16th week of 2018 patent applcation highlights part 20 |
Patent application number | Title | Published |
20180105487 | PROCESS FOR THE PREPARATION OF LOMITAPIDE - The present invention relates to a process for preparing Lomitapide or its pharmaceutically acceptable salt thereof having high purity with acceptable levels of impurities. | 2018-04-19 |
20180105488 | CYANATE ESTER COMPOUND, CURABLE RESIN COMPOSITION CONTAINING THE COMPOUND, AND HARDENED PRODUCT THEREOF - The present invention provides a novel cyanate ester compound which has excellent solvent solubility and from which a hardened product having a low coefficiency of thermal expansion and excellent flame retardancy and heat resistance is obtained. The present invention is a cyanate ester compound obtained by cyanating a naphthol-dihydroxynaphthalene aralkyl resin or a dihydroxynaphthalene aralkyl resin. | 2018-04-19 |
20180105489 | Separation Method and Method for Producing Isocyanate - Disclosed is a method for separating, with a multi-stage distillation column, a mixture containing an active hydrogen-containing compound (A) and a compound (B) that reversibly reacts with the active hydrogen containing compound (A), the method comprising distillation-separating the active hydrogen-containing compound (A) and the compound (B) with the multi-stage distillation column in the presence of an intermediate-boiling-point inactive compound (C) that has a normal boiling point between a normal boiling point of the active hydrogen-containing compound (A) and a normal boiling point of the compound (B) and is chemically inactive for both of the (A) and the compound (B). | 2018-04-19 |
20180105490 | PROCESSES FOR THE PREPARATION OF UNSATURATED MALONATES - Disclosed is a process for preparing unsaturated malonates and/or their isomers. The process includes the step of reacting an aldehyde and a dialkyl malonate in the presence of a Lewis acid and a carboxylic acid thereby forming an unsaturated malonate. | 2018-04-19 |
20180105491 | PHARMACEUTICAL COMPOUNDS - This invention relates to compounds that are agonists of the muscarinic M | 2018-04-19 |
20180105492 | COMPOUNDS DERIVED FROM 3-ALKYLAMINE-1H-INDOLYL ACRYLATE AND THEIR USE IN THE TREATMENT OF NEURODEGENERATIVE DISEASES - The invention relates to the methods for producing derivatives of 3-alkylamino-1H-indole acrylate (I) with transcription factor Nrf2-inducing activity, free radical scavenging activity and neuroprotective ability. The invention also relates to the use of the derivatives according to the invention for the treatment of diseases, the pathogenesis of which involves oxidative stress, or diseases involving the deregulation of the activity of phase II genes activated by the factor Nrf2, such as Alzheimer's disease, Parkinson's disease, Huntington's disease, multiple sclerosis, ictus or amyotrophic lateral sclerosis. | 2018-04-19 |
20180105493 | CATIONIC LIPID - The present invention provides a cationic lipid which can be used for nucleic acid delivery to a cytoplasm and which is possible to solve the problem of physical stability of a lipid complex. This cationic lipid is a compound represented by the general formula (3) or a pharmaceutically acceptable salt thereof: | 2018-04-19 |
20180105494 | N1-CYCLIC AMINE-N5-SUBSTITUTED BIGUANIDE DERIVATIVES, METHODS OF PREPARING THE SAME AND PHARMACEUTICAL COMPOSITION COMPRISING THE SAME - The present invention provides an N1-cyclic amine-N5-substituted biguanide derivative compound represented by Formula 1, a method of preparing the same and a pharmaceutical composition including the biguanide derivative or the pharmaceutically acceptable salt thereof as an active ingredient. The biguanide derivatives have an effect of inhibiting cancer cell proliferation, cancer metastasis and cancer recurrence by activation of AMPK, even when administered in a small dose compared with conventional drugs. | 2018-04-19 |
20180105495 | AZO-QUATERNARY PYRIDINIUM SALTS WITH ACID-ENHANCED ANTIBACTERIAL EFFICACY, METHODS OF USE, METHODS OF SYNTHESIS, AND USES THEREOF - A new azo-type quaternary pyridinium salt (Azo-QPS) shows enhanced activity at acidic conditions (e.g., pH=5); in neutral or basic conditions, this new Azo-QPS shows a much lower level (2-50 times less) anti-bacterial activity. The use of such a “stimulus-enhance” antibiotic can response to the proliferation of bacteria directly. It helps reduce or prevent the build-up of potent antibacterial agents in the oral environment. The antibacterial properties of Azo-QPS are “activated” when the environmental pH becomes acidic; this acidic pH may be indicative of the accumulation of | 2018-04-19 |
20180105496 | PYRAZOLE COMPOUNDS AND THEIR USE AS T-TYPE CALCIUM CHANNEL BLOCKERS - The invention relates to compounds of formula (I) | 2018-04-19 |
20180105497 | ARGININE METHYLTRANSFERASE INHIBITORS AND USES THEREOF - Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described. | 2018-04-19 |
20180105498 | COMPOSITIONS AND METHODS FOR TREATING METABOLIC DISORDERS - Methods and compounds useful for reducing, treating, preventing, or sustaining the reduction of a metabolic disease or disorder are provided herein. Also provided herein are compositions and kits for practicing any of the methods described herein. | 2018-04-19 |
20180105499 | PROCESS FOR PREPARING ALKYL ESTERS OF 4-(5-(BIS(2-HYDROXYETHYL)AMINO-1-METHYL-1H-BENZO[D]IMIDAZOL-2-YL)BUTYRIC ACID - An alkyl ester of 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid, such as ethyl 4-(5-(bis(2-hydroxyethyl)amino)-1-methyl-1H-benzo[d]imidazol-2-yl)butanoate, is obtained by reacting an alkyl ester of 4-(5-amino-1-methyl-1H-benzo[d]imidazol-2-yl)butyric acid with 2-hydroxyacetaldehyde under reducing conditions. | 2018-04-19 |
20180105500 | NOVEL INHIBITORS OF TRANSFORMING GROWTH FACTOR KINASE AND METHODS OF USE THEREOF - The present invention provides novel inhibitors of TAK1 and methods of using such compounds to treat various diseases. | 2018-04-19 |
20180105501 | PYRIMIDINYLOXY BENZENE DERIVATIVES AS HERBICIDES - Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, | 2018-04-19 |
20180105502 | PROCESS FOR PREPARING 1,4-DIBENZODIAZEPINES VIA BUCHWALD-HARTWIG CHEMISTRY - The present application provides a one-pot catalytic process which involves the formation of 1,4-dibenzodiazepines from o-haloaldimines (either pre-formed or formed in situ) of formula (I) and o-haloanilines of formula (II) via a palladium catalyzed Buchwald-Hartwig reaction and a cyclization sequence, to afford the 1,4-dibenzodiazepine products of formula (III). The present application describes the preparation of the 1,4-dibenzodiazepine products of formula (III) from simple commercial raw materials by efficient processes. | 2018-04-19 |
20180105503 | NEPRILYSIN INHIBITORS - In one aspect, the invention relates to compounds having the formula: | 2018-04-19 |
20180105504 | THERAPEUTIC COMPOUNDS AND METHODS OF USE THEREOF - The invention provides a compound of formula I: | 2018-04-19 |
20180105505 | GLUTATHIONE-CLEAVABLE PRODRUG AND METHODS OF USE THEREOF - A glutathione-cleavable prodrug is provided herein, as well as methods for its use in treating cancer, including triple negative breast cancer. The prodrug can be cleaved by glutathione under physiological conditions to generate a biologically active agent. The compound described herein is advantageous as the compound is fluorescent and can therefore be monitored within a subject. | 2018-04-19 |
20180105506 | TOCOPHEROL AND TOCOPHERYL QUINONE DERIVATIVES AS CORRECTORS OF LYSOSOMAL STORAGE DISORDERS - The subject invention relates to improved tocopheryl quinine derivatives and tocopherol derivatives having improved pharmacokinetics in vivo that can, in some embodiments, be useful in the treatment of Lysosomal Storage Disorder, restoration of normal mitochondrial ATP production, modulation of intracellular calcium ion concentration and other treatments or therapies. The tocopheryl quinone derivatives and tocopherol derivatives have side chains that have terminally halogenated carbon atoms. | 2018-04-19 |
20180105507 | ANTIIFLAMMATORY AND ANTITUMOR 2-OXOTHIAZOLES ABD 2-OXOTHIOPHENES COMPOUNDS - A compound of formula (I) | 2018-04-19 |
20180105508 | INHIBITORS OF PHOSPHOGLYCERATE DEHYDROGENASE (PHGDH) AND USES THEREOF - The present invention provides compounds pounds of Formula (II), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, pro-drugs, and compositions thereof. Also provided are methods and kits involving the compounds of Formula (I), (II) or (III) for treating diseases associated with the over-expression of phosphoglycerate dehydrogenase (PHGDH) in a subject, such as proliferative diseases (e.g., cancers (e.g., breast cancer, ER negative breast cancer, melanoma, cervical cancer), benign neoplasms, diseases associated with angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases). Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the activity of PHGDH or inhibit the serine biosynthetic pathway, or both. | 2018-04-19 |
20180105509 | AMINO-SUBSTITUTED HETEROCYCLIC DERIVATIVES AS SODIUM CHANNEL INHIBITORS - The present invention relates to novel aminoindazolyl derivative compounds of Formula (I), the use of said compounds in treating diseases mediated by modulation of voltage-gated sodium channels in particular Nav1.7 AND to compositions containing said derivatives. | 2018-04-19 |
20180105510 | SALT AND CRYSTALLINE FORMS THEREOF OF A DRUG - A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed. | 2018-04-19 |
20180105511 | SYNTHESIS OF CHIRAL 2-(1H-INDAZOL-6-YL)-SPIRO[CYCLOPROPANE-1,3'-INDOLIN]-2'-ONES - The present invention is directed to novel synthetic methods for preparing cyclopropyl indolinone compound represented by Structural Formula (A): (A) or its pharmaceutically acceptable salt thereof. Also included are synthetic intermediates described herein. | 2018-04-19 |
20180105512 | SUBSTITUTED BENZIMIDAZOLIUM COMPOUNDS USEFUL IN THE TREATMENT OF RESPIRATORY DISEASES - The present invention relates to compounds of formula (I), or the tautomers or pharmacologically acceptable acid addition salts thereof, characterized by a topological polar surface area value (TPSA) of at least 145, wherein R | 2018-04-19 |
20180105513 | PYRAZOLE COMPOUNDS OR SALTS THEREOF, PREPARATION METHODS THEREFOR, HERBICIDAL COMPOSITIONS AND USE THEREOF - The present invention relates to the technical field of pesticides, particularly relates to a pyrazole compound or a salt thereof, a preparation method therefor, a herbicidal composition and use thereof. A pyrazole compound of formula (I) or a salt thereof: | 2018-04-19 |
20180105514 | HETEROCYCLIC AMIDES USEFUL AS PROTEIN MODULATORS - Disclosed are compounds having the formula: | 2018-04-19 |
20180105515 | PYRIDYL BENZOTHIOPHENES AS KINASE INHIBITORS - This invention is directed to compounds, which are useful as protein kinase (PK) inhibitors and can be used to treat such diseases as cancer, blood vessel proliferative disorders, fibrotic disorders, mesangial cell proliferative disorders, metabolic diseases inflammatory disorders and neurodegenerative disorders. | 2018-04-19 |
20180105516 | ARYL SULTAM DERIVATIVES AS RORc MODULATORS - Compounds of the formula I: | 2018-04-19 |
20180105517 | Process for the Preparation of Aclidinium Bromide - A process for preparing (3R)-3-[2-Hydroxy(di-2-thienyl)acetoxy]-1-(3-phenoxypropyl)-1-azoniabicyclo[2.2.2]octane bromide (aclidinium bromide) comprises reacting 2-hydroxy-2,2-dithien-2-ylacetic acid 1-azabicyclo[2.2.2]oct-3(R)yl methyl ester and 3-phenoxypropyl bromide, wherein the reaction takes place in a solvent or mixture of solvents selected from the group of amides and/or the group of solvents with a sulfoxide group. Also provided is a crystalline aclidinium bromide characterized by a powder XRPD pattern having peaks at 7.7±0.2° 2θ, 10.4±0.2° 2θ, 13.2±0.2° 2θ, 13.8±0.2° 2θ, 19.9±0.2° 2θ, 20.3±0.2° 2θ, 20.8±0.2° 2θ, 24.2±0.2° 2θ, 25.7±0.2° 2θ, 26.1±0.2° 2θ, 29.2±0.2° 2θ, 30.8±0.2° 2θ. A pharmaceutical composition comprises aclidinium bromide according to the invention and a pharmaceutically acceptable excipient. | 2018-04-19 |
20180105518 | TRKA KINASE INHIBITORS, COMPOSITIONS AND METHODS THEREOF - The present invention is directed to bicyclic heteroaryl benzamide compounds of formulas (I): which are tropomyos-in-related kinase (Trk) family protein kinase inhibitors, and hence are useful in the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA. | 2018-04-19 |
20180105519 | ISOXAZOLYL SUBSTITUTED IMIDAZOPYRIDINES - A compound which is an isoxazolyl imidazopyridine of formula (I): wherein: R | 2018-04-19 |
20180105520 | AZAINDOLE ACETIC ACID DERIVATIVES AND THEIR USE AS PROSTAGLANDIN D2 RECEPTOR MODULATORS - The present invention relates to azaindole acetic acid derivatives of formula (I), | 2018-04-19 |
20180105521 | HISTONE DEMETHYLASE INHIBITORS - 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. | 2018-04-19 |
20180105522 | N-SULFONYLATED PYRAZOLO[3,4-b]PYRIDIN-6-CARBOXAMIDES AND METHOD OF USE - The present invention provides for compounds of formula (I) | 2018-04-19 |
20180105523 | NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I): | 2018-04-19 |
20180105524 | NOVEL ANXIOLYTIC COMPOUNDS - The present invention relates to chemical compounds of general formula (I) | 2018-04-19 |
20180105525 | ANTIBACTERIAL CYCLOPENTA[C]PYRROLE SUBSTITUTED 3,4-DIHYDRO-1H-[1,8]NAPHTHYRIDINONES - 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. | 2018-04-19 |
20180105526 | COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY - Provided herein are compounds, compositions thereof and uses therewith for treating spinal muscular atrophy. | 2018-04-19 |
20180105527 | HETEROARYL DERIVATIVE OR PHARMACEUTICALLY ACCEPTABLE SALT THEREOF, PREPARATION METHOD THEREFOR, AND PHARMACEUTICAL COMPOSTION FOR PREVENTING OR TREATING DISEASES ASSOCIATED WITH PI3 KINASES, CONTAINING SAME AS ACTIVE INGREDIENT - 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. | 2018-04-19 |
20180105528 | PREPARATION AND USE OF NOVEL PROTEIN KINASE INHIBITORS - The invention provides novel compounds and methods of using such compounds to treat or prevent cancer. | 2018-04-19 |
20180105529 | RSV ANTIVIRAL PYRAZOLO- AND TRIAZOLO-PYRIMIDINE COMPOUNDS - 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. | 2018-04-19 |
20180105530 | SUBSTITUTED PYRAZOLOPYRIMIDINES AND METHOD OF USE - Compounds of formula (I) | 2018-04-19 |
20180105531 | METHODS AND COMPOSITIONS FOR INHIBITING THE INTERACTION OF MENIN WITH MLL PROTEINS - 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. | 2018-04-19 |
20180105532 | HETEROCYCLIC COMPOUNDS AND THEIR USES - 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 p110δ 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 Lymphoblastic leukaemia (T-ALL) B-cell Acute Lymphoblastic leukaemia (B-ALL) Non Hodgkins Lymphoma (NHL) B-cell lymphoma and solid tumors, such as breast cancer. | 2018-04-19 |
20180105533 | BILE ACID RECEPTOR MODULATORS AND METHODS OF USE THEREOF - Disclosed herein, inter alia, compounds and methods of use thereof for the modulation of bile acid receptor activity. | 2018-04-19 |
20180105534 | ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE - 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: | 2018-04-19 |
20180105535 | Biologically Active Taxane Analogs and Methods of Treatment by Oral Administration - 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. | 2018-04-19 |
20180105536 | BICYCLIC AND TRICYCLIC PYRIMIDINE TYROSINE KINASE INHIBITORS WITH ANTITUBULIN ACTIVITY AND METHODS OF TREATING A PATIENT - 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. | 2018-04-19 |
20180105537 | PREPARATION OF HIGH-PURITY GADOBUTROL - 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. | 2018-04-19 |
20180105538 | BORONIC ACID DERIVATIVES - Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies. | 2018-04-19 |
20180105539 | BORONIC ACID DERIVATIVES - Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies. | 2018-04-19 |
20180105540 | NOVEL HYDROGEN PEROXIDE-ACTIVABLE, ANTI-OXIDANT COMPOUNDS AND METHODS USING SAME - 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. | 2018-04-19 |
20180105541 | Carbon Bridged Aminosilane Compounds for High Growth Rate Silicon-Containing Films - 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: | 2018-04-19 |
20180105542 | Method Of Producing Organohalosilanes - 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 R | 2018-04-19 |
20180105543 | ORIENTED PEROVSKITE CRYSTALS AND METHODS OF MAKING THE SAME - An aspect of the present disclosure is a method that includes combining a first organic salt (A | 2018-04-19 |
20180105544 | CONCERTED PROCESSES FOR FORMING 1,2,4-TRIHYDROXYBENZENE FROM HYDROQUINONE - 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. Methods for forming 1,2,4-trihydroxybenzene can include: oxidizing hydroquinone in a first reaction to form p-benzoquinone, converting the p-benzoquinone in a second reaction to form 1,2,4-triacetoxybenzene, deacetylating the 1,2,4-triacetoxybenzene in a third reaction to form 1,2,4-trihydroxybenzene, and isolating the 1,2,4-trihydroxybenzene after performing the first reaction, the second reaction and the third reaction consecutively. | 2018-04-19 |
20180105545 | HARDENER AND CURE ACCELERANT WITH FLAME RETARDANCY EFFECT FOR CURING EPOXY RESINS (II) - 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): | 2018-04-19 |
20180105546 | Methods for Chemical Synthesis of Biologically Active Compounds Using Supramolecular Protective Groups and Novel Compounds Obtainable Thereby - 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. | 2018-04-19 |
20180105547 | METHODS FOR THE TREATMENT AND PREVENTION OF INFLAMMATORY DISEASES - The inventors demonstrate that treatment of young, suckling mice with a glycolipid derived from | 2018-04-19 |
20180105548 | A novel compound (KS-513) isolated from Pseudolysimachion rotundum var. subintegrum, the composition comprising the same preventing or treating allergic disease, inflammatory disease, asthma or chronic obstructive pulmonary disease and the use thereof - (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. | 2018-04-19 |
20180105549 | HCV POLYMERASE INHIBITORS - The invention provides compounds of the formula: | 2018-04-19 |
20180105550 | CYTIDINE DERIVATIVE DIMERS AND APPLICATIONS THEREOF - 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): | 2018-04-19 |
20180105551 | TRINUCLEOTIDE MRNA CAP ANALOGS - What is described is a trinucleotide cap analog comprising m | 2018-04-19 |
20180105552 | NOVEL ANTIVIRAL COMPOUNDS, A PROCESS FOR THEIR PREPARATION, AND THEIR USE FOR TREATING VIRAL INFECTIONS - 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. | 2018-04-19 |
20180105553 | POLYPEPTIDES, PEPTIDES, AND PROTEINS FUNCTIONALIZED BY ALKYLATION OF THIOETHER GROUPS VIA RING-OPENING REACTIONS - 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. | 2018-04-19 |
20180105554 | USE OF DEXTRAN SULFATE TO ENHANCE PROTEIN A AFFINITY CHROMATOGRAPHY - In certain embodiments, the invention provides a method of purifying a protein of interest from a mixture by using a dextran polymer. | 2018-04-19 |
20180105555 | USE OF DEXTRAN FOR PROTEIN PURIFICATION - 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. | 2018-04-19 |
20180105556 | OXIDATIVE MODIFICATION IMPROVES THE DRUGABILITY OF CELL PENETRATING PEPTIDES AS DRUG CARRIERS - 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. | 2018-04-19 |
20180105557 | Melanocortin Receptor Ligands - The present invention is directed to compounds according to formula, | 2018-04-19 |
20180105558 | NOVEL CYCLOSPORIN DERIVATIVES AND USES THEREOF - The present invention relates to a compound of the Formula (I)): | 2018-04-19 |
20180105559 | AAV VECTORS WITH HIGH TRANSDUCTION EFFICIENCY AND USES THEREOF FOR GENE THERAPY - 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. | 2018-04-19 |
20180105560 | IMMUNOGLOBULIN-BINDING PROTEIN AND AFFINITY CARRIER USING SAME - 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 | 2018-04-19 |
20180105561 | ANALOGS OF SODIUM CHANNEL PEPTIDE TOXIN - The present invention also relates to pharmaceutical compositions useful for treating or preventing a disorder responsive to the blockade of sodium ion channels, especially Na | 2018-04-19 |
20180105562 | IMMUNE MODULATOR FOR IMMUNOTHERAPY AND VACCINE FORMULATION - 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-κB-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. | 2018-04-19 |
20180105563 | AGENT FOR PREVENTION OR TREATEMENT OF CORNEAL DISORDERS - 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. | 2018-04-19 |
20180105564 | USE OF ENDOGENOUS PROMOTERS TO EXPRESS HETEROLOGOUS PROTEINS - 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. | 2018-04-19 |
20180105565 | Compositions and Methods for Inhibiting Tumor Cells by Inhibiting the Transcription Factor ATF5 - 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. | 2018-04-19 |
20180105566 | MYELIN OLIGODENDROCYTE GLYCOPROTEIN, MYELIN BASIC PROTEIN, AND PROTEOLIPID PROTEIN COMPOSITIONS AND METHODS OF USE - 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. | 2018-04-19 |
20180105567 | PEPTIDE DERIVED FROM GPC3, PHARMACEUTICAL COMPOSITION FOR TREATMENT OR PREVENTION OF CANCER USING THE SAME, IMMUNITY INDUCER, AND METHOD FOR PRODUCING ANTIGEN-PRESENTING CELLS - 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. | 2018-04-19 |
20180105568 | Peptide Analogs for Treating Diseases and Disorders - 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. | 2018-04-19 |
20180105569 | ANALOGS OF GLUCAGON EXHIBITING GIP RECEPTOR ACTIVITY - 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. | 2018-04-19 |
20180105570 | METHOD FOR PREPARATION OF A RECOMBINANT PROTEIN FROM A PRECUSOR - 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. | 2018-04-19 |
20180105571 | GAL-1 Variants Having Immuno-Modulating Properties and Methods of Using the Same - Galectin-1 polypeptide variants that include a mutation of the histidine residue corresponding to position 52 of the full-length amino acid sequence of native human Gal-1 as shown in SEQ ID NO: 1, the mutation being a substitution of the histidine to tyrosine or asparagine, providing resistance to acidosis otherwise resulting in deactivation of the native human Gal-1. The Galectin-1 polypeptide variants may include one or more additional mutation(s) of the cysteine residue corresponding to a position selected from 2, 16, 88, or combinations thereof of the full-length amino acid sequence of native human Gal-1 as shown in SEQ ID NO: 1, the additional mutation being a substitution of the cysteine to serine, and providing resistance to oxidation. | 2018-04-19 |
20180105572 | NOVEL CYCLIC MONOMER AND DIMER PEPTIDES HAVING INTEGRIN ANTAGONIST ACTIVITY - The invention relates to C to N cyclized (C-N cyclic) monomer and dimer peptide molecules, as well as peptide dimers which are connected by linker moieties at the N terminus and the C terminus of each peptide subunit, which inhibit binding of α4β7 to the mucosal addressin cell adhesion molecule (MAdCAM) in vivo, and show high selectivity against α4β1 binding. | 2018-04-19 |
20180105573 | NUCLEIC ACID CONSTRUCT FOR EXPRESSING MORE THAN ONE CHIMERIC ANTIGEN RECEPTOR - The present invention provides a nucleic acid construct comprising the following structure: A-X—B in which A and B are nucleic acid sequences encoding a first and a second chimeric antigen receptor (CAR); and X is a nucleic acid sequence which encodes a cleavage site, wherein the first and second CAR recognise different antigens; the first and second CAR comprise or associate with activating endodomains; and (a) the first and/or second CAR comprises an intracellular retention signal; and/or (b) the signal peptide of the first or second CAR comprises one or more mutation(s) such that it has fewer hydrophobic amino acids. | 2018-04-19 |
20180105574 | ISOLATED PEPTIDES AND FRAGMENTS THEREOF FROM FIBRINOGEN FOR USE AS DRUGS, PARTICUARLY IN SKIN INFLAMMATORY DISEASES - A present invention relates to isolated peptides obtained from human fibrinogen for their use as drug, particularly for the prevention and/or the treatment of inflammatory skin diseases, more particularly acne. The present invention also relates to fragments of these polypeptides, nucleic acid molecules encoding them, expression vectors, host cells, a pharmaceutical composition and a combination product containing them, and their use for treating and/or preventing inflammatory skin diseases, particularly acne. | 2018-04-19 |
20180105575 | METHOD OF PURIFYING ALBUMIN-FUSION PROTEINS - The present invention relates to a method of purifying albumin-fusion proteins to reduce the level of oxidation of susceptible amino acid residues. The method comprises an affinity matrix chromatography step and an anion exchange chromatography step. The purified albumin-fusion proteins have low levels of oxidation and retain their enhanced half-life in vivo and its bioactivity. In some embodiments, the albumin-fusion protein comprises a scaffold, such as human Tenascin C scaffold. Compositions comprising the albumin-fusion protein are further disclosed. | 2018-04-19 |
20180105576 | ALBUMIN VARIANTS - The present invention relates to variants of a parent albumin having altered plasma half-life compared with the parent albumin. The present invention also relates to fusion polypeptides and conjugates comprising said variant albumin. | 2018-04-19 |
20180105577 | ALBUMIN VARIANTS - The present invention relates to variants of a parent albumin having altered plasma half-life compared with the parent albumin. The present invention also relates to fusion polypeptides and conjugates comprising said variant albumin. | 2018-04-19 |
20180105578 | ALBUMIN VARIANTS - The present invention relates to variants of a parent albumin having altered plasma half-life compared with the parent albumin. The present invention also relates to fusion polypeptides and conjugates comprising said variant albumin. | 2018-04-19 |
20180105579 | ANTIBODIES THAT POTENTLY NEUTRALIZE RABIES VIRUS AND OTHER LYSSAVIRUSES AND USES THEREOF - The invention relates to antibodies, and antigen binding fragments thereof that potently neutralize infection of both RABV and non-RABV lyssaviruses. The invention also relates to antigenic sites to which the antibodies and antigen binding fragments bind, as well as to nucleic acids that encode and immortalized B cells and cultured plasma cells that produce such antibodies and antibody fragments. In addition, the invention relates to the use of the antibodies and antibody fragments of the invention in screening methods as well as in the diagnosis, prophylaxis and treatment of RABV infection and infection with non-RABV lyssaviruses. | 2018-04-19 |
20180105580 | FILOVIRUS THERAPY - The present invention provides antibodies, for use in the treatment, suppression prevention of Filovirus disease, particularly Ebola virus disease. Also provided immunogens for use in eliciting such antibodies. | 2018-04-19 |
20180105581 | MONOVALENT, BIVALENT AND TRIVALENT ANTI HUMAN RESPIRATORY SYNCYTIAL VIRUS (HRSV) NANOBODY CONSTRUCTS FOR THE PREVENTION AND/OR TREATMENT OF RESPIRATORY TRACT INFECTIONS - Amino acid sequences are provided that are directed against/and or that can specifically bind protein F of hRSV, as well as to compounds or constructs, and in particular proteins and polypeptides, that comprise or essentially consist of one or more such amino acid sequences. The amino acid sequences, polypeptides and therapeutic compounds and compositions provided by the invention show an improved stability, less immunogenicity and/or improved affinity and/or avidity for protein F of hRSV. | 2018-04-19 |
20180105582 | THERAPEUTIC COMPOSITION - A therapeutic composition can include an herbal composition having solid material or liquid extracts from the solid material of at least one of | 2018-04-19 |
20180105583 | ANTIBODIES THAT BIND ZIKA VIRUS ENVELOPE PROTEIN AND USES THEREOF - Isolated monoclonal antibodies which bind to Zika virus envelope protein and related antibody-based compositions and molecules are disclosed. Also disclosed are therapeutic and diagnostic methods for using the antibodies. | 2018-04-19 |
20180105584 | ANTIBODY DIRECTED AGAINST IMMUNOGLOBULIN-BINDING PROTEINS OF S. AUREUS - A monoclonal antibody that counteracts | 2018-04-19 |
20180105585 | ANTIBODIES TO AMYLOID BETA - Antibody for human amyloid beta. Antibody selectively binds human amyloid beta 42 peptide over human amyloid beta 40 peptide. Antibodies specific for amyloid beta 42 as therapeutic agents for binding amyloid beta 42 peptide and treating conditions associated with amyloidosis, such as Alzheimer's disease. | 2018-04-19 |
20180105586 | SECRETED aP2 AND METHODS OF INHIBITING SAME - A method of reducing a symptom of a clinical disorder characterized by aberrantly elevated circulating aP2 is carried out by administering to a subject an inhibitor of secreted aP2, secretion of aP2, or a serum aP2 blocking agent. For example, glucose intolerance is reduced following administration of such an inhibitor or agent. Exemplary compositions inhibit cellular secretion of aP2 or bind to circulating aP2, thereby reducing the level or activity of aP2 in blood or serum. | 2018-04-19 |