Abstract: The invention relates to the use of perfluoroalkyl-containing metal complexes that have a critical micelle formation concentration <10?3 mol/l, a hydrodynamic micelle diameter (2 Rh)>1 nm and a proton relaxivity in plasma (R1)>10 l/mmol·s as contrast media in MR imaging for visualization of intravascular thrombi.

Abstract: A new use in magnetic resonance imaging employing a field greater than 1.5 Tesla, of a porphyrin compound of the following general formula I is provided: in which R0 and R?0 are such that the compound is soluble in a biological medium, and M denotes a paramagnetic metal ion, advantageously Mn3+. The present invention also relates to novel porphyrin compounds.

Abstract: Cyclen-based chelates can be used as contrast agents for multi-modal imaging of tissue cells. The cyclen-based chelates are preferably polyazamacrocyclic molecules formed from 1,4,7,10 tetraazacyclododecane (“cyclen”) having varying chelating ions, phosphoester chains, and light harvesting moieties. By changing the chelating ion, phosphoester chain length and/or the light harvesting moiety different imaging techniques, such as MRI, CT, fluorescence and absorption, x-ray and NIR, may be employed to image the tissue cells. Additionally, the cyclen-based chelates may be conjugated to provide for site-specific delivery of the cyclen-based chelate to the desired tissue cells. The cyclen-based chelates may also be delivered to the tissue cells by attaching the cyclen-based chelates to a polymeric delivery vehicle. Although these cyclen-based chelates have a wide variety of application, the preferred use is for imaging of cancer cells, such as brain cancer, for improving resection of a cancerous tissue.

Abstract: Method for selective targeting of one or more effector moiety such as diagnostic or a therapeutic agent to a cell or population of cells expressing a folate-receptor comprising simultaneous or sequential administration of an antifolate with a folate- or pteroate-conjugate comprising said one or more effector moiety.

Abstract: Compounds useful for associating with nanoparticle or microparticle emulsions to obtain magnetic resonance images permit control of the relaxivity of the signal and readily associate with the particulate components.

Abstract: Provided herein are image-enhancing agents that are useful for managing disease by imaging disease tissue using magnetic resonance imaging techniques, optical imaging techniques, and a combination of magnetic resonance imaging techniques and optical imaging techniques. Also provided are methods of imaging disease tissue and managing disease using the image-enhancing agents.

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: The invention relates to new, monomeric, perfluoroalkyl-substituted metal complexes, processes for their production, and their use in diagnosis and therapy. The compounds according to the invention are suitable especially as in vivo contrast media in nuclear spin tomography (MRT). They can preferably be used as blood-pool agents and as lymphographic agents.

Abstract: A detectably labeled porphyrin compound for identifying a sentinel lymph node in patients, particularly those with cancer. A method of identifying a sentinel lymph node, comprising the steps of: injecting the detectably labeled porphyrin compound into a tumor, wherein the porphyrin compound is detectably labeled with a radiolabel which is a ?-emitting radioactive metal; and detecting radioactive emission or a color so as to detect and thereby identify the sentinel lymph node. A method of identifying a sentinel lymph node, comprising the steps of injecting the detectably labeled porphyrin compound into tissue surrounding a tumor, wherein the porphyrin compound is detectably labeled with a non-radioactive metal; and taking a series of magnetic resonance images to identify the sentinel lymph node by viewing the images showing the injected detectably labeled porphyrin compound.

Abstract: The use of contrast agents of molecular weight lower than 5000 Dalton and including at least one residue of a biliary acid for the preparation of diagnostic contrast compositions for the microvascular permeability assessment is disclosed.

Abstract: The invention relates to hydroxypyridinone derivatives, their metal complexes, their preparation and their use for preparing conjugates with biomolecules. The conjugates are suitable as contrast agents in NMR diagnosis. A high relaxivity is achieved and the NMRD maximum is raised through a specific design of the ligands.

Abstract: The invention relates to conjugates of hydroxypyridinone derivative metal complexes and to their preparation. The conjugates are suitable as contrast agents in NMR diagnosis. A high relaxivity is achieved and the NMRD maximum is raised through a specific design of the ligands.

Abstract: A compound comprising a chemical combination of a photodynamic tetra-pyrrolic compound with a plurality of radionuclide element atoms such that the compound may be used to enhance MR imaging and also be used as a photodynamic compound for use in photodynamic therapy to treat hyperproliferative tissue. The preferred compounds have the structural formula: where R1, R2, R2a R3, R3a R4, R5, R5a R6, R7, R7a, and R8 cumulatively contain at least two functional groups that will complex or combine with an MR imaging enhancing element or ion. The compound is intended to include such complexes and combinations and includes the use of such compounds for MR imaging and photodynamic therapy treatment of tumors and other hyperproliferative tissue.

Abstract: The present invention relates to magnetic resonance imaging (MRI) contrast agent. In particular, the present invention provides MRI contrast agents that are sensitive to the enzyme beta-glucoronidase. The MRI contrast agents provide compositions and methods for non-invasive diagnostic imaging of tissues, including necrotic tumors.

Abstract: The invention relates to a novel class of magnetic resonance imaging agents that can cross the blood brain barrier and provide accurate magnetic resonance imaging of the brain, especially magnetic resonance images of amyloid deposits associated with Alzheimer's disease.

Abstract: A contrast agent for magnetic resonance imaging comprising a complex of a paramagnetic cation, preferably Gd+3, Dy+3, and Fe+3 with three equivalents of a charge neutralizing chelator that provides a lipid soluble complex of the paramagnetic cation is described. The complex is retained intracellularly when introduced into a mammalian cell. A method of providing an image of an internal pathology of a patient by magnetic resonance imaging (MRI) by administering the MRI contrast agent or tagged cells to the patient and scanning the patient using magnetic resonance imaging to obtain visible images of the internal pathology of the patient is also set forth.

Abstract: Modifications of the peptide pyrrhocoricin permit the production of a variety of anti-bacterial or anti-fungal peptides having general formula R1-Asp-Lys-Gly-X-Y-Leu-Pro-Arg-Pro-Thr-Pro-Pro-Arg-Pro-Ile-Tyr-X?-Y?-R2 SEQ ID NO: 1 or multimeric compositions containing more than a single peptide of that formula. These peptides may be straight chain or cyclic peptides, and may contain one or more non-cleavable bonds. These peptides are characterized by anti-bacterial or anti-fungal activity and metabolic stability in mammalian serum. These peptides are useful in anti-bacterial or anti-fungal pharmaceutical compositions and for further drug development or identification of other antibiotic or anti-fungal compounds.

Abstract: The present invention provides a triaminetetraacetatesaccharide coordinating to metal ion to form bioactive metal complexes. The bioactive metal complexes of the present invention can be used as contrast agents for magnetic resonance imaging (MRI).

Abstract: Compounds of general formula (I): in which: R1 through R5 are as defined in the specification FG, which can be the same or different, are carboxy, —PO3H2 or —RP(O)OH groups, wherein R is hydrogen, or an optionally substituted group selected from C1-C20 alkyl, C3-C10 cycloalkyl, C4-C20 cycloalkylalkyl, aryl, arylalkyl, a group bearing an acidic moiety, and a group bearing an amino moiety, each of which may be further optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; 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, 51Cr, 167Tm, 141Ce, 168Yb, 88Y, 165Dy, 166Dy, 97Ru, 103Ru, 186Re, 188Re, 99mTc, 211Bi, 212Bi,

Abstract: The present invention relates to a novel compound comprising a detectable moiety covalently linked to a structural moiety. Upon cleavage of the covalent bond linking the two moieties, the detectable moiety becomes capable of complexing a lanthanide ion, and the lanthanide-detectable moiety complex provides a detectable signal. The structural moiety of the compound is a homo- or hetero-multimer of amino acids, nucleotides, or saccharides. A library comprising at least two member compounds with different structural moieties is also provided in this application.

Abstract: The invention relates to new, monomeric, perfluoroalkyl-substituted metal complexes, processes for their production, and their use in diagnosis and therapy. The compounds according to the invention are suitable especially as in vivo contrast media in nuclear spin tomography (MRT). They can preferably be used as blood-pool agents and as lymphographic agents.

Abstract: The present invention relates to novel imaging probes and methods for using the probes in diagnostic imaging processes and other imaging processes to determine physiological functions.

Abstract: An analytical method and apparatus using principal component analysis of nuclear magnetic resonance (NMR) data for rapid molecular structure/function pattern recognition. The presence of a molecular substructure in an organic compound is determined by comparing principal components calculated from chemical shift values of the substructure in selected compounds with those calculated from the chemical shift values of the organic compound. Alternatively, principal components are calculated from the intensities of NMR signals for a full spectrum, or selected regions thereof, to determine whether an organic compound belongs to or is excluded from a set of structurally related compounds. Also, the presence of a pharmacophore in an organic compound can be determined by comparing the principal components derived from data on a set of compounds known to bind to a particular receptor, or have a common biological effect, with the principal components of the data set of the organic compound.

Abstract: The present invention is generally directed to luminescent lanthanide compounds with phosphine oxide, phosphine oxide-sulfide, pyridine N-oxide, and phosphine oxide-pyridine N-oxide ligands. It also relates to electronic devices in which the active layer includes a lanthanide complex.

Abstract: The present invention is generally directed to luminescent lanthanide compounds with phosphine oxide, phosphine oxide-sulfide, pyridine N-oxide, and phosphine oxide-pyridine N-oxide ligands. It also relates to electronic devices in which the active layer includes a lanthanide complex.

Abstract: The present invention is generally directed to luminescent lanthanide compounds with phosphine oxide, phosphine oxide-sulfide, pyridine N-oxide, and phosphine oxide-pyridine N-oxide ligands. It also relates to electronic devices in which the active layer includes a lanthanide complex.

Abstract: The present invention is directed, in general, to contrast agents (CA), and methods and systems of using such agents for producing image contrast based on a magnetization transfer (MT) mechanism. The CA comprises a tetraazacyclododecane ligand having pendent arms R, R?, R? and R?? that are amides having a general formula: —CR1H—CO—NH—CH2—R2. R1 includes organic substituents and R2 is not hydrogen. A paramagnetic metal ion (M) is coordinated to the ligand. The method, comprises subjecting a CA, in a sample, to a radio frequency pulse. The CA has pendent arms R, R?, R? and R?? comprising organic substituents and the ligand further includes a M and a water molecule. A signal is obtained by applying a radio frequency pulse at a resonance frequency of the water molecule. The magnetic resonance system, comprises a magnetic resonance apparatus and the CA, the agent containing a ligand having the above described general formula.

Abstract: Tripodal polyaminophosphonate chelants are disclosed, as well as chelates of the chelants with metal ions to form radiopharmaceutical and radioactive, MRI and X-ray or CT imaging compounds and compositions. Therapeutic and imaging methods of use are also disclosed.

Abstract: The invention relates to cerium compounds having general formulas (I) Rni+Yin− and (II) Rb+Yb+ and their application as medicaments in the prophylaxis and/or treatment of cancer diseases.

Abstract: Described is a method of using gadolinium-containing compounds as agents for neutron capture therapy to treat neoplastic cell growth. The subject is exposed to a gadolinium-containing compound for a time sufficient to allow the compound to accumulate in neoplastic cells. The subject is then exposed to a thermal and/or epithermal neutron flux, thereby initiating a neutron capture reaction in the gadolinium atoms that results in specific death of neoplastic cells.

Abstract: The present invention relates to the use of thioredoxin as, inter alia, a cell growth stimulator, as well as a screen for agents that are useful in reducing or preventing thioredoxin-associated apoptosis inhibition and agents that are useful in inhibiting thioredoxin stimulated cell growth.

Abstract: The present invention features biarsenical molecules. Target sequences that specifically react with the biarsenical molecules are also included. The present invention also features kits that include biarsenical molecules and target sequences. Tetraarsenical molecules are also featured in the invention.

Abstract: Thus the present invention describes diagnostic agents comprising a diagnostic metal and a compound, wherein the compound comprises: 1-10 targeting moieties;a chelator; and 0-1 linking groups between the targeting moiety and chelator; wherein the targeting moiety is a matrix metalloproteinase inhibitor; and wherein the chelator is capable of conjugating to the diagnostic metal. The present invention also provides novel compositions of the compounds of the invention, kits, and their uses in diagnosis of diseases associated with MMPs.

Abstract: The present invention relates to contrast agents for diagnostic imaging. In particular, this invention relates to novel multimeric compounds which exhibit improved relaxivity properties upon binding to endogenous proteins or other physiologically relevant sites. The compounds consist of: a) two or more Image Enhancing Moieties (IEMs) (or signal-generating moiety) comprising multiple subunits; b) two or more Target Binding Moieties (TBMs), providing for in vivo localization and multimer rigidification; and c) a scaffold framework for attachment of the above moieties. d) optional linkers for attachment of the IEMs to scaffold. This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for contrast enhancement of diagnostic imaging.

Abstract: N-substituted 3-hydroxy-4-pyridinones and metal chelates, methods of preparing N-substituted 3-hydroxy-4-pyridinones and metal chelates, and pharmaceutical compositions containing new N-substituted 3-hydroxy-4-pyridinones and/or their metal chelates. Use of N-substituted 3-hydroxy-4-pyridinones and their metal chelates as pharmaceutical agents for the treatment of diseases, such as parasitic and viral infections, conditions associated with inflammation and infection, and conditions mediated by cell-proliferation or collagen formation.

Abstract: Macrocyclic chelant are disclosed, as well as chelates of the chelants with metal ions to form radiopharmaceutical and radioactive, MRI and X-ray or CT imaging compounds and compositions. Therapeutic and imaging methods of use are also disclosed.

Abstract: The present invention relates to contrast agents for diagnostic imaging with prolonged blood retention. In particular, this invention relates to novel compounds that are characterized by an image enhancing moiety (IEM); a protein plasma binding moiety (PPBM); and a blood half-life extending moiety (BHEM). This invention also relates to pharmaceutical compositions comprising these compounds and to methods of using the compounds and compositions for blood half-life extension and contrast enhancement of diagnostic imaging.

Abstract: Cascade polmer complexes with at least 16 ions of an element of atomic numbers 20 to 29, 39, 42, 44 or 57-83, useful NMR or x-ray lymphography imaging.

Abstract: Pharmaceuticals and Apparatus used in combination for diagnosis and tissue necrosis applicable to provide effective and selective therapy using the Mossbauer absorption phenomenon. Selected pharmaceutical compounds containing a radiation absorber isotope are administered to a tissue and excited by a radiation source which provides energy at the corresponding resonant Mossbauer absorption frequency of isotope containing pharmaceutical, where excitation effects nuclear transitions to cause highly selective energy absorption in the selected target tissue. For diagnostic purposes, de-excitation fluorescence of the isotope is monitored. For therapeutic purposes, the energy is converted to particle radiation by the isotope at the target tissue by internal conversion followed by an Auger electron cascade which results in radiolysis of DNA resulting in lethal double strand breaks in the DNA molecules of the target tissue.

Abstract: The present invention relates to bioconjugates and the delivery of bioactive agents which are preferably targeted for site-specific release in cells, tissues or organs. More particularly, this invention relates to bioconjugates which comprise of bioactive agent and an organocobalt complex. The bioactive agent is covalently bonded directly or indirectly to the cobalt atom of the organocobalt complex. The bioactive agent is released from the bioconjugate by the cleavage of the covalent bond between the bioactive agent and the cobalt atom in the organocobalt complex. The cleavage may occur as a result of normal displacement by cellular nucleophiles or enzymatic action, but is preferably caused to occur selectively at a predetermined release site by application of an external signal. The external signal may be light or photoexcitation, i.e. photolysis, or it may be ultrasound, i.e. sonolysis.

Abstract: Cascade polymers, containing complex-forming ligands, optionally at least five ions of an element of atomic numbers 21-29, 39, 42, 44 or 57-83, as well as, if desired, cations of inorganic and/or organic bases, amino acids or amino acid amides, are valuable complexing compounds and complexes for diagnostics and therapy.

Abstract: A compound of formula (I): wherein, R1 is independently selected from methyl and ethyl and R2 is independently selected from hydrogen, alkyl, and substituted alkyl. The compound is capable of functioning as a ligand and complexing with paramagnetic Fe(III) ion for use as a second-sphere contrast enhancing agent for magnetic resonance imaging of tissue. The present invention also relates to a method of administering the second sphere contrast agent.

Abstract: The invention provides a composition of matter of the formula (I): V—L—R where V is an organic group having binding affinity for an angiotensin II receptor site, L is a linker moiety or a bond, and R is a moiety detectable in in vivo imaging of a human or animal body, with the provisos that where V is angiotensin or a peptidic angiotensin derivative or analog then V—L—R is other than a non-metal radionuclide substituted peptide (e.g. 125I substituted angiotensin II) and L—V is other than simply a peptide with a chelating agent amide bonded to a side chain thereof. This composition of matter may be used to image cardiovascular diseases and disorders.

Abstract: Cascade polymer complexes with at least 16 ions of an element of atomic numbers 20 to 29, 39, 42, 44 or 57-83, useful NMR or x-ray lymphography imaging.