18th week of 2020 patent applcation highlights part 25 |
Patent application number | Title | Published |
20200131128 | METHOD FOR PREPARING 2,6-DICHLOROPYRIDINE THROUGH LIQUID PHASE PHOTOCHLORINATION OF PYRIDINE - The present invention relates to a method for preparing 2,6-dichloropyridine with product purity greater than or equal to 99.0% by using trifluoromethyl chlorobenzene as a solvent for reaction between pyridine and chlorine gas. The preparation process comprises the following steps: enabling pyridine and chlorine gas to continuously experience chlorination reaction under irradiation of ultraviolet light by using pyridine and chlorine gas as starting materials and using trifluoromethyl chlorobenzene as a solvent, and cooling a chlorination reaction product and the solvent to obtain pyridine chlorination solution. Advantages: firstly, it pioneers the precedent of direct and high-selectivity preparation of 2,6-dichloropyridine through liquid phase photochlorination, and not only can the 2,6-dichloropyridine product with purity greater than or equal to 99.0% be obtained, but also industrial production is facilitated; and secondly, not only can the reuse of the separated solvent in the preparation process of the 2,6-dichloropyridine product with purity greater than or equal to 99.0% be realized, but also the purposes of low pollution, low energy consumption and low cost in the preparation process can be realized. | 2020-04-30 |
20200131129 | 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. | 2020-04-30 |
20200131131 | NOVEL 5-HYDROXY PYRIDINE-BASED COMPOUND FOR USE AS P2X1 AND P2X3 RECEPTOR ANTAGONIST AND PHARMACEUTICAL COMPOSITION COMPRISING SAME - The present invention relates to novel 5-hydroxy pyridine-based compounds useful as P2X1 and P2X3 receptor antagonists and compositions comprising the same. The compounds according to the present invention have an activity of strongly antagonizing P2X1 and P2X3 receptors, and thus can be effectively used as a drug for treating or preventing chronic inflammatory diseases or neuropathic pain diseases caused by P2X1 and P2X3 receptor activity. | 2020-04-30 |
20200131132 | 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. | 2020-04-30 |
20200131133 | HETEROCYCLIC COMPOUND AND ORGANIC LIGHT EMITTING DEVICE COMPRISING SAME - The present specification relates to a heterocyclic compound represented by Chemical Formula 1, and an organic light emitting device comprising the same. | 2020-04-30 |
20200131134 | 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. | 2020-04-30 |
20200131135 | COMPOSITIONS AND METHODS FOR TREATING CANCER - Disclosed herein, inter alia, are compositions and methods for modulating Ras and treating cancer. | 2020-04-30 |
20200131136 | PROCESS FOR MANUFACTURING CHAIN-EXTENDED HYDROXYETHYLETHYLENEAMINES, ETHYLENEAMINES, OR MIXTURES THEREOF - The present disclosure pertains to a process for preparing hydroxyethylethyleneamines, ethyleneamines, or mixtures thereof, and/or ethylene urea derivatives thereof. The process includes reacting diethanolamine with an amine-functional compound that includes at least two —NH— units of which at least one is selected from the group of primary amine groups and cyclic secondary amine groups. The amine-functional compound includes at least one —NH—CH2-CH2-NH— unit wherein one or more —NH—CH2-CH2-NH— units in the amine-functional compound may be present in the form of cyclic ethylene urea moieties, piperazine moieties, or linear ethylene urea moieties, in the presence of a carbon oxide delivering agent. | 2020-04-30 |
20200131137 | CONTINUOUS PROCESS FOR THE PREPARATION OF 2-(1H-IMIDAZOL-4-YL) ETHANAMINE AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - The invention relates to a commercially viable, cost effective and energy efficient process for the preparation of 2-(1H-Imidazol-4-yl)ethanamine or pharmaceutically acceptable salts thereof in high purity and yield via application of continuous flow technology. | 2020-04-30 |
20200131138 | FLUORENE DERIVATIVE AND ORGANIC LIGHT EMITTING DEVICE COMPRISING SAME - Provided is a fluorene derivative of Chemical Formula 1: | 2020-04-30 |
20200131139 | SMALL MOLECULE INHIBITORS OF BCL-2- ASSOCIATED DEATH PROMOTER (BAD) PHOSPHORYLATION - The invention relates to compounds of general formula (I): wherein R | 2020-04-30 |
20200131140 | CONTROLLED CYCLIZATION OF PEPTOIDS TO FORM CHIRAL DIKETOPIPERAZINES - The present disclosure provides improved methods for controlled cyclization of peptoid dimers to form N,N′-2,5-diketopiperazines (N,N′-2,5-DKPs) with significant selectivity. In at least some examples, selectivity is based on a serendipitous conglomeration of slow exchange of amide rotamers, steric repulsion from the degree of α-substitution, and the geometric bulk of an amine nucleophile. By varying reaction conditions, the selectivity of the reaction and formation of a particular N,N′-2,5-DKP can be switched. The cyclization works in the presence of a variety of protection groups and diverse functionalities. The teachings herein provide techniques for synthesizing N,N′-2,5-DKPs that can be readily docked with drug candidates for shuttling across the blood brain barrier. This method provides a facile way to produce substituted DKPs containing groups ready for post-modification to include docking drug candidates. | 2020-04-30 |
20200131141 | CHEMICAL COMPOUNDS - The present disclosure relates to compounds of Formula (I): and to their pharmaceutically acceptable salts, pharmaceutical compositions, methods of use, and methods for their preparation. The compounds disclosed herein inhibit the maturation of cytokines of the IL-1 family by inhibiting inflammasomes and may be used in the treatment of disorders in which inflammasome activity is implicated, such as inter alia autoinflammatory and autoimmune diseases and cancers. | 2020-04-30 |
20200131142 | 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. | 2020-04-30 |
20200131143 | DEUTERATED 1-PIPERAZINO-3-PHENYL INDANES FOR TREATMENT OF SCHIZOPHRENIA - The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D | 2020-04-30 |
20200131144 | AMINE OR (THIO)AMIDE CONTAINING LXR MODULATORS - The present invention relates to derivatives of formula (I) which bind to the liver X receptor (LXRα and/or LXRβ) and act preferably as inverse agonists of LXR. | 2020-04-30 |
20200131145 | NOVEL SYNTHESIS OF INTERMEDIATES FOR THE PREPARATION OF ALPHA-TOCOPHEROL - The present invention relates to a novel synthetic pathway for alpha-tocopherol. The invention discloses different reactions yielding some new intermediates in a very high yield and stereoselectivity. | 2020-04-30 |
20200131146 | APPARATUS AND METHOD FOR REMOVING A COMPONENT FROM A SOLUTION - An apparatus and method for removing a compound from a solution are disclosed. The apparatus includes a vessel, a solution heater, and an aeration device, wherein the solution heater and the aeration device are connected to the vessel. The solution is contained in the vessel and heated by the solution heater. The aeration device provides aeration to the heated solution for agitating the heated solution, and the component is thereby removed from the solution. | 2020-04-30 |
20200131147 | PEGYLATED THIOXANTHONE PHOTOINITIATOR AND PHOTOSENSITIVE RESIN COMPOSITION - The present invention discloses a PEGylated thioxanthone photoinitiator and a photosensitive resin composition, the PEGylated thioxanthone compound is eco-friendly and has low toxicity, high initiation efficiency and good thermal stability, meanwhile, as a kind of photoinitiator, the compound has a small amount of fragment residue after cured, and may improve the compatibility of the photoinitiator and photosensitive resin composition system. The photosensitive resin composition provided by the present invention has reasonable allocation of ingredients and content in the components thereof, capable of 3D-printing a hydrogel having a specific structure; the hydrogel has lower cytotoxicity and better biocompatibility, and may applied in bioengineering fields, e.g., 3D cell culture. | 2020-04-30 |
20200131148 | PYRIMIDINE TRICYCLIC ENONE DERIVATIVES FOR INHIBITION OF ROR-GAMMA AND OTHER USES - Disclosed herein are compounds of the formulas: as well as analogs thereof, wherein the variables are defined herein. Also provided are pharmaceutical compositions thereof. In some aspects, the compounds and compositions provided herein may be used to inhibit RORγ and/or reduce the expression of IL-17. Also provided are methods of administering compounds and composition provided herein to a patient in need thereof, for example, for the treatment or prevention of diseases or disorders associated with inflammation or autoimmune disorders. | 2020-04-30 |
20200131149 | CRYSTALLINE 4-AMINO-2-(2,6-DIOXOPIPERIDINE-3-YL)ISOINDOLINE-1,3-DIONE DIHYDRATE, COMPOSITIONS AND METHODS OF USE THEREOF - Provided herein is a crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate. Pharmaceutical compositions comprising the crystalline 4-amino-2-(2,6-dioxopiperidine-3-yl)isoindoline-1,3-dione dihydrate are also disclosed. | 2020-04-30 |
20200131150 | CONDENSED CYCLIC COMPOUND, COMPOSITION INCLUDING THE SAME AND ORGANIC LIGHT-EMITTING DEVICE INCLUDING THE SAME - A condensed cyclic compound represented by Formula 1 or Formula 2: | 2020-04-30 |
20200131151 | NOVEL PYRIDAZINES - The present invention relates to novel pyridazines, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment and/or prevention of diseases and disorders mediated by Autotaxin. | 2020-04-30 |
20200131152 | PHARMACEUTICAL FORMULATIONS OF N-(2-(2-(DIMETHYLAMINO) ETHOXY)-4-METHOXY-5-((4-(1-METHYL-1H-INDOL -3-YL)PYRIMIDIN-2-YL)AMINO)PHENYL)ACRYLAMIDE AND SALTS THEREOF - A pharmaceutical formulation of N-(2-(2-(dimethylamino)ethoxy)-4-methoxy-5-((4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)amino)phenyl)acrylamide (compound 1), in particular methanesulfonic acid salt thereof, and methods of using the pharmaceutical formulation for the treatment or prevention of diseases or medical conditions mediated through mutated forms of epidermal growth factor receptor (EGFR), such as various cancers, are disclosed. | 2020-04-30 |
20200131153 | PYRAZOLYL QUINOXALINE KINASE INHIBITORS - The invention relates to new quinoxaline derivative compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds in the treatment of diseases, e.g. cancer. | 2020-04-30 |
20200131154 | PYRAZOLYL COMPOUNDS AND METHODS OF USE THEREOF - Compounds having activity as chemotherapeutic agents are provided. The compounds have the following structure (I): | 2020-04-30 |
20200131155 | SOLID FORMS OF 4-(2-FLUORO-4-(1-METHYL-1H-BENZO[d]IMIDAZOL-5-YL)BENZOYL)PIPERAZIN-1-YL)(- 1-HYDROXYCYCLOPROPYL)METHANONE - The present disclosure reports solid forms of (4-(2-fluoro-4-(1-methyl-1H-benzo[d]imidazol-5-yl)benzoyl)piperazin-1-yl)(1-hydroxycyclopropyl)methanone. | 2020-04-30 |
20200131156 | ARYLSULFONYLPYROLECARBOXAMIDE DERIVATIVES AS Kv3 POTASSIUM CHANNEL ACTIVATORS - The present invention provides novel compounds which activate the Kv3 potassium channels. The compounds have the structure | 2020-04-30 |
20200131157 | PYRAZOLE DERIVATIVES FOR THE TREATMENT OF CYSTIC FIBROSIS - The present invention relates to compounds of Formula (I) or pharmaceutically acceptable salts or solvates thereof. It further discloses a pharmaceutical composition comprising the compounds of Formula (I) and their uses, in particular to modulate CFTR protein or ABC protein activities. | 2020-04-30 |
20200131158 | TYPE II TOPOISOMERASE INHIBITORS AND METHODS OF MAKING AND USING THEREOF - Disclosed are Type II Topoisomerase Inhibitors, analogs thereof, pharmaceutical compositions thereof and methods of making and using these compounds and compositions. Methods of using the disclosed compounds to treat infections, such as MRSA, MDR | 2020-04-30 |
20200131159 | POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1 - Described are positive allosteric modulators of muscarinic acetylcholine receptor M | 2020-04-30 |
20200131160 | ZINC INDICATORS FOR CELLULAR IMAGING - The present disclosure provides compounds of the formula: | 2020-04-30 |
20200131161 | NOVEL POCHONIOLIDE COMPOUND AND USE THEREOF - It is known that foods containing a carbohydrate, e.g., starch, in a large amount produce acrylamide upon heating at high temperatures. Some documents state that acrylamide is formed by the Maillard reaction of an amino acid, e.g., asparagine, with a reducing sugar. The purpose of the present invention is to provide a novel compound which is effective in inhibiting such foods from yielding acrylamide when treated at a high temperature. Specifically, the present invention provides a compound represented by General Formula (I). | 2020-04-30 |
20200131163 | NOVEL PROCESS FOR PREPARATION OF EMPAGLIFLOZIN OR ITS CO-CRYSTALS, SOLVATES AND THEIR POLYMORPHS THEREOF - The present invention relates to process for the preparation of Empagliflozin or its co-crystals, solvates and/or polymorphs thereof. The present invention also relates to novel intermediates used therein, and process for the preparation thereof. The present invention further relates to process for preparation of amorphous and crystalline form of Empagliflozin. | 2020-04-30 |
20200131164 | DIMETHYLAMINOETHANOL SALT OF A GLP-1 RECEPTOR MODULATOR - Crystalline 2-hydroxy-N,N-dimethylethanaminium 1-(2-(5-(tert-butyl)-thiophene-2-carboxamido)-3-(4-(5-(4′-ethyl-[1,1′-bi(cyclohexan)]-3-en-4-yl)pyrimidin-2-yl)phenyl)propanoyl)azetidine-3-carboxylate salt, and methods related to synthesis and therapeutic use of the same. | 2020-04-30 |
20200131165 | Bicycloheteroaryl-Heteroaryl-Benzoic Acid Compounds as Retinoic Acid Receptor Beta (RARBeta) Agonists - The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain bicycloheteroaryl-heteroaryl-benzoic acid compounds of the following formula (for convenience, collectively referred to herein as “BHBA compounds”), which, inter alia, are (selective) retinoic acid receptor beta (RARβ) (e.g., RARβ2) agonists. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to (selectively) activate RARβ (e.g., RARβ2), to cause or promote neurite development, neurite outgrowth, and/or neurite regeneration, and in the treatment of diseases and conditions that are mediated by RARβ (e.g., RARβ2), that are ameliorated by the activation of RARβ (e.g., RARβ2), etc., including, e.g., neurological injuries such as spinal cord injuries. | 2020-04-30 |
20200131166 | BENZISOXAZOLES - The present invention relates to novel fatty acid esters of the reversible Iloperidone metabolite P-88-8991, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them. | 2020-04-30 |
20200131167 | DIAMINO-ALKYLAMINO-LINKED ARYLSULFONAMIDE COMPOUNDS WITH SELECTIVE ACTIVITY IN VOLTAGE-GATED SODIUM CHANNELS - Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R | 2020-04-30 |
20200131168 | HEPATITIS B CORE PROTEIN MODULATORS - The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound. | 2020-04-30 |
20200131169 | 1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES - The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients. | 2020-04-30 |
20200131170 | Compounds for Pain Treatment, Compositions Comprising Same, and Methods of Using Same - The invention relates to compounds of formula (I), compositions containing the same, and methods for treating and/or diminishing pain in a subject. The compounds of formula (I) are effective for treating opioid-induced tachyphylaxis and opioid-induced hyperalgesia. | 2020-04-30 |
20200131171 | DUAL MECHANISM INHIBITORS FOR THE TREATMENT OF DISEASE - Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved. | 2020-04-30 |
20200131172 | DYNAMIN-1-LIKE PROTEIN INHIBITORS - This application is directed to inhibitors of dynamin-1-like protein (Drp1) represented by the following structural formula (I): and methods for their use, such as to treat one or more DRP1-related diseases. | 2020-04-30 |
20200131173 | VMAT2 INHIBITOR COMPOUNDS AND COMPOSITIONS THEREOF - Provided is a compound selected from compounds of Formula (I) and pharmaceutically acceptable salts, solvates, and hydrates thereof: (I) wherein R | 2020-04-30 |
20200131174 | HETEROCYCLIC COMPOUND - The present invention provides a compound or a salt thereof having a calcium-sensing receptor antagonistic activity, and being expected to be useful as an agent for preventing or treating heart failure, pulmonary hypertension, or the like. The compounds represented by formula (I) or a salt thereof has a calcium-sensing receptor antagonistic activity, and is expected to be useful as an agent for preventing or treating heart failure, pulmonary hypertension, or the like, wherein each symbol is as described in the specification. | 2020-04-30 |
20200131175 | NEW AZAQUINOLINE DERIVATIVES - The present invention covers azaquinoline compounds of general formula (I), with A being (A1) or (A2), and in which T, R | 2020-04-30 |
20200131176 | SELECTIVE INHIBITORS OF CLINICALLY IMPORTANT MUTANTS OF THE EGFR TYROSINE KINASE - The present invention provides compounds of Formula (I) or a subgeneric structure or species thereof, or a pharmaceutically acceptable salt, ester, solvate, and/or prodrug thereof, and methods and compositions for treating or ameliorating abnormal cell proliferative disorders, such as cancer, wherein A, R | 2020-04-30 |
20200131177 | PESTICIDALLY ACTIVE HETEROCYCLIC DERIVATIVES WITH SULFUR CONTAINING SUBSTITUENTS - Compounds of formula (I), wherein the substituents are as defined in claim | 2020-04-30 |
20200131178 | 2-AZABICYCLO HEXANE JAK INHIBITOR COMPOUND - The invention provides a compound of formula 1 | 2020-04-30 |
20200131179 | CRYSTALLINE FORMS OF MNK INHIBITORS - The present invention provides crystalline solids of 6′-((6-aminopyrimidin-4-yl)amino)-8′-methyl-2′H-spiro[cyclohexane-1,3′-imidazo[1,5-a]pyridine]-1′,5′-dione: | 2020-04-30 |
20200131180 | POSITIVE ALLOSTERIC MODULATORS OF THE MUSCARINIC ACETYLCHOLINE RECEPTOR M1 - Described are positive allosteric modulators of muscarinic acetylcholine receptor M | 2020-04-30 |
20200131181 | POLYMORPHS - The present invention relates to solid forms of the insecticide of formula I: I, compositions comprising the solid forms and methods of their use as insecticides. | 2020-04-30 |
20200131182 | POLYMORPHS - The present invention relates to solid forms of the insecticide of formula (I): (I) compositions comprising the solid forms and methods of their use as insecticides. | 2020-04-30 |
20200131184 | [1,2,4]TRIAZOLO[1,5-C]PYRIMIDINE DERIVATIVE AS A2A RECEPTOR INHIBITOR - Provided are a compound represented by formula (I), an isomer or a pharmaceutically acceptable salt thereof, and an application of the same in preparing a drug for treating a disease related to A | 2020-04-30 |
20200131185 | PYRROLOTRIAZINE COMPOUNDS AS TAM INHIBITORS - This application relates to compounds of Formula I: | 2020-04-30 |
20200131186 | PROCESS FOR THE PREPARATION OF PIPERAZINE RING FOR THE SYNTHESIS OF PYRAZINOCARBAZOLE DERIVATIVES - The present disclosure relates to an improved process for the synthesis of piperazine ring, particularly for the preparation of heterocyclic compounds useful as intermediates in the synthesis of pyrazinocarbazoles such as the antidepressant Pirlindole. The process described is useful to prepare Pirlindole enantiomers, or a pharmaceutically accepted salt thereof. | 2020-04-30 |
20200131187 | HETEROARYL-PYRAZOLE DERIVATIVE, AND PREPARATION METHOD THEREFOR AND MEDICAL APPLICATION THEREOF - A heteroaryl-pyrazole derivative, and a preparation method therefor and a medical application thereof are described. Specifically, a new heteroaryl-pyrazole derivative as shown in formula (I), a preparation method for the derivative, a pharmaceutical composition containing the derivative, and a use of the derivative as a therapeutic agent, in particular as a TLR7 agonist, are described. The substituents in formula (I) have the same definitions as in the description. | 2020-04-30 |
20200131188 | PYRAZOLO-QUINAZOLINE DERIVATIVES AS CHOLINE KINASE INHIBITORS - The present invention relates to substituted pyrazolo-quinazoline derivatives which modulate the activity of Choline Kinase (ChoK). The compounds of this invention are therefore useful in treating diseases caused by an altered choline metabolism, such as cancer, cell proliferative disorders, infectious diseases of different origin, immune-related disorders and neurodegenerative disorders. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing pharmaceutical compositions comprising these compounds. | 2020-04-30 |
20200131189 | Compounds, Compositions, and Methods for Modulating CDK9 Activity - Inhibitors of CDK9 that are pyrazolo[1,5-a]pyrimidine derivatives and salts thereof, corresponding to formula (I): | 2020-04-30 |
20200131190 | HETEROAROMATIC NMDA RECEPTOR MODULATORS AND USES THEREOF - Provided is 5-(3-chloro-4-fluorophenyl)-7-cyclopropyl-3-(2-(3-fluoro-3-methylazetidin-1-yl)-2-oxoethyl)-3,7-dihydro-4H-pyrrolo[2,3-d]pyrimidin-4-one and pharmaceutically acceptable salts thereof, and their uses in the treatment of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system. | 2020-04-30 |
20200131191 | ATROPISOMERISM FOR INCREASED KINASE INHIBITOR SELECTIVITY - The invention provides a series of conformationally stable kinase inhibitors, and methods of using the kinase inhibitors. The effect of atropisomerism on kinase selectivity was assessed, finding improved selectivity compared to rapidly interconverting parent compounds. | 2020-04-30 |
20200131192 | IMIDAZO[1,2-b]PYRIMIDO[4,5-d]PYRIDAZIN-5(6H)-ONES AND THE USE THEREOF - Disclosed are imidazo[1,2-b]pyrimido[4,5-d]pyridazin-5(6H)-one compounds, specifically represented by the Formula I: | 2020-04-30 |
20200131193 | PYRANOQUINAZOLINE DERIVATIVES AND NAPHTHOPYRAN DERIVATIVES - [Problem] A problem is presented in that conventional photochromic compounds cannot be considered adequate in terms of the colorizing/decolorizing rate and durability, and the production process therefore has many steps. The present invention provides an industrially applicable photochromic compound that has both a rapid colorizing/decolorizing reaction and high durability and can also be synthesized at a low cost. | 2020-04-30 |
20200131194 | FMS-LIKE TYROSINE KINASE INHIBITORS - The present invention relates to Fms-like tyrosine kinase (FLT3) inhibitors. The present invention provides novel 4-quinolinone derivatives used as FLT3 inhibitors and for treatment and/or prevention of tumors. | 2020-04-30 |
20200131195 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles of Formula (I): | 2020-04-30 |
20200131196 | Rapamycin Analog - The present invention relates to a novel rapamycin analogue (e.g., of Formula I or Formula II), mixtures, methods for its production, and its use in cancer therapy (e.g., prevention and/or treatment). | 2020-04-30 |
20200131197 | CRYSTAL OF CEPHALOSPORIN INTERMEDIATE 7alpha-METHOXY CEPHALOTHIN AND METHOD FOR PREPARING SAME - The present invention relates to a crystal of cephalosporin intermediate 7α-methoxy cephalothin (I) and a method for preparing same. The crystal of 7α-methoxy cephalothin (I) undergoes Cu-Ka radiation and X-ray powder diffraction expressed in terms of angle 2θ; the crystal of 7α-methoxy cephalothin (I) has characteristic absorption peaks at positions of 7.34°±0.20°, 12.71°±0.20°, 14.25°±0.20°, 14.68°±0.20°, 16.52°±0.20°, 17.99°±0.20°, 19.98°±0.20°, and 22.69°±0.20°. The crystal of 7α-methoxy cephalothin provided by the present invention is easy to prepare. Related test data shows that the crystal of 7α-methoxy cephalothin has high purity, low impurity content, and good stability. The preparation cost is low, the preparation method is simple to operate, conditions are mild and easy to control, and crystals of 7α-methoxy cephalothin can be obtained stably. The invention is applicable to industrial production. | 2020-04-30 |
20200131198 | Substituted pyrimidinium compounds and derivatives for combating animal pests - The present invention relates to substituted pyrimidinium compounds of formula (I), to the stereoisomers, salts, tautomers and N-oxides thereof and to compositions comprising such compounds. The invention also relates to methods and uses of these substituted pyrimidinium compounds and of compositions thereof, for combating and controlling animal pests. Furthermore the invention relates also to pesticidal methods of applying such substituted pyrimidinium compounds. | 2020-04-30 |
20200131199 | IMIDAZOOXAZOLE DERIVATIVE HAVING ANTITUMOR EFFECT, AND PHARMACEUTICAL COMPOSITION INCLUDING SAME - Provided is a pharmaceutical composition for preventing and treating tumors, the pharmaceutical composition including an imidazooxazole derivative compound, a solvate, a stereoisomer, or a pharmaceutically acceptable salt thereof as an active ingredient. The pharmaceutical composition is administered to an entity which has developed a tumor or is in danger of developing a tumor, and thus tumors can be prevented or treated. | 2020-04-30 |
20200131200 | SPIROHEPTANE SALICYLAMIDES AND RELATED COMPOUNDS AS INHIBITORS OF ROCK - The present invention provides compounds of Formula (I): | 2020-04-30 |
20200131201 | TYK2 INHIBITORS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders. | 2020-04-30 |
20200131202 | ORGANIC COMPOUND, AND ORGANIC PHOTOELECTRIC DEVICE, IMAGE SENSOR, AND ELECTRONIC DEVICE INCLUDING THE ORGANIC COMPOUND - An organic compound, an organic photoelectric device, an image sensor, and an electronic device, the organic compound being represented by Chemical Formula 1: | 2020-04-30 |
20200131203 | ALDOSE REDUCTASE INHIBITORS AND USES THEREOF - The present invention relates to boronic acid and boronate ester compounds that are inhibitors of aldose reductase, and to compositions that contain the compounds and methods of using the compounds. | 2020-04-30 |
20200131204 | SILICON-CONTAINING ELECTRON TRANSPORTING MATERIAL AND ITS APPLICATION - A silicon-containing electron transporting material and its application are disclosed. The silicon-containing electron transporting material employs a silicon-containing compound with a novel structure containing one or more silicon atoms and a specific group. The compound can be used as an electron transporting layer of an electroluminescent device, which can effectively improve the lifetime of the device and improve device performance. An electroluminescent device and compound formulation are also disclosed. | 2020-04-30 |
20200131205 | COMPOSITION FOR DEPOSITING SILICON-CONTAINING THIN FILM INCLUDING DISILYLAMINE COMPOUND AND METHOD FOR MANUFACTURING SILICON-CONTAINING THIN FILM USING THE SAME - Provided are a novel disilylamine compound, a method for preparing same, and a composition for depositing a silicon-containing thin film including the same. A disilylamine compound of the present invention has excellent reactivity, is thermally stable, and has high volatility, and thus, is used as a silicon-containing precursor, thereby manufacturing a high-quality silicon-containing thin film. | 2020-04-30 |
20200131206 | PHOSPHORUS-CONTAINING COMPOUND AND PREPARATION AND USE THEREOF - The present invention provides a phosphorus-containing compound characterized by being a compound represented by the following structure: | 2020-04-30 |
20200131207 | OPTICALLY-ACTIVE 2-AMINO-PHOSPHONOALKANE ACID, OPTICALLY-ACTIVE 2-AMINOPHOSPHONOALKANE ACID SALT, AND HYDRATES OF THESE - A novel compound has pharmacological activities comparable to those of Nahlsgen and is storable excellently stably. The compound can be produced by a method according to the present invention for producing an optically active 2-amino-phosphonoalkanoic acid salt. In the method, a starting material DL-2-amino-phosphonoalkanoic acid represented by Formula (1) or a hydrate thereof is reacted with an optically active basic compound other than an optically active lysine, to give a diastereomeric salt mixture including a first salt (including a hydrate salt) between a D-2-amino-phosphonoalkanoic acid represented by Formula (1-1) and the optically active basic compound, and a second salt (including a hydrate salt) between an L-2-amino-phosphonoalkanoic acid represented by Formula (1-2) and the optically active basic compound. The diastereomeric salt mixture is fractionally crystallized to isolate one of the first and second diastereomeric salts. | 2020-04-30 |
20200131208 | TRIPHENYLPHOSPHONIUM-TETHERED TETRACYCLINES FOR USE IN TREATING CANCER - This invention relates to compounds that are useful as cancer therapies. The compounds comprise derivatives of tetracycline antibiotics, e.g. doxycycline, having a phosphonium cation tethered to the tetracycline tetracycle. The invention also relates to methods of using said compounds and to pharmaceutical formulations comprising said compounds. | 2020-04-30 |
20200131209 | NOVEL STING AGONISTS - The present invention provides compounds of Formula I′: | 2020-04-30 |
20200131210 | ALVOCIDIB PRODRUGS HAVING INCREASED BIOAVAILABILITY - Compounds having the following structure (I): | 2020-04-30 |
20200131211 | Salts of Antiviral Phosphonate Analogues and Process for Preparation Thereof - The present invention relates to certain acid salts of (((1-(6-amino-9H-purin-9-yl)propan-2-yloxy)methyl)(phenoxy) phosphoryloxy)methyl pivalate of Formula (I), | 2020-04-30 |
20200131212 | COMPOUND FOR TREATING METABOLIC DISEASES AND PREPARATION METHOD AND USE THEREOF - Provided are a compound for treating metabolic diseases having the structure as shown in formula (I) or formula (II), or a racemate, stereoisomer, geometric isomer, tautomer, solvate, hydrate, metabolite, pharmaceutically acceptable salt or prodrug thereof. The compound is an activator of FXR and/or a TGR5 receptor, and thus has the activity of activating FXR and/or a TGR5 receptor, and can be used in the preparation of drugs for treating chronic liver diseases, metabolic diseases or portal hypertension. | 2020-04-30 |
20200131213 | Remote Heteroaryl Alkenylation With Catalytic Bifunctional Template - We report the design of a catalytic, bifunctional template that binds heterocyclic substrate via reversible coordination instead of covalent linkage, allowing remote site-selective C—H olefination of heterocycles. The two metal centers coordinated to this template play different roles; anchoring substrates to the proximity of catalyst and cleaving the remote C—H bonds respectively. Using this strategy, we demonstrate remote site-selective C—H olefination of heterocyclic substrates which do not have functional group handles for covalently attaching templates. For instance the olefination can be an alkenylation of a 3-phenylpyridine with an acrylate alkyl ester selective for the meta position of the phenyl group with respect to the pyridine, or can be an alkenylation of a quinoline with an acrylate alkyl ester selective for the 5-position of the quinoline. | 2020-04-30 |
20200131214 | CRYSTAL STRUCTURE-MODULATED ZEOLITIC IMIDAZOLATE FRAMEWORK NANOPARTICLES AND METHOD OF PRODUCING THE SAME - The present invention relates to nanoparticles including a crystal structure-controlled zeolitic imidazolate framework (ZIF) and a method of producing the same. Nanoparticles according to the present invention comprise: metal ions; and an organic ligand coupled to the metal ions, wherein the organic ligand includes an imidazolate-based organic ligand and an alkylamine-based organic ligand. | 2020-04-30 |
20200131215 | SIALIC ACID ANALOGS - The present invention provides sialic acid analogs and their compositions useful for the treatment of sialic acid deficiencies. | 2020-04-30 |
20200131216 | CRYSTAL FORM OF SODIUM-GLUCOSE COTRANSPORTER 2 INHIBITOR - The present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof. Specifically, the present invention relates to a crystalline form of a co-crystal of an inhibitor against sodium-glucose cotransporter 2 represented by formula (1), i.e., (2S,3R,4R,5S,6R)-2-(3-(4-(((1R,3s,5S)-bicyclo[3.1.0]hexan-3-yl)oxy)benzyl)-4-chlorophenyl)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol, with L-proline, a method for preparing the same, a pharmaceutical composition comprising the same, and use thereof. | 2020-04-30 |
20200131217 | HEPARAN SULFATE GLYCOMIMETIC COMPOUNDS AND THEIR PHARMACEUTICAL AND COSMECEUTICAL USES - The invention relates to dendritic compounds, the use of these compounds as pharmaceuticals, pharmaceutical and cosmeceutical compositions containing the compounds, and methods of treating cancer, inflammation, diabetic nephropathy, neurodegenerative disorders, Niemann-Pick Type C disease, or dermatological conditions. | 2020-04-30 |
20200131218 | MITHRAMYCIN OXIME AND HYDRAZINE DERIVATIVES HAVING INCREASED SELECTIVITY AND ANTI-CANCER ACTIVITY - Compounds described herein are mithramycin (MTM) oxide (OX) derivatives and MTM Hydrazine (HY) derivatives. These compounds are useful for treatment of cancers and neuro-diseases. | 2020-04-30 |
20200131219 | Novel uses of a saponin and method for its isolation - The present invention relates to the novel use of saponins having acetyl residues on one of their sugar residues. These saponins are able to enhance the transfection efficiency to a surprisingly much higher extent than already known saponins and even than Lipofectamin. | 2020-04-30 |
20200131220 | CYPHOMYCIN, COMPOSITIONS AND USES THEREOF - Cyphomycin, an isolated compound of Formula I or IA is provided. A compound isolated from insect | 2020-04-30 |
20200131221 | METHOD FOR EXTRACTING PHYTOSTEROLS FROM TALL OIL PITCH - The invention relates to the wood chemical industry and concerns a method for extracting phytosterols from tall oil pitch. The present method of extracting phytosterols from tall oil pitch involves saponifying tall oil pitch using an alkali in a polyatomic alcohol, extracting unsaponified matter from the alkali-alcohol solution using a hydrocarbon solvent, subsequently removing the solvent by distillation, and concentrating the phytosterols, wherein a mixture of paraffin hydrocarbons is used as said hydrocarbon solvent, and, following extraction from the extraction solution, betulin is isolated by crystallization and the phytosterols are then concentrated by means of rectification. This method makes it possible to increase the rate of extraction of phytosterols from saponified tall oil pitch to up to 95% and allows an end product to be produced that has a phytosterol content of at least 65% with unwanted betulin impurities at no more than 0.3%. | 2020-04-30 |
20200131222 | COMPOSITION FOR ENHANCING EXERCISE ABILITY OR ANTI-FATIGUE COMPRISING NOVEL GINSENOSIDE - The present specification relates to a composition containing novel (20S,24R)-6-O-β-D-glucopyranosyl(1->2)-β-D-glucopyranoside-dammar-3-one-20,24-epoxy-6a,12b,25-triol, a pharmaceutically acceptable salt thereof, a hydrate or a solvate thereof as an active ingredient. The composition exhibits an excellent exercise ability enhancing effect and anti-fatigue effect. | 2020-04-30 |
20200131223 | COMPOUND FOR TREATING CLOSTRIDIUM DIFFICILE - The invention relates to compounds, compositions and polymers comprising a first component adapted to promote germination of | 2020-04-30 |
20200131224 | Methods for Synthesis of Radionuclide Complex - The present disclosure relates to the synthesis of radionuclide complex solutions, in particular for their use in the commercial production of radioactive drug substances, for diagnostic and/or therapeutic purposes. In particular, the synthesis method comprises the following steps in the following order:
| 2020-04-30 |
20200131225 | METHODS OF PURIFICATION OF ALBUMIN FUSION PROTEINS - The present invention provides a chromatographic separation method for improving the quality of albumin fusion protein solutions by removing impurities from the albumin fusion protein solution. This invention provides albumin fusion protein solution with a significantly reduced amount of the (yellow) coloured impurities and HCP. | 2020-04-30 |
20200131226 | SYSTEM AND METHOD FOR PRODUCING INTERLEUKIN RECEPTOR ANTAGONIST (IRA) - A system and method for producing high levels of autologous IL- | 2020-04-30 |
20200131227 | POLYPEPTIDE WITH TUMOUR BINDING ACTIVITY - The present invention relates to a polypeptide with tumor binding activity, and its use in the treatment and diagnosis of cancer. | 2020-04-30 |
20200131228 | BICYCLIC PEPTIDE LIGANDS AND USES THEREOF - The present invention provides compounds, compositions thereof, and methods of using the same. | 2020-04-30 |
20200131229 | Method for Promoting Bacillus subtilis to Synthesize Surfactin based on Multi-gene Synergy - The present invention discloses a method for promoting | 2020-04-30 |
20200131230 | THROMBOSPONDIN 1-BINDING PEPTIDE - Provided is a compound that can promote angiogenesis by inhibiting the function of TSP1, and is useful for the treatment or prophylaxis of diseases such as critical limb ischemia. | 2020-04-30 |