公开(公告)号：EP3630291A1

公开(公告)日：2020-04-08

申请号：EP18730042.1

申请日：2018-05-25

申请人： Cancer Research Technology Limited ,  The Institute of Cancer Research: Royal Cancer Hospital

发明人： BELLENIE, Benjamin Richard ,  CARTER, Michael Keith ,  CHEUNG, Kwai Ming Jack ,  DAVIS, Owen Alexander ,  HOELDER, Swen ,  LLOYD, Matthew Garth ,  VARELA RODRÍGUEZ, Ana ,  WOODWARD, Hannah ,  INNOCENTI, Paolo

IPC分类号： A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/4184

公开(公告)号：EP4374858A3

公开(公告)日：2024-08-21

申请号：EP24150697.1

申请日：2018-05-25

申请人： Cancer Research Technology Limited ,  The Institute of Cancer Research: Royal Cancer Hospital

发明人： BELLENIE, Benjamin Richard ,  CARTER, Michael Keith ,  CHEUNG, Kwai Ming Jack ,  DAVIS, Owen Alexander ,  HOELDER, Swen ,  LLOYD, Matthew Garth ,  VARELA RODRÍGUEZ, Ana ,  WOODWARD, Hannah ,  INNOCENTI, Paolo

IPC分类号： A61P35/00 ,  C07D401/12 ,  C07D403/12 ,  C07D413/14 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  A61K31/4184

CPC分类号： C07D403/12 ,  C07D413/14 ,  C07D401/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  A61P35/00

摘要： The present invention relates to compounds of Formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity:

wherein X1, X2, R1, R2 and R3 are each as defined herein. 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 BCL6 activity is implicated.

公开(公告)号：EP4374858A2

公开(公告)日：2024-05-29

申请号：EP24150697.1

申请日：2018-05-25

申请人： Cancer Research Technology Limited ,  The Institute of Cancer Research: Royal Cancer Hospital

发明人： BELLENIE, Benjamin Richard ,  CARTER, Michael Keith ,  CHEUNG, Kwai Ming Jack ,  DAVIS, Owen Alexander ,  HOELDER, Swen ,  LLOYD, Matthew Garth ,  VARELA RODRÍGUEZ, Ana ,  WOODWARD, Hannah ,  INNOCENTI, Paolo

IPC分类号： A61K31/4184

CPC分类号： C07D403/12 ,  C07D413/14 ,  C07D401/12 ,  C07D403/14 ,  C07D409/14 ,  C07D417/14 ,  A61P35/00

摘要： The present invention relates to compounds of Formula I that function as inhibitors of BCL6 (B-cell lymphoma 6) activity:

wherein X1, X2, R1, R2 and R3 are each as defined herein. 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 BCL6 activity is implicated.

公开(公告)号：EP2892889B1

公开(公告)日：2017-10-18

申请号：EP13760106.8

申请日：2013-09-09

申请人： Cancer Research Technology Limited

发明人： HOELDER, Swen ,  BLAGG, Julian ,  SOLANKI, Savade ,  WOODWARD, Hannah ,  NAUD, Sebastien ,  BAVETSIAS, Vassilios ,  SHELDRAKE, Peter ,  INNOCENTI, Paolo ,  CHEUNG, Kwai-Ming J. ,  ATRASH, Butrus

IPC分类号： C07D401/14 ,  C07D413/14 ,  C07D401/04 ,  C07D405/04 ,  C07D471/04 ,  C07D519/00 ,  A61P35/00 ,  A61K31/4725 ,  A61K31/4375 ,  A61K31/519

CPC分类号： C07D471/04 ,  A61K31/519 ,  C07D401/04 ,  C07D401/14 ,  C07D405/04 ,  C07D413/14 ,  C07D519/00

摘要： The present invention relates to compounds of formula I wherein R 1 , R 4 , 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.