Method of treating cancer, such as a metastatic cancer, with inhibitors of homeodomain interacting protein kinase 4 (HIPK4) are provided. Related therapeutic compositions are also disclosed.

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

The present disclosure relates to [.sup.18F]-labeled benzothiazole derivatives or salts thereof as positron emission tomography (PET) radiotracers suitable for imaging the stress-signaling non-receptor tyrosine kinase c-abl, and their use in in vivo diagnosis, preclinical and clinical imaging, patient stratification on the basis of mutational status of c-abl and assessing response to therapeutic treatments. The present disclosure further relates to the use of [.sup.18F]-labeled benzothiazole derivatives as PET radiotracers. The disclosure also provides a process for the radiosynthesis of [.sup.18F]-labeled benzothiazole derivatives.

The present invention provides an α-synuclein aggregate binding agent that has high binding selectivity for an α-synuclein aggregate.

The α-synuclein aggregate binding agent contains a compound represented by a formula (I), a pharmaceutically acceptable salt thereof, or a solvate thereof:

##STR00001##

in the formula (I), R.sub.1 and R.sub.2 are each independently selected from the group consisting of hydrogen, alkyl, alkenyl, acyl, and hydroxyalkyl; R.sub.3 is hydrogen or halogen; the ring A is a benzene or pyridine ring; the ring B is represented by the following formula (i) or (ii):

##STR00002##

R.sub.4 and R.sub.5 are each independently selected from the group consisting of hydrogen, hydroxy, alkoxy, haloalkoxy, halohydroxyalkoxy, and aminoalkyl.

Provided is a method for producing a radiohalogen-labeled compound, the method comprises: a step in which a radiohalogen-labeling precursor compound (S-L) having a leaving group (L) capable of being nucleophilically substituted by a radioactive halide ion (X.sup.−) is subjected to a radiohalogenation reaction to obtain a reaction mixture RM1 which contains the radiohalogen-labeling precursor compound (S-L) and a reaction product (S—X) resulting from the radiohalogenation reaction; a step in which the reaction mixture RM1 is mixed with a polyvalent acid or a salt thereof to obtain a reaction mixture RM2; and a step in which the reaction product (S—X) is purified from the reaction mixture RM2 by a solid phase extraction method.

Disclosed herein is a complex, a contrast agent and the method for treating a disease related to CXCR4 receptor. The complex is configured to bind the CXCR4 receptor, and is used as a medicament for diagnosis and treatment of cancers and other indications related to the CXCR4 receptor.

The invention relates to 9H-pyrrolo-dipyridine derivatives of formula I, processes for preparing them, pharmaceutical compositions containing them and their use as radiopharmaceuticals in particular as imaging agents for the detection of Tau aggregates. ##STR00001##

The present invention relates to novel compounds of the formula (II) and formula (III) ##STR00001##
that can be employed in the selective Tau detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease and other tauopathies using Positron Emission Tomography (PET) Imaging.

The fluorine-containing compound includes: two nitroxide radical-containing groups represented by Formula (1) (R.sup.1, R.sup.2, R.sup.3, and R.sup.4 are each independently a C1-10 alkyl group unsubstituted or substituted with a substituent containing no fluorine atoms); and one to three —O—C(CF.sub.3).sub.3 groups, in which the nitroxide radical-containing groups are bound to the —O—C(CF.sub.3).sub.3 groups through a chain structure with 2 to 17 atoms.

##STR00001##

The invention relates to water soluble .sup.18F-prosthetic groups and the synthesis and use of .sup.18F-labeled biological molecules containing the .sup.18F-prosthetic groups for imaging various processes within the body, for detecting the location of molecules associated with disease pathology, and for monitoring disease progression are disclosed.