Abstract: An objective of the present invention is to provide methods of producing a cyclic organic compound using a continuous stirred tank reactor(s) (CSTR), the methods being capable of achieving excellent impurity-suppressing effects (quality improvement), reduction in reaction-tank size, continuous production, and such. The present inventors conducted studies on cyclization reactions using a CSTR(s), which had not been conventionally used for cyclization reactions for cyclic compounds. As a result, the inventors have found that the present methods can achieve excellent impurity-suppressing effects (quality improvement), reduction in reaction-tank size, continuous production, and such, as compared with conventional cyclization methods.

Abstract: Disclosed are non-natural peptides useful for the treatment and prevention of ischemia-reperfusion injury (e.g., cardiac ischemia-reperfusion injury) or myocardial infarction.

Abstract: Provided is an organic compound represented by the general formula [1]: in the formula [1], R1 to R18 each represent a hydrogen atom, an alkyl group having 1 or more and 8 or less carbon atoms, an aromatic hydrocarbon group having 6 or more and 18 or less carbon atoms, or an aromatic heterocyclic group having 3 or more and 15 or less carbon atoms, and may be identical to or different from each other, and the plurality of R17's or the plurality of R18's may be identical to or different from each other, and the R1 to the R18 may each further have a substituent selected from a halogen atom and an alkyl group having 1 or more and 8 or less carbon atoms, and n represents an integer of 1 or more and 3 or less.

Abstract: Provided herein are benzimidazole derivatives, for example, of Formula I, and pharmaceutical compositions thereof. Also provided herein are methods of their use for treating, preventing, or ameliorating one or more symptoms of a proliferative disease.

Abstract: Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy.

Abstract: In one aspect, use of compounds as active agents to treat a hearing impairment and to prevent a hearing impairment, and methods of treating and/or preventing hearing impairments or disorders using the compositions are disclosed. Momelotinib and Fedratinib exhibit excellent protection against antibiotic-induced hearing loss in zebrafish and mice when administered prophylactically. In one aspect, Momelotinib or Fedratinib can be used as a therapy for the treatment and/or prevention of hearing loss. 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.

Abstract: A compound represented by the following formula (1), wherein X1 is O or S, and two or more of Y1, Y2 and Y3 are N, provided that the case where one or both of —Ar1-Ar2 and —Ar3-Ar4 is a p-terphenyl-3-yl group is excluded.

Abstract: Disclosed herein are compositions, supramolecular assemblies, crystalline compositions, and methods of making and using the same. The composition comprises an organic ion and a counterion, wherein the organic ion comprises a molecular hub and arms extending therefrom and wherein the organic ion is capable of adopting a tripodal conformation.

Abstract: A color vision correction filter includes a least one type of dye material and the lowest value of transmittance of the color vision correction filter in a wavelength band ranging from 440 nm to 600 nm, inclusive, is in the range of plus or minus 50 nm of 535 nm.

Abstract: The present disclosure relates to novel synthetic method of making 1, 4-diazo N-heterocycles via intermolecular amphoteric diamination of allenes, and to the compounds made by the novel synthetic method.

Abstract: The invention relates to compositions and methods for inhibiting macrophage activation via modulating PARP9 and/or PARP14 expression or activity, such as small molecules, RNAi and antibodies.

Abstract: The present application discloses a color resist material, a filter, and a preparation method thereof. The color resist material is a trimer structure formed by polymerizing phthalocyanine dyes, wherein groups with double bonds are introduced on the phthalocyanine dyes to construct a three-molecule complex by a complexing agent, and the phthalocyanine dyes are connected by the double bonds to form a trimer structure. The color resist material with the trimer structure is stably stored in a photoresist liquid and has excellent solvent resistance, while maintains good solubility. Accordingly, a filter made of the color resist material has high transmittance and good optical performance.

Abstract: A 5A5B6C tricyclic spironolactone derivative is provided with a formula XI: The present invention also relates to its preparation method and its applications in the areas of insecticide, nematicide, fungicide and anti-viral agent. The 5A5B6C tricyclic spironolactone derivatives in the present invention are high-performance, broad-spectrum, low-toxicity and low-ecological risk compounds with a wide range of applications in the areas of agriculture, horticulture, forestry and health.

Abstract: A process for preparing pyrimido[4,5-g]pteridine-2,4,7,9-tetraol, or a salt thereof, is provided. A process for the preparation of 3,6-diaminopyrazine-2,5-dicarboxylic acid, or a salt thereof, from pyrimido[4,5-g]pteridine-2,4,7,9-tetraol, or a salt thereof, is further provided. A process for preparing a substituted pteridine compound, or a salt thereof, is further provided. A process for the preparation of a N-substituted 3,6-diaminopyrazine-2,5-dicarboxylic acid from a substituted pteridine compound, or a salt thereof, is further provided.

Abstract: Some embodiments of the invention include inventive compounds (e.g., compounds of Formula (I)). Other embodiments include compositions (e.g., pharmaceutical compositions) comprising the inventive compound. Still other embodiments of the invention include compositions (e.g., pharmaceutical compositions) for treating, for example, certain diseases using the inventive compounds. Some embodiments include methods of using the inventive compound (e.g., in compositions or in pharmaceutical compositions) for administering and treating (e.g., diseases such as cancer). Further embodiments include methods for making the inventive compounds. Additional embodiments of the invention are also discussed herein.

Abstract: Various aspects of this patent document relate to the rapid purification of cannabinoids by vaporization and condensation.

Abstract: This invention relates to macrocyclic deaza-purinones derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.

Abstract: An antitumor agent for treating a malignant tumor patient expressing EGFR having at least one mutation selected from the group consisting of G719X mutation of exon 18, E709X mutation of exon 18, and L861X mutation of exon 21, wherein X represents an arbitrary amino-acid residue, the antitumor agent comprising (S)-N-(4-amino-6-methyl-5-(quinolin-3-yl)-8,9-dihydropyrimido[5,4-b]indolizin-8-yl)acrylamide or a salt thereof.

Abstract: A genus of proteolysis-targeting chimeras (PROTACs)-type compounds/antiestrogens has now been found that act as selective estrogen receptor degraders (SERDs) and estrogen receptor antagonists by degrading and antagonizing ERa in breast cancer cells. The compounds are of the following genus: The compounds described herein exhibit anti-proliferative effects, and are potentially useful, alone or in combination with other therapies, for the treatment of breast cancer. In general, these compounds combine a tight binding ERa targeting ligand tethered to a recognition motif or degron. Once bound, the degron recruits destructive cellular components and the targeted receptor (i.e., ERa) is degraded (i.e., destroyed) or antagonized.

Abstract: The disclosure relates to rifamycin analog compounds, intermediates and precursors thereof, and pharmaceutical compositions capable of inhibiting bacterial growth (e.g., S. aureus growth) and treating bacterial infections (e.g., S. aureus infections). The disclosure further relates to antibody-drug conjugates of rifamycin analog compounds and antibodies, for example, antibodies specific for infectious disease-related targets such as membrane glycoprotein receptor (MSR1), wall teichoic acids (WTA) or Protein A, and methods of use thereof to inhibit bacterial growth and treat bacterial infections.