Abstract: The present invention relates to a novel process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof using novel intermediates.

Abstract: Certain embodiments useful as HIV-inhibitor agents are directed to fullerene derivatives tetrahydro-1H—C60-fulleropyrrolo[1,2-c][1,3]thiazine salts (Formula I) or tetrahydro-1H—C70-fulleropyrrolo[1,2-c][1,3]thiazine salts (Formula II), while further embodiments are directed to ?, ?, ?, and/or ? isomer of tetrahydro-1H—C70-fulleropyrrolo[1,2-c][1,3]thiazine salt.

Abstract: Provided herein, inter alia, is the synthesis of ETP derivatives. The uses of the ETP derivatives described herein include treatment of cancer.

Abstract: Provided herein are substituted pyrazolopyridine compounds, and pharmaceutical compositions thereof, useful for the treatment of, for example, central nervous system and metabolic diseases and disorder.

Abstract: The invention is directed to the preparation of fluorinated compounds and their use in organic synthesis. In particular, the invention is directed to methods of reacting compounds of structure with Rf—CH?N2 or (CF3)2C?N2 to form a perfluoroalkylate or -arylated compounds, and products derived from these reactions, where X, YB, and Rf are described herein.

Abstract: In general, the invention features compounds useful for the synthesis of analogs of halichondrin B, such as eribulin or pharmaceutically acceptable salts thereof, e.g., eribulin mesylate.

Abstract: The present invention relates to a method for the purification of lecithin, comprising the steps of (a) mixing lecithin with active carbon to form a dispersion; then (b) mixing an organic solvent into the dispersion; then (c) separating the active carbon and contaminants from the lecithin preferably through gravitational forces. The invention further relates to a lecithin substantially free of contaminants, and a food or feed product comprising said lecithin.

Abstract: An object of the present invention is to provide a lysophosphatidylserine derivative or a salt thereof. The present invention provides a lysophosphatidylserine derivative or a salt thereof, or a pharmaceutical composition or a lysophosphatidylserine receptor function modulator comprising said compound or a salt thereof.

Abstract: Provided are piperazine compounds of Formula I useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described here.

Abstract: The invention relates to a method for producing aqueous preparations of complexes of platinum group metals (PGM) Pt, Pd, Rh and Ir having the general formula [MA/MB/MC(L)a(H2O)b(O2—)c(OH?)d](OH—)e(H+)f, wherein MA=PtII or PdII, MB=PtIV, MC=Rh or Ir, L is a neutral monodentate or bidentate donor ligand, and a is an integer between 1 and 4 (or 2) and/or between 1 and 6 (or 3), b is an integer between 0 and 3 (or 5), c is an integer between 0 and 3 (or 4), d is an integer between 0 and 3 (or 5), e is an integer between 0 and 2 (or 3 or 4) and f is an integer between 0 and 4 (or 5). In the method according to the invention, the hydroxo complexes H2Pd(OH)4 (in the case of MA=PdII), H2Pt(OH)6 (in the case of MA=PtII and MB=PtIV) or H3MC(OH)6 (for MC=RhIIIIrIII) are converted in the presence of the donor ligands, wherein at least one hydroxo group of the hydro complex is exchanged. Preferably, the reaction occurs at temperatures in the range of 40 to 110° C.

Abstract: A solid-state material comprising a solid-state compound is provided. The solid-state compound has the formula: [Cluster1][Cluster2]n, where Cluster1 can be a metal chalcogenide molecular cluster, Cluster2 a carbon cluster, and n the number of Cluster2 clusters in the solid-state compound. A method of forming a solid-state material is also provided.

Abstract: Objects of the present invention are to provide a novel dehydrogenation reaction catalyst, to provide a method that can produce a ketone, an aldehyde, and a carboxylic acid with high efficiency from an alcohol, and to provide a method for efficiently producing hydrogen from an alcohol, formic acid, or a formate, and they are accomplished by a catalyst containing an organometallic compound of Formula (1).

Abstract: There are provided, inter alia, methods for decreasing mucus elasticity or decreasing mucus viscosity in a subject in need thereof, the methods including administering to the subject an effective amount of a thiosaccharide mucolytic agent, and compounds and pharmaceutical compositions useful for the methods.

Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N-(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.

Abstract: The present invention discloses a method of harnessing versatile phosphoramidation reactions to regioselectively link a group of alkynyl-/azido-containing compounds to post-synthetic nucleic acids primed with phosphate at the 5? termini. The method includes steps of: (a) monophosphoramidating H2N(CH2)nNH2 to the 5? end of the nucleic acid to form an intermediate 1 where n is an integer from 2 to 6, and the intermediate 1 has a formula of: (b) amidating the free —NH2 group of the intermediate 1 with to form an intermediate 2; and (c) reacting the terminal —N3 group of the intermediate 2 with 1-{3-{[4-(2-cyclooctyn-1-ylmethyl)benzoyl]amino}propyl}-4-{2-[4-(dimethylamino)phenyl]ethenyl}pyridinium hexafluorophosphate (Alkyne MegaStokes dye 608) by the SPAAC reaction to form modified nucleic acids. Without the presence of Cu(I), the modified nucleic acids were subjected to azide-alkyne cycloaddition in an aqueous solution to obtain various nucleic acid conjugates with a high yield.

Abstract: The present invention relates generally to the compound: N-((4aS,6aR,6bS,8aR,12aS,14aR,14bS)-11-cyano-2,2,6a,6b,9,9,12a-heptamethyl-10,14-dioxo-1,2,3,4,4a,5,6,6a,6b,7,8,8a,9,10,12a,14,14a,14b-octadecahydropicen-4a-yl)-2,2-difluoropropanamide, polymorphic forms thereof, methods for preparation and use thereof, pharmaceutical compositions thereof, and kits and articles of manufacture thereof.

Abstract: A method of refolding proteins expressed in non-mammalian cells present in concentrations of 2.0 g/L or higher is disclosed. The method comprises identifying the thiol pair ratio and the redox buffer strength to achieve conditions under which efficient folding at concentrations of 2.0 g/L or higher is achieved and can be employed over a range of volumes, including commercial scale.

Abstract: Disclosed are a tripeptide epoxyketone compound, a preparation method thereof, and a use thereof in the preparation of anti-tumor drugs.

Abstract: The invention provides peptides that can reactivate p53 mutants efficiently and specifically, as well as methods that allow the identification, selection and isolation of such peptides, in a precise, cost and time effective manner. In particular, there are provided mutant p53 reactivating peptides that can restore the native wild type p53 folding, and hence the tumor suppressor activity, to the mutant p53 protein. Such peptides are useful for treating various conditions and diseases in which p53 is mutated.

Abstract: The present disclosure provides glycosylated oligopeptides having the sequence Palmitoyl-X1-Lys-X2-X3-Lys-X4-OH, where: X1 is: absent, Ser having a glycosylated side chain, or Asn having a glycosylated side chain; X2 is: Thr, Thr having a glycosylated side chain, Asn having a glycosylated side chain, or Ser having a glycosylated side chain; X3 is: Thr, or Thr having a glycosylated side chain; X4 is: Ser, or Ser having a glycosylated side chain. At least one of X1, X2, X3 and X4 is an amino acid having a glycosylated side chain. Each glycosylated side chain is, independently, glycosylated with a carbohydrate selected from the group consisting of: glucose, N-acetyl-glucosamine, galactose, N-acetyl-galactosamine, mannose, maltose, lactose, rhamnose, cellobiose, xylose, and fucose. Each hydroxyl group on the carbohydrate is, independently, OH or acetylated.

Abstract: A synthetic peptide that targets cancer stem cells is provided. The peptide consists of the amino acid sequence of anyone of SEQ ID NO: 1 to SEQ ID NO: 15. Also provided is a composition comprising said synthetic peptide with a therapeutic agent fused thereto, and a pharmaceutically acceptable carrier or diluent. Further provided is a method of screening a peptide specifically targeting to a cancer stem cell. The method comprises the steps of establishing an oligopeptide library by using a phage expression system, contacting the library with a culture of bulk tumor cells of a cancer cell line, contacting the phages which do not bind to the bulk tumor cells with a culture of cancer stem cells of said cancer cell line, and screening a peptide specifically targeting to a cancer stem cell from the phages which bind to the cancer stem cells.

Abstract: The present disclosure provides compounds which are immunomodulators and thus are useful for the amelioration of various diseases, including cancer and infectious diseases.

Abstract: A synthetic peptide having nestin expression inducing ability which allows induction of expression of nestin in astrocytes; an agent for inducing nestin expression including the peptide as an active ingredient; and a method for producing high nestin expressing cells derived from astrocytes, the method being characterized in that the agent for inducing nestin expression is supplied. The agent for inducing nestin expression provided by the present invention includes, as an active ingredient, a synthetic peptide including a nestin-inducing peptide sequence consisting of an amino acid sequence of SEQ ID NO: 1 or an amino acid sequence formed by conservative replacement of 1, 2 or 3 amino acid residues in the amino acid sequence. The method for producing high nestin expressing cells derived from astrocytes provided by the present invention includes preparing an astrocyte culture, and supplying, at least once, the agent for inducing nestin expression to the astrocyte culture.

Abstract: The invention relates to novel cyclodecapeptide compounds having formula (I) for use as drugs and, more specifically, for use in the diagnosis, prevention and/or treatment of neurodegenerative diseases, such as Wilson's disease and Alzheimer's disease, and for use in the diagnosis, prevention and/or treatment of poisoning with metal ions, such as copper and mercury ions. The invention also relates to pharmaceutical compositions comprising at least one compound having formula (I) as an active principle.

Abstract: The present invention provides vectors that contain and express in vivo or in vitro FeLV antigens that elicit an immune response in animal or human against FeLV, compositions comprising said vectors and/or FeLV polypeptides, methods of vaccination against FeLV, and kits for use with such methods and compositions.

Abstract: The present invention provides mutant polypeptides useful as hypoallergens. More specifically the present invention provides mutant Bet v 1 proteins and the use of such polypeptides as hypoallergens for desensitizing against birch pollen allergies. Furthermore, the invention provides vaccine formulations comprising such polypeptides; the use of such formulations; and to methods of vaccination against birch pollen allergy.

Abstract: The invention relates to plant transcription factor polypeptides, polynucleotides that encode them, homologs from a variety of plant species, and methods of using the polynucleotides and polypeptides to produce transgenic plants having improved tolerance to drought, shade, and low nitrogen conditions, as compared to wild-type or reference plants.

Abstract: The invention relates to modified antibiotic peptides, in particular derivatives of apidaecin and oncocin, preferably having increased stability, reduced immunoreaction, and improved pharmacokinetics. In the invention, the peptide antibiotics are reversibly protected by means of a linker having the polymer polyethylene glycol (PEG). The peptide linker contains a recognition sequence for trypsin-like serum proteases. In the apidaecin derivatives, the linker and the PEG are bonded to a side chain. In the serum, the linker is cut by serum proteases and PEG is separated off. The released peptide still contains remnants of the linker, which are still bonded to the amino group in the side chain. Astonishingly, said remaining remnants of the linker impair the activity of the antimicrobial peptide only a little or not at all.

Abstract: The present invention relates to use of an antagonist of BIR1 (B cell immunoglobulin receptor 1) related to the present invention, a method for screening the antagonist, in addition to subtype polypeptides of BIR1, the polynucleotide encoding them and antibodies for the polypeptides. BIR1 functions as an immunosuppressive receptor, and the antagonist of BIR1 has immunopotentive activity, which is able to use for preventing and/or treating a cancer, an immunodeficiency disease or an infectious disease.

Abstract: Disclosed are compositions and methods for modulating Dpy-30 binding activity. The compositions may include peptides or peptidomimetics thereof that are related to radial spoke protein 3 (RSP3) or absent, small, homeotic discs 2-like protein (Ash2L) and that bind to Dumpy-30 protein (Dpy-30).

Abstract: The invention relates to novel therapeutic approaches to cancer treatment that exploits tumor suppressor functions of DKK3b by site-specific delivery of DKK3b. Novel therapeutics and methods for treating tumors and cancers utilizing DKK3b tumor suppressor functions are disclosed.

Abstract: An antimicrobial peptide which is a derivative of the peptide P-113. The amino acid sequence of the antimicrobial peptide is SEQ ID NO: 4 or SEQ ID NO: 5, in which the C-terminus is or is not modified with a NH2.

Abstract: The invention provides peptides and the nucleic acid sequences that encode them. The invention further provides therapeutic, diagnostic and research methods for diagnosis, treatment, and prevention of apoptosis associated disorders.

Abstract: Provided are a new peptide, a vector inserting a DNA that codes said peptide, a transformant obtained by transformation with that vector, and applications of said peptide, vector and transformant. The peptide comprises an amino acid sequence set forth in SEQ ID NO: 1, or an amino acid sequence obtained by substituting, deleting or adding one or more amino acids to/from the amino acid sequence set forth in SEQ ID NO: 1. This peptide and the vector inserting a DNA that codes this peptide are suitable for use in an agent for promoting the proliferation of pancreatic hormone-producing cells, or a differentiation induction promoter that induces differentiation to pancreatic hormone-producing cells.

Abstract: The invention relates to novel designer osteogenic proteins having altered affinity for a cognate receptor, nucleic acids encoding the same, and methods of use therefor. More preferably, the novel designer osteogenic proteins are designer BMPs and have altered affinity for a cognate BMP receptor. The designer BMPs demonstrate altered biological characteristics and provide potential useful novel therapeutics.

Abstract: Described herein are methods of syntheses and therapeutic uses of covalently modified peptides and/or proteins. The covalently modified peptides and/or proteins allow for improved pharmaceutical properties of peptide and protein-based therapeutics.

Abstract: The present invention relates to soluble monomeric Anti-Mullerian Hormone Receptor type II (AMHRII) fusion proteins and uses thereof, in particular for detection or quantification of the bioactive cleaved form of Anti-Müillerian Hormone in a sample. In particular, the present invention relates to a soluble monomeric AMHRII fusion protein wherein one AMHRII extracellular domain is fused to a heterologous polypeptide. A further aspect of the present invention relates to a method for detecting or quantifying the presence of bioactive cleaved AMH in a sample, said method comprising contacting the sample with a soluble monomeric AMHRII fusion protein of the invention.

Abstract: A recombinant fusion protein comprising the moieties Band CT, and optionally REP, wherein B is comprising at least one immunoglobulin fragment, which provides the capacity of selective interaction with an organic target; CT is a moiety of from 70 to 120 amino acid residues and is derived from the C-terminal fragment of a spider silk protein; and REP is a moiety of from 70 to 300 amino acid residues and is derived from the repetitive fragment of a spider silk protein.

Abstract: The present invention relates to fibronectin based scaffold domain proteins that bind PCSK9. The invention also relates to the use of the innovative proteins in therapeutic applications to treat atherosclerosis, hypercholesterolemia and other cholesterol related diseases. The invention further relates to cells comprising such proteins, polynucleotides encoding such proteins or fragments thereof, and to vectors comprising the polynucleotides encoding the innovative protein.

Abstract: The present invention provides UTI fusion proteins, DNA sequences for producing the same, and pharmaceutical compositions and methods of using the same.

Abstract: Libraries of immunoglobulins which each have one or more amino acid modifications in at least one structural loop region of such immunoglobulins, where the modified loop region specifically binds to an epitope of an antigen to which an unmodified immunoglobulin does not significantly bind.

Abstract: The present invention relates to a binding molecule having influenza A virus-neutralizing activity derived from a human B cell, and the binding molecule having the influenza A virus-neutralizing activity, according to the present invention, is a binding molecule that is derived from a B cell that is selected from the blood of a patient infected with an influenza A virus, and has neutralizing activity against influenza A viruses, and thus is useful in preventing and treating disease derived from the influenza A virus, and can be useful in diagnosing the influenza A virus by using the binding molecule according to the present invention.

Abstract: The present invention relates to an epitope peptide (or a variant thereof) which can be used in the prevention of respiratory syncytial virus (RSV) infection, a recombinant protein comprising the epitope peptide (or a variant thereof) and a carrier protein, and uses of the epitope peptide (or a variant thereof) and the recombinant protein. The present invention also relates to an antibody against the epitope peptide, a cell line for generating the antibody, and uses thereof. Furthermore, the present invention also relates to a vaccine or a pharmaceutical composition comprising the recombinant protein or the antibody according to the invention, for preventing one or more symptoms associated with RSV infection.

Abstract: The invention relates generally to activatable antibodies and methods of making and using these activatable antibodies in a variety of therapeutic, diagnostic and prophylactic indications.

Abstract: The disclosure features over 5000 methylation and acetylation sites identified in human cell line, human serum and mouse tissues, peptides (including AQUA peptides) comprising a methylation or acetylation site of the disclosure, antibodies specifically bind to a methylation or acetylation site of the disclosure, and diagnostic and therapeutic uses of the above.

Abstract: This disclosure generally relates to antibodies or antibody fragments which specifically bind to M-CSF. In particular antibodies and antibody fragments are disclosed which bind to M-CSF and which inhibit binding of M-CSF to the M-CSF receptor with an IC50 of 10 pM or less. The invention also relates to nucleic acids, vectors and host cells capable of expressing the antibodies or fragments thereof of the invention, pharmaceutical compositions comprising the antibodies or fragments thereof and uses of said antibodies or fragments thereof and compositions for treatment of specific diseases.

Abstract: Specific binding members, in particular human anti-IL-13 antibody molecules and especially those which neutralize IL-13 activity. Methods for using anti-IL-13 antibody molecules in diagnosis or treatment of IL-13 related disorders, including asthma, atopic dermatitis, allergic rhinitis, fibrosis, inflammatory bowel disease and Hodgkin's lymphoma.

Abstract: A pharmaceutical composition comprising an active agent that causes reduction of the level of systemic immunosuppression in an individual for use in treating a disease, disorder, condition or injury of the CNS that does not include the autoimmune neuroinflammatory disease, relapsing-remitting multiple sclerosis (RRMS), is provided. The pharmaceutical composition is for administration by a dosage regimen comprising at least two courses of therapy, each course of therapy comprising in sequence a treatment session followed by an interval session.

Abstract: Engineered monovalent binding proteins that bind to one or more ligands (such as an antigen) via one binding domain are provided, along with methods of making and uses in the prevention, diagnosis, and/or treatment of disease.

Abstract: The disclosure provides a method for immunotherapy of a cancer patient, comprises administering to the patient an Ab that inhibits signaling from the PD-1/PD-L1 signaling pathway, or a combination of such Ab and an anti-CTLA-4 Ab. This disclosure also provides a method for immunotherapy of a cancer patient comprising selecting a patient who is a suitable candidate for immunotherapy based on an assessment that the proportion of cells in a test tissue sample from the patient that express PD-L1 on the cell surface exceeds a predetermined threshold level, and administering an anti-PD-1 Ab to the selected subject. The disclosure additionally provides rabbit mAbs that bind specifically to a cell surface-expressed PD-L1 antigen in a FFPE tissue sample, and an automated IHC method for assessing cell surface expression in FFPE tissues using the provided anti-PD-L1 Abs.