Prochelator for the preparation of radiometal labeled molecules having improved biological properties
OwnerHelmut MAECKE, Klaus-Peter EISENWIENERinventors
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Abstract
Chelating compounds for labeling bioactive molecules with a radiometal, having general formula (I) in which: both Y groups may be positioned either trans as shown or cis; A is an effector molecule, such as a peptide, in particular octreotide, CCK, substance P, gastrine, a protein, in particular an antibody or enzyme, sugars or radiosensitizing agents, like doxorubicin; R is a hydrogen, a C1-C3 alkyl or a alcohol; X is a spacer, in particular (CH2)n—X′, in which n is 1-10 and X′ is COOH, NH2, SH, OH or O-halogen, in which halogen is in particular Br, I or Cl, or a molecule of the formula (a) or of the formula (b), Y is COO—, CH2CONH2, CH2CH2OH, optionally complexed with a radiometal.
Claims18
Polyazamacrocyclic compounds for radiometal labeling, comprising an Nn system, wherein n is 4, 5 or 6, with varying ring size, and wherein at least one of the N atoms is substituted with a free carboxylate group for coupling to an amino function in a bioactive effector molecule, while all N atoms carry a protected sidechain.
Chelating compounds for labeling bioactive molecules with a radiometal, having the general formula:
- in which:
- both Y groups may be positioned either trans as shown or cis;
- A is an effector molecule, such as a peptide, in particular octreotide, CCK, substance P, gastrine, a protein, in particular an antibody or enzyme, sugars or radiosensitizing agents, like doxorubicin;
- R is a hydrogen, a C1-C3 alkyl or a alcohol;
- X is a spacer, in particular(CH2)n—X′, in which n is 1-10 and X′ is COOH, NH2, SH, OH or O-halogen, in which halogen is in particular Br, I or Cl or a molecule of the formula
- or of the formula
- Y is COO−, CH2CONH2, CH2CH2OH, optionally complexed with a radiometal.
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Dependencies are inferred from the claim text.