- Synthesis process of anti-tumor drug Sapanisertib
-
The invention discloses a synthesis process of anti-tumor drug Sapanisertib. The synthesis process comprises the following steps: step 1, carrying out carboxyl halogenation reaction on a compound I and a halogenating reagent in a proper solvent to obtain
- -
-
-
- Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors
-
Minor structural modifications - sometimes single atom changes - can have a dramatic impact on the properties of compounds. This is illustrated here on structures related to known mTOR inhibitor Sapanisertib. Subtle changes in the hinge binder lead to strikingly different overall profiles with changes in physical properties, metabolism, and kinase selectivity.
- Ouvry, Gilles,Clary, Laurence,Tomas, Lo?c,Aurelly, Michèle,Bonnary, Laetitia,Borde, Emilie,Bouix-Peter, Claire,Chantalat, Laurent,Defoin-Platel, Claire,Deret, Sophie,Forissier, Mathieu,Harris, Craig S.,Isabet, Tatiana,Lamy, Laurent,Luzy, Anne-Pascale,Pascau, Jonathan,Soulet, Catherine,Taddei, Alessandro,Taquet, Nathalie,Thoreau, Etienne,Varvier, Emeric,Vial, Emmanuel,Hennequin, Laurent F.
-
p. 1561 - 1567
(2019/10/14)
-
- KINASE INHIBITOR POLYMORPHS
-
Polymorphs, hydrates, and solvates of chemical compounds that modulate kinase activity, including mTOR activity, and chemical compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including mTOR activity, are described herein.
- -
-
-