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 integrase, pharmaceutical compositions containing such compounds, and methods for using these compounds in the treatment of HIV infection.

Abstract: Disclosed herein are compounds, pharmaceutical compositions, and related methods for the treatment of viral infection, including RNA viral infection in subjects. The compounds, pharmaceutical compositions, and methods can modulate the innate immune antiviral response in vertebrate cells, including activating the RIG-I pathway.

Abstract: Disclosed herein are boronate intermediates in the synthesis of antimicrobial compounds and the use and preparation thereof. Some embodiments relate to crystalline boronate salt derivatives and their use in the synthesis of therapeutic compounds.

Abstract: A process for the hydrosilylation of an unsaturated compound comprising reacting (a) a silyl hydride with (b) an unsaturated compound in the presence of (c) a platinum based hydrosilylation catalyst comprising a platinum-diene complex with chelating anions. The use of the present catalysts in the process provides silylated products in good yields and allows for using lower platinum loadings than conventional catalysts, reduced cycle times, and may reduce yellowing in the product.

Abstract: The present invention features compounds effective in inhibiting active against Hepatitis C virus (“HCV”) polymerase. The invention also features processes of making such compounds, compositions comprising such compounds, and methods of using such compounds to treat HCV infection.

Abstract: The present invention provides compounds that bind to mitochondrial aldehyde dehydrogenase-2 (ALDH2), methods of using said compounds to treat patients with Fanconi Anemia, and methods of preparing said compounds.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is a phosphonate substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduces the excessive activation of complement.

Abstract: The invention provides for compositions comprising phosphorous containing tricyclic compounds, including phthalazin-1(2H)-one derivatives. The compounds are potent inhibitors of the enzyme poly(ADP-ribose)polymerase (PARP), particularly PARP-1 and potentially PARP-2. The also show good cellular activity in inhibiting poly(ADP-ribose) oligomer formation. The compounds may be useful as mono-therapy or in combination with other therapeutic agents in the treatment conditions where PARP is implicated, such as cancer, inflammatory diseases and ischemic conditions. Thus, also provided are methods for the treatment of a condition where PARP is implicated comprising administering to an effective amount of a compound of the invention to an individual in need thereof.

Abstract: The invention relates to a universally usable process for reducing the chlorine content of organobisphosphites.

Abstract: The current invention provides metal ion complexes with an organic ligand, compositions comprising such complexes. In particular, these complexes are capable of reacting with a reactive oxygen species in a subject and increase their T1-weighted relaxivities so a clinical MRI scanner can detect an oxidative stress hotspot in the subject. The disclosed complexes also exhibit excellent anti-oxidant properties and low cell toxicity, therefore can be used as a therapeutic agent to relieve oxidative stress in the subject, or as both a MRI contrast agent and therapeutic agent in a composition.

Abstract: The present invention relates to the use of trisaccharide derivates comprising a substituted trisaccharide core, which trisaccharide core is fully substituted with fatty acid ester groups, and optionally one or more anionic groups as adjuvants, to the trisaccharide derivates as such, to a method for preparing such trisaccharides, to trisaccharides obtained with such method, to adjuvant compositions comprising such trisaccharide derivates and to a vaccine or kit comprising such adjuvant compositions.

Abstract: The present invention relates to a process for obtaining Tiacumicin B with a well defmed crystal habit and particle size. The process according to the invention comprises repeating cycles of heating and cooling under controlled conditions of temperature and stirring.

Abstract: The present invention provides a phenyl C-glucoside derivative containing a deoxyglucose structure as represented by formula I, preparation method thereof, a pharmaceutical composition comprising the same, and uses thereof in the preparation of medicaments for treating diabetes, wherein substituents R1-R7 are as defined in the specification. The present invention also provides a method for synthesizing the phenyl C-glucoside derivative containing a deoxyglucose structure and an intermediate product. The method has advantages of being simple to manage and of low cost, which is suitable for large-scale industrial production. The present invention further provides a cocrystal of (1S)-1-[4-chloro-3-(4-ethoxybenzyl)phenyl]-1,6-dideoxy-D-glucose and L-proline, and preparation method and uses thereof.

Abstract: The present invention relates to a pure polymorph of Nor-UDCA or Bis-nor-UDCA, or of a pharmaceutically acceptable salt thereof. The invention further provides a pharmaceutical composition comprising the polymorph of the invention, and a method for preparing the polymorph. The invention includes the pharmaceutical use of the polymorph or of the pharmaceutical composition of the invention.

Abstract: Disclosed is a method of liberating a peptide, the method comprising a step of bringing a self-aggregate of albumin containing a peptide incorporated therein into contact with a solution that contains a compound represented by Formula (I) or (II) defined in the specification at a concentration of 80 mM to 1000 mM and allowing the peptide to be liberated from the self-aggregate of albumin into the solution.

Abstract: Provided herein is a novel method of purifying an IgG antibody from a preparation by use of an electropositive membrane having a defined porosity.

Abstract: Compounds, methods of use, and processes for making inhibitors of complement Factor D comprising Formula I, or a pharmaceutically acceptable salt or composition thereof wherein R12 or R13 on the A group is an ether substituent (R32) are provided. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade. The inhibitors of Factor D described herein reduce the excessive activation of complement.

Abstract: Provided are methods of treating a cancer characterized by the presence of a mutant allele of IDH1/2 comprising administering to a subject in need thereof a compound described here.

Abstract: The present disclosure provides aromatic-cationic peptide compositions and methods of using the same. The methods comprise use of the peptides in inhibiting cholesterol-induced cytochrome c peroxidase activity, promoting reduction of cytochrome c, and inhibition of cardiolipin peroxidation to treat, prevent or ameliorate cholesterol-induced mitochondrial dysfunction.

Abstract: The instant invention describes macrocyclic compounds having therapeutic activity, and the mechanism and methods of treating disorders such as autoimmune diseases, inflammation, and cancer, tumors and cell proliferation related disorders.

Abstract: The present disclosure is directed to providing: a new cell-penetrating peptide; and a composition for delivering a biologically active substance, a composition for gene therapy, a method for delivering a biologically active substance and a method for gene therapy using the same. The cell-penetrating peptide of the present disclosure can effectively deliver a protein into human cells and tissues, can deliver a protein with higher efficiency in comparison with a TAT peptide that is commercially used as a cell-penetrating peptide, and can also be usefully used in delivering a biologically active substance such as a protein, a genetic material, a chemical compound, etc. which may be used for a therapeutic purpose into cells.

Abstract: The invention relates to an antimicrobial surface, in particular a surface functionalised with a peptide comprising an antimicrobial moiety. The invention comprises a surface functionalised with a peptide comprising an antimicrobial moiety and a binder moiety, wherein the peptide is immobilized on the surface by electrostatic interactions between the binder moiety and the surface. Further provided is a medical device, a peptide and a method for the immobilization of a peptide.

Abstract: The invention relates to novel peptides having an HDM-2 targeting sequence that target the human minute binding protein-2. The invention also relates to fusion proteins comprising a HDM-2 targeting sequence. The invention also relates to methods of using the peptides to treat cancer.

Abstract: The present invention refers to proteins and bioactive peptides with immunomodulating and antiviral activity. Present peptide complexes have three-dimensional structure and are described by the following structural formula (SEQ ID NO: 23): wherein: X1 is preferably absent or is selected from among Gln, Ser, Asn, Val, Ala, Phe, and Asp, and R1 and R2 are peptide chains containing the amino acid residues His or Cys that interact with transition metal ions, wherein R1 is preferably selected from among Cys-Val-Val-Thr-Gly- (SEQ ID NO: 31), Cys-Gly-, Val-Ser-Gly-, and His-Gly- or alternatively is absent and R2 is preferably selected from among -Val-His-Gly, -Val-Phe-Val, -Val-His, -Val-Asp or alternatively is absent. Such histidine-rich peptide complexes, primarily alloferon family peptides with Zn ions, enable the creation of drugs with a targeted mechanism of action, and the design thereof with regard to understanding of drug target structure.

Abstract: Disclosed are: a composition for organ, tissue or cell transplantation, containing, as an active ingredient, a peptide comprising the amino acid sequence of SEQ ID NO: 1, a peptide having at least 80% sequence homology with the amino acid sequence, or a peptide which is a fragment thereof; a kit comprising the composition; or a method using the composition. By using the composition, the kit, or the method, the viability and/or function of an organ, tissue, or cell after transplantation are strengthened and an organ, tissue or cell isolated from a living body is preserved temporarily without damage.

Abstract: The present invention is directed to a novel class of antimicrobial agents called ?-AApeptides. The current invention provides various categories of ?-AApeptides, for example, linear ?-AApeptides, cyclic ?-AApeptides, and lipidated ?-AApeptides. ?-AApeptides of the current invention are designed to exert antimicrobial activity while being stable and non-toxic. ?-AApeptides also do not appear to lead to the development of microbial resistance in treated microorganisms. Thus, the disclosed ?-AApeptides can be used for the treatment of various medical conditions associated with pathogenic microorganisms.

Abstract: Aspects of the present invention relate to chimeric polypeptides including HCV NS3/4A sequences and T-cell epitopes. Embodiments include nucleic acids encoding the chimeric NS3/4A polypeptides, the encoded polypeptides, compositions containing said nucleic acids, compositions containing said chimeric polypeptides, as well as methods of making and using the aforementioned compositions including, but not limited to medicaments and vaccines.

Abstract: Provided are compositions are methods for discovery of new materials and interactions under extreme environmental conditions such as elevated temperatures at or in excess of 60° C. A synthetic thermostable protein is provided that is linked to a target peptide. A library of target peptides may be linked to a plurality of the thermostable proteins for expression on the cell surface of a thermophilic organism. The composition employs a modified form of the T. thermophilus TtoA protein that has a non-naturally occurring N-terminus for associating with a target peptide thereby expressing the target peptide on the outer cell membrane where the thermophilic protein is stable at high temperatures for discovery of materials useful in extreme environments or for us in study conditions that require or suffer under elevated temperatures.

Abstract: The invention provides a polypeptide that is not full length Anthrax Lethal Factor (LF) or a fusion thereof, comprising or consisting of one or more sequences selected from the group of LF457-486, LF467-486, LF101-120, LF171-190, LF241-260, LF251-270, LF261-280, LF281-300, LF457-476, LF467-486, LF547-567, LF574-593, LF584-603, LF594-613, LF604-623, LF644-663, LF674-693, LF694-713 and LF714-733, and further provides a polynucleotide encoding such a polypeptide or a vector comprising such a polynucleotide, optionally wherein the vector is an adenoviral vector. A method for vaccinating a subject against anthrax or B. anthracis comprising the step of exposing the subject to a polypeptide, polynucleotide, vector, host cell or composition of the invention, optionally wherein the subject is a human or a livestock or domestic animal.

Abstract: This invention relates to novel recombinant clostridial neurotoxins exhibiting increased duration of effect and to methods for the manufacture of such recombinant clostridial neurotoxins. These novel recombinant clostridial neurotoxins comprise a random coil domain, and the methods comprise the steps of inserting a nucleic acid sequence coding for a random coil domain into a nucleic acid sequence coding for a parental clostridial neurotoxin and expression of the recombinant nucleic acid sequence comprising the random coil domain-coding sequence in a host cell. The invention further relates to novel recombinant single-chain precursor clostridial neurotoxins used in such methods, nucleic acid sequences encoding such recombinant single-chain precursor clostridial neurotoxins, and pharmaceutical compositions comprising the recombinant clostridial neurotoxin with increased duration of effect.

Abstract: The present invention provides amyloid fibrils comprising a plurality of modified ? solenoid protein (mBSP) monomers. The mBSP monomers are modified to enhance self-assembly and are useful in a variety of applications.

Abstract: This invention provides polypeptides that were identified as interacting with Vip3 toxin. This invention also provides a method of identifying agents that bind to Vip3 interacting polypeptides, which agents may act as insecticidal agent, cytotoxic agents and/or modulate the activity of Vip3 interacting polypeptides.

Abstract: A cDNA, including the nucleotide sequence represented by SEQ ID NO: 2. A cDNA, including a nucleotide sequence encoding a complete protein, a protein fragment, a protein analogue, or a protein derivative each including the amino acid sequence represented by SEQ ID NO: 1. A cDNA, including the nucleotide sequence encoding the amino acid sequence represented by SEQ ID NO: 1.

Abstract: The present invention relates to methods and pharmaceutical compositions for the treatment of cancer. In particular, the present invention relates to a polypeptide comprising or consisting of i) an amino acid sequence ranging from the phenylalanine residue at position 380 to the leucine residue at position 384 in SEQ ID NO: 1 or, ii) an amino acid sequence having at least 70% of identity with the amino acid sequence ranging from the phenylalanine residue at position 380 to the leucine residue at position 384 in SEQ ID NO: 1, or iii) an amino acid sequence which is a retro-inverso of the amino acid sequence ranging from the phenylalanine residue at position 380 to the leucine residue at position 384 in SEQ ID NO: 1 or, iv) an amino acid sequence which is retro-inverso of the amino acid sequence having at least 70% of identity with the amino acid sequence ranging from the phenylalanine residue at position 380 to the leucine residue at position 384 in SEQ ID NO: 1.

Abstract: A dual targeting drug carrier is provided. The dual targeting drug carrier comprises a first targeting molecule and a second targeting molecule, wherein the targeting molecule comprises peptide, protein or antibody. The targeting molecule can bind to specific receptors, proteins, or glycoproteins to recognize the specific tumor cells, tissues, or organs.

Abstract: The present invention relates to novel monomeric fusion proteins derived from human GAG binding proteins such as chemokines with increased glycosaminoglycan (GAG) binding affinity and knocked-out or reduced GPCR activity compared to wild type GAG binding proteins, which are highly selectively competitive and are of increased bioavailability, and to their use for prevention or treatment of pathological cell movement as in metastasis.

Abstract: Peptide hormone analogues of the formula X-V are provided herein, wherein X is a glucagon analogue or a GLP1 analogue, and V is a C-terminal extension amino acid sequence comprising at least four amino acid residues, at least three of said residues being His. Also provided herein are pharmaceutical compositions comprising said analogues, and methods of using said analogues for the treatment of conditions such as obesity and diabetes.

Abstract: The invention relates to a derivative of a GLP-1 analogue, which analogue comprises a first K residue at a position corresponding to position 27 of GLP-1(7-37) (SEQ ID NO: 1); a second K residue at a position corresponding to position T of GLP-1(7-37), where T is an integer in the range of 7-37 except 18 and 27; and a maximum of ten amino acid changes as compared to GLP-1(7-37); wherein the first K residue is designated K27, and the second K residue is designated KT; which derivative comprises two albumin binding moieties attached to K27 and KT, respectively, via a linker, wherein the albumin binding moiety comprises a protracting moiety selected from HOOC—(CH2)x—CO— and HOOC—C6H4—O—(CH2)y—CO—; in which x is an integer in the range of 6-16, and y is an integer in the range of 3-17; wherein the linker comprises an element of the formula —NH—(CH2)2—(O—(CH2)2)k—O—(CH2)n—CO—, wherein k is an integer in the range of 1-5, and n is an integer in the range of 1-5; or a pharmaceutically acceptable salt, amide, or este

Abstract: Methods and compositions for clonally inhibiting or clonally stimulating T-cells are provided.

Abstract: In certain aspects, the present invention provides compositions and methods for modulating (promoting or inhibiting) growth of a tissue, such as bone, cartilage, muscle, fat, and/or neuronal tissue. The present invention also provides methods of screening compounds that modulate activity of an ActRIIB protein and/or an ActRIIB ligand. The compositions and methods provided herein are useful in treating diseases associated with abnormal activity of an ActRIIB protein and/or an ActRIIB ligand.

Abstract: Provided herein are materials and methods for delivering immunoglobulins (e.g. therapeutic immunoglobulins) across the blood-brain barrier.

Abstract: A process for synthesizing and separating secretory IgA from a mixture of IgA monmer and IgA dimer is provided. The process includes covalently binding affinity tagged or epitope tagged recombinant secretory component to the IgA dimer in the mixture and binding the affinity tagged or an epitope tagged secretory IgA to immobilized moieties on the solid phase support resin to which the affinity tag or epitope tag binds and then eluting the affinity tagged or an epitope tagged secretory IgA with release buffer. A process for synthesizing and separating secretory IgM from a mixture of IgM and other plasma proteins is also provided. The process includes covalently binding affinity tagged or an epitope tagged recombinant secretory component to the IgM in the mixture and binding the affinity tagged or an epitope tagged secretory IgM to immobilized moieties on the solid phase support resin and then eluting the peptide tagged secretory IgM with a release buffer.

Abstract: The present invention relates to the purification of immunoglobulins and the problem of providing a method for purifying an immunoglobulin in an efficient and cost-effective manner and with satisfactory purity and yield. In particular, the present invention addresses the aspect of the re-use of the rather cost-intensive chromatography materials, in particular the lifetime of the chromatography materials used in the capture step of the downstream process, and how this can be increased while reducing the technical complexity of the purification process.

Abstract: An antibody preparation suitable for intravenous administration in humans includes IgG, IgA and at least 5% IgM antibodies by weight of the total amount of antibodies. The preparation is prepared from human plasma, has specific complement activating activity, and, in an in vitro assay with human serum suitable to determine the ability of the antibody preparation to activate complement unspecifically, the antibody preparation generates substantially no C5a and/or substantially no C3a. The antibody preparation can have medical uses.

Abstract: The present invention relates to the field of biochemistry and pharmaceutical technologies. The present invention provides nanobodies that bind to human pulmonary surfactant protein A (SP-A) as well as the preparing methods and use of the same. The nanobody comprise an amino acid sequence having the formula of Q(x)2LVESGG(x)2V (x)2G(x) SL(x) LS(x)24E (x)n2KG(x)4S(x)n3T(x)2Y(x) C(x)n4S(x)n5V(x)n6R; wherein x is any amino acid; n2˜n6 are positive integers; 1?n2?21; 1?n3?19; 1?n4?50; 1?n5?22; 1?n6?8. The present invention take fresh frozen sections of lung as antigen, gene sequences with high affinity with hSP-A were obtained by constructing an SP-A antibody library and affinity selection, and nanobodies with high affinity and small molecule weight were obtained by induced expression of the gene sequences through a prokaryotic expression vector. Immunohistochemistry and in vivo imaging in nude mice showed the nanobodies have high specificity for targeting lung tissue.

Abstract: The present invention relates to variable domains of a camelid heavy-chain antibodies directed against a phosphorylated tau protein and conjugates thereof. The present invention also relates to the use of these domains or conjugates for treating or diagnosing disorders mediated by neurofibrillary tangles, neuropil threads or dystrophic neurites, such as tauopathies.

Abstract: The invention provides antibodies that specifically bind transthyretin (TTR). The antibodies can be used for treating or effecting prophylaxis of diseases or disorders associated with TTR accumulation or accumulation of TTR deposits (e.g., TTR amyloidosis). The antibodies can also be used for diagnosing TTR amyloidosis and inhibiting or reducing aggregation of TTR, among other applications.

Abstract: Provided herein is an isolated antibody or antigen-binding fragment that specifically binds tau, the antibody or fragment comprising a heavy chain variable (VH) region and a light chain variable (VL) region having amino acid sequences set forth herein. Also provided are methods of preventing or treating a tauopathy in a subject, comprising administering to a human in need of therapy for a tauopathy with one or more antibodies or fragments as described herein, wherein the antibodies or antigen-binding fragment are administered under conditions and in an amount effective to prevent or treat the tauopathy.

Abstract: This application provides methods of treating cancer and/or inhibiting angiogenesis with an anti-Ang2 antibody or functional part thereof either alone or in combination with at least one additional therapeutic agent.

Abstract: Described herein are novel compositions comprising IL-27 or NFIL-3 modulators (i e , inhibitors or activators), and methods using these agents for targeting cells, such as functionally exhausted or unresponsive immune cells, and modulating TIM-3 activity or expression. These compositions, methods, and uses are useful for the treatment of chronic immune conditions, such as persistent infections, cancer, and autoimmune diseases.