Abstract: The present invention relates to new rhenium compounds of formula (I) with medical utility, corresponding pharmaceutical compositions as well as medical uses thereof.

Abstract: The present invention relates to new rhenium compounds of formula (I) with medical utility, corresponding pharmaceutical compositions as well as medical uses thereof.

Abstract: A method for synthesizing a complex having the formula: [L3MO3]? wherein L3 represents a tridentate ligand, M represents a metal selected from Tc an Re, and n is a charge from ?2 to +1, the method comprising: a) reaction of pertechnetate or perrhenate with a reducing agent and L3, or b) reaction of pertechnetate or perrhenate with a Lewis acid and L3, wherein the synthesis (a) or (b) is carried out in an aqueous medium.

Abstract: The present invention relates to novel histidine derivates that can be used for the labeling of biomolecules with radioactive metal tricarbonyls. The new derivatives have a histidine that is derivatized at the N? and at least protected at the N? and optionally at the N?; or derivatized at the N? and at least protected at the N? and optionally at the N?; or derivatized at the N? and N? and at least protected at the N? and optionally at the N?; or derivatized at the N?; or derivatized at the N?; or derivatized at the N? and N?; or at least protected at the N? and optionally at the N?.

Abstract: The present invention relates to new rhenium compounds of formula (I) with medical utility, corresponding pharmaceutical compositions as well as medical uses thereof.

Abstract: A method for synthesizing a complex having the formula: [L3MO3]? wherein L3 represents a tridentate ligand, M represents a metal selected from Tc an Re, and n is a charge from ?2 to +1, the method comprising: a) reaction of pertechnetate or perrhenate with a reducing agent and L3, or b) reaction of pertechnetate or perrhenate with a Lewis acid and L3, wherein the synthesis (a) or (b) is carried out in an aqueous medium.

Abstract: The present invention relates to a metal complex of the general formula M(L)n, wherein each L is independently selected and represents a ligand and at least one L is vitamin B12 (cyanocobalamin) or a derivative thereof bound through the nitrogen atom of its cyanide group to M, which is an element selected from the transition metals, thus, forming a M-NC-[Co] moiety with [Co] representing vitamin B12 without cyanide and wherein n is 1, 2, 3, 4, 5 or 6. The complex can be prepared by mixing a precursor molecule with vitamin B12. The metal complexes can be used for radiodiagnostics, chemotherapy and radionuclide therapy.

Abstract: The invention relates to cobalamin derivatives having no or low binding affinity to the transport protein transcobalamin II (TCII) and retaining activity as a vitamin B12 substitute, optionally carrying a therapeutic and/or diagnostic agent, such as a radioactive metal. These compounds have a much reduced accumulation rate in blood and benign organs, such as kidney and liver, compared to the accumulation rate in neoplastic tissues, and are more rapidly eliminated from blood. The invention further relates to a method of diagnosis and a method of treatment of a neoplastic disease or an infection by microorganisms in a mammal by exposing the mammal to a period of a vitamin B12 free diet, and subsequently applying a cobalamin derivative of the invention carrying a diagnostic and/or therapeutic agent. By selecting cobalamin derivatives acting as vitamin B12 substitutes, the risk of the formation of resistant off-spring in neoplastic tissue is much reduced.

Abstract: The present invention relates to a metal complex of the general formula M(L)n, wherein each L is independently selected and represents a ligand and at least one L is vitamin B12 (cyanocobalamin) or a derivative thereof bound through the nitrogen atom of its cyanide group to M, which is an element selected from the transition metals, thus, forming a M-NC—[Co] moiety with [Co] representing vitamin B12 without cyanide and wherein n is 1, 2, 3, 4, 5 or 6. The complex can be prepared by mixing a precursor molecule with vitamin B12. The metal complexes can be used for radiodiagnostics, chemotherapy and radionuclide therapy.

Abstract: The invention relates to cobalamin derivatives (a) having no binding affinity or low binding affinity to the transport protein transcobalamin II TCII) and (b) retaining activity as a vitamin B12 substitute, optionally carrying a therapeutic and/or diagnostic agent, such as a radioactive metal. These compounds have a much reduced accumulation rate in blood and benign organs, such as kidney and liver, compared to the accumulation rate in neoplastic tissues, and are more rapidly eliminated from blood. The invention further relates to a method of diagnosis and a method of treatment of a neoplastic disease or an infection by microorganisms in a mammal comprising (a) exposing the mammal to a period of a vitamin B12-free diet, and (b) subsequently applying a cobalamin derivative of the invention carrying a diagnostic and/or therapeutic agent. By selecting cobalamin derivatives acting as vitamin B12 substitutes, the risk of the formation of resistant offspring in neoplastic tissue is much reduced.

Abstract: The present invention relates to novel histidine derivatives that can be used for the labeling of biomolecules with radioactive metal tricarbonyls. The new derivatives have a histidine that is derivatized at the N? and at least protected at the N? and optionally at the N?; or derivatized at the N? and at least protected at the N? and optionally at the N?; or derivatized at the N? and N? and at least protected at the N? and optionally at the N?; or derivatized at the N?; or derivatized at the N?; or derivatized at the N? and N?; or at least protected at the N? and optionally at the N?.

Abstract: The invention relates to the use of metal tricarbonyl compounds of the general formula [M(CO),L,]?, wherein M is rhenium or technetium or an isotope thereof and L is a ligand, for the preparation of a medicament for the treatment of cancer that is both radiotherapeutic and chemotoxic when a radioactive metal is used and chemotoxic when cold rhenium or macroscopic amounts of long-lived Tc-99 is used. The medicament is in particular chemotoxic by causing intrastrand linkages in DNA. In a specific embodiment at least one of L is not OH2. The invention further relates to novel compounds of the general formula IM(CO)3XIX2X3]+ and their use, wherein M is rhenium or technetium or an isotope thereof and at least one X1. X2 and X3 is a monodentate ligand; or two of X, X2 and X3 are part of a bidentate ligand and the other one is optionally a monodentate ligand.

Abstract: Boranocarbonates are described for administration to a human or other mammal for delivery of carbon monoxide. The boranocarbonate is a compound or ion adapted to make CO available for physiological effect, and may be administered with a guanylate cyclase stimulant or stabilizer. The physiological effect may be stimulation of neurotransmission, vasodilation or smooth muscle relaxation.

Abstract: The present invention relates to kits including compounds that may be used as a carbon monoxide source and optionally as a reducing agent in the preparation of transition metal carbonyl complexes.

Abstract: The present invention relates to a process for generating a water soluble metal complexed agent, comprising contacting a solid phase bound organic conjugate represented by the formula I with [M(H2O)3(CO)3]n+, under suitable conditions to cause the formation of a coordinate bond between [M(H2O)3(CO)3]n+ and the tertiary amine nitrogen atom of the solid phase bound organic conjugate and thereby the release of the metal complexed agent thus formed from the support. The invention further relates to the conjugate of formula (I) and to a kit for performing the process.

Abstract: The present invention relates to compounds that have a novel use as a carbon monoxide source and optionally as a reducing agent in the preparation of transition metal carbonyl complexes. The compounds are in general compounds of formula (I) wherein X1, X2 and X3 are the same or different and either a Lewis base or hydride and Y is a sigma donating group. The invention furthermore relates to a method for the preparation of borane carbonate and to the use of H3BCO as a reducing agent.

Abstract: The present invention relates to kits including compounds that may be used as a carbon monoxide source and optionally as a reducing agent in the preparation of transition metal carbonyl complexes.

Abstract: The invention relates to novel aminocarboxylate ligands that are suitable for complexing with a radionuclide, and are useful as imaging agents for diagnostic purposes. In accordance with the present invention, a method of preparing a compound of formula (I): fac-[M(CO)3(OH2)3]+, wherein M is Mn, 99mTc, 186Re or 188Re, involves reacting a metal in permetallate form with carbon monoxide and a reducing agent, wherein a mixture of a basic borate buffer and a reducing agent soluble in water but not substantially decomposed by water is solved in a water containing solvent system containing a solution of the metal in permanganate, pertechnetate or perrhenate form in the presence of carbon monoxide. The compound of formula (I) can be reacted with a ligand Lx to form a compound of formula (II): fac-[M(CO)3(X)2L1]n, wherein M is as defined above Lx is a multidentate ligand, and n is a charge of the ligand Lx increased with one + charge.

Abstract: The invention relates to molecules for treatment and diagnosis of tumors and malignancies, comprising a tumor seeking biomolecule, which is coupled to an intercalating moiety, which is capable of complexing a metal, which metal is preferably a radioactive metal, to the use of these molecules and to therapeutic and diagnostic compositions containing them.

Abstract: The invention relates to a method of preparing facial metal tricarbonyl compounds and further coordinated facial metal tricarbonyl compounds in water or an aqueous medium. The invention further relates to the use of said facial metal tricarbonyl compounds in the labelling of biologically active substrates and other ligands, and to a kit for preparing a facial metal tricarbonyl compound or further coordinated facial metal tricarbonyl compounds.