公开(公告)号：US10188642B2

公开(公告)日：2019-01-29

申请号：US15852639

申请日：2017-12-22

Applicant: Cancer Research Technology Limited

Inventor： Swen Hoelder ,  Julian Blagg ,  Kwai-Ming Jack Cheung ,  Butrus Atrash ,  Peter Sheldrake

IPC: A61K31/496 ,  A61K31/506 ,  A61K31/519 ,  A61K31/541 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  A61K31/4375 ,  A61K31/4725 ,  A61K31/4747 ,  A61K31/4985 ,  A61K31/5355 ,  C07D491/107

Abstract: The present invention relates to compounds of formula II wherein X, Y, R2, R3, R4 and Ar are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. 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：US09902721B2

公开(公告)日：2018-02-27

申请号：US15121432

申请日：2015-02-27

Applicant: Cancer Research Technology Limited

Inventor： Hannah Woodward ,  Paolo Innocenti ,  Sebastien Naud ,  Julian Blagg ,  Swen Hoelder

IPC: A01N43/90 ,  A61K31/519 ,  C07D471/00 ,  C07D487/00 ,  C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I: wherein R1, R2, R3 and R4 are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. 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：US11897877B2

公开(公告)日：2024-02-13

申请号：US17319231

申请日：2021-05-13

Applicant: Cancer Research Technology Limited

Inventor： Swen Hoelder ,  Julian Blagg ,  Savade Solanki ,  Hannah Woodward ,  Sebastien Gaston Andre Naud ,  Vassilios Bavetsias ,  Peter Sheldrake ,  Paolo Innocenti ,  Kwai-Ming J. Cheung ,  Butrus Atrash

IPC: C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  C07D405/04 ,  C07D519/00 ,  A61K31/519

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D413/14 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I




wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. 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：US09447092B2

公开(公告)日：2016-09-20

申请号：US14409042

申请日：2013-06-21

Applicant: CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Julian Blagg ,  Vassilios Bavetsias ,  Andrew S. Moore ,  Spyridon Linardopoulos

IPC: C07D471/04 ,  A61K31/496 ,  C07D471/06

CPC classification number: C07D471/04 ,  C07D471/06

Abstract: The present invention relates to compounds of formula I: wherein R1 and R2 are as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The compounds of formula I are inhibitors of aurora kinase and/or FLT3. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of proliferative disorders, such as cancer, as well as other diseases or conditions in which aurora kinase and/or FLT3 activity is implicated.

公开(公告)号：US20160222009A1

公开(公告)日：2016-08-04

申请号：US15091887

申请日：2016-04-06

Applicant: Cancer Research Technology Limited

Inventor： Swen Hoelder ,  Julian Blagg ,  Savade Solanki ,  Hannah Woodward ,  Sebastien Naud ,  Vassilios Bavetsias ,  Peter Sheldrake ,  Paolo Innocenti ,  Kwai-Ming J. Cheung ,  Butrus Atrash

IPC: C07D471/04 ,  C07D519/00 ,  C07D401/04 ,  C07D405/04 ,  C07D401/14 ,  C07D413/14

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D413/14 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. 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：US20160220570A1

公开(公告)日：2016-08-04

申请号：US15091980

申请日：2016-04-06

Applicant: Cancer Research Technology Limited

Inventor： Swen Hoelder ,  Julian Blagg ,  Savade Solanki ,  Hannah Woodward ,  Sebastien Naud ,  Vassilios Bavetsias ,  Peter Sheldrake ,  Paolo Innocenti ,  Kwai-Ming J. Cheung ,  Butrus Atrash

IPC: A61K31/519

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D413/14 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. 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：US09334286B2

公开(公告)日：2016-05-10

申请号：US14426574

申请日：2013-09-09

Applicant: Cancer Research Technology Limited

Inventor： Swen Hoelder ,  Julian Blagg ,  Kwai-Ming J. Cheung ,  Butrus Atrash ,  Peter Sheldrake

IPC: C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D401/14 ,  C07D405/14 ,  A61K31/4375 ,  A61K31/472 ,  A61K31/496 ,  A61K31/4985 ,  C07D491/107 ,  C07D413/14 ,  C07D401/04 ,  C07D401/12

CPC classification number: A61K31/4725 ,  A61K31/4375 ,  A61K31/4747 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/541 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107

Abstract: The present invention relates to compounds of formula II wherein X, Y, R2, R3, R4 and Ar are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. 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: 本发明涉及式II化合物，其中X，Y，R 2，R 3，R 4和Ar全部如本文所定义。 已知本发明的化合物通过与Mps1激酶本身的相互作用直接或间接地抑制单轴1（Mps1，也称为TTK）激酶的心轴检查点功能。 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：US20220402912A1

公开(公告)日：2022-12-22

申请号：US17319231

申请日：2021-05-13

Applicant: Cancer Research Technology Limited

Inventor： Swen Hoelder ,  Julian Blagg ,  Savade Solanki ,  Hannah Woodward ,  Sebastien Gaston Andre Naud ,  Vassilios Bavetsias ,  Peter Sheldrake ,  Paolo Innocenti ,  Kwai-Ming J. Cheung ,  Butrus Atrash

IPC: C07D471/04 ,  A61K31/519 ,  C07D413/14 ,  C07D401/14 ,  C07D405/04 ,  C07D401/04 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I wherein R1, R4, Ar, W, X and Z are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. 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：US20180194761A1

公开(公告)日：2018-07-12

申请号：US15861287

申请日：2018-01-03

Applicant: Cancer Research Technology Limited

Inventor： Hannah Woodward ,  Paolo Innocenti ,  Sebastien Naud ,  Julian Blagg ,  Swen Hoelder

IPC: C07D471/04 ,  C07D519/00

CPC classification number: C07D471/04 ,  A61K31/519 ,  C07D519/00

Abstract: The present invention relates to compounds of formula I: wherein R1, R2, R3 and R4 are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. 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：US20180117032A1

公开(公告)日：2018-05-03

申请号：US15852639

申请日：2017-12-22

Applicant: Cancer Research Technology Limited

Inventor： Swen Hoelder ,  Julian Blagg ,  Kwai-Ming Jack Cheung ,  Butrus Atrash ,  Peter Sheldrake

IPC: A61K31/4725 ,  C07D491/107 ,  A61K31/4375 ,  C07D471/04 ,  C07D417/14 ,  C07D413/14 ,  C07D405/14 ,  C07D401/14 ,  C07D401/12 ,  C07D401/04 ,  A61K31/541 ,  A61K31/5355 ,  A61K31/519 ,  A61K31/506 ,  A61K31/4985 ,  A61K31/496 ,  A61K31/4747 ,  C07D487/04

CPC classification number: A61K31/4725 ,  A61K31/4375 ,  A61K31/4747 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5355 ,  A61K31/541 ,  C07D401/04 ,  C07D401/12 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107

Abstract: The present invention relates to compounds of formula II wherein X, Y, R2, R3, R4 and Ar are all as defined herein. The compounds of the present invention are known to inhibit the spindle checkpoint function of Monospindle 1 (Mps1—also known as TTK) kinases either directly or indirectly via interaction with the Mps1 kinase itself. 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.