A61K51/0461

ORGAN PROTECTION IN PSMA-TARGETED RADIONUCLIDE THERAPY OF PROSTATE CANCER

A method of reducing radiation exposure of a non-cancerous tissue of a patient diagnosed with a cancer includes administering to the patient an agent capable of competing for binding sites on a surface of the non-cancerous tissue, provided that the administration is carried out after a waiting period that follows administration of a compound including a radionuclide to the patient, the compound having affinity for both a cancerous tissue and the non-cancerous tissue, and, further provided that the binding sites have an affinity for both the agent and the compound.

Small molecule imaging of fungi by positron emission tomography scanning

Disclosed herein are isotopically labeled calcofluor derivatives and uses of such to detect fungi, such as filamentous fungi, including Aspergillus species, such as by positron emission tomography (PET) scanning. In some examples, the disclosed compounds have a formula of ##STR00001## wherein R.sup.1 is an amine, a hydroxyl group, a sulfide, a carboxylic acid, an amide, an alkyl, or aryl; R.sup.2 is NHC(O)R.sup.3L or C(O)NHR.sup.3L, wherein R.sup.3 is an aryl or an aliphatic group (such as alkyl); each R.sup.4 independently may be selected from halogen, aliphatic (such as alkyl), aryl, amine, hydroxyl, haloalkyl, carboxylic acid, amide, aralkyl, cyano, ester, thiol, thioether, or alkoxy; each R.sup.5 independently may be selected from hydrogen, aralkyl, alkyl, or aryl, with any one of the aralkyl, alkyl, or aryl groups optionally being substituted with any one of the substituents provided for R.sup.4; each n independently is 1, 2, 3, 4, or 5; and L is .sup.18F or a chelator capable of chelating a radiolabel (such as chelators for [.sup.18F]AlF, .sup.64Cu, .sup.68Ga),1,4,7,10-tetraazacyclododecane-tetraacetic acid (DOTA) or 1,4,7-triazacyclononane-triacetic acid (NOTA).

Organ protection in PSMA-targeted radionuclide therapy of prostate cancer

A method of reducing radiation exposure of a non-cancerous tissue of a patient diagnosed with a cancer includes administering to the patient an agent capable of competing for binding sites on a surface of the non-cancerous tissue, provided that the administration is carried out after a waiting period that follows administration of a compound including a radionuclide to the patient, the compound having affinity for both a cancerous tissue and the non-cancerous tissue, and, further provided that the binding sites have an affinity for both the agent and the compound.

METHODS OF DIAGNOSING AND TREATING NEURODEGENERATIVE DISEASES
20250170124 · 2025-05-29 ·

This disclosure provides compounds, pharmaceutical compositions, imaging compositions and methods useful for the diagnosis and/or treatment of neurodegenerative diseases. In particular, this disclosure provides compounds, including radiolabeled compounds, compositions, and methods useful for the diagnosis and/or treatment of neurodegenerative diseases associated with a-synuclein aggregation, such as Parkinson's disease, dementia with Lewy bodies, multiple systems atrophy or prodromal REM sleep behavior disorder.

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.