Abstract: The present invention relates to compound (I) or a salt thereof which has a ROR?t inhibitory action. In the formula (I), each symbol is as defined in the specification.

Abstract: Hydridosilapyrroles and hydridosilaazapyrrole are a new class of heterocyclic compounds having a silicon bound to carbon and nitrogen atoms within the ring system and one or two hydrogen atoms on the silicon atom. The compounds have formula (I): in which R is a substituted or unsubstituted organic group and R? is an alkyl group. These compounds react with a variety of organic and inorganic hydroxyl groups by a ring-opening reaction and may be used to produce silicon nitride or silicon carbonitride films.

Abstract: The present invention provides a zwitterionic silatrane-based material and an antifouling substrate containing the same, wherein zwitterionic silatrane-based material has a structure as shown in Formula (I):

Abstract: A method of stabilizing imino-functional silane involving adding thereto at least one Brønsted-Lowry base to inhibit, suppress or prevent the addition reactions of the imino-functional silane with itself to form a imino- and amino-functional silane and the subsequent deamination reactions to form conjugated carbon-carbon double bond-containing imino-functional silanes and stabilized imino-functional silanes containing the at least one Brønsted-Lowry base.

Abstract: A process produces a C3- to C20-alkyltrialkoxysilane by hydrosilylation, wherein alkoxy represents methoxy, ethoxy or propoxy. Initially, a mixture is charged of at least one hydroalkoxysilane from the group of hydrotrialkoxysilane, hydroalkyldialkoxysilane, and hydrodialkylalkoxysilane, and a Pt catalyst. The mixture is then heated to a temperature of 30° C. to 60° C. Subsequently, with mixing, an omega-unsaturated or mono-unsaturated C3- to C20-hydrocarbon, at least one carboxylic acid and at least one alcohol as cocatalysts are added to the mixture. The mixture is then reacted and subsequently worked up to obtain the product.

Abstract: The present invention relates to a GPR84 receptor antagonist and use thereof. The GPR84 receptor antagonist of the present invention has a structure as represented by formula (I), the definitions of R1, R2, R3, R4, L1, L2, L3, L4, L5, L6, Y, Z, and rings A, B, C, and D are as described in the description and claims. The GPR84 receptor antagonist of the present invention can competitively inhibit the activation of the receptor caused by an agonist of GPR84, and can be used in the preparation of a medicament for treating related diseases caused by high expression or high excitability of GPR84 receptor, the diseases including multiple sclerosis, inflammatory bowel disease, arthritis and the like.

Abstract: Crystalline forms of brigatinib, pharmaceutical compositions comprising the same, and methods of their preparation and use of the same are disclosed herein.

Abstract: A method for forming 1,3,5,7-tetraalkyl-6-(2,4-dimethoxyphenyl)-2,4,8-trioxa-6-phosphaadamantane includes obtaining a solution comprising an ethereal solvent and an aluminum hydride, adding dichloro(2,4-dimethoxyphenyl)phosphine to the solution to produce 2,4-dimethoxyphenylphosphine, and reacting the 2,4-dimethoxyphenylphosphine with an acidic mixture comprising diones to produce 1,3,5,7-tetraalkyl-6-(2,4-dimethoxyphenyl)-2,4,8-trioxa-6-phosphaadamantane. The solution has a temperature from IN greater than ?20 C. to 50 C. throughout the method. Another method for forming 1,3,5,7-tetraalkyl-6-(2,4-dimethoxyphenyl)-2,4,8-tri-oxa-6-phosphaadamantane includes obtaining dichloro(2,4-dimethoxyphenyl)phosphine, forming 2,4-dimethoxyphenylphosphine by adding the dichloro(2,4-dimethoxyphenyl)phosphine to a solution comprising at least one solvent and an aluminum hydride, reacting the 2,4-dimethoxyphenylphosphine with a mixture to produce 1,3,5,7-tetraalkyl-6-(2,4-dimethoxyphenyl)-2,4,8-trioxa-6-phosphaadamantane.

Abstract: A 1, 4 bidentate ligand comprising first and second ligand centres, wherein the first ligand centre is an sp2-hybridised carbon or a nitrogen atom; wherein the second ligand centre is a nitrogen atom in a five- or six-membered aromatic or hetero-aromatic ring, said ring having a substantially linear substituent T1 meta or para to the nitrogen atom; wherein T1 has the formula 1: —Ar1a—Y1b—Ar2—[Y2c—Ar2]d—S—B??(1) and wherein T1 is attached to the ring by X1, wherein X1 is a bond, a methylene group, a substituted methylene group, an oxygen atom or a sulphur atom, wherein each Ar1 and Ar2 are independently selected from the group of C6 to C20 aromatic and C4 to C20 heteroaromatic groups, wherein Y1 and each Y2 is independently an optionally substituted C2 or acetonitrile trans double-bond linking moiety, wherein a is 0, 1, 2 or 3, wherein b is 0, 1 or 2, wherein each c is independently 0, 1 or 2, wherein d is 0, 1, 2, 3 or 4, S is a flexible spacer, and B represents a moiety having one or more cross-l

Abstract: The invention provides a method for preparing a technetium-99m tricarbonyl intermediate. The method comprises reacting a manganese carbonyl compound used as a carbon monoxide source with pertechnetate and water to obtain the technetium-99m tricarbonyl intermediate. The method for preparing a technetium-99m tricarbonyl intermediate in an embodiment of the invention can complete the preparation of the intermediate at atmospheric pressure and room temperature. The method is easy to operate, uses easily obtained raw materials, has a high labeling yield, and can be used to prepare various types of technetium tricarbonyl labeled probes.

Abstract: The present invention relates to a stevioside M crystal form, a preparation method therefor and a use thereof, and specifically, relates to a naturally extracted high-intensity sweetener, i.e., a stevioside M crystal form A, the preparation method therefor and the user thereof. By means of comprehensive characterization of the new crystal form, the new crystal form is found to have advantages such as a high degree of crystallinity, good stability, and low hygroscopicity, and is applicable to a more comprehensive field of application. The preparation method in the present invention is simple and easy to operate, has high selectivity and good reproducibility, and can stably obtain the target crystal form.

Abstract: The present invention provides immune stimulating macrolides of formula (I), wherein the substituents are as defined in the claims. The macrolides have utility in treating viral diseases and cancer.

Abstract: The present invention provides immune stimulating macrolide of formula (I). The macrolide has utility in treating intracellular bacterial, fungal, and protozoal infections.

Abstract: Metaphosphate compounds can directly phosphorylate other compounds to provide easy synthetic access to phosphorylated compounds, including cyclic phosphate compounds.

Abstract: Disclosed are cyclic-di-nucleotide cGAMP analogs, methods of synthesizing the compounds, pharmaceutical compositions comprising the compounds thereof, and use of compounds and compositions in medical therapy.

Abstract: The present invention relates to a new approach for the synthesis of multiphosphorylated peptides. Specifically, the present invention provides a process, which enables the synthesis of multiphosphorylated peptides with up to seven phosphorylated Serine (pSer) and Threonine (pThr) residues, including such residues that are close in sequence.

Abstract: Provided herein are methods of producing a heterologous polypeptide and compositions comprising same.

Abstract: The present technology relates to compounds, kits, compositions, and methods useful for the treatment of numerous pathologies including dementia, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, and other neurodegenerative diseases, spinal cord injury, traumatic brain injury, diabetes and metabolic syndrome, defective wound healing, and/or sensorineural hearing and vision loss.

Abstract: Described are compounds for targeting proteases, e.g. serine proteases and their use in the diagnostic methods and methods for treatment of respiratory diseases such as cystic fibrosis. The compounds have the structure [H]—[B]-[A]; wherein [H] is a hydrophilic group, [B] is a subsite recognition group and [A] is a binding group; wherein A has the formula: —C(0)—CH2—NR1—COOR2 and wherein [B] has the structure: (i) —[CO—CH2—NR3]m-, or (ii) -[AA1-AA2]- or (iii) -(AA1-C0-CH2NR3)— or (iv) —(CO—CH2—NR3-AA1)- or (v) —(C0—CH2—NR4-AA1-AA3)-.

Abstract: Cyclic lipopeptides having one or more modifications relative to daptomycin, and methods of making them are provided. The cyclic lipopeptides can be used as antibacterial agents. The daptomycin analogues are generated by chemical synthesis, which makes introduction of an unnatural amino acid and any modification into daptomycin possible. Pharmaceutical compositions and method of use thereof for the disclosed daptomycin analogues are also provided.

Abstract: The invention disclosed herein relates to peptide inhibitors for transthyretin (TTR) aggregation and methods of inhibiting TTR aggregation, cytotoxicity, and/or TTR amyloidosis. Illustrative embodiments of the invention include a composition of matter comprising at least one peptide designed to inhibit the aggregation of TTR, with this peptide typically being coupled to a heterologous amino acid tag. A pharmaceutically acceptable carrier selected to be compatible with the inhibitory peptide may also be included. A method for blocking or inhibiting the aggregation of transthyretin TTR is also provided.

Abstract: The present invention is directed to glypican-3-specific peptide reagents, methods for detecting hepatocellular carcinoma cells using the peptide reagents, and methods for targeting hepatocellular carcinoma cells using the peptide reagents.

Abstract: The present invention relates to spexin-based agonists specific for galanin receptor type 2 and use thereof. More specifically, the present invention provides peptide-based agonists with high specificity for galanin receptor type 2 and improved stability. The peptide-based agonists are involved in the regulation of in vivo physiological functions, such as food intake, anxiety, emotion, and addiction, for which galanin receptors type 2 is responsible, to effectively suppress appetite, help recover from anxiety disorder, and reduce pleasure addiction. Therefore, the peptide-based agonists can be used to prevent or treat galanin receptor type 2-mediated diseases.

Abstract: Provided herein are modified recombinant adeno-associated virus (rAAV) capsid proteins, such as modified rAAV1, rAAV5, and rAAV6 capsid proteins, rAAV particles comprising such capsid proteins, nucleic acid molecules encoding such capsid proteins, as well as compositions, kits and methods of use thereof.

Abstract: Provided herein relate to modified or mutant forms of secretin and compositions comprising the same. In particular, the modified or mutant forms of secretin permits efficient capture and/or translocation of an analyte through the modified or mutant secretin nanopores. Methods for using unmodified secretin or the modified or mutant forms of secretin and compositions, for example, for characterizing an analyte, e.g., a target polynucleotide, are also provided.

Abstract: The present disclosure provides materials and methods for cell-free expression of epitopes for immunotherapy applications. In particular, the present disclosure provides materials and methods for expressing concatenated epitopes using a cell-free protein synthesis platform for high throughput, large scale, and unbiased epitope screening and the generation of multi-epitope vaccines.

Abstract: The present invention relates to a nucleic acid molecule encoding a fusion protein, wherein the nucleic acid molecule comprises: (a) a first nucleic acid sequence encoding a first biosensor, wherein said first biosensor is a first molecule capable of interacting with a second molecule; (b) a second nucleic acid sequence encoding an effector-activating module, wherein the effector-activating module comprises a nucleic acid sequence encoding a first part of a protease, wherein said first part of the protease is capable of interacting with a second part of said protease to form an active form of said protease; (c) a third nucleic acid sequence encoding a third biosensor comprising a protease cleavage site, wherein the protease cleavage site is sterically occluded in the absence of a stimulus for said third biosensor and wherein the protease cleavage site becomes accessible in the presence of said stimulus.

Abstract: Compositions and methods for controlling pests are provided. The methods involve transforming organisms with a nucleic acid sequence encoding an insecticidal protein. In particular, the nucleic acid sequences are useful for preparing plants and microorganisms that possess insecticidal activity. Thus, transformed bacteria, plants, plant cells, plant tissues and seeds are provided. Compositions are insecticidal nucleic acids and proteins of bacterial species. The sequences find use in the construction of expression vectors for subsequent transformation into organisms of interest including plants, as probes for the isolation of other homologous (or partially homologous) genes. The pesticidal proteins find use in controlling, inhibiting growth or killing Lepidopteran, Coleopteran, Dipteran, fungal, Hemipteran and nematode pest populations and for producing compositions with insecticidal activity.

Abstract: The present invention is related to the recombinant production of proteins by using a synthetic gene for high protein expression in Pichia pastoris. More specifically, the invention describes the production of Sm14 Schistosoma mansoni recombinant protein, where a synthetic gene was created to promote high expression of such protein, a gene which was cloned under control of two types of Pichia pastoris promoters: methanol-inducible promoter (AOXI) and constituent promoter (GAP). With these constructions, Pichia pastoris strains were genetically manipulated to efficiently produce vaccine antigen Sm14. The processes to produce and purify this protein from P. pastoris cells, which can be escalated for their industrial production, were also improved.

Abstract: Disintegrin variants that bind specifically to one or more of ?5?1 and ?v integrins, such as ?v=1, ?v?3, ?v?5, ?v?6 and ?v?8, but with reduced binding activity to ?IIb?3, are described. Also described are uses of the disintegrin variants for the treatment or prevention of a disease associated with an ?v integrin or an ?5?1 integrin.

Abstract: The present invention relates to bacteriocins for control of Salmonella enterica (salmocins). The bacteriocins are derived from Salmonella. The salmocins can be expressed in plants and can be used in a method of preventing or reducing infection or contamination of an object with Salmonella.

Abstract: The present invention relates to an immunogenic fragment peptide of an EN2 protein or an antibody composition specifically recognizing the same. In the present invention, EN2 protein can be quantified through a method of specifically recognizing the peptide. Also, an antibody prepared using the peptide has vastly superior detection sensitivity compared to existing EN2 protein antibodies and thus can be useful in a diagnostic agent for diagnosing prostate cancer.

Abstract: The present invention relates to nuclease protein fusions for enhancing genome editing by homology-directed transgene integration (HDI). The inventors found that the rate of HDI mediated by the CRISPR/Cas9 system may be substantially improved by providing the Cas9 nuclease in the form of a fusion protein with at least the N-terminal domain of the CtIP protein. CtIP proteins are involved in the early steps of homologous recombination. In addition, the inventors identified the subdomains of the N-terminal domain of the CtIP protein that are important for improving the HDI rate. Thus, the invention relates to fusion proteins comprising a Cas9 protein, a tetramerization domain of a CtIP protein and a dimerization domain of a CtIP protein. Particularly, the inventors have tested these fusion proteins HEK293 cells, RG37DR cells and Sprague-Dawley rats.

Abstract: The invention relates to the use of a uromodulin polypeptide in prevention or therapy of vascular calcification or a disease caused by, or related to, vascular calcification, particularly vascular calcification in chronic kidney disease, in diabetes, in aging and in atherosclerosis.

Abstract: This invention relates to a truncated dysferlin nucleic acid and protein, vectors (e.g., adeno-associated virus vectors) comprising the nucleic acid and methods of using the same for delivery of dysferlin to a cell or a subject and treating dysferlinopathy.

Abstract: The present invention relates to a recombinant fusion protein comprising a fragment of the cardioprotective protein neuregulin-1 (NRG-1) fused to a monoclonal antibody (mAb) backbone and to a method of treating a disease or condition in a subject in need thereof comprising administering a therapeutically effective amount of the recombinant fusion protein or the pharmaceutical composition comprising the recombinant fusion protein disclosed herein.

Abstract: Recombinant proteins that comprise a bone morphogenic protein 2 backbone onto which was grafted a Müllerian-inhibiting substance type II receptor binding region of the Müllerian-inhibiting substance protein are provided. These proteins bind to this receptor on the surface of epithelial cancer cells, and induce apoptosis of such cells. These proteins are useful, for example, in the treatment of cancers such as ovarian, uterine, endometrial, fallopian tube, breast, prostate, and lung cancers.

Abstract: The present invention relates to novel fragments of AIMP1 protein and a composition comprising the same as an active ingredient for preventing skin-aging, anti-wrinkle, and improving skin flexibility or elasticity.

Abstract: A process is described for purifying insulin and insulin analogs that comprises high-pressure liquid chromatography with an acidic cation exchange medium performed in the presence of a water miscible organic modifier and at an elevated temperature followed by reverse phase chromatography performed in the presence of a water miscible organic modifier and at an elevated temperature.

Abstract: A peptide that binds specifically to neuropilin-1 (NRP1) without binding to neuropilin-2 (NRP2) is provided. A fusion protein, a fusion antibody, small-molecule drug, a nanoparticle, or a liposome, which comprises the peptide, and a pharmaceutical composition for treating or preventing cancer or angiogenesis-related diseases, and a composition for diagnosing cancer or angiogenesis-related diseases are provided. A polynucleotide encoding the peptide that binds specifically to NRP1 and a method for screening the peptide that binds specifically to NRP1 are provided. An antibody heavy-chain constant region Fc-fused peptide binding specifically to NRP1 has the property of binding specifically to NRP1, and thus when it is administered in vivo, it accumulates selectively in tumor tissue, and widens the intercellular space between tumor-associated endothelial cells to promote its extravasation and increases its tumor tissue penetration.

Abstract: Compositions and methods are provided for peptide sequences that are ligands for a T cell receptor (TCR) of interest, in a given MHC context.

Abstract: The present disclosure provides methods of modulating an immune response in an individual. The present disclosure provides methods of treatment. The present disclosure provides methods comprising administering a multimeric polypeptide (synTac) and an immune checkpoint inhibitor to an individual. The present disclosure provides methods comprising administering a multimeric polypeptide (synTac) to an individual who is undergoing treatment with immune checkpoint inhibitor.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: Compositions, reagents and methods to treat disease such as autoimmune diseases and allergy are described. The method involves isolating the immune cells specific to disease related pMHC multimer, in vitro expansion and then transferring the cells to the subject in need to treat related disease.

Abstract: The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules.

Abstract: The invention provides a method for separating a Factor VIII (FVIII) protein from a first composition comprising the FVIII protein, which contains at least the light chain of FVIII, and a von-Willebrand-Factor (vWF) protein which comprises at least the FVIII binding domain of vWF, wherein the FVIII protein can form a complex with the vWF protein, the method comprising the steps: contacting the first composition with an affinity resin comprising a ligand and a matrix, wherein the ligand has an affinity to the light chain of FVIII, and separating the affinity resin from the mixture to obtain a modified first composition and a second composition, wherein the second composition contains the affinity resin, and a complex of the FVIII protein and the vWF protein.

Abstract: The present invention relates to modified serpins for use in the treatment of bradykinin-mediated diseases. The modified serine protease inhibitors (serpins) have mutations in one or more of the P4, P3, P2, P1 and P1? residues of their reactive center loop, which mutations increase the serpin's inhibition of plasma kallikrein (PK) as compared to the corresponding unmodified serpin. The mutations in the modified serpins of the invention further ensure that serpins display substantially no inhibition of at least thrombin and activated protein C. A modified serpin of the invention further preferably shows increased inhibition of at least one of an active form of Factor XII (FXII) and plasmin as compared to the corresponding unmodified serpin, and, preferably, the serpin inhibits at least one of an active form of FXII and PK stronger than they are inhibited by C1 esterase inhibitor. Preferably the modified serpin is a modified ?1-antitrypsin.

Abstract: The present invention relates to a monoclonal antibody that inhibits immunosuppressive functions of pathogens, antigen-binding fragment thereof, and hybridomas producing such antibody. The monoclonal antibody or antigen-binding fragment thereof bind to a peptide consisting an amino acid sequence represented by MEKVGKDGVITVE (SEQ ID NO: 1). The present invention also discloses use of the invented monoclonal antibody or antigen-binding fragment thereof, and method of preparation for such hybridomas.

Abstract: An isolated monoclonal antibody or antigen-binding fragment thereof binds to F. tularensis lipopolysaccharide (Ft LPS). The antibody preferably lacks an Fc region or has an impaired Fc-region. The antibody may be formulated into a pharmaceutical composition along with a pharmaceutically acceptable carrier, excipient or diluent. It may be provided in a kit with means for detection of the antibody and instructions for use. A therapeutically effective amount of such an antibody can be used for prophylaxis, treatment or amelioration of Ft infection and for inhibiting Ft uptake by cells in a subject. The antibody can also be used to detect Ft infection. Also disclosed is an isolated nucleic acid molecule encoding the antibody, an expression vector having the isolated nucleic acid molecule, and a host cell transfected with such an expression vector.

Abstract: The present disclosure is directed to antibodies binding to prefusion and postfusion forms of both human S. aureus and human metapneumovirus F proteins, including neutralizing antibodies, and methods for use thereof.