Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted pyrrolopyridine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like.

Abstract: The present invention provides for compounds of formula (I) wherein R1, R2, R3, R4, R5, and R6 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).

Abstract: The present invention relates to chemical compounds of general formula (I): which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.

Abstract: The present invention relates to chemical compounds of general formula (I) which may possess useful therapeutic activity in a range of central nervous system disorders, and in particular, anxiety disorders.

Abstract: The present invention is related to novel compounds of formula (I) that inhibit the activity of the FabI enzyme which are therefore useful in the treatment of bacterial infections. It further relates to pharmaceutical compositions comprising these compounds, and chemical processes for preparing these compounds.

Abstract: Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy.

Abstract: The present invention relates to a heteroaryl derivative or a pharmaceutically acceptable salt thereof, a preparation method therefor, and a pharmaceutical composition for preventing or treating diseases associated with PI3 kinases, containing the same as an active ingredient. The heteroaryl derivative according to the present invention has an excellent effect of selectively inhibiting PI3 kinases, thereby being useful in preventing or treating PI3 kinase diseases such as: cancers, autoimmune diseases, and respiratory diseases.

Abstract: The invention provides novel compounds and methods of using such compounds to treat or prevent cancer.

Abstract: The invention concerns novel substituted pyrazolo- and triazolo-pyrimidine compounds of formula (I) having antiviral activity, in particular, having an inhibitory activity on the replication of the respiratory syncytial virus (RSV). The invention further concerns pharmaceutical compositions comprising these compounds and the compounds for use in the treatment of respiratory syncytial virus infection.

Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, L1 and G1 are as defined in the specification, are useful in treating conditions or disorders prevented by or ameliorated by positive allosteric modulation of the ?-aminobutyric acid B (GABA-B) receptor. Methods for making the compounds are described. Also described are pharmaceutical compositions of compounds of formula (I), and methods for using such compounds and compositions.

Abstract: The present disclosure provides compositions and methods of use to inhibit the interaction of menin with MLL1, MLL2 and MLL-fusion oncoproteins. The compositions and methods of use are useful for the treatment of leukemia, solid cancers, diabetes and other diseases dependent on activity of MLL1, MLL2, MLL fusion proteins, and/or menin.

Abstract: Substituted bicyclic heteroaryls and compositions containing them, for the treatment of general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, including but not restricted to autoimmune diseases such as systemic lupus erythematosis (SLE), myestenia gravis, rheumatoid arthritis, acute disseminated encephalomyelitis, idiopathic thrombocytopenic purpura, multiples sclerosis, Sjoegren's syndrome and autoimmune hemolytic anemia, allergic conditions including all forms of hypersensitivity, The present invention also enables methods for treating cancers that are mediated, dependent on or associated with p110? activity, including but not restricted to leukemias, such as Acute Myeloid leukaemia (AML) Myelo-dysplastic syndrome (MDS) myelo-proliferative diseases (MPD) Chronic Myeloid Leukemia (CML) T-cell Acute Lympho

Abstract: Disclosed herein, inter alia, compounds and methods of use thereof for the modulation of bile acid receptor activity.

Abstract: The present invention provides an organic electroluminescent compound and an organic electroluminescent device using the organic electroluminescent compound, the compound has the following structural formula: wherein R1, R2 and R4 are, each independently, selected from a group consisting of a hydrogen atom, a C1-C20 linear or branched alkyl group, a substituted or unsubstituted N-(phenylmethyl)imino group, a phenyl group, phenylamine, diphenylamine, phenyl pyridinylamine, bipyridinylamine, phenyl naphthylamine, binaphthylamine, phenyl phenanthrylamine, biphenanthrylamine, phenyl anthrylamine, bianthrylamine, phenanthridine, biphenyl, a pyridyl group, a pyrimidinyl group, a quinolinyl group and a triazinyl group; R3 is selected from a group consisting of hydrogen atom, a C1-C10 linear or branched alkyl group, a substituted or unsubstituted N-(phenylmethyl)imino group, a phenyl group, phenylamine, diphenylamine, phenyl pyridinylamine, bipyridinylamine, phenyl naphthylamine, binaphthylamine, phenyl phenanthr

Abstract: The present invention relates to a novel chemical compound for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.

Abstract: Bicyclic and tricyclic pyrimidine tyrosine kinase inhibitors with antitubulin activity are provided in the present invention. The compositions of the present invention possess dual activity in a single agent of potent vascular endothelial growth factor receptor inhibitory activity as well as antitubulin activity. Water soluble salts of these compositions are also described. Methods of treating a patient having cancer, macular degeneration, and arthritis with the compositions and salts thereof of the present invention are disclosed.

Abstract: A process for producing high-purity gadobutrol in a purity (according to HPLC) of more than 99.7 or 99.8 or 99.9% and the use for preparing a pharmaceutical formulation for parenteral administration is described. The process is carried out using specifically controlled crystallization conditions.

Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.

Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.

Abstract: The present invention includes 4-(hydroxymethyl)phenylboronic esters, which react with hydrogen peroxide to form 4-hydroxybenzyl alcohol, which is an anti-inflammatory and/or anti-oxidant compound, as well as microparticles and compositions thereof. In certain embodiments, the compositions of the invention may be used to treat or prevent oxidative stress and/or inflammation, including ischemic disease.

Abstract: Described herein are compositions and methods for forming silicon oxide films. In one aspect, the film is deposited from at least one precursor, wherein the at least one precursor has a structure represented by Formula A: wherein R, R1, R2, R3, R4, and R5 are defined herein.

Abstract: A method for producing an organohalosilanes comprising reacting an organic compound comprising a halogen-substituted or unsubstituted alkane, a halogen-substituted or unsubstituted alkene, or an aromatic compound and at least one hydridohalosilane of formula RnSiHmX4-m-n, wherein each R is independently C-1-C-1 4 hydrocarbyl or C-1-C-1 4 hologen-substituted hydrocarbyl, X is fluoro, chloro, bromo, or iodo, n is 0, 1, or 2, m is 1, 2 or 3, and m+n=1, 2 or 3, in the presence of a heterogeneous catalyst comprising an oxide of one or more of the elements Sc, Y, Ti, Zr, Hf, B, Al, Ga, In, C, Si, Ge, Sn, or Pb, at a temperature greater than 100° C., and at a pressure of at least 690 kPa, to produce a crude reaction product comprising the organohalosilane.

Abstract: An aspect of the present disclosure is a method that includes combining a first organic salt (A1X1), a first metal salt) a second organic salt (A2X3), a second metal salt (M2Cl2), and a solvent to form a primary solution, where A1X1 and M1(X2)2 are present in the primary solution at a first ratio between about 0.5 to 1.0 and about 1.5 to 1.0, and A2X3 to M2Cl2 are present in the primary solution at a second ratio between about 2.0 to 1.0 and about 4.0 to 1.0. In some embodiments of the present disclosure, at least one of A1 or A2 may include at least one of an alkyl ammonium, an alkyl diamine, cesium, and/or rubidium.

Abstract: Flow batteries incorporating an active material with one or more catecholate ligands can have a number of desirable operating features. Commercial syntheses of catechol produce significant quantities of hydroquinone as a byproduct, which presently has limited value in the battery industry and can represent a significant waste disposal issue at industrial production scales. Using a concerted, high-yield process, low-value hydroquinone can be transformed into high-value 1,2,4-trihydroxybenzene, which can be a desirable ligand for active materials of relevance in the flow battery industry.

Abstract: The present invention relates to novel hardeners for curing epoxy resins and to cure accelerants for the accelerated curing of epoxy resins comprising, in each case, at least one compound from the group of esters of phosphorus-containing acids according to Formula (I), wherein there applies to Formula (I): wherein there applies to the radicals R1, R2, R3, R6, X and indices m, n, p, simultaneously or independently of one another: R1, R2=simultaneously or independently of one another, hydrogen or alkyl, R3=alkyl, aryl, —O-alkyl, —O-aryl, —O-alkylaryl or —O-arylalkyl, R6=hydrogen, alkyl or —NHC(O)NR1R2, X=oxygen or sulphur, m=1, 2 or 3, n=0, 1 or 2, wherein there applies: m+n=3 p=0, 1 or 2.

Abstract: The invention relates to drug development and synthetic chemistry, in particular to the manufacture of biologically active compounds based on naturally occurring molecules. It also relates to novel biologically active compounds, for example aminoglycoside antibiotics, in a substantially pure regioisomeric form. More particularly, the present invention relates to methods for the chemo- or regioselective derivatization of a target compound with multiple reactive groups, some of which may be derivatezed, and other which will not be derivatized.

Abstract: The inventors demonstrate that treatment of young, suckling mice with a glycolipid derived from Helicobacter pylori activates NKT cells in a CD1d-restricted fashion, and is protective against AHR in a model of allergen-induced asthma. The inventors further found that this protective effect can be transferred by NKT cells exposed to the glycolipid, and is associated with the expansion of a suppressive double-negative NKT cells and Foxp3+ TReg cells. The inventors also demonstrate herein that pretreatment of adult mice with a glycolipid derived from Helicobacter pylori partially suppresses airway hyperreactivity and inhibits BAL inflammation in an ozone-exposure model. Accordingly, provided herein are compositions and methods for the treatment and prevention of inflammatory diseases, such as asthma or autoimmune diseases, in a subject in need thereof.

Abstract: (1aS,1bS,2S,4S,5aR,6S,6aS)-1a-(hydroxymethyl)-4-methoxy-2-(((2S,3R,5S5,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)tetrahydro-2H-pyran-2-yl)oxy)octahydrooxireno[2?,3?:4,5]cyclopenta[1,2-c]pyran-6-yl 4-hydroxybenzoate}, the isomer thereof, the pharmaceutically acceptable salt or solvates thereof, a composition comprising the same as an active ingredient for treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease (COPD) and the use thereof.

Abstract: The invention provides compounds of the formula: wherein B is a nucleobase selected from the groups (a) to (d): and the other variables are as defined in the claims, which are of use in the treatment or prophylaxis of hepatitis C virus infection, and related aspects.

Abstract: The present disclosure provides cytidine derivative dimers, salts and compositions of the cytidine derivative dimers, and methods of making and using the cytidine derivative dimers that are useful for treating a neoplasm in mammalian subjects. A cytidine derivative dimer may have the following general formula (I): By molecularly designing such cytidine-based compounds, the disclosed cytidine-based derivative dimers/salts show significant inhibiting effects on HCT-116 human colon cancer cells, and exhibit strong growth inhibiting effects on HCT-116 human colon cancer xenografts grown in nude mice. The disclosed cytidine derivative dimers/salts provide high anti-tumor activity with low toxicity and are useful for treating cancers.

Abstract: What is described is a trinucleotide cap analog comprising m7G(5?)p3-N1pN2 for increased efficiency of in vitro transcription of m7G(5?)p3-RNA, wherein m7G is N7-methylguanosine or analog, (5?)p3 is a 5?,5?-triphosphate bridge, and N1 or N2 or both ribonucleotide analogs linked to each other by a phosphate, p, and wherein the trinucleotide cap analog increases the efficiency of in vitro transcription.

Abstract: The present invention relates to novel pro-drugs of L-2?-deoxythreose nucleoside phosphonates, such as phosphoramidate, phosphorodiamidate and phospho-diester pro-drugs. The invention also relates to a process for preparing these novel prodrugs of nucleoside phosphonates. The invention also relates to the use of these novel phosphonate-modified nucleosides to treat or prevent viral infections and their use to manufacture a medicine to treat or prevent viral infections, particularly infections with viruses belonging to the HBV family.

Abstract: Some embodiments of the invention involve methods for introduction of various functional groups onto polypeptides, peptides and proteins by alkylation of thioether (a.k.a. sulfide) groups by ring opening reactions, creating new compositions of matter that may be useful for medical therapeutic or diagnostic applications. The thioether groups may either be present in the polypeptides, or may be added to polypeptides by chemical modification, such as by alkylation of thiol (sulfhydryl) groups.

Abstract: In certain embodiments, the invention provides a method of purifying a protein of interest from a mixture by using a dextran polymer.

Abstract: In certain embodiments, the invention provides a method of purifying a protein of interest from a mixture which comprises the protein of interest and one or more contaminants, comprising: (a) contacting the mixture with a dextran polymer under conditions suitable for the dextran polymer to bind to one or more contaminants, thereby to form a contaminant precipitate; (b) separating the contaminant precipitate from the mixture to form a solution, thereby purifying the protein of interest.

Abstract: The present invention provides a cell penetrating peptide dimer by oxidative modification, in which each monomer is connected with each other by the disulfide linkage. The drugability of the peptide dimer has been improved through enhancing stability, reducing proteolysis, retaining permeability and increasing heparan sulfate binding specificity. The modified peptide products can be used to deliver drug molecules as a suitable drug carrier for targeted therapy.

Abstract: The present invention is directed to compounds according to formula, (R2R3)-A1-c(A2-A3-A4-A5-A6-A7-A8-A9)-A10-R1, and pharmaceutically-acceptable salts thereof that act as ligands for one or more of the melanocortin receptors, to methods of using such compounds to treat mammals and to pharmaceutical compositions comprising said compounds.

Abstract: The present invention relates to a compound of the Formula (I)): or pharmaceutically acceptable salt thereof, wherein the symbols are as defined in the specification; a pharmaceutical composition comprising the same, a method for treating or preventing viral infections, inflammation, dry eye, central nervous disorders, cardiovascular diseases, cancer, obesity, diabetes, muscular dystrophy, and hair loss.

Abstract: The present invention provides AAV capsid proteins comprising modification of one or a combination of the surface-exposed lysine, serine, threonine and/or tyrosine residues in the VP3 region. Also provided are rAAV virions comprising the AAV capsid proteins of the present invention, as well as nucleic acid molecules and rAAV vectors encoding the AAV capsid proteins of the present invention. Advantageously, the rAAV vectors and virions of the present invention have improved efficiency in transduction of a variety of cells, tissues and organs of interest, when compared to wild-type rAAV vectors and virions.

Abstract: Provided is an affinity chromatography carrier that maintains high immunoglobulin-binding capacity and high alkali resistance. An immunoglobulin-binding protein including at least one modified immunoglobulin-binding domain, the modified immunoglobulin-binding domain being a polypeptide consisting of an amino acid sequence of an immunoglobulin-binding domain selected from the group consisting of the B domain, Z domain, C domain, and variants thereof of Staphylococcus aureus protein A, in which at least one amino acid residue is inserted between positions corresponding to the 3-position and position 4 of the amino acid sequence of the B domain, Z domain or C domain.

Abstract: The present invention also relates to pharmaceutical compositions useful for treating or preventing a disorder responsive to the blockade of sodium ion channels, especially Nav1.7 sodium ion channels. The present invention further provides methods of treating a disorder responsive to the blockade of sodium channels, and particularly Nav1.7 sodium channels, in a mammal suffering from excess activity of said channels, compositions and methods for providing analgesia by administering a peptide of the invention.

Abstract: A recombinant Flagrp170 protein and pharmaceutical compositions comprising a Flagrp170 protein and related molecules encoding same, and cells presenting such a protein are provided. The Flagrp170 protein comprises an NF-?B-activating domain of Flagellin and an ATP-binding domain truncated Grp170. The pharmaceutical compositions of the invention can be used for the treatment or prevention of cancer or infectious disease.

Abstract: An object of the invention is to provide an agent for preventing or treating corneal disorders, such as corneal epithelial disorder, dry eye, and reduction in corneal sensitivity. This object is achieved by using angiopoietin-like protein 7 as an active ingredient.

Abstract: The present invention provides methods for using endogenous transcriptional control systems to regulate the expression of heterologous protein(s). In particular, targeted genome editing is used to integrate a sequence encoding the heterologous protein(s) in-frame with an endogenous coding sequence such that the expression of the heterologous and endogenous sequences is regulated by the endogenous control system.

Abstract: The present invention relates to methods for treating and/or preventing tumors and/or promoting apoptosis in a neoplastic cell comprising contacting the neoplastic cell with an cell-penetrating dominant-negative ATF5 (“CP-d/n-ATF5”), wherein the CP-d/n-ATF5 is capable of inhibiting ATF5 function and/or activity.

Abstract: Disclosed is a protein comprising no more than three human autoantigenic proteins, wherein a first human autoantigenic protein comprises a truncated myelin oligodendrocyte glycoprotein (MOG) amino acid sequence, a second human autoantigenic protein comprises a myelin basic protein (MBP) amino acid sequence, and a third human autoantigenic protein comprises a truncated proteolipid protein (PLP) amino acid sequence. Also disclosed are related nucleic acids, pharmaceutical compositions, methods of treating a demyelinating disease, and methods of producing the proteins.

Abstract: The present invention provides a peptide containing 8 or more consecutive amino acid residues in an amino acid sequence of any of SEQ ID NOS: 1 to 11 and consisting of 11 or less amino acid residues.

Abstract: Provided herein are methods for the treatment of type I diabetes, Type II diabetes, metabolic syndrome, or obesity, or of appetite suppression, or for mitigating insulin resistance, or for reducing an undesirably high fasting serum glucose level, or for reducing an undesirably high peak serum glucose level, or for reducing an undesirably high peak serum insulin level, or for reducing an undesirably large response to a glucose tolerance test in synergistic combination with metformin. A peptide selected from sequences SEQ ID NO: 12, SEQ ID NO: 15 and SEQ ID NO: 17 are administered.

Abstract: Provided herein are glucagon analogs which exhibit potent activity at the GIP receptor, and, as such are contemplated for use in treating diabetes and obesity. In exemplary embodiments, the glucagon analog of the present disclosures exhibit an EC50 at the GIP receptor which is within the nanomolar or picomolar range.

Abstract: The method for preparation of a recombinant protein from a precursor, preferably mammalian insulins, including human insulins and their analogues, characterised in that a protease is used which hydrolyses one or more peptide bonds in this protein, wherein the protease disrupts the peptide bond from the C-end side of a basic amino acid, when the amino acid is the second one after other basic or neutral amino acid, and such an order enables specific recognition of both amino acids by the protease. The invention is applicable in biotechnology and pharmaceutical industry.