A61K51/0453

LIGANDS FOR IMAGING CARDIAC INNERVATION

Novel compounds that find use as imaging agents within nuclear medicine applications (PET imaging) for imaging of cardiac innervation are disclosed. These PET based radiotracers may exhibit increased stability, decreased NE release (thereby reducing side effects), improved quantitative data, and/or high affinity for VMAT over prior radiotracers. Methods of using the compounds to image cardiac innervation are also provided. In some instances the compounds are developed by derivatizing certain compounds with 18F in a variety of positions: aryl, alkyl, a keto, benzylic, beta-alkylethers, gamma-propylalkylethers and beta-proplylalkylethers. Alternatively or additionally, a methyl group a is added to the amine, and/or the catechol functionality is either eliminated or masked as a way of making these compounds more stable.

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.

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Contrast agents for myocardial perfusion imaging

The present disclosure is directed, in part, to compounds and methods for imaging myocardial perfusion, comprising administering to a patient a contrast agent which comprises a compound that binds MC-1, and an imaging moiety, and scanning the patient using diagnostic imaging.

IMIDAZOTHIADIAZOLE AND IMIDAZOPYRAZINE DERIVATIVES AS PROTEASE ACTIVATED RECEPTOR4 (PAR4) INHIBITORS FOR TREATING PLATELET AGGREGATION

The present invention provides thiazole compounds of Formula I wherein W, Y, 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.

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Dose synthesis card for use with automated biomarker production system

Microfluidic radiopharmaceutical production system and process for synthesizing per run approximately, but not less than, ten (10) unit doses of radiopharmaceutical biomarker for use in positron emission tomography (PET). A radioisotope from an accelerator or other radioisotope generator is introduced into a reaction vessel, along with organic and aqueous reagents, and the mixture heated to synthesize a solution of a pre-selected radiopharmaceutical. The solution is purified by passing through a combination of solid phase extraction purification components, trap and release components, and a filter. The synthesis process reduces waste and allows for production of biomarker radiopharmaceuticals on site and close to the location where the unit dose will be administered to the patient. On-site, as-needed production of radiopharmaceuticals in small doses reduces the time between synthesis of the radiopharmaceutical and administration of that radiopharmaceutical, minimizing loss of active isotopes through decay and allowing production of lesser amounts of radioisotopes overall.

COMPOUND FOR SPECIFICALLY BINDING TO AMYLOID ß-PROTEIN
20180298037 · 2018-10-18 ·

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.

Labeled pkg-1-alpha-binding compounds and their use in imaging and quantifying pain

The present invention relates to the use of compounds that selectively bind to activated protein kinase G 1 alpha for imaging the anatomic basis for chronic pain. Such imaging may also be used to objectively quantify chronic pain.

AZETIDINE DERIVATIVES FOR TAU IMAGING

The present invention provides a novel compound of the formula: methods of making this compound, methods of using this compound for tau imaging, and preparations of tau imaging formulations.

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Half-curcuminoids as amyloid-beta pet imaging agents

Provided herein are curcumin analogues that are able to interact with amyloid beta (A?) and to attenuate the copper-induced crosslinking of A?. Also provided herein are methods of using the compounds as imaging agents of amyloid beta and for the treatment of diseases associated with amyloid beta. Methods of preparing unlabeled and radiolabeled compounds useful for interacting with amyloid beta and pharmaceutical compositions are also provided.

Imidazothiadiazole and imidazopyrazine derivatives as protease activated receptor 4 (PAR4) inhibitors for treating platelet aggregation

The present invention provides thiazole compounds of Formula I wherein W, Y, 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.