39th week of 2017 patent applcation highlights part 21 |
Patent application number | Title | Published |
20170275237 | COMPOUNDS AND MIXTURES WITH ANTIDEGRADANT AND ANTIFATIGUE EFFICACY AND COMPOSITIONS INCLUDING SAID COMPOUNDS - A compound represented by the formula: | 2017-09-28 |
20170275238 | METHODS OF MAKING COMPOUNDS AND MIXTURES HAVING ANTIDEGRADANT AND ANTIFATIGUE EFFICACY - Methods of making antidegradant compounds are disclosed in which a p-phenylenediamine is reacted with a diol to obtain mixtures comprising the antidegradant compounds. | 2017-09-28 |
20170275239 | COMPOUNDS AND MIXTURES WITH ANTIDEGRADANT AND ANTIFATIGUE EFFICACY AND COMPOSITIONS INLUDING SUCH COMPOUNDS - Antidegradant compounds are disclosed, and methods of making them, that are represented by the formula I: | 2017-09-28 |
20170275240 | METHOD FOR PREPARING CHIRAL gamma-SECONDARY AMINO ALCOHOL - A method for preparing chiral γ-secondary amino alcohol includes: adding into a solvent an acid addition salt of β-secondary amino ketone represented by general formula (1), an alkali, a metal salt additive and a diphosphine-rhodium complex, so as to carry out a reaction in a hydrogen atmosphere and obtain a chiral γ-secondary amino alcohol compound represented by general formula (2). In general formula (2), Ar represents an aryl group with or without substituent group(s), R represents an alkyl group or an aralkyl group, and HY represents an acid. The synthesis scheme has a simple process, the metal salt additive remarkably improves the effect of a rhodium-catalyzed asymmetric hydrogenation technology, and accordingly, the reaction yield and the optical purity of a product are improved, the production process is simplified, production costs are reduced, and the synthesis scheme is highly suitable for mass industrial production. | 2017-09-28 |
20170275241 | TRANSESTERIFICATION REACTION BY MEANS OF IRON CATALYST - Provided is a catalyst for transesterification reactions, which contains an iron salen complex. Also provided is a method for producing an ester compound, which is characterized by carrying out a transesterification reaction between a starting material ester and a starting material alcohol with use of the catalyst. | 2017-09-28 |
20170275242 | METHOD FOR PRODUCING CATIONIC LIPID - A method for producing a cationic lipid, wherein a cationic lipid represented by formula (1) is mixed with a tetraalkylammonium salt having X | 2017-09-28 |
20170275243 | Lipids and Lipid Compositions for the Delivery of Active Agents - This invention provides for a compound of formula (I), or a pharmaceutically acceptable salt thereof, wherein R | 2017-09-28 |
20170275244 | C7-Fluoro Substituted Tetracycline Compounds - The present invention is directed to a compound represented by Structural Formula (A): | 2017-09-28 |
20170275245 | Modularized System and Method for Urea Production Using Stranded Natural Gas - A modular system and method for producing urea from stranded natural gas includes removal of foreign particulate matter to obtain a substantially homogeneous gas. The gas is processed by controlling the quality of the stranded natural gas to maintain a substantially homogenous mixture The resultant gas stream is further cleaned and compressed to a high pressure of about 3,000 psi. The resultant ammonia stream is processed in a bypass recycling loop system at 30% conversion rate at a high pressure of about 6,000 to 7,000 psi. The equipment associated with each of the process steps may be skid mounted for portability and/or contained within the footprint of a standard 48-foot flatbed trailer. | 2017-09-28 |
20170275246 | NOVEL ANTAGONISTS OF THE GLUCAGON RECEPTOR - The present invention provides for novel compounds of Formula (I) and pharmaceutically acceptable salts and co-crystals thereof which have glucagon receptor antagonist or inverse agonist activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucagon receptor antagonist is indicated, including Type I and II diabetes, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formula I, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same. | 2017-09-28 |
20170275247 | METHOD FOR PRODUCING METHIONINE - A method for producing methionine involves contacting 2-amino-4-(methylthio)butanenitrile with water in the presence of an oxide catalyst containing cerium. The 2-amino-4-(methylthio)butanenitrile may be 2-amino-4-(methylthio)butanenitrile, produced by contacting 2-hydroxy-4-(methylthio)butanenitrile with ammonia water or 2-amino-4-(methylthio)butanenitrile, produced by contacting 3-(methylthio)propionaldehyde with hydrocyanic acid and ammonia water. | 2017-09-28 |
20170275248 | Carbondisulfide Derived Zwitterions - Amines and amine derivatives that improve the buffering range, and/or reduce the chelation and other negative interactions of the buffer and the system to be buffered. The reaction of amines or polyamines with various molecules to form polyamines with differing pKa's will extend the buffering range, derivatives that result in polyamines that have the same pKa yields a greater buffering capacity. Derivatives that result in zwitterionic buffers improve yield by allowing a greater range of stability. | 2017-09-28 |
20170275249 | SMALL LIPOPEPTIDOMIMETIC INHIBITORS OF GHRELIN O-ACYL TRANSFERASE - Compositions and methods are disclosed that relate to small molecule lipopeptidomimetic inhibitors of mammalian ghrelin O-acyl transferase (GOAT). Compounds of general Formula (I) and substructures thereof, i.e., Formulae (II), (IIa), (IIa1), (IIa2), (IIb), (IIb1), (IIb2), (IIc) and (III), are shown to exhibit potent inhibition of the octanoylation of ghrelin peptide, where the resulting non-octanoylated (des-acyl) form of ghrelin lacks GHSr ligand activity that is associated with weight gain and insulin resistance. These and related embodiments will find uses for treating subjects known to have, or suspected of being at risk for having, a condition that would benefit from a decreased level of acylated ghrelin peptide, such as type II diabetes, impaired glucose tolerance, insulin resistance, Prader-Willi syndrome (PWS) and obesity. | 2017-09-28 |
20170275250 | PIPERIDINE COMPOUNDS, PHARMACEUTICAL COMPOSITION COMPRISING THE SAME AND ITS USE - Piperidine compounds and pharmaceutically useful salts thereof, a pharmaceutical composition including an effective amount of the racemic or enantiomerically enriched piperidine compounds to treat gastrointestinal diseases, and a method of treating gastrointestinal diseases in a mammal are provided. | 2017-09-28 |
20170275251 | Malate salt of N-(4-phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and crystalline forms thereof for the treatment of cancer - Disclosed are malate salts of N-(4-{[6,7-bis(methyloxy)-quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclo-propane-1,1-dicarboxamide, including a (L)-malate salt, a (D)-malate salt, a (DL) malate salt, and mixtures thereof; and crystalline and amorphous forms of the malate salts. Also disclosed are pharmaceutical compositions comprising at least one malate salts of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)-cyclopropane-1,1-dicarboxamide; and methods of treating cancer comprising administering at least one malate salt of N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide. | 2017-09-28 |
20170275252 | ASYMMETRIC BISAMINOQUINOLINES AND BISAMINOQUINOLINES WITH VARIED LINKERS AS AUTOPHAGY INHIBITORS FOR CANCER AND OTHER THERAPY - The invention provides novel asymmetric and symmetric bisaminoquinolmes and related compounds, methods of treatment and syntheses. The novel compounds exhibit effective anticancer activity and are useful in the treatment of a variety of autophagy-related disorders. | 2017-09-28 |
20170275253 | BENZAZEPINE SULFONAMIDE COMPOUNDS - This invention relates to novel benzazepine sulfonamide compounds of the formula | 2017-09-28 |
20170275254 | PYRAZOLES - The invention relates to pyrazole derivatives which are NMDA NR2B receptor inhibitors, useful in treating central nervous system diseases. | 2017-09-28 |
20170275255 | CRYSTALLINE FORM OF ELTROMBOPAG FREE ACID - The present invention relates to crystalline form of Eltrombopag free acid and its process for preparation. | 2017-09-28 |
20170275256 | COMPOSITIONS AND METHODS FOR MODULATING FARNESOID X RECEPTORS - The present invention relates to compounds of Formula I, | 2017-09-28 |
20170275257 | 2-THIOPYRIMIDINONES - Myeloperoxidase inhibitor, pharmaceutical compositions containing the inhibitor and the use of the inhibitor to treat, for example, cardiovascular conditions. | 2017-09-28 |
20170275258 | METHOD FOR PRODUCING EPOXY COMPOUND CONTAINING HYDROGEN PEROXIDE STABILIZER - The present invention provides a method for producing an epoxy compound by a reaction of an olefin compound with hydrogen peroxide, wherein the epoxy compound is stably and safely produced using a hydrogen peroxide stabilizer for reducing an oxygen gas generated from hydrogen peroxide. A method for producing an epoxy compound by a reaction of an olefin compound with hydrogen peroxide, wherein the reaction is carried out in the presence of an organophosphorus compound in such a reaction medium that the pH is maintained within a range of more than 7.5 and less than 12.0. The olefin compound may be 1,3,5-tris-(alkenyl)-isocyanurate. The alkenyl group in the olefin compound may be 3-butenyl group, 4-pentenyl group, 5-hexenyl group, 6-heptenyl group, or 7-octenyl group. The epoxy compound may be 1,3,5-tris-(epoxyalkyl)-isocyanurate. The reaction medium may be such a reaction medium that the pH is maintained within a range of 8.0 to 10.5. | 2017-09-28 |
20170275259 | CRYSTALLINE(2S,4R)-5-(5'-CHLORO-2'-FLUORO-[1,1'-BIPHENY]-4-YL)-2-(ETHOXYME- THYL)-4-(3-HYDROXYISOXAZOLE-5-CARBOXAMIDO)-2-METHYLPENTANOIC ACID AND USES THEREOF - In one aspect, the invention relates to a crystalline form of the structure: | 2017-09-28 |
20170275260 | ALLOSTERIC MODULATORS OF NICOTINIC ACETYLCHOLINE RECEPTORS - The present disclosure relates to compounds of formula I that are useful as modulators of α7 nAChR, compositions comprising such compounds, and the use of such compounds for preventing, treating, or ameliorating disease, particularly disorders of the central nervous system such as cognitive impairments in Alzheimer's disease, Parkinson's disease, and schizophrenia, as well as for L-DOPA induced-dyskinesia and inflammation | 2017-09-28 |
20170275261 | 1,3,4-THIADIAZOLES HAVING A HERBICIDAL ACTIVITY, THEIR AGRONOMICAL COMPOSITIONS AND RELATIVE USE - The present invention relates to new thiadiazoles having general formula (I): | 2017-09-28 |
20170275262 | CYCLOPROPANE DERIVATIVES IN FLAVOR AND FRAGRANCE COMPOSITIONS - The present invention relates to novel cyclopropane derivatives represented by Formula I: | 2017-09-28 |
20170275263 | Compounds for the treatment of HPV-induced carcinoma - A compound of Formula 1 | 2017-09-28 |
20170275264 | CARBAMATE/UREA DERIVATIVES - The invention relates to compound of the formula I | 2017-09-28 |
20170275265 | 4-(3-CYANOPHENYL)-6-PYRIDINYLPYRIMIDINE MGLU5 MODULATORS - The disclosures herein relate to novel compounds of formula wherein R | 2017-09-28 |
20170275266 | HISTONE DEMETHYLASE INHIBITORS - Provided herein are substituted pyrazolylpyridine, pyrazolylpyridazine, and pyrazolylpyrimidine derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition histone demethylase. Furthermore, the subject compounds and compositions are useful for the treatment of cancer, such as prostate cancer, breast cancer, bladder cancer, lung cancer and/or melanoma and the like. | 2017-09-28 |
20170275267 | SUBSTITUTED CYCLOALKENOPYRAZOLES AS BUB1 INHIBITORS FOR THE TREATMENT OF CANCER - Compounds of formula (I), processes for their production and their use as Bub1 kinase inhibitors for the treatment of hyperproliferative diseases and/or disorders responsive to induction of cell death. | 2017-09-28 |
20170275268 | HETEROARYL SUBSTITUTED INDAZOLES - Compounds of formula (I), which are inhibitors of Bub 1 kinase, processes for their production and their use as pharmaceuticals. | 2017-09-28 |
20170275269 | BENZYL SUBSTITUTED INDAZOLES AS BUB1 KINASE INHIBITORS - Compounds of formula (I) and their use as pharmaceuticals. | 2017-09-28 |
20170275270 | BENZYL SUBSTITUTED INDAZOLES - Compounds of formula (I) and their use as pharmaceuticals. | 2017-09-28 |
20170275271 | 6-(5-HYDROXY-1H-PYRAZOL-1-YL)NICOTINAMIDE INHIBITORS OF PHD - The present invention provides compounds of the formula: | 2017-09-28 |
20170275272 | 6-HYDROXY-4-OXO-1,4-DIHYDROPYRIMIDINE-5-CARBOXAMIDES AS APJ AGONISTS - The present invention provides compounds of Formula (I): | 2017-09-28 |
20170275273 | ESTROGEN RECEPTOR MODULATORS AND USES THEREOF - Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors. | 2017-09-28 |
20170275274 | ISOQUINOLINE DERIVATIVES USEFUL AS INHIBITORS OF DIACYLGLYCERIDE O-ACYLTRANSFERASE 2 - The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio-renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions. | 2017-09-28 |
20170275275 | BENZENESULFONAMIDES USEFUL AS SODIUM CHANNEL INHIBITORS - The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to a new sulfonamide Nav1.7 inhibitors of formula (I), or a pharmaceutically acceptable salt thereof, wherein X, R | 2017-09-28 |
20170275276 | N-PYRIDINYL ACETAMIDE DERIVATIVES AS INHIBITORS OF THE WNT SIGNALING PATHWAY - Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment. | 2017-09-28 |
20170275277 | NEW BICYCLIC DERIVATIVES HAVING BETA2 ADRENERGIC AGONIST AND M3 MUSCARINIC ANTAGONIST ACTIVITIES - The present invention relates to novel compounds having β2 adrenergic agonist and M3 muscarinic antagonist dual activity, to pharmaceutical compositions containing them, to the process for their preparation and to their use in respiratory therapies. | 2017-09-28 |
20170275278 | Mammalian and Bacterial Nitric Oxide Synthase Inhibitors - Disclosed are compounds that are shown to inhibit the biological activity of nitric oxide synthases (NOSs). Also disclosed are pharmaceutical compositions comprising the compounds, and methods of using the compounds and pharmaceutical compositions for treating a subject in need thereof. Because the disclosed compounds are shown to inhibit the activity of nitric oxide synthases (NOSs), the disclosed compounds and pharmaceutical compositions may be utilized in methods for treating a subject having or at risk for developing a disease or disorder that is associated with NOS activity. | 2017-09-28 |
20170275279 | SPECIFIC INHIBITORS OF METHIONYL-TRNA SYNTHETASE - The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS. | 2017-09-28 |
20170275280 | NOVEL CAPSAZEPINE ANALOGS FOR THE TREATMENT OF CANCER AND OTHER PROLIFERATIVE DISEASES - The present disclosure relates generally to derivatives of capsazepine and methods of use thereof In some aspects, the present disclosure relates to using capsazepine derivatives to treat cancer or other hyperproliferative diseases. In some aspects of the present disclosure, the disclosure provides capsazepine derivatives which may be useful in the treatment of cancer. Such cancers that the compounds may be used to treating include but are not limited to breast, cervical, oral, head, neck, or prostate cancer. In some aspects, the compounds may be useful in treating a tumor by direct injection of the compound into the tumor, particularly an oral tumor. In other aspects, the compounds are administered systemically. The compounds of the present disclosure may also be used to treat the pain associated with a tumor for which it is being administered. | 2017-09-28 |
20170275281 | IMIDAZO[4,5-C]PYRIDINE DERIVED SSAO INHIBITORS - A compound of formula (I) or a pharmaceutically acceptable salt, or N-oxide thereof and the use of the same in therapy: wherein Z, Y, R | 2017-09-28 |
20170275282 | FACTOR XIA-INHIBITING PYRIDOBENZAZEPINE AND PYRIDOBENZAZOCINE DERIVATIVES - The invention relates to substituted pyridobenzazepine and pyridobenzazocine derivatives and to processes for preparation thereof, and also to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders. | 2017-09-28 |
20170275283 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. | 2017-09-28 |
20170275284 | Macrocyclic Compounds as IRAK1/4 Inhibitors and Uses Thereof - The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors. | 2017-09-28 |
20170275285 | INHIBITING THE TRANSIENT RECEPTOR POTENTIAL A1 ION CHANNEL - The present invention relates to pharmaceutical compounds of the Formula (I), or a pharmaceutically acceptable salt or composition thereof, and methods of their use for the treatment of pain, respiratory conditions, as well as inhibiting the Transient Receptor Potential A1 ion channel (TRPA1). | 2017-09-28 |
20170275286 | Novel Sulfonimidoylpurinone Compounds and Derivatives for the Treatment and Prophylaxis of Virus Infection - The present invention relates to compounds of formula (I), | 2017-09-28 |
20170275287 | NOVEL N2, N4, N7, 6-TETRASUBSTITUTED PTERIDINE-2,4,7-TRIAMINE AND 2, 4, 6, 7-TETRASUBSTITUTED PTERIDINE COMPOUNDS AND METHODS OF SYNTHESIS AND USE THEREOF - Compounds as immune system modulators bearing a pteridine core are described. A pharmaceutical composition comprising the same, methods of making the same, and a method for treating or preventing autoimmunity disease using the same are described. | 2017-09-28 |
20170275288 | PTERIDINES USEFUL AS HCV INHIBITORS AND METHODS FOR THE PREPARATION THEREOF - The present invention relates to the use of pteridines as inhibitors of HCV replication as well as their use in pharmaceutical compositions aimed to treat or combat HCV infections. In addition, the present invention relates to compounds per se and their use as medicines. The present invention also concerns processes for the preparation of such compounds, pharmaceutical compositions comprising them, and combinations of said compounds with other anti-HCV agents. | 2017-09-28 |
20170275289 | THERAPEUTIC COMPOUNDS AND USES THEREOF - The present invention relates to methods for treating PCAF and GCN5 mediated disorders using a compound of formula (I) or a pharmaceutically acceptable salt thereof: | 2017-09-28 |
20170275290 | PYRROLOTRIAZINE COMPOUNDS AS TAM INHIBITORS - This application relates to compounds of Formula I: | 2017-09-28 |
20170275291 | INDAZOLE COMPOUNDS AS FGFR KINASE INHIBITOR, PREPARATION AND USE THEREOF - The present invention provides an indazole compound as a FGFR kinase inhibitor, preparation and use thereof. Specifically, the present invention provides a compound represented by formula (I), wherein the definitions of each group are described in the specification. The compound of the present invention has good FGFR kinase-inhibiting activity, and can be used in preparing a series of medicines for treating FGFR kinase activity related diseases. | 2017-09-28 |
20170275292 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I: (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. | 2017-09-28 |
20170275293 | Novel Alpha-Hydroxy Carboxylic Acid and Derivatives and Other GRAS Based Prodrugs of Oxycodone and Uses thereof - The invention describes pharmaceutical compounds and compositions comprised of a ligand attached to the opioid oxycodone, in a manner that substantially decreases or deters the potential for opioid abuse, addiction, illicit and illegal use, and overdose. When delivered at the proper dosage, the pharmaceutical composition provides therapeutic activity similar to that of the parent active agent. | 2017-09-28 |
20170275294 | Nalmefene Salts as Medicaments for Reducing Alcohol Consumption or for Preventing Excessive Alcohol Consumption - The present invention relates to new nalmefene salts which salts fall within at least one of the two following categories: non-hydrate forming salts and non-solvate forming salts. In particular, the invention relates to the hydrogen adipate salt, the hydrogen malonate salt, the lactate salt, the hydrogen fumarate salt, the hydrogen succinate salt, the benzene sulfonate salt, the hydrogen maleate salt and the salicylate salt of nalmefene. The present invention also relates to such salts for use in therapy. | 2017-09-28 |
20170275295 | METHOD FOR CONDITIONING A DIANHYDROHEXITOL, AQUEOUS SOLUTION OF CONDITIONED DIANHYDROHEXITOL, AND USES THEREOF - The invention relates to a method for conditioning a dianhydrohexitol in the form of an aqueous solution in a container comprising a polyolefin-based layer. The invention also relates to the aqueous solution of thus-conditioned dianhydrohexitol, and to all the uses thereof, in particular those intended for food and pharmaceutical purposes. | 2017-09-28 |
20170275296 | THERAPEUTIC AGENT FOR MOTOR DISORDERS - Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R | 2017-09-28 |
20170275297 | INHIBITORS OF IRAK4 ACTIVITY - The present invention relates to inhibitors of IRAK4 of Formula (I) and provides compositions comprising such inhibitors, as well as methods therewith for treating IRAK4-mediated or -associated conditions or diseases. | 2017-09-28 |
20170275298 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula I and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. | 2017-09-28 |
20170275299 | PREPARATION METHOD FOR BENZOXAZOLEOXAZINE KETONE COMPOUND AND INTERMEDIATE AND CRYSTAL FORM THEREOF - A preparation method for a high-purity benzoxazoleoxazine ketone compound, a crystal form thereof, and an intermediate compound for preparing a compound of formula (I), and a preparation method therefor. | 2017-09-28 |
20170275300 | SYNTHESIS OF CEPHALOSPORIN COMPOUNDS - Provided herein is a method for the synthesis of cephalosporin antibiotic compounds comprising a palladium-catalyzed coupling reaction. Provided herein are methods for the synthesis of cephalosporin compounds of formula (I) employing a palladium-catalyzed alkylation reaction, as well as compositions related to the same. In an aspect, provided herein is a method for preparing a compound of formula (II), or a salt thereof, comprising the step of admixing, e.g., reacting, a compound of formula (III), or a salt thereof, with a nucleophile (Nuc) in the presence of reagents comprising: (a) a palladium source; and (b) a palladium-binding ligand, to form a compound of formula (II), or a salt thereof. | 2017-09-28 |
20170275301 | Benzenesulfonyl-Asymmetric Ureas and Medical Uses Thereof - Benzenesulfonyl-asymmetric ureas are provided for the treatment of conditions modulated by the ghrelin receptor. | 2017-09-28 |
20170275302 | INHIBITORS OF THE RENAL OUTER MEDULLARY POTASSIUM CHANNEL - The present invention provides compounds of Formula (I) and the pharmaceutically acceptable salts thereof, which are inhibitors of the ROMK (Kir1.1) channel. The compounds may be used as diuretic and/or natriuretic agents and for the therapy and prophylaxis of medical conditions including cardiovascular diseases such as hypertension, heart failure and chronic kidney disease and conditions associated with excessive salt and water retention. | 2017-09-28 |
20170275303 | CHIRAL BINUCLEAR METAL COMPLEXES FOR STEREOSELECTIVE GLYCOSIDE HYDROLYSIS OF SACCHARIDES - Disclosed herein is a class of chiral binuclear metal complexes for stereoselective glycoside hydrolysis of saccharides, and more particular chiral binuclear transition metal complex catalysts that discriminate epimeric glycosides and α- and β-glycosidic bonds of saccharides in aqueous solutions at near physiological pHs. The chiral binuclear metal complexes include a Schiff-base-type ligand derived from a chiral diamino building block, and a binuclear transition metal core, each which can be varied for selectivity. The metal core is a Lewis-acidic metal ion, such as copper, zinc, lanthanum, iron and nickel. The Schiff-base may be a reduced or non-reduced Schiff-base derived from aliphatic linear, aliphatic cyclic diamino alcohols or aromatic aldehydes. The ligand can be a penta- or heptadentate ligand derived from pyridinecarbaldehydes, benzaldehydes, linear or cyclic diamines or diamino alcohols. | 2017-09-28 |
20170275304 | HIGHLY DISPERSIBLE ANTIMICROBIAL AND ADHESION AGENTS - Compositions of matter that have antimicrobial properties and adhesion properties and are highly dispersible in aqueous solutions. The presence of a large number of silanols on the molecules of this invention creates a solubility or disperseability of these molecules in aqueous solutions that is not obtainable from prior art antimicrobial monomers. | 2017-09-28 |
20170275305 | METHOD FOR PRODUCING POLYALKYLENE GLYCOL DERIVATIVE HAVING AMINO GROUP AT END, POLYMERIZATION INITIATOR FOR USE IN THE SAME, AND ALCOHOL COMPOUND AS RAW MATERIAL FOR THE POLYMERIZATION INITIATOR - A method for producing a narrowly distributed and high-purity polyalkylene glycol derivative having an amino group at an end, a polymerization initiator for use in the method, and a precursor of the polymerization initiator are provided. | 2017-09-28 |
20170275306 | Method For Producing Aryl-Functional Silanes - A method for preparing a reaction product including an aryl-functional silane includes sequential steps (1) and (2). Step (1) is contacting, under silicon deposition conditions, (A) an ingredient including (I) a halosilane such as silicon tetrahalide and optionally (II) hydrogen (H | 2017-09-28 |
20170275307 | PREPARATION OF FLUOROSILICON COMPOUNDS - Methods of synthesizing fluorosilanes containing cyano-substituted alkyl groups are provided. For example, 3-cyano-propyldimethylfluorosilane may be produced by reacting tetramethyldisiloxane and boron trifluoride to obtain fluorodimethylsilane and then reacting the fluorodimethylsilane with allyl cyanide, in the presence of a hydrosilylation catalyst | 2017-09-28 |
20170275308 | Process For Production of Halosilanes From Silicon-Containing Ternary Intermetallic Compounds - A process for preparing a reaction product including a halosilane includes: contacting an unsaturated hydrocarbyl halide and a ternary intermetallic compound at a temperature of 300° C. to 700° C. to form the reaction product. The ternary intermetallic compound includes copper, silicon and a transition metal. The halosilane in the reaction product has formula R1 | 2017-09-28 |
20170275309 | NOVEL ORGANIC TITANIUM COMPOUND, METHOD FOR PRODUCING SAME, AND ROOM TEMPERATURE-CURABLE RESIN COMPOSITION - The present invention provides: a novel organic titanium compound having an effect as an adhesion promoter by itself; a production method of such organic titanium compound; and a room temperature-curable resin composition containing such organic titanium compound both as a curing catalyst and as an adhesion promoter. Provided are an organic titanium compound represented by an average composition formula (I): | 2017-09-28 |
20170275310 | ELECTROLYTIC SOLUTION AND NOVEL FLUORINATED PHOSPHORIC ACID ESTER - The present invention provides a novel electrolyte solution capable of providing electrochemical devices having a high storage capacity retention. The electrolyte solution of the present invention contains a fluorinated phosphoric acid ester containing a non-fluorinated alkylene group having one or more carbon atoms as a linking group. | 2017-09-28 |
20170275311 | NON-AQUEOUS LIQUID ELECTROLYTE, ELECTRICITY STORAGE DEVICE USING SAME, AND PHOSPHORUS COMPOUND USED THEREIN - The present invention is concerned with a nonaqueous electrolytic solution having an electrolyte salt dissolved in a nonaqueous solvent, the nonaqueous electrolytic solution containing a compound represented by the following general formula (X), in which a polar group (X) is bound to a phosphorus atom (P), and capable of improving electrochemical characteristics in a broad temperature range; an energy storage device using the same; and a novel compound. | 2017-09-28 |
20170275312 | PHOSPHINIC VANADIUM COMPLEX, CATALYTIC SYSTEM COMPRISING SAID PHOSPHINIC VANADIUM COMPLEX AND PROCESS FOR THE (CO) POLYMERIZATION OF CONJUGATED DIENES - Vanadium phosphinic complex having general formula (I) or (II): V(X)M3P̂WFys-nMO V(X)3[(R3)2P(R4)P(R3)2] (ID wherein: X represents an anion selected from halogens such as, for example, chlorine, bromine, iodine, preferably chlorine; or is selected from the following groups: thiocyanate, isocyanate, sulfate, acid sulfate, phosphate, acid phosphate, carboxylate, dicarboxylate; Ri, identical or different among them, represent a hydrogen atom, or an allyl group (CH2=CH—CH2-); or are selected from alkyl groups CrC2o, preferably CrĈ, linear or branched, optionally halogenated, optionally substituted cycloalkyl groups; —n is an integer ranging from 0 to 3; R2, identical or different among them, are selected from optionally substituted aryl groups; R3, identical or different among them, represent a hydrogen atom, or an allyl group (CH2=CH—CH2-); or are selected from alkyl groups C1-C2o, preferably CrĈ, linear or branched, optionally halogenated, optionally substituted cycloalkyl groups, optionally substituted aryl groups; R4 represents a group —NR5 wherein R5 represents a hydrogen atom, or is selected from C1-C20 alkyl groups, preferably CrC15, linear or branched; or R4 represents an alkylene group —(CH2) p- wherein p represents an integer ranging from 1 to 5; provided that in the general formula (I), in case n is equal to 1 and Ri is methyl, R2 is different from phenyl. Said phosphinic vanadium complex having general formula (I) or (II) can be advantageously used in a catalytic system for the (co)polymerization of conjugated dienes. | 2017-09-28 |
20170275313 | MODIFIED MITO-METFORMIN COMPOUNDS AND METHODS OF SYNTHESIS AND USE THEREOF - The present invention provides mito-metformin compounds, pharmaceutical compositions thereof, and methods of using the mito-metformin compounds in the treatment of cancer. | 2017-09-28 |
20170275314 | ALKYLIDENE PHOSPHONATE ESTERS AS P-GLYCOPROTEIN INDUCERS - The present invention relates to the alkylidene phosphonate esters of formula I wherein, R | 2017-09-28 |
20170275315 | FORMS OF R)-3-(4-(2-(2-METHYLTETRAZOL-5-YL)PYRIDIN-5-YL)-3-FLUOROPHENYL)-5- -HYDROXYMETHYL OXAZOLIDIN-2-ONE DIHYDROGEN PHOSPHATE - A crystalline form of crystalline (R)-3-(4-(2-(2-methyltetrazol-5-yl)-pyridin-5-yl)-3-fluorophenyl)-5-hydroxymethyl oxazolidin-2-one dihydrogen phosphate, methods of making the crystalline form and pharmaceutical compositions comprising the crystalline form are useful antibiotics. Further, the derivatives of the present invention may exert potent antibacterial activity versus various human and animal pathogens, including Gram-positive bacteria such as | 2017-09-28 |
20170275316 | BISPHOSPHITES HAVING AN UNSYMMETRIC OUTER BIPHENOL UNIT - Bisphosphites having at least one unsymmetric outer biphenol unit are useful for the hydroformylation of an olefin. | 2017-09-28 |
20170275317 | COMPLEXES AND METHODS FOR THEIR PREPARATION - Disclosed are methods for the preparation of ligands for complexes, methods for preparing complexes and complexes having those ligands. Also provided is the use of a complex as a catalyst in a method of synthesis. | 2017-09-28 |
20170275318 | SOLID-SUPPORTED PALLADIUM (II) COMPLEX AS A HETEROGENEOUS CATALYST FOR CROSS COUPLING REACTIONS AND METHODS THEREOF - A solid-supported catalyst ligand which chelates palladium (II) species to form a complex that functions as a heterogeneous catalyst that is stable and can be recycled without significantly losing any catalytic activity in a variety of chemical transformations, a method for producing the solid-supported catalyst ligand and a method for catalyzing a palladium cross-coupling reaction, such as the Suzuki-Miyaura, Mizoroki-Heck, and Sonagashira reactions. | 2017-09-28 |
20170275319 | PLATINUM DERIVATIVES FOR HYDROPHOBIC FORMULATIONS - New derivatives of a Pt (II) complex provided which are liposoluble and useful as anticancer agents. Also disclosed are platinum II complexes in delivery systems such as liposomes, emulsions, nanoemulsions, and lipid excipients. | 2017-09-28 |
20170275320 | First Row Transition Metal Amino Borohydrides - A transition metal amino borohydride material includes a first row transition metal in conjunction with an amine ligand and borohydride, in a condition of having been thermally treated to a temperature of at least 70° C. and up to but not including 800° C. An exemplary such material, Fe(DETA)(BH | 2017-09-28 |
20170275321 | First-Row Transition Metal Hydrogenation and Hydrosilylation Catalysts - Transition metal compounds, and specifically transition metal compounds having a tetradentate and/or pentadentate supporting ligand are described, together with methods for the preparation thereof and the use of such compounds as hydrogenation and/or hydrosilylation catalysts. | 2017-09-28 |
20170275322 | METHODS FOR THE PREPARATION OF DIASTEREOMERICALLY PURE PHOSPHORAMIDATE PRODRUGS - Methods for the preparation of diastereomerically pure phosphoramidate prodrugs of nucleosides, and intermediates useful for the preparation are provided. The nucleosides are useful for the treatment of hepatitis C and cancer. | 2017-09-28 |
20170275323 | GLYCOLIPIDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR USE IN THERAPY - A compound of Formula I: R1-L1-C(A)(A′)-CH | 2017-09-28 |
20170275324 | Novel Diterpene Glycosides, Compositions and Purification Methods - A novel diterpene glycoside and methods for preparing and purifying the same are provided herein. In addition, compositions comprising the novel diterpene glycoside, as well as methods of using the diterpene glycoside are provided. | 2017-09-28 |
20170275325 | Novel Diterpene Glycosides, Compositions and Purification Methods - Novel diterpene glycosides and methods for purifying the same are provided herein. In addition, compositions comprising the novel diterpene glycosides, as well as methods of using the diterpene glycosides are provided. | 2017-09-28 |
20170275326 | IDIOPATHIC PULMONARY FIBROSIS-DETECTION, MONITORING, PREDICTION METHODS - Provided is a compound of the general formula (I): | 2017-09-28 |
20170275327 | SUBSTITUTED PHOSPHORAMIDATE COMPOUNDS AND USES THEREOF - The present invention is directed to Compounds of Formula (I) and salts thereof, wherein R | 2017-09-28 |
20170275328 | DI- AND TRIPHOSPHATE PRODRUGS - Compounds which can be used as prodrugs, in particular nucleoside diphosphate and triphosphate prodrugs, and a method for producing these compounds. The aim is to provide improved di- and/or triphosphate prodrugs, in particular nucleotide or nucleotide analog prodrugs. This is achieved in one aspect by providing bioreversibly and asymmetrically masked di- and triphosphate compounds, in particular nucleoside diphosphate and nucleoside triphosphate compounds or the analogs thereof. The masking only occurs at the terminal phosphate, i.e. at the β- or γ-phosphate, whereas the masking of the internal phosphate is omitted. | 2017-09-28 |
20170275329 | ALKYNYL NUCLEOSIDE ANALOGS AS INHIBITORS OF HUMAN RHINOVIRUS - The present invention provides a compound of Formula (I) or a salt thereof; | 2017-09-28 |
20170275330 | POLYMORPHIC FORMS OF AN OXYSTEROL AND METHODS OF MAKING THEM - Compositions and methods for preparing an OXY133 polymorph are provided. This compositions and methods include subjecting a slurry of OXY133 to conditions sufficient to convert OXY133 to the OXY133 polymorph Form A, polymorph Form B, polymorph Form C, polymorph Form D, polymorph Form E, polymorph Form F, polymorph Form G, polymorph Form H, polymorph Form I or a mixture thereof. A polymorph of OXY133 is also provided and that polymorph can be polymorph Form A, polymorph Form B, polymorph Form C, polymorph Form D, polymorph Form E, polymorph Form F, polymorph Form G, polymorph Form H, polymorph Form I or a mixture thereof. Pharmaceutical compositions including OXY133 polymorphs are also provided. | 2017-09-28 |
20170275331 | SITE-SELECTIVE FUNCTIONALIZATION OF PROTEINS USING TRACELESS AFFINITY LABELS - The present disclosure relates to site-selective labeling compounds, and methods of using such compounds. | 2017-09-28 |
20170275332 | POLYPEPTIDE MODIFICATION METHOD FOR PURIFYING POLYPEPTIDE MULTIMERS - The present invention provides efficient methods based on alteration of the protein A-binding ability, for producing or purifying multispecific antibodies having the activity of binding to two or more types of antigens to high purity through a protein A-based purification step alone. The methods of the present invention for producing or purifying multispecific antibodies which feature altering amino acid residues of antibody heavy chain constant region and/or variable region. Multispecific antibodies with an altered protein A-binding ability, which exhibit plasma retention comparable or longer than that of human IgG1, can be efficiently prepared in high purity by introducing amino acid alterations of the present invention into antibodies. | 2017-09-28 |
20170275333 | NOVEL PEPTIDE COMPOSITIONS - The present invention provides, among other things, novel peptides and compositions for treating disease. | 2017-09-28 |
20170275334 | LINEAR PEPTIDE ANTIBIOTICS - Provided herein are antibacterial compounds, wherein the compounds in some embodiments have broad spectrum bioactivity. The compounds provided herein can in other embodiments overcome the resistance conferred by single amino acid mutations at defined positions of bacterial Signal Peptidases (SPases) and in other embodiments provide for a broad spectrum of antibiotic bioactivity. Pharmaceutical compositions and methods for treatment using the compounds described herein are also provided. | 2017-09-28 |
20170275335 | IMPROVED PROCESS FOR PREPARATION OF AMORPHOUS LINACLOTIDE - The present application relates to an improved process for the formation of disulfide bonds in linaclotide. The present application also relates to an improved process for the purification of linaclotide. | 2017-09-28 |
20170275336 | NOVEL PEPTIDE AND USE THEREOF - An object of the present invention is to provide a novel peptide and a novel immunostimulant or hair grower containing the peptide as an active ingredient. The present invention provides a peptide of 23 or less amino acids comprising the amino acid sequence LHRLKRLRKRL (SEQ ID NO: 1), preferably the amino acid sequence LHRLKRLRKRLK (SEQ ID NO: 9), and also provides an immunostimulant containing the peptide, a vaccine adjuvant containing the peptide, a vaccine composition containing the peptide, and a hair grower containing the peptide. | 2017-09-28 |