cas 938443-21-1, 4-(2,7-dichloropyrido[2,3-d]pyrimidin-4-yl)morpholine

Articles about 938443-21-1Total 5 be found

Pyridine and miazines mTOR inhibitors
The invention belongs to the technical field of medicines, and particularly relates to a pyridopyrimidine mammalian target of rapamycin (mTOR) inhibitor which is shown as a general formula (I), pharmaceutically acceptable salts and stereoisomers thereof, and deuterated pyridopyrimidine mammalian mTOR inhibitors, wherein Z, Z, Z, R, R, R, X and W are defined in the specifications. The invention also relates to preparation methods for the compounds, medicinal inhibitors and medicinal compositions which contain the compounds, and the application of the compounds to preparation of medicines for treating and/or preventing post-transplant lymphoproliferative diseases which have response to inhibition of mTOR activity.
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(2016/10/17)

Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014
The optimization of a potent and highly selective series of dual mTORC1 and mTORC2 inhibitors is described. An initial focus on improving cellular potency whilst maintaining or improving other key parameters, such as aqueous solubility and margins over hERG IC50, led to the discovery of the clinical candidate AZD8055 (14). Further optimization, particularly aimed at reducing the rate of metabolism in human hepatocyte incubations, resulted in the discovery of the clinical candidate AZD2014 (21).
Pike, Kurt G.,Malagu, Karine,Hummersone, Marc G.,Menear, Keith A.,Duggan, Heather M.E.,Gomez, Sylvie,Martin, Niall M.B.,Ruston, Linette,Pass, Sarah L.,Pass, Martin
p. 1212 - 1216
(2013/03/14)

The discovery and optimisation of pyrido[2,3-d]pyrimidine-2,4-diamines as potent and selective inhibitors of mTOR kinase
We describe a novel series of potent inhibitors of the kinase activity of mTOR. The compounds display good selectivity relative to other PI3K-related kinase family members and, in cellular assays, inhibit both mTORC1 and mTORC2 complexes and exhibit good antiproliferative activity.
Malagu, Karine,Duggan, Heather,Menear, Keith,Hummersone, Marc,Gomez, Sylvie,Bailey, Christine,Edwards, Peter,Drzewiecki, Jan,Leroux, Frederic,Quesada, Mar Jimenez,Hermann, Gesine,Maine, Stephanie,Molyneaux, Carrie-Anne,Le Gall, Armelle,Pullen, James,Hickson, Ian,Smith, Lisa,Maguire, Sharon,Martin, Niall,Smith, Graeme,Pass, Martin
scheme or table
p. 5950 - 5953
(2010/07/05)

2-METHYLMORPHOLINE PYRIDO-, PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS MTOR INHIBITORS
There is provided a compound of Formula (I), or a pharmaceutically acceptable salt thereof. There are also provided processes for the manufacture of a compound of Formula (1), and the use of a compound of Formula (1) as a medicament and in the treatment of cancer
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Page/Page column 101-102

(2008/06/13)

PYRIDO-,PYRAZO- AND PYRIMIDO-PYRIMIDINE DERIVATIVES AS mTOR INHIBITORS
There is provided compounds of formula (I), which are suitable for the treatment of cancer.
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Page/Page column 57; 59

(2008/06/13)