This disclosure relates to methylsulfonamide derivatives and uses as imaging agents and other uses related to CXCR4 inhibition. In certain embodiments, the disclosure relates to pharmaceutical compositions comprising compounds disclosed herein, derivatives, or pharmaceutically acceptable salts or prodrugs thereof. In certain embodiments, the compositions disclosed herein are used for imaging to study CXCR4 related conditions.

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. ##STR00001##

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.

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.

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.

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.

The present invention provides radiolabeled trimethoprim which are useful in imaging tests such as PET scans. The compounds show robust bacterial uptake in vitro and identify infections from inflammation or tumor when administered to a subject. The compounds show rapid and sensitive detection of Ec DHFR containing tumors from control tumors and background tissue. In one aspect, a compound having the structure of formula (I) is provided or a pharmaceutically acceptable salt or prodrug thereof, wherein R is defined herein. Also provided are compositions containing these compounds, positron emission tomography reporter probe comprising these compounds, and methods of imaging a bacterial infection, tracking or monitoring bacteria, distinguishing a bacterial infection from inflammation or tumor, monitoring genetically fused protein expression, and monitoring genetically engineered cells in clinical scenarios such as immunotherapy for cancer treatment. ##STR00001##

The present invention provides an in vivo imaging method that facilitates the diagnosis of Diffuse Intrinsic Pontine Glioma (DIPG) at an early stage. Early diagnosis is particularly advantageous as neuroprotective treatment can be applied to healthy neural cells to delay or even prevent the onset of debilitating clinical symptoms. The present invention also provides methods for producing an in vivo imaging agent useful for early diagnosis of DIPG, where embodiments of the imaging agent include a lipophilic azomycin-based hypoxic cell sensitizer labelled with an in vivo imaging moiety, and embodiments including [18F]FMISO as the lipophilic azomycin-based hypoxic cell sensitizer labelled with an in vivo imaging moiety.

The present invention provides an in vivo imaging method that facilitates the diagnosis of Acute Lymphoblastic Leukemia (ALL) at an early stage. Early diagnosis is particularly advantageous as a tool to select more aggressive therapy, to estimate the success rate for visualizing ALL at the time of diagnosis.

The present invention addresses the problem of providing a technique for detecting a lesion of a heart disease in a non-invasive manner. The present invention provides a non-invasive diagnostic imaging agent for a heart disease, which contains a radioactively labeled compound capable of binding to an aldosterone synthase or a salt thereof as an active ingredient.