Patent classifications
A61K51/0453
MARKERS, CONJUGATES, COMPOSITIONS AND METHODS FOR HYPOXIA IMAGING, MAPPING, AND THERAPY
Described herein are markers, conjugates, compositions and methods for hypoxia imaging, mapping, and therapy. A compound comprising bio-reductively activated (BA) arm, linker arm and a mapping click wherein BA contains one for more of substituted or unsubstituted 2/4/5-substituted nitroimidazoles, or substituted benzotriazene-1,4-dioxides, or substituted 1,2,3/1,2,4-triazoles, or substituted 1,4-benzoquinones, or a combination of two homo-or hetero BA moieties, wherein linker arm contains C1-16 alkane, alkene, alkyne, alicyclic or aromatic linkers with or without hetero atoms as in ethers, amine, esters, acid, amides, 5 and 6 membered sugar sings with the substitution as described above, both monosaccharides and disaccharides, wherein mapping click contains one of substituted or unsubstituted N3-, CN, SCN, substituted alkynes for click chemistry. Said compound undergoes in situ click reaction after its distribution in cells or tissues to link to a reporting group which may be unchelated or chelated with a metal-radioactive or non-radioactive-, or a radiohalogen for PET/SPECT, or a dye for fluorescent/optical reporting group, thus accomplishing hypoxia imaging
Method for producing radiopharmaceutical composition
A simple method for producing a clinically applicable radiopharmaceutical composition containing 1-(2,2-dihydroxymethyl-3-[.sup.18F]fluoropropyl)-2-nitroimidazole ([.sup.18F]DiFA) or a salt thereof as an active ingredient, is provided which includes a synthesis step of obtaining a crude product of [.sup.18F]DiFA from a labeling precursor compound for [.sup.18F]DiFA; and a purification step of purifying the crude product, in which the purification step includes purifying [.sup.18F]DiFA using two or more different types of reverse phase solid phase extraction cartridges.
Compound for specifically binding to amyloid β-protein
Provided is a compound for specifically binding to amyloid -protein. The compound has thereon a nuclide with a large thermal neutron capture cross section and the compound is capable of specifically binding to the amyloid -protein. The property of the compound allows it to be used in conjunction with a neutron capture therapy device to eliminate amyloid -protein. Similarly, when the compound is labelled with radioactive element .sup.11C, the compound can also be used in conjunction with PET/CT for determining the part of the brain where amyloid -protein is deposited, for diagnosing Alzheimer's disease. Also disclosed is a preparation process for the compound. The beneficial effect of the present disclosure is to make the therapy and diagnosis of Alzheimer's disease more targeted by providing the compound for specifically binding to amyloid -protein.
COMPOUNDS USEFUL AS IMAGING AGENTS OF HYPOXIA
The application relates to a compound with the following formula (I):
##STR00001## its preparation method, its synthesis intermediates and its uses as an imaging agent of hypoxia.
Method for removing acetaldehyde
A method for removing or controlling or quantifying the presence of aldehydes, in particular acetaldehyde, is described. Such a method is useful in prolonging the shelf life of a pharmaceutical product.
Heterocyclic compounds for cancer imaging and treatment and methods for their use
Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R.sup.1, R.sup.2, R.sup.3, R.sup.11a, R.sup.11b, R.sup.11c, R.sup.11d, X, n.sup.1, n.sup.2, and n.sup.3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided. ##STR00001##
METHOD FOR PRODUCING RADIOHALOGEN-LABELED COMPOUND AND METHOD FOR PRODUCING RADIOPHARMACEUTICAL
Provided is a method for producing a radiohalogen-labeled compound, the method comprises: a step in which a radiohalogen-labeling precursor compound (S-L) having a leaving group (L) capable of being nucleophilically substituted by a radioactive halide ion (X.sup.) is subjected to a radiohalogenation reaction to obtain a reaction mixture RM1 which contains the radiohalogen-labeling precursor compound (S-L) and a reaction product (SX) resulting from the radiohalogenation reaction; a step in which the reaction mixture RM1 is mixed with a polyvalent acid or a salt thereof to obtain a reaction mixture RM2; and a step in which the reaction product (SX) is purified from the reaction mixture RM2 by a solid phase extraction method.
IMIDAZOTHIADIAZOLE AND IMIDAZOPYRAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION
The present invention provides thiazole compounds of Formula I
##STR00001##
wherein W, Y,
##STR00002##
R.sup.0, R.sup.2, R.sup.4, R.sup.5, R.sup.6, R.sup.7, X.sup.1, X.sup.2, X.sup.3 and X.sup.4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
PSMA TARGETED FLUORESCENT AGENTS FOR IMAGE GUIDED SURGERY
Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.
COMBINATION THERAPIES FOR THE TREATMENT OF ALZHEIMER'S DISEASE AND RELATED DISORDERS
The present invention relates to combination therapies for treating Alzheimer's disease or an amyloidosis-associated pathological condition comprising co-administering a therapeutically effective amount of a first compound, and a therapeutically effective amount of a second compound. In certain embodiments, the first compound or the second compound inhibits AB peptide polymerization; is an anti-inflammatory; improves cognitive function, mood, or social behavior; is associated with Tau or alpha-synuclein; or regulates amyloid peptide washout.