , C07D413/10 , C07D413/06 , C07D498/04
Abstract: 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:US10351530B2
公开(公告)日:2019-07-16
申请号:US15765377
申请日:2016-10-06
Inventor: James Callahan , Jeffrey K. Kerns , Tindy Li , Brent W. McCleland , Hong Nie , Joseph E. Pero , Thomas Glanmor Davies , Charlotte Mary Griffiths-Jones , Thomas Daniel Heightman , Steven Howard , David Norton , Marinus Leendert Verdonk , Alison Jo-Anne Woolford
IPC: C07D231/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D403/14
Abstract: The present invention relates to arylcyclohexyl 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:US20190002454A1
公开(公告)日:2019-01-03
申请号:US16122968
申请日:2018-09-06
Inventor: Jeffrey Charles BOEHM , Thomas Glanmor DAVIES , Alison Jo-Anne WOOLFORD , Charlotte Mary GRIFFITHS-JONES , Hendrika Maria Gerarda WILLEMS , David NORTON , Gordon SAXTY , Thomas Daniel HEIGHTMAN , Tindy LI , Jeffrey K. KERNS , Roderick S. DAVIS , Hongxing YAN
IPC: C07D417/10 , C07D405/12 , C07D249/18 , C07D281/02 , C07D291/08 , C07D401/12 , C07D403/12 , C07D417/14 , C07D419/10 , C07D419/14 , C07D471/04 , C07D513/04 , C07D515/04
Abstract: The present invention relates to bis aryl analogs, pharmaceutical compositions containing them and their use as Nrf2 regulators.
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