Abstract: The invention provides imaging agents comprising a label in association with a plaque specific targeting molecule. Methods for using the imaging agents to diagnose or monitor plaque formation and growth and kits containing the cardiovascular agents or components suitable for production of the imaging agents are also provided.

Abstract: The method for diagnosing lactose intolerance in patients by the oral administration of defined amounts of lactose, followed by assaying metabolites of lactose, is performed in a way where the lactose administered contains 99% 13C-labeled lactose, preferably from 5 to 30 mg, and after the administration of the lactose, the content of 13C-labeled lactose is determined in a serum sample taken at a defined time after the administration. A diagnostic kit for performing the method consists of a capsule with from 5 to 30 mg of 99% 13C-labeled lactose, a patient instruction manual, a blood sampling device, sample containers for collecting the blood sample, and optionally a spatula and sample container for a stool specimen.

Abstract: The present invention discloses radioligands of 9-arylsulfone of the formula (X) or a pharmaceutically acceptable salt or enantiomer thereof, which are useful in diagnosing depression, obesity and other CNS disorders.

Abstract: Preparations whereby reduction or acceleration of the gastric emptying rate can be noninvasively evaluated: and a method of evaluating the gastric emptying rate by using these preparations. Thus, reduction or acceleration of the gastric emptying rate can be safely and conveniently examined. Namely, theses preparations are useful in objectively diagnosing the gastric motor function, as well as in evaluating and judging the drug effect or therapeutic effect of a drug concerning the gastric motor function on individual patients.

Abstract: An 18F isotope-labeled FDG radiopharmaceutical is stabilized against degradation in radiochemical purity due to radiolysis using selected amounts of ethyl alcohol that depend on the activity concentration of the 18F with due regard to limits set by various pharmacopoeia standards. Any of the well-know production methods for the FDG may be used and the ethyl alcohol added at several stages, preferably as part of the standard hydrolysis step. This particular radiopharmaceutical is used extensively in diagnostic imaging with a Positron Emission Tomography technique.

Abstract: One aspect of the present invention relates to novel compounds that can be used to prepare radiolabeled compounds in an effective manner. A second aspect of the present invention relates to a method of synthesizing radiolabeled compounds.

Abstract: Methods, systems, devices and computer program products monitor in vivo detected radiation in a target localized site within a subject, over a selected time period, to do one or more of: (a) quantify a radiation dose received at a local site; (b) assess bioreceptiveness to a particular treatment time or type; (c) evaluate the pharmacokinetics of a radiolabeled analyte corresponding to a non-radiolabeled analyte; (d) monitor or evaluate metabolic activity; or (e) evaluate a tumor prior to or after a therapeutic treatment.

Abstract: Tropane derivatives having a high binding affinity and selectivity for dopamine transporters bear, on the tropane backbone either a carboxylic ester or isoxazole moiety, as well as a substituted phenyl moiety. The compounds have utility both as pharmaceutical and as imaging agents, when one or more atoms are radioactive.

Abstract: In certain embodiments, methods of the present invention obtain NMR spectroscopy signal data that corresponds to the behavior of the polarized 129Xe at a selected site(s) in selected environments in vivo. The gas exchange signal data can be used to evaluate: (a) the thickness of a barrier, such as a membrane, lining, wall or width of a lumen; (b) the operational condition or function of a membrane, body system or portion thereof; (c) cerebral perfusion; and/or (c) the efficacy of a therapeutic treatment used to treat a diagnosed disorder, disease, or condition. Thus, the present invention provides methods for screening and/or diagnosing a disorder or disease, and/or methods for monitoring the efficacy of therapeutics administered to subject to treat a disorder or disease.

Abstract: A method for the detection of fibrin in a source, in particular the in vivo detection of a fibrin in a patient, the method comprising supplying to the source or patient an amount of a detectable reagent comprising a plurality of discrete particles, each of the particles comprising a plurality of layers of carbon and being capable of binding to fibrin; and detecting the presence of the particles in the source. The particles may also comprise a detectable marker encased in said plurality of layers of carbon, the presence of said marker being capable of detection in said source.

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: A method of detecting inflammatory processes comprises (a) administering per-orally or per-rectally a composition comprising a diagnostically effective amount of L-[guanido-15N2]-arginine, L-[guanido-15N]-arginine, their mixtures and pharmaceutically acceptable salts thereof, and a pharmaceutically acceptable carrier; (b) collecting a sample of exhaled air, saliva or urine; (c) determining 13NO in the air sample or its transformation products 15IN-nitrite and/or 15N-nitrate in the saliva sample or urine. Also disclosed is a corresponding diagnostic composition for use in diagnosing inflammatory processes and a method for its manufacture.

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: The present invention is directed to radiolabeled neuropeptide Y Y5 receptor antagonists which are useful for the labeling and diagnostic imaging of neuropeptide Y Y5 receptors in mammals.

Abstract: The present invention provides isotopically labeled oxazinocarbazole derivatives having a ring connecting position 8 (C-8) and position 9 (N-9), and more specifically, provides compounds of formula (I) wherein R1, R2, R3 and R4 are described herein. These compounds are useful in the diagnostic analysis of diseases wherein modulation of 5-HT activity is desired.

Abstract: This relates to partially acetalized polyvinyl alcohol embolization particles suitable for implanting in the human body, to compositions containing those particles, and to methods of making and using them.

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: A “reverse isotope dilution assay” herein, wherein a pathway that produces a given metabolite is assayed by diluting a labelled metabolite produced by a second constitutive pathway. In one aspect, the invention relates to a method for monitoring lactose maldigestion or lactose intolerance in humans. Specifically, the method requires administering a reverse tracer of labeled glucose and unlabeled lactose to an individual and assessing labeled carbon dioxide in breath or blood. If the lactose is digested, the labeled CO2 produced by the labeled glucose is diluted by the metabolism of the lactose.

Abstract: One embodiment of the invention is a composition that comprises a radioactive 32P or 33P phosphine oxide molecule. The said composition is designed to bind to the transient potential receptor-M8 (TRP-M8) receptor of cells. The radioactive 32P or 33P phosphine oxide ligand may be used for radioreceptor binding studies and for diagnostic studies of cancerous tissues. The TRP-M8 receptor is selectively expressed in malignant tissues such as prostate cancer cells. Affinity of the 32P or 33P phosphine oxide ligand for the TRP-M8 receptor confers selectively and specificity in delivering lethal radiation to the diseased cells.

Abstract: A method of using radiolabelled and/or radiopharmaceutical small molecule inhibitors of beta-amyloid peptide production for the diagnosis of neurological and other disorders involving APP processing and beta-amyloid production. Radiolabelled small molecule inhibitors identified by the methods of the present invention would be useful in the diagnosis of neurological disorders, such as Alzheimer's disease, which involve elevated levels of A? peptides.

Abstract: This invention is directed to the use of radiopharmaceuticals in diagnosing Alzheimer's disease. In particular the radiopharmaceuticals of the invention are able to pass through the blood-brain barrier and bind to the CCR1 receptor present in brain tissue of patients having Alzheimer's disease.

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

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 present invention provide a method for assessing the sensitivity to a pyrimidine drug such as 5-FU which is degraded in the pyrimidine metabolic pathway, specifically in vivo pyrimidine metabolizing activity, of an individual subject; and a preparation useful for the assessment. The present invention can be carried out by: administering a preparation comprising as an active ingredient a pyrimidine compound or its metabolite which acts as a substrate for a pyrimidine metabolizing enzyme, in which compound or metabolite at least one of C, O and N is labeled with an isotope; and assessing in vivo pyrimidine metabolizing activity based on the amount of excreted metabolite.

Abstract: The present invention is directed to labeled compounds, [2H1, 13C], [2H2, 13C] and [2H3, 13C]methyl aryl sulfones and [2H1, 13C], [2H2, 13C] and [2H3, 13C]methyl aryl sulfoxides, wherein the 13C methyl group attached to the sulfur of the sulfone or sulfoxide includes exactly one, two or three deuterium atoms and the aryl group is selected from the group consisting of 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, and phenyl groups with the structure: wherein R1, R2, R3, R4 and R5 are each independently, hydrogen, a C1-C4 lower alkyl, a halogen, an amino group from the group consisting of NH2, NHR and NRR′ where R and R′ are each a C1-C4 lower alkyl, a phenyl, or an alkoxy group. The present invention is also directed to processes of preparing methyl aryl sulfones and methyl aryl sulfoxides.

Abstract: The present invention relates to a new method for radiolabeling chemical compounds. The new method attains the goals of simplicity, high radiochemical yields, speed, versatility, and automation. An HPLC injection loop on an HPLC injection valve is loaded with a solution of precursor and the radiolabeling reagent is passed through the loop. The contents of the loop are then quantitatively injected onto the HPLC column for purification. Radiochemical yields are equal to or superior to conventional solution methods in all cases, even though no heat need be applied. Since no vials, transfer lines, cooling, heating, or sealing valves are required, no transfer losses occur, yields are high, and clean-up is minimal. This “loop method” is ideal for the preparation of radiolabeled compounds, in particular those prepared from [11C]-iodomethane.

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: Methods of measuring gastric emptying time comprising providing to a patient a meal comprising a breath test food additive substrate, wherein the substrate is a linear or cyclic acyl aminoacid peptidomimetic that includes a radioactive or non-radioactively labeled carbon atom; having the patient digest the meal so that the carbon labeled nutrients therein are absorbed in the small intestine and metabolized to labeled CO2; and, at periodic intervals, detecting the level of labeled CO2 in breath samples taken from the patient to determine the rate of gastric emptying are disclosed.

Abstract: This invention relates to a novel method of screening for inhibitors of beta-amyloid production, and thereby identifying such inhibitors as therapeutics for neurological and other disorders involving APP processing and beta-amyloid production. This invention also relates to identifying macromolecules involved in APP processing and beta-amyloid production. Furthermore, inhibitors identified by the screening method of the present invention are useful in the treatment of neurological disorders, such as Alzheimer's disease, which involve elevated levels of A&bgr; peptides.

Abstract: The present invention is directed to labeled compounds, [2-13C]dithane wherein the 13C atom is directly bonded to one or two deuterium atoms. The present invention is also directed to processes of preparing [2-13C]dithane wherein the 13C atom is directly bonded to one or two deuterium atoms. The present invention is also directed to labeled compounds, e.g., [2H1-2, 13C]methanol (arylthio)-, acetates wherein the 13C atom is directly bonded to exactly one or two deuterium atoms.

Abstract: The present invention is directed to labeled compounds, [2H1, 13C], [2H2, 13C] and [2H3, 13C]methyl aryl sulfides wherein the 13C methyl group attached to the sulfur of the sulfide includes exactly one, two or three deuterium atoms and the aryl group is selected from the group consisting of 1-naphthyl, substituted 1-naphthyl, 2-naphthyl, substituted 2-naphthyl, and phenyl groups with the structure wherein R1, R2, R3, R4, and R5 are each independently, hydrogen, a C1-C4 lower alkyl, a halogen, an amino group from the group consisting of NH2, NHR and NRR′ where R and R′ are each a C1-C4 lower alkyl, a phenyl, or an alkoxy group. The present invention is also directed to processes of preparing [2H1, 13C], [2H2,13C] and [2H3, 13C]methyl aryl sulfides wherein the 13C methyl group attached to the sulfur of the sulfide includes exactly one, two or three deuterium atoms.

Abstract: Compounds of general formula (I) wherein m is 0 or 1, and n is 1 or 2; 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.

Abstract: The present invention is directed to labeled compounds, for example, isotopically enriched mustard gas metabolites including: [1,1′,2,2′-13C4]ethane, 1,1′-sulfonylbis[2-(methylthio); [1,1′,2,2′-13C4]ethane, 1-[[2-(methylsulfinyl)ethyl]sulfonyl]-2-(methylthio); [1,1′,2,2′-13C4]ethane, 1,1′-sulfonylbis[2-(methylsulfinyl)]; and, 2,2′-sulfinylbis([1,2-13C2]ethanol of the general formula where Q1 is selected from the group consisting of sulfide (—S—), sulfone (—S(O)—), sulfoxide (—S(O2)—) and oxide (—O—), at least one C* is 13C, X is selected from the group consisting of hydrogen and deuterium, and Z is selected from the group consisting of hydroxide (—OH), and —Q2—R where Q2 is selected from the group consisting of sulfide (—S—), sulfone(—S(O)—), sulfoxide (—S(O2)—) an

Abstract: A compound having the structure: wherein R1 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R2 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; wherein R3 is H or OH; wherein R4 is H, OH, a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety; and wherein at least one of R1, R2, R3, or R4 is a photoactivatable moiety, a fluorescent moiety, or a radioactive moiety. Optically pure enantiomers and salts of the compound are also described. Also, the synthesis of the compound, and uses of the compound, such as in a method for detecting the localization of, or identifying, receptors, enzymes or other targets, whether in a cell or in a subject.

Abstract: Detectably-labeled compounds of formula (I) wherein A,B,C,D,E,F,R,X,Y and Z have any of the meanings given in the specification, and their pharmaceutically acceptable salts, are useful in competitive assays to assay for the presence of 2 receptors. Also disclosed are pharmaceutical compositions containing such a compound of formula (I), methods for their use and intermediates useful for preparing such compounds of formula (I).

Abstract: A muscarinic acetylcholine nervous system labeled compound for positron emission tomography measurement of the present invention has a structure represented by undermentioned general formula (I): [in the formula, W represents one selected from the group consisting of groups represented by undermentioned formulae (II) and (III): (in the formulae, R represents one selected from the group consisting of an 11C-labeled ethyl group and an 11C-labeled propyl group), and in the case that W is a group represented by above-mentioned formula (II), above-mentioned formula (I) is the (+)-isomer].

Abstract: The present invention relates to 8-azabicyclo[3.2.1]oct-2-ene derivatives in their labelled form. Furthermore, the present invention relates to the use of said derivatives in their labelled or unlabelled form in diagnostic methods, in particular for in vivo receptor imaging (neuroimaging).

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: The invention provides methods for diagnosing and treating amyloid-related conditions and compounds useful for the same. The invention provides for detecting, imaging, monitoring, diagnosing, and treating conditions characterized by the binding or aggregation of amyloid fibrils. More particularly, the invention relates to using quinolinehydrazone compounds for diagnosing and treating amyloidotic conditions and also as an antioxidant.

Abstract: The invention provides derivatives of 5-arylsulfonyl indole and 5-arylsulfonyl indoline compounds which may be in the form of pharmaceutical acceptable salts or compositions that are useful in treating central nervous system diseases such as anxiety and depression. The invention also includes intermediates and processes to make the compounds, isotopically-labeled forms of the compounds and the use of the isotopically labeled forms of the compounds to perform nuclear magnetic resonance imaging and positron emission tomography.

Abstract: Radiolabeled epidermal growth factor receptor tyrosine kinase (EGFR-TK) irreversible inhibitors and their use as biomarkers for medicinal radioimaging such as Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) and as radiopharmaceuticals for radiotherapy are disclosed.

Abstract: A meat-free, algae-free, standardized, test meal kit used in the measurement of delayed gastric emptying is provided. The kit contains at least a standardized test meal dry mix and tracer. A method of using the kit is also provided.

Abstract: The present invention provide a method for measuring and assessing the capacity in an individual subject to metabolize a variety of fluorouracil drugs, such as 5-fluorouracil, which are degraded in the pyrimidine metabolic pathway, and a preparation useful for the measurement and assessment. The present invention can be carried out by: administering a preparation for determining pyrimidine metabolic capacity comprising as an active ingredient a pyrimidine compound or pyrimidine metabolic compound that acts as a substrate for a pyrimidine metabolizing enzyme, in which at least one of the carbon, oxygen, and nitrogen atoms is labeled with an isotope; and assessing in vivo pyrimidine metabolic capacity based on the behavior of an excreted metabolite.

Abstract: The present invention is directed to labeled compounds, [2-13C]dithiane wherein the 13C atom is directly bonded to one or two deuterium atoms. The present invention is also directed to processes of preparing [2-13C]dithiane wherein the 13C atom is directly bonded to one or two deuterium atoms. The present invention is also directed to labeled compounds, e.g., [2H1−2, 13C]methanol (arylthio)-, acetates wherein the 13C atom is directly bonded to exactly one or two deuterium atoms.

Abstract: Iodinated neuroprobes for mapping monoamine reuptake sites in the brain, and particularly iodinated neuroprobes that can also serve as radiotracers for use in single-photon emission computed tomography (SPECT) and positron emission tomography (PET) for imaging of such reuptake sites, are disclosed. Precursors of radiolabeled iodinated neuroprobes, both with and without a radiotracer atom, and kits for preparing the radiolabeled iodinated neuroprobes are also disclosed.

Abstract: The invention relates to the diagnosis in a human or lower animal subject of a gastrointestinal disorder of the upper gastrointestinal tract caused by bacteria using a breath test. In one aspect the invention provides a process for the preparation of a reactive pharmaceutical product for the detection of gastrointestinal disorder caused by bacteria in the superior gastrointestinal tract, characterized by the preparation of a dense powdered vehicle or granules of sugar, or granules of Nu-pareil seeds, of a specific diameter between 0.12 to 3.0 mm and soluble in gastric fluids; dispersing in or coating on the vehicle a micro dose of 14C-urea; and coating or encapsulating the resulting blend with an inert gelatin substance that dissolves rapidly, thereby obtaining a capsule, wherein the density of the vehicle is such that it allows deposition of the isotope contained in the capsule onto the gastrointestinal tract mucosa.

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 relates to a diagnostic agent for diabetes, comprising a compound labelled with 13C at least at one specific position selected from the group consisting of the following (a) to (g): (a) galactose, fructose or xylose labelled with 13C at least atone specific position, or a starch composed of glucose units labelled with 13C at least at one specific position; (b) an amino acid labelled with 13C at least at one specific position; (c) lactic acid or citric acid labelled with 13C at least at one specific position; (d) a fatty acid labelled with 13C at least at one specific position; (e) a glyceride labelled with 13C at least at one specific position; (f) glycerol labelled with 13C at least at one specific position; and (g) aminopyrin of which the dimethylamino group at position 4 is labelled with 13C, phenacetin of which the ethoxy group is labelled with 13C at position 1, or methacetin of which the methoxy group is labelled with 13C.

Abstract: A “reverse isotope dilution assay” herein, wherein a pathway that produces a given metabolite is assayed by diluting a labelled metabolite produced by a second constitutive pathway. In one aspect, the invention relates to a method for monitoring lactose maldigestion or lactose intolerance in humans. Specifically, the method requires administering a reverse tracer of labeled glucose and unlabeled lactose to an individual and assessing labeled carbon dioxide in breath or blood. If the lactose is digested, the labeled CO2 produced by the labeled glucose is diluted by the metabolism of the lactose.

Abstract: According to a first aspect of the invention, a process is disclosed for the preparation of radiolabelled haloaromatic compounds. According to a second aspect of the invention, intermediate precursor insoluble polymer compounds used in the preparation of the radiolabelled haloaromatic are disclosed, as well as processes for the preparation of the intermediate precursor insoluble polymer compounds.