公开(公告)号：US09926319B2

公开(公告)日：2018-03-27

申请号：US15129338

申请日：2015-03-10

Applicant: MERCK PATENT GMBH ,  CANCER RESEARCH TECHNOLOGY LIMITED

Inventor： Kai Schiemann ,  Frank Stieber ,  Michel Calderini ,  Julian Blagg ,  Aurelie Mallinger ,  Dennis Waalboer ,  Christian Rink ,  Simon Ross Crumpler

IPC: A61P19/02 ,  A61P35/00 ,  C07D471/10 ,  A61K31/444 ,  A61P25/16 ,  C07D401/14 ,  C07D471/20 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/499 ,  A61K31/5377 ,  A61K45/06 ,  C07D417/14 ,  C07D498/10 ,  C07D519/00

CPC classification number: C07D471/20 ,  A61K31/444 ,  A61K31/4709 ,  A61K31/4725 ,  A61K31/499 ,  A61K31/5377 ,  A61K45/06 ,  C07D401/14 ,  C07D417/14 ,  C07D471/10 ,  C07D498/10 ,  C07D519/00

Abstract: The invention provides novel substituted pyridyl piperidine compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.

公开(公告)号：US09895364B2

公开(公告)日：2018-02-20

申请号：US15069012

申请日：2016-03-14

Applicant: Cancer Research Technology Limited

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

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

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.

公开(公告)号：US09409907B2

公开(公告)日：2016-08-09

申请号：US14426549

申请日：2013-09-09

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: A01N43/90 ,  A61K31/519 ,  C07D471/00 ,  C07D487/00 ,  C07D471/04 ,  C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  C07D405/04 ,  C07D519/00

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.

Abstract translation: 本发明涉及式Ⅰ化合物，其中R 1，R 4，Ar，W，X和Z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：US20150266868A1

公开(公告)日：2015-09-24

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

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.

Abstract translation: 本发明涉及式I化合物：其中R 1和R 2如本文所定义，或其药学上可接受的盐或溶剂合物。 式I化合物是极光激酶和/或FLT3的抑制剂。 本发明还涉及制备这些化合物的方法，包含它们的药物组合物及其在治疗增殖性疾病如癌症中的用途，以及其中极光激酶和/或FLT3的其它疾病或病症 涉及活动。

公开(公告)号：US20150218181A1

公开(公告)日：2015-08-06

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: C07D491/107 ,  C07D401/14 ,  C07D413/14 ,  C07D471/04 ,  C07D401/12 ,  C07D401/04 ,  C07D487/04 ,  C07D405/14 ,  C07D417/14

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。