82657-71-4Relevant articles and documents
AN IMPROVED PROCESS FOR THE PREPARATION REMOGLIFLOZIN ETABONATE OR PHARMACEUTICALLY ACCEPTABLE SALT, SOLVATE, HYDRATE THEREOF
-
Paragraph 14, (2019/10/29)
The present invention relates to an improved process for the preparation of Remogliflozin, Remogliflozin etabonate or pharmaceutically acceptable salt, solvate, hydrate thereof. The present invention relates to an improved process for preparation of Remog
COMPOUNDS, SALTS THEREOF AND METHODS FOR TREATMENT OF DISEASES
-
Paragraph 00203; 00204; 00303-00305, (2019/03/12)
The present disclosure relates to compounds according to Formulae (I), (II) and (VIII), useful for treating diseases.
Ligand Specific Efficiency (LSE) Index for PET Tracer Optimization
Auberson, Yves P.,Briard, Emmanuelle,Sykes, David,Reilly, John,Healy, Mark
, p. 1415 - 1427 (2016/07/16)
Ligand efficiency indices are widely used to guide chemical optimization in drug discovery, due to their predictive value in the early steps of optimization. At later stages, however, as more complex properties become critical for success, indices relying on calculated, rather than experimental, parameters become less informative. This problem is particularly acute when developing positron emission tomography (PET) imaging agents, for which nonspecific binding (NSB) to membranes and non-target proteins is a frequent cause of failure. NSB cannot be predicted using in silico parameters. To address this gap, we explored the use of the experimentally determined chromatographic hydrophobicity index on immobilized artificial membranes, CHI(IAM), to guide the optimization of NSB. The ligand specific efficiency (LSE) index was defined as the ratio between affinity (pIC50or pKd) and the logarithmic value of CHI(IAM). It allows for quantification of binding affinity to the target of interest, relative to NSB. Its use was illustrated by the optimization of PET tracer candidates for the prostacyclin receptor.