Abstract: The present invention provides a compound of formula I? having BACE1 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease.

Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: The present application relates to novel benzyl-1H-pyrazolo[3,4-b]pyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.

Abstract: A method for the purification of lecithin, comprising the steps of: a. reducing the viscosity of lecithin to a viscosity of less than about 10 Pa·s; then b. mixing the lecithin with granulated active carbon; then c. separating the lecithin from the granulated active carbon and recover purified lecithin. Lecithin substantially free of poly-aromatic hydrocarbons, and a food or feed product comprising said lecithin.

Abstract: Novel monophosphite compounds having a methyl group, and a process for preparing these compounds, which are especially suitable for use as ligands in hydroformylation reactions.

Abstract: Novel monophosphite compounds having an ether group, and a process for preparing these compounds, which are especially suitable for use as ligands in hydroformylation reactions.

Abstract: The described invention provides organometallic complexes capable of spin transfer, comprising at least three different metals and the use of pharmaceutical compositions comprising such complexes in detoxification of reactive oxygen species in inflammatory conditions.

Abstract: The invention relates to hemin derivatives of general formula (I), preparing and use thereof as antibacterial and/or antiviral agents, including, as a component in a pharmaceutical compositions. Advantages of the antibacterial and antiviral agents based on the hemin derivatives are in their biocompatibility, biodegradability, a high efficacy against resistant bacteria and widespread viruses which are dangerous to humans, and the lack of toxicity.

Abstract: The present invention relates to novel glycomimetic compounds that are rationally designed to inhibit the binding of various pathogens to cell surface sialylated galactose and methods of use thereof. Specifically sialic acid glycosides and C-glycosides are disclosed that form a lactam ring structure or a cyclic ether/amine ring structure with the adjacent monosaccharide residue.

Abstract: The present invention relates to a novel polyene compound similar to nystatin, a method for preparing the same, and an antifungal drug comprising the novel polyene compound as an active ingredient. Compared to nystatin comprising one sugar, NNP, which is the polyene compound similar to nystatin, displays 300 times higher solubility and ten times lower cytotoxicity while maintaining antifungal activity, and thus can be useful in developing a novel polyene antifungal agent having improved solubility and less toxicity in terms of pharmacokinetics.

Abstract: Disclosed is a process for the preparation of partricin alkyl esters which involves reacting partricin in a solvent with primary alkyl alcohols in the quantity of 5 to 1000 moles per mole of partricin in the presence of carbodiimides, and optionally in the presence of acylation catalysts and/or nitrogen bases or anhydrous acids.

Abstract: The subject matter of the invention is novel 2?,5?-dideoxy-5-fluorouridine derivatives of general formula 1. wherein R1 denotes cinchona alkaloid fragment with defined absolute configuration at C-8 and C-9 atoms. In a second aspect, the subject matter of the invention is a process for the manufacture of 2?,5?-dideoxy-5-fluorouridine derivatives of general formula 1. In a third aspect, the subject matter of the invention is an application of 2?,5?-dideoxy-5-fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

Abstract: Disclosed herein are phosphorothioate nucleotide analogs, methods of synthesizing phosphorothioate nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with the phosphorothioate nucleotide analogs.

Abstract: The present application, among other things, provides technologies, e.g., reagents, methods, etc. for preparing oligonucleotides comprising phosphorothiotriesters linkages, e.g., oligonucleotides having the structure of IIIa, IIIb or IIIc. In some embodiments, provided methods comprise reacting an H-phosphonate of structure Ia or Ib with a silylating reagent to provide a silyloxyphosphonate, and reacting the silyloxyphosphonate with a thiosulfonate reagent of structure IIa or IIb to provide an oligonucleotide of structure IIIa or IIIb.

Abstract: A method for producing a dipeptide that has a protected N-terminal and is represented by formula (1) or a salt of the dipeptide, said method comprising condensing an ?-monosubstituted amino acid that has a protected N-terminal and is represented by formula (2) or glycine or a salt thereof with a disubstituted amino acid that is represented by formula (3) or a salt thereof in the presence of a condensing agent [in each of the formulae, substituents are as defined in the description or the like].

Abstract: Granzyme B inhibitor compounds, compositions that include the compounds, and methods for using the compounds. The compounds of the invention have advantageous water solubility and effectively inhibit Granzyme B.

Abstract: There are disclosed compounds that modulate the activity of inhibitors of apoptosis (IAPs), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.

Abstract: The present invention provides an application of an SP peptide or a derivative thereof in preparing medicines for preventing or treating asthma. The peptide or the derivative thereof is the SP peptide shown in Formula I or a pharmaceutically acceptable salt or ester thereof. The present invention also provides a method for treating asthma, the method comprises: administering to a patient with medicine containing the peptide or the derivative thereof with an effective therapeutic dosage. It proves through researches of the present invention that, the peptide or the derivative thereof can effectively alleviate pathological symptoms of asthma, especially pathological symptoms of allergic asthma. In the formula (I), Xaa1 is deletion, Ala, Gly, Val, Leu or Ile; Xaa2 is Thr or Ser; Xaa3 is Tyr, Phe or Trp; and Xaa4 is deletion, Ala, Gly, Val, Leu, Ile or Pro.

Abstract: Protease activated receptor 4 (PAR4) agonist peptides are disclosed. These peptides are useful for developing robust PAR4 receptor assays.

Abstract: Antagonist peptide of the bond between CD47 and a protein belonging to the thrombospondin family has the sequence S1 R1-R2-R3-S-Q-L-L-K-G-R4-R5-R6 and interacts specifically with the C-terminal end of the TSP, at the site of the bond between the TSP and the CD47 receptor. Interaction between the CD47 receptor and the protein is prevented. The peptide can be used in the context of cancer treatments.

Abstract: The present invention relates to peptidomimetics for reactivating p53. Methods of using the peptidomimetics are also disclosed.

Abstract: The present invention relates to novel linear and cyclic polypeptides that bind to IL-23 receptor and inhibit the binding of IL-23 to its corresponding receptor and cell signaling thereof. The novel polypeptides of the present invention has a core structure of WX1X2X3W, where W is tryptophan, and X1, X2 and X3 are amino acids, with the proviso that when one of X1, X2 or X3 is W, the remaining two of X1, X2 or X3 cannot be W. Preferred core structures include WVDYW or WQDYW. The present invention relates a composition containing the novel polypeptides (linear or cyclic), and use of same in inhibiting cell functions including production of IL-22 and IL-17F from immune cells as well as in treating IL-23 associated human diseases including, for example, inflammatory bowel diseases, psoriasis and Crohn's disease, ulcerative colitis and multiple sclerosis.

Abstract: The invention provides compounds of formula (I): and salts thereof, wherein X and Y have any of the values defined herein. The compounds inhibit bacterial RNA polymerase, inhibit bacterial growth, and have applications in, analysis of RNA polymerase structure and function, control of bacterial gene expression, control of bacterial growth, antibacterial chemistry, antibacterial therapy, and drug discovery.

Abstract: Polypeptides which have binding activity to an Fc region of immunoglobulin G and can be favorably used in detecting, purifying, immobilizing or removing an antibody, immunoglobulin G or a protein containing an Fc region of immunoglobulin G, are described. Methods for detecting, purifying, immobilizing or removing an antibody, immunoglobulin G or a protein containing an Fc region of immunoglobulin G, by using the peptide, are also described.

Abstract: The invention relates to a method for rapid immunogen selection (RIS) based on the binding a library of recombinant viruses containing randomized HIV gp120 variants of a surface polypeptide displayed to said neutralizing antibodies. The invention relates as well to the use of the HIV gp120 immunogens isolated according to the RIS method of the invention in medicine for the treatment of diseases caused by a virus and in diagnosis for the identification of neutralizing antibodies in a patient.

Abstract: The invention provides compositions of matter comprising a cowpea chlorotic mottle virus capsid protein (CCMV CP) and a ribonucleic acid, as well as methods for using such compositions. In such compositions, the cowpea chlorotic mottle virus capsid protein envelops the ribonucleic acid so as to for a capsid that can inhibit the degradation of the ribonucleic acid (e.g. by RNAses). A method of delivering a ribonucleic acid into the cytoplasm of a mammalian cell is also provided. Typically, the method comprises the steps of combining the mammalian cell with a composition of matter described herein under conditions selected to allow the cowpea chlorotic mottle virus capsid to contact the mammalian cell and deliver the ribonucleic acid into the cytoplasm of a mammalian cell.

Abstract: The present invention concerns gp19 immunoreactive compositions for E. canis and compositions related thereto, including vaccines, antibodies, polypeptides, peptides, and polynucleotides. In particular, epitopes for E. canis gp19 are disclosed.

Abstract: The present invention concerns gp19 immunoreactive compositions for E. canis and compositions related thereto, including vaccines, antibodies, polypeptides, peptides, and polynucleotides. In particular, epitopes for E. canis gp19 are disclosed.

Abstract: Provided are compositions are methods for discovery of new materials and interactions under extreme environmental conditions such as elevated temperatures at or in excess of 60° C. A synthetic thermostable protein is provided that is linked to a target peptide. A library of target peptides may be linked to a plurality of the thermostable proteins for expression on the cell surface of a thermophilic organism. The composition employs a modified form of the T. thermophilus TtoA protein that has a non-naturally occurring N-terminus for associating with a target peptide thereby expressing the target peptide on the outer cell membrane where the thermophilic protein is stable at high temperatures for discovery of materials useful in extreme environments or for us in study conditions that require or suffer under elevated temperatures.

Abstract: The present invention concerns VLPT immunoreactive compositions for E. chaffeensis and compositions related thereto, including vaccines, antibodies, polypeptides, peptides, and polynucleotides. In particular, epitopes for E. chaffeensis VLPT are disclosed.

Abstract: The present invention concerns VLPT immunoreactive compositions for E. chaffeensis and compositions related thereto, including vaccines, antibodies, polypeptides, peptides, and polynucleotides. In particular, epitopes for E. chaffeensis VLPT are disclosed.

Abstract: The present invention relates to isolated polypeptides having cellulolytic enhancing activity and isolated polynucleotides encoding the polypeptides. The invention also relates to nucleic acid constructs, vectors, and host cells comprising the polynucleotides as well as methods of producing and using the polypeptides.

Abstract: The present invention relates to a fusion peptide comprising dhFas-1 domain and MMP substrate and use thereof. More specifically, the present invention relates to a fusion peptide, comprising a) a dhFas-1 domain which is the fourth fas-1 domain of ?ig-h3 lacking H1 and H2 regions; b) a MMP (Matrix metalloproteinase) substrate; and c) a peptide comprising RGD motif and an use thereof for preventing and treating inflammatory disease. The fusion peptide of the present invention inhibits expension of rheumatoid arthritis by adhesion and migration of sinoviocytes and may be used for preventing or treating inflammatory disease by inhibiting infiltration of immune cells.

Abstract: Disclosed herein are proteins that include an immunoglobulin fold and that can be used as scaffolds. Also disclosed herein are nucleic acids encoding such proteins and the use of such proteins in diagnostic methods and in methods for evolving novel compound-binding species and their ligands.

Abstract: Nutritive proteins are provided. In some embodiments the nutritive proteins comprise at least one of a level of a) a ratio of branch chain amino acid residues to total amino acid residues present in the nutritive protein equal to or greater than the ratio of branch chain amino acid residues to total amino acid residues present in whey protein; b) a ratio of leucine residues to total amino acid residues present in the nutritive protein equal to or greater than the ratio of leucine residues to total amino acid residues present in whey protein; and c) a ratio of essential amino acid residues to total amino acid residues present in the nutritive protein equal to or greater than the ratio of essential amino acid residues to total amino acid residues present in whey protein.

Abstract: The invention provides a previously uncharacterized protein (gamma secretase activating protein or gSAP) that activates ?-secretase to produce ?-amyloid protein (A?). Deposition of A? has been associated with Alzheimer's disease and other pathologies. The invention thus additionally provides, e.g., screening methods and novel research tools, inhibitors of this novel protein, and methods of diagnosis, treatment and control of Alzheimer's disease and other neurodegenerative conditions associated with deposition of A?.

Abstract: Disclosed herein are isolated polypeptides, antibody preparations, treatment methods, diagnostic methods, and screening methods related to tauopathy. Generally, the isolated polypeptide includes a core pentapeptide, with the proviso that the isolated polypeptide is not a native full-length tau protein. Generally, the antibody preparations include antibody that specifically binds to SEQ ID NO:12. Generally, the treatment methods include administering to a subject a composition that includes the isolated polypeptide. Generally, the diagnostic methods includes contacting a sample from a subject with an antibody preparation that includes antibody that specifically binds to SEQ ID NO:12, and then detecting a ligand in the sample that specifically binds the antibody preparation.

Abstract: The present invention relates to a fusion protein resulting from the fusion of a cancer-specific antibody and an angiogenesis inhibitor, and relates to an anti-cancer composition including the same. More specifically, in the present invention, it is preferable that the cancer-specific antibody is trastuzumab or a fragment thereof, and the angiogenesis inhibitor is a VEGF-Trap. When the fusion protein according to the present invention is used, there are advantages in that angiogenesis and cancer cell growth can be effectively inhibited as compared to trastuzumab or VEGF-Trap, and side effects can also be reduced.

Abstract: The instant invention provides methods and compositions for modulation of the immune system. Specifically, the invention provides methods and compositions for increasing T cell mediated immune response useful in the treatment of cancer and chronic infection.

Abstract: A plastid transformation vector for stably transforming a plastid genome, comprising, as operably-linked components, a first flanking sequence, a DNA sequence coding for synthetic insulin-like growth factor-1 (IGF-1s) (SEQ ID NO. 1) or a substantially homologous DNA sequence of IGF-1s, which is capable of expression in the plastid genome, and a second flanking sequence.

Abstract: The present invention provides novel PAR 1 derived cytoprotective oligopeptides or polypeptides which typically contain at least the first 4 N-terminal residues that are substantially identical to the corresponding N-terminal residues of Met1-Arg46 deleted human PAR 1 sequence. These cytoprotective oligopeptides or polypeptides are capable of activating PAR 1 and promoting PAR 1 cytoprotective signaling activities. The invention also provides engineered cells or transgenic non-human animals which harbor in their genome an altered PAR 1 gene that is resistant to cleavage at Arg41 and/or Arg46 residues. Additionally provided in the invention are methods of screening candidate compounds to identity additional cytoprotective compounds or cytoprotective proteases. The invention further provides therapeutic use or methods of employing a PAR 1 derived cytoprotective oligopeptide or polypeptide to treat conditions associated with tissue injuries or undesired apoptosis.

Abstract: The technology described herein is directed to agents that reduce the level of oxidant-modified ET-B Cys405, Cys403, or Cys402 and the identification and use of such agents for, e.g. to treat hypertension.

Abstract: The present invention relates to compositions and methods for modulating angiogenesis in vivo, ex vivo or in vitro. More particularly, the invention relates to a soluble CD 146 protein usable in the context of human therapy, as well as to corresponding antibodies. Particular forms of CD 146, herein described, may be used to mobilize, in vivo or ex vivo, both mature and immature endothelial cells, as well as to increase their influence on angiogenesis. The invention also relates to compositions comprising such compounds, particularly pharmaceutical or diagnostic compositions, including kits and the like, as well as methods of therapy or diagnosis using said compounds, compositions and cells.

Abstract: The present invention relates to a chimeric receptor capable of signaling both a primary and a co-stimulatory pathway, thus allowing activation of the co-stimulatory pathway without binding to the natural ligand. The cytoplasmic domain of the receptor contains a portion of the 4-1BB signaling domain. Embodiments of the invention relate to polynucleotides that encode the receptor, vectors and host cells encoding a chimeric receptor, particularly including T cells and natural killer (NK) cells and methods of use.

Abstract: A chemoenzymatic method for the preparation of a homogeneous glycoprotein or glycopeptide, including (a) providing an acceptor selected from the group consisting of GlcNAc-protein and GlcNAc-peptide; and (b) reacting the acceptor with a donor substrate including an activated oligosaccharide moiety, in the presence of a catalyst comprising endoglycosidase (ENGase), to transfer the oligosaccharide moiety to the acceptor and yield the homogeneous glycoprotein or glycopeptide. The donor substrate includes, in a specific implementation, a synthetic oligosaccharide oxazoline. A related method of glycoprotein or glycopeptide remodeling with a predetermined natural N-glycan or a tailor-made oligosaccharide moiety, and a method of remodeling an antibody including a heterogeneous sugar chain, are also described. The disclosed methodology enables glycoprotein drugs to be modified for prolonged half-life in vivo, reduced immunogenicity, and enhanced in vivo activity, and for targeting and drug delivery.

Abstract: The invention encompasses formulations and methods for the production thereof that permit the delivery of concentrated protein solutions. The inventive methods can yield a lower viscosity liquid formulation or a higher concentration of therapeutic or nontherapeutic proteins in the liquid formulation, as compared to traditional protein solutions.

Abstract: A method for extracting IgY (?-livetin) from yolk is disclosed, which comprises the following steps: (A) providing a buffer solution, a yolk sample, and an inorganic salt solution; (B) diluting the yolk sample with the buffer solution to obtain a mixture, stirring the mixture for a predetermined time, and performing a centrifugation on the mixture to obtain a supernatant; and (C) adding the inorganic salt solution into the supernatant to salt out IgY, wherein a pH value of the buffer solution is in a range from 4.6 to 5.4, a salt concentration of the buffer solution is in a range from 0.05 M to 0.15 M, and a saturation degree of the inorganic salt solution is in a range from 30% to 60%.

Abstract: Provided is an anti-influenza virus antibody that exhibits neutralizing activity beyond the barrier of the two groups of influenza viruses categorized according to the conservativeness of hemagglutinin amino acids, a method of producing the same, and a test method for determining whether the subject carries the neutralizing antibody.

Abstract: The present invention is a composition and method for the prevention and treatment of a tauopathy. The composition of the invention includes N-terminal amino acid residues of the tau protein, which have been identified as being involved in toxic activation of a PP1/GSK3 signaling cascade and inhibition of fast axonal transport in human tauopathies.

Abstract: Compositions and methods are provided for treating diseases associated with CD100, including certain autoimmune diseases, inflammatory diseases, and cancers. In particular, anti-CD100 monoclonal antibodies have been developed to neutralize CD100.