C07B59/001

Isobaric Multiplex Reagents for Carbonyl Containing Compound High-Throughput Quantitative Analysis

The present invention provides a set of novel isobaric chemical tags, also referred herein as SUGAR (Isobaric Multiplex Reagents for Carbonyl Containing Compound). These labeling tags are compact and easy to synthesize at high yield and purity in just a few steps using commercially available starting materials. The tagging reagents of the present invention comprise: a) a reporter group, having at least one atom that is optionally isotopically labeled; b) a balancing group, also having at least one atom that is optionally isotopically labeled, and c) an aldehyde, ketone, or carboxylic acid reactive group. The multiplex SUGAR tags are able to react with an aldehyde, ketone, or carboxylic acid group of the molecule to be tagged, which offers the capability for labeling and quantitation of glycans, proteins/peptides, and fatty acids.

DEUTERATED NICLOSAMIDE
20230102999 · 2023-03-30 ·

This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt, and/or hydrate, and/or cocrystal, and/or drug combination of the compound) that exhibit activity as mitochondrial uncoupling agents. Said chemical entities are useful, e.g., for treating one or more symptoms of a pathology characterized by an abnormal inflammatory response (e.g., inflammatory bowel diseases) in a subject (e.g., a human). This disclosure also features compositions containing the same as well as methods of using and making the same.

A NEW METHOD OF 18F LABELLING AND INTERMEDIATE SALTS

##STR00001##

Disclosed herein is a salt of formula I: where R.sup.1, X, n, R, R.sup.1, Y, m, p, q, Z and o are as defined herein. Also disclosed herein are methods of using said salts in chemical synthesis, such as to prepare compounds isotopically enriched in 18F for use in PET & imaging, as well as methods to make the compounds of formula I.

ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC DEVICE

An organic EL device includes a first emitting layer and a second emitting layer, in which the first emitting layer contains a first host material, the second emitting layer contains a second host material, the first and the second host material are mutually different, the first emitting layer and the second emitting layer at least contains a compound that emits fluorescence having a main peak wavelength of 500 nm or less, respectively, the compound contained in the first emitting layer and that emits fluorescence having a main peak wavelength of 500 nm or less is the same as or different from the compound contained in the second emitting layer, and a triplet energy T.sub.1(H1) of the first host material and a triplet energy T.sub.1(H2) of the second host material satisfy a numerical formula (Numerical Formula 1),


T.sub.1(H1)>T.sub.1(H2)  (Numerical Formula 1).

ORGANIC ELECTROLUMINESCENT ELEMENT AND ELECTRONIC DEVICE
20220348523 · 2022-11-03 · ·

An organic electroluminescence device includes an anode, a cathode, a first emitting layer, and a second emitting layer provided between the first emitting layer and the cathode, in which the first emitting layer includes, as a first host material, a first compound that includes at least one group represented by a formula (11) below, the first compound being represented by a formula (1) below, the second emitting layer includes a second compound represented by a formula (2A) below as a second host material, and the first emitting layer is in direct contact with the second emitting layer.

##STR00001##

ISOTOPES OF ALPHA KETOGLUTARATE AND RELATED COMPOUNDS AND THEIR USE IN HYPERPOLARIZED IMAGING

A compound of the Formula I or a pharmaceutically acceptable salt thereof, wherein R.sub.1, Ca, Cb, Cd, and n are the same as described in the specification. Disclosed is a method of diagnosing or monitoring a patient suffering from cancer, the method comprising: administering a pharmaceutical composition comprising an effective amount of an active agent, wherein the active agent is the compound of Formula I, a pharmaceutically acceptable salt of any of the foregoing thereof, or a combination thereof, together with a pharmaceutically acceptable carrier to the patient and diagnosing or monitoring the patient by hyperpolarized .sup.13C-MRI. Also disclosed is a method of synthesizing 1-.sup.13C-5-.sup.12C-diacid.

##STR00001##

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 Z allylic 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.

ORGANIC COMPOUND, LIGHT-EMITTING DEVICE, DISPLAY APPARATUS, ELECTRONIC DEVICE, LIGHT-EMITTING APPARATUS, AND LIGHTING DEVICE

A novel organic compound that is highly convenient, useful, or reliable is provided. The organic compound is represented by General Formula (G1). Note that at least one of R.sup.1 to R.sup.26 represents deuterium. At least one of R.sup.1 to R.sup.7 represents any one of an alkyl group, a cycloalkyl group, a trialkylsilyl group, and an aryl group. The others of R.sup.1 to R.sup.7 each independently represent any one of hydrogen, an alkyl group, a cycloalkyl group, a trialkylsilyl group, and an aryl group. R.sup.8 to R.sup.26 each independently represent any one of hydrogen, an alkyl group, a cycloalkyl group, a trialkylsilyl group, and an aryl group. The alkyl group has 3 to 10 carbon atoms, the cycloalkyl group has 3 to 10 carbon atoms, the trialkylsilyl group has 3 to 12 carbon atoms, and the aryl group has 6 to 25 carbon atoms.

HETEROCYLIC COMPOUND AND LIGHT-EMITTING DEVICE AND ELECTRONIC APPARATUS INCLUDING THE HETEROCYCLIC COMPOUND

A light-emitting device includes: a first electrode; a second electrode facing the first electrode; and an interlayer between the first electrode and the second electrode and including an emission layer, wherein the interlayer includes a heterocyclic compound of Formula 1:


A.sub.1private use character BrketopenstB.sub.1].sub.n1  Formula 1

wherein, in Formula 1, the variables are defined herein.

Neuro-attenuating ketamine and norketamine compounds, derivatives thereof, and methods

The present invention is directed to novel neuro-attenuating norketamine (NANKET) compounds according to any one of formulas (I—shown below), (I-A) and (I-B), or any of the compounds described in Tables A-D, or in any of the Examples provided herein, and pharmaceutically acceptable salts thereof, novel pharmaceutical formulations and novel methods of uses thereof. The present invention also features novel oral neuro-attenuating ketamine (NAKET) and neuro-attenuating norketamine (NANKET) modified-release pharmaceutical formulations, and novel methods of administration thereof, which ensure the steady release of a therapeutically effective amount of ketamine, norketamine, or derivatives thereof from the oral modified-release pharmaceutical formulations without neurologically toxic spikes in plasma concentration of the ketamine, norketamine, or derivatives during the release periods. ##STR00001##