40th week of 2021 patent applcation highlights part 25 |
Patent application number | Title | Published |
20210309636 | INDAZOLE AMINE DERIVATIVE, PREPARATION METHOD THEREFOR AND MEDICAL USE THEREOF - Indazole derivatives represented by formula (I) or stereoisomers, tautomers, and pharmaceutically acceptable salts thereof are provided. A preparation method of indazole derivatives represented by formula (I) and a method of use of the indazole derivatives as therapeutic agents is also provided. The indazole derivatives of formula (I) are especially useful as interleukin-1 receptor-associated kinase 4 (IRAK4) inhibitors | 2021-10-07 |
20210309637 | SOLID FORMS OF A COT INHIBITOR COMPOUND - Disclosed are solid forms of a Cot (cancer Osaka thyroid) inhibitor and corresponding methods of preparation thereof, wherein the Cot inhibitor has the following formula: | 2021-10-07 |
20210309638 | 3-(1-OXOISOINDOLIN-2-YL)PIPERIDINE-2,6-DIONE DERIVATIVES AND USES THEREOF - The present disclosure provides a compound of Formula (I′): | 2021-10-07 |
20210309639 | SOLID STATE FORMS OF IVOSIDENIB - Solid state forms of Ivosidenib, processes for preparation thereof, pharmaceutical compositions thereof, and uses thereof are disclosed. | 2021-10-07 |
20210309640 | PHARMACEUTICAL SALTS OF PYRIMIDINE DERIVATIVES AND METHOD OF TREATING DISORDERS - The present disclosure relates to pharmaceutical salts and polymorphic forms of forms of pyrimidine derivatives that have inhibitory activities against mutant epidermal growth factor receptor (EGFR). The present disclosure further relates to the processes for the preparation of the pyrimidine derivatives and to the pharmaceutical salts and the polymorphic forms of the pyrimidine derivatives. | 2021-10-07 |
20210309641 | AMIDINES AND AMIDINE ANALOGS FOR THE TREATMENT OF BACTERIAL INFECTIONS AND POTENTIATION ANTIBIOTICS - Compounds and methods for the treatment of a bacterial infection or the potentiation of an antibiotic in treating a bacterial infection are described herein. | 2021-10-07 |
20210309642 | Process for Manufacture of (S)-N-(3-((2-((4-((1-acetylpyrrolidin-3-yl)(methyl)amino)phenyl)amino)-5-- methoxypyrimidin-4-yl)oxy)phenyl)acrylamide, and Formulations Thereof - The invention relates to solid forms of certain N-(pyrimidinyloxy)acrylamide derivatives that are useful in the treatment of proliferation and immunological disorders and other diseases related to the dysregulation of kinases including EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK. The invention provides methods of making these materials and their salts and polymorphs, and intermediates for preparing these materials, as well as pharmaceutical compositions comprising these materials. The solid forms and pharmaceutical compositions comprising them are useful to treat conditions including a proliferation disorder, a tumor, an inflammatory disease, an autoimmune disease, psoriasis, dry eye, rheumatoid arthritis, or lupus. | 2021-10-07 |
20210309643 | FUNCTIONALIZED MATERIALS AND COMPOUNDS - Processes for chemical functionalization of materials is described. The processed generally include chemical reaction between a thiol group of a first compound or material and an alkane group or alkyne group of a second compound or material. Also disclosed are functionalized materials and compounds suitable for functionalizing a material. | 2021-10-07 |
20210309644 | SUBSTITUTED 3-AZABICYCLO[3.1.0]HEXANES AS KETOHEXOKINASE INHIBITORS - Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof. | 2021-10-07 |
20210309645 | pH DEPENDENT PHOTOACOUSTIC COMPOUNDS AND APPLICATIONS THEREOF - In one aspect, photoacoustic compounds are described herein. A photoacoustic compound, for example, comprises two multicyclic ring moieties coupled by a rotationally restricted linkage, wherein the photoacoustic compound exhibits at least one of a pH dependent absorption spectrum, pH dependent emission spectrum and pH dependent photoacoustic spectrum. In being pH dependent, the absorption, emission and/or photoacoustic spectra of the photoacoustic compound can vary in response to environmental pH changes. Accordingly, the photoacoustic compound can provide differing photoacoustic responses based on the local pH environment. | 2021-10-07 |
20210309646 | DIACYLGLYCEROL ACYL TRANSFERASE 2 INHIBITORS - Compounds of Formula I that inhibit the activity of the diacylglycerol acyltransferase 2 (DGAT2) and their uses in the treatment of diseases linked thereto in animals are described herein. | 2021-10-07 |
20210309647 | Apoptosis Inhibitors - The invention provides compounds that are inhibitors or covalent modifiers of succinate dehydrogenase subunit B (SDHB) and/or inhibitors of apoptosis, and pharmaceutically acceptable salts, hydrates and stereoisomers thereof. The compounds are employed in pharmaceutical compositions, and methods of making and use, including treating a person in need thereof with an effective amount of the compound or composition. | 2021-10-07 |
20210309648 | MALEATE SALT OF BENZOTHIOPHENE COMPOUND, CRYSTALLINE FORM THEREOF, AND USE THEREOF - The present disclosure relates to a maleate salt of a benzothiophene compound, a crystalline form thereof, and a use thereof. Specifically, the present disclosure relates to a compound represented by formula (I-A), a crystalline form A thereof, a preparation method of a pharmaceutical composition including the same, and a use of the pharmaceutical composition in the preparation of drugs for preventing or treating diseases of the central nervous system. The compound represented by formula (I-A) and the crystalline form A thereof in the present disclosure have excellent physical and chemical properties, high oral bioavailability, excellent drugability, and are well-suited for pharmaceutical preparation, application, and preservation. | 2021-10-07 |
20210309649 | SUBSTITUTED GLUTARIMIDE DERIVATIVES - The invention relates to glutarimide compounds of formula I, (I) wherein the variables have the meanings as defined in the specification, to compositions comprising them, to active compound combinations comprising them, and to their use for protecting growing plants and animals from attack or infestation by invertebrate pests, furthermore, to seed comprising such compounds. | 2021-10-07 |
20210309650 | Process for the Prepartion of an Orexin Receptor Antagonist - The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is further directed to crystalline forms of this diazepane compound and pharmaceutical compositions thereof. | 2021-10-07 |
20210309651 | LPXC INHIBITOR AND METHODS OF MAKING - Provided herein is an LpxC inhibitor compound, as well as methods of making and pharmaceutical compositions comprising said compound, and methods of use thereof in the treatment of disease that would benefit from treatment with an LpxC inhibitor, including gram-negative bacterial infections such as urinary tract infections and the like. | 2021-10-07 |
20210309652 | ISOXAZOLINE COMPOUNDS FOR CONTROLLING INVERTEBRATE PESTS - Disclosed are Compounds of Formula 1 or 1′, | 2021-10-07 |
20210309653 | PHENOXYTRIAZOLES - The present invention relates to a compound of formula I, HetAr is a five or six membered heteroaryl group, selected from wherein R | 2021-10-07 |
20210309654 | 5-SUBSTITUTED 4-AMINO-1H-BENZO[c][1,2,6]THIADIAZINE 2,2-DIOXIDES AND FORMULATIONS AND USES THEREOF - Disclosed herein are 5-Substituted 4-amino-1H-benzo[c] [1,2,6]thiadiazine 2,2-dioxide compounds useful as sweet flavor modifiers. Also disclosed herein are ingestible compositions that include one or more of these compounds in combination with a natural or artificial sweetener. | 2021-10-07 |
20210309655 | KINASE INHIBITORS AND METHODS FOR MAKING AND USING - Disclosed embodiments concern kinase inhibitors, such as interleukin receptor associated kinases (IRAK) inhibitors, and compositions comprising such inhibitors. Also disclosed are methods of making and using the compounds and compositions. The disclosed compounds and/or compositions may be used to treat or prevent a kinase-associated disease or condition, particularly an IRAK-associated disease or condition. | 2021-10-07 |
20210309656 | COMPOUNDS USEFUL IN MODULATING THE FARNESOID X RECEPTOR AND METHODS OF MAKING AND USING THE SAME - Provided are compounds that can act as a modulator of a farnesoid X receptor (FXR) and that can be useful in the treatment of diseases and/or disorders associated with the FXR. Compositions including such compounds are also provided along with methods for preparing compounds of the present invention and their use. | 2021-10-07 |
20210309657 | TRICYCLIC COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF BACTERIAL INFECTION - The present invention relates to novel compounds of formula (I), | 2021-10-07 |
20210309658 | ARYL COMPOUNDS FOR THE TREATMENT AND PROPHYLAXIS OF BACTERIAL INFECTION - The present invention relates to novel compounds of formula (I), | 2021-10-07 |
20210309659 | 5,7-DIHYDRO-PYRROLO-PYRIDINE DERIVATIVES - The present invention provides, in part, compounds of Formula I: | 2021-10-07 |
20210309660 | (4-HYDROXYPYRROLIDIN-2-YL)-HETEROCYCLIC COMPOUNDS AND METHODS OF USE THEREOF - The present disclosure relates to bifunctional compounds, which can be used as modulators of targeted ubiquitination. In particular, the present disclosure is directed to compounds which contain on one end a VHL ligand moiety, which binds to the VHL E3 ubiquitin ligase, and on the other end a moiety that binds a target protein such that degradation of the target protein/polypeptide is effectuated. Also disclosed are VHL ligands. | 2021-10-07 |
20210309661 | IMIDAZO[1,5-a]PYRIMIDINYL CARBOXAMIDE COMPOUNDS AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS - The invention provides substituted imidazo[1,5-a]pyrimidinyl carboxamide and related organic compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat medical disorders, e.g., Gaucher disease, Parkinson's disease, Lewy body disease, dementia, or multiple system atrophy, in a patient. Exemplary substituted imidazo[1,5-a]pyrimidinyl carboxamide compounds described herein include substituted 2-heterocyclyl-4-alkyl-imidazo[1,5-a]pyrimidine-8-carboxamide compounds and variants thereof. | 2021-10-07 |
20210309662 | TREATMENT OF COGNITIVE AND MOOD SYMPTOMS IN NEURODEGENERATIVE AND NEUROPSYCHIATRIC DISORDERS WITH ALPHA5-CONTAINING GABAA RECEPTOR AGONISTS - Provided herein are alpha5-containing GABA | 2021-10-07 |
20210309663 | COMPOUNDS AND COMPOSITIONS FOR INHBITING THE ACTIVITY OF SHP2 - The present invention relates to compounds of formula I: | 2021-10-07 |
20210309664 | BENZODIAZEPINE DERIVATIVES AS GABA A GAMMA1 PAM - Compounds having the general formula (I) | 2021-10-07 |
20210309665 | COMPOUND HAVING TRKA INHIBITORY ACTIVITY AND PHARMACEUTICAL COMPOSITION, FOR PREVENTING OR ALLEVIATING PAIN, CONTAINING SAME AS ACTIVE INGREDIENT - The present invention relates to a compound having TrkA inhibitory activity and a pharmaceutical composition for preventing or treating pain containing the same as an active ingredient. The compound provided in one aspect of the present invention has excellent TrkA inhibitory activity and exhibits excellent pain inhibitory effects in an animal model of pain after a surgery, and thus can be effectively used as an analgesic. | 2021-10-07 |
20210309666 | SMALL MOLECULE MDM2 PROTEIN DEGRADERS - The present disclosure provides compounds represented by Formula I: | 2021-10-07 |
20210309667 | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2- -TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF - The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process. | 2021-10-07 |
20210309668 | BICYCLIC COMPOUNDS AS KINASE MODULATORS, METHODS AND USES THEREOF - The present disclosure relates to derivatives of bicyclic compounds and their uses in therapy. In particular, the present disclosure relates to derivatives of bicyclic compounds for use in modulating kinase enzymatic activity and accordingly modulating kinase-dependent diseases and conditions such as cancer and in specific embodiments, hepatocellular carcinoma (HCC). The present disclosure also relates to methods of synthesizing these compounds. | 2021-10-07 |
20210309669 | Heterocyclic Spiro Compounds As MAGL Inhibitors - The present invention provides, in part, a compound selected from the group consisting of:
| 2021-10-07 |
20210309670 | DIISOCYANATE COMPOUND HAVING ANHYDROSUGAR ALCOHOL CORE AND PREPARATION METHOD THEREFOR - The present invention relates to a diisocynate compound having anhydrosugar alcohol core and a preparation method therefor and, more specifically, to a diisocynate compound having anhydrosugar alcohol core and a preparation method therefor, wherein the diisocynate compound is prepared through a reaction with a nitrile compound, a hydrogenation reaction, and an end-group substitution reaction while a recyclable, plant-based anhydrosugar alcohol or anhydrosugar alcohol-alkylene glycol is used as a raw material, and the diisocynate compound can be utilized in various fields, such as soft or hard polyurethane expanded foams, molded foams, coating, adhesives or glues, fibers, and polymer synthesis. | 2021-10-07 |
20210309671 | TRICYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS - The present invention relates to Tricyclic Heterocycle Compounds of Formula (I): (I) and pharmaceutically acceptable salts or prodrug thereof, where-in R | 2021-10-07 |
20210309672 | 2-(4-{1-[6-(4-Isopropyl-phenyl)-imidazo[2,1-b][1,3,4]thiadiazol-2-yl]-pipe- ridin-4-ylmethyl}-piperazin-1-yl)-ethanol and use thereof - The present disclosure is directed to a compound of formula (I) (E266) and its acceptable pharmaceutical salts, to pharmaceutical compositions comprising the compound and its use in the manufacture of medicaments for treating diseases. | 2021-10-07 |
20210309673 | ALKALI METAL MONOHYDROGEN CYANURATE COMPOUND, CRYSTAL THEREOF, PREPARATION METHOD THEREFOR AND USE THEREOF - An alkali metal monohydrogen cyanurate compound of the chemical formula AM(HC | 2021-10-07 |
20210309674 | ENERGY-EFFICIENT SOLVENT-FREE METHOD FOR PRODUCING METAL CHELATES - The invention relates to a method for producing, amongst other things, amino-acid and/or hydroxycarboxylic-acid metal chelates, a solvent-free mixture of at least one metal oxide, metal hydroxide, metal carbonate or oxalate, and the solid organic acid is subjected to intensive mechanical stress. According to the invention, this is done in that the reaction partners are introduced in particle form into a fluid stream of a fluid-bed countercurrent mill operating without grinding elements, wherein mechanical activation of at least one of the reaction partners is effected by collision processes within a reaction chamber formed in a region of the fluid stream, and a solid body reaction to form the metal chelate is triggered. The novel method operates very energy-efficiently and with a high specific yield. It leads to a product having compact particles in the small, single-digit micrometer range having a comparatively narrow particle size distribution and a large surface. The product is homogenous and very pure. Thermal loading or decomposition of the organic chelate ligands, in particular of the amino acids, is likewise avoided, as are contaminants from milling and grinding element abrasion. | 2021-10-07 |
20210309675 | Compound, A Display Panel and A Display Device - The present invention relates to a compound, a display panel and a display device. The compound has a structure represented by Formula I. The compound takes a spiro structure as a non-conjugated connecting unit, and a boron-containing group as an electron-accepting group. A light-emitting compound obtained by taking the group as a building block has a narrower half-peak width and higher color purity. The boron-containing spirt structure is connected with an electron-donating group to obtain a bipolar compound, and as a thermal activation delay fluorescence material, the bipolar compound can be used a light-emitting layer material, particularly a doped material, and can also be used as a fluorescent host material or a phosphorescent host material. The compound provided herein can achieve low drive voltages and high luminescence efficiencies when applied to organic electroluminescent devices. | 2021-10-07 |
20210309676 | COMPONENTS AND CATALYSTS FOR THE POLYMERIZATION OF OLEFINS - A solid catalyst component for the polymerization of olefins CH | 2021-10-07 |
20210309677 | NOVEL AMINOPHOSPHINIC DERIVATIVES AS AMINOPEPTIDASE A INHIBITORS - The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to a compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma. | 2021-10-07 |
20210309678 | AMINOPEPTIDASE A INHIBITORS AND PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME - The present invention relates to a novel compound, to a composition comprising the same, to methods for preparing the compound, and the use of this compound in therapy. In particular, the present invention relates to a compound that is useful in the treatment and prevention of primary and secondary arterial hypertension, ictus, myocardial ischaemia, cardiac and renal insufficiency, myocardial infarction, peripheral vascular disease, diabetic proteinuria, Syndrome X and glaucoma. | 2021-10-07 |
20210309679 | BISPHOSPHONATE DRUG CONJUGATES - Provided herein are novel conjugates of TGF-beta inhibitors and bisphosphonates, pharmaceutical compositions comprising the conjugates, methods of preparing the conjugates, and methods of using the conjugates, for example, for the treatment of a bone disease or disorder, such as osteoarthritis. | 2021-10-07 |
20210309680 | PROTEIN PROXIMITY ASSAY IN FORMALIN FIXED PAFFAFIN EMBEDDED TISSUE USING CAGED HAPTENS - Disclosed herein are caged haptens and caged hapten-antibody conjugates useful for enabling the detection of targets located proximally to each other in a sample. | 2021-10-07 |
20210309681 | PREPARATION METHOD AND USE OF GRAPHITE FELT (GF)-SUPPORTED METAL-ORGANIC FRAMEWORK (MOF) CATHODE MATERIAL - A preparation method and use of a graphite felt (GF)-supported metal-organic framework (MOF) cathode material is disclosed. The preparation method includes the following steps: preparing an iron salt, Pluronic F127, a weak acid, 2-aminoterephthalic acid, and a carbon felt; adding the iron salt and Pluronic F127 to deionized water and stirring a resulting mixture; adding the weak acid and 2-aminoterephthalic acid to the mixture, and stirring a resulting mixture to obtain an MOF precursor solution; adding the MOF precursor solution together with a pretreated carbon felt to a reactor, and sealing the reactor for hydrothermal reaction; and washing and vacuum drying a reaction product to obtain the cathode material. With a porous structure and a large specific surface area (SSA), the cathode material significantly increases the output of H | 2021-10-07 |
20210309682 | PROCESS FOR PREPARING MANNOSE DERIVATIVES - The invention relates to a process to prepare a compound of the following formula (I): (I), in which P represents a protective group of a hydroxyl function which is a —COR | 2021-10-07 |
20210309683 | Method for Synthesizing O-Antigen Saccharide Chain of Helicobacter pylori serotype O:6 - Disclosed is a method for synthesizing an 0-antigen saccharide chain of | 2021-10-07 |
20210309684 | Analogs of the Natural Product Icariin - Provided herein are analogs of the natural product icariin represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The analogs can be used to modulate (e.g., inhibit, such as by competitive inhibition) PDE5 and thereby treat a wide range of PDE5-mediated diseases, including cardiovascular, gastrointestinal, pulmonary, musculoskeletal, neurological and reproductive diseases. Also provided herein are compositions and methods including compounds of Structural Formula (I). | 2021-10-07 |
20210309685 | AMINO ACID SALTS OF NICOTINIC ACID MONONUCLEOTIDE AND NICOTINAMIDE MONONUCLOETIDE AS ANTI-AGEING AGENTS - The present invention relates to amino acid salts of nicotinic acid mononucleotides and nicotinamide mononucleotides and compositions thereof of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in NAD | 2021-10-07 |
20210309686 | QUATERNARY AMMONIUM SALTS OF NICOTINIC ACID AND NICOTINAMIDE MONONUCLOETIDES AND RIBOSIDES AS ANTI-AGING AGENTS - The present invention relates to amino acid salts of nicotinic acid and nicotinamide and compositions thereof of Formula I, useful in the treatment of disorders and diseases associated with deficiencies in NAD | 2021-10-07 |
20210309687 | PRMT5 INHIBITORS - The present invention provides a compound of formula (I) Formula (I) and the pharmaceutically acceptable salts, esters, and prodrugs thereof, are PRMT5 inhibitors. Also provided are methods of making compounds of formula (I), pharmaceutical compositions comprising compounds of formula (I), and methods of using these compounds to treat cancer, sickle cell, and hereditary persistence of foetal hemoglobin (HPFH) mutations. | 2021-10-07 |
20210309688 | PRMT5 INHIBITORS - The present invention provides a compound of Formula (I) or the pharmaceutically acceptable salts thereof, which are PRMT5 inhibitors. | 2021-10-07 |
20210309689 | METHODS OF PREPARING 1'-CYANO NUCLEOSIDES - The present disclosure generally describes methods of preparing 1′-cyano nucleosides, such as a compound of Formula (I). For example, the compound of Formula (I) can be prepared from a compound of Formula (II-a) in a flow reactor. | 2021-10-07 |
20210309690 | OLIGONUCLEOTIDE SYNTHESIS - The invention relates to a process for the manufacture of an oligonucleotide comprising at least one non-chiral phosphorothioate intemucleoside linkage of formula (I) wherein R | 2021-10-07 |
20210309691 | METHODS AND COMPOSITIONS FOR NUCLEOSIDE TRIPHOSPHATE AND RIBONUCLEIC ACID PRODUCTION - Provided herein, in some embodiments, are methods and composition for the production of nucleoside triphosphates and ribonucleic acids. | 2021-10-07 |
20210309692 | COMPOUNDS, COMPOSITIONS, AND METHODS FOR THE TREATMENT OF DISEASE - Disclosed are compounds and compositions for the activation or induction of expression of a pattern recognition receptor (e.g., STING, RIG-I, MDA5), and methods of use thereof. | 2021-10-07 |
20210309693 | NOVEL GINSENOSIDE AND ANTI-INFLAMMATORY COMPOSITION COMPRISING SAME - The present specification relates to (20S,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20,24-epoxy-6a,12b,25-triol, which is a novel ginsenoside, a pharmaceutically acceptable salt thereof, a hydrate thereof or a solvate thereof. The novel ginsenoside exhibits excellent anti-inflammatory effects. | 2021-10-07 |
20210309694 | DEUTERATED COMPOUNDS, COMPOSITIONS, AND METHODS FOR TREATING CANCERS ASSOCIATED WITH ETBR ACTIVATION - Disclosed herein are deuterated compounds, pharmaceutical compositions thereof, and methods for treating ETBR-related cancers. Also disclosed herein is a delivery system for the controlled, systemic release of at least one deuterated ETBR antagonist, optionally in conjunction with an additional anti-oncologic agent. | 2021-10-07 |
20210309695 | PROTEASOME INHIBITORS - Unique compounds useful for inhibiting a proteasome in a cell, pharmaceutical compositions and methods of their use are provided herein. | 2021-10-07 |
20210309696 | NEW CONJUGATES OF MONTELUKAST AND PEPTIDES - There is provided a peptide-containing compound that comprises a peptide component which is an amino acid sequence of from 2 to 45 (e.g. from 6 to 15) amino acids, which peptide component is covalently bonded to one or more compounds of the formula I: | 2021-10-07 |
20210309697 | COMPOSITIONS AND METHODS FOR TREATING CD40-MEDIATED DISEASES - A cell-penetrating peptide includes a membrane transduction domain linked to a CD40-TRAF2,3 blocking peptide that includes an amino acid sequence substantially identical to the amino acid sequence of the TRAF2,3 binding domain to CD40 or a retro-inverso amino acid sequence thereof. | 2021-10-07 |
20210309698 | METHODS FOR TREATMENT AND DIAGNOSIS OF NON-ALCOHOLIC STEATOHEPATITIS AND/OR HEPATOCELLULAR CARCINOMA - Methods for treating non-alcoholic steatohepatitis and/or hepatocellular carcinoma include administering a polypeptide antagonist of a Na/K ATPase/Src receptor complex to a subject in need thereof. Methods and assays for diagnosis or prognosis of non-alcoholic steatohepatitis and/or hepatocellular carcinoma in a subject are also provided and include the steps of providing a biological sample from the subject, determining an expression level or activity in the sample of at least one biomarker selected from Caveolin-1, Survivin, and SMAC; and comparing the expression level or activity of the at least one biomarker in the sample, if present, to a control expression level or activity of the at least one biomarker. Prophylaxis or treatment of the non-alcoholic steatohepatitis and/or hepatocellular carcinoma in a subject can then be initiated based on the expression level or activity of Caveolin-1, Survivin, and SMAC in the sample. | 2021-10-07 |
20210309699 | METHOD OF MANUFACTURING A PHARMACEUTICAL COMPOSITION - The present invention relates to crystalline forms of carbetocin, a method of their manufacture, and pharmaceutical compositions thereof. | 2021-10-07 |
20210309700 | MODIFIED PEPTIDE NUCLEIC ACID COMPOSITIONS - The present disclosure relates to compounds useful for the detection or modulation of target nucleic acids, including DNA and RNA. The present disclosure further relates to methods for treatment of trinucleotide repeat disorders, which can include administration of oligonucleotide analogues that can bind pathogenic nucleotide repeats in DNA or RNA. | 2021-10-07 |
20210309701 | Inducible, Tunable, and Multiplex Human Gene Regulation Using CRISPR-Cpf1 - Drug-inducible, tunable, and multiplexable Clustered Regularly Interspaced Short Palindromic Repeats from | 2021-10-07 |
20210309702 | Programmable Designer Therapeutic Fusogenic Secreted Gectosome Vesicles For Macromolecule Delivery And Genome Modification - The invention includes systems, methods, and compositions for designing secreted fusogenic ectosome vesicles, or gectosomes, that selectively encapsulate specific target proteins, nucleic acids and/or other small molecules in a predetermined manner. These engineered gectosomes can be used to deliver desired cargos to receipt cells in vitro, ex vivo, or in vivo and may further reprogram target cellular phenotypes in a dose-dependent manner, as well as perform genome editing functions, among others. | 2021-10-07 |
20210309703 | ENTEROCINS AND METHODS OF USING THE SAME - The present disclosure relates to the identification, cloning, and expression of a genetic locus within an | 2021-10-07 |
20210309704 | WNT SIGNALING AGONIST MOLECULES - Novel therapeutic agents, particularly those capable of activating (GPR)124/RECK/Frizzled/lipoprotein receptor-related protein (LRP)-mediated Wnt signaling, while not activating Frizzled/LRP-mediated Wnt signaling in the absence of RECK and/or GPR124. The agents are particularly useful for the prevention or treatment of neurovascular disorders or central nervous system (CNS) disorders including neurovascular dysfunction. | 2021-10-07 |
20210309705 | SYSTEMS AND METHODS FOR INHIBITING gamma-SECRETASE PRODUCTION OF AMYLOID-beta PEPTIDES - Inhibitors are provided for targeting γ-secretase to reduce amyloid load as a viable strategy in Alzheimer's disease treatment and drug discovery. γ-secretase has been shown to cleave amyloid precursor protein, causing an increase in extracellular concentration of amyloid-β peptides. This extracellular concentration increase can lead to build-up amyloid plaques in patients and associated health complications for them. The inhibitors bind to a C-terminal lysine cluster adjacent the transmembrane domain of amyloid precursor protein through both covalent and non-covalent interactions. These interactions inhibit the ability of γ-secretase to cleave the amyloid precursor protein, halting the build-up of extracellular amyloid-β peptides. The inhibitors exhibit specificity for amyloid precursor proteins, reducing concerns of potential off-target effects. | 2021-10-07 |
20210309706 | METHOD OF RESPONSE PREDICTION FOR BCL2 FAMILY PROTEIN TARGETING DRUG - Provided are a method for prediction of a response to a BCL2 family protein-targeting drug and a method for selection of a subject suitable for treatment with a BCL2 family protein-targeting drug. | 2021-10-07 |
20210309707 | INTERFERON-GAMMA BIASED AGONISTS - Disclosed herein are compositions and methods for modulating IFN-γ-mediated signaling by completely or partially agonizing the downstream signal transduction mediated through at least one of the IFN-γ receptors. More particularly, the disclosure provides novel IFN-γ polypeptide variants with reduced binding affinity to at least one of its receptors. The disclosure also provides compositions and methods useful for producing such molecules, as well as methods for the treatment of health diseases associated with the perturbation of signal transduction mediated by IFN-γ. | 2021-10-07 |
20210309708 | GLUCAGON-LIKE-PEPTIDE-2 (GLP-2) ANALOGUES - GLP-2 analogues are disclosed which comprise one of more substitutions as compared to [hGly2]GLP-2 and which improved biological activity in vivo and/or improved chemical stability, e.g., as assessed in in vitro stability assays. More particularly, preferred GLP-2 analogues disclosed herein comprise substitutions at one or more of positions 8, 16, 24 and/or 28 of the wild-type GLP-2 sequence, optionally in combination with further substitutions at position 2 (as mentioned in the introduction) and one or more of positions 3, 5, 7, 10 and 11, and/or a deletion of one or more of amino acids 31 to 33 and/or the addition of a N-terminal or C-terminal stabilizing peptide sequence. The analogues are particularly useful for the prophylaxis or treatment of stomach and bowel-related disorders and for ameliorating side effects of chemotherapy. Also disclosed are methods and kits for selecting a patient from populations suited for treatment with GLP-2 analogues. | 2021-10-07 |
20210309709 | ULTRA-LONG ACTING INSULIN-FC FUSION PROTEINS AND METHODS OF USE - The present disclosure provides recombinantly manufactured ultra-long acting insulin-Fc fusion proteins for use in treating diabetes. The insulin-Fc fusion proteins comprise an insulin polypeptide linked via a peptide linker to an Fc-fragment of human origin. Based on the results obtained, creating a treatment that is amenable to low cost manufacturing, exhibits sufficient in vivo bioactivity, displays extended duration of bioactivity, and does not exhibit immunogenicity requires a non-obvious combination of insulin polypeptide, peptide linkers, and Fc fragment, in addition to selective mutations on one or more of these components. Exemplary ultra-long acting insulin-Fc fusion proteins, polynucleotides encoding these insulin-Fc fusion proteins, and pharmaceutical formulations of exemplary insulin-Fc fusion proteins are provided, in addition to methods of use and preparation. | 2021-10-07 |
20210309710 | METHOD FOR PRODUCING ACTIVE FORM OF LONG-ACTING INSULIN ANALOGUE DERIVATIVE USING CLOSTRIPAIN - The present invention relates to a method for producing an active form of a long-acting insulin analogue derivative, in which the amino acid at position 22 of the insulin B-chain is substituted from arginine (Arg) to lysine (Lys), so that the insulin analogue can be converted to an active form without cleavage of the B-chain even when it is reacted with clostripain. In a conventional method of converting pro-insulin to an active form by use of trypsin, an albumin binding domain is cleaved, making it difficult to convert the long-acting insulin analogue derivative to an active form. The production method according to the present invention overcomes this difficulty, and thus it can be effectively used for the production of a long-acting therapeutic agent for treatment of diabetes. | 2021-10-07 |
20210309711 | ANTI-LYPD3 CAR T-CELL THERAPY FOR THE TREATMENT OF CANCER - The present disclosure relates to a chimeric antigen receptor (CAR) molecule that specifically binds LYPD3, and also provides compositions comprising CAR T-cell-derived effector cells specific for LYPD3 and methods of making and using same. | 2021-10-07 |
20210309712 | CAR-EXPRESSING T CELLS AND CAR EXPRESSION VECTOR - The present invention provides immune cells (such as CAR-T cells) having higher antitumor activity than immune cells (such as CAR-T cells) expressing a CAR alone (not expressing cytokines and/or chemokines). A T cell provided in one aspect of the present invention expresses (1) a chimeric antigen receptor (CAR), (2) at least one selected from the group consisting of interleukin-15 (IL-15), interleukin-18 (IL-18), interleukin-21 (IL-21), and interleukin-27 (IL-27), and (3) CC chemokine ligand 19 (CCL19). | 2021-10-07 |
20210309713 | Chimeric Antigen Receptor and Method for Treating Cancers - The present disclosure provides a chimeric antigen receptor and a combination of the chimeric antigen receptor and DAP10. The present disclosure provides an expression vector and a host cell for expressing the chimeric antigen receptor and said combination of the chimeric antigen receptor and DAP10. The present disclosure also provides use of the chimeric antigen receptor and the combination of the chimeric antigen receptor and DAP10 in the treatment of cancers or in the preparation of pharmaceutical compositions for treating cancers. The chimeric antigen receptor and the drugs provided in the present disclosure can effectively treat liver cancer, lung cancer and the like. | 2021-10-07 |
20210309714 | REDIRECTED CELLS WITH MHC CHIMERIC RECEPTORS AND METHODS OF USE IN IMMUNOTHERAPY - Chimeric receptors featuring major histocompatibility molecules grafted onto T cell receptor molecules and surrogate co-receptors featuring cell surface receptor ligands fused with signaling molecule domains. The chimeric receptors can be used to redirect cells, altering their specificity. T cells expressing chimeric receptors may bind to TCRs of target T cells for which their chimeric receptors are specific. Surrogate co-receptors may be used to help enhance TCR-CD3 signaling as part of this modular receptor system. The chimeric receptors and surrogate coreceptors may be used to help eliminate autoreactive T cells or program T cells to desired effector functions. | 2021-10-07 |
20210309715 | UTERINE CANCER TREATMENTS - The present invention relates to peptides, proteins, nucleic acids and cells for use in immunotherapeutic methods. In particular, the present invention relates to the immunotherapy of cancer. The present invention furthermore relates to tumor-associated T-cell peptide epitopes, alone or in combination with other tumor-associated peptides that can for example serve as active pharmaceutical ingredients of vaccine compositions that stimulate anti-tumor immune responses, or to stimulate T cells ex vivo and transfer into patients. Peptides bound to molecules of the major histocompatibility complex (MHC), or peptides as such, can also be targets of antibodies, soluble T-cell receptors, and other binding molecules. | 2021-10-07 |
20210309716 | CHIMERIC ANTIGEN RECEPTOR - The present invention provides a chimeric antigen receptor (CAR) comprising a CD21− binding domain, a transmembrane domain and an intracellular domain. | 2021-10-07 |
20210309717 | Novel Recombinant Cell Surface Markers - The present disclosure relates to EGFR-derived polypeptides containing short juxtamembrane sequences, nucleic acids encoding them, and methods of using them to improve cell surface expression of truncated EGFR markers. | 2021-10-07 |
20210309718 | SOLUBLE FIBROBLAST GROWTH FACTOR RECEPTOR 3 (SFGFR3) POLYPEPTIDES AND USES THEREOF - The invention features soluble fibroblast growth factor receptor 3 (sFGFR3) polypeptides. The invention also features methods of using sFGFR3 polypeptides to treat skeletal growth regardation disorders, such as achondroplasia. | 2021-10-07 |
20210309719 | ARGININE-FREE TNFR:FC-FUSION POLYPEPTIDE COMPOSITIONS AND METHODS OF USE - Aspects of the invention are directed to arginine-free polypeptide-containing compositions and methods for treating disorders associated with inflammation or the autoimmune response. In particular, the polypeptide is etanercept. | 2021-10-07 |
20210309720 | QTY FC Fusion Receptor Proteins - The present invention is directed to QTY CCR9 and CXCR2 variant Fc receptor fusion proteins, methods for the preparation thereof and methods of use thereof. | 2021-10-07 |
20210309721 | I DOMAIN CHIMERIC ANTIGEN RECEPTOR SPECIFIC TO ICAM-1 - The present invention relates to chimeric antigen receptors (CARs) specific to ICAM-1 comprising I domain of the (XL subunit of human lymphocyte function-associated antigen 1 (LFA-1). The invention particularly relates to CARs comprising human I domains having different affinities (1 mM to 1 nM Kd) to ICAM-1. CAR T cells comprising human I domain having a low affinity (1 to 200 μM Kd) to ICAM-1 can avoid targeting healthy tissues with basal ICAM-1 expression while simultaneously exhibiting increased potency and long-term efficacy against tumor tissues with high ICAM-1 expression. The present invention also relates to an adoptive cell therapy method for treating cancer by administering the CAR-T cells comprising human I domain to a subject suffering from cancer, whereby the CAR T cells bind to the cancer cells overexpressing ICAM-1 and kill the cancer cells. | 2021-10-07 |
20210309722 | DUAL AGONIST FUSION PROTEINS - Disclosed herein are fusion proteins including an elastin-like peptide domain, a GLP-1 receptor agonist domain attached N to a N-terminal end of the ELP domain, and a FGF21 receptor agonist domain attached to the C-terminal end of the ELP domain. Also disclosed are methods of making the fusion proteins, compositions including a plurality of fusion proteins, and uses of the fusion proteins and compositions. | 2021-10-07 |
20210309723 | RECOMBINANT PRODUCTION OF A COLLAGEN PEPTIDE PREPARATION AND USE THEREOF - The present invention relates to a method for producing collagen peptide preparations comprising recombinant collagen peptides, to collagen peptide preparations produced by means of said methods, to products containing the collagen peptide preparations and to uses of the aforementioned preparations and products. | 2021-10-07 |
20210309724 | COMPOSITIONS AND METHODS FOR THE DELIVERY OF THERAPEUTIC BIOLOGICS FOR TREATMENT OF DISEASE - The present disclosure provides compositions and methods for treating a disease or condition in a subject in need thereof, comprising administering to the subject a pharmaceutically effective amount of a composition comprising a plurality of particles comprising at least one therapeutic biologic suspended in a pharmaceutically acceptable liquid carrier. | 2021-10-07 |
20210309725 | TREATMENT OF MOST BOTHERSOME SYMPTOM (MBS) ASSOCIATED WITH MIGRAINE USING ANTI-CGRP ANTIBODIES - Methods for treatment of most bothersome symptom (MBS) associated with migraine are provided. Exemplary methods provide improvement in MBS associated with migraine within 1 month of administration og anti-CGRP antibodies of the invention. Also provided are methods for improvement of patient impression of change (PGIC) associated with migraine. Exemplary methods comprise administration of an anti-CGRP antagonistic antibody to a patient in need thereof. | 2021-10-07 |
20210309726 | TREATMENT OF MELANOMA BRAIN METASTASIS BY INHIBITION OF AMYLOID PRECURSOR PROTEIN CLEAVAGE - Provided are methods for treating cancer brain metastases by inhibiting amyloid precursor protein (APP) cleavage or the activity of the APP cleavage products, or both in the brain. The process may be inhibited by an inhibitor of α-, β-, or γ-secretase, or by an antibody specific for one or more of sAPPα, sAPPβ, CTF83, CTF99, p3, Aβ, and AICD. | 2021-10-07 |
20210309727 | ACTIVATABLE ANTIBODIES HAVING NON-BINDING STERIC MOIETIES AND METHODS OF USING THE SAME - The invention relates generally to activatable antibodies and methods of making and using these activatable antibodies in a variety of therapeutic, diagnostic and prophylactic indications. | 2021-10-07 |
20210309728 | FUSION PROTEIN CONSTRUCTS FOR COMPLEMENT ASSOCIATED DISEASE - Provided herein are fusion protein constructs that can bind a complement-associated antigen, comprising a targeting moiety and a complement modulator protein, or a fragment thereof or a variant thereof. The targeting moiety is an antibody or an antigen binding fragment thereof, in some examples. Further provided are methods of using the fusion protein constructs, for example, in treating complement mediation conditions. | 2021-10-07 |
20210309729 | NETRIN G1 AS A BIOMARKER FOR ENHANCING TUMOR TREATMENT EFFICACY - The present disclosure provides methods of inducing desmoplastic stroma to express a normal phenotype by detecting increased levels of NetG1 or NGL1 in tumor or in desmoplastic stroma isolated from a human subject, and/or detecting NetG1 in circulating extracellular vesicles, and/or detecting increased pFAK in the stroma, and treating the human subject with a therapeutic regimen; and by detecting NetG1 in a microvesicle isolated from a human subject, and/or treating the human subject with a therapeutic regimen. | 2021-10-07 |
20210309730 | MULTISPECIFIC ANTIBODIES - The present invention relates to multispecific antibodies, their manufacture and use. | 2021-10-07 |
20210309731 | COMPOSITION OF A DRUG CARRIER, PHARMACEUTICAL COMPOSITION THEREOF, PREPARATION METHOD AND USE METHOD THEREOF - A composition of a drug carrier, a pharmaceutical composition thereof, a preparation method and a use method thereof are provided. The composition of a drug carrier includes a first mixture and a second mixture. The first mixture includes a hydrophilic polymer, tricalcium phosphate and a water-soluble dispersant. The second mixture includes a water-absorbing material and a divalent cation salt. The pharmaceutical composition includes the composition of a drug carrier above and a drug for preparing an anti-inflammatory or antibiotic medicine. The preparation method of the composition of a drug carrier includes mixing the first mixture and the second mixture. The use method of the composition of a drug carrier includes mixing the first mixture with a drug and then adding the second mixture. Accordingly, topically applying the pharmaceutical composition on a surgical site may effectively release the drug thereon. | 2021-10-07 |
20210309732 | ANTIBODIES TO GRANULOCYTE-MACROPHAGE COLONY STIMULATING FACTOR AND USES THEREOF - Disclosed herein are anti-GM-CSF antibodies capable of binding to human GM-CSF and blocking its biological activities. Also provided herein are pharmaceutical compositions comprising the anti-GM-CSF antibodies and therapeutic and diagnostic uses of such antibodies. | 2021-10-07 |
20210309733 | METHODS FOR TREATING CORONAVIRUS INFECTION AND RESULTING INFLAMMATION-INDUCED LUNG INJURY - The present invention provides methods for treating a subject infected with 2019 coronavirus (SARS-CoV-2) comprising administering to the subject a therapeutically effective amount of a GM-CSF antagonist or a therapeutically effective amount of a GM-CSF antagonist and a second drug, including an anti-viral agent, an anti-SARS-CoV-2 vaccine, and serum containing human polyclonal antibodies to SARS-CoV-2. | 2021-10-07 |
20210309734 | ANTIBODY MOLECULES WHICH BIND IL-17A AND IL-17F - The invention relates to antibody molecules having specificity for antigenic determinants of both IL-17A and IL-17F, therapeutic uses of the antibody molecules and methods for producing said antibody molecules. | 2021-10-07 |
20210309735 | ANTI-IL-17A ANTIBODIES AND USE THEREOF - The present disclosure provides an antibody, or an antigen binding fragment thereof, which specifically binds to IL-17A with high affinity. The present disclosure also provides a method for preparing and using said antibody. | 2021-10-07 |