The present invention provides certain compounds, Formula (I), or salts or solvates thereof, which can be used as matrix metalloproteinase-targeted inhibitors or imaging agents.

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The invention provides a novel trifunctional targeting construct and related compositions and methods that are useful in therapeutic, diagnostic (including imaging) of various biological and/or pathological conditions and diseases such as cancers and diabetes. The trifunctional targeting construct of the invention provides enhanced clearing step and reduced non-specific background via complete clearance of undesired antibody conjugates.

Compounds comprising R-G-Cysteic Acid (i.e., R-G-NHCH(CH.sub.2SO.sub.3H)COOH or Arg-Gly-NHCH(CH.sub.2SO.sub.3H)COOH) and derivatives thereof, including pharmaceutically acceptable salts, hydrates, stereoisomers, multimers, cyclic forms, linear forms, drug-conjugates, pro-drugs and their derivatives. Also disclosed are methods for making and using such compounds including methods for inhibiting cellular adhesion to RGD binding sites or delivering other diagnostic or therapeutic agents to RGD binding sites in human or animal subjects.

The present invention provides a radioactive labeling method for neuropeptide Y (NPY) compound and a mammalian diagnostic radioactive targeting medicine with NPY peptide being modified at position 27.sup.th to 36.sup.th, and after binding with the chelating agent and labeling the radiation nucleus .sup.66Ga, .sup.67Ga, .sup.68Ga, .sup.177Lu or .sup.111In to provide a radioactive targeting medicine for multi-type breast cancer diagnosis and treatment.

Compositions and methods are disclosed for assessing macrophage involvement in the inflammation of one or more joints of a subject. In certain aspects, the disclosed method includes the steps of administering to the subject a composition comprising a mannosylated dextran construct with an imaging moiety conjugated thereto; acquiring one or more planar images of a first joint of the subject; defining a region of interest (ROI) comprising the first joint; defining a joint specific reference region (RR); determining a MARTAD value of the joint by assessing the ratio of average pixel intensity of the ROI to the average pixel intensity of the RR; and comparing the MARTAD of the first joint to a normal MARTAD value for a corresponding joint, and wherein macrophage involvement is indicated by a joint specific MARTAD value that exceeds the normal MARTAD value by a predetermined threshold.

The present invention provides hydrophilic bilirubin derivative particles containing a metal, a use thereof, and a preparation method therefor. The bilirubin derivative particles of the present invention form coordinate bonds with various metals, and thus can be used in MR diagnosis, CT diagnosis, photo-acoustic diagnosis, PET diagnosis, or optical diagnosis. The bilirubin derivative particles of the present invention can release an anticancer drug encapsulated therein to the outside by the combination with a platinum-based anticancer drug and the degradation by a stimulation of light/reactive oxygen species, and exhibit anti-inflammatory and anticancer activities, and thus the bilirubin derivative particles of the present invention have a concept of theranostics in which the bilirubin derivative particles can be for therapeutic uses as well as diagnostic uses.

The present invention provides a method for the purification of .sup.227Th from a mixture comprising .sup.227Th and .sup.223Ra, said method comprising: i) preparing a first solution comprising a mixture of .sup.227Th and .sup.223Ra ions dissolved in an aqueous solution of first mineral acid; ii) loading said first solution onto a strong base anion exchange resin; iii) eluting .sup.223Ra from said strong base anion exchange resin using a second mineral acid in an aqueous solution; iv) optionally rinsing said strong base anion exchange resin using a first aqueous medium; v) eluting .sup.227Th from said strong base anion exchange resin using a third mineral acid in an aqueous solution whereby to generate a second solution comprising .sup.227Th. The invention further provides a purified .sup.227Th solution, a corresponding pharmaceutical formulation and methods of treatment of neoplastic disease.

Various embodiments of the present invention are directed to polyrotaxanes comprising a poloxamer core and at least one cyclodextrin and methods for treating Niemann-Pick type C (NPC) and imaging (e.g., MRI) using the polyrotaxanes various embodiments of the present invention.

Salicylic acid-based polymeric CEST contrast agents targeting prostate-specific membrane antigen, pharmaceutical composition comprising the same and methods of use thereof are disclosed.

The present invention provides multi-armed high MW polymers containing hydrophilic groups and one or more functional agents, and methods of preparing such polymers.