Abstract: This invention relates to a process for preparing a calixarene compound by reacting a phenolic compound and an aldehyde in the presence of at least one nitrogen-containing base as a catalyst to form the calixarene compound. The invention also relates to processes for high-yield, high solid-content production of a calixarene compound, with high selectivity toward a high-purity calix[8]arene compound, without carrying out a recrystallization step.

Abstract: What is proposed is a continuous process for producing limonene which has the feature that beta-pinene or beta-pinene-containing starting materials are isomerized in a trickle-bed reactor in the presence of acid catalysts.

Abstract: The present disclosure relates to a process and a device for producing vinyl acetate by an ethylene process. By additionally arranging an ethylene recovery membrane assembly in a vinyl acetate synthesis section, the content of inert components such as nitrogen in a circulating system is controlled, ethylene gas is recovered from non-condensable gas, and a recovery rate of the ethylene reaches 58% or above. By adding sideline extraction at a refined VAC tower in a vinyl acetate refining section, a vinyl acetate product with purity higher than 99.98% is obtained, a mass fraction of acetic acid is less than or equal to 20 ppm, a mass fraction of acetaldehyde is less than or equal to 20 ppm, and a mass fraction of water is less than or equal to 100 ppm. In synthesis and refining processes of the vinyl acetate, a cooling method is adopted.

Abstract: Methods for preparing conjugated dienes are described. An ?,?-unsaturated E olefin intermediate may be prepared via cross-metathesis using a catalyst comprising a transition metal (e.g., ruthenium), a first carbene ligand (e.g., a substituted indenylidene) and an N-heterocyclic carbene ligand (e.g., an imidazolidinylidene). The catalyst further includes a phenylphosphine ligand, a tri(isopropoxy)phosphine ligand, a dimethylsulfoxide ligand, an acetonitrile ligand, or a pyridine ligand. Following the cross metathesis-step, the ?,?-unsaturated aldehyde intermediate may be converted to the conjugated diene product via reaction with a phosphonium ylide. Products obtained via the methods of the disclosure include (7E,9Z)-dodeca-7,9-dien-1-yl acetate, a pheromone produced by Lobesia botrana (European grapevine moth), and other insect pheromones.

Abstract: The present invention provides: novel compounds capable of producing monomethyl fumarate after the compounds are administered; pharmaceutical compositions comprising same as active ingredients; and pharmaceutical uses thereof for treating or alleviating various diseases including immune system abnormalities, neurodegeneration, and/or inflammatory diseases.

Abstract: A compound represented by the general formula (V) wherein all the symbols are as defined in the specification, has an improved balance of the agonist activity against the S1P5 receptor relative to the S1P1 receptor, and can thus serve as a therapeutic agent for S1P5-mediated diseases such as schizophrenia and Binswanger's disease and other neurodegenerative diseases.

Abstract: Provided herein are formulations, processes, solid forms and methods of use relating to (E)-1-(4-(1-(((4-cyclohexyl-3-(trifluoromethyl)benzyl)oxy)imino)ethyl)-2-ethylbenzyl)azetidine-3-carboxylic acid.

Abstract: The present disclosure provides a composition comprising crystalline forms A, B, and C of psilocin and psilocybin. Solvent screen, X-ray powder diffractogram, thermogravimetric mass spectroscopy, differential scanning calorimetry, 1H-NMR, dynamic vapor sorption, and UPLC data on each of the crystalline forms is presented, along with methods preparing each of the crystalline forms.

Abstract: Described herein, in part, are dosage forms and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a T-type calcium channel, such as epilepsy and epilepsy syndromes (e.g., absence seizures, juvenile myoclonic epilepsy, or a genetic epilepsy), tremor (e.g., essential tremor), and psychiatric disorder (e.g., mood disorders (e.g., major depressive disorder)). The present invention further comprises methods for modulating the function of a T-type calcium channel.

Abstract: Methods of hydromethylation of alkenes and ketones, including methods that use Tebbe's reagent. The methods may include contacting Cp2Ti(?-Cl)(?-CH2)AlMe2 and an alkene or a ketone to produce an intermediate product that may include a titanacyclobutane. The intermediate product may be contacted with an acid to produce a methylated product.

Abstract: The invention relates to the field of pesticide technology, and in particular a type of pyridyloxy carboxylate derivative, preparation method, herbicidal composition and application thereof. The pyridyloxy carboxylate derivative is represented by formula I, wherein, A, B each independently represent halogen, or alkyl or cycloalkyl with or without halogen; C represents hydrogen, halogen, alkyl or haloalkyl; Q represents halogen, cyano, cyanoalkyl, hydroxyalkyl, amino, nitro, formyl, alkyl with or without halogen or the like; M represents -alkyl-R, R represents unsubstituted or substituted heterocyclyl, aryl or heteroaryl; Y represents O or S; X represents nitro or NR1R2. The compound has excellent herbicidal activity and higher crop safety, especially good selectivity for key crops such as rice and soybean.

Abstract: Highly efficient process for the preparation of 4-Fluoro-1H-pyrazole or salts thereof by reaction of pyrazole with an electrophilic fluorinating reagent is disclosed.

Abstract: The invention relates to new 1:1 olaparib:hydroxybenzoic acid cocrystals. The invention also relates to new 2:1 olaparib:hydroxybenzoic acid cocrystals which may contain no water (anhydrous) or may optionally be hydrated. The invention also relates to pharmaceutical compositions containing an olaparib hydroxybenzoic acid cocrystal of the invention and a pharmaceutically acceptable carrier. The olaparib hydroxybenzoic acid cocrystals of the invention may be useful for the treatment of diseases that benefit from inhibition of poly (ADP-ribose) polymerase (PARP).

Abstract: A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic ?-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.

Abstract: A 5-((2-isopropyl-5-methylphenoxy)methyl)-3-(naphthalen-1-yl)-1,2,4-oxadiazole compound, its synthesis, and its use as an antimicrobial agent.

Abstract: The disclosure provides therapeutic compositions (i.e., therapeutic agents) and methods of preventing or treating Friedreich's ataxia in a mammalian subject, reducing risk factors, signs and/or symptoms associated with Friedreich's ataxia (e.g., Complex I deficiency), and/or reducing the likelihood or severity of Friedreich's ataxia. The disclosure further provides novel intermediates for the production of said therapeutic compositions and related reduced versions of said therapeutic compositions, which reduce forms may also be used as therapeutic agents (or prodrugs of the therapeutic agent(s)).

Abstract: The present disclosure provides processes for the purification of 2,5-furandicarboxylic acid (FDCA). The present disclosure further provides crystalline preparations of purified FDCA, as well as processes for making the same. In addition, the present disclosure provides mixtures used in processes for the purification of FDCA.

Abstract: A process for preparing a batch of highly purified, pharmaceutical grade tasimelteon comprises analyzing a batch of tasimelteon synthesized under GMP conditions for the presence of one or more identified impurities.

Abstract: A compound of formula IVa includes two or three R1a to R4a groups which represent hydrogen, and the R1a to R4a groups not being hydrogen represent a group CH2—O—R6, CH2—O—C(?O)—R7, or —CH2—NR8R9, with R6 to R9 being a linear or branched alkyl group, alkoxy group, polyalkoxy group, or alkenyl group with at maximum 30 carbon atoms.

Abstract: A compound 3-(4,5-Diphenyl-2-(pyridin-3-yl)-1H-imidazol-1-yl)-N,N-dimethylpropan-1-amine, its synthesis, and its use as an anticancer agent.

Abstract: Disclosed herein are nitrogen-containing bicyclic compounds of Formula (I), including pharmaceutically acceptable salts thereof, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein.

Abstract: This invention provides quinazoline derivatives represented by the structural formula: (I); wherein: R2 is hydrogen, NR?R?, C1-7alkyl, arylC1-7 alkyl or C3-10 cycloalkyl; R4 is amino, C1-7alkyl, C2-7 alkenyl, C3-10 cycloalkyl, C3-10 cycloalkenyl, aryl, heterocyclic, arylalkyl, heterocyclic-substituted C1-7alkyl or C3-10 cycloalkyl-C1-7 alkyl; R5 is hydrogen or C1-7 alkyl, or R5 and R4 together with the nitrogen atom to which they are attached form a heterocyclic ring; Y is a single bond, C1-7alkylene, C2-7 alkenylene or C2-7 alkynylene; R6 is halogen, heteroaryl or aryl; R? and R? are each independently hydrogen, C1-7 alkyl-carbonyl or C1-7 alkyl; provided that R4 is not phenyl substituted with morpholino when R2 is H and R5 is H, and provided that when NR4R5 is piperazinyl, said NR4R5 is either non-substituted or substituted with methyl or acetyl; a pharmaceutically acceptable addition salt, a stereoisomer, a mono- or a di-N-oxide, a solvate or a pro-drug thereof, for the treatment of viral infections.

Abstract: The present disclosure relates to tri-substituted aryl and heteroaryl derivatives. pharmaceutical compositions containing them, and methods of using them, including methods for modulating autophagy or preventing, reversing, slowing or inhibiting the PI3K-AKT-MTOR pathway, and methods of treating diseases that are associated with autophagy or the PI3K-AKT-MTOR pathway.

Abstract: The present disclosure relates to a novel crystalline form of Tolebrutinib (hereinafter referred to as “Compound I”) and preparation methods thereof, pharmaceutical compositions containing the crystalline form, and uses of the crystalline form for preparing BTK inhibitor drugs and drugs for treating multiple sclerosis.

Abstract: BRD9 protein degradation compounds or pharmaceutically acceptable salts thereof are provided for the treatment of disorders mediated by BRD9, including but not limited to abnormal cellular proliferation.

Abstract: The present invention is directed to compounds of Formula I: or a pharmaceutically acceptable salt thereof, wherein the substituents A, R1, R2, R3a, R3b, R4a, R4b and n are as defined herein. The inventions also directed to pharmaceutical compositions comprising the compounds, methods of treatment using the compounds and methods of preparing the compounds.

Abstract: The present disclosure relates to compounds of formula (I?) and pharmaceutically acceptable salts thereof useful as inhibitors of Ubiquitin Specific Peptidase 30 (USP30), pharmaceutical compositions thereof, and methods of use thereof. Compounds as disclosed herein can be useful in the treatment of a disease or disorder involving mitochondrial dysfunction, including neurodegenerative diseases.

Abstract: This disclosure features chemical entities (e.g., a compound or a pharmaceutically acceptable salt thereof, or an N-oxide thereof) of formula (I), which are positive allosteric modulators of one or more GABA-A receptors, e.g., which are peripherally restricted, positive allosteric modulators of one or more GABA-A receptors; e.g., which are positive allosteric modulators of one or more GABA-A receptors and which selectively target the peripheral nervous system and organs of the body, and which do not substantially pass through the blood-brain barrier. Said compounds are useful e.g., for the treatment of systemic diseases of the body, e.g., diseases in which modulation of one or more peripherally restricted GABA-A receptors is beneficial (e.g., diseases or disorders which are mediated by GABA-A neuronal activity. This disclosure also features pharmaceutical compositions containing the chemical entities described herein as well as methods of using same for the treatment of systemic diseases of the body.

Abstract: The present disclosure relates to a plurality of host materials comprising a compound represented by formula 1 and a compound represented by formula 2, and an organic electroluminescent device comprising the same. By comprising the plurality of host materials comprising a specific combination of compounds, it is possible to provide an organic electroluminescent device having long lifespan characteristics.

Abstract: A compound in which a xanthene colorant is bonded to an optical absorber (Dye) with optical absorption in the wavelength range of 350 to 700 nm.

Abstract: The present disclosure provides novel synthetic intermediates useful in the synthesis of MK2 kinase inhibitors.

Abstract: Compounds, compositions, and methods for use in inhibiting the E3 enzyme Cbl-b in the ubiquitin proteasome pathway are disclosed. The compounds, compositions, and methods can be used to modulate the immune system, to treat diseases amenable to immune system modulation, and for treatment of cells in vivo, in vitro, or ex vivo. Also disclosed are pharmaceutical compositions comprising a Cbl-b inhibitor and a cancer vaccine, as well as methods for treating cancer using a Cbl-b inhibitor and a cancer vaccine; and pharmaceutical compositions comprising a Cbl-b inhibitor and an oncolytic virus, as well as methods for treating cancer using a Cbl-b inhibitor and an oncolytic virus.

Abstract: The present specification relates to a heterocyclic compound represented by Chemical Formula 1, and an organic light emitting device including the same.

Abstract: Provided are an organometallic compound, an organic light-emitting device including the same, and a diagnostic composition including the same.

Abstract: Disclosed are acyclic nucleoside prodrugs with improved metabolic stability and oral bioavailability. In general, the prodrugs are derivatives of acyclic nucleoside phosphonates containing a lipid-like moiety that can increase oral absorption and subsequent stability in the liver and plasma. Preferably, the lipid-like moiety can resist enzyme-mediated ?-oxidation, such as ?-oxidation catalyzed by cytochrome P450 enzymes. Also disclosed are pharmaceutical formulations of the acyclic nucleoside prodrugs. The acyclic nucleoside prodrugs and pharmaceutical formulations thereof can be used to treat viral infections, such as HIV infections, and/or viral-associated cancer, such as HPV-associated cancers.

Abstract: Provided herein are novel conjugates of TGF-beta inhibitors and bisphosphonates, pharmaceutical compositions comprising the conjugates, methods of preparing the conjugates, and methods of using the conjugates, for example, for the treatment of a bone disease or disorder, such as osteoarthritis.

Abstract: The present invention provides processes for preparing soluble salts of inositol phosphate characterized by a low level of impurities. Processes for preparing soluble salts (e.g., alkali-metal or ammonium) of inositol phosphates (e.g., hexasodium or dodecasodium salts), and of inositol hexaphosphate in particular (e.g., Na6IP6 and Na12IP6), are described. Also provided are pharmaceutical compositions, methods of use, combination treatments, kits, and articles of manufacture comprising soluble salts of inositol phosphates prepared according to the method of the invention.

Abstract: The invention provides novel compounds that are derivatives of Azithromycin and that have been found by the current inventors to have low antimicrobial activity but significant epithelial barrier enhancement properties. The invention further provides use of the compounds as a medicament, in particular in the treatment or prophylaxis of a disease or condition that is caused by a defect in epithelial cells or tissue, or a disease or condition that benefits from enhancement or restoration of epithelial barrier function, for example diseases of the respiratory tract.

Abstract: The present invention provides methods and compositions comprising an adeno-associated virus (AAV) capsid protein, comprising one or more amino acids substitutions, wherein the substitutions introduce a new glycan binding site into the AAV capsid protein.

Abstract: Provided herein is a nucleic acid comprising consensus amino acid sequence of foot-and-mouth disease FMDV VP1-4 coat proteins of FMDV subtypes A, Asia 1, C, O, SAT1, SAT2, and SAT3 as well as plasmids and vaccines expressing the sequences. Also provided herein is methods for generating an immune response against one or more FMDV subtypes using the vaccine as described above as well as methods for deciphering between vaccinated mammals with the vaccine and those that are infected with FMDV.

Abstract: The present invention relates to a virus-derived particle comprising one or more Cas protein(s), as well as to kits and methods using the same for altering a target nucleic acid.

Abstract: The present application relates to silk fibroin-based hydrogels, methods for making and using the same.

Abstract: The present disclosure relates to therapeutic methods and clinically useful molecular switches, for which activity or degradation of a switch-presenting polypeptide can be precisely induced via administration or withdrawal of an FDA-approved drug. Certain aspects of the disclosure relate to an engineered drug-inducible heterodimeric system including a first polypeptide presenting a CRBN polypeptide disrupted for or lacking a DDB 1-interacting domain and a second polypeptide presenting a CRBN polypeptide substrate, where binding between the CRBN polypeptide and the CRBN polypeptide substrate are inducible via administration of an CFDA-approved thalidomide analog immunomodulatory drug (IMiD). Another aspect of the disclosure relates to a chimeric antigen receptor (CAR) that presents a minimal fragment of the CRBN polypeptide substrate IKZF3 capable of triggering proteasomal degradation of CAR upon administration of an FDA-approved IMiD.

Abstract: Provided are proteins or peptides, which may be referred to as monobodies. Fusion proteins and proteolysis targeting chimeras (PROTACs) comprising the proteins or peptides are also provided. Also provided are compositions of the proteins or peptides of the present disclosure, as well as compositions of fusion proteins and compositions of PROTACs. Methods of treating an individual in need of treatment are also provided. The methods may be to treat an individual suffering from or suspected of having KRAS(G12V), KRAS(G12S), KRAS(G12A) and/or KRAS(G12C)-associated cancers. A method may be for inhibiting ERK activation and/or proliferation of KRAS(G12V), KRAS(G12S), KRAS(G12A) and/or KRAS(G12C)-associated cancers.

Abstract: The invention is in the field of medicine. More specifically, it is in the field of diagnosing tumor angiogenesis status and in the field of medical treatment of a subject who is suffering, suspected to suffer, or might suffer from a tumor in the future. In particular, the invention relates to a fusion polypeptide comprising a foreign antigen and a self antigen, wherein said foreign antigen consists of a polypeptide comprising an amino acid sequence of at least 12-15 amino acid residues, 12-24% of which residues are hydrophilic, bulky amino acid residues selected from the group consisting of histidine, glutamate, arginine, glutamine, aspartic acid and/or lysine.

Abstract: The present invention provides methods for targeting interleukin-2 receptor-expressing cells, and, in particular, inhibiting the growth of such cells by using an interleukin-2 (IL-2) variant conjugated to a biologically active molecule that will affect cells expressing the interleukin-2 receptor.

Abstract: In certain embodiments novel PAC1 receptor agonists are provided wherein the agonists comprise a targeting sequence that binds to the PAC1 receptor and said targeting sequence is attached to an amino acid sequence comprising a fragment of the maxadilan amino acid sequence, wherein the targeting sequence comprises a full-length 38 amino acid PACAP peptide or an N-terminus fragment thereof containing the amino acid sequence HSDGIF, wherein said targeting sequence optionally comprises an amino acid insertion between residues 11 and 12 of said PACAP peptide or fragment thereof; and the fragment of the maxadilan amino acid sequence comprises a fragment of the maxadilan sequence effective to activate PAC1 signaling.

Abstract: Provided are a universal chimeric antigen receptor (CAR) T cell and preparation method and application thereof. The binding of the cell HLA-A/HLA-B to the TCR is inhibited; the TCR gene expression is silenced; the invention may be used for allogeneic tumor treatment and does not cause GVHD and HVG reaction during allogeneic infusion, and thus improves the survival and antineoplastic effect of allogeneic CAR-T cells in the recipient.

Abstract: Modular synthetic receptors are provided. The synthetic receptors may include an extracellular domain capable of binding to one or more ligand molecules and may be released from the synthetic receptor after binding, a transmembrane domain derived from the Notch receptor, and an intracellular domain which may have one or more functional activities when released from the synthetic receptor. A method of use for the synthetic receptors is also provided, wherein upon binding of the extracellular domain to a specific ligand, the synthetic receptor undergoes proteolytic cleavage to release either or both the extracellular and intracellular domains. The extracellular binding domain, if released, may continue to bind to its cognate ligand and may carry one or more additional functional activities and the intracellular domain, if released, may stimulate or inhibit one or more intracellular activities.

Abstract: The present disclosure pertains to methods for producing aflibercept from a host cell cultured in a chemically defined medium (CDM) including purification of aflibercept, wherein aflibercept following purification includes aflibercept variants that have at least one oxidized amino acid residue selected from the group consisting of tryptophan, histidine and a combination thereof.