Abstract: This invention relates to radiolabeled peptides and methods for producing such peptides. Specifically, the invention relates to peptides, methods and kits for making such peptides, and methods for using such peptides to image sites in a mammalian body labeled with technetium-99m (Tc-99m) via (Tc-99m) binding moieties. In particular, the peptide reagents of the invention are covalently linked to a polyvalent linker moiety, so that the polyvalent linker moiety is covalently linked to a multiplicity of the specific-binding peptides, and the Tc-99m binding moieties are covalently linked to a plurality of the specific-binding peptides, the polyvalent linker moiety, or to both the specific-binding peptides and the polyvalent linker moiety.

Abstract: The invention provides a composition of matter of the formula (I): V-L-R where V is an organic group having binding affinity for an angiotensin II receptor site, L is a linker moiety or a bond, and R is a moiety detectable in in vivo imaging of a human or animal body, with the provisos that where V is angiotensin or a peptidic angiotensin derivative or analog then V-L-R is other than a non-metal radionuclide substituted peptide (e.g. 125I substituted angiotensin II) and L-V is other than simply a peptide with a chelating agent amide bonded to a side chain thereof. This composition of matter may be used to image cardiovascular diseases and disorders.

Abstract: The present invention relates to a method of preparing technetium or rhenium complex for radiopharmaceuticals, through reaction of pertechnetate or perrhenate with a ligand in the presence of a reducing agent, wherein the reducing agent is a borohydride exchange resin (BER) . The borohydride exchange resin of the present invention has advantages of being stable in a wide range of Ph, including acidic or alkaline condition(Ph 2˜14) and thus being applicable to biological materials as well as being easily removable through filtration when being administrated. Also since the radiolabelled complex is produced under conditions milder than those required for the conventional reducing agents as well as has high radiochemical purity and high labeling efficiency, the conventional reducing agents can be replaced by the BER of the present invention.

Abstract: Novel compounds of the formula and novel complexes of these compounds with metals are useful in diagnostic and therapeutic methods.

Abstract: The present invention provides novel imaging agents for clinical diagnosis of injuries and diseases, in the form of a radionuclide in spatial proximity to a substantially pure stereoisomer of a fatty acid analog. The invention also provides methods for using the novel imaging agents, and kits containing one or more of the novel imaging agents of the invention.

Abstract: There is provided a method of labeling a biomolecule with a transition metal or radiometal in a site specific manner to produce a diagnostic or therapeutic pharmaceutical compound by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radio metal or a transition metal, and covalently linking the resulting metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. Also provided is a method of synthesizing the —PR2 containing biomolecules by synthesizing a P2N2-bifunctional chelating agent intermediate, complexing the intermediate with a radiometal or a transition metal, and covalently linking the resulting radio metal-complexed bifunctional chelating agent with a biomolecule in a site specific manner. There is provided a therapeutic or diagnostic agent comprising a —PR2 containing biomolecule.

Abstract: The present invention relates to a method for labelling a sulfide compound with technetium or rhenium, comprising the reaction of a disulfide compound with pertechnetate or perrhenate in the presence of borohydride exchange resin to obtain a complex of technetium or rhenium with the sulfide compound. The method can directly label disulfide compounds with technetium or rhenium, can skip the synthetic step of thiol-protected S-precursor, and is useful for high value-added radiopharmaceuticals.

Abstract: Novel 2-pyrrolylthione derived metal chelate compounds are disclosed as imaging and therapeutic agents. Compositions and methods for their preparation and use as diagnostic imaging and therapeutic agents are also disclosed.

Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

Abstract: A compound for use as a diagnostic or therapeutic pharmaceutical and method of using the same where the compound consists essentially of an alpha-melanotropin stimulating hormone analog which has integrally located a radionuclide. The radionuclide is administered to the body in an amount sufficient to allow uptake and retention by the tumor cells.

Abstract: Compounds of formula (I) where: X1 is OH or SH or NH2 or -L-Z; X2 and X3 are the same or different and each is H, C1-4 alkyl, benzyl a protecting group or -L-Z, X4 is H or C1-4 alkyl, L is a linker comprising a chain of 0-10 atoms, Z is a group comprising a detectable moiety which comprise at least one detectable moiety are useful in the diagnosis and prognosis and radiotherapy of metastatic bone disease.

Abstract: This invention relates to a method of imaging amyloid deposits and to labeled compounds, and methods of making labeled compounds useful in imaging amyloid deposits. This invention also relates to compounds, and methods of making compounds for inhibiting the aggregation of amyloid proteins to form amyloid deposits, and a method of delivering a therapeutic agent to amyloid deposits.

Abstract: Methods and compositions for medical imaging, evaluating intracellular processes and components, radiotherapy of intracellular targets, and drug delivery by the use of novel cell membrane-permeant peptide conjugate coordination and covalent complexes having target cell specificity are provided. Kits for conjugating radionuclides and other metals to peptide coordination complexes are also provided.

Abstract: The present invention relates to a complex comprising one or more radioisotopes selected from the group consisting of 99mTc, 188Re and 186Re chelated to a glucose derivative having an intramolecular nitrogen or sulfur atom, which is very useful as tumor diagnostic agents. It also relates to a kit for the preparation thereof comprising the glucose derivative and a reducing agent.

Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The present invention further provides novel compounds useful for imaging atherosclerosis, restenosis, cardiac ischemia and myocardial reperfusion injury. The present invention still further provides novel compounds useful for the treatment of rheumatoid arthritis. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety.

Abstract: This invention relates to new macrocyclic chelants and metal chelates thereof, methods of preparing the chelants and metal chelates, and pharmaceutical compositions comprising the macrocyclic chelants and metal chelates. This invention relates particularly to the use of the new metal chelates as contrast agents in X-ray or CT, MRI imaging, and radiopharmaceuticals for the diagnosis of cardiovascular disorders, infectious disease and cancer. This invention also relates to new bifunctional chelants (BFCs) for attaching diagnostic metals and therapeutic isotopes to target-specific biomolecules such as proteins, peptides, peptidomimetics, and non-peptide receptor ligands. In addition, the macrocyclic chelants are useful for heavy metal detoxification.

Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.

Abstract: The present invention provides a pharmaceutical compound, or pharmaceutically acceptable salt thereof, for use in medicine, wherein said compound is of formula I wherein R is a pharmaceutically active moiety; Ar is an aromatic moiety; X is a linker group; and Y is a moiety comprising two phosphonate groups. Further aspects of the invention relate to a method for palliative and curative treatment of bone disorders and cancer related disorders, such as breast cancer.

Abstract: Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.

Abstract: The present invention relates to a new method for the preparation of radiopharmaceuticals based on technetium and rhenium. The method involves the reaction of a salt of the formula [M(CO)3(Xm)3](1+3m), wherein M is selected from a radioisotope of rhenium, technetium and any other radioisotope that binds in a similar fashion, X is any suitable ligand and m is the formal charge for ligand X, with a nido-dicarbollide dianion of the formula [nido-(C2B9H11)]2− and functional derivatives thereof. The method has been shown to be applicable to the preparation of radiopharmaceuticals at the tracer level.

Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.

Abstract: A compound comprising a chemical combination of a photodynamic tetra-pyrrolic compound with a plurality of radionuclide element atoms such that the compound may be used to enhance MR imaging and also be used as a photodynamic compound for use in photodynamic therapy to treat hyperproliferative tissue.

Abstract: Compositions that are a chemical combination of porphyrins, chlorins, bacteriochlorins, and related tetra-pyrrolic compounds with radioactive elements such as Technetium99, Gadolinium, Indium111 and radioactive iodine. When the element can form cations, the compound is usually a chelate with the porphyrin or chlorin structure. When the element forms anions, the compound is usually a direct chemical combination of the radioactive element into the porphyrin or chlorin structure. The invention further includes the method of using the compounds of the invention for diagnostic imaging of hyperproliferative tissue such as tumors and new blood vessel growth as is associated with the wet form of age related macular degeneration and methods of making the compounds.

Abstract: Steroid receptor analogs having good binding affinity for steroid receptors and “binding arms” for chelation to metal species such as radionuclides are prepared with all carbon backbones. The analogs very closely approximate the geometries present in natural steroids which are important for effective binding to receptor sites. In addition, metal species binding arms are strategically incorporated into the analog structure in a manner that does not disrupt the analog's receptor binding efficacy. Furthermore, the metal species binding arms may be designed to chelate one or more radionuclides, including radionuclides effective in diagnostic or therapeutic applications. With incorporation of an appropriate steroid receptor binding group, these metal species-bound analogs may be used, for example, to bind androgen receptor sites in the diagnosis or treatment of prostate cancer, or estrogen receptor sites in the diagnosis or treatment of breast and ovarian cancers.

Abstract: This invention relates to novel highly functionalized phosphine ligands as ancillary ligands in radiopharmaceuticals. Also, this invention provides radiopharmaceuticals comprised of highly functionalized phosphine ligated 99mTc labeled HYNIC-conjugated biomolecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. The invention also provides methods of use of the radiopharmaceuticals as imaging agents for the diagnosis of cardiovascular disorders such as thromboembolic disease or atherosclerosis, infectious disease and cancer.

Abstract: The present invention provides for substituted metal chelating compounds in which at least two of the chelating atoms are nitrogen which are directly attached to aromatic rings and one or more of those nitrogen atoms has attached thereto a substituent other than hydrogen, and methods for making and using these compounds.

Abstract: The present invention provides novel radiopharmaceuticals comprising one to three pentapeptides, X1X2X3X4X5, independently attached to a metal chelator or bonding moiety, Ch, to which is attached a Tc-99m, Re-186, or Re-188, optionally further comprising a linking group, Ln, between-the peptides and the chelator or bonding moiety. The pentapeptide sequence binds to the tuftsin receptor and is attached at the N-terminus to Ln or Ch. These radiopharmaceuticals are useful for the diagnosis of infection and inflammation, reagents and kits useful for preparing the radiopharmaceuticals, methods of imaging sites of infection and/or inflammation in a patient, and methods of diagnosing diseases associated with infection or inflammation in patients in need of such diagnosis.

Abstract: The present invention describes novel compounds of the formula: (Q)d—Ln—Ch, useful for the diagnosis and treatment of cancer, methods of imaging tumors in a patient, and methods of treating cancer in a patient. The present invention also provides novel compounds useful for monitoring therapeutic angiogenesis treatment and destruction of new angiogenic vasculature. The pharmaceuticals are comprised of a targeting moiety that binds to a receptor that is upregulated during angiogenesis, an optional linking group, and a therapeutically effective radioisotope or diagnostically effective imageable moiety. The imageable moiety is a gamma ray or positron emitting radioisotope, a magnetic resonance imaging contrast agent, an X-ray contrast agent, or an ultrasound contrast agent.

Abstract: Macrocyclic chelant are disclosed, as well as chelates of the chelants with metal ions to form radiopharmaceutical and radioactive, MRI and X-ray or CT imaging compounds and compositions. Therapeutic and imaging methods of use are also disclosed.

Abstract: A 99mTc complex which contains the moiety Tc═NR, Tc—N═NY or Tc(—N═NY)2, and as a synthetic organic ligand which confers biological target-seeking properties on the technetium complex, where: R is an aryl group, a substituted or unsubstituted alkyl group or the group —NR1R2; Y is an aryl group or a substituted or unsubstituted alkyl group; R1 and R2 are H, aryl groups or substituted or unsubstituted aliphatic or cyclic alkyl groups, and are the same or different provided that both are not hydrogen; where at least one of the R or Y groups comprises an aryl group which chelates the 99mTc.

Abstract: This invention relates to calcitonin receptor binding reagents Comprising Compounds which are Covalently linked to a radiometal chelator. The invention is embodied as calcitonin receptor binding peptide derivatives and analogues of calcitonin which may be radiolabeled with a suitable isotope and used as radiodiagnostic or radiotherapeutic agents. Methods and kits for making, radiolabeling and using such reagents diagnostically and therapeutically in a mammalian body are also provided.

Abstract: A detectably labeled porphyrin compound for identifying a sentinel lymph node in patients, particularly those with cancer. A method of identifying a sentinel lymph node, comprising the steps of: injecting the detectably labeled porphyrin compound into a tumor, wherein the porphyrin compound is detectably labeled with a radiolabel which is a &ggr;-emitting radioactive metal; and detecting radioactive emission or a color so as to detect and thereby identify the sentinel lymph node. A method of identifying a sentinel lymph node, comprising the steps of injecting the detectably labeled porphyrin compound into tissue surrounding a tumor, wherein the porphyrin compound is detectably labeled with a non-radioactive metal; and taking a series of magnetic resonance images to identify the sentinel lymph node by viewing the images showing the injected detectably labeled porphyrin compound.

Abstract: Amphiphilic, polyhedron-shaped p-sulfonatocalix[4]arene building blocks, which have been shown previously to assemble into bilayers in an antiparallel fashion, assemble in a parallel alignment into spherical and helical tubular structures on the addition of pyridine N-oxide and lanthanide ions. The addition of greater amounts of pyridine N-oxide changed the curvature of the assembling surface and led to the formation of extended tubules. The inventive compositions and methods are useful for drug delivery and construction of nano-devices.

Abstract: This invention describes the use of metal complexes that have a plasma protein bond of at least 10% as imaging diagnostic agents for locating an infarction or a necrosis using lasting positive visualization.

Abstract: New chelating agents as well as their tricarbonyl complexes with technetium and rhenium and the use of these compounds in radiodiagnosis and radiotherapy are described. The new chelating agents are coupled to substances that accumulate in the diseased tissue.

Abstract: A metallocene compound having an indenyl ligand substituted by a heteroaromatic group, which is useful as an olefin polymerization catalyst. The metallocene compound has the following structure wherein M is a transition metal atom; each Ra is a monocyclic or polycyclic heteroaromatic group; each R1 is halogen, a hydrocarbon group of 1-20 carbons, a halogenated hydrocarbon group of 1-20 carbons, etc., or adjacent R1's may be joined together to form a ring of 6-8 carbons; p and q are each 1-7; n and l are each 0 or 1-6; and each X is halogen, a hydrocarbon group of 1-20 carbons, a halogenated hydrocarbon group of 1-20 carbons, etc.

Abstract: The invention concerns radiopharmaceutical products suitable for the selective labeling of lymphomas containing a metal complex with the formula: [M(R1CS2)(R1CS3)2] in which M is chosen from among 99mTc, 186Re and 188Re, and R1 represents an alkyl, cycloalkyl, aralkyl or aryl group, optionally substituted, obtained by reaction of a pertechnetate or a perrhenate with a reducing agent such as SnCl2ZP2O in the presence of a dithiocarboxylate having the formula: (R1CS2)−Z2+.

Abstract: The invention relates to novel aminocarboxylate ligands that are suitable for completing with a radionuclide, and are useful as therapeutic agents and as imaging agents for diagnostic purposes.

Abstract: Processes for the large scale production of tetrapyrrolic compounds useful as photosensitizers in photodynamic therapy, such as meso-formyl porphyrins, meso-acrylate porphyrins, purpurins and benzochlorins. In particular, tin ethyl etiopurpurin (SnET2) and the intermediates necessary for its production without chromatography are disclosed.

Abstract: The invention relates to macrocyclic perfluoroalkylamides, their production and their use in diagnosis.

Abstract: A diagnostic imaging agent useful for selection of a therapy for cancerous bone metastasis is provided, which comprises 99mTc(V)-dimercaptosuccinic acid as an effective ingredient. The agent is administered to a patient, and a scintigram is taken. This is especially useful for identifying osteoclastic type or mixed type bone metastasis or for identifying a disease in which the bone resorption due to osteoclast is enhanced, and thus allows a proper selection of therapies for such diseases.

Abstract: Radiopharmaceutical compounds are disclosed. A tropane compound is linked through the N atom at the 8-position to a chelating ligand capable of complexing technetium or rhenium to produce a neutral labeled complex that selectively binds to the dopamine transporter over the serotonin transporter with a ratio of 10 or more. These compounds can be prepared as separate diastereoisomers as well as a mixture of diastereoisomers. Also disclosed are radiopharmaceutical kits for preparing the labeled radiopharmaceutical compounds.

Abstract: Detectably labeled macrophage scavenger receptor antagonists useful for the diagnosis and monitoring of various cardiovascular diseases including but not limited to atherosclerosis, vulnerable plaque, coronary artery disease, renal disease, thrombosis, transient ischemia due to clotting, stroke, myocardial infarction, organ transplant, organ failure and hypercholesterolemia.

Abstract: Metal chelates of the amides of formula in which R has the formula Use in medical imaging.

Abstract: The invention relates to a process for therapeutic treatment of proliferative diseases, which is characterized in that first an administration catheter is placed on the site of the lesion, and a radioactive substance is administered topically via the catheter, then the catheter is again removed, and the radioactive substance remains on the site of the lesion.

Abstract: Radioimaging agents, which exhibit high uptake and retention in the myocardium are disclosed.

Abstract: Transition metal-cyclopentadienyl-tropane conjugate compounds are described. Methods for preparing transition metal-cyclopentadienyl-tropane conjugate compounds are also described. Transition metal-cyclopentadienyl-tropane conjugate compounds of the invention exhibit an affinity for monoamine transporters and are useful as diagnostic and/or therapeutic agents.

Abstract: The present invention relates to the stabilization of radiopharmaceutical preparations and to the stabilization of components of radiopharmaceutical kits. In particular, the present invention relates to stabilization of lyophilized components of radiopharmaceutical kits by the addition of a cyclic oligosaccharide, such as, a modified or unmodified cyclodextrin, to the kit.

Abstract: Novel 2-pyrrolylthione derived metal chelate compounds are disclosed as imaging and therapeutic agents. Compositions and methods for their preparation and use as diagnostic imaging and therapeutic agents are also disclosed.

Abstract: Compounds of formula (I) and (II) wherein the R, R1, R2, R3 and R4 groups have the meanings defined in the disclosure, are useful chelants for metal ions. The complexes of compounds (I) and (II) with paramagnetic ions are useful as contrast agents for M.R.I. imaging.