100644-65-3Relevant articles and documents
Impact of Minor Structural Modifications on Properties of a Series of mTOR Inhibitors
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)
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.
ADENOSINE A2A RECEPTOR ANTAGONISTS AND USES THEREOF
-
Paragraph 00280-00281, (2021/02/12)
Disclosed herein are compounds, compositions, and methods for modulating the A2A2A adenosine receptor with the compounds and compositions disclosed herein. Also described are methods of treating diseases or disorders that are mediated by the A
Development of18f-labeled radiotracers for pet imaging of the adenosine a2a receptor: Synthesis, radiolabeling and preliminary biological evaluation
Lai, Thu Hang,Schr?der, Susann,Toussaint, Magali,Duki?-Stefanovi?, Sladjana,Kranz, Mathias,Ludwig, Friedrich-Alexander,Fischer, Steffen,Steinbach, J?rg,Deuther-Conrad, Winnie,Brust, Peter,Moldovan, Rare?-Petru
, p. 1 - 26 (2021/03/01)
The adenosine A2A receptor (A2AR) represents a potential therapeutic target for neuro-degenerative diseases. Aiming at the development of a positron emission tomography (PET) radio-tracer to monitor changes of receptor density and/or occupancy during the