Abstract: Compounds having a structure of formula (I), including stereoisomers and pharmaceutically acceptable salts and solvates thereof: wherein R1 is as defined herein. Such compounds are inhibitors of the vesicular monoamine transporter 2 (VMAT2) and have utility for treating, for example, hyperkinetic disorders. Also disclosed are compositions containing these compounds in combination with a pharmaceutically acceptable carrier or diluent, as well as methods relating to the use in a subject in need thereof.

Abstract: The present invention relates to compounds of formula (I) that are useful as hepatitis C virus (HCV) NS5A inhibitors, the synthesis of such compounds, and the use of such compounds for inhibiting HCV NS5A activity, for treating or preventing HCV infections and for inhibiting HCV viral replication and/or viral production in a cell-based system.

Abstract: Disclosed are compounds of Formula (I) N-oxides, or salts thereof, wherein G, A, R1, R5, and n are defined herein. Also disclosed are methods of using such compounds as inhibitors of signaling through Toll-like receptor 7, or 8, or 9, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating inflammatory and autoimmune diseases.

Abstract: Use of particular substituted heterocycle fused gamma-carboline compounds as pharmaceuticals for the treatment of agitation, aggressive behaviors, posttraumatic stress disorder or impulse control disorders.

Abstract: The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer.

Abstract: The present invention provides compounds of Formula (1): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.

Abstract: The present invention relates to novel [1,2,4]triazolo[1,5-a]pyrimidin-yl derivatives as inhibitors of phosphodiesterase 2 (PDE2). The invention is also directed to pharmaceutical compositions comprising the 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 PDE2 is involved, such as neurological and psychiatric disorders.

Abstract: The present invention relates generally to proteasome inhibiting ?-lactam compounds useful for the treatment of cancer and neurodegenerative disorders. The invention also provides pharmaceutical compositions and extended release formulations of said compounds, and medical uses of said compounds and/or pharmaceutical compositions to treat cancer and neurodegenerative disorders.

Abstract: A compound of Formula (I): pharmaceutically acceptable salts thereof, deuterated analogs thereof, compositions thereof, and methods of treating disease using a compound thereof are disclosed.

Abstract: Described herein are GPR35 modulators and methods of using these compounds in the treatment of diseases, disorders or conditions. Also described herein are pharmaceutical compositions containing such compounds.

Abstract: Fused cyclic pyrimidine compounds, including tautomers thereof, and pharmaceutically acceptable salts, prodrugs, solvates and hydrates thereof, are disclosed having the general Formula I: These compounds are useful in methods for treating cancer, selectively targeting cancerous cells via the proton coupled folate transporter, folate receptor alpha, and/or folate receptor beta pathways, inhibiting GARFTase in cancerous cells, and selectively targeting activated macrophages in a patient having an autoimmune disease, such as rheumatoid arthritis.

Abstract: Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

Abstract: Synthesis and characterization of novel crystalline mitomycin C forms suitable for pharmaceutical compositions in drug delivery systems to treat human or warm-blooded diseases.

Abstract: Disclosed herein are methods of synthesizing mahanine and related compounds. The synthesis features an intramolecular aryl-alkyne isomerization, transition metal catalyzed cross-coupling and intramolecular carbazole forming reaction.

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

Abstract: The present invention provides a production method of a thienopyrimidine derivative or a salt thereof which has a gonadotropin releasing hormone (GnRH) antagonistic action with high quality in high yield. The present invention provides a method of producing a thienopyrimidine derivative, which comprises reacting 6-(4-aminophenyl)-1-(2,6-difluorobenzyl)-5-dimethylaminomethyl-3-(6-methoxypyridazin-3-yl)thieno[2,3-d]pyrimidine-2,4(1H,3H)-dione or salt thereof, 1,1?-carbonyldiimidazole or a salt thereof and methoxyamine or a salt thereof, and the like.

Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds to treat disorders associated with GSK-3.

Abstract: The present invention relates to a crystal of cephalosporin intermediate 7?-methoxy cephalothin (I) and a method for preparing same. The crystal of 7?-methoxy cephalothin (I) undergoes Cu-Ka radiation and X-ray powder diffraction expressed in terms of angle 2?; the crystal of 7?-methoxy cephalothin (I) has characteristic absorption peaks at positions of 7.34°±0.20°, 12.71°±0.20°, 14.25°±0.20°, 14.68°±0.20°, 16.52°±0.20°, 17.99°±0.20°, 19.98°±0.20°, and 22.69°±0.20°. The crystal of 7?-methoxy cephalothin provided by the present invention is easy to prepare. Related test data shows that the crystal of 7?-methoxy cephalothin has high purity, low impurity content, and good stability. The preparation cost is low, the preparation method is simple to operate, conditions are mild and easy to control, and crystals of 7?-methoxy cephalothin can be obtained stably. The invention is applicable to industrial production.

Abstract: Disclosed in the present invention are a compound represented by formula (I), a tautomer thereof or a pharmaceutically acceptable salt, and applications thereof in the preparation of drugs for treating HBV-related diseases.

Abstract: The present disclosure encompasses solid state forms of Ixazomib Citrate and pharmaceutical compositions thereof. Also disclosed are processes for preparation of Ixazomib Citrate.

Abstract: The present invention relates to compound (I) or a salt thereof which has a ROR?t inhibitory action. In the formula (I), each symbol is as defined in the specification.

Abstract: A trichlorogermanide of formula (I): [R4N]/[R4P]Cl[GeCl3] (I), where R is Me, Et, iPr, nBu, or Ph, tris(trichlorosilyl)germanide of formula (II): [R4N]/[RrP][Ge(SiCl3)3] (II), where R is Me, Et, iPr, nBu, or Ph, a tris(trichlorosilyl)germanide adduct of GaCl3 of formula (III): [Ph4P][Ge(SiCl3)3*GaCl3], and a tris(trichlorosilyl)germanide adduct of BBr3 of formula (IV): [Ph4P][Ge(SiCl3)3*BBr3]. Also, methods for preparing the trichlorogermanides of formula (I), the tris(trichlorosilyl)germanide of formula (II), the tris(trichlorosilyl)germanide adduct of BBr3 of formula (IV).

Abstract: A limonene-based flame-retardant compound, a method of making a flame-retardant polymer, and an article of manufacture comprising a material that includes a limonene-based flame-retardant compound are provided. In an embodiment, the method includes forming a limonene-based derivative; forming a phosphorus-based flame-retardant molecule; reacting the limonene-based derivative with the phosphorus-based flame-retardant molecule to form a limonene-based flame-retardant compound; and forming a flame-retardant polymer from the limonene-based flame-retardant compound. In some embodiments, the limonene-based flame-retardant compound has variable functionality including vinyl, epoxide, methylene bridges, and thioethers.

Abstract: An optically active 2,3-bisphosphinopyrazine derivative represented by the following general formula (1): wherein R1 represents a group selected from a branched alkyl group having 3 or more carbon atoms, an adamantyl group, an optionally substituted cycloalkyl group, and an optionally substituted aryl group; R2 represents a group selected from a branched alkyl group having 3 or more carbon atoms, an adamantyl group, and an optionally substituted cycloalkyl group, provided that when R1 is a tert-butyl group, R1 and R2 are not the same; R3 represents a monovalent substituent; n represents an integer of 0 to 4; and * represents an asymmetric center on a phosphorus atom.

Abstract: Disclosed herein are caged haptens and caged hapten-antibody conjugates useful for enabling the detection of targets located proximally to each other in a sample.

Abstract: To provide an electrochromic compound, represented by the following general formula (I): where X1, X2, X3, X4, X5, X6, X7 and X8 are each independently a hydrogen atom or a monovalent substituent; R1 and R2 are each independently a monovalent substituent; A? and B? are each independently a monovalent anion; and Y is represented by the following general formula (II) or (III): where X9, X10, X11, X12, X13, X14, X15, X16, X17, and X18 are each independently a hydrogen atom or a monovalent substituent.

Abstract: A metal tetradentate complex is disclosed in which an imidazole moiety is used as a linker in the ligand. The complex is useful as an emitter or other functional roles in an OLED device.

Abstract: Unsymmetrical metallocene compounds based on cyclopentadienyl ligands are disclosed, as well as catalytic compositions comprising the compounds supported on solid support materials. The compounds and compositions are useful as catalysts in the polymerisation of olefins. In particular, the compounds and compositions are useful catalysts in the preparation of low molecular weight polyethylene (e.g. polyethylene wax) and copolymers formed from the polymerisation of ethylene and other ?-olefins.

Abstract: Disclosed are novel drug molecules and use of the novel drug molecules in the treatment of neurodegenerative diseases, such as Parkinson's disease.

Abstract: The disclosure provides methods and compositions for the integration (insertion) of a donor DNA molecule into a target DNA molecule. In general, the methods include contacting a target DNA molecule with a linear donor DNA molecule and a Cas 1 protein, where the target DNA molecule includes an AT-rich region (e.g., in some cases positioned 5 and within 50 nucleotides of a region that forms a DNA cruciform structure), where the contacting is not in a bacterial or archaeal cell (e.g., the contacting is in vitro outside of a cell, inside of a eukaryotic cell, etc.), and provides for integration of the donor DNA molecule into the target DNA molecule.

Abstract: A cyclic dinucleotide compound of Formula (I): wherein X1 is H or F; X2 is H or F; at least one among X1 and X2 is a fluorine atom; Z is OH, OR1, SH or SR1, wherein: R1 is Na or NH4, or R1 is an enzyme-labile group which provides OH or SH in vivo such as pivaloyloxymethyl; B1 and B2 are bases chosen from Adenine, Hypoxanthine or Guanine, and B1 is a different base than B2 and a pharmaceutically acceptable salt thereof. Pharmaceutical compositions including the cyclic dinucleotide, as well as their use in the treatment of a bacterial infection, a viral infection or a cancer are also described.

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) comprising the steps of a) reacting a compound of formula (II) with a silylating or an acylating agent to produce compound of formula (III), wherein P1 is a protecting group selected from R2—Si—R3R4 or R1CO—, R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) halogenation or sulfinylation of the compound of formula (III) to produce a compound of formula (IV); wherein X is halo, or —O—SO—R5, and R5 is a group selected from C6-10aryl or heteroaryl, each group being optionally substituted by one or more substituents independently selected from chloro or C1-4alkyl; c) dehalogenation or desulfinylation of t

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) said process comprising the steps of: a) reacting a compound of formula (II), with an acylating or a silylating agent to produce a compound of formula (III), wherein P1 and P2 are each independently a protecting group selected from R2—Si—R3R4, or R1CO—, wherein R1 is a group selected from C1-6alkyl or C3-6cycloalkyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; R2, R3 and R4 are each independently a group selected from C1-6alkyl or phenyl, each group being optionally substituted by one or more substituents independently selected from fluoro or C1-4alkyl; b) reacting the compound of formula (III) in the presence of palladium acetate or a derivative thereof to produce compound of formula (IV); and c) reacting the compound of formula (IV) with a reducing agent to produce compound of formula (I).

Abstract: Provided herein is a method of preparing a bile acid derivative using a continuous flow reaction. When bile acid derivatives are synthesized using a continuous flow reaction according to the present invention, the reaction is very safe compared to an existing batch-type reaction, the reaction time is significantly reduced, and high-quality bile acid derivatives may be synthesized with high efficiency. In particularly, according to the present invention, a hydrogenation reaction proceeds under substantially water-free reaction conditions, and thus the conversion rate (UDCA: CDCA) of a UDCA hydrogenation reaction may be significantly enhanced.

Abstract: This disclosure relates to progesterone phophate derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation such as those resulting from traumatic brain injury or stroke.

Abstract: The present invention relates to a novel process for preparation of peptides having amino acid chain length in the range of 2-40 comprises the steps: i) attaching an end-blocked amino acid with an ionic liquid based solid support in presence of an ionic solvent to obtain an end-terminal blocked amino acid attached ionic liquid; ii) removing end-terminal blocking agent from the end-terminal blocked amino acid attached ionic liquid of step i) followed by work up to obtain an amino acid attached ionic liquid; iii) repeating steps i) through ii) one or more times to obtain a polypeptide attached ionic liquid; and iv) detaching the polypeptide from the polypeptide attached ionic liquid of step iii) to obtain the polypeptide. Said process does not use any auxiliary reagents like dehydrating agent or activating agent. The use of ionic liquids as supports as well as solvents result in the faster kinetics of the process, the separation issues are reduced, and the process has no racemization issues.

Abstract: Provided herein are methods for refolding proteins that are denatured. Exemplary methods comprise solubilizing the denatured protein with a denaturing agent, e.g., a chaotropic agent, and renaturing the protein using a buffer exchanging system, e.g., tangential flow filtration (TFF).

Abstract: The present invention relates to a method for site-selective coupling of a first agent to a second agent, comprising the steps of: contacting a first agent comprising at least one furan moiety with an activation signal and with a second agent comprising at least one hydrazine moiety or at least one hydroxylamine moiety, thereby activating said furan moiety to an activated furan moiety; and reacting said activated furan moiety with the hydrazine moiety or the hydroxylamine moiety, thereby site-selectively coupling said first agent to said second agent.

Abstract: The present disclosure pertains to compositions comprising aflibercept and methods for producing such compositions in chemically defined media and using chromatography to reduce amounts of certain aflibercept variants.

Abstract: Disclosed herein are peptoids and related compounds, including peptoid affinity ligands for binding and/or purifying immunoglobulins, immunoglobulin fragments or immunoglobulin fusion proteins thereof. Methods of making peptoid affinity ligands and using the same to bind, purify and/or isolate immunoglobulins and related compounds are also disclosed. Such peptoid affinity ligands comprise a peptoid compound consisting of sequentially coupled peptoid residues forming a peptoid backbone, with one or more functional groups appended to a nitrogen of the peptoid residues of the peptoid backbone configured to provide the desired binding affinity.

Abstract: Disclosed herein are peptoids and related compounds, including peptoid affinity ligands, and hybrid peptoids, for binding and/or purifying immunoglobulins, immunoglobulin fragments or immunoglobulin fusion proteins thereof. Methods of making peptoid affinity ligands and using the same to bind, purify and/or isolate immunoglobulins and related compounds are also disclosed. Such peptoid affinity ligands comprise a peptoid compound consisting of sequentially coupled peptoid residues forming a peptoid backbone, with one or more functional groups appended to a Nitrogen of the peptoid residues of the peptoid backbone configured to provide the desired binding affinity. The peptoids can further comprise a peptoid backbone with at least one functional group coupled to an alpha carbon (C) of a peptide bond in the peptoid backbone thereby forming a hybrid peptoid.

Abstract: The present invention relates to a method for removal of large contaminants, such as virus, in a chromatographic process for purification of a target molecule, preferably monoclonal antibodies, mAbs, by using a specifically designed chromatographic bead having a thin outer layer and a core functionalized with a ligand adsorbing the mAbs or parts thereof.

Abstract: Processes for preparing compounds of Formula (1) and Formula (2) are described, wherein X, Y, Z, R1-R7, L and n are defined herein. Intermediates useful in the preparation of the compounds of Formula (1) and Formula (2) are also described.

Abstract: The present invention relates, in general, to human immunodeficiency virus (HIV), and in particular to a vaccine for HIV-1 and to methods of making and using same.

Abstract: The present invention relates to the stabilisation of foot-and-mouth disease virus (FMDV) capsids, by specific substitution of amino acids in a specific region of FMDV VP2. The invention provides stabilised FMDV capsids and vaccines against FMD.

Abstract: Methods for increasing carbon-based chemical product yield in an organism by increasing carbon uptake and/or altering a pathway to or from an overflow metabolite in the organism, nonnaturally occurring organisms having increased carbon-based chemical product yield with increased carbon uptake and/or an altered pathway to or from an overflow metabolite, and methods for producing a carbon-based chemical product with these organisms are provided.

Abstract: The present invention provides methods and compositions for generating transgenic animals, including transgenic mammals, as well as plasma cells that allow for cell surface capture of secreted immunoglobulin molecules produced endogenously in the plasma cells.

Abstract: Yeast having modified chromosomes are provided. The chromosomes are modified such that at least one of yeast histones H3, H4, H2A or H2B are fully or partially replaced by their human histone counterparts H3, H4, H2A or H2B, respectively. Histone amino acid substitutions are included. Cell fusions with the yeast having the modified chromosomes and non-yeast cells are provided. Methods for screening test agents using the yeast are also provided. Yeast with a mutated yeast DAD1 gene, the mutated DAD1 gene encoding an E50D mutation in yeast DAD1 protein, are provided, and provide a useful genetic background for making the yeast with partially or fully replaced histone(s).

Abstract: Embodiments of the present disclosure provide polypeptides, related materials and compositions, and methods for their use. In certain embodiments, the present disclosure provides a monomeric Tamm-Horsfall Protein polypeptide, or a biologically active truncation thereof. Other embodiments provide polynucleotides encoding a polypeptide described herein, nucleic acid expression vectors including the polynucleotides, and recombinant host cells including the expression vector. Yet other embodiments provide pharmaceutical compositions including a polypeptide described herein. Also provided are methods for treating a renal disease, disorder, or condition in a subject and/or modulating an immune response in a subject.

Abstract: The present invention provides methods and compositions for treating and/or preventing age related macular degeneration and other conditions involving macular degeneration, ocular neovascularization, or inflammation, including ocular inflammation. In some embodiments, the methods comprise administering an expression vector that delivers a secretable and cell penetrating Nrf2 to a subject in need thereof.