938443-19-7Relevant articles and documents
Pyridopyrimidine KRAS G12C mutant protein inhibitor
-
Paragraph 0081; 0086-0087, (2021/06/02)
The invention belongs to the technical field of medicines, and particularly relates to a pyridopyrimidine KRAS G12C mutant protein inhibitor shown in a general formula (I), pharmaceutically acceptable salts, stereoisomers and deuterated substances thereof. The invention also relates to a preparation method of the compounds, and a preparation method of the pharmaceutically acceptable salts, pharmaceutical preparations and pharmaceutical compositions containing the compounds. The invention also relates to the application of the compounds, pharmaceutically acceptable salts containing the compounds, pharmaceutical preparations and pharmaceutical compositions of the compounds in treatment of cancer proliferative diseases caused by KRAS G12C mutant protein.
PYRIDOPYRIMIDINE COMPOUNDS ACTING AS MTORC 1/2 DOUBLE-KINASE INHIBITORS
-
Paragraph 0094-0095, (2020/11/30)
Disclosed are a series of pyridopyrimidine compounds and a use of same in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors, and specifically disclosed is a use of the compounds as shown in formula (IV), tautomers thereof or pharmaceutically acceptable salts thereof in the preparation of drugs associated with mTORC 1/2 dual complex inhibitors.
Optimization of potent and selective dual mTORC1 and mTORC2 inhibitors: The discovery of AZD8055 and AZD2014
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 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).