Abstract: The present invention provides 1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-ones and 1,5-dihydro-4H-pyrazolo[4,3-c]pyridin-4-ones of formula (I) as PDE1 inhibitors and their use as a medicament, in particular for the treatment of neurodegenerative disorders and psychiatric disorders.

Abstract: Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): where R1, X1, and X2 are as described herein.

Abstract: Provided herein are compounds, pharmaceutical compositions comprising the compounds, methods of preparing the compounds, and methods of using the compounds and compositions in treating conditions associated with voltage-gated sodium channel function where the compounds are 11,13-modified saxitoxins according to Formula (I): where R4, R4a, R7, R7a, and X2 are as described herein.

Abstract: The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts thereof. The invention further relates to the use of the compounds of Formula (I) as A2A inhibitors. The invention also relates to the use of the compounds of Formula (I) for the treatment and/or prevention of proliferative disorders, including cancers.

Abstract: Provided are compounds and compositions for prevention and/or elimination of Zika virus infection. Also provided are methods for preventing and treating a subject in need of prevention or treatment of Zika virus.

Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, prodrug or stereoisomer thereof, wherein R1, R2a, R3a, R3b, R4a, R4b, G1, G2, L1, L2, m1, m2, A, B, W, X, Y, Z and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.

Abstract: The present invention relates to a cyano-substituted heteroarylpyrimidinone derivative represented by formula (I), a preparation method therefor and a use thereof as a therapeutic agent, in particular a use as an acetyl-CoA carboxylase (ACC) inhibitor, and the definition of each substituent in formula (I) is the same as the definition in the description.

Abstract: The present invention provides compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, and methods of using the same.

Abstract: Described herein is a compound of Formula (I), and pharmaceutically acceptable salts thereof. Also described herein are compositions and the use of such compositions in methods of treating a variety of diseases and conditions, in particular Krabbe's Disease (KD) and Metachromatic leukodystrophy (MLD).

Abstract: The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same.

Abstract: The present invention provides methods of preparing a MK2 inhibitor, and intermediates related thereto.

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

Abstract: Provided are imaging agents comprising a compound of Formula I, or a pharmaceutically acceptable salt thereof, and methods of their use.

Abstract: Specifically substituted hetero- or carbon-bridged phenylquinazolines of the general formulae (Ia) and (Ib) and a process for their preparation, an electronic device comprising at least one of these compounds, an emitting layer, preferably present in an electronic device, comprising at least one compound of general formulae (Ia) and (Ib) and the use of compounds according to general formulae (Ia) and (Ib) in an electronic device as a host material, a charge transporting material, charge and/or exciton blocking material, preferably as a host material or an electron transporting material.

Abstract: The present disclosure shows a molecular probe SF-1 which is useful for selective detection of hypochlorous acid (HOCl) over other reactive oxygen species (ROS) and a process for the preparation thereof.

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: The present document describes compounds resulting from the complexation of quaternary ammonium compounds with boric acid and/or its derivatives, and methods of making the same, and methods of using the same for the treatment of pathogenic infections.

Abstract: The present invention relates to 1-acyl-lysophosphatidyl derivatives of general formula 1; in which R is C4 to C30 aliphatic hydrocarbyl chain, R1 is selected from H or C1 to C10 alkyl, preferably C1 to C6 alkyl, R2 is selected from H, C10 to C30 acyl or C1 to C10 alkyl, preferably C1 to C6 alkyl, and R3, when present, is selected from H or C1 to C10 alkyl, preferably C1 to C6 alkyl. These derivatives are intended for the treatment of cancer, in particular melanoma, hepatocarcinoma or GIT carcinomas.

Abstract: Compounds of the general formula (I): or a pharmaceutically acceptable salt thereof, processes for the preparation of these compounds, compositions containing these compounds, and the uses of these compounds.

Abstract: Embodiments of the present invention are directed to processes for purifying ligands such as organopolyphosphite ligands. In one embodiment, a process comprises: (a) receiving a solid organopolyphosphite compound that has been recrystallized or triturated at least once, wherein the solid organopolyphosphite compound comprises greater than one weight percent of an oxidized phosphite impurity and wherein the organopolyphosphite compound is substantially free of solvent; (b) slurrying the solid organopolyphosphite compound in a C2 or higher alcohol at a temperature of at least 60° C. for at least 20 minutes to reduce the oxidized phosphite impurity in the solid phase; and (c) removing liquid comprising dissolved oxidized phosphite impurity from the slurry, wherein the residual oxidized phosphite impurity content of the organopolyphosphite compound following step (c) is 1 weight percent or less.

Abstract: The present invention provides a novel cationic ruthenium complex which is easy to produce and handle and can be procured at a relatively low cost and a production method for the ruthenium complex, a method for producing an alcohol or the like using the ruthenium complex as a catalyst, a method for producing a carbonyl compound using the ruthenium complex as a catalyst, and a method for producing a N-alkylamine compound using the ruthenium complex as a catalyst. The present invention pertains to a ruthenium complex represented by general formula (1): [RuX(CO)2(PNP)]Y (wherein, X represents a monovalent anionic monodentate ligand, Y represents a counter anion, PNP represents a tridentate ligand, and CO represents carbon monoxide), a production method for the ruthenium complex, a catalyst containing the ruthenium complex, and a production method for various organic compounds using the catalyst.

Abstract: The present invention relates to low temperature process for preparing nanoparticles of porous crystalline Fe-, Al- or Ti-based MOF carboxylate materials with low polydispersity index, and uses thereof, particularly as catalyst support for carrying out heterogeneously catalyzed chemical reactions, or as gas storage/separation/purification material, or as matrix for encapsulating active principles (medicine, cosmetics).

Abstract: The present invention relates to a process for the selective isolation of highly purified, crystalline D-mannose from complex sugar mixtures, in particular from mixed wood sugars, more particularly from spent sulfite liquor (SSL). The process of the present invention is based on converting mannose into essentially pure mannose bisulfite adducts. Subsequent oxidative recovery of mannose from the mannose bisulfite adducts renders crystalline mannose in improved yields and purities.

Abstract: The present invention relates to sulphated disaccharides of formula (I) for use in the treatment of neuropathic pain. The present invention also relates to a pharmaceutical composition comprising the compound of formula (I) and at least one pharmaceutically acceptable excipient for use in the treatment of neuropathic pain. The compounds of formula (I) were effective in several experimental models of neuropathic pain for which reason these compounds can be used effectively for the treatment of different types of neuropathic pain and the clinical manifestations thereof, for example, mechanical allodynia or cold allodynia.

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 invention relates to a newly developed resorcinarene-based amphipathic compound, a method for producing the same, and a method for extracting, solubilizing, stabilizing, crystallizing, or analyzing a membrane protein by using the same. In addition, compared to a conventional compound, the compound can efficiently extract, from a cell membrane, membrane proteins having a greater variety of structures and characteristics, and can stably store such membrane proteins for a long time in an aqueous solution. Therefore, the compound can be used to analyze the functions and structures of such membrane proteins. Analysis of the structures and functions of membrane proteins, being closely related to the development of new drugs, is one of the fields of greatest interest in biology and chemistry today.

Abstract: Cyclic-GMP-AMP synthase (cGAS) and cyclic-GMP-AMP (cGAMP), including 2?3-cGAMP, 2?2-cGAMP, 3?2?-cGAMP and 3?3?-GAMP, are used in pharmaceutical formulations (including vaccine adjuvants), drug screens, therapies, and diagnostics.

Abstract: The present invention provides an oligomer which efficiently enables to cause skipping of the 53rd exon in the human dystrophin gene. Also provided is a pharmaceutical composition which causes skipping of the 53rd exon in the human dystrophin gene with a high efficiency.

Abstract: Chemical entities that are novel compounds, pharmaceutical compositions and methods of treatment of cancer are described.

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

Abstract: Methods of enhancing efficiency of downstream chromatography steps for purification of proteins comprising: (a) passing a composition comprising a polypeptide of interest and various contaminants through an ion exchange membrane, wherein the polypeptide and the membrane have opposite charge, at operating conditions comprised of a buffer having a pH sufficiently distinct from the pi of the polypeptide to enhance the charge of the polypeptide and a low ionic strength effective to prevent the shielding of charges by buffer ions, which cause the membrane to bind the polypeptide and at least one contaminant, (b) overloading the ion exchange membrane such that at least one contaminant remains bound to the membrane while the polypeptide of interest is primarily in the effluent; (c) collecting the effluent from the ion exchange membrane comprising the polypeptide of interest; (d) subjecting the membrane effluent comprising the polypeptide of interest to a purification step of similar charge as the previous membrane,

Abstract: Disclosed herein are compositions, methods, and systems for the purification and/or detection of recombinant and other proteins. In some embodiments, compositions may comprise recombinant protein with one or more sequences having substantial homology to RP-Tag Small or RP-Tag Large. In some cases, the disclosed compositions may be useful in binding or recognizing target proteins.

Abstract: In one aspect, this disclosure features compounds of formula (I) or a pharmaceutically acceptable salt thereof: AA1-Arg-Val-AA4-AA5-His-Pro-AA8-OH ??(I), in which AA1, AA4, AA5, and AA8 are defined in the specification. The compounds of formula (I) can be used to treat hypertension (e.g., hypertension induced by pregnancy), preeclampsia, or a renal disease induced by pregnancy.

Abstract: The present invention is directed to EGFR-specific and ErbB2-specific peptide reagents, methods for detecting pre-cancer, early cancer and/or cancer using the peptide reagents alone or in a multiplex format, and methods for targeting pre-cancer cells, early cancer cells and/or cancer cells using the peptide reagents.

Abstract: The present disclosure relates to a peptide that regulates fat metabolism and uses thereof in the preparation of a medicament for the treatment of diseases associated with abnormalities in energy metabolism, particularly fat metabolism. The peptide of the present disclosure can reduce fat absorption, reduce fat accumulation in the liver and regulate fat metabolism, and has an advantage of being orally administered as compared with other general peptide products, and thus can also be used as an active ingredient of a health care product for regulating fat metabolism.

Abstract: The present invention provides novel peptidomimetic macrocycles and methods of using such macrocycles for the treatment of disease.

Abstract: The present invention relates to novel adenovirus strains with an improved seroprevalence. In one aspect, the present invention relates to isolated polypeptides of adenoviral capsid proteins such as hexon, penton and fiber protein and fragments thereof and polynucleotides encoding the same. Also provided is a vector comprising the isolated polynucleotide according to the invention and adenoviruses comprising the isolated polynucleotides or polypeptides according to the invention and a pharmaceutical composition comprising said vector, adenovirus, polypeptide and/or polynucleotide. The invention also relates to the use of the isolated polynucleotides, the isolated polypeptides, the vector, the adenoviruses and/or the pharmaceutical composition for the therapy or prophylaxis of a disease.

Abstract: Disclosed is human endogenous retroviral protein. This human endogenous retroviral protein is herein generally referred to as HEMO. The application relates more particularly to shed forms of the HEMO protein, more particularly to those shed forms, which are released in the circulating blood. The application also relates to products deriving from the shed forms of HEMO, such as antibodies, nucleic acid vectors and engineered cells, as well as to the medical or biotechnological applications of these shed forms or derived products, notably in the fields of placental development, fetus protection, cancer treatment and stem cell production.

Abstract: Human cytomegalovirus vectors comprising heterologous antigens are disclosed. The vectors derived from the TR strain, are ganciclovir-sensitive, include active US2, US3, US6, US7 and UL131A genes, and have a deleterious or inactivating mutation in the UL82 gene preventing the expression of pp71.

Abstract: The present invention provides for a fusion protein comprising (1) a bacterial microcompartment (BMC) shell protein comprising one or more subunit, and (2) a first component of a specific-binding pair, operably linked to the BMC shell protein such that the first component faces (i) a lumen (inside) side, or (ii) outside of a BMC shell formed incorporating the fusion protein and the fusion protein does not disrupt or prevent the folding of the BMC shell protein or the ability of the BMC shell protein to integrate with other BMC shell proteins into a BMC shell; wherein the first component is capable of forming a stable or irreversible interaction with a second component of the specific-binding pair.

Abstract: The invention may include engineered antimicrobial peptides to treat HLB disease, preferably in citrus plants. Specifically, the invention may include novel antimicrobial peptide derived from amphipathic helical peptides that may further be used to treat HLB disease in citrus plants. In one embodiment, the invention may include an engineered antimicrobial peptide formed by coupling two amphipathic helical peptides. Specifically, a generalized antimicrobial peptide of the invitation may include a first amphipathic helical peptide coupled with a second amphipathic helical peptide by a linker domain forming a helix-turn-helix scaffold formation. Such amphipathic helical peptides may be endogenous to a target host, preferably a citrus plant.

Abstract: The present disclosure provides a polypeptide and method for treating and/or preventing nephrotic syndrome, such as but not limited to those associated with minimal change disease and membranous nephropathy, and conditions related to nephrotic syndrome, such as but not limited to, proteinuria and edema, as well as diabetic nephropathy, diabetes mellitus, lupus nephritis or primary glomerular disease. The present disclosure further provides methods for reducing proteinuria and other disease states as discussed herein. Such methods comprise the therapeutic delivery of an Angptl4 polypeptide or Angptl4 polypeptide derivative to a subject.

Abstract: Certain embodiments are directed to NEIL2 compositions and method of using NEIL2 composition to treat subjects in need of such treatment.

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 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 invention relates to a viral expression construct and related viral vector and nucleic acid molecule and composition and to their use wherein said construct and vector are suitable for expression in a mammal and comprise a nucleotide sequence encoding a Fibroblast growth factor 21 (FGF21) to be expressed in liver, adipose tissue and/or skeletal muscle.

Abstract: The present invention relates to a tumor necrosis factor receptor (TNFR) binding protein complex comprising 12 or more protein ligands (PLs) that specifically bind to the extracellular part of the same TNFR. Preferably, the TNFR binding protein complex binds to the extracellular part of TNFR2. Preferably, the TNFR binding protein complex of the present invention further comprises two or more polymerization domains (PD).

Abstract: The present disclosure relates to polynucleotides encoding tethered interleukin-12 (IL-12) polypeptides comprising an IL-12 polypeptide and a membrane domain. The present disclosure also relates to vectors comprising the polynucleotides; host cells comprising the polynucleotides or vectors, polypeptides encoded by the polynucleotides; compositions comprising the polynucleotides, vectors, host cells, or polypeptides and a delivery agent; and uses thereof, including treatment of cancer.

Abstract: The present invention provides a fusion polypeptide comprising a first domain and a second domain, wherein the first domain comprises a polypeptide ligand which binds to a cell surface-associated antigen and the second domain comprises aglycosylated interferon ? 2b (IFN?2b) having a sequence of SEQ ID NO: 1 or SEQ ID NO: 2. The aglycosylated IFN?2b further comprises one or more amino acid substitutions or deletions which attenuate the activity of the aglycosylated IFN?2b.

Abstract: Imaging agents that can bind to ghrelin O-acyltransferase (GOAT) without binding to the ghrelin receptor (GHS-R1a). The imaging agents comprise a base structure for selective binding to GOAT that is coupled via an amino acid linker to a chemical group to enable imaging such as a fluorescent label, radioactive tracer, or metal chelator. For example, the imaging agent may comprise a ghrelin substrate mimetic inhibitor incorporating an unmodified 2,3-diaminopropanoic acid (Dap) group at the site analogous to serine 3. These agents enable specific detection and imaging of GOAT versus the GHS-R1a receptor in a variety of biological contexts.