Abstract: This disclosure is directed to agonists of the apelin receptor (APJ) and uses of such agonists.

Abstract: Proteinopathies result from the proteasome not acting efficiently enough to eliminate harmful proteins and prevent the formation of the pathogenic aggregates. As described herein, inhibition of proteasome-associated deubiquitinase Usp14 results in increased proteasome efficiency. The present invention therefore provides novel compositions and methods for inhibition of Usp14, enhancement of proteasome activity and treatment of proteinopathies.

Abstract: The present invention provides a compound of Formula I: wherein R is H, a methyl group, an ethyl group, a n-propyl group, an iso-propyl group, or a n-butyl group; and R1 is H, a 4?-methyl group, a 4?-OH, a 4?-OMe group, a 2?,3?-C2H4 group, a 3?,4?-C2H4 group, a 3?,4?-diF, a 3?,4?,5?-triF, or a 4?-OCF3; and optionally including a salt or a hydrate of said compound, and further provides a pharmaceutical composition comprising the compound of Formula I and one or more acceptable pharmaceutical carriers. A method of treating a patient having cancer comprising administering a therapeutically effective amount of a compound of Formula I, or a pharmaceutical composition comprising a compound of Formula I and one or more acceptable pharmaceutical carriers to the patient is disclosed.

Abstract: The present disclosure relates to novel macrocyclic compounds and libraries thereof containing heteroaryl moieties that are useful as research tools for drug discovery efforts. The present disclosure also relates to methods of preparing these compounds and libraries and methods of using these libraries, such as in high throughput screening. In particular, these libraries are useful for evaluation of bioactivity at existing and newly identified pharmacologically relevant targets, including G protein-coupled receptors, nuclear receptors, enzymes, ion channels, transporters, transcription factors, protein-protein interactions and nucleic acid-protein interactions. As such, these libraries can be applied to the search for new pharmaceutical agents for the treatment and prevention of a range of medical conditions.

Abstract: Marinopyrrole derivatives and methods for their synthesis and use are described herein. Novel cyclic and symmetric marinopyrroles with triazole substituents having antibacterial activity against resistant bacterial strains, such as MRSA are introduced. Also provided are methods of using the compounds for treating or preventing cancer and/or microbial infections.

Abstract: The present disclosure relates generally to novel molecules, compositions, and formulations for treatment of bacterial infections in general and more specifically to bacterial infections with antibiotic resistant pathogens.

Abstract: This invention relates to compounds which selectively bind to the survival protein MCL-1 with high affinity and selectivity, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for modulating MCL-1 activity and for treating hyperproliferative disorders, angiogenesis disorders, cell cycle regulation disorders, autophagy regulation disorders, inflammatory disorders, and/or infectious disorders and/or for enhancing cellular engraftment and/or wound repair, as a sole agent or in combination with other active ingredients.

Abstract: The present invention relates to a novel compound having an antiviral effect, more specifically, a pyridone derivative having HIV integrase inhibitory activity, and a medicament containing the same, in particular, an anti-HIV agent. The compound of the present invention has integrase inhibitory activity and/or cell proliferation inhibitory activity against viruses, in particular, HIV and drug-resistant strains thereof. Thus, the compound is useful in preventing or treating various diseases, viral infections (for example, AIDS), and the like in which integrase participates.

Abstract: An organic metal compound-containing composition, comprising: at least one organic metal compound (A) selected from the group consisting of metal alkoxides and metal chelates, and a polymerizable compound (B) having a polymerizable functional group and a carboxyl group.

Abstract: Acyl germanium compound according to general formula [RmAr—(C?O)—]4—Ge and process for the preparation thereof. The compound is suitable as initiator for radical polymerization.

Abstract: Disclosed are novel branched amphiphilic lipids, in particular novel branched amphiphilic lipids of general formula (II). Also disclosed is a method of synthesis for the compounds of formula (II), from unsaturated amphiphilic compounds of general formula (I). Further disclosed is the use of the compounds of general formula (II) and of the lipoplexes obtained by formulation of the compounds of general formula (II) for applications, particularly transfection, in which improved fusion properties are desired.

Abstract: The present invention relates primarily to a process for producing particular phosphinates (phosphonous acid monoesters) and use thereof for producing biologically active substances which may be used in the pharmaceutical or agrochemical sector, preferably for producing phosphorus-containing amino acids.

Abstract: The present invention relates to novel crystalline forms of salts and/or co-crystals of tenofovir alafenamide, the pharmaceutical formulations, and the therapeutic uses thereof in treating viral infections.

Abstract: The invention encompasses the novel class of compounds represented by the Formula (I) below, which are inhibitors of the TC-PTP enzyme. The invention also encompasses pharmaceutical compositions which include the compounds shown above and methods of treating or preventing TC-PTP mediated diseases, including cancer, via their use in the activation of antigen-presenting cells, like dendritic cells, for applications in the immunotherapeutic treatment of diseases.

Abstract: This invention relates generally to metal carbene olefin metathesis catalyst compounds, to the preparation of such compounds, compositions comprising such compounds, methods of using such compounds, articles of manufacture comprising such compounds, and the use of such compounds in the metathesis of olefins and olefin compounds. The invention has utility in the fields of catalysts, organic synthesis, polymer chemistry, and industrial and fine chemicals industry.

Abstract: A process for obtaining a mixture of C4-C8 and C9-C18 alkyl monoether of saccharide, comprising: a) a first step of acetalization or trans-acetalization of a saccharide or of a mixture of saccharides with a C4-C8 aliphatic aldehyde or the acetal thereof, b) a second consecutive or simultaneous step of acetalization or trans-acetalization of the product obtained in a) of the saccharide or mixture of saccharides with a C9-C18 aliphatic aldehyde or the acetal thereof, c) a step of catalytic hydrogenolysis of the saccharide acetals obtained, and d) a step of recovery of a mixture of C4-C8 and C9-C18 alkyl saccharide monoethers. The invention further relates to a mixture of C4-C8 and C9-C18 alkyl saccharide monoethers and the use thereof as a surfactant.

Abstract: The subject matter of the present invention is a compound characterized in that it has the general formula (I): in which P1, X, n, A, L and L1 are as defined in Claim 1. The present invention also relates to a process for preparing said compounds (I) and to the use thereof for targeting the cation-independent mannose 6-phosphate receptor (CI-M6PR). The subject matter of the invention is also a conjugate of formula (III): in which P1, X, n, A, L and L?1 are as defined in Claim 6, and the use thereof: in a method for therapeutic treatment of the human or animal body, in particular chosen from enzyme replacement therapy, photodynamic therapy or cancer treatment, and/or in a method of diagnosis, in particular of diseases or of ailments associated with an increase or with a decrease in CI-M6PR expression.

Abstract: Novel pseudo-disaccharide and pseudo-trisaccharide aminoglycosides, represented by Formulae I or Ia, as defined in the instant specification, designed to exhibit stop codon mutation readthrough activity, are provided. Also provided are pharmaceutical compositions containing the same, and uses thereof in the treatment of genetic diseases and disorders, such as diseases and disorders associated with stop codon mutations.

Abstract: The present invention relates to the use of avermectin derivative as a drug for the treatment of parasitic infections. The avermectin derivative is represented by the formula (I) wherein: (i) R1 is chosen from the group constituted of —CH(CH3)2, —CH(CH3)CH2CH3, or cyclohexyl, (ii) X represents —CH2—CH2—, or —CH?CH—, (iii) R2 is chosen from or an OH group, (iv) R3 is OH or NOH, (v) represents a single bond when R3 is OH, or a double bond when R3 is NOH, as an inhibitor of a membrane-bound protein which transports exogenous compounds out of target cells.

Abstract: This invention claims aqueous compositions that comprise triphosphates of 2?-deoxynucleoside derivatives that have, instead of a 3?-OH moiety, a 3?-ONH2 moiety; wherein said compositions contain less than 0.5 mole percent contaminating triphosphate having a 3?-OH moiety, as well as processes for providing such compositions. The compositions further must contain insubstantial amounts of hydroxylamine.

Abstract: The present invention relates to a thiol compound suitable for forming a chain of oligomers that can be grafted to an oligonucleotide. The invention also relates to an oligonucleotide grafted by such a compound, thus having one or more thiol functions, suitable for being immobilized on a gold surface or on a grafted surface.

Abstract: A hydroprocessing catalyst has been developed. The catalyst is formed from a unique transition metal molybdotungsten oxy-hydroxide material. The hydroprocessing using the transition metal molybdotungsten oxy-hydroxide material-based catalyst may include hydrodenitrification, hydrodesulfurization, hydrodemetallation, hydrodesilication, hydrodearomatization, hydroisomerization, hydrotreating, hydrofining, and hydrocracking.

Abstract: A process is provided for the making of estetrol starting from a 3-A-oxy-estra-1,3,5(10),15-tetraen-17-one, wherein A is an C1-C5 alkyl group, preferably a methyl group, or a C7-C12 benzylic group, preferably a benzyl group. This process is particularly suitable to industry.

Abstract: The present invention accordingly provides novel compounds of formula (I) wherein R1, R2, R3 and R4 are as defined in the claims. The invention further relates to their in treatment or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of the 17?-HSD1 enzyme and/or requiring the lowering of the endogenous estradiol concentration.

Abstract: Ligand functionalized substrates, methods of making ligand functionalized substrates, and methods of using functionalized substrates are disclosed.

Abstract: The present disclosure relates generally to methods of producing, processing, or purifying antibodies. The present disclosure also relates to methods of producing, processing, or purifying a target antibody from cell cultures to remove host cell proteins.

Abstract: The present invention relates to a method for the separation of antibodies, specifically antibodies having different degrees of fucosylation. The method is based on binding affinity of antibodies to Fc receptors. The invention further relates to the use of Fc receptors for the separation of antibodies having different degrees of fucosylation.

Abstract: The present invention describes a new peptide aldehyde produced naturally by Streptomyces lividans 66, which we have called livipeptin. Using genome mining of natural products, we predicted that SLl0883-5 genes encode an unprecedented biosynthetic system, unusually small (4.6 Kbp), which produces an acylated peptide aldehyde. Because of the chemical characteristics of the predicted compound, we postulated its anti-proteolytic activity, which we confirmed by identifying and purifying this compound through metabolic profiles of HPLC and MS of the mutated strain lacking these three genes and the wild strain. To this objective, we identified the conditions wherein these genes are strongly expressed. The livipeptin was purified and its inhibitory activity on the proteolytic activity of selected proteases was demonstrated in vitro. The design of an expression cassette for its heterologous expression is also described plus its use for heterologous protein production.

Abstract: The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib.

Abstract: The invention relates generally to the synthesis of modified amino acids and modified peptides in the presence of cyclometalated catalysts. The invention has utility in the fields of catalysis, organic synthesis, polymer chemistry, and industrial and fine chemicals chemistry.

Abstract: Disclosed are compound exhibiting highly active and selective binding to ???6 integrin, which are represented by the following general formula (I): Cyclo-(Arg-X1-Asp-X2-X3-X4-X5-X6-X7) (I) wherein the variables groups X to X have the following meanings X1: Ser, Gly, Thr, X2: Leu, Ile, Nle, Val, Phe, X3: Gly, Ala, X4: Leu, He, Nle, Val, Phe, Lys, Tyr, Trp, Arg, X5: D-Pro, N-Me-D-lipophilic amino acids, X6: Pro, N-Me-amino acids, N-Me-Lys, N-Me-Lys(Ac), and X7; Ala, Leu, He, Nle, Val, Phe, Tyr, Trp or wherein the sub-sequence -X5-X6- represents a ?-turn mimetic differing from the meanings above, or pharmaceutically acceptable salts, esters, solvates, polymorphs or modified forms thereof represented by the following general formula (II): (X0)n1L(X8)n2 wherein X0 represents the compound of the general formula (I) as specified above (excluding one hydrogen atom to allow bonding to the linker), L represents a linker, X8 represents the effector moiety and wherein n1 and n2 are each independently selected from the ra

Abstract: The invention relates to a polypeptide #including the following amino acid sequence: W-S-X1-W-X2-X3-C-S-X4-C-G (SEQ ID NO: 59), wherein X1, X2 and X3 are, independently of one another, S or G, X4 is R-S or V-S or V-T or R-T, and both cysteines form a disulfide bridge.

Abstract: The present invention provides therapies, vaccines, and predictive methods for Flaviviruses, including Zika virus, Dengue virus, and Japanese encephalitis virus, and provides compounds for diagnosing, preventing, and treating outbreaks of Zika virus, Dengue virus, and Japanese encephalitis virus.

Abstract: The invention generally relates to recombinant human cytomegalovirus (CMV) gB proteins and immunogenic fragments thereof, which do not comprise a transmembrane (TM) domain; and comprise one or more mutations that reduce the aggregation between the monomeric trimers of gB, and/or adhesion of the monomeric trimer of gB to the host cell.

Abstract: The present invention relates to novel fusion polypeptides and the uses thereof. The invention particularly relates to conjugated coat proteins derived from nepoviruses, virus-like particles made with such proteins, and the uses thereof. The particles of the invention can expose and/or encage molecules of interest and have utility in various fields such as the pharmaceutical, agro, or veterinary areas.

Abstract: According to the invention, immunogenicity of an antigenic peptide is increased by administering a fusion protein, which comprises an antigenic peptide and an adjuvant protein, wherein the adjuvant protein comprises two or more proteins selected from the group consisting of a Shiga toxin 2e B subunit (Stx2eB), an Escherichia coli heat-labile toxin B subunit (LTB), and a cholera toxin B subunit (CTB). or a transformant transformed by a gene coding for the fusion protein.

Abstract: It has been found that an extracellular polypeptide derived from Akkermansia municiphila is capable of modulating and/or promoting gut mucosal immune system function and/or maintaining and/or restoring metabolic status and/or increasing the physical integrity of the gut mucosal barrier in a mammal. The polypeptide or host cells including such polypeptide may be employed to prevent and/or treat a variety of conditions that benefit from an increased physical integrity of the gut mucosal barrier and/or an improved gut mucosal immune system function and metabolic status.

Abstract: A method for producing a fibroin-like protein is provided. A fibroin-like protein is produced by a method of culturing Escherichia coli having a gene encoding the fibroin-like protein in a medium, inducing expression of the gene encoding the fibroin-like protein, and collecting the fibroin-like protein, wherein accumulation of an organic acid at the time of inducing the expression is reduced, and wherein the gene is expressed under control of a tryptophan promoter.

Abstract: Provided are a novel Dermatophagoides farinae protein, and a diagnostic drug, a prophylactic drug and a therapeutic drug for an allergic disease caused by Dermatophagoides farinae. A Dermatophagoides farinae protein selected from the group consisting of the following (a) to (c), or a fragment peptide thereof: (a) a protein including an amino acid sequence set forth in SEQ ID NO:2; (b) a protein including an amino acid sequence in which one or several amino acids have been substituted, deleted, or added relative to the amino acid sequence set forth in SEQ ID NO:2, and having allergenicity of Dermatophagoides farinae; and (c) a protein including an amino acid sequence having 90% or higher identity with the amino acid sequence set forth in SEQ ID NO:2, and having allergenicity of Dermatophagoides farinae.

Abstract: The present invention relates to a pharmaceutical composition comprising complement split product C4d for use in treating an inflammatory condition, such as graft rejection, graft versus host disease, an autoimmune disease or atopy. The C4d to be used may be a multimer. Accordingly, also C4d multimers and their use in medicine, like the treatment of inflammatory conditions, is provided. Furthermore, the present invention provides a protein complex comprising C4d interacting with its ILT4 receptor. This protein complex may be used in screening methods Also antibodies specifically binding to the C4d multimer or the C4d/ILT4-protein complex are subject of the present invention.

Abstract: A modified FGF-1 polypeptide that has an increased binding affinity for heparin relative the wild-type human FGF-1's binding affinity for heparin is described. The modified FGF-1 polypeptide has at least 80% amino acid sequence identity to wild-type human FGF-1 having SEQ ID NO: 1. The serine at an amino acid position of the modified FGF-1 polypeptide corresponding to amino acid position 116 of SEQ ID NO: 1 is substituted by an amino acid that increases the modified FGF-1 polypeptide's binding affinity for heparin relative to the binding affinity of SEQ ID NO: 1 to heparin.

Abstract: We describe an ELABELA polypeptide comprising a sequence CXXXRCXXXHSRVPFP (SEQ ID NO: 1), in which X signifies an amino acid residue, such as a sequence selected from the group consisting of: SEQ ID NO: 2 to SEQ ID NO: 18, preferably CLQRRCMPLHSRVPFP (SEQ ID NO: 2), or a fragment, homologue, variant or derivative thereof, which polypeptide is capable of maintaining self-renewal and/or pluripotency of a stem cell.

Abstract: A single-chain insulin comprises a C-domain of 6 to 11 amino acid residues comprising at least two acidic residues at the N-terminal side of the C-domain and at least two basic residues at the C-terminal side of the C-domain peptide, a basic amino acid residue at the position corresponding to A8 of human insulin, and an acidic amino acid residue at the position corresponding to A14 of human insulin. The C-domain may contain a 2 to 4 amino acid joint region between the acidic and basic residues. Residues C1 and C2 may have a net negative charge of ?1 or ?2; and the remaining C-domain segment may culminates with two basic residues. A pharmaceutical composition comprises the single-chain insulin, formulated at a pH within the range 7.0 to 8.0, and may be formulated at a concentration of 0.6 mM to 5.0 mM and/or at a strength of U-100 to U-1000.

Abstract: Provided herein are freeze-dried preparations comprising a high-purity parathyroid hormone (PTH) peptide and one or more PTH analogs, and methods for the production thereof. Also provided is a test method for detecting PTH analogs to confirm the purity of a freeze-dried preparation containing PTH peptide, and the like.

Abstract: The present invention discloses cryopreserved recombinant cells for screening drug candidates that transiently overexpress one or more drug transporter proteins and/or drug metabolizing enzymes. Advantageously, such cells provide a cost-efficient consumable product that streamlines the process of screening whether drug candidates are substrates or inhibitors of drug transporter proteins and/or drug metabolizing enzymes.

Abstract: The present invention discloses cryopreserved recombinant cells for screening drug candidates that transiently overexpress one or more drug transporter proteins and/or drug metabolizing enzymes. Advantageously, such cells provide a cost-efficient consumable product that streamlines the process of screening whether drug candidates are substrates or inhibitors of drug transporter proteins and/or drug metabolizing enzymes.

Abstract: Herein is a fusion polypeptide with the formula R1-FC-R2, wherein R1 denotes a first Fc-receptor, R2 denotes a second Fc-receptor, and FC denotes a heavy chain Fc-region polypeptide, wherein R1 or R2 or both are present, wherein FC does not substantially bind to R1 and/or R2 and uses thereof.

Abstract: The present invention relates to compositions and methods for treating of a HIV infected mammal using a CD4 membrane-bound chimeric receptor or a HIV specific scFvs CARs. One aspect includes a modified T cell and pharmaceutical compositions comprising the modified cells for adoptive cell therapy and treating a disease or condition associated with HIV infection.

Abstract: The technology relates generally to the field of immunology and relates in part to compositions and methods for controlling the proliferation of T cells, for example, therapeutic T cells. The methods further relate to compositions and methods for inducing an immune response in a subject.

Abstract: The present invention provides interleukin-33 (IL-33) antagonists comprising one or more IL-33-binding domains and one or more multimerizing domains and methods of using the same. According to certain embodiments of the invention, the IL-33-binding domains can comprise an IL-33-binding portion of an ST2 protein and/or an extracellular portion of an IL-1RAcP protein. The IL-33 antagonists of the invention are useful for the treatment of diseases and disorders associated with IL-33 signaling and/or IL-33 cellular expression, such as infectious diseases, inflammatory diseases, allergic diseases and fibrotic diseases.