Near infrared fluorescent contrast agent and method for...

A - Human Necessities – 61 – K

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A61K 49/00 (2006.01)

Patent

CA 2478272

A near infrared fluorescent contrast agent which is excellent in permeability in a living tissue and enables specific imaging of tumor and/or blood vessel, comprising a compound represented by formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R7, and R8 represent a C1-C10 alkyl group or the like; R3, R4, R5, R6, R9, R10, R11, and R12 represent a hydrogen atom, a C1-C6 alkyl group, an aryl group or the like; X1 and X2 represent a C1- C15 alkyl group or an aryl group and X1 and X2 in total have 0 to 4 carboxyl groups; m1, m2, and m3 represents 0 or 1; L1 to L7 independently represent a methine group; M represents a hydrogen atom, a metal, or a quaternary ammonium salt; and n represents an integer of 1 to 7 necessary for neutralizing charge.

L'invention concerne un agent de contraste fluorescent proche de l'infrarouge, qui présente une excellente perméabilité dans un tissu vivant et permet de mettre en oeuvre une imagerie spécifique de tumeur et/ou de vaisseau sanguin. Cet agent de contraste comprend un composé représenté par la formule ÝI¨ ou un sel pharmaceutiquement acceptable de celui-ci. Dans la formule, R¿1?, R¿2?, R¿7? et R¿8? représentent un groupe alkyle en C¿1?-C¿10? ou analogue ; R?3¿, R?4¿, R?5¿, R?6¿, R?9¿, R?10¿, R?11¿ et R?12¿ représentent un atome d'hydrogène, un groupe alkyle en C¿1?-C¿6?, un groupe aryle ou analogue ; X?1¿ et X?2¿ représentent un groupe alkyle en C¿1?-C¿15? ou un groupe aryle, X?1¿ et X?2¿ possédant au total de 0 à 4 groupes carboxyle ; m?1¿, m?2¿ et m?3¿ représentent 0 ou 1 ; L?1¿ à L?7¿ représentent indépendamment un groupe méthine ; M représente un atome d'hydrogène, un métal ou un sel d'ammonium quaternaire ; et n représente un nombre entier compris entre 1 et 7, nécessaire pour neutraliser la charge.?¿

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