New indotricarbocyanine dyes are conjugated to biomolecules, used in fluorescence diagnosis of e.g. tumors

摘要

Indotricarbocyanine dyes (I) are new. Indotricarbocyanine dyes of formula (I) and their salts and solvates are new. [Image] X : O, S or C (di-substituted by methyl, ethyl, propyl, isopropyl and/or butyl); Y' : CH 2-CH 2 or CH 2-CH 2-CH 2; Z' : 1-5C alkyl (substituted by O or S) or -(1,4-phenylene)-O-; R 1- R 4SO 3H or H; R 5-CO-NH-R 8-R 9, -NH-CS-NH-R 8-R 9, -NH-CO-R 8-R 9, COOH or NH 2; R 8unbranched 2-13C alkyl (having C optionally replaced by O or S); R 9-NH-C(=O)-CH 2-Br, 2,5-dioxo-pyrrolyl, chloroacetyl, bromoactyl, iodoacetyl, chloroacetamido, iodoacetamido, chloroalkyl, bromoalkyl, iodoalkyl, pyridyl disulfide or vinyl sulfonamide; and R 6, R 7CH or connected to a hexyl ring (optionally substituted in para-position by 1-4C alkyl) by 1-3C alkyl. Provided that: at least three of R 1-R 4 are SO 3H. Independent claims are included for the following: (1) prepararion of (I); (2) a conjugate (II) of (I) with a biomolecule(s); and (3) a diagnostic kit comprising (I) and/or (II) together with additional adjuvants for implementing an in vivo diagnosis of e.g. tumors.