Conjugated biomolecules and 1,4,7,10 - tetraazaciclododecanos, a process for their preparation, their use for the preparation of Diagnostic means, nuclear magnetic resonance or radiodiagnosis and radiotherapy, Pharmaceutical agents containing them, and sets or kits

摘要

Conjugated biomolecules and 1,4,7,10 - tetraazaciclododecanos, formula (1), where z represents a hydrogen Atom or at least two z represent an equivalent of a Metal Ion; b represents a hydrogen Atom or a c1-4 alkyl radical; R represents a hydrogen Atom or a Radi Cal C1 alkyl - or aryl 10 linear, branched, or cyclic, saturated or unsaturated,Optionally, which is replaced by a carboxyl Group, or - PO3H2 - SO3H, and where the alkyl Chain of the alkyl radical C1 - 10 contains an aryl Group and / or 1 - 2 Atoms of Oxygen, with the condition that the radical B and R are not at the same time Oxygen Atoms; re Presents a Hydrocarbon Chain C1 - 30 linear or branched, saturated or unsaturated,Optionally containing Oxygen Atoms 1 - 5, 1 - 5 nitrogen Atoms and / or 1 - 5 radical id ', where r' is defined as r, but that can be selected independently, which is optionally substituted with 1 to 3 carboxyl groups, 1 - 3 - 1 - 3 - SO3H, 1 - 3 PO3H2 and / or Halogen Atoms. Where are optionally 1 to 3 carbon Atoms and carbonyl groups.Where a part of the chain or Chain can be arranged in a Ring shape, and is formed such that X 'is linked at least through 3 Atoms with the nitrogen Atom to which it is joined; X' represents the radical of a group X which reacted with a biomolecule, and Bio represents the radical of a biomolecule, their salts, on condition thatWhen B is a hydrogen Atom and a radical R is c1-4 alkyl, a is not the radical chr3 - C (o) - (CH2) - NH - NH - 6 - 1 D - Where R3 is a hydrogen Atom or a c1-4 alkyl radical; d is a group alquileno C1 - 4, linear chain or branched, saturated or unsaturated, which can optionally be interr Umpido or replaced by a carbonyl Group and D is bound to X.These Conjugates are suitable as contrast media in the diagnosis by MRI and radiodiagnostic and radiotherapeutic as substance. With the Special ligands of macrocycles and achieves a high relaxation allows a fine adjustment of the relaxation.A procedure for the preparation of Conjugates of formula (1), use of the latter for the preparation of Diagnostic methods for Nuclear magnetic resonance or Radiology or radiation therapy, Pharmaceutical agents containing them, and sets or Kits for prepa Rar Radiopharmaceuticals comprising such Conjugates.