Novel substituted azabenzoxazoles

Details Novel substituted azabenzoxazoles Novel substituted azabenzoxazoles

A - Human Necessities

61

K

A61K 31/437 (2006.01) A61K 31/5377 (2006.01) A61K 49/00 (2006.01) A61K 51/00 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2741668

The present invention relates to novel MAO-B binding compounds and methods for measuring effects of the compounds, by measuring changes of MAO-B levels in living patients. More specifically, the present invention relates to use of the compounds of this invention as therapeutic agents for inhibition of MAO-B activity as well as a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study MAO-B levels in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel MAO-B binding compounds as diagnostic, as well as a therapeutic, agents. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted azabenzoxazole derivatives, compositions, and therapeutic uses and processes for making such compounds.

La présente invention concerne de nouveaux composés se liant à la MAO-B et des procédés permettant de mesurer les effets des composés par la mesure des changements des taux de MAO-B chez des patients vivants. Plus précisément, la présente invention concerne lutilisation des composés de la présente invention en tant quagents thérapeutiques pour inhiber lactivité de la MAO-B, ainsi quun procédé dutilisation des composés de la présente invention comme traceurs pour limagerie par tomographie par émission de positons (PET) de manière à étudier in vivo les taux de MAO-B dans le cerveau afin de diagnostiquer la maladie dAlzheimer. La présente invention concerne donc lutilisation des nouveaux composés se liant à la MAO-B comme agents de diagnostic et agents thérapeutiques. Linvention concerne en outre un procédé de mesure de lefficacité clinique dagents thérapeutiques permettant de traiter la maladie dAlzheimer. Plus précisément, la présente invention concerne de nouveaux dérivés dazabenzoxazole substitués avec un aryle ou un hétéroaryle, des compositions, lutilisation de ces composés en thérapie et leurs procédés de préparation.

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