The present disclosure relates platinum(IV) and texaphyrin linked conjugates and compositions comprising a texaphyrin and a platinum(IV) agent. The present disclosure also provides pharmaceutical compositions of the conjugates and compositions. Also, provided herein are methods of using the instant compounds in the treatment of cancer such as a platinum resistant cancer.

The present disclosure relates platinum(IV) and texaphyrin linked conjugates and compositions comprising a texaphyrin and a platinum(IV) agent. The present disclosure also provides pharmaceutical compositions of the conjugates and compositions. Also, provided herein are methods of using the instant compounds in the treatment of cancer such as a platinum resistant cancer.

The present invention relates to a compound of formula (I), a pharmaceutical composition comprising or consisting of said compound, a kit comprising or consisting of said compound or pharmaceutical composition and use of the compound or pharmaceutical composition in the diagnosis or treatment of a disease characterized by overexpression of fibroblast activation protein (FAP).

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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.

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.

A method for preparing an NMR material, comprising generating parahydrogen in gas or liquid form at a first location; transporting the parahydrogen away from the first location; mixing a precursor compound including a metabolite component with a catalyst for hydrogenation; hydrogenating the precursor compound using the parahydrogen; transferring polarization in the precursor compound to a nuclear spin of the metabolite component; cleaving a side arm of the precursor compound in a chemical reaction, with the metabolite molecule being one of the products of the reaction; separating the metabolite molecule from the catalyst for hydrogenation and other products of the reaction; and generating metabolite molecules for use in an MRI scanner by extracting a sample of the metabolite molecule having at least 5% polarization.

A method for preparing an NMR material, comprising generating parahydrogen in gas or liquid form at a first location; transporting the parahydrogen away from the first location; mixing a precursor compound including a metabolite component with a catalyst for hydrogenation; hydrogenating the precursor compound using the parahydrogen; transferring polarization in the precursor compound to a nuclear spin of the metabolite component; cleaving a side arm of the precursor compound in a chemical reaction, with the metabolite molecule being one of the products of the reaction; separating the metabolite molecule from the catalyst for hydrogenation and other products of the reaction; and generating metabolite molecules for use in an MRI scanner by extracting a sample of the metabolite molecule having at least 5% polarization.

The disclosure provides multifunctional compounds for use in medical imaging and therapy, the compounds comprising two or more of (i) a chelating ligand moiety (CL); (ii) an optical probe moiety (OP); and (iii) a biological targeting moiety (BT). The disclosure further provides related compositions and methods.

The disclosure provides multifunctional compounds for use in medical imaging and therapy, the compounds comprising two or more of (i) a chelating ligand moiety (CL); (ii) an optical probe moiety (OP); and (iii) a biological targeting moiety (BT). The disclosure further provides related compositions and methods.

A conjugate for treating an individual suffering from a disease, wherein the conjugate is comprised of: a targeting peptide comprising a sequence substantially identical to CAR, or a variant thereof; and at least one therapeutic molecule and methods for making and administering same. Also disclosed is a combination product for use in the treatment of a disease, wherein the combination product comprises: (a) a targeting peptide comprising a sequence substantially identical to CAR, or a variant thereof; (b) a liposome, wherein the targeting peptide is encapsulated within the liposome; and (c) an effective amount of an anti-inflammatory agent and methods for making and administering same.