57279-73-9Relevant articles and documents
Rapid Discovery of Pyrido[3,4-d]pyrimidine Inhibitors of Monopolar Spindle Kinase 1 (MPS1) Using a Structure-Based Hybridization Approach
Innocenti, Paolo,Woodward, Hannah L.,Solanki, Savade,Naud, Sébastien,Westwood, Isaac M.,Cronin, Nora,Hayes, Angela,Roberts, Jennie,Henley, Alan T.,Baker, Ross,Faisal, Amir,Mak, Grace Wing-Yan,Box, Gary,Valenti, Melanie,De Haven Brandon, Alexis,O'Fee, Lisa,Saville, Harry,Schmitt, Jessica,Matijssen, Berry,Burke, Rosemary,Van Montfort, Rob L. M.,Raynaud, Florence I.,Eccles, Suzanne A.,Linardopoulos, Spiros,Blagg, Julian,Hoelder, Swen
supporting information, p. 3671 - 3688 (2016/05/19)
Monopolar spindle 1 (MPS1) plays a central role in the transition of cells from metaphase to anaphase and is one of the main components of the spindle assembly checkpoint. Chromosomally unstable cancer cells rely heavily on MPS1 to cope with the stress arising from abnormal numbers of chromosomes and centrosomes and are thus more sensitive to MPS1 inhibition than normal cells. We report the discovery and optimization of a series of new pyrido[3,4-d]pyrimidine based inhibitors via a structure-based hybridization approach from our previously reported inhibitor CCT251455 and a modestly potent screening hit. Compounds in this novel series display excellent potency and selectivity for MPS1, which translates into biomarker modulation in an in vivo human tumor xenograft model.
SULFONAMIDE DERIVATIVE AND MEDICINAL USE THEREOF
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Paragraph 1295-1296, (2015/02/25)
Provided are sulfonamide derivatives of a specific chemical structure in which a sulfonamide group having, as a substituent, a phenyl group or a heterocyclic group having a hetero atom(s) as a constituent element(s) is present at its terminal, and pharmaceutically acceptable salts thereof. These compounds are novel compounds having excellent α4 integrin-inhibitory action.
INHIBITOR COMPOUNDS
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Paragraph 00267-00269, (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
MACROCYCLIC FACTOR VIIA INHIBITORS USEFUL AS ANTICOAGULANTS
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Page/Page column 210, (2008/06/13)
The present invention relates generally to novel macrocycles of Formula (I): or stereoisomers, tautomers, pharmaceutically acceptable salts, solvates, thereof, wherein the variables A, B, L, M, W, Z, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein. These compounds are selective inhibitors of the serine protease coagulation factor VIIa which can be used as medicaments.
Aryl carbamate derivatives, preperation and use thereof
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Page/Page column 6, (2010/02/06)
The present invention relates to novel compounds, the preparation and use, particularly therapeutic, thereof. More specifically, it relates to compounds derived from aryl carbamates, the preparation and use thereof, particularly in the field of human and animal health. The compounds according to the invention are preferably 5-HT4 serotoninergic receptor ligands and can therefore be used in the therapeutic or prophylactic treatment of any disorder involving a 5-HT4 receptor. The invention also relates to pharmaceutical compositions comprising such compounds, the preparation and use thereof and treatment methods using said compounds.