Abstract: The compounds represented by Formula (I) and pharmaceutically acceptable salts thereof are useful as inhibitors of DNA-PK: where each of R1, R2, X, Ring A, Ring B and Ring C is as described herein. Pharmaceutically acceptable compositions comprise said compounds. These compounds and pharmaceutical compositions are used in the treatment of various disease, conditions, or disorders.

Abstract: A compound or its pharmaceutically acceptable salt, optionally including both individual enantiomeric forms, a racemate, diastereomers and mixtures thereof, composition and method are disclosed that can provide analgesia and reduce inflammation. A contemplated compound has a structure that corresponds to Formula A, wherein the R group substituents, d, e, f, k, n, m, D, E, F, K, G, P, Q, W, and Z are defined within.

Abstract: The present invention provides a method for treating lupus in a subject, comprising the step of administering to the subject Compound A.

Abstract: What is described is a process for continuously esterifying halosilanes of the formula I with alcohols of the formula II to give silane esters of the formula III in a single column (1) R1aSiHalb??(I) R2—(OH)??(II) R1aS—(OR2)b??(III) in which R1 is hydrogen or a monovalent organic radical, where any two R1 radicals within a molecule may be different within the scope of the given definitions, Hal is a halogen atom, a plurality of Hal atoms within a molecule may be different within the scope of the given definitions, R2 is a monovalent organic radical, a and b are integers from 0 to 4 and the sum total of a and b is 4, comprising the measures of: i) feeding the total amount of the halosilane of the formula I required for the reaction in liquid form through line (6) into the upper third of the column (1), ii) feeding at least 60% by weight of the alcohol of the formula II required for the reaction in liquid form through line (7) into the upper third of the column (1), iii) feeding the remainder of the a

Abstract: There is provided a novel organic silicon compound that can be used for a silane coupling agent. An organic silicon compound of Formula (1): (where A? is Formula (2) or Formula (3): E is Formula (4) or Formula (5): R1 and R2 are each independently a C1-5 alkyl group, R3 is a hydrogen atom or a methyl group, R4 and R5 are each independently a C1-5 alkyl group, m, n, and p are each independently an integer of 1 to 5, and q is an integer of 1 to 3).

Abstract: A chromatographic material comprising a zwitterionic ligand covalently bound to a substrate, the ligand preferably has a formula II: wherein R1, R2, R3 are independently selected from an oxygen atom that is configured to connect to a substrate atom in the substrate, an oxygen atom that is configured to connect to a silicon atom of an adjacent ligand, a hydroxyl group, a halogen atom, an alkoxy group, a dialkylamino group, an acyl group, an alkyl group, or an aryl group; L1, L2 and L3 are independently hydrophobic moieties; each containing 2 to 30 carbon atoms, wherein there are at least 10 carbon atoms in the combined chain lengths of L1, L2 and L3; X is an O atom, S atom, amide group or sulfonamide group; n is 0 or 1; R4, R5 are independently selected from a hydrogen atom or a hydrocarbon moiety containing 1 to 20 carbon atoms; and Rf is a negatively charged moiety comprising a sulfonic, carboxylic, or phosphonic functional group.

Abstract: Disclosed herein are crystalline compounds of formula (I) wherein A+ represents a hydroxylated aliphatic ammonium species; and X and Y independently represent leaving groups.

Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.

Abstract: Preparation and characterization of novel forms of (1-hydroxy-2-imidazol-1-yl-1-phosphono-ethyl) phosphonic acid, suitable for pharmaceutical compositions in drug delivery systems for humans.

Abstract: The invention pertains to the use of fused bicyclo heterocyclic adducts of thiohydroxy pyridines or pyrimidines as diacylglycerol O-acyltransferase 1 (DGAT-1) inhibitors to treat hyperlipidiemias and various diseases and disorders associated therewith. Other conditions also can be ameliorated or avoided, such as high postprandial triglycerides or diet-related hypertriglyceridemia, cardiovascular risk associated with excessive triglycerides, and insulin resistance/glucose intolerance in overweight patients, those with diabetes or other glucose metabolic disorders such as Syndrome X and/or polycystic ovary disease.

Abstract: The invention relates to novel compositions of 1,3-disubstituted ferrocenes useful for the modification of electrodes.

Abstract: Crystalline solid forms of the anti-HCV compound (S)-isopropyl 2-((S)-(((2R,3R,4R,5R)-5-(2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-4-fluoro-3-hydroxy-4-methyltetrahydrofuran-2- yl)methoxy)(phenoxy)phosphorylamino)propanoate (Compound I) are described Also provided are processes of making and methods of using the crystalline forms.

Abstract: Certain bile acids, including novel bile acids, and derivatives thereof can be used to inhibit the germination of C. difficile spores and/or the growth of C. difficile cells. The methods and compositions of the invention are useful for preventing and treating C. difficile-associated diseases, including but not limited to C. difficile colitis.

Abstract: Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

Abstract: The invention relates to a process for the purification of crude abiraterone acetate by treatment with polymer resins in aqueous solvent. The purified product is recovered by simple concentration and filtration.

Abstract: The invention provides epoxytaccalonolide microtubule stabilizers and their use as anti-proliferative microtubule stabilizing agents.

Abstract: Disclosed are compounds of Formula (I) or pharmaceutically acceptable salts thereof, wherein W, Y, Z, R1, R2, R3 and R4 are as described in this application, and methods of using the compounds in the treatment of cancer.

Abstract: Novel protein tyrosine phosphatase (PTP) inhibitor compounds synthesized from phosphonodifluoromethyl phenylalanine (F2Pmp) are provided. Use of these compounds for inhibiting a PTP enzyme (such as PTP-MEG2), as well as treating a disease, disorder, or condition associated with inappropriate activity of a PTP (such as type 2 diabetes), is also provided.

Abstract: Novel urotensin II receptor (UT) agonists and antagonists are described herein. More specifically, novel derivatives of urotensin II-related peptide (URP) are described herein.

Abstract: The invention relates to methods for treating depression, anxiety, and other related diseases by administering a peptide NMDAR partial agonist.

Abstract: The present invention provides the means and methods for selecting immunogenic peptides and the immunogenic peptide compositions capable of specifically binding glycoproteins encoded by HLA alleles and inducing T cell activation in T cells restricted by the allele. One such peptide, NMLSTVLGV (SEQ ID NO: 183) is useful to elicit an immune response against influenza. The present invention also provides a heteropolymer of an isolated immunogenic peptide less than 15 amino acids in length comprising the oligopeptide NMLSTVLGV (SEQ ID NO: 183) and at least one different peptide.

Abstract: Grhelin O-acyltransferase inhibitors using a triazole linkage to incorporate aromatic and alkyl substituents to mimic the natural octanoyl group attached to ghrelin. Inhibitors include a triazole portion, an alkyl linker, and a hydrophobic aromatic group on a side chain. The hydrophobic aromatic group may include various length alkyl linkers.

Abstract: A DPP-4 inhibitor comprising a peptide represented by the formula (1): Xe-Pro/Ala/Hyp-Xa-Xb-Xc-Xd (SEQ ID NO: 16) (wherein Xe is an amino acid residue with an isoelectric point of 5.9 to 6.3; Pro/Ala/Hyp represents Pro, Ala, or Hyp; Xa is an amino acid residue other than Hyp, Pro, and Arg, or deletion; 5 Xb is Gly, Pro, or deletion; Xc is Pro, Ala, or deletion; and Xd is an amino acid residue or deletion) as an active component. The inhibitor can be expected to bring out an effect of lowering blood glucose levels by enhancing effects of incretins; and the inhibitor may be used as a therapeutic agent for diabetes and, in addition, can act on the immune system or the like to be thus used in 10 treatment for skin diseases or the like.

Abstract: The present invention relates to peptides comprising multiple MHC Class II-binding T cell epitopes for tolerization therapy.

Abstract: A method for identifying a molecule that binds an irradiated tumor in a subject and molecules identified thereby. In some embodiments, the method includes the steps of (a) exposing a tumor to ionizing radiation; (b) administering to a subject a library of diverse molecules; and (c) isolating from the tumor one or more molecules of the library of diverse molecules, whereby a molecule that binds an irradiated tumor is identified. Also provided are targeting ligands that bind an irradiated tumor and therapeutic and diagnostic methods that employ the disclosed targeting ligands.

Abstract: The invention provides a bioconjugates comprising a synthetic polypeptide of Formula I? (SEQ ID NO: 1): or an amide, an ester or a salt thereof, wherein X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, X12 and X13 are defined herein and a half-life extending moiety wherein the peptide and the half-life extending moiety are covalently linked or fuse, optionally via a linker. The polypeptides are agonist of the APJ receptor.

Abstract: The invention relates to composition comprising a pharmaceutically effective amount of one or more functional vasoactive intestinal peptide (VIP) fragments, and the use of those compositions in the treatment of fibrosis, hypertension and other disorder.

Abstract: The invention features compositions based on thioredoxin-like fold protein domains described as engineered thioredoxin-like fold proteins (ETRXs). These proteins include one or more artificially diversified thioredoxin-like fold protein domains; each domain may be originated from the same or different thioredoxin-like fold protein domains. Features of the invention also include methods for identifying and preparing an enriched composition of target binding, loop-diversified ETRXs with additional sequence variations to improve affinity, stability, selectivity, or solubility. The invention also features compositions of ETRXs substituted with prosthetic groups, polymers, proteins, nucleic acids, carbohydrates, metals, natural or synthetic small molecules and toxins.

Abstract: The present invention concerns a new competence stimulating peptide identified in Firmicutes, in particular Streptococcus, and more preferably S. thermophilus and methods of producing transformation competent Firmicutes, in particular Streptococcus, and more preferably S. thermophilus bacteria.

Abstract: The present invention relates to antigens more particularly antigens of Streptococcus pyogenes (also called group A Streptococcus (GAS)) bacterial pathogen which are useful as vaccine component for therapy and/or prophylaxis.

Abstract: This invention relates to botulinum toxin formulations that are stabilized without the use of any proteinaceous excipients. The invention also relates to methods of preparing and using such botulinum toxin formulations.

Abstract: Among the fewer than 10 proteins primarily secreted by the species Lactobacillus plantarum, there is one of 30 kDa that contains an internal fragment without cleavage sites for the most important intestinal proteases and characterized by having a serine and threonine content of at least 50%. The genetic information encoded in this fragment, designated ST peptide, has been used for producing and purifying the peptide, thus making it possible to conduct various tests in vitro. To summarize, the ST peptide is considered to promote the process of immunologic ignorance of our gastrointestinal immune system toward the commensal bacteria of our gastrointestinal tract, thus favoring the mechanisms of oral tolerance. Therefore the ST peptide could be used in immunotherapy, especially in the context of certain autoimmune diseases and certain inflammatory diseases.

Abstract: Provided herein are compositions comprising light-activated chimeric proteins expressed on plasma membranes and methods of using the same to selectively depolarize excitatory or inhibitory neurons.

Abstract: Disclosed is a composition of matter comprising an isolated polypeptide, which is a peripherally-restricted Nav1.7 inhibitor. In some disclosed embodiments, the isolated polypeptide is an inhibitor of Nav1.7 and/or Nav1.3. Other embodiments are conjugated embodiments of the inventive composition of matter and pharmaceutical compositions containing the inventive composition of matter. Isolated nucleic acids encoding some embodiments of inventive polypeptides and expression vectors, and recombinant host cells containing them are disclosed. A method of treating or preventing pain is also disclosed.

Abstract: The present invention relates, in general, to agents that modulate the pharmacological activity of nucleic acid molecules and, in particular, to agents that bind therapeutic or diagnostic nucleic acid molecules in a sequence independent manner and modulate (e.g., inhibit or reverse) their activity. The invention also relates to compositions comprising such agents and to methods of using same.

Abstract: The invention concerns the field of cell culture technology. The invention describes production host cell lines comprising vector constructs comprising a CERT S132 A expression cassette. Those cell lines have improved growth characteristics and high CERT S132A expression levels. The invention especially concerns two cell lines deposited with the DSMZ under the number DSM ACC2989 (CHO/CERT 2.20) and DSM AC-C2990 (CHO/CERT 2.41). The invention further concerns a method of generating such preferred production host cells and a method of producing proteins using the two cell lines deposited with the DSMZ under the number DSM ACC2989 (CHO/CERT 2.20) and DSM ACC2990 (CHO/CERT 2.41).

Abstract: The present invention provides substantially purified peptide portions of adipokine polypeptides, including, for example, C1q/TNF-related protein-12 (CTRP12), a functional homolog or function fragment of CTRP12, and a fusion polypeptide comprising any of the above.

Abstract: Ophthalmic formulations of a vascular endothelial growth factor (VEGF)-specific fusion protein antagonist are provided suitable for intravitreal administration to the eye. The ophthalmic formulations include a stable liquid formulation and a lyophilizable formulation. Preferably, the protein antagonist has an amino acid sequence of SEQ ID NO:4.

Abstract: Crosslinked proteins, proteins and polymers, and polymers and methods of making the same are disclosed. In one illustrative embodiment, a method is provided comprising the steps of attaching a chelator to one or more polymers; creating a coordination complex between the first protein, the second protein, and a metal ion; and crosslinking the first and second proteins by exposing the coordination complex to an oxidant.

Abstract: Provided is a fusion protein comprising a tumor necrosis factor related apoptosis inducing ligand (TRAIL), integrin ligands of ?V?3 and ?V?5 and a linking peptide. Also provided are the expression method and simple separation and purification process for the production of the fusion protein which is soluble and has high content of the polymer, and use of the fusion protein for the manufacturing of a medicament for the treatment of tumor. The fusion protein has good tumor tissue targeting property, significantly enhanced anti-tumor effect, which can also reduce the dose of the needed protein for the target treatment effect, improve the bioavailability, reduce the treatment cost, decrease and overcome the potential toxic and side effects of the tumor necrosis factor-related apoptosis inducing ligand.

Abstract: The present invention provides polypeptide variants of neuregulin-1? (NRG-1?) that have enhanced or decreased binding affinity to ErbB3 and/or ErbB4. The invention also provides methods of screening and producing polypeptide variants of NRG-1? and methods of using polypeptide variants of NRG-1? for treating diseases.

Abstract: The present invention is directed to novel tissue protective peptides. The tissue protective peptides of the invention may bind to a tissue protective receptor complex. In particular, the present invention is drawn to tissue protective peptides derived from or sharing consensus sequences with portions of cytokine receptor ligands, including Erythropoietin (EPO), that are not involved in the binding of the ligand to the receptor complex, e.g., to the EPO receptor homodimer. Accordingly, the tissue protective peptides of the invention are derived from the amino acid sequences of regions of cytokine receptor ligands that are generally located on or within the region of the ligand protein that is opposite of the receptor complex, i.e., are generally derived from amino acid sequences of regions of the ligand protein that face away from the receptor complex while the ligand is bound to the receptor.

Abstract: The present invention refers to single-chain fusion proteins comprising three soluble TNF superfamily (TNFSF) cytokine domains and nucleic acid molecules encoding these fusion proteins. The fusion proteins are substantially non-aggregating and suitable for therapeutic, diagnostic and/or research applications.

Abstract: Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.

Abstract: The present invention relates to a novel form of human EGFR found in certain tumors and conditions. The protein is termed here mLEEK, and the cDNA that encodes it has also been isolated. The mLEEK protein is capable of efficiently inducing the transcription of multiple genes resulting in various physiologic processes. Antibodies directed against the protein can be used for improving the diagnosis of diseases or for the treatment of diseases. The protein itself can be directly used or blocked for therapeutic purposes. Nucleic acid based probes or PCR primers specific for the mLEEK sequence can be used for diagnostic purposes. Inhibitory nucleic acid based molecules, such as antisense, siRNA, or shRNA, may be used for therapeutic purposes. The mLEEK sequence is essentially formed by the skipping of exons 2 through 22 in the EGF receptor gene leading to a fusion of exon 1 to exon 23. Other mutants are disclosed, which include the fusion of exon 1 to exon 24 and the fusion of exons 1 to exon 28.

Abstract: Chemoattractant polypeptide compounds for progenitor cells and compositions and drug products comprising the compounds are provided herein. Methods for attracting progenitor cells to a location in or on a patient also are provided along with methods of growing and repairing bone.

Abstract: The invention relates to antibodies, and antigen binding fragments thereof, that bind to hemagglutinin and neutralize a group 1 subtype and a group 2 subtype of influenza A virus. The invention also relates to nucleic acids that encode, immortalized B cells and cultured single plasma cells that produce, and to epitopes that bind to such antibodies and antibody fragments. In addition, the invention relates to the use of the antibodies, antibody fragments, and epitopes in screening methods as well as in the diagnosis, treatment and prevention of influenza A virus infection.

Abstract: This invention is directed to an antibody construct or fragment thereof derived from an RSV-infected human, such that the antibody construct binds with specificity to RSV fusion protein antigenic region II/A with an affinity of greater than 1×10?9 M. Preferably, the antibody construct is capable of neutralizing RSV strains, including at least one RSV strain that is resistant to palivizumab. The invention further relates to nucleic acids encoding the antibody construct or portions thereof, and cell lines expressing the antibody. This invention further relates to methods for producing said antibody construct, and to the use of said antibody construct for treating or preventing infection of a patient by RSV having a normal or mutated version of F protein.

Abstract: The present invention relates to a VHH which binds to a growth factor or is an antagonist for a growth factor, or binds to an implant.

Abstract: The present invention provides methods of immunization against Alzheimer's Disease and compositions for use in such methods.