C07B59/00

MESCALINE DERIVATIVES WITH MODIFIED ACTION

A composition for use in substance-assisted therapy, wherein: R is hydrogen, methyl, or ethyl, and R′ is C.sub.1-C.sub.5 branched or unbranched alkyl with the alkyl optionally substituted with F.sub.1-F.sub.5 fluorine substituents up to a fully fluorinated alkyl, C.sub.3-C.sub.6 cycloalkyl optionally and independently substituted with one or more substituents such as F.sub.1-F.sub.5 fluorine and/or C.sub.1 - C.sub.2 alkyl, (C.sub.3-C.sub.6 cycloalkyl)-C.sub.1-C.sub.2 branched or unbranched alkyl optionally substituted with one or more substituents such as F.sub.1-F.sub.5 fluorine and/or C.sub.1-C.sub.2 alkyl, or C.sub.2-C.sub.5 branched or unbranched alkenyl with E or Z vinylic, cis or trans allylic, E or Zallylic or other double bond position in relation to the attached ether function, where any of the carbons of the branched or unbranched alkenyl substituent is optionally substituted independently with one or more C.sub.1-C.sub.2 alkyl, with F.sub.1-F.sub.5 fluorine or with D.sub.1-D.sub.5 deuteron substituents.

AMIDE-SUBSTITUTED HETEROCYCLIC COMPOUNDS FOR THE TREATMENT OF CONDITIONS RELATED TO THE MODULATION OF IL-12, IL-23 AND/OR IFN-ALPHA

Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFNα, by acting on Tyk-2 to cause signal transduction inhibition.

VISIBLE-LIGHT MEDIATED ORGANOPHOTOREDOX CATALYTIC DEUTERATION OF AROMATIC AND ALIPHATIC ALDEHYDES
20230016922 · 2023-01-19 ·

Described are methods for preparing a deuterated aldehyde using with a photocatalyst and a hydrogen atom transfer agent in a H.sub.2O free solvent comprising D.sub.2O and an organic solvent under an inert gas. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions.

VISIBLE-LIGHT MEDIATED ORGANOPHOTOREDOX CATALYTIC DEUTERATION OF AROMATIC AND ALIPHATIC ALDEHYDES
20230016922 · 2023-01-19 ·

Described are methods for preparing a deuterated aldehyde using with a photocatalyst and a hydrogen atom transfer agent in a H.sub.2O free solvent comprising D.sub.2O and an organic solvent under an inert gas. The methods may be used to convert a wide variety of aldehydes (e.g., aryl, alkyl, or alkenyl aldehydes) to C-1 deuterated aldehydes under mild reaction conditions.

IMAGING METHODS USING DEUTERATED COMPOUNDS

The present invention relates to deuterated and optionally detectably labeled compounds of formula (I) and formula (V):

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and salts thereof, wherein R.sup.1, R.sup.2, A, and X.sub.10-X.sub.19 have any of the values defined in the specification. Also included are pharmaceutical compositions comprising such compounds and salts, and methods of using such compounds and salts as imaging agents.

METHOD FOR PREPARING DEUTERATED AROMATIC COMPOUND, AND DEUTERATED REACTIVE COMPOSITION
20230018666 · 2023-01-19 ·

The present specification relates to a method for producing a deuterated aromatic compound and a deuterated reaction composition.

Composition, and Electronic Device and Organic Light-Emitting Device Comprising Same

The present specification relates to a composition including two or more compounds represented by Chemical Formula 1 and having a different number of deuterium substitution, wherein, in the composition, the number of deuterium of an isotope having a highest isotope content among each isotope content for each mass number of the two or more compounds having a different number of deuterium substitution is 13 or greater, and an electronic device and an organic light emitting device including the same.

Compounds and methods for DCAF-mediated protein degradation

Disclosed herein are methods and compounds for inducing DDB1- and CUL4-associated factor 16 (DCAF16)-mediated protein degradation in mammalian cells. In some embodiments, also disclosed herein are methods of modulating the substrate selectivity of a DCAF16-CUL4-RBX1-DDB1 complex (CRL4) for modulating protein degradation.

2-alkoxy-6-[18F]fluoronicotinoyl substituted lys-c(O)-glu derivatives as efficient probes for imaging of PSMA expressing tissues

6-[.sup.18F]Fluoro-2-alkoxynicotinoyl substituted Lys-C(O)-Glu derivatives were identified as efficient imaging probes for PSMA expressing tissues in comparison to other known PSMA specific ligands like [.sup.18F]DCFPyL, [.sup.68Ga]HBED-CC-PSMA, [.sup.18F]PSMA-1007 and [Al.sup.18F]HBED-CC-PSMA. Unexpectedly, the 6-[.sup.18F]fluoro-2-alkoxy and 6-[.sup.18F]fluoro-4-alkoxy substituted analogs showed significant differences in accumulation in PSMA expressing prostate tumor cells. Whereas the 2-alkoxy derivative showed cellular uptake values higher than [.sup.18F]DCFPyL, the cellular uptake of the corresponding 4-alkoxy substituted derivative was significantly lower. Furthermore, in vivo PET studies with 2-alkoxy-substituted probes demonstrated excellent visualization of PSMA positive ganglia with extremely high target to background ratio. In contrast, the 4-alkoxy substituted derivatives showed less favorable biodistribution with significantly lower uptake in PSMA positive tissues. Especially, the .sup.18F-labeled 2-methoxy derivate ((2S)-2-({[(1S)-1-carboxy-5-[(6-[.sup.18F]fluoro-2-methoxypyridin-3-yl)formamido]pentyl]carbamoyl}-amino)pentanedioic acid) demonstrated exceptional clinical efficiency in detecting small PCa lesions, including those which could not be visualized with [.sup.68Ga]HBED-CC-PSMA representing currently the gold standard for the diagnosis of recurrent PCa. Furthermore, this probe is easily accessible on a preparative scale in commercially available automated synthesis modules like GE FASTlab and TRACERlab FX N Pro. Consequently, the novel probe is a valuable tool for the visualization of ganglia and reendothelialization as well as for the diagnosis of glioma, neuropathic pain and atherosclerotic plaques.

Low affinity poly(AD-ribose) polymerase 1 dependent cytotoxic agents

The present disclosure provides compounds of Formula (I) or (II), pharmaceutically acceptable salt, isotopic variant, stereoisomer, or a mixture thereof. Also provided are pharmaceutical compositions comprising a compound, methods of treating a poly(ADP-ribose)polymerase-1-mediated disease or disorder in a subject, methods of detecting a poly(ADP-ribose)polymerase-1-mediated neurodegenerative disease or disorder, or methods of monitoring cancer treatment in a subject. In some embodiments, the poly(ADP-ribose)polymerase-1-mediated disease or disorder is a neurodegenerative disease or cancer. ##STR00001##