Abstract: In accordance with this invention, there is provided a polymer comprising units comprising the residue of a chelating agent linked to a poly(alkylene oxide) moiety, and a method for the preparation thereof. The polymer is particularly useful in therapeutic and diagnostic imaging compositions and as an antistatic agent.

Abstract: Radionuclide chelating compounds are provided for conjugation to targetting molecules such as proteins, peptides or antibodies. The resulting labelled targetting molecules may be used in diagnosis and therapy.

Abstract: The present invention is directed to novel radiopharmaceutical imaging agents incorporating Tc-99m as a radiolabel. In particular, the novel imaging agents disclosed herein have relatively high renal extraction efficiencies, and hence are useful for conducting renal function imaging procedures. The novel Tc-99m compounds of a present invention have the following general formula: ##STR1## wherein X is S or N; and wherein Y is H or wherein Y is ##STR2## and where R.sub.1 is --H, --CH.sub.3, or --CH.sub.2 CH.sub.3 ; R.sub.2 is --H, --CH.sub.2 CO.sub.2 H, --CH.sub.2 CONH.sub.2, --CH.sub.2 CH.sub.2 CO.sub.2 H, --CH.sub.2 CH.sub.2 CONH.sub.2, --CH.sub.3, --CH.sub.2 CH.sub.3, CH.sub.2 C.sub.6 H.sub.5, or --CH.sub.2 OH; and Z is --H, --CO.sub.2 H, --CONH.sub.2, --SO.sub.3 H, --SO.sub.2 NH.sub.2, or --CONHCH.sub.2 CO.sub.2 H; and the Tc is Tc-99m; and water-soluble salts thereof.

Abstract: Lanthanide chelates which contain three heterocyclic rings covalently coupled to each other (either one 2,6-pyridylene and two five-membered unsaturated heterocyclic ring moieties or two 2,6-pyridylene and one five-membered unsaturated heterocyclic ring moiety) and two chelating groups so seated that they together chelate the same lanthanide ion even in aqueous solutions. These lanthanide chelates can optionally contain a reactive group for coupling to biologically active molecules. The new chelates are suitable for classical lanthanide chelate applications and are also useful as probes in time-resolved fluorescence microscopy, cytometry, multilabelling techniques and in process controls in industry.

Abstract: The present invention provides radiation synovectomy compositions for treating inflamed synovium containing a radionuclide complex bound to a hydroxyapatite-like matrix as the radiolabelled synovectomy agent in a sufficient amount to provide satisfactory synovectomy of the inflamed synovium together with a pharmaceutically acceptable vehicle, the radionuclide being a beta emitter that will substantially ablate the inflamed synovium, but not significantly damage underlying articular cartilage, the radionuclide complex being substantially kinetically stable, and if said radionuclide or radionuclide complex leaks from said joint it will be excreted from the body, the agent having a particle size such that there is essentially little or no leakage of the radionuclide complex from the joint after administration.

Abstract: A chemically defined polymeric carrier comprising a series of .alpha.-amino acids in any combination containing side chains to which diagnostic/therapeutic and chelating agents can be covalently joined through cleavable linkers either directly or covalently joined through cleavable linkers after chemical modification of the side chains. Hydrazone, disulfide, and ester linkages in any combination can be present in the polymeric carrier between the side chains of the .alpha.-amino acids and the agents. The presence of a particular covalent linkage between the side chain and the agent in the carrier is determined by the functional group present in the side chain of the .alpha.-amino acid and the functional group present in the agent. The .alpha.-amino acids with side chains to which agents do not covalently join can function as spacers to minimize interaction between bulky molecules attached to the polymeric carrier. In addition, those .alpha.

Abstract: The invention relates to cyctopentadienylcarbonyl.sup.99m Tc complexes of general formula I ##STR1## in which --XR can have various meanings. These new complexes of .sup.99m technetium can be used in the field of medical diagnosis. The invention further relates to a process for the production of complexes according to the invention.

Abstract: The present invention relates to non-lethal methods of conditioning a recipient for bone marrow transplantation. In particular, it relates to the use of sublethal doses of total body irradiation, cell type-specific antibodies, especially antibodies directed to bone marrow stromal cell markers, cytotoxic drugs, or a combination thereof. The methods of the invention have a wide range of applications, including, but not limited to, the conditioning of an individual for hematopoietic reconstitution by bone marrow transplantation for the treatment of hematologic malignancies, hematologic disorders, autoimmunity, infectious diseases such as acquired immunodeficiency syndrome, and the engraftment of bone marrow cells to induce tolerance for solid organ, tissue and cellular transplantation.

Abstract: Processes for manufacturing diethylenetriaminepentaacetic acid ("DTPA") bis(amide) magnetic resonance imaging ("MRI") agents are disclosed. Specifically, processes for manufacturing [N,N"-Bis[N-(2-methoxyethyl)carbamoylmethyl]diethylenetriamine-N,N',N"-tri acetato]gadolinium(III) are disclosed.

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: Rhenium complexes of formula (I), radiolabelled complexes thereof or pharmaceutically acceptable salts thereof: ##STR1## wherein R is straight or branched chain C.sub.1-10 alkyl, C.sub.1-10 alkenyl, C.sub.1-10 alkynyl optionally substituted by cycloalkyl or aryl; C.sub.1-10 cycloalkyl optionally substituted by straight or branched chain alkyl, alkenyl, alkynyl or aryl; or aryl optionally substituted by straight or branched chain alkyl, alkenyl, alkynyl or cycloalkyl for use in liver cancer therapy and metastasis of cancer.

Abstract: Novel compounds show high affinity for specific cocaine receptors in the brain, particularly dopamine transporter sites, and have the formula ##STR1## Wherein Y=CONRR.sub.2, R.sub.1 =hydrogen, C.sub.1-5 alkyl,X=H, C.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.1-4 alkoxy, C.sub.1-6 alkynyl, halogen, amino, acylamido,R and R.sup.2 may be saturated or unsaturated substituents of 1-6 carbon atoms, aromatic, or combine to form pyrrolidinyl, morpholinyl or piperidinyl moieties, andZ=H, I, Br, Cl, F, CN, CF.sub.3 NO.sub.2, N.sub.3, OR.sub.1, CO.sub.2 NH.sub.2, CO.sub.2 R.sub.1, C.sub.1-6 alkyl, NR.sub.4 R.sub.5, NHCOF.sub.5, NHCO.sub.2 R.sub.6,wherein R.sub.4 -R.sub.6 are each C.sub.1-6 alkyl.

Abstract: Additives are proposed for compositions comprising radiolabelled organic compounds e.g. 32P-labelled nucleotides. Stabilisers are selected from tryptophan, para-aminobenzoate, indoleacetate and the azole group. Dyes are selected from Sulphorhodamine B, Xylene Cyanol, Azocarmine B and New Coccine. Preferred compositions contain both stabiliser and dye.

Abstract: Disclosed are certain cocaine analogs useful for imaging of cocaine receptors and dopamine receptors. Also disclosed are analogs useful for imaging diagnostics for Parkinson's disease.

Abstract: Methods of detecting and/or treating lesions in a patient are provided.

Abstract: Novel, substituted benzamides in radioiodinated form are useful in radiopharmaceutical compositions in nuclear medicine as imaging agents to detect, visualize, and analyze the distribution and function of the dopamine D2 receptor in the mammalian brain. These compounds have a specific combination of lipophilicity and dopamine D2 receptor affinity required to attain a required image contrast. The iodinated benzamides identified by the above discovery can be made by reacting a trialkyltin substituted benzamide with an acid in the presence of radioactive iodine which, in turn, is generated by in situ oxidation of an appropriate iodide nuclide salt.

Abstract: The present invention relates to a new group of compounds (e.g., N,N"-bis(2,6-dimethylcarbaniloylmethylene diethylene triamino triacetic acid, N,N"-bis(pyridoxylamine)diethylene triamino triacetic acid) which can be used as metal chelating agents and can be complexed with paramagnetic metal atoms form new complexes with improved and unexpected stability which make them extremely useful as contrast agents in magnetic resonance imaging and other types of diagnostic imaging. The chelating agents and corresponding paramagnetic metal complexes are derivatives of diethylene triamino pentaacetic acid and triethylene tetraamino hexaacetic acid.

Abstract: Proteins containing one or more dtsulfide bonds or monosulfides are labeled with medically useful metal ions for use in diagnosis and treatment of a variety of pathologtc conditions. Labeling is accomplished with a variety of metals, including radiometals, by using a reducing agent to reduce the disulfide bonds to thiolate groups; excess reducing agent, reaction by-products and any impurities are removed; and, a source of Sn (II) agent is added to the thiolate-containing protein. The resulting product may be stored frozen or lyophilized, with labeling accomplished by the addition of the medically useful metal ions.

Abstract: A method for performing boron neutron capture therapy for the treatment of tumors is disclosed. The method includes administering to a patient an iodinated sulfidohydroborane, a boron-10-containing compound. The site of the tumor is localized by visualizing the increased concentration of the iodine labelled compound at the tumor. The targeted tumor is then irradiated with a beam of neutrons having an energy distribution effective for neutron capture. Destruction of the tumor occurs due to high LET particle irradiation of the tissue secondary to the incident neutrons being captured by the boron-10 nuclei. Iodinated sulfidohydroboranes are disclosed which are especially suitable for the method of the invention. In a preferred embodiment, a compound having the formula Na.sub.4 B.sub.12 I.sub.11 SSB.sub.12 I.sub.11, or another pharmaceutically acceptable salt of the compound, may be administered to a cancer patient for boron neutron capture therapy.