Abstract: In the present invention, different strategies are used to improve the bioavailability of triterpene glycosides and triterpenes including, for example, (a) a covalent approach involving modification with polyethylene glycol and (b) a formulation approach involving non-covalent encapsulation in antibody targeted pol(DL-lactic acid) nanoparticles.

Abstract: Disclosed are carriers for drugs and/or MR imaging agents having a lipid bilayer shell comprising a phospholipid having two terminal alkyl chains, one being a short chain having a chain length of at most seven carbon atoms, the other being a long chain having a chain length of at least fifteen carbon atoms. The mixed long/short chain phospholipids serve to tune the release properties of the carrier. Preferred phospholipids are phosphatidylcholines.

Abstract: A method of determining the thrombogenicity of an implantable medical device is disclosed. The implanted device is exposed in vitro to platelet rich plasma, the activity of an indicator is assayed, and the thrombogenicity is determined.

Abstract: Radiolabeled glutaminylcyclase (QC) inhibitors as imaging agents, in particular, but not exclusively, as medical imaging agents for the detection of neurological disorders; and pharmaceutical compositions, methods and kits for detecting neurological disorders, using the radiolabeled inhibitors.

Abstract: A method for dynamic enhancement of chemical reactions by nanomaterials under hard X-ray irradiation. The nanomaterials were gold and platinum nanoparticles, and the chemical reaction employed was the hydroxylation of coumarin carboxylic acid. The reaction yield was enhanced 2000 times over that predicted on the basis of the absorption of X-rays only by the nanoparticles, and the enhancement was found for the first time to depend on the X-ray dose rate. The maximum turnover frequency was measured at 1 16×10-4 s-1 Gy-1. We call this process chemical enhancement, which is defined as the increased yield of a chemical reaction due to the chemical properties of the added materials. The chemical enhancement described here is believed to be ubiquitous and may significantly alter the outcome of chemical reactions under X-ray irradiation with the assistance of nanomaterials.

Abstract: The present invention provides compositions and methods useful for diagnosing, monitoring the progression, identifying the location, and monitoring the treatment response in ovarian cancer based on detecting and locating VCAM-1 expression.

Abstract: A sensitive method of assessing treatment using molecular and anatomical imaging scans provides automatic tumor identification and quantification within anatomical zones based on treatment criteria. Absolute or comparative measures of tumors in pre- and/or post-scans are thereby isolated from other tissue to accentuate the progress of the treatment when multiple scattered disease lesions are present.

Abstract: The present invention generally relates to methods and system for the synthesis of imaging agents, and precursors thereof. The methods may exhibit improved yields and may allow for the large-scale synthesis of imaging agents, including imaging agents comprising a radioisotope (e.g., 18F). Various embodiments of the invention may be useful as sensors, diagnostic tools, and the like. In some cases, methods for evaluating perfusion, including myocardial perfusion, are provided. Synthetic methods of the invention have also been incorporated into an automated synthesis unit to prepare and purify imaging agents that comprise a radioisotope. In some embodiments, the present invention provides a novel methods and systems comprising imaging agent 1, including methods of imaging in a subject comprising administering a composition comprising imaging agent 1 to a subject by injection, infusion, or any other known method, and imaging the area of the subject wherein the event of interest is located.

Abstract: A target tissue can be treated with a radioisotope. Some methods for treating a target tissue with a radioisotope include determining a distance between a target tissue and a surface of a matrix material to be positioned adjacent the target tissue and, based on the determined distance, determining an activity to be mixed with the matrix material to obtain a desired activity concentration. Some methods further include mixing the radioisotope with the matrix material. In some embodiments, the matrix material comprises bone cement, and the target tissue is a tumor in a bone. The radioisotope may be a beta-emitting radioisotope mixed in the cement at a concentration to form a radioactive cement.

Abstract: The invention provides for a method of enhancing immunological responses to an antigen in a vaccine formulation, and for a vaccine formulation that provides for an enhanced immunological response to an antigen. In the method and formulation the antigen is administered with an adjuvant which adjuvant comprises a solution of nitrous oxide gas in a pharmaceutically acceptable carrier solvent for the gas and which adjuvant includes at least one fatty acid or ester or other suitable derivative thereof selected from the group consisting of oleic acid, linoleic acid, alpha-linolenic acid, gamma-linolenic acid, arachidonic acid, eicosapentaenoic acid [C20: 5?3], decosahexaenoic acid [C22: 6?3], ricinoleic acid and derivatives thereof selected from the group consisting of the C1 to C6 alkyl esters thereof, the glycerol-polyethylene glycol esters thereof and the reaction product of hydrogenated natural oils composed largely of ricinoleic acid based oils, such as castor oil with ethylene oxide.

Abstract: A method of detecting and/or labeling myelin in an animal's peripheral nervous system tissue includes administering to the animal a fluorescent stilbenzene derivative and visualizing the animal's peripheral nervous system tissue using an in vivo imaging modality.

Abstract: Disclosed are a conjugate of a metal nanoparticle including a magnetic core and at least one light emitting material linked to the metal nanoparticle through a linker, wherein the linker has an affinity for a biological material and has changed structure after contacting a biological material, a biosensor including the conjugate, and a method of measuring a concentration of specific biological material in a biological sample using the conjugate or the biosensor.

Abstract: The present invention is directed to novel non-invasive diagnostic tools to image cancers, especially, leukemia and non-Hodgkin's lymphomas (NHL) with minimal toxicity in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probe is capable of detecting precancerous cells, as well as their metastatic spread in tissues. 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 chemotherapy treatments and other interventions or therapies used in the treatment of NHL. 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.

Abstract: The use of an imaging system, cell compartment markers, and molecular markers in methods for correlating the movement of molecules within a cell to a particular compartment are provided, including measuring and correlating molecule movement in adherent and non-adherent cells.

Abstract: A composition comprising: a benefit agent; at least one polymer including a poly(monostearoyl glycerol-co-succinate) polymer; at least one lower alcohol; and at least one co-solvent; and a method for enhancing topical delivery of a benefit agent are disclosed.

Abstract: The present invention relates to an active substance release system containing two compounds. The first compound comprises a nanoparticle, combined with an oligonucleotide inhibition strand that is hybridized with a catalytically active nucleic acid. The second compound comprises a carrier, combined with a substrate molecule that is coupled to a therapeutic active substance. By means of external stimulation, the catalytically active nucleic acid of the first compound is released and specifically binds to the substrate molecule of the second compound. This leads to cleavage of the substrate molecule, whereby the active substance bound thereto is released.

Abstract: The present invention relates to a novel composition useful in targeted diagnostic and/or therapy of a target site, such as cancerous tissue. The composition and methods disclosed herein find particular use in diagnosing and imaging cancerous tissue. The present invention provides a new diagnostic tool for the utilization of positron emission tomography (PET) imaging technique.

Abstract: A drug using the magnetic properties of a metal salen complex as represented by the following general formula in order to magnetize the intended drug by chemically binding the drug to a metal salen complex so that the drug can be delivered to the target diseased site. The drug can be delivered to the diseased site using the magnetic properties of the drug per se without using a carrier made of a magnetic substance as in the conventional methods.

Abstract: The present invention relates to bispecific molecules that are immunoreactive to an activating receptor of a companion animal immune effector cell and to B7-H3, and to the use of such bispecific molecules in the treatment of cancer in companion animals.

Abstract: Tin-117m somatoostatin analogs or antagonist are used to treat tumors and symptoms associated with these tumors which express somatostatin receptors, such as gastroenteropancreatic neuroendocrine tumors. The tin-117m somatostatin receptor binding compounds can be administered at a dosage which is effectively apoptotic and not necrotic. Also, if desired, it can be administered at a dose that is necrotic and/or induces necrosis, but only to cells within 290 microns of the tin-117m atom. A novel somatostatin analog is also disclosed, as well as novel methods to produce the tin labeled analogs and antagonists.

Abstract: The invention relates to a process for preparation of a compound of formula (I): R1 is selected from C1-6alkyl, C2-6alkenyl, and C2-6alkynyl; which comprises: (i) reaction with fluoride, suitably [18F]fluoride, of a corresponding compound of formula (II): wherein R2 is selected from hydrogen, C1-10alkyl, C1-10haloalkyl, C6-14aryl, C6-14arylalkyl, —(CH2CH2O)q—CH3 wherein q is an integer of from 1 to 10; R1 is as defined for the compound of formula (I); and R3 is a leaving group. Certain novel precursors of formula (II) and radiopharmaceutical kits containing such precursors are also claimed.

Abstract: The present invention provides novel compounds and methods for hydrocyanines derived from near-infrared cyanine dyes, as reactive oxygen species probes in imaging. In certain embodiments, the present invention provides reduced dyes as substrates for ELISA and Western blots.

Abstract: Described is a pretargeting method, and related kits, for targeted medical imaging and/or therapeutics, wherein use is made of abiotic reactive chemical groups that exhibit bio-orthogonal reactivity towards each other. The invention involves the use of [4+2] inverse electron demand (retro) Diels-Alder chemistry in providing the coupling between a Pre-targeting Probe and an Effector Probe. To this end one of these probes comprises an electron-deficient tetrazine or other suitable diene, and the other an E-cyclooctene which has one or more axial substituents.

Abstract: The present invention relates to pyrimidine hydroxy amide compounds, the use of such compounds in the inhibition of HDAC6, and the use of such compounds in the treatment of various diseases, disorders, or conditions related to HDAC6.

Abstract: Compounds according to Formula I and Formula II are potent inhibitors of PSMA. Pharmaceutical compositions may include a complex of a radionuclide and a Formula I compound or a Formula II compound. Methods include using the radionuclide complex of a Formula I compound or a Formula II compound for treating or diagnosis of a disease or a condition associated with PSMA activity.

Abstract: The present invention relates to tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives, a preparation method thereof, and a pharmaceutical composition containing the derivative as an active ingredient for use in the diagnosis or treatment (radiotherapy) of angiogenesis-related diseases. The tricarbonyl technetium-99m or rhenium-188 labeled cyclic RGD derivatives of the present invention has a high subnanomolar affinity to integrin ?v?3 (also called as a vitronectin receptor) that is activated in an angiogenic action induced by a tumor, and acts exclusively upon cancer cells having selectively activated integrin ?v?3 because of a substantially low intake into the liver and intestines.

Abstract: Inhibitors of Bcl-2/Bcl-xL and compositions containing the same are disclosed. Methods of using the Bcl-2/Bcl-xL inhibitors in the treatment of diseases and conditions wherein inhibition of Bcl-2/Bcl-xL provides a benefit, like cancers, also are disclosed.

Abstract: The present invention is directed to novel non-invasive diagnostic tools/compounds comprising a cyclic peptide wherein the compound binds to a MSH receptor to image and treat cancers, especially, melanoma, including metastatic melanoma in vivo. The present invention represents a clear advance in the art which presently relies on tissue biopsy for diagnoses of these cancers. The novel imaging probes are capable of detecting cancerous melanoma cells, as well as their metastatic spread in tissues. This represents a quantum step forward in the diagnosis and treatment of melanoma, including metastatic melanoma using non-invasive molecular imaging techniques. The novel probes of the present invention will also be useful to initiate therapy for melanoma as well as monitor patients response to chemotherapy treatments and other interventions or therapies used in the treatment of melanoma/metastatic melanoma.

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: Compounds which specifically inhibit legumain, also known as asparaginyl endopeptidase are provided. The compounds have an epoxide or N-Michael acceptor warhead, and have an asparagine side chain attached to a nitrogen atom in the backbone adjacent the warhead. The compounds also preferably comprise a proline residue adjacent the asparagine, and the compound may also contain a third residue and/or a label for cellular or in vivo imaging of active legumain.

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: Nanoparticles are used as a contrast agent for magnetic resonance imaging and computed tomography. Each of the nanoparticles includes a metal alloy core and a plurality of hydrophilic molecules covalently bound to the surface of the metal alloy core. Also disclosed is a method for using the contrast agent.

Abstract: Provided are a photosensitizer-metal nanoparticle complex and a composition for photodynamic therapy or diagnosis having the same. The complex includes a photosensitizer, a metal nanoparticle, and a backbone linking the photosensitizer with the metal nanoparticle. The backbone has a polypeptide substrate capable of being specifically degraded by a protease. When the complex is administered to a patient, fluorescence and production of reactive oxygen species from the conjugated photosensitizers are inhibited in normal tissues due to the resonance energy transfer between the photosensitizer and metal nanoparticles, but in tumor tissues, fluorescence and production of reactive oxygen species from the released photosensitizers are activated, thereby effectively destroying the tumor tissues. In addition, the selective fluorescence in the tumor tissues can further improve accuracy of tumor diagnosis using the protease-activatable photosensitizer-metal nanoparticle complex.

Abstract: Glucagon formulations that resist fibril formation are disclosed. The formulations comprise curcumin derivatives such as ferulic acid and/or tetrahydrocurcumin and can further comprise human serum albumin, polysorbate-80, and L-methionine.

Abstract: Compounds of the formulae, (I), wherein each variable is as defined herein are provided which are useful in (i) diagnostic methods for detecting and/or identifying cells presenting PSMA; (2) compositions comprising a compound of the invention together with a pharmaceutically acceptable carrier, excipient, and/or diluent; (3) methods for inhibiting or treating prostrate cancer; and (4) methods for blocking or destabilizing neovasculature of a tumor.

Abstract: This invention relates to a low cost rapid response diagnostic system to determine cortisol levels in patients selected as potential candidates for GCR (glucocorticoid receptor) antagonist therapy utilizing a GCR antagonist, such as ORG 34517. The rapid, sensitive, and inexpensive test can be used to determine patients who have non-normal cortisol production or disordered circadian rhythms as a method for selecting subjects for GCR antagonist therapy for whom it is likely to have beneficial and/or therapeutic effects, and can also be used to monitor changes in cortisol levels in response to treatment.

Abstract: The invention is directed to a method for preventing nasolacrimal duct obstruction (NLDO) in a patient receiving high dose radioactive iodine for treatment of cancer. The method includes administering an effective amount of perchlorate anion to the eyes of the patient.

Abstract: The present invention provides a method useful in the diagnosis and monitoring of cancer wherein there is an abnormal expression of PBR. The method of the invention is particularly useful in evaluating the severity of the cancer, e.g. PBR expression correlates with cell proliferation rates, metastatic potential, tumor aggressiveness, malignancy progression. The method of the invention can therefore be applied in the determination of likely disease progression and in making an associated prognosis. Furthermore, the method of the invention can find use in determining the likely success of certain therapeutic approaches, or in the evaluation of the efficacy of certain proposed new treatments.

Abstract: Injectable and oral formulations of a tetracycline compound are described. In one embodiment, the invention pertains to an oral formulation of a 9-aminomethyl tetracycline compound, or a salt thereof, in tablet form or capsule. The formulations may be used, for example, to treat infections.

Abstract: A medical device is presented for use in tissue characterization and treatment. The device comprises: a tissue characterization probe comprising an elongated carrier carrying an array of tissue characterization sensors arranged in a spaced-apart relationship at least along an axis of said carrier, such that progression of the probe through a tissue mass provides for locating and determining a dimension of an abnormal tissue specimen inside said tissue mass based on characterization signals from the sensors in the array, thereby enabling consequent treatment of the abnormal tissue specimen by a treatment tool.

Abstract: The present invention is directed towards new trifunctional folate-conjugates comprising a folate, an albumin binder and a radionuclide-based therapeutic or diagnostic moiety as well as pharmaceutical compositions thereof, their method of production and their use in diagnostic and therapeutic medical applications, such as diagnostic nuclear imaging and radionuclide therapy.

Abstract: The present invention relates to a compound having formula (I): wherein: —X is in particular 125I Or 211At; —R1 and R?1 are independently from each other chosen preferably from the group consisting of electron-withdrawing groups and alkyl groups; —R2 is chosen from the group consisting of: H, alkyl groups, functional groups being able to bind a vector, and functional groups having targeting properties which make the compound of the invention a vector itself; —Z is a heteroatom, R5, R8 and R9 are preferably H; —Y is preferably an electron withdrawing group.

Abstract: The present invention relates to a method for preparing a radiolabeled macromolecule, the method comprising contacting a macromolecule with a carbon encapsulated nanoparticle composite having a radioactive particulate core in an aqueous medium comprising a pH selected to promote short-range attractive forces between the nanoparticles and the macromolecule by attenuating repulsive electrostatic forces.

Abstract: The present invention is directed to the use of an irreversible ligand of a serine protease selected from the group consisting of leukocyte elastase, thrombin, tissue plasminogen activator (t-PA) and plasmin for the molecular imaging of said serine protease and the diagnosis of pathophysiological conditions associated with said serine protease activity.

Abstract: The present invention is directed ?-particle emitting nanoparticles that comprise a lanthanide phosphate sequestration shell enclosing an ?-emitting-radioisotope-doped lanthanide phosphate core such that the shell allows at least some of the ? emissions from the ?-emitting radioisotope to pass therethrough and prevents at least some radioactive decay products of the ?-emitting radioisotope from exiting the ?-particle emitting nanoparticle. Further, such ?-particle emitting nanoparticles may be coated with gold and functionalized. Additionally, a method for making and using the same are disclosed.

Abstract: This invention is directed to non-benzenoid aromatic compounds. Other aspects include methods of using non-benzenoid aromatic compounds for imaging and phototherapeutic uses thereof. Non-benzenoid compounds provided herein generally have one or more substituent groups which allow tailoring of the spectral properties or provide photoreactivity or targeting ability.

Abstract: An indole-based in vivo imaging agent is provided by the present invention that binds with high affinity to PBR, has good uptake into the brain following administration, and which has good selective binding to PBR. The invention also includes a precursor compound useful in the synthesis of the in vivo imaging agent of the invention, as well as a method for synthesis of said in vivo imaging agent comprising use of said precursor compound, and a kit for carrying out said method. Also provided is a cassette for automated synthesis of the in vivo imaging agent. Further aspects of the invention include a radiopharmaceutical composition comprising the in vivo imaging agent of the invention, and methods for the use of said in vivo imaging agent.

Abstract: Methods are provided for the treatment of diseases and disorders using systematically-introduced nanoparticles to create a focused localized hyperthermia in a target area to enhance the effect of additional treatment therapies such as ionizing radiation. Advantages include an enhancement of the therapeutic effect of other therapies by increasing perfusion or reducing hypoxia in the treatment area, further, the methods herein may also result in the disruption of the vasculature, which provide further impetus for such treatments, singly and in combination with conventional therapies such as chemotherapy and radiation therapy.

Abstract: Various compounds, compositions, and methods for binding to ?-amyloid plaque and norepinephrine transporters are presented. Especially preferred compounds include those with a PET-detectable label.

Abstract: A device for use in an aerosol inhalation system for delivering aerosolized medication includes a housing that is operatively connected to a source of aerosolized medication such that the aerosolized medication is delivered to the housing. The device also includes a patient interface member removably connected to the housing and being separate therefrom. The patient interface member is in the form of a face mask for placement about a face of the patient and in communication with a mouth of the patient for delivering the aerosolized medication. The patient interface member incorporates an integral inhalation valve and safety feature for protecting against displacement of the inhaltation valve.