Patent classifications
A61K51/0453
PROINFLAMMATORY PRODRUGS
Provided herein are prodrugs comprising targeting moieties that specifically bind extracellular antigens, enzyme-cleavable linkers, and innate immune system activators. An enzyme-cleavable linker can covalently link a targeting moiety to an innate immune system activator. Also provided are methods of treating cancer, methods of imaging cancer, and methods of monitoring treatment of cancer.
Treatment of meningiomas using phenylbenzothiazole, stilbene, biphenylalkyne, or pyridine derivatives
A method and composition for treating a meningioma in a subject are disclosed. The method includes the step of administering to the subject a therapeutically effective amount of a composition including a cytotoxic agent associated with a phenylbenzothiazole derivative or a stilbene derivative or a biphenylalkyne derivative that accumulates within meningiomas. In one version of the method, the phenylbenzothiazole derivative is a compound of formula (V): ##STR00001##
Deuterium substituted positron emission tomography (PET) imaging agents and their pharmacological application
The present invention relates to deuterated compounds according to Formula I-A, Formula II-A, Formula II-D, and Formula III-A. These compounds can be used as PET imaging agents for evaluating Parkinson's Disease, Alzheimer Disease, and for determining specific serotonin reuptake inhibitor (SSRIi) activity for treatment of depression. The present invention also relates to pharmaceutical compositions comprising a pharmaceutical acceptable carrier and a compound of Formula I-A, Formulae II-A, Formula II-D, or Formula III-A, or a pharmaceutically acceptable salt thereof.
Nrf and HIF activators/HDAC inhibitors and therapeutic methods using the same
Compounds that inhibit histone (HDACI) and/or activate Nrf2 and HIF, and compositions containing the same are disclosed. Methods of treating diseases and conditions wherein inhibition of HDAC and/or activation of Nrf2 and HIF provide a benefit, like a cancer, a neurodegenerative disorder, a peripheral neuropathy, a neurological disease, traumatic brain injury, stroke, hypertension, malaria, an autoimmune disease, autism, autism spectrum disorders, and inflammation, also are disclosed.
PSMA Imaging Agents
Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.
METHODS OF DETECTING NEURODEGENERATIVE DISEASE
Among the various aspects of the present disclosure is the provision of a method for detecting neurodegenerative diseases, disorders, or conditions. Briefly, the present disclosure is directed to a non-invasive method for measuring foveal area and thickness, which has been shown to correlate with the detection of biomarkers used in the detection of neurodegenerative diseases such as Alzheimer's disease and clinical dementia.
Probes for imaging huntingtin protein
- Celia Dominguez ,
- John Wityak ,
- Jonathan Bard ,
- Christopher John Brown ,
- Michael Edward Prime ,
- Derek Alexander Weddell ,
- Daryl Simon WALTER ,
- Paul Richard GILES ,
- Ian James Wigginton ,
- Malcolm George Taylor ,
- Sébastien René Gabriel GALAN ,
- Peter David Johnson ,
- Thomas Martin KRÜLLE ,
- Inaki Morao ,
- Daniel Clark-Frew
Provided are imaging agents comprising a compound of Formula (I), or a pharmaceutically acceptable salt thereof, and methods of their use. ##STR00001##
HALOGENATED BIOTIN-MODIFIED DIMER AND USE THEREOF
An object of the present invention is to provide a halogenated biotin-modified dimer, which is capable of imaging diagnosis or treatment by labeling with a halogen, a biotin-modified dimer having a high affinity for a mutant streptavidin with a low affinity for natural biotin. The present invention provides a compound represented by the following formula (1) or a salt thereof:
##STR00001##
wherein the meaning of each symbol is the same as that described in the specification.
TRICARBONYL COMPLEXES OF TRANSITION METALS WITH BENZO-HETEROCYCLIC DERIVATIVES OF THE CYCLOPENTADIENYL ANION
Complex compounds of transition metals according to formula (1) wherein the M(CO).sub.3.sup.+ tricarbonyl-metal core forms a complex with the cyclopentadienyl anion linked to heterocyclic moieties of the benzothiazole, benzimidazole and benzoxazole families. The compounds exhibit high blood-brain barrier permeability and can be used in the diagnosis and/or treatment of diseases of the Central Nervous System.
##STR00001##
PSMA Imaging Agents
Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.