19th week of 2019 patent applcation highlights part 28 |
Patent application number | Title | Published |
20190135727 | Continuous method for producing muconic acid from aldaric acid - According to an example aspect of the present invention, there is provided a continuous method of producing muconic acid from aldaric acid in the presence of a solid heterogeneous catalyst and an alcohol solvent with short reaction time. Another aspect of the present invention is the use of a non-expensive solid heterogenous catalyst, which is automatically separated from the product. | 2019-05-09 |
20190135728 | Method for Purifying an Aqueous Lactic Acid Solution - The present invention concerns a method for purifying an aqueous lactic acid solution, obtained from a fermentation medium or from any other source previously cleared of solid substances and/or of biomass that may be present and ionic substances, characterised in that it comprises the two following steps: a. Concentration of the lactic acid solution until a concentration of between 85 and 95% is reached, preferably of between 90 and 95%, i.e. between 15 and 5% free water or preferably between 10 and 5% free water; b. Distillation in a multi-stage column comprising three areas and allowing the separation, in a single step, of the lactic acid, volatile compounds and the heaviest impurities. | 2019-05-09 |
20190135729 | PRODUCTION OF SALTS OF 4-HYDROXYBUTYRATE USING BIOBASED RAW MATERIALS - Gamma-butyrolactone (“GBL”) and Gamma-hydroxybutyrate (“GHB”) having a unique carbon footprint as defined by the percent modern carbon (pmc) are described herein. The percent modern carbon can be controlled by varying the amounts of biobased, renewable starting materials and petroleum-based starting materials to prepare GBL or GHB having a defined pmc or by preparing mixtures of GBL or GHB prepared from biobased renewable starting materials and GBL or GHB prepared from petroleum-based starting materials. | 2019-05-09 |
20190135730 | COMPOUND FOR ORGANIC ELECTRIC ELEMENT, ORGANIC ELECTRIC ELEMENT USING SAME, AND ELECTRONIC DEVICE COMPRISING SAME ORGANIC ELECTRONIC ELEMENT - Provided are an organic electric element and an electronic device comprising the same. According to the present invention, the organic electric element uses a mixture of compounds as a phosphorescent host material which can achieve a high light-emitting efficiency and a low driving voltage and can greatly improve a lifespan in an organic electric element. | 2019-05-09 |
20190135731 | N,N-DIMETHYLAMINOETHYL ACRYLATE COMPOSITION STABILIZED IN RESPECT OF DISCOLORING EFFECTS - The invention relates to the use of 2,6,-di-tert-butyl-4-methylphenol at a moiety of 25 to 200 ppm for stabilizing N,N-dimethylaminoethyl acrylate in respect of discoloring effects. The invention also relates to an N,N-dimethylaminoethyl acrylate stabilized in said manner and to a method for producing the same. | 2019-05-09 |
20190135732 | CRYSTAL FORMS AND METHODS OF SYNTHESIS OF (2R, 6R)-HYDROXYNORKETAMINE AND (2S, 6S)-HYDROXYNORKETAMINE - The disclosure provides a method for synthesizing free base forms of (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine. In an embodiment synthesis of (2R,6R)-hydroxynorketamine (HNK) includes preparation of (R)-norketamine via chiral resolution from racemic norketamine via a chiral resolution with L-pyroglutamic acid. The disclosure also provided crystal forms of the corresponding (2R,6R)-hydroxynorketamine (HNK) and (2S,6S)-hydroxynorketamine hydrochloride salts. | 2019-05-09 |
20190135733 | CASPASE INHIBITOR AND PHARMACEUTICAL COMPOSITION, USE AND THERAPEUTIC METHOD THEREOF - Disclosed are a class of compounds as a caspase inhibitor, and in particular the compound as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the use of the compound in treating caspase-related diseases. | 2019-05-09 |
20190135734 | METHOD FOR PRODUCING SURFACTANTS - The present invention relates to a method in which an amino acid is reacted with an acyl group donor to obtain an N-acylamino acid in the presence of an amine. | 2019-05-09 |
20190135735 | METHOD FOR PRODUCING N-(ALPHA-ALKOXYETHYL)FORMAMIDE - Provided are a method for producing N-(α-alkoxyethyl)formamide, comprising adding an acid catalyst to the mixed liquid within 3 hours from start of mixing after mixing of N-(α-hydroxyethyl)formamide with an alcohol has been started, by which the N-(α-alkoxyethyl)formamide can be produced at a high yield without additional investment in plant and equipment while suppressing an increase in the temperature of the mixed liquid and preventing corrosion of a pipe; and a method for producing N-(α-alkoxyethyl)formamide, comprising degassing carbon dioxide in the reaction of N-(α-hydroxyethyl)formamide with an alcohol, by which the N-(α-alkoxyethyl)formamide having a decreased carbonate concentration can be produced. | 2019-05-09 |
20190135736 | PROCESS FOR REDUCING CPI IN A DINITRILE STREAM - Disclosed is a process for removing 2-cyanocyclopentylideneimine (CPI) from a mixture containing CPI and dinitrile. The process comprises reacting CPI with an amine. The reaction may take place in the presence of water, and optionally, a catalyst. CPI is converted to products with a low volatility compared to the dinitrile. | 2019-05-09 |
20190135737 | METHOD FOR PRODUCING XYLYLENE DIISOCYANATE (XDI) - Disclosed is to a method for producing xylylene diisocyanate (XDI), in particular meta-xylylene diisocyanate (mXDI), including the following steps: a) phosgenation of xylylene-diamine (XDA), in particular m-xylylene-diamine (mXDA) in the case of mXDI; b) eliminating the hydrochloric acid from the reaction medium obtained in step (a) at a temperature of between 120 and 190° C. and a pressure of between 1 mbar and 20 bar. | 2019-05-09 |
20190135738 | TUNABLE NITRIC OXIDE-RELEASING MACROMOLECULES HAVING MULTIPLE NITRIC OXIDE DONOR STRUCTURES - Provided here are nitric oxide-releasing compounds that include at least two different NO donor functional groups of the same class. In some embodiments, such nitric oxide-releasing compounds are macromolecules such as dendrimer and co-condensed silica. Pharmaceutical compositions, wound dressings, kits and methods of treatments are also provided herein. | 2019-05-09 |
20190135739 | PROCESS FOR PRODUCING TAURINE - There is disclosed a process for producing taurine by reacting 2-oxazolidinone with ammonium sulfite, or ammonium bisulfite, or a mixture of ammonium sulfite and ammonium bisulfite in an aqueous solution to form ammonium taurinate and ammonium bicarbonate. Taurine is obtained by decomposing ammonium taurinate to taurine and ammonia and recovered by solid-liquid separation. | 2019-05-09 |
20190135740 | SYNTHESIS OF 2,2,2-TRIFLUOROETHANETHIOL - A method of making CF | 2019-05-09 |
20190135741 | Methods of Making Deuterium-Enriched N-acetylcysteine Amide (D-NACA) and (2R, 2R')-3,3'-Disulfanediyl BIS(2-Acetamidopropanamide) (DINACA) and Using D-NACA and DINACA to Treat Diseases Involving Oxidative Stress - The present invention includes pharmaceutical composition comprising (2R,2R′)-3,3′-disulfanediyl bis(2-acetamidopropanamide)(diNACA) or D | 2019-05-09 |
20190135742 | PLEUROMUTILIN DERIVATIVE HAVING 2-AMINO PHENYL MERCAPTAN SIDE CHAIN AS WELL AS PREPARATION METHOD AND APPLICATION THEREOF - A pleuromutilin derivative having a 2-amino phenyl mercaptan side chain as well as a preparation method and application thereof are provided. The derivative has a structure represented by formula 2 or formula 3, wherein, R1, R2 and R3 are each independently selected from a hydrogen atom, hydroxyl, amino, sulfydryl, hydroxymethyl, amine methyl, nitro, halogen, trihalogenated methyl, methyl, natural amino acid acylamino and C1-6 alkoxy. The plueuromutilin derivative in the disclosure has good activity of inhibiting drug-resistant | 2019-05-09 |
20190135743 | NOVEL PROSTAGLANDIN DERIVATIVE - The present invention relates to a novel prostaglandin derivative having an alkynyl group on ω-chain, particularly, a novel prostaglandin derivative having a double bond at the 2-position and an alkynyl group on the ω-chain and a medicament containing the compound as an active ingredient. | 2019-05-09 |
20190135744 | IDENTIFYING PATIENT RESPONSE TO S1P RECEPTOR MODULATOR ADMINISTRATION - The invention provides a method of assessing the appropriate therapeutic dose of 1-{4-[1-(4-cyclohexyl-3-trifluoromethyl-benzyloxyimino)-ethyl]-2-ethyl-benzyl}-azetidine-3-carboxylic acid to administer to a patient in need thereof, comprising the steps of:
| 2019-05-09 |
20190135745 | IMMUNOMODULATOR COMPOUNDS - Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I): | 2019-05-09 |
20190135746 | INDOLINE DERIVATIVES AND METHOD FOR USING AND PRODUCING THE SAME - The present invention relates to a compound of the formula: where n, R and R are those defined herein. The present invention also relates to use of a compound of Formula 1 in treating a clinical condition associated with fibrotic disorder. | 2019-05-09 |
20190135747 | INDOLE AND INDAZOLE CYANOCINNAMATE COMPOUNDS AND THERAPEUTIC USES THEREOF - Disclosed are Indole and Indazole cyanocinnamate compounds, method for preparing these compounds, and methods for treating cancer. | 2019-05-09 |
20190135748 | METHODS OF MANUFACTURE OF 2-ARYL-3,3-BIS(4-HYDROXYARYL)PHTHALIMIDINES, AND POLYMERS DERIVED THEREFROM - A method for the manufacture of a 2-aryl-3,3-bis(hydroxyaryl)phthalimidine including heating a reaction mixture comprising a phenolphthalein compound and a primary arylamine in the presence of an acid catalyst, and a heterocyclic aromatic amine co-catalyst, to form the 2-aryl-3,3-bis(hydroxyaryl) is provided. Polymers including structural units derived from the 2-aryl-3,3-bis(hydroxyaryl)phthalimidine are provided. Methods for the manufacture of a polycarbonate, including manufacturing the 2-aryl-3,3-bis(hydroxyaryl)phthalimidine, and polymerizing the 2-aryl-3,3-bis(hydroxyaryl)phthalimidine in the presence of a carbonate source are provided. | 2019-05-09 |
20190135749 | Production of Cyclic Imides Suitable for Oxidation Catalysis - Disclosed are novel processes for the production of cyclic imide compounds such as N-hydroxyphthalimide (NHPI). The processes may be particularly well-suited for commercial-scale production of cyclic imides such as NHPI. Such cyclic imide compounds are suitable for use as oxidation catalysts, and specifically may be used to oxidize cyclohexylbenzene to cyclohexyl-1-phenyl-1-hydroperoxide. Such an oxidation may be particularly useful in a process for the production of phenol and/or cyclohexanone from benzene via a process comprising hydroalkylation of benzene to cyclohexylbenzene, oxidation of the cyclohexylbenzene to cyclohexyl-1-phenyl-1-hydroperoxide, and cleavage of the cyclohexyl-1-phenyl-1-hydroperoxide to phenol and cyclohexanone. The cyclic imide production process may advantageously include water washing and reactant recovery steps to maximize purity and yield. | 2019-05-09 |
20190135750 | METHODS AND SYSTEMS FOR THE MANUFACTURE OF AN AROMATIC PHTHALIC BISIMIDE AND A POLYETHERIMIDE - A method for producing an aromatic bisimide includes reacting a dialkali metal salt of a dihydroxy aromatic compound with a reactive substituted phthalimide under conditions effective to form a product mixture, introducing the product mixture to a liquid-liquid extraction column including an aqueous alkali metal hydroxide solution, and recovering from the liquid-liquid extraction column a purified aromatic bisimide having less than 500 ppm of residual dialkali metal salt of the dihydroxy aromatic compound, the corresponding dihydroxy aromatic compound, the corresponding mono-substituted salt of the dihydroxy aromatic compound, or a combination including at least one of the foregoing. A method for the manufacture of a polyetherimide from an aromatic bisimide prepared by the above method is also disclosed. A polyetherimide having less than 100 ppb of residual bisphenol A and an article made therefrom are also described. | 2019-05-09 |
20190135751 | SMALL MOLECULE N-(ALPHA-PEROXY) CARBAZOLE COMPOUNDS AND METHODS OF USE - The invention relates to novel N-(α-peroxy)carbazole compounds of Formula I and methods for use. (I) The N-(α-peroxy)carbazole compounds described herein are useful for treating or preventing parasitic infections, bacterial infections, and cancer in subjects. The methods include administering an N-(α-peroxy)carbazole compound as described herein to a subject. Also described herein are methods for synthesizing N-(α-peroxy)carbazole compounds. | 2019-05-09 |
20190135752 | SUBSTITUTED (1,2,3,4-TETRAHYDROCYCLOPENTA[b]INDOL-3-YL)ACETIC ACID DERIVATIVES USEFUL IN THE TREATMENT OF AUTOIMMUNE AND INFLAMMATORY DISORDERS - The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. | 2019-05-09 |
20190135753 | PIPERIDINYL DERIVATIVES - Compounds of the formula I | 2019-05-09 |
20190135754 | METHODS FOR ENANTIOSELECTIVE ALLYLIC ALKYLATION OF ESTERS, LACTONES, AND LACTAMS WITH UNACTIVATED ALLYLIC ALCOHOLS - The present disclosure provides methods for enantioselective synthesis of cyclic and acyclic α-quaternary carboxylic acid derivatives via nickel-catalyzed allylic alkylation. | 2019-05-09 |
20190135755 | CRYSTAL POLYMORPHISM OF KCNQ2-5 CHANNEL ACTIVATOR - Crystal polymorphism may exist in a crystalline compound. In the case where crystal polymorphism exists, depending on the crystal form, solubility, dissolution rate, stability against heat, light, humidity, etc. or the like is different. Accordingly, in the production of a pharmaceutical product, it is a very important task to select a crystal form of a drug substance most suitable for a disease indication and a dosage form. The present invention relates to novel crystal forms (A crystal, W crystal, and a hydrate crystal (H crystal)) of a compound I having a strong opening action with respect to KCNQ2-5 channels. | 2019-05-09 |
20190135756 | 3,4-DI-SUBSTITUTED PYRIDINE COMPOUND, METHODS OF USING AND COMPOSITIONS COMPRISING THE SAME - 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is useful in the modulation of blood or serum uric acid levels. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used in the treatment or prevention of disorders related to aberrant levels of uric acid. In some embodiments, 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid is used for reducing serum uric acid levels in a human. Also described herein are compositions comprising 2-((3-(4-cyanonaphthalen-1-yl)pyridin-4-yl)thio)-2-methylpropanoic acid, and their use in the modulation of blood or serum uric acid levels. | 2019-05-09 |
20190135757 | ACETYL-COA CARBOXYLASE MODULATORS - Provided herein are compounds that exhibit activity as acetyl-CoA carboxylase modulators (e.g., inhibitors) and are useful, for example, in methods for the control of fungal pathogens in plants. | 2019-05-09 |
20190135758 | INHIBITORS OF INDOLEAMINE 2,3-DIOXYGENASE AND METHODS OF THEIR USE - There are disclosed compounds that modulate or inhibit the enzymatic activity of indoleamine 2,3-dioxygenase (IDO), pharmaceutical compositions containing said compounds and methods of treating proliferative disorders, such as cancer, viral infections and/or inflammatory disorders utilizing the compounds of the invention. | 2019-05-09 |
20190135759 | METHOD OF TREATING PAIN - The instant application discloses methods of treating, reducing, or preventing pain in a mammal, which may include administering a compound capable of modulating a transient receptor potential channel. In one aspect, the TRP channel may be TRPC4. Types of pain contemplated by the present disclosure include acute, chronic, neuropathic, and nociceptive pain. | 2019-05-09 |
20190135761 | COMPOSITION COMPRISING 3-(HALOALKYL OR FORMYL)-1H-PYRAZOLE-4-CARBOXYLIC ACIDS OR ESTERS, ITS MANUFACTURE AND ITS USE FOR THE PREPARATION OF CARBOXAMIDES - The present invention concerns compositions comprising (i) a 3-(haloalkyl or formyl)-1H-pyrazole wherein R | 2019-05-09 |
20190135762 | COMPOUNDS USEFUL AS KINASE INHIBITORS - This invention relates to novel compounds. The compounds of the invention are tyrosine kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Bruton's tyrosine kinase (BTK). The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Bruton's tyrosine kinase, for example cancer, lymphoma, leukemia and immunological diseases. | 2019-05-09 |
20190135763 | PYRIDYL ANALOGS OF 1-(2-CYANO-3,12-DIOXOOLEANA-1,9(11)DIEN-28-OYL) IMIDAZOLE - Pyridyl analogs of 1-(2-cyano-3,12-dioxooleana-1,9(11)-dien-28-oyl) imidazole and pharmaceutical compositions containing the same are provided. | 2019-05-09 |
20190135764 | UREA COMPOUNDS AND THEIR USE AS ENZYME INHIBITORS - A compound having the following structure: | 2019-05-09 |
20190135765 | NOVEL PYRIMIDINE-4-CARBOXYLIC ACID DERIVATIVE HAVING ANTICANCER ACTIVITY - The present invention relates to a novel pyrimidine-4-carboxylic acid derivative having an anticancer activity, and the compound of the present invention is useful as a drug for treating and preventing tumor diseases. | 2019-05-09 |
20190135766 | METHOD OF SYNTHESIZING PROTHIOCONAZOLE AND OPTICALLY ACTIVE ISOMERS THEREOF AND INTERMEDIATES - Disclosed are a method of synthesizing prothioconazole and optically active isomers thereof and intermediates. The method includes reacting hydrazine with glyoxylic acid to produce a hydrazono acetic acid as an intermediate, and then reacting the intermediate with thiocyanate to produce the target product prothioconazole. The present method is very specific in terms of regioselectivity, resulting in minimum byproducts and a high product yield. The present method does not require special equipment, nor anhydrous or oxygen-free manipulations. The process is simple and generates minimum wastes, suitable for industrial production. | 2019-05-09 |
20190135767 | Heterocyclic Compounds Useful In The Treatment Of Disease - A method for treating a lysophosphatidic acid-dependent disease or condition in a subject in need thereof is provided. The method includes administering to the subject a therapeutically effective amount of a heterocyclic compound. The heterocyclic compound is a lysophosphatidic acid receptor ligand. Lysophosphatidic acid-dependent diseases and conditions include diseases involving fibrosis, such as fibrosis of the heart, kidney, liver and lung, and scleroderma; inflammatory diseases such as diabetic nephropathy and inflammatory bowel disease; ocular diseases such as diseases involving retinal degeneration; nerve diseases such as pruritus and pain. | 2019-05-09 |
20190135768 | ARYL DIHYDRO-2H-BENZO[B][1,4]OXAZINE SULFONAMIDE AND RELATED COMPOUNDS FOR USE AS AGONISTS OF RORY AND THE TREATMENT OF DISEASE - The invention provides aryl dihydro-2H-benzo[b] [1,4]oxazine sulfonamide and related compounds, pharmaceutical compositions, methods of promoting RORy activity, methods of increasing the amount of IL-17 in a subject, and methods of treating cancer and other medical disorders using such compounds. | 2019-05-09 |
20190135769 | COMPOUNDS AS DNA PROBES, METHODS AND APPLICATIONS THEREOF - The present disclosure relates to the field of pharmaceutical chemistry and biotechnology. The present disclosure also relates to a compound of Formula I and a process of preparation thereof. The disclosure furthermore relates to methods/use of Formula I compounds as DNA probes. Said Formula I compounds are employed for recognizing specific DNA sequences by near Infra-red (NIR)-Fluorescence Switch-on mechanism, and have related applications including but not limited to cell imaging. Also, method of treating parasitic infections by employing the present compound of Formula I is provided. | 2019-05-09 |
20190135770 | HETEROCYCLIC DERIVATIVES FOR THE TREATMENT OF RSV - Disclosed herein are compounds and compositions for treating or inhibiting RSV and related members of the pneumovirus and paramyxovirus families such as human metapneumovirus, mumps virus, human parainfluenzaviruses, and Nipah and hendra virus, and methods of treatment or prevention thereof. | 2019-05-09 |
20190135771 | FLUOROCHEMICAL PIPERAZINE CARBOXAMIDES - The present invention provides a novel partially fluorinated piperazine carboxamide compound, and polymer composition comprising the fluorinated compound and a thermoplastic or thermoset polymer. The polymer composition is useful in preparing shaped articles such as fibers and films which have desirable oil- and water repellency properties. | 2019-05-09 |
20190135772 | MODULATORS OF THE INTEGRATED STRESS PATHWAY - Provided herein are compounds, compositions, and methods useful for modulating the integrated stress response (ISR) and for treating related diseases; disorders and conditions. | 2019-05-09 |
20190135773 | NOVEL COMPOSITIONS AND METHODS FOR CANCER TREATMENT - The present invention relates to the composition and methods of use of Stat3 pathway inhibitors or cancer stem cell inhibitors in combination treatment of cancer. | 2019-05-09 |
20190135774 | BIOMOLECULE PROCESSING FROM FIXED BIOLOGICAL SAMPLES - Molecular characterization of disease has become the dominant trend in modern medicine, and it has recently become increasingly important to obtain qPCR, microarray, and next-generation sequencing (NGS) data for both research and clinical applications. Formalin-fixed, paraffin-embedded (“FFPE”) samples have become the standard way of storing clinical biopsies throughout the world. Unfortunately, the poor quality and quantity of nucleic acids obtained from such specimens has posed severe limitations on the types of studies that can be accomplished. Existing methods for retrieval of the biomolecules from their crosslinked matrices are poorly effective and rely on harsh conditions which further damage the biomolecules being extracted. The invention provides compositions and methods for retrieval, analysis and use of biomolecules, including nucleic acids, from such samples. | 2019-05-09 |
20190135775 | PROCESSES FOR THE PREPARATION OF A DIARYLTHIOHYDANTOIN COMPOUND - Disclosed are processes and intermediates for the preparation of compound (X), which is currently being investigated for the treatment of prostate cancer. | 2019-05-09 |
20190135776 | THERAPEUTICS TARGETING TRUNCATED ADENOMATOUS POLYPOSIS COLI (APC) PROTEINS - The described invention provides small molecule anti-cancer compounds that selectively target and inhibit measurable biological activity of truncated APC proteins, an immortalized Human Colonic Epithelial Cell (HCEC) model, and pharmaceutical compositions comprising at least one of the small molecule anti-cancer compounds and a pharmaceutically acceptable carrier. | 2019-05-09 |
20190135777 | QUINOLINE COMPOUNDS SUITABLE FOR TREATING DISORDERS THAT RESPOND TO THE MODULATION OF THE SEROTONIN 5-HT6 RECEPTOR - The present invention relates to quinoline compounds of formula I | 2019-05-09 |
20190135778 | THERAPEUTICALLY ACTIVE BICYCLIC-SULPHONAMIDES AND PHARMACEUTICAL COMPOSITIONS - Pharmaceutical compounds have a bicyclic-sulphonamide structure and pharmaceutical compositions including the compounds may be used in therapy as brain-cell-death protectants and may be used, for example, in the treatment of chronic neurodegenerative diseases. The compounds are active as inhibitors of N-acylethanolamine-hydrolysing acid amidase (NAAA) and may be used for the therapeutic treatment and prevention of pain and inflammatory disorders and other disorders which benefit from the modulation of fatty acid ethanolamides, particularly palmitoylethanolamide (PEA). | 2019-05-09 |
20190135779 | CRYSTALS OF QUINAZOLINE DERIVATIVE AND PREPARATION METHOD THEREFOR - The invention relates to Crystal form I and Crystal form II of dihydrochloride of N-(4-((3-chloro-4-fluorophenyl)amino)-7-((7-methyl-7-azaspiro[3.5]nonan-2-yl)methoxy)quinazoli n-6-yl)acrylamide represented by the following Formula (I), and preparation methods therefor, wherein the Crystal form I has an X-ray powder diffraction pattern having characteristic peaks at the 2θ positions of 6.0±0.2°, 7.3±0.2°, 11.7±0.2°, 12.9±0.2°, 18.4±0.2°, 24.7±0.2°, and 26.3±0.2°, as determined by using Cu-Kα radiation, and the Crystal form II has an X-ray powder diffraction pattern having characteristic peaks at the 2θ positions of 5.0±0.2°, 7.0±0.2°, 10.1±0.2°, 17.0±0.2°, 26.0±0.2°, and 26.5±0.2°, as determined by using Cu-Kα radiation. | 2019-05-09 |
20190135780 | ARYLMETHOXY ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - Provided are 4′-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 2019-05-09 |
20190135781 | PYRIDINYL QUINOLINONE DERIVATIVES AS MUTANT-ISOCITRATE DEHYDROGENASE INHIBITORS - The invention relates to methods of reducing the level of | 2019-05-09 |
20190135782 | COMPOUNDS, COMPOSITIONS, AND METHODS FOR MODULATING FERROPTOSIS AND TREATING EXCITOTOXIC DISORDERS - The present invention provides, inter alia, a compound having the structure: | 2019-05-09 |
20190135783 | SMALL MOLECULE INHIBITORS OF SHARED EPITOPE-CALRETICULIN INTERACTIONS AND METHODS OF USE - This invention is in the field of medicinal chemistry. In particular, the invention relates to a new class of small-molecules having a triazole-methyl-piperidinyl-pyrolyl-propenone structure which function as modulators of shared epitope (SE)—calreticulin (CRT) binding and/or interaction, and their use as therapeutics for the treatment of immunoregulatory abnormalities (e.g., autoimmune diseases, inflammatory diseases (e.g., chronic inflammatory disease), and bone erosive diseases) by selectively inhibiting SE-CRT interactions and/or signal transduction pathways commonly overactive or dysregulated in arthritic and/or other diseases or conditions. | 2019-05-09 |
20190135784 | ANTIPROLIFERATIVE PYRIMIDINE-BASED COMPOUNDS - This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers. | 2019-05-09 |
20190135785 | QUINOLINE DERIVATIVE - A compound represented by general formula (I) has a strong Axl inhibitory activity by introducing a distinctive bicyclic structure in which a saturated carbon ring is fused to a pyridone ring, and can be a therapeutic agent for Axl-related diseases, for example, cancer such as acute myeloid leukemia, melanoma, breast cancer, pancreatic cancer, and glioma, kidney diseases, immune system diseases, and circulatory system diseases | 2019-05-09 |
20190135786 | HETEROCYCLIC COMPOUND AND PHARMACEUTICAL COMPOSITION COMPRISING SAME - The present invention relates to a novel heterocyclic compound inhibiting a cyclin-dependent kinase (CDK) and a pharmaceutical composition comprising the same as an effective ingredient. The heterocyclic compound according to the present invention or pharmaceutically acceptable salt thereof can be effectively used in treating or preventing cancers, degenerative brain diseases, etc. | 2019-05-09 |
20190135787 | PYRIMIDINE COMPOSITIONS, ULTRA-PURE COMPOSITIONS AND SALTS THEREOF, METHODS OF MAKING THE SAME, AND METHODS OF USING THE SAME FOR TREATING HISTAMINE H4 RECEPTOR (H4) MEDIATED DISEASES AND CONDITIONS - The present application relates to ultra-pure compositions containing N | 2019-05-09 |
20190135788 | DIHYDROPYRIMIDINYL BENZAZEPINE CARBOXAMIDE COMPOUNDS - This invention relates to new benzazepine carboxamide compounds of the formula | 2019-05-09 |
20190135789 | INHIBITING ATAXIA TELANGIECTASIA AND RAD3-RELATED PROTEIN (ATR) - Novel compounds inhibiting ATR protein kinase include compounds of formula (I) disclosed herein, as well as liposome formulations comprising ATR protein kinase inhibitor compounds. The compositions are useful for the treatment of cancer. | 2019-05-09 |
20190135790 | DIAMINOPYRIMIDINE BENZENESULFONE DERIVATIVES AND USES THEREOF - The present invention provides compounds of Formula (II) (e.g., compounds of Formula (I)), and pharmaceutically compositions thereof. Compounds of Formula (II) are believed to be binders of bromodomains and/or bromodomain-containing proteins (e.g., bromo and extra terminal (BET) proteins). Also provided are methods, uses, and kits using the compounds and pharmaceutical compositions for inhibiting the activity (e.g., increased activity) of bromodomains and/or bromodomain-containing proteins and for treating and/or preventing in a subject diseases associated with bromodomains or bromodomain-containing proteins (e.g., proliferative diseases, cardiovascular diseases, viral infections, fibrotic diseases, metabolic diseases, endocrine diseases, and radiation poisoning). The compounds, pharmaceutical compositions, and kits are also useful for male contraception. | 2019-05-09 |
20190135791 | SUBSTITUTED 1,2,3-TRIAZOLES AS NR2B-SELECTIVE NMDA MODULATORS - Substituted 1,2,3-triazoles as NR2B receptor ligands. Such compounds may be used in NR2B receptor modulation and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by NR2B receptor activity. | 2019-05-09 |
20190135792 | CRYSTALLINE FORM OF COMPOUND SUPPRESSING PROTEIN KINASE ACTIVITY, AND APPLICATION THEREOF - Provided are a compound as represented by structural formula (I) ({5 -[(1R)-1-(2,6-dichloro-3-fluorophenyl)ethoxy]-6-aminopyridazin-3-yl}-N-{4-[((3S,5R)-3,5-di methylpiperazinyl)carbonyl]phenyl}carboxamide hydrochloride) and a novel crystalline form of a hydrate or solvate of the compound. Further provided are a manufacturing method of the compound and crystalline form, a related intermediate, a pharmaceutical composition comprising the compound, an application using the compound or the crystalline form for preparing a pharmaceutical product for treating a disease, symptom, or disorder, and a therapeutic method for treating a disease, symptom, or disorder. | 2019-05-09 |
20190135793 | HETEROCYCLIC INHIBITORS OF KDM5 FOR THE TREATMENT OF DISEASE - The present invention relates to compounds and methods useful as inhibitors of KDM5 for the treatment or prevention of cancer. | 2019-05-09 |
20190135794 | BENZIMIDAZOLE-LINKED INDOLE COMPOUND ACTING AS NOVEL DIVALENT IAP ANTAGONIST - The present invention discloses a benzimidazole-linked indole compound acting as novel divalent IAP antagonist, specifically disclosing the compound shown in formulas (I) or a pharmaceutically acceptable salt thereof. | 2019-05-09 |
20190135795 | MONOGLYCIDYL ISOCYANURATE COMPOUND AND PRODUCTION METHOD THEREFOR - There are provided a novel isocyanurate compound having a glycidyl group as a substituent to be bonded to a nitrogen atom. A monoglycidyl isocyanurate compound of the following Formula (1), (2), or (3). | 2019-05-09 |
20190135796 | EZH2 INHIBITORS AND USES THEREOF - The present disclosure provides compounds of any one of Formulae (I), (II), and (III). The compounds described herein are inhibitors of histone methyltransferases (e.g., enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2)) and are useful in treating and/or preventing a broad range of diseases (e.g., proliferative diseases). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein. | 2019-05-09 |
20190135797 | COMPOUND AND ORGANIC LIGHT-EMITTING DISPLAY DEVICE - The present disclosure provides a compound having property of thermally activated delayed fluorescence (TADF) and a display device. The compound has a structure represented by Formula (I), in which X is S, O, Se, or C; D is an electron donor, A is an electron acceptor; m is a number of the electron donor D, and the m electron donors D are the same or different; n is a number of the electron acceptor, and the n electron acceptors are the same or different, m and n are integers each independently selected from 1, 2, 3, 4 or 5, and m+n≤6. The above compound provides a high luminescence efficiency. The organic light-emitting display device has advantages of improved luminescence efficiency, lower cost and long service life by using the above compound as a light-emitting material, a host material, or a guest material. | 2019-05-09 |
20190135798 | Substituted Oxadiazoles for Combating Phytopathogenic Fungi - The present invention relates to novel oxadiazoles of the formula I, or the N-oxides and/or their agriculturally useful salts and to their use for controlling phytopathogenic fungi, or to a method for combating phytopathogenic harmful fungi, which process comprises treating the fungi or the materials, plants, the soil or seeds to be protected against fungal attack, with an effective amount of at least one compound of the formula I, or an N-oxide, or an agriculturally acceptable salt thereof; the present invention also relates to mixtures comprising at least one such compound of the formula I and at least one further pesticidally active substance selected from the group consisting of herbicides, safeners, fungicides, insecticides, and plant growth regulators; and to agrochemical compositions comprising at least one such compound of the formula I and to agrochemical compositions further comprising seeds. | 2019-05-09 |
20190135799 | HETEROCYCLIC COMPOUND - The present invention provides a heterocyclic compound having a HDAC inhibitory action, and useful for the treatment of central nervous system diseases including neurodegenerative disease, and the like, and a medicament comprising the compound. | 2019-05-09 |
20190135800 | HALO-SUBSTITUTED PIPERIDINES AS OREXIN RECEPTOR MODULATORS - The present application relates to certain halo-substituted piperidine compounds, pharmaceutical compositions containing them, and methods of using them, including methods for treating substance addiction, panic disorder, anxiety, post-traumatic stress disorder, pain, depression, seasonal affective disorder, an eating disorder, or hypertension. | 2019-05-09 |
20190135801 | COMPOUNDS THAT INDUCE DEGRADATION OF ANTI-APOPTOTIC BCL-2 FAMILY PROTEINS AND THE USES THEREOF - The present disclosure provides compositions and methods for selectively killing senescent cells, wherein the composition comprises a compound of Formula (I) or a compound of Formula (II). The selective killing of senescent cells may delay aging and/or treat age-related disorders. | 2019-05-09 |
20190135802 | MODULATION OF N-ACYLETHANOLAMINE-HYDROLYSING ACID AMIDASE (NAAA) FOR DISEASE TREATMENT - Pharmaceutical compositions make up a compound acting as inhibitor of N-acylethanolamine-hydrolysing acid amidase (NAAA), may be used for the therapeutical treatment and prevention of pain and inflammatory disorders and other disorders which benefit from the modulation of fatty acid ethanolamines, particularly palmitoylethanolamide (PEA). The compound is used in methods of inhibiting NAAA and methods of therapeutical treatment and prevention of pain and inflammation. | 2019-05-09 |
20190135803 | NOVEL PROCESS FOR PREPARATION OF TETRABENAZINE AND DEUTETRABENAZINE - The present invention provides process for preparation of dihydroxy benzoquinoline compound (III) comprising reacting dihydroxy isoquinoline compound (IV) or a salt thereof with (2-acetyl-4-methyl-pentyl)-trimethyl-ammonium iodide (V) and further converting it to tetrabenazine (I) and deutetrabenazine (II). | 2019-05-09 |
20190135804 | COMPOSITIONS AND METHODS FOR THE INHIBITION OF PRURITUS - Pharmaceutical compositions comprising a molecular inhibitor of Npr1 are disclosed. Also disclosed are methods of treating, reducing, or preventing acute and/or chronic pruritus in a mammal comprising administering a pharmaceutical composition comprising a molecular inhibitor of Npr1. | 2019-05-09 |
20190135805 | OCTAHYDRO FUSED AZADECALIN GLUCOCORTICOID RECEPTOR MODULATORS - The present invention provides octahydro fused azadecalin compounds and methods of using the compounds as glucocorticoid receptor modulators. | 2019-05-09 |
20190135806 | SOLID STATE FORMS OF VENETOCLAX AND PROCESSES FOR PREPARATION OF VENETOCLAX - Solid state forms of Venetoclax, pharmaceutical compositions thereof, and uses thereof are disclosed. Also disclosed are processes for the preparation of Venetoclax. | 2019-05-09 |
20190135807 | PYRAZOLYL PYRROLO[2,3-B]PYRMIDINE-5-CARBOXYLATE ANALOGS AND METHODS OF MAKING THE SAME - The present invention relates to new pyrrolopyridine compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK1 and JAK3 kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis. | 2019-05-09 |
20190135808 | SUBSTITUTED PYRROLOPYRIDINE JAK INHIBITORS AND METHODS OF MAKING AND USING THE SAME - The present invention relates to new pyrrolopyridine compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibition of JAK1 and JAK3 kinase activity in a human or animal subject are also provided for the treatment diseases such as pruritus, alopecia, androgenetic alopecia, alopecia areata, vitiligo and psoriasis. | 2019-05-09 |
20190135809 | Pro-Neurogenic Compounds - Compounds and methods for stimulating neurogenesis (e.g., post-natal neurogenesis, including post-natal hippocampal and hypothalamic neurogenesis) and/or protecting neuronal cell from cell death are disclosed herein. In vivo activity tests suggest that these compounds may have therapeutic benefits in neuropsychiatric and/or neurodegenerative diseases such as schizophrenia, major depression, bipolar disorder, normal aging, epilepsy, traumatic brain injury, post-traumatic stress disorder, Parkinson's disease, Alzheimer's disease, Down syndrome, spinocerebellar ataxia, amyotrophic lateral sclerosis, Huntington's disease, stroke, radiation therapy, chronic stress, abuse of a neuro-active drug, retinal degeneration, spinal cord injury, peripheral nerve injury, physiological weight loss associated with various conditions, as well as cognitive decline associated with normal aging, chemotherapy, and the like. | 2019-05-09 |
20190135810 | PROCESSES FOR THE PREPARATION OF SUBSTITUTED TETRAHYDRO BETA-CARBOLINES - Provided herein are improved processes for the synthesis of substituted tetrahydro beta-carboline derivatives. In particular, provided herein are improved processes useful for the preparation of (S)-4-chlorophenyl 6-chloro-1-(4-methoxyphenyl)-3,4-dihydro-1H-pyrido[3,4-b]indole-2(9H)-carboxylate. Formula (I): | 2019-05-09 |
20190135811 | PYRIMIDINE-BASED ANTIPROLIFERATIVE AGENTS - This invention is in the area of pyrimidine-based compounds for the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers. | 2019-05-09 |
20190135812 | NOVEL ARYL HYDROCARBON RECEPTOR LIGANDS DERIVED FROM KYNURENINE - The present invention relates to novel compounds which are aryl hydrocarbon receptor (AHR) ligands and uses thereof. | 2019-05-09 |
20190135813 | CYCLOBUTYL SUBSTITUTED PYRROLOPYRIDINE AND PYRROLOPYRIMIDINES DERIVATIVES AS JAK INHIBITORS - The present invention provides cyclobutyl substituted pyrrolopyrimidines and pyrrolopyridines of Formula I: | 2019-05-09 |
20190135814 | MATERIALS FOR ORGANIC ELECTROLUMINESCENT DEVICES - The present invention relates to compounds of formula (1). The compounds are suitable for use in electronic devices, in particular organic electroluminescent devices, comprising these compounds. In some embodiments, the compounds are used as matrix materials for phosphorescent or fluorescent emitters as well as a hole-blocking or electron-transport | 2019-05-09 |
20190135815 | METABOTROPHIC GLUTAMATE RECEPTOR 5 MODULATORS AND METHODS USE THEREOF - Compounds that modulate GluR5 activity and methods of using the same are disclosed. | 2019-05-09 |
20190135816 | SUBSTITUTED PYRIMIDINE COMPOUNDS AND METHODS OF USE AND MANUFACTURE - This invention provides substituted pyrimidine compounds having the formula: | 2019-05-09 |
20190135817 | CDK2/4/6 Inhibitors - This invention relates to compounds of general Formula (I) | 2019-05-09 |
20190135818 | 5-MEMBERED HETEROCYCLE FUSED WITH [3,4-D] PYRIDAZINONE, AND MANUFACTURING METHOD, PHARMACEUTICAL COMPOSITION, AND APPLICATION THEREOF - The present invention provides a compound comprising a 5-membered heterocycle fused with a pyridazinone, wherein the compound is used as an FGFR kinase inhibitor, and a manufacturing method and application thereof. The invention specifically provides a compound as represented by formula (I). Various radicals are as defined in the specification. The compound provided by the invention effectively inhibits an activity of an FGFR kinase, and can be used to manufacture a pharmaceutical product for treating a disease related to the activity of the FGFR kinase. | 2019-05-09 |
20190135819 | CARM1 INHIBITORS AND USES THEREOF - Provided herein are compounds of Formula (I): | 2019-05-09 |
20190135820 | SYNTHESIS OF N-(HETEROARYL)-PYRROLO[3,2-D]PYRIMIDIN-2-AMINES - This invention is in the area of synthesizing pyrimidine-based compounds useful in the treatment of disorders involving abnormal cellular proliferation, including but not limited to tumors and cancers. | 2019-05-09 |
20190135821 | SMALL MOLECULES ACTIVE AGAINST GRAM-NEGATIVE BACTERIA - Disclosed are compounds that accumulate in Gram-negative bacteria. Also disclosed are method of antimicrobial treatment using the compounds. | 2019-05-09 |
20190135822 | NEW ANTIMICROBIAL COMPOUND - The invention provides a new compound, a method to produce it and use of it as an antimicrobial agent, as well as pharmaceutical compositions comprising it. It is also disclosed use of actinomycetes bacteria to produce the compound (Formula III). | 2019-05-09 |
20190135823 | PYRAZOLE COMPOUNDS AS MODULATORS OF FSHR AND USES THEREOF - The present invention relates to pyrazole compounds, and pharmaceutically acceptable compositions thereof, useful as positive allosteric modulators of follicle stimulating hormone receptor (FSHR). | 2019-05-09 |
20190135824 | ANTI-CANCER COMPOUNDS TARGETING RAL GTPASES AND METHODS OF USING THE SAME - Methods of inhibiting the growth or metastasis of a cancer in a subject by inhibiting a Ral GTPase in the subject, and small molecule inhibitors of Ral GTPases useful in the methods of the invention. Pharmaceutical compositions containing the compounds of the invention, and methods of using the same. | 2019-05-09 |
20190135825 | Quinazoline and Indole Compounds to Treat Medical Disorders - Compounds, methods of use, and processes for making inhibitors of Complement Factor B are provided. | 2019-05-09 |
20190135826 | PROCESS FOR MANUFACTURING DIANHYDROHEXITOL CRYSTALS WITH A STEP OF EVAPORATIVE CRYSTALLIZATION OF THE FIRST CRYSTALLIZATION MOTHER LIQUORS - A process for manufacturing crystals of 1,4:3,6-dianhydrohexitols, by manufacturing a solution of an internal dehydration product of at least one hexitol, distilling the solution, crystallizing, and wherein the crystallization mother liquors undergo a step of evaporative crystallization. Unlike the prior art processes that seek to recycle the crystallization mother liquors, evaporative crystallization economically and efficiently replaces the succession of steps consisting of at least one concentration, then at least one step of purification by distillation, chromatography, or crystallization. | 2019-05-09 |
20190135827 | Substituted Tricyclics and Method of Use - The present invention provides for compounds of formula (I) | 2019-05-09 |