Patent classifications
A61K51/0406
PSMA-BASED MOLECULAR-GENETIC REPORTER SYSTEM
The presently disclosed subject matter provides methods, reporter gene constructs, and kits for using prostate-specific membrane antigen (PSMA) as an imaging reporter to image a variety of cells and tissues.
LABELED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PSMA-EXPRESSING CANCERS
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##
PRECURSOR COMPOUND OF RADIOACTIVE HALOGEN-LABELED ORGANIC COMPOUND
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.
Radiopharmaceutical compositions of radioactive halogenated benzylguanidine
The present disclosure concerns radiopharmaceutical compositions of radioactive halogenated benzylguanidine (such as radioiodinated MIBG) or a pharmaceutically acceptable salt, hydrate, or solvate thereof. In a preferred embodiment, the composition has at least 97% of radiochemical purity for at least 4 days. Advantageously, the compositions of the present disclosure may be devoid of parabens, which are carcinogenic and yet are used in known radioactive MIBG compositions. The present disclosure also provides processes of preparing a radioactive halogenated benzylguanidine composition. The compositions of the present disclosure can be used in diagnosis and treatment of various diseases.
Chelated PSMA Inhibitors
Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells.
##STR00001##
COMPOSITIONS AND METHODS TO DETECT GLUA1 IN BRAIN AND TO IDENTIFY THE PRESENCE OF GLUA1-MEDIATED PTSD
The present invention provides compositions and methods for detecting GluA1, as a subunit protein and/or as a GluA1-containing, GluA2-lacking AMPAR complex. The invention further provides composition and methods for detecting and/or diagnosing PTSD. The invention further relates to compositions that can be detected using radiological imaging techniques, and processes for performing such imaging techniques using the compositions, to identify elevated GluA1 expression or activity in a subject, which is a biological marker of PTSD.
COMPOSITIONS, METHODS, AND SYSTEMS FOR THE SYNTHESIS AND USE OF IMAGING AGENTS
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.
Chelated PSMA inhibitors
Provided herein are compounds of Formula (I) or a pharmaceutically acceptable salt thereof. Also provided are compositions including a compound of Formula (I) together with a pharmaceutically acceptable carrier, and methods for imaging prostate cancer cells. ##STR00001##
Compositions and methods to detect GluA1 in brain and to identify the presence of GluA1-mediated PTSD
The present invention provides compositions and methods for detecting GluA1, as a subunit protein and/or as a GluA1-containing, GluA2-lacking AMPAR complex. The invention further provides composition and methods for detecting and/or diagnosing PTSD. The invention further relates to compositions that can be detected using radiological imaging techniques, and processes for performing such imaging techniques using the compositions, to identify elevated GluA1 expression or activity in a subject, which is a biological marker of PTSD.
Compositions, methods, and systems for the synthesis and use of imaging agents
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.