Embodiments of the present disclosure provide for -AApeptides, -AApeptide building blocks, methods of making -AApeptides and libraries of -AApeptides, methods of screening the -AApeptide libraries for desired peptidomimetic activity, and the like. The present disclosure also provides for -AApeptides that are inhibitors of A peptide aggregation, methods of inhibiting and disassembling A peptide aggregation, methods of inhibiting the toxicity of A aggregates towards N2a neuroblasotma cells, as well as methods and compounds for treating Alzheimer's disease.

A PSMA-specific imaging agent comprising a compound according to formula I: ##STR00001##
are described, wherein S.sup.1 is an organic spacer group having from 5 to 30 carbons, A is an amino acid forming a portion of a negatively charged peptide oligomer, n is from 3 to 6, S.sup.2 is an organic spacer group having from 5 to 15 carbons, and I is an imaging group, and pharmaceutically acceptable salts thereof. The PSMA-specific imaging agents can be used to image PSMA within a tissue region to guide the treatment of diseases such as prostate cancer.

This application describes a compound represented by Formula (I): (I) wherein: Y is a biologically active organic core group comprising one or more of an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group, to which Z is covalently bonded; n is 1, 2, 3, 4 or 5; m is 1 or 2; Z is O, NR, or N; X.sup.1 is a covalent bond or CH.sub.2CH.sub.2, X.sup.2 is O or NR; and R comprises H or a substituted or unsubstituted group selected from an aryl group, a heteroaryl aryl group, a nonaromatic hydrocarbyl group, and a nonaromatic heterocyclic group. Methods of preparing the compounds, methods of using the compounds, and pharmaceutical compositions comprising the compounds are described as well.

The prostate-specific membrane antigen (PSMA) is increasingly recognized as a viable target for imaging and therapy of cancer. Various 99mTc/Re-labeled compounds were prepared by attaching known Tc/Re chelating agents to an amino-functionalized PSMA inhibitor with or without a variable length linker moiety. Ex vivo biodistribution and in vivo imaging demonstrated the degree of specific binding to engineered PSMA+PC3 PIP tumors.

The present invention generally relates to novel synthetic methods, systems, kits, salts, and precursors useful in medical imaging. In some embodiments, the present invention provides compositions comprising an imaging agent precursor, which may be formed using the synthetic methods described herein. An imaging agent may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in .sup.18F. In some cases, an imaging agent including salt forms (e.g., ascorbate salt) may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

The present invention relates to new combinations of treatments for abnormal dopamine deficiency disorders, and related conditions, comprising deuterated catecholamine derivatives and catechol-O-methyltransferase (COMT) inhibitors.

The present invention relates to a compound of formula (1)

##STR00001##

or a pharmaceutically acceptable salt or solvate thereof, wherein Y.sup.3 is O or S, wherein s, t, u and w are, independently of each other, 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 independently of each other, selected from the group consisting of CO.sub.2H, SO.sub.2H, SO.sub.3H, OSO.sub.3H, and OPO.sub.3H.sub.2, R.sup.1 is CH.sub.3 or H, preferably H, X is selected from the group consisting of alkylaryl, aryl, alkylheteroaryl and heteroaryl, Y.sup.1 and Y.sup.2 are independently, of each other, 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 (Ia), (Ib) and (Ic)

##STR00002##

wherein R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are, independently of each other, selected from the group consisting of H, CH.sub.2COOH and CH.sub.2C(O)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 independently of each other, 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 (Ia) or (Ib), or (C) wherein A is not

##STR00003##

Further, the present invention relates to a complex comprising (a) a radionuclide, and (b) the compound, as described above or below, or a salt, solvate, metabolite or prodrug thereof.

Further, the present invention relates to a pharmaceutical composition comprising a compound, as described above or below, or a complex, as described above or below. Further, the present invention relates to a compound, as described above or below, or a complex, as described above or below, or a pharmaceutical composition, as described above or below, for use in treating, ameliorating or preventing PSMA-expressing cancer and/or metastases thereof, in particular prostate cancer and/or metastases thereof. Further, the present invention relates to a compound, as described above or below, or a complex, as described above or below, or a pharmaceutical composition, as described above or below, for use in diagnostics. In addition, the present invention relates to a compound, as described above or below, or a complex, as described above or below, or a pharmaceutical composition, as described above or below, for use in the diagnosis of cancer, in particular of PSMA-expressing cancer and/or metastases there

Embodiments of the present disclosure provide for -AApeptides, -AApeptide building blocks, methods of making -AApeptides and libraries of -AApeptides, methods of screening the -AApeptide libraries for desired peptidomimetic activity, and the like. The present disclosure also provides for -AApeptides that are inhibitors of A peptide aggregation, methods of inhibiting and disassembling A peptide aggregation, methods of inhibiting the toxicity of A aggregates towards N2a neuroblasotma cells, as well as methods and compounds for treating Alzheimer's disease.

The invention relates to fluorinated compounds and their use as anti-epileptic, muscle-relaxing, fever-reducing and peripherally analgesically acting medications and as imaging agents. Novel fluorinated 2-amino-4-(benzylamino)phenyl carbamate derivatives of ezogabine and pharmaceutically acceptable salts or solvates thereof and their use are described.

The present invention provides a method of treating cancer with a proteasome inhibitor. The invention provides a method for treating a patient with a proteasome inhibitor based on measurements of tumor features using biomedical imaging techniques. The invention also provides a method of treating a patient with cancer based on levels of GLUT4, as measured by a biomedical imaging technique. The invention also provides a method of treating a cancer patient with a proteasome inhibitor based on the effect of the treatment on tumor features measured by a biomedical imaging technique.