51st week of 2021 patent applcation highlights part 25 |
Patent application number | Title | Published |
20210395211 | Production of Hydroxyethylpiperazine - Embodiments relate to a continuous process for the production of hydroxyethylpiperazine that includes feeding neat piperazine, recycled piperazine, and ethylene oxide to a reactor to form crude hydroxyethylpiperazine, in which the reactor is a continuous stirred tank reactor or a plug flow reactor. The process further includes continuously feeding the crude hydroxyethylpiperazine from the reactor to a distillation system that includes at least one distillation column, the distillation system produces at least a recycled piperazine stream and a hydroxyethylpiperazine stream, the recycled piperazine stream includes the recycled piperazine that is fed to the reactor to form the crude hydroxyethylpiperazine, and the hydroxyethylpiperazine stream includes at least 60 wt % of hydroxyethylpiperazine based on a total weight of the hydroxyethylpiperazine stream. | 2021-12-23 |
20210395212 | DECALIN DERIVATIVES, A PROCESS FOR THE PREPARATION AND PHARMACEUTICAL COMPOSITION THEREOF - Decalin derivative compounds of formula (I) are provided, including processes for preparation thereof, and pharmaceutical compositions including the decalin derivative compounds. Methods are provided for treating blood related disorders, such as sickle cell anemia, in a subject in need thereof using a compound of formula (I). | 2021-12-23 |
20210395213 | HYDROFLUOROETHERS AND METHODS OF USING SAME - A compound is represented by the following general formula (I): (I) wherein each of Rf1 and Rf2 is, independently, F, CF3, C2F5, C3F7, or C4F9, with the proviso that if either of Rf1 and Rf2 is fluorine, then the other is not fluorine; Rf3 is F, CF3, C2F5, C3F7 or CF(CF3)2; Rf4 is F, CF3, C2F5, C3F7 or CF(CF3)2; and Rh is CH3 or C2H5. | 2021-12-23 |
20210395214 | USNIC ACID DERIVATIVE HAVING TSLP SECRETION INHIBITORY ABILITY AND USE THEREOF - The present invention relates to a novel Usnic acid derivative exhibiting an inhibitory effect on TSLP secretion or pharmaceutically acceptable salts thereof, and a use thereof. | 2021-12-23 |
20210395215 | ORGANIC ELECTROLUMINESCENT COMPOUND AND ORGANIC ELECTROLUMINESCENT DEVICE COMPRISING THE SAME - The present disclosure relates to an organic electroluminescent compound and an organic electroluminescent device comprising the same. The organic electroluminescent compound of the present disclosure may be comprised in a light-emitting layer, and is effective for producing an organic electroluminescent device having high luminescent efficiency and/or excellent lifespan characteristic. | 2021-12-23 |
20210395216 | THIOCYCLOHEPTYNE DERIVATIVES AND THEIR USE - The present invention pertains to novel thiocycloheptyne derivatives of general formula (I): and in particular to thiacycloalkynesulfoimine derivatives and their synthesis. The invention also relates to the use of the novel thiocycloheptyne derivatives in coupling reactions with linkers and drugs. The invention further relates to the use of the novel thiocycloheptynes in bioorthogonal (copper-free) click reactions. The invention further pertains to the use of the novel thiocycloheptyne derivatives in the generation of advanced multifunctional drug delivery systems (drug-loaded) nanoparticles. | 2021-12-23 |
20210395217 | PESTICIDALLY ACTIVE AZOLE-AMIDE COMPOUNDS - Compounds of formula (I) wherein the substituents are as defined in claim | 2021-12-23 |
20210395218 | 3-(1,2,3,6-TETRAHYDROPYRIDIN-2-YL) PYRIDINE GLUTARATE OR A PHARMACEUTICALLY ACCEPTABLE SOLVATE THEREOF - The present invention relates to 3-(1,2,3,6-tetrahydropyridin-2-yl)pyridine glutarate or a pharmaceutically acceptable solvate thereof, to a crystal thereof and to a polymorph of this crystal It further relates to the medicinal use of each of these, in particular in the treatment or prophylaxis of substance addiction or inflammation | 2021-12-23 |
20210395219 | NICOTINE SALTS, CO-CRYSTALS, AND SALT CO-CRYSTAL COMPLEXES - The invention provides certain nicotine salts, co-crystals, and salt co-crystals and provides novel polymorphic forms of certain nicotine salts. In particular, nicotine salts with mucic acid, 3,5-dihydroxybenzoic acid, and 2,3-dihydroxybenzoic acid, and crystalline polymorphic forms of nicotine 4-acetamidobenzoate, nicotine gentisate, and nicotine 1-hydroxy-2-naphthoate are described. The invention further provides methods of preparation and characterization of such nicotine salts, co-crystals, and salt co-crystals and polymorphic forms thereof. In addition, tobacco products, including smoking articles, smokeless tobacco products, and electronic smoking articles comprising nicotine salts, co-crystals, and/or salt co-crystals are also provided. | 2021-12-23 |
20210395220 | QUINONE REDUCTASE 2 INHIBITOR COMPOUNDS AND USES THEREOF - Provided herein according to some embodiments is a compound of Formula (I): [Formula], or a pharmaceutically acceptable salt or prodrug thereof. Compositions comprising the compound, and uses thereof for inhibiting the activity of quinone reductase-2, as well as in methods of treatment, are also provided. | 2021-12-23 |
20210395221 | THERAPEUTIC INHIBITORY COMPOUNDS - Provided herein are heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds that are useful for inhibiting plasma kallikrein. Furthermore, the subject compounds and compositions are useful for the treatment of diseases wherein the inhibition of plasma kallikrein inhibition has been implicated, such as angioedema and the like. | 2021-12-23 |
20210395222 | Fused Bicyclic Heterocycles as Therapeutic Agents - This disclosure relates to compounds, pharmaceutical compositions comprising them, and methods of using the compounds and compositions for treating diseases related to nicotinamide phosphoribosyltransferase (NAM FT) expression. More particularly, this disclosure relates to fused bicyclic heterocyclic compounds and pharmaceutical compositions thereof, methods of inhibiting NAM FT with these compounds, and methods of treating diseases related to NAMPT expression. | 2021-12-23 |
20210395223 | PRODRUGS OF CGRP ANTAGONISTS - Disclosed are prodrugs of CGRP antagonists, methods of treating CGRP related disorders, e.g., migraine, by administering to a patient in need thereof the prodrugs, pharmaceutical compositions comprising prodrugs and kits including the pharmaceutical compositions and instructions for use. | 2021-12-23 |
20210395224 | 3-(1H-PYRAZOL-4-YL)PYRIDINE ALLOSTERIC MODULATORS OF THE M4 MUSCARINIC ACETYLCHOLINE RECEPTOR - The present invention is directed to cinnolinyl and quinolinyl pyrazol-4-yl-pyridine compounds which are allosteric modulators of the M4 muscarinic acetylcholine receptor. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which M4 muscarinic acetylcholine receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved. | 2021-12-23 |
20210395225 | FUNCTIONALIZED AMINOTRIAZINES - The present invention relates to novel antagonists of the A2B adenosine receptor and pharmaceutical compositions comprising said antagonists as well as their uses for the treatment and prevention of disorders known to be susceptible to improvement by antagonism of the A2B receptor such as asthma, chronic obstructive pulmonary disorder (COPD), pulmonary fibrosis, vascular diseases, allergic diseases, hypertension, retinopathy, diabetes mellitus, inflammatory gastrointestinal tract disorders, inflammatory diseases, autoimmune diseases, renal diseases, neurological disorders and, in particular, cancers. In particular, the present invention relates to compounds of formula (I), wherein R1 represents 1 to 3 identical or different R1 substituents, wherein said R1 is independently at each occurrence selected from hydrogen, halogen, C | 2021-12-23 |
20210395226 | SUBSTITUTED ARYL COMPOUND AND PREPARATION METHOD THEREFOR AND USE THEREOF - The present application relates to a substituted aryl compound or a pharmaceutically acceptable salt, a stereoisomer, a polymorph, a solvate, a N-oxide, an isotope-labeled compound, a metabolite or a prodrug thereof, and a preparation method therefor and use thereof, also relates to a pharmaceutical composition containing the compound and a therapeutic use thereof. The compound or a pharmaceutical composition thereof can inhibit the activity of adenosine A2a receptor, and can be used for treating or preventing a disease related to adenosine A2a receptor, especially for treating a tumor. | 2021-12-23 |
20210395227 | THERAPEUTIC COMPOUNDS - The present invention relates to compounds that are antagonists of the orexin-1 receptor. The compounds have the structural formula (I) defined herein. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or disorders associated with orexin-1 receptor activity. | 2021-12-23 |
20210395228 | PESTICIDALLY ACTIVE BENZENE- AND AZINE-AMIDE COMPOUNDS - Compounds of formula (I) wherein the substituents are as defined in claim | 2021-12-23 |
20210395229 | CRYSTALLINE FORMS OF POTASSIUM CHANNEL MODULATORS - Provided herein are crystalline and amorphous forms of a compound having structural formula (1). Also provided are pharmaceutical compositions comprising the crystalline and amorphous forms, methods for their manufacture, and uses thereof for treating a variety of diseases, disorders or conditions, associated with potassium channels. | 2021-12-23 |
20210395230 | EGFR INHIBITOR COMPOUNDS - Disclosed herein are nitrogen-containing bicyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein. | 2021-12-23 |
20210395231 | RECEPTOR INHIBITORS, PHARMACEUTICAL COMPOSITIONS COMPRISING THE SAME AND USE THEREOF - The present invention discloses a receptor inhibitor of formula (I), a composition comprising the same and the usage thereof. | 2021-12-23 |
20210395232 | CO-CRYSTAL FORMS OF SELINEXOR - The present invention is directed to selinexor co-crystal forms; more particularly to two co-crystal forms with succinic acid as the coformer and a co-crystal form with vanillin as the coformer. The present disclosure is also related to processes for the preparation of selinexor co-crystal forms. Further, the present invention also relates to pharmaceutical compositions comprising a selinexor co-crystal form and method for treating disease using a selinexor co-crystal form. | 2021-12-23 |
20210395233 | NEW COMPOUND AND ORGANIC ELECTROLUMINESCENCE DEVICE - A compound having a structure represented by the following formulas (a) and (b):
| 2021-12-23 |
20210395234 | NOVEL INDAZOLE COMPOUND OR SALT THEREOF - An indazole compound represented by the following Formula (I) or a salt thereof: | 2021-12-23 |
20210395235 | COMPOUND AS TGF-beta R1 INHIBITOR AND APPLICATION THEREOF - The present application relates to a compound as a TGF-β R1 inhibitor and application thereof. Specifically, provided are a compound of formula I, or an isomer, pharmaceutically acceptable salt, solvent, crystal, or prodrug thereof, preparation methods therefor, and pharmaceutical compositions comprising these compounds, and applications of these compounds or compositions in treating and/or preventing TGF-β R1-related diseases, such as cancer, tissue proliferation diseases, fibrosis, and inflammatory diseases. The compound represents a significant inhibitory activity for TGF-β R1 kinase, and is promising as a treatment agent for TGF-β R1-related diseases. | 2021-12-23 |
20210395236 | N-HETEROARYL INDAZOLE DERIVATIVES AS LRRK2 INHIBITORS, PHARMACEUTICAL COMPOSITIONS, AND USES THEREOF - The present invention is directed to substituted certain N-heteroaryl indazole derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R | 2021-12-23 |
20210395237 | COMPOUNDS FOR THE TREATMENT OF GLYCOGEN STORAGE DISORDERS - Compounds represented by general Formulae I to IV as described herein are disclosed. Further disclosed are composition utilizing the herein disclosed compounds and using the same for the treatment of glycogen storage disorders. | 2021-12-23 |
20210395238 | NADPH OXIDASE 4 INHIBITORS - The invention relates to 2,5-disubstituted benzoxazole and benzothiazole derivatives of Formula (I) | 2021-12-23 |
20210395239 | HETEROCYCLYL COMPOUNDS FOR THE TREATMENT OF AUTOIMMUNE DISEASE - The present invention relates to compounds of formula (I), wherein R | 2021-12-23 |
20210395240 | NOVEL SUBSTITUTED PYRAZOLE COMPOUNDS AS INDOLEAMINE 2,3-DIOXYGENASE INHIBITORS - Disclosed herein are compounds of formula (I) which are inhibitors of an IDO enzyme: (I). Also disclosed herein are uses of the compounds in the potential treatment or prevention of an IDO-associated disease or disorder. Also disclosed herein are compositions comprising these compounds. Further disclosed herein are uses of the compositions in the potential treatment or prevention of an IDO-associated disease or disorder. | 2021-12-23 |
20210395241 | NLRP MODULATORS - In one aspect, compounds of Formula AA, or a pharmaceutically acceptable salt thereof, are featured: or a pharmaceutically acceptable salt thereof, wherein the variables shown in Formula A can be as defined anywhere herein. | 2021-12-23 |
20210395242 | HETEROCYCLIC COMPOUNDS AS AHR MODULATORS - The present invention relates compounds of the general formula (I) or (III) which are ARH inhibitors, methods for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds and pharmaceutical compositions for the treatment or prevention of diseases, in particular cancer or conditions with dysregulated immune functions, or other conditions associated with aberrant AHR signalling, as a sole agent of in combination with other active ingredients. Such compounds may also be of utility in the expansion of hematopoietic stem cells (HSCs) and the use of HSCs in autologous or allogenic transplantation for the treatment of patients with inherited immunological and autoimmune diseases and diverse hematopoietic disorders. | 2021-12-23 |
20210395243 | PESTICIDAL COMPOUNDS - The present invention relates to the compounds of formula (I), and the N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof wherein the variables are defined according to the description, (I) The compounds of formula (I), as well as the N-oxides, stereoisomers, tautomers and agriculturally or veterinarily acceptable salts thereof, are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds. | 2021-12-23 |
20210395244 | MITOGEN-ACTIVATED PROTEIN KINASE KINASE (MEK) DEGRADATION COMPOUNDS AND METHODS OF USE - This disclosure relates to heterobifunctional compounds (e.g., bi-functional small molecule compounds), compositions comprising one or more of the heterobifunctional compounds, and to methods of use the heterobifunctional compounds for the treatment of certain disease in a subject in need thereof. The disclosure also relates to methods for identifying such heterobifunctional compounds. | 2021-12-23 |
20210395245 | ORGANIC COMPOUND, EL DEVICE, LIGHT-EMITTING APPARATUS, ELECTRONIC APPLIANCE, LIGHTING DEVICE, AND ELECTRONIC DEVICE - An object is to provide an organic compound with a low refractive index. Alternatively, a novel organic compound with a low refractive index and an electron-donating property is provided. Alternatively, an EL device with high emission efficiency is provided. An organic compound having an arylamine skeleton including a fluorine atom or an acridine skeleton including a fluorine atom and an EL device using the organic compound are provided. The EL device preferably includes a hole-injection layer containing the organic compound having an arylamine skeleton including a fluorine atom or an acridine skeleton including a fluorine atom and a substance showing an electron-accepting property with respect to the organic compound. | 2021-12-23 |
20210395246 | BICYCLIC HETEROCYCLES AS FGFR INHIBITORS - The present invention relates to bicyclic heterocycles, and pharmaceutical compositions of the same, that are inhibitors of one or more FGFR enzymes and are useful in the treatment of FGFR-associated diseases such as cancer. | 2021-12-23 |
20210395247 | BTK INHIBITORS, PHARMACEUTICALLY ACCEPTABLE SALTS, POLYMORPHS AND APPLICATION THEREOF - The present invention provides a BTK inhibitor, a pharmaceutically acceptable salt, a polymorph and an application thereof. Specifically, the present invention provides (R)-6-((1-acryloylpiperidin-3-yl)amino)-7-fluoro-4-((2-fluoro-4-morpholinophenyl)amino)-1,2-dihydro-3H-pyrrolo[3,4-c]pyridin-3-one, or the polymorph of a pharmaceutically acceptable salt thereof, and an application thereof. In addition, the present invention further discloses a pharmaceutical composition comprising the inhibitor and an application thereof. | 2021-12-23 |
20210395248 | INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - Compounds of Formula I, and pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth: | 2021-12-23 |
20210395249 | NEW ALKOXYAMINOPYRIDINE DERIVATIVES FOR TREATING PAIN AND PAIN RELATED CONDITIONS - The present invention relates to new compounds of formula (I) that show dual activity towards the subunit α2δ of voltage-gated calcium channels (VGCC), especially the α2δ-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions comprising them, and to their use as medicaments. | 2021-12-23 |
20210395250 | NOVEL CRYSTAL OF (3S)-3-[2-(6-AMINO-2-FLUOROPYRIDIN-3-YL)-4-FLUORO-1H-IMIDAZOL-5-YL]-7-[5-- CHLORO-2-(1H-TETRAZOL-1-YL)PHENYL]-2,3-DIHYDROINDOLIZIN-5(1H)-ONE - A novel crystal form of (3S)-3-[2-(6-amino-2-fluoropyridin-3-yl)-4-fluoro-1H-imidazol-5-yl]-7-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]-2,3-dihydroindolizin-5(1H)-one, which is (3S)-3-[2-(6-amino-2-fluoropyridin-3-yl)-4-fluoro-1H-imidazol-5-yl]-7-[5-chloro-2-(1H-tetrazol-1-yl)phenyl]-2,3-dihydroindolizin-5(1H)-one-3-hydroxybenzoic acid (1/1). | 2021-12-23 |
20210395251 | NAPHTHYRIDINONE COMPOUNDS AS JAK2 V617F INHIBITORS - The present application provides naphthyridinone compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer. | 2021-12-23 |
20210395252 | 3,9-DIAZASPIRO[5,5]UNDECANE COMPOUND AS FLT3 AND AXL INHIBITORS - Disclosed in the present invention is a novel compound as FLT3 and AXL inhibitors. Specifically, disclosed are a compound represented by formula (I) and a pharmacologically acceptable salt thereof. (I) | 2021-12-23 |
20210395253 | FARNESOID X RECEPTOR AGONISTS AND USES THEREOF - Described herein are compounds that are farnesoid X receptor agonists, 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 associated with farnesoid X receptor activity. | 2021-12-23 |
20210395254 | NEW TETRAHYDROPYRIMIDODIAZEPIN AND TETRAHYDROPYRIDODIAZEPIN COMPOUNDS FOR TREATING PAIN AND PAIN RELATED CONDITIONS - The present invention relates to new compounds of general formula (I) that show dual activity towards subunit α2δ of voltage-gated calcium channels (VGCC), especially α2δ-1 subunit of voltage-gated calcium channels, and noradrenaline transporter (NET). The invention is also related to the process for the preparation of said compounds as well as to compositions composing them, and to their use as medicaments. | 2021-12-23 |
20210395255 | SUBSTITUTED AMINO TRIAZOLOPYRIMIDINE AND AMINO TRIAZOLOPYRAZINE ADENOSINE RECEPTOR ANTAGONISTS, PHARMACEUTICAL COMPOSITIONS AND THEIR USE - In its many embodiments, the present invention provides certain substituted amino triazolopyrimidine and amino triazolopyrazine compounds of Formula (IA) and Formula (IB): or and pharmaceutically acceptable salts thereof, wherein, R | 2021-12-23 |
20210395256 | TYROSINE KINASE INHIBITORS, COMPOSITIONS AND METHODS THERE OF - The present invention relates to compounds of Formula I, methods of using the compounds as Trk inhibitors, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. | 2021-12-23 |
20210395257 | PYRROLOTRIAZINE COMPOUNDS AS JAK2 V617F INHIBITORS - The present application provides pyrrolotriazine compounds that modulate the activity of the V617F variant of JAK2, which are useful in the treatment of various diseases, including cancer. | 2021-12-23 |
20210395258 | HETEROCYCLIC DERIVATIVES AS PI3K INHIBITORS - This application relates to compounds of Formula (I): | 2021-12-23 |
20210395259 | CDK INHIBITORS - Compounds of Formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors. | 2021-12-23 |
20210395261 | METHYL (R)-2-(FLUOROMETHYL)-5-OXO-4-PHENYL-4,5,6,7-TETRAHYDRO-1H-CYCLOPENT- A[B]PYRIDINE-3-CARBOXYLATE AND METHYL (R)-2-(FLUOROMETHYL)-5-OXO-4-PHENYL-1,4,5,7-TETRAHYDROFURO[3,4-B]PYRIDINE- -3-CARBOXYLATE AS CAV1.2 ACTIVATORS - The present disclosure provides for a compound according to formula (I) | 2021-12-23 |
20210395262 | INHIBITORS OF HUMAN IMMUNODEFICIENCY VIRUS REPLICATION - Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth. | 2021-12-23 |
20210395263 | HETEROCYCLIC COMPOUND, ORGANIC LIGHT EMITTING DIODE COMPRISING SAME, COMPOSITION FOR ORGANIC LAYER OF ORGANIC LIGHT EMITTING DIODE, AND METHOD FOR MANUFACTURING ORGANIC LIGHT EMITTING DIODE - The present specification provides a heterocyclic compound represented by Chemical Formula 1, an organic light emitting device comprising the same, a composition for an organic material layer of an organic light emitting device, and a method for manufacturing an organic light emitting device. | 2021-12-23 |
20210395264 | XANTHONIC COMPOUNDS AND THEIR USE AS ANTIFOULING AGENTS - Synthetic small molecules from an important class of heterocyclic derivatives and homologs and their use as antifouling agents for protection against marine biofouling. The antifouling compounds disclosed herein are environmentally friendly and are able to reduce marine biofouling without inducing toxic effects to target and non-target species. The claimed antifouling compounds also possess ability to be incorporated as antifouling additives in polymeric formulations. Thus, allowing its further application for the preparation of antifouling polymeric matrices, such as coatings, with no hazard effects for the environment. | 2021-12-23 |
20210395265 | ANTI-CANCER AGENTS AND PREPARATION THEREOF - Embodiments provide, among other compounds, a family of compounds that can be used as therapeutic anti-cancer agents, methods for using such compounds to treat cancer, and methods of making such compounds. | 2021-12-23 |
20210395266 | IN-FLOW PHOTOOXYGENATION OF AMINOTHIENOPYRIDINONES GENERATES NOVEL PTP4A3 PHOSPHATASE INHIBITORS - The disclosure provides compounds that inhibit protein tyrosine phosphatase, such as protein tyrosine phosphatase 4A3 (PTP4A3). The disclosure also provides pharmaceutical compositions, uses, and methods of using the compounds, such as in the treatment of cancers. (I), wherein X is O or NH. | 2021-12-23 |
20210395267 | Novel Thienopyrimidones - This invention relates to thienopyrimidinones and their use as inhibitors of TRPA1 activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of fibrotic diseases, inflammatory and auto-immune diseases and CNS-related diseases. | 2021-12-23 |
20210395268 | CHEMICAL COMPOUNDS AS INHIBITORS OF INTERLEUKIN-1 ACTIVITY - The present disclosure relates to novel sulfonylurea and sulfonyl thiourea compounds and related compounds and their use in treating a disease or condition responsive to modulation of cytokines such as IL-1β and IL-18, modulation of NLRP3 or inhibition of the activation of NLRP3 or related components of the inflammatory process. | 2021-12-23 |
20210395269 | COMPOUND HAVING AZABENZOXAZOLE RING STRUCTURE AND ORGANIC ELECTROLUMINESCENT ELEMENT - An object of the present invention is to provide, as a material for a highly efficient and highly durable organic EL element, an organic compound having excellent properties, including excellent electron-injecting/transporting capability, hole-blocking capability, and high stability in the form of a thin film. Another object of the present invention is to provide a highly efficient and highly durable organic EL element by using this compound. The compound having an azabenzoxazole ring structure of the present invention has excellent heat resistance, and good electron-transporting capability. An organic EL element having an electron-transporting layer, a hole-blocking layer, a light-emitting layer, or an electron-injecting layer including the compound had favorable element characteristics. | 2021-12-23 |
20210395270 | TRIAZOLO-AZEPINE DERIVATIVES - The present invention relates to a compound of formula (I) wherein Ar is (II) or (II); R is CH | 2021-12-23 |
20210395271 | COMPOSITION FOR EL DEVICE - An object is to provide a novel composition for an EL device. Another object of one embodiment of the present invention is to provide a composition for an EL device capable of easily manufacturing an EL device with stable characteristics. Another object of one embodiment of the present invention is to provide a composition for an EL device capable of manufacturing an EL device with stable characteristics at low cost. The present inventors have studied a composition for an EL device in which different substances are mixed in advance and which does not cause change in characteristics of the EL device even when evaporation is repeated with use of the composition. As a result, a composition for an EL device in which a difference in the 5% weight loss temperature under a pressure lower than or equal to 0.1 Pa between contained substances is less than or equal to 50° C. is provided. | 2021-12-23 |
20210395272 | PHOTOACTIVE COMPOUND - A compound of formula (I): Each R | 2021-12-23 |
20210395273 | CRYSTALLINE FORMS OF IRAK DEGRADERS - The present disclosure relates generally to various forms, salts and compositions of compounds useful for the modulation of one or more interleukin-1 receptor-associated kinases (“IRAK”) via ubiquitination and/or degradation and uses of the same in the treatment various diseases. | 2021-12-23 |
20210395274 | POLYCYCLIC AROMATIC COMPOUND AND LIGHT EMISSION LAYER-FORMING COMPOSITION - The objective of the invention is to provide a polycyclic aromatic compound in which solubility to a solvent, film formability, wet coatability, thermal stability, and in-plane orientation are improved. This objective is achieved by alight emission layer-forming composition comprising: as a first component, at least one type of dopant material selected from the group consisting of polycyclic aromatic compounds represented by general formula (A) and polycyclic aromatic oligomer compounds including a plurality of structures represented by general formula (A); as a second component, a specific low-molecular-weight host material; and, as a third component, at least one type of organic solvent. In formula (A), ring A, ring B, and ring C each independently represent an aryl ring or a hetero aryl ring, Y | 2021-12-23 |
20210395275 | COMPOSITIONS AND METHODS FOR SELECTIVE SEPARATION OF HYDROCARBON ISOMERS - The present disclosure relates to novel metal-organic frameworks (MOFs) comprising tetratopic linkers with small pore apertures. In certain aspects, the disclosure provides Zr-MOFs, non-limiting examples include Zr(bptc), Zr(abtc), and Zr(tptc-(Me) | 2021-12-23 |
20210395276 | ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES - Provided are spiro-bisilepine compounds. Also provided are formulations comprising these spiro-bisilepine compounds. Further provided are OLEDs and related consumer products that utilize these spiro-bisilepine compounds. | 2021-12-23 |
20210395277 | COMPOSITION FOR ORGANIC OPTOELECTRONIC DEVICE, ORGANIC OPTOELECTRONIC DEVICE, AND DISPLAY DEVICE - A composition for an organic optoelectronic device, an organic optoelectronic device, and a display device, the composition including a first compound represented by Chemical Formula 1 and a second compound represented by Chemical Formula 2, | 2021-12-23 |
20210395278 | FUNCTIONALIZED HYDROXYSILANES, SILYLATED POLYURETHANES, AND COMPOSITIONS COMPRISING SAME - The present invention relates to a compound of formula (I): | 2021-12-23 |
20210395279 | METHOD OF FORMING A CRYSTALLINE OR POLYCRYSTALLINE LAYER OF AN ORGANIC-INORGANIC METAL HALIDE PEROVSKITE - The present invention provides a method of forming a crystalline or polycrystalline layer of an organic-inorganic metal halide perovskite material comprising a three-dimensional crystal structure represented by the formula AMX | 2021-12-23 |
20210395280 | Targeting Redox-Active Pyridinium Cations to Mitochondria to Inhibit Proliferation of Drug-Resistant Cancer Cells - The present invention provides novel mito-pyridinium compounds, prodrugs and the uses thereof for the treatment of cancer, particularly drug resistant cancer. | 2021-12-23 |
20210395281 | MACROCYCLIC CHELATES AND USES THEREOF - The present disclosure relates to macrocyclic chelates including a macrocyclic chelating moiety of a metal complex thereof, a bifunctional linker, and a therapeutic or targeting moiety. Also disclosed are methods for preparation of the same, and use thereof. | 2021-12-23 |
20210395282 | CATALYST FOR ASYMMETRIC HYDROGENATION OF COMPOUND CONTAINING CARBON DOUBLE BOND - The present invention may provide an asymmetric hydrogenation catalyst capable of resolving enantiomers with excellent enantioselectivity from a carbon-carbon double bond-containing compound. The catalyst according to one embodiment of the present invention includes: an iridium cation; and a ligand bonded to the iridium cation. | 2021-12-23 |
20210395283 | COMPOUND, COMPLEX, PREPARATION METHOD THEREOF, AND USE THEREOF - The present disclosure provides a compound, a complex, a preparation method thereof, and a use thereof. The compound is represented by the following structural formula, in which R | 2021-12-23 |
20210395284 | OLIGOSACCHARIDE PREPARATIONS AND COMPOSITIONS - The present disclosure relates oligosaccharide preparations suitable for use in nutritional compositions such as animal feed and methods of manufacturing the described oligosaccharide preparations. The present disclosure further relates to nutritional compositions that comprise the oligosaccharide preparations. The disclosed oligosaccharide preparations can be advantageous as an animal feed due to, at least in part, their prebiotic utility and the presence of anhydro-subunit containing oligosaccharides, which can be used to detect and/or determine the presence and content of the disclosed oligosaccharide preparations in the nutritional composition. | 2021-12-23 |
20210395285 | SALTS OF CONJUGATES FOR CANCER THERAPY - The present invention relates to pharmaceutically acceptable salts of conjugates comprising a chemotherapeutic drug and an amino acid or a derivative thereof, which are readily taken up by a target cell and reduce side effects induced by the chemotherapeutic drug. In particular, the present invention relates to pharmaceutically acceptable salts of conjugates comprising cytidine analog drugs and aspartic or glutamic acid and analogs thereof, pharmaceutical compositions comprising these conjugates and use thereof for the treatment of cancer or a pre-cancer condition or disorder. | 2021-12-23 |
20210395286 | PHYSICALLY PRETREATED BIOMASS COMPOSITION COMPRISING A HIGH CONCENTRATION OF BIOMASS - The present disclosure relates to a physically pretreated biomass composition, which enables chemical treatment in a biomass composition comprising a high concentration of a biomass substrate, and a preparation method thereof. | 2021-12-23 |
20210395288 | SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALAOGS THEREOF - Disclosed herein are compounds of the Formula (I) and pharmaceutically acceptable salts thereof: (I) where the variables in Formula (I) are described herein. Methods of synthesizing such compounds and methods of using them to treat diseases and/or conditions such as a Picornaviridae, Flaviviridae, Filoviridae, Pneumoviridae and/or Coronaviridae viral infections are also disclosed. | 2021-12-23 |
20210395289 | NOVEL BENZIMIDAZOLE DERIVATIVES, PREPARATION METHOD THEREOF AND USE THEREOF AS ANTI-CANCER AGENT OR ANTI-VIRUS AGENT COMPRISING THE SAME - The present invention provides a benzimidazole derivative represented by the following Chemical Formula 1, a preparation method thereof, and use thereof as an anticancer or anti-virus agent: | 2021-12-23 |
20210395290 | PHOSPHORAMIDATES FOR THE TREATMENT OF HEPATITIS B VIRUS - Disclosed are compounds to the treatment of infectious diseases and methods of treating such diseases. The compounds are derivatives of clevudine. | 2021-12-23 |
20210395291 | CRYSTALLINE FORMS OF A CD73 INHIBITOR AND USES THEREOF - Crystalline forms of the compound of Formula (I), which modulates the conversion of AMP to adenosine by 5′-nucleotidase, ecto, and compositions containing the compound and methods for preparing the crystalline forms, are described herein. The use of such crystalline form of Formula (I) and compositions for the treatment and/or prevention of a diverse array of diseases, disorders and conditions, including cancer and immune-related disorders, that are mediated by 5′-nucleotidase, ecto is also provided. | 2021-12-23 |
20210395292 | Detection Method for Natural and Modified Small Nucleic Acids - The invention relates to a method for the detection of natural or modified nucleic acids by their sequence specific hybridization with charge-modified oligonucleotide probes having charge-modifying groups attached to their backbones. The charge-modifying groups partially or fully neutralize the net negative charge of the backbone of the oligonucleotide probes or render them with a net positive charge. The charge-modified oligonucleotide probes may or may not be labeled, for example, with fluorescent, visible or near-infrared dye, with radioactive or stable isotopes, or with high specific affinity binding groups. The charge-modified oligonucleotide probes facilitate the separation of their hybrids with the targeted nucleic acids from the unhybridized probes or from any other components of the analyzed sample. They also allow for the modification and optimization of the properties of the hybrids with the targeted nucleic acids, such as melting temperature, chromatographic properties and off-target specificity. | 2021-12-23 |
20210395293 | PREPARATION AND USES OF OBETICHOLIC ACID - The present invention relates to obeticholic acid: | 2021-12-23 |
20210395294 | PROGESTERONE PHOSPHATE ANALOGS AND USES RELATED THERETO - This disclosure relates to progesterone phophate derivatives and uses related thereto. In certain embodiments, the disclosure relates to compounds disclosed herein and uses for managing inflammation such as those resulting from traumatic brain injury or stroke. | 2021-12-23 |
20210395295 | INHIBITORS OF GLUCOCORTICOID RECEPTOR - The present invention relates generally to compositions and methods for treating cancer and hypercortisolism. Provided herein are substituted steroidal derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of glucocorticoid receptors. Furthermore, the subject compounds and compositions are useful for the treatment of cancer and hypercortisolism. | 2021-12-23 |
20210395296 | NOVEL SALTS AND POLYMORPHS OF SCY-078 - SCY-078 is a glucan synthase inhibitor with antimicrobial activity. Novel salts and polymorph forms of SCY-078 are disclosed herein. The disclosure also relates to pharmaceutical compositions, methods of use, and methods of preparing the novel salts and polymorphs of SCY-078. | 2021-12-23 |
20210395297 | Preparation Method of Vascular Leakage Blockers With a High Yield - The present invention relates to a preparation method of a novel vascular leakage blocker with a high yield. The preparation method is easy to react and more productive and economical than the conventional method by using an intermediate that can easily remove impurities generated during the reaction. In addition, the preparation method can produce a novel vascular leakage blocker with a high yield by using a new reagent that has not been previously used in the step of generating an isomer, and is very advantageous in producing a high-quality active pharmaceutical ingredient. | 2021-12-23 |
20210395298 | DOWNSTREAM PROCESSING OF BISPECIFIC ANTIBODY CONSTRUCTS - The present invention provides an improved manufacturing method for the production of bispecific antibody products, which comprise at least two binding domains. The process comprises at least the method comprising a step of refolding the construct, wherein one or more of the domains comprise a disulfide bond, and wherein the construct is contacted with a refolding buffer to refold the construct to its native form, the buffer comprising (i) a redox and/or oxidizing agent having a concentration of at least 0.1 mM and (ii) a chaotropic agent having a concentration >1 M, and wherein the pH of the refolding buffer corresponds to +/−4.5 of the pI value of the first domain or +/−4.0 of the pI value of the entire construct. | 2021-12-23 |
20210395299 | NOVEL DIPEPTIDE COMPOUNDS AND USES THEREOF - Provided herein are novel compounds of Formula I, or a pharmaceutically acceptable salt thereof or pharmaceutical compositions comprising the same. Also provided are methods of preparing the compounds of Formula I, or pharmaceutically acceptable salt thereof. Further provided are methods of using the novel compounds of Formula I, or a pharmaceutically acceptable salt thereof, for example, for inhibiting thrombin and/or for the use in the prevention and/or treatment of thrombin-mediated and thrombin-related diseases. | 2021-12-23 |
20210395300 | PEPTIDOMIMETICS FOR THE TREATMENT OF NOROVIRUS INFECTION - The present invention is directed to compounds, compositions and methods for preventing, treating or curing Norovirus infection in human subjects or other animal hosts. | 2021-12-23 |
20210395301 | SYNTHESIS OF BORONIC ESTER AND ACID COMPOUNDS - The invention relates to the synthesis of boronic ester and acid compounds. More particularly, the invention provides improved synthetic processes for the large-scale production of boronic ester and acid compounds, including the peptide boronic acid proteasome inhibitor bortezomib. | 2021-12-23 |
20210395302 | PEPTIDES FOR ACTIVATION OF CELL SIGNALING IN OSTEOPROGENITOR CELLS - The present invention provides compounds and pharmaceutical compositions of peptidomimetic ligands. The peptidomimetic ligands can be conjugated with phosphonate drugs. The compounds and pharmaceutical compositions of the present invention are useful in the treatment of osteoporosis and for the promotion of bone growth due to their specificity for the α | 2021-12-23 |
20210395303 | MINI-NUCLEOSOME CORE PROTEINS AND USE IN NUCLEIC ACID DELIVERY - The present disclosure provides compositions and methods relating to mini-nucleosome core proteins and/or delivery of nucleic acids. In particular, the present disclosure includes, among other things, non-viral proteinaceous vehicles for delivery of nucleic acids. In various embodiments, non-viral proteinaceous vehicles provided herein include (a) a nucleic acid binding domain; (b) a targeting domain; and, optionally, (c) a nucleic acid release domain, stability domain, and/or an oligomerization domain, and/or a linker domain. | 2021-12-23 |
20210395304 | BIOMIMETIC PEPTIDES DERIVED FROM BIOLOGICAL SOURCE AND THEIR USES IN RETARDING AGING AND IMPROVING SKIN - The present disclosure provides peptides comprising a motif having four amino acids, wherein each of the amino acids at N-terminus and C-terminus of the sequence independently has a same or different positively charged side chain, and each of the amino acids between the N-terminal and C-terminal of the motif independently has a same or different uncharged side chain. The present disclosure surprisingly found that these peptides have advantageous effects in inhibiting or decreasing collagen breakdown, increasing production of collagen, elastin and/or hyaluronic acid, retarding aging, improving skin and inhibiting inflammation. | 2021-12-23 |
20210395305 | PEPTIDE FOR COSMETIC APPLICATION - The present invention relates to the use of a peptide comprising the sequence ID No. 1 and a cosmetic composition thereof in the treatment and prevention of skin aging and photo-aging. | 2021-12-23 |
20210395306 | POLYPEPTIDES FOR THE TREATMENT OF STRESS, IMMUNOREACTION AND STROKE SYNDROMES - A polypeptide having the general amino acid sequence written in the single letter code | 2021-12-23 |
20210395307 | PEPTIDE THAT REGULATES FAT METABOLISM AND METHOD FOR REGULATING FAT METABOLISM - The present disclosure relates to a peptide for regulating fat metabolism and a method of regulating fat metabolism in an individual. The peptide is a variant of a SEQ ID NO: 2 having an amino acid sequence of YLYQWLGAPVPYPDPLEP, the variant comprises peptides selected from the group consisting of: (a) a first amino acid sequence consisting of the SEQ ID NO: 2, no more than 5 amino acids inserted to a C-terminal of the SEQ ID NO: 2, and no more than 5 amino acids inserted to a N-terminal of the SEQ ID NO: 2; (b) a second amino acid sequence consisting of a modified SEQ ID NO: 2; and (c) a third amino acid sequence consisting of at least 6 contiguous amino acids of the SEQ ID NO: 2 or the modified SEQ ID NO: 2. | 2021-12-23 |
20210395308 | ANG (1-7) DERIVATIVE OLIGOPEPTIDES AND METHODS FOR USING AND PRODUCING THE SAME - The present invention provides oligopeptides, in particular, Ang-(1-7) derivatives, and methods for using and producing the same. In one particular embodiment, oligopeptides of the invention have higher blood-brain barrier penetration and/or in vivo half-life compared to the native Ang-(1-7), thereby allowing oligopeptides of the invention to be used in a wide variety of clinical applications including in treatment of cognitive dysfunction and/of impairment. | 2021-12-23 |
20210395309 | PEPTIDE-DRUG CONJUGATES - Provided herein are Bradykinin-potentiating peptide chemotherapeutic drug conjugates useful as cancer therapeutics, pharmaceutical compositions comprising the same, and methods of preparation and use thereof. | 2021-12-23 |
20210395310 | Cyclic Peptide - The purpose of the present invention is to provide a cyclic peptide having any unit structure selected from the structures represented by the following formula (1): | 2021-12-23 |
20210395311 | CYCLIC PEPTIDE DIMERS - Provided are cyclic peptide dimers. The cyclic peptide dimer include a first cyclic peptide attached to a second cyclic peptide. The present disclosure also provides compositions containing the cyclic peptide dimers. Also provided are methods of using the cyclic peptide dimers and/or compositions thereof to inhibit the growth of malignant cells in, for example, tumors. | 2021-12-23 |
20210395312 | QUANTUM CONFINED PEPTIDE ASSEMBLIES AND USES THEREOF - Self-assembled structures formed of a plurality of cyclic peptides which are in association with metal ions is provided. The cyclic peptides are each of from 2 to 6 amino acid residues, and two or more of the amino acid residues are each independently an aromatic amino acid residue. The self-assembled structures exhibit photoluminescence and can be used or incorporated in light emitting systems. | 2021-12-23 |