Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.

Abstract: The invention provides a diagnostic test for gastrointestinal disorders by providing a safe, convenient, reliable method for measuring gastric emptying. In this test, a tracer amount of 13C-glutamine or 13C-glutamic acid is added to a liquid meal, or 13C-glutamic acid added to a solid meal. After digestion in the stomach, the meal is emptied into the small bowel, where the labeled 13C-tracer is immediately taken up and metabolized by the cells lining the small bowel. The released 13CO2 is detected in the breath. The measurement of rise in the level of 13CO2 as a function of time is correlated to the rate of gastric emptying.

Abstract: The present invention relates to a radiolabeled non-steroidal compound having the formula: 1

Abstract: Ligands for nAChRs are provided based on various derivatives of methyllycaconitine (MLA) such as radiolabeled MLA, and MLA containing a fluorimetric marker group and their use in imaging for detection of Alzheimer's and other CNS diseases, and combinatorial assays for detection of compounds having affinity for nAChRs, as well as injectable compositions containing the same and kits for performing the imaging studies.

Abstract: The present invention is directed to radiolabeled compounds of Formula I: or salts thereof, where R1 represents R8, R8O, R8SO2, R8SO or R8S in which R8 is tritiated or deuterated methyl; X is halo, cyano, C1-6 alkoxycarbonyl, C2-6 alkynyl, optionally substituted C6-14 aryl or an optionally substituted 5- to 7-membered heteroaromatic ring linked to thiazole via a carbon-carbon bond; R2 is hydrogen or amino; and R3-R7 are defined in the specification. The invention is also directed to methods of using such compounds for demonstrating specific insect GABA receptors, qualitatively screening for compounds acting on an insect GABA receptor or quantitatively assaying concentrations of a compound acting on an insect GABA receptor.

Abstract: The invention concerns a radio-labeled antithrombogenic polymer and its use as part of therapeutic means to prevent excessive cell proliferation or scarring, and means which comprise the radiolabeled antithrombogenic polymer, such as emplastrum or artificial implants with a biocompatible coating.

Abstract: Compounds of general formula I are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain. Intermediates to the compounds of the formula I are also claimed.

Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: wherein RF is a fluorinated radical, X is a linear or branched alkylene, R1 is H or CH3, R2 is a radical having at least one OH group, R3 is a radical derived from an amino acid or a peptide, 1≦n≦50 and 0≦m≦200 with 0.2≦n/n+m≦1. These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.

Abstract: A method of enhancing the efficiency and increasing the duration of action of drugs (e.g. dihydropyridines and anti-bacterials) and particularly of nifedipine and penicillins wherein one or more hydrogen atoms are deuterated and wherein the deuterated drug has unexpectedly improved properties when used in much lower concentrations than unmodified drug. A method for determining the identity and bioequivalency of a new drug is also disclosed wherein the molecular and isotope structure of a new drug is determined by isotope ratio mass spectrometry and compared with the molecular and isotope structure of a known human drug.

Abstract: The nucleoside analog 2′-fluoro-5-methyl-1-&bgr;-D-arabinofuranosyluracil (FMAU) has been found to have an especially desirable combination of properties for use as an imaging agent, including in particular limited in vivo catabolism. Methods for the preparation of the [11C]-and [18F]-labeled FMAU and for the use of the labeled material are also provided.

Abstract: The present invention provides a tablet containing isotope-labeled urea and an inorganic compound.

Abstract: It is an object of the present invention to provide in vivo analytical methods that allow for diagnosis and management of therapy for diseases involving discrete biochemical pathways. In the method of the invention, a labelled tracer probe, a specifically designed substrate of a “gateway” enzyme, an enzyme marking a regulatory point in a discrete biochemical pathway, is administered to a subject; a labelled product of the action of the enzyme is measured; and the appearance and concentration of the product are related to the disease condition of interest. Determination of the rate of substrate-product conversion of the gateway enzyme allows for the analysis to be made. The method involves administering a defined amount of a labelled “metaprobe” substrate of the gateway enzyme to a subject, at a site that provides access to a desired pool of the gateway enzyme in the subject, and measuring the amount of the chosen labelled product.

Abstract: A method for labeling &bgr;-amyloid plaques and neurofibrillary tangles in vivo and in vitro, comprises contacting a compound of formula (I): with mammalian tissue.

Abstract: Provided herein is a novel breath test for assessing bacterial overgrowth. The test involves administration of a labeled sorbitol or sorbitol derivative to a subject and measurement of the label in breath and/or blood.

Abstract: The present invention relates to a class of compounds having affinity for certain cancer cells, e.g. lung carcinomas, colon carcinomas, renal carcinomas, prostate carcinomas, breast carcinomas, malignant melanomas, gliomas, neuroblastomas and pheochromocytomas. The compounds of the present invention can also bind with high specificity to cell surface sigma receptors and can therefore be used for diagnostic imaging of any tissue having an abundance of cells with sigma receptors. The present invention provides such compounds as agents for diagnostic imaging and for detecting and treating tumors containing the cancer cells described above.

Abstract: The present invention provides a 13C-labeled oligosaccharide or polysaccharide or a salt thereof excluding U-13C-maltose, 13C-starch, 1-13C-maltotetraose and 1-13C-amylose; a derivative of the 13C-labeled oligosaccharide or polysaccharide or salt thereof; a 13C-labeled inclusion complex or a salt thereof, which comprises a cyclodextrin or a modified derivative thereof as a host molecule; a 13C- or 14C-labeled fluorescein ester compound or a salt thereof; and a diagnostic agents for pancreatic exocrine function comprising these compounds 13C- or 14C-labeled.

Abstract: The present invention concerns the compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is O or S; n is 2, 3, 4 or 5; R1 is hydrogen, C1-6alkyl, C1-6alkyloxy or halo; R2 is hydrogen, C1-6alkyl, phenyl, phenylC1-6alkyl or phenylcarbonyl; R3 and R4 each independently are selected from hydrogen, halo, nitro, C1-6alkyl, C1-6alkyloxy, haloC1-6alkyl, aminosulfonyl, mono- or di(C1-4alkyl)aminosulfonyl; or R3 and R4 may also be taken together to form a bivalent radical of formula —CH═CH—CH═CH—; it further relates to processes for their preparation, compositions comprising them as well as their use as a medicine; compounds of formula (I) containing a radioactive isotope; a process of marking dopamine D4 receptor sites; and a process for imaging an organ are disclosed.

Abstract: Therapeutic methods and compositions using deuterated enriched 2-[(2-aminoethoxy)methyl]-4-(2-chlorophenyl)-1,4-dihydro-6-methyl-3,5-pyridinedicarboxylic acid 3-ethyl 5-methyl ester and other deuterated dihydropyridine compounds are described. The deuterated compounds exhibit enhanced efficacy in blocking calcium channels over non-deuterated dihydropyridines.

Abstract: Bifunctional aromatic compounds which are capable of linking metal ions to biologically useful molecules. The bifunctional compounds are characterized as having a hydrazine or hydrazide group and a protein reactive group. The hydrazine or hydrazide group may be protected as a lower alkyl hydrazone. Conjugates of the bifunctional compounds with macromolecules are also described and labelled macromolecules comprised of the conjugates and metal ions are provided. Additionally, a method is provided for forming a labelled macromolecule by reacting a conjugate with a metal species. The compounds and method of this invention are particularly useful in the fields of biology and medicine for imaging and/or therapy.

Abstract: This invention relates to therapeutic reagents and peptides, including radiotherapeutic reagents and peptides, radiodiagnostic reagents and peptides, and methods for producing labeled radiodiagnostic agents. Specifically, the invention relates to cyclic peptide derivatives and analogs of somatostatin, and embodiments of such peptides radiolabeled with a radioisotope, as well as methods and kits for making, radiolabeling and using such peptides for radiodiagnostic and radiotherapeutic purposes. The invention specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with technetium-99m and uses thereof as scintigraphic imaging agents. The invention also specifically relates to cyclic peptide derivatives and analogues of somatostatin radiolabeled with cytotoxic radioisotopes such as rhenium-186 (186Re) and rhenium-188 (188Re) for use as radiotherapeutic agents.

Abstract: Carboranyl-containing nucleosides and oligonucleotides are provided for use in boron neutron capture therapy (BNCT) and for other therapeutic and diagnostic purposes.