Abstract: The present invention discloses methods for treating bacterial infections in a subject comprising administering to the subject a sub-growth inhibiting amount of a 5?-methylthioinosine phosphorylase (MTIP) inhibitor, as well as assays for identifying such inhibitors, and compounds and pharmaceutical compositions comprising the inhibitors.

Abstract: The present invention relates to the use of pteridines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents.

Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.

Abstract: The present invention relates to 6-5 membered fused pyridine ring compounds according to formula (I) or a pharmaceutically acceptable salt thereof or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of 6-5 membered fused pyridine ring compounds according to formula I in the treatment of Brutons Tyrosine Kinase (Btk) mediated disorders.

Abstract: The present disclosure relates to compounds that are Syk inhibitors and to their use in the treatment of various disease states, including cancer and inflammatory conditions. In particular embodiments, the structure of the compounds is given by Formula I: wherein R1, R2, R3, and R4 are as described herein. The present disclosure further provides pharmaceutical compositions that include a compound of Formula I, or pharmaceutically acceptable salts or co-crystals thereof, and methods of using these compounds and compositions to treat conditions mediated by Syk.

Abstract: The present invention is related to processes for preparing chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines of Formula III, and related synthetic intermediate compounds. The chiral substituted pyrazolyl pyrrolo[2,3-d]pyrimidines are useful as inhibitors of the Janus Kinase family of protein tyrosine kinases (JAKs) for treatment of inflammatory diseases, myeloproliferative disorders, and other diseases.

Abstract: The present invention encompasses compounds of general formula (1) where in the groups R0 to R3 and L are defined as in claim 1, which are suitable for the 5 treatment of diseases characterized by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.

Abstract: The present invention relates to a method for preparing high purity anhydrosugar alcohols using hydrogenated sugar, and more specifically, to a method for preparing high purity anhydrosugar alcohols (particularly, isosorbide, isomannide, isoidide, and the like) with a purity of 97.5% or higher (more preferably, 98.5% or higher) and a pH of a distillate of 3.7 or higher (more preferably, 4.0 or higher) in a distillation yield of 87% or higher (more preferably, 90% or higher) by adding an acid to hexitol so as to convert the same into anhydrosugar alcohols, and single-stage distilling the converted product by using an internal condenser type thin film evaporator.

Abstract: An improved, high yielding process is disclosed for making bisglycidyl ether derivatives of isosorbide, isomannide and/or isoidide, wherein up to quantitative yields overall are demonstrated. In another related aspect, a process is disclosed for making novel monoallyl, monoglycidyl ether derivatives or a combination of monoallyl, monoglycidyl ether derivatives and bisglycidyl ether derivatives via the same diallyl isohexide intermediate.

Abstract: A polymer compound including a structural unit represented by formula (I) or a structural unit represented by formula (III) and a structural unit represented by formula (II) has high photoelectric conversion efficiency when used in an organic photoelectric conversion device. wherein Ar1 and Ar2 are the same or different and represent trivalent heterocyclic group; Z represents a divalent group; Y represents a divalent heterocyclic group; wherein Ar1 and Ar2 are the same or different and represent trivalent heterocyclic group; Z represents a divalent group; Y represents a divalent heterocyclic group; two Ar1s may be the same or different; two Ar2s may be the same or different; and two Z's may be the same or different. -D-??(II) wherein D represents an arylene group or a heteroarylene group having a fused ring, provided that a divalent heterocyclic group represented by Y is different from a group represented by D.

Abstract: The present invention provides compounds of formula (I): (Formula (I); wherein A, R1, R2, R3I, V, X, and Z are defined herein, which are potassium channel inhibitors. The invention further provides pharmaceutical compositions comprising the compounds of formula (I) and their use in therapy, in particular in treatment of diseases or conditions that are mediated by Kir3.1 and/or Kir3.4 or any heteromultimers thereof, or that require inhibition of Kir3.1 and/or Kir3.4 or any heteromultimers thereof.

Abstract: Disclosed are pyruvate kinase M2 activators, which are, bis sulfonamide piperazinyl compounds of Formula (I) and 2,4-disubstituted 4H-thieno[3,2-b]pyrrole-2-(substituted benzyl)pyridazin-3(2H)ones of Formula (II), wherein L and R1 to R16 are as defined herein, that are useful in treating a number of diseases that are treatable by the activation of PKM2, for example, cancer and anemia, Formulas (I); (II).

Abstract: Disclosed is a compound represented by Formula 1 or Formula 2, and an organic electric element comprising a first electrode, a second electrode, and an organic material layer between the first electrode and the second electrode, wherein the organic material layer comprises the compound of Formula 1 or 2 to improve luminous efficiency, stability, and life span.

Abstract: The present invention relates to tricyclic heterocycles of Formula (I), which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer.

Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof wherein A represents a group represented by one of formulae (i)-(iii); B represents a group represented by formula (v) or (vi); and E represents a substituted or unsubstituted heterocyclic group having a cationic nitrogen atom.

Abstract: A benzobis(thiadiazole) derivative represented by the formula (1): in which R represents a group containing at least one fluorine atom (with the proviso that fluorine atom (F) and trifluoromethyl group (—CF3) are excluded), and m represents an integer of from 1 to 10.

Abstract: Novel compounds of the structural formula (I) are activators of AMP-protein kinase and may be useful in the treatment, prevention and suppression of diseases mediated by the AMPK activated protein kinase. The compounds of the present invention may be useful in the treatment of Type 2 diabetes, hyperglycemia, metabolic syndrome, obesity, hypercholesterolemia, and hypertension.

Abstract: An efficient, one step solution state processing of Proton Conducting Homochiral Metal Organic Framework has been achieved by using derivate of amino acid and Zn(II) salt as a MOF constructor. Control over MOF solubility as well as proton conductivity has also been achieved by judicious selection of the ligand architecture. This invention will lead the way for ease preparation of MOF films for industrial application.

Abstract: Pyridyldiamido transition metal complexes are disclosed for use in alkene polymerization.

Abstract: Diol derived blocked mercaptofunctional silane compositions in which the silanes comprise cyclic and bridged alkoxy groups derived from hydrocarbon-based diols and processes for their preparation are provided. Also provided are rubber compositions comprising the cyclic diol-derived blocked mercaptofunctional silanes, processes for their preparation and articles of manufacture comprising the rubber compositions, in particular, automotive tires and components thereof.

Abstract: A novel method of simultaneously protecting two functions which are same or different, namely hydroxyl, amine, or thiol ones, particularly in sugars, polyalcohols, nucleosides, nucleotides, peptides, and nucleic acids during an organic synthesis, and to novel compounds for implementing this method, as well as to the method of obtaining these compounds. Method of simultaneously protecting two hydroxyl, amine, or thiol functions according to the invention by carrying out a protecting reaction between a compound having at least two free hydroxyl, amine, or thiol groups, and the disilane of formula 1, where R stands for Cl or Br, or I, or a substituent of formula 2, where X1, X2, X3, X4 are the same or different.

Abstract: The invention relates both to processes for the production of functionalised materials containing alkyl sulfonic acids groups and their use as heterogeneous catalysts. The invention also relates to precursors of these new products and new organopolysiloxane sulfonic acids.

Abstract: The invention relates to a process for preparing urea-containing silanes of the general formula I wherein a diamine of the general formula II H2N—R—S—S—R—NH2??(II) is reacted with isocyanatosilane of the general formula III (R1)3Si—R—NCO??(III) in water.

Abstract: Methods for producing functionalized graphene from graphite oxide or graphite are disclosed in which ionic liquids are used as a reaction medium to promote chemical functionalization of the graphene through electrochemically interacted exfoliation of graphene sheets.

Abstract: An object of the present invention is to provide a production method that can efficiently produce a cyclic silane compound or a salt thereof with a high yield and to provide a novel salt having a cyclic silane dianion that is easy to handle and a cyclic silane dianion salt-containing composition. The method for producing a cyclic silane compound or a salt thereof of the present invention includes the step of allowing a halosilane compound to react in the presence of at least one of a phosphonium salt and an ammonium salt, and a compound represented by a specific formula.

Abstract: The present invention relates to novel compounds, compositions containing same and methods for inhibiting human farnesyl pyrophosphate synthase or for the treatment or prevention of disease conditions using said compounds;

Abstract: The invention relates to a method for producing 6-chlorodibenzo[d,f][1,3,2]-dioxaphosphepin (formula 1), comprising the following steps: a) addition of 2,2?-dihydroxybiphenyl, which is suspended in an inert solvant. into a reactor to an excess of phosphorous trichloride under inert gas and stirring; b) discharge and neutralization of the resulting gases from the reaction mixture; c) separation of the excess phosphorous trichloride and the solvant; d) obtention of 6-chlorodibenzo[d,f][1,3,2]-dioxaphosphepin.

Abstract: The presently-disclosed subject matter includes light-activated ruthenium compounds. In some embodiments the compounds release one or more ligands when exposed to light, and in specific embodiments the light includes a wavelength of about 500 nm to about 1000 nm. The present compounds can also comprise an overall charge, wherein the overall charge can be a positive overall charge or a negative overall charge. Further still, embodiments include methods of treating cancer in a subject by administering a compound and then exposing a site of the subject to light.

Abstract: Derivatives of boron cluster compounds of general formula I and their pharmaceutically acceptable salts and solvates, and their specific inhibition effect on the enzyme carbonic anhydrase IX, a protein overexpressed in cancer tissues. Methods of synthesis and the use of the novel derivatives. These inhibitors of human carbonic anhydrase IX can be used as active compounds of pharmaceuticals for diagnostics and/or therapy of cancer diseases.

Abstract: The present invention provides a one-pot multi-enzyme method for preparing UDP-sugars from simple sugar starting materials. The invention also provides a one-pot multi-enzyme method for preparing oligosaccharides from simple sugar starting materials.

Abstract: The present invention relates to synthetic lipoteicoic acid (LTA) mimetics which are useful as vaccine components for therapy and/or prophylaxis of bacterial infection.

Abstract: The present invention provides a novel sialo-sugar chain, a process for producing the sialo-sugar chain, and a device for producing the sialo-sugar chain. A sialo-sugar chain can be easily and efficiently mass-produced by reacting a sugar wherein a hydroxy groups is substituted with an alkynyl group (herein sometimes referred to as “alkynylated sugar”) with a specific sialic acid donor in the presence of a sialic acid-introducing enzyme.

Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2?-deoxy-?-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2?-deoxy-?-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.

Abstract: The present disclosure describes oligomeric compounds having at least one bicyclic nucleoside attached to the 3? or 5? termini by a neutral internucleoside linkage and methods of using the oligomeric compounds. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.

Abstract: The present invention relates to a new uridine nucleoside-based amphiphilic gadolinium complex and a magnetic resonance imaging (MRI) contrast agent including the gadolinium complex. The MRI contrast agent has high relaxivity, high binding affinity for and stability in human serum albumin, pH response, and high liver specificity.

Abstract: Disclosed herein are novel C4-monomethyl triterpenoid compounds and derivatives thereof, including those of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds. Methods and intermediates useful for making the compounds, and methods of using the compounds, for example as antioxidant inflammation modulators, and compositions thereof are also provided.

Abstract: The present invention relates to a method for cross-linking peptides using an activated furan-moiety. In particular, the present invention provides a method for cross-linking peptides comprising the steps of: a) providing a composition comprising furan-peptides, said furan-peptides comprising at least one amino acid comprising a furan-moiety; b) contacting said composition comprising furan-peptides with second peptides, thereby obtaining a mixture comprising furan-peptides and second peptides; c) adding an activation signal to said mixture of step b), thereby activating said furan-peptides to activated furan-peptides, and d) reacting said activated furan-peptides with said second peptides, thereby cross-linking said activated furan-peptides with said second peptides.

Abstract: Protein kinase inhibitors and more specifically inhibitors of the protein kinase c-Jun amino terminal kinase are herein described. Additionally, JNK inhibitor sequences, chimeric peptides, nucleic acids encoding same as well as pharmaceutical compositions for treating pathophysiologies associated with JNK signaling are herein provided.

Abstract: A MC1R peptide ligand-elastic vesicle complex for preventing skin maladies. The MC1R peptide ligand is modified by coupling the melanocortin 1 receptor (MC1R) ligand to a functionality or linker, such as a click functionality, for conjugation to a surface or agent. The modified MC1R peptide ligand can be coupled, e.g., via a click reaction with a complementary click functionality attached, to a moiety to form an MC1R-targeted agent. Drugs, contrast agents, polymers, particles, micelles, elastic vesicles, surfaces of larger structures, or other moieties can be targeted to the MC1R. The MC1R peptide ligand-elastic vesicle complex is prepared as a patch or viscous emulsion that can be applied to human skin.

Abstract: The invention relates to novel pharmaceutically-useful peptides, in particular cyclic peptides that are agonists of the AngII type 2 receptor (AT2 receptor). The invention further relates to the use of such peptides as medicaments, to pharmaceutical compositions containing them, and to their production.

Abstract: Provided are TCL1 peptides that bind to MHC I (HLA-A2) on tumor cells or other antigen-presenting cells and are recognized by T-cell receptors on T cells. The TCL1 peptides may be therapeutically used to treat a cancer, such as a B cell malignancy, leukemia, or lymphoma. Methods for expanding a population of T cells that target TCL1 are also provided.

Abstract: The present invention provides a pharmaceutical composition for preventing or treating arteriosclerosis, comprising: a pharmaceutically effective amount of a protein comprising the amino acid sequence of SEQ ID NO: 1; and a pharmaceutically acceptable carrier. The composition of the present invention exhibits no toxicity in the liver or kidney and effectively reduces the formation of atherosclerotic plaques, thereby exhibiting efficacy in treating arteriosclerosis.

Abstract: Compositions and methods for the therapy and diagnosis of Inflammatory Bowel Disease (IBD), including Crohn's Disease and Ulcerative Colitis, are disclosed. Illustrative compositions comprise one or more bacterial polypeptides, immunogenic portions thereof, polynucleotides that encode such polypeptides, antigen presenting cell that expresses such polypeptides, and T cells that are specific for cells expressing such polypeptides. The disclosed compositions are useful, for example, in the diagnosis, prevention and/or treatment of IBD.

Abstract: The invention provides molecular switches which couple external signals to functionality, and combinatorial methods of making and using the same involving circular permutation of nucleic acid and amino acid sequences. The switches according to the invention can be used, for example, to regulate gene transcription, target drug delivery to specific cells, transport drugs intracellularly, control drug release, provide conditionally active proteins, perform metabolic engineering, and modulate cell signaling pathways. Libraries comprising the switches, expression vectors and host cells for expressing the switches are also provided.

Abstract: The invention provides compositions, kits and methods utilizing polypeptides having a viral alpha-helix heptad repeat domain in a stabilized ?-helical structure (herein also referred to as SAH). The compositions are useful for treating and/or preventing viral infections. The invention is based, at least in part, on the result provided herein demonstrating that viral hydrocarbon stapled alpha helical peptides display excellent proteolytic, acid, and thermal stability, restore the native alpha-helical structure of the peptide, are highly effective in interfering with the viral fusogenic process, and possess superior pharmacokinetic properties compared to the corresponding unmodified peptides.

Abstract: Improved anti-HIV immunogens and nucleic acid molecules that encode them are disclosed. Immunogens disclosed include those having consensus sequences for HIV Subtype A Envelope protein, those having consensus sequences for HIV Subtype B Envelope protein, those having consensus sequences for HIV Subtype C Envelope protein, those having consensus sequences for HIV Subtype D Envelope protein, those having consensus sequences for HIV Subtype B consensus Nef-Rev protein, and those having consensus sequences form HIV Gag protein subtypes A, B, C and D. Improved anti-HPV immunogens and nucleic acid molecules that encode them; improved anti-HCV immunogens and nucleic acid molecules that encode them; improved hTERT immunogens and nucleic acid molecules that encode them; and improved anti-Influenza immunogens and nucleic acid molecules that encode them are disclosed as well methods of inducing an immune response in an individual against HIV, HPV, HCV, hTERT and Influenza are disclosed.

Abstract: Disclosed are yeast-based immunotherapeutic compositions, hepatitis B virus (HBV) antigens, and fusion proteins for the treatment and/or prevention of HBV infection and symptoms thereof, as well as methods of using the yeast-based immunotherapeutic compositions, HBV antigens, and fusion proteins for the prophylactic and/or therapeutic treatment of HBV and/or symptoms thereof.

Abstract: A nucleic acid encoding a chimeric protein, the chimeric protein including (i) at least one amino acid sequence having at least 50% sequence identity with any of the amino acid sequences selected from the group consisting of SEQ ID NOS: 1-5, and (ii) at least one amino acid sequence having at least 80% sequence identity with any of the amino acid sequences selected from the group consisting of SEQ ID NOS: 6-8. The chimeric protein includes at least one amino acid sequence of (i) and at least one amino acid sequence of (ii) that are from different Borrelia strains or species.

Abstract: The present invention relates to a chromatography ligand, which comprises Domain C from Staphylococcus protein A (SpA), or a functional fragment or variant thereof. The chromatography ligand presents an advantageous capability of withstanding harsh cleaning in place (CIP) conditions, and is capable of binding Fab fragments of antibodies. The ligand may be provided with a terminal coupling group, such as arginine or cysteine, to facilitate its coupling to an insoluble carrier such as beads or a membrane. The invention also relates to a process of using the ligand in isolation of antibodies, and to a purification protocol which may include washing steps and/or regeneration with alkali.

Abstract: The invention relates to the use of a combination of SP1298 and SP2205 proteins or functional fragments thereof or homologous proteins or protein fragments thereof of S. pneumoniae for preventing or treating a S. pneumoniae infection, their use for the preparation of a vaccine for the preventive treatment of a S. pneumoniae infection, compositions comprising said proteins of S. pneumoniae or functional fragments thereof, vaccines comprising said proteins or functional fragment thereof, and to a method for in vivo immune protection.