48th week of 2017 patent applcation highlights part 23 |
Patent application number | Title | Published |
20170342023 | ISOCYANATE COMPOUND MANUFACTURING METHOD - By reacting 3-methyl-2-methoxymethylaniline, etc. with a phosgene compound in the presence of a tertiary amine at 10° C. to 14° C. in at least one kind of solvent selected from a group consisting of chlorobenzene and ortho-dichlorobenzene, an isocyanate compound such as 3-methyl-2-methoxymethyl-1-isocyanatobenzene can be manufactured with good yields. | 2017-11-30 |
20170342024 | MONOFUNCTIONAL OR MULTIFUNCTIONAL URETHANE ACRYLATE OLIGOMERS WITHOUT ISOCYANATES - The present invention relates to an acrylated and/or methacrylated urethane oligomer obtained by reaction of a specific polyamine a) with a cyclic carbonate compound b) carrying m cyclic carbonate groups, giving an intermediate product c) carrying m formed urethane groups which carry residual reactive amine —NH— groups, and subsequently an addition reaction of each of the said residual reactive amine groups of the said product c) with an acrylate group of a compound d) carrying, in addition to the said acrylate group, p additional acrylate and/or methacrylate groups, with each residual reactive amine —NH— group of the said product c) being thus converted into a carbon-nitrogen bond carrying the said acrylate and/or methacrylate groups, and thus production of the said urethane oligomer, with each carbon-nitrogen bond formed carrying p acrylate and/or methacrylate groups and the said urethane oligomer carrying m urethane groups and m hydroxyl groups in the alpha or beta position with respect to the said urethane and having a functionality in acrylates and/or methacrylates ranging from m*p(n−1) to m*p(2n−2). | 2017-11-30 |
20170342025 | ANTIMICROBIAL COMPOUNDS, COMPOSITIONS AND METHODS - The invention discloses compounds of the formula wherein A, B, X, Y and Z are defined. The compounds of the invention show activity against a range of bacteria, and are useful in the treatment or prophylaxis of a bacterial infection in an animal. | 2017-11-30 |
20170342026 | ISOPROPOXY-PHENYLGUANIDINE SERIES SALT AND APPLICATION THEREOF IN PREPARING GROWTH PROMOTERS FOR ANIMAL FEED - Isopropoxy-phenylguanidine series salt as shown by the Formula (I) and an application thereof in preparing growth promoters for animal feed, wherein R is DL-lactic acid, methanesulfonic acid, 2-hydroxyethanesulfonic acid, citric acid, tartaric acid, benzoic acid, succinic acid, fumaric acid, maleic acid, acetic acid, sulfuric acid, phosphoric acid, or oxalic acid. | 2017-11-30 |
20170342027 | CHIRAL RESOLUTION METHOD OF N-[4-(1-AMINOETHYL)-PHENYL]-SULFONAMIDE DERIVATIVES - The present specification relates to a chiral resolution method of a stereoisomer mixture, comprising a step of mixing a stereoisomer mixture of compounds, in which an amine group is bound to an asymmetric carbon atom, with a chiral auxiliary and salt-forming auxiliary compound, wherein the chiral auxiliary is an O,O′-diacyltartaric acid derivative, more specifically, a 2,3-dibenzoyl-tartaric acid or O,O′-di-p-toluoyl tartaric acid, the salt-forming auxiliary compound is mandelic acid or camphorsulfonic acid, and an optical isomer having a high level of optical purity can be obtained by using the method. Therefore, according to one aspect of the present invention, the method can be useful in pharmaceutical or cosmetic field when preparing an optical isomer having a high optical purity. | 2017-11-30 |
20170342028 | PROCESS FOR PRODUCING METHYL MERCAPTAN FROM DIMETHYL SULFIDE - The present invention generally relates to the manufacture of methyl mercaptan using recycled dimethyl sulfide. In particular, the invention relates to a process for the continuous production of methyl mercaptan via the catalytic conversion of dimethyl sulfide using a non-promoted Al | 2017-11-30 |
20170342029 | CATALYTIC OXIDATION OF BUT-3-ENE-1,2-DIOL - The invention concerns a synthesis process of a compound of the following formula (I) or one of the salts thereof, | 2017-11-30 |
20170342030 | METHOD AND CATALYST FOR SYNTHESISING AZIRIDINE - The present invention relates to methods of synthesizing aziridines including isotopically labelled aziridines, said methods comprising contacting an imine or one or more precursors thereof with a diazo compound in the presence of a phosphoramide or a phosphoramide-derived catalyst. The present invention also relates to aziridines, modified aziridines and aziridine-derived compounds preparable by the aforementioned methods, and to phosphoramide or phosphoramide-derived catalysts suitable for use in such methods. | 2017-11-30 |
20170342031 | QUENCHER - A quencher is disclosed having a compound represented by the following general formula (1): | 2017-11-30 |
20170342032 | CARBAMATE COMPOUND AND USE THEREOF - A carbamate compound represented by formula (I), | 2017-11-30 |
20170342033 | Multi-Tyrosine Kinase Inhibitors Derivatives and Methods of Use - The present invention is directed to multi-tyrosine kinase inhibitor compounds. The present invention is further directed to compositions comprising those compounds. Finally, the present invention is directed to methods of treating eye conditions including, but not limited to, diabetic background retinopathy, diabetic macular edema, diabetic proliferative retinopathy, diabetic macular edema with proliferative retinopathy, proliferative fibrovascular disease, diabetic macular edema with proliferative fibrovascular disease, retinopathy of prematurity, dry macular degeneration, dry macular degeneration with drusen and wet macular degeneration, using compounds and compositions of the invention. | 2017-11-30 |
20170342034 | NOVEL ARYL-CYANOGUANIDINE COMPOUNDS - The present invention relates to protein-lysine N-methyltransferase SMYD2 (SET and MYND domain-containing protein 2) inhibitors, in particular SMYD2-inhibitory substituted cyanoguanidine-pyrazolines of general formula (I) wherein R | 2017-11-30 |
20170342035 | 2-AMINOPYRIMIDINE DERIVATIVES FOR THE TREATMENT OF VIRAL INFECTIONS - This invention relates to 2-aminopyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections. | 2017-11-30 |
20170342036 | SIK INHIBITOR FOR USE IN A METHOD OF TREATING AN INFLAMMATORY AND/OR IMMUNE DISORDER - The present invention relates to the discovery that salt inducible kinases (SIKs) suppress the formation of anti-inflammatory molecules such as IL-10, which are important for the resolution of inflammation and identifies SIK inhibitors that may be used to treat disorders associated with undesirable inflammation, such as inflammatory bowel disease and/or autoimmune disorders. | 2017-11-30 |
20170342037 | A CRYSTAL FORM OF NEPTINIB di-P-METHYLBENZENESULFONATE, PREPARATION METHOD THEREOF, AND PHARMACEUTICAL COMPOSITION CONTAINING SAME - Provided is a composition of N-[4-[(3-chloro-4-fluorophenyl)amino]-7-[3-(ethoxy)-6-quinazolinyl]-4-(dimethylamino)-2-butenamide p-toluene sulfonate 1.5 hydrate α-polymorph. The α-polymorph has a stable form, a defined melting point, a good chemical stability, and a good endurance to high temperature and light irradiation, and is suitable for pharmaceutical use. | 2017-11-30 |
20170342038 | A METHOD FOR PREPARING GADOBUTROL - The present disclosure relates to a novel method for preparing high-purity gadobutrol. The present disclosure can be easily applied to a large scale production because purity of intermediate can be managed via simple and mild process and accordingly, high-purity or ultra high-purity gadobutrol that has higher purity than previous gadobutrol can be prepared in high yield therethrough. | 2017-11-30 |
20170342039 | CREATINE PRODRUGS, COMPOSITIONS AND METHODS OF USE THEREOF - The invention describes membrane permeable creatine prodrugs, pharmaceutical compositions comprising membrane permeable creatine prodrugs, and methods of treating diseases such as ischemia, heart failure, neurodegenerative disorders and genetic disorders affecting the creatine kinase system comprising administering creatine prodrugs or pharmaceutical compositions thereof. The invention also describes treating a genetic disease affecting the creatine kinase system, such as, for example, a creatine transporter disorder or a creatine synthesis disorder comprising administering creatine prodrugs or pharmaceutical compositions thereof. | 2017-11-30 |
20170342040 | NOVEL COMPOUNDS, SYNTHESIS METHOD THEREOF AND USE OF SAME IN MEDICINE AND IN COSMETICS - Novel compounds, synthesis methods and use of the same in medicine and in cosmetics are disclosed. Also disclosed, are novel compounds and ligands that modulate RARs. | 2017-11-30 |
20170342041 | METHODS OF CHEMICAL SYNTHESIS OF DIAMINOPHENOTHIAZINIUM COMPOUNDS INCLUDING METHYLTHIONINIUM CHLORIDE (MTC) - Methods of synthesizing and purifying certain 3,7-diamino-phenothiazin-5-ium compounds (referred to herein as “diaminophenothiazinium compounds”) including Methythioninium Chloride (MTC) (also known as Methylene Blue) are provided. | 2017-11-30 |
20170342042 | PROCESS FOR PRODUCING POLYVALENT GLYCIDYL COMPOUND - A polyvalent glycidyl compound is produced from a compound having one or more 2-alkenyl ether groups and two or more 2-alkenyl groups using a hydrogen peroxide aqueous solution as an oxidizing agent to oxidize the 2-alkenyl ether groups and the 2-alkenyl groups. A 2-alkenyl ether compound having two or more (un)substituted 2-alkenyl groups and one or more (un)substituted 2-alkenyl ether groups is oxidized using a hydrogen peroxide aqueous solution as an oxidizing agent in the presence of a tungsten compound and a quaternary ammonium salt as catalysts and of phosphoric acid as a co-catalyst, while controlling the pH of the reaction solution to 1.0-4.0 using an acid other than phosphoric acid. During the oxidation, the step of adding the hydrogen peroxide aqueous solution to the reaction solution and the step of adding the acid other than phosphoric acid thereto are alternately repeated at intervals two or more times. | 2017-11-30 |
20170342043 | FUMIGILLOL COMPOUNDS AND METHODS OF MAKING AND USING SAME - The disclosure provides fumagillol type compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of using, e.g. in the treatment of obesity are provided. | 2017-11-30 |
20170342044 | ISOFLAVONOID COMPOSITIONS AND METHODS FOR THE TREATMENT OF CANCER - Provided herein is a pharmaceutical composition comprising an isoflavonoid derivative and a cyclodextrin. Also provided herein are methods of treating cancer, sensitizing cancer cells, and inducing apoptosis in cancer cells by administering such compositions. In specific instances, provided herein are intravenous compositions and therapies. | 2017-11-30 |
20170342045 | KETAL ESTER COMPOUNDS AND USES THEREOF - The invention describes methods of preparation and compositions of plasticizers. The ketal diester products described are useful as components of polymer compositions. The products are excellent plasticizers for a variety of polymers, such as poly(vinylchloride) plastisols. | 2017-11-30 |
20170342046 | Fatty Acid Cysteine-Based Conjugates and Their Use in Treating Medical Disorders - The invention relates to fatty acid cysteine-based conjugates, compositions comprising a fatty acid cysteine-based conjugates, and methods for using such conjugates and compositions to treat disease, such as a disease caused by dysregulation of autophagy or mitochondrial bioenergetics. | 2017-11-30 |
20170342047 | Cancerous Cell Growth Inhibiting Compounds - The present invention provides a compound of Formula I, II or III or a salt or prodrug or derivative thereof that is useful for skin-whitening by inhibiting melanin formation and removing existing melanin and the inhibition of melanoma growth and/or the removal of existing melanoma cells. | 2017-11-30 |
20170342048 | GDF-8 Inhibitors - Described are GCF-8 inhibitors of the formula (I), | 2017-11-30 |
20170342049 | NOVEL 1,3,5 -TRIAZINE BASED PI3K INHIBITORS AS ANTICANCER AGENTS AND A PROCESS FOR THE PREPARATION THEREOF - The present invention describes heterocyclic compounds of general Formula 1 and their method of preparation thereof. The present invention describes general Formula 1 which inhibits phosphoinositide 3-kinase (PI3K) and can be used as the anticancer agents. | 2017-11-30 |
20170342050 | SOLID FORMS OF 3-(5-AMINO-2-METHYL-4-OXO-4H-QUINAZOLIN-3-YL)-PIPERIDINE-2,6-DIONE, AND THEIR PHARMACEUTICAL COMPOSITIONS AND USES - Solid forms comprising 3-(5-amino-2-methyl-4-oxo-4H-quinazolin-3-yl)-piperidine-2,6-dione, compositions comprising the solid forms, methods of making the solid forms and methods of their uses are disclosed | 2017-11-30 |
20170342051 | INDOLE AND PYRROLE COMPOUNDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Compounds of formula (I): | 2017-11-30 |
20170342052 | PYRROLIDINE OREXIN RECEPTOR ANTAGONISTS - The present invention is directed to pyrrolidine compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such diseases in which orexin receptors are involved. | 2017-11-30 |
20170342053 | CRYSTAL FORMS OF A CCR5 ANTAGONIST - The present disclosure relates to forms of a CCR5 inhibitory compound, (4,6-dimethylpyrimidin-5-yl)(4-((3S)-4-((1R)-2-methoxy-1-(4-(trifluoromethyl)phenyl)ethyl)-3-methyl-piperazin-1-yl)-4-methylpiperidin-1-yl)methanone. | 2017-11-30 |
20170342054 | COMPOUNDS AND METHODS OF USE THEREOF - Indole compounds are disclosed. Also disclosed are methods for using the compounds to treat human and animal disease, pharmaceutical compositions of the compounds, and kits including the compounds. | 2017-11-30 |
20170342055 | EGFR INHIBITOR COMPOUNDS - Disclosed herein are nitrogen-containing bicyclic compounds, together with pharmaceutical compositions and methods of ameliorating and/or treating a cancer described herein with one or more of the compounds described herein. | 2017-11-30 |
20170342056 | NOVEL COMPOUNDS - Imidazolone and pyrazolone derivatives of formula (I) described herein exhibit human neutrophil elastase inhibitory properties and are useful for the therapy of diseases and conditions in which HNE is implicated. | 2017-11-30 |
20170342057 | A PLURALITY OF HOST MATERIALS AND AN ORGANIC ELECTROLUMINESCENCE DEVICE COMPRISING THE SAME - The present invention relates to a plurality of host materials and an organic electroluminescent device comprising the same. By comprising a specific combination of a plurality of host compounds, the organic electroluminescent device according to the present invention provides high efficiency and long lifespan. | 2017-11-30 |
20170342058 | FUMAGILLOL HETEROCYCLIC COMPOUNDS AND METHODS OF MAKING AND USING SAME - Disclosed herein, in part, are fumagillol compounds and methods of use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making fumagillol compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2. | 2017-11-30 |
20170342059 | PYRIDINECARBOXAMIDE DERIVATIVES, PREPARATION METHOD THEREOF AND PHARMACEUTICAL USES THEREOF - Pyridinecarboxamide derivatives, preparation methods, and a pharmaceutical uses thereof are provided. In particular, pyridinecarboxamide derivatives represented by general formula (I), wherein the substituents of the formula (I) are defined in the specification are provided. Also provided are a preparation method for the pyridinecarboxamide derivatives of formula (I), a pharmaceutical composition containing the pyridinecarboxamide derivatives, and uses of the pyridinecarboxamide derivatives as therapeutic agents, especially as inhibitors of the Renal Outer Medullary Potassium channel (ROMK) and in the preparation of medicaments for treating and/or preventing hypertension and heart failure. | 2017-11-30 |
20170342060 | HETEROCYCLIC COMPOUNDS AS IMMUNOMODULATORS - Disclosed are compounds of Formula (I), methods of using the compounds as immunomodulators, and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders such as cancer or infections. | 2017-11-30 |
20170342061 | CRYSTAL FORM I OF CANAGLIFLOZIN AND PREPARATION METHOD THEREOF - Disclosed in the present invention is a crystal form I of Canagliflozin, and an X-ray powder diffraction spectrum of the crystal form I has characteristic diffraction peaks when 2θ is at the position of 4.4±0.2°, 8.4±0.2°, 16.8±0.2°, 17.5±0.2°, 18.0±0.2°, and 22.8±0.2°. The crystal form is physically and chemically stable and is suitable for manufacturing of various preparations. | 2017-11-30 |
20170342062 | INDAZOLE SULFONAMIDE DERIVATIVES AS INVERSE AGONISTS OF RETINOID-RELATED ORPHAN RECEPTOR GAMMA (ROR GAMMA (T)) - Indazole sulfonamide derivatives of formula (I), the pharmaceutically acceptable addition salts thereof, the hydrates and/or solvates thereof, and the use of same as inverse agonists of retinoid-related orphan receptor gamma RORγt are described. | 2017-11-30 |
20170342063 | BLOCKERS OF THE GROWTH HORMONE RECEPTOR IN DISEASE PREVENTION AND TREATMENT - Compounds and methods for treating diseases or conditions affected by the activity or expression of genes/proteins related to human GH, GHR, STAT | 2017-11-30 |
20170342064 | COMPOUNDS FOR THE TREATMENT OF CANCER - The present invention relates to prodrug derivatives of Mps-1 kinase inhibitors, and their use for the treatment and/or prophylaxis of diseases. | 2017-11-30 |
20170342065 | PESTICIDALLY ACTIVE HETEROCYCLIC DERIVATIVES WITH SULPHUR CONTAINING SUBSTITUENTS - Compounds of formulaI(I), wherein the substituents are as defined in claim | 2017-11-30 |
20170342066 | P2X7 MODULATORS - The present invention is directed to compounds of Formula (I), which includes enantiomer and diasteromers thereof: | 2017-11-30 |
20170342067 | THERAPEUTIC COMPOUNDS AND USES THEREOF - The present invention relates to compounds of formula (I): | 2017-11-30 |
20170342068 | COMPOUNDS FOR THE TREATMENT OF HEPATITIS B VIRUS INFECTION - The present disclosure generally relates to compounds and pharmaceutical compositions which may be used in methods of treating a hepatitis B virus infection. | 2017-11-30 |
20170342069 | NOVEL 2-OXO-6, 7-DIHYDROBENZO[a]QUINOLIZINE-3-CARBOXYLIC ACID DERIVATIVES FOR THE TREATMENT AND PROPHYLAXIS OF HEPATITIS B VIRUS INFECTION - The invention provides novel compounds having the general formula: | 2017-11-30 |
20170342070 | CYCLOPROPYLAMINES AS LSD1 INHIBITORS - The present invention is directed to cyclopropylamine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer. | 2017-11-30 |
20170342071 | MACROCYCLIC FACTOR XIA INHIBITORS CONDENSED WITH HETEROCYCLES - The present invention provides compounds of Formula (Ia): | 2017-11-30 |
20170342072 | SUBSTITUTED 6-ANILINO-9-HETEROCYCLYLPURINE DERIVATIVES FOR INHIBITION OF PLANT STRESS - The invention relates to substituted 6-anilino-9-heterocyclylpurine derivatives of formula I wherein R denotes one to five substituents independently selected from the group hydrogen, halogen, hydroxy, amino, alkyloxy and alkyl group, R2 is selected from the group comprising amino, halogen, hydroxy, thio, and alkylthio group, Cyc is five- or six-membered heterocyclic ring containing one oxygen atom. The derivatives are useful for inhibition of plant stress. | 2017-11-30 |
20170342073 | SMALL-MOLECULE HSP90 INHIBITORS - Hsp90 inhibitors havin are rovided havin the formula: (I) with a 2′,4′,5′-substitution pattern on the right-side aryl moiety. X1 represents two substituents, which may be the same or different, disposed in the 4′ and 5′ positions on the aryl group, wherein X1 is selected from halogen, alkyl, alkoxy, halogenated alkoxy, hydroxyalkyl, pyrollyl, optionally substituted aryloxy, alkylamino, dialkylamino, carbamyl, amido, alkylamido dialkylamido, acylamino, alkylsulfonylamido, trihalomethoxy, trihalocarbon, thioalkyl, SO | 2017-11-30 |
20170342074 | OPTIONALLY FUSED HETEROCYCLYL-SUBSTITUTED DERIVATIVES OF PYRIMIDINE USEFUL FOR THE TREATMENT OF INFLAMMATORY, METABOLIC, ONCOLOGIC AND AUTOIMMUNE DISEASES - Disclosed are compounds active towards nuclear receptors, pharmaceutical compositions containing the compounds and use of the compounds in therapy. | 2017-11-30 |
20170342075 | Salt of Pyrrolo[2,3-D]pyrimidine Compound and Novel Polymorph of Salt - The present invention relates to novel crystalline forms of 7-cyclopentyl-2-(5-piperazin-1-yl-pyridin-2-ylamino)-7H-pyrrolo[2,3-d]pyrimidine-6-car boxylic acid dimethylamide(compound I), its salts, and process for preparation thereof. Crystalline forms in the present invention have good stability, low hygroscopicity, good processability, easy treatability and other favorable properties. In addition, the process is simple, low cost, and has an important value for future optimization and development of the drug. | 2017-11-30 |
20170342076 | TERTIARY ALCOHOL IMIDAZOPYRAZINE BTK INHIBITORS - The present invention provides Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, Formula I or to pharmaceutical compositions comprising these compounds and to their use in therapy. In particular, the present invention relates to the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders. | 2017-11-30 |
20170342077 | DIAZENE DIRECTED MODULAR SYNTHESIS OF COMPOUNDS WITH QUATERNARY CARBON CENTERS - Diazene-directed modular synthesis is described for the preparation Csp2-Csp3 and Csp3-Csp3 linkages where one or more stereogenic quaternary carbon centers are formed. The disclosed methods are directed to the preparation of compounds of Formula (I), or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, from compounds of Formula (II): | 2017-11-30 |
20170342078 | HETEROCYCLIC INHIBITORS OF PTPN11 - The present invention relates to compounds which may be useful as inhibitors of PTPN11 for the treatment or prevention of cancer and other PTP-mediated diseases. Disclosed herein are new compounds and compounds based on pyrazolopyrazines and their application as pharmaceuticals for the treatment of disease. | 2017-11-30 |
20170342079 | COMPOUNDS AND METHODS FOR ANTIVIRAL TREATMENT - Compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections are provided. The compounds and compositions are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections. | 2017-11-30 |
20170342080 | PYRAZINO[2,3-b]PYRAZINE mTOR KINASE INHIBITORS FOR ONCOLOGY INDICATIONS AND DISEASES ASSOCIATED WITH THE mTOR/PI3K/AKT PATHWAY - Provided herein are Heteroaryl Compounds having the following structure: | 2017-11-30 |
20170342081 | TRIAZOLO[4,5-D] PYRAMIDINE DERIVATIVES AND THEIR USE AS PURINE RECEPTOR ANTAGONISTS - Compounds of formula (I) that are capable of acting as purine receptor antagonists, pharmaceutical compositions including the compounds, and methods of making the compounds, are disclosed. The compounds and compositions can be used in treating or preventing disorders related to purine receptor hyperfunctioning. | 2017-11-30 |
20170342082 | [8-(PHENYLSULFONYL)-3,8-DIAZABICYCLO[3.2.1]OCT-3-YL](1H-1,2,3-TRIAZOL-4-YL- )METHANONES - The present invention covers [8-(phenylsulfonyl)-3,8-diazabicyclo[3.2.1]oct-3-yl](1H-1,2,3-triazol-4-yl)methanone compounds of general formula (I): | 2017-11-30 |
20170342083 | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-ALPHA]PYRROLO[2,3-E]-PYRAZIN-8-YL)-N-(2- ,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF - The present disclosure relates to processes for preparing (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-c]pyrrolo[2,3-e]pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide, solid state forms thereof, and corresponding pharmaceutical compositions, methods of treatment (including treatment of rheumatoid arthritis), kits, methods of synthesis, and products-by-process. | 2017-11-30 |
20170342084 | REDUCTION OF ALPHA, BETA-UNSATURATED KETONE LEVELS IN MORPHINAN DERIVATIVE COMPOSITIONS - The disclosure relates to processes for reducing the amount of a compound of formula (I) or a salt or a solvate thereof present in a composition comprising compounds of formulae (I) and (II) or a salt or a solvate thereof. | 2017-11-30 |
20170342085 | ANTIVIRAL COMPOUNDS - The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds. | 2017-11-30 |
20170342086 | Compounds and methods for the treatment of drug resistance in cancer cells against paclitaxel - The disclosure provides compounds and methods for treating cancer by inhibiting the formation of cancer cells resistant to paclitaxel by preventing the formation of GBP1:PIM1 protein interaction during a chemotherapeutic treatment. These compounds and methods are able to treat cancer individually or in conjunction with paclitaxel. | 2017-11-30 |
20170342087 | BIS-THIENOBENZOTHIENOTHIPOHENE COMPOUNDS AND PROCESS FOR THEIR PREPARATION - The present invention relates to bis-thienobenzothienothiophene compounds and a process for their preparation. More in particular, the present invention relates to a new angular bis-thienobenzothienothiophene compound and the process for its preparation wherein said process comprises reacting at least one dihalogenated dithiophene compound with at least one terminal alkyne and the subsequent double annulation reaction. Said bis-thienobenzothienothiophene compounds can be appropriately functionalized and polymerized to produce electron donor compounds that can be advantageously used in the construction of photovoltaic devices or semiconductor polymers. Furthermore, said bis-thienobenzothienothiophene compounds, after functionalization, may be advantageously used as spectral converters in luminescent solar concentrators. | 2017-11-30 |
20170342088 | NOVEL ULK1 INHIBITORS AND METHODS USING SAME - In certain aspects, the invention provides a method for treating a disease or condition in a subject, the method comprising co-administering to a subject in need thereof a therapeutically effective amount of at least one ULK1-inhibiting pyrimidine, and a therapeutically effective amount of an mTOR inhibitor. | 2017-11-30 |
20170342089 | NOVEL COMPOUNDS AS MODULATORS OF GPR-119 - The present invention relates to novel compounds of formula (A) and (B) as modulators of GPR-119, methods of preparing them, pharmaceutical compositions containing them and methods of treatment, prevention and/or amelioration of GPR-119 mediated diseases or disorders with them. | 2017-11-30 |
20170342090 | Lanthanide Toolbox for Organelle Specific Molecular Imaging - The present invention relates to a water-soluble, simple, stable tris(N-(tert-butyl)acetamide) cyclen-based europium complex HGEu001 which exhibits the specific subcellular localization in the primary cilium with a quantum yield as high as 10% in water and a lifetime of 0.56 ms lifetime. In particular, the present invention provides simplicity of the design and synthesis of a complex. Comprehensive studies were performed in numerous cell lines, such as HeLa, SN-K-SH and MRC | 2017-11-30 |
20170342091 | NEAR-INFRARED ABSORPTION COMPOSITION, CURED FILM, NEAR-INFRARED CUT FILTER, SOLID-STATE IMAGING DEVICE, INFRARED SENSOR, AND COMPOUND - To provide a near-infrared absorption composition which contains a squarylium compound having excellent solvent solubility, a cured film which uses the near-infrared absorption composition, a near-infrared cut filter, a solid-state imaging device, an infrared sensor, and a compound. A near-infrared absorption composition includes a compound represented by the following Formula (1) and a resin. R | 2017-11-30 |
20170342092 | BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections. | 2017-11-30 |
20170342093 | BETA-LACTAMASE INHIBITORS - Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections. | 2017-11-30 |
20170342094 | HETEROARYL INHIBITORS OF PDE4 - The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of inflammatory diseases and other diseases involving elevated levels of cytokines and proinflammatory mediators. | 2017-11-30 |
20170342095 | ORGANOFUNCTIONAL SILICON PARTICLES, PROCESS FOR THE PRODUCTION THEREOF AND USE THEREOF - Organofunctional silicon particles are covalently functionalized on their surface with at least one organic compound, for example a plurality of —O—(C | 2017-11-30 |
20170342096 | LENS OIL HAVING A NARROW MOLECULAR WEIGHT DISTRIBUTION FOR INTRAOCULAR LENS DEVICES - A silicone oil having a mean molecular weight average greater than about 20,000 Daltons, with no more than about 3% to about 4% of the total silicone oil by weight being comprised of components having a molecular weight less than about 15,000 Daltons. In some embodiments, the silicone oil is used in intraocular lens devices. | 2017-11-30 |
20170342097 | METHODS AND COMPOSITIONS TO TREAT TYPE-1 AND TYPE-2 DIABETES - The present disclosure is directed to novel methods of treating type-1 or type-2 diabetes by inactivating TLR2 and TLR4 genes together in cells capable of producing insulin and/or regenerating β cells, and providing the cells to a subject in need thereof. | 2017-11-30 |
20170342098 | Pyridine-Oxyphenyl Coordinated Iridium (III) Complexes and Methods of Making and Using - Iridium (III) complexes are described together with methods to prepare and use such complexes. Also described are devices that utilize the iridium (III) complexes. | 2017-11-30 |
20170342099 | Bicyclic Bridged Metallocene Compounds and Polymers Produced Therefrom - Disclosed herein are catalyst compositions containing bicyclic bridged metallocene compounds. These catalyst compositions can be used for the polymerization of olefins. For example, ethylene polymers produced using these catalyst compositions can be characterized by low molecular weights and high melt flow rates, and can be produced without the addition of hydrogen. | 2017-11-30 |
20170342100 | PROCESSES FOR THE PREPARATION OF ERTUGLIFLOZIN - The present invention relates to processes for the preparation of ertugliflozni. The present invention also provides compounds of Formula (III), Formula (IV), and Formula (VII), processes for their preparation, and their use for the preparation of ertugliflozin. The processes of the present invention involve protecting the ertugliflozin intermediate compound with a suitable protecting group which provides ertugliflozin having high purity and yield. | 2017-11-30 |
20170342101 | SYNTHETIC BILE ACID COMPOSITIONS AND METHODS - Bile acids and related compositions and methods of synthesis and use. More specifically, deoxycholic acid and related compositions, said compositions being free of all moieties of animal origin and free of pyrogenic moieties. | 2017-11-30 |
20170342102 | COMPOSITIONS AND METHODS FOR TREATING CNS DISORDERS - Described herein are neuroactive steroids of the Formula (II): or a pharmaceutically acceptable salt thereof; wherein A, R | 2017-11-30 |
20170342103 | 3,3 DISUBSTITUTED 19-NOR PREGNANE COMPOUNDS, COMPOSITIONS, AND USES THEREOF - Provided herein are 3,3-disubstituted 19-nor-steroidal compounds according to Formula (I) and (III): | 2017-11-30 |
20170342104 | COUPLING METHOD FOR PEPTIDE SYNTHESIS AT ELEVATED TEMPERATURES - An improved method for coupling amino acids into peptides or peptidomimetics is disclosed that includes the steps of combining an amino acid, a carbodiimide, an activator additive, and a base at less than 1 equivalent compared to the amino acid to be activated; and carrying out the activation and coupling at a temperature greater than 30° C. | 2017-11-30 |
20170342105 | METHOD OF PROTEIN MANUFACTURE - The present invention provides a novel method for manufacturing a protein, particularly where said protein is to be coupled with another molecule. The invention further provides a method for industrial scale protein manufacturing to obtain proteins, e.g., for therapeutic purposes. | 2017-11-30 |
20170342106 | METHOD OF MAKING PRODRUGS AND TARGETED THERAPEUTIC COMPOUNDS - Provided is a method for making the compound of Formula 1. Various compounds utilized in that method are also provided, as are methods of making those compounds. Also provided is a compound having the formula XO—CO—(CH | 2017-11-30 |
20170342107 | MELANOCORTIN LIGANDS AND METHODS OF USE THEREOF - Certain embodiments of the invention provide a compound of formula (I): | 2017-11-30 |
20170342108 | CELL PENETRATING STAPLED PEPTIDE, MANUFACTURING METHOD THEREFOR, AND USE THEREOF - The present invention relates to a stapled peptide, a preparation method thereof and the use thereof, and more specifically to an amphipathic alpha-helical stapled peptide comprising hydrophobic amino acids and hydrophilic amino acids, a preparation method thereof, and the use thereof for intracellular delivery of an active substance. | 2017-11-30 |
20170342109 | Natural IGM Antibodies and Inhibitors Thereof - The invention provides natural IgM antibody inhibitors that may be used to treat various inflammatory diseases or disorders. | 2017-11-30 |
20170342110 | GLYCOPEPTIDES AND USES THEREOF - The present disclosure provides a compound of Formula I or its stereoisomers, prodrugs and pharmaceutically acceptable salts thereof. The present disclosure also relates to process of preparation of vancomycin-sugar conjugates of Formula I, its stereoisomers, prodrugs, pharmaceutically acceptable salts thereof, and to pharmaceutical compositions containing them. The compounds of the present disclosure are useful in the treatment, prevention or suppression of diseases mediated by microbes. | 2017-11-30 |
20170342111 | Markers for the Diagnosis of Celiac Disease - The invention relates to isolated antibodies that bind to specific peptides and to their use in the diagnosis of celiac disease. | 2017-11-30 |
20170342112 | VACCINES AND VACCINE COMPONENTS FOR INHIBITION OF MICROBIAL CELLS - The invention encompasses components from microbial cells which are useful for antibody production, including peptides, polypeptides comprising these peptides, polynucleotides which encode these peptides or polypeptides, and antibodies directed to these peptides, polypeptides, or polynucleotides. The invention also encompasses to expression vectors and host cells for producing these peptides, polypeptides, polynucleotides, and antibodies. The invention further encompasses methods and compositions, especially vaccine compositions, for detecting, targeting, and inhibiting microbial cells, especially methanogen cells, using one or more of the disclosed peptides, polypeptides, polynucleotides, antibodies, expression vectors, and host cells. | 2017-11-30 |
20170342113 | RECOMBINANT H7 HEMAGGLUTININ AND USE THEREOF - A recombinant H7 hemagglutinin derived from Chinese hamster ovary (CHO) cell. The recombinant H7 hemagglutinin includes a H7 hemagglutinin domain, a GCN4-pII trimerization motif, and a His-tag. The recombinant H7 hemagglutinin can be prepared as a protective vaccine composition with a pharmaceutically acceptable adjuvant. H7 hemagglutinin specific antibodies are elicited, and protection against H7N9 influenza virus is provided. | 2017-11-30 |
20170342114 | NOVEL RHTB PROTEIN VARIANTS AND THE METHOD OF PRODUCING O-PHOSPHOSERINE USING THE SAME - The present invention relates to an RhtB (homoserine/homoserine lactone export transporter) protein variant having an enhanced ability to export O-phosphoserine (OPS) that is a precursor of L-cysteine, a polynucleotide encoding the protein, a vector comprising the polynucleotide, an OPS-producing microorganism comprising the protein variant, a method of producing O-phosphoserine using the microorganism, and a method for preparing cysteine or its derivatives, which comprises reacting O-phosphoserine, produced by the method above, with a sulfide in the presence of O-phosphoserine sulfhydrylase (OPSS) or a microorganism that expresses OPSS. | 2017-11-30 |
20170342115 | NOVEL RHTB PROTEIN VARIANTS AND THE METHOD OF PRODUCING O-PHOSPHOSERINE USING THE SAME - The present invention relates to an RhtB (homoserine/homoserine lactone export transporter) protein variant having an enhanced ability to export O-phosphoserine (OPS) that is a precursor of L-cysteine, a polynucleotide encoding the protein, a vector comprising the polynucleotide, an OPS-producing microorganism comprising the protein variant, a method of producing O-phosphoserine using the microorganism, and a method for preparing cysteine or its derivatives, which comprises reacting O-phosphoserine, produced by the method above, with a sulfide in the presence of O-phosphoserine sulfhydrylase (OPSS) or a microorganism that expresses OPSS. | 2017-11-30 |
20170342116 | TREATMENT OF ISCHEMIA - A system, including methods and compositions, for treatment of ischemia. | 2017-11-30 |
20170342117 | GHRELIN SPLICE VARIANT FOR TREATING NEURONAL DAMAGE,NEURODEGENERATIVE DISEASE, PARKINSONS DISEASE, ALZHEIMERS DISEASE, AND/OR DEPRESSION - The present disclosure relates, in one aspect, to use of ghrelin splice variant or an analogue thereat: or a ghrelin splice variant-like compound for the preparation of a medicament for one or more of: treatment and/or prevention of neuronal damage and/or neurodegeneration and, prophylaxis or treatment of neuronal damage and/or neurodegenerative disease, Parkinson's disease, Alzheimer's disease, depression stimulation of neuronal activity. A further aspect relates to a number of new ghrelin splice variant like compounds and uses thereof, as well as to pharmaceutical compositions and medical packaging comprising the new ghrelin splice variant-like compounds. | 2017-11-30 |
20170342118 | METHODS AND COMPOSITIONS FOR TREATING HEMOPHILIA - Disclosed herein are methods and compositions for insertion of transgene sequences encoding proteins involved in clotting into the genome of a cell for treating conditions including hemophilias. | 2017-11-30 |
20170342119 | CONSTRUCTION AND CHARACTERIZATION OF MULTIMERIC IL-15-BASED MOLECULES WITH CD3 BINDING DOMAINS - The invention features soluble fusion protein complexes comprising at least two soluble fusion proteins. For example, the first fusion protein is an anti-CD3 antibody covalently linked to an interleukin-15 (IL-15) polypeptide or functional fragment thereof. The second fusion protein comprises a binding domain that recognizes disease antigens, wherein this domain is covalently linked to a soluble interleukin-15 receptor alpha (IL-15Rα) polypeptide or a functional fragment thereof. One or both of the first and second fusion proteins further includes an immunoglobulin Fc domain or a functional fragment thereof, and the IL-15 domain of first fusion protein binds to the soluble IL-15Rα domain of the second fusion protein to form a soluble fusion protein complex. The invention further provides methods for making and using the complexes of the invention. | 2017-11-30 |
20170342120 | USE OF RELAXIN TO TREAT ATRIAL FIBRILLATION - Disclosed herein are methods of using relaxin polypeptides and analogs, or nucleic acid molecules encoding such polypeptides to treat or inhibit atrial fibrillation. | 2017-11-30 |
20170342121 | GLUCAGON/GLP-1 AGONISTS FOR THE TREATMENT OF OBESITY - This disclosure provides GLP-1/glue agon agonist peptides for the treatment of metabolic diseases, e.g., obesity. | 2017-11-30 |
20170342122 | Novel Oxyntomodulin Derivatives and Pharmaceutical Composition For Treating Obesity Comprising The Same - The present invention relates to a novel peptide showing more excellent activities on a glucagon like peptide-1 receptor and a glucagon receptor than native oxyntomodulin, and a composition for the prevention or treatment of obesity comprising the peptide as an active ingredient. Unlike native oxyntomodulin, the novel peptide of the present invention reduces food intake, suppresses gastric emptying, and facilitates lipolysis with reduced side-effects, and also shows excellent receptor-activating effects. Thus, it can be widely used in the treatment of obesity with safety and efficacy. | 2017-11-30 |