A61K51/0463

CANCER TREATMENT BY COMBINED INHIBITION OF POLO-LIKE KINASE AND MICROTUBULE POLYMERIZATION
20230263783 · 2023-08-24 ·

An effective amount of one or more microtubule polymerization inhibitors is administered in combination with one or more polo-like kinase (Plk) inhibitors for treating cancer. Administration of the combination of the active agents can be effective to reduce cancer cell proliferation or viability in a subject with cancer to the same degree, or a greater degree, than administering to the subject the same amount of either active agent alone. The active agents can be administered together or separately. Methods of selecting and treating subjects with cancers are also provided.

Small Molecules for Dual Function Positron Emission Tomography (PET) and Cell Suicide Switches
20220133917 · 2022-05-05 ·

The present invention includes an engineered cell comprising a chimeric antigen receptor (CAR) further comprising a nucleic acid molecule comprising a suicide gene comprising a ligand binding domain and a suicide domain wherein the ligand binding domain is capable of binding to radiolabeled tracer or a small molecule suicide switch. This invention also includes methods for inducing apoptosis of an engineered cell, methods for assessing the efficacy or toxicity of an adoptive cell therapy in a subject, methods for detecting the quantity of engineered T cells in a subject, methods for monitoring an immunotherapy treatment in a subject and methods of imaging engineered T cells in a subject. In some embodiments, the imaging is performed via Positron Emission Topography (PET). This invention further includes a chemical inducer of dimerization (CID), wherein the CID is a Bis-Trimethoprim (Bis-TMP).

9H-pyrrolo-dipyridine derivatives

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##

MACROCYCLIC COMPLEXES OF RADIONUCLIDES AND THEIR USE IN RADIOTHERAPY OF CANCER

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”) where the compounds are represented by the following Formulas (I), or a pharmaceutically acceptable salt thereof (IA), or a pharmaceutically acceptable salt thereof (II), or a pharmaceutically acceptable salt thereof, wherein M.sup.1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.

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MACROCYCLIC COMPLEXES OF ALPHA-EMITTING RADIONUCLIDES AND THEIR USE IN TARGETED RADIOTHERAPY OF CANCER

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”) where the compounds are represented by the following:

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or a pharmaceutical y acceptable salt thereof,

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or a pharmaceutically acceptable salt thereof,

##STR00003##

or a pharmaceutically acceptable salt thereof,
wherein M.sup.1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.

9H-PYRROLO-DIPYRIDINE DERIVATIVES

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##

MACROCYCLIC COMPLEXES OF ALPHA-EMITTING RADIONUCLIDES AND THEIR USE IN TARGETED RADIOTHERAPY OF CANCER

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”) where the compounds are represented by the following:

##STR00001## or a pharmaceutically acceptable salt thereof,

##STR00002## or a pharmaceutically acceptable salt thereof,

##STR00003## or a pharmaceutically acceptable salt thereof,
wherein M.sup.1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.

Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer

The present technology provides compounds as well as compositions including such compounds useful in targeted radiotherapy of cancer and/or mammalian tissue overexpressing prostate specific membrane antigen (“PSMA”) where the compounds are represented by the following: ##STR00001## or a pharmaceutically acceptable salt thereof, ##STR00002## or a pharmaceutically acceptable salt thereof, ##STR00003## or a pharmaceutically acceptable salt thereof,
wherein M.sup.1 is independently at each occurrence an alpha-emitting radionuclide. Equivalents of such compounds are also disclosed.

Near-infrared fluorescent nerve contrast agents and methods of use thereof

The instant invention provides near-infrared fluorescent nerve contrast agents and methods of using them.

9H-PYRROLO-DIPYRIDINE DERIVATIVES

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##