Abstract: The present invention provides novel compounds that find use as imaging agents within nuclear medicine applications (e.g., PET imaging and SPECT imaging). The present invention also provides imaging compositions for use within nuclear medicine applications. Additionally, the present invention provides methods of imaging.

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

Abstract: The present invention relates to compounds particularly asymmetric urea compounds which are labeled with one or more radioisotopes and which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors which express NAALADase and/or PSMA. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled compounds of the invention, particularly tissues, organs, or tumors which express NAALADase and/or PSMA to which the compounds of the invention have an affinity.

Abstract: Presented is a method for assessing dopamine transporter levels in a selected area of a subject's central nervous system by SPECT imaging comprising administering an injection of a labeled dopamine transporter ligand at approximately the time the subject is positioned for SPECT imaging and initiating a SPECT acquisition for a duration of about 30 minutes commencing at about 15 minutes after administration of labeled dopamine transporter ligand; and assessing, based on said SPECT acquisition, the amount of labeled dopamine transporter ligand that is bound to dopamine transporter.

Abstract: The present invention relates to novel therapeutic and diagnostic dendrimers. In particular, the present invention is directed to dendrimer based multifunctional compositions and systems for use in disease diagnosis and therapy (e.g., cancer diagnosis and therapy). The compositions and systems comprise one or more components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and monitoring the response to therapy of a cell or tissue (e.g., a tumor).

Abstract: It is an objective of the present invention to provide a positron tomography method applicable to the diagnosis of specific brain diseases and to provide a positron-emitting compound for use in the method. The present invention method relates to a positron tomography method for measuring a distribution and concentration of a positron-emitting source, and is characterized in using the compound (I) as the positron-emitting source.

Abstract: The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.

Abstract: Methods of determining rate of biosynthesis or breakdown of biological molecules from metabolic derivatives and catabolic products are disclosed herein. In particular, methods of measuring the rates of biosynthesis and breakdown of biological molecules inaccessible or not easily accessible to direct sampling by sampling metabolic derivatives and catabolic products in accessible biological samples are disclosed herein.

Abstract: The present invention relates to novel 5-pyrrolidinylsulfonyl isatin derivatives, non-peptidyl Caspase binding Radioligands (CbRs) and CbR-transporter conjugates derived from said isatin derivatives, diagnostic compositions comprising said compounds of the invention and their use for non-invasive diagnostic imaging.

Abstract: Novel benzamide compounds of Formula (I), Formula (II), and Formula (III), salts, water soluble salts, analogs and radiolabeled counterparts thereof as sigma-2 receptor radiotracers for imaging the proliferative status of solid tumors. A method for diagnosing a mammal for the presence of a mammalian tumor therein comprises administering to the mammal a diagnostic imaging detectable effective amount of a benzamide compound having a structure illustrated in Formula (I), Formula (II) and Formula (III) and detecting binding of the compound to a tumor in the mammal. A method for diagnostic imaging of a mammalian tissue having cell surface sigma-2 receptors comprising administering to a mammal a diagnostic imaging amount of a compound having a structure illustrated in Formula (I) Formula (II) and Formula (III) and detecting an image of a tissue having an ample cells with sigma-2 receptors.

Abstract: The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.

Abstract: A compound having structure I: wherein xC is selected from the group consisting of 11C, 12C, and 13C; R is selected from the group consisting of —OH, —O?R4+ wherein R4 is selected from the group consisting of Na and K, —OR3 wherein R3 is selected from the group consisting of C1-8 alkyl and C1-8 alkenyl, —NH2, and NHR3; R? is selected from the group consisting of —H, —Cl, —F, —Br, and —I; R? is selected from the group consisting of —H, —Cl, —F, —Br, and —I; and R?? is selected from the group consisting of —H, —Cl, —F, —Br, —I, 18F, 19F, 75Br, 76Br, 77Br, 123I, 124I, and 131I; provided, when xC is 12C, R?? is selected from the group consisting of 18F, 19F, 75Br, 76Br, 77Br, 123I, 124I, and 131I.

Abstract: A compound is represented by Structural Formula A1: C—B-L-A??A1 or a pharmaceutically acceptable salt or solvate thereof. A is a prostate specific membrane antigen (PSMA) ligand; L is an optionally substituted aliphatic or heteroaliphatic linking group; B includes at least one optionally substituted moiety selected from the group consisting of a sugar, a charged group, an aryl ring, and a heteroaryl ring, wherein B optionally includes a drug or a labeling agent; and C is H, a drug, or a labeling agent, wherein CB together comprises the drug or the labeling agent. The compounds are useful as PSMA agents and in pharmaceutical compositions, methods for treating and detecting diseases such as cancer in a subject, methods for identifying cancer cells in a sample, methods for inhibiting tumor neovascularization, methods for identifying drugs that can treat cancer, and the like.

Abstract: In vivo determination of regional damage with neural and organ injury specific imaging agents. Rapid, and non-invasive imaging compositions and methods for assessment of the extent of neurotoxic cell loss or nervous system damage resulting from nervous system injury due to ischemia, stroke, trauma, chemical or electrical insult, acute drug overdose or exposure to substance abuse (such as “recreational drugs”) infection or other insults. The same or similar rapid, and non-invasive imaging compositions and methods for assessment of the extent of the organ injury comprises any damage, injury or infection, functional failure to specific organs such as liver, kidney, prostate, lung, skeletal muscle, heart, pancreas, stomach, small and large intestine, bladder and the reproductive system as well as damage, injury or infection, functional failure to multi-organs, trauma-hemorrhagic shock and sepsis.

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 compounds that selectively bind to cells undergoing perturbations and alterations of their normal plasma membrane organization, such as cells undergoing apoptosis or activated platelets. The invention further provides methods for utilizing said compounds in medical practice, for diagnostic and therapeutic purposes.

Abstract: Racemic mixtures and enantiomerically pure forms of novel 1-[(2?-substituted)-piperazin-1?-yl]-isoquinolines are norepinephrine (NE) transporter (NET) inhibitor compounds. Compounds of the invention are considered therapeutic agents for central nervous system (CNS) diseases and disorders, without limitation, including neurodegeneration, anxiety, depression, attention deficit disorders, drug dependency, and post traumatic stress disorder. Examples of the chemical syntheses of the compounds of the invention are provided. The isoquinoline compounds of the invention competitively bind at NET at nanomolar concentrations. The isoquinoline agents of the invention bind selectively to NET over other competitive transporter targets and receptor binding sites, including those of serotonin and dopamine, amongst others. The chemical syntheses of the invention are suitable for labeling with radionuclide atoms.

Abstract: The inventors propose to label a chlorotoxin with I-123 or I-124 for a diagnostic agent, and with I-124 or I-131 for a therapeutic agent to reduce tumors and then to use a process they previously invented to stabilize the radiopharmaceutical. The inventors propose to reconstitute the preferred agents and administer them cyclically to diagnose and treat tumors. The inventors also propose a TETA or DOTA link to a metal radioisotope.

Abstract: The present invention relates in part to a method of imaging cardiovascular plaque formation in a mammal comprising administering to the mammal an effective amount of 18F-2-fluorodeoxy-D-glucose and then detecting the 18F-2-fluorodeoxy-D-glucose.

Abstract: Hsp90 inhibitors are provided having the formula: with a 2?,4?,5?-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4? and 5? positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO2. alkyl, COO-alkyl, KH2, OH, CN, SO2X5, NO2, NO, C?SR2 NSO2X5, C?OR2, where X5 is F, NH2, alkyl or H, and R2 is alkyl, NH2, NH-alkyl or O-alkyl, C1 to C6 alkyl or alkoxy; or wherein X1 has the formula -0-(CH2)n-0-, wherein n is an integer from O to 2, preferably 1 or 2, and one of the oxygens is bonded at the 5?-position and the other at the 4?-position of the aryl ring. The compounds are useful in cancer therapy and as radioimaging ligands.

Abstract: Screening and diagnostic reagents, kits and methods for metastatic colorectal cancer or primary and/or metastatic stomach or esophageal cancer are disclosed. Compounds, compositions and methods of treating patients with metastatic colorectal cancer or stomach or esophageal cancer and for imaging metastatic colorectal cancer or stomach or esophageal tumors in vivo are disclosed. Compositions and methods for delivering active compounds such as drugs, gene therapeutics and antisense compounds to metastatic colorectal cancer or stomach or esophageal cells are disclosed. Vaccines compositions and methods of for treating and preventing metastatic colorectal cancer or primary and/or metastatic stomach or esophageal cancer are disclosed.

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: This invention relates to new radiohalogenated benzamide derivatives and their use in tumor diagnosis and tumor therapy. The radiohalogenated benzamide derivatives according to the invention exhibit novel and especially advantageous properties, in particular with respect to tumor concentration and retardation, liver concentration and blood accumulation. The radiation-therapy doses to be achieved in the tumor, compared to healthy body tissue, are advantageous for the compounds according to the invention.

Abstract: The present invention provides an automated method for the preparation of 123I-labelled radiopharmaceutical compositions, together with disposable cassettes for use in the method. The use of an automated synthesizer apparatus in the preparation of 123I-labelled radiopharmaceuticals is also described. Also described is the use of cassettes of the present invention in the preparation of 123I-labelled radiopharmaceuticals.

Abstract: The present invention relates to novel modified fatty acid analogs, where a positron or gamma-emitting label is placed at a position on a fatty acid backbone and an organic substituent is substituted at the 2,3; 3,4; 4,5; 5,6 and other sequence positions of a fatty acid backbone. These novel fatty acid analogs are designed to enter the tissues of interest by the same long chain fatty acid carrier mechanism as natural fatty acids, however, functional substituents in the 2,3; 3,4; 4,5; 5,6 and other sequence positions, block the catabolic pathway, thus trapping these analogs in a virtually unmodified form in the tissues of interest.

Abstract: Compounds derived from phenylethyl imidazole carboxylic acid esters have shown selective accumulation of radioactivity in the adrenal cortex, when labeled with a radioactive halogen. In particular, these compounds bind selectively to adrenocortical tissue facilitating the diagnosis of adrenal cortical masses such as incidentaloma, adenoma, primary and metastatic cortical carcinoma. Trace amounts are injected intravenously and accumulate rapidly in the adrenals, maintaining a high radioactivity plateau, which permits external imaging using computed SPECT (single photon emission) or PET (positron emission) techniques. Independent of the position and type of the radioactive label, the compounds according to the invention are potent inhibitors of steroid P450c11 hydroxylation and bind with high affinity on sites of cortisol secretion. In order to avoid saturation of receptor sites, high specific activity labeling is mandatory for application in patients.

Abstract: The invention provides a composition of matter of the formula (I): V-L-R, where V is a vector moiety having affinity for an angiogenesis-related endothelias cell receptor, L is a linker moiety or a bond and R is a detectable moiety, characterised in that V is a non-peptidic organic group, or V is peptidic and R is a macromolecular or particulate species providing a multiplicity of labels detectable in in vivo imaging.

Abstract: Provided is a class of radiolabeled androgen receptor targeting agents (ARTA), useful for prostate cancer imaging and in treating or preventing prostate cancer. The agents define a new subclass of radiolabeled compounds, which are selective androgen receptor modulators (SARM), which demonstrate antiandrogenic activity of a nonsteroidal ligand for the androgen receptor, and/or which bind irreversibly to the androgen receptor. The present invention further provides methods for a) imaging of cancer in a subject, b) imaging an androgen receptor-containing tissue in a subject, c) in-vivo imaging in a subject, d) treating a subject suffering from prostate cancer, e) delaying the progression of prostate cancer in a subject suffering from prostate cancer, f) preventing the recurrence of prostate cancer in a subject suffering from prostate cancer, and g) treating the recurrence of prostate cancer in a subject suffering from prostate cancer, which comprise using the radiolabeled compounds of the present invention.

Abstract: New intracorporeal photodynamic medicaments and certain medical uses and methods for use of such photodynamic medicaments for treatment of disease in human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene or halogenated xanthene derivative. In preferred embodiments, such medicaments are used for treatment of a variety of conditions affecting the skin and related organs, the mouth and digestive tract and related organs, the urinary and reproductive tracts and related organs, the respiratory tract and related organs, the circulatory system and related organs, the head and neck, the endocrine and lymphoreticular systems and related organs, various other tissues, such as connective tissues and various tissue surfaces exposed during surgery, as well as various tissues exhibiting microbial or parasitic infection.

Abstract: The invention relates to radiolabeled compounds and their use in methods of imaging amyloid deposits, as well as to methods of their manufacture. The invention also relates to compounds for inhibiting the aggregation of amyloid proteins that form amyloid deposits, methods for delivering therapeutic agents to amyloid deposits, as well as methods of making compounds that inhibit the aggregation of amyloid proteins.

Abstract: New intracorporeal photodynamic medicaments and certain medical uses and methods for use of such photodynamic medicaments for treatment of disease in human or animal tissue are described, wherein a primary active component of such medicaments is a halogenated xanthene or halogenated xanthene derivative. In preferred embodiments, such medicaments are used for treatment of a variety of conditions affecting the skin and related organs, the mouth and digestive tract and related organs, the urinary and reproductive tracts and related organs, the respiratory tract and related organs, the circulatory system and related organs, the head and neck, the endocrine and lymphoreticular systems and related organs, various other tissues, such as connective tissues and various tissue surfaces exposed during surgery, as well as various tissues exhibiting microbial or parasitic infection.

Abstract: High energy phototherapeutic agents or radiosensitizer agents comprised of a halogenated xanthene, or other related agents that exhibit a preference for concentration in biologically sensitive structures in diseased tissue, and methods of treating and imaging using such radiosensitizer agents in such diseased tissue are described herein.

Abstract: A one-step procedure for sentinel lymph node identification and biopsy using a single compound, a radiolabeled, low molecular weight dye (e.g., 125I-labeled methylene blue). This radiolabled dye is mixed with an unlabeled, similar molecular weight dye (e.g., isosulfan or methylene blue). The mixture is injected at the time of surgery, and rapidly migrates to reach the lymph nodes in less than 20 min, more preferably in less than 15 min and most preferably in less than 10 min. Using rabbits, rapid transit of 125I-methylene blue to regional lymph nodes with limited systemic biodistribution has been confirmed. By admixing small amounts of radiolabeled dye with a large amount of unlabeled dye, the sentinel lymph node identification was similar to that for the prior two-step dual mapping process, but with enhanced SLN localization because of the lower energy gamma emission of 125I as compared with 99mTc.

Abstract: The present invention provides novel compounds that bind selectively to cells undergoing perturbations and alterations of the normal organization of their plasma membrane, while binding to a lesser degree to cells having membranes of normal organization, and their uses as diagnostic probes. Said compounds and methods used therein may be useful in medical practice, for applications such as diagnosis of disease and monitoring of response to therapy.

Abstract: Radiopharmaceutical compositions which are stabilized by addition of a hydrophilic thioether.

Abstract: This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's Disease, familial Alzheimer's Disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.

Abstract: Radiopharmaceutical compositions which are stabilized by addition of a hydrophilic 6-hydroxy-chroman derivative.

Abstract: Novel epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors, pharmaceutical compositions including same and their use in the treatment of EGFR-TK related diseases or disorders are disclosed. Novel radiolabeled EGFR-TK inhibitors as 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 further disclosed. The disclosed EGFR-TK inhibitors comprise a polyalkylene glycol moiety and/or a hydroxy-containing moiety and are characterized by improved solubility, biostability and bioavailability. Processes of preparing the disclosed EGFR-TK inhibitors and of radiolabeling same, via, for example, one-step radiosyntheses, are also disclosed.

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: This invention provides novel cyclooxygenase-2 selective agents that are particularly useful as imaging probes in non-invasive imaging techniques, such as PET and SPECT. Preferred cyclooxygenase-2 selective agents inhibit cyclooxygenase-2 activity with greater potency and specificity than conventional cyclooxygenase-2 inhibitors. Other aspects of the invention include pharmaceutical compositions including the cyclooxygenase-2 selective agents as well as methods for detecting and/or inhibiting cyclooxygenase-2. These methods are particularly useful for diagnosing and treating disorders, such as inflammation, which is characterized by elevated cyclooxygenase-2 levels.

Abstract: A radioactive iodine-labeled compound represented by the following formula (I): wherein X represents a radioactive iodine atom which may substitute at an arbitrary position on the benzene ring (preferably 123I, 125I and the like.), n represents an integer of 1 to 3, R1 and R2 each independently represent a substituted or unsubstituted alkyl group, Y represents an alkylene group having 1 to 6 carbon atoms (preferably methylene group), M represents a counter ion, and m represents the number of ions required to neutralize the charge of the molecule. A radioactive iodine-labeled compound that can selectively accumulate in tumor cells or tumor tissue and a scintillation imaging agent containing the compound are provided.

Abstract: The present invention provides novel imaging agents for clinical diagnosis of injuries and diseases, in the form of a radionuclide in spatial proximity to a substantially pure stereoisomer of a fatty acid analog. The invention also provides methods for using the novel imaging agents, and kits containing one or more of the novel imaging agents of the invention.

Abstract: A laparoscopic tumor therapy method and an articulated electron beam transport system are provided for use with a high power, long focus electron source for tumor therapy. The high power, long focus electron source generates an e-beam. The e-beam is transported through a laparoscopic tube proximate a target tumor for electron irradiation therapy.

Abstract: Highly hydrophilic indole and benzoindole derivatives that absorb and fluoresce in the visible region of light are disclosed. These compounds are useful for physiological and organ function monitoring. Particularly, the molecules of the invention are useful for optical diagnosis of renal and cardiac diseases and for estimation of blood volume in vivo.

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 haloaromatics are disclosed, as well as processes for the preparation of the intermediate precursor insoluble polymer compounds.

Abstract: This invention relates to novel thioflavin derivatives, methods of using the derivatives in, for example, in vivo imaging of patients having neuritic plaques, pharmaceutical compositions comprising the thioflavin derivatives and method of synthesizing the compounds. The compounds find particular use in the diagnosis and treatment of patients having diseases where accumulation of neuritic plaques are prevalent. The disease states or maladies include but are not limited to Alzheimer's disease, familial Alzheimer's disease, Down's Syndrome and homozygotes for the apolipoprotein E4 allele.

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: Radiolabeled conjugates are disclosed which have a component that is effective to target tumor cells, which cells selectively take up and degrade the conjugate, thereby delivering to the tumor cell nucleus a radioisotope capable of being incorporated into the nuclear material, so as to produce a cytotoxic effect and/or to render the cell detectable by radioimaging.

Abstract: This invention pertains to methods, mixtures, kits and/or compositions for the determination of analytes by mass analysis using unique labeling reagents or sets of unique labeling reagents. The labeling reagents can be isomeric or isobaric and can be used to produce mixtures suitable for multiplex analysis of the labeled analytes.

Abstract: A method of simply and quickly determining ?-ray releasing nuclides having long half-life without carrying out a chemical separation is provided. By inputting a data of pulses incident to an ?-ray detector in a computer, obtaining time distribution of the incident pulses by using a very short time measuring timer and plotting, and fitting the linear originated in a random event corresponding to the background and the non-linear originated in the correlated events of parent nuclides-progenies by using the least squares method, the whole generating probability P (t) from the parent nuclide to the progeny thereof is obtained. By subtracting the random events portion from the P(t), the correlated events portion is extracted. The radioactivity per unit can be obtained by dividing the extracted correlated events portion by the measured time, the amount of the supplied sample and the counting efficiency.