公开(公告)号：US11814370B2

公开(公告)日：2023-11-14

申请号：US16339056

申请日：2017-10-06

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Matthew D. Cheeseman ,  A. Elisa Pasqua ,  Michael J. Tucker

IPC: C07D405/12 ,  C07B59/00 ,  A61P35/00

CPC classification number: C07D405/12 ,  C07B59/002 ,  A61P35/00 ,  C07B2200/05

Abstract: The present invention relates to N-(5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-fluorophenyl)-2-((4-ethylpiperazin-1-yl)methyl)quinoline-6-carboxamide, or a pharmaceutically acceptable salt or solvate thereof, wherein at least one hydrogen atom has been substituted with a deuterium atom. Other aspects include pharmaceutical compositions comprising said compounds and medical uses and methods of treatment using said compounds.

公开(公告)号：US20220220097A1

公开(公告)日：2022-07-14

申请号：US17406640

申请日：2021-08-19

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Carl Rye ,  Nicola Chessum ,  Matthew D. Cheeseman ,  Adele E. Pasqua ,  Kurt G. Pike ,  Paul F. Faulder

IPC: C07D405/12 ,  C07D405/14 ,  C07D319/18 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/056

Abstract: The present invention relates to compounds of formula I wherein A1, A2 R4 and Q are as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

公开(公告)号：US20170037036A1

公开(公告)日：2017-02-09

申请号：US15332472

申请日：2016-10-24

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Carl Rye ,  Nicola Chessum ,  Matthew Cheeseman ,  Adele E. Pasqua ,  Kurt G. Pike ,  Paul F. Faulder

IPC: C07D405/12 ,  C07D471/04 ,  C07D417/12 ,  C07D405/14 ,  C07D407/12 ,  C07D319/18

CPC classification number: C07D405/12 ,  C07D319/18 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/056

Abstract: The present invention relates to compounds of formula I as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及本文定义的式I化合物。 本发明的化合物是热休克因子1（HSF1）的抑制剂。 特别地，本发明涉及这些化合物作为治疗和/或预防增殖性疾病如癌症的治疗剂的用途。 本发明还涉及制备这些化合物的方法以及包含它们的药物组合物。

公开(公告)号：US10647678B2

公开(公告)日：2020-05-12

申请号：US15563501

申请日：2016-04-01

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Matthew Cheeseman ,  Nicola Chessum ,  Elisa Pasqua ,  Lindsay Evans ,  Michael Tucker ,  Birgit Wilding ,  Ngai Yi Mok

IPC: C07D215/48 ,  C07D405/12

Abstract: The present invention relates to compounds of formula I wherein R, R4 and Q are each as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 pathway (HSF1 pathway). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

公开(公告)号：US20180093955A1

公开(公告)日：2018-04-05

申请号：US15563501

申请日：2016-04-01

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Matthew Cheeseman ,  Nicola Chessum ,  Elise Pasqua ,  Lindsay Evans ,  Michael Tucker ,  Birgit Wilding ,  Ngal Yi Mok

IPC: C07D215/48 ,  C07D405/12

CPC classification number: C07D215/48 ,  C07D405/12

Abstract: The present invention relates to compounds of formula I wherein R, R4 and Q are each as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 pathway (HSF1 pathway). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

公开(公告)号：US20160289216A1

公开(公告)日：2016-10-06

申请号：US15026911

申请日：2014-10-03

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Keith Jones ,  Carl Rye ,  Nicola Chessum ,  Matthew Cheeseman ,  Adele E. Pasqua ,  Kurt G. Pike ,  Paul F. Faulder

IPC: C07D405/12 ,  C07D471/04 ,  C07D417/12 ,  C07D405/14 ,  C07D407/12 ,  C07D319/18

CPC classification number: C07D405/12 ,  C07D319/18 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/056

Abstract: The present invention relates to compounds of formula I as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

Abstract translation: 本发明涉及本文定义的式I化合物。 本发明的化合物是热休克因子1（HSF1）的抑制剂。 特别地，本发明涉及这些化合物作为治疗和/或预防增殖性疾病如癌症的治疗剂的用途。 本发明还涉及制备这些化合物的方法以及包含它们的药物组合物。

公开(公告)号：US11787786B2

公开(公告)日：2023-10-17

申请号：US17406640

申请日：2021-08-19

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Carl Rye ,  Nicola Chessum ,  Matthew D. Cheeseman ,  Adele E. Pasqua ,  Kurt G. Pike ,  Paul F. Faulder

IPC: C07D405/14 ,  A61K31/496 ,  A61P35/00 ,  C07D405/12 ,  C07D319/18 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/056

CPC classification number: C07D405/12 ,  C07D319/18 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/056

Abstract: The present invention relates to compounds of formula I wherein A1, A2 R4 and Q are as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

公开(公告)号：US20200039965A1

公开(公告)日：2020-02-06

申请号：US16339056

申请日：2017-10-06

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Matthew D. Cheeseman ,  A. Elisa Pasqua ,  Michael J. Tucker

IPC: C07D405/12

Abstract: The present invention relates to N-(5-(2,3-dihydrobenzo[b][1,4]dioxine-6-carboxamido)-2-fluorophenyl)-2-((4-ethylpiperazin-1-yl)methyl)quinoline-6-carboxamide, or a pharmaceutically acceptable salt or solvate thereof, wherein at least one hydrogen atom has been substituted with a deuterium atom. Other aspects include pharmaceutical compositions comprising said compounds and medical uses and methods of treatment using said compounds.

公开(公告)号：US20190106413A1

公开(公告)日：2019-04-11

申请号：US16212455

申请日：2018-12-06

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Carl Rye ,  Nicola Chessum ,  Matthew Cheeseman ,  Adele E, Pasqua ,  Kurt G, Pike ,  Paul F. Faulder

IPC: C07D405/12 ,  C07D491/056 ,  C07D487/08 ,  C07D471/04 ,  C07D417/14 ,  C07D405/14 ,  C07D409/12 ,  C07D407/12 ,  C07D319/18 ,  C07D417/12

Abstract: The present invention relates to compounds of formula I as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.

公开(公告)号：US10189821B2

公开(公告)日：2019-01-29

申请号：US15332472

申请日：2016-10-24

Applicant: Cancer Research Technology Limited

Inventor： Keith Jones ,  Carl Rye ,  Nicola Chessum ,  Matthew Cheeseman ,  Adele E. Pasqua ,  Kurt G. Pike ,  Paul F. Faulder

IPC: C07D405/12 ,  C07D405/14 ,  C07D319/18 ,  C07D407/12 ,  C07D409/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D487/08 ,  C07D491/056

Abstract: The present invention relates to compounds of formula I as defined herein. The compounds of the present invention are inhibitors of heat shock factor 1 (HSF1). In particular, the present invention relates to the use of these compounds as therapeutic agents for the treatment and/or prevention of proliferative diseases, such as cancer. The present invention also relates to processes for the preparation of these compounds, and to pharmaceutical compositions comprising them.