Abstract: The present invention relates to imaging agents suitable for in vivo optical imaging, which comprise conjugates of pentamethine cyanine dyes having reduced non-specific binding, e.g. to plasma proteins. This is achieved by control of the nature and location of the sulfonic acid substituents, in particular the sulfoalkyl groups. Also disclosed are pharmaceutical compositions and kits, as well as in vivo imaging methods.

Abstract: Disclosed are cyanine dyes that are useful for labelling and detecting biological and other materials. The dyes are of formula (I): in which at least one of groups R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 R11, R12, R13 and R14 is -L-M or -L-P, where L is a linking group, M is a target bonding group and P is a conjugated component, and at least one of groups R3, R4, R5, R6, R7, R8, R9 and R19 comprises fluorine. The use of cyanine dyes substituted by fluorine and having additional substitution with three or more sulphonic acid groups for labelling biological target molecules results in a labelled product in which there is reduced dye-dye aggregation and improved photostability, compared with cyanine dyes having no such substitutions.

Abstract: Disclosed are cyanine dyes that are useful for labelling and detecting biological and other materials. The dyes are of formula (I): in which at least one of groups R1, R2, R3, R4, R5, R6, R7, R8, R9, R10 R11, R12, R13 and R14 is -L-M or -L-P, where L is a linking group, M is a target bonding group and P is a conjugated component, and at least one of groups R3, R4, R5, R6, R7, R8, R9 and R10 comprises fluorine. The use of cyanine dyes substituted by fluorine and having additional substitution with three or more sulphonic acid groups for labelling biological target molecules results in a labelled product in which there is reduced dye-dye aggregation and improved photostability, compared with cyanine dyes having no such substitutions.

Abstract: The present invention relates to improved conjugates of biological molecules with an improved class of water-soluble, green to near infra-red (NIR) cyanine labelling dyes. The dyes are asymmetric fluoro-substituted polymethines, and exhibit a high degree of photostability and reduced dye-dye quenching, as well as a high fluorescence quantum yield. The conjugates are useful for in vivo optical imaging, as well as fluorescence detection methods. Also disclosed are pharmaceutical compositions containing the conjugates, kits for the preparation of such compositions, and methods of in vivo imaging using the conjugates.