Conjugates of an active agent attached to a targeting moiety, such as at least one HSP90 binding moiety, via a linker, have been designed. Such conjugates can provide improved temporospatial delivery of the active agent, improved biodistribution and penetration in tumor, and/or decreased toxicity. Methods of making the conjugates and the formulations thereof are provided. Methods of administering the formulations to a subject in need thereof are provided, for example, to treat or prevent cancer.

The present invention relates to novel compounds having a capacity for PDE1 inhibition which may be used as tracers for use in diagnostic techniques, biomarkers for phosphodiesterase 1 (PDE1) in vivo, methods for treating and/or developing novel therapies for PDE1-associated conditions, and to methods of detection and treatment.

Methods and compositions for treating, diagnosing and staging cancers, in particular overexpressing the Human Epidermal growth factor Receptor 2 protein (HER2+) given rise to in breast, gastric, gastroesophageal, ovarian, pancreatic cancer and brain tumors, which may be metastatic to the brain or other site. More specifically, the invention provides for Targeted Radionuclide Therapy (TRNT) with a compound of the invention having a peptide that targets the HER2+ cells, a second component for combining metals into complexes through a ring structure (DOTA), and a third radioisotope component, Lu-177 and Ga-68, in which embodiments further include a companion diagnostic, and in which embodiments further include anti-integrin precision medicines for cancers expressing αvβ3 and αvβ5 integrins, HER2+, vascular endothelial growth factor, vitronectin, fibronectin, tenascin, reelin, kindlin and talin. TRNT may be administered alone or in combination with standard-of-care; an immunooncologic and/or chemotherapeutic, adjuvantly or neoadjuvantly.

Compounds having a structure of Formula I: ##STR00001##
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.

Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use. ##STR00001##

The present invention relates to radiolabelled 4-(furo[3,2-c]pyridin-4-yl) derivatives and their use as radioactive tracers, and in particular their use as imaging agents.

The present invention provides a system and method for performing a single-scan rest-stress cardiac measurement. In one aspect, the system includes a positron emission tomography (PET) imaging system, a source of a first PET radiotracer for administration to a subject, a source of a second PET radiotracer for administration to a subject, and a processor. The processor has non-transient computer readable media programmed with instructions to obtain PET images of the subject administered with the radiotracer. Furthermore, the computer readable media is programmed with instructions to process the PET images with a non-steady-state, multi-compartment parametric model. An output of the non-steady-state, multi-compartment parametric model is a measure of myocardial blood flow for both a rest state and a stress state of the subject.

A method of imaging a bacterial infection in a host mammal using Triazolo[4,5-d]pyrimidine derivatives of formula (I):

##STR00001##

Also disclosed are compositions including the triazolo[4,5-d]pyrimidine derivative.

The present application provides stable heterobiligands made up of peptide-based FOLR1 ligands and folate (the ligand of FOLR1) and methods of use of the heterobiligands as detection, imaging, diagnostic, and therapeutic agents. The application further provides methods of manufacturing FOLR1 heterobiligands, capture agents, and imaging agents.

The present invention relates to a method for diagnosing a pancreatic function, including: a step of administering a diagnostic agent for a pancreatic function which contains a compound represented by General Formula (1-0) as an active component to a subject; a step of detecting the compound (1-0) accumulated in the pancreas; and a step of quantitatively analyzing an amount of compound (1-0) accumulated in the pancreas.

##STR00001##

[In General Formula (1-0), R represents —O(CH.sub.2).sub.n—, —O(CH.sub.2).sub.nOC.sub.2H.sub.4—, —CH.sub.2O(CH.sub.2).sub.n—, or —CH.sub.2O(CH.sub.2).sub.nOC.sub.2H.sub.4—, n represents an integer of 1 to 5, and Q.sup.1 represents F or —OCH.sub.3].