49th week of 2020 patent applcation highlights part 25 |
Patent application number | Title | Published |
20200377491 | Prodrug Modulators of the Cystic Fibrosis Transmembrane Conductance Regulator Protein and Methods of Use - The present invention relates to prodrug compounds and their use in the treatment of Cystic Fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treating cystic fibrosis by administering a compound of the invention. | 2020-12-03 |
20200377492 | ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE INCLUDING THE SAME - Disclosed is a novel organic electroluminescent compound represented by Formula (I): | 2020-12-03 |
20200377493 | NOVEL INHIBITORS - The invention relates to a compound of formula (I): A-B-D-E (I) or a pharmaceutically acceptable salt, solvate or polymorph thereof, including all tautomers and stereoisomers thereof, wherein: A is selected from monocyclic and bicyclic heteroaryl, which may independently substituted by alkyl or amino; B is selected from alkyl, heteroalkyl, alkyl-amino, aryl, heteroaryl, cycloalkyl, heterocyclyl and alkylene, wherein said groups may independently be substituted by alkyl; D is selected from aryl-amino, heteroaryl-amino, cycloalkyl-amino, heterocyclyl, heterocyclyl-amino, urea, thioamide, thiourea, sulfonamide, sulfoximine and sulfamoyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted; and E is selected from aryl, heteroaryl, cycloalkyl, heterocyclyl, wherein said aryl, heteroaryl, cycloalkyl and heterocyclyl groups may independently be substituted. The compounds of formula (I) are inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water. | 2020-12-03 |
20200377494 | COMPOSITIONS AND METHODS FOR MODULATING INFLAMMATORY AND DEGENERATIVE DISORDER - The disclosure provides compounds and method useful for modulating gp130 biological activity. The disclosure also provides methods and compositions for treating disease and disorders associated with gp130 activity, particularly those associated with inflammation. | 2020-12-03 |
20200377495 | POLYMORPHIC FORMS OF DASATINIB - The present invention provides for the dasatinib-thymine co-crystal and dasatinib-adenine co-crystal. The present invention further provides dasatinib-butanediol solvate. The present invention further provides for crystalline dasatinib-(±)-1,2-Butane diol, crystalline dasatinib (R)-1,2-Butanediol, crystalline dasatinib (S)-1,2-Butanediol and crystalline dasatinib (±)-2,3-Butanediol and processes for preparation thereof. The present invention also provides for a process for preparation of amorphous dasatinib using dasatinib-butanediol solvate. The present invention further provides for the preparation of anhydrous dasatinib. The present invention also provides for a process for preparation of dasatinib monohydrate from anhydrous dasatinib | 2020-12-03 |
20200377496 | INDOLE AND BENZIMIDAZOLE DERIVATIVES AS DUAL 5-HT2A and 5-HT6 RECEPTOR ANTAGONISTS - The invention relates to new 4-(piperazin-1-yl)-2-(trifluoromethyl)-1H-indoles and 4-(piperazin-1-yl)-2-(trifluoromethyl)-1H-benzimidazoles represented by formula (I), wherein all symbols and variables are as defined in the description. The compounds can find use in a method of prevention and/or treatment of diseases selected from the group consisting of Alzheimer's disease, Parkinson's disease, Levy body dementia, dementia-related psychosis, schizophrenia, delusional syndromes and other psychotic conditions related and not related to taking psychoactive substances, depression, anxiety disorders of various aetiology, sleep disorders of various aetiology. | 2020-12-03 |
20200377497 | NONTOXIC COMPOUNDS FOR THE TREATMENT AND PREVENTION OF HERPESVIRUS INFECTIONS - Compositions for preventing or treating virus infections inhibit the biogenesis of cytoplasmic viral assembly compartment (cVAC). The preferred compounds are dihydroquinazolinones. | 2020-12-03 |
20200377498 | NOVEL PYRROLOPYRIDINE DERIVATIVE, METHOD FOR PRODUCING SAME, AND USE THEREOF - Provided is a novel pyrrolopyridine compound represented by Chemical Formula I, a racemate or a stereoisomer thereof, or a pharmaceutically acceptable salt thereof; and to a method for preparing the same. A compound represented by Chemical Formula I shows high selectivity and antiviral activity against human immunodeficiency virus (HIV), with low toxicity; therefore, it is useful as a therapeutic agent for viral infection, in particular, HIV infection. | 2020-12-03 |
20200377499 | ION CHANNEL MODULATORS - Provided, in part, are compounds of Formula I: | 2020-12-03 |
20200377500 | META TYROSINE DERIVATIVES AS RHO-KINASE INHIBITORS - The invention relates to compounds of formula (I) inhibiting Rho Kinase that are meta tyrosine derivatives, processes for preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH). | 2020-12-03 |
20200377501 | DEGRADERS OF EGFR AND METHODS OF USE THEREOF - The application relates to a compound having Formula X: (X), wherein: the Targeting Ligand is capable of binding to EGFR, including drug resistant forms of EGFR; the Linker is a group that covalently binds to the Targeting Ligand and the Degron; and the Degron is capable of binding to a ubiquitin ligase, such as an E3 ubiquitin ligase (e.g., cereblon), wherein the Targeting Ligand is of Formula Ia or Ib: (Ia) or (Ib), or a pharmaceutically acceptable salt, hydrate, or solvate thereof, which modulates the activity of EGFR, a pharmaceutical composition comprising the compound, and a method of treating or preventing a disease in which EGFR plays a role. | 2020-12-03 |
20200377502 | 1H-PYRROLO[2,3-c]PYRIDIN-7(6H)-ONES AND PYRAZOLO[3,4-c]PYRIDIN-7(6H)-ONES AS INHIBITORS OF BET PROTEINS - The present invention relates to substituted pyrrolopyridinones and substituted pyrazolopyridinones which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 2020-12-03 |
20200377503 | EGFR DIMER DISRUPTORS AND USE OF THE SAME - Provided herein are compounds that modulate EGFR and methods of using the same, for example to treat cancer. | 2020-12-03 |
20200377504 | SUBSTITUTED TRICYCLIC COMPOUNDS AS FGFR INHIBITORS - The present invention relates to tricyclic compounds, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. | 2020-12-03 |
20200377505 | BENZIMIDAZOLES AND AZA-BENZIMIDAZOLES, AND METHODS OF USE THEREOF - Disclosed are compounds according to Formula (I) or (II), and pharmaceutical compositions comprising them. Also disclosed are therapeutic methods, e.g., of treating kidney diseases, using the compounds of Formula (I) or (II). | 2020-12-03 |
20200377506 | COMPOUNDS AND THEIR METHODS OF USE - The present invention is directed to, in part, fused heteroaryl compounds and compositions useful for preventing and/or treating a disease or condition relating to aberrant function of a voltage-gated, sodium ion channel, for example, abnormal late/persistent sodium current. Methods of treating a disease or condition relating to aberrant function of a sodium ion channel including Dravet syndrome or epilepsy are also provided herein. | 2020-12-03 |
20200377507 | ION CHANNEL MODULATORS - Provided, in part, are compounds of Formula I | 2020-12-03 |
20200377508 | sGC STIMULATORS - The present disclosure relates to stimulators of soluble guanylate cyclase (sGC), pharmaceutically acceptable salts, pharmaceutical formulations comprising them as well as their phosphate ester prodrugs, and their uses alone or in combination with one or more additional agents, for treating various diseases, wherein an increase in the concentration of nitric oxide (NO) and/or an increase in the concentration of cyclic Guanosine Monophosphate (cGMP), or both, or the upregulation of the NO pathway is desirable. The compounds are of Formula I. | 2020-12-03 |
20200377509 | SUBSTITUTED CYCLYL-ACETIC ACID DERIVATIVES FOR THE TREATMENT OF METABOLIC DISORDERS - Provided is a novel aromatic ring compound which may have a GPR40 agonist activity and a GLP-1 secretagogue action. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof may have a GPR40 agonist activity and a GLP-1 secretagogue action, may be useful for the prophylaxis or treatment of cancer, obesity, diabetes, hypertension, hyperlipidemia, cardiac failure, diabetic complications, metabolic syndrome, sarcopenia and the like, and may afford superior efficacy. | 2020-12-03 |
20200377510 | DERIVATIVES OF PIPERLONGUMINE AND USES THEREOF - The present invention relates to a group of 1-[(E)-3-(3,4,5-trimethoxyphenyl)prop-2-enoyl]-2,3-dihydropyridin-6-one (piperlongumine) derivatives, analogs and pharmaceutically acceptable salts thereof. The present invention also relates to a pharmaceutical composition and formulation containing a derivative of piperlongumine; and use of the derivatives and analogs for treating cancer, reducing inflammation and/or treating an autoimmune or inflammatory disease. | 2020-12-03 |
20200377511 | Bicyclic-Fused Heteroaryl or Aryl Compounds - Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, | 2020-12-03 |
20200377512 | SUBSTITUTED 1-OXO-ISOINDOLINE-5-CARBOXAMIDE COMPOUNDS, COMPOSITIONS THEREOF, AND METHODS OF TREATMENT THEREWITH - Provided herein are 1-oxo-isoindoline-5-carboxamide compounds having the following structure: | 2020-12-03 |
20200377513 | NOVEL COMPOUND AND ORGANIC ELECTROLUMINESCENCE DEVICE - A compound represented by the following formula (1): | 2020-12-03 |
20200377514 | KV1.3 INHIBITORS AND THEIR MEDICAL APPLICATION - Disclosed are compounds within the scope of formula (II) or a salt or solvate thereof, medical uses involving them, and methods for their preparation | 2020-12-03 |
20200377515 | PROCESS FOR THE PREPARATION OF DIHALOBENZOPHENONES, NEW CHEMICALS USEFUL FOR ITS IMPLEMENTATION AND METHODS FOR PREPARING SAID CHEMICALS - The invention relates to new compounds of formulae (IV) and (VII): (IV) (VII) wherein X represents a halogen atom selected from the group consisting of fluorine, chlorine, bromine and iodine and R is a hydrocarbyl radical, said compounds being useful as precursors and/or intermediates for the preparation of 4,4′dihalobenzophenones of formula (I): (I) wherein X is as defined above. | 2020-12-03 |
20200377516 | NOVEL COMPOUNDS AND METHOD OF PREVENTING OR TREATING CANCER USING THE SAME - The present disclosure relates to novel compounds and a method of preventing or treating cancer using the same, and more particularly to compounds having structural formulae 1 to 3. The compounds of the present disclosure exhibit an excellent activity of inhibiting various cancer cells, and thus can be effectively used in a composition or method for preventing, alleviating, or treating cancer. | 2020-12-03 |
20200377517 | ANTI-HBVTETRAHYDROISOXAZOLO[4,3-C]PYRIDINE COMPOUNDS - Disclosed are a class of anti-HBV tetrahydroisoxazolo[4,3-c]pyridine compounds and pharmaceutically acceptable salts thereof or isomers thereof, the compounds being represented by the formula (I). | 2020-12-03 |
20200377518 | METHOD OF PREVENTING AND TREATING THROMBOSIS - A method of preventing or treating thrombosis in a patent is disclose, wherein the method comprises administering to the patient an amount of fostamatinib or a form or metabolite thereof effective to prevent or treat the thrombosis, respectively. | 2020-12-03 |
20200377519 | HEPATITIS B ANTIVIRAL AGENTS - The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof: | 2020-12-03 |
20200377520 | MACROCYCLIC DERIVATIVE OF PYRAZOL[3,4-D]PYRIMIDIN-3-ONE, PHARMACEUTICAL COMPOSITION AND USE THEREOF - A macrocyclic derivative of pyrazol[3,4-d]pyrimidin-3-one as represented by formula (I) and/or a pharmaceutically acceptable salt thereof, a composition comprising the compound as represented by formula (I) and/or a pharmaceutically acceptable salt thereof, a preparation method therefor, use thereof as a Wee1 inhibitor and use thereof as a sensitizer in chemotherapy or a radiotherapy of cancers. The macrocyclic derivative of pyrazol[3,4-d]pyrimidin-3-one can effectively inhibit Wee1 and relating signaling pathways, having good therapeutic and relieving effects on cancers. | 2020-12-03 |
20200377521 | PROCESS FOR THE PREPARATION OF CYCLOPROPYLDIKETOPIPERAZINES AND OF A KEY INTERMEDIATE OF DS-5272 - Object of the present invention is an improved process for the preparation of cyclopropyldiketopiperazines and thereof key intermediates. | 2020-12-03 |
20200377522 | XANTHINE DERIVATIVES AND USES THEREOF AS INHIBITORS OF BROMODOMAINS OF BET PROTEINS - The present invention relates to a compound having the following formula (I): (I) wherein: —R is a (C | 2020-12-03 |
20200377523 | DIAGNOSIS, TREATMENT AND PREVENTION OF NEUROTENSIN RECEPTOR-RELATED CONDITIONS - The present invention describes a compound of formula (I) which can be used in the diagnosis, treatment or prevention of neurotensin receptor-related conditions such as tumors and hematological malignancies. | 2020-12-03 |
20200377524 | PROCESS FOR PURIFYING ACETOXYSILOXANES - Processes are described for purifying acidic, preferably superacidic, in particular trifluoromethanesulfonic acid-acidified, end-equilibrated acetoxysiloxanes, wherein the acidic, preferably superacidic, in particular trifluoromethanesulfonic acid-acidified, acetic anhydride-containing and optionally acetic acid-containing equilibrated, preferably end-equilibrated acetoxysiloxane, which is optionally dissolved in an inert solvent, is contacted with a base, the precipitate is filtered off thereafter and then the filtrate obtained is optionally purified by distillation. | 2020-12-03 |
20200377525 | ACETOXY SYSTEMS - Reaction system for preparing acetoxy function-bearing siloxanes having chain lengths of more than 3 silicon atoms, comprising silanes and/or siloxanes bearing alkoxy groups, silanes and/or siloxanes bearing acetoxy groups, silanes and/or siloxanes bearing hydroxy groups and/or simple siloxane cycles and/or DT cycles, and also a reaction medium comprising acetic anhydride, Brønsted acid and acetic acid, wherein Brønsted acids having a pKa ≤−1.30 are used, and wherein the acetic acid is present in the reaction system in amounts of 0.4 to 15.0 percent by weight, based on the reaction system, wherein the molar ratio of Brønsted acid used to acetic acid is in a defined range, with the proviso that either the sole use of trifluoromethanesulfonic acid and also of trifluoromethanesulfonic acid and acetic acid is excluded, and/or that the Brønsted acid used at least in part has a pKa between −1.3 and >−13.5. | 2020-12-03 |
20200377526 | PROCESS FOR PRODUCING ACETOXY-BEARING SILOXANES - Described is a process for producing preferably trifluoromethanesulfonic acid-acidified, end-equilibrated, acetoxy-bearing siloxanes which comprises reacting cyclic siloxanes, in particular comprising D | 2020-12-03 |
20200377527 | IN-CHAIN FUNCTIONALIZED ELASTOMER, RUBBER COMPOSITION AND PNEUMATIC TIRE - The present invention is directed to a functionalized elastomer, wherein the functionalized elastomer is a copolymer of a first monomer and a second monomer, the first monomer selected from the group consisting of conjugated diene monomers and vinyl aromatic monomers, and the second monomer of formula 1 | 2020-12-03 |
20200377528 | PREPARATION OF AROMATIC-SUBSTITUTED SILYLAMINES BY THE DEHYDROGENATIVE COUPLING OF AROMATIC-SUBSTITUTED AMINE N-H AND Si-H BONDS - The present disclosure is directed at methods of forming an N—Si silyl bond, the method comprising contacting an organic substrate comprising an aromatic amine having at least one N—H bond with a mixture comprising of (a) at least one hydrosilane and (b) at least one hydroxide or alkoxide, under conditions sufficient to form the N—Si bond. The disclosure is further directed to the compositions involved in these methods and the products that result therefrom. | 2020-12-03 |
20200377529 | NOVEL HETEROAROMATIC SILICON-FLUORIDE-ACCEPTORS USEFUL FOR 18F LABELING OF MOLECULES AND BIOMOLECULES, AND METHODS OF PREPARING SAME - The present disclosure sets forth novel compounds and compositions including heteroaromatic silicon-fluoride-acceptors, which are useful for PET scanning. The present disclosure further includes novel methods of | 2020-12-03 |
20200377530 | SILANE MIXTURES AND PROCESS FOR PREPARING SAME - The invention relates to silane mixtures comprising a silane of the formula I | 2020-12-03 |
20200377531 | SILANE MIXTURES AND PROCESS FOR PREPARING SAME - The invention relates to silane mixtures comprising a silane of the formula I | 2020-12-03 |
20200377532 | PEROVSKITE SOLUTION FOR MAKING A PEROVSKITE LAYER AT HIGH SPEED - A Perovskite solution is described for use in making a uniform Perovskite layer at high speed to enable low cost production of high efficiency Perovskite devices. The Perovskite solution contains a solvent, an organic Perovskite precursor material, and an inorganic Perovskite precursor material, wherein the amount of solvent is greater than 30 percent by weight and the Perovskite solution has a total solids concentration that is between 30 percent and 70 percent by weight of the Perovskite solution's saturation concentration at a solution temperature of from 20 to 25 degrees Celsius. | 2020-12-03 |
20200377533 | SEQUESTERING COMPOSITIONS AND MATERIALS - The present disclosure relates to a composition that includes a sequestering material capable of binding a target material, where the sequestering material includes a first component that includes at least one of a functional group, a molecule, an oligomer, or a polymer, and the target material includes at least one of an element, a chemical, and/or a compound. In some embodiments of the present disclosure, the element may include at least one element from at least one of Rows 4, 5, 6, and 7 of the Periodic Table and/or an inner transition metal. | 2020-12-03 |
20200377534 | Organic Long Persistence Luminescence Compositions - Provided herein are organic long persistent luminescence compositions and methods of use and preparation thereof and articles comprising the same. | 2020-12-03 |
20200377535 | PRODRUGS OF PYRIDONE AMIDES USEFUL AS MODULATORS OF SODIUM CHANNELS - The invention relates to prodrug compounds of formula I: | 2020-12-03 |
20200377536 | OPTICALLY ACTIVE 2,3-BISPHOSPHINOPYRAZINE DERIVATIVE, METHOD FOR PRODUCING SAME, TRANSITION METAL COMPLEX, AND METHOD FOR PRODUCING ORGANIC BORON COMPOUND - An optically active 2,3-bisphosphinopyrazine derivative represented by the following general formula (1): | 2020-12-03 |
20200377537 | ORGANOMETALLIC COMPOUND AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME - An organometallic compound is represented by Formula 1. An organic light-emitting device includes: a first electrode; a second electrode facing the first electrode; an organic layer between the first electrode and the second electrode and including an emission layer; and at least one of the organometallic compound represented by Formula 1. | 2020-12-03 |
20200377538 | Metal Precursors With Modified Diazabutadiene Ligands For CVD And ALD And Methods Of Use - Metal coordination complexes comprising at least one diazabutadiene based ligand having a structure represented by: | 2020-12-03 |
20200377539 | METHOD OF PRODUCING LIGNIN WITH REDUCED AMOUNT OF ODOROUS SUBSTANCES - The present invention relates to a method of producing lignin with reduced amount of odorous substances comprising the step of: providing a solid phase lignin containing starting material to be contacted with a water solution comprising carboxylic acid; dissolving the guaiacol and etylguaiacol content from the lignin into the water solution, and draining off the water solution with its content of guaiacol or etylguaiacol; obtaining a lignin material with a reduced content of guaiacol or etylguaiacol. The invention also relates to a lignin product with reduced odour obtained and/or obtainable by the method obtained lignin as a component in polymer blends, an additive or filler in building materials, as binding agent in adhesives, and/or for the production of a carbon fibre, especially in indoor applications. | 2020-12-03 |
20200377540 | METHOD FOR EFFICIENT PRODUCTION OF PSICOSE - The present invention relates to a method for effectively utilizing fructose raffinate obtained in the process for separating psicose conversion product with a high purity chromatography in the process for preparing psicose, and more specifically, it is utilized for preparation of fructose-containing raw material solution for preparation of psicose by putting fructose raffinate obtained in the process for preparing psicose into the process for preparing fructose. | 2020-12-03 |
20200377541 | STEVIA-DERIVED MOLECULES, METHODS OF OBTAINING SUCH MOLECULES, AND USES OF THE SAME - A purified composition of steviol glycoside molecules is described. The composition imparts desirable taste, flavor and flavor modifying properties to food, beverages, and other consumable products. | 2020-12-03 |
20200377542 | MACROLIDES WITH MODIFIED DESOSAMINE SUGARS AND USES THEREOF - Provided herein are macrolide compounds of Formula (I) and (I-N) for the treatment of infectious diseases and inflammatory conditions. The 14-membered ketolides and 14-, 15-, and 16-membered azaketolides described herein comprise modified sugars which are desosamine or mycaminose analogs. Pharmaceutical compositions and methods of treating infection diseases and inflammatory conditions using the inventive macrolides are also provided. This disclosure additionally provides methods of preparing the macrolides by the coupling of an eastern and western half. | 2020-12-03 |
20200377543 | Synthesis of Protected 3'-Amino Nucleoside Monomers - Orthogonally protected 3′-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3′-amino group in the presence of the unprotected nucleoside base. | 2020-12-03 |
20200377544 | PROGRAMMABLE SOFT ROBOT - Described are a combinatorial library of DNA molecules that can induce shape changes within specific regions of hydrogels up to centimeter scales. The DNA molecules include polymerizing hairpins, terminating hairpins, reversal strands, and crosslink nucleic acid sequences. | 2020-12-03 |
20200377545 | NOVEL ANTI-TUMOR COMPOUND AND APPLICATION THEREOF IN PREPARING ANTI-TUMOR DRUGS - The present invention belongs to the technical field of biomedicine, and discloses a novel anti-tumor compound. The anti-tumor compound is an immune activator cisplatin complex prepared from an innate immune pathway agonist and cisplatin drug molecules through a reaction. The anti-tumor drug has dual anti-tumor effects, achieves the two-pronged effects of activating innate immune pathways (generating immune T cells to fight tumors) and fighting tumors by a cisplatin chemotherapy drug, and has the significant effects of fighting tumors, increasing effect and decreasing toxicity as compared with the monofunctional cisplatin anticancer chemotherapy drug. Therefore, the novel immune activator cisplatin anti-tumor drug has an efficient clinical application prospect. | 2020-12-03 |
20200377546 | ESTROGEN RECEPTOR BETA SELECTIVE LIGANDS - An estrogen receptor β selective ligand can be a compound according to Structure 1: | 2020-12-03 |
20200377547 | NEUROACTIVE STEROIDS AND COMPOSITIONS THEREOF - Provided herein is a compound of Formula (I): | 2020-12-03 |
20200377548 | Method for Preparing Peptides - The invention relates to a method for preparing peptides comprising the step of forming a peptide bond wherein the carboxyl group of a first amino acid or first peptide is activated and an amino group of the first activated amino acid or first peptide is protected by a protecting group having a water-solubility enhancing group and the activated carboxyl group of the first amino acid or first peptide is reacted with an amino group of a second amino acid or second peptide wherein said carboxyl group of the first amino acid or first peptide is activated in the absence of the second amino acid or second peptide. The invention further relates to peptides comprising a protecting group having a water-solubility enhancing group being bound to the amino group and an activated or free carboxyl group. | 2020-12-03 |
20200377549 | PSMA Imaging Agents - Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging. | 2020-12-03 |
20200377550 | PEPTIDE HAVING CYTOPROTECTIVE EFFECT AGAINST ENVIRONMENTAL POLLUTANT AND USE THEREOF - Provided are a peptide with a cytoprotective effect against environmental pollutants and a use thereof. The peptide consisting of an amino acid sequence of SEQ ID NO: 1, 2, or 3 directly binds to 2,3,7,8-tetrachlorodibenzo-p-dioxin (hereinafter, referred to as TCDD), known as being the most toxic among the class of dioxins, to prevent dermal penetration and the activation mechanism of AhR by TCDD and polycyclic aromatic hydrocarbons contained in fine dust. Such a direct cytoprotective effect against environmental pollutants is distinguished from preexisting methods that are configured to indirectly block opportunities to contact these materials or to reduce toxicity through barrier reinforcement. | 2020-12-03 |
20200377551 | PEPTIDE CONSTRUCTS AND METHODS FOR ENHANCEMENT OF INTERFERON PRODUCTION - Peptide constructs comprising a mitochondrial antiviral-signaling protein (MAVS) peptide and a cell penetration peptide are disclosed, which are useful for stimulating interferon production in vitro and in vivo. Lactate has been discovered to inhibit glycolysis-mediated retinoic acid-inducible gene I (RIG-I) like receptor signaling by directly binding to the MAVS transmembrane (TM) domain and preventing MAVS aggregation; peptide constructs according to the disclosure can prevent or reverse this inhibition to stimulate interferon production. Methods for stimulating interferon production in a cell are also described, as well as methods for the treatment of viral infections and cancer. | 2020-12-03 |
20200377552 | ONE-BEAD-TWO-COMPOUND MACROCYCLIC LIBRARY AND METHODS OF PREPARATION AND USE - A one-bead-two-compound combinatorial synthesis technique provides libraries of macrocyclic peptidomimetic compounds and compositions with use as ligands for the Ephrin type-A receptor 2 (EphA2). The one-bead-two-compound technique and libraries of macrocyclic compounds are useful as research tools in drug discovery and/or to treat or prevent a range of diseases or disorders. | 2020-12-03 |
20200377553 | ANTIBODY SPECIFIC CAPTURE AGENTS, COMPOSITIONS, AND METHODS OF USING AND MAKING - The present application provides stable peptide-based antibody capture agents and methods of use as detection and diagnosis agents. The application further provides methods of manufacturing antibody capture agents using iterative on-bead in situ click chemistry. | 2020-12-03 |
20200377554 | NOVEL AAV'S AND USES THEREOF - The invention in some aspects relates to recombinant adeno-associated viruses having distinct tissue targeting capabilities. In some aspects, the invention relates to gene transfer methods using the recombinant adeno-associate viruses. In some aspects, the invention relates to isolated AAV capsid proteins and isolated nucleic acids encoding the same. | 2020-12-03 |
20200377555 | INFLUENZA VIRUS VACCINES AND USES THEREOF - Provided herein are influenza hemagglutinin stem polypeptides, nucleic acids encoding said polypeptides, vectors comprising said nucleic acid and pharmaceutical compositions comprising the same, as well as methods of their use, in particular in the prevention and/or treatment of influenza virus infections. | 2020-12-03 |
20200377556 | DISPLAY OF HETEROLOGOUS MOLECULES ON BACTERIAL CELLS AND MEMBRANE VESICLES - The present invention concerns Gram-negative bacterial cells or Outer Membrane Vesicles (OMVs) which display on their outer surface an autotransporter (AT) fusion protein covalently coupled via an isopeptide bond to a heterologous molecule. These bacterial cells and OMVs are suitable for use in vaccines or targeted drug delivery of antigens or therapeutic agents to specific cells or tissues. | 2020-12-03 |
20200377557 | NOVEL POLYPEPTIDE AND METHOD OF PRODUCING IMP USING THE SAME - The present disclosure relates to a novel polypeptide having an activity of exporting 5′-inosine monophosphate, a microorganism comprising the same, a method for preparing 5′-inosine monophosphate using the same, and a method for increasing export of 5′-inosine monophosphate. | 2020-12-03 |
20200377558 | NOVEL POLYPEPTIDE AND METHOD OF PRODUCING IMP USING THE SAME - The present disclosure relates to a novel protein variant having an activity of exporting 5′-inosine monophosphate, a microorganism comprising the protein variant, and a method for preparing 5′-inosine monophosphate using the microorganism. | 2020-12-03 |
20200377559 | REDUCTION OF ACETATE AND GLYCEROL IN MODIFIED YEAST HAVING AN EXOGENOUS ETHANOL-PRODUCING PATHWAY - Described are compositions and methods relating to the over-expression of sugar transporter-like polypeptides to reduce the amount of glycerol and acetate produced by modified yeast having an exogenous pathway that cause it to produce more ethanol and acetate than its parental yeast. | 2020-12-03 |
20200377560 | ANTIBODIES TO ROYALACTIN AND USES THEREOF - Antibodies specific for royalactin (RA) can be used in methods for purifying royalactin, including native royalactin. These methods produce can produce compositions enriched for native royalactin. The purified royalactin can be used to produce cosmetic products that include native royalactin. An isolated nucleic acid encodes a monoclonal antibody that binds specifically to royalactin. | 2020-12-03 |
20200377561 | ANTIMICROBIAL PEPTIDES AND METHODS OF TREATING GRAM-NEGATIVE PATHOGEN INFECTIONS: POLAR AND NON-POLAR FACE ANALOGS - Antimicrobial agents, including antimicrobial peptides (AMPs) and uses thereof. Compositions and methods of using dermaseptin-type and piscidin-type antimicrobial peptide variants that demonstrate activity and improved therapeutic indices against microbial pathogens. The peptide compositions demonstrate the ability to not only maintain or improve antimicrobial activity against bacterial pathogens including Gram-negative microorganisms | 2020-12-03 |
20200377562 | HISTONE ANTI-CANCER VACCINES - The present invention pertains to novel immunogenic peptide sequences that can be used as vaccines in the treatment of cancer diseases such as brain cancers and specifically glioma. The cancer vaccines of the invention are designed based on the K27M mutated variant of the human Histone 3. Provided are further fusion proteins comprising the sequences of the cancer vaccines, nucleic acids encoding such vaccines, such as RNA vaccines, and vectors and host cells comprising these sequences. Furthermore the invention pertains to T cells and T cell receptors binding the cancer vaccines of the invention, preferably when presented by the human Major Histocompatibility Complex (MHC). The peptide immunogens of the invention elicit a HLA restricted immune response and therefore are of use in the treatment of cancer diseases, in particular glioma. Further aspects of the invention pertain to pharmaceutical compositions as well as diagnostic methods based on the immunogenic capacity of the disclosed peptides. | 2020-12-03 |
20200377563 | NOVEL SPECIFIC-BINDING POLYPEPTIDES AND USES THEREOF - The present invention relates to novel, specific-binding therapeutic and/or diagnostic polypeptides directed against the target of Swiss Prot Q16552 and novel, specific-binding therapeutic and/or diagnostic polypeptides directed against the target of Swiss Prot Q9NPF7. In addition, the present invention relates to novel, specific-binding therapeutic and/or diagnostic polypeptides directed against one or both of Swiss Prot Q16552 and Swiss Prot Q9NPF7. The invention also relates to nucleic acid molecules encoding such polypeptides and to methods for generation of such polypeptides and nucleic acid molecules. In addition, the invention is directed to compositions comprising the polypeptides, and therapeutic and/or diagnostic uses of these polypeptides. | 2020-12-03 |
20200377564 | REGULATED SYNTHETIC GENE EXPRESSION SYSTEMS - The technology described herein is directed to regulated synthetic gene expression systems. In one aspect described herein are synthetic transcription factors (synTFs) comprising a DNA binding domain, a transcriptional effector domain, and a regulator protein. In other aspects described herein are gene expression systems comprising said synTFs and methods of treating diseases and disorders using said synTFs. | 2020-12-03 |
20200377565 | Brown Fat-Selective Adipokines - Methods of treating or reducing the risk of obesity and/or obesite-related disorders, e.g., metabolic syndrome, hepatic and non-hepatic steatosis, and diabetes, using C20orf27 proteins or nucleic acids. | 2020-12-03 |
20200377566 | MODIFIED LIGAND-GATED ION CHANNELS AND METHODS OF USE - This document relates to materials and methods for controlling ligand gated ion channel (LGIC) activity. For example, modified LGICs including at least one LGIC subunit having a modified ligand binding domain (LBD) and/or a modified ion pore domain (IPD) are provided. Also provided are exogenous LGIC ligands that can bind to and activate the modified LGIC, as well as methods of modulating ion transport across the membrane of a cell of a mammal, methods of modulating the excitability of a cell in a mammal, and methods of treating a mammal having a channelopathy. | 2020-12-03 |
20200377567 | METHODS OF TREATMENT USING G-CSF PROTEIN COMPLEX - This disclosure provides a method of preventing, alleviating, or treating a condition (i.e., neutropenia) in a patient in need thereof, the condition characterized by compromised white blood cell production in the patient. The method includes administering to the patient a therapeutically effective amount of a protein complex comprising a modified human granulocyte-colony stimulating factor (hG-CSF) covalently linked to an immunoglobulin Fc region via a non-peptidyl polymer. The non-peptidyl polymer is site-specifically linked to an N-terminus of the immunoglobulin Fc region, and the modified hG-CSF comprises substitutions in at least one of Cys17 and Pro65. | 2020-12-03 |
20200377568 | Novel IL-4-/IL-13-derived peptide compounds for the treatment or prevention of neurodegenerative or neuroinflammatory diseases - The present invention relates to a compounds consisting of one or more peptides comprising the structure in the following order: A-L1-B-L2-C wherein A corresponds to a first amino acid sequence that is derived from A or C alpha helical region of human or animal IL-4 or IL-13, B corresponds to a second amino acid sequence that is derived from A or C alpha helical region of human or animal IL-4 or IL-13, C corresponds to a third amino acid sequence that is derived from D or B alpha helical region of human or animal IL-4, or D alpha helical region of human or animal IL-13. L1 and L2 correspond to one or more linking amino acids, wherein said compound is capable of stimulating neuronal axon outgrowth. | 2020-12-03 |
20200377569 | SYNTAC POLYPEPTIDES AND USES THEREOF - Methods and compositions for clonally inhibiting or clonally stimulating T-cells are provided. | 2020-12-03 |
20200377570 | IMPROVED LAMP CONSTRUCTS - The present invention provides improved LAMP Constructs comprising specific fragments of the LAMP lumenal domain to deliver antigens to immune cells for enhanced processing. These LAMP Constructs can be used for the treatment of disease and in particular, allergies, infectious disease, diabetes, hyperproliferative disorders and/or cancer. The improved LAMP Constructs allow for presentation of properly configured three dimensional epitopes for production of an immune response when administered to a subject. The improved LAMP Constructs can be multivalent molecules, and/or can be provided as part of a multivalent vaccine containing two or more LAMP Constructs. The improved LAMP Constructs as described herein can also be used to generate antibodies when administered to a non-human vertebrate. | 2020-12-03 |
20200377571 | MULTISPECIFIC MOLECULES AND USES THEREOF - Multispecific molecules comprising (i) a TGF-beta inhibitor and (ii) a binding moiety that binds to CSF1R or CCR2, and methods of using the same, are disclosed. | 2020-12-03 |
20200377572 | METHOD FOR STABILIZING HEMOGLOBIN-HAPTOGLOBIN COMPLEX AND A PRESERVATION SOLUTION FOR PRESERVING SPECIMENS CONTAINING HEMOGLOBIN - A method for stabilizing a hemoglobin-haptoglobin complex according to the present invention comprises: preserving the hemoglobin-haptoglobin complex in the presence of a degradation product of hemoglobin. According to such a method, the hemoglobin-haptoglobin complex can be stabilized. | 2020-12-03 |
20200377573 | PEPTIDE FOR TREATING AGE-RELATED MACULAR DEGENERATION - It is intended to provide a novel peptide. The present invention provides a peptide which comprises the amino acid sequence shown in SEQ ID NO: 30 and inhibits protease activity. | 2020-12-03 |
20200377574 | IMMUNOGLOBULIN PURIFICATION - The current invention reports a method for purifying an immunoglobulin, wherein the method comprises applying an aqueous, buffered solution comprising an immunoglobulin in monomeric and in aggregated form to a cation exchange material under conditions whereby the immunoglobulin in monomeric form does not bind to the cation exchange material, and recovering the immunoglobulin in monomeric form from the solution after the contact with the cation exchange material. | 2020-12-03 |
20200377575 | HUMAN ANTIBODIES TO INFLUENZA HEMAGGLUTININ - The present invention provides monoclonal antibodies, or antigen-binding fragments thereof, that bind to the influenza hemagglutinin (HA) protein, pharmaceutical compositions comprising the antibodies and methods of use. The antibodies of the invention are useful for inhibiting or neutralizing influenza virus activity, thus providing a means of treating or preventing influenza infection in humans. In some embodiments, the invention provides for use of one or more antibodies that bind to the influenza HA for preventing viral attachment and/or entry into host cells. The antibodies of the invention may be used prophylactically or therapeutically and may be used alone or in combination with one or more other anti-viral agents or vaccines. | 2020-12-03 |
20200377576 | HIV-1 SPECIFIC IMMUNOGEN COMPOSITIONS AND METHODS OF USE - Disclosed herein are methods and compositions for treating a subject having or at risk of having an HIV infection. Disclosed herein are peptide immunogens and nucleic acids that have epitopes in which mutations are most likely to have deleterious effects on the HIV virus. An algorithm is disclosed for the selection of the epitopes based on the HIV fitness landscape, and it accounts for the effect of coupling mutations. | 2020-12-03 |
20200377577 | MULTI-VALENT HUMAN IMMUNODEFICIENCY VIRUS ANTIGEN BINDING MOLECULES AND USES THEREOF - This disclosure provides a multimeric human immunodeficiency virus (HIV) protein binding molecule, e.g., an dimeric IgA or a pentameric or hexameric IgM binding molecule, comprising at least two bivalent binding units, or variants or fragments thereof, each comprising at least two antibody heavy chain constant regions or fragments thereof, wherein each heavy chain constant region or fragment thereof is associated with an HIV antigen binding domain. Also provided are compositions comprising the multimeric binding molecules, polynucleotides encoding the multimeric binding molecules, and methods to make and use the multimeric binding molecules. | 2020-12-03 |
20200377578 | NEUTRALISING ANTIBODIES TO THE MAJOR EXOTOXINS TCDA AND TCDB OF CLOSTRIDIUM DIFFICILE - This present invention describes the derivation and selection of antibodies capable of neutralising the major exotoxins; TcdA and TcdB of | 2020-12-03 |
20200377579 | COMPOSITIONS AND METHODS FOR TREATING SYNUCLEINOPATHIES - Dosage regimens of anti-α-synuclein antibodies are provided. These dosage regimens find use in the treatment of synucleinopathies such as Parkinson's disease (PD), Parkinson's Disease Dementia (PDD), dementia with Lewy bodies (DLB), Lewy body variant of Alzheimer's disease (LBVAD), pure autonomic failure (PAF), multiple system atrophy (MSA), and neurodegeneration with brain iron accumulation type-1 (NBIA-I). | 2020-12-03 |
20200377580 | ANTI-CKAP4 MONOCLONAL ANTIBODY - The purpose of the present invention is to provide an anti-CKAP4 monoclonal antibody that inhibits the binding of DKK1 and CKAP4 and exhibits an exceptional antitumor effect. Provided is an anti-CKAP4 monoclonal antibody that recognizes at least part of the 451-455 region, at least part of the 481-485 region, at least part of the 502-510 region, at least part of the 503-524 region and at least part of the 585-590 region, or at least part of the 585-592 region of the amino acid sequence (amino acid sequence of CKAP4) represented by SEQ ID NO:1 as an epitope, the anti-CKAP4 monoclonal antibody effectively inhibiting the binding of DKK1 and CKAP4, the activation of AKT of S2-CP8 cells, and the proliferative ability of S2-CP8 cells or the migratory ability of S2-CP8 cells, and exhibiting an exceptional antitumor effect. The ability to develop ELISA methods in which these anti-CKAP4 monoclonal antibodies are used furthermore makes it possible, for example, to measure the serum CKAP4 in pancreatic cancer patients, and therefore also contributes to the development of companion diagnostic agents. | 2020-12-03 |
20200377581 | Antagonist Antibodies Directed Against Calcitonin Gene-Related Peptide and Methods Using Same - The invention features methods for preventing or treating CGRP associated disorders such as vasomotor symptoms and/or headaches (e.g., migraine, cluster headache, and tension headache) by administering an anti-CGRP antagonist antibody. Compositions for use in the disclosed methods are also provided. Antagonist antibody G1 and antibodies derived from G1 directed to CGRP are also described. | 2020-12-03 |
20200377582 | HIGH DOSE TREATMENTS FOR ALZHEIMER'S DISEASE - Methods of treating Alzheimer's Disease (AD) in patients suffering from early AD, including amyloid positive patients, ApoE4 positive patients, and patients suffering from prodromal or mild AD are provided. | 2020-12-03 |
20200377583 | METHODS FOR TREATING HYPERLIPIDEMIA WITH AN ANGPTL8 INHIBITOR AND AN ANGPTL3 INHIBITOR - The present invention provides methods for treating patients suffering from hyperlipidemia, wherein the patient is non-responsive to, inadequately controlled by, or intolerant to treatment with a standard lipid modifying therapy. The methods of the invention provide for lowering at least one lipid parameter in the patient by administering a therapeutically effective amount of an antibody or antigen-binding fragment thereof that specifically binds to angiopoietin-like protein 8 (ANGPTL8) in combination with a therapeutically effective amount of an antibody that specifically binds to angiopoietin-like protein 3 (ANGPTL3). The combination of an anti-ANGPTL8 antibody with an anti-ANGPTL3 antibody is useful in treating diseases such as hypercholesterolemia, including familial hypercholesterolemia (FH), both heFH and hoFH, as well as hyperlipidemia, hyperlipoproteinemia and dyslipidemia, including hypertriglyceridemia, chylomicronemia, and to prevent or treat diseases or disorders, for which abnormal lipid metabolism is a risk factor, such as cardiovascular diseases. | 2020-12-03 |
20200377584 | IL-17A/F HETEROLOGOUS POLYPEPTIDES AND THERAPEUTIC USES THEREOF - The present invention is directed to a novel naturally occurring human cytokine that is comprised of a heterodimer of interleukin-17 and interleukin-17F designated herein as interleukin 17A/F (IL-17A/F). Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, specific antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Further provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases. | 2020-12-03 |
20200377585 | IL-17A/F HETEROLOGOUS POLYPEPTIDES AND THERAPEUTIC USES THEREOF - The present invention is directed to a novel naturally occurring human cytokine that is comprised of a heterodimer of interleukin-17 and interleukin-17F designated herein as interleukin 17A/F (IL-17A/F). Also provided herein are vectors and host cells comprising those nucleic acid sequences, chimeric polypeptide molecules comprising the polypeptides of the present invention fused to heterologous polypeptide sequences, specific antibodies which bind to the polypeptides of the present invention and to methods for producing the polypeptides of the present invention. Further provided herein are methods for treating degenerative cartilaginous disorders and other inflammatory diseases. | 2020-12-03 |
20200377586 | IL-18 BINDING PROTEIN (IL-18BP) AND ANTIBODIES IN INFLAMMATORY DISEASES - The present invention provides means and methods for treating Interleukin 18 (IL-18)-associated diseases and disorders. In particular, the present invention discloses antibodies specific for free IL-18 and IL-18 Binding Protein (IL-18BP) for use in such treatments and for the diagnosis of the diseases and disorders. | 2020-12-03 |
20200377587 | IL8 Blocking EMT Pathway and Overcoming Cancer Stem Cells - Compositions, methods, and uses of recombinant IL-8 antibody, fragment thereof or single chain variable fragment (scFv) having high affinity to IL-8 to target tumor-expressed or endogenous IL-8 are presented. Preferably, the recombinant IL-8 antibody or scFv fragment includes a V | 2020-12-03 |
20200377588 | Highly Versatile Method of Presenting Cyclic Peptide on Protein Structure - The present invention provides a method of presenting a cyclic peptide on a protein having a loop structure. The cyclic peptide has a chemically crosslinked structure for forming an intramolecular cyclic structure. The method includes replacing the chemically crosslinked structure of the cyclic peptide with two amino acid residues constituting the loop structure, thereby fusing the cyclic peptide with the protein having a loop structure. | 2020-12-03 |
20200377589 | TARGETING CYTOTOXIC CELLS WITH CHIMERIC RECEPTORS FOR ADOPTIVE IMMUNOTHERAPY - The present invention provides compositions and methods for regulating the specificity and activity of immune effector cells for use in immunotherapy. In one embodiment, the invention provides a type of chimeric antigen receptor (CAR) wherein the CAR is termed a “NKR-CAR” which is a CAR design comprising a component of a receptor naturally found on natural killer (NK) cells. In one embodiment, the NK receptor includes but is not limited to a naturally occurring activating and inhibitory receptor of NK cells known as a killer cell immunoglobulin-like receptor (KIR). | 2020-12-03 |
20200377590 | VH-VL INTERDOMAIN ANGLE BASED ANTIBODY HUMANIZATION - Herein is reported a method for selecting one or more variant antibody Fv fragments derived from a parent antibody Fv fragment comprising the steps of i) generating a multitude of variant antibody Fv fragments by grafting/transferring one or more specificity determining residues from the parent antibody Fv fragment on an acceptor antibody Fv fragment, whereby each variant antibody Fv fragment of the multitude of variant antibody Fv fragments differs from the other variant antibody Fv fragments by at least one amino acid residue, ii) determining the VH-VL-orientation for the parent Fv fragment and for each of the variant antibody Fv fragments of the multitude of variant antibody Fv fragments based on a sequence fingerprint of the antibody Fv fragment, and iii) selecting those variant antibody Fv fragments that have the smallest difference in the VH-VL-orientation compared to the parent antibody's VH-VL-orientation and thereby selecting one or more variant antibody Fv fragments derived from a parent antibody Fv fragment, whereby the one or more variant antibody Fv fragments bind to the same antigen as the parent antibody Fv fragment. | 2020-12-03 |