150025-93-7Relevant articles and documents
HETEROCYCLIC COMPOUNDS AS MUTANT IDH INHIBITORS
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Paragraph 0238-0239, (2020/07/16)
The present disclosure relates generally to compounds useful in treatment of conditions associated with mutant isocitrate dehydrogenase (mt-IDH), particularly mutant IDH1 enzymes. Specifically, the present invention discloses compound of formula (IA), which exhibits inhibitory activity against mutant IDH1 enzymes. Method of treating conditions associated with excessive activity of mutant IDH1 enzymes with such compound is disclosed. Uses thereof, pharmaceutical composition, and kits are also disclosed.
3-PYRIMIDIN-4-YL-OXAZOLIDIN-2-ONES AS INHIBITORS OF MUTANT IDH
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Page/Page column 158; 159; 172, (2014/09/29)
The invention is directed to a formula (I), or a pharmamceutically acceptable salt thereof, wherein R1, R2a, R2b and R3-R7 are herein. The invention is also directed to compositions containing a compound of formula (I) and to the use of such compounds in the inhibition of mutant IDH proteins having a neomorphic activity. The invention is further directed to the use of a compound of formula (I) in the treatment of diseases or disorders associated with such mutant IDH proteins including, but not limited to, cell-proliferation disorders, such as cancer.
2-Mercaptoimidazoles, a new class of potent CCR2 antagonists
Van Lommen, Guy,Doyon, Julien,Coesemans, Erwin,Boeckx, Staf,Cools, Marina,Buntinx, Mieke,Hermans, Bart,VanWauwe, Jean
, p. 497 - 500 (2007/10/03)
We describe the synthesis and SAR of a new class of CCR2 antagonists based on a 2-mercaptoimidazole scaffold. The initial lead 1a was optimized to the 3,4-disubstituted analogues 1p-(S) and 1q-(S), which have IC50 values in the MCP-1 induced Ca