公开(公告)号：US11261171B1

公开(公告)日：2022-03-01

申请号：US16680969

申请日：2019-11-12

Applicant: ASTEX THERAPEUTICS LIMITED ,  CANCER RESEARCH TECHNOLOGY LIMITED

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: C07D401/06 ,  A61K31/5377 ,  A61K31/506 ,  A61K31/501 ,  A61K31/496 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/4439 ,  A61P35/00 ,  C07D417/14 ,  C07D409/14 ,  C07D407/14 ,  C07D403/06 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D403/14 ,  C07D487/04 ,  C07B59/00 ,  C07D487/08 ,  A61K45/06

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.

公开(公告)号：US20210276984A1

公开(公告)日：2021-09-09

申请号：US17164045

申请日：2021-02-01

Applicant: ASTEX THERAPEUTICS LIMITED ,  CANCER RESEARCH TECHNOLOGY LIMITED

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.

公开(公告)号：US11059816B2

公开(公告)日：2021-07-13

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: A61K31/553 ,  A61P9/04 ,  A61P11/00 ,  C07D498/04 ,  C07D419/12 ,  C07D249/04 ,  C07D401/12 ,  C07D419/14 ,  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：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：US09783538B2

公开(公告)日：2017-10-10

申请号：US15105360

申请日：2014-12-19

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 Elisabeth Wilsher

IPC: C07D471/04 ,  A61K31/5377

CPC classification number: C07D471/04 ,  A61K31/5377

Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.

公开(公告)号：US09676768B2

公开(公告)日：2017-06-13

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: A61K31/497 ,  A61K31/501 ,  C07D403/04 ,  C07D419/00 ,  C07D471/04 ,  C07D401/06 ,  C07D471/10 ,  C07D403/06 ,  C07D487/10 ,  C07D403/14 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/5377 ,  C07D413/14 ,  C07D487/04 ,  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：US20170000796A1

公开(公告)日：2017-01-05

申请号：US15203424

申请日：2016-07-06

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Gordon SAXTY ,  Christopher Charles Frederick HAMLETT ,  Valerio BERDINI ,  Christopher William MURRAY ,  Patrick René ANGIBAUD ,  Olivier Alexis Georges QUEROLLE ,  Virginie Sophie PONCELET

IPC: A61K31/519

CPC classification number: A61K31/519 ,  A61K45/06 ,  C07D475/00

Abstract: The invention relates to new pteridine 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.

Abstract translation: 本发明涉及新的蝶啶衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法以及所述化合物在治疗疾病中的用途。 癌症。

公开(公告)号：US20160108034A1

公开(公告)日：2016-04-21

申请号：US14855986

申请日：2015-09-16

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Patrick Rene ANGIBAUD ,  Michel OBRINGER ,  Julien Jeremie Joseph MARIN ,  Matthieu JEANTY

IPC: C07D471/04 ,  A61K45/06 ,  A61K31/4545 ,  A61K31/444 ,  A61K31/4375 ,  A61K31/506

CPC classification number: A61K31/4375 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/506 ,  A61K45/06 ,  C07D471/04

Abstract: The invention relates to new naphthyridine 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.

Abstract translation: 本发明涉及新的萘啶衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法以及所述化合物在治疗疾病中的用途。 癌症。

公开(公告)号：US09309242B2

公开(公告)日：2016-04-12

申请号：US14354832

申请日：2012-10-26

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Valerio Berdini ,  Gordon Saxty ,  Patrick Rene Angibaud ,  Olivier Alexis Georges Querolle ,  Virginie Sophie Poncelet ,  Bruno Roux ,  Lieven Meerpoel

IPC: A61K31/4985 ,  C07D241/36 ,  C07D471/04 ,  A61K31/506 ,  A61K31/5377

CPC classification number: A61K31/4985 ,  A61K31/506 ,  A61K31/5377 ,  C07D471/04

Abstract: The invention relates to new pyridopyrazine 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.

Abstract translation: 本发明涉及新的吡啶并吡嗪衍生物化合物，包含所述化合物的药物组合物，用于制备所述化合物的方法以及所述化合物在治疗疾病中的用途。 癌症。

公开(公告)号：US20150353537A1

公开(公告)日：2015-12-10

申请号：US14436319

申请日：2013-10-18

Applicant: ASTEX THERAPEUTICS LIMITED

Inventor： Gianni CHESSARI ,  Christopher Norbert JOHNSON ,  Lee William PAGE ,  Ildiko Maria BUCK ,  James Edward Harvey DAY ,  Steven HOWARD ,  Gordon SAXTY ,  Christopher William MURRAY

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D403/14 ,  C07D471/04 ,  C07D519/00

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.