43rd week of 2021 patent applcation highlights part 23 |
Patent application number | Title | Published |
20210332026 | MORPHIC FORMS OF COMPLEMENT FACTOR D INHIBITORS - This invention provides stable, highly crystalline forms of Complement Factor D inhibitor Compound 3 for therapeutic applications. | 2021-10-28 |
20210332027 | ALKYNYL-SUBSTITUTED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF - The present invention relates to an alkynyl-substituted heterocyclic compound acting as an FGFR inhibitor, a preparation method therefor and a medical use thereof. In particular, the present invention relates to a compound as shown in general formula (I) and a pharmaceutically acceptable salt thereof; a pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof; a method for treating and/or preventing FGFR-associated diseases, particularly tumors, by using the compound or a pharmaceutically acceptable salt thereof; and a preparation method for the compound or a pharmaceutically acceptable salt thereof. The present invention also relates to the use of the compound or a pharmaceutically acceptable salt thereof, or the pharmaceutical composition including the compound or a pharmaceutically acceptable salt thereof in the preparation of a drug for treating and/or preventing FGFR-associated diseases, particularly tumors, wherein the definition of each substituent group in general formula (I) is the same as that in the description. | 2021-10-28 |
20210332028 | NOVEL HYDROCHLORIDE SALT FORMS OF A SULFONAMIDE STRUCTURED KINASE INHIBITOR - The present invention relates to novel hydrochloride salt forms of N-(2′,4′-difluoro-5-(5-(1-methyl-1H-pyrazol-4-yl)-1H-benzo[d]imidazol-1-yl)-[1,1′-biphenyl]-3-yl)cyclopropanesulfonamide (I). Compound (I) is a selective inhibitor of FGFR/VEGFR kinase families and is useful in the treatment of cancer. | 2021-10-28 |
20210332029 | ISOINDOLIN-1-ON DERIVATIVE, METHOD FOR PREPARING SAME, AND PHARMACEUTICAL COMPOSITION COMPRISING SAME AS EFFECTIVE COMPONENT FOR PREVENTING OR TREATING CANCER - The present invention relates to an isoindolin-1-on derivative, a method for preparing same, and a pharmaceutical composition comprising same as an effective component for preventing or treating tumors, wherein the isoindolin-1-on derivative exhibits a high inhibitory effect on EGFR mutations, and thus can be beneficially used for the treatment of EGFR-mutated tumors, and the isoindolin-1-on derivative exhibits a significant synergistic effect when co-administered, and thus can be beneficially used in concomitant therapy. | 2021-10-28 |
20210332030 | INHIBITOR COMPOUNDS FOR MALE CONTRACEPTION - Pyrazole compounds and piperazine compounds that are inhibitors of ALDH1A1 and ALDH1A2 and methods for using the pyrazole compounds and piperazine compounds in male contraceptive compositions for preventing spermatogenesis. | 2021-10-28 |
20210332031 | MULTI-AZIRIDINE COMPOUND - The present invention relates to a multi-aziridine compound having: a) from 2 to 6 of the following structural units (A): (A) whereby R′, R″, R | 2021-10-28 |
20210332032 | BENZONITRILE DERIVATIVE, LIGHT-EMITTING MATERIAL, AND LIGHT-EMITTING ELEMENT USING SAME - A compound represented by formula (I). | 2021-10-28 |
20210332033 | NICOTINAMIDE MONONUCLEOTIDE DERIVATIVES AND USE THEREOF IN THE TREATMENT OF VIRAL INFECTIONS - The present disclosure relates to Nicotinamide mononucleotide derivatives of formula (I) | 2021-10-28 |
20210332034 | GLP-1 Receptor Agonists and Uses Thereof - Provided herein are 6-carboxylic acids of benzimidazoles and 4-aza-, 5-aza-, and 7-aza-benzimidazoles as GLP-1R agonists, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof. | 2021-10-28 |
20210332035 | 3-ARYLOXYL-3-FIVE-MEMBERED HETEROARYL PROPYLAMINE COMPOUND AND USE THEREOF - Disclosed are a 3-aryloxyl-3-five-membered heteroaryl propylamine compound and use thereof. Specifically disclosed is a compound or a pharmacologically acceptable salt thereof or a prodrug thereof. The compound has the structure of formula I. The compound or the pharmacologically acceptable salt thereof or the prodrug thereof has excellent inhibition to transient receptor potential (TPR) channel proteins, and has good therapeutic effect on diseases related to the TPR channel proteins. | 2021-10-28 |
20210332036 | PYRIMIDINE AND PYRAZINE HDAC1,2 INHIBITORS - Provided herein are compounds, pharmaceutical compositions comprising such compounds, and methods of using such compounds to treat diseases or disorders associated with HDAC1 and/or HDAC2 activity. | 2021-10-28 |
20210332037 | Scopolamine Production - The invention provides an improved method for the production of Scopolamine by extraction. | 2021-10-28 |
20210332038 | 6H-IMIDAZO[4,5,1-ij]QUINOLONE, SYNTHESIS METHOD AND USE THEREOF - The present invention relates to the technical field of chemical synthesis of pharmaceutical chemicals, and provides a 6H-imidazo[4,5,1-ij]quinolone, a synthesis method and use thereof. 6H-imidazo[4,5,1-ij]quinolone derivatives provided by the present invention are a novel group of active quinolone derivatives, which have tumor cell inhibition activity and exhibit IC | 2021-10-28 |
20210332039 | PESTICIDALLY ACTIVE POLYCYCLIC DERIVATIVES WITH SULFUR CONTAINING SUBSTITUENTS - Polycyclic derivatives of formula I | 2021-10-28 |
20210332040 | SUBSTITUTED 4-AMINO-1H-IMIDAZO[4,5-c]QUINOLINE COMPOUNDS AND IMPROVED METHODS FOR THEIR PREPARATION - Improved methods and intermediates thereof for preparing substituted 4-amino-1H-imidazo[4,5-c]quinoline compounds are described. These compounds are useful as NLRP3 modulators. | 2021-10-28 |
20210332041 | TETRAHYDROPYRIDOPYRIMIDINE DERIVATIVES AS AHR MODULATORS - The present disclosure relates to compounds of formula (I), which are suitable as AhR modulators, in particular AhR inhibitors. The disclosure also relates to compositions comprising said compounds and use of said compounds or compositions in treatment, in particular in the treatment of cancer. The disclosure further relates to methods of preparing said compounds. | 2021-10-28 |
20210332042 | A GABAA Receptor Ligand - The present invention relates to 2-(3-(3-(2,4-dimethoxypyrimidin-5-yl)phenyl)-3H- imidazo[4,5-b]pyridin-6-yl)propan-2-ol, which is useful as a GABA receptor modulator. In one embodiment, said compound is useful in the treatment of pain, neuropathic pain and/or itch. | 2021-10-28 |
20210332043 | 1,7-NAPHTHYRIDINE DERIVATIVE AND PREPARATION METHOD AND USE THEREFOR - A compound represented by formula (I) or a tautomer, an optical isomer, a nitrogen oxide, a solvate, a pharmaceutically acceptable salt or prodrug thereof are useful for treating or relieving an HIF-related and/or EPO-related disease or condition in patient. | 2021-10-28 |
20210332044 | SYNTHESIS OF COELENTERAZINE SYNTHESIS INTERMEDIATE - Disclosed herein are synthesis methods for coelenterazine and intermediates. Also disclosed are articles including the coelenterazine and coelenterazine derivatives. Representative absorbent articles include disposable diapers and adult incontinence products. | 2021-10-28 |
20210332045 | HETEROCYCLIC COMPOUND - Provided is a compound that can have an effect of inhibiting MALT1 and is expected as useful as a prophylactic or therapeutic drug for cancer, etc. A compound represented by formula (I) [wherein each symbol is as defined in the description], a salt thereof, or a cocrystal, a hydrate or a solvate of the same. | 2021-10-28 |
20210332046 | NICOTINIC ACETYLCHOLINE RECEPTOR SILENT AGONISTS - Derivatives of N,N-diethyl-N′-phenyl-piperazine, a silent agonist of the mammalian α7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor. | 2021-10-28 |
20210332047 | QUINAZOLINONES AS INHIBITORS OF HUMAN PHOSPHATIDYLINOSITOL 3-KINASE DELTA - Compounds that inhibit PI3Kδ activity, including compounds that selectively inhibit PI3Kδ activity, are disclosed. Methods of inhibiting phosphatidylinositol 3-kinase delta isoform (PI3Kδ) activity, and methods of treating diseases, such as disorders of immunity and inflammation in which PI3Kδ plays a role in leukocyte function, using the compounds also are disclosed. | 2021-10-28 |
20210332048 | MEROPENEM DERIVATIVES AND USES THEREOF - The present invention provides novel derivative of β-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection). | 2021-10-28 |
20210332049 | CRYSTALLINE FORMS OF (S)-7-(1-(BUT-2-YNOYL)PIPERIDIN-4-YL)-2-(4-PHENOXYPHENYL)-4,5,6,7-TETRAHY- DROPYRAZOLO[1,5-a]PYRIMIDINE-3-CARBOXAMIDE, PREPARATION, AND USES THEREOF - The present invention relates to a crystalline form of (S)-7-(1-(but-2-ynoyl) piperidin-4-yl)-2-(4-phenoxyphenyl)-4,5,6,7-tetrahydropyrazolo [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. | 2021-10-28 |
20210332050 | POLYPROLINE MIMETICS OF PROLINE-DERIVED MODULE-15 - The present invention relates to chemical compounds which can be used in particular as structural mimetics of proline-rich peptides. The compounds of the present invention are capable of selectively inhibiting Ena/VASP-EVH1-mediated protein-protein interactions. The invention further relates to the use of these compounds as pharmaceutical agents and the use of the pharmaceutical agents for the treatment of tumor diseases. | 2021-10-28 |
20210332051 | METHODS FOR INHIBITING FASCIN - Provided are compositions and methods for treating a condition or disorder mediated by fascin activity in a subject in need thereof which method comprises administering to the subject a therapeutically effective amount of at least one compound of any one of Formula I-a to I-n, II, II-a, II-b or III or a pharmaceutically acceptable salt thereof. | 2021-10-28 |
20210332052 | PYRROLO AND PYRAZOLOPYRIMIDINES AS UBIQUITIN-SPECIFIC PROTEASE 7 INHIBITORS - The invention relates to inhibitors of USP7 inhibitors useful in the treatment of cancers, neurodegenerative diseases, immunological disorders, inflammatory disorders, cardiovascular diseases, ischemic diseases, viral infections and diseases, and bacterial infections and diseases, having the Formula: | 2021-10-28 |
20210332053 | HETEROCYCLIC COMPOUND AND USE THEREOF - The present invention provides a heterocyclic compound having an antagonistic action on an NMDA receptor containing the NR2B subunit, and expected to be useful as an agent for the prophylaxis or treatment of major depression, bipolar disorder, migraine, pain, behavioral and psychological symptoms of dementia and the like. | 2021-10-28 |
20210332054 | [1,3]DIAZINO[5,4-d]PYRIMIDINES AS HER2 INHIBITORS - The present invention relates to new [1,3]diazino[5,4-d]pyrimidines and derivatives of Formula (I) | 2021-10-28 |
20210332055 | TRIAZOLOTRIAZINE DERIVATIVES AS A2A RECEPTOR ANTAGONISTS - The present invention provides triazolotriazine derivatives of formula (1) as A2A receptor antagonists. Compounds of formula (1) and pharmaceutical compositions including the compounds can be used for the treatment of disorders related to A2A receptor hyperfunctioning, such as certain types cancers. Compounds of formula (1) and methods of preparing the compounds are disclosed in the invention. | 2021-10-28 |
20210332056 | CRYSTAL OF PYRAZOLO[3,4-D]PYRIMIDINE - An object of the invention is to provide a crystal of (R)-1-(1-acryloylpiperidin-3-yl)-4-amino-N-(4-(2-(dimethylamino)-2-oxoethyl)-2,3-dimethylphenyl)-1H-pyrazolo[3,4-d]pyrimidine-3-carboxamide which is excellent in stability and preferable from the viewpoint of manufacturing and formulation. The present invention provides a crystal having an X-ray powder diffraction spectrum having characteristic peaks at diffraction angles (2θ±0.2°) of 6.0°, 7.7°, 8.9°, 10.6°, 12.1°, 13.1°, 14.0°, 14.7°, 15.5°, 15.8°, 16.8°, 17.7°, 18.1°, 18.4°, 19.4°, 23.4°, 24.1°, 24.7°, 25.1° and 25.7°. | 2021-10-28 |
20210332057 | AMINONORBORNANE DERIVATIVE AND MANUFACTURE METHOD THEREFOR AND USE THEREOF - The present invention relates to a compound of formula I or a pharmaceutically acceptable salt, a solvate, an active metabolite, a polymorph, an ester, an optical isomer or a prodrug thereof, a pharmaceutical composition comprising the compound of formula I, and use of the compound, as a Bruton's tyrosine kinase inhibitor with high selectivity for BTK (C481S) mutant, in the manufacture of a medicament for preventing or treating a heteroimmune disease, an autoimmune disease or a cancer. | 2021-10-28 |
20210332058 | Compounds, Compositions and Methods - The present disclosure relates generally to methods and compositions for preventing or arresting cell death and/or inflammation. | 2021-10-28 |
20210332059 | USE OF PYRAZOLOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF PI3K-DELTA RELATED DISORDERS - The present application provides methods of treating PI3Kδ related disorders using compounds of Formula I: | 2021-10-28 |
20210332060 | A Simple Process for Preparing Avibactam - The present invention provides a simple process of preparing avibactam. Piperidine-5-one-2S-carboxylate II as the raw material is subjected to condensation reaction with O-protecting hydroxylamine hydrochloride; the resulting compound is subjected to reduction and chiral resolution to obtain 5R-substituted oxyaminopiperidine-2S-carboxylic acid V in a basic condition; then, the compound of formula V is subjected to urea cyclization, acyl chlorination, and amidation with phosgene, solid phosgene, or diphosgene in a “one-pot” process, and then subjected to deprotection, sulfation, and tetrabutylammonium salt formation reaction to obtain (2S,5R)-2-carbamoyl-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl]oxy}sulfonyl tetra-n-butyl ammonium salt VII, and finally, the compound of formula VII is subjected to ion exchange to obtain avibactam I. | 2021-10-28 |
20210332061 | NMDA RECEPTOR MODULATORS AND USES THEREOF - Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 2021-10-28 |
20210332062 | HETERO-SUBSTITUTED CYCLIC LACTONE ANALOGUES AND USES THEREOF - The present disclosure provides SL and SL derivatives comprising a polar substituent adjacent to the lactone ring. Additionally, the present disclosure provides methods of using the SL and SL derivatives to inhibit the growth of leukemic cancer cells. | 2021-10-28 |
20210332063 | METHOD FOR SYNTHESIZING THIENO[3,2-B]PYRIDINE-5(4H)-ONE DERIVATIVE COMPOUND, USING GOLD CATALYST, AND USE THEREFOR - Disclosed are a method for synthesizing a thieno[3,2-b]pyridine-5(4H)-one derivative by using a gold catalyst and a use of the derivative compound, wherein the novel thieno[3,2-b]pyridine-5(4H)-one derivative of the present disclosure, which is a compound synthesized using gold as a catalyst, has fluorescence characteristics with a wide range of emission wavelengths and thus can be helpfully used in various industrial fields, such as physics, chemistry, and biomedicine research. | 2021-10-28 |
20210332064 | ISOQUINOLINE COMPOUNDS FOR THE TREATMENT OF CANCER - 3-Carbonylaminoisoquinoline compounds of formula (I): | 2021-10-28 |
20210332065 | BCL-2 INHIBITORS - The disclosure includes compounds of Formula (A), wherein R | 2021-10-28 |
20210332066 | NITROGEN-CONTAINING HETEROCYCLIC ORGANIC COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE - A nitrogen-containing heterocyclic organic compound and an organic electroluminescent device are provided. The nitrogen-containing heterocyclic organic compound has a structure represented by the following general formula (I): | 2021-10-28 |
20210332067 | TRICYCLIC HETEROARYL COMPOUNDS AS STING ACTIVATORS - The present application provides tricyclic heteroaryl compounds that activate the STING pathway to produce interferons, which are useful in the treatment of various diseases including infectious diseases and cancer. | 2021-10-28 |
20210332068 | Arginase Inhibitors and Methods of Use thereof - Disclosed include crystalline (S)-2-amino-N-((3R,5R)-8-hydroxy-6-oxo-7-oxa-1-aza-8-boraspiro[4.7]dodecan-3-yl)-3-methylbutanamide in Form D and in Form E: | 2021-10-28 |
20210332069 | Borate-Based Drug And Use Thereof - The present application provides a borate ester compound suitable for being used as a proteasome inhibitor, a preparation method and use thereof, and the compound has the following structure | 2021-10-28 |
20210332070 | Compositions and Methods for Synthesis of Phosphorylated Molecules - The invention provides compositions and methods for synthesis of phosphorylated organic compounds, including nucleoside triphosphates. | 2021-10-28 |
20210332071 | CDK9 Inhibitors and Polymorphs Thereof For Use As Agents For Treatment of Cancer - A crystalline form and/or polymorph of a compound having the following structure (I), including tautomeric and zwitterionic forms thereof, are provided: | 2021-10-28 |
20210332072 | ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES - A compound having a formula: | 2021-10-28 |
20210332073 | PROCESS FOR THE PREPARATION OF FERRIC CITRATE - Method are provided for obtaining ferric citrate that includes the step(s) of reacting ferric chloride with a suitable base to obtain ferric hydroxide; reacting the ferric hydroxide with citric acid to obtain ferric citrate; and processing the ferric citrate to obtain ferric citrate. The resulting ferric citrate has a specific surface area greater than 16 sq. m/g, but less than 20 sq. m/g. | 2021-10-28 |
20210332074 | COBALT PRECURSOR, METHOD OF PREPARING SAME AND METHOD OF MANUFACTURING THIN FILM USING SAME - The present invention relates to a vapor deposition compound enabling thin-film deposition through vapor deposition, and more particularly to a novel cobalt precursor, which can be applied to atomic layer deposition (ALD) or chemical vapor deposition (CVD) and exhibits superior reactivity, volatility and thermal stability, a method of preparing the same and a method of manufacturing a thin film using the same. | 2021-10-28 |
20210332075 | Novel Transition Metal Compound and Method of Preparing Polypropylene Using the Same - Provided are a novel transition metal compound of the following Chemical Formula 1 that exhibits excellent catalytic activity, allows formation of a macromonomer which is a polymer in which a double bond is formed at the end of a chain, and improves a melt strength characteristic when used in polymerizing polypropylene, and a method of preparing a polypropylene using the same. | 2021-10-28 |
20210332076 | ENZYMATIC SYNTHESIS OF HOMOGENEOUS CHONDROITIN SULFATE OLIGOSACCHARIDES - Methods of synthesizing chondroitin sulfate oligosaccharides are provided. Enzymatic schematic approaches to synthesizing structurally defined homogenous chondroitin sulfate oligosaccharides at high yields are provided. Synthetic chondroitin sulfate oligosaccharides ranging from 3-mers to 15-mers are provided. | 2021-10-28 |
20210332077 | Glycosylated Sphingoid Bases and Production Thereof - The present invention relates to several novel 1-O-glycosylated sphingoid bases and to a production method thereof, as well as to uses of the 1-O-glycosylated sphingoid bases. | 2021-10-28 |
20210332078 | COMPOSITIONS AND METHODS FOR NUCLEIC ACID AMPLIFICATION - The present disclosure provides compositions, methods and systems for the efficient removal of a non-target nucleic acid sequence from a double stranded nucleic acid amplification product. A non-target nucleic acid sequence may be a primer sequence incorporated into the double stranded nucleic acid molecule during a nucleic acid synthesis or amplification reaction. The non-target nucleic acid sequence may include a nucleobases that are not canonical DNA nucleobases, such as uracil, that can be selectively removed as part of the non-target sequence removal process. | 2021-10-28 |
20210332079 | SQUALAMINE SOLID FORMS AND METHODS OF MAKING THE SAME - Provided herein are crystalline solid forms of squalamine phosphate designated as Form 1 and Form 2, compositions containing one or both forms, and methods of their preparation and of their use. | 2021-10-28 |
20210332080 | HYDROPHILIC LINKERS FOR ANTIBODY DRUG CONJUGATES - Described herein protein drug conjugates and compositions thereof that are useful, for example, for the target-specific delivery of drugs to cells. By administering these compounds, compositions, and conjugates as described herein to specific target cells, side-effects due to non-specific binding phenomena, for example, to non-target cells are reduced. In certain embodiments, compounds, compositions, and conjugates are provided, which include hydrophilic residues in linker-payloads and protein conjugates thereof. | 2021-10-28 |
20210332081 | METHOD FOR SEPARATING COLLAGEN FROM LIPOSUCTION EFFLUENT USING SUPERCRITICAL PROCESS - The present invention relates to a method for extracting collagen from liposuction effluent, wherein collagen is extracted by treating collagen-containing liposuction effluent in the presence of a supercritical fluid. According to the present invention, conventionally discarded collagen in liposuction effluent can be extracted at high purity, and the extracted high purity collagen can be widely used in medical, pharmaceutical, and cosmetic products. | 2021-10-28 |
20210332082 | TRACELESS REDUCTIVELY CLEAVABLE LINKER MOLECULES FOR PEPTIDE PURIFICATION - The present invention relates to linker molecules of formula (1), X-T | 2021-10-28 |
20210332083 | Netrin-1 Compounds and Compositions Thereof for Treating Pulmonary Hypertension - Disclosed herein are netrin-1 compounds and compositions thereof and methods of using thereof to treat pulmonary hypertension. In some embodiments, the present invention provides methods of treating, reducing, or inhibiting pulmonary hypertension or reducing a subjects mean pulmonary arterial pressure (mPAP) and/or the subjects right ventricular systolic pressure (RVSP), which methods comprise administering to the subject a therapeutically effective amount of one or more netrin-1 compounds. | 2021-10-28 |
20210332084 | OPTIMIZED ZIKA VIRUS ENVELOPE GENE AND EXPRESSION THEREOF - The present invention is directed to the expression and secretion the Zika virus envelope protein. Elements of the pre-membrane and envelope sequence have been modified to enhance the expression of the envelope protein as a secreted product in the culture medium of transformed insect cell lines. The expressed and purified product is suitable as a vaccine antigen. | 2021-10-28 |
20210332085 | CoV-2 (CoV-n) antibody neutralizing and CTL vaccines using protein scaffolds and molecular evolution - The embodiment of the invention is to innovate immunogenic CoV-2, CoV-n B cell epitopes, which are selected from the loop regions constrained by the two constraining beta strands; or between one beta strand and one alpha-helical strand; or between two alpha-helical strands of CoV-2, CoV-n proteins, and such selected loops replace the native loops of the thermostable protein scaffolds, which provide thermostable constraint of the transplanted CoV-2, CoV-n loop antigens as well as CD4 helper T cell determinants to elicit CD4 dependent neutralizing and blocking antibodies against viral entry, replication and viral clearance. The B cell loops can be cleaved and processed as CD8 T cell epitopes for eliciting cytotoxic T lymphocyte (CTL) responses against and clear viral infected cells. MHCI viral peptide epitopes in nonamers, octamers, or decamers will be used as peptide vaccines along with viral CD4 helper peptide epitopes. These CTL peptides will be also inserted into the loop or replacing the native loop of the protein scaffolds. All the above sequences can be embodied in RNA vaccines to augment protection or suppress cytokine storms. And the embodiment of the invention is to employ CTL peptides and CD4 helper peptides inserted into each respective candidate loop of the protein scaffolds as CTL vaccines. Thus, the CTL vaccines safely eliminate infectious foci and reservoir of the offending virus and mutant viral strains. | 2021-10-28 |
20210332086 | MERS-COV INHIBITOR PEPTIDES - The MERS-CoV inhibitor peptides include a set of peptides designed by modification or mutation of a wild type MERS-CoV fusion protein. The MERS-CoV inhibitor peptides are capable of inhibition of MERS-CoV membrane fusion, and thereby may prevent or slow the spread of MERS-CoV infections. Thus, the MERS-CoV inhibitor peptides may be used in pharmaceuticals to prevent and/or treat MERS-CoV infection. The pharmaceuticals may be formulated to comprise at least one of the MERS-CoV inhibitor peptides and a carrier, or they may include one or more expression systems capable of promoting cellular expression of one or more MERS-CoV inhibitor peptides. The MERS-CoV inhibitor peptides may also be used as reagents for MERS-CoV inhibition assays as a standard or reference inhibitors. | 2021-10-28 |
20210332087 | VACCINES AND VACCINE COMPONENTS FOR INHIBITION OF MICROBIAL CELLS - The invention encompasses components from microbial cells which are useful for antibody production, including peptides, polypeptides comprising these peptides, polynucleotides which encode these peptides or polypeptides, and antibodies directed to these peptides, polypeptides, or polynucleotides. The invention also encompasses to expression vectors and host cells for producing these peptides, polypeptides, polynucleotides, and antibodies. The invention further encompasses methods and compositions, especially vaccine compositions, for detecting, targeting, and inhibiting microbial cells, especially methanogen cells, using one or more of the disclosed peptides, polypeptides, polynucleotides, antibodies, expression vectors, and host cells. | 2021-10-28 |
20210332088 | Multimerizing Polypeptides Derived From Jelly Roll Fold Domain of Adenovirus Penton Base - The present invention relates to novel polypeptide scaffolds for optimized presentation of oligopeptides, polypeptide sequences, protein domains, proteins and protein complexes made up of two, several or many subunits. These oligopeptides, polypeptide sequences, protein domains and proteins presented by the polypeptide scaffolds of the invention can include antigenic entities that stimulate the immune system to trigger an immune response, for example for vaccination purposes, or for preparing antibodies or other binder molecules in cell culture, or in vitro in a test tube. In a preferred embodiment, the polypeptides of the invention are assembled into Virus Like Particles (VLPs) optimized for presentation of antigens useful in the context of vaccination against infectious agents or tumors. | 2021-10-28 |
20210332089 | HEPATITIS B VIRUS REPLICATION INHIBITOR AND PHARMACEUTICAL COMPOSITION FOR TREATING HEPATITIS B COMPRISING THE SAME - The purpose of the invention is to develop and provide a novel therapeutic agent for hepatitis B that differs from the conventional therapeutic agent for hepatitis B in the mechanism of action, or target of interest. | 2021-10-28 |
20210332090 | MULTIPLE ANTIGEN PRESENTING IMMUNOGENIC COMPOSITION, AND METHODS AND USES THEREOF - The present embodiments provide for an immunogenic multiple antigen presenting system comprising a polymer to which antigens are associated by complementary affinity molecules. For example, the polymer can be a polysaccharide, or antigenic polysaccharide, to which protein or peptide antigens from the same or different pathogens are indirectly linked. The present immunogenic compositions can elicit both humoral and cellular immune responses to one or multiple antigens at the same time. | 2021-10-28 |
20210332091 | OVER-EXPRESSION OF GDS1 IN YEAST FOR INCREASED ETHANOL AND DECREASED ACETATE PRODUCTION - Described are compositions and methods relating to modified yeast that over-express the glycerol-deficient suppressor, GDS1. The yeast produces an increased amount of ethanol and a deceased amount of acetate compared to parental cells. Such yeast is particularly useful for large-scale ethanol production from starch substrates where acetate in an undesirable end product. | 2021-10-28 |
20210332092 | ARTICLES COMPRISING A SILK POLYPEPTIDE FOR ANTIGEN DELIVERY - The present invention relates to a polypeptide comprising a silk polypeptide and an antigen. Further, the present invention relates to an article comprising the polypeptide. Furthermore, the present invention relates to a pharmaceutical composition comprising the article. In addition, the present invention relates to the article or pharmaceutical composition for use as a pharmaceutical, for inducing an immune response and/or for use in a prophylactic and/or therapeutic treatment of a disease. | 2021-10-28 |
20210332093 | FUSED IN SARCOMA (FUS) NUCLEAR TRANSLOCATION INHIBITORS FOR PREVENTING FIBROSIS - Disclosed herein are compositions and methods for inhibiting collagen production mediated by the Fused in Sarcoma (FUS) ribonucleoprotein. As disclosed herein, the C terminal domain of FUS contains an uncommon nuclear localization sequence (NLS) motif called PY-NLS that binds the nuclear import receptor transportin. Phosphorylation of FUS leads to its association with transportin and nuclear translocation with consequent increased in collagen production. Therefore, disclosed herein is an isolated peptide having a transportin-binding moiety, which inhibits FUS from binding transportin, linked to a membrane translocating motif. These compositions and methods can be used to inhibit FUS-mediated collagen production, and treat fibrotic disease involving FUS-mediated collagen accumulation in kidneys and other organs displaying fibrotic diseases. | 2021-10-28 |
20210332094 | NOVEL TRANSCRIPTION ACTIVATOR - The present invention provides a transcription activator consisting of not more than 200 amino acid sequences and containing VP64 and a transcription activation site of RTA. The present invention also provides a complex of a nucleic acid sequence-recognizing module specifically binding to a target nucleotide sequence in a double-stranded DNA and the transcription activator. | 2021-10-28 |
20210332095 | INFECTION-INDUCED ENDOTHELIAL AMYLOID COMPOSITIONS AS ANTIMICROBIALS - The present disclosure relates to compositions and methods for the production of antimicrobial amyloid compositions, and further relates to use of such antimicrobial preparations for the treatment of subjects having drug-resistant microbial infections. Advantageous and/or therapeutic amyloid oligomer immunodepletion methods are also disclosed. | 2021-10-28 |
20210332096 | ENGINEERED TGF-BETA MONOMERS AND THEIR USE FOR INHIBITING TGF-BETA SIGNALING - Recombinant transforming growth factor (TGF)-β monomers modified to inhibit dimerization and block TGF-β signaling are described. The recombinant TGF-β monomers lack the ability to bind and recruit TGF-β type I receptor (TβRI), but retain the capacity to bind the high affinity TGF-β type II receptor (TβRII), and in some instances, include mutations that increase their affinity for TβRII. Nucleic acid molecules and vectors encoding the recombinant TGF-β monomers are also described. Isolated cells, such as T cells, can be re-programmed with a TGF-β monomer-encoding nucleic acid or vector to secrete the monomer. Use of the recombinant TGF-β monomers and/or cells producing the recombinant TGF-β monomers, to inhibit TGF-β signaling, such as to treat disorders associated with aberrant TGF-β signaling, are also described. | 2021-10-28 |
20210332097 | COMPOSITIONS FOR TREATMENT OF VASCULAR DISEASE - Provided are various embodiments relating to compositions and methods for treating vascular disease, including core NOX1 promoters and variants thereof for regulating expression of transgenes in response to vascular pathology and allowing for increased transgene loading capacity. Also provided are variant FOXP polypeptides having a zinc finger and leucine zipper region of a different FOXP polypeptide. Further provided are vectors comprising the core NOX1 promoters and/or a coding sequence for variant FOXP polypeptides described herein and optionally coding sequence(s) for one or more additional therapeutic polypeptide(s), such as IL10, for treating inflammation-associated diseases, such as vascular disease. Also provided is a screening model for testing therapeutic agents capable of treating established and ongoing atherosclerotic pathology. | 2021-10-28 |
20210332098 | NSP-INTERLEUKIN-10 PROTEINS AND USES THEREOF - Disclosed herein are Nsp-IL10 polypeptides comprising an Nsp polypeptide and an IL10 polypeptide. In some embodiments, Nsp-IL10 polypeptide is capable of activating an NGF signaling pathway, an IL10 signaling pathway, or both. Also disclosed are methods for treating a disease comprising administering an Nsp-IL10 polypeptide. The methods include treating diseases associated with joint inflammation, such as osteoarthritis. | 2021-10-28 |
20210332099 | PHARMACEUTICAL PREPARATION - Preparations including recombinant FSH (rFSH). | 2021-10-28 |
20210332100 | NOVEL PRO-INSULIN ASPART STRUCTURE AND METHOD FOR PREPARING INSULIN ASPART - Provided in the present invention are a novel pro-insulin aspart structure design and a method for preparing insulin aspart. The main steps comprise designing the pro-insulin aspart sequence, constructing recombinant insulin aspart engineered bacteria, inducing an insulin fusion protein expressed in the form of an inclusion body by means of the engineered bacteria, and obtaining a mature insulin aspart material drug by means of denaturing, renaturing enzymatic digestion, and separation purification, By means of changing the recombinant leading peptide and C-peptice sequences, the invention avoids the dangerous and tedious step of cleavage using cyanogen bromide. The C-peptide is shortened to one amino acid, reducing the quality loss of enzymatic digestion conversion. | 2021-10-28 |
20210332101 | COMPOSITIONS AND METHODS FOR T CELL ENGINEERING - The present disclosure relates to an engineered immune cell and use thereof. The present disclosure provides an engineered immune cell comprising a CAR or engineered TCR, which CAR or engineered TCR can comprise a first antigen binding domain and a second antigen binding domain. The engineered immune cells of the present disclosure, when administered into a subject, can inhibit the host immune cells such as T cells and/or NK cells and enhance the survival and persistence of the engineered immune cells in vivo, thereby exhibiting more effective tumor killing activity. | 2021-10-28 |
20210332102 | HIGH-AFFINITY T CELL RECEPTOR AGAINST PRAME - Provided is a T cell receptor (TCR) having a feature of binding to a VLDGLDVLL-HLA A2 complex. The binding affinity of the TCR to the VLDGLDVLL-HLA-A0201 complex is at least 2 times of the binding affinity of a wild-type TCR to the VLDGLDVLL-HLA-A0201 complex. Also provided is a fusion molecule of the TCR and a therapeutic agent. The TCR can be used alone or in combination with a therapeutic agent to target a tumor cell presenting the VLDGLDVLL-HLA-A0201 complex. | 2021-10-28 |
20210332103 | POLYPEPTIDES, CELLS, AND METHODS INVOLVING ENGINEERED CD16 - This disclosure describes, generally, a modified form of CD16, genetically-modified cells that express the modified CD16, and methods that involve the genetically-modified cells. The modified form of CD16 can exhibit increased anti-tumor and/or anti-viral activity due, at least in part, to reduced susceptibility to ADAM17-mediated shedding upon NK cell stimulation. | 2021-10-28 |
20210332104 | THERAPEUTIC PEPTIDES AND METHODS FOR TREATING AUTOIMMUNE RELATED DISEASE - Methods and materials for preventing and modulating atherosclerosis. In particular, small peptides that are capable of interacting with CD40, thereby interfering with the ability of CD40 to interact with CD154, which impacts inflammation and atherosclerosis. The use of such peptides in reducing atherosclerosis, and in particular, the autoimmune inflammatory response that may be a driving factor thereof. The use of such short peptides to lower LDL cholesterol. Methods and materials for detecting T-cells that express CD40 (Th40 cells). Methods and materials for preventing, modulating, reducing and/or reversing type 2 diabetes and auto-inflammatory disease. In particular, small peptides that are capable of interacting with CD40, thereby interfering with the ability of CD40 to interact with CD154, which impacts inflammation and type 2 diabetes. The use of such peptides in reducing type 2 diabetes, and in particular, the autoimmune inflammatory response that may be a driving factor thereof. The use of such short peptides to lower IL2, INFγ, and IL17a. The use of such peptides to increase glucose transport protein (GLUT4). Methods and materials for detecting T-cells that express CD40 (Th40 cells). | 2021-10-28 |
20210332105 | COMPOSITIONS AND METHODS OF TREATING CANCER WITH CHIMERIC ANTIGEN RECEPTORS - This disclosure relates to compositions and methods for treating cancer using armored chimeric antigen receptor cells. | 2021-10-28 |
20210332106 | NANOCARRIERS FOR LUNG INFLAMMATION THERAPY - Disclosed are lung-targeted extracellular vesicles (EVs) loaded with an anti-inflammatory cargo, as well as compositions, systems, and methods for making same. The disclosed EVs can contain a lung targeted ligand, such as a fusion protein containing a lung targeting moiety. Also disclosed is a composition comprising an EV containing the disclosed fusion protein. In some embodiments, the EV is loaded with an anti-inflammatory cargo. Also disclosed is an EV-producing cell engineered to produce the disclosed EVs. Also disclosed is a method for making the disclosed EVs that involves culturing the disclosed EV-producing cells under conditions suitable to produce EVs. | 2021-10-28 |
20210332107 | MODIFIED SERINE PROTEINASE INHIBITORS AND APPLICATIONS THEREOF - In one aspect, the disclosure relates to modified serine proteinase inhibitors with an enhanced affinity to components of the extracellular matrix, including glycosaminoglycans. The modified serine proteinase inhibitors maintain their original structure and bioactivity while simultaneously exhibiting a higher positive charge density at their glycosaminoglycan-binding surface. Furthermore, the ECM-binding affinity can be tuned by systematically increasing the number of cationic amino acid residues and/or decreasing the number of anionic amino acid residues at the glycosaminoglycan-binding surface. Also disclosed are vectors for producing the modified serine proteinase inhibitors and pharmaceutical conditions incorporating the modified serine proteinase inhibitors. | 2021-10-28 |
20210332108 | METHOD FOR PREPARING PEPTIDE FRAGMENTS, METHOD FOR PREPARING PROTEASE TO BE USED THEREIN, AND KIT FOR PREPARING PEPTIDE FRAGMENTS - The method according to the present invention for preparing peptide fragments comprises bringing an antibody, which includes a Fc domain immobilized in pores of a porous body, into contact with a protease immobilized on surface of microparticles. Thus, the Fab domain of the antibody is site-specifically cleaved by the protease and a sample containing Fab domain-derived peptide fragments at a high concentration can be obtained. The protease to be used in the present invention is an animal-derived trypsin contaminated with chymotrypsin wherein the chymotrypsin is inactivated and the trypsin is chemically modified at amino group in lysine residues. | 2021-10-28 |
20210332109 | ANTI-VARICELLA-ZOSTER VIRUS ANTIBODY, IMMUNOLOGICAL MEASUREMENT METHOD, AND IMMUNOLOGICAL MEASUREMENT DEVICE - An object of the present invention is to provide a means for rapidly diagnosing infection with VZV. The present invention relates to an antibody against VZV gE or an antibody fragment thereof, and an immunological measurement method and an immunological measurement device using the antibody or the antibody fragment thereof, etc. | 2021-10-28 |
20210332110 | Neutralizing Anti-SARS-CoV-2 Antibodies and Methods of Use Thereof - This disclosure provides novel broadly neutralizing anti-SARS-CoV-2 antibodies or antigen-binding fragments thereof. The disclosed anti-SARS-CoV-2 antibodies constitute a novel therapeutic strategy in protection from SARS-CoV-2 infections. | 2021-10-28 |
20210332111 | ANTIBODIES TO ZIKA VIRUS AND METHODS OF USE THEREOF - The present disclosure relates to antibodies specific to Zika virus and methods for detecting Zika virus infection in a subject. The present disclosure also relates to therapeutic antibodies useful in reducing viral load. | 2021-10-28 |
20210332112 | STABILIZED PERTUSSIS ANTIBODIES WITH EXTENDED HALF-LIFE - The present invention relates, in part, to modified humanized antibodies which bind the pertussis toxin protein and their use as therapeutic agents. In particular, the present invention is directed, in part, to improved humanized 1B7 and 11E6 antibodies with extended in vivo half-lives. | 2021-10-28 |
20210332113 | METHODS OF SCREENING ANTIBODIES FOR TREATING AND/OR PREVENTING NECROTIZING ENTEROCOLITIS (NEC) - Provided are antibodies that bind to bacteria associated with necrotizing enterocolitis (NEC), methods of detecting the same, and methods of using the same for treating and/or preventing NEC. The antibodies that bind to bacteria associated with NEC are detected by, e.g., detecting binding of the antibody to a bacterium in a bacterial array that includes the bacteria associated with NEC. | 2021-10-28 |
20210332114 | ANTI-TAU ANTIBODIES AND METHODS OF USE - The invention provides anti-Tau antibodies and methods of using the same. | 2021-10-28 |
20210332115 | HUMANIZED ANTI-COMPLEMENT FACTOR BB ANTIBODIES AND USES THEREOF - Provided herein are humanized anti-factor Bb antibodies, methods of producing the antibodies and methods of using the antibodies. | 2021-10-28 |
20210332116 | SINGLE DOMAIN BINDING MOLECULE - The present invention provides a single domain specific binding molecule having the structure | 2021-10-28 |
20210332117 | METHODS FOR INHIBITING MYOSTATIN ACTIVATION BY ADMINISTERING ANTI-PRO/LATENT MYOSTATIN ANTIBODIES - The present invention relates to antibodies that specifically bind pro-myostatin and/or latent myostatin, and methods and uses thereof. | 2021-10-28 |
20210332118 | MONOCLONAL ANTIBODY AND ANTIGENS FOR DIAGNOSING AND TREATING LUNG DISEASE AND INJURY - The present invention provides methods for diagnosing a patient with emphysema, COPD of lung injury caused by tobacco use by detecting the levels of EMAP II in a sample. Disclosed herein are the hypervariable regions for a rat monoclonal antibody that binds to a form of EMAP II. This disclosure also includes a polypeptide sequence included in EMAP II that is the target for the binding of the antibody to its target protein. This epitope serves as the basis for a humanized antibody that can be used to treat patients that suffer from pathologies that exhibit elevated levels of EMAP II expression. | 2021-10-28 |
20210332119 | BINDING MEMBERS TO TNF ALPHA - The present invention relates to anti-TNF alpha binding members and in particular to monovalent, high potency TNF alpha-binding antibody fragments being highly stable and soluble. Such binding members may be used in the treatment of inflammatory and other diseases as well as in diagnostics. Also provided are related nucleic acids, vectors, cells, and compositions. | 2021-10-28 |
20210332120 | TRISPECIFIC ANTIBODIES AGAINST IL-17A, IL-17F AND OTHER PRO-INFLAMMATORY MOLECULE - The present invention relates to the field of biotechnology and provides monoclonal tri-specific binding molecules that specifically bind to human IL-17A, human IL-17F, and a human pro-inflammatory molecule (in particular, TNFα) with high affinity. The invention also relates to DNA constructs encoding said binding molecules, related expression vectors and methods of production, and methods of treatment using said binding molecules. | 2021-10-28 |
20210332121 | COMBINATION THERAPY USING AN IL-20 ANTAGONIST AND AN IMMUNE CHECKPOINT INHIBITOR - Methods and compositions relating to combination therapy using an IL-20 antagonist and an immune checkpoint inhibitor are provided. | 2021-10-28 |
20210332122 | DYSREGULATION OF COVID-19 RECEPTOR ASSOCIATED WITH IBD - Provided herein are methods, systems and kits for use in identifying a subject with an increased risk of developing severe forms of inflammatory bowel disease (IBD), based at least in part, on an expression of one or more biomarkers detected in a biological sample obtained from the subject. Also provided are methods, systems and kits for treating, or optimizing the treatment for, the IBD based, at least in part, on the expression the one or more biomarkers. In some embodiments, the one or more biomarkers is angiotensin-converting enzyme 2 (ACE2), the host receptor for severe acute respiratory syndrome (SARS) coronavirus 2 (SARS-CoV-2). | 2021-10-28 |
20210332123 | ANTI-IL-25 ANTIBODIES AND USE THEREOF - The present invention provides anti-IL-25 antibodies that are directed against (human) IL-25, nucleic acids that encode such antibodies, compositions, and in particular pharmaceutical compositions that comprise such antibodies; and uses of such antibodies and compositions. | 2021-10-28 |
20210332124 | CHROMATOGRAPHY COLUMN QUALIFICATION IN MANUFACTURING METHODS FOR PRODUCING ANTI-IL12/IL23 ANTIBODY COMPOSITIONS - The present disclosure is directed to a method of operating a chromatography column in methods of manufacture for producing anti-IL-12/IL-23p40 antibodies, e.g., the anti-IL-12/IL-23p40 antibody STELARA® (ustekinumab), specific pharmaceutical compositions of the antibodies, and antigen binding fragments thereof. This method involves collecting column outlet signal and accumulated flow parameters at two or more intervals of at least one mobile phase transition front during operation of the chromatography column comprising column packing. A model gamma cumulative distribution curve is determined based on the collected column outlet signal and accumulated flow parameters for the at least one mobile phase transition front. The height equivalent theoretical plate (HETP) value is calculated for the at least one mobile phase transition front using parameters of the model gamma cumulative distribution curve and the quality of the chromatography column packing is assessed based on the calculated HETP value. If during routine column monitoring, an adverse trend in HETP is observed or the control limits are exceeded, the eluate product quality, column process performance, and/or impurity removal data should be evaluated to ensure product quality for the identified batch. Should any of the product quality or column performance fail the criteria set, appropriate corrective action, such as conditioning, repacking or replacing the column, and qualification should be performed prior to release for further use. | 2021-10-28 |
20210332125 | BIOPHARMACEUTICAL COMPOSITIONS - The present disclosure relates to compositions, for treating interleukin 5 (IL-5) mediated diseases, and related methods. | 2021-10-28 |