KUPPLUNGSMITTEL, DEREN AKTIVE ZWISCHENVERBINDUNGEN UND KONJUGATE SOWIE DIE VERWENDUNG DIESER KONJUGATE FÜR DIAGNOSTISCHE ZWECKE

• Main Author: LACOUX, XAVIER
• Format: Patent
• Language: German
• Published: 15.04.2011
• Subjects: CHEMISTRY; HETEROCYCLIC COMPOUNDS; INVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIRCHEMICAL OR PHYSICAL PROPERTIES; MEASURING; METALLURGY; ORGANIC CHEMISTRY; PHYSICS; TESTING

Heterobifunctional functional coupling agents (I), comprising peptide derivatives containing at least one 8-amino-3,6-dioxa-octanoic acid unit and aminooxy and maleimide functional groups, are new. Heterobifunctional functional coupling agents of formula (I), comprising peptide derivatives containing at least one 8-amino-3,6-dioxa-octanoic acid unit and aminooxy and maleimide functional groups, are new. W = NH-(CH2)2O(CH2)2-OCH2CO; A = (W')p-CO-(CH2)u-Mal (a), (W')p-CO-CH-((CH2)rNH-(W')p-CO-(CH2)u-Mal)2 (b) or (W')p-CO-CH(-(CH2)rNH-(W')p-CO-CH(-(CH2)r-NH-(W')p-CO-(CH2)u-Mal)2)-(CH2)q-NH-(W')p-CH(-(CH2)r-NH-(W')p-CO-(CH2)u-Mal)2 (c); D = group (a), (b), (c) or CO-(CH2)u-Mal (d); Mal = maleimide; Y = group terminated by CONH2 and inert with respect to the remainder of the molecule; W' = COCH2O-(CH2)2O(CH2)2-NH; n = 0-3; m, o = 0-3; p = 1-4; q = 0-3; r = 2-5; s = 0 or 1; t = 1-7, and u = 2-10. Independent claims are also included for: (1) new activated intermediates (II) comprising (I) and a molecule (II') having at least one surface aldehyde and/or ketone function before conjugation; (2) new activated intermediates (III) comprising (I) and 1-8 (preferably 1-4) molecule(s) (III') having at least one surface thiol function before conjugation; and (3) new conjugates (IV) comprising (I) bonded to (II') and to 1-8 molecule(s) (III').