Patent classifications
C07B59/001
ISOTOPE-ENRICHED 3-AMINO-1-PROPANESULFONIC ACID DERIVATIVES FOR THE TREATMENT OF CEREBROVASCULAR DISEASE
There are provided methods for treating or preventing a cerebrovascular disease in a subject in need thereof comprising administering to the subject a therapeutically effective amount of an isotope-enriched compound or a pharmaceutical composition thereof, where the isotope-enriched compound has the general Formula (I) or is a pharmaceutically acceptable salt or ester thereof:
R.sup.1R.sup.2X—CR.sub.2—CH.sub.2—CH.sub.2—SO.sub.3H (I).
ORGANIC LIGHT EMITTING DEVICE
The present disclosure relates to an organic light emitting device that includes a substrate; and an organic light emitting diode positioned on the substrate and including a first electrode; a second electrode facing the first electrode; a first emitting material layer including a first dopant of a boron derivative and a first host of an anthracene derivative and positioned between the first and second electrodes; a first electron blocking layer including an electron blocking material of amine derivative and positioned between the first electrode and the first emitting material layer; and a first hole blocking layer including a hole blocking material and positioned between the second electrode and the first emitting material layer, wherein the first host is deuterated.
PROCESS FOR THE PRODUCTION OF SUBSTITUTED 2-[2-(PHENYL)ETHYLAMINO]ALKANEAMIDE DERIVATIVES
The present invention refers to a process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R is (C.sub.3-C.sub.10)alkyl, or ω-trifluoro(C.sub.3-C.sub.10)alkyl; R.sub.1 and R.sub.2 are, independently, hydrogen, hydroxy, (C.sub.1-C.sub.8) alkoxy, (C.sub.1-C.sub.8) alkylthio, halo, trifluoromethyl or 2,2,2-trifluoroethyl; or one of R.sub.1 and R.sub.2 is in ortho position to the R—O— group and, taken together with the same R—O—, represents a Formula (A) group where R.sub.0 is (C.sub.2-C.sub.9)alkyl; R.sub.3 and R.sub.4 are, independently, hydrogen, (C.sub.1-C.sub.4)alkyl; or R.sub.4 is hydrogen and R.sub.5 is a group selected from —CH.sub.2—OH, —CH.sub.2—O—(C.sub.1-C.sub.6)alkyl, —CH(CH.sub.3)—OH, —(CH.sub.2).sub.2—S—CH.sub.3, benzyl and 4-hydroxybenzyl; or R.sub.4 and R.sub.5, taken together with the adjacent carbon atom, form a (C.sub.3-C.sub.6)cycloalkyl residue; R.sub.5 and R.sub.6 are independently hydrogen or (C.sub.1-C.sub.6)alkyl; or taken together with the adjacent nitrogen atom form a 5-6 membered monocyclic saturated heterocycle, optionally containing one additional heteroatom chosen among —O—, —S— and —NR.sub.7— where R.sub.7 is hydrogen or (C.sub.1-C.sub.6) alkyl; and wherein optionally one or more hydrogen atom in the groups R, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6, preferably in the R group, can be substituted by a deuterium atom.
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Resveratrol derivative and anti-fibrotic method using the same
A resveratrol derivative of the compound of formula I or a pharmaceutically acceptable salt thereof are effective for treating a fibrotic disease.
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In formula I, R.sub.1 is hydrogen or C.sub.1-C.sub.4 alkyl, R.sub.2 and R.sub.3 are each independently C.sub.1-C.sub.3 alkyl or C.sub.1-C.sub.3 deuterated alkyl, and R.sub.2 and R.sub.3 are the same or different; the C.sub.1-C.sub.4 alkyl or C.sub.1-C.sub.3 alkyl is optionally substituted with one or more substituents each independently selected from the group consisting of halogen (for example, fluorine, chlorine, bromine, iodine), methyl, hydroxyl, ethyl, amino, methoxy, and nitro; and R.sub.4 and R.sub.5 are substituted or unsubstituted C.sub.1-C.sub.3 alkyl. The fibrotic disease is selected from the group consisting of liver fibrosis, lung fibrosis, kidney fibrosis, and cardiac fibrosis.
Radiopharmaceutical compositions of radioactive halogenated benzylguanidine
The present disclosure concerns radiopharmaceutical compositions of radioactive halogenated benzylguanidine (such as radioiodinated MIBG) or a pharmaceutically acceptable salt, hydrate, or solvate thereof. In a preferred embodiment, the composition has at least 97% of radiochemical purity for at least 4 days. Advantageously, the compositions of the present disclosure may be devoid of parabens, which are carcinogenic and yet are used in known radioactive MIBG compositions. The present disclosure also provides processes of preparing a radioactive halogenated benzylguanidine composition. The compositions of the present disclosure can be used in diagnosis and treatment of various diseases.
DIRECT AROMATIC CARBON-OXYGEN AND CARBON-HYDROGEN BOND FUNCTIONALIZATION VIA ORGANIC PHOTOREDOX CATALYST
The invention generally relates to methods of making substituted arenes via direct C—H, C—O, C—S, or C—N bond conversion and methods of synthesizing isotopically-labeled substituted arenes via direct carbon-halogen bond conversion. The invention also relates to anaerobic catalyst systems comprising an acridinium photocatalyst and a nucleophile selected from a halide, a cyanide, and an isotopically-labeled amine. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
Arylcyclohexylamine derivatives and their use in the treatment of psychiatric disorders
Provided herein are arylcyclohexylamine derivatives and their use in the treatment of psychiatric disorders.
4-HYDROXYBUTYRIC ACID ANALOGS
This invention relates to novel derivatives of 4-hydroxybutyric acid and prodrugs thereof, and pharmaceutically acceptable salts of the foregoing. This invention also provides pharmaceutical compositions comprising a compound of this invention and the use of such compositions in methods of treating narcolepsy, fibromyalgia, other disorders or conditions that are beneficially treated by improving nocturnal sleep or by administering sodium oxybate.
CERAMIDES AND THEIR USE IN DIAGNOSING CVD
The present invention inter alia provides a method, and use thereof, of predicting CV complications such as AMI, ACS, stroke, and CV death by determining the concentrations of at least one ceramide of Group A and at least one ceramide of Group B in a biological sample and comparing those concentrations to a control. Finding a decreased concentration of at least one Group A ceramide and an increased concentration of at least one Group B ceramide indicates that the subject has an increased risk of developing one or more CV complications. Also provided are a newly identified subset of ceramide molecules, labelled versions thereof, and kits and compositions comprising the same for use in predicting and/or diagnosing CV complications.
FLUORINATION METHOD
The invention relates to a process for producing a compound comprising the anion [CF.sub.2.sup.18FSO.sub.2]−, which process comprises treating a difluorocarbene source with (i) a source of .sup.18F.sup.− and (ii) a source of SO.sub.2. The invention relates to a compound which comprises that anion. The invention also relates to the use of the compound comprising the anion [CF.sub.2.sup.18FSO.sub.2].sup.− to produce a compound comprising an .sup.18F-trifluormethyl functionalised aromatic group. Compounds comprising an .sup.18F-trifluoromethyl functionalised aromatic group are also the subject of the present invention.