Abstract: The invention relates to a method of preparing facial metal tricarbonyl compounds and further coordinated facial metal tricarbonyl compounds in water or an aqueous medium. The invention further relates to the use of said facial metal tricarbonyl compounds in the labelling of biologically active substrates and other ligands, and to a kit for preparing a facial metal tricarbonyl compound or further coordinated facial metal tricarbonyl compounds.

Abstract: This invention relates to novel highly functionalized phosphine ligands as ancillary ligands in radiopharmaceuticals. Also, this invention provides radiopharmaceuticals comprised of highly functionalized phosphine ligated 99mTc labeled HYNIC-conjugated biomolecules that selectively localize at sites of disease and thus allow an image to be obtained of the loci using gamma scintigraphy. The invention also provides methods of use of the radiopharmaceuticals as imaging agents for the diagnosis of cardiovascular disorders such as thromboembolic disease or atherosclerosis, infectious disease and cancer.

Abstract: Provided is a method of fluorescence imaging of living tissue using functionalized nanocrystals. The method comprises contacting an effective amount of functionalized nanocrystals with the living tissue; exposing the tissue to a spectrum of light suitable for exciting functionalized nanocrystals, present in fluorescently labeled tissue, to emit a emission spectrum comprising a fluorescence peak; and detecting any fluorescence peak emitted by the tissue exposed to the excitation spectrum of light, and obtaining a fluorescence image of the tissue. Also provided is a composition comprising a functionalized nanocrystal which is bound to a substrate in a living tissue.

Abstract: Provided are methods for purifying functionalized fluorescent nanocrystals having affinity ligand operably bound thereto by using a solid support matrix in a reactor through which solutions are circulated, and by using an immobilized solid phase formed by operably binding functionalized fluorescent nanocrystals to the solid support matrix. Also provided are purified functionalized fluorescent nanocrystals having affinity ligand operably bound thereto which are purified using the methods according to the present invention to be substantially free of free affinity ligand.

Abstract: Novel gas filled microspheres useful as magnetic resonance imaging (MRI) contrast agents are provided.

Abstract: Provided are a fluorescent microsphere comprised of a plurality of fluorescent nanocrystals operably bound to a polymeric microsphere, and a method of producing the fluorescent microspheres which comprises contacting the polymeric microsphere with a plurality of fluorescent nanocrystals under suitable conditions in which the fluorescent naocrystals become operably bound to the polymeric microsphere. Also provided is a method of using the fluorescent microspheres capable of determining the presence or absence of a predetermined number of analytes in a sample by contacting the sample with the fluorescent microspheres, and detecting the fluorescence signal pattern of excited fluorescent microspheres bound to one or more analytes of the predetermined number of analytes, if present in the sample.

Abstract: Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble polymer such as poly-glutamic acid, poly-aspartic acid or poly-lysine. Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis. Other embodiments include the coating of implantable stents for prevention of restenosis.

Abstract: A method for the assessment of pulmonary ventilation and lung perfusion through Magnetic Resonance Imaging (MRI), comprising the steps of:

Abstract: Linear extended polymeric paramagnetic chelates for use as MRI contrast agents are synthesized by conjugating DTPA chelator moieties to higher than 90% of the monomer residues of the polyamino acid backbone chain. The resulting polymer can be labeled with Gd, since each chelator moiety holds a Gd ion, and the resulting conformation is of an unfolded, extended linear type, capable of entering small pores and moving around obstacles in the extracellular space of tissues. The efficient production of these extended polymers is critical for the application of such contrast agents to medical imaging. One such agent is a reptating polymer containing technetium-99.

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: Chelate compounds of general formula I wherein X is a hydrogen atom and/or a metal ion equivalent of an element of atomic numbers 21-29, 31, 32, 37-40, 42-44, 49 or 57-83, and Z1, Z2, R1, R2, R3 and R4 are as defined herein, as well as their salts with inorganic and/or organic bases, amino acids or amino acid amides, are valuable pharmaceutical agents, e.g., for NMR imaging.

Abstract: Superparamagnetic particles consist of superparamagnetic one-domain particles and aggregates of superparamagnetic one-domain particles to whose surfaces are bound inorganic and optionally organic substances optionally having further binding sites for coupling to tissue-specific binding substances, diagnostic or pharmacologically active substances. The superparamagnetic particles consist of a mixture of small superparamagnetic one-domain particles with a particle size from 3 to 50 nm and stable, degradable aggregates of small superparamagnetic one-domain particles with a particle size from 10 to 1000 nm. They are made of iron hydroxyide, iron oxide hydrate, iron oxides, iron mixed oxides or iron to the surface of which are bound silicate group containing substances among the orthosilicic acids and their condensation products and phosphate-group containing substances among the ortho- or metaphosphoric acids and their condensation products. These substances may have further binding sites.

Abstract: Disclosed are water soluble compositions of paclitaxel and docetaxel formed by conjugating the paclitaxel or docetaxel to a water soluble chelator, polyethylene glycol or polymer such as poly (1-glutamic acid) or poly (1-aspartic acid). Also disclosed are methods of using the compositions for treatment of tumors, auto-immune disorders such as rheumatoid arthritis and for prediction of paclitaxel uptake by tumors and radiolabeled DTPA-paclitaxel tumor imaging. Other embodiments include the coating of implantable stents for prevention of restenosis.

Abstract: The present invention relates generally to methods and compositions for targeting the vasculature of solid tumors using immunological- and growth factor-based reagents. In particular aspects, antibodies carrying diagnostic or therapeutic agents are targeted to the vasculature of solid tumor masses through recognition of tumor vasculature-associated antigens, such as, for example, through endoglin binding, or through the specific induction of endothelial cell surface antigens on vascular endothelial cells in solid tumors.

Abstract: Cascade polymer complexes containing a) complexing ligands of general formula I A—{X—[Y—(Z—( W—Kw)z)y]x}a  (I)  in which A stands for a nitrogen-containing cascade nucleus of base multiplicity a, X and Y, independently of one another, stand for a direct bond or a cascade reproduction unit of reproduction multiplicity x or y, Z and W, independently of one another, stand for a cascade reproduction unit of reproduction multiplicity z or w, K stands for the radical of a complexing agent, a stands for numbers 2 to 12, x, y, z and w, independently of one another, stand for numbers 1 to 4, provided that at least two reproduction units are different and that 16≦a·x·y·z·w≦64 holds true for the product of the multiplicities, b) at least 16 ions of an element of atomic numbers 20 to 29, 39, 42, 44 or 57-83 and c) optionally cations of inorganic and/or organic bases, amino acids or amino acid amides are valuab

Abstract: In a method for characterizing the angiogenesis status of a tumor in a living subject, timed magnetic resonance images of the subject into whom a reptating polymer contrast agent containing chelating diethylentriaminepentacetic acid dosed with gadolinum has been introduced are obtained. At least two images taken at different times are compared in order to determine the percentage image enhancement in a tumor region of interest.

Abstract: A delivery vehicle is described that is capable of being specifically bound to and taken into targeted cells, delivering numerous paramagnetic ions for magnetic resonance imaging (MRI) of the cells. The delivery vehicle comprises a polymeric molecule having a net positive charge complexed with another polymeric molecule having a net negative charge. Cell targeting moieties and MRI contrast agents are attached to one or both of the polymeric molecules. In one embodiment, the polymeric molecule having a net negative charge is a nucleic acid. Thus, the delivery vehicles can be used in clinical protocols in which nucleic acids for gene therapy and agents for MRI contrast are co-transported to specific cells allowing medical imaging monitoring of nucleic acid delivery.

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: The present invention concerns injectable blood pool contrast agents for NMR and X-ray imaging purpose. These blood pool agents carry imaging contrast enhancers, e.g. paramagnetic or, respectively, radio-opaque compounds for imaging the circulation and/or circulation targeted organs. The blood pool agent compositions are formulated to protect the contrast agents from early removal by the reticulo-endothelial (RES) system of the liver and the spleen, so that they stay in the circulation long enough to provide good images of the blood vessels and blood perfused organs. X-ray and NMR imaging of the circulation and of targeted organs can strongly assist in diagnosing possible ailments in human and animal patients.

Abstract: A magnetically controllable, or guided, carrier composition and methods of use and production are disclosed, the composition for carrying biologically active substances to a treatment zone in a body under control of a magnetic field. The composition comprises composite, volume-compounded paclitaxel-adsorbed particles of 0.2 to 5.0 &mgr;m in size, and preferably between 0.5 and 5.0 &mgr;m, containing 1.0 to 95.0% by mass of carbon, and preferably from about 20% to about 60%. The particles are produced by mechanical milling of a mixture of iron and carbon powders. The obtained particles are placed in a solution of a biologically active substance to adsorb the substance onto the particles. The composition is generally administered in suspension. Magnetic carrier particles having therapeutic quantities of adsorbed paclitaxel, doxorubicin, Tc99, and antisense-C Myc oligonucleotide, an hematoporphyrin derivative, 6-mercaptopurine, Amphotericin B, and Camptothecin have been produced using this invention.

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: 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: 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.