A61K51/0459

NON-INVASIVE PET IMAGING OF CDK4/6 ACTIVATION IN CANCER
20210338670 · 2021-11-04 ·

Disclosed are compounds having the following structure:


CDK-L-(X).sub.n,

where CDK is a CDK4/6 inhibitor group, L is a linking group, X is a radiolabel or hydrogen, n is 1, 2, 3, 4, or 5, and when there are a plurality of X groups, at least one X is a radiolabel. Also described are methods of making and using the compounds. The compounds may be used in PET imaging to quantify CDK4/6 expression in cancers and to treat cancer patients exhibiting tumors which express CDK4/6.

Compositions, methods, and systems for the synthesis and use of imaging agents

The present invention provides compounds with imaging moieties for imaging a subject. The present invention also relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, a composition or plurality of imaging agents is enriched in .sup.18F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs.

AGENT FOR DETECTING INTERACTION BETWEEN TISSUES AND ORGANS
20230364273 · 2023-11-16 · ·

The present invention relates to an agent for detecting an interaction between tissues and organs, the agent containing a compound represented by General Formula (1-0) as an active component.

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[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].

SYSTEM AND METHOD FOR SINGLE-SCAN REST-STRESS CARDIAC PET
20230346324 · 2023-11-02 ·

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.

3-(5-substituted-4-oxoquinazolin-3(4H)-yl)-3-deuteropiperidine-2,6-dione derivatives and compositions comprising and methods of using the same
11820720 · 2023-11-21 · ·

The invention provides 3-deuterium-enriched 3-(5-substituted-4-oxoquinazolin-3(4H)-yl)-piperidine-2,6-diones, deuterated derivatives thereof, stereoisomers thereof, pharmaceutically acceptable salt forms thereof, and methods of treatment using the same, such as in the treatment of cancer, an immune-related disease, or an inflammatory disease.

Synthetic cannabinoid combination therapy compositions and methods for personalized and targeted therapies including the treatment of infectious diseases
11554184 · 2023-01-17 · ·

Compositions and methods for the personalized and targeted therapeutic treatment of diseases and disorders, including the treatment of pain, inflammation, and infectious diseases in a subject. In particular, labeled synthetic cannabinoid therapeutic compositions are provided that include a conjugate of a synthetic cannabinoid compound, a chelator, and a label, that when coupled with imaging may be used to determine in real time optimal dosing and targeting of particular pathways and tissues to provide personalized therapies. Combination therapies are also provided that include one or more synthetic cannabinoid compound and at least one active pharmaceutical ingredient.

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.

Anti-neoplastic combinations and dosing regimens using CDK4/6 inhibitor compounds to treat Rb-positive tumors

This invention directed to methods for treating select RB-positive cancers and other Rb-positive abnormal cellular proliferative disorders using CDK4/6 inhibitors in specific dosing and combination or alternation regimes. In one aspect, treatments of select RB-positive cancers are disclosed using specific CDK4/6 inhibitors in combination or alternation with a Bruton's tyrosine kinase (BTK) inhibitor.

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.

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BIOREDUCTIVELY-ACTIVATED COMPOUNDS, THEIR PRODRUGS, RADIOPHARMACEUTICALS, THE COMPOSITIONS, AND THEIR APPLICATIONS IN MULTIMODAL THERANOSTIC MANAGEMENT OF HYPOXIA DISEASES INCLUDING CANCER

Described herein are bioreductively-activated compounds, their prodrugs, radiopharmaceuticals, the compositions, and their application in multimodal theranostic management of hypoxia diseases including cancer.