Abstract: An anti-tumor agent comprising combination of a radioactive diacetyl-bis(N4-methylthiosemicarbazone) copper complex and a metabolic inhibitor.

Abstract: The invention relates to a method for diagnosing a kidney disease state. The method comprises the steps of administering to a patient a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises a diagnostic marker, and diagnosing the kidney disease state. The invention also relates to a method for treating a kidney disease state. The method comprises the steps of administering to a patient suffering from the disease state an effective amount of a composition comprising a conjugate or complex of the general formula V-L-D where the group V comprises a vitamin receptor binding ligand that binds to kidney proximal tubule cells and the group D comprises an antigen, a cytotoxin, or a cell growth inhibitor, and eliminating the disease state.

Abstract: A method for identifying a molecule that binds an irradiated tumor in a subject and molecules identified thereby. In some embodiments, the method includes the steps of (a) exposing a tumor to ionizing radiation; (b) administering to a subject a library of diverse molecules; and (c) isolating from the tumor one or more molecules of the library of diverse molecules, whereby a molecule that binds an irradiated tumor is identified. Also provided are targeting ligands that bind an irradiated tumor and therapeutic and diagnostic methods that employ the disclosed targeting ligands.

Abstract: The present invention discloses a method for the enzyme-mediated, site-specific, in-vivo precipitation of a water soluble molecule in an animal. The enzyme is either unique to tumor cells, or is produced within a specific site (e.g., tumor) at concentrations that are higher than that in normal tissues. Alternatively, the enzyme is conjugated to a targeting moiety such as an antibody or a receptor-binding molecule.

Abstract: It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula: wherein n is an integer of 0 or of 1 to 4; R1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR2; R2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R3 is a protective group.

Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.

Abstract: In accordance with the purpose(s) of the present disclosure, as embodied and broadly described herein, embodiments of the present disclosure, in one aspect, relate to methods of detecting the over-expression of epidermal growth factor receptor (EGFR) in a subject or sample, methods of diagnosing the presence of one or more angiogenesis related diseases or related biological events in a subject or sample, method of monitoring the progress of one or more angiogenesis related diseases or related biological events in a subject or sample, a 18F-FBEM-CYS-ZEGFR:1907 probe, compositions including a 18F-FBEM-CYS-ZEGFR:1907 probe, and pharmaceutical compositions including a 18F-FBEM-CYS-ZEGFR:1907 probe and the like.

Abstract: Methods are disclosed for using stable isotopes of carbon and nitrogen in hair and feces to predict disease in animals such as predicting the susceptibility of dairy cows to periparturient production-related metabolic diseases (PRMDs). Other methods that are disclosed are for using stable isotopes of carbon and nitrogen in blood components, erythrocytes and plasma proteins, to predict dairy cow susceptibility to PRMDS; yet other disclosed methods are for using stable isotopes of carbon and nitrogen in hair and feces of horses as a prognostic indicator after surgical or medical correction of gastrointestinal colic. Other methods that are disclosed also include using stable isotopes of carbon and nitrogen in blood components, erythrocytes and plasma proteins, of horses as a prognostic indicator before or after surgical or medical correction of gastrointestinal colic.

Abstract: A radiolabeled annexin comprising at least 2 up to 20 histidine residues at its N-terminus is disclosed. At least two of said histidine residues are adjacent or separated by no more than one other amino acid. The radiolabeled annexin is a stable complex with a radionuclide such as technetium 99m. The radiolabeled annexin can be used in a method of imaging cell death in a nucleated cell within a region of a mammalian subject in vivo.

Abstract: The present invention relates to compounds and related technetium and rhenium complexes thereof which are suitable for imaging or therapeutic treatment of tissues, organs, or tumors. In another embodiment, the invention relates to methods of imaging tissues, organs, or tumors using radiolabeled metal complexes, particularly tissues, organs, or tumors which express certain receptors to which the compounds or complexes of the invention have an affinity. The present invention also relates to methods of treating cancer, particularly those cancer lines which express certain receptors to which the compounds or complexes of the invention have an affinity. In yet another embodiment, the present invention provides methods of imaging and/or inhibiting receptors or neuroreceptors using compounds or complexes of the invention which have an affinity for the receptor or neuroreceptor to be imaged and/or inhibited.

Abstract: This invention relates, e.g., to a method for designing or selecting on a computer a candidate small molecule amyloid binder or inhibitor, comprising: a) docking test compounds to the binding site or binding surface determined from the three-dimensional structure of a co-crystal of a protofilament of an amyloid protein bound to a small molecule which is known to bind to the amyloid protein, and (b) selecting test compounds which exhibit an energy below that of the small molecule used to form the co-crystal made in a), as candidate amyloid binders.

Abstract: A method and a kit for detecting myelin basic protein are provided. The method comprises administering an agent, which binds to myelin basic protein (MBP), to a subject at risk of or diagnosed with a myelin-associated neuropathy, and determining myelination by detecting the agent resided in the subject. The amount of the agent present in the subject is indicative of a myelin-associated neuropathy. A method of quantifying an amount of MBP present in a tissue sample is also provided, wherein the method comprises contacting the tissue sample with the same agent, detecting the agent present in the tissue sample; and quantifying an amount of the agent present in the tissue sample.

Abstract: Compounds having formula I, or pharmaceutically acceptable salts, hydrates or N-oxides thereof are provided and are useful for binding to CXCR7, and treating diseases that are dependent, at least in part, on CXCR7 activity. Accordingly, the present invention provides in further aspects, compositions containing one or more of the above-noted compounds in admixture with a pharmaceutically acceptable excipient.

Abstract: The present invention concerns a therapeutically labeled napthodianthrone or phenanthro[1,10,9,8-opqra]perylene-7,14-dione compound, which comprises a chemical element or an isotope that has an unstable nucleus and emits radiation during its decay to a stable form sufficient to destroy neighboring cells or tissues for use in a targeted radiotherapy to enhance curability of a warm-blooded animal that has been subjected to a necrosis-inducing antitumor therapy. A particular advantage of present invention is that viable rim resistant to a necrosis-inducing antitumor therapy such as vascular targeting agent (VTA) can be supplemented by one single or repeated doses of a therapeutically radiolabeled small molecule necrosis-avid chemical compound treatment to enhance the curability.

Abstract: The present invention describes oxidized avidin, suitable for inhalation, for conditioning the lung affected by inoperable/diffuse diseases, enabling the targeted delivery of biotinylated therapeutic agents to it.

Abstract: The present application discloses compositions and methods of synthesis and use of 18F- or 19F-labeled molecules of use in PET, SPECT and/or MR imaging. Preferably, the 18F or 19F is conjugated to a targeting molecule by formation of a complex with a group IIIA metal and binding of the complex to a bifunctional chelating agent, which may then be directly or indirectly attached to the targeting molecule. In other embodiments, the 18F or 19F labeled moiety may comprise a targetable construct used in combination with a bispecific antibody to target a disease-associated antigen. The disclosed methods and compositions allow the simple and reproducible labeling of molecules at very high efficiency and specific activity in 30 minutes or less. In preferred embodiments, the bifunctional chelating agent bound to 18F- or 19F-metal complex may be conjugated to the molecule to be labeled at a reduced temperature, e.g. room temperature.

Abstract: The invention relates to an oil-in-water adjuvant emulsion which comprises at least: squalene, an aqueous solvent, a polyoxyethylene alkyl ether nonionic surfactant, a hydrophobic nonionic surfactant, which emulsion is thermoreversible, and wherein 90% of the population by volume of the oil drops has a size less than 200 nm. The invention also relates to a process for preparing an immunogenic composition according to which at least one vaccine antigen is mixed with an oil-in-water emulsion, wherein the oil-in-water emulsion is obtained by means of a temperature-variation phase-inversion process.

Abstract: The present disclosure provides inhibitors of Hsp90 and methods of making and using the same. Such compounds are useful as radioimaging ligands and for the treatment of cancer and other conditions where cell growth or maintenance depend on Hsp90 activity.

Abstract: The present invention relates to an adrenomedullin derivative including an adrenomedullin peptide chelated with at least one active agent. Examples of active agents include a paramagnetic element, a radioactive element and a fibrinolytic agent, among others. Paramagnetic agents have a distribution that is relatively easily shown through Magnetic Resonance Imaging (MRI). Radioactive agents have applications in imaging and delivery of radiations, depending on the specific element included in the active agent. Delivery of fibrinolytic agents mainly to a specific organ, such us for example to the lungs, allows to substantially improve the specificity and efficacy of thrombolytic therapy by allowing local delivery of the fibrinolytic agent, thereby reducing the risks of major bleeding in the therapy of the organ. If the organ is the lungs, a non-limiting example of pathology treatable with the fibrinolytic is pulmonary embolus.

Abstract: The present invention relates to modulated (e.g., magnetically modulated) chemical sensors. In particular, the present invention relates to particles comprising fluorescent indicator dyes and methods of using such particles. Magnetic fields and/or Brownian motion modulate an optical property of the particle to distinguish it from background signals. The present invention thus provides improved methods of detecting a wide variety of analytes in fluids, fluid samples, cells and tissues.

Abstract: The invention relates to micelles that are elaborated with functionality useful for imaging and/or selectively targeting tissue, e.g., in the delivery of hydrophobic agents.

Abstract: This invention provides benzothiazole derivative compounds, compositions comprising such compounds, methods of preparing such compounds, and methods of using such compounds for detecting amyloid deposit(s) and for diagnosing a disease, disorder or condition characterized by amyloid deposit(s).

Abstract: This invention relates to a method of producing and dispensing a foam using a “high lower alcohol content” (>40% v/v of a C1-4 alcohol) liquid composition. The liquid compositions comprise an alcohol, C1-4 (>40% v/v), a silicone-based surfactant of at least 0.001% by weight to prepare a foamable composition, 0-10% w/w of additional minor components added to obtain the desired performance (a foamable composition), and the balance being purified water. The compositions may include emulsifier-emollients and moisturizers, secondary surfactants, foam stabilizers, fragrances, antimicrobial agents, other type of medicinal ingredients, and the like ingredients or additives or combinations thereof commonly added to alcohol gels or foams, aerosol compositions or to toiletries, cosmetics, pharmaceuticals and the like.

Abstract: The present disclosure describes techniques used for colorectal cancer detection. Position and distribution of colorectal cancer tumor are detected through nuclear imaging. Alternatively, stage of colorectal cancer is identified by shading value in tumor. Thus, the present disclosure provides a safe and noninvasive clinical method for diagnosing and tracing level and distribution of colorectal cancer before and after treatment.

Abstract: Imaging agents of formulas (I)-(V) and methods for detecting neurological disorders comprising administering to a patient in need compounds of formulas (I)-(V) capable of binding to tau proteins and ?-amyloid peptides are presented herein. The invention also relates to methods of imaging A? and tau aggregates comprising introducing a detectable quantity of pharmaceutical formulation comprising a radiolabeled compound of formulas (I)-(V) and detecting the labeled compound associated with amyloid deposits and/or tau proteins in a patient. These methods and compositions enable preclinical diagnosis and monitoring progression of AD and other neurological disorders.

Abstract: The invention provides a microsphere comprising an organic lanthanide metal complex wherein the lanthanide metal is present in an amount of more than 20 wt %, based on total microsphere. The invention further provides a suspension comprising such a microsphere. In addition, the invention relates to a method for preparing said microsphere, and the use of the microsphere(s) or suspension for treating a malignancy and/or obtaining a scanning image.

Abstract: Provided are methods to treat cancer, in which (1) a patient is first identified as having a cancer that is likely to be susceptible to gallium therapy, by the use of a gallium scan or other procedure that shows whether the cancer is gallium-avid, and (2) the patient is then treated with a pharmaceutically acceptable gallium composition.

Abstract: One aspect of the invention relates to complexes of a radionuclide with various heteroaryl ligands, e.g., imidazolyl and pyridyl ligands, and their use in radiopharmaceuticals for a variety of clinical diagnostic and therapeutic applications. Another aspect of the invention relates to imidazolyl and pyridyl ligands that form a portion of the aforementioned complexes. Methods for the preparation of the radionuclide complexes are also described. Another aspect of the invention relates to imidazolyl and pyridyl ligands based on derivatized lysine, alanine and bis-amino acids for conjugation to small peptides by solid phase synthetic methods. Additionally, the invention relates to methods for imaging regions of a mammal using the complexes of the invention.

Abstract: This invention relates to a “high lower alcohol content” (>40% v/v of a C1-4 alcohol) liquid composition able to be dispensed as a stable foam with the use of non-propellant foam dispensing devices from non-pressurized containers. The liquid compositions comprise a C1-4 alcohol, (>40% v/v), a silicone-based surfactant of at least 0.001% by weight for foaming to prepare a foamable composition, 0-10% w/w of additional minor components added to obtain the desired performance (a foamable composition), and the balance being purified water. The compositions may include emulsifier-emollients and mosturizers, secondary surfactants, foam stabilizers, fragrances, antimicrobial agents, other type of medicinal ingredients, and the like ingredients or additives or combinations thereof commonly added to alcohol gels or foams, aerosol compositions or to toiletries, cosmetics, pharmaceuticals and the like.

Abstract: This invention relates to molecular imaging agents comprising an S78C mutant synaptotagmin I C2A domain. These agents may be useful in detecting or assessing cell death in vitro and in vivo, for example in tumors following cancer treatment.

Abstract: The invention provides a family of agents that target integrins, which can be used as imaging agents and/or therapeutic agents. The agents can be used to image angiogenesis, inflammation or other physiological processes in a subject.

Abstract: Preferred embodiments relate to compositions of inherently radiopaque, biocompatible, bioresorbable polymeric particles and methods of using them for embolizing a body lumen.

Abstract: The present invention is directed to novel non-invasive diagnostic tools to diagnose numerous infectious disease states or conditions. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these disease states. The novel imaging probe is capable of detecting infected cells, as well tissue. This represents a quantum step forward in the diagnosis and staging of NHL using non-invasively molecular imaging techniques. This novel probe will also be useful to monitor patients response to therapeutic treatments and other interventions or therapies used in the treatment of these disease states or conditions. Compounds according to the present invention may be used as diagnostic tools for a number of conditions and diseases states as well as therapeutic agents for treating such conditions and disease states. Pharmaceutical compositions are also described.

Abstract: The invention relates to a new class of compounds able to inhibit with high affinity and selectivity the 5-HT7 receptor. The invention also relates to the utilization of such compounds as medicaments useful in the treatment and prevention of 5-HT7 receptor relating disorders of the central nervous system. The invention also relates to the isotopically labeled compounds for use in vivo diagnosis or imaging of a 5-HT7 condition.

Abstract: Surface coatings including microparticles immobilized in a matrix of polymeric material on a substrate are described. The microparticles can also include an agent which can be useful for various applications, such as medical applications. This invention relates to the field of surface coatings for use in various applications. More particularly, the invention relates to surface coating useful for drug delivery, imaging and other uses of microparticles immobilized via a polymeric matrix.

Abstract: This invention relates to a “high lower alcohol content” (>40% v/v of a C1-4 alcohol) liquid composition able to be dispensed as a stable foam with the use of non-propellant foam dispensing devices from non-pressurized containers. The liquid compositions comprise an alcohol, C1-4 (>40% v/v), a silicone-based surfactant of at least 0.001% by weight to prepare a foamable composition, 0-10% w/w of additional minor components added to obtain the desired performance (a foamable composition), and the balance being purified water. The compositions may include emulsifier-emollients and moisturizers, secondary surfactants, foam stabilizers, fragrances, antimicrobial agents, other type of medicinal ingredients, and the like ingredients or additives or combinations thereof commonly added to alcohol gels or foams, aerosol compositions or to toiletries, cosmetics, pharmaceuticals and the like.

Abstract: The invention relates to radiodiagnostic and radiotherapeutic agents, including biologically active vectors labelled with radionuclides. It further relates to methods of making such radiodiagnostic and radiotherapeutic agents and the compounds used in such methods. The resultant labelled conjugates are useful as diagnostic agents, for example, as radiopharmaceuticals more specifically for use in Positron Emission Tomography (PET) or Single Photon Emission Computed Tomography (SPECT) or for radiotherapy.

Abstract: This invention includes agents and compositions having MRI, PET, CT, X-ray, SPECT or optical signals, and methods for their use in the determination of a target. In some cases, a MRI, PET, CT, X-ray, SPECT, optical or other signal produced by the agent or composition can be affected by the presence of the target. Examples of targets that can be determined by this invention include, but are not limited to zinc, copper, iron ions and other biological targets. Example of application for imaging in vivo includes the function of pancreas and other organs.

Abstract: Described herein are compositions and methods relating to particles comprising at least one component of a cellular-derived microparticle. Aspects of technology described herein relate to compositions and methods for treating inflammation, wounds, and pain.

Abstract: The present invention relates to novel compounds, pharmaceutical compositions comprising the same, use of said compounds for the manufacture of a medicament for treatment of inter alia compromised lactation conditions as well as to a method for treatment of said conditions, wherein said compounds are administered. The compounds are represented by the general formula (I), as further defined in the specification.

Abstract: The present invention relates to microspheres useful for embolization which comprises polyvinylalcohol. The present invention also relates to an injectable suspension suitable for embolization which comprises the polyvinylalcohol microspheres and a suitable liquid carrier. The present invention further relates to a method for prophylactic or therapeutic embolization which comprises administering to a mammal an injectable suspension containing the polyvinylalcohol microspheres and a suitable liquid carrier. Finally, the present invention relates to a process for producing the polyvinylalcohol microspheres.

Abstract: The cancer-imaging agent and method of radioimaging relates to the use of a radioimaging agent for the imaging increased choline uptake to detect cancerous tissue. The radioimaging agent includes choline or a pharmaceutically acceptable salt thereof labeled with technetium-99m. Preferably, the radioimaging agent is [methyl]-choline chloride labeled with 99mTcO4, which carries technetium-99m. In use, a patient is administered an effective amount of the radioimaging agent by injection and then scanned with a radioimaging device. The radioimaging agent is used to image select soft tissues in the patient, such as the liver or gallbladder, the upper abdominal organs, or the like, and to detect increased choline uptake. Choline is known to accumulate in cancerous cells. Thus, the radioimaging agent is particularly effective in the detection of potentially cancerous tissues.

Abstract: An embodiment of the invention comprises method of imaging a target site comprising administrating ligand of Formula I complexed to 99mTc wherein R1 and R2 are independently an alkyl or cycloalkyl; R3 is and alkyl; X is CO or SO2; Y is (CH2)n, C6H4, (OCH2CH2)n (NHCH2CH2)n and (OCH2CH2CH2)n, or a combination thereof; Z is linker group capable of conjugating to a vector; and n is an integer between 0 and 10.

Abstract: Iodinated amphiphilic compound of formula (I): AG1-X—R??(I) wherein AG1 represents an unsaturated (C8-C52) aliphatic hydrocarbon chain found in fatty acids having specific location of double bonds, the chain including at least one iodine atom directly linked to a carbon atom of a non-conjugated double bond by a covalent link, the second carbon atom of the double bond bearing a halogen atom different from a iodine atom, X represents a polyethylene glycol including 1 to 50 ethylene glycol groups, R represents a hydrogen atom or a group AG2 being identical to or different from AG1, AG1, X, R and AG2 being selected so that the amphiphilic compound has a hydrophilic/lipohilic balance included between 4 and 30.

Abstract: The invention relates to a method of treating or diagnosing a disease state mediated by monocytes. The method utilizes a composition comprising a conjugate or complex of the general formula Ab-X wherein the group Ab comprises a ligand that binds to monocytes, and when the conjugate is being used for treatment of the disease state, the group X comprises an immunogen, a cytotoxin, or a compound capable of altering monocyte function, and when the conjugate is being used for diagnosing the disease state, the group X comprises an imaging agent.

Abstract: The invention enables high-throughput screening of compounds in living systems to detect unanticipated or unintended biological actions. The invention also allows for screening, detection, and confirmation of new indications for approved drugs. Screening and detection of toxic effects of compounds also can be achieved by using the methods of the invention. The methods comprise administering isotope-labeled substrates to a living system so that the label is incorporated into molecules in a manner that reveals flux rates through metabolic pathways thought to be involved in a disease. Comparisons between living systems exposed to compounds and living systems not so exposed reveals the effects of the compounds on the flux rates through the metabolic pathways. Combinations or mixtures of compounds can be systematically screened to detect unanticipated or unintended biological actions, including synergistic actions, in the same manner.

Abstract: The invention provides compositions and methods for therapeutic and diagnostic applications.

Abstract: The invention relates to a method of treating or monitoring/diagnosing a disease state mediated by activated macrophages. The method comprises the step of administering to a patient suffering from a macrophage mediated disease state an effective amount of a composition comprising a conjugate or complex of the general formula Ab-X where the group Ab comprises a ligand capable of binding to activated macrophages, and when the conjugate is being used for treatment of the disease state, the group X comprises an immunogen, a cytotoxin, or a compound capable of altering macrophage function, and when the conjugate is being used for monitoring/diagnosing the disease state, X comprises an imaging agent. The method is useful for treating a patient suffering from a disease selected from the group consisting of rheumatoid arthritis, ulcerative colitis, Crohn's disease, inflammation, infections, osteomyelitis, atherosclerosis, organ transplant rejection, pulmonary fibrosis, sarcoidosis, and systemic sclerosis.

Abstract: The present invention relates to agents capable of binding to myelin basic protein in a subject. Also provided are methods for the detection of myelin-associated neuropathy comprising identifying a subject at risk of or diagnosed with a myelin-associated neuropathy, administering to a subject an agent that binds specifically to myelin basic protein, and determining myelination in the subject by detecting the agent present in the subject. A kit containing the agent or its derivatives for use in detecting myelin basic protein is also provided.

Abstract: A method for producing a radioactive diagnostic imaging agent containing a radioactive 18 fluorine-labeled organic compound represented by the following formula (1): as an effective ingredient in which radiolysis of the effective ingredient is inhibited, involves providing a solution containing the radioactive 18fluorine-labeled organic compound represented by the above formula (1), adding an acid to the solution obtained in the first step in an amount sufficient for the solution to be kept within a pH of 2.0-5.9 in the following third step, and diluting the solution obtained in the second step in order to adjust the solution to a desired radioactive concentration within a pH of 2.0-5.9.