Abstract: The invention relates to particular prodrugs of substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT2A receptor, the serotonin transporter (SERT), pathways involving the dopamine D1 and D2 receptor signaling system, and/or the ?-opioid receptor.

Abstract: Novel pyrimido[1?,6?:1,5]pyrazolo[4,3-b][1,7]naphthyridine, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The pyrimido[1?,6?:1,5]pyrazolo[4,3-b][1,7]naphthyridine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases.

Abstract: The present invention relates to salts and crystalline forms of 2-(3-(8-Amino-6-(trifluoromethyl)imidazo[1,2-a]pyrazin-3-yl)-4-methylphenyl)-3,3,3-trifluoro-2-hydroxypropanamide, crystalline forms of 8-amino-N-(2-hydroxy-2-methylpropyl)-3-(2-methyl-5-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl)imidazo[1,2-a]pyrazine-6-carboxamide, and crystalline forms of 8-amino-N-(2-hydroxy-2-methylpropyl)-3-(2-(methyl-d3)-5-(1,1,1-trifluoro-2-hydroxypropan-2-yl)phenyl)imidazo[1,2-a]pyrazine-6-carboxamide, which are PI3K inhibitors useful in the treatment of cancer and other diseases.

Abstract: The present application discloses compounds having the following formula: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification, as well as methods of making and using the compounds disclosed herein for treating or ameliorating an IL-17 mediated syndrome, disorder and/or disease.

Abstract: The present invention relates to heteroaryl heterocyclic compounds of formula (I), pharmaceutical compositions comprising same, methods for preparing same, and uses thereof, wherein the variables are as defined in the description.

Abstract: This invention is directed to compounds of formula (I): where r, q, R, R2, R3, R4, R5a, R5b, R5c, R6a, R6b, R6c, R7, R8, and R9 are described herein, as single stereoisomers or as mixtures of stereoisomers, or pharmaceutically acceptable salts, solvates, clathrates, polymorphs, ammonium ions, N-oxides or prodrugs thereof; which are leukotriene A4 hydrolase inhibitors and therefore useful in treating inflammatory disorders. Pharmaceutical compositions comprising the compounds of the invention and methods of preparing the compounds of the invention are also disclosed.

Abstract: Provided herein are novel heterocyclic compounds, for example, compounds having Formula I. Also provided herein are methods of preparing the compounds and methods of using the same, for example, in inhibiting TGF-beta mediated signaling and/or for treating cancer.

Abstract: The present document is directed to methods for producing therapeutically active limonoids as well as new limonoid-type compounds.

Abstract: Equipotent indolocarbazole-derived analogs of staurosporine identified herein are prepared through C—H borylation chemistry. Functionality resides at C2 and C10 of the indolocarbazole aromatic region. Introducing functionality in this previously inaccessible region does not abrogate kinase activity and is shown to change the selectivity profile.

Abstract: The invention provides synthetic intermediates and synthetic processes that are useful for preparing the antibacterial agent TXA709:

Abstract: The invention provides a facile process for preparing various Group VI precursor compounds, set forth below as Formula (I), useful in the vapor deposition of certain Group VI metals onto solid substrates, especially microelectronic semiconductor device substrates. Also provided is a process for the preparation of such precursor compounds. Additionally, the invention provides a method for vapor deposition of Group VI metals onto microelectronic device substrates utilizing the precursor compounds of the invention.

Abstract: The invention provides a new process for producing ruthenium complexes represented by the Formula 1. Invention provides also the use of ruthenium complexes represented by the Formula 1 as precatalysts and/or catalysts in olefin metathesis reactions.

Abstract: The application relates to a strongly-polarized molecule of the following general formula: wherein A denotes a group having a polarizability greater than 2 C·m2/V; R1 and R2 are respectively hydrogen, halogen, a hydroxyl group, an amino group, a cyano group, a nitro group, a carboxyl group, a C1-12 alkyl group, a C1-12 alkoxy group, a halogenated C1-12 alkyl group, a halogenated C1-12 alkoxy group, a hydroxyl C1-12 alkyl group, a hydroxyl C1-12 alkoxy group, or a C1-12 alkyl amino group; x1 and x2 denote 0 or an integer no less than 1, respectively; and y1 and y2 denote 0 or an integer no less than 1, respectively. The application further relates to a strongly-polarized molecule-graphene molecule heterojunction, and a single molecule field effect transistor comprising a substrate, a gate, a dielectric layer and the strongly-polarized molecule-graphene molecule heterojunction; and the dielectric layer is located between the gate and the strongly-polarized molecule-graphene molecule heterojunction.

Abstract: A BMOFs nanosheet based on a ZIF/MIL topology, and a preparation method and an application thereof are provided. The preparation method includes dispersing a MOF material of a ZIFs series in an organic phase, then adding an aqueous phase to obtain a mixture; and adding a MOF material of a MILs series into the mixture, sealing, standing for 1-5 days, filtering, performing centrifugal washing, drying, and performing acetone ultrasonic exfoliation to obtain the BMOFs nanosheet based on the ZIF/MIL topology. The preparation method is simple to operate and moderate in conditions, and the prepared ZIF/MIL BMOFs nanosheet has good electrocatalytic activity and stability in an OER.

Abstract: Described herein are certain boron-containing compounds, compositions, preparations and their use as modulators of the transpeptidase function of bacterial penicillin-binding proteins and as antibacterial agents. In some embodiments, the compounds described herein inhibit penicillin-binding proteins. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.

Abstract: Disclosed herein are caged haptens and caged hapten-antibody conjugates useful for enabling the detection of targets located proximally to each other in a sample.

Abstract: Oxazolidinones having structures represented by structural formula I, preparation methods therefor, and pharmaceutical uses thereof, in particular an application of said compounds and salts or compositions thereof in the treatment of a bacterial infection. In the formula: R1 is a methyl group, an ethyl group, a propyl group, a cyclopropyl group, or a vinyl group; R2 is F; and R3 is F, CH3, C2H5, CF3, CHF2, CH2F, or a cyclopropyl group.

Abstract: Provided are novel prodrugs of treprostinil, as well as methods of making and methods of using these prodrugs.

Abstract: The present invention provides a method for preparing RNA by a phosphoramidite solid-phase synthesis using an porous inorganic carrier containing a primary amino group, the method being able to bring about an increased purity even in the synthesis of medium-stranded to long-stranded RNA. In the method for producing RNA, an amount of the primary amino group contained in the porous inorganic carrier satisfies the following formula (1): 0.7?(I×R)/S?1.8 [wherein, I is an amount of the amino group per unit mass of the porous inorganic carrier (?mol/g), as measured by a 2-nitrobenzenesulfonic acid adsorption method; R is a ratio of the primary amino group in the total amino groups contained in the porous inorganic carrier (amount of primary amino group/amount of total amino groups); and S is a specific surface area (m2/g) of the porous inorganic carrier as measured by a nitrogen adsorption method].

Abstract: A crystal of a compound represented by the following formula 5: in which R1 represents a protecting group for a hydroxyl group, and R2 represents a leaving group.

Abstract: Disclosed is a method for synthesizing an O-antigen saccharide chain of Helicobacter pylori serotype O:6 using seven glycosylation building blocks. Inexpensive and easily available D-glucosamine, D-galactose, D-mannose and L-fucose are used as starting materials, and seven glycosylation building blocks are obtained through a series of chemical reactions. The saccharide building blocks are then selectively linked together to produce O-antigen oligosaccharide chains of Helicobacter pylori serotype O:6 with different saccharide configuration through a series of glycosylation reactions. Also disclosed is a method to assemble an amino linker at the reducing end of the O-antigen saccharide chain of Helicobacter pylori serotype O:6, and the synthesized oligosaccharide chain with an amino linker can be coupled to a carrier molecule or immobilized on a matrix.

Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.

Abstract: The present invention provides a compound of Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, which are PRMT5 inhibitors. Also provided are methods of making compounds of Formula I, pharmaceutical compositions comprising compounds of Formula I, and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations.

Abstract: Using nucleotide architectures to very closely and precisely placed chromophores that produce quantum coherent excitons, biexcitons, and triexcitons upon excitement to create excitonic quantum wires, switching, and gates that would then form the basis of quantum computation. Creating the various excitons and controlling the timing of the excitons would be performed using light of the corresponding wavelength and polarization to stimulate the corresponding chromophores.

Abstract: A process for preparing a glycoside compound represented by formula (3), which includes reacting a glycoside compound represented by formula (1) with an ether compound represented by formula (2) in the presence of an oxidizing agent and an acid to prepare a glycoside compound represented by formula (3), where the oxidizing agent is added to a reaction system, followed by adding an acid thereto, where Ba represents a cytosine group which may be optionally substituted with acyl group, or an uracil group, R1 represents a C1 to C6 alkyl group or a phenyl group, and n is 0 or 1, where an oxidizing agent is selected from N-halogenated succinimide and N-halogenated hydantoin, and an acid is selected from perfluoroalkylcarboxylic acid, alkylsulfonic acid, arylsulfonic acid, periluoroalkylsulfonic acid, and salts thereof, and any combinations thereof, which can provide a synthesis of a desired compound with high purity.

Abstract: Compounds, including antiviral prodrugs, and pharmaceutical formulations including the compounds, which may be orally bioavailable or formulated for intramuscular injection. Methods for producing compounds, such as antiviral prodrugs. Methods for treating coronavirus and other RNA virus infection in mammals. Methods of producing a drug triphosphate.

Abstract: The invention provides compositions and methods for suppressing autoimmune components of neurodegenerative diseases and thereby providing therapeutic effects to patients suffering from such diseases. Compositions and methods include immunosuppressive moieties such as regulatory T cells (Tregs) and proteins expressed by Tregs coupled to a chimeric antigen receptor or protein that specifically binds one or more glial cell markers. Therapeutically effective doses of said compounds for treating neurodegenerative diseases including progressive supranuclear palsy (PSP), Parkinson's disease (PD), Alzheimer's, Huntington's disease, amyotrophic lateral sclerosis (ALS), chronic traumatic encephalopathy (CTE), and prion diseases are disclosed.

Abstract: The present disclosure is directed to conjugates of a specific binding entity and an oligomer, i.e. [Specific Binding Entity]-[Oligomer]n, wherein n is an integer ranging from 1 to 12, and where the Oligomer includes, in some embodiments, a PNA sequence having at least one substituent at a gamma carbon position. In some embodiments, the substituent at the gamma carbon position, e.g. an amino acid, a peptide, a miniPEG, or a polymer, includes at least one reporter moiety.

Abstract: Embodiments herein report compositions, methods, uses and manufacturing procedures for rotavirus constructs and immunogenic compositions thereof. Some embodiments concern compositions that include, but are not limited to, chimeric rotaviruses of use in immunogenic compositions against rotavirus infection as well as against other pathogenic virus infection in a subject. In certain embodiments, constructs of use herein can be generated and used where a rotavirus expression system further includes one or more nucleic acid molecules encoding one or more polypeptides of another pathogen (e.g. another enteric or mucosal pathogen).

Abstract: The present invention relates to an immunogenic fusion protein comprising a first amino acid sequence having at least 80% sequence identity with the amino acid sequence of the N-terminal region of a first group B Streptococcus surface protein, which is fused to a second amino acid sequence having at least 80% sequence identity with the amino acid sequence of the N-terminal region of a second group B Streptococcus surface protein. Each of the first and the second group B Streptococcus surface protein is selected from the group consisting of Rib protein, Alp1 protein, Alp2 protein, Alp3 protein, Alp4 protein and AlpC protein. The immunogenic fusion protein further comprises at least one amino acid sequence having at least 80% sequence identity with the amino acid sequence of the N-terminal region of the group B Streptococcus surface protein Alp1, Alp2, Alp3 or Alp4.

Abstract: The present invention provides a miniaturized hemagglutinin complex protein having function inhibitory activity against E-cadherin, wherein (a) all or a part of at least HA1 subcomponent, and/or a part of HA3 subcomponent are/is deleted, (b) regions in HA2 and HA3 subcomponents that contribute to binding with E-cadherin are present, and (c) the HA3 subcomponent is derived from Clostridium botulinum type A or type B, and an E-cadherin function inhibitor containing the hemagglutinin complex protein.

Abstract: Polynucleotides and polypeptides useful in the manufacture of a class of chemical compounds known as alkaloids are provided. The polynucleotides and polypeptides may be used to synthesize alkaloids, including reticuline, thebaine and morphine, in vivo and in vitro. The polynucleotides further may be used to examine the presence of the polynucleotides in a cell or a cell extract, and to modulate expression thereof in living cells.

Abstract: The present invention relates to in vitro expression of proteins and particularly, although not exclusively, to expression of proteins in mammalian cell lines. In particular, the present invention relates to the provision of a novel vector for protein expression, and methods of using such vector in the expression of proteins in mammalian cell lines.

Abstract: In one aspect the present invention is directed to mutant NGAL proteins that have the ability to bind to siderophores, such as enterochelin, and to chelate and transport iron, and that are excreted in the urine. Such NGAL mutants, and complexes thereof with siderophores, can be used to clear excess iron from the body, for example in the treatment of iron overload. The NGAL mutants of the invention also have antibacterial activity and can be used in the treatment of bacterial infections, such as those of the urinary tract.

Abstract: The present invention relates to a cluster of differentiation 98 heavy chain (CD98hc)-specific binding protein, wherein the CD98hc-specific binding protein is a lipocalin 2 (Lcn2)-derived binding protein and binds to CD98hc with a KD of 200 nM or lower.

Abstract: Among the various aspects of the present disclosure is the provision of targeting TPL2 kinase as a novel strategy to block oncogenic KRAS-driven signaling, detection of TPL2 mutations, and uses of TPL2 inhibiting agents alone or in combination with chemotherapy in subjects having TPL2- or RAS-associated cancer.

Abstract: A composition comprising a synthetic growth factor analogue comprising a non-growth factor heparin binding region, a linker and a sequence that binds specifically to a cell surface receptor and an osteoconductive material where the synthetic growth factor analogue is attached to and can be released from the osteoconductive material and is an amplifier/co-activator of osteoinduction.

Abstract: Methods of treating a cancer in a patient are provided. The methods can include obtaining a tumor sample from a patient, detecting whether CCNG1 gene expression is present in the tumor sample, diagnosing the patient with a CCNG1 inhibitor-responsive cancer when the presence of CCNG1 gene expression in the tumor sample is detected, and/or administering an effective amount of a CCNG1 inhibitor to the diagnosed patient. CCNG1 inhibitors can include a viral vector having a binding peptide that is configured to bind one or more signature (SIG) elements of an invading tumor and at least one cytocidal gene. CCNG1 inhibitors including cell penetrating peptides are also provided.

Abstract: The current disclosure relates to methods for treating ovarian cancer based on specific antigen expression of the cancer. Furthermore, the expressed antigen may be used in immunotherapeutic methods for treatment of the ovarian cancer. Aspects of the disclosure relate to immunotherapies targeting CT45 polypeptides, methods for treating ovarian cancer based on CT45 expression, and kits for detecting CT45 polypeptides and nucleotides.

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

Abstract: The present invention relates to compositions comprising an interleukin-12 (IL-12) protein having a first and second subunit, an extra domain B (ED-B)-binding domain, and a linker between the IL-12 protein and the ED-B-binding domain.

Abstract: T cell receptors that specifically recognize hAFP158 and methods of their use are provided.

Abstract: The present invention relates to polypeptide consisting of three TNF homology domains of TNF-ligand family members proteins (THD) that specifically bind to the extracellular part of TNFR2, wherein C-terminal and N-terminal reference points are defined by consensus sequences. The THIDs are linked by short stretches of further C-terminal and/or N-terminal amino acids of the THD or variants thereof as well as by peptide linkers. These peptides have an improved stability. Furthermore the invention relates to polypeptide multimers comprising several of the polypeptides of the present invention.

Abstract: This disclosure provides a collagen fiber-based ink for bioprinting comprising a high solid content of collagen fiber particles that are suitable for manufacturing collagen-based scaffolds and tissue equivalent implants for regenerative medicine applications.

Abstract: Provided herein, inter alia, are compositions and methods for culturing mammalian cells. In certain aspects, the composition is a medium containing one or more of a lithium ion source, one or more fatty acids, and/or ethanol. Use of any of the cell culture media described herein to culture cells that have been genetically engineered to produce one or more recombinant polypeptides (for example, antibodies) can result in increased titers, a more favorable glycosylation profile, and/or modulated (e.g. decreased) amounts of high and low molecular weight species, and/or modulated (e.g. decreased) amounts of acidic or basic charge variants, compared to cells cultured in a medium that does not contain one or more of a lithium ion source, one or more fatty acids, and/or ethanol.

Abstract: This application provides antibodies and functional equivalents thereof which are capable of specifically binding RSV, as well as means and methods for producing them.

Abstract: The invention is directed to bispecific molecules comprising an HIV-1 envelope targeting arm and an arm targeting an effector cell, compositions comprising these bispecific molecule and methods of use. In certain aspects, the bispecific molecules of the present invention can bind to two different targets or epitopes on two different cells within the first epitope is expressed on a different cell type than the second epitope, such that the bispecific molecules can bring the two cells together. In certain aspects, the bispecific molecules of the present invention can bind to two different cells, wherein the bispecific molecules comprises an arm with the binding specificity of A32, 7B2, CH27, CH28 or CH44.

Abstract: Embodiments of the present invention are directed to compositions and methods for anti-HIV (anti-CD4 binding site) broadly neutralizing antibodies having improved potency and breadth for neutralizing a range of HIV strains. Combinations of broadly neutralizing antibodies can also improve potency over a single antibody composition.

Abstract: The invention is in the field of therapy of antibody deficiencies. Inventors demonstrate for the first time in both controls and IgA-deficient patients. systemic anti-microbiota IgG responses correlate with reduced inflammation suggesting that systemic IgG responses contribute to the gut microbiota confinement. Furthermore. SIgAd-associated inflammation is inversely correlated with systemic anti-commensal IgG responses, which may thus serve as a second line of defense. Altogether, these data suggest that systemic IgG and intestinal IgA cooperate in different body compartments to limit systemic pro-inflammatory pathways. As selective IgA deficient patients harbour elevated seric anti-commensal IgG levels. these findings suggest that in selective IgA deficiency, microbiota confinement is obtained at the price of a strong inflammatory response. Accordingly. the invention relates to a composition containing immunoglobulins A (IgA). more particularly secretory IgA.

Abstract: Described herein is a polypeptide comprising an immunoglobulin chain variable domain comprising three complementarity determining regions (CDR1-CDR3) and four framework regions, wherein: (a) at least one lysine residue in CDR1, CDR2 and/or CDR3 has been substituted with at least one histidine residue, and/or (b) at least one arginine residue in CDR1, CDR2 and/or CDR3 has been substituted with at least one histidine residue. The polypeptides of this disclosure possess increased intestinal stability relative to a corresponding polypeptide not having the histidine substitutions.