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 are a functionalized, encapsulated fluorescent nanocrystal comprising a liposome having encapsulated therein one or more fluorescent nanocrystals; use of the functionalized, encapsulated fluorescent nanocrystals in detection systems; and a method of producing functionalized, encapsulated fluorescent nanocrystals. A method of using the functionalized encapsulated fluorescent nanocrystals having affinity molecule bound thereto comprises contacting the functionalized encapsulated fluorescent nanocrystals with a sample so that complexes are formed between the functionalized encapsulated fluorescent nanocrystals and substrate for which the affinity molecule has binding specificity, if the substrate is present; exposing the complexes in the detection system to an excitation light source, and detecting a fluorescence peak emitted from the complexes, if present.

Abstract: Peptides and peptide-targeted multimeric contrast agents are described, as well as methods of making and using the contrast agents.

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: 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: Described are new cascade polymer complexes, compositions containing them and use of the complexes in diagnosis and therapy, particularly for magnetic resonance imaging and computer tomography imaging.

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: The invention relates to metal complex compounds, contrast agents for MRI and in vivo NMR markers for NMR spectroscopy comprising said metal complex compounds and methods for in vivo determination of physiological parameters, e.g. enzyme activity or pH using said metal complex compounds.

Abstract: Compounds of general formula (I): in which: R1 is hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl, arylalkyl, or two R1, taken together, form a straight or cyclic C2–C10 alkylene group or an ortho disubstituted arylene; R2 is hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl or aryl alkyl optionally substituted with functional groups which allow conjugation with a suitable molecule able to interact with physiological systems; R3, R4 and R5 are hydrogen, C1–C20 alkyl, C3–C10 cycloalkyl, C4–C20 cycloalkylalkyl, aryl, arylalkyl; and their chelates with bi-trivalent ions of the metal elements having atomic number ranging between 20 and 31, 39, 42, 43, 44, 49, and between 57 and 83, and radioisotopes chosen among 203Pb 67Ga 68Ga 72As 111In 113In 90Y 97Ru 62Cu 64Cu 52Fe 52mMn 140La 175Yb 153Sm 166Ho 149Pm 177Lu 142Pr 159Gd 212Bi 47Sc 149Pm 67Cu, 111Ag, 199Au, 161Tb and 51Cr as well as the salts thereof with physiologically compatible bases or acids

Abstract: In certain embodiments, methods of the present invention obtain dynamic data sets of an NMR spectroscopy signal of polarized 129Xe in a selected structure, environment, or system. The signal data can be used to evaluate: (a) the physiology of a membrane or tissue; (b) the operational condition or function of a body system or portion thereof (when at rest or under stimulation); and/or (c) the efficacy of a therapeutic treatment used to treat a diagnosed disorder, disease, or condition. Thus, the present invention provides methods for screening and/or diagnosing a respiratory, cardiopulmonary disorder or disease such as chronic heart failure, and/or methods for monitoring the efficacy of therapeutics administered to subject to treat the disorder or disease.

Abstract: The present invention relates to a contrast-enhanced diagnostic imaging method for monitoring the efficacy of interventional therapies. The contrast agents useful in this method comprise an image-enhancing moiety (IEM) and a state-dependent tissue binding moiety (SDTBM). These contrast agents exhibit state-dependent binding to one or more components of a targeted tissue or tissue component and provide a detectable change in the signal characteristics of the agent once bound to the targeted tissue. As a result, these agents exhibit a binding affinity for, and thus image contrast of, the targeted tissue which changes as the tissue-state changes during therapy.

Abstract: In part, the present invention is directed to compositions comprising a carrier with a metal binding domain, a metal ion, and an active agent.

Abstract: The invention concerns a ligand comprising wherein n is an integer from 1 to 5, X represents —NO2, —NH2, —NCS, —NHCOCH2-Z. NHCO—W—COCNHS, —NH-Q, —NHCS-Q, —NHCOCH2-Q, or —NHCO(CH2)m ?-Q where Q is an hapten chosen from the group consisting of steroids, enzymes, proteins, monoclonal antibodies, chimeric antibodies, or fragments thereof or any activated linker ready for coupling reaction, Y is CO2H or PO3H2 W is —(CH2)m— m is an integer from 1 to 10.

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 present invention is a technique and apparatus for acquiring anatomic information used in diagnosing and characterizing abdominal aortic aneurismal disease and the like. This technique provides anatomic information, in the form of images, using a combination of a plurality of magnetic resonance angiography sequences, including a spin-echo and four contrast enhanced (e.g., gadolinium) magnetic resonance angiography sequences. The anatomic images may be used in, for example, pre-operative, operative and post-operative evaluation of aortic pathology, including aneurysms, atherosclerosis, and occlusive disease of branch vessels such as the renal arteries. The gadolinium-enhanced magnetic resonance angiography provides sufficient anatomic detail to detect aneurysms and all relevant major branch vessel abnormalities seen at angiography operation.

Abstract: Compounds of formula I wherein Z1, Z2, X, R2 and R3 are as defined herein, are suitable as NMR shift reagents.

Abstract: Provided are a functionalized, encapsulated fluorescent nanocrystal comprising a liposome having encapsulated therein one or more fluorescent nanocrystals; use of the functionalized, encapsulated fluorescent nanocrystals in detection systems; and a method of producing functionalized, encapsulated fluorescent nanocrystals. A method of using the functionalized encapsulated fluorescent nanocrystals having affinity molecule bound thereto comprises contacting the functionalized encapsulated fluorescent nanocrystals with a sample so that complexes are formed between the functionalized encapsulated fluorescent nanocrystals and substrate for which the affinity molecule has binding specificity, if the substrate is present; exposing the complexes in the detection system to an excitation light source, and detecting a fluorescence peak emitted from the complexes, if present.

Abstract: The invention concerns a ligand comprising (I) wherein n is an integer from 1 to 5 Y is CO2H or PO3H2T represents —X or -phenyl-X, wherein X represents NO2, NH2, NCS, NHCOCH2-Z, NHCO—W—COCNHS, —NH-Q, —NHCS-Q, —NHCOCH2-Q, or NHCO(CH2)m-Q where Q is a hapten chosen from the group consisting of steroids, enzymes, proteins, monoclonal antibodies, chimeric antibodies, or fragments thereof or any activated linker ready for coupling reaction, W is —(CH2)m- m is an integer from 1 to 10 Z is chloride, bromide or iodine

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 method of evaluating novel stroke treatments includes generating a risk map indicative of the probability of tissue infarction on voxel-by-voxel basis and selecting a probability range for evaluating the therapeutic effect of the novel treatment. In one particular embodiment, tissue having a fifty percent probability of tissue infarction is selected. A novel treatment that has a reduced level of overall actual infarction as compared to the predicted value is indicative of therapeutic effect.

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: The invention shows a method for obtaining temporally spaced images of tissues, including blood vessels, to reveal blood flow abnormalities within those tissues and vessels.

Abstract: Novel degradable macromolecular magnetic resonance imaging contrast agents for use in various diagnostic procedures, and methods for synthesizing, using and degrading these agents, are disclosed. The macromolecule contrast agents disclosed in various aspects of this invention are degradable gadolinium compounds which show prolonged plasma retention, and enhanced permeability and retention in solid tumors, but are still capable of being rapidly cleared from the body.

Abstract: The invention relates to novel aminocarboxylate ligands that are suitable for complexing with a radionuclide, and are useful as imaging agents for diagnostic purposes. In accordance with the present invention, a method of preparing a compound of formula (I): fac-[M(CO)3(OH2)3]+, wherein M is Mn, 99mTc, 186Re or 188Re, involves reacting a metal in permetallate form with carbon monoxide and a reducing agent, wherein a mixture of a basic borate buffer and a reducing agent soluble in water but not substantially decomposed by water is solved in a water containing solvent system containing a solution of the metal in permanganate, pertechnetate or perrhenate form in the presence of carbon monoxide. The compound of formula (I) can be reacted with a ligand Lx to form a compound of formula (II): fac-[M(CO)3(X)2L1]n, wherein M is as defined above Lx is a multidentate ligand, and n is a charge of the ligand Lx increased with one + charge.

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: The present invention provides a kit and a method for targeting of a diagnostic or therapeutic agent to a target site in a mammal having a pathological condition. The kit comprises, in separate containers, (a) a first conjugate comprising a targeting moiety and a Morpholino oligomer, wherein the targeting moiety selectively binds to a primary, target-specific binding site of the target site or to a substance produced by or associated with the target site; (b) optionally, a clearing agent; and (c) a second conjugate comprising a complementary Morpholino oligomer and a diagnostic agent or therapeutic agent. The method comprises administering (a), optionally (b), and (c) to a mammal.

Abstract: The present invention provides a coating that emits magnetic resonance signals and a method for coating medical devices therewith. The coating includes a paramagnetic metal ion-containing polymer complex that facilitates diagnostic and therapeutic techniques by readily visualizing medical devices coated with the complex. The present invention also provides methods by which pre-existing polymers and medical devices may be made MR-imageable. The invention also provides methods of improving MR-imageability of polymers and medical devices by encapsulating the polymers and medical devices with hydrogels.

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: The present invention relates to a contrast-enhanced diagnostic imaging method for monitoring the efficacy of interventional therapies. The contrast agents useful in this method comprise an image-enhancing moiety (IEM) and a state-dependent tissue binding moiety (SDTBM). These contrast agents exhibit state-dependent binding to one or more components of a targeted tissue or tissue component and provide a detectable change in the signal characteristics of the agent once bound to the targeted tissue. As a result, these agents exhibit a binding affinity for, and thus image contrast of, the targeted tissue which changes as the tissue-state changes during therapy.

Abstract: The present invention provides a composition comprising fluorescent semiconductor nanocrystals associated to a compound, wherein the nanocrystals have a characteristic spectral emission, wherein said spectral emission is tunable to a desired wavelength by controlling the size of the nanocrystal, and wherein said emission provides information about a biological state or event.

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: Small dendrimer-based MRI contrast agents are disclosed to accumulate in renal tubules. The accumulation enables visualization of renal structure and function, permitting assessment of structural and functional damage to the kidneys. In a disclosed embodiment, six, small dendrimer-based MRI contrast agents were synthesized, and their pharmacokinetics, whole body retention, and renal MRI images were evaluated in mice. Surprisingly, despite having unequal renal clearance properties, all of the dendrimer agents clearly visualized the renal anatomy and proximal straight tubules of the mice better than Gd-[DTPA]-dimeglumine. Dendrimer conjugate contrast agents prepared from PAMAM-G2D, DAB-G3D, and DAB-G2D dendrimers were excreted rapidly and may be acceptable for use in clinical applications.

Abstract: The present invention relates to improved chelator conjugates with biological targeting molecules, suitable for forming metal complexes with radiometals. The radiometal complexes, especially with the radiometal99mTc, are useful as radiopharmaceuticals.

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 plaque, lymph nodes, infarcted and necrotic tissue and for independent visualization of necrotic tissue and tumor tissue.

Abstract: MR spectroscopy and imaging methods for imaging pulmonary and cardiac vasculature and the cardiac region and evaluating blood flow or circulatory deficits use dissolved phase polarized 129Xe gas and large flip angle excitation pulses. Pulmonary and cardiac vasculature MRI images are obtained by delivering gas to a patient via inhalation such as with a breath-hold delivery-procedure, exciting the dissolved phase gas with a large flip angle pulse, and generating a corresponding image. Preferably, the image is obtained using multi-echo imaging techniques. Blood flow is quantified using low field MR spectroscopy and an RF excitation pulse with a frequency which corresponds to the resonance of the dissolved phase 129Xe.

Abstract: This invention comprises nanoparticles for use with biosensors. The nanoparticles have core/shell architecture. The nanoparticles can be detected by two means, magnetic and optical by virtue of the nanoparticles magnetic core and fluorescent semiconductor shell. Methods of making the nanoparticles and their composition are described.

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: There is disclosed a method for visualizing a body lumen. The method of the invention uses contrast material that preferably adheres to the interior wall of a target body lumen for a period of time sufficient to permit real-time visualization of the lumen and to enable the performance of image-guided diagnostic and therapeutic procedures. Lumens from the cardio-vascular, pulmonary, digestive, reproductive, excretory and central nervous systems may conveniently be visualized. Radiography, nuclear medicine, ultrasound and MRI visualizing systems may be used. Contrast materials for use in the invention are non-toxic, especially non-toxic to the kidney, do not produce allergic reactions, do not stimulate atherogenesis, and preferably comprise iodine or a metal.

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 present invention relates to improved diagnostic agents for Magnetic Resonance Imaging and optical imaging. In particular, this invention relates to MRI and optical imaging agents that allow for the sensitive detection of a specific bioactivity within a tissue. These agents are prodrug contrast agents which are bioactivated in vivo in the presence of the specific bioactivity. This invention also relates to pharmaceutical compositions comprising these agents and to methods of using the agents and compositions comprising the agents.

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 invention relates to novel magnetic resonance imaging contrast agents and methods of detecting physiological signals or substances.

Abstract: Provided are a functionalized, encapsulated fluorescent nanocrystal comprising a liposome having encapsulated therein one or more fluorescent nanocrystals; use of the functionalized, encapsulated fluorescent nanocrystals in detection systems; and a method of producing functionalized, encapsulated fluorescent nanocrystals. A method of using the functionalized encapsulated fluorescent nanocrystals having affinity molecule bound thereto comprises contacting the functionalized encapsulated fluorescent nanocrystals with a sample so that complexes are formed between the functionalized encapsulated fluorescent nanocrystals and substrate for which the affinity molecule has binding specificity, if the substrate is present; exposing the complexes in the detection system to an excitation light source, and detecting a fluorescence peak emitted from the complexes, if present.

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 (R)>10 l/mmol s as contrast media in MR imaging for visualization of intravascular thrombi.

Abstract: The present invention relates to improved diagnostic agents for Magnetic Resonance Imaging and optical imaging. In particular, this invention relates to MRI and optical imaging agents that allow for the sensitive detection of a specific bloactivity within a tissue. These agents are prodrug contrast agents which are bioactivated in vivo in the presence of the specific bioactivity. This invention also relates to pharmaceutical compositions comprising these agents and to methods of using the agents and compositions comprising the agents.

Abstract: An annexin, annexin analogue or phosphatidylserine binding compound (PSC) labeled with an MR, CT, or optical contrast agent. The conjugate is administered into a subject and specifically binds to the surface of apoptotic and necrotic cells. The subject is imaged using conventional MRI, CT and optical imaging techniques and dead and dying tissue is identified. The identification and development of analogues specific for phosphatidylserine for purposes of non-invasive imaging of dead or dying cells.

Abstract: This invention describes a novel strategy to produce phosphine-functionalized biomolecules (e.g. peptides or proteins) for potential use in the design and development of site-specific radiopharmaceuticals for diagnosis or therapy of specific cancers. Hydrophilic alkyl phosphines, in general, tend to be oxidatively unstable. Therefore, incorporation of such phosphine functionalities on peptide (and other biomolecule) backbones, without oxidizing the PIII centers, is difficult. In this context this discovery reports on a new technology by which phosphines, in the form of bifunctional chelating agents, can be directly incorporated on biomolecular backbones using manual synthetic or solid phase peptide synthesis methodologies. The superior ligating abilities of phosphine ligands, with various diagnostically (e.g. TC-99m) or therapeutically (e.g.

Abstract: A semiconductor nanocrystal compound is described capable of linking to an affinity molecule. The compound comprises (1) a semiconductor nanocrystal capable of emitting electromagnetic radiation and/or absorbing energy, and/or scattering or diffracting electromagnetic radiation—when excited by an electromagnetic radiation source or a particle beam; and (2) at least one linking agent, having a first portion linked to the semiconductor nanocrystal and a second portion capable of linking to an affinity molecule. The compound is linked to an affinity molecule to form a semiconductor nanocrystal probe capable of bonding with a detectable substance. Subsequent exposure to excitation energy will excite the semiconductor nanocrystal in the probe, causing the emission of electromagnetic radiation.

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.