Abstract: Compounds that modulate GluR5 activity and methods of using the same are disclosed.

Abstract: The present invention provides a pyrone derivative and a pyridone derivative, which are novel intermediates for synthesizing an anti-influenza drug, a method of producing the same, and a method of using the same.

Abstract: The present disclosure relates to substituted isothiazolo[5,4-b]pyridine-2-carboxamides of the formula I, in which R1, R2, R3, R10, R11 and X are as defined in the claims. The compounds of the formula I are inhibitors of transglutaminases, in particular transglutaminase 2 (TGM2), and are suitable for the treatment of various diseases, for example degenerative joint diseases such as osteoarthritis. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use as pharmaceuticals, and pharmaceutical compositions comprising them.

Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I, wherein the variables R1 and R2 are as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

Abstract: The invention relates to a process for preparing metal difluorochelatoborates, in which a metal bis(chelato)borate of the formula M[BL2] is reacted with boron trifluoride and a metal fluoride (MF) and/or a metal salt of the chelating ligand (M2L) where M+ is a monovalent cation selected from the group consisting of lithium, sodium, potassium and ammonium NR4+, where R?H, alkyl (C1 to C8) and L is a chelating agent having two terminal oxygen atoms and having the general formula (II), where: when m=1 and Y1 and Y2 together with C1 form a carbonyl group, n=0 or 1 and o=0 or 1 and R1 and R2 are each, independently of one another, H or alkyl having from one to eight carbon atoms (C1-C8) and Y3, Y4 are each, independently of one another, OR3 (R3?C1-C8-alkyl), then n or o?1: p=0 or 1 and when n and o=0, p=1; or Y1, Y2, Y3, Y4 are each, independently of one another, OR3 (R3?C1-C8-alkyl), m=1, n=0 or 1, o=1 and p=0; or C2 and C3 are members of a 5- or 6-membered aromatic or heteroaromatic ring (with N, O or S as heter

Abstract: The present invention relates to a novel ligand compound, a preparation method thereof, a transition metal compound including the ligand compound, and a preparation method thereof. The ligand compound of novel structure according to the present invention and the transition metal compound including the same may be used as a polymerization reaction catalyst for preparing olefin polymers.

Abstract: A method of producing an organic silicon compound includes a step of reaction of the following: (A) a reactive silane compound represented by General Formula (1) below: R1mSiY(4-m) (wherein R1 is a monovalent organic group (except for the group represented by Y) or a hydrogen atom; Y indicates a chlorine atom or a group represented by —OR2; R2 indicates a monovalent hydrocarbon group having 1 to 30 carbon atoms; and m is a number in the range of 0 to 3), (B) a halogenated organic compound represented by General Formula (2) below: R3—X (wherein R3 indicates a monovalent organic group; and X is a halogen atom), and (C) metallic magnesium (Mg) in the presence of (D) an organic solvent containing at least one type of ether type compound.

Abstract: A 4,6-hexadecadiene-2,4-dicarboxylic acid derivative represented by the following general formula (1) or a pharmaceutically acceptable salt thereof, each of which has an anti-tumor activity, and the like, are provided. [wherein, R1 represents hydroxy, —OR3 (wherein R3 represents optionally substituted lower alkyl or an optionally substituted aliphatic heterocyclic group), or —NR4R5 (wherein R4 and R5 may be the same or different, and each represents a hydrogen atom or optionally substituted lower alkyl) and R2 represents hydroxy or —OR6 (wherein R6 represents optionally substituted lower alkyl or optionally substituted aralkyl)].

Abstract: The present invention relates to chiral ligands deriving from ?- and ?-amino acids, and from metal complexes formed from the same. The ligands are useful with catalytic gold complexes, particularly Au(I) complexes.

Abstract: Water-soluble derivatives and/or prodrugs of acacetin are described herein. The compounds can be used as cardioprotection agents against myocardial infarction induced by ischemia-reperfusion. In one embodiment the compounds are used to treat ischemic cardiac diseases. In the preferred embodiment, the compounds are used to treat and/or prevent myocardial infarction in humans.

Abstract: Provided herein are synthetic methods for preparing a compound of formula (I): Also provided herein are synthetic methods for preparing a compound of formula (XIII): The disclosure also provides useful intermediates, derivatives, prodrugs, and pharmaceutically acceptable salts, solvates and hydrates of the formula (I) and formula (XIII) compounds. These compounds are useful for treating diseases associated with molybdenum cofactor deficiency.

Abstract: As a novel substance having a novel skeleton, a novel organometallic complex that can emit phosphorescence in the green to red wavelength region and has high emission efficiency and a high yield of synthesis is provided. One embodiment of the present invention is an organometallic complex in which a diketone having a five-membered or six-membered alicyclic structure composed of carbon and hydrogen is a ligand. In the formula, L represents a bidentate aromatic ligand and has at least a bond between carbon of an aromatic ring in the aromatic ligand and Ir. X represents a five-membered or six-membered alicycle composed of carbon and hydrogen. Further, R1 represents a substituted or unsubstituted alkyl group having 1 to 4 carbon atoms.

Abstract: There is provided a process for recovery of lignin from a black liquor that contains either soluble or dispersed lignin, generating a “liquid lignin” at high yield. Soluble lignin at elevated pH is precipitated by reducing the pH of the black liquor stream by countercurrent reaction with carbon dioxide, at elevated temperature and pressure, creating two bulk fluid phases: a heavy lignin-rich phase and a light lignin-depleted phase. The heavy lignin-rich phase is separated and washed countercurrently with a strong acid to displace metal cations from the lignin, creating a low-salt lignin, which is then formed into a low-dust high-bulk-density lignin fuel pellet. If needed, especially for lignin recovered from kraft papermaking black-liquor streams, an oxidation step is included to eliminate negative odor for high-value green-chemistry applications.

Abstract: This invention relates to novel aminoglycoside antibiotics, which have potent antimicrobial activity against bacteria, which induce infectious diseases, particularly MRSA, and has no significant nephrotoxicity, and process for producing them. More particularly, the present invention relates to compounds represented by formula (Ia) or their pharmacologically acceptable salts or solvates, or their diastereomer mixtures, antimicrobial agents comprising them, and a process for producing them.

Abstract: A method for suppressing activation of pancreatic stellate cells of a subject includes administering a composition comprising a therapeutically effective amount of Eruberin A. A method of preventing, alleviating or treating pancreatic tumors or pancreatic tumors related diseases includes administering a composition comprising a therapeutically effective amount of Eruberin A. The Eruberin A may be extracted from Pronephrium penangianum.

Abstract: Sialic acid derivatives of the formula (I) in which the symbols have the definitions stated in the description are suitable as medicaments, more particularly for diseases whose course is influenced by Siglec ligands.

Abstract: The subject matter of the invention is novel 2,3?-anhydro-2?-deoxy-5-fluorouridine derivatives of general formula 1 where R is a trifluoromethyl, 2,2,2-trifluoroethyl, difluoromethyl, perfluoroethyl, 1-fluoroethyl, 2-fluoroethyl, 1,1-difluoroethyl, 1,2-difluoroethyl, 2,2-difluoroethyl, 1,1,2-trifluoroethyl, 1,2,2-trifluoroethyl, 1,1,2,2-tetrafluoroethyl, 1,2,2,2-tetrafluoroethyl group. In a second aspect, the subject matter of the invention is a process for the manufacture of 2,3?-anhydro-2?-deoxy-5-fluorouridine derivatives of general formula 1. In a third aspect, the subject matter of the invention is an application of 2,3?-anhydro-2?-deoxy-5-fluorouridine derivatives of general formula 1 in the anticancer treatment of breast cancer, cervical cancer, lung cancer and nasopharynx cancer.

Abstract: The invention is directed to processes for synthesizing bicyclic nucleoside antiviral compounds and for synthesizing the intermediates used in the process. The invention is also directed to novel intermediate compounds useful in the process. The antiviral compounds are useful in the treatment of herpes zoster (i.e., varicella zoster virus, VZV, shingles) and for the prevention of post herpetic neuralgia (PHN) resulting from this viral infection.

Abstract: The present invention relates to a novel siRNA structure and the use thereof, and more particularly to a double-stranded siRNA molecule comprising an antisense strand and a sense strand, wherein the siRNA molecule has at least one single nucleotide bulge formed by introducing a single nucleotide into the antisense strand, particularly at position 2 from the 5? end, and to a method of using the same to silence a target gene. The siRNA molecule of the invention shows high target gene silencing efficiency while minimizing off-target effects caused by the antisense strand, and thus has improved target selectivity. Accordingly, the siRNA molecule of the invention can be substituted for conventional siRNA molecules and can be widely be used in siRNA-based gene silencing techniques, including gene therapy.

Abstract: The present invention relates to compounds, compositions, and methods for the study, diagnosis, and treatment of traits, diseases and conditions that respond to the modulation of gene expression and/or activity, and/or modulate a gene expression pathway. Specifically, the invention relates to double-stranded nucleic acid molecules including small nucleic acid molecules, such as short interfering nucleic acid (siNA) molecules that are capable of mediating or that mediate RNA interference (RNAi) against target gene expression.

Abstract: Modified human four helical bundle (4HB) polypeptides and uses thereof are provided.

Abstract: Bivalent multifunctional A? oligomerization inhibitors (BMAOIs) that target multiple risk factors involved in Alzheimer's disease are provided. The BMAOIs are useful for the treatment and/or prevention of Alzheimer's disease, as well as for diagnostic imaging of A? plaques in brain tissue. The BMAOIs comprise i) an A? oligomer (ApO)-inhibitor moiety which may have antioxidant activity (e.g. curcumin, curcumin derivatives, curcumin hybrids, resveratrol, etc.); ii) a cell membrane/lipid raft (CM/LR) anchoring moiety (e.g. cholesterol, cholesterylamine, a steroid, etc.); and iii) a spacer or linker moiety that stably links i) and ii) together.

Abstract: Provided is a method for solid phase synthesis of liraglutide, comprising the following steps: A), Fmoc-Gly-resin being obtained by coupling resin solid phase carrier with glycine with N-end protected by Fmoc(Fmoc-Gly-OH) in the presence of activator system; B) according to the peptide sequence of the main chain of liraglutide, successively coupling with amino acids with N-ends protected by Fmoc and protected side chains by the method for solid phase synthesis, wherein lysine employs Fmoc-Lys(Alloc)-OH; C) removing the protective group, Alloc, from the side chain of lysine; D) coupling the side chain of lysine with Palmitoyl-Glu-OtBu by the method for solid phase synthesis; E) cleavage, removing protection groups and resin to obtain crude liraglutide; F) purifying and lyophilizing to obtain liraglutide.

Abstract: Lysing may include agitating a specimen in a chamber along with a medium that includes a particulate lysing material that has an affinity for a biological material. Lysing material may include beads or other material which may be coated that facilitates binding. The medium may include a fluid with a high salt or low pH level. The biological material may be eluted by lowering a concentration of salt or increasing a pH level. Lysing materials with two or more different affinities may be employed. Heating may be used. Lysing may be performed in a flow through apparatus.

Abstract: Disclosed are RNA targeting compounds, methods for using the subject RNA targeting compounds to treat myotonic dystrophy and other diseases are also disclosed.

Abstract: The present invention provides a family of novel cytotoxic pentapeptides, which show potent antitumor activities against several cancer lines. The antibody-drug conjugates prepared from those pentapeptides can efficiently kill cancer cells.

Abstract: Macrocyclization of amino acids or linear peptides upon reaction with amphoteric amino aldehydes and isocyanides is provided.

Abstract: The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degareiix, its amino-protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degareiix itself. The manufacturing process comprises the step of cleaving the ?-amino protecting group P? from a Degareiix precursor according to formula {P4)(P?)Ac-AA1-AA10-NH2 in an organic solvent comprising the precursor and a cleaving agent dissolved therein: wherein P4 is a hydroxyl-protecting group or hydrogen, preferably hydrogen.

Abstract: The present invention relates to antibiotic compounds, methods for producing said compounds, pharmaceutical compositions comprising said compounds, and methods of treatment comprising administering said compounds and/or compositions comprising said compounds.

Abstract: Synthetic peptides which have non-narcotic type of analgesic action which may be used in medicine and pharmacology as anesthetic anodynes according to the general formula 1 [SEQ ID NO:1] H-XDL-XDL1-XDL2-L-Lys-L-Leu-XDL3-L-Thr-R2 (I) are disclosed.

Abstract: The present invention relates to the field of molecular imaging, i.e. nuclear and fluorescent imaging using metal ion radionuclides in combination with chelates highly functionalized with peptidic, nonpeptidic or protein ligands or additional signalling moieties.

Abstract: A method of inhibiting a binding event between a target protein and a binding protein, comprising administering to a cell in vitro an effective amount of a non-naturally occurring bifunctional inhibitor molecule including (a) protein binding moiety, and (b) an effector region, wherein the protein binding moiety binds to a blocking protein, and wherein the effector region binds to the target protein in order to bind the target protein and the blocking protein and prevent access of the binding protein to the target protein. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

Abstract: Disclosed is a Fusarium strain producing novel cyclic pentadepsipeptides which are of excellent multidrug resistance-reversing activity and inhibitory activity against cancer cells. Also, novel cyclic pentadepsipeptides are provided as active ingredients of the compositions useful in the treatment of cancer and diseases associated with multidrug resistance.

Abstract: The present invention relates to cGMP protein kinase (PKG) and regulatory domains and methods of use thereof. The structural determination of PKG domains is also described. cGMP independent PKG activators and uses thereof are also described.

Abstract: Compositions and methods for conferring pesticidal activity to bacteria, plants, plant cells, tissues and seeds are provided. Compositions comprising a coding sequence for pesticidal polypeptides are provided. The coding sequences can be used in DNA constructs or expression cassettes for transformation and expression in plants and bacteria. Compositions also comprise transformed bacteria, plants, plant cells, tissues, and seeds. In particular, isolated pesticidal nucleic acid molecules are provided. Additionally, amino acid sequences corresponding to the polynucleotides are encompassed. In particular, the present invention provides for nucleic acid molecules comprising nucleotide sequences encoding the amino acid sequence shown in SEQ ID NO:2, 3, or 4, the nucleotide sequence set forth in SEQ ID NO:1, 9, 10, or 11, as well as variants and fragments thereof.

Abstract: The invention provides recombinant Streptococcus mutans strains that can be used to improve oral health. An embodiment of the invention provides a method of reducing the incidence or severity of dental caries in a dental caries-susceptible host comprising administering orally to the host an isolated recombinant S. mutans strain of the invention in an amount effective for replacement of dental caries-causing S. mutans host strains in the oral cavity of the host. The isolated recombinant S. mutans strain 10 can be contained in a mouthwash, toothpaste, chewing gum, floss, chewable tablet, food, or beverage.

Abstract: The present disclosure generally provides non-naturally-occurring polynucleotide sequences that facilitate high-level expression of one or more gene products (e.g., polypeptides, RNA) of interest in Neisseria meningitidis. Methods of use of such sequences, e.g., use in vaccine production, are also provided.

Abstract: The present invention relates generally to the field of molecular biology and concerns a method for enhancing yield related traits by modulating expression in a plant of a nucleic acid encoding a BET1-like polypeptide. The present invention also concerns plants having modulated expression of a nucleic acid encoding this BET1-like polypeptide, which plants have enhanced yield-related traits relative to corresponding wild type plants or other control plants. The invention also provides constructs useful in the methods of the invention. The present invention relates generally to the field of molecular biology and concerns a method for improving various plant growth characteristics by modulating expression in a plant of a nucleic acid encoding a CRT (Calreticulin). The present invention also concerns plants having modulated expression of a nucleic acid encoding a Calreticulin, which plants have improved growth characteristics relative to corresponding wild type plants or other control plants.

Abstract: It is an object of the present invention to provide a protein that can successfully treats almost all patients with cedar pollinosis and can be ingested as a food. That is, the present invention provides a protein comprising an amino acid sequence represented by SEQ ID NO:1 or comprising an amino acid sequence having a mutation(s) in said amino acid sequence, and having an immunogenicity of a cedar pollen; a polynucleotide encoding said protein; a vector comprising said polynucleotide; a transformant comprising said polynucleotide or said vector; and intended uses of said protein, said polynucleotide, and said transformant.

Abstract: Described are specific-binding therapeutic and/or diagnostic proteins directed against Glypican-3 (GPC3), which proteins include muteins of a lipocalin protein, such as lipocalin 2 (Lcn2 or NGAL). The invention also relates to nucleic acid molecules encoding such proteins and to methods for generation and use of such proteins and nucleic acid molecules. Accordingly, the invention also is directed to pharmaceutical and/or diagnostic compositions comprising such lipocalin proteins, including uses of these proteins.

Abstract: The disclosure provides fusion polypeptides and constructs useful in delivering anionically charged nucleic acid molecules including diagnostics and therapeutics to a cell or subject. The fusion constructs include a protein transduction domain and a nucleic acid binding domain, or a protein transduction domain and a nucleic acid that is coated with one or more nucleic acid binding domains sufficient to neutralize an anionic charge on the nucleic acid. Also provided are methods of treating disease and disorders such as cell proliferative disorders.

Abstract: Increased in vivo and/or in vitro stability is imparted to a biologically active protein by fusing to an amino acid sequence consisting of at least about 100 amino acid residues, which consist essentially of Alanine, Serine and Proline, which form a random coil conformation. Specific examples are described. Also described are related nucleic acids, vectors and cells encoding such amino acids; compositions of biologically active proteins fused to a random coil domain, and methods of making and using the compounds and compositions of the invention.

Abstract: The present invention provides, among other things, compositions and methods for treatment of Friedrich's Ataxia based on effective targeting of a therapeutic moiety to mitochondria that can substitute for natural FXN protein activity or rescue one or more phenotypes or symptoms associated with frataxin-deficiency. In some embodiments, the present invention provides a targeted therapeutic comprising a therapeutic moiety, which is a polypeptide having an N-terminus and a C-terminus, a mitochondrial targeting sequence associated with the therapeutic moiety at the N-terminus, and a mitochondrial membrane-penetrating peptide associated with the therapeutic moiety at the C-terminus, wherein the therapeutic moiety is targeted to mitochondria upon cellular entry.

Abstract: The present invention relates to fibronectin based scaffold domain protein that bind interleukin 23 (IL-23). The invention also relates to the use of the innovative proteins in therapeutic applications to treat autoimmune diseases. The invention further relates to cells comprising such proteins, polynucleotide encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative proteins.

Abstract: The present invention relates to a use of mutant haptoglobin having angiogenesis-promoting activity and, more particularly, to a mutant haptoglobin polypeptide, a recombinant vector containing a polynucleotide encoding the polypeptide, or a composition for promoting angiogenesis containing, as an active ingredient, a transformant transformed with the recombinant vector. The mutant haptoglobin according to the present invention includes an amino acid sequence of SEQ ID NO: 1 in which the 143rd amino acid is substituted with an amino acid other than Arg. The mutant haptoglobin according to the present invention has excellent angiogenesis-promoting activity and excellent capillary-like tube formation capability as compared with wild-type haptoglobin, and promotes cell migration, and thus is useful as a therapeutic agent for treating diseases caused by non-angiogenesis.

Abstract: The present invention relates to a polypeptide, described as a lectin, its encoding nucleic acid sequence and antibodies to the polypeptide and their use in various medical applications, particularly for treating or preventing an autoimmune disorder, an inflammatory disorder or damaged skin in an animal.

Abstract: Disclosed is a peptide consisting of the identical amino acid sequence or a substantially identical amino acid sequence to the amino acid sequence depicted in SEQ ID NO:4, wherein the peptide binds to an HLA antigen and is recognized by cytotoxic T cells. The peptide of the present invention can be used in vivo or in vitro as an agent for inducing CTL, that is, cancer vaccine, and exerts therapeutic or ameliorating effects on tumors such as osteosarcoma, renal cancer, and others. The peptide of the present invention is also useful as a tumor marker directed to tumors such as sarcoma, renal cancer, and others.

Abstract: The present invention aims to provide a peptide having a superior Y2 receptor agonist action and useful as an agent for the prophylaxis or treatment of obesity and the like. A peptide represented by the formula: P1—X1-A25-A26-A27-A28-A29-A30-A31-A32-A33-A34-A35-A36-NH2 wherein each symbol is as described in the specification, or a salt thereof.

Abstract: Insulins to which there is connected an amino acid oligomer have satisfactory properties.

Abstract: The present invention relates to novel insulin analogs comprising mutations at position A14 in the A chain and at positions B27, B28, B29 and B30 in the B chain and exhibiting resistance towards protease; a method for the preparation of such insulin analogs; insulin preparations containing the insulin analogs of the invention; and, a method of treating diabetes mellitus using these insulin analogs.