Alkylphosphocholine analogs incorporating a chelating moiety that is chelated to gadolinium are disclosed herein. The alkylphophocholine analogs are compounds having the formula: ##STR00001##
or a salt therof. R.sub.1 includes a chelating agent that is chelated to a gadolinium atom; a is 0 or 1; n is an integer from 12 to 30; m is 0 or 1; Y is —H, —OH, —COOH, —COOX, —OCOX, or —OX, wherein X is an alkyl or an arylalkyl; R.sub.2 is —N.sup.+H.sub.3, —N.sup.+H.sub.2Z, —N.sup.+HZ.sub.2, or —N.sup.+Z.sub.3, wherein each Z is independently an alkyl or an aroalkyl; and b is 1 or 2. The compounds can be used to detect solid tumors or to treat solid tumors. In detection/imaging applications, the gadolinium emits signals that are detectable using magnetic resonance imaging. In therapeutic treatment, the gadolinium emits tumor-targeting charged particles when exposed to epithermal neutrons.

The present invention provides a compound of Formula (I) as defined herein. The present invention also provides a nanoparticle comprising a plurality of the conjugates of the present invention, and methods of using the nanoparticles for drug delivery, treating a disease, and methods of imaging.

The present invention relates to a drug delivery system with a micelle structure comprising a PEG.sub.2000-DSPE polymerized lipid and an APT.sub.EDB-PEG.sub.2000-DSPE polymer, and a preparation method thereof. The drug delivery system targets extra-domain B of fibronectin (EDB-FN), which is overexpressed in a brain tumor, and can pass through the blood-brain barrier (BBB) or the blood-brain tumor barrier (BBTB) to deliver a drug specifically to the brain tumor cells. In addition, the present invention can provide a pharmaceutical composition for diagnosing or treating a brain tumor, comprising the drug-loaded drug delivery system as an active ingredient. The composition can be accumulated inside the brain tumor and incorporated into the tumor cells to specifically inhibit tumor growth, and thus can be efficiently utilized for diagnosing or treating a brain tumor.

The present invention relates to a drug delivery system with a micelle structure comprising a PEG.sub.2000-DSPE polymerized lipid and an APT.sub.EDB-PEG.sub.2000-DSPE polymer, and a preparation method thereof. The drug delivery system targets extra-domain B of fibronectin (EDB-FN), which is overexpressed in a brain tumor, and can pass through the blood-brain barrier (BBB) or the blood-brain tumor barrier (BBTB) to deliver a drug specifically to the brain tumor cells. In addition, the present invention can provide a pharmaceutical composition for diagnosing or treating a brain tumor, comprising the drug-loaded drug delivery system as an active ingredient. The composition can be accumulated inside the brain tumor and incorporated into the tumor cells to specifically inhibit tumor growth, and thus can be efficiently utilized for diagnosing or treating a brain tumor.

The present disclosure provides peptide constructs for diagnostic imaging and therapeutic applications, using pegylated peptides which exhibit specific binding for a target molecule of interest, such as a biomarker of a disease or disorder.

Described herein is a contrast agent for administration to a subject. The contrast agent includes a targeting portion that includes a hydrazide functional group; a metal ion bound to a metal-complexable portion; and a linker joining the targeting portion and the metal-complexable portion of the contrast agent. The portion that is not bound to a metal ion localizes the contrast agent to necrotic tissue in the subject.

The invention relates to Cathepsin-binding compounds bound to a carrier comprising a diagnostic moiety, for use in the diagnosis of inflammatory diseases, and/or for use in the diagnosis of neoplastic diseases, wherein the Cathepsin-binding compound binds to inflammatory cells of the tumour stroma. The invention also relates to Cathepsin B-targeting compounds and Cathepsin B-binding and liposome-binding compounds.

Provided are macrocyclic compounds and compounds with two or more macrocyclic groups, iron coordinated macrocyclic compounds, and iron coordinated compounds with two or more macrocyclic groups. The iron is high-spin iron(III). The iron coordinated compounds may exhibit a negative redox potential (e.g., relative to a normal hydrogen electrode at a biologically relevant pH, for example, a pH of 6.5-7.5). The compounds can be used as MRI contrast agents.

There are provided methods for diagnosing coronary heart disease in a subject in need thereof comprising administering an admixture comprising CO.sub.2 to a subject to reach a predetermined PaCO.sub.2 in the subject to induce hyperemia, monitoring vascular reactivity in the subject and diagnosing the presence or absence of coronary heart disease in the subject, wherein decreased vascular reactivity in the subject compared to a control subject is indicative of coronary heart disease. There are also provided methods for increasing sensitivity and specificity of BOLD MRI.

There are provided methods for diagnosing coronary heart disease in a subject in need thereof comprising administering an admixture comprising CO.sub.2 to a subject to reach a predetermined PaCO.sub.2 in the subject to induce hyperemia, monitoring vascular reactivity in the subject and diagnosing the presence or absence of coronary heart disease in the subject, wherein decreased vascular reactivity in the subject compared to a control subject is indicative of coronary heart disease. There are also provided methods for increasing sensitivity and specificity of BOLD MRI.