Abstract: A crystalline methyl (4R,12aS)-7-(benzyloxy)-4-methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-pyrido[1?,2?:4,5] pyrazino[2,1-b][1,3]oxazine-9-carboxylate of the formula (U2):

Abstract: A process for preparing a compound represented by formula (Y1) or (Y2) [wherein Rx is an optionally substituted carbocyclyl lower alkyl, or the like] or a salt thereof, using a novel process for preparing a pyridone derivative represented by formula (X4) [wherein R1d is hydrogen, halogen, or the like; R2d is hydrogen, a lower alkyl optionally substituted with substituent E, or the like; R4d is a lower alkyl optionally substituted with substituent E, or the like; and R6d is a lower alkyl group optionally substituted with substituent group E, or the like].

Abstract: The disclosure generally relates to compounds of formula I, including compositions and methods for treating human immunodeficiency virus (HIV) infection. The disclosure provides novel inhibitors of HIV, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

Abstract: Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction. Provided herein are methods for the synthesis of cephalosporin compounds of formula (I) employing a palladium-catalyzed alkylation reaction, as well as compositions related to the same. In an aspect, provided herein is a method for preparing a compound of formula (II), or a salt thereof, comprising the step of admixing, e.g., reacting, a compound of formula (III), or a salt thereof, with a nucleophile (Nuc) in the presence of reagents comprising: (a) a palladium source; and (b) a palladium-binding ligand, to form a compound of formula (II), or a salt thereof.

Abstract: The present invention is related to crystalline forms of (S)-7-(1-(9H-purin-6-ylamino)ethyl)-6-(3-fluorophenyl)-3-methyl-5H-thiazolo[3,2-a]pyrimidin-5-one which is a PI3K inhibitor useful in the treatment of cancer and other diseases.

Abstract: Provided herein are the metalloborane compounds, MOF-metalloborane compositions, and hydrogen storage system used for high density hydrogen storage. The compounds and compositions may have the structure M2B6H6 or MOF-M2B6H6-dicarboxylic acid. Particularly the transition metal M may be titanium or scandium and the MOF may be MOF5. The hydrogen storage systems hydrogen absorbed to the metalloborane compounds or to the MOF-metalloborane compositions. Methods of storing hydrogen are provided comprising flowing or passing hydrogen gas for absorptive contact with the metalloborane compounds or to the MOF-metalloborane compositions. Also provided is a method for calculating the hydrogen storage capacity of a metalloborane is provided in which random sampling of the thermodynamic states of a two-system model of hydrogen in the presence of a metal organic framework-metalloborane crystal structure is used to calculate probability of hydrogen absorption.

Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Abstract: The present invention describes chemical systems and methods for silylating N—H bonds of aliphatic amines, said system or method comprising or consisting essentially of a mixture of (a) at least one organosilane and (b) at least one hydroxide, especially KOH, said system being preferably, but not necessarily substantially free of a transition-metal compound, and said methods comprising contacting a quantity of the organic substrate with a mixture of (a) at least one organosilane and (b) at least one strong base, under conditions sufficient to replace an N—H bond with a silyl N—Si bond.

Abstract: A fluorine-containing alkylsilane compound represented by the general formula: CF3(CF2)n(CH2CF2)a(CF2CF2)b(CH2)3SiR3-dXd??[I] wherein n is an integer of 0 to 5; a is 1 or 2; b is an integer of 0 to 3; R is a C1-C3 alkoxy group, a fluorine-containing alkoxy group, or an alkenyl group; X is halogen; and d is an integer of 0 to 3. The fluorine-containing alkylsilane compound is produced by reacting, in the presence of a transition metal catalyst, a polyfluoroalkyl allyl compound represented by the general formula: CF3(CF2)n(CH2CF2)a(CF2CF2)bCH2CH?CH2??[II] wherein n, a, and b are as defined above, with: an alkoxysilane, or a chlorosilane, followed by a reaction with lower alcohol or metal alkenyl. The production method gives a fluorine-containing alkylsilane compound that can remove free iodine derived from the raw material compound, before a hydrosilylation reaction is performed, without using a metal reagent having a high environmental load, and that also has excellent handling properties.

Abstract: The invention relates to novel silane-modified formamides and/or pre-polymers for bonding and/or sealing diverse substrate materials, such as, for example metal, wood, glass and/or plastic. The invention also relates to a reactive single-component adhesive system comprising the claimed silane-modified formamide and/or pre-polymers.

Abstract: The present invention relates to a process for preparing a tris[3-(alkoxysilyl)propyl] isocyanurate from the group of tris[3-(trialkoxysilyl)propyl] isocyanurate, tris[3-(alkyldialkoxysilyl)propyl] isocyanurate and tris[3-(dialkylalkoxysilyl)propyl] isocyanurate by hydrosilylation, by in step A initially charging a mixture comprising 1,3,5-triallyl-1,3,5-triazine-2,4,6(1H,3H,5H)-trione as olefin component, at least one carboxylic acid and a Pt catalyst, heating the mixture to a temperature of 50 to 140° C., in step B adding at least one hydroalkoxysilane from the group of hydrotrialkoxysilane, hydroalkyldialkoxysilane, hydrodialkylalkoxysilane [called H-silane(s) for short] to the mixture from step A while mixing, in step C leaving the mixture from step B to react while mixing, with addition of at least a defined amount of alcohol to the mixture as further cocatalyst, and in step D working up the product mixture thus obtained.

Abstract: The present invention relates to novel derivatives of oxazaphosphorines that are pre-activated, to the methods for preparing same, to the pharmaceutical compositions containing same and to the therapeutic use thereof, in particular for treating cancer.

Abstract: A method for manufacturing tris(?-diketonato)iridium by reacting ?-diketone with an iridium compound, in which an activation treatment including (a) an alkali treatment and (b) an acid treatment described below is applied to the iridium compound to activate the iridium compound, and to subsequently react the ?-diketone, (a) an alkali treatment: a treatment of adding alkali to a solution of the iridium compound to raise pH of the solution to a more alkaline side than that before the alkali addition and to not less than 10, and (b) an acid treatment: a treatment of adding acid to the solution subjected to the alkali treatment to lower pH of the solution to a more acidic side than that before the acid addition and to make the pH difference between solutions before and after the acid addition be not less than 0.1 and not more than 10. The present invention allows manufacture of tris(?-diketonato)iridium utilizing a wide variety of ?-diketones.

Abstract: A functionalized magnetic nanoparticle including an organometallic sandwich compound and a magnetic metal oxide. The functionalized magnetic nanoparticle may be reacted with a metal precursor to form a catalyst for various C—C bond forming reactions. The catalyst may be recovered with ease by attracting the catalyst with a magnet.

Abstract: A method of making benzidine hydrogen selenite complex with Cobalt and Platinum as surfactants is discussed. The resultant benzidine hydrogen selenite complex with either Cobalt or Platinum was characterized for its unique and superior properties. The complexes were characterized by elemental analysis, FTIR, and spectroscopy. The critical micelle concentration and thermodynamic parameters were calculated. The Values of IC50 were also calculated for the prepared complexes as well as their parent complex. The method of using the benzidine hydrogen selenite complex with cobalt and platinum as an antitumor agent to treat cancer is also demonstrated.

Abstract: Solid, free-flowing, and substantially completely dissolvable preparations with high betalain content are presented. Most typically, the betalain profile of the preparations is near natural and includes betalains in an amount of between 10-40 wt %. As the preparations of the inventive subject matter maintain chemical stability and flowability over extended periods of time, it should be noted that the betalain preparations are now amenable to compounding in small and measured quantities. Furthermore, new biological activities of betalains are shown, and especially include significant induction of SIRT and reduction of serum triglyceride.

Abstract: Described herein are oligosaccharide-oligonucleotide conjugates useful as vaccines against one or more human or veterinary therapeutic indications, and methods of synthesizing and identifying them. The conjugates may be identified using non-human antibodies as binding targets, thereby expanding the power and scope of the invention. Efficacious conjugates may be identified through an iterative screening process.

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

Abstract: The invention relates to a process for solution-phase synthesis of D-Arginyl-2,6-dimethyl-L-tyrosyl-L-lysyl-L-phenylalaninamide, an active ingredient used for both common and rare diseases including a mitochondrial targeted therapy for ischemia reperfusion injury.

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

Abstract: Provided herein is a novel epitope that can be used as a tag in methods for rapid and effective characterization, purification, and subcellular localization of polypeptides of interest, which comprise the tag. The tag is specifically recognized by an epitope specific antibody, which can be used to detect, capture, quantify, and/or purify polypeptides of interest that are tagged with the epitope. Also provided is novel epitope specific antibody.

Abstract: Provided herein are compounds and compositions having antibiotic activity against methicillin resistant Staphylococcus aureus (MRSA). In particular, provided herein is a synbody that bactericidal against multiple strains of MRSA and that can be used in conjugation with currently approved ?-lactam antibiotics to treat MRSA strains having resistance to ?-lactam treatment. Also provided are methods of using the compounds and compositions for treating, preventing or reducing MRSA infections.

Abstract: Provided is a method for adjusting the balance of TNF-R1 and TNF-R2 in cells present at a target organ, tissue or site. In the adjustment method provided, when increasing the relative presence of TNF-R2 compared to the presence of TNF-R1 in the cells, a synthetic peptide is supplied to the cells, with the peptide being essentially made of at a TNF-R1 signal peptide motif or a modified amino acid sequence thereof; and when decreasing the relative presence of TNF-R2 compared to the presence of TNF-R1 in the cells, a synthetic peptide is supplied to the cells, with the peptide being essentially made of a TNF-R2 signal peptide motif or a modified amino acid sequence thereof.

Abstract: An N-terminally protected peptide having the sequence (SEQ ID NO: 1) X-Glu-Cys-Lys-Ile-Lys-Gln-Ile-Ile-Asn-Met-Trp-Gln, wherein X is a group protecting the N-terminal of the peptide.

Abstract: Herein disclosed are bioactive peptides and proteins having immunomodulating and antiviral activity, more particularly histidine-rich bioactive peptide complexes having the following structural formula (SEQ ID NO: 29): wherein: X1 is preferably absent or is selected from among Gln, Ser, Asn, Val, Ala, Phe, and Asp, and R1 and R2 are peptide chains optionally contain the amino acid residues His and/or Cys that interact with transition metal ions. Whereas R1 is preferably selected from among His-Gly-Val-Ser-Gly(SEQ ID NO: 30), CysVal-Val-Thr-Gly- (SEQ ID NO: 31), Cys-Gly-, Val-Ser-Gly-, and His-Gly- or alternatively is absent, R2 is preferably selected from among -Val-His-Gly, -Val-Phe-Val, -Val-His, -Val-Asp or alternatively is absent. Such histidine-rich peptide complexes, primarily alloferon family peptides such as Alloferon-1 (SEQ ID NO: 1) with Zn ions, enable the creation of drugs with a targeted mechanism of action, and the design thereof with regard to understanding of drug target structure.

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

Abstract: In some embodiments, the present invention provides respiratory syncytial virus (RSV) F proteins, polypeptides and protein complexes that comprise one or more cross-links to stabilize the protein, polypeptide or protein complex in its pre-fusion conformation. In some embodiments the present invention provides RSV F proteins, polypeptides and protein complexes comprising one or more mutations to facilitate such cross-linking. In some embodiments the present invention provides compositions comprising such proteins, polypeptides or protein complexes, including vaccine compositions, and methods of making and using the same.

Abstract: The invention provides methods, compositions and kits for treating and or preventing an HIV infection. For example, HIV envelope-like polypeptides (wild-type HIV polypeptides and mimotopes) may be administered to an individual so as to induce a protective immune response to HIV. Alternatively, antibodies directed to the HIV envelope-like polypeptides may be administered to an individual to treat or prevent an HIV infection and/or one or more symptoms associated with the infection (e.g., AIDS).

Abstract: Herpes Simplex Virus (HSV) antigens that elicit an HSV-specific immune response and can be used to treat or prevent HSV infection are provided. Nucleic acid sequences, polypeptides, vectors, and compositions, as well as methods to induce an immune response against HSV, treat or prevent HSV disease, induce a T cell response against HSV, and induce an antibody response against HSV also are provided.

Abstract: A method for enhancing immunogenicity of an epitope peptide of an HPV antigen, the method including: assembling a gene of an HPV antigen into a gene of HBc, exogenously expressing a resulting assembled gene to acquire a fusion protein, allowing the fusion protein to automatically assemble to form a virus-like particle including the HPV antigen on a surface of the virus-like particle, to obtain HBc-HPV virus-like particle. A virus-like particle capable of expressing the antigen peptide of HPV acquired by the method. The virus-like particle includes a HBc-L2 fusion protein. A genome for encoding the HBc-L2 fusion protein is represented by SEQ ID NO. 3. A method for preparing an HPV vaccine includes using the virus-like particle.

Abstract: The present invention relates to a secretagogue compound derived from oxalate degrading bacteria, for use in the treatment of an oxalate related disease and/or oxalate related imbalance in a subject, wherein the administration of the secretagogue results in a reduction of urinary oxalate and/or plasma oxalate in the subject. The invention further relates to a pharmaceutical composition comprising such a secretagogue compound, a method for treating a subject suffering from an oxalate related disease, and to a method for preparing a secretagogue.

Abstract: A Treponema pallidum triplet antigen construct is disclosed which includes three Treponema pallidum antigens (TP15, TP17, and TP47), as well as a ten amino acid leader sequence (tag 261) and human copper zinc superoxide dismutase (hSOD). This construct is optimized for in vitro diagnosis of syphilis infection. Plasmids containing DNA encoding the triplet antigen, host cells, production methods, detection methods, and kits are also disclosed.

Abstract: The present invention relates to increasing xylose utilization in industrial microbe by inducing mutations in the regulator genes, crp and xylR. Thus the invention is directed to isolated nucleic acid sequences that encode mutations in the crp gene and the xylR gene and recombinant bacterium that express mutated CRP and XylR. In some embodiments, the mutation results in a point mutation at residue 142 of the CRP protein and/or at point mutation at residues 121, 182 and/or 363 of the XylR protein (based on the protein sequences in E. coli). The invention also includes methods of using the recombinant bacterium.

Abstract: The present invention relates to an RhtB (homoserine/homoserine lactone export transporter) protein variant having an enhanced ability to export O-phosphoserine (OPS) that is a precursor of L-cysteine, a polynucleotide encoding the protein, a vector comprising the polynucleotide, an OPS-producing microorganism comprising the protein variant, a method of producing O-phosphoserine using the microorganism, and a method for preparing cysteine or its derivatives, which comprises reacting O-phosphoserine, produced by the method above, with a sulfide in the presence of O-phosphoserine sulfhydrylase (OPSS) or a microorganism that expresses OPSS.

Abstract: Disclosed are new recombinant isoforms of human-like lubricin or PRG4 glycoprotein having outstanding lubrication properties and a novel glycosylation pattern, and methods for their manufacture at high levels enabling commercial production.

Abstract: A thermostable human epidermal growth factor-spider venom fusion protein with increased skin cell proliferation effect has the amino acid sequence of SEQ ID NO: 2, a gene of E. coli codon-optimized nucleotide sequence of SEQ ID NO: 1 for encoding the human epidermal growth factor-spider venom fusion protein, a recombinant vector including the gene, a host cell transformed with the recombinant vector, and a method for producing in a host cell a human epidermal growth factor-spider venom fusion protein by transforming a host cell with the recombinant vector, and a cosmetic composition for improving skin wrinkle and maintaining skin elasticity including a human epidermal growth factor-spider venom fusion protein, and as the cosmetic composition has excellent thermostability and has an effect of enhancing the activity of improving skin wrinkle and maintaining skin elasticity, it can be advantageously used in future in the field of cosmetics or cosmetic plastic surgery.

Abstract: Peptide hormone analogs of the formula X-V are provided herein, wherein X is a glucagon analog or a GLP1 analog, and V is a C-terminal extension amino acid sequence comprising at least four amino acid residues, at least three of said residues being His. Also provided herein are pharmaceutical compositions comprising said analogs, and methods of using said analogs for the treatment of conditions such as obesity and diabetes.

Abstract: The present invention provides a decoy peptide or polypeptide capable of inhibiting the binding of AMIGO2 and 3-phosphoinositide-dependent kinase 1 (PDK1), and a pharmaceutical composition, containing the decoy peptide or polypeptide as an active ingredient, for preventing or treating cancer or an angiogenic disease. Furthermore, the present invention provides a method for screening a material for preventing or treating cancer or an angiogenic disease. According to the present invention, it is worth noting that the decoy peptide or polypeptide of the present invention induces apoptosis through the inhibition of the binding of AMIGO2 and 3-phosphoinositide-dependent kinase 1 (PDK1); reduces migration and adhesion of endothelial cells; significantly reduces vascular induction, survival, and growth.

Abstract: Disclosed herein are several apoplipoprotein E (ApoE) polypeptides, and nucleic acids encoding these polypeptides, that can be used to treat or prevent a hepatitis infection in a subject, such as a hepatitis C virus infection. These ApoE polypeptides can inhibit the entry of hepatitis C virus into cells, and inhibit viral replication. Nucleic acids encoding these polypeptides are also disclosed, as well as methods.

Abstract: The invention features thrombospondin-1 (TSP-1) polypeptides (e.g., 3TSR-Fc fusion proteins), nucleic acid molecules encoding the TSP-1 polypeptides, and compositions thereof. The invention also features methods of making and using the TSP-1 polypeptides of the invention (e.g., using 3TSR-Fc fusion proteins to treat a subject having a disorder associated with pathological angiogenesis, e.g., cancer, e.g., epithelial ovarian cancer (EOC)).

Abstract: Compositions are provided, which can be used as frameworks for the creation of very stable and soluble single-chain Fv antibody fragments. These frameworks have been selected for intracellular performance and are thus ideally suited for the creation of scFv antibody fragments or scFv antibody libraries for applications where stability and solubility are limiting factors for the performance of antibody fragments, such as in the reducing environment of a cell. Such frameworks can also be used to identify highly conserved residues and consensus sequences which demonstrate enhanced solubility and stability.

Abstract: This invention provides antibodies or fragments thereof that are capable of specifically binding to at least one conformational epitope of enterovirus 71 (EV71), wherein the antibody individually comprises at least one variable light chain and at least one variable heavy chain. There is also provided a method of producing an antibody capable of specifically binding to at least one conformational epitope of enterovirus 71 (EV71).

Abstract: The present invention provides fully human antibodies that bind to respiratory syncytial virus F protein, compositions comprising the antibodies and methods of use. The antibodies of the invention are useful for preventing fusion of the virus with the cell membrane and preventing cell to cell spread of the virus, thereby providing a means of preventing the infection, or treating a patient suffering from the infection and ameliorating one or more symptoms or complications associated with the viral infection. The antibodies may also be useful for diagnosis of an infection by RSV.

Abstract: The present invention relates to a new and improved method for preparing a highly concentrated immunoglobulin composition from pooled plasma for subcutaneous injection. A composition comprising 20% or more immunoglobulin suitable for subcutaneous use is also described.

Abstract: The invention relates to the diagnosis and treatment of diseases, including cancer and inflammatory disorders. The invention provides, and involves the use of, antibodies that bind collagen.

Abstract: The present application relates to methods and compositions employing an antibody that inhibits activation of the complement system and can be used to prevent or treat a pulmonary disease or condition.

Abstract: The present disclosure encompasses NGF binding proteins, specifically to antibodies that are chimeric, CDR grafted and canonized antibodies, and methods of making and uses thereof. The antibodies, or antibody portions, of the disclosure are useful for detecting NGF and for inhibiting NGF activity, e.g., in a mammal subject suffering from a disorder in which NGF activity is detrimental.

Abstract: Provided are methods of generating chimeric antigen receptors (CAR). In some embodiments, library screening of CAR is performed by generating a vector encoding the CAR from random attachment of vectors from libraries of vectors encoding antigen-binding domains (e.g., scFv regions), hinge regions, and endodomains. In some embodiments, the vectors contain a transposon.

Abstract: The present invention relates to: a dual targeting antibody of a novel form having a water-soluble ligand fused to the N-terminus of a heavy chain or light chain of an antibody; a DNA encoding the dual targeting antibody; a recombinant expression vector containing the DNA; a host cell which is transformed with the recombinant expression vector; a method for preparing the dual targeting antibody by culturing the host cell; and a pharmaceutical composition including the dual targeting antibody.

Abstract: The present invention relates to a stable, low viscosity antibody formulation, wherein the formulation comprises a high concentration of anti-INFAR1 antibody. In some embodiments, the invention relates in general to a stable antibody formulation comprising about 100 mg/mL to about 200 mg/mL of an antibody or fragment thereof that specifically binds human interferon alpha 1 (INFAR1); about 20 mM to about 80 mM of a lysine or a salt thereof; about 0.02% to about 0.06% of a surfactant; an uncharged excipient; and a formulation buffer. In some embodiments, the invention is directed to a container, dosage form and/or kit. In some embodiments, the invention is directed to a method of making and using the stable antibody formulation.