Abstract: The invention relates to inhibitors of glucosylceramide synthase (GCS) useful for the treatment of metabolic diseases, such as lysosomal storage diseases, either alone or in combination with enzyme replacement therapy, and for the treatment of cancer.

Abstract: The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations.

Abstract: This invention relates to benzodiazepine derivatives, compositions comprising therapeutically effective amounts of those derivatives and methods of using those derivatives or compositions in treating cognitive impairment associated with CNS disorders. It also relates to the use of an ?5-containing GABAA receptor agonist (e.g., an ?5-containing GABAA receptor positive allosteric modulator) in treating cognitive impairment associated with CNS disorders in a subject in need or at risk thereof, including age-related cognitive impairment, Mild Cognitive Impairment (MCI), amnestic MCI, Age-Associated Memory Impairment, Age Related Cognitive Decline, dementia, Alzheimer's Disease (AD), prodromal AD, PTSD, schizophrenia, bipolar disorder, ALS, cancer-therapy-related cognitive impairment, mental retardation, Parkinson's disease, autism spectrum disorders, fragile X disorder, Rett syndrome, compulsive behavior, and substance addiction. It also relates to the use of an ?5-containing GABAA receptor agonist (e.g.

Abstract: This invention relates to opioid ketal compounds of Formula (I), Formula (II), or Formula (III): or a pharmaceutically acceptable salts thereof, wherein R1 is H or CH3, R2 is H or OH, n is 0, 1, 2 or 3, R3 and R4 are independently or optionally substituted C1-C4 alkyl, or when n is 0, then R3 and R4 and the carbon atoms to which they are attached together form six, or seven membered ring, which is optionally mono or disubstituted by C1-C4 alkyl. The invention also relates to oxycodone ketal compounds of Formula (IV) or (V): or a pharmaceutically acceptable salts thereof. The invention also relates to the use of such compounds for the treatment, prevention, or amelioration of pain.

Abstract: Disclosed in the present invention is an aminopyrimidine five-membered heterocyclic compound, and an intermediate, preparation method, pharmaceutical composition and application thereof. The aminopyrimidine five-membered heterocyclic compound provided by the present invention has a significant antagonistic effect on adenosine A2A receptors, and may be used as an antagonist for adenosine A2A receptors to effectively relieve or treat immune tolerance, diseases of the central nervous system, inflammatory diseases and like related diseases, while the preparation method is simple.

Abstract: The invention describes a method for purification of naltrexone base from reaction mixtures concentrated by evaporation and/or from mixtures containing naltrexone in the presence of other organic or inorganic substances by trituration and/or extraction and crystallization from cyclopentyl methyl ether (CPME), optionally from a mixture of cyclopentyl methyl ether and another organic solvent. Naltrexone of high purity is obtained by this method and can be used in a parenteral dosage form.

Abstract: The present invention relates to a method for synthesizing a 3-phenyl-2,3,4,8,9,10-hexahydropyrano[2,3-f]chromene derivative and an optical isomer thereof, and an intermediate Compound which may be used for the synthesis method, and when the method and the intermediate Compound are used, the 3-phenyl-2,3,4,8,9,10-hexahydropyrano[2,3-f]chromene derivative and the optical isomer thereof may be effectively synthesized.

Abstract: The present invention provides a novel compound of an amine derivative including a spiro compound. The novel compound has excellent hole transport characteristics. Thus, when the novel compound is applied to a hole transport layer, an auxiliary hole transport layer and an electron blocking layer of an organic light-emitting device, the device realizes low driving voltage, high efficiency, high thermal stability and long life-span. Further, when the novel compound is applied as a blue light-emitting material, the device realizes a low driving voltage and high efficiency.

Abstract: A composition for preventing or treating an aging-related disease includes a novel decursin derivative as an active ingredient, wherein the novel decursin derivative has exhibited an excellent effect of inhibiting progerin expression and excellent effect of inhibiting binding between progerin and lamin A, and it has been confirmed that the novel decursin derivative prolongs the survival period of animal models in which progerin was induced.

Abstract: This invention relates to a process for preparing (±)-2-exo-(2-Methylbenzyloxy)-1-methyl-4-iso-propyl-7-oxabicyclo[2.2.1]heptane of the formula (I), (I) any one of its individual enantiomers or any non-racemic mixture thereof comprising the steps of (a) deprotonating (±)-2-exo-hydroxy-1-methyl-4-isopropyl-7-oxabicyclo[2.2.

Abstract: The present disclosure provides compounds of Formula (I-a), Formula (I), and Formula (II). The compounds described herein may be Myc modulators (e.g., Myc inhibitors) and may be useful in treating in a subject in need thereof diseases associated with Myc and proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including a compound described herein.

Abstract: The present application provides compounds that modulate CDK protein function. Methods of making the compounds, compositions containing the compounds, and uses of the compounds for treating or ameliorating of diseases, disorders, or conditions associated with CDK proteins, are also disclosed.

Abstract: Piperidino-dihydrothienopyrimidine sulfoxides of formula I wherein: Ring A is a 6-membered aromatic ring optionally comprising one or two nitrogen atoms and R is Cl and is located in the para-, meta-, or ortho-position of Ring A, S* is a sulphur atom that represents a chiral center, and all pharmaceutically acceptable salts, enantiomers and racemates, hydrates and solvates thereof and the use of these compounds for the treatment of inflammatory or allergic diseases of the respiratory tract such as COPD or asthma.

Abstract: The present invention provides novel ROR gamma-t inhibitors and pharmaceutical compositions thereof, formula (A).

Abstract: Provide herein are compounds and pharmaceutical compositions suitable as modulators of hemoglobin, methods and intermediates for their preparation, and methods for their use in treating disorders mediated by hemoglobin and disorders that would benefit from tissue and/or cellular oxygenation.

Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where R1 and R2 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent DNA-PK mediated disease, including cancer. The specification further relates to pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating DNA-PK mediated disease, including cancer, using such compounds and salts.

Abstract: A method for producing a particulate aluminum alloy involves pulverizing an aluminum alloy in a hydrocarbon solvent in the presence of an organic aluminum compound. Methods for producing trialkylaluminum involve reacting an aluminum-magnesium alloy with an alkyl halide in the presence of a nitrogen-containing organic compound to obtain a trialkylaluminum-containing reaction product, and reacting an aluminum-magnesium alloy and an alkyl halide. A highly active, low viscosity composition containing the particulate aluminum alloy and a method for producing the particulate aluminum alloy-containing composition are also described.

Abstract: The present invention provides a composition for substrate surface modification and a method using the same, and the composition for substrate surface modification is composed of a compound of the general formula structure shown in formula 1: wherein n1 is an integer of 1 to 6, and R is a zwitterionic group. The composition for substrate surface modification uses water as a medium to perform modifying reaction over a substrate surface, and at the same time has biological modification characteristics, and abilities of immobilizing biomolecules and anti-biofouling.

Abstract: A composition according to the present invention contains 100 parts by mass of a component (A) and 1-200 parts by mass of a component (B) and is solid at 25° C., the solid form being achieved at 25° C. without spray drying, impregnation into wax, or the like, and said composition is useful as an additive for a paint composition and an adhesive composition. The component (A) is an organic silicon compound represented by general formula (1), and the component (B) is at least one of organic silicon compounds represented by general formulas (2) and (3) (R1 and R2 represent, independently of each other, an alky group having 1-10 carbon atoms or the like, R3 and R4 represent, independently of each other, a divalent hydrocarbon group having 1-20 carbon atoms, m represents an integer from 1 to 3, R5 represents an alkyl group having 1-10 carbon atoms or the like, and R6 represents a divalent hydrocarbon group having 1-20 carbon atoms; however, an oxygen atom, a sulfur atom, etc.

Abstract: The invention relates to benzothiazole-containing silanes of the formula I which are prepared by reacting benzothiazole-containing silanes of the formula II with a compound of formula III R2—H??(III). The benzothiazole-containing silanes of the formula I can be used in rubber mixtures.

Abstract: A composition, and chemical vapor deposition method, is provided for producing a dielectric film. A gaseous reagent including the composition is introduced into the reaction chamber in which a substrate is provided. The gaseous reagent includes a silicon precursor that includes a silicon compound according to Formula I as defined herein. Energy is applied to the gaseous reagents in the reaction chamber to induce reaction of the gaseous reagents and to thereby deposit a film on the substrate. The film as deposited is suitable for its intended use without an optional additional cure step applied to the as-deposited film. A method for making the composition is also disclosed.

Abstract: A polyfluoroalkyl phosphoric acid ester represented by the general formula [CnF2n+1(CH2CF2)a(CF2CF2)b(CH2CH2)cO]mP(O)(OH)3?m [I] n: 1 to 6, a: 1 to 4, b: 1 to 3, c: 1 to 3, m: 1 to 3) or a salt thereof. The polyfluoroalkyl phosphoric acid ester represented by the general formula [I] is produced by subjecting a polyfluoroalkyl alcohol represented by the general formula CnF2n+1(CH2CF2)a(CF2CF2)b(CH2CH2)2OH [II] (n: 1 to 6, a: 1 to 4, b: 1 to 3, c: 1 to 3) to a dehydration condensation reaction with phosphoric acid. The polyfluoroalkyl phosphoric acid ester can be easily synthesized without passing through dialkyl ester as in the case of phosphonic acid, and used for a mold-releasing agent comprising the same or a salt thereof as an active ingredient.

Abstract: The invention features compounds of the general formula (I) in which the variable groups are as defined herein, and to their preparation and use.

Abstract: The present invention describes a process for producing tris-orthometalated metal compounds which can be used as coloring components as functional materials in a number of diverse applications that can be broadly attributed to the electronics industry.

Abstract: A compound comprising a first ligand selected from Formula I, and Formula II, is disclosed. In these structures, Y1 to Y12 and Z3 and Z4 are independently CR or N; where each R, R?, R?, RF, and RG is hydrogen or a substituent, where at least one dashed arc represents Rs joined into a 5-membered or 6-membered carbocyclic or heterocyclic ring; where the first ligand is complexed to a metal M; where ring G is a fused ring structure comprising five or more fused heterocyclic or carbocyclic rings, of which at least one ring is of Formula III where the fused heterocyclic or carbocyclic rings of Ring G are 5- or 6-membered; where Y is selected from BR?, NR?, PR?, O, S, Se, C?O, S?O, SO2, CR?R?, SiR?R?, and GeR?R?. Organic light emitting devices and consumer products containing the compounds are also disclosed.

Abstract: Provided herein is a method of synthesis of Pt(II) complexes, a pharmaceutical composition comprises thereof. Also provided herein are the methods for the treatment and prevention of cancer/tumor in patients in need thereof by the administration of the Pt(II) complexes. Also provided is a method of detecting the Pt(II) complex in a biological system. Also provided is a method of making the Pt(II) complex The Pt(II) complexes possess anticancer activity such as the induction of cell death, inhibition of cellular proliferation, and inhibition of tumor growth in vivo.

Abstract: The disclosure relates to a method for depolymerizing lignin. The method includes reacting a lignin compound with a thiol compound to depolymerize the lignin compound and to form a depolymerized lignin product having a reduced molecular weight relative to the lignin compound prior to reacting. The method can further include forming an oxidized thiol reaction product between two thiol groups from one or more thiol compounds, and then reducing the oxidized thiol reaction product to re-form or regenerate the thiol compound for further lignin depolymerization.

Abstract: A Stevia extract made from leaves of the Stevia rebaudiana plant is described. The extract has desired levels of steviol glycosides and is useful in food, beverage, and other consumable products.

Abstract: This invention describes new hydrated and anhydrous polymorphs of 2?-0-ficosyllactose (2?FL): Polymorph A 2?FL-3/2H2O, Polymorph B 2TL-5/2H2O and anhydrous Polymorph C. There is also a description of the methods for obtaining them, and of a new method for preparing Polymorph I already known in the literature.

Abstract: This invention describes new hydrated and anhydrous polymorphs of 2?-O-fucosyllactose (2?FL): Polymorph A 2?FL-3/2H2O, Polymorph B 2TL-5/2 H2O and anhydrous Polymorph C. There is also a description of the methods for obtaining them, and of a new method for preparing Polymorph I already known in the literature.

Abstract: The present invention generally relates to the field of detecting and preventing infectious diseases caused by Enterococcus faecalis and/or Enterococcus faecium.

Abstract: Provided are a newly developed tandem malonate-based amphipathic molecule, a method of preparing the same, and a method of extracting, solubilizing, stabilizing, crystallizing or analyzing a membrane protein using the same. In addition, the compound may be used to efficiently extract membrane proteins having various structures and characteristics from a cell membrane, compared to a conventional compound, to stably store the proteins in an aqueous solution for a long time, and may be used in functional and structural analysis thereof. The analysis of the structures and functions of the membrane proteins is one of the most attractive fields in current biology and chemistry, which are closely related to new drug development.

Abstract: Novel diterpene glycosides isolated from Stevia are provided herein. Compositions and consumables comprising the novel diterpene glycosides are also provided herein. Methods of enhancing the sweetness and/or flavor of consumables using the novel diterpene glycosides, methods of preparing compositions and consumables comprising the novel diterpene glycosides and methods of purifying the novel diterpene glycosides are also provided.

Abstract: Disclosed herein are a liver specific delivery (LSD)-based antiviral prodrug nucleoside cyclophosphate compound and uses thereof. Specifically, this application provides a compound of formula (I), or an isomer, a pharmaceutically acceptable salt, a hydrate, a solvate or a pharmaceutical composition thereof. This application also provides an application of the compound alone or in combination with other antiviral drugs in the treatment for viruses, particularly hepatitis C virus (HCV).

Abstract: Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (1): and pharmaceutical compositions thereof. Such compounds are contemplated useful for the prevention and treatment of a variety of CNS-related conditions, for example, treatment of sleep disorders, mood disorders, schizophrenia spectrum disorders, disorders of memory and/or cognition, movement disorders, personality disorders, autism spectrum disorders, pain,traumatic brain injury, vascular diseases, substance abuse disorders and/or withdrawal syndromes, tinnitus, and status epilepticus.

Abstract: The present invention relates to the unexpected discovery of novel monomer compounds capable of crosslinking interpenetrating polymer networks (IPNs). In certain embodiments, the monomer compounds of the invention each comprise at least one methacrylate functionality capable of forming polymeric bonds with other methacrylate and vinyl functionalities, and at least one epoxide functionality capable of forming polymeric bonds with epoxide functionalities, amine functionalities, and/or reactive oxygen species.

Abstract: Disclosed is a multi-channel peptide synthesizer, including a gas-bath thermotank, a plurality of reactor tubes, a motor, a rotating rack, a liquid-feeding tube, a feeding device, a vacuum tube and a nitrogen tube. The gas-bath thermotank body provides a desired constant temperature for reaction. The reactor tube provides a place for peptide synthesis and resin washing. The motor and the rotating rack are used to fully mix the reaction and cleaning solutions. Various liquid reagents required are fed to the reactor tube through the liquid-adding tube. Various materials required are prepared in advance in the feeding device and directly fed to the reactor tube. The reaction or washing solution in the reactor tube is pumped to a waste liquid tank through the vacuum tube. Nitrogen is introduced into each reactor tube through the nitrogen tube. This device can be applied in batch-wise peptide synthesis using solid-phase methods.

Abstract: The present invention provides a new methodology combining MD simulations and database-guided high-throughput screening to rationally design pore forming membrane-active peptides. The present inventive methodology is able to allow tuning of a range of structural and functional properties such as pore size and selectively targeting membranes with specific lipid compositions. The present inventive methods will ultimately allow de novo design of membrane-active peptides for a wide range of biomedical applications, including for example, antimicrobial agents.

Abstract: The present invention relates to an in vitro method for production of heterodimeric proteins.

Abstract: The present invention describes compositions containing cholesterol-linker-glutathione conjugates for targeting the brain by overcoming barrier entry to the CNS through the blood brain barrier (BBB), including micelle and liposome forms of such compositions. In addition, methods for treating subjects by administering such compositions are also disclosed.

Abstract: This invention describes an ICE inhibitor prodrug (I) having good bioavailability. Compound I is useful for treating IL-1 mediated diseases such as rheumatoid arthritis, inflammatory bowel disease, Crohn's disease, ulcerative colitis, inflammatory peritonitis, septic shock, pancreatitis, traumatic brain injury, organ transplant rejection, osteoarthritis, asthma, psoriasis, Alzheimer's disease, myocardial infarction, congestive heart failure, Huntington's disease, atherosclerosis, atopic dermatitis, leukemias and related disorders, myelodysplastic syndrome, uveitis or multiple myeloma.

Abstract: This invention relates to methods for removing bacterial toxins such as lipopolysaccharide and lipoteichoic acid from a biological fluid. In such method a peptide, selected from the list of KKIRVRLSA, RRIRVRLSA, KRIRVRLSA and RKIRVRLSA, is covalently attached to a solid support through its C-terminus, optionally with the interposition of a linker, and is used to capture the toxins. This invention also relates to such derivatised solid supports and to cartridges, columns, and medical apparatuses comprising such derivatised solid supports.

Abstract: The present invention relates to novel compounds, in particular peptidic macrocyclic peptides, that are capable of binding to and/or neutralizing influenza viruses, in particular influenza A viruses comprising HA of the H1 subtype 1, and to pharmaceutical compositions comprising such compounds. The invention also relates to the use of the peptidomimetic 5 compounds in the diagnosis, prophylaxis and/or treatment of influenza virus infections.

Abstract: Water dispersible, multivalent ligand-lipid constructs that spontaneously and stably incorporate into membranes are disclosed.

Abstract: Disclosed herein are compounds (such as peptides or peptide mimetics) that bind to HIV RRE RNA. In some examples, the compounds inhibit (for example, decrease) binding of Rev to the RRE RNA. In some embodiments, the compounds include two moieties, each of which bind to one of the Rev binding sites in the RRE. In some examples, the moieties include peptides or small molecules. In some examples, the peptides include an arginine-rich motif. The RRE binding compounds may be further linked to a detectable label or cargo moiety. Also disclosed are methods of treating or inhibiting HIV including administering one or more of the disclosed compounds to a subject.

Abstract: Embodiments of a recombinant human Parainfluenza Virus (hPIV) F ectodomain trimer stabilized in a prefusion conformation are provided. Also disclosed are nucleic acids encoding the hPIV F ectodomain trimer and methods of producing the hPIV F ectodomain trimer. Methods for inducing an immune response in a subject are also disclosed. In some embodiments, the method can be a method for treating or inhibiting a hPIV infection in a subject by administering a effective amount of the recombinant hPIV F ectodomain trimer to the subject.

Abstract: The disclosure concerns a polypeptide suitable for detecting antibodies against Zika virus in an isolated biological sample having a Zika virus NS1 wing domain specific amino acid sequence and variants thereof, wherein no further Zika virus specific amino acid sequences are present in the polypeptide. This polypeptide does not immunologically cross-react with antibodies raised against structurally related antigens from tick-borne encephalitis virus, Dengue virus 1-4, West Nile virus, yellow fever virus or Japanese encephalitis virus, but immunologically reacts with antibodies raised against full length Zika virus NS1 antigen. Also disclosed is a method of producing a soluble and immunoreactive Zika virus NS1 polypeptide as well as methods and kits for detecting antibodies specific for Zika virus in an isolated sample.

Abstract: The disclosure relates to a polypeptide suitable for detecting antibodies against a flavivirus in an isolated biological sample having a flavivirus NS1 wing domain specific amino acid sequence, wherein no amino acid sequences from the NS1 ß-ladder domain of said flavivirus are present in the polypeptide. In an embodiment, the flavivirus is selected from Zika virus (ZIKV), West-Nile virus (WNV), Dengue virus types 1-4 (DENV1-4), tick-borne encephalitis virus (TBEV), yellow fever virus (YFV) and Japanese encephalitis virus (JEV). Also disclosed is a method for producing said flaviviral NS1 wing domain specific polypeptides, a method for detecting antibodies specific for a first flavivirus species, the use of said flaviviral NS1 wing domain specific polypeptides for detecting antibodies as well as a reagent kit for detecting said flavivirus antibodies that has a flavivirus NS1 wing domain polypeptide.

Abstract: Some embodiments of the disclosure provide a protein of ‘Dangshan Suli’ for promoting the growth of a pollen tube and an encoding gene PbrTTS1. An amino acid sequence of the protein is shown in SEQ ID No.1 of the Sequence Listing. A nucleotide sequence of the encoding gene PbrTTS1 is shown in SEQ ID No.2 of the Sequence Listing. Other embodiments of the disclosure provide a primer for amplifying the encoding gene PbrTTS1. The primer includes a forward primer and a reverse primer. The nucleotide sequence of the forward primer is shown in SEQ ID No. 3 of the Sequence Listing, and the nucleotide sequence of the reverse primer is shown in SEQ ID No. 4 of the Sequence Listing.

Abstract: In order to provide: a method for producing an HSL protein with increased catalytic activity to oxidize a 4-HPPD inhibitor in a 2-oxoglutarate-dependent manner; and a method for producing a plant with increased resistance to a 4-HPPD inhibitor using the method for producing the HSL protein, it has been revealed that, by mutating position 140 to a basic amino acid in an HSL protein, the catalytic activity of the protein to oxidize a 4-HPPD inhibitor in a 2-oxoglutarate-dependent manner can be increased, and an activity of the protein to decompose the inhibitor can be increased.