Abstract: Compositions and methods relating to epitopes of sclerostin protein, and sclerostin binding agents, such as antibodies capable of binding to sclerostin, are provided.

Abstract: The invention provides monoclonal antibodies and related binding proteins that bind specifically to the envelope glycoprotein of H5 subtypes of avian influenza virus (“AIV”). The monoclonal antibodies and related binding proteins are useful for the detection of H5 subtypes of AIV, including the pathogenic H5N1 subtypes. Virus may be detected in formalin preserved, paraffin embedded specimens as well as frozen specimens and biological fluids. Accordingly, the invention provides for the diagnosis and surveillance of dangerous viral infections.

Abstract: The invention provides monoclonal antibodies and related binding proteins that bind specifically to the envelope glycoprotein of H5 subtypes of avian influenza virus (“AIV”). The monoclonal antibodies and related binding proteins are useful for the detection of H5 subtypes of AIV, including the pathogenic H5N1 subtypes. Virus may be detected in formalin preserved, paraffin embedded specimens as well as frozen specimens and biological fluids. Accordingly, the invention provides for the diagnosis and surveillance of dangerous viral infections.

Abstract: The invention provides variants of human growth hormone having an amino acid substitution at amino acid residue R77, numbered from the N-terminus of 191-amino add human growth hormone as well as nucleic acid molecules encoding these variants.

Abstract: A method has for selectively acylating an amino group in a peptide or protein which has two or more reactive nucleophilic functional groups is described.

Abstract: This invention relates generally to compositions comprising noribogaine and an excipient to facilitate transport across the blood brain barrier.

Abstract: A method of preparing a ribofuranose derivative essentially free of pyranose compounds includes a step of contacting a solution of MDR containing MDRP as an impurity in a solvent including methanol and/or tetrahydrofuran with at least one alkali metal periodate under conditions sufficient to oxidize at least a portion of the MDRP. MDR containing at most 5 wt % of MDRP based on the total weight of MDR and MDRP may be produced.

Abstract: The invention relates to novel classes of nucleotides that can be used as substrates for enzymes, e.g. for labeling nucleic acids.

Abstract: The present invention relates to recombinant cells and microorganisms of the phylum Labyrinthulomycota and their use in heterologous protein production. Novel promoter, terminator, and signal sequences for efficient production and, optionally, secretion of polypeptides from recombinant host cells and microorganisms are also encompassed by the present invention.

Abstract: The present invention provides screening kits, compositions, and diagnostic methods for determining whether a subject has a predisposition to, or likelihood of having, a substance use disorder by determining a nucleic acid methylation profile from a biological sample from the subject, wherein a given profile indicates that the subject has a predisposition to a substance use disorder.

Abstract: We have developed a versatile plant viral vector system based on Alternanthera mosaic virus (AltMV), suitable for infection by agroinfiltration or in vivo T7 transcripts from the same clone; agroinfection is enhanced by coinfiltration of a T7 RNA polymerase construct. Variants adapted for efficient protein expression, or for virus-induced gene silencing (VIGS), are based on a specific amino acid substitution (L88P) in the triple gene block 1 (TGB1) protein affecting RNA silencing suppression. A bipartite delivery system developed for AltMV delivers replicase (RdRp) functions separately from movement and encapsidation (TGB and coat protein, CP) functions by agroinfiltration, resulting in precise recombination of RdRp and TGB-CP constructs in planta. The bipartite delivery system has potential for high throughput protein expression or VIGS with the appropriate TGB1 variant, for hosts including Nicotiana benthamiana and Arabidopsis thaliana.

Abstract: This invention relates to a ribonucleic acid (RNA) based assay system for body fluid identification, and in particular to a novel, multiplex, parallel assay system based on messenger RNA expressed in human tissue, and to a method for using the same.

Abstract: Disclosed are methods for gender determination in the intron 1 region of the amelogenin locus and a newly discovered single nucleotide polymorphism (SNP) within the X chromosome of the amelogenin locus which can cause allelic dropout. Also disclosed are kits useful in gender determination.

Abstract: The present invention provides a novel aptamer for IgG and a method for utilizing the same and the like. More specifically, the present invention provides an aptamer that binds to an Fc region of IgG (e.g., human IgG); a complex comprising an aptamer and a functional substance bound thereto (e.g., affinity substance, labeling substance, enzyme, drug, toxin, drug delivery vehicle); a solid phase carrier with an aptamer or complex immobilized thereon; medical equipment comprising a solid phase carrier; a method for antibody purification comprising adsorbing an IgG antibody to a solid phase carrier, and eluting the adsorbed IgG antibody with an eluent; a method for producing a purified antibody, comprising preparing an IgG antibody and purifying the prepared IgG antibody with a solid phase carrier and the like.

Abstract: The present invention relates to methods of inhibiting S. aureus comprising inhibiting siderophore-mediated iron uptake, for example, staphyloferrm-mediated iron uptake Such methods of inhibiting S. aureus include the inhibition of staphyloferrm A- and staphyloferrm B-mediated uptake either by inhibiting expression or activity of staphyloferrm A and B or by inhibiting transport of staphyloferrm A and B The methods as provided would be useful for treating S. aureus infection.

Abstract: Bis-diazo, triaryl and aryldiazo-N-arylphenazonium quencher moieties, substituted with electron-withdrawing and electron-donating substituents which induce polarity in the delocalized aryl/diazo ring systems, are useful as labels when attached to biomolecules such as polynucleotides, nucleosides, nucleotides and polypeptides. The quencher moieties are non-fluorescent and accept energy transfer from fluorescent reporter labels by any energy-transfer mechanism, such as FRET. Fluorescence quencher compositions are useful in preparing quencher labeled biomolecules for various molecular biology assays based on fluorescence detection.

Abstract: The present invention relates to a novel family of monosaccharide derivatives and disaccharide derivatives and to a method of preparation thereof. A mono- and disaccharide derivatives according to the invention comprises at least one fatty acid ester and may further comprise one or more anionic groups and are useful for, inter alia, medical, pharmaceutical, cosmetic and food applications.

Abstract: A process for the preparation of water-soluble cellulose hydrolysis products, which comprises admixing cellulose with an ionic liquid in which the cellulose has at least some solubility, said ionic liquid state at a temperature at or below 150 -C, and treating the resulting solution with an acid in the presence of water, said acid having a pKa in water of less than 2 at 25 -C.

Abstract: A process is described for the preparation of water-soluble cellulose hydrolysis product. The process comprise admixing cellulose with an ionic liquid capable of solvating or dissolving at least some of the cellulose, said ionic liquid being a compound comprises solely of cations and anions and which exists in a liquid state at a temperature at or below 150° C., and in which the anions are selected from halide and cyanate; and treating the resulting solvate or solution with an acid in the presence of water, said acid having a pKa in water of less than 2 at 25° C.

Abstract: Novel glucocorticosteroids that are derivatives of isoxazolidine are useful as anti-inflammatory and antiallergic compounds.

Abstract: Inhibitors of HCV replication of formula (I) and the salts and stereoisomers thereof, wherein each dashed line (represented by represents an optional double bond; X is N, CH and where X bears a double bond it is C; R1 is —OR7, —NH—SO2R8; R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl; R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl; n is 3, 4, 5, or 6; R4 is C1-6alkyl or C3-7cycloalkyl; R5 is hydrogen, halo, C1-6alkyl, hydroxy, C1-6alkoxy, polyhaloC1-6alkyl; R6 is hydrogen, C1-6alkoxy, mono- or diC1-6alkylamino; or R5 and R6 may form a 5- or 6-membered unsaturated or partially unsaturated ring, optionally comprising one or two selected from O, N and S; R7 is hydrogen; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl; R8 is C3-7cycloalkyl optionally substituted with C1-6alkyl; C1-6alkyl optionally substituted with C3-7cycloalkyl; or —NR8aR8b; R8a and R8b are C1-6alkyl, or both may form a 5- or 6-membered saturat

Abstract: A compound of formula (I); or a salt or solvate thereof, wherein: the dotted line indicates the optional presence of a double bond between C2 and C3; R2 is selected from —H, —OH, =0, ?CH2, —CN, —R, OR, halo, ?CH—R, O—SO2—R, CO2R and COR; R7 is selected from H, R, OH, OR, SH, SR, NH2, NHR, NRR?, nitro, Me3Sn and halo, where R and R? are independently selected from optionally substituted C1-7 alkyl, C3-20 heterocyclyl and C5-20 aryl groups; R10 and R11 either together form a double bond, or are selected from H and YRY, where Y is selected from O, S and NH and R is H or C1-7 alkyl or H and SOxM, where x is 2 or 3 and M is a monovalent pharmaceutically acceptable cation; each X is independently a heteroarylene group; n is from 1 to 6; and RE is C1-4 alkyl. The compound is useful for the treatment of proliferative diseases.

Abstract: A compound of general formula 9, useful as potential antitumor agents against human cancer cell line and a process for the preparation of Pyrrolo[2,1-c] [1,4]benzodiazepine-benzothiazole or benzoxazole conjugates linked through piperazine of general formula 9 wherein: R, R1=H, F, OCF3, Cl, OMe; R2=OCH3 or H; n1 n2=3, 4; x=S or O.

Abstract: A method of preparing a compound represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and claims, comprises the step of: a) cyclizing a compound represented by Structural Formula A: under suitable reductive cyclization conditions to form a compound represented by Structural Formula B: wherein R10 is LG1 or —X1R1, and -LG1 is a suitable leaving group; and b) optionally, when R10 of Structural Formula (B) is LG1, further comprising the step of replacing the -LG1 of Structural Formula (B) with —X1R1 to form the compound represented by Structural Formula (I).

Abstract: Provided is a method for preparing (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors, and said method using 1-fluoro-4-nitrobenzen as a starting material. According to the method of the present invention, (S)-5-chloro-N-((3-(4-(5,6-dihydro-4H-1,2,4-oxadiazin-3-yl)phenyl)-2-oxooxazolidin-5-yl)methyl)thiophene-2-carboxamide derivatives of Formula (I) which are useful as blood coagulation factor Xa inhibitors can be prepared in a high purity and a high yield.

Abstract: Process for preparing a cyclic tertiary methylamine of the formula I where A is a C4-alkylene group, a C5-alkylene group or a —(CH2)2—B—(CH2)2— group, where B is oxygen (O) or an N—R1 radical and R1 is C1-C5-alkyl, aryl or C5-C7-cycloalkyl, wherein an amino alcohol II from the group consisting of 1,4-aminobutanol, 1,5-aminopentanol, aminodiglycol (ADG) or aminoethylethanolamine of the formula IIa where R1 is as defined above or is hydrogen (H), in which case R1?CH3 in the amine I, is reacted with methanol in a reactor at a temperature in the range from 150 to 270° C. in the liquid phase in the presence of a copper-comprising heterogeneous catalyst.

Abstract: The present invention relates to an improved method of preparing adefovir dipivoxil of Formula 1. The method of the present invention is characterized by using dimethylsulfoxide as a reaction solvent, and comprises a process of preparing adefovir dipivoxil of Formula 1 by allowing adefovir of Formula 2 to react with chloromethylpivalate at a reaction temperature of 30 to 50° C. under the presence of dimethylsulfoxide and triethylamine solvents.

Abstract: The present invention provides the compounds of formula (I): The present invention relates to imidazo[4,5-c]quinoline derivatives of formula (I), process for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases mediated by phosphatidylinositol-3-kinase (PBK) and/or mammalian target of rapamycin (mTOR) and/or tumor necrosis factor-? (TNF-oc) and/or interleukin-6 (IL-6), particularly in the treatment of cancer and inflammation.

Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.

Abstract: The disclosed compounds are useful in the treatment of mammalian cancers and especially human cancers. Compounds, pharmaceutical compositions, and methods of Formula I are disclosed: or a pharmaceutically acceptable salt, hydrate, solvate, enantiomer, stereoisomer, or tautomer thereof.

Abstract: Process for preparing 2,2-difluoroethylamine derivatives, wherein compounds of the general formula (IV) are hydrogenated to the corresponding 2,2-difluoroethylamine derivatives of the general formula (III), where the A, R1 and R2 radicals are each as defined in the description:

Abstract: The present invention provides pyrazole derivative compounds and pharmaceutically acceptable salts thereof. The compounds of the present invention have an excellent effect of preventing and treating osteoporosis.

Abstract: Pyridine compounds effective in modulation STAT3 and/or STAT5 activation are provided that are useful in the prevention and treatment of proliferative disease and conditions including cancer, inflammation and proliferative skin disorders.

Abstract: The invention is directed to compounds having the formula: wherein: Ar, r, n, X, R2-3 and R5-7 are as defined in the specification, and pharmaceutically acceptable salts thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. The invention is also directed to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.

Abstract: Organic dicarboxylic acid compounds, salts and preparation methods thereof are described. The compounds have activity of resisting oxidation damage to crystalline lens of eyes. The structures of the above organic dicarboxylic acid compounds are shown as wherein R is a hydrogen atom, a C1-3 alkyl group, a C1-3 alkoxyl group, or a halogen atom.

Abstract: The present invention relates to methods of initiating a reaction represented by scheme (1), wherein Q is optionally substituted aryl or optionally substituted heteroaryl; X is halogen or a sulphonate; P is an organic radical; R is hydrogen or an organic radical; wherein the catalyst comprises copper and a ligand; comprising providing the compound of formula III in liquid form prior to contacting the compound of formula III with the catalyst.

Abstract: The present invention relates to two main components, mahanine and mahanimbine (dehydroxy-mahanine) from Murraya koenigii for the treatment of glioblastoma and cervical carcinoma. Mahanimbine exhibited anti-cancer activity against lymphoid leukemia, myeloid leukemia, glioma, cervical carcinoma, pancreatic, colon and lung cancers in nineteen cells of different genetic status. C-3 hydroxy and NH groups are responsible contributing groups for their cytotoxicity. Mahanine reduced the doses of cisplatin and paclitaxel in cervical cancer showing better efficacy and useful as an adjunct chemotherapeutic agent to reduce toxicity these two drugs. A new cheap process for this preparation was established. EtOAc extract containing alkaloids enriched with mahanimbine and mahanine, is active against glioma and cervical cancers.

Abstract: Provided are a squarylium dye having a carboxyindolenine structure and an N-alkyl substituent, and a photoelectric conversion element having high photoelectric conversion efficiency in a near-infrared region and a dye-sensitized solar cell, both of which are produced using the squarylium dye. The photoelectric conversion element or dye-sensitized solar cell uses a compound represented by the formula (1) as the squarylium dye. In the formula (1), R1 and R2 represent a substituted or unsubstituted C5 to C30 alkyl group; X represents C(CH3)2; and A and B represent a carboxy group.

Abstract: Provided are pyrrolyl substituted dihydroindol-2-one derivatives represented by formula (I), pharmaceutically acceptable salts or solvates of said derivatives, or solvates of said salts, which are effective tyrosine kinase inhibitors. Also provided are the preparation methods of the above compounds, pharmaceutical compositions containing these compounds, and the use of these compounds in manufacturing drugs useful for the treatment or adjunctive treatment of tumors medicated by tyrosine kinases or proliferation or migration of tumor cells driven by tyrosine kinases in mammals (including human).

Abstract: The present invention relates to novel benzoyl derivatives of 3-aminocarbazole, to a pharmaceutical composition containing them, to a method for preparing them and to the use of such compounds for the production of a drug that is useful in the treatment or prevention of disturbances associated with the production of prostaglandin E2 (PGE2), for instance inflammatory processes, pain, fever, tumours, Alzheimer's disease and atherosclerosis.

Abstract: The present invention provides compounds represented by formula (1): wherein, R1, R2, R3 and R4 are as defined in the specification, in all their stereoisomeric and tautomeric forms and mixtures thereof in all ratios, and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates, pharmaceutically acceptable polymorphs and prodrugs. The invention also relates to processes for the manufacture of compounds of formula (1) and pharmaceutical compositions containing them. The compounds and the pharmaceutical compositions of the present invention are useful for the treatment of cancer. The present invention further provides a method of treatment of cancer by administering a therapeutically effective amount of the said compound of formula (1) or its pharmaceutical composition, to a mammal in need thereof.

Abstract: The present invention relates to tautomycetin (TTN) and analogs thereof. Also provided are methods of using TTN and analogs thereof in the treatment of various diseases relating to SHP2 function.

Abstract: The invention provides fluorescent schweinfurthin analogs of formula (I) which are useful as probes and for the treatment of cancer and other diseases.

Abstract: Provided herein are novel alkynyl and azide containing amino acids; kits containing these amino acids; peptides containing these amino acids; peptide macrocycles whose secondary structures are stabilized with linkers containing triazoles synthesized by reacting the side chains of the alkynyl and azide containing amino acids; and methods of making and using the alkynyl and azide containing amino acids, kits, peptides, triazole containing linkers, and peptide macrocycles.

Abstract: Provided are processes for making an amide of a carboxylic acid by reacting an amine of the formula (I) H—NR1R2??(I) wherein R1 and R2 are the same or different, R1 comprising a C1-C4-alkyl, and R2 comprising hydrogen or a C1-C4-alkyl, the amine having a lower boiling point than water, with a carboxylic acid with at least 3 carbon atoms per molecule, said carboxylic acid optionally comprising at least one alcoholic hydroxyl group per molecule, and selecting a molar ratio of amine to carboxylic acid in the range of from 1.5:1 to 1:1. The reaction step occurs under temperature and pressure conditions at which water and amine according to formula (I) are gaseous, and in a single reactor, the water formed together with any unreacted amine is distilled off, any unreacted amine is separated from the water and said the unreacted amine is reintroduced into the reaction mixture.

Abstract: The present invention relates to pharmaceutical dosage forms for topical administration comprising a tri-substituted glycerol compound or a pharmaceutically acceptable salt thereof. The invention also relates to a corresponding method for preparing such dosage forms as well as to their use as medicaments for the treatment of cancer and immune diseases.

Abstract: Provided herein are processes for preparing estolides and estolide base oils from fatty acid reactants utilizing catalysts. Further provided herein are processes for preparing carboxylic esters from at least one carboxylic acid reactant and at least one olefin.

Abstract: The invention relates to a novel hybrid organic-inorganic material containing an inorganic network of metal centers based on the element gallium, connected to each other by organic bridges, to the preparation and to the use thereof. The invention also relates to an intermediate solid obtained during the synthesis of said hybrid organic-inorganic material.

Abstract: The present techniques relate to catalyst compositions, methods, and polymers encompassing a Group 4 metallocene compound comprising bridging ?5-cyclopentadienyl-type ligands, typically in combination with a cocatalyst, and a activator. The compositions and methods presented herein include ethylene polymers with low melt elasticity.

Abstract: The present invention is directed to a manufacturing process for 1,2-diamino-cyclohexane-platinum(II) complexes, specifically to a manufacturing process for oxaliplatin. The process is straightforward, economical and applicable to industrial production. It comprises the reaction of (DACH)PtCl2 with silver sulfate (Ag2SO4) and the subsequent reaction of the resulting Pt sulfate complex (DACH)Pt(aq)2SO4 with barium oxalate (BaC2O4) or an equimolar mixture of barium hydroxide and oxalic acid to yield oxaliplatin in high purity with a low silver and low nitrate content.