Abstract: The invention includes methods and compounds for labelling conjugates with metals which comprise the steps of coupling the conjugate to a support surface; introducing a complex-forming metal to the support; and collecting the metal-conjugate complex released from the support. The metal catalyzes cleavage of the conjugate from the support upon complex formation resulting in a solutions substantially free of unlabeled conjugate.

Abstract: The present invention is to invent a novel method for testing the radiochemical purity of Tc-99m-TRODAT-1 through a high performance liquid chromatography on a widely available C-18 column.

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: New types of hydroxamic acid-based bifunctional chelators are provided. These chelators are designed to chelate metal ions that can be detected either by their paramagnetic or radioactive properties. Conjugation with peptides or protein can be achieved by the presence of a linker moiety in the molecular structure of these chelators.

Abstract: Disclosed herein is a method of preparing a 188Re-tricarbonyl complex for radiopharmaceutical use and of preparing a precursor thereof, and a contrast agent using the same. Particularly, this invention provides a method of preparing a 188Re-tricarbonyl precursor by reacting perrhenate with borane-ammonia (BH3.NH3), potassium boranocarbonate (K2[H3BCO2]) and phosphate in the presence of borohydride exchange resin as a reducing agent, and a method of preparing a 188Re-tricarbonyl complex by reacting the 188Re-tricarbonyl precursor with a ligand. According to the method of this invention, the borohydride exchange resin is used as a reducing agent and as an anion scavenger, thereby obtaining the 188Re-tricarbonyl precursor and complex having high radiolabeling yield and high purity. In addition, the 188Re-tricarbonyl complex can be used as a contrast agent having excellent plasma stability.

Abstract: Described are new cascade polymer complexes, compositions containing them and use of the complexes in diagnosis and therapy, particularly for magnetic resonance imaging and computer tomography imaging.

Abstract: Compounds of general formula (I): in which: R1 is hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl, arylalkyl, or two R1, taken together, form a straight or cyclic C2–C10 alkylene group or an ortho disubstituted arylene; R2 is hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl or aryl alkyl optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; R3, R4 and R5 are hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl, arylalkyl; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among 203Pb 67Ga 68Ga 72As 111In 113In 90Y 97Ru 62Cu 64Cu 52Fe 52mMn 140La 175Yb 153Sm 166Ho 149Pm 177Lu 142Pr 159Gd 212Bi 47Sc 149Pm 67Cu, 111Ag, 199Au, 161Tb and 51Cr as well as the salts thereof with physiologically compatible bases or acids

Abstract: The disclosure provides pendant fatty acid compounds for use in diagnostic imaging, (particularly the cardiovascular system), as well as kits comprised of the same. The disclosure also provides for a method administering a imaging agent with a high specificity for the myocardium.

Abstract: The invention provides detectably labeled cobalamin derivatives which are useful for medical treatment and diagnosis.

Abstract: Provided herein are compounds for detection, diagnosis and treatment of target tissues or target compositions, including hyperproliferative tissues such as tumors, using photodynamic methods. In particular, photosensitizer compounds that collect in hyperproliferative tissue are provided. In another embodiment, compounds that absorb light at a wavelength of from about 700 to about 850 nm are provided. In a further embodiment, compounds that are detectable by magnetic resonance imaging are provided.

Abstract: Substituted 1,4,7-triazacyclononane-N,N?,N?-triacetic acid compounds with a pendant donor amino group, metal complexes thereof, compositions thereof, and methods of use in diagnostic imaging and treatment of a cellular disorder.

Abstract: The present invention describes a method of concurrent imaging in a mammal comprising: a) administering to said mammal a vitronectin receptor targeted imaging agent and a perfusion imaging agent; and b) concurrently detecting the vitronectin receptor targeted imaging agent bound at the vitronectin receptor and the perfusion imaging agent; and c) forming an image from the detection of said vitronectin targeted imaging agent and said perfusion imaging agent.

Abstract: The invention provides a complex comprising a) a compound formula I: wherein R1, X and n have any of the values described in the specification, or a pharmaceutically acceptable salt thereof; and b) a radionuclide. The complexes are useful as diagnostic agents and as therapeutic agents. The invention also provides methods and intermediates useful for preparing the complexes of the invention, as well as therapeutic and diagnostic methods.

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. The preferred compounds have the structural formula: where R1, R2, R2a R3, R3a R4, R5, R5a R6, R7, R7a, and R8 cumulatively contain at least two functional groups that will complex or combine with an MR imaging enhancing element or ion. The compound is intended to include such complexes and combinations and includes the use of such compounds for MR imaging and photodynamic therapy treatment of tumors and other hyperproliferative tissue.

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: Substituted 1,4,7-triazacyclononane-N,N?,N?-triacetic acid compounds with a pendant donor amino group, metal complexes thereof, compositions thereof, and methods of use in diagnostic imaging and treatment of a cellular disorder.

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: Stable isotope labeling and neutron activation to measure biological functions are provided, as are the use and method of adding a chemical monitor to correct for neutron flux to sample vials prior to the addition of sample is presented, and the use of stable isotopes as a chemical bar code for vials and other items. Methods are provided also for measuring glomerular filtration rate and glomerular sieving function in a subject, and for measuring other physiological functions.

Abstract: The invention relates to a method of preparing a solution of a radioactive rhenium complex, by reacting at elevated temperature a radioactive perrhenate in a substantially aqueous solution with a ligand in the presence of a reductant and optionally an antioxidant under substantially anaerobic conditions, wherein said reaction is carried out at a pH from approx. 1.5 to approx. 5 and by heating the reaction components for at least 10 min. at a temperature of at least 100° C. The invention further relates to a kit for performing said method.

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: The present invention is directed, in general, to a contrast agent comprising a tetraazacyclododecane ligand and comprising a macrocyclic ring and a paramagnetic metal ion coordinated to the tetraazacyclododecane ligand. Pendent arms R, R?, R? and R?? attached to a ring nitrogen. The pendent arms have the general formula: ?C?HR1R2 and for three or more of the pendant arms a chirality of the carbon atoms C? are identical for each of three or more of the pendant arms. The R1 group is larger than hydrogen and R2 is selected from the group consisting of: an alcohol, amides, a carboxylate, phosphinates and a phosphonate. One or more substituents R6 is a group larger than a methyl group and is located on one or more ring carbons.

Abstract: Metallopeptides and metallopeptide combinatorial libraries specific for opioids receptors are provided, for use in biological, pharmaceutical and related applications. The metallopeptides and combinatorial libraries are made of peptides, peptidomimetics and peptide-like constructs, in which the peptide, peptidomimetic or construct is conformationally fixed in a biologically active configuration specific for one or more opioid receptors on complexation of a metal ion-binding portion thereof with a metal ion.

Abstract: Fluorescent chelates of lanthanide, terbium, europium and dysprosium with tetraazamacrocyclic compounds are discussed which can be used as fluorescent in vitro or in vivo diagnostic agents. These chelates are tissue specific imaging agents for soft tissue cancers.

Abstract: Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comprising a metal, preferably radionuclide of rhenium or technetium; a hypoxia-localizing moiety; and, a complexing ligand, wherein said ligand and said radionuclide combined have cell membrane permeabilities greater than that of sucrose, are disclosed.

Abstract: The present invention covers halogenated derivatives of boronated phorphyrins containing multiple carborane cages having the formula which selectively accumulate in neoplastic tissue within the irradiation volume and thus can be used in cancer therapies including, but not limited to, boron neutron-capture therapy and photodynamic therapy. The present invention also covers methods for using these halogenated derivatives of boronated porphyrins in tumor imaging and cancer treatment.

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: 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 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: This invention relates to macrocyclic chelants comprised of one or two heteroatom-containing bridges, compositions containing them and their use in medicine, particularly in diagnostic imaging and radiotherapy. This invention relates especially to the use of metal chelates of the macrocyclic chelants as metallopharmaceuticals in Magnetic Resonance Imaging (MRI) and radiopharmaceuticals. This invention also relates to macrocyclic chelants as bifunctional chelating agents (BFC's) for the labeling of biologically active targeting molecules such as proteins, peptides, peptidomimetics, and non-peptide receptor ligands, with metal ions and radioisotopes.

Abstract: The present invention is directed to particular bisphosphonate compounds, and in particular, to bisphosphonate conjugates that are useful in the treatment of soft tissues surrounding bone and bone-related diseases, such as bone cancer and osteoporosis.

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: 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: The invention provides detectably labeled cobalamin derivatives which are useful for medical treatment and diagnosis.

Abstract: The present invention describes a method of concurrent imaging in a mammal comprising: a) administering to said mammal a vitronectin receptor targeted imaging agent and a perfusion imaging agent; and b) concurrently detecting the vitronectin receptor targeted imaging agent bound at the vitronectin receptor and the perfusion imaging agent; and c) forming an image from the detection of said vitronectin targeted imaging agent and said perfusion imaging agent.

Abstract: One aspect of the present invention relates to a method of purifying radiolabelled compounds comprising a) loading onto a fluorous polymer a radiolabelled compound precursor comprising a fluoroalkyl tin moiety; b) reacting the radiolabelled compound precursor with a radiolabel delivering compound to give a radiolabelled compound, wherein the fluoroalkyl tin moiety is replaced by a radiolabel; and c) eluting the radiolabelled compound from the fluorous polymer.

Abstract: The present invention provides novel diagnostic compositions comprising a radiolabeled LTB4 binding agent and a radiolabeled perfusion imaging agent, diagnostic kits comprising such compositions, and methods of concurrent imaging in a mammal comprising administering a radiolabeled LTB4 binding agent and a radiolabeled perfusion imaging agent, and concurrently detecting the radiolabeled LTB4 binding agent bound at the LTB4 receptor and the radiolabeled perfusion imaging 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: A method wherein a radiolabelled compound is localized at a thrombus. Two-dimensional images, representing a physical property associated with the radiolabelled thrombus, are acquired and assembled into a three-dimensional matrix of data. The three-dimensional matrix of data is then scanned along an array of parallel lines to determine a maximum value along each line. The maximum value along each line is then assigned to a pixel in a two-dimensional array, where the relative position of the pixel in the two-dimensional array corresponds to the relative position of the line in the array of parallel lines.

Abstract: A compound of formula corresponding to either formula (Ia) or (Ib): 1

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 novel diagnostic compositions comprising a radiolabeled LTB4 binding agent and a radiolabeled perfusion imaging agent, diagnostic kits comprising such compositions, and methods of concurrent imaging in a mammal comprising administering a radiolabeled LTB4 binding agent and a radiolabeled perfusion imaging agent, and concurrently detecting the radiolabeled LTB4 binding agent bound at the LTB4 receptor and the radiolabeled perfusion imaging agent.

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: Emissive phosphorescent organometallic compounds that produce electroluminescence and organic light emitting devices employing such emissive phosphorescent organometallic compounds are provided. More specifically the present invention is directed to novel primarily non-emitting ligands which produce a blue shift in emitted light when associated with a cyclometallated ligand.

Abstract: The invention provides radiopharmaceuticals for diagnostic and therapeutic applications, conjugates of antioxidants with metal chelating ligands, intermediate compounds, methods of making such radiopharmaceuticals, ligands, and intermediate compounds, and kits for preparing the radiopharmaceutical complexes.

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: Novel methods, processes and metal complexes attached to a hypoxia-localizing moiety comprising a metal, preferably radionuclide of rhenium or technetium; a hypoxia-localizing moiety; and, a complexing ligand, wherein said ligand and said radionuclide combined have cell membrane permeabilities greater than that of sucrose, are disclosed.

Abstract: The invention provides, in a general sense, a new labeling strategy employing 99mTc chelated with ethylenedicysteine (EC). EC is conjugated with a variety of ligands and chelated to 99mTc for use as an imaging agent for tissue-specific diseases. The drug conjugates of the invention may also be used as a prognostic tool or as a tool to deliver therapeutics to specific sites within a mammalian body. Kits for use in tissue-specific disease imaging are also provided.

Abstract: This invention relates to macrocyclic chelants comprised of one or two heteroatom-containing bridges, compositions containing them and their use in medicine, particularly in diagnostic imaging and radiotherapy. This invention relates especially to the use of metal chelates of the macrocyclic chelants as metallopharmaceuticals in Magnetic Resonance Imaging (MRI) and radiopharmaceuticals. This invention also relates to macrocyclic chelants as bifunctional chelating agents (BFC's) for the labeling of biologically active targeting molecules such as proteins, peptides, peptidomimetics, and non-peptide receptor ligands, with metal ions and radioisotopes.

Abstract: A radiopharmaceutical for diagnostic imaging containing as an active ingredient a technetium-99m nitride heterocomplex comprising technetium-99m nitride and two different ligands coordinated therewith, i.e., a bisphosphinoamine compound as a &pgr; electron acceptor and a bidentate ligand as a &pgr; electron donor and represented by the following formula (I): [99mTc(N)(PNP)(XY)]+ (I)wherein 99mTc(N) is technetium-99m nitride, PNP is a bisphosphinoamine compound and XY is a bidentate ligand, is markedly accumulated in heart and adrenal glands and hence is useful for radiodiagnostic imaging of heart and adrenal glands.

Abstract: The present invention provides novel sigma-2 ligands (labeled and unlabeled) and the use of the compounds in medical therapy or diagnosis.