The subject matter of the invention is PSMA inhibitor-HYNIC derivatives of PSMA-L.sub.1-L.sub.2-HYNIC formula, aromatic and aliphatic hydrazone derivatives, a radiopharmaceutical kit for 99mTc isotope labelling, radiopharmaceutical preparation and its application for prostate cancer and its metastasis diagnostics.

A nanoparticle is provided. The nanoparticle includes a magnetic core including a magnetic nanocrystal, a fluorophore coupled to the magnetic core, at least one chelating compound coupled to the magnetic core, the at least one chelating compound being a compound that chelates copper-64 (.sup.64Cu), a compound that chelates technetium-99m (.sup.99mTc), or a combination thereof, and an iodine chelator coupled to the magnetic core. Methods of making the nanoparticle and of using the nanoparticle as a multi-modal contrast agent are also provided.

This invention relates to a chemistry branch, particularly to the field of compounds' organic synthesis that belongs to the aromatic bicyclic or naphthalene category, used in the detection of amyloid sheets. These new naphthalene derivatives have a general formula: Wherein R represents mutually independent groups. In I: R.sub.1:-alkylenyl-C(O)NH-alkylenyl-R.sub.3, -alkylenyl-C(O)O—R.sub.4, R.sub.3:—COOH, —OH, —SH, —NH.sub.2, -alkyl-NH-alkyl-N-dithiocarbamate alkaline earth metal salts, R.sub.4: H, succinimidyl group, R.sub.2: —H,-alkyl. In II: R.sub.1: -alkyl, -alkylenyl-halide-alkylenyl-hydroxyl-alkylenyl-O-aryl, —O-alkylsulfonate alkylenyl, R.sub.2: -halide-alkylenyl-O-aryl, -alkylenyl-O-alkylsulfonate, -alkylenyl-halide-, —CH(O), —HC═C(CN).sub.2, —HC═CHNO.sub.2, -alkylenyl-NH.sub.2, -alkylenyl-NH-alkyl, -alkylenyl-alkyl-N-dithiocarbamate alkaline salts. The terms “alkyl” and “alkylenyl” refer to linear or branched aliphatic chains, preferably from 1 to 4 carbon atoms and the term halide to fluorine, bromine or iodine. These compounds are neutral, lipophilic and have low molecular weight and therefore they cross the blood brain barrier and attach to the amyloid sheets. The present invention provides procedures for obtaining naphthalene derivatives with good yields, which can be practical, economical and adapted to a larger-scale manufacturing. We are unaware whether the compounds presented in this invention have been previously reported.

Described herein are prostate specific membrane antigen (PSMA) binding conjugates that are useful for delivering therapeutic, diagnostic and imaging agents. Also described herein are pharmaceutical composition containing them and methods of using the conjugates and compositions. Also described are processes for manufacture of the conjugates and the compositions containing them.

The present invention provides positron emitter radiolabeled versions of PABA, metabolites and derivatives, with good radiochemical yield, high specific activity, high chemical and radiochemical purity and having excellent characteristics for PET imaging. The inventive composition and methods provide high quality dynamic images of the kidneys while reducing the radiation exposure. The short biological half-life of PABA, added to the short physical half-life of positron emitters such as .sup.11C will also benefit patients that require multiple renography assessments in a short period of time.

The inventive method relates to a method for the determination of susceptibility or diagnosis of autism or autism spectrum disorders. Diagnosis or determination of susceptibility determinations are predicated on quantitative analysis of endocannibinoid levels or endocannibinoid receptor expression.

This application relates to compounds of Formula I. R.sup.1a, R.sup.1b and R.sup.1c is —CO.sub.2H, —SO.sub.2H, —SO.sub.3H, —SO.sub.4H, —PO.sub.2H, —PO.sub.3H or —PO.sub.4H. R.sup.2 is a linker, e.g. butylene. R.sup.3 is a linkage, e.g. —O—, —S—, —S(O)—, S(O).sub.2—, —NHC(O)—, —C(O)NH—, or 1,2,3-triazole. R4 is —(CH.sub.2).sub.0-3CH(R.sup.7)(CH.sub.2).sub.0-3— wherein R.sup.7 is —(CH.sub.2).sub.5CH.sub.3 or certain aromatic fused-ring systems. R.sup.5 and R.sup.6 are hydrogen or methyl. Each Xaa.sup.1 (if present) is an amino acid. R.sup.X is a radiolabeling group, e.g.: a radiometal chelator optionally bound by a radiometal; an aryl substituted with a radioisotope; a prosthetic group containing a trifluoroborate; or a prosthetic group containing a silicon-fluorine-acceptor moiety. The compounds may be useful for imaging prostate-specific membrane antigen (PSMA)-expressing tissues or for treating PSMA-expressing diseases (e.g. cancer).

##STR00001##

The present invention relates to a compound of formula (1) (I), wherein Y.sup.3 is O or S, wherein s, t, u and w are 0 or 1, wherein i is an integer of from 1 to 3, wherein j is an integer of from 3 to 5, and wherein Z.sup.1, Z.sup.2 and Z.sup.3 are selected from the group consisting of CO.sub.2H, —SO.sub.2H, —SO3H, —OSO3H, and -0P0.sub.3H.sub.2, R.sup.1 is —CH.sub.3 or H, X is selected from the group consisting of alkylaryl, aryl, alkylheteroaryl and heteroaryl, Y.sup.1 and Y.sup.2 are selected from the group consisting of aryl, alkylaryl, cycloalkyl, heterocycloalkyl, heteroaryl and alkylheteroaryl, and wherein A is a chelator residue having a structure selected from the group consisting of (la), (lb) and (lc), wherein R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are selected from the group consisting of H, —CH.sub.2—COOH and —CH.sub.2—C(=0)-NH.sub.2 or wherein R.sup.2 and R.sup.4 form a —(CH.sub.2).sub.n— bridge with n being an integer of from 1 to 3, wherein n is preferably 2, and wherein r, v and q are 0 or 1, with the proviso that in case u and w are 0, q and v are 0, and (A) wherein u and w are 1, or (B) wherein u is 0 and w is 1, and wherein A is selected from (la) or (lb), or (C) wherein A is not The compound is disclosed for use in the treatment of PSMA-expressing cancer.

##STR00001##

The present disclosure relates to methods of administering [.sup.18F]-FACBC. The present disclosure also relates to use of [.sup.18F]-FACBC in methods for imaging, diagnosing and monitoring metastasis or recurrence of cancer.

It is intended to provide a novel amino acid organic compound which can be used as a labeling precursor compound for radioactive halogen-labeled amino acid compounds including [.sup.18F]FACBC, and which prevents methanol from remaining in the radioactive halogen-labeled amino acid compounds produced therefrom. The novel amino acid organic compound is a compound represented by the following formula:

##STR00001##

wherein n is an integer of 0 or of 1 to 4; R.sup.1 is an ethyl, 1-propyl or isopropyl substituent; X is a halogen substituent or a group represented by —OR.sup.2; R.sup.2 is a straight-chain or branched-chain haloalkylsulfonic acid substituent with one to 10 carbon atoms, trialkylstannyl substituent with 3 to 12 carbon atoms, fluorosulfonic acid substituent or aromatic sulfonic acid substituent; and R.sup.3 is a protective group.