A61K51/0455

Fibroblast activation protein (FAP) targeted imaging and therapy in fibrosis

Excessive deposition of extracellular matrix is a hallmark of Idiopathic pulmonary fibrosis (IPF), it is advantageous to target the cells and the mechanisms associated with this process. By targeting myofibroblasts (specialized contractile fibroblasts) that are key for the development of IPF with drugs conjugated with fibroblast activation protein (FAP), this technology helps minimize the production of extracellular matrix in the lungs and provides a new treatment option for patients diagnosed with IPF.

METAL OXIDE CATALYZED RADIOFLUORINATION

Inter alia, the first titania-catalyzed [.sup.18F]-radiofluorination in highly aqueous medium is provided. In embodiments, the method utilizes titanium dioxide, 1:1 acetonitrile-thexyl alcohol solvent mixture and tetrabutylammonium bicarbonate as a base. Radiolabeling may be directly performed with aqueous [.sup.18F]fluoride without the need for drying/azeotroping step, which reduces radiosynthesis time while keeping high fluoride conversion. The general applicability of the synthetic strategy to the synthesis of the wide range of PET probes from tosylated precursors is demonstrated.

NATURAL CANNABINOID COMBINATION THERAPY COMPOSITIONS AND METHODS FOR PERSONALIZED AND TARGETED THERAPIES INCLUDING THE TREATMENT OF INFECTIOUS DISEASES
20220305148 · 2022-09-29 ·

Compositions and methods for the personalized and targeted therapeutic treatment of diseases and disorders, including the treatment of pain, inflammation, and infectious diseases in a subject. In particular, labeled natural cannabinoid therapeutic compositions are provided that include a conjugate of a natural cannabinoid compound, a chelator, and a label, that when coupled with imaging may be used to determine in real time optimal dosing and targeting of particular pathways and tissues to provide personalized therapies. Combination therapies are also provided that include one or more natural cannabinoid compound and at least one active pharmaceutical ingredient.

6-amido derivatives of 4, 5-a epoxymorphinans for the treatment of pain

Compounds of formula: ##STR00001##
in which R.sup.4 is chosen from substituted phenyl, optionally substituted naphthylene, optionally substituted anthracene and optionally substituted aromatic heterocycle, are useful as analgesics.

Highly selective sigma receptor ligands and radioligands as probes in nociceptive processing and the pathphysiological study of memory deficits and cognitive disorders

A method for localizing and quantifying S1R role in nociceptive processing; for providing a guide to providing an analgesic therapy; of using an S1R selective ligand as a biomarker for pathphysiological study of memory deficits and cognitive disorders; or of detecting increased S1R density at the site of nerve injury arising from neuropathic pain comprising using as a probe at least one SR1 selective compound or radioligand of the general formula III′, or IV′: ##STR00001##

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.

DESIGN AND DEVELOPMENT OF NEUROKININ-1 RECEPTOR-BINDING AGENT DELIVERY CONJUGATES
20170216465 · 2017-08-03 ·

Neurokinin-1 (NK-1) receptor-binding agent delivery conjugates, compositions comprising NK-1 receptor-binding agent delivery conjugates, and methods for making and administering NK-1 receptor-binding agent delivery conjugates are provided. A conjugate may include an NK-1 receptor-binding moiety, a linker group containing at least one linker selected from the group of a releasable linker and a spacer linker, and an active agent linked to the linker group. The active agent may be selected from the group of fluorophore-containing compounds, radionuclide-containing compounds, and therapeutic agents for treatment of tumor cells characterized by over-expression of the NK-1 receptor.

Fluorinated 2-arylbenzo heterocyclic compound with high affinity to Aβ 946; plaques and containing chiral side chain substituent, and preparation method and usage thereof

A fluorinated 2-arylbenzo heterocyclic compound with high affinity to Aβ plaques and containing a chiral side chain substituent, has a general formula (I) as follows: ##STR00001## wherein X is N; Y is S or O; Z is N or CH; R.sub.1 is a 5 or 6-substituent and is ##STR00002##
F is .sup.19F or .sup.18F; R.sub.2 is NHCH.sub.3 or N(CH.sub.3).sub.2. The compound of the present invention has high affinity to Aβ plaques and can be used to make appropriate radioactive nuclide labeling probes for early diagnosis of AD.

Labeled iodinated tropane formulation

A diagnostic formulation is provided comprising a tropane having a radioactive concentration of at least 1.6 mCi/mL at least about 51 hours post creation. The diagnostic formulation optionally comprises a radiolabeled dopamine transporter (DAT) ligand useful in the diagnosis of Parkinson's disease (PS). One example of a radiolabeled dopamine transporter (DAT) ligand example is [.sup.123I]-2β-carbomethoxy-3β-(4-flurophenyl)-N-(3-iodo-E-allyl) nortropane.

Microtubule-associated protein Tau imaging compounds for Alzheimer's disease and precursors thereof

The present invention discloses a series of nuclear medicine tracers that are combined with brain microtubule-associated protein Tau targeting compounds to produce a group of compounds of nuclear medicine that can be utilized for imaging of microtubule-associated protein Tau. When the positrons released by the decay encounter the electrons of the cells in the sample, utilizing the positron decay characteristics of fluorine-18 or iodine-124 isotope to generate mutual destruction reactions, a pair of opposite gamma rays is formed which are imaged by positron emission tomography. The compounds can be applied for the in vivo detection of microtubule-associated protein Tau deposits in the brain. The invention provides a strategy for diagnosis of Alzheimer's disease and a method to measure the efficacy of therapeutic drugs targeting microtubule-associated protein Tau.