Abstract: The present invention relates to novel amyloid binding compounds of formula (I) and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET/) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents.

Abstract: The present invention relates to novel amyloid binding compounds and methods for measuring effects of the compounds, by measuring changes of amyloid plaque level in living patients. More specifically, the present invention relates to a method of using the compounds of this invention as tracers in positron emission tomography (PET) imaging to study amyloid deposits in brain in vivo to allow diagnosis of Alzheimer's disease. Thus, the present invention relates to use of the novel amyloid binding compounds as a diagnostic. The invention further relates to a method of measuring clinical efficacy of Alzheimer's disease therapeutic agents. Specifically, the present invention relates to novel aryl or heteroaryl substituted pyrazole derivatives, compositions, and therapeutic uses and processes for making such compounds.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds.

Abstract: The present invention provides methods of detecting a cancer cell in an individual, methods of grading a cancer, and methods of treating a cancer. The methods involve use of functionalized magnetic nanoparticles that comprise a moiety that provides for selective association with, and/or metabolic uptake into, a cancer cell.

Abstract: A drug delivery balloon (10) has a drug thereon in the form of crystalline particles (12), the drug having a predetermined size distribution. Optionally marker particles (14, 16) are also provided. A texturized coating (18), a cap layer (20) and/or other methods may be used to increase particle loading capacity of the balloon.

Abstract: Substituted 1,4,7-triazacyclononane-N,N?,N?-triacetic acid and 1,4,7,10-tetraazacyclcododecane-N,N?,N?,N??-tetraacetic acid compounds with a pendant amino or hydroxyl group, metal complexes thereof, compositions thereof, and methods of making and use in diagnostic imaging and treatment of cellular disorders.

Abstract: Radiolabeled 2-amino-4-alkyl-6-(haloalkyl)pyridine compounds are disclosed. In some aspects, the compounds bind to inducible nitric oxide synthase (iNOS) with high specificity. In some configurations, a compound comprising a radioisotope can be used for diagnostic imaging of iNOS distribution in a mammalian subject such as a human, using a scanning method such as positron emission tomography (PET scanning). Methods of synthesis of the compounds are also disclosed.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds of the formula R—Y—X—Z—R where each R denotes a triiodinated phenyl residue further substituted by hydrophilic moieties, Y and Z are urea and urethane groups and X is a alkylene group which may be further substituted. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging, and to contrast media containing such compounds.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds.

Abstract: An aqueous negative contrast agent for CT imaging of the gastrointestinal tract and the preparation method thereof. The agent is used in biological and pharmaceutical field. Its components and the weight percent are: hydrogel matrix 0.01-1%, micro-/nano-particles of the materials with low densities 5-50%, stabilization agents 0.1-5%, the rest is deionized water. The preparation method is: stabilization agents are added into the hydrogel matrix made of natural or synthetic hydrophilic polymers, then micro-/nano-particles of the materials with low CT densities are added or prepared, and uniformly dispersed in the hydrogel matrix. The CT density of the resulted aqueous negative contrast agent for CT imaging of the gastrointestinal tract is ?30HU to ?500HU. It can decrease the CT density inside the intestine lumen to lower than ?30HU. The intestine wall can be depicted clearly and the CT signals intensities inside lumen are uniform.

Abstract: The invention relates to the use of at least one ascorbic acid derivative for the functionalisation of matrices, and to specific ascorbic acid derivatives and processes for the preparation thereof.

Abstract: Compositions of nanoparticles functionalized with at least one zwitterionic moiety, methods for making a plurality of nanoparticles, and methods of their use as diagnostic agents are provided. The nanoparticles have characteristics that result in minimal retention of the particles in the body compared to other nanoparticles. The nanoparticle comprises a core, having a core surface essentially free of silica, and a shell attached to the core surface. The shell comprises at least one silane-functionalized zwitterionic moiety.

Abstract: Use of ivabradine, or 3-{3-[{[(7S)-3,4-dimethoxybicyclo[4.2.0]octa-1,3,5-trien-7-yl]-methyl}(methyl)amino]propyl}-7,8-dimethoxy- 1,3,4,5-tetrahydro-2H-3-benzazepin-2-one, of its addition salts with a pharmaceutically acceptable acid and of their hydrates, as a diagnostic agent in the method of coronary angiography by multislice computed tomography.

Abstract: Example compositions of liposomes with hydrophilic polymers on their surface, and containing relatively high concentrations of contrast-enhancing agents for computed tomography are provided. Example pharmaceutical compositions of such liposomes, when administered to a subject, provide for increased contrast of extended duration, as measured by computed tomography, in the bloodstream and other tissues of the subject. Also provided are example methods for making the liposomes containing high concentrations of contrast-enhancing agents, and example methods for using the compositions.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing a saturated triaza cyclic central moiety containing carbonyl functions allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract: The present invention relates to a capsule used for measuring flow information using X-rays and a method of measuring flow information using the same. More particularly, the present invention relates to a capsule used for measuring flow information using X-rays including a biocompatible polymer, an organic contrast agent or deionized water, and a cross-linking agent, wherein the biocompatible polymer that is cross-linked with the cross-linking agent is filled with an organic contrast agent or is empty. Thereby, it is possible to remarkably increase the image-capturing time, to accurately and quantitatively measure the blood flow, and to gain accurate in vivo flow information.

Abstract: In certain aspects, the present invention relates to metal coordinating complexes for use as imaging contrast agents. For instance, in some embodiments, the present invention is directed to an imaging contrast agent including a metal chelator and a halogen-substituted phenol, thiophenol, resorcinol, thioresorcinol, or dithioresorcinol derivative.

Abstract: The present disclosure encompasses heterodimeric compositions for delivering radiolabeled and other ligands to a cell or tissue, and particularly to compositions and methods of use thereof for targeting and imaging cells and tissues expressing both an integrin and gastrin-releasing peptide receptor, in particular prostate cancer cells. The disclosure, therefore, firstly encompasses compositions that can comprise a heterodimeric probe comprising a first peptide domain comprising a moiety capable of selectively binding to an integrin; a second peptide domain comprising a moiety capable of selectively binding to a gastrin-releasing peptide receptor; a linker connecting the first peptide domain and the second peptide domain; and a prosthetic group. The first peptide domain comprises at least one tripeptide comprising the amino acid sequence of arginine-glycine-aspartate, and the second domain can be the peptide bombesin(7-14).

Abstract: A method of detecting an accessory cancer lesion, comprising an administration step wherein indocyanine green is administered to a living body, an irradiation step wherein a target organ suspected of having cancer is surgically exposed and irradiated with excitation light of indocyanine green, an imaging step wherein a near-infrared fluorescence intensity distribution image from the excited indocyanine green in the target organ is obtained, and an identification step wherein an area having the near-infrared fluorescence in the intensity distribution image, excluding the area detected in preoperative examination or intraoperative macroscopic observation, is identified as an accessory cancer lesion.

Abstract: The present disclosure is directed to compounds, diagnostic agents, and related methods. In some cases, methods for treating patients are provided. More specifically, the disclosure provides compounds, diagnostic agents, and kits for detecting and/or imaging and/or monitoring elastin rich tissues. In addition, the disclosure provides methods of detecting and/or imaging and/or monitoring the presence of coronary plaque, carotid plaque, iliac/femoral plaque, aortic plaque, renal artery plaque, plaque of any arterial vessel, aneurism, vasculitis, other diseases of the arterial wall, and/or damage or structural changes in ligaments, uterus, lungs or skin, as indicated by changes in total vessel wall area, internal lumen size, and exterior arterial perimeter.

Abstract: The present invention relates to a quinoline or quinazoline derivative having the general formula (A): in which R3, R4, W, Y and Q are indicated in the description and the claims, the use of the compounds of the general formula (A) for the treatment of various disorders, and the preparation of compounds of the general formula (A).

Abstract: This invention relates to novel compounds suitable for labelling or already labelled by 18F, methods of preparing such a compound, compositions comprising such compounds, kits comprising such compounds or compositions and uses of such compounds, compositions or kits for diagnostic imaging by positron emission tomography (PET).

Abstract: The present invention provides novel alpha-fluoroalkyl dihydrotetrabenazine compounds I wherein R1 is a C1-C10 fluorinated aliphatic radical; R2 is hydrogen or a C1-C10 aliphatic radical; R3 is hydrogen or a C1-C10 aliphatic radical; and R4 is a C1-C10 aliphatic radical, a C3-C10 cycloaliphatic radical, or a C3-C10 aromatic radical. The alpha-fluoroalkyl dihydrotetrabenazine compounds are provided in both racemic and enantiomerically enriched forms and may comprise either or both of fluorine-18 and fluorine 19. The alpha-fluoroalkyl dihydrotetrabenazine compounds are believed to possess high affinity for VMAT-2, a biomarker implicated in human diabetes. The alpha-fluoroalkyl dihydrotetrabenazine compounds comprising a fluorine-18 group are useful as PET imaging agents targeting the VMAT-2 biomarker. The non-radiolabled alpha-fluoroalkyl dihydrotetrabenazine compounds are useful as probes for the discovery of PET imaging agents.

Abstract: A molecular probe for use in the detection of amyloid in a subject includes a dibenzothiazole derivative.

Abstract: The present application discloses methods for identifying inhibitors with high binding-affinity for the carbonic anhydrase-IX (CA-IX) enzyme using click chemistry and uses the candidates thereof as positron emission tomography (PET) imaging agents.

Abstract: The present invention is related to a compound of formula (I), wherein A is a nonaromatic heterocyclic ring, Ar is either absent or phenylene; ? is a radical of formula (II), R2 is a hydrophobic moiety; and G is a radical containing one or more moieties selected from the group consisting of NH, OH and a basic moiety. The compounds are inhibitors of integrins, especially antagonists of the fibronectin receptor alpha5beta1, useful as anti-angiogenic agents.

Abstract: The instant invention provides a method for diagnosing an infection in a subject by administering to the subject a compound suitable for imaging which binds to a thymidine kinase present in the infecting organism, and obtaining an image of the subject to determine the presence and location of the compound, wherein a localization of the compound is indicative that the subject has an infection.

Abstract: This invention relates to new fluorescent chemical entities that are designed to attach to biocompatible molecules to form in vivo optical imaging agents.

Abstract: A method of identifying a patient as prodromal to a disease associated with amyloid deposition by imaging techniques is provided. In addition, a method of identifying amyloid deposition diseases in patients who present with a dementing disorder of questionable etiology by imaging techniques is provided. The methods discloses substances which are used for imaging and generating data which can be used to determine progress of an asymptomatic patient to a disease associated with amyloid deposition, or to identify amyloid deposition diseases in patients who present with a dementing disorder of questionable etiology.

Abstract: The present invention relates to a class of compounds of Formula (I) and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing a cyanuric acid scaffolding moiety allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract: This invention relates to new fluorescent chemical entities, including fluorescent molecules that comprise a carboxyl or carbonyl functionalized pyridine moiety. This invention also relates to the corresponding reactive versions of such molecules. This invention also relates to the corresponding conjugates with moieties such as peptides, proteins, various biomolecules, carbocyclic and heterocyclic compounds, sugars, and their uses thereof.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing an aliphatic N-heterocyclic central moiety such as pyrrolidine or piperidine heterocycles allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging, in particular in X-ray imaging, and to contrast media containing such compounds.

Abstract: A positive contrast agent composition containing meglumine diatrizoate, sodium diatrizoate, simethicone, famotidine and aspartame in predetermined amounts that is orally administered to a patient for clinical evaluations of appendicitis wherein a positive contrast effect is achieved. Methods of use include orally administering individual doses of the composition approximately 50 minutes prior to appendix visualization using computerized axial tomography.

Abstract: This invention provides a method of administering methotrexate triglutamate (MTXglu3), an inhibitor of the neurocarboxypeptidase activity of prostate specific membrane antigen, to a subject so as to inhibit release of glutamate by N-acetylaspartylglutamic acid (NAAG) hydrolysis in the subject.

Abstract: The present invention relates to radiolabelled compounds of formula (I), which are useful for the labelling and diagnostic imaging of histamine H3 receptor functionality.

Abstract: The present invention provides indeno[2,1a]indene and isoindolo[2,1-a]indole derivatives of the Formula I, its salts and its stereoisomers, wherein X, R1, R2, R3, R4, R6, R7, R8, R9, R11, R12, R13 and R14 are as described in the specification. The invention also provides a method to prepare the compound of formula I, pharmaceutical composition containing such compounds, and method to manufacture a medicament. These compounds are useful in the treatment of various CNS disorders, hematological disorders, eating disorders, diseases associated with pain, respiratory diseases, genito-urological disorders, cardio vascular diseases and cancer.

Abstract: The present invention is directed to low toxicity boronated compounds and methods for their use in the treatment, visualization, and diagnosis of tumors. More specifically, the present invention is directed to low toxicity carborane-containing porphyrin compounds with halide, amine, or nitro groups and methods for their use particularly in boron neutron capture therapy (BNCT), X-ray radiation therapy (XRT), and photodynamic therapy (PDT) for the treatment of tumors of the brain, head and neck, and surrounding tissue. The invention is also directed to using these carborane-containing porphyrin compounds in methods of tumor imaging and/or diagnosis such as MRI, SPECT, or PET.

Abstract: New diagnostic agents for positron emission tomography (PET) and methods for use of such agents for imaging of human or animal tissue are described, wherein a primary active component of such agents is a radiolabeled halogenated xanthene or halogenated xanthene derivative. Preferably, the radiolabeled halogenated xanthene is radiolabeled Rose Bengal or a functional derivative of Rose Bengal.

Abstract: The present invention relates to a class of compounds and to diagnostic compositions containing such compounds where the compounds are iodine containing compounds. More specifically the iodine containing compounds are chemical compounds containing a cyanuric acid scaffolding moiety allowing for the arrangement of three iodinated phenyl groups bound thereto. The invention also relates to the use of such diagnostic compositions as contrast agents in diagnostic imaging and in particular in X-ray imaging and to contrast media containing such compounds.

Abstract: The present invention relates to Halogenated amino acid analogues for use in diagnosis, which compounds have the general formula (I) wherein: R is (C1–C6) alkyl optionally substituted with thioether or ether oxygen atom when n=0, or a substituted aromatic or heteraromatic ring when n=1–6; and m=0 or 1; and X is a halogen atom.

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: 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: Methods, compounds, compositions and kits that relate to pretargeted delivery of diagnostic and therapeutic agents are disclosed. In particular, methods for radiometal labeling of biotin and for improved radiohalogenation of biotin, as well as related compounds, are described. Also, clearing agents, anti-ligand-targeting moiety conjugates, target cell retention enhancing moieties and additional methods are discussed.

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: The present invention provides a novel paramagnetic metal-phthalocyanine complexes and pharmaceutically acceptable salts thereof, which are useful as contrast agents for MRI(Magnetic Resonance Imaging), diagnostic X-ray imaging and computed tomography(CT). The present invention also provides contrast agents for imaging, comprising the new paramagnetic metal-phthalocyanine complexes. The new contrast agents of the present invention show high imaging enhancement effects at lower concentration and are safer than the previously reported contrast agents.

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: The invention is based in part on the discovery that nonselective ? agonists that possess ? receptor-mediated effects in addition to their ? agonist effects can decrease cocaine self-administration more effectively and with fewer undesirable side effects than can highly selective ? agonists. The invention includes a number of new compounds having both nonselective ? opioid receptor agonist activity and additional activity at ? opioid receptors. These compounds are useful for the treatment of cocaine abuse, and can also be radiolabeled for use as imaging agents, e.g., the N-fluoroalkyl and iodoalkyl derivatives can be used, respectively, for positron emission tomography (PET) and single photon computed tomography (SPECT) brain 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: Systems and methods for radiographic imaging of tissue using a radio-opaque imaging agent that in one embodiment accumulates intracellularly in tissue in proportion to its functional, or physiological, activity. In one embodiment, the imaging agent is a cell membrane-permeable, radio-opaque, high affinity ligand for an intracellular target. The imaging agent is administered to a patient, and after an accumulation interval, radiographic images are acquired. The imaging agent preferentially accumulates in certain types of tissue and increases its radio-opacity. The tissue being examined is transilluminated by X-ray beams with preselected different mean energy spectra, and a separate radiographic image is acquired during transillumination by each beam. An image processing system may perform a weighted combination of the acquired images to produce a single displayed image. The system and method thus provides a functional image displayed with the anatomical detail and spatial resolution of a radiographic image.

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.