公开(公告)号：US20180282349A1

公开(公告)日：2018-10-04

申请号：US15765354

申请日：2016-10-06

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics Limited

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.

公开(公告)号：US20180169110A1

公开(公告)日：2018-06-21

申请号：US15735977

申请日：2016-06-15

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics Limited

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.

公开(公告)号：US20200071310A1

公开(公告)日：2020-03-05

申请号：US16467148

申请日：2017-12-11

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  ASTEX THERAPEUTICS LIMITED

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):

公开(公告)号：US20180179187A1

公开(公告)日：2018-06-28

申请号：US15736075

申请日：2016-06-15

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics, Limited

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.

公开(公告)号：US20170334907A1

公开(公告)日：2017-11-23

申请号：US15585908

申请日：2017-05-03

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 ,  C07D487/10 ,  C07D487/04 ,  C07D471/10 ,  C07D413/14 ,  C07D403/14 ,  A61K31/496 ,  C07D401/06 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/5025 ,  A61K31/501 ,  A61K31/497 ,  C07D403/06 ,  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：US20250084077A1

公开(公告)日：2025-03-13

申请号：US18808878

申请日：2024-08-19

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Anthony William James COOPER ,  Nicole Cathleen GOODWIN ,  Charlotte Mary GRIFFITHS-JONES ,  Thomas Daniel HEIGHTMAN ,  Jeffrey K. KERNS ,  Hendrika Maria Gerarda WILLEMS ,  Hongxing YAN

IPC: C07D419/12 ,  C07D249/04 ,  C07D401/12 ,  C07D419/14 ,  C07D498/04 ,  C07D513/04

Abstract: The present invention relates to ether-linked triazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the invention relates to compounds of Formula(I), and pharmaceutically acceptable salts thereof:

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.

公开(公告)号：US20200071317A1

公开(公告)日：2020-03-05

申请号：US16468777

申请日：2017-12-11

Applicant: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED ,  ASTEX THERAPEUTICS LIMITED

Inventor： Anthony William James COOPER ,  Nicole Cathleen GOODWIN ,  Charlotte Mary GRIFFITHS-JONES ,  Thomas Daniel HEIGHTMAN ,  Jeffrey K. KERNS ,  Hendrika Maria Gerarda WILLEMS ,  Hongxing YAN

IPC: C07D419/12 ,  C07D419/14 ,  C07D513/04 ,  C07D249/04 ,  C07D401/12 ,  C07D498/04

Abstract: The present invention relates to ether-linked triazole compounds, methods of making them, pharmaceutical compositions containing them and their use as NRF2 activators. In particular, the invention relates to compounds of Formula (I), and pharmaceutically acceptable salts thereof:

公开(公告)号：US20180282283A1

公开(公告)日：2018-10-04

申请号：US15765377

申请日：2016-10-06

Applicant: GlaxoSmithKline Intellectual Property Development Limited ,  Astex Therapeutics Limited

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.