938443-20-0Relevant articles and documents
Pyridopyrimidine KRAS G12C mutant protein inhibitor
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Paragraph 0081; 0088-0089, (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
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Paragraph 0096-0097, (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.
Discovery of 1-methyl-1 H-imidazole derivatives as potent Jak2 inhibitors
Su, Qibin,Ioannidis, Stephanos,Chuaqui, Claudio,Almeida, Lynsie,Alimzhanov, Marat,Bebernitz, Geraldine,Bell, Kirsten,Block, Michael,Howard, Tina,Huang, Shan,Huszar, Dennis,Read, Jon A.,Rivard Costa, Caroline,Shi, Jie,Su, Mei,Ye, Minwei,Zinda, Michael
, p. 144 - 158 (2014/02/14)
Structure based design, synthesis, and biological evaluation of a novel series of 1-methyl-1H-imidazole, as potent Jak2 inhibitors to modulate the Jak/STAT pathway, are described. Using the C-ring fragment from our first clinical candidate AZD1480 (24), optimization of the series led to the discovery of compound 19a, a potent, orally bioavailable Jak2 inhibitor. Compound 19a displayed a high level of cellular activity in hematopoietic cell lines harboring the V617F mutation and in murine BaF3 TEL-Jak2 cells. Compound 19a demonstrated significant tumor growth inhibition in a UKE-1 xenograft model within a well-tolerated dose range.