1578245-39-2Relevant academic research and scientific papers
Introduction of a Methyl Group Curbs Metabolism of Pyrido[3,4- d]pyrimidine Monopolar Spindle 1 (MPS1) Inhibitors and Enables the Discovery of the Phase 1 Clinical Candidate N2-(2-Ethoxy-4-(4-methyl-4 H-1,2,4-triazol-3-yl)phenyl)-6-methyl- N
Woodward, Hannah L.,Innocenti, Paolo,Cheung, Kwai-Ming J.,Hayes, Angela,Roberts, Jennie,Henley, Alan T.,Faisal, Amir,Mak, Grace Wing-Yan,Box, Gary,Westwood, Isaac M.,Cronin, Nora,Carter, Michael,Valenti, Melanie,De Haven Brandon, Alexis,O'Fee, Lisa,Saville, Harry,Schmitt, Jessica,Burke, Rosemary,Broccatelli, Fabio,Van Montfort, Rob L. M.,Raynaud, Florence I.,Eccles, Suzanne A.,Linardopoulos, Spiros,Blagg, Julian,Hoelder, Swen
, p. 8226 - 8240 (2018/09/18)
Monopolar spindle 1 (MPS1) occupies a central role in mitosis and is one of the main components of the spindle assembly checkpoint. The MPS1 kinase is an attractive cancer target, and herein, we report the discovery of the clinical candidate BOS172722. Th
Woodward, Hannah L.,Innocenti, Paolo,Cheung, Kwai-Ming J.,Hayes, Angela,Roberts, Jennie,Henley, Alan T.,Faisal, Amir,Mak, Grace Wing-Yan,Box, Gary,Westwood, Isaac M.,Cronin, Nora,Carter, Michael,Valenti, Melanie,De Haven Brandon, Alexis,O'Fee, Lisa,Saville, Harry,Schmitt, Jessica,Burke, Rosemary,Broccatelli, Fabio,Van Montfort, Rob L. M.,Raynaud, Florence I.,Eccles, Suzanne A.,Linardopoulos, Spiros,Blagg, Julian,Hoelder, Swen
, p. 8226 - 8240 (2018/09/18)
Monopolar spindle 1 (MPS1) occupies a central role in mitosis and is one of the main components of the spindle assembly checkpoint. The MPS1 kinase is an attractive cancer target, and herein, we report the discovery of the clinical candidate BOS172722. Th
INHIBITOR COMPOUNDS
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Paragraph 00412, (2014/03/26)
The present invention relates to compounds of formula (I), wherein R, R, 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
