Abstract: Presently provided are inhibitors of IDO and TDO and pharmaceutical compositions thereof, useful for modulating an activity of indoleamine 2,3-dioxygenase and tryptophan 2,3 dioxygenase; treating immunosuppression; treating a medical conditions that benefit from the inhibition of tryptophan degradation; enhancing the effectiveness of an anti-cancer treatment comprising administering an anti-cancer agent; treating tumor-specific immunosuppression associated with cancer; and treating immunosuppression associated with an infectious disease.

Abstract: Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof.

Abstract: Synthetic noribogaine preferably free of ibogaine and, optionally, one or more of other naturally occurring Tabernanth iboga alkaloids, is provided.

Abstract: The present invention provides, in part, compounds of Formula I: and pharmaceutically acceptable salts thereof and N-oxides thereof; processes and intermediates for preparation of; and compositions and uses thereof. The present invention further provides D1 agonists with reduced D1R desensitization, D1 agonists with a reduced ?-arrestin recruitment activity relative to Dopamine, D1 agonists interacting significantly with the Ser188 but not significantly with the Ser202 of a D1R when binding to the D1R, D1 agonists interacting less strongly with the Asp103 and interacting less strongly with the Ser198 of a D1R when binding to the D1R, and their uses.

Abstract: Macrocycle containing carbamate compounds that inhibit HIV proteolytic enzymes and processes for preparing them are described. Compositions and methods for treating a patient infected with HIV are described.

Abstract: Monomers having the structure and a polymer comprising as part of its polymer backbone a moiety of Formula (II): where one of R6 to R10 represents A-O— and one of R6 to R10 represents —O—B and the remainder of R6 to R10 represent H, where A and B represent the remainder of the polymer backbone and may be the same or different.

Abstract: Provided are compounds which are useful for controlling microorganisms in aqueous or water-containing systems or in systems which are exposed to moisture, including at elevated temperature. The antimicrobial compounds are of the formula I: wherein n, R1, R2, R3, and X are as defined herein.

Abstract: The present invention provides thiazole compounds of Formula I wherein X1, X2, X3, X4, X5, R1, R2, R4, R5, R6, R7, and W, and ring AA, are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrugs, or esters or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.

Abstract: The present invention relates to novel spiro-oxazine analogues of Formula-I and Indolinone compounds of Formula-II or positional isomers, or stereoisomers, or derivatives, or pharmaceutically acceptable salt thereof. Formula-I Formula-II Further the invention provides transition-metal free multicomponent reaction (MCR) process for the preparation of said compounds of Formula-I and II using aryne precursor, N-substituted isatin and N-heteroaromatic compound as the nucleophile, under mild condition leading to formation of desired complex of spiro-oxazine analogues (I) and indolinone analogues (II) in high yield and selectivity.

Abstract: The present invention relates to new imidazo[2,1-b]thiazole derivatives having a great affinity for sigma receptors, especially sigma-1 receptors, as well as to the process for the preparation thereof, to compositions comprising them, and to their use as medicaments.

Abstract: Provided are compounds of Formula (I), or pharmaceutically acceptable salts thereof, wherein i.a. Ring A is phenylene or 5- to 6-membered heteroarylene; Ring B is phenylene, 5- to 6-membered heterocycloalkylene or 5- to 6-membered heteroarylen; R4 is absent, heteroarylene, arylene, C1-3 alkylene, or R4 and R3 taken together with the nitrogen to which they are bound form a 3- to 7-membered heterocycloalkyl ring; R5 is absent, C(O)NR51, NR52 or O; R6 is C2-10 alkylene or alkenylene, wherein one or two of the carbon atoms in the alkylene chain is optionally replaced by an O, S, SO, SO2 or NR61, and wherein two of the carbon atoms in the alkylene chain are optionally connected by a two or three carbon atom alkylene chain to form a 5- to 7-membered ring; R7 is absent, NR71 or O. The compounds are IRAK4 inhibitors useful for the treatment of inflammatory diseases.

Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. 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 vapor deposition (MOCVD) or metal organic vapor phase epitaxy (MOVPE). The novel method according to the invention is characterized 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: Provided are compounds useful for controlling endoparasites both in animals and agriculture. Further provided are methods for controlling endoparasite infestations of an animal by administering an effective amount of a compound as described above, or a pharmaceutically acceptable salt thereof, to an animal, as well as formulations for controlling endoparasite infestations using the compounds described above or an acceptable salt thereof, and an acceptable carrier.

Abstract: The present invention relates to fungicidal N-[(trisubstitutedsilyl)methyl]carboxamide or its thiocarboxamide derivatives with formula: their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.

Abstract: Mercaptosilanes are disclosed of the formula I wherein R1 is an alkyl polyether group —O—(R5—O)m—R6. They are prepared by a procedure in which a silane of the formula II is subjected to a catalyzed reaction with an alkyl polyether R1—H, R7—OH being split off, the molar ratio of the alkyl polyethers R1—H to the silane of the formula II is at least 0.5 and R7—OH is separated off from the reaction mixture continuously or discontinuously. They can be used in shaped articles.

Abstract: A method of preparing racemic or optically active D or L-?-glycerophosphorylcholine in large amounts by subjecting choline phosphate or a salt thereof, and racemic or optically highly pure (S) or (R)-3-halo-1,2-propanediol to a substitution reaction in a medium at high temperature in the presence of an inorganic base which increases the activity of the reaction. The method is cost-effective because of the use of starting materials which are inexpensive compared to those in a conventional method. Moreover, the method is simple and convenient because it is performed via a one-pot reaction without a separate purification process. In addition, it enables a large amount of racemic or optically active D or L-?-glycerophosphorylcholine, or a salt thereof, to be quantitatively produced in a medium without side reactions by using the inorganic base which increases the reaction activity.

Abstract: Inhibitors of RSV replication of formula RI including stereochemically isomeric forms, and salts or solvates thereof, wherein R22, W, Q, V, Z p, s, and Het have the meaning as defined herein. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other RSV inhibitors, in RSV therapy.

Abstract: Bisphosphites having an outer naphthyl-phenyl unit.

Abstract: Tetradentate and octahedral metal complexes suitable for use as phosphorescent or delayed fluorescent and phosphorescent emitters in display and lighting applications.

Abstract: The purpose of the invention is to provide a novel organometallic compound that can be utilized as a catalyst having high generality, high activity, and excellent functional group selectivity. The invention pertains to a novel organometallic compound represented by general formula (1) that catalyzes a reductive amination reaction.

Abstract: Compounds of Formula (A) are described herein and the uses thereof for the treatment of diseases, conditions and/or disorders mediated by pharmaceutical compositions and the uses thereof as asialoglycoprotein receptor (ASGPR) targeting agents.

Abstract: Provided herein are formulations, methods and substituted 2?-chloro aminopyrimidinone and pyrimidine dione compounds of Formula (I) for treating Pneumovirinae virus infections, including respiratory syncytial virus infections, as well as methods and intermediates for synthesis of substituted 2?-chloro aminopyrimidinone and pyrimidine dione compounds.

Abstract: The disclosure relates generally to methods, systems, compositions and kits for breaking a water-in-oil emulsion including one or more biomolecules dispersed in an aqueous phase of the water-in-oil emulsion. In some embodiments, the disclosure relates to obtaining a first emulsion including a continuous hydrophobic fraction and a discontinuous aqueous fraction, the aqueous fraction having one or more biomolecules dispersed therein, breaking the first emulsion by contacting the first emulsion with a breaking solution including a second emulsion, where the second emulsion includes a discontinuous phase of organic extraction solvent dispersed in a continuous aqueous phase, and centrifuging to separate the phases of the resulting mixture.

Abstract: The present disclosure relates to methods of increasing the extraction of an apoplast-targeted recombinant protein in a plant tissue and to methods of increasing the purity of an apoplast-targeted recombinant protein recovered from a plant tissue. The methods involve contacting plant tissue with a rinse fluid on a plurality of occasions to release recombinant protein from the apoplast into the rinse fluid to create an apoplast wash fluid. The resulting content of the recombinant protein in the apoplast wash fluid is higher than the content of the recombinant protein in the apoplast wash fluid from comparable plant tissue contacted with rinse fluid on a single occasion.

Abstract: Disclosed is a collagen powder and/or a collagen derivative powder, which are obtained by dispersing in a hydrophilic organic solvent a crude collagen precipitate which comprises 12 to 50% by mass of a collagen precipitate and/or a collagen derivative precipitate having an average particle size of 1 to 1,000 ?m, recovering solids and then drying the solids. By dispersing the crude collagen precipitate in the hydrophilic organic solvent, the resulting precipitates can be dehydrated, so that drying of the thus obtained solids can be done by air-drying. In addition, the resulting collagen powder and/or collagen derivative powder exhibit excellent solubility due to an increased specific surface area and also have excellent ease of handling with the average particle size being 8 to 1,000 ?m.

Abstract: A method of purifying a fusion protein, including: (1) adjusting the pH of an aqueous phase, containing a fusion protein which is a fusion of a protein having a self-assembly capability and a tamet protein, and which aqueous phase has a first pH, to a second pH, to obtain a remaining aqueous phase and a solid fraction containing an amount of the fusion protein; (2) separating the solid fraction from the remaining aqueous phase, to obtain a separated solid fraction; and (3) dissolving the separated solid fraction in a solution having a pH of 12 or lower but higher than the second pH by at least 0.1 pH units, wherein the protein having a self-assembly capability is a cell surface protein.

Abstract: An excellent peptidyl peptidase-IV inhibitor and the like are provided. A peptide consisting of Val-Pro-X wherein X represents an amino acid residue (except for L-proline residue); the aforementioned X is preferably one selected from a basic amino acid residue, an aliphatic neutral amino acid residue, an amide group-carrying neutral amino acid residue, or an aromatic group-carrying neutral amino acid residue; the aforementioned X is preferably one selected from an alanine residue, a glutamine residue, a methionine residue, an asparagine residue, a glycine residue, a valine residue, a tyrosine residue, a serine residue, and a lysine residue; a dipeptidyl peptidase-IV inhibitor, a blood sugar rise suppressing agent, a vascular endothelial disorder suppressing agent, and an angiotensin converting enzyme inhibitor containing the aforementioned peptide as an active ingredient.

Abstract: Potent compounds having combined antioxidant, anti-inflammatory, anti-radiation and metal chelating properties are described. Short peptides having these properties, and methods and uses of such short peptides in clinical and cosmetic applications are described.

Abstract: The invention relates to a peptide compound and its pharmaceutical composition for inhibiting platelet aggregation and preventing/treating thrombogenic diseases. The invention develops pentapeptides and hexapeptides derived from snake venom C-type lectin-like proteins (CLPs) fragments, which can inhibit platelet aggregation and have antithrombotic activity without hemorrhagic tendency. Accordingly, they can be used as potential agents for the prevention and therapy of thrombogenic diseases.

Abstract: Sustained-release compositions wherein a water-soluble physiologically active peptide is substantially uniformly dispersed in a microcapsule comprised of a lactic acid polymer or a salt thereof, and the physiologically active substance is contained in an amount of 15 to 35 wt/wt % to the total microcapsules and weight-average molecular weight (Mw) of the lactic acid polymer is about 11,000 to about 27,000, which is characterized by having a high content of the physiologically active substance, and suppression of the initial excessive release within one day after the administration and a stable drug sustained-release over a long period of time, and method for producing the same.

Abstract: The present invention relates to a novel endocytic motif, and in particular, to a fusion polypeptide including the motif represented by an amino acid sequence of SEQ ID NO. 1 and a protein transduction domain, a pharmaceutical composition for preventing or treating cancer including the same, and a method for treating cancer including the step of administering the composition. The present invention shows the effects of suppressing metastasis, infiltration, angiogenesis, and growth of cancer by specifically inhibiting c-Met endocytosis and effectively inhibiting HGF/c-Met signaling pathway associated with metastasis and growth of various types of cancer cells. Therefore, the present invention can be applied to an anticancer agent for various types of cancer.

Abstract: The present invention provides pharmaceutical compositions and methods of treating lower gastrointestinal disorders, including inflammatory bowel disease (IBD), diverticulitis, colon cancer, an inflammatory disorder, obesity, congestive heart failure, benign prostatic hyperplasia (BPH), pain, salt retention or fluid retention.

Abstract: In an embodiment, the present disclosure pertains to a composition for inhibiting calcium oxalate monohydrate crystal growth comprising at least one isolated polypeptide comprising a plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal; and a plurality of amino acids spacers, wherein the amino acid spacers are arranged in varying sequences between the plurality of amino acids that bind the surface of the calcium oxalate monohydrate crystal. In some embodiments, the present disclosure related to a method of controlling calcium oxalate monohydrate crystal growth in a subject in need thereof comprising administering to the subject therapeutically effective amount of the calcium oxalate monohydrate inhibiting polypeptide. In some embodiments, the present disclosure relates to a method of identifying calcium oxalate monohydrate inhibiting peptides.

Abstract: Polypeptides belonging to the family of late proteins of the cornified envelope (LCE), fragments of the polypeptide, isolated nucleotide sequences encoding the polypeptides, and cosmetic and/or pharmaceutical compositions containing such polypeptides are described. The polypeptides have cosmetic and/or therapeutic use to reinforce the barrier function of the epidermis, prevent and/or treat the signs of skin dryness and prevent and/or treat disorders of the barrier function or the weakening of the epidermis.

Abstract: ?-Hairpin peptidomimetics of the general formula cyclo(-Tyr1-His2-Xaa3-Cys4-Ser5-Xaa6-DPro7-Xaa8-Arg9-Tyr10-Cys11-Tyr12-Xaa13-Xaa14-Xaa15-Pro16-), disulfide bond between Cys4 and Cys11, and pharmaceutically acceptable salts thereof, with Xaa3, Xaa6, Xaa8 Xaa13, Xaa14 and Xaa15 being amino acid residues of certain types which are defined in the description and the claims, have favorable pharmacological properties and can be used for preventing HIV infections in healthy individuals or for slowing and halting viral progression in infected patients; or where cancer is mediated or resulting from CXCR4 receptor activity; or where immunological diseases are mediated or resulting from CXCR4 receptor activity; or for treating immunosuppression; or during apheresis collections of peripheral blood stem cells and/or as agents to induce mobilization of stem cells to regulate tissue repair. These peptidomimetics can be manufactured by a process which is based on a mixed solid-and solution phase synthetic strategy.

Abstract: The present invention provides a new type of alpha-helix nucleating cross-link (“staple”) formed by olefin metathesis of a proline derivative with an alkenyl side chain and another amino acid derivative with an alkenyl side chain. The proline derivatives as described herein have been found to be strong nucleators of alpha-helix formation. The invention also provides moieties for shielding the free amide N—H's at the N-terminus of an alpha-helix, thereby further stabilizing the helix. The proline derivatives, precursors prior to cross-linking, and the cross-linked peptides are provided as well as methods of using and preparing these compounds and peptides.

Abstract: Compounds of formula I: or pharmaceutically acceptable salts thereof, wherein the various substituents are defined herein, methods of using said compounds, and pharmaceutical compositions containing said compounds.

Abstract: Disclosed herein is a synthetic peptide, which has an amino acid sequence that has 20-39 amino acid residues. The synthetic peptide has at least 80% amino acid sequence identity to SEQ ID NO: 1, and includes at least 20 consecutive residues that has at least 90% amino acid sequence identity to residues 11-30 of SEQ ID NO: 1. Also disclosed herein are compositions containing the synthetic peptide and applications thereof. According to various embodiments of the present disclosure, the synthetic peptide is useful in promoting stem cells proliferation or wound healing.

Abstract: Described herein are small peptide domains and consensus sequences that bind small target molecules of industrial importance, e.g., metals such as nickel, ? carotene, and isoflavones such as genistein. Also described are fusion proteins containing such binding domains fused to proteins or to peptide domains like GST or CBD that bind other ligands and can be used to immobilize the target binding domain on a support. One class of fusion proteins that is useful in industrial settings are fusions that contain concatemers of target binding domains, which increases the binding equivalents per molecule.

Abstract: A process of purifying copolymer peptides such as COP-1 polypeptides by ultrafiltration can be improved by treating the polypeptide solution with an acid before, or during the early stages of, the ultrafiltration. By adding the acid and/or forming an acid addition salts of the polypeptide before ultrafiltration is conducted permits for faster ultrafiltration. Likewise, adding the acid in the ultrafiltration process but before polypeptide precipitation or clogging occurs can also improve the efficiency/convenience of the ultrafiltration step.

Abstract: The present invention relates to novel bacteriophages specific to Klebsiella pneumoniae strains, and compositions comprising the same. Particularly, polypeptides and their coding nucleic acid molecule of the novel bacteriophages are provided. The invention also relates to applications of the novel bacteriophages and the polypeptides in the detection/treatment/prevention of infection caused by Klebsiella pneumoniae strains. Development of immunogen and vaccine on the basis of the polypeptides are also provided.

Abstract: An artificial polypeptide fiber of the present invention is an artificial fiber containing a polypeptide as a main component, and has a stress of 350 MPa or more and a toughness of 138 MJ/m3 or more. A method for producing an artificial polypeptide fiber of the present invention is a method for producing the artificial polypeptide fiber obtained by spinning a spinning solution (6) containing a polypeptide derived from natural spider silk proteins and performing drawing of at least two stages. The drawing of at least two stages includes a first-stage drawing (3) in wet heat and a second-stage drawing (4) in dry heat. Thereby, the present invention provides high-toughness artificial polypeptide fibers having favorable stress and rupture elongation, and a method for producing the same.

Abstract: Described are mutant Nav1.7 sodium channel alpha-subunits and nucleic acid sequences encoding such mutants. Further described are methods for characterizing a nucleic acid sequence that encodes a Nav1.7 sodium channel alpha-subunit, methods for determining a Nav1.7 haplotype, methods for determining a subject's predisposition to a neurologic disorder associated with a sodium channel mutation, and methods of identifying a compound that modulates mutant Nav1.7 sodium channels. Other materials, compositions, articles, devices, and methods relating to mutant Nav1.7 sodium channels are also described herein.

Abstract: The invention relates to cellular localization signals. In particular, the invention relates to endoplasmic reticulum localization signals in monomeric or multimeric form. The localization signals are utilized as research tools or are linked to therapeutics. Disclosed are methods of making and using polypeptides and modified polypeptides as signals to localize therapeutics, experimental compounds, peptides, proteins and/or other macromolecules to the endoplasmic reticulum of eukaryotic cells. The polypeptides of the invention optionally include linkage to reporters, epitopes and/or other experimental or therapeutic molecules. The invention also encompasses polynucleotides encoding the localization signals and vectors comprising these polynucleotides.

Abstract: A cDNA, including the nucleotide sequence represented by SEQ ID NO: 2. A cDNA, including a nucleotide sequence encoding a complete protein, a protein fragment, a protein analog, or a protein derivative each including the amino acid sequence represented by SEQ ID NO: 1. A cDNA, including the nucleotide sequence encoding the amino acid sequence represented by SEQ ID NO: 1.

Abstract: In certain aspects, the present invention provides compositions and methods for inducing utrophin expression in muscle with an ActRIIB protein as therapy for muscular dystrophy. The present invention also provides methods of screening compounds that modulate activity of an ActRIIB protein and/or an ActRIIB ligand.

Abstract: Four and a Half LIM domains protein 1 (FHL-1) mutations at positions 128 or 224 that are associated with X-linked muscular myopathy, methods of screening subjects to identify those susceptible to muscular myopathy including muscular dystrophy and cardiomyopathy and kits.

Abstract: The present invention relates to tumor immunotherapy, in particular to tumor vaccination, using chimeric proteins comprising all or a portion of a hepatitis B virus core antigen protein and an amino acid sequence comprising an epitope derived from the extracellular portion of a tumor-associated antigen. In particular, the present invention provides virus-like particles comprising said chimeric proteins, which are useful for eliciting a humoral immune response in a subject against the tumor-associated antigen, in particular against cells carrying said tumor-associated antigen on their surface, wherein the tumor-associated antigen is a self-protein in said subject.

Abstract: The present invention relates to a proNGF mutant and to uses thereof, in particular the use of a proNGF mutant for producing human beta-NGF. The present invention discloses a method of preparing a biologically active human beta-NGF from an inactive insoluble proNGF mutant. A proNGF mutant of the invention is substituted by any amino acid but not Arg or Lys at the native protease cleavage site R1SK3R4 at least at positions R1 and K3 corresponding to positions 101 and 103 of the human wildtype proNGF sequence.