Compounds and methods of identifying, synthesizing,...

C - Chemistry – Metallurgy – 12 – Q

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C12Q 1/02 (2006.01) C12Q 1/48 (2006.01) G01N 33/68 (2006.01)

Patent

CA 2631182

This invention relates to methods of identifying, synthesizing, optimizing and profiling compounds that are inhibitors or activators of proteins, both naturally occurring endogenous proteins as well as certain variant forms of endogenous proteins, and novel methods of identifying such variants. The method accelerates the identification and development of compounds as potential therapeutically effective drugs by simplifying the pharmaceutical discovery and creation process through improvements in hit identification, lead optimization, biological profiling, and rapid elimination of toxic compounds. Implementation results in overall cost, reductions in the drug discovery process resulting from the corresponding increases in efficiency.

La présente invention concerne des procédés d~identification, de synthèse, d~optimisation et de création de profils de composés qui sont des inhibiteurs ou des activateurs de protéines, qu'il s'agisse de protéines endogènes apparaissant naturellement ou de certaines formes variantes de protéines endogènes, et de procédés atypiques d~identification de telles variantes. Le procédé accélère l~identification et le développement de composés en tant que médicaments potentiellement effectifs au niveau thérapeutique, en simplifiant le processus de découverte et de création pharmaceutique par le biais d~améliorations dans l~identification de tête de série, optimisation de médicaments chefs de file, création de profils biologiques et élimination rapide de composés toxiques. L~implémentation entraîne des réductions générales de frais dans le processus de découverte de médicaments, découlant de l'augmentation d'efficacité correspondante.

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