Abstract: Triazolo(4,5-d)pyrimidine derivatives for use in treatment or prevention of bacterial infection in a host mammal in need of such treatment or use as inhibitor of biofilm formation on a surface of biomaterial or medical device, particularly of cardiovascular device such as prosthetic heart valve or pacemakers.

Abstract: Pyrazolo-quinazoline derivatives of formula (Ia) or (Ib) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.

Abstract: To provide an organic electroluminescence device having a high luminous efficiency and a novel compound that can be used as a material for an organic electroluminescence device having a high luminous efficiency. A compound represented by the following formula (1) or (2): wherein in the formulas (1) and (2), one or more pairs of adjacent two or more of R1 to R7 and R10 to R16 may form a substituted or unsubstituted, saturated or unsaturated ring; R17, and R1 to R7 and R10 to R16 that do not form the substituted or unsubstituted, saturated or unsaturated ring are independently a hydrogen atom, a substituted or unsubstituted aryl group including 6 to 20 ring carbon atoms or a substituted or unsubstituted monovalent heterocyclic group including 5 to 20 ring atoms; two R17s may be the same or different; and Ar1 to Ar4 are independently a substituted or unsubstituted aryl group including 6 to 20 ring carbon atoms.

Abstract: The present invention provides compounds of Formula (I), and pharmaceutically acceptable salts thereof, as well as pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

Abstract: The invention is among others concerned with novel polyketides, their method of production, purification and use. The method can entail providing a bacterium that synthesizes the compound.

Abstract: Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.

Abstract: An organic electroluminescence device including an anode, a cathode, and an emitting layer between the anode and the cathode, in which the emitting layer comprises a compound represented by the formula (1) and a compound represented by the formula (2).

Abstract: Novel tetrahydroisoquinoline derivative compounds are disclosed herein that may be used as an active ingredient for a pharmaceutical composition, and in particular, for a pharmaceutical composition useful for preventing or treating a disease or condition responsive to modulation of the contractility of the skeletal sarcomere. This may be accomplished, for example, by modulation of the troponin complex of the fast skeletal muscle sarcomere through one or more of fast skeletal myosin, actin, tropomyosin, troponin C, troponin I, and troponin T, and fragments and isoforms thereof. The tetrahydroisoquinoline derivative compounds can thus be used as an agent for preventing or treating 1) neuromuscular disorders, 2) disorders of voluntary muscle, 3) CNS disorders in which muscle weakness, atrophy, and fatigue are prominent symptoms, 4) muscle symptoms stemming from systemic disorders, and 5) dysfunctions of pelvic floor and urethral/anal sphincter muscle.

Abstract: A hydrogenated Diels-Alder adduct of the formula (III) a hydrogenated Diels-Alder adduct of the formula (IV) and a lactone compound of formula (V) are disclosed and described.

Abstract: Embodiments of the present invention feature novel Bryoid compositions, methods of making and methods of treating disease

Abstract: Provided herein are formulations, methods and substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted thieno[3,2-d]pyrimidine, furo[3,2-d]pyrimidine, and pyrrolo[3,2-d]pyrimidine compounds.

Abstract: The present invention provides compounds as bacterial topoisomerase inhibitors with antibacterial activity.

Abstract: The disclosure provides compounds having formula (I), where the substituents are as defined herein. The compounds are useful for modulating the dopamine D3 receptor and for treating conditions associated therewith, such as addictions, drug dependency, and psychiatric conditions.

Abstract: Fused [1,2]Imidazo[4,5-c] ring compounds (e.g., imidzao[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) substituted on the fused ring with a group that contains a guanidine or substituted guanidine moiety, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are also disclosed.

Abstract: The disclosure provides compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: Also provided are methods of making the compounds of Formula (I) and their methods of use.

Abstract: Derivatives of 1,2,4-Triazolo-[3,4-b]-1,3,4-thiadiazoles according to formula (I), as set forth below: processes for production thereof, pharmaceutical compositions containing the same and the use thereof in treatment of cancer.

Abstract: The invention relates to a method for the cost-effective and environmentally friendly production of alkyl indium sesquichloride in high yield and with high selectivity and purity. The alkyl indium sesquichloride produced according to the invention is particularly suitable, also as a result of the high purity and yield, for the production, on demand, of indium-containing precursors in high yield and with high selectivity and purity. As a result of the high purity, the indium-containing precursors that can be produced are particularly suitable for metal organic chemical vapour deposition (MOCVD) or metal organic vapour phase epitaxy (MOVPE). The novel method according to the invention is characterised by the improved execution of the method, in particular a rapid process control. Owing to targeted and extensive use of raw materials that are cost-effective and have a low environmental impact, the method is also suitable for use on an industrial scale.

Abstract: The present invention relates to a process for the preparation of crisaborole of formula (I): by preparing intermediates of formulas (II) and (III):

Abstract: Here are described boroxine-containing compounds and their compositions for the treatment of wood. For instance, the treatment of wood includes its protection against moisture and/or degradation caused by insects or microbes.

Abstract: A metal-organic framework of the present disclosure includes tetravalent Group IV element ions or rare earth ions as metal ions, first ions of organic molecules having a trimesic acid framework as tridentate ligands, and second ions of organic molecules having a heterocycle and two carboxy groups as bidentate ligands.

Abstract: Vanadium phosphinic complex having general formula (I) or (II): V(X)3[P(R1)n(R2)3-n]2??(I) V(X)3[(R3)2P(R4)P(R3)2]??(II) wherein: X represents an anion selected from halogens such as, for example, chlorine, bromine, iodine, preferably chlorine; or is selected from the following groups: thiocyanate, isocyanate, sulfate, acid sulfate, phosphate, acid phosphate, carboxylate, dicarboxylate; R1, identical or different among them, represent a hydrogen atom, or an allyl group (CH2?CH—CH2—); or are selected from alkyl groups C1-C20, preferably C1-C15, linear or branched, optionally halogenated, optionally substituted cycloalkyl groups; n is an integer ranging from 0 to 3; R2, identical or different among them, are selected from optionally substituted aryl groups; R3, identical or different among them, represent a hydrogen atom, or an allyl group (CH2?CH—CH2—); or are selected from alkyl groups C1-C20, preferably C1-C15, linear or branched, optionally halogenated, optionally substituted cycloalkyl groups, opti

Abstract: Metal complexes having heterocycle substituted ligands are disclosed, which can be used as emitters in the emissive layer of an organic electroluminescent device. The application of these novel compounds as emitters in phosphorescent OLED devices enables to obtain deep red and near infrared colors. Also disclosed are an electroluminescent device and a formulation containing the complexes.

Abstract: Method for the production of tetrakis(trihydrocarbylphosphane)palladium(0) in organic solvent, whereby 50 to 100% by weight of the organic solvent consist of at least one polar-aprotic solvent, characterised in that a) at least one palladium compound selected from the group consisting of palladium(II) compounds and palladium(IV) compounds that are soluble in the organic solvent is reacted with b) at least one base, selected from the group consisting of alkali metal hydroxides, alkali metal carbonates, alkali metal hydrogen carbonates, alkali metal-C1-C4-alcoholates, ammonium carbonate, ammonium hydrogen carbonate, alkaline earth metal hydroxides, alkaline earth metal carbonates, alkaline earth metal hydrogen carbonates, alkaline earth metal-C1-C4-alcoholates, and alkylamines with a total of 2 to 12 carbon atoms; c) at least one trihydrocarbylphosphane; and d) at least one organic reducing agent that is different from the remaining components that are used in the method.

Abstract: The present invention discloses a class of antibiotics designed to target non-protein transporters. Further, a method is described to treat infections by targeted binding of a lipid transporter utilizing organometallic compounds, coordination compounds, metal centers, or any combination thereof. The antibiotics described herein are designed to halt or negatively affect the reproduction of bacteria by disrupting the biosynthesis of the cell wall and other important bacterial compounds such as lipopolysaccharide and techoic acids.

Abstract: An organometallic compound represented by Formula 1: wherein, in Formula 1, groups and variables are the same as described in the specification.

Abstract: Catalyst systems and methods for making and using the same are disclosed. In an example, a method of synthesizing a monocyclopentadienyl compound is provided. The method includes melting a dicyclopentadienyl compound including the following structure: As used herein, M is hafnium or zirconium. Each R is independently an H, a hydrocarbyl group, a substituted hydrocarbyl group, a heteroatom group. Each X is a leaving group selected from a halogen or a heteroatom group.

Abstract: Provided herein are methods for preparing prebiotic oligosaccharides by non-enzymatic methods of glycosylation of monosaccharides and/or disaccharides or by hydrolysis of polymeric sugars to monosaccharides and simultaneous glycosylation of hydrolytic products. The methods may include mixing one or more types of monosaccharides and/or disaccharides with a water-deficient system at a temperature sufficient to form one or more types of prebiotic oligosaccharides. Also provided are methods of preparing prebiotic oligosaccharides comprising mixing starch, cellulose and/or lignocellulosic biomass with a water-deficient system at a temperature sufficient to form one or more types of prebiotic oligosaccharides that collectively make up at least 25% of the products of the synthesis.

Abstract: A method for purifying rebaudioside M, which method comprises: (a) providing a solution comprising rebaudioside M at a concentration of at least about 10 g/L and at a purity of at least about 10% by weight on a dry basis; and (b) crystallizing from the solution a high purity composition comprising rebaudioside M, thereby to purify rebaudioside M.

Abstract: The present invention relates to a pharmaceutical composition comprising an acanthoside B compound as an effective ingredient for preventing or treating dementia or for improving a cognitive function. In the present invention, a desalted glasswort extract, and acanthoside B, which is isolated from the extract and acts as an effective ingredient inhibitory of acetylcholine esterase, were found to have an excellent neuroprotective activity through the inhibition of neuroinflammation and to improve memory retention and remarkably enhance spatial cognitive ability as measured by passive avoidance test and Y-maze test in a scopolamine-induced amnesic animal model. The acanthoside B or glasswort extract of the present invention can be applied to a pharmaceutical composition for preventing or treating dementia, a pharmaceutical composition for improving a cognitive function, or a health functional food or feed for improving memory retention and cognitive function.

Abstract: Aspects of the present disclosure include compositions that make use of phosphorus and/or nucleobase protecting groups which find use in the synthesis of long polynucleotides. Phosphorus protecting groups are provided that help increase the stepwise coupling yield and/or phosphorous protecting groups that can be removed during the oxidation step. Amidine nucleobase protecting groups are provided that find use in the subject compositions and methods which provides for e.g., increased resistance to depurination during polynucleotide synthesis. In some instances, the methods and compositions disclosed herein utilize a combination of the phosphorus and amidine nucleobase protecting groups in the synthesis of polynucleotides having a sequence of 200 or more monomeric units in length. Also provided are methods for synthesizing a polynucleotide (e.g., a DNA) using one or more compounds disclosed herein.

Abstract: This invention relates to methods of stimulating the activity of the human and animal enteric nervous system. The method comprises orally administering an aminoserol, such as squalamine, a naturally occurring aminosterol isolated from Squalus acanthias, or derivatives thereof, to a subject in need.

Abstract: This invention relates to methods of stimulating the activity of the human and animal enteric nervous system. The method comprises orally administering an aminoserol, such as squalamine, a naturally occurring aminosterol isolated from Squalus acanthias, or derivatives thereof, to a subject in need.

Abstract: The present invention provides compounds of Formula I, pharmaceutical compositions comprising these compounds and methods of using these compounds to prevent or treat FXR-mediated or TGR5-mediated diseases or conditions.

Abstract: An improved method of deprotection in solid phase peptide synthesis is disclosed. In particular the deprotecting composition is added in high concentration and small volume to the mixture of the coupling solution, the growing peptide chain, and any excess activated acid from the preceding coupling cycle, and without any draining step between the coupling step of the previous cycle and the addition of the deprotection composition for the successive cycle. Thereafter, the ambient pressure in the vessel is reduced with a vacuum pull to remove the deprotecting composition without any draining step and without otherwise adversely affecting the remaining materials in the vessel or causing problems in subsequent steps in the SPPS cycle.

Abstract: Cell culture devices, and related methods and kits, for modeling isotropic-to-anisotropic cellular transitions are provided. The devices can include a substrate having an isotropic film surface with one or more regions of aligned fibers dispersed thereon.

Abstract: The present disclosure provides methods and compositions for separating polypeptide glycoforms using a medium that includes an Fc receptor. In certain embodiments, a medium includes an Fc receptor which comprises an extracellular portion of an Fc gamma RIII receptor.

Abstract: The present invention relates to a novel polypeptide having affinity for proteins partially including a CH1-CL domain forming a non-native three-dimensional structure and capable of being suitably used for detecting, immobilizing, or removing these proteins and relates to use of the polypeptide. Specifically, disclosed are a polypeptide consisting of an amino acid sequence represented by any one of the following formulas 1 to 3: (1) P-Q-x-I-x-L-x-[IL]-[NT]-[YW] (SEQ ID NO: 1), (2) Y-D-P-E-T-G-T-W-P-Q-x-I-x-L-x-[IL]-[NT]-[YW] (SEQ ID NO: 4), and (3) P—N-S-G-G-G-G-S-Y-D-P-E-T-G-T-W-P-Q-x-I-x-L-x-[IL]-[NT]-[YW] (SEQ ID NO: 7) (wherein x represents an amino acid residue; and brackets represent any one of the amino acid residues within the brackets), and a method of using the polypeptide to detect, purify, or remove a protein partially including a CH1-CL domain forming a non-native three-dimensional structure.

Abstract: A process for separating aggregated proteins from monomeric proteins in a biological solution, the process including: providing at least one filter element having a contacting surface, wherein the filter element comprises filter media comprising: a porous substrate; and disposed on the porous substrate, a polymer comprising a hydrocarbon backbone and a plurality of pendant groups attached to the hydrocarbon backbone, wherein each of a first plurality of pendant groups comprises: (1) at least one acidic group or salt thereof; and (2) a spacer group that directly links the at least one acidic group or salt thereof to the hydrocarbon backbone by a chain of at least 6 catenated atoms; and allowing an initial biological solution to contact the contacting surface of the filter element N under conditions effective to separate the aggregated proteins from the monomeric proteins such that a final biological solution includes purified monomeric proteins.

Abstract: The present disclosure relates to methods of preparing and crystallizing ?-turn cyclic peptidomimetic salts of formula I: where R1, R2, R3, R4, R5, R6, R7, R8, R10, X, Y and n are as defined in the specification. The present disclosure provides a more efficient route for preparing a crystalline form of ?-turn cyclic peptidomimetic compounds and salts thereof.

Abstract: Compounds having activity for lowering parathyroid hormone levels are described. In one embodiment, the compounds are comprised of a contiguous sequence of subunits, X1-X2-X3-X4-X5-X6-X7, wherein the X1 subunit comprises a thiol-containing moiety and the distribution of charge on the X2-X7 subunits provides the desired activity. Methods of using the compounds for treating hyperparathyroidism, bone disease and/or hypercalcemic disorders are also described, and in particular, methods for lowering plasma PTH and serum calcium are provided. The compounds can be used to treat subjects having, for example: primary, secondary or tertiary hyperparathyroidism; hypercalcemia of malignancy; metastatic bone disease; or osteoporosis.

Abstract: Isolated peptides are disclosed. The peptide comprises an amino acid sequence selected from the group consisting of SEQ ID NOs: 1-5 and 11-15, with the proviso that the amino acid sequence does not consist of SEQ ID NO: 11, SEQ ID NO: 15 or SEQ ID NO: 1, wherein the peptide is no longer than 50 amino acids. Pharmaceutical compositions comprising same and uses thereof for treatment of diseases associated with serotonin transport and/or ?V?3 activity are also disclosed.

Abstract: In some aspects, the present invention provides cell-reactive compstatin analogs and compositions comprising cell-reactive compstatin analogs. In some aspects, the invention further provides methods of using cell-reactive compstatin analogs, e.g., treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides long-acting compstatin analogs and compositions comprising long-acting compstatin analogs. In some aspects, the invention further provides methods of using long-acting compstatin analogs, e.g., to treat a complement-mediated disorder, e.g., to inhibit complement-mediated damage to a cell, tissue, or organ. In some aspects, the invention provides targeted compstatin analogs and compositions comprising targeted compstatin analogs. In some aspects, the invention further provides methods of using targeted compstatin analogs, e.g., to treat a complement-mediated disorder, e.g.

Abstract: The ?c-family cytokines, Interleukin-2 (IL-2), Interleukin-4 (IL-4), Interleukin-7 (IL-7), Interleukin-9 (IL-9), Interleukin-15 (IL-15), and Interleukin-21 (IL-21), are associated with important human diseases, such as leukemia, autoimmune diseases, collagen diseases, diabetes mellitus, skin diseases, degenerative neuronal diseases and graft-versus-host disease (GvHD). Thus, inhibitors of ?c-cytokine activity are valuable therapeutic and cosmetic agents as well as research tools. Peptide and/or peptide derivative antagonists based on the consensus ?c-subunit binding site to inhibit ?c-cytokine activity are described. Also described are peptide and/or peptide derivative antagonists exhibiting Simul-Block activity, and inhibiting the activity of multiple ?c-cytokine family members.

Abstract: Solid state forms of Linaclotide, processes for their preparation, compositions comprising them and medical uses thereof are provided. The solid state forms of Linaclotide are useful in the preparation of other solid state forms of Linaclotide, particularly the amorphous form.

Abstract: Vasopressin-2 receptor agonists, pharmaceutical compositions thereof and methods for using the foregoing for treating diabetes insipidus, primary nocturnal enuresis, and nocturia.

Abstract: A method of controlling the impurities in a cyclosporin A eye gel. A high performance liquid chromatography is performed, and chromatographic conditions are as follows: the detection wavelength is 210-230 nm; the column temperature is 60-68° C.; the flow rate is 0.8-1 ml/min; and the mobile phase A is: THF-water-phosphoric acid. The method of controlling impurities solves the problem of excipients interference and separation of many impurities at the same time, it also provides an effective method for the formulation of quality standard of impurities in this kind of preparation.

Abstract: The present invention relates to embedding live or dead microrganisms and/or bioactive materials in a protective dry formulation matrix, wherein the formation includes the bioactive microorganism or material, a formulation stabilizer agent, and a protective agent. The formulation agent is prepared by dispersing all the solid components in a solution, with or without a vacuum, and cooling the solution to a temperature above its freezing temperature. The methods include a primary drying step of the formulation at a desired temperature and time period, and an accelerated secondary drying step under maximum vacuum and elevated temperature, to achieve a final desirable water activity of the dry material.

Abstract: The present disclosure relates to attenuated Zika viruses and vaccines, attenuated chimeric Zika viruses and vaccines, and to multivalent immunogenic compositions comprising Zika vaccines and vaccines to other flaviviruses. The chimeric Zika viruses includes a first nucleotide sequence encoding at least one structural protein from a Zika virus (ZIKV), a second nucleotide sequence encoding at least one nonstructural protein from a first flavivirus, and a third nucleotide sequence of a 3? untranslated region from a second flavivirus. The multivalent immunogenic compositions comprise an attenuated ZIKV vaccine or an attenuated chimeric ZIKV vaccine (or their combination) together with one or more of a first attenuated virus that is immunogenic against dengue serotype 1, a second attenuated virus that is immunogenic against dengue serotype 2, a third attenuated virus that is immunogenic against dengue serotype 3, and a fourth attenuated virus that is immunogenic against dengue serotype 4.

Abstract: The invention provides a recombinant polypeptide comprising the EDIII domain of each of Dengue virus serotype DENV-1, DENV-2, DENV-3, and DENV-4 linked to the N-terminal of HBsAg.

Abstract: The invention relates to an engineered outer domain (eOD) of HIV gp120 and mutants thereof and methods of making and using the same. The mutant eODs may be advantageous for the elicitation of CD4-binding site (CD4bs)-directed broadly-neutralizing antibodies (bnAbs) and/or improve binding to mature VRC01 and/or improve binding to germline VRC01 and the germlines of other VH1-2 derived broadly-neutralizing antibodies. The mutant eODs may also include glycan-masking mutations on eOD. The present invention also includes fusions of eOD to various protein multimers to enhance immunogenicity as well as the design of cocktails of different eODs that represent the full diversity of HIV sequences within the VRC01 epitope and surroundings.