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 are novel compounds of Formula (I): pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful in the treatment of diseases and disorders mediated by ROR. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I) and methods for their use in treating one or more inflammatory, metabolic, autoimmune and other diseases or disorders.

Abstract: The present invention is directed to compounds, tautomers and pharmaceutically acceptable salts of the compounds which are disclosed, wherein the compounds have the structure of Formula I, and the variable R1 is as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.

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: Compounds of formula (I) wherein R1, R2, A1 and A2 are as described herein, compositions including the compounds and methods of using the compounds as autotaxin inhibitors.

Abstract: A silicon-containing intermediate is synthesized by reacting a lanthanum tris[bis(trialkylsilyl)amide] complex with an alkylcyclopentadiene. A lanthanum compound is synthesized by reacting the silicon-containing intermediate with a dialkylamidine-based compound.

Abstract: The disclosure provides for thermal, solvent, and/or acid resistant metal organic frameworks and the use of these frameworks in devices and methods for gas separation, gas storage, and catalysis. The disclosure further provides for MOFs that are strong solid acids, and the use of these strong solid acid MOFs in catalytic devices and catalytic methods.

Abstract: The present invention provides carbonate prodrugs which comprise a carbonic phosphoric anhydride prodrug moiety attached to the hydroxyl or carboxyl group of a parent drug moiety. The prodrugs may provide improved physicochemical properties over the parent drug. Also provided are methods of treating a disease or condition that is responsive to the parent drug using the carbonate prodrugs, as well as kits and unit dosages.

Abstract: A method of preparing racemic or optically active D or L-?-glycerophosphorylcholine in large amounts by subjecting choline phosphate or a salt thereof, and racemic or optically highly pure (S) or (R)-3-halo-1,2-propanediol to a substitution reaction in a medium at high temperature in the presence of an inorganic base which increases the activity of the reaction. The method is cost-effective because of the use of starting materials which are inexpensive compared to those in a conventional method. Moreover, the method is simple and convenient because it is performed via a one-pot reaction without a separate purification process. In addition, it enables a large amount of racemic or optically active D or L-?-glycerophosphorylcholine, or a salt thereof, to be quantitatively produced in a medium without side reactions by using the inorganic base which increases the reaction activity.

Abstract: The present invention relates to compounds according to general formula (I) which are analogues of epoxymetabolites produced by cytochrome P450 (CYP) enzymes from omega-3 (n-3) polyunsaturated fatty acids (PUFAs). The present invention further relates to compositions containing one or more of these compounds and to the use of these compounds or compositions for C the treatment or prevention of conditions and diseases associated with inflammation, proliferation, hypertension, coagulation, immune function, pathologic angiogenesis, heart failure and cardiac arrhythmias.

Abstract: The present invention relates to a novel crystal form of oxazolidinone antibiotics. The new crystalline form has advantages in the aspects of solubility, hygroscopicity, crystallinity and stability. The present invention also relates to a method for preparing the new crystalline form, a pharmaceutical composition thereof and the use thereof in the preparation of drugs for treating and/or preventing diseases caused by microbial infection.

Abstract: Described herein, in certain embodiments, are steroidal derivatives, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat androgen receptor mediated diseases or conditions.

Abstract: The invention relates to C-3 novel triterpenone with C-28 reverse amide derivatives, related compounds, and pharmaceutical compositions useful for the therapeutic treatment of viral diseases and particularly HIV mediated diseases.

Abstract: The present invention provides a particular branched chain-containing aromatic compound. The branched chain-containing aromatic compound of the present invention is easily-soluble in isopropyl acetate superior in liquid-separation operability, and can be used for a production method of peptide and the like, which provides a final product simply by extraction separation, without crystallization and isolation of each intermediate in each step.

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: Pyrrolidine carboxamido derivatives, optical isomers thereof, and salts thereof that are able to prevent, improve, and/or treat inflammatory conditions, including inflammatory bowel disease, and methods for preparing and using the same are provided.

Abstract: The disclosure provides aromatic-cationic peptide compositions and methods of preventing or treating disease using the same. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof.

Abstract: A binding agent is capable of binding to rare earth materials such as rare earths and inorganic compounds thereof. A rare earth material-binding agent includes a peptide capable of binding to a rare earth material including a rare earth and a rare earth inorganic compound.

Abstract: An artificial catalyst system substitutable for an in vivo histone acylation function has been successfully established by such an approach of synthetic chromosome acylation using a combination of a chromosome-localizable nucleophilic catalyst and a chromosome-localizable acylating agent.

Abstract: The invention relates to cholecystokinin (CCK) derivatives of the general formula I: P-L-X1-X2-X3-Gly-Trp-X6-DMeAsp-X8-NH2, wherein P is Chem. 1: HOOC—(CH2)x—CO—*, wherein x is an integer in the range of 12-18; L is absent, or L comprises at least one linker element selected from Chem. 2: *—NH—CH(COOH)—(CH2)2—CO—*, Chem. 3: *—NH—(CH2)2—[O—(CH2)2]k—O—[CH2]n—CO—* wherein k is an integer in the range of 1-11 and n is an integer in the range of 1-5, Chem. 4: *—NH—CH(CH2OH)—CO—*, Chem. 5: *—NH—CH2—CO—*, and/or Chem. 6: *—NH—CH[(CH2)4—NH2]—CO—*; X1 is absent, Asp, DAsp, bAsp, DbAsp, Glu, or DGlu; X2 is Phe(4-sulfomethyl) or sTyr; X3 is Nle, Leu, Ala, Ile, Lys, Arg, Pro, Met, Phe, Ser, His, or Val; X6 is Nle, Ile, Gln, Met, Met(O2), Leu, Val, Pro, Hpg, or Ala; X8 is Phe, MePhe, 1Nal, Me1Nal, 2Nal, Me2Nal, Trp, or MeTrp. The invention also relates to the corresponding CCK peptides, as well as to methods for preparing the peptides and the derivatives.

Abstract: The subject invention concerns peptide mimetics of SOCS proteins and methods of use. In one embodiment, a peptide mimetic of the invention binds to a SOCS1 and a SOCS3 target protein. In a specific embodiment, a peptide mimetic of the invention comprises the amino acid sequence of SEQ ID NO:1 and/or SEQ ID NO:2 and/or SEQ ID NO:51, or a functional fragment or variant thereof. In a further embodiment, a peptide of the invention can comprise multiple copies of the mimetic sequence. In one embodiment, a peptide of the invention comprises two or more copies of SEQ ID NO:1 and/or SEQ ID NO:2 and/or SEQ ID NO:51. In a specific embodiment, a peptide mimetic of the invention comprises the amino acid sequence of SEQ ID NO:3 and/or SEQ ID NO:4 to and/or SEQ ID NO:52, or a functional fragment or variant thereof. The subject invention also pertains to methods of treating and/or preventing autoimmune conditions and/or disorders.

Abstract: Novel polypeptides and methods of making and using the same are described herein. The polypeptides include cross-linking (“hydrocarbon stapling”) moieties to provide a tether between two amino acid moieties, which constrains the secondary structure of the polypeptide. The polypeptides described herein can be used to treat diseases characterized by excessive or inadequate cellular death.

Abstract: Melanocortin receptor-specific cyclic hexapeptides of the formula where R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the claims, compositions and formulations including the hexapeptides of the foregoing formula or salts thereof, and methods of preventing, ameliorating or treating melanocortin-1 receptor-mediated or responsive diseases, indications, conditions and syndromes.

Abstract: The present invention relates to compositions comprising Moraxella catarrhalis (M. catarrhalis) Ubiquitous surface protein A2 (UspA2). More particularly, the present application relates to UspA2 protein constructs and immunogenic compositions comprising the constructs, vaccines comprising such immunogenic compositions and therapeutic uses of the same. The invention further relates to compositions comprising UspA2 in combination with at least one antigen from Haemophilus influenzae, immunogenic compositions comprising the antigens, vaccines comprising such immunogenic compositions and therapeutic uses of the same.

Abstract: Modified meningococcal fHbp polypeptides with increased stability.

Abstract: The present invention relates to a new isolated polypeptide nominated microcin S, isolated nucleic acid molecules encoding the microcin S polypeptide and primers and probes hybridizing to the nucleic acid molecules. The invention also relates to plasmids and cells comprising the nucleic acid molecules, an antibody binding to the polypeptide, compositions as well as methods for producing and using the polypeptides. The present invention further relates to medical uses for treating or preventing microbial infections, functional gastrointestinal disorders or treating a tumor. The invention further relates to a method for preserving food and a method for coating dressing material.

Abstract: A novel, mutated Salmonella enterica serovar Typhimurium vaccine is generated and imparts protective immunity in vaccinated animals for a range of S. enterica serovars. The vaccine can be attenuated or inactivated, including bacterial ghosts or membrane fractions thereof. Immunogenic compositions are included in the invention and methods of generating an immune response.

Abstract: Populations of polypeptide variants based on a common scaffold, each polypeptide in the population comprising the scaffold amino acid sequence EXXXAXXEIX XLPNLTXXQX XAFIXKLXDD PSQSSELLSE AKKLNDSQ (SEQ ID NO: 1) or AKYAKEXXXAXX EIXXLPNLTX XQXXAFIXKL XDDPSQSSEL LSEAKKLNDS Q (SEQ ID NO: 2), wherein each X individually corresponds to an amino acid residue which is varied in the population are disclosed. Also populations of polynucleotides, wherein each member encodes a member of a polypeptide population are disclosed. Furthermore, combinations of such polypeptide populations and such polynucleotide populations are disclosed, wherein each member of polypeptide population is physically or spatially associated with the polynucleotide encoding that member via means for genotype-phenotype coupling.

Abstract: Clostridium difficile is a leading cause of antibiotic-associated infection in hospitals worldwide. There is a need for a vaccine to Clostridium difficile that can target toxic proteins, or that can elicit adequate immunity to prevent infection or reduce the severity of infection. Modified Clostridium difficile toxin A and B (TcdA and TcdB) proteins are described herein, which comprise mutations that reduce toxin A and B toxicity compared to the native toxin. The proteins described are highly similar to the native toxin of Clostridium difficile, but toxicity is reduced.

Abstract: The present invention relates to polymer particles and uses thereof. In particular the present invention relates to functionalised polymer particles, processes of production and uses thereof in the diagnosis, treatment or prevention of tuberculosis.

Abstract: Disclosed herein are isolated polypeptides capable of preventing collapsin response mediator protein 2 (CRMP2)-small ubiquitin-like modifier (SUMO)ylation mediated trafficking of voltage gated sodium channel 1.7 (Nav1.7) function. In some examples, the disclosed peptides comprise three to twenty amino acids and include the amino acid sequence KMD. Also disclosed are methods of decreasing nociception including administering an effective amount of one or more disclosed peptides to a subject in need thereof, such as a subject experiencing chronic pain.

Abstract: The present technology relates to isolated MUC17, Muc3 or MUC3 derived polypeptides and polynucleotides encoding the same. The MUC17, Muc3 or MUC3 derived polypeptides and polynucleotides can be used to treat gastrointestinal tract diseases and disorders. Also described herein are pharmaceutical compositions comprising MUC17, Muc3 or MUC3 derived polypeptides and/or polynucleotides encoding the same alone or in combination along with a pharmaceutically acceptable carrier, diluent or excipient for the treatment of gastrointestinal disorders and diseases, including, irritable bowel disease and its associated colitides, for example, Crohn's Disease.

Abstract: Herein is reported a method for the purification of a protein comprising erythropoietin and a single poly (ethylene glycol) residue from reaction by-products or not reacted starting material by a cation exchange chromatography method. It has been found that by employing a cation exchange SP Sephacryl™ S 500 HR chromatography material conditioned to a conductivity of 21 mS/cm and a linear gradient elution a fusion protein of erythropoietin and a single poly (ethylene glycol) residue can be obtained in a single step with high purity and yield.

Abstract: The invention relates to IL-22 polypeptides, IL-22 Fc fusion proteins and IL-22 agonists, composition comprising the same, methods of making and methods of using the composition for the treatment of diseases. The invention also relates to IL-22 receptor associated reagents and methods of use thereof.

Abstract: The invention relates to derivatives of glucagon analogues comprising the substitutions Imp1 and His3, a substituent having three to ten negatively charged moieties covalently attached to a side chain of a lysine as well as intermediates and compositions thereof and their use in medicine.

Abstract: The present invention relates to dual GLP-1/glucagon receptor agonists and their medical use, for example in the treatment of disorders of the metabolic syndrome, including diabetes and obesity, as well as for reduction of excess food intake.

Abstract: The present invention is in the therapeutic fields of drugs for medical conditions relating to diabetes. More specifically the invention relates to novel acylated derivatives of human insulin analogues. The invention also provides pharmaceutical compositions comprising such insulin derivatives, and relates to the use of such derivatives for the treatment or prevention of medical conditions relating to diabetes.

Abstract: The present invention concerns the field of ion channels, and in particular relates to peptides which are suitable for use in the treatment of conditions where the L-type calcium channel (LTCC) density and function is altered. LTCCs are located on the membrane of all excitable cells and control the small voltage gradient across the plasma membrane by allowing the flow of Ca2+ ions down their electrochemical gradient. This Ca2+ flux is critical for numerous processes including cardiac action potential propagation, muscle contraction, Ca2+-dependent gene expression, synaptic efficacy, and cell survival by contributing to various signaling cascades. Reduction of the inward calcium current (I Ca) conducted through the LTCCs is seen in several diseases and medications to improve or restores impaired intracellular Ca2+ homeostasis are limited. The present invention reports mimetic peptides (MPs) that through a novel mechanism directly targets LTCCs and, by modulation of LTCC density and function, increases I Ca.

Abstract: This disclosure relates to recombinant cellular expression of chimeric proteins with peptide sequences derived from lymphocyte receptors and uses for treating cancer. In certain embodiments, the disclosure relates to a recombinant vector comprising a nucleic acid that encodes a chimeric protein with a segment with a targeting moiety based on a variable lymphocyte receptor (VLR) capable of binding a tumor associated antigen and a segment with a T cell signal transduction subunit. In certain embodiments, the recombinant vectors are used in immune based cancer treatments.

Abstract: Among other aspects, the present invention relates to cell culture conditions for producing high molecular weight vWF, in particular, highly multimericWF with a high specific activity and ADAMTS13 with a high specific activity. The cell culture conditions of the present invention can include, for example, a cell culture medium with an increased copper concentration and/or cell culture supernatant with a low ammonium (NH4+) concentration. The present invention also provides methods for cultivating cells in the cell culture conditions to express high molecular weight vWF and rA13 having high specific activities.

Abstract: Herein is reported the use of a conjugate of a subunit of a multi-subunit structure and one biologically active entity for targeted delivery of the biologically active entity to the multi-subunit structure.

Abstract: The present invention provides a compound having the structure: A-B-----Z wherein A is a biologically active structure of the compound; wherein Z is a protein component of the compound, which protein component comprises one or more polypeptides, wherein at least one of the one or more polypeptides comprises consecutive amino acids which (i) are identical to a stretch of consecutive amino acids present in a chain of an Fc domain of an antibody; (ii) bind to an Fc receptor; and (iii) have at their N-terminus a sequence selected from the group consisting of a cysteine or selenocysteine; wherein the dashed line between B and Z represents a peptidyl linkage; and wherein the solid line between A and B represents a nonpeptidyl linkage, as well as intermediates dimers thereof, and processes of producing the compounds of the invention.

Abstract: The present invention relates to biologically active fusion proteins containing the IgG2 hinge as a multimerization domain capable of multimerizing proteins, peptides and small molecules which are active or more active in multimeric form; compositions comprising such fusion proteins; and methods of making and using such fusion proteins.

Abstract: The invention provides means and methods for selecting and producing stable antibodies against an antigen of interest, using stable ex vivo B cell cultures.

Abstract: The present invention relates to methods and compositions for preventing and treating Staphylococcus aureus in a subject. Therapeutic compositions of the present invention comprise leukocidin E and/or D proteins or polypeptides and anti-leukocidin E and/or D antibodies. The invention further relates to methods of identifying inhibitors of LukE/D cytotoxicity and inhibitors of LukE/D-leukocyte binding.

Abstract: The invention is directed to compositions and methods for stimulating, enhancing or modulating the immune system of a patient before or after infection by a pathogen, and in particular MTB. Compositions of the invention contain non-naturally occurring antigens that generate an effective cellular and/or humoral immune response to MTB and/or antibodies that are specifically reactive to MTB antigens. The greater activity of the immune system generated by a vaccine of the invention increases generation of memory T cells that provide for a greater and/or extended response to an MTB infection. Responses involve an increased generation of antibodies that enhance immunity against MTB infection and promote an enhanced phagocytic response. Monoclonal antibodies produced by the non-naturally occurring antigens enhance phagocytosis and killing of mycobacteria by phagocytic cells, enhance clearance of MTB from the blood and modulate immunity and cytokine responses.

Abstract: Provided herein are humanized antibodies or antigen-binding fragments thereof, that can bind to a cyclic peptide comprising the amino acid sequence SNK, wherein the K (Lysine) is solvent-accessible and methods of treating and/or preventing amyloid-beta associated diseases such as Alzheimer's disease.

Abstract: The present invention provides compositions and methods which involve specifically antagonizing GDF8 and Activin A. In certain embodiments, compositions are provided which comprise a GDF8-specific binding protein and an Activin A-specific binding protein. For example, the invention includes compositions comprising an anti-GDF8 antibody and an anti-Activin A antibody. In other embodiments, antigen-binding molecules are provided which comprise a GDF8-specific binding domain and an Activin A-specific binding domain. For example, the invention includes bispecific antibodies that bind GDF8 and Activin A. The compositions of the present invention are useful for the treatment of diseases and conditions characterized by reduced muscle mass or strength, as well as other conditions which are treatable by antagonizing GDF8 and/or Activin A activity.

Abstract: This invention provides methods and compositions of antibody therapeutics that are therapeutically effective in the digestive tract or below the mucosal barrier of the digestive tract but do not deliver levels of antibody to the systemic circulation that have been shown to be necessary for clinical benefit following systemic administration of antibody. This invention further describes therapeutic compositions of antibody therapeutics that are therapeutically effective in the digestive tract or below the mucosal barrier of the digestive tract but do not deliver levels of antibody to the systemic circulation that have been associated with adverse events and systemic immunosuppression following systemic administration of antibody.

Abstract: The invention provides anti-oncostatin M receptor-? (OSMR) antigen binding proteins, e.g., antibodies and functional fragments, derivatives, muteins, and variants thereof. OSMR antigen binding proteins interfere with binding of OSM and/or IL-31 to OSMR. In some embodiments, anti-OSMR antigen binding proteins are useful tools in studying diseases and disorders associated with OSMR and are particularly useful in methods of treating diseases and disorders associated with OSMR and binding of OSM and/or IL-31 to OSMR.