Abstract: Isoquinoline ether compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.

Abstract: The present invention provides with an oxoisoquinoline derivative represented by the formula (I) (in the formula, Q and R1 are as defined in the description) or a pharmaceutically acceptable salt thereof, which is useful as a Bruton's kinase inhibitor for treating cancer, B-cell lymphoma, chronic lymphocytic leukemia and the like.

Abstract: The present invention relates to a heterocyclic compound represented by Chemical Formula 1 that can be used for the prevention or treatment of diseases caused by abnormality in a PRS (prolyl-tRNA synthetase) activity, or a pharmaceutically acceptable salt thereof, a method for preparing the same, and a pharmaceutical composition comprising the same.

Abstract: Compounds of Formula (I) or pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising these compounds, the use of these compounds and compositions in the treatment of diseases in which LRRK-2 kinase is involved.

Abstract: The present disclosure relates to novel processes for the preparation of short acting benzodiazepines as well as to novel intermediates in this process. More particularly the disclosure relates to processes and intermediates for preparation of Methyl 3-[(4S)-8-bromo-1-methyl-6-(pyridin-2-yl)-4H-imidazo[1,2-a][1,4]benzodiazepin-4-yl]propanoate, commonly known as Remimazolam. The present disclosure also relates to solid state forms of Remimazolam salts, processes for the preparation thereof, pharmaceutical formulations/compositions thereof, and methods of use thereof.

Abstract: The invention relates to new substituted heteroaryls of formula 1 wherein A is selected from the group consisting of N and CH D is selected from the group consisting of CH, N, NH, S and O, E is selected from the group consisting of C and N, T is selected from the group consisting of C and N, G is selected from the group consisting of C and N, and wherein each of the broken (dotted) double bonds in ring 1 are selected from either a single bond or a double bond under the proviso that all single and double bonds of ring 1 are arranged in such a way that they all form together with ring 2 an aromatic ring system, and wherein R1, M and R3 are defined according to claim 1, and to the above compounds for the treatment of a disease selected from the group consisting of asthma, COPD, allergic rhinitis, allergic dermatitis, lupus erythematodes, lupus nephritis and rheumatoid arthritis.

Abstract: A compound of formula (I) of formula (II) or of formula (III) wherein R1 and R2 independently from each other are a C1- to C8-alkyl group and R3 to R12 independently from each other are a hydrogen or a C1- to C4-alkyl group.

Abstract: The present disclosure provides compounds of any one of Formulae (I?), (I), (IA), (II?), (II), (IIA), (IIIA), (III?), (III?), (III), (IIIA), (IV), (V?), (V), (VI), (VII), (VIII?), (VIII), (IX?), (IX), and (X). The compounds described herein may be useful in treating and/or preventing abroad range of diseases (e.g., proliferative disease (e.g., cancers (e.g., non-small cell lung cancer, or glioma), inflammatory diseases, autoimmune diseases), CNS disorder (e.g., drug addiction), metabolic disorder (e.g., diabetes), or infectious disease (e.g., bacterial infection or parasitic infection (e.g., malaria))). Also provided in the present disclosure are pharmaceutical compositions, methods of synthesis of a compound described herein, kits, methods, and uses including or using a compound described herein.

Abstract: Provided are novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, compositions containing them and their use in the treatment of or prevention of diseases associated with or characterized by LRRK2 kinase activity, for example Parkinson's disease, Alzheimer's disease and amyotrophic lateral sclerosis (ALS).

Abstract: Provided are sugar-based compounds, method so making such compounds, gels comprising such compounds, methods of making gels, methods of using such compounds for containing spill of a hydrocarbon, and methods for reclaiming solvent from gels comprising such compounds.

Abstract: The present invention relates to an improved process for preparing [(1S,2R)-3-[[(4-aminophenyl)-sulfonyl](2-methyl-propyl)amino]-2-hydroxy-1-(phenylmethyl)-propyl]-carbamic acid (3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl ester—which compound is also known under its INN as darunavir—by reacting carbonic acid 2,5-dioxo-1-pyrrolidinyl[(3R,3aS,6aR)-hexahydrofuro[2,3-b]furan-3-yl]ester with 4-amino-N-[(2R,3S)-3-amino-2-hydroxy-4-phenylbutyl]-N-(2-methylpropyl)-benzenesulfonamide in ethanol as solvent. Furthermore said process allows for darunavir to be isolated immediately in its ethanolate form, i.e. darunavir monoethanolate, which is the marketed form of darunavir under the tradename Prezista™.

Abstract: Various embodiments relate to a compound of the formula (I) and (II), wherein X, X1, X2, X3, and R1-R4 are defined herein, as well as pharmaceutical compositions comprising compounds of the formula (I) and/or (II) and methods of treating an HIV infection comprising administering a therapeutically effective amount of one or more compounds of formula (I) and/or (II), or a pharmaceutical composition comprising compounds of the formula (I) and/or (II), to a patient in need thereof.

Abstract: The present invention provides a compound having the structure:

Abstract: The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: (I), where R1, R2, R3, R4, R4?, R5, R6, X, and n are described herein.

Abstract: The disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R5, X1, X2, n, and m are described herein.

Abstract: The present invention provides tricyclic compounds, and pharmaceutically acceptable salts thereof, having antimitotic activity, anti-multidrug resistance activity, for example P-glycoprotein inhibition, and antitumor activity, and which inhibit paclitaxel sensitive and resistant tumor cells. Also provided are methods of utilizing these compounds for treating tumor cells and inhibiting mitosis of cancerous cells.

Abstract: Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.

Abstract: The present invention relates to a method for the manufacture of 2-(3-(alkyl or alkenyl)morpholino)-ethan-1-ols by reduction of 8a-(alkyl and alkenyl)hexahydrooxazolo[2,3-c][1,4]oxazines encompassing a process for producing 2-(3-(4-propylheptyl)morpholino)ethan-1-ol with the INN name delmopinol. The invention also relates to 1-chloro-4-propylhept-3-ene, 1-iodo-4-propylhept-3-ene, 8a-(4-5 propylheptyl)hexahydrooxazolo[2,3-c][1,4]oxazine, 8a-(4-propylhept-3-en-1-yl)hexahydrooxazolo[2,3-c][1,4]oxazine and 2-(3-(4-propylhept-3-en-1-yl)morpholino)ethan-1-ol which are intermediates in the delmopinol process.

Abstract: The present specification provides a heterocyclic compound of Chemical Formula 1, and an organic light emitting device comprising the same. The heterocyclic compound used as a material of an organic material layer of an organic light emitting device provides enhanced efficiency, low driving voltage, and enhanced lifetime properties of the organic light emitting device.

Abstract: Provided are compounds of Formulas (I?), (I), (II?) and (II), or pharmaceutically acceptable salts thereof, and methods for their use and production.

Abstract: The disclosure relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, X1, X2, X3, n, and m are described herein.

Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: Bisaminoalkoxysilanes of Formula I, and methods using same, are described herein: R1Si(NR2R3)(NR4R5)OR6??I where R1 is selected from hydrogen, a C1 to C10 linear alkyl group, a C3 to C10 branched alkyl group, a C3 to C10 cyclic alkyl group, a C3 to C10 alkenyl group, a C3 to C10 alkynyl group, a C4 to C10 aromatic hydrocarbon group; R2, R3, R4, and R5 are each independently selected from hydrogen, a C4 to C10 branched alkyl group, a C3 to C10 cyclic alkyl group, a C3 to C10 alkenyl group, a C3 to C10 alkynyl group, and a C4 to C10 aromatic hydrocarbon group; R6 is selected from a C1 to C10 linear alkyl group, a C3 to C10 branched alkyl group, a C3 to C10 cyclic alkyl group, a C3 to C10 alkenyl group, a C2 to C10 alkynyl group, and a C4 to C10 aromatic hydrocarbon group.

Abstract: Disclosed herein, inter alia, are acyclic nucleotide analogs and methods of using an acyclic nucleotide analog for treating and/or ameliorating a papillomavirus infection.

Abstract: A compound having a first ligand LA of Formula I, is disclosed. In the structure of Formula I, Z1 through Z7 are each independently C or N; ring B is a 5-membered or 6-membered ring; each RA, RB, and RC is independently hydrogen or one of a variety of substituents; any two substituents in RC may be joined or fused together to form a ring. In the compound, LA is complexed to a metal M, which is optionally coordinated to other ligands. In addition, ligand LA is optionally linked with other ligands to comprise a tridentate, tetradentate, pentadentate, or hexadentate ligand. Organic light emitting devices, consumer products, formulations, and chemical structures containing the compounds are also disclosed.

Abstract: Metal complexes containing substituted allyl ligands and methods of using such metal complexes to prepare metal-containing films are provided.

Abstract: In an embodiment, a composition including a chiral solvating agent to resolve nuclear magnetic resonance signals of an enantiomer of at least one analyte, where the chiral solvating agent facilitates in the at least one analyte binding to a C2 face or a C3 face of the chiral solvating agent, and where the chiral solvating agent causes an upfield shift or a downfield shift in at least one nuclear magnetic resonance signals corresponding to a 1H, 19F{1H}, or 31P{1H} signal, and where the chiral solvating agent includes a cobalt cation. In another embodiment, a method that includes mixing a chiral solvating agent, including a cobalt cation, with at least one analyte to form a solution, obtaining nuclear magnetic resonance spectra of the solution, and identifying an enantiomer of the at least one analyte. In some embodiments, the method further includes determining enantiomeric purities of the at least one analyte.

Abstract: Provided are a novel ionic solid usable for a secondary battery and demonstrating a high ionic conductivity, and an ionic conductor containing the same. An ionic solid, wherein an anionic heterometallic complex composed of one metal M1 selected from the group consisting of Ir, Rh, Co, Os, Ru, Fe, Ni, Cr and Mn, one metal M2 selected from the group consisting of Zn, Cd, Hg, Au, Ag and Cu (provided that when W is Rh, M2 is not Zn) and a ligand aggregates to form a crystal lattice in which a cationic species is present in an interstice in the crystal lattice.

Abstract: An embodiment of the present invention relates to a compound of the general formula. The compound of formula is suitable for use in a method for treating a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human. Furthermore an embodiment of the present invention concerns a method for treatment of a disorder relating to the binding of a galectin, such as galectin-3 to a ligand in a mammal, such as a human.

Abstract: The invention provides synthetic processes and synthetic intermediates that can be used to prepare compounds having useful anti-HIV properties.

Abstract: The present disclosure relates to 2?3?-cyclic dinucleotides comprising a carbocyclic nucleotide and derivatives thereof, that can modulate the activity of the STING adaptor protein.

Abstract: Compounds are provided according to Formula (III) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R2, R3, R5, and n are as defined herein, and at least one hydrogen is replaced with a deuterium. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.

Abstract: Compounds having drug and bio-affecting properties, their pharmaceutical compositions and methods of use are set forth. In particular, betulinic acid derivatives that possess unique antiviral activity are provided as HIV maturation inhibitors, as represented by compounds of Formula I: These compounds are useful for the treatment of HIV and AIDS.

Abstract: SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078.

Abstract: The present invention is related to a separating agent for the purification of human insulin, ensuring that human insulin can be recovered in high yield when isolating human insulin from a solution containing human insulin and a specific insulin under specific liquid chromatography separation conditions by using the separating agent.

Abstract: Described herein are methods to produce keratin protein-based biomaterials, the parameters required to achieve improved extraction, the parameters required to improve isolation, the parameters of lyophilization and the grinding process to achieve consistent particulate sizes of protein materials.

Abstract: The present invention provides homing peptides that localize in central nervous system tissue characterized by neuroinflammation and methods of using the same.

Abstract: To provide a peptide that selectively activates type 2 neuromedin U receptor and is chemically stable under physiological conditions. A peptide represented by Formula (1) described in the specification.

Abstract: Provided are ligands comprising a non-naturally occurring peptide that binds a cysteine rich domain (CRD) of the Frizzled7 (FZD7) receptor. Additionally, provided are therapeutic methods of using such ligands, as well as compositions comprising such ligands.

Abstract: The present disclosure generally relates to a circularized peptide for treating cancer. An cyclic peptide is disclosed that has an amino acid sequence selected from Lys-X5-Glu-X1-X2-Gln-Met-Glu-Asp-Asp-X3-X4 (SEQ ID NO: 3), (SEQ ID NO: 4), Lys-Gly-X6-Val-Leu-Gln-Met-X7-X8-X9-Leu-Val (SEQ ID NO: 5), Lys-X5-Glu-X1-X2-Gln-X12-Glu-Asp-Asp-X3-X4 (SEQ ID NO: 9), and X10-X5-X6-Val-Leu-Gln-Met-Glu-Asp-X9-X3-X4 (SEQ ID NO: 10). The amino acids X1, X2, X3, and X4 can be each independently valine, leucine, isoleucine, or alanine; X5 can be glycine, alanine, leucine, isoleucine, or valine; X6, X7, X8, and X9 can be each independently glutamic acid or asparagine; X10 can be lysine or arginine; X11 can be methionine or cysteine; and X12 can be methionine or norleucine. The cyclic peptide can have the amino acid sequence Lys-Gly-Glu-Val-Leu-Gln-Met-Glu-Asp-Asp-Leu-Val (SEQ ID NO: 1).

Abstract: Disclosed are peptides comprising a monomeric Fc fragment of an immunoglobulin recognized by a neonatal receptor (FcRn); an influenza HA protein; and a trimerization domain. Disclosed are compositions comprising one or more of the peptides described herein. Disclosed are nucleic acid sequences capable of encoding any one of the peptides described herein. Disclosed are methods for eliciting a protective immune response against influenza comprising administering to a subject an effective amount of a composition comprising a monomeric Fc fragment of an immunoglobulin recognized by a FcRn; an influenza HA protein; and a trimerization domain, wherein the administering is to a mucosal epithelium.

Abstract: The present invention generally relates to polypeptides, polynucleotides, expression vectors, infectious clones, virus particles and immunogenic compositions of recombinant alphaviruses which can be used as vaccines. The present disclosure also relates to methods for eliciting an immune response against alphavirus infection using the immunogenic composition comprising the alphavirus mutants described herein.

Abstract: The present invention provides multivalent CD20-binding molecules and compositions thereof, such as enriched compositions comprising large proportions of multivalent CD20-binding molecules relative to monovalent CD20-binding molecules. Certain multivalent CD20-binding molecules of the present invention comprise (i) two or more CD20-binding regions and (ii) one or more Shiga toxin effector polypeptide regions derived from an A Subunit of a member of the Shiga toxin family. Certain multivalent CD20-binding molecules of the present invention, and compositions thereof, have uses for selective killing of specific cell types and as therapeutics for the treatment of a variety of diseases, including cancers, tumors, and immune disorders.

Abstract: The present invention relates to treatment of diabetes, toll-like receptor 4 (TLR-4) modulators and methods for using the same. Particularly, the present invention provides an isolated peptide from pneumolysin (PLY peptide) which is effective in treatment of diabetes. In addition, the PLY peptide of the present invention is a TLR-4 antagonist and thus can be used in the treatment of a disease or condition associated with TLR-4 activation. The present invention also provides treatment of diabetes with a TLR-4 antagonist.

Abstract: This disclosure describes compositions and methods for enhanced production of enduracidin in genetically engineered strains of Streptomycesfungicidicus. In particular, the present disclosure describes the genetic manipulation of regulatory genes orf24 and orf18 associated with the enduracidin (enramycin) biosynthesis gene cluster from Streptomyces fungicidicus to generate vector constructs and recombinant strains producing greater yields of enduracidin.

Abstract: The present disclosure provides peptide biomarkers, including methods and kits employing the same, for diagnosis of peanut allergy, and tolerance thereto, and for determining whether an allergic subject is likely to outgrow the allergy.

Abstract: This invention, in one aspect, relates generally to methods for optically modulating pain in animals and human. The invention provides method for the use of opsin for modulating pain, wherein optical stimulation of specific neurons and/or other cells in targeted regions of the nervous system sensitized by opsin, using genetic technologies, leads to significant reduction of pain perception to noxious stimuli. Further, the invention provides a method for inhibition of pain without use of exogenous opsin, wherein visual stimulation of eye (having endogenous opsin) is carried out. The invention also includes device(s) for controlled modulation neural and/or cellular activities in brain, eye and peripheral nervous system in order to treat different forms of chronic pain.

Abstract: This invention relates to peptides and their use for modulating sodium channels. More particularly, the present invention relates to peptides from the venom of the tarantula Pamphobeteus nigricolor and their use in methods of inhibiting Nav1.7 and for treating or preventing conditions associated with Nav1.7 activity such as neuropathic, inflammatory and nociceptive pain.

Abstract: The purpose of the present invention is to provide: a liver-type fatty acid-binding protein standard by which, in a measurement using a specifically binding substance, the range of variation of a measured value caused by a liver-type fatty acid-binding protein can be narrowed; a method of evaluating the standard; a method of drawing a calibration curve of a liver-type fatty acid-binding protein; and a method of quantifying the protein. A liver-type fatty acid-binding protein standard in which a coefficient of change in oxidation, said coefficient being represented by the ratio of a measured value obtained by using a liver-type fatty acid-binding protein standard having been subjected to an oxidation treatment with 10 mM of an oxidant for 1 hour at 25° C. to a measured value obtained by using the liver-type fatty acid-binding protein standard not subjected to the oxidation treatment, is set to 1.

Abstract: The present invention relates to the use of Rspondins, particularly Rspondin2 (Rspo2) or Rspondin3 (Rspo3) or Rspondin nucleic acids, or regulators or effectors or modulators of Rspondin, e.g. Rspo2 and/or Rspo3 to promote or inhibit angiogenesis and/or vasculogenesis, respectively. The invention is based on the demonstration that Rspo3 and Rspo2 are angiogenesis promoters, and the identification of Rspo2 and 3 as positive regulators of vascular endothelial growth factor (VEGF). These results indicate a major role for Rspondins, particularly Rspo3 and/or Rspo2 in the signaling system during angiogenesis. The invention also relates to the use of regulators or effectors or modulators of Rspondin3, including agonists and antagonists, in the treatment of conditions where treatment involves inhibiting or promoting angiogenesis and/or vasculogenesis.