A fluorescent photoprobe for the imaging of endothelin...

A - Human Necessities – 61 – K

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A61K 49/00 (2006.01) C09B 23/08 (2006.01) C09B 57/00 (2006.01)

Patent

CA 2619879

The present invention relates to a endothelin receptor antagonist conjugate of the formula (I) wherein R2 is an alkoxy group and one of R1 and R3 represents an alkoxy group and the other represents a group of the formula: (OCH2CH2)n-NH- X, wherein n is an integer of 1 to 100 and X represents a fluorescent dye and tautomers thereof. Furthermore, the present invention relates to a diagnostic composition comprising the compounds of the invention. The present invention also relates to the use of the compounds of the invention for the preparation of a diagnostic composition for the the diagnosis of cancer, the evaluation of cancer biology and/or monitoring of anticancer therapy. In a further aspect, the present invention relates to kits comprising the compounds of the invention.

La présente invention concerne un conjugué d'antagoniste du récepteur de l'endothéline de formule (I), où R2 représente un groupe alkoxy et un élément parmi R1 et R3 représente un groupe alkoxy et les autres éléments représentent un groupe de la formule : (OCH2CH2)n-NH-X, dans laquelle n est un nombre entier compris entre 1 et 100 et X représente un colorant fluorescent et des tautomères associés. Par ailleurs, ladite invention a pour objet une composition diagnostique contenant les composés susmentionnés, ainsi que l'utilisation desdits composés dans la préparation d'une composition diagnostique destinée à diagnostiquer un cancer, évaluer une biologie du cancer et/ou surveiller une thérapie anticancer. Dans un autre aspect, l'invention a trait à des kits contenant lesdits composés.

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