Radioactive transition metal nitride heterocomplex
AssigneeNihon Medi-Physics Co., Ltd.
InventorsAdriano Duatti, Cristina Bolzati, Licia Uccelli, Fiorenzo Refosco, Francesco Tisato
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Abstract
The present invention provides a single radioactive transition metal nitride heterocomplex which permits labeling of a physiologically active substance such as a peptide, hormone or the like without impairing the activity of the substance. The radioactive transition metal nitride heterocomplex of the present invention is represented by the following formula (I): (M≡N)XY (I) wherein a radioactive transition metal M is radioactive technetium or radioactive rhenium, N is a nitrogen atom, X is a diphosphine compound or a diarsine compound, and Y is a bindentate ligand having a combination of electron-donating atoms.
Claims33
A radioactive transition metal nitride heterocomplex comprising a radioactive transition metal nitride and two different ligands coordinated therewith which is represented by the following formula (I):
- (M≡N)XY (I)
- wherein a radioactive transition metal M is selected from the group consisting of 99mTc, 186Re, and 188Re, N is a nitrogen atom, X is a bisphosphine compound represented by the following formula (II):
- wherein,
- each of R1, R2, R3 and R4, which may be the same or different, is one member selected from the group consisting of a hydrogen atom, an alkyl group, a substituted alkyl group, an aryl group, and a substituted aryl group,
- R5 is a methylene group,
- Z is one member selected from the group consisting of a sulfur atom and NR6, wherein,
- N is a nitrogen atom and R6 is a hydrogen atom, an alkyl group, a substituted alkyl group, an aryl group, a substituted aryl group, an amino group, an amino acid chain, a biologically active group or a —(═O)R7 group,
- wherein R7 is a hydrogen atom, an alkyl group, a substituted alkyl group, an aryl group, a substituted aryl group, an amino group, an amino acid chain or a biologically active group,
- P is a phosphorous atom,
- and n is an integer in a range of 1≦n≦5
- and Y is a bidentate ligand having a combination of two electron-donating atoms which are selected from the group consisting of O, S, and N and may be either charged or not.
A radiopharmaceutical containing, as an active ingredient, a radioactive transition metal nitride heterocomplex comprising a radioactive transition metal nitride and two different ligands coordinated therewith which is represented by the following formula(I):
- (M≡N)XY (I)
- wherein a radioactive transition metal M is selected from the group consisting of 99mTc, 186Re, and 188Re, N is a nitrogen atom, X is a bisphosphine compound represented by the following formula (II):
- wherein,
- each of R1, R2, R3 and R4, which may be the same or different, is one member selected from the group consisting of a hydrogen atom, an alkyl group, a substituted alkyl group, an aryl group, and a substituted aryl group,
- R5 is a methylene group,
- Z is one member selected from the group consisting of a sulfur atom and NR6, wherein,
- N is a nitrogen atom and R6 is a hydrogen atom, an alkyl group, a substituted alkyl group, an aryl group, a substituted aryl group, an amino group, an amino acid chain, a biologically active group or a —(═O)R7 group,
- wherein R7 is a hydrogen atom, an alkyl group, a substituted alkyl group, an aryl group, a substituted aryl group, an amino group, an amino acid chain or a biologically active group,
- P is a phosphorous atom,
- and n is an integer in a range of 1≦n≦5
- and Y is a bidentate ligand having a combination of two electron-donating atoms which are selected from the group consisting of O, S, and N and may be either charged or not.
Dependencies are inferred from the claim text.