18th week of 2021 patent applcation highlights part 29 |
Patent application number | Title | Published |
20210130347 | HETEROARYL-BIPHENYL AMINES FOR THE TREATMENT OF PD-L1 DISEASES - Compounds are provided that are useful as immunomodulators. The compounds have the Formula (I) | 2021-05-06 |
20210130348 | POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1 - Described are positive allosteric modulators of muscarinic acetylcholine receptor M | 2021-05-06 |
20210130349 | NOVEL PHOSPHODIESTERASE INHIBITORS AND USES THEREOF - The invention provides for novel benzonaphthyridine derivatives and compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the compounds are phosphodiesterase inhibitors. The invention further provides for methods for inhibition of phosphodiesterase comprising contacting phosphodiesterase with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. The invention further provides for methods for treatment of neurodegenerative diseases, increasing memory or long term potentiation with novel benzonaphthyridine derivatives or compositions comprising novel benzonaphthyridine derivatives. In some embodiments, the phosphodiesterase is PDE5. | 2021-05-06 |
20210130350 | Solid State Forms Of Venetoclax And Its Process For The Preparation There Of - The present invention provides solid state forms of Venetoclax, particularly relates to novel alkali metal salt and/or DMF solvate form of Venetoclax or its salt. The present invention also relates to process for the preparation Venetoclax by using the said solid state form of Venetoclax. | 2021-05-06 |
20210130351 | JAK KINASE INHIBITOR COMPOUNDS FOR TREATMENT OF RESPIRATORY DISEASE - The invention provides compounds of formula (I): | 2021-05-06 |
20210130352 | OGA INHIBITOR COMPOUNDS - The present invention relates to O-GlcNAc hydrolase (OGA) inhibitors. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention and treatment of disorders in which inhibition of OGA is beneficial, such as tauopathies, in particular Alzheimer's disease or progressive supranuclear palsy; and neurodegenerative diseases accompanied by a tau pathology, in particular amyotrophic lateral sclerosis or frontotemporal lobe dementia caused by C9ORF72 mutations. | 2021-05-06 |
20210130353 | FGFR INHIBITOR AND APPLICATION THEREOF - An azatricyclic compound (as represented by formula I) which acts as an inhibitor of fibroblast growth factor receptors (FGFR), as well as a pharmaceutical composition thereof, a preparation method, and a use therefor in the treatment of FGFR-mediated diseases. The azatricyclic compound exerts an effect by means of participating in the regulation of a plurality of processes such as cell proliferation, apoptosis, migration, neovascularization, and the like. AA %%% Formula (I). | 2021-05-06 |
20210130354 | MULTI-KINASE INHIBITOR COMPOUND, AND CRYSTAL FORM AND USE THEREOF - The present invention relates to a method for treating a cancer mediated by abnormality of multi-kinases, comprising administrating a compound as represented by formula (I) or a pharmaceutically acceptable salt and stereoisomer thereof, wherein R | 2021-05-06 |
20210130355 | COMPOUND, ELECTRON TRANSPORT MATERIAL, DISPLAY PANEL AND DISPLAY APPARATUS - The present disclosure provides a compound having a structure represented by Formula 1, where X | 2021-05-06 |
20210130356 | 6-DITHIO-SUBSTITUTED-2'-DEOXYGUANOSINE COMPOUND, PREPARATION METHOD THEREOF AND USE THEREOF - The present invention provides a 6-dithio-substituted-2′-deoxyguanosine compound and a preparation method thereof and use thereof in anti-tumor drugs. According to the present invention, a series of brand-new thioredoxin-1 (Trx-1) inhibitors are designed and synthesized by using 2′-deoxyguanosine as a structure mother nucleus. The compound according to the present invention is a structure of formula I, and Trx-1 activity inhibition testing is performed on the type of compounds, showing apparent inhibitory activity. It is indicated from in vitro and vivo researches that these compounds show significant anti-tumor effects on multiple types of tumors, can be applied to drugs for tumors related to human body cell proliferation, and provide a new path for the research of anticancer drugs. | 2021-05-06 |
20210130357 | FGFR INHIBITOR - Disclosed are an FGFR inhibitor and the use thereof in the preparation of a drug for treating FGFR-related diseases. In particular, disclosed are a compound as shown in formula (I) and a pharmaceutically acceptable salt thereof. | 2021-05-06 |
20210130358 | Pyrrolotriazine Derivatives as Kinase Inhibitor - The present invention relates to a compound represented by the Chemical Formula 1 defined in the present specification, or a pharmaceutically acceptable salt thereof. The compound according to the present invention can be usefully used for the prevention or treatment of diseases which are associated with kinase inhibitory actions. | 2021-05-06 |
20210130359 | SULFONYLUREAS AND SULFONYLTHIOUREAS AS NLRP3 INHIBITORS - The present invention relates to sulfonylureas and sulfonylthioureas comprising a 5-membered nitrogen-containing heteroaryl ring attached to the sulfonyl group, wherein the heteroaryl ring is substituted with a nitrogen-containing group R | 2021-05-06 |
20210130360 | Crystalline Forms of Acalabrutinib - The present invention provides crystalline forms of Acalabrutinib, Specific crystalline forms provided by the present invention include Acalabrutinib Form APO-I, a co-crystal of Acalabrutinib and urea; APO-II, a co-crystal of Acalabrutinib and nicotinamide; APO-III, a co-crystal of Acalabrutinib and L-sorbitol; APO-IV, a crystalline form of Acalabrutinib; and APO-V, a co-crystal of Acalabrutinib and urea. | 2021-05-06 |
20210130361 | TGF- INHIBITORS - Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure | 2021-05-06 |
20210130362 | MEDICAL USE OF COMPOUND III - The present invention relates to compound III | 2021-05-06 |
20210130363 | CRYSTALLINE FORM OF (S)-7-(1-ACRYLOYLPIPERIDIN-4-YL)-2-(4-PHENOXYPHENYL)-4,5,6,7-TETRA-HYDROP- YRAZOLO[1,5-a]PYRIMIDINE-3-CARBOXAMIDE, PREPARATION, AND USES THEREOF - The present invention relates to a crystalline form of (S)-7-(1-acryloylpiperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetra-hydropyrazolo[1,5-a]pyrimidine-3-carboxamide for inhibiting Btk, methods of preparation thereof and pharmaceutical compositions, and use of the crystalline form above in the treatment of a disease, or in the manufacturing of a medicament for the treatment of a disease. | 2021-05-06 |
20210130364 | SPIRO-CYCLIC AMINE DERIVATIVES AS S1P MODULATORS - The present invention relates spiro-cyclic amine derivatives of the formula (I) wherein R1; R2; R3; Q; —W-T-; R5; Z; and A have the definitions provided in the claims; or a pharmaceutically acceptable salt, a solvate or hydrate thereof or one or more N-oxides thereof. The compounds of the invention have affinity to S1P receptors and may be used in the treatment, alleviation or prevention of diseases and conditions in which (a) S1P receptor (s) is (are) involved. | 2021-05-06 |
20210130365 | 2-AZASPIRO[3.4]OCTANE DERIVATIVES AS M4 AGONISTS - Provided herein are compounds according to Formula (I) | 2021-05-06 |
20210130366 | PDE9 INHIBITOR AND USE THEREOF - The present invention falls within the technical field of medicine, and in particular relates to PDE9 inhibitor compounds as shown in formula (I) or pharmaceutically acceptable salts or stereoisomers thereof, and also relates to pharmaceutical preparations and pharmaceutical compositions of the compounds and the uses thereof. X | 2021-05-06 |
20210130367 | 6H-THIENO[2,3-e][1,2,4]TRIAZOLO[3,4-c][1,2,4]TRIAZEPINE DERIVATIVE - The 6H-thieno[2,3-e][1,2,4]triazolo[3,4-c][1,2,4]triazepine derivatives or salts thereof of the present invention have BRD4 inhibitory activity, and thus, they are useful as medicaments, in particular, as prophylaxis and/or therapeutic agents for diseases associated with BRD4. | 2021-05-06 |
20210130368 | HETEROBIFUNCTIONAL COMPOUNDS WITH IMPROVED SPECIFICITY - Disclosed are heterobifunctional compounds that effectuate selective degradation of a target protein, and which include a targeting ligand that binds a target protein and at least one other protein, a ligand that binds an E3 ubiquitin ligase or a component of E3 ubiquitin ligase, and a specificity modulating linker that links the first ligand and the second ligand. Pharmaceutical compositions containing the compounds, and methods of using and making the compounds are also disclosed. | 2021-05-06 |
20210130369 | RAS INHIBITORS - The disclosure features macrocyclic compounds, and pharmaceutical compositions and protein complexes thereof, capable of inhibiting Ras proteins, and their uses in the treatment of cancers. | 2021-05-06 |
20210130370 | MITORIBOSCINS: MITOCHONDRIAL-BASED THERAPEUTICS TARGETING CANCER CELLS, BACTERIA, AND PATHOGENIC YEAST - The present disclosure relates to inhibitors of mitochondrial function. Methods of screening compounds for mitochondrial inhibition are disclosed. Also described are methods of using mitochondrial inhibitors called mitoriboscins—mitochondrial-based therapeutic compounds having anti-cancer and antibiotic properties—to prevent or treat cancer, bacterial infections, and pathogenic yeast, as well as methods of using mitochondrial inhibitors to provide anti-aging benefits. Specific mitoriboscin compounds and groups of mitoriboscins are also disclosed. | 2021-05-06 |
20210130371 | PYRUVATE KINASE ACTIVATORS FOR USE IN TREATING BLOOD DISORDERS - Described herein are compounds that activate pyruvate kinase R, pharmaceutical compositions and methods of use thereof. These compounds are represented by Formula (I): wherein R | 2021-05-06 |
20210130372 | BRANCHED METAL-ORGANIC FRAMEWORK NANOPARTICLES AND ASSOCIATED METHODS - Compositions and methods relating to compositions that include metal-organic frameworks are generally described. In some embodiments, branched nanoparticles made at least in part of metal-organic frameworks are described. In some embodiments, the morphology and size of the branched nanoparticles are controlled by the presence of a chemical modulator during synthesis. | 2021-05-06 |
20210130373 | COMPOUND AND FILM AND PHOTOELECTRIC DIODE AND ORGANIC SENSOR AND ELECTRONIC DEVICE - Disclosed are a compound represented by Chemical Formula 1, a film, a photoelectric diode, an organic sensor, and an electronic device. | 2021-05-06 |
20210130374 | CATALYSIS OF DEHYDROCOUPLING REACTIONS BETWEEN AMINES AND SILANES - A method for dehydrocoupling silanes and amines. The method comprises contacting: (a) an aliphatic amine; (b) a silane; and (c) a catalyst which is ZnX | 2021-05-06 |
20210130375 | METHOD FOR PRODUCING TRICHLOROSILYLSULFIDE ANION AND ITS USE IN THE PREPARATION OF ORGANOSULFUR COMPOUNDS - Preparation of sulfur fine chemicals from sulfur sources is described. | 2021-05-06 |
20210130376 | BETA-AMINO PHOSPHONIC ACID DERIVATIVE AND PREPARATION METHOD THEREFOR - A method for preparing a β-amino phosphonic acid derivative includes: dissolving N-(arylvinyl)benzamide, dialkyl phosphite, manganese acetate, and potassium carbonate in a solvent and reacting at room temperature to obtain (2-benzamido-1-arylvinyl)dialkyl-phosphonate derivative; and hydrolyzing (2-benzamido-1-arylethyl) dialkylphosphonate derivative to obtain β-amino phosphonic acid derivative. The N-(arylvinyl) benzamide derivative is used as starting material. The raw materials are easy to obtain and are of many different types. A method of preparing β-aminophosphonic acid derivative includes: dissolving N-(arylvinyl)benzamide, dialkyl phosphite, manganese acetate and potassium carbonate in a solvent, reacting at room temperature to obtain (2-benzamide-1-arylvinyl) dialkyl phosphonate derivative, and then reducing and hydrolyzing the compound to obtain β-aminophosphonic acid derivative. The method of the invention has the advantages of short synthesis route, mild reaction conditions, simple reaction operation and post-treatment process, good yield, and is suitable for large-scale production. | 2021-05-06 |
20210130377 | BETA-PHOSPHONYL-ENAMINE DERIVATIVE AND PREPARATION METHOD THEREFOR - The present invention discloses the preparation method of β-phosphonyl-enamine derivative. The preparation method comprising the following steps: dissolving the enamine derivative, organic phosphine compound, manganese acetate and potassium carbonate in the solvent, reacting at room temperature to obtain the β-phosphonyl-enamine derivative. The enamine derivative was as the starting material, and the raw materials are easy to obtain and a great many varieties. The various forms of the products obtained therein can be directly applied and can be used in further reactions. The reaction conditions are mild, the reaction speed is high, the reaction operation and the post-treatment process are simple, the production is convenient, and the method is suitable for large-scale production. | 2021-05-06 |
20210130378 | PHOSPHINE OXIDE COMPOUND, RARE EARTH COMPLEX, AND LIGHT-EMITTING MATERIAL - A phosphine oxide compound represented by the following formula (I) and a rare earth complex containing the same are disclosed: | 2021-05-06 |
20210130379 | SYNTHESIS OF FMOC-PROTECTED MORPHOLINO MONOMERS AND THEIR USE IN THE SYNTHESIS OF MORPHOLINO OLIGOMER - Present invention relates to stable Fmoc protected Morpholino monomers and corresponding oligonucleotides (PMO) and efficient synthesis of the same involving chlorophosphoramidate and H-Phosphonate chemistry. Successful syntheses of the oligonucleotide with higher yield and lesser time have been accomplished employing solid phase synthesis and easy deprotection of Fmoc group with Piperidine. | 2021-05-06 |
20210130380 | PHOSPHONIUM ION CHANNEL BLOCKERS AND METHODS FOR USE - The invention provides compounds of Formula (I), or pharmaceutically acceptable salts thereof: | 2021-05-06 |
20210130381 | One-Step Synthesis of Phosphate-Based Inhibitors and Applications Thereof - One-step methods for forming phosphate-based enzyme inhibitors are disclosed. Methods include reacting o-phosphorylethanolamine with an acyl chloride at acidic conditions. Acyl chlorides can be derivatized. The phosphate-based enzyme inhibitors can inhibit enzymes of the pentose phosphate pathway including D-ribose-5-phosphate aldose-ketose isomerase enzymes such as | 2021-05-06 |
20210130382 | ORGANOMETALLIC COMPOUND, ORGANIC LIGHT EMITTING DIODE AND ORGANIC LIGHT EMITTING DEVICE INCLUDING THE SAME - The present disclosure provides an organometallic compound below and an organic light emitting diode and an organic light emitting display device including the organometallic compound. | 2021-05-06 |
20210130383 | ORGANIC ELECTROLUMINESCENT MATERIAL AND DEVICE - A compound having a first ligand of the following | 2021-05-06 |
20210130384 | PROCESS FOR PRODUCING 2'-O-FUCOSYLLACTOSE - The present invention relates to a method for preparing 2′-O-fucosyllactose, the intermediates obtainable by this method and the use of these intermediates. The preparation comprises the reaction of a protected fucose of the general formula (I) with a tri(C | 2021-05-06 |
20210130385 | SURFACTANT COMPOUNDS-CLIPS FOR EXTRACTION AND STABILIZATION IN SOLUTION OF MEMBRANE PROTEINS - The present invention relates to a compound of formula (I): (I) as defined in the description. The present invention also relates to a method for extracting biological membrane-associated membrane proteins, comprising a step of bringing an aqueous solution of biological membrane-associated membrane proteins into contact with at least one compound of the invention. The present invention also relates to a method for stabilizing membrane proteins in solution in an aqueous solution, comprising a step (i) consisting in bringing an aqueous solution of a membrane protein in solution into contact with at least one compound of the invention. | 2021-05-06 |
20210130386 | DOT1L DEGRADERS AND USES THEREOF - Provided herein are bifunctional compounds with a moiety (e.g., lenalidomide, thalidomide) that is a binder of an E3 ubiquitin ligase (e.g., Cereblon) and another moiety that is a binder of a target protein DOT1L to induce degradation of DOT1L. Also provided are pharmaceutical compositions comprising the bifunctional compounds, and methods of treating and/or preventing diseases (e.g., proliferative diseases, such as cancers). Provided also are methods of inducing the degradation of DOT1L by administering a bifunctional compound or composition described herein, wherein one component of the bifunctional compound is a binder of an E3 ubiquitin ligase (e.g., lenalidomide, thalidomide) and another component of the compound is a binder of the target protein DOT1L in a subject. | 2021-05-06 |
20210130387 | PHOSPHORAMIDATE NUCLEOSIDE DERIVATIVES AS ANTICANCER AGENTS - This invention relates to derivatives of cladribine. The compounds are phosphoramidate derivatives in which the phosphoramidate moiety is situated on the 3′-hydroxyl group of cladribine. The invention also relates to pharmaceutical formulations of the cladribine derivatives and their use in methods of treatment. The compounds are useful in the treatment of cancer. | 2021-05-06 |
20210130388 | SELECTIVE INHIBITORS OF PROTEIN ARGININE METHYLTRANSFERASE 5 (PRMT5) - The disclosure is directed to compounds of Formula I, Formula II, Formula III, Formula IV, Formula V, or Formula VI: Methods of their use in inhibiting a protein arginine methyltransferase 5 (PRMT5) enzyme and treating disease, as well as methods of their preparation are also described. | 2021-05-06 |
20210130389 | CD73 INHIBITORS - Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases. | 2021-05-06 |
20210130390 | CD73 INHIBITORS - Described herein are CD73 inhibitors and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of cancer, infections, and neurodegenerative diseases. | 2021-05-06 |
20210130391 | METHODS FOR TARGETED PROTEIN QUANTIFICATION BY BAR-CODING AFFINITY REAGENT WITH UNIQUE DNA SEQUENCES - Provided herein are affinity reagents having affinity for particular target, each reagent having a unique DNA barcode, and methods for using the same to measure the abundance of targets in a sample. In particular, methods are provided in which unique barcodes linked to affinity reagents are contacted to a sample to bind antigens if present in said sample. In cases in which the affinity reagents are antibodies and the targets are antigens, antibodies that are bound to their target antigens can be separated from unbound antibodies and the DNA barcode associated with the affinity reagent is amplified, such as with a PCR reaction. In some cases, amplified barcode DNA is subjected to DNA sequencing as a measure of the levels of the target protein in the sample. | 2021-05-06 |
20210130392 | USE OF STEROIDAL GLYCOSIDES, PHARMACEUTICAL FORMULATIONS, USE OF FURCRAEA FOETIDA PLANT EXTRACTS, PROCESS FOR PRODUCING FURCRAEA FOETIDA PLANT EXTRACTS AND METHOD FOR TREATING SKIN DISORDERS - The present invention relates, in its broadest aspects, to steroidal glycosides useful in the treatment of skin disorders. Particularly, the invention relates to the use of certain steroidal glucosides, per se, or in the form aglycona, derivatives of spirostanol, of its precursor furastanol, or mixtures thereof, used in the treatment of skin disorders, for instance, psoriasis. The invention further relates to formulations containing steroidal glycosides, the process of obtaining extract from the | 2021-05-06 |
20210130393 | METHOD FOR PRODUCING AMIDE - A method for producing an amide includes: dehydrating and condensing carboxylic acids and then reacting them with a base, and reacting them with an amine. | 2021-05-06 |
20210130394 | PREPARATION OF BIOLOGICALLY ACTIVE COMPLEXES - The invention provides a method for preparing a biologically active complex, said method comprising dissolving a mixture of a polypeptide element, such as alphalactalbumin or fragments thereof, in powder form and oleic acid or a pharmaceutically acceptable salt thereof also in solid form, in an aqueous solvent comprising a mixture of at least two and preferably three salts, wherein the method is carried out at moderate temperatures. The preparation does not require extensive heating and so is simple and efficient to carry out. | 2021-05-06 |
20210130395 | PROXIMITY INDUCED SITE-SPECIFIC ANTIBODY CONJUGATION - The present disclosure provides methods for proximity-induced antibody conjugation of target agents). | 2021-05-06 |
20210130396 | METHOD FOR PURIFYING PROTEINS - The present invention relates to a method for purifying proteins, such as Fc fusion proteins or antibodies, from a sample comprising said proteins and impurities, through the use of a three-chromatographic columns procedure, including a chromatography on hydroxyapatite- and/or Fluorapatite-containing material. The invention is also concerned with pharmaceutical compositions comprising the purified proteins obtainable by the process of the invention. | 2021-05-06 |
20210130397 | METHODS FOR PURIFYING ANTIBODIES HAVING REDUCED HIGH MOLECULAR WEIGHT AGGREGATES - Provided herein, in some embodiments, are methods and compositions for purifying antibodies from cellular cultures using one or more thiol containing additives during a purification process, for example in a chromatographic purification process. | 2021-05-06 |
20210130398 | PROTEIN PURIFICATION - A method for purifying a polypeptide by ion exchange chromatography is described in which a gradient wash is used to resolve a polypeptide of interest from one or more contaminants. | 2021-05-06 |
20210130399 | PROTEIN PURIFICATION - A method for purifying a polypeptide by ion exchange chromatography is described in which a gradient wash is used to resolve a polypeptide of interest from one or more contaminants. | 2021-05-06 |
20210130400 | NUCLEANT ENHANCING NUCLEATION OF A PROTEIN CRYSTAL AND PROTEIN CRYSTALLIZATION METHOD WITH THE SAME - A balanced-lattice-ledge nucleant having ledge inducing local densification of proteins and a balanced-lattice inducing self-organized crystal packing. Using this balanced-lattice-ledge nucleant enhances nucleation of protein crystals. | 2021-05-06 |
20210130401 | PEPTIDOMIMETIC INHIBITORS OF THE WDR5-MLL INTERACTION - The present disclosure provides compounds represented by Formula I: and the pharmaceutically acceptable salts and solvates thereof, wherein R | 2021-05-06 |
20210130402 | AROMATIC-CATIONIC PEPTIDES AND USES OF SAME - The disclosure provides compositions and methods relating to aromatic-cationic peptides. The methods comprise administering to the subject an effective amount of an aromatic-cationic peptide to subjects in need thereof. For example, the peptides may be administered to subjects in need of a mitochondrial-targeted antioxidant. | 2021-05-06 |
20210130403 | INHIBITORS OF METASTASIS - The present invention relates to methods and compounds for treating or preventing cancer. Methods and compositions provided include including inhibiting or suppressing the development, maintenance, and proliferation of cancers, including blocking or inhibiting cancer cell metastasis. | 2021-05-06 |
20210130404 | PEPTIDE TAG AND TAGGED PROTEIN INCLUDING SAME - A peptide comprising the sequence shown below is added as a peptide tag to a useful protein, followed by allowing its expression. | 2021-05-06 |
20210130405 | NEW STAPLED PEPTIDES AND USES THEREOF - The present invention relates to peptidomimetic macrocycles comprising at least one macrocycle-forming linker and an amino acid sequence chosen from the group consisting of: i) an amino acid sequence with at least about 50%, 60%, 70%, 80%, 90%, or 95% sequence identity to a human sequence IRAK2 54-71 (SEQ ID No 1) and 100% identity with the amino acids in the positions 5-6, 9-11, 14-15 or ii) an amino acid sequence with at least about 50%, 60%, 70, 80%, 90%, or 95% sequence identity to a human sequence IRAKM 66-83 (SEQ ID No2) and 100% identity with the amino acids in the positions 5-6, 9-11, 13-14, wherein the peptidomimetic macrocycle comprises an α-helix and at least two natural or two non-natural amino acids crosslinked by a macrocycle-forming linker. It also concerns method of preparation of said peptidomimetic macrocycles and uses thereof, pharmaceutical composition and uses thereof, in particular as inhibitors of inflammatory pathways. | 2021-05-06 |
20210130406 | PEPTIDE, COMPOSITION, AND METHOD FOR TREATING, PREVENTING, OR AMELIORATING MOOD DISORDER - The present invention addresses the problem of providing a novel peptide capable of treating, preventing, or ameliorating a mood disorder. The present invention provides a peptide having an amino acid sequence represented by SEQ ID NO: 1 and having an amino acid length of 6 to 20. | 2021-05-06 |
20210130407 | SYNTHETIC PEPTIDES THAT MODULATE THE NMDA RECEPTOR - The invention provides a series of peptides with N-methyl-D-aspartate (NMDA) receptor modulating activity. Specifically it contains two synthetic peptides acting as ion inflow antagonists through the NMDA receptor with specificity GluN2B and GluN2A NMDA receptor subunits and a peptide having agonist activity regarding the NMDA receptor in rat hippocampal neuron cultures. | 2021-05-06 |
20210130408 | COMPOUND AND METHOD FOR PRODUCING THE SAME - Disclosed is a method for producing a compound, the method including polymerizing an amino acid carboxyanhydride-based compound using a catalyst. The method for producing the compound may improve a polymerization reaction rate and provide a compound having a narrower molecular weight distribution and having a polymer ring structure bonded to the catalyst. | 2021-05-06 |
20210130409 | Method for the Solid-Phase Synthesis of Cyclic Pentapeptides - A method for the synthesis of a cyclic ornithine-proline-D-cyclohexylalanine-tryptophan-arginine pentapeptide of Formula A; | 2021-05-06 |
20210130410 | CYCLIC PEPTIDES AND USES THEREOF - The present disclosure is directed to a peptide of formula (I), or a pharmaceutically acceptable salt thereof, and uses thereof: R | 2021-05-06 |
20210130411 | CYCLIC HEXAPEPTIDES COMPOUNDS WITH ANTI-MALARIAL ACTIVITY - The present invention relates generally to compositions for medical treatment of malaria. In particular, the present invention relates to novel cyclic hexapeptides compounds of formula (I) with anti-malarial activity, a method for the synthesis of said compounds and pharmaceutical compositions containing said cyclic hexapeptides compounds which are useful for treating malaria. | 2021-05-06 |
20210130412 | METHOD FOR SYNTHESIZING AMANITINS - The invention relates to novel methods for synthesizing amanitin derivatives having a hydroxy group attached to the central tryptophan moiety. The invention furthermore relates to novel amanitin derivatives having a hydroxy group attached to position 4′, 5′ or 7′ of the central tryptophan moiety, novel conjugates of such amanitin derivatives, and pharmaceutical compositions comprising such conjugates. | 2021-05-06 |
20210130413 | MODIFIED AAV CAPSIDS AND USES THEREOF - The present disclosure provides modified adeno-associated virus (AAV) virions with altered capsid proteins, where the modified AAV virions exhibit greater infectivity of retinal cells when administered to the eye or greater infectivity of liver cells when administered intravenously. The present disclosure further provides methods of delivering a gene product to a retinal cell in an individual, methods of treating ocular diseases and disorders, methods of delivering a gene product to the liver in an individual, and methods of treating liver diseases and disorders. | 2021-05-06 |
20210130414 | TREATING CANCER WITH VIRAL NUCLEIC ACID - This document provides methods and materials related to the use of nucleic acid coding for viruses to reduce the number of viable cancer cells within a mammal. For example, methods for using infectious nucleic acid to treat cancer, engineered viral nucleic acid, methods for making engineered viral nucleic acid, methods for identifying infectious nucleic acid for treating cancer, methods and materials for controlling virus-mediated cell lysis, and methods and materials for assessing the control of virus-mediated cell lysis are provided. | 2021-05-06 |
20210130415 | CHEMICALLY-MODIFIED ADENO-ASSOCIATED VIRUS - The invention relates to chemically modified adeno-associated (AAV) virus and their use in gene therapy. | 2021-05-06 |
20210130416 | METHODS OF OPTIMIZING NUCLEOTIDE SEQUENCES ENCODING ENGINEERED INFLUENZA PROTEINS - The disclosure provides methods for generating an optimized nucleotide sequence encoding an engineered influenza structural protein and the optimized nucleotide sequences obtained therefrom. The optimized nucleotide sequences can be used in a reverse genetics system to facilitate the rescue of infectious influenza virus containing the engineered structural proteins and/or enhance viral titers. Also provided are methods of preparing an influenza vaccine composition using the optimized nucleotide sequences, as well as methods of inducing an immune response using the influenza vaccine composition. | 2021-05-06 |
20210130417 | SYSTEMS AND METHODS FOR DESIGNING SYNTHETIC ANTIMICROBIAL PEPTIDES - Methods for generating synthetic antimicrobial peptides include (i) identifying a peptide fragment of an antimicrobial peptide that includes a cluster of cationic residues and at least about 25% hydrophobic residues, preferably between about 40%-60% hydrophobic residues and (ii) generating a peptide variant library based on the peptide fragment by varying a hydrophobicity and charge of residues that make up the peptide fragment. Resulting synthetic peptides can include linear synthetic peptide variants of an AS-48-like bacteriocin having increased antimicrobial activity. | 2021-05-06 |
20210130418 | CLAUDIN-TARGETING AGENTS AND USES THEREOF - There are provided polypeptide constructs targeting claudin proteins that are useful for transiently disrupting tight junctions in a tissue. Pharmaceutical compositions and uses thereof in methods for enhancing delivery of therapeutic agents, for stem cell transplantation, and for treatment of male infertility are also provided. | 2021-05-06 |
20210130419 | TUMOR HOMING AND CELL PENETRATING PEPTIDE-IMMUNO-ONCOLOGY AGENT COMPLEXES AND METHODS OF USE THEREOF - Peptide-immuno-oncology agent complexes (“peptide-I/O complexes”) that can home, target, migrate to, are directed to, are retained by, accumulate in, penetrate, or bind to the tumor microenvironment, tumor tissues, or cells or compartments or cytosol of cells thereof, or any combination thereof, are disclosed. Additionally disclosed are peptide-I/O complexes that can cross the blood-brain barrier. Pharmaceutical compositions and uses for peptide-I/O complexes comprising such peptides are also disclosed. Such compositions can be formulated for targeted delivery of an immuno-oncology agent (“I/O”) to the tumor microenvironment. Targeted compositions of the disclosure can deliver peptide-I/O complexes to target regions, tissues, structures or cells targeted by the peptide. | 2021-05-06 |
20210130420 | RECOMBINANT BINDING PROTEINS TARGETING HER2 AND SERUM ALBUMIN, AND THEIR USES - New recombinant binding proteins, comprising designed ankyrin repeat domain(s) with binding specificity for HER2, and comprising designed ankyrin repeat domain(s) with binding specificity for serum albumin, are disclosed, as well as nucleic acids encoding such recombinant binding proteins, pharmaceutical compositions comprising such recombinant binding proteins or nucleic acids and the use of such recombinant binding proteins, nucleic acids or pharmaceutical compositions in the treatment of diseases. | 2021-05-06 |
20210130421 | DUAL-AAV VECTOR-BASED SYSTEMS AND METHODS FOR DELIVERING OVERSIZED GENES TO MAMMALIAN CELLS - Disclosed are materials and methods for treating diseases of the mammalian eye, and in particular, Usher syndrome 1B (USH1B). The invention provides AAV-based, dual-vector systems that facilitate the expression of full-length proteins whose coding sequences exceed that of the polynucleotide packaging capacity of an individual AAV vector. In one embodiment, vector systems are provided that include i) a first AAV vector polynucleotide that includes an inverted terminal repeat at each end of the polynucleotide and a suitable promoter followed by a partial coding sequence that encodes an N-terminal portion of a full-length polypeptide: and ii) a second AAV vector polynucleotide that includes an inverted terminal repeat at each end of the polynucleotide and a partial coding sequence that encodes a C-terminal portion of a full-length polypeptide, optionally followed by a polyadenylation (pA) signal sequence. In another embodiment, the vector system includes i) a first AAV vector polynucleotide comprising an inverted terminal repeat at each end, a suitable promoter followed by a partial coding sequence that encodes an N-terminal portion of a full-length polypeptide followed by a splice donor site and intron and ii) a second AAV vector polynucleotide comprising an inverted terminal repeat at each end, followed by an intron and a splice-acceptor site for the intron, followed by a partial coding sequence that encodes a C-terminal portion of a full-length polypeptide, optionally followed by a polyadenylation (pA) signal sequence. The coding sequence or the intron sequence in the first and second AAV vectors preferably includes a sequence region that overlaps. | 2021-05-06 |
20210130422 | Novel Fusion Protein, and Pharmaceutical Composition For Preventing Or Treating Cancer, Containing Same - The present invention relates to a fusion protein comprising an extracellular domain of leucine-rich and immunoglobulin-like domains-1 (Lrig-1) protein and an immunoglobulin Fc region. The fusion protein provided in the present invention can interact with a ligand for Lrig-1 protein, which is present on effector T cells, to inhibit the interaction between the effector T cells and regulatory T cells (Treg cells) having the Lrig-1 protein on their surface, so that activity of the regulatory T cells is inhibited and activity of the effector T cells is maintained or elevated, thereby effectively inhibiting growth of cancer cells, in particular, solid cancer cells. | 2021-05-06 |
20210130423 | COMPOSITION FOR IMPROVING SKIN CONDITIONS COMPRISING A FRAGMENT OF HUMAN HEAT SHOCK PROTEIN 90A AS AN ACTIVE INGREDIENT - Liposomal and/or nano-liposomal encapsulated peptides of HSP90a, HPf polypeptide (115 aa) and novel polypeptides HPfΔC1 (101 aa) and HPfΔC2 (87 aa), and methods for manufacturing/preparing and using the compositions, are disclosed. Chimeric fusion proteins that include HSP90a, HPf, HPfAC, HPfAC2 polypeptide, or combinations thereof, are presented. Transformed cell lines and expression vectors capable of expressing the chimeric fusion proteins, are provided. Methods for producing large amounts of recombinant HSP90a, HPf polypeptide, HPfΔC1 or HPfΔC2 polypeptide, using expression vectors and transformed cell lines, are described. Topical and other delivery form preparations, including microneedle preparations, and methods for using the preparations for improving skin conditions (atopic dermatitis, wrinkles, skin elasticity, dark spots (over pigmentation), overall skin rejuvenation, skin ageing) and other therapeutic (anti-cancer, anti-ALS, anti-Huntington's disease, obesity) and cosmeceutical uses are presented. Wound healing preparations with the Hsp90a and related peptides are disclosed. | 2021-05-06 |
20210130424 | DUAL IL-2R AND IL-7R BINDING COMPOUNDS - Dual receptor binding compounds comprising IL-2Rβ, IL-7Rα, and Rγc ligands, and pharmaceutical compositions comprising the dual receptor binding compounds are disclosed. The dual receptor binding compounds can act as IL-2R and IL-7R agonists and are useful in treating cancer, viral diseases, autoimmune diseases, and inflammatory diseases. | 2021-05-06 |
20210130425 | TREATMENT OF RETINITIS PIGMENTOSA - A polynucleotide comprising a nucleotide sequence encoding the retinitis pigmentosa GTPase regulator ORF15 isoform (RPGR | 2021-05-06 |
20210130426 | Treatment of Muscular Dystrophies - There is described a nucleic acid molecule comprising a nucleotide sequence encoding a functional dystrophin protein. Also described is a vector, a host cell and a pharmaceutical composition comprising the nucleic acid molecule; use of the nucleic acid molecule in therapy, such as in the treatment of a muscular dystrophy; and a method of treating muscular dystrophy, the method comprising administering a therapeutically effective amount of the nucleic acid molecule to a patient suffering from a muscular dystrophy. | 2021-05-06 |
20210130427 | PRODUCTION OF RECOMBINANT LUBRICIN - Disclosed are new recombinant isoforms of human-like lubricin or PRG4 glycoprotein having outstanding lubrication properties and a novel glycosylation pattern, and methods for their manufacture at high levels enabling commercial production. | 2021-05-06 |
20210130428 | METHODS FOR TREATING DISEASE USING INHIBITORS OF BONE MORPHOGENETIC PROTEIN 6 (BMP6) - The present invention relates methods of treatment using BMP6 antagonists. | 2021-05-06 |
20210130429 | RECOMBINANT ADENO-ASSOCIATED VIRUS-MEDIATED EXPRESSION OF FRACTALKINE FOR TREATMENT OF NEUROINFLAMMATORY AND NEURODEGENERATIVE DISEASES - The subject invention pertains to the use of fractalkine (FKN, CX3CL1) and its receptor CX3CR1 for treatment of neuroinflammation and/or neurodegeneration. In one embodiment, the present invention provides a method for treatment of neuroinflammation and/or neurodegenerative diseases, comprising: administering, to cells of a subject in need of such treatment, an adeno-associated virus that comprises a functional fractalkine gene operably linked to transcriptional control elements. In one embodiment, the subject invention is used to treat or ameliorate Parkinson's disease. The present invention can also be used to treat or ameliorate neuroinflammatory and/or neurodegenerative diseases including, but not limited to, Alzheimer's disease, epilepsy, aging, and traumatic brain injury. | 2021-05-06 |
20210130430 | ACTIVATABLE CYTOKINE POLYPEPTIDES AND METHODS OF USE THEREOF - The disclosure features fusion proteins that are conditionally active variants of a cytokine of interest. In one aspect, the full-length polypeptides of the invention have reduced or minimal cytokine-receptor activating activity even though they contain a functional cytokine polypeptide. Upon activation, e.g., by cleavage of a linker that joins a blocking moiety, e.g. a steric blocking polypeptide, in sequence to the active cytokine, the cytokine can bind its receptor and effect signaling. Typically, the fusion proteins further comprise an in vivo half-life extension element, which may be cleaved from the cytokine in the tumor microenvironment. | 2021-05-06 |
20210130431 | T CELL RECEPTORS FOR IMMUNOTHERAPY - Provided are T cell receptors (TCR) and TCR variable regions that can selectively bind the T-cell leukemia/lymphoma 1 (TCL1) oncoprotein. The TCR may be utilized in various therapies, such as autologous TCL1-TCR adoptive T cell therapy, to treat a cancer, such as a B-cell malignancy or a solid tumor expressing TCL1. Methods for expanding a population of T cells that target TCL1 are also provided. | 2021-05-06 |
20210130432 | ANTI-HUMAN PAPILLOMAVIRUS 16 E7 T CELL RECEPTORS - Disclosed is a synthetic T cell receptor (TCR) having antigenic specificity for an HLA-A2-restricted epitope of human papillomavirus (HPV) 16 E7, E711-19. Related polypeptides and proteins, as well as related nucleic acids, recombinant expression vectors, host cells, and populations of cells are also provided. Antibodies, or an antigen binding portion thereof, and pharmaceutical compositions relating to the TCRs of the invention are also provided. Also disclosed are methods of detecting the presence of a condition in a mammal and methods of treating or preventing a condition in a mammal, wherein the condition is cancer, HPV 16 infection, or HPV-positive premalignancy. | 2021-05-06 |
20210130433 | ANTI-HUMAN PAPILLOMAVIRUS 16 E6 T CELL RECEPTORS - Disclosed is a T cell receptor (TCR) having antigenic specificity for an HLA-A2-restricted epitope of human papillomavirus (HPV) 16 E6, E6 | 2021-05-06 |
20210130434 | NKG2D-IG FUSION PROTEIN FOR CANCER IMMUNOTHERAPY - Methods and compositions for cancer immunotherapy are provided. The methods involve the use of a chimeric molecule (e.g., fusion protein) comprising a dimeric NKG2D portion and an Fc portion, which binds one or more NKG2D ligands. In some embodiments, the molecule further comprises a drug moiety (e.g., an IL15/Ra moiety). The methods disclosed herein are useful for the treatment of cancer that is associated with abnormal expression of one or more NKG2D ligands. | 2021-05-06 |
20210130435 | TRIFUNCTIONAL T CELL-ANTIGEN COUPLER AND METHODS AND USES THEREOF - A trifunctional molecule comprising a target-specific ligand, a ligand that binds a protein associated with the TCR complex and a T cell receptor signaling domain polypeptide is provided Engineering T cells with this novel receptor engenders antigen specific activation of numerous T cell functions, including cytokine production, degranulation and cytolysis. | 2021-05-06 |
20210130436 | CD80 VARIANT IMMUNOMODULATORY PROTEINS AND USES THEREOF - Provided herein are variant CD80 polypeptides, immunomodulatory proteins comprising variant CD80 polypeptides, and nucleic acids encoding such proteins. The immunomodulatory proteins provide therapeutic utility for a variety of immunological and oncological conditions. Compositions and methods for making and using such proteins are provided. | 2021-05-06 |
20210130437 | PD-L2 VARIANT IMMUNOMODULATORY PROTEINS AND USES THEREOF - Provided herein are immunomodulatory proteins comprising variant PD-L2 and nucleic acids encoding such proteins. The immunomodulatory proteins provide therapeutic utility for a variety of immunological and oncological conditions. Compositions and methods for making and using such proteins are provided. | 2021-05-06 |
20210130438 | PAN-CANCER T CELL EXHAUSTION GENES - The present invention provides novel pan-cancer T cell exhaustion regulators. CXCR6 expressed in CD8+ T cells was specifically identified as regulating anti-tumor immunity. Modulating CXCR6-CXCL16 interaction is useful in modulating anti-tumor immunity. The identified genes may be modulated in T cells for use in adoptive cell transfer. The identified genes may be modulated in vivo. | 2021-05-06 |
20210130439 | METHOD FOR MANUFACTURE OF DEMINERALIZED BIOCOMPOSITE MATERIALS - The invention comprises several embodiments of a multi-step method for processing hard tissues, including bone, teeth, tooth enamel and dentin, mollusk shells, crustacean shells, deep sea sponge, coral, radiolarians, diatoms, antler bone, and other naturally occurring mineralized biocomposites, and soft tissues, including connective tissue, cartilage, tendon, ligament, vertebral discs, pathological mineralized soft tissues and other soft tissues, including at least processing a portion of tissue by one or more of contacting, immersing, adding and mixing a portion of tissue with a first solution, obtaining a first material, derived from processing the portion of tissue with the first solution, processing the first material using one or more alkali metal and ammonium salts of citrate, acetate, phosphate, sulfate, tartarate and chloride, and obtaining a resulting material, derived from processing the first material with the one or more salts. | 2021-05-06 |
20210130440 | METHODS FOR PRODUCING BIOTHERAPEUTICS WITH INCREASED STABILITY BY SEQUENCE OPTIMIZATION - The invention relates to methods of optimizing an antibody with enhanced stability, the method comprising mutating somatic hypermutation with germline amino acid residues and therefore providing enhanced thermal stability, improved biophysical properties and shelf-life while preserving the affinity for the antigen. | 2021-05-06 |
20210130441 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF IMMUNODEFICIENCY - The present invention relates to compositions and methods for the treatment of immunodeficiency (e.g., primary immunodeficiency disease). In particular, the invention provides human plasma immunoglobulin compositions containing select antibody titers specific for a plurality of respiratory pathogens, methods of identifying human donors and donor samples for use in the compositions, methods of manufacturing the compositions, and methods of utilizing the compositions (e.g., for prophylactic administration and/or therapeutic treatment (e.g., passive immunization (e.g., immune-prophylaxis))). | 2021-05-06 |
20210130442 | ANTI-PSEUDOMONAS PSL BINDING MOLECULES AND USES THEREOF - This disclosure relates to an anti- | 2021-05-06 |
20210130443 | HIGH-AFFINITY MYCOBACTERIUM TUBERCULOSIS CAPSULE-SPECIFIC HUMAN MONOCLONAL ANTIBODY - Provided are high affinity | 2021-05-06 |
20210130444 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF NEUROMYELITIS OPTICA - The present invention is directed to antibodies binding to aquaporin 4 (AQP4) and methods of using such antibodies to treat neuromyelitis optica (NMO) either as a monotherapy or in combination with standard NMO therapies such as immunosuppressives or plasmaphersis. | 2021-05-06 |
20210130445 | CGRP Antagonists and Botulinum Toxins for the Treatment of Inflammatory and Neurologic Disorders - The application is related to the treatment of diseases and disorders associated with pain by the administration of a CGRP-antagonist and a clostridial derivative. | 2021-05-06 |
20210130446 | COMPOSITIONS AND METHODS FOR TREATING LIVER DISEASE - Disclosed are methods of treating a subject, particularly a human individual, more particularly a pediatric individual, having a biliary disorder, via administration of a therapeutically effective amount of a C5 inhibitor. The biliary disorder may include biliary atresia and post-Kasai biliary atresia. | 2021-05-06 |