Abstract: The invention relates to ligands and complexes of metal ions with the ligands useful in various applications, including therapeutic and diagnostic applications.

Abstract: The invention relates to ligands and complexes of metal ions with the ligands useful in various applications, including therapeutic and diagnostic applications.

Abstract: A tissue-targeting complex comprising a tissue targeting moiety, an octadentate hydroxypyridinone-containing ligand comprising four HOPO moieties and the ion of an alpha-emitting thorium radionuclide, where at least one of the four HOPO moieties is substituted at the N-position with a hydroxyalkyi solubilising group and wherein the tissue targeting moiety has binding affinity for the CD33 receptor. A corresponding pharmaceutical formulation and method and use in treatment, as well as methods of manufacture are provided.

Abstract: Disclosed herein is a method for the preparation of radioisotope-labeled compounds using CNT. It comprises filling the carbon nanotube with a radioisotope; and labeling a physiologically active material with the radioisotope charged in the carbon nanotube. Taking advantage of CNT, the method can prepare a radioisotope-labeled compound invention at a high yield and in a simple manner. Also, the radioisotope, when remaining unreacted, can be recovered by the filtration of the CNT, thereby achieving the prevention of radioactive contamination and the reduction of radioactive waste. Further, the radioisotope-labeled compound is useful as a contrast medium for imaging the hepatobiliary system.

Abstract: Method of producing anhydrous thorium(IV) tetrahalide complexes, utilizing Th(NO3)4(H2O)x, where x is at least 4, as a reagent; method of producing thorium-containing complexes utilizing ThCl4(DME)2 as a precursor; method of producing purified ThCl4(ligand)x compounds, where x is from 2 to 9; and novel compounds having the structures:

Abstract: The invention provides compounds such as chelating agents useful in chelating metal ions, particularly radionuclides, to provide metal ion complexes. The invention also provides methods of using the compounds and complexes of the invention, such as in therapeutic and diagnostic applications.

Abstract: A test indicator for quantifying remaining liver function is provided. A novel liver receptor imaging agent with liver targeting property is utilized to develop a method for quantifying remaining liver function to serve as test indicator for judging the liver failure outcome in clinic, particularly for judging the necessity of liver transplantation for patients with liver failure or liver disease. The radioactivity uptake of the test indicator was negatively correlated with the extent of liver reserve. The cutoff value of liver reserve for liver transplantation is also disclosed.

Abstract: The present invention relates to trifunctional imaging agents that include an antibody for cell targeting, as well as a chelating moiety for sequestering radioisotopes and a fluorescing moiety for imaging. The invention also provides methods using the conjugates for medical diagnostic imaging.

Abstract: Polymeric chelating agents and metal chelates, particularly those of lanthanide metals and more specifically those of Gd(III), useful as contrast agents in magnetic resonance imaging (MRI) for therapeutic and diagnostic applications as well as clinical and biomedical research applications. The polymeric chelates are generated using ring-opening metathesis polymerization (ROMP). Polymers can have multiple sites for functionalization allowing for the synthesis of multimodal and targeted contrast agents. Hydroxypyridonate (HOPO)-based chelating moieties are integrated into a ROMP-derived polymer. More specifically, the HOPO-based chelating moiety is integrated into a benzonorbornadiene unit that constitutes the backbone of the polymer. The ROMP-derived polymer chelators can comprise multiple metal ions, particularly Gd(III) ions, in polymers of varying lengths to provide a series of agents with controlled relaxivites. Polymer chelates include those that are water-soluble.

Abstract: A process for isolating low molecular weight (“LMW”) peptides from tissue in situ comprising the steps: a) homogenizing the tissue; b) mixing the homogenized tissue with an organic solvent to form a fully-wetted slurry; c) standing or agitating the slurry to denature the proteins in situ within the tissue; d) removing the organic solvent from the tissue; e) mixing the organic solvent-treated tissue of step d) with a sufficient volume of water or an aqueous solution to extract the peptides; f) separating a liquid extract from the tissue residue of step e) to obtain an aqueous solution containing the low molecular weight peptide fraction removed from the tissue.

Abstract: The invention relates to a compound comprising a labeled nickel complex (FIG. 1) that is used to detect and purify nucleic acid sequences by forming an adduct between a specific nucleic acid base and the labeled nickel complex.

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 compounds useful as radiosensitizers in tumor therapy.

Abstract: A radiopharmaceutical capable of localizing at a site of thrombus containing activated platelets within a mammalian body is provided wherein the radiopharmaceutical comprises a linear peptidomimetic containing ligand capable of specifically binding to the GPIIb/IIIa integrin receptor of platelets in the thrombus and a radionuclide covalently bound to the peptidomimetic containing ligand. The ligand compositions of the invention are provided complexed with a selected metal radionuclide to form a diagnostic or therapeutic radiopharmaceutical to image a site of thrombus or provide radiotherapy to the site of thrombus, respectively.

Abstract: Novel organometallic compounds for binding amyloid are described. Methods using such compounds for determining by imaging the localization or quantification of amyloid fibrils in a mammal, for diagnosing the degree of progression of Alzheimer's disease in a mammal, for monitoring the response to a therapy in a mammal having Alzheimer's disease, for identifying an agent useful for treating Alzheimer's disease, for treating Alzheimer's disease, and for detecting the presence of the infectious form of the prion protein, are also described.

Abstract: This invention relates to new bifunctional chelating agents with intermittent chalcogen atoms, pharmaceuticals containing these compounds, their use in radiodiagnostics and radiotherapy, and methods for the production of these compounds.The compound according to the invention has the general formula (I)M--Lwhere M represents a radionuclide and L a ligand of the general formula (II).It was found, surprisingly, that these new, bifunctional chelating agents with intermittent chalcogen atoms and their coupling products with compounds that accumulate specifically are excellently suited for producing radiopharmaceuticals for diagnostic and therapeutic purposes.

Abstract: Novel Schiff base quinone complexes are provided. They are useful as anti-fading agents and filter dyes. The anti-fading agents are applicable to heat developable photosensitive materials, silver halide photosensitive materials, and optical recording materials.

Abstract: A method for preparing functionalized derivatives of organic or inorganic compounds and tetrapyrrolic compounds in particular, all of which compounds have at least one sulfonic acid group, by first preparing a sulfonyl halide intermediate of the compound then reacting the intermediate with a second compound having a reactive hydroxyl or amine group to yield the desired sulfonylamide or sulfonic esters thereof. The method may be used to produce a variety of photosensitive compounds having different functionality. For example, sulfonamide or sulfonic ester reaction products of the tetrapyrrolic compounds or other photosensitive organic molecules may exhibit an enhanced ability to localize at a particular target site for phototherapy.

Abstract: Novel compounds obtainable by reacting together an imido-reagent such as diphenylphosphonimido-triphenylphosphorane), or a phosphine oxide such as p-tolyldiphenylphosphine oxide, with a chelate of a transition or lanthanide or actinide metal, such as tris(dibenzoylmethide)europium III, have the property of fluorescing in UV radiation. The invention includes solid polymer bodies containing such compounds, or chelates of transition or lanthanide or actinide metals generally, the bodies having the property of emitting light or infra-red radiation when subjected to a flux of ultra-violet or ionising radiation by virtue of internally generated, e.g. by tritium ionising radiation. The body is preferably of polystyrene formed by polymerising the monomer in the presence of the compound or metal chelate.

Abstract: There are provided chelating agents particularly useful for the preparation of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula IX--CHR.sub.1 --NZ--(CHR.sub.1).sub.n --A--(CHR.sub.1).sub.m --NZ--CHR.sub.1 --X (I)wherein n and m are 2, 3 or 4; and A, X, R.sub.1 and Z are as defined in the specification.

Abstract: Purified imines of porphyrins, chlorins, bateriochlorins, chlorophylls, bacteriochlorophylls, purpurins, reduced purpurins, verdins, Diels Alder adducts, benzochlorins and metal complexes of the foregoing imines are disclosed. The formulas of the benzochlorinimines and of the benzochlorinimine metal complexes are set forth below: ##STR1## In specific examples, M in the metal complexes is a copper cation that is complexed with two of the nitrogens of the benzochlorinimine R' and R"" are methyl, and R1 through R8 are ethyl.

Abstract: Novel compounds obtainable by reacting together an imido-reagent such as diphenylphosphonimidotriphenylphosphorane) with a chelate of a transition or lanthanide or actinide metal, such as tris(dibenzoylmethide) europium III, has the property of fluorescing in UV radiation. The invention includes solid polymer bodies containing such compounds, or chelates of transition or lanthanide or actinide metals generally, the bodies having the property of emitting light by virtue of internally generated, e.g. by tritium ionising radiation. The body is preferably of polystyrene formed by polymerising the monomer in the presence of the compound or metal chelate.

Abstract: Purified imines of porphyrins, chlorins, bateriochlorins, chlorophylls, bacteriochlorophylls, purpurins, reduced purpurins, verdins, Diels Alder adducts, benzochlorins and metal complexes of the foregoing imines are disclosed for retarding growth of cancer tumors such as bladder tumors. The formulas of the benzochlorinimines and of the benzochlorinimine metal complexes are set forth below: ##STR1## In specific examples, M in the metal complexes is a copper cation that is complexed with two of the nitrogens of the benzochlorinimine R' and R"" are methyl, and R1 through R8 are ethyl.

Abstract: A process is disclosed for site-directed chemical modification of peptides and proteins that consists of two steps; (a) selective oxidation of a 2-hydroxyethylamine moiety, --CH(NH.sub.2)--CH(OH)--, in the peptide or protein to generate an aidehyde, and (b) reaction of the new aldehyde with a second reagent to form a product in which the native biological properties of the peptide are augmented by new and useful properties conferred by the second reagent. Additionally, the invention pertains to certain specified types of product formed by the above process.

Abstract: Compounds of the formula ##STR1## in which R is alkyl having up to 4 carbon atoms, n has an average value of at least 9, X is a radical of the formula --C(.dbd.O)--(NH--SO.sub.2).sub.m -- in which m is 0 or 1 and, if m is 1, the carhonyl group may be bonded to the oxygen atom or to the nitrogen atom, and each of the radicals A.sub.1, A.sub.2 and A.sub.3, independently of the others, is hydrogen or an acyl radical, and salts of salt-forming compounds of formula I, as well as metal complexes of compounds of formula I, in which A.sub.1, A.sub.2 and A.sub.3 are hydrogen can be used as metal chelators and as auxiliaries in diagnosis.

Abstract: A family of benzochlorins, a family of verdins, a family of porphyrin derivatives and metal complexes thereof are disclosed. The benzochlorins have the formula of FIG. 3 of the attached drawings; their metal complexes have the formula of FIG. 1 . The verdins have the formulas of FIGS. 4 and 6 of the attached drawings; their metal complexes have the formulas of FIGS. 2 and 5. The porphyrin derivatives have the formula of FIG. 9 of the attached drawings; their metal complexes have the formula of FIG. 10 . Solutions of the benzochlorins, verdins, porphyrin derivatives and metal complexes which are physiologically acceptable for intravenous administration are also disclosed, as are emulsions or suspensions of the solutions, and compositions which additionally include cyclodextrin, and wherein the molecules of the benzochlorin, verdin, porphyrin derivative or metal complex are encapsulated within the molecules of the cyclodextrin.

Abstract: There are provided chelating agents particularly useful for the preparations of diagnostic and therapeutic agents for magnetic resonance imaging, scintigraphy, ultrasound imaging, radiotherapy and heavy metal detoxification, said agents being compounds of formula X--CHR.sub.1 --NZ--(CHR.sub.1).sub.n --A--(CHR.sub.1).sub.m --NZ--CHR.sub.1 --X wherein (each of the groups Z is a group --CHR.sub.1 X or the groups Z together are a group --(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --, where A' is an oxygen or sulphur atom or a group --N--Y; A is a group --N--Y or A--(CHR.sub.1).sub.m -- represents a carbon-nitrogen bond or, when the groups Z together are a group --(CHR.sub.1).sub.q --A'--(CHR.sub.1).sub.r --, A may also represent an oxygen or sulphur atom; each Y, which may be the same or different, is a group --(CHR.sub.1).sub.p --N(CHR.sub.1 X).sub.2 or a group --CHR.sub.1 X; each X, which may be the same or different, is a carboxyl group or a derivative thereof or a group R.sub.1 ; each R.sub.

Abstract: A family of benzochlorins, a family of verdins, a family of porphyrin derivatives and metal complexes thereof are disclosed. the benzochlorins have the formula of FIG. 3 of the attached drawings; their metal complexes have the formula of FIG. 1. The verdins have the formula of FIG. 4 of the attached drawings; their metal complexes have the formula of FIG. 2. The porphyrin derivatives have the formula of FIG. 9 of the attached drawings; their metal complexes have the formula of FIG. 10. Solutions of the benzochlorins, verdins, porphyrin derivatives and metal complexes which are physiologically acceptable for intravenous administration are also disclosed, as are emulsions or suspensions of the solutions, and compositions which additionally include cyclodextrin, and wherein the molecules of the benzochlorin, verdin, prophyrin derivative or metal complex are encapsulated within the molecules of the cyclodextrin. The solvent for the solutions can be a product of the reaction of ethylene oxide with castor oil.

Abstract: This invention provides particle compositions possessing ferromagnetic, paramagnetic or diamagnetic properties. The particles are especially useful when used in the disease diagnostic and treatment regimens as described in U.S. Pat. Nos. 4,106,448, 4,136,683 and 4,303,636.

Abstract: A family of benzochlorins, a family of verdins, a family of porphyrin derivatives and metal complexes thereof are disclosed. The benzochlorins have the formula of FIG. 3 of the attached drawings; their metal complexes have the formula of FIG. 1. The verdins have the formula of FIG. 4 of the attached drawings; their metal complexes have the formula of FIG. 2. The porphyrin derivatives have the formula of FIG. 9 of the attached drawings; their metal complexes have the formula of FIG. 10. Solutions of the benzochlorins, verdins, porphyrin derivatives and metal complexes which are physiologically acceptable for intravenous administration are also disclosed, as are emulsions or suspensions of the solutions, and compositions which additionally include cyclodextrin, and wherein the molecules of the benzochlorin, verdin, porphyrin derivatives or metal complex are encapsulated within the molecules of the cyclodextrin. The solvent for the solutions can be a product of the reaction of ethylene oxide with castor oil.

Abstract: A 13 or 14 member macrocyclic compound having the following ring nucleus: ##STR1##This work was supported by grants from the National Institutes of Health (GM-34841) and the National Science Foundation (CHE-8706616).

Abstract: A detectable molecule of the formulaA.sup.3 --(--X--R.sup.1 --E--Det.sup.b).sub.mwhere A.sup.3 is A.sup.2 or a polymer, where A.sup.3 has at least one modifiable reactive group selected from the group consisting of amino, hydroxy, cis OH, halides, aryl, imidazoyl, carbonyl, carboxy, thiol or a residue comprising an activated carbon; --X-- is selected from the group consisting of ##STR1## a C.sub.1 -C.sub.10 branched or unbranched alkyl or aralkyl, which may be substituted by --OH; --Y-- is a direct bond to --E--, or --Y-- is --E--R.sup.2 -- where R is a C.sub.1 -C.sub.10 branched or unbranched alkyl; Z.sub.a is chlorine, bromine or iodine; E is O, NH or an acyclic divalent sulfur atom; Det.sup.b is a chemical moiety capable of being detected, preferably comprising biotin or a metal chelator of the formula: ##STR2## or the 4-hydroxy or acyloxy derivative thereof, where R.sup.3 is C.sub.1 -C.sub.4 alkyl or CH.sub.

Abstract: Metal-chelating liquids having the formula ##STR1## wherein Y is oxygen or ##STR2## R.sub.

Abstract: A fugitive binder composition for compression molding uranium dioxide nuclear fuel comprising the reaction product of a strongly alkali water solution of a diamine and oxalate ions with uranium oxide which is free of carbonates and carbamates, and having the formula:[.sup.+ NH.sub.3 (CH.sub.2).sub.2 NH.sub.3.sup.+ ][UO.sub.2 (C.sub.2 O.sub.4).sub.2 (H.sub.2 O).sub.2 ][.sup.+ NH.sub.3 (CH.sub.2).sub.2 NH.sub.3.sup.+ ].

Abstract: This invention provides particle compositions possessing ferromagnetic, paramagnetic or diamagnetic properties. The particles are especially useful when used in the disease diagnostic and treatment regimens as described in U.S. Pat. Nos. 4,106,448, 4,136,683 and 4,303,636.

Abstract: This invention relates to a process of recovering trivalent actinides, trivalent lanthanides or mixtures thereof from an aqueous acid solution by contacting the aqueous solution with an organic solution containing the diamides of the formula: ##STR1## where R is C.sub.2 -C.sub.10 alkyl. This process affords a good extraction efficiency level for the recovery of lanthanides and actinides, both of which are present in the trivalent state, or mixtures thereof, from installations for the reprocessing of irradiated nuclear fuels.

Abstract: A boron-containing heterocyclic compound prepared by reacting a primary amine or ammonia with an alkylene oxide or epoxide and then reacting concurrently or subsequently this reaction intermediate with a boric acid. This boron-containing heterocyclic compound may further be reacted with a metal, metalloid or other metal compound and even further contain sulfur, such as a sulfide group.The boron-containing heterocyclic compound provides extreme pressure anti-wear properties when provided in a lubricating composition. The lubricating composition may also comprise anti-oxidants, copper corrosion inhibitors, and lead corrosion inhibitors. The anti-wear properties of a lubricating composition can be enhanced using the borates of the present invention in conjunction with a copper compound.

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: 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.