23rd week of 2018 patent applcation highlights part 23 |
Patent application number | Title | Published |
20180155303 | RIBONUCLEOTIDE REDUCTASE INHIBITORS AND METHODS OF USE - Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme, as well as methods of synthesizing these novel compounds. The compounds may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases. | 2018-06-07 |
20180155304 | CATIONIC LIPID - The present invention aims to provide a cationic lipid that can be used as a nucleic acid delivery carrier, a lipid membrane structure using a cationic lipid, a nucleic acid-introducing agent using a cationic lipid, and a method of achieving nucleic acid introduction by using a nucleic acid-introducing agent containing a cationic lipid. A lipid membrane structure containing a cationic lipid represented by the formula (1) | 2018-06-07 |
20180155305 | CATALYTIC HYDROLYSIS AND DEHYDRATION OF SACCHARIDES - In one aspect, methods of HMF production are described herein. A method of HMF production, in some embodiments, comprises providing a saccharide feedstock including glucose and bringing the saccharide feedstock into contact with a solid state catalytic structure at a temperature sufficient to effectuate dehydration of the glucose to provide HMF. The solid state catalytic structure comprises a substrate having one or more surfaces functionalized with saccharide solubilization functionalities and acid functionalities, wherein the saccharide solubilization functionalities comprise one or more imidazolium salts pendant along chains of a first polymeric species attached to the substrate surface. | 2018-06-07 |
20180155306 | PROCESS FOR PURIFYING A CRUDE COMPOSITION OF DIALKYL ESTER OF 2,5-FURANDICARBOXYLIC ACID - An ester composition including at least 90% wt of the dialkyi ester of 2,5-furandicarboxylic acid as starting dialkyi ester concentration and up to 5% wt of the monoalkyi ester of 2,5-furandicarboxylic acid as starting monoalkyi ester concentration, the percentages being based on the weight of the ester composition, is purified in a process which includes subjecting the ester composition to melt crystallization to yield a purified dialkyi ester composition containing a dialkyi ester concentration higher than the starting dialkyi ester concentration and a melt residue containing a monoalkyi ester concentration higher than the starting monoalkyi ester concentration. From the melt residue a purified monoalkyi ester composition and a contaminants-rich residue can be prepared via melt crystallization. The purified dialkyi ester composition and/or the purified monoalkyi ester composition can be hydrolyzed to yield purified 2,5-furandicarboxylic acid. | 2018-06-07 |
20180155307 | REACTIVE DISTILLATION PROCESS FOR THE ESTERIFICATION OF FURANDICARBOXYLIC ACID - A process for efficiently esterifying furan dicarboxylic acid, especially 2,5-furan dicarboxylic acid in the presence of an alcohol and, optionally, a catalyst is disclosed. The process provides high yields of the diesters of furan dicarboxylic acid and comprises a multi-stage esterification process wherein a portion of a gas phase is removed at each stage of the multi-stage process. | 2018-06-07 |
20180155308 | PROCESS FOR THE PREPARATION OF A PURIFIED ACID COMPOSITION - A purified acid composition including 2,5-furandicarboxylic acid is prepared in a process, including oxidizing a feedstock containing 5-alkoxymethylfurfural to an oxidation product including 2,5-furandicarboxylic acid (FDCA) and 2-formyl-furan-5-carboxylic acid (FFCA), and esters of FDCA and, optionally, esters of FFCA; hydrolyzing the at least part of the oxidation product in the presence of water, thereby hydrolyzing at least esters of FDCA and, optionally, esters of FFCA to obtain an aqueous solution of an acid composition including FDCA, FFCA and ester of FDCA in an amount below the amount of ester of FDCA in the solution of the oxidation product; contacting at least part of the solution of the acid composition with hydrogen in the presence of a hydrogenation catalyst to hydrogenate FFCA to hydrogenation products, yielding a hydrogenated solution; and separating at least a portion of the FDCA from at least part of the hydrogenated solution by crystallization. | 2018-06-07 |
20180155309 | PROCESS FOR THE PREPARATION OF A PURIFIED ACID COMPOSITION - A purified acid composition including 2,5-furandicarboxylic acid is prepared by a process including a) providing an acid composition solution of a crude acid composition in a polar solvent, the crude acid composition including 2,5-furandicarboxylic acid (FDCA) and 2-formyl-furan-5-carboxylic acid (FFCA); b) contacting the acid composition solution with hydrogen in the presence of a hydrogenation catalyst to hydrogenate FFCA to hydrogenation products, such that the hydrogenation products contain a minor amount of 2-methyl-furan-5-carboxylic acid (MFA) or no MFA, yielding a hydrogenated solution; c) separating at least a portion of the FDCA from the hydrogenated solution by crystallization. | 2018-06-07 |
20180155310 | INHIBITORS OF PSEUDOMONAS AERUGINOSA LECB - The present invention relates to compounds derived from deoxy fucose. These compounds are useful as lectin inhibitors, especially as inhibitors of LecB. The invention also relates to pharmaceutical compositions comprising these compounds. The invention further relates to therapeutic uses of these compounds, especially to the prophylaxis or treatment of infections involving | 2018-06-07 |
20180155311 | SEPARATION OF CHIRAL ISOMERS BY SFC - The present invention relates to the field of separating chiral isomers from each other. Particularly, it relates to the field of separating of chiral isomers of chromane or chromene compounds, particularly tocopherols, 3,4-dehydro-tocopherols and tocotrienols, as well as the protected forms thereof. It has been found that the use of supercritical carbon dioxide as mobile phase combined with the very specific chiral phase as stationary phase leads to a very efficient separation of the individual chiral isomers. As the method is very efficient and fast combined with advantageous in view of ecology it is of big industrial interest. | 2018-06-07 |
20180155312 | COMPOUND AND ORGANIC ELECTRONIC DEVICE USING THE SAME - Provided are a novel compound and an organic electronic device using the same. The novel corn pound is represented by the following Formula (I): | 2018-06-07 |
20180155313 | METHOD AND DEVICE FOR MANUFACTURING LACTIDE - A method and a device for manufacturing lactide, whereby crude lactide, being prepared by means of depolymerization of lactic acid oligomers, is purified by means of a distillation step. The prepared crude lactide is maintained for a period of at least 5 hours in a reaction vessel at a temperature between 97° C. and 200° C. prior to the distillation step. Keeping the lactide during a period of time in a reaction vessel leads to a decrease of the lactic acid content and an increase of the lactic acid oligomer concentration, so that the resulting crude lactide can be more efficiently purified during subsequent distillation. A pre-distilling step gives additional advantages. | 2018-06-07 |
20180155314 | PIPERDINYL NOCICEPTIN RECEPTOR COMPOUNDS - The present invention provides novel piperidinyl-containing nociceptin receptor ligand compounds and pharmaceutical compositions useful in the treatment of neurological diseases and conditions where such ligands mediate the negative effects of the condition. Such neurological diseases and conditions include acute and chronic pain, substance abuse/dependence, alcohol addiction, anxiety, depression, sleep disorders, gastrointestinal disorders, renal disorders, cardiovascular disorders and Parkinson's disease. | 2018-06-07 |
20180155315 | MUSCARINIC AGONISTS - This invention relates to compounds that are agonists of the muscarinic M | 2018-06-07 |
20180155316 | 4'-O-SUBSTITUTED ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - Provided are 4′-O substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 2018-06-07 |
20180155317 | NUCLEAR TRANSPORT MODULATORS AND USES THEREOF - The present invention relates to compounds of formula I: | 2018-06-07 |
20180155318 | METHODS OF USE OF CYCLIC AMIDE DERIVATIVES TO TREAT SCHIZOPHRENIA - Disclosed herein are compositions and methods for treating schizophrenia and symptoms of schizophrenia, including negative symptoms of schizophrenia. | 2018-06-07 |
20180155319 | DEOXYURIDINE TRIPHOSPHATASE INHIBITORS - Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions. | 2018-06-07 |
20180155320 | 2-OXO-1,2-DIHYDROPYRIDINE-3-CARBOXAMIDE COMPOUNDS AND THEIR USE AS INHIBITORS OF PDK1 - The present invention concern a 2-oxo-1,2-dihydropyridine-3-carboxamide compound of Formula (I) and new 2-oxo-1,2-dihydropyridine-3-carboxamide compounds of Formula (II) in the treatment of pathologies which require an inhibitor of PDK1 enzyme such as diabetes, neurodegenerative diseases such as Alzheimer's and Prion Diseases, and tumours such as breast, and pancreatic cancers and glioblastoma, particularly glioblastoma. | 2018-06-07 |
20180155321 | VIOLOGEN COMPOUND, AND ELECTROLYTE, LIGHT-TRANSMITTANCE-VARIABLE PANEL AND DISPLAY DEVICE INCLUDING THE VIOLOGEN COMPOUND - A display device comprises a light-transmittance-variable panel including a first substrate and a second substrate facing each other; a first transparent electrode on the first substrate; a second transparent electrode on the second substrate; and an electrochromic layer between the first transparent electrode and the second transparent electrode and containing a viologen compound; and a display panel on one side of the light-transmittance-variable panel and including a plurality of display units and a plurality of transparent units. | 2018-06-07 |
20180155322 | TETRAHYDRONAPHTHALENE AND TETRAHYDROISOQUINOLINE DERIVATIVES AS ESTROGEN RECEPTOR DEGRADERS - The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end at least one of a Von Hippel-Lindau ligand, a cereblon ligand, Inhibitors of Apoptosis Proteins ligand, mouse double-minute homolog 2 ligand, or a combination thereof, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure. | 2018-06-07 |
20180155323 | ISOQUINOLIN-3-YL CARBOXAMIDES AND PREPARATION AND USE THEREOF - Isoquinoline compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an isoquinoline compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states. | 2018-06-07 |
20180155324 | 2-(2,4-DIFLUOROPHENYL)-1,1-DIFLUORO-1-(5-SUBSTITUTED-PYRIDIN-2-YL)-3-(1H-T- ETRAZOL-1-YL)PROPAN-2-OLS AND PROCESSES FOR THEIR PREPARATION - Provided herein are 2-(2,4-difluorophenyl)-1,1-difluoro-1-(5-substituted-pyridin-2-yl)-3-(1H-tetrazol-1-yl)propan-2-ols and 1-(2,4-difluorophenyl)-2,2-difluoro-2-(5-substituted-pyridin-2-yl)ethanones and processes for their preparation. | 2018-06-07 |
20180155325 | COMPOUND FOR ORGANIC OPTOELECTRONIC DEVICE, COMPOSITION FOR ORGANIC OPTOELECTRONIC DEVICE AND ORGANIC OPTOELECTRONIC DEVICE AND DISPLAY DEVICE - Disclosed are a compound for an organic optoelectronic device represented by Chemical Formula 1, a composition for an organic optoelectronic device, an organic optoelectronic device including the same, and a display device. Details of Chemical Formula 1 are the same as defined in the specification. | 2018-06-07 |
20180155326 | METHOD FOR PREPARING TRITYL CANDESARTAN - The present invention uses a candesartan cyclic compound as a starting material and performs thereon a three-step reaction of forming tetrazole, hydrolysis and adding a protecting group to directly obtain trityl candesartan without separating an intermediate product via crystallization. The operating process is simple and thus is more applicable to industrial production. | 2018-06-07 |
20180155327 | PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS AND THEIR THERAPEUTICAL APPLICATIONS - The present invention provides antitumor agents comprising substituted pyrimidine derivatives and pharmaceutically-acceptable formulations thereof, methods for making novel compounds and methods for using the compounds. The compounds and compositions in accordance with the invention have utility in treatment of a variety of diseases and have kinase inhibitory activities. | 2018-06-07 |
20180155328 | MONOMERS AND POLYMERS FOR FUNCTIONAL POLYCARBONATES AND POLY(ESTER-CARBONATES) AND PEG-CO-POLYCARBONATE HYDROGELS - The invention generally relates to functional polymers and hydrogels. More particularly, the invention provides versatile monomers and polymers with well-defined functionalities, e.g., polycarbonates and poly(ester-carbonates), compositions thereof, and methods for making and using the same. The invention also provides cytocompatible poly(ethylene glycol)-co-polycarobonate hydrogels (e.g., crosslinked by copper-free, strain-promoted “click” chemistry). | 2018-06-07 |
20180155329 | ANHYDROUS CRYSTALLINE FORM OF (1S)-1,5-ANHYDRO-1-[3-[[5-(4-FLUOROPHENYL)-2-THIENYL]METHYL]-4-METHYLPHEN- YL]-D-GLUCITOL - The present invention is directed to an anhydrous crystalline for of (1S)-1,5-anhydro-1-[3-[[5-(4-fluorophenyl)-2-thienyl]methyl]-4-methylphenyl]-D-glucitol, pharmaceutical compositions containing said anhydrous crystalline form and its use in the treatment glucose-related disorders such as Type 2 diabetes mellitus and Syndrome X. | 2018-06-07 |
20180155330 | N-(HETEROARYL)-SULFONAMIDE DERIVATIVES USEFUL AS S100-INHIBITORS - A compound of formula (I), or a pharmaceutically acceptable salt thereof and a pharmaceutical composition comprising the compound. The compound is an inhibitor of interactions between SI 00A9 and interaction partners such as RAGE, TLR4 and EMMPRIN and as such is useful in the treatment of disorders such as cancer, autoimmune disorders, inflammatory disorders and neurodegenerative disorders. | 2018-06-07 |
20180155331 | DIARYL ISOXAZOLINE COMPOUND - The present invention concerns compounds of formula (I) or an N-oxide or salt thereof and their use for controlling parasites in and on warm-blooded animals or fish. | 2018-06-07 |
20180155332 | SMALL MOLECULE BASED ANTIBODY-RECRUITING COMPOUNDS FOR CANCER TREATMENT - The present invention relates to chimeric (including bifunctional) compounds, compositions comprising those compounds and methods of treating cancer in a patient or subject, especially including metastatic cancer where cancer cells exhibit overexpression (heightened expression) of cell surface urokinase-type plasminogen activator receptor (urokinase receptor) compared to normal (non-cancerous) cells. The compounds bind to the urokinase-type plasminogen activator receptor (uPAR) on the surface of a cancer cell, including a metastatic cancer cell, and consequently recruit native antibodies of the patient or subject where the antibodies can selectively degrade and/or deactivate targeted cancer cells through antibody-dependent cellular phagocytosis and antibody-dependent cellular cytotoxicity (ADCC) and/or complement dependent cytotoxicity (CDC) against a large number and variety of cancers, thus providing cancer cell death and an inhibition of growth, elaboration and/or metastasis of the cancer, including remission and cure of the patient's cancer. | 2018-06-07 |
20180155333 | Heterocyclic Compound - The present invention provide a compound having an orexin receptor antagonistic activity, which is expected to be useful as medicaments such as agents for the prophylaxis or treatment of sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease and the like. | 2018-06-07 |
20180155334 | NOVEL PROCESSES - The present invention provides novel processes for preparing compounds of formula (IV) and salts thereof | 2018-06-07 |
20180155335 | SALT AND CRYSTAL FORMS OF PLK-4 INHIBITOR - A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are also disclosed. The present invention also provides methods of treating a subject with a cancer. Compound (I) | 2018-06-07 |
20180155336 | PROCESS FOR THE PREPARATION OF 2-{4-[2-({[2-(4-CHLOROPHENYL)-1,3-THIAZOL-4-YL]METHYL}SULFANYL)-3,5-DICYA- N0-6-(PYRROLIDIN-1-YL)PYRIDIN-4-YL]PHENOXY}ETHYL-L-ALANYL-L-ALANINATE MONOHYDROCHLORIDE - The present application relates to a novel and improved process for preparing the compound 2-{4-[2-({[2-(4-chlorophenyl)-1,3-thiazol-4-yl]methyl}sulphanyl)-3,5-dicyano-6-(pyrrolidin-1-yl)pyridin-4-yl]phenoxy}ethyl-L-alanyl L-alaninate monohydrochloride of the formula (I) | 2018-06-07 |
20180155337 | CRYSTALLINE FORMS OF (3-AMINO-OXETAN-3-YLMETHYL)-[2-(5,5-DIOXO-5,6,7,9-TETRAHYDRO-5LAMBDA*6*-T- HIA-8-AZA-BENZOCYCLOHEPTEN-8-YL)-6-METHYL-QUINAZOLIN-4-YL]-AMINE - The present invention relates to novel crystalline forms of compound (I), | 2018-06-07 |
20180155338 | ORGANIC THIN FILM TRANSISTOR, METHOD OF MANUFACTURING ORGANIC THIN FILM TRANSISTOR, ORGANIC THIN FILM TRANSISTOR MATERIAL, ORGANIC THIN FILM TRANSISTOR COMPOSITION, ORGANIC SEMICONDUCTOR FILM, AND COMPOUND - An object of the present invention is to provide an organic thin film transistor that has an organic semiconductor film manufactured by using a compound having excellent solubility to an organic solvent and that has excellent carrier mobility, a novel compound, an organic thin film transistor material, an organic semiconductor film, an organic thin film transistor composition, and a method of manufacturing an organic thin film transistor using this. The organic thin film transistor according to the present invention has an organic semiconductor film containing a compound represented by Formula (1). | 2018-06-07 |
20180155339 | METHOD FOR THE PRODUCTION OF PRAZIQUANTEL - The present invention relates to a method for the racemization of enantiomerically pure or enantiomerically enriched Praziquantel under basic conditions and a method for the production of (R)-Praziquantel in enantiopure or enantiomerically enriched form, which comprises the racemization method. | 2018-06-07 |
20180155340 | QUINOLONE DERIVATIVES AS FGFR INHIBITORS - Compounds that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds. | 2018-06-07 |
20180155341 | Antibacterial Compounds - The present invention relates to the following compounds | 2018-06-07 |
20180155342 | INHIBITORS OF INFLUENZA VIRUSES REPLICATION - Methods of inhibiting the replication of influenza viruses in a biological sample or patient, of reducing the amount of influenza viruses in a biological sample or patient, and of treating influenza in a patient, comprises administering to said biological sample or patient an effective amount of a compound represented by Structural Formula (I): | 2018-06-07 |
20180155343 | SPIRO-ISOQUINOLINE-3,4'-PIPERIDINE COMPOUNDS HAVING ACTIVITY AGAINST PAIN - The present invention relates to compounds having pharmacological activity towards the sigma (σ) receptor, and more particularly to spiro-isoquinoline-3,4′-piperidine compounds having this pharmacological activity, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain. | 2018-06-07 |
20180155344 | TRICYCLIC PIPERIDINE COMPOUNDS - The present invention relates to compounds of the formula (I) | 2018-06-07 |
20180155345 | sGC STIMULATORS - The present patent application discloses at least the compounds according to Formula I′ shown below, or pharmaceutically acceptable salts thereof, | 2018-06-07 |
20180155346 | COMPOUNDS USEFUL AS INHIBITORS OF ATR KINASE - The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. | 2018-06-07 |
20180155347 | PHARMACEUTICAL COMPOSITIONS COMPRISING PERILLYL ALCOHOL DERIVATIVES - A pharmaceutical composition is provided which includes perillyl alcohol conjugated with a therapeutic agent and further includes and a hydrolyzable acylated aliphatic tail. A method of using the pharmaceutical composition is also provided for treating a condition or disease of a patient, e.g., cancer. | 2018-06-07 |
20180155348 | INHIBITORS OF KRAS G12C MUTANT PROTEINS - Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): | 2018-06-07 |
20180155349 | 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. | 2018-06-07 |
20180155350 | CELL IMPERMEABLE COELENTERAZINE ANALOGUES - Described are coelenterazine analogues, methods for making the analogues, kits comprising the analogues, and methods of using the compounds for the detection of luminescence in luciferase-based assays. | 2018-06-07 |
20180155351 | PYRROLOPYRIMIDINE COMPOUNDS AND THEIR USES - The disclosed compounds relate to treatments and therapies for protein kinase-associated disorders. There is also a need for compounds useful in the treatment or prevention or amelioration of one or more symptoms of cancer, transplant rejections, and autoimmune diseases. Furthermore, there is a need for methods for modulating the activity of protein kinases, such as CDK1, CDK2, CDK4, CDK5, CDK6, CDK7, CDK8 and CDK9, using the compounds provided herein. | 2018-06-07 |
20180155352 | CRYSTALLINE FORMS OF A BRUTON'S TYROSINE KINASE INHIBITOR - Described herein is the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-1-yl)prop-2-en-1-one, including crystalline forms, solvates and pharmaceutically acceptable salts thereof. Also disclosed are pharmaceutical compositions that include the Btk inhibitor, as well as methods of using the Btk inhibitor, alone or in combination with other therapeutic agents, for the treatment of autoimmune diseases or conditions, heteroimmune diseases or conditions, cancer, including lymphoma, and inflammatory diseases or conditions. | 2018-06-07 |
20180155353 | Antimicrobial Compounds and Methods - Antimicrobial compounds are provided that are polymerizable. The compounds include monomers with antimicrobial properties. The compounds have cross-linking properties. The compounds may be utilized in dental and/or medical applications, including dental composites, dentures, bonding agents, sealants, resins and medical devices. | 2018-06-07 |
20180155354 | SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF - Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed. | 2018-06-07 |
20180155355 | CRYSTALS OF DISPIROPYRROLIDINE DERIVATIVES - Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3′R,4′S,5′R)-N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6″-chloro-4′-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2″-oxo-1″,2″-dihydrodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indole]-5′-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same. | 2018-06-07 |
20180155356 | Crystals of Dispiropyrrolidine Derivatives - Crystals of a dispiropyrrolidine compound or a salt thereof which inhibits the action of Mdm2 are provided. The present invention provides crystals of (3′R,4′S,5′R)—N-[(3R,6S)-6-carbamoyltetrahydro-2H-pyran-3-yl]-6″-chloro-4′-(2-chloro-3-fluoropyridin-4-yl)-4,4-dimethyl-2″-oxo-1″,2″-dihydrodispiro[cyclohexane-1,2′-pyrrolidine-3′,3″-indole]-5′-carboxamide or a salt thereof which inhibits Mdm2 and has anti-tumor activity. The present invention also provides a medicament comprising the same. | 2018-06-07 |
20180155357 | ISOSORBIDE DIESTER AS PEARLIZING AGENT AND OPACIFIER - A description is given of a composition comprising at least one isosorbide diester, at least one isosorbide monoester and at least one fatty acid, and also of a process for the preparation thereof. In addition, the present invention relates to the use of this composition as pearlizing agent and opacifier in cosmetic compositions and detergents. | 2018-06-07 |
20180155358 | ERTUGLIFLOZIN CO-CRYSTALS AND PROCESS FOR THEIR PREPARATION - The present invention relates to processes for the preparation of an ertugliflozin-L-pyroglutamic acid (1:1) and co-crystal ertugliflozin-L-proline (1:1) co-crystal. The present invention further relates to an ertugliflozin-L-proline (1:2) co-crystal, processes for its preparation, and its use for the treatment of type 2 diabetes mellitus. | 2018-06-07 |
20180155359 | SHIP1 MODULATORS AND METHODS RELATED THERETO - Compounds of formula (II): | 2018-06-07 |
20180155360 | ETHER ANALOGUES OF GALIELLALACTONE - Ether analogues of galiellalactone, methods of preparing the analogues, and use of the analogues in the treatment of cancer are disclosed. The analogues are of formula (I) or (II): | 2018-06-07 |
20180155361 | PALLADIUM-MEDIATED KETOLIZATION - Provided herein are palladium-mediated coupling reactions useful in the preparation of ketone-containing organic molecules. The provided methods can be used for the preparation of natural products and pharmaceutical agents, including Eribulin, halichondrins, and analogs thereof. The present invention also provides novel halichondrin analogs which can be prepared via the palladium-mediated coupling reactions. The novel halichondrin analogs can be used in the prevention and/or treatment of diseases or conditions (e.g., proliferative diseases such as cancer). | 2018-06-07 |
20180155362 | MCL-1 INHIBITORS AND METHODS OF USE THEREOF - Disclosed is a compound which is 17-chloro-5,13,14,22-tetramethyl-28-oxa-2,9-dithia-5,6,12,13,22-pentaazaheptacyclo[27.7.1.1 | 2018-06-07 |
20180155363 | COMPOUNDS FOR THE TREATMENT OF ISCHEMIA-REPERFUSION-RELATED DISEASES - The present invention relates to compounds of formula (I) useful in the treatment of ischemia-reperfusion-related pathologies. | 2018-06-07 |
20180155364 | NOVEL PROCESS FOR THE PREPARATION OF DOLUTEGRAVIR AND PHARMACEUTICALLY ACCEPTABLE SALTS THEREOF - The present invention relates to a novel process for the preparation of dolutegravir and pharmaceutically acceptable salts thereof using novel intermediates. | 2018-06-07 |
20180155365 | TETRACYCLIC HETEROCYCLE COMPOUNDS USEFUL AS HIV INTEGRASE INHIBITORS - The present invention relates to Tetracyclic Heterocycle Compounds of Formula (I). | 2018-06-07 |
20180155366 | THIAZOLOPYRIMIDINONE COMPOUNDS AND PREPARATION METHODS AND USE THEREOF - The present invention provides structural details of a thiazolopyrimidinone compound, a preparation method thereof, and use thereof in the manufacture of a medicament for the treatment of central nervous system diseases. | 2018-06-07 |
20180155367 | ETP DERIVATIVES - Provided herein, inter alia, is the synthesis of ETP derivatives. The uses of the ETP derivatives described herein include treatment of cancer. | 2018-06-07 |
20180155368 | METHOD FOR PREPARING L-BPA - Provided is a method for preparing L-BPA, which includes steps of: reacting N-protected (S)-4-halophenylalanine of Formula I, a boronating agent, Grignard reagent and bis(2-methylaminoethyl)ether to obtain a reaction mixture, wherein the reaction mixture comprises N-protected (S)-4-boronophenylalanine of Formula II and the R | 2018-06-07 |
20180155369 | A PROCESS FOR THE PREPARATION OF BIS(CHLOROMETHYL)DICHLOROSILANE AND BIS(CHLOROMETHYL)(ARYL)CHLOROSILANE - The instant invention provides a process for the preparation of bis(chloromethyl)dichlorosilane (BCMCS) or bis(chloromethyl) (aryl)chlorosilane (BCMACS) comprising reacting bis(chloromethyl) diphenylsilane and one or more chloride compounds in the presence of a Lewis acid in an inert solvent and under an inert atmosphere. | 2018-06-07 |
20180155370 | THERMOSETTING ALKOXYSILYL COMPOUND HAVING TWO OR MORE ALKOXYSILYL GROUPS, COMPOSITION AND CURED PRODUCT COMPRISING SAME, USE THEREOF, AND METHOD FOR PREPARING ALKOXYSILYL COMPOUND - The present invention relates to: a thermosetting alkoxysilyl compound (hereinafter, referred to as “alkoxysilyl compound”)having two or more alkoxysilyl groups showing excellent heat-resistance characteristics in a composite; a composition and a cured product comprising the same; a use thereof; and a method for preparing an alkoxysilyl compound. The composition of an alkoxysilyl compound, comprising a novel alkoxysilyl compound according to the present invention shows, in a composite, improved heat-resistance characteristics, i.e., an effect of decreasing the CTE of the composition of an alkoxysilyl compound and not showing a glass transition temperature (hereinafter, referred to as “Tg-less”). Further, the cured product comprising an alkoxysilyl compound according to the present invention shows excellent flame retardant properties due to the alkoxysilyl groups. | 2018-06-07 |
20180155371 | PROCESS FOR PREPARING AN ACRYLOYLOXYSILANE - A process for preparing an acryloyloxysilane, comprising: reacting a metal salt of a carboxylic acid having the formula [CR | 2018-06-07 |
20180155372 | TIN COMPOUND, METHOD OF SYNTHESIZING THE SAME, TIN PRECURSOR COMPOUND FOR ATOMIC LAYER DEPOSITION, AND METHOD OF FORMING TIN-CONTAINING MATERIAL FILM - A tin compound, tin precursor compound for atomic layer deposition (ALD), a method of forming a tin-containing material film, and a method of synthesizing a tin compound, the tin compound being represented by Chemical Formula (I): | 2018-06-07 |
20180155373 | Cysteine-Modifying Substrate Analogue Inhibitors of Ribose 5-Phosphate Isomerase for Parasitic Diseases, Along with Methods of Their Formation and Use - Compounds are generally provided, along with pharmaceutical compositions including such compounds. Methods are also generally provided for inhibiting ribose 5-phosphate isomerase in a human, such as via administering to the human the pharmaceutical composition that includes such a compound. Methods are also generally provided for treating a mammal that is infected by a parasitic organism, such as via administering to the mammal the pharmaceutical composition that includes such a compound. Methods are also generally provided for forming a pharmaceutical composition. | 2018-06-07 |
20180155374 | BISPHOSPHONATES VINYLIC MONOMERS AND POLYMERS AND USES THEREOF - A compound or a polymer is claimed. A first formula can be | 2018-06-07 |
20180155375 | NOVEL CHIRAL DIHYDROBENZOOXAPHOSPHOLE LIGANDS AND SYNTHESIS THEREOF - This invention relates to novel phosphorous ligands useful for organic transformations. Methods of making and using the ligands in organic synthesis are described. The invention also relates to processes for preparing the novel ligands. | 2018-06-07 |
20180155376 | ALLYL-PHENOXY-CYCLOPHOSPHAZENE COMPOUND, AND PRODUCTION METHOD THEREFOR - An object of the present invention is to provide a mixture of cyclophosphazenes suitably substituted with phenoxy having a polymerizable functional group, such as allyl, on the phenyl ring and a production method for the mixture. The invention relates to a mixture of cyclophosphazene compounds that each contain a plurality of constituent units linked to each other, each constituent unit being represented by formula (I): | 2018-06-07 |
20180155377 | NOVEL CHIRAL DIHYDROBENZOAZAPHOSPHOLE LIGANDS AND SYNTHESIS THEREOF - This invention relates to novel phosphorous ligands useful for organic transformations. Methods of making and using the ligands in organic synthesis are described. The invention also relates to processes for preparing the novel ligands. | 2018-06-07 |
20180155378 | ANTIBACTERIAL BISMUTH COMPLEXES - Provided herein are organobismuth (III) phosphinate complexes, which comprise a phosphinate group and an aromatic carbocyclyl or aromatic heterocyclyl group. The complexes find use as antibacterial agents, and accordingly also provided herein are products, devices, compositions and materials comprising the complexes, for example medical products such as wound dressings and bandages. | 2018-06-07 |
20180155379 | Ruthenium Precursors For ALD And CVD Thin Film Deposition And Uses Thereof - Metal coordination complexes comprising a metal atom coordinated to at least one diazabutadiene ligand having a structure represented by: | 2018-06-07 |
20180155380 | PLATINUM COMPLEX, OLED AND APPARATUS FOR PROVIDING VISIBLE EMISSION OR NEAR-INFRARED EMISSION - A platinum complex, an OLED and an apparatus for providing visible emission or near-infrared (NIR) emission using the same are described. The platinum complex has a structure represented by formula (I): | 2018-06-07 |
20180155381 | ORGANIC ELECTROLUMINESCENT MATERIALS AND DEVICES - Metal complexes with cyclic ligands having Formula (I), | 2018-06-07 |
20180155382 | CYTOTOXIC PLATINUM COMPLEX, ITS PREPARATION AND THERAPEUTIC USE - Platinum(IV) complexes especially suitable for antitumor therapy and methods for their preparation. Further provided is a method for treating a subject, in particular a human, suffering from a disease comprising administering a platinum(IV) complex of the present invention, which disease is especially preferably but not exclusively a cancer. Further provided is a method of inhibiting the growth of tumor cells by contacting the cells with a platinum(IV) complex of the present invention and a pharmaceutical composition comprising a platinum(IV) complex of the present invention. The platinum(IV) complexes of the present invention represent a novel class of platinum anticancer prodrugs for the treatment of diseases especially of cancer. The platinum(IV) complexes of the present invention exhibit advantageously high cytotoxic activity in various cancer types superior to commonly used platinum-based complexes. In addition, the complexes proved to be highly effective even against cisplatin-resistant cancers. | 2018-06-07 |
20180155383 | ORGANOMETALLIC COMPOUNDS USEFUL FOR CHEMICAL PHASE DEPOSITION - Organometallic compounds, useful in chemical phase deposition processes, having a structure: [{R | 2018-06-07 |
20180155384 | SUBSTITUTED NUCLEOSIDES, NUCLEOTIDES AND ANALOGS THEREOF - Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus infection with one or more nucleosides, nucleotides and nucleotide analogs. | 2018-06-07 |
20180155385 | NUCLEOTIDES FOR THE TREATMENT OF CANCER - The present invention relates to novel nucleoside derivatives, pharmaceutical compositions comprising the compounds, processes of preparation thereof, and methods of use thereof for treating cancer. | 2018-06-07 |
20180155386 | PROGESTERONE ANTAGONISTS - Described herein are compounds which either act as pure antiprogestins or as antiprogestins with partial agonistic activity and methods of treating cancer using such compounds. | 2018-06-07 |
20180155387 | PRODUCTION OF STEROLS - Method of recovering sterols from tall oil pitch which contains steryl esters. In the method the tall oil pitch is subjected to a transefterification reaction with a lower alcohol in a reaction zone to provide a reaction product mixture containing lower alkyl fatty acid esters, free sterols, and at least some unreacted steryl esters. The invention comprises separating the transesterified esters from the reaction product mixture to form a sterol rich fraction which contains free sterols and unreacted steryl esters, liberating sterols from the unreacted steryl esters to form further free sterols, and recovering and optionally purifying the free sterols. The recovery of free sterols can be increased to up to 80 wt % or more while avoiding the formation of undesired side streams containing troublesome impurities. | 2018-06-07 |
20180155388 | SELECTIVE PROGESTERONE RECEPTOR MODULATOR (SPRM) REGIMEN - The invention is directed to a pharmaceutical composition comprising a progesterone receptor antagonist namely (11β,17β)-17-Hydroxy-11-[4-(methylsulphonyl)phenyl]-17-(pentafluoroethy)estra-4,9-dien-3-one for the treatment and/or prophylaxis of Uterine Fibroids (myomas, uterine leiomyoma) that is administered to a patient diagnosed with Uterine Fibroids following a specific regimen. Additionally, the invention is directed to a method for treating Uterine Fibroids (myomas, uterine leiomyoma) and/or for reducing Uterine Fibroids (myomas, uterine leiomyoma) size and symptoms related to Uterine Fibroids following a specific regimen as well as treatment of Heavy Menstrual Bleeding (HMB). | 2018-06-07 |
20180155389 | STEROIDS AND PROTEIN-CONJUGATES THEREOF - Described herein protein steroid conjugates that are useful, for example, for the target-specific delivery of glucocorticoids (GCs) to cells. | 2018-06-07 |
20180155390 | SURFACE NEUTRALIZATION OF APATITE - The present invention discloses methods of neutralizing apatite surfaces, for example during chromatography and before protein elution. | 2018-06-07 |
20180155391 | Method for extracting proteins and functional lipid from soybean liquid by directional continuous catalysis with nano magnetic immobilized enzymes - The present invention relates to fields of continuous directional catalysis of soybean slurry to extract protein and functional oil with nano-magnetic immobilized enzymes. The present invention discloses soybean slurry as raw material and continuous mobile phase, and nano-magnetic immobilized enzymes as stationary phase applied in three-phase magnetic fluidized bed. The present invention provides a method of enzymatic disrupting cell walls by nano-magnetic immobilized enzyme cocktail including cellulose, pectinase and alkaline protease. The method can he used to break down lipoprotein, lipopolysaccharide complex and break lipoprotein film on the surface of lipoprotein to release the lipid. The present invention also provides a method to catalyze phospholipid using nano-magnetic immobilized phospholipase to change the polarity of phospholipids and control liquid emulsification phenomenon. The enzymes disclosed in the present invention do not interfere with each other. The preparation method can be used to catalyze soybean slurry continuously using the nano-magnetic immobilized enzymes to extract protein and functional lipid simultaneously. | 2018-06-07 |
20180155392 | CYSTARGOLIDE COMPOUNDS AND USES THEREOF - There is provided herein compounds of formula I, wherein R | 2018-06-07 |
20180155393 | HEPATITIS C VIRUS INHIBITORS - The present disclosure relates to methods for making asunaprevir, useful treatment of Hepatitis C virus (HCV) infection, and its intermediates. | 2018-06-07 |
20180155394 | CANCER CELL-TARGETING PEPTIDE AND USE THEREOF - The present invention relates to a peptide targeting a tumor cell and use of the peptide, and more particularly, to a peptide consisting of SEQ ID NO: 1 to SEQ ID NO: 4 and specifically binding to a tumor cell, a composition including the peptide as an effective ingredient for detecting a tumor cell, a composition including the peptide as an effective ingredient for delivering a drug, and a composition including the peptide as an effective ingredient for imaging. The peptide of the present invention can be used for detection or imaging of a tumor cell in vitro and in vivo by specifically binding to a tumor cell. | 2018-06-07 |
20180155395 | PEPTIDOMIMETICS FOR IMAGING THE GHRELIN RECEPTOR - The present invention concerns compositions comprising and methods of identification and use of imaging agents. The imaging agents comprise a growth hormone secretagogues having a conjugated fluoride. The imaging agents of the present invention may be used for detection, diagnosis and/or staging of prostate or other forms of cancer, and may also be used for cardiac disease. | 2018-06-07 |
20180155396 | STRUCTURE-BASED PEPTIDE INHIBITORS OF P53 AGGREGATION AS A NEW APPROACH TO CANCER THERAPEUTICS - This invention relates, e.g., to an inhibitory peptide or CPP inhibitor which specifically binds to p53 having an aberrant conformation (e.g., is aggregated or misfolded) and inhibits p53 amyloidogenic aggregation or restores proper folding of the misfolded protein. Methods of using the inhibitory peptide or CPP inhibitor (e.g. to treat subjects having tumors that comprise aggregated p53) are described. | 2018-06-07 |
20180155397 | Novel Anti-Infective Compound - The invention relates to novel infective agents, the use thereof for the production of a pharmaceutical composition for the treatment and prophylaxes of a disease, preferably an infectious disease, a pharmaceutical composition comprising said compound, and to methods of producing said compounds. The invention further relates to a new probiotic configured for preventing or reducing the colonization by a pathogenic microorganism of an organ of a living being. | 2018-06-07 |
20180155398 | Flavivirus-Binding, Entry-Obstructing, Protease-Resistant Peptide (RI57) - The invention pertains to inhibitors bindable to regions of a virus. More particularly, the invention relates to inhibitors bindable to regions of flaviviral envelope glycoprotein, or flaviviral virus E protein, a class II viral E protein. Even more particularly, the invention relates to peptides inhibitory to virus-to-cell fusion and virus entry into animal cells. The invention also contains methods of determining said inhibitors, bindable to regions of the flaviviral E protein complex, (e.g., those of dengue and zika viruses) as candidates for in vivo anti-viral compounds that are also resistant to degradation by peptidases and thus extraordinarily suitable for oral, in addition to other, routes of administration. | 2018-06-07 |
20180155399 | TFPI INHIBITORS AND METHODS OF USE - The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. Peptide complexes also are provided. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, treat a blood coagulation disorder in a subject, purify TFPI, and identify a TFPI-binding compound. | 2018-06-07 |
20180155400 | COMPRESSED PATHWAYS FOR NONRIBOSOMAL MOLECULAR BIOSYNTHESIS - Provided herein are synthetic pathways from | 2018-06-07 |
20180155401 | Method for the Synthesis of Phycocyanin - The invention discloses microorganism cell culture conditions that result in increased cellular and media concentrations of a biological pigment. The invention has applications in use as a natural food colouring, as antioxidants in the food supplement industries, in the nutraceutical, pharmaceutical, and cosmeceutical industries, and a non-toxic ink. The method results in pigment that is relatively easy to separate from the microorganism culture. | 2018-06-07 |
20180155402 | RECOMBINANT BINDING PROTEINS TARGETING HER2 AND SERUM ALBUMIN, AND THEIR USES - New recombinant binding proteins, comprising designed ankyrin repeat domain(s) with binding specificity for HER2, and comprising designed ankyrin repeat domain(s) with binding specificity for serum albumin, are disclosed, as well as nucleic acids encoding such recombinant binding proteins, pharmaceutical compositions comprising such recombinant binding proteins or nucleic acids and the use of such recombinant binding proteins, nucleic acids or pharmaceutical compositions in the treatment of diseases. | 2018-06-07 |