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公开(公告)号:US20180282349A1
公开(公告)日:2018-10-04
申请号:US15765354
申请日:2016-10-06
Inventor: 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 Leedert VERDONK , Alison Jo-Anne WOOLFORD , Hendrika Maria Gerarda WILLEMS
IPC: C07D515/14 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D403/14 , C07D413/14 , A61P11/00 , A61K9/00
CPC classification number: C07D515/14 , A61K9/0019 , A61K9/0053 , A61K9/0078 , A61P11/00 , C07D401/04 , C07D401/06 , C07D401/10 , C07D401/12 , C07D401/14 , C07D403/08 , C07D403/10 , C07D403/14 , C07D405/14 , C07D413/08 , C07D413/14 , C07D417/14
Abstract: 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:US20180169110A1
公开(公告)日:2018-06-21
申请号:US15735977
申请日:2016-06-15
Inventor: Jeffrey K. KERNS , Jamas Francis CALLAHAN , Hongxing YAN , Thomas Daniel HEIGHTMAN , Jeffrey Charles BOEHM , Alison Jo-Anne WOOLFORD
IPC: A61K31/5513 , A61K31/421 , A61K31/403 , A61P11/00
CPC classification number: A61K31/5513 , A61K31/403 , A61K31/421 , A61P11/00 , C07D267/14 , C07D403/06 , C07D413/06 , C07D413/10 , C07D498/04 , C07D519/00
Abstract: The present invention relates to aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.
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3.
公开(公告)号:US20160083377A1
公开(公告)日:2016-03-24
申请号:US14836326
申请日:2015-08-26
Applicant: ASTEX THERAPEUTICS LIMITED
Inventor: Ildiko Maria BUCK , Gianni CHESSARI , Steven HOWARD , David Charles REES , Alison Jo-Anne WOOLFORD
IPC: C07D471/04
CPC classification number: C07D471/04 , A61K31/437 , A61K31/4985 , A61K31/519 , A61K31/5383 , A61K31/5386 , A61K45/06 , C07D498/04 , C07D498/10 , A61K2300/00
Abstract: 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, R2, R3, A, W, U and V 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.
Abstract translation: 本发明涉及式(I)的双环杂环化合物:或互变异构体或立体化学异构形式,N-氧化物,药学上可接受的盐或其溶剂合物; 其中R1,R2,R3,A,W,U和V如本文所定义; 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:US20240199607A1
公开(公告)日:2024-06-20
申请号:US18499940
申请日:2023-11-01
Applicant: ASTEX THERAPEUTICS LIMITED
Inventor: 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: C07D471/04 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , C07D401/06 , C07D403/06 , C07D403/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/10 , C07D519/00
CPC classification number: C07D471/04 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , C07D401/06 , C07D403/06 , C07D403/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/10 , C07D519/00
Abstract: 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:US20210122749A1
公开(公告)日:2021-04-29
申请号:US17034926
申请日:2020-09-28
Applicant: ASTEX THERAPEUTICS LIMITED
Inventor: 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: 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
Abstract: 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.
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公开(公告)号:US20180282283A1
公开(公告)日:2018-10-04
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 , C07D403/10 , C07D401/10 , C07D403/08 , C07D401/14 , C07D403/14
CPC classification number: 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:US20180179167A1
公开(公告)日:2018-06-28
申请号:US15735971
申请日:2016-06-15
Inventor: Jeffrey K. KERNS , Tindy LI , Hongxing YAN , Thomas Daniel HEIGHTMAN , Alison Jo-Anne WOOLFORD , Charlotte Mary GRIFFITHS-JONES , Hendrika Maria Gerarda WILLEMS
IPC: C07D249/18 , A61P11/00
CPC classification number: C07D249/18 , A61P11/00
Abstract: The present invention relates to aryl analogs Formula (I), pharmaceutical compositions containing them and their use as Nrf2 regulators.
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8.
公开(公告)号:US20150291586A1
公开(公告)日:2015-10-15
申请号:US14663534
申请日:2015-03-20
Applicant: ASTEX THERAPEUTICS LIMITED
Inventor: 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: C07D471/04 , A61K31/496 , C07D403/14 , C07D471/10 , C07D487/10 , C07D519/00 , C07D413/14 , C07D487/04 , A61K31/5025 , A61K31/506 , A61K31/501 , A61K31/497 , C07D403/06 , A61K31/5377
CPC classification number: C07D471/04 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/5025 , A61K31/506 , A61K31/5377 , C07D401/06 , C07D403/06 , C07D403/14 , C07D413/14 , C07D471/10 , C07D487/04 , C07D487/10 , C07D519/00
Abstract: 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.
Abstract translation: 本发明涉及式(I)的双环杂环化合物:或互变异构体或立体化学异构形式,N-氧化物,药学上可接受的盐或其溶剂合物; 其中R1,R2a,R2b,R3a,R3b,R5,R6,R7,R8,R9,p和E如本文所定义; 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: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:US20180179187A1
公开(公告)日:2018-06-28
申请号:US15736075
申请日:2016-06-15
Inventor: 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
IPC: C07D403/10 , C07D413/10 , C07D471/04 , C07D413/14 , C07D255/04 , C07D498/04 , C07D405/10 , C07D487/04 , C07D273/01 , C07D401/14 , C07D403/14 , C07D405/14 , C07D233/64 , C07D401/10
CPC classification number: C07D403/10 , A61P9/00 , A61P11/00 , A61P25/00 , A61P27/00 , A61P35/00 , A61P37/00 , C07D233/60 , C07D233/64 , C07D249/18 , C07D255/04 , C07D267/14 , C07D273/01 , C07D401/10 , C07D401/14 , C07D403/14 , C07D405/10 , C07D405/14 , C07D413/10 , C07D413/14 , C07D451/02 , C07D471/04 , C07D487/04 , C07D487/08 , C07D498/04
Abstract: Provided are aryl analogs, pharmaceutical compositions containing them and their use as NRF2 regulators.
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