Targeting multimeric imaging agents through multilocus binding

Details Targeting multimeric imaging agents through multilocus binding Targeting multimeric imaging agents through multilocus binding

A - Human Necessities

61

K

A61K 49/00 (2006.01) A61K 49/06 (2006.01) A61K 49/08 (2006.01) A61K 49/10 (2006.01) A61K 49/14 (2006.01)

Patent

CA 2384565

The present invention relates to contrast agents for diagnostic imaging. In particular, this invention relates to novel multimeric compounds which exhibit improved relaxivity properties upon binding to endogenous proteins or other physiologically relevant sites. The compounds consist of: a) two or more Image Enhancing Moieties (IEMs) (or signal-generating moiety) comprising multiple subunits; b) two or more Target Binding Moieties (TBMs), providing for in vivo localization and multimer rigidification; c) a scaffold framework for attachment of the above moieties; and d) optional linkers for attachment of the IEMs to scaffold. This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for contrast enhancement of diagnostic imaging.

La présente invention porte sur des agents de contraste utilisés dans l'imagerie diagnostique, et notamment sur de nouveaux composés multimères qui présentent de meilleures propriétés de relaxivité lors de la liaison aux protéines endogènes ou autres sites de nature physiologique. Les composés comprennent : a) au moins deux fractions d'amélioration d'image (ou fraction génératrice de signal) constituées de plusieurs sous-unités ; b) au moins deux fractions de liaison de cibles pour la localisation in vivo et la rigidification multimère ; c) une structure de squelette se liant aux fractions précitées ; et d) d'éventuels lieurs permettant de relier les fractions d'amélioration d'image au squelette. Cette invention porte également sur des compositions pharmaceutiques comprenant ces composés, et sur des procédés utilisant ces composés et compositions pour améliorer le contraste de l'imagerie diagnostique.

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