1699749-05-7Relevant academic research and scientific papers
Structure-activity relationship around PI-2620 highlights the importance of the nitrogen atom position in the tricyclic core
Kroth, Heiko,Oden, Felix,Serra, Andreia Monica,Molette, Jerome,Mueller, Andre,Berndt, Mathias,Capotosti, Francesca,Gabellieri, Emanuele,Schmitt-Willich, Heribert,Hickman, David,Pfeifer, Andrea,Dinkelborg, Ludger,Stephens, Andrew
, (2021/11/30)
Tau aggregates represent a critical pathology in Alzheimer's disease (AD) and other forms of dementia. The extent of Tau neurofibrillary tangles across defined brain regions corresponds well to the observed level of cognitive decline in AD. Compound 1 (PI-2620) was recently identified as a promising Tau positron emission tomography tracer for AD and non-AD tauopathies. To evaluate the impact of the N-atom position with respect to Tau- and off-target binding, tricyclic core analogs of PI-2620 with nitrogen atoms at different positions were prepared. Affinity to aggregated Tau was evaluated using human AD brain homogenates, and their off-target binding was evaluated in a monoamine oxidase A (MAO-A) competition assay. The novel tricyclic core derivatives all displayed inferior Tau binding or MAO-A off-target selectivity, indicating PI-2620 to be the optimal design for high affinity binding to Tau and high MAO-A selectivity.
TAU-PROTEIN TARGETING COMPOUNDS AND ASSOCIATED METHODS OF USE
-
Paragraph 2298; 2299, (2021/02/12)
The present disclosure relates to bifunctional compounds, which find utility as modulators of tan protein. In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a VHL or cereblon ligand which binds to the E3 ubiquitin ligase and on the other end a moiety which binds tan protein, such that tan protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of tan. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of tan protein. Diseases or disorders that result from aggregation or accumulation of tan protein are treated or prevented with compounds and compositions of the present disclosure.
NOVEL METHOD OF PREPARING AN IMAGING COMPOUND
-
Page/Page column 36; 37, (2019/08/12)
The present invention relates to a novel method of preparing a compound of the formula I. Diagnostic compositions and their use in the selective detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease (AD) and other tauopathies, for example, using Positron Emission Tomography (PET) imaging are also disclosed.
DIAGNOSTIC COMPOSITIONS FOR PET IMAGING, A METHOD FOR MANUFACTURING THE DIAGNOSTIC COMPOSITION AND ITS USE IN DIAGNOSTICS
-
Page/Page column 39; 40, (2019/08/12)
The present application relates to a diagnostic composition comprising: a. a compound of Formula I, b. ethanol, c. water, and d. a hydroxycarboxylic acid, a salt of a hydroxycarboxylic acid or a mixture thereof. The diagnostic composition can be used in the selective detection of disorders and abnormalities associated with Tau aggregates such as Alzheimer's disease (AD) and other tauopathies, for example, using Positron Emission Tomography (PET). The present invention also relates to a method of preparing the claimed diagnostic composition.
AZACARBOLINE COMPOUNDS FOR THE DETECTION OF TAU AGGREGATES
-
Page/Page column 40; 41, (2019/08/14)
The present invention relates to novel compounds of the formula (II) 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 Emissio
COMPOUNDS FOR IMAGING TAU PROTEIN AGGREGATES
-
Page/Page column 28; 29, (2018/02/22)
The present invention relates to novel compounds of the formula (I) 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.
COMPOUNDS FOR IMAGING TAU PROTEIN AGGREGATES
-
Page/Page column 30; 31, (2018/02/23)
The present invention relates to novel compounds of the formula (II) 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.
DIHYDROPYRIDOPYRROLE DERIVATIVES AS TAU-PET-LIGANDS
-
Paragraph 0102; 0107; 0108, (2017/07/31)
The present invention relates to novel compounds of formula (I) 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 Tom
Carbazole and Carboline Compounds for Use in the Diagnosis, Treatment, Alleviation or Prevention of Disorders Associated with Amyloid or Amyloid-Like Proteins
-
Paragraph 0760; 0767; 0768; 0769, (2017/01/23)
The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.
CARBAZOLE AND CARBOLINE COMPOUNDS FOR USE IN THE DIAGNOSIS, TREATMENT, ALLEVIATION OR PREVENTION OF DISORDERS ASSOCIATED WITH AMYLOID OR AMYOLID-LIKE PROTEINS
-
Page/Page column 160, (2015/08/06)
The present invention relates to novel compounds that can be employed in the diagnosis, treatment, alleviation or prevention of a group of disorders and abnormalities associated with amyloid proteins and amyloid-like proteins, such as Alzheimer's disease. Precursors for the preparation of the compounds according to the present invention are also provided.
