07th week of 2022 patent applcation highlights part 21 |
Patent application number | Title | Published |
20220048848 | POLYMORPHIC FORMS OF RAD1901-2HCL - Various polymorphic forms of RAD1901-2HCl, including three crystalline and amorphous forms, are prepared and characterized. Uses of the various polymorphic forms of RAD1901-2HCl for cancer treatment are also disclosed. | 2022-02-17 |
20220048849 | DECARBOXYLASE INHIBITORS FOR TREATING PARKINSON'S DISEASE - Provided are inhibitors of pathogenic, bacterial metabolite production and conjugates of the inhibitors. Also provided are pharmaceutical compositions containing the inhibitors or conjugates and methods of using the same. | 2022-02-17 |
20220048850 | COMPOSITIONS AND METHODS FOR THE TREATMENT OF INFLAMMATION - The disclosures herein provide compounds of formula I or its pharmaceutical acceptable salts, as well as polymorphs, enantiomers, stereoisomers, solvates, and hydrates thereof. These compounds may be formulated as pharmaceutical compositions. The pharmaceutical compositions may be formulated for oral administration, intravenous, spray, parenteral, lozenge, solution, syrup, sachet, transdermal administration, or injection. Such compositions may be used to treatment of inflammation or its associated complications. | 2022-02-17 |
20220048851 | MIXED METAL OXIDE CATALYSED AND CAVITATION INFLUENCED PROCESS FOR HYDRATION OF NITRILE - The present invention discloses a metal-catalyzed process for hydration of nitrile under the influence of the ultrasonic cavitation effect. The present invention further discloses a catalyst of formula (I), wherein the catalyst is used for process for hydration of nitrile and process for preparation thereof. | 2022-02-17 |
20220048852 | PROCESS OF PREPARING IOSIMENOL - The present invention relates to a 5-step process for preparing iosimenol starting from ammonium 3-amino-5-(aminocarbonyl)benzoate which is first converted to 3-amino-5-(aminocarbonyl)-2,4,6-triiodobenzoic acid using sodium iodine dichloride (NaICl | 2022-02-17 |
20220048853 | PROCESS FOR THE PRODUCTION OF UREA FORMALDEHYDE CONCENTRATE - Parallel co-production process for the production of methanol and urea product from a hydrocarbon containing feed-stock by means of primary and secondary reforming, intermediary methanol and ammonia formation and conversion of the ammonia to urea product and catalytic oxidation of methanol to formaldehyde. | 2022-02-17 |
20220048854 | PROCESS FOR THE PRODUCTION OF UREA FORMALDEHYDE CONCENTRATE - Parallel co-production process for the production of methanol and urea product from a hydrocarbon containing feed-stock by means of autothermal reforming, intermediary methanol and ammonia formation and conversion of the ammonia to urea product and catalytic oxidation of the methanol to formaldehyde. | 2022-02-17 |
20220048855 | METHOD FOR PRODUCING METHIONINE - The present invention pertains to a method for producing methionine or salts or derivatives thereof from hydrogen cyanide (HCN), the method comprising a step of producing 2-hydroxy-4-(methylthio)butyronitrile (MMP-CN), or a crude product mixture comprising MMP-CN, by contacting a hydrogen cyanide (HCN) process gas mixture prepared according to the Andrussow process from methane, ammonia and oxygen, with 3-methylmercaptopropionaldehyde (MMP), wherein the HCN process gas mixture is obtained from the crude HCN process gas mixture by adjusting the amount of ammonia to between 20% (v/v) and 60% (v/v) of the amount of the ammonia in the crude HCN process gas mixture. | 2022-02-17 |
20220048856 | METHOD FOR PREPARING BRIVARACETAM AND INTERMEDIATE THEREOF - The present application relates to a method (I) for preparing a brivaracetam intermediate, comprising the steps of dissolving the compound represented by B-P and 1S,2S-diphenylethylenediamine in a solvent for resolution, crystallizing, filtering, and recrystallizing to obtain the compound represented by B-Q, which is then converted to the brivaracetam intermediate represented by B-R. This method can effectively resolve the compound represented by B-P. The present application also provides a method for preparing brivaracetam using the compound represented by B-R. The method can separate the effective components only through simple steps such as extraction, washing, drying, and concentration without requiring use of chiral chromatography column to separate isomers in the preparation process, and thus the separation process is simple, greatly reducing the production cost of brivaracetam. | 2022-02-17 |
20220048857 | PLANT GROWTH INHIBITING AGENT, AND PLANT GROWTH INHIBITING METHOD USING SAME - An object of the present invention is to provide a novel plant growth inhibiting agent and a plant growth inhibiting method using the same. The plant growth inhibiting agent of the present invention comprises, as an active ingredient, a compound represented by the following formula (I′) and/or a salt thereof. In the formula (I′), R | 2022-02-17 |
20220048858 | Aza (Indole)-, Benzothiophene-, And Benzofuran-3-Sulfonamides - Disclosed are sulfonamide compounds with GPR17 modulating properties, which are useful for treating or preventing a variety of CNS and other diseases, in particular for preventing and treating myelinating diseases or disorders. | 2022-02-17 |
20220048859 | SYNTHETIC PROCESS - The invention generally relates to a process for preparing compounds, including Compound of Formula (I), useful as key intermediates in the preparation of compounds having RORγt antagonist properties. | 2022-02-17 |
20220048860 | TRICYCLIC OCTACATIONIC CYCLOPHANE AND ITS USE IN COMPLEXATION WITH PERLENE DIIMIDE DYES - Disclosed herein is a tricyclic octacationic cyclophane and complexes comprising the tricyclic octacationic cyclophane and a perylene diimide dye complexed therein and methods of using and making the cyclophane and complexes. | 2022-02-17 |
20220048861 | QUINOLINE-BASED PROTEASOME INHIBITORS AND USES THEREOF - Described herein are quinoline compounds useful for, among other things, inhibition of the proteasome and for treatment of cancer and inflammation. | 2022-02-17 |
20220048862 | High-Purity Quinoline Derivative and Method for Manufacturing Same - Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less. | 2022-02-17 |
20220048863 | DNA2 INHIBITORS FOR CANCER TREATMENT - Disclosed herein, inter alia, are compositions and methods for inhibiting DNA2. | 2022-02-17 |
20220048864 | METHOD FOR PRODUCING AMIDATE COMPOUND, AND AMIDATE COMPOUND - A method for producing an amidate compound represented by Formula (4), comprising reacting an iminium salt represented by Formula (1) and an organic compound represented by Formula (3), wherein Formulas (1), (3), and (4) are as defined in the description. | 2022-02-17 |
20220048865 | Novel Phenyl Derivatives - The present application provides a novel phenyl derivative, 5-[(2,4-dinitrophenoxy)methyl]-1-methyl-2-nitro-1H-imidazole or a pharmaceutically acceptable salt thereof, which is useful for regulating mitochondria activity, reducing adiposity, treating diseases including diabetes and diabetes-associated complications. | 2022-02-17 |
20220048866 | NOVEL INHIBITORS OF GUANOSINE MONOPHOSPHATE SYNTHETASE AS THERAPEUTIC AGENTS - The invention provides a series of GMPS enzyme inhibitors. The invention includes potent GMPS inhibitors that specifically and covalently bind to GMPS, exhibit broad anti-cancer activity, block the infection efficiency of viruses, and have the potentials to suppress undesired immune responses. These novel inhibitors of GMPS, and their derivatives, have tremendous potentials to be used as therapeutic agents for the treatment of cancers, viral infection and immune disorders. | 2022-02-17 |
20220048867 | STEREOCHEMICALLY ENRICHED COMPOSITIONS FOR DELIVERY OF NUCLEIC ACIDS - Provided, in part, is a composition comprising one or more chemical entities of formula I, each of which is a compound of formula I: | 2022-02-17 |
20220048868 | Microcrystalline Diketopiperazine Compositions and Methods - Disclosed herein are DKP microcrystals made by an improved method where they do not irreversibly self-assemble into microparticles. The microcrystals can be dispersed by atomization and re-formed by spray drying into particles having spherical shell morphology. Active agents and excipients can be incorporated into the particles by spray drying a solution containing the components to be incorporated into microcrystalline diketopiperazine particles. In particular, the microcrystalline particle compositions are suitable for pulmonary drug delivery of one or more peptides, proteins, nucleic acids and/or small organic molecules. | 2022-02-17 |
20220048869 | PHENAZINE-BASED COMPOUND, ELECTROLYTIC LIQUID COMPRISING SAME FOR REDOX FLOW BATTERY, AND REDOX FLOW BATTERY - The present invention relates to: a phenazine-based compound having a particular substituent; an electrolytic liquid comprising same for a redox flow battery; and a redox flow battery. The phenazine-based compound is a multi-redox organic substance capable of inducing a two-stage reversible redox reaction and shows high solubility in a non-aqueous solvent. Thus, the employment of the phenazine-based compound can provide an electrolytic liquid for a redox flow battery, capable of expressing high energy density, and a redox flow battery. | 2022-02-17 |
20220048870 | NOVEL HIGH-PERFORMING METAL-FREE PRIMARY EXPLOSIVE - The present disclosure relates to a novel compound suitable for a metal-free primary explosive, and the method of making and using the novel compound. The novel compound can undergo a deflagration to detonation transition (DDT) to initiate detonation of a larger body of secondary explosive. The compound has a structure of Formula I: | 2022-02-17 |
20220048871 | Crystalline form of 4-amino-N-tert-butyl-4,5-dihydro-3-isopropyl-5-oxo-1,2,4-1H-triazole-1-ca- rboxamide and a process for producing thereof - The invention provides a novel crystalline form of 4-amino-N-tert-butyl-4,5-dihydro-3-isopropyl-5-oxo-1,2,4-1H-triazole-1-carboxamide and a process for preparation of said crystalline form. The invention also relates to formulations and method for controlling weeds using said formulations. | 2022-02-17 |
20220048872 | PSMA TARGETED FLUORESCENT AGENTS FOR IMAGE GUIDED SURGERY - Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed. | 2022-02-17 |
20220048873 | PESTICIDALLY ACTIVE CYCLOPROPYL METHYL AMIDE DERIVATIVES - The present invention relates to compounds of formula (I) wherein the substituents are as defined in claim | 2022-02-17 |
20220048874 | Method for Producing (5S)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-2-me- thyl-Benzoic Acid - The present invention relates to a novel method for preparing (5S)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-2-methyl-benzoic acid, which can preferably be used in the synthesis of (5S)-4-[5-(3,5-dichlorophenyl)-5-(trifluoromethyl)-4H-isoxazol-3-yl]-N-[2-oxo-2-(2,2,2-trifluoroethylamino)ethyl]-2-methyl-benzamide. | 2022-02-17 |
20220048875 | CRYSTALLINE FORMS OF 3-SUBSTITUTED 1,2,4- OXADIAZOLE - The invention relates to crystalline forms of a 3-substituted 1,2,4-oxadiazole compound, methods of their preparation, and related pharmaceutical preparations thereof. The invention also relates to preparations suitable for pharmaceutical, veterinary, and agriculturally-relevant uses. | 2022-02-17 |
20220048876 | INSECTICIDAL COMPOUNDS - Compounds of formula (I), wherein the substituents are as defined in claim | 2022-02-17 |
20220048877 | PROCESS FOR THE PRODUCTION OF FURFURAL - The present invention refers to a method of producing furfural and optionally further basic chemicals from biomass material comprising treatment of the biomass material at elevated pressures and temperatures, to the condensates and solid product obtained by the method of the invention, as well as to their use. | 2022-02-17 |
20220048878 | IMPROVEMENT IN OR RELATING TO ORGANIC COMPOUNDS - The present invention is concerned with fragrance ingredients and with fragrance preparations, for imparting desirable odor notes to consumer products, in particular it is concerned with (2S,4R)-4-methyl-2-((Z)-2-methylbut-1-en-1-yl)tetrahydro-2H-pyran that can be used as replacements for 4-methyl-2-(2-methylprop-1-en-1-yl)tetrahydro-2H-pyran. | 2022-02-17 |
20220048879 | Synthesis of small molecules inspired by Phomoxanthone A - Methods, compositions, and kits are provided for synthesizing bioactive chromane, the method including: constructing a tertiary ether stereocenter enantioselectively by catalyzed alkynylation of a substituted chromenone to obtain a chromanone; reducing alkyne and ketone in the chromanone to obtain a chroman; and converting ester to methyl group thereby obtaining chromane. | 2022-02-17 |
20220048880 | METHODS FOR ENRICHING ALPHA-TOCOTRIENOL FROM MIXED TOCOL COMPOSITIONS - Provided herein are methods for making an alpha-tocotrienol enriched tocol mixture, such as from a plant or plant-derived material. Also provided herein are simulated moving bed purification methods for tocotrienol compounds such as alpha tocotrienol. | 2022-02-17 |
20220048881 | TRICYCLIC SPIRO COMPOUND - A medicinal agent for the prevention and/or treatment of diseases caused by EP | 2022-02-17 |
20220048882 | FLUORINE-CONTAINING ETHER COMPOUND, LUBRICANT FOR MAGNETIC RECORDING MEDIUM, AND MAGNETIC RECORDING MEDIUM - The fluorine-containing ether compound is represented by the following formula (1): R | 2022-02-17 |
20220048883 | NOVEL FGFR INHIBITORS AND USES THEREOF - The invention provides novel FGFR inhibitors based on the pyridinylpyrimidine. The invention includes inhibitors with broad inhibitory activity against all FGFR isoforms, and inhibitors with selective inhibition against FGFR4. These novel pyridinylpyrimidine-based FGFR inhibitors, or their derivatives, have strong potential to be used to treat cancer. | 2022-02-17 |
20220048884 | NRF2 ACTIVATOR - Provided are compounds of Formula A or I, or pharmaceutically acceptable salts thereof, and methods for their use and production. | 2022-02-17 |
20220048885 | HETEROAROMATIC COMPOUNDS AS VANIN INHIBITORS - The present invention encompasses compounds of the formula I | 2022-02-17 |
20220048886 | ORGANIC ELECTROLUMINESCENT COMPOUND, A PLURALITY OF HOST MATERIALS, AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME - The present disclosure relates to an organic electroluminescent compound, a plurality of host materials, and an organic electroluminescent device comprising the same. By comprising the organic electroluminescent compound according to the present disclosure as a single host material, or a specific combination of compounds according to the present disclosure as a plurality of host materials, it is possible to produce an organic electroluminescent device having an improved luminous efficiency. | 2022-02-17 |
20220048887 | IMPURITIES OF AMIDE-LIKE DERIVATIVES AND USE THEREOF - An impurity A, an impurity B and an impurity G and preparation methods therefor, and an application as a reference standard for quality control of a compound as represented by formula VI are described. | 2022-02-17 |
20220048888 | PYRIMIDINYL-HETEROARYLOXY-NAPHTHYL COMPOUNDS AND METHODS OF USE - Described herein are phenoxy-pyridazinyl-pyrimidine or phenoxy-pyrimidinyl-pyrimidine compounds and pharmaceutically acceptable salts thereof for use in the treatment of Ire1-mediated diseases and cancer. | 2022-02-17 |
20220048889 | HETEROAROMATIC COMPOUNDS AS VANIN INHIBITORS - The present invention encompasses compounds of the formula I | 2022-02-17 |
20220048890 | METHODS AND COMPOSITIONS FOR MODULATING SPLICING - Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, pharmaceutical compositions comprising the same, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions. | 2022-02-17 |
20220048891 | AMINOPYRIMIDINE COMPOUND USED FOR INHIBITING ACTIVITY OF PROTEIN KINASE - The present invention relates to an aminopyrimidine compound having an inhibitory effect on the activity of protein kinase as well as the preparation and use thereof. Specifically, disclosed by the present invention is an aminopyrimidine compound represented by formula (I), or a pharmaceutically acceptable salt, stereoisomer, solvate or hydrate thereof, as well as a pharmaceutical composition comprising said compound and a use method therefor. The method comprises a method for treating cell proliferative diseases and conditions such as cancer and immune diseases. | 2022-02-17 |
20220048892 | HETEROCYCLIC DERIVATIVES AS NAV1.7 AND NAV1.8 BLOCKERS - The present invention relates to heterocyclic derivatives which have blocking activities of voltage gated sodium channels as the Nav1.7 and Nav1.8 channels, and which are useful in the treatment or prevention of disorders and diseases in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which voltage gated sodium channels are involved. | 2022-02-17 |
20220048893 | Compounds for Treating Neurodegenerative Diseases and Cancers - The present invention relates to novel substituted aromatic-aliphatic amines capable of penetrating blood brain barrier and mediating pathogenic process in neurodegenerative diseases. | 2022-02-17 |
20220048894 | ENZYME INHIBITORS - The present invention provides compounds of formula (I): | 2022-02-17 |
20220048895 | SUBSTITUTED BENZAZEPINE COMPOUNDS, CONJUGATES, AND USES THEREOF - Benzazepine compounds and salts thereof, conjugates and pharmaceutical compositions for use in the treatment of disease, such as cancer, are disclosed herein. The disclosed benzazepine compounds and salts thereof are useful, among other things, in treating of cancer and activating an immune response. Additionally, benzazepine compounds or salts thereof attached to an antibody construct to form an antibody conjugate are described herein. | 2022-02-17 |
20220048896 | PYRAZOLE COMPOUNDS SUBSTITUTED WITH HETEROARYL AND PHARMACEUTICAL USE THEREOF - Pyrazole compounds substituted with heteroaryl or pharmaceutically acceptable salts thereof that have an SGLT1 inhibitory activity and are useful for a drug, pharmaceutical compositions comprising the same, and pharmaceutical use thereof are disclosed. Specifically, a compound of Formula [X]: | 2022-02-17 |
20220048897 | INHIBITORS OF INFLUENZA VIRUS REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient a safe and effective amount of a compound represented by Formula I, or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a safe and effective amount of such a compound or pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier, adjuvant or vehicle. | 2022-02-17 |
20220048898 | QUINOLINES THAT MODULATE SERCA AND THEIR USE FOR TREATING DISEASE - Provided herein are compounds of Formula I, pharmaceutical compositions thereof, and methods of their use for treating, preventing, or ameliorating one or more symptoms of a neurological disease, neurodegenerative disorder, or diabetes. | 2022-02-17 |
20220048899 | HETEROCYCLIC COMPOUND, ORGANIC LIGHT-EMITTING DEVICE COMPRISING SAME, METHOD FOR MANUFACTURING SAME, AND COMPOSITION FOR ORGANIC MATERIAL LAYER - The present specification relates to a heterocyclic compound represented by Chemical Formula 1, an organic light emitting device comprising the same, a method for manufacturing the same, and a composition for an organic material layer. | 2022-02-17 |
20220048900 | AMORPHOUS SPARSENTAN COMPOSITIONS - An amorphous form of a compound having structure (I), or a pharmaceutically acceptable salt thereof, is provided. Such compounds may be used for the treatment of kidney diseases or disorders. | 2022-02-17 |
20220048901 | COMPOSITIONS AND METHODS FOR MODULATING INFLAMMATORY AND DEGENERATIVE DISORDER - The disclosure provides compounds and method useful for modulating gp130 biological activity. The disclosure also provides methods and compositions for treating disease and disorders associated with gp130 activity, particularly those associated with inflammation. | 2022-02-17 |
20220048902 | METHODS AND COMPOSITIONS FOR MODULATING SPLICING - Described herein are small molecule splicing modulator compounds that modulate splicing of mRNA, such as pre-mRNA, encoded by genes, pharmaceutical compositions comprising the same, and methods of use of the small molecule splicing modulator compounds for modulating splicing and treating diseases and conditions. | 2022-02-17 |
20220048903 | Anthelminthic Heterocyclic Compounds - A compound of formula (I), (IA) or formula (II) or a composition comprising the compound of formula (I), (IA) or formula (II) in association with a veterinarily acceptable carrier are described. A method of controlling helminths using same is described. | 2022-02-17 |
20220048904 | Improved Method for the Manufacture of 3-[(1S)-1-imidazo[1,2-a]pyridin-6-ylethyl]-5-(1-methylpyrazol-4-yl)triazo- lo[4,5-b]pyrazine and polymorphic forms thereof - This specification generally relates to an improved method for the manufacture of 3-[(1S)-1-imidazo[1,2-a]pyridin-6-ylethyl]-5-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyrazine (I), or pharmaceutically acceptable salts thereof, polymorphic forms thereof, and intermediates useful in the manufacture of such compounds and salts thereof. | 2022-02-17 |
20220048905 | METHOD OF MANUFACTURING A SOLID FORM OF A BET BROMODOMAIN INHIBITOR - The invention relates to solid crystalline forms of Compound (I), such as e.g., Form VII, including pharmaceutical compositions thereof and processes for preparing crystalline Compound (I), Form VII. Compound (I) modulates or inhibits the activity of BET bromodomain-containing proteins, and is useful in the treatment of diseases such as cancer, inflammatory and cardiovascular diseases. | 2022-02-17 |
20220048906 | COMPOUNDS AND USES THEREOF - The present invention relates to methods and compositions for the treatment of BAF-related disorders such as cancers and viral infections. | 2022-02-17 |
20220048907 | METHYL {4,6-DIAMINO-2-[5-FLUORO-1-(2-FLUOROBENZYL)-1H-PYRAZOLO[3,4-B]PYRID- IN-3-YL]PYRIMIDIN-5-YL}CARBAMATE ACTIVE COMPOUND PRODUCT HAVING IMPROVED PROPERTIES, PRODUCTION AND FORMULATION THEREOF - The present invention relates to methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1H-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate in the form of a novel active compound product having improved properties, for example in respect of the isolability of the active compound product, the dischargeability of the active compound product after isolation and drying and also conveyability, sieveability and micronizability of the active compound product, and to processes for the production and formulation thereof. | 2022-02-17 |
20220048908 | COMPOSITIONS AND METHODS FOR MODULATING HAIR GROWTH - The present disclosure relates to compounds that are capable of inhibiting the mitochondrial pyruvate carrier and promoting hair growth. The disclosure further relates to methods of promoting hair growth or treating conditions or disorders affecting hair growth, such as baldness or alopecia. | 2022-02-17 |
20220048909 | HETEROARYL SUBSTITUTED SPIROPIPERIDINYL DERIVATIVES AND PHARMACEUTICAL USES THEREOF - The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof; | 2022-02-17 |
20220048910 | ORGANIC COMPOUNDS - Please add the following heading and paragraph on a separate sheet, after the claims: The invention relates to particular substituted heterocycle fused gamma-carbolines, in free, solid, pharmaceutically acceptable salt and/or substantially pure form as described herein, pharmaceutical compositions thereof, and methods of use in the treatment of diseases involving the 5-HT | 2022-02-17 |
20220048911 | CO-CRYSTALS, METHOD AND APPARATUS FOR FORMING THE SAME - Disclosed herein is a method and apparatus for synthesizing co-crystals from the vapor phase without the need for liquid solvent. Also disclosed herein are co-crystals formed from the vapor phase, substrates coated with said co-crystals, pharmaceutical compositions thereof and apparatuses for producing said co-crystals. | 2022-02-17 |
20220048912 | CYCLOBUTYL NUCLEOSIDE ANALOGS AS ANTI-VIRALS - Described herein are cyclobutyl nucleoside analogs of Formula (I), pharmaceutical compositions that include one or more cyclobutyl nucleoside analogs and methods of using the same to treat HBV, HDV and/or HIV. | 2022-02-17 |
20220048913 | ANTAGONISTS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M4 - Disclosed herein are cyclopropylpiperidine compounds, which may be useful as antagonists of the muscarinic acetylcholine receptor M4 (niAChR M4). Also disclosed herein are methods of making the compounds, pharmaceutical compositions comprising the compounds, and methods of treating disorders using the compounds and compositions. | 2022-02-17 |
20220048914 | PREPARATION FOR 6-AMINO-1H-PYRAZOLO[3,4-D]PYRIMIDINE-BASED JAK KINASE INHIBITOR AND APPLICATION THEREOF - A medicament with excellent JAK kinase (Janus Kinase) inhibitory activity can be used to prevent, treat and/or improve an autoimmune disease (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus and the like). The present invention also provides a pharmaceutically acceptable composition containing the compound and a method for preparing these compounds. | 2022-02-17 |
20220048915 | Nitrogen-containing Heterocyclic Compound and Composition Thereof, Preparation Method Therefor, and Application Thereof - Disclosed by the present invention are a nitrogen-containing heterocyclic compound, and a composition thereof, a preparation method therefor and an application thereof. The structure of the nitrogen-containing heterocyclic compound according to the present invention is shown in Formula I. The nitrogen-containing heterocyclic compound according to the present invention or a pharmaceutically acceptable salt thereof has better inhibitory activity on p38 protein kinase and/or higher bioavailability. In addition, the preparation method is simple. | 2022-02-17 |
20220048916 | 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. | 2022-02-17 |
20220048917 | HIGHLY EFFICIENT PROCESS FOR THE PREPARATION OF SITAGLIPTIN VIA RHODIUM CATALYZED ASYMMETRIC HYDROGENATION - The present invention provides highly efficient process for the preparation of enantiomerically enriched Sitagliptin of Formula (Ia). More particularly, a direct rhodium catalyzed asymmetric hydrogenation in the presence of bis-phosphine chiral ligand has been developed to yield enantiopure Sitagliptin product with the highest enantiomeric excess of 85-99.9%. | 2022-02-17 |
20220048918 | PKC INHIBITOR SOLID STATE FORMS - The present disclosure relates to various solid state forms of 5-{[(2S,5R)-2,5-dimethyl-4-(tetrahydro-2H-pyran-4-ylmethyl)piperazin-1-yl]carbonyl}-N-(5-fluoro-2-methylpyrimidin-4-yl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-amine and methods of making the same. Such forms of 5-{[(2S,5R)-2,5-dimethyl-4-(tetrahydro-2H-pyran-4-ylmethyl)piperazin-1-yl]carbonyl}-N-(5-fluoro-2-methylpyrimidin-4-yl)-6,6-dimethyl-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazol-3-amine are useful in preparation of pharmaceutical compositions and dosage forms for the treatment of cancer, immune disorders and inflammation. | 2022-02-17 |
20220048919 | HETEROARYLDIHYDROPYRIMIDINE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS - Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject. | 2022-02-17 |
20220048920 | PROCESS FOR THE CYCLOADDITION OF A (HETERO)ARYL 1,3-DIPOLE COMPOUND WITH A (HETERO)CYCLOALKYNE - A process is provided, comprising reacting a (hetero)aryl 1,3-dipole compound with a (hetero)cycloalkyne, wherein the (hetero)aryl 1,3-dipole compound comprises a 1,3-dipole functional group bonded to a (hetero)aryl group, and wherein the (hetero)aryl 1,3-dipole compound is a (hetero)aryl azide or a (hetero)aryl diazo compound; wherein:
| 2022-02-17 |
20220048921 | PYRAN FUSED RING COMPOUND, PREPARATION METHOD THEREFOR AND USE THEREOF - The present invention relates to pyran-fused ring compounds, preparation methods thereof and use thereof, especially to pyran-fused ring compounds usable for preparing Halichondrin, Eribulin, or analogues thereof, preparation methods thereof and use thereof. Use of any of the compounds of formula (I) to (XIII) of the present invention in preparation of Halichondrin B, Eribulin, analogues thereof or C1-C13 moieties thereof. Provided in the present invention are intermediates usable for preparing Halichondrin B, Eribulin, or analogues thereof, especially the key product of C1-C13 moieties, preparation methods thereof and use thereof. The starting material for the synthesis pathway of the present invention is inexpensive and readily available with sustainable source and reliable quality. Since the structural characteristics of the reactants of theirself are made full use in choosing the method of constructing the chiral centers, the efficiency in the synthesis is considerably increased, the difficulty in and the risk on quality control of the product are reduced; and using a highly toxic and expensive high-valent osmium catalyst is avoided, which have the cost and environmental friendliness significantly improved. | 2022-02-17 |
20220048922 | COMPOUNDS TARGETING PRMT5 - Provided herein are compounds of Formula (I), or pharmaceutically acceptable salts thereof, pharmaceutical compositions that include a compound described herein (including pharmaceutically acceptable salts of a compound described herein) and methods of synthesizing the same. Also provided herein are methods of treating diseases and/or conditions with a compound of Formula (I), or a pharmaceutically acceptable salt thereof. | 2022-02-17 |
20220048923 | LUMINOGENS FOR BIOLOGICAL APPLICATIONS - A compound comprises a donor and an acceptor, wherein at least one donor (“D”) and at least one acceptor (“A”) may be arranged in an order of D-A; D-A-D; A-D-A; D-D-A-D-D; A-A-D-A-A; D-A-D-A-D; and A-D-A-D-A. The compound may be selected from the group consisting of: MTPE-TP, MTPE-TT, TPE-TP A-TT, PTZ-BT-TP A, NPB-TQ, TPE-TQ-A, MTPE-BTSe, DCDPP-2TP A, DCDPP-2TPA4M, DCDP-2TPA, DCDP-2TPA4M, TTS, ROpen-DTE-TPECM, and RClosed-DTE-TPECM. The compound may be used as a probe and may be functionalized with special targeted groups to image biological species. As non-limiting examples, the compound may be used in cellular cytoplasms or tissue imaging, blood vessel imaging, in vivo fluorescence imaging, brain vascular imaging, sentinel lymph node mapping, and tumor imaging, and the compound may be used as a photoacoustic agent. | 2022-02-17 |
20220048924 | SOMATOSTATIN MODULATORS AND USES THEREOF - Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity. | 2022-02-17 |
20220048925 | Substituted 3,4,12,12a-Tetrahydro-1H-[1,4]Oxazino[3,4-c]Pyrido[2,1-f][1,2,4]Triazine-- 6,8-dione, Pharmaceutical Composition, Method for the Production and Use Thereof - Influenza is an acute infectious respiratory disease caused by the influenza virus. It is part of the group of Acute Respiratory Viral Infections (ARVI). It occasionally spreads in the form of epidemics and pandemics. Currently, more than 2000 variants of the influenza virus differing in the antigen spectrum have been identified. Given that influenza is a serious threat to public health (worldwide, these annual epidemics lead to 3-5 million cases of severe illness, millions of hospitalizations, and up to 650,000 deaths), it seems appropriate to search for new anti-influenza drugs with improved characteristics. | 2022-02-17 |
20220048926 | POLYMORPHIC MIXTURE OF RIFAXIMIN AND ITS USE FOR THE PREPARATION OF SOLID FORMULATIONS - A Rifaximin polymorphic mixture of α/β form in a relative ratio of 85/15±3 and a process for its preparation. The polymorphic mixture of Rifaximin is for use as a medicament, in particular in the treatment of traveler's diarrhea and hepatic encephalopathy. A pharmaceutical composition comprises the polymorphic mixture of Rifaximin as active ingredient, in particular, a solid formulation, more in particular, a film coated tablet. A polymorphic form of crude wet rifaximin and of purified wet rifaximin their use are used as intermediates in a process for the preparation of Rifaximin polymorphic mixture of α/β form in a relative ratio of 85/15±3. | 2022-02-17 |
20220048927 | COMPOUNDS FOR THE MODULATION OF MYC ACTIVITY - The present invention provides novel compounds of Formulas (I) and (II) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases, e.g., cancers (e.g., breast cancer, prostate cancer, lymphoma, lung cancer, pancreatic cancer, ovarian cancer, neuroblastoma, or colorectal cancer), benign neoplasms, angio genesis, inflammatory diseases, fibrosis (e.g., polycystic kidney disease), autoinflammatory diseases, and autoimmune diseases in a subject. | 2022-02-17 |
20220048928 | MUSCARINIC RECEPTOR AGONISTS - This invention relates to compounds that are agonists of the muscarinic M | 2022-02-17 |
20220048929 | Methods of Synthesizing and Recycling Metal-Organic Framework Systems - Provided herein are methods of novel methods of synthesizing a metal-organic framework system by vapor-phase appending of a plurality of ligands appended to a metal-organic framework. Also, provided are methods of recycling metal-organic framework systems by detaching the ligand and re-appending the same ligand or appending a different ligand to the metal-organic framework to provide a recycled or repurposed metal-organic framework system. | 2022-02-17 |
20220048930 | INHIBITORS OF COMPLEMENT FACTORS AND USES THEREOF - Disclosed are compounds of formula I and II and pharmaceutically acceptable salts thereof. Also disclosed are methods of treating a neurodegenerative disorder, an inflammatory disease, an autoimmune disease, an ophthalmic disease or a metabolic disorder using the compounds disclosed herein. | 2022-02-17 |
20220048931 | ANTICANCER INDENES, INDANES, AZAINDENES, AZAINDANES, PHARMACEUTICAL COMPOSITIONS AND USES - Disclosed are compounds for medical uses, for example, compounds of formula Ia, | 2022-02-17 |
20220048932 | PROCESS FOR CONTINUOUS PURIFICATION OF HIGH-PURITY TRIMETHYLALUMINUM - A process for continuous purification of high-purity trimethylaluminum is provided. The process includes preparing a membrane separator, which is placed vertically for use, and arranging a condenser tube inside of the membrane separator and a heating tube outside of the membrane separator, and a disperser at the top of the membrane separator for dispersing a liquid. The liquid naturally flows down along the inner wall of the heating tube by gravity to form a membrane. The process further includes concentrating liquid components having a low boiling point which are collected by the condenser at different stages and concentrating liquid components having a high boiling point which are collected by the heating wall. | 2022-02-17 |
20220048933 | METHOD FOR THE SYNTHESIS OF ASYMMETRIC POLYSULFIDES - The present invention is directed to a method of making an asymmetric polysulfide, comprising the step of simultaneously reacting an olefinically unsaturated compound, elemental sulfur, and a thiol in the presence of a catalytic amount of a base to produce the asymmetric polysulfide. | 2022-02-17 |
20220048934 | Organic Solvent Processable Carbon Phosphonitride Pre-Polymers - Described herein is the preparation of carbon phosphonitride pre-polymers that are soluble in organic solvents and can be further thermoset into carbon phosphonitride extended solids (i.e. films, monoliths, etc.) with an approximate empirical formula of C | 2022-02-17 |
20220048935 | Radioactive Phospholipid Metal Chelates for Cancer Imaging and Therapy - Alkylphosphocholine analogs incorporating a chelating moiety that chelates a radioactive metal isotope are disclosed herein. The alkylphophocholine analogs, which can be used to treat or detect solid tumors, have the formula: | 2022-02-17 |
20220048936 | NOVEL STING AGONISTS - The present invention provides compounds of Formula I′: | 2022-02-17 |
20220048937 | COMPOSITION AND ORGANIC LIGHT-EMITTING DEVICE - A composition comprising a semiconducting host compound having a glass transition temperature (Tg) of less than 100° C., and a phosphorescent compound wherein the phosphorescent compound is a metal complex of formula (II): M is Ir (III) or Pt (II). p is at least 1. q is 0, 1 or 2. L is a bidentate ligand substituted with one or two groups X wherein each X independently comprises an aromatic or heteroaromatic group Ar | 2022-02-17 |
20220048938 | Processes and Materials for the Synthesis of Sugar Esters Found in Natural Tobacco - A process and materials method for making a glucose tetraester may include reacting glucose with a carboxylic acid to create a glucose pentaester. The glucose pentaester was reacted with a basic reagent to create a glucose tetraester. Glucose was reacted with a carboxylic acid anhydride in the presence of 4-dimethylaminopyridine to create a glucose pentaester product. The glucose pentaester reaction product was separated. The glucose pentaester reaction product was reacted with a basic reagent, wherein the reaction steps may take place at a temperature of about 0° C. to about 60° C. and about ambient pressure, wherein the ratio of the carboxylic acid to the glucose was from about 5:1 to about 50:1, and wherein the ratio of the glucose pentaester to the basic reagent was from about 1:50 to about 1:150. | 2022-02-17 |
20220048939 | AROMATIC RING COMPOUND - A novel aromatic ring compound is represented by general formula (I). This compound, isomer, prodrug, solvate, pharmaceutically acceptable salt and pharmaceutical composition thereof are useful in preparing medicaments for treating depression and related symptoms. | 2022-02-17 |
20220048940 | DISULFIDE-LINKED REVERSIBLE TERMINATORS - The present disclosure provides methods of sequencing polynucleotides and compounds, compositions useful for sequencing of polynucleotides. The chemical compounds include nucleotides and their analogs which possess a sugar moiety comprising a cleavable chemical group capping the 3′-OH group and a base that is attached to a detectable label through a cleavable linker comprising a disulfide bond. In addition, the disulfide bond(s) can be cleavable by a reducing reagent. In addition, after the disulfide bond(s) is/are cleaved by the reducing reagent, there is no free thiol group linked to the nucleotides. Examples of chemical compounds according to the present disclosure are shown as Formulae (IV) and (V). | 2022-02-17 |
20220048941 | MODIFIED NUCLEOSIDE PHOSPHORAMIDITES - A method of making a compound represented by Formula (I): | 2022-02-17 |
20220048942 | DOT1L DEGRADERS AND USES THEREOF - Provided herein are bifunctional compounds with a moiety or domain that is a binder of the ubiquitin receptor RPN13 and another moiety or domain that is a binder of a target protein DOT1L to induce degradation of DOT1L. Also provided are pharmaceutical compositions comprising the bifunctional compounds, and methods of treating and/or preventing diseases (e.g., proliferative diseases, such as cancers). Provided also are methods of inducing the degradation of DOT1L by administering a bifunctional compound or composition described herein, wherein one domain of the bifunctional compound is a binder of the ubiquitin receptor RPN13 and another domain of the compound is a binder of the target protein DOT1L in a subject. | 2022-02-17 |
20220048943 | OXYSTEROLS AND METHODS OF USE THEREOF - Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein R | 2022-02-17 |
20220048944 | FUNCTIONALIZED PEPTIDES AS ANTIVIRAL AGENTS - The present invention discloses compounds of Formula (I), and pharmaceutically acceptable salts, thereof: | 2022-02-17 |
20220048945 | PEPTIDE INHIBITING ACTIVITY OF ARYL HYDROCARBON RECEPTOR AND COSMETIC COMPOSITION USING SAME - Disclosed is a peptide and a cosmetic composition using the same. The peptide inhibits the activity of an aryl hydrocarbon receptor (AhR), whereby the peptide may be used to alleviate skin troubles caused by fine dust. | 2022-02-17 |
20220048946 | CYCLIC TETRAPEPTIDE STEREOISOMERS - Cyclic tetrapeptide stereochemical isomers of CJ-15,208, pharmaceutical compositions from such cyclic tetrapeptides, and methods of using such pharmaceutical compositions. The cyclic tetrapeptide compounds and pharmaceutical compositions disclosed herein are potent analgesics active in several pain models with generally minimal tolerance and reduced likelihood to induce addiction relative to other known opiates. | 2022-02-17 |
20220048947 | EPITOPE TAGS RECOGNIZED BY SPECIFIC BINDERS - The present invention provides peptides useful as epitope tags, which may be fused to a polypeptide of interest, as well as antibodies that specifically bind to these peptides. The peptides and/or antibodies can be used for detecting, immobilizing, isolating or purifying a molecule that is conjugated to such a peptide and/or antibody. | 2022-02-17 |