| 23rd week of 2016 patent applcation highlights part 24 |
| Patent application number | Title | Published |
|---|
| 20160159718 | MONOPHOSPHITES COMPRISING AN ANTHROL - Monophosphites comprising an anthrol are useful for catalyzing hydroformylation of an olefin to an aldehyde. | 2016-06-09 |
| 20160159719 | METHOD OF REGULATING THE WATER CONTENT IN A CONTINUOUS METHOD FOR PRODUCING METHACROLEIN - The present invention concerns regulating the water content in a process for production of methacrolein. Methacrolein is used in chemical synthesis particularly as an intermediate for production of methacrylic acid, methyl methacrylate or else of active, aroma or flavour chemicals. The present invention is particularly concerned with regulating the water content in a process for production of methacrolein from formaldehyde and propionaldehyde via a Mannich condensation. | 2016-06-09 |
| 20160159720 | USE OF PHOSPHATE SALTS IN THE PRODUCTION OF CARBOXYLIC ACIDS - The use of a metal phosphate compound in a transition metal catalyzed carbonylation reaction to increase the rate of carbonylation reaction is provided. In some aspects, the metal phosphate compound is used in conjunction with a rhodium catalyzed carbonylation process for producing glacial acetic acid including a carbonylation method which comprises LiI. | 2016-06-09 |
| 20160159721 | PROCESSES FOR PRODUCING AN ACETIC ACID PRODUCT HAVING LOW BUTYL ACETATE CONTENT - A process for producing an acetic acid product having low butyl acetate content via a carbonylation reaction. The carbonylation reaction is carried out at a temperature from 100 to 300° C., a hydrogen partial pressure from 0.3 to 2 atm, and a metal catalyst concentration from 100 to 3000 wppm, based on the weight of the reaction medium. The butyl acetate concentration in the acetic acid product may be controlled by removing acetaldehyde from a stream derived from the reaction medium and/or by adjusting at least one of reaction temperature, hydrogen partial pressure, and metal catalyst concentration. | 2016-06-09 |
| 20160159722 | METHOD FOR PRODUCING OXIDE - Provided is a method of oxidizing a substrate with excellent oxidizing power to yield a corresponding oxide. The method can employ a commercially available imide compound as intact as a catalyst and can produce the oxide in a high yield under mild conditions. | 2016-06-09 |
| 20160159723 | PURIFICATION OF LONG CHAIN DIACIDS - The present disclosure relates to methods for separating and purifying a long chain diacid from other long chain diacids, monocarboxylic acids, hydroxyl acids or alkanes by simulated or actual moving bed chromatography. | 2016-06-09 |
| 20160159725 | METHOD FOR CONTINUOUS PRODUCTION OF LIGHT ACRYLATES BY ESTERIFICATION OF A RAW ESTER-GRADE ACRYLIC ACID - The present invention relates to methods by which the thermal dissociation of Michael adducts present in a stream of crude acrylic acid, called “crude ester grade”, and the esterification reaction of acrylic acid present in the stream of crude acrylic acid, or generated in situ by thermal dissociation, with a light alcohol, are carried out simultaneously. | 2016-06-09 |
| 20160159726 | PLASTICIZER COMPOSITION COMPRISING DI(2-ETHYLHEXYL) TEREPHTHALATE - A method for preparing an aromatic di-ester includes combining an aromatic di-acid and a linear or branched C4-C13 alcohol to form a mixture. The method also includes heating the mixture from a first temperature (T1) to a second temperature (T2) without a catalyst present in the mixture. The method further includes combining a titanium catalyst with the mixture after the mixture is at the second temperature (T2). The method further includes increasing pressure from a first pressure (P1) to a second pressure (P2) after the mixture is at the second temperature (T2). The method further includes increasing the temperature of the mixture from the second temperature (T2) to a third temperature (T3) while maintaining the second pressure (P2). | 2016-06-09 |
| 20160159727 | USE OF IMMOBILIZED MOLYBDENUM- AND TUNGSTEN-CONTAINING CATALYSTS IN OLEFIN CROSS METATHESIS - Method of forming an olefin from a first olefin and a second olefin in a metathesis reaction, comprising step (i): (i) reacting the first olefin with the second olefin in the presence of a silica supported Mo- or W-alkylidene catalyst, wherein the first olefin and the second olefin are different from one another. | 2016-06-09 |
| 20160159728 | PREPARATION OF METHYL METHACRYLATE VIA AN OXIDATIVE ESTERIFICATIN PROCESS - A process for producing methyl methacrylate, the process comprising contacting reactants comprising methacrolein, methanol and an oxygen-containing gas, under reaction conditions in the presence of a solid catalyst comprising palladium, bismuth and at least one third element X, where X is selected from the group consisting of P, S, Sc, V, Ga, Se, Y, Nb, Mo, La, Ce, and Nd, wherein the solid catalyst further comprises a support selected from at least one member of the group consisting of silica, alumina, calcium carbonate, active carbon, zinc oxide, titanium oxide and magnesium oxide. | 2016-06-09 |
| 20160159729 | METHOD OF PRODUCING OPTICALLY ACTIVE -AMINOCARBONYL COMPOUND - In a method of producing an optically active β-aminocarbonyl compound using a column reactor, a column for a column reactor is charged with asymmetric catalyst particles to form a column reactor. Compounds for a Mannich-type reaction are introduced into the column reactor to be brought into contact with the asymmetric catalyst particles, to thereby convert the compounds to an optically active β-aminocarbonyl compound. The preferable asymmetric catalyst particles are resin particles that are prepared from a monomer composition containing a proline derivative monomer having an unsaturated bond and a radical polymerization initiator, and that act as a catalyst for an asymmetric Mannich-type reaction. | 2016-06-09 |
| 20160159730 | New Salts, Crystals, Complexes, and Derivatives of Threonine Diacetic Acid, a Process to Prepare threonine Diacetic Acid, and the Use Thereof - The present invention relates to new salts, complexes, crystals, solutions, dispersions, and slurries of threonine-N,N-diacetic acid or derivatives thereof, to formulations containing those, to processes to prepare those, and to the use thereof. | 2016-06-09 |
| 20160159731 | Bifunctional AKR1C3 Inhibitors/Androgen Receptor Modulators and Methods of Use Thereof - The invention includes compositions comprising selective AKR1C3 inhibitors. The invention also includes compositions comprising bifunctional AKR1C3 inhibitors and selective androgen receptor modulators. The invention further includes methods of treatment using the compositions of the invention. | 2016-06-09 |
| 20160159732 | ALKYNES AND METHODS OF REACTING ALKYNES WITH 1,3-DIPOLE-FUNCTIONAL COMPOUNDS - 1,3-Dipole-functional compounds (e.g., azide functional compounds) can be reacted with certain alkynes in a cyclization reaction to form heterocyclic compounds. Useful alkynes (e.g., strained, cyclic alkynes) and methods of making such alkynes are also disclosed. The reaction of 1,3-dipole-functional compounds with alkynes can be used for a wide variety of applications including the immobilization of biomolecules on a substrate. | 2016-06-09 |
| 20160159733 | REACTION ACCELERATOR AND METHOD OF PRODUCING URETHANE COMPOUND, THIOURETHANE COMPOUND, AMIDE COMPOUND, OR UREA COMPOUND USING SAME - A reaction accelerator is provided which is used in a reaction of a compound including an isocyanate group that is not directly bonded to an aromatic ring in a molecule with a compound including an active hydrogen-containing group and is formed of a compound including a halogenated carbamoyl group. A production method is provided which includes reacting a compound including an isocyanate group that is not directly bonded to an aromatic ring in a molecule with a compound including an active hydrogen-containing group to produce a urethane compound, a thiourethane compound, an amide compound or a urea compound, in which the reaction is performed in the presence of the reaction accelerator. | 2016-06-09 |
| 20160159734 | PROCESS FOR OBTAINING ORGANIC ISOCYANATES FROM DISTILLATION RESIDUES FROM ISOCYANATE PREPARATION - The present invention relates to a process for obtaining organic isocyanate from a phosgenation product comprising the isocyanate, comprising the following steps: a) workup to the phosgenation product, the workup comprising at least one distillation step in which a first portion of the organic isocyanate is removed as distillate and a distillation residue comprising a second portion of the organic isocyanate is obtained, b) workup of the distillation residue obtained in a), the workup comprising at least one distillation step which is conducted at a temperature of up to 110° C. at a pressure of not more than 1 mbar, wherein at least 50% by weight of the second portion of the organic isocyanate is removed from the distillation residue. | 2016-06-09 |
| 20160159735 | COMPLEXES OF AGOMELATINE AND SULPHONIC ACIDS, A PROCESS FOR THEIR PREPARATION AND PHARMACEUTICAL COMPOSITIONS CONTAINING THEM - Complexes of agomelatine and sulphonic acids of formula (I): | 2016-06-09 |
| 20160159736 | Deuterated Rigosertib - This invention relates to novel substituted styryl benzylsulfones that are multikinase inhibitors and pharmaceutically acceptable acid addition salts thereof. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating diseases and conditions beneficially treated by an agent that inhibits kinases, such as phosphatidylinositol 3-kinase (PI3-K) and polo-like kinase (PLK-1). | 2016-06-09 |
| 20160159737 | PROCESS FOR THE PREPARATION OF A POLYUNSATURATED KETONE COMPOUND - The invention relates to the manufacture of certain polyunsaturated compounds employing a particular application of the Mitsonobu reaction in the presence of at least one anti-oxidant. We have found a method of making a pharmaceutically-acceptable polyunsaturated ester or thioester compound directly, which can ultimately be converted to the advantageous ketone compounds, in which unwanted oxidation and cis/trans isomerization are substantially reduced or eliminated using particular Mitsonobu chemistry. | 2016-06-09 |
| 20160159738 | COVALENT INHIBITORS OF KRAS G12C - Irreversible inhibitors of G12C mutant K-Ras protein are provided. Also disclosed are methods to modulate the activity of G12C mutant K-Ras protein and methods of treatment of disorders mediated by G12C mutant K-Ras protein. | 2016-06-09 |
| 20160159739 | AZACYCLIC CONSTRAINED ANALOGS OF FTY720 - Small molecules comprised of azacyclic constrained analogs of FTY720 are provided. Formulations and medicaments are also provided that are directed to the treatment of disease, such as, for example, leukemia, and other diseases. Therapeutics are also provided containing a therapeutically effective dose of one or more small molecule compounds, present either as pharmaceutically effective salt or in pure form, including, but not limited to, formulations for oral, intravenous, or intramuscular administration. | 2016-06-09 |
| 20160159740 | INDOLE-3-CARBINOL DERIVATIVES - The present invention relates to novel stable indole-3-carbinol derivatives of Formula-I and its pharmaceutical composition and biological activity. The present invention includes compositions and methods for the treatment and prevention of conditions associated with Inflammation. | 2016-06-09 |
| 20160159741 | METHODS AND COMPOSITIONS FOR TREATING EWINGS SARCOMA FAMILY OF TUMORS - Compounds, compositions and methods relating to EWS-FLI1 protein inhibitors are provided. The compounds have utility in the treatment of cancers including the Ewing's sarcoma family of tumors. | 2016-06-09 |
| 20160159742 | PROCESS FOR THE PREPARATION OF 4-AMINO-5-FLUORO-3-CHLORO-6-(SUBSTITUTED)PICOLINATES - 4-Amino-5-fluoro-3-chloro-6-(substituted)picolinates are prepared from trifluoroacetic acid, p-methoxyaniline, a C | 2016-06-09 |
| 20160159743 | FUSED HETEROCYCLIC COMPOUND - There is provided a compound having an excellent controlling effect on pests represented by the formula (1): | 2016-06-09 |
| 20160159744 | Quinoline Carboxamide and Quinoline Carbonitrile Derivatives as mGluR2-Negative Allosteric Modulators, Compositions, and Their Use - The present invention provides quinoline carboxamide and quinoline carbonitrile compounds of formula (I) | 2016-06-09 |
| 20160159745 | PREPARATION OF (-)-HUPERZINE A - The present invention relates to a method for preparing (−)-huperzine A. The method involves: allowing a mixture of (±)-huperzine A obtained from chemical synthesis and a chiral acid to form (±)-huperzine A chiral acid salt under suitable conditions; recrystallizing the chiral acid salt from an organic solvent and basifying with an alkali to obtain optically pure (−)-huperzine A. The method is convenient to operate and suitable for industrial production. The chemical purity and optical purity of (−)-huperzine A obtained by the method are each greater than 99.5%, satisfying the requirement for raw pharmaceutical purity in the pharmaceutical industry. | 2016-06-09 |
| 20160159746 | HYDANTOINS THAT MODULATE BACE-MEDIATED APP PROCESSING - In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition. | 2016-06-09 |
| 20160159747 | METHOD FOR PREPARATION OF BENZIMIDAZOLE DERIVATIVES - The present invention provides a method for preparing a compound with a benzimidazole structure with an excellent yield using a low-cost starting material, not requiring an additional separation process, or not using a dangerous reagent during the manufacturing process. Furthermore, the present invention also provides an intermediate and a final product produced by the preparing method. | 2016-06-09 |
| 20160159748 | Novel Solid Forms Of Bendamustine Hydrochloride - Novel solid forms of bendamustine hydrochloride are described, as well as methods of their preparation and use. | 2016-06-09 |
| 20160159749 | METHODS OF REGIOSELECTIVE SYNTHESIS OF 2,4-DISUBSTITUTED PYRIMIDINES - The present invention relates to the novel regioselective syntheses of 2,4-disubstituted pyrimidines through sequential nucleophilic aromatic substitutions. | 2016-06-09 |
| 20160159750 | POLYMER FILM, RETARDATION FILM, POLARIZING PLATE, LIQUID CRYSTAL DISPLAY, AND COMPOUND - Provided is a polymer film containing at least one of a compound represented by formula (1) of hydrates, solvates, or salts thereof. Y is a methine group or nitrogen atom. Q | 2016-06-09 |
| 20160159751 | NOVEL QUINAZOLINES AS BIOGENIC AMINE TRANSPORT MODULATORS - The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2016-06-09 |
| 20160159752 | PIPERAZINE DERIVATIVES AS HIV PROTEASE INHIBITORS - The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. | 2016-06-09 |
| 20160159753 | Methods for the synthesis of activated ethylfumarates and their use as intermediates - Disclosed embodiments relate to improved methods for the synthesis of activated fumarate intermediates and their use in chemical synthesis. Disclosed embodiments describe the synthesis of activated fumarate esters including those derived from activating groups including: 4-nitrophenyl, diphenylphophoryl azide, pivaloyl chloride, chlorosulfonyl isocyanate, p-nitrophenol, MEF, trifluoroacetyl and chlorine, for example, ethyl fumaroyl chloride and the subsequent use of the activated ester in situ. Further embodiments describe the improved synthesis of substituted aminoalkyl-diketopiperazines from unisolated and unpurified intermediates allowing for improved yields and reactor throughput. | 2016-06-09 |
| 20160159754 | COMPOUNDS FOR TREATMENT OF CYSTIC FIBROSIS - Described herein are compounds, compositions, and methods of their use for the treatment of cystic fibrosis. | 2016-06-09 |
| 20160159755 | TETRAZOLINONE COMPOUND AND USE THEREOF - A tetrazolinone compound represented by formula (1): | 2016-06-09 |
| 20160159756 | FORMULATION OF METAXALONE - Dosage forms of metaxalone containing submicron particles of metaxalone and uses thereof are described. The submicron dosage forms have improved bioavailability compared to certain conventional metaxalone dosage forms. | 2016-06-09 |
| 20160159757 | OXAZINE DERIVATIVES - The present invention provides, for example, a compound mentioned below as a medicament for treating or preventing the diseases induced by production, secretion or deposition of amyloid-β proteins.
| 2016-06-09 |
| 20160159758 | 3-(2-AMINO-ETHYL)-ALKYLIDENE)-THIAZOLIDINE-2,4-DIONE AND 1-(2-AMINO-ETHYL)-ALKYLIDENE-1,3-DIHYDRO-INDOL-2-ONE DERIVATIVES AS SELECTIVE SPHINGOSINE KINASE 2 INHIBITORS - 3-(2-amino-ethyl)-5-[3-(4-substituted-phenyl)-alkylidene)-thiazolidine-2,4-dione and 1-(2-amino-ethyl)-3-alkylidene-1,3-dihydro-indol-2-one and derivatives thereof are provided for use as selective SphK2 inhibitors and for use in the treatment of human diseases, such as cancer. | 2016-06-09 |
| 20160159759 | OXATHIAZINE DERIVATIVES AS ANTIBACTERIAL AND ANTICANCER AGENTS - New oxathiazin-like compounds and their derivatives are useful as antineoplastic and antimicrobial agents. Compositions and methods of using oxathiazin-like compounds and their derivatives are disclosed. | 2016-06-09 |
| 20160159760 | ORGANO-1-OXA-4-AZONIUM CYCLOHEXANE COMPOUNDS - Novel 1-oxa-4-azonium cyclohexane salts are described. These compounds can be used as structure directing agents, and they overcome many of the typical problems associated with OSDA synthesis and subsequent zeolite synthesis. Methods for synthesis of the 1-oxa-4-azonium cyclohexane salts from a variety of starting materials are also described. | 2016-06-09 |
| 20160159761 | ASSEMBLY FOR PRODUCING ALKYLENE OXIDES AND GLYCOL ETHERS - There is provided a manufacturing assembly for the production of an alkylene oxide and a stream of glycol ethers. The manufacturing assembly produces the alkylene oxide and stream of glycol without the use of equipment for separating substantially all of the alkyl alcohol from the alkylene oxide product stream. Thus, the use of additional pieces of equipment can be avoided, or the equipment required to effectuate any required further separation and/or purification may be smaller and/or cheaper to purchase and/or operate. | 2016-06-09 |
| 20160159762 | PROCESS FOR PRODUCING FURAN FROM FURFURAL FROM BIOMASS - A process is described for producing furan from furfural from biomass, wherein furfural in an aqueous mass or stream from the liquefaction of biomass or a biomass fraction including one or more furfural precursors is extracted into an organic solvent which is readily separable from furan by simple distillation at atmospheric pressure, furfural is catalytically decarbonylated to furan in the organic solvent and furan is separated from the organic solvent by simple distillation. The furan from the distillation step may be hydrogenated to provide tetrahydrofuran. | 2016-06-09 |
| 20160159763 | POLYMERIZABLE COMPOUNDS AND THE USE THEREOF IN LIQUID-CRYSTAL DISPLAYS - The present invention relates to polymerisable compounds, to processes and intermediates for the preparation thereof, and to the use thereof for optical, electro-optical and electronic purposes, in particular in liquid-crystal (LC) media and LC displays, especially in LC displays of the PS (“polymer sustained”) or PSA (“polymer sustained alignment”) type. | 2016-06-09 |
| 20160159764 | METHOD FOR PRODUCING ELLAGIC ACID COMPOSITION - Provided is a production method for an ellagic acid composition excellent in solubility in water. The production method for an ellagic acid composition includes the steps of: mixing an aqueous medium with a raw material which contains a guava leaf extract and which contains, in solids thereof, 1 to 5% by mass of free ellagic acid to prepare a material for heat treatment; and subjecting the material for heat treatment to heat treatment at from 100 to 180° C. | 2016-06-09 |
| 20160159765 | LIQUID CRYSTAL COMPOUND HAVING 2, 6-DIFLUOROPHENYLETHER STRUCTURE, AND LIQUID CRYSTAL COMPOSITION CONTAINING THE SAME - The present invention relates to a compound having a 2,6-difluorophenylether structure useful as organic electronic materials, pharmaceuticals and agrochemicals, and in particular, liquid crystal display device materials. | 2016-06-09 |
| 20160159766 | PESTICIDAL COMPOSITIONS AND PROCESSES RELATED THERETO - This document discloses molecules having the following formula (“Formula One”): | 2016-06-09 |
| 20160159767 | CHEMICAL COMPOUNDS - The invention relates to pyrrolone compounds of the formula (I) wherein X, R | 2016-06-09 |
| 20160159768 | ARYLMETHOXY ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - Provided are 4′-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 2016-06-09 |
| 20160159769 | Pyrimidine Compounds for the Treatment of Hepatitis C - The disclosure provides compounds of formula I, including pharmaceutically acceptable salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV. | 2016-06-09 |
| 20160159770 | Herbicidal Azines - The present invention relates to diaminotriazine compounds of the formula (I) | 2016-06-09 |
| 20160159771 | THERAPEUTICALLY ACTIVE COMPOUNDS AND THEIR METHODS OF USE - Provided are compounds useful for treating cancer and methods of treating cancer comprising administering to a subject in need thereof a compound described herein. | 2016-06-09 |
| 20160159772 | ARYLMETHOXY ISOINDOLINE DERIVATIVES AND COMPOSITIONS COMPRISING AND METHODS OF USING THE SAME - Provided are 4′-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed. | 2016-06-09 |
| 20160159773 | HETEROCYCLIC COMPOUND - The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. | 2016-06-09 |
| 20160159774 | HETEROARYL COMPOUNDS AND USES THEREOF - The present invention provides compounds, pharmaceutically acceptable compositions thereof, and methods of using the same. | 2016-06-09 |
| 20160159775 | BENZOIMIDAZOL-2-YL PYRIMIDINE MODULATORS OF THE HISTAMINE H4 RECEPTOR - Benzoimidazol-2-yl pyrimidines, purification methods for the same, and pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H | 2016-06-09 |
| 20160159776 | BENZIMIDAZOLE-2-PIPERAZINE HETEROCYCLIC COMPOUND, PHARMACEUTICAL COMPOSITION CONTAINING THE SAME, PREPARATION METHOD AND USE THEREOF - The present invention relates to a class of benzimidazole-2-piperazine heterocyclic derivatives, a preparation method and medical use thereof. Specifically, the present invention relates to a new benzimidazole-2-piperazine heterocyclic derivative of general Formula (I), a preparation method, a pharmaceutical composition containing the same, and use thereof as a therapeutic agent and especially as a poly(ADP-ribose)polymerase (PARP) inhibitor. | 2016-06-09 |
| 20160159777 | CROSSLINKING REAGENTS, METHODS, AND COMPOSITIONS FOR STUDYING PROTEIN-PROTEIN INTERACTIONS - The invention provides reagents, methods, and compositions for studying protein-protein interactions. The inventive system and methods allow the analysis of protein-protein interactions in vivo and in vitro. Advantages offered by various embodiments of the inventive system and methods compared to existing photocrosslinking approaches include, for example, (i) novel reversible crosslinking reagents that allow easy isolation, purification, and enrichment of the crosslinked products; (ii) trifiuoromethyl phenyldiazirine- or perfluorinaled phenylazide-bascd photocrosslinking reagents that provide high specific labeling, no side product, and higher photocrosslinking efficiency; (iii) versatile spacer groups that allow systematic contact site mapping; (iv) novel methods for isolating, purifying, and detecting crosslinked products based on the reversible-link chemistry; and (v) the ability to study the interaction sites in vitro, in situ, or in vivo. | 2016-06-09 |
| 20160159778 | NOVEL UREIDO DERIVATIVES OF NAPHTHALENESULFONIC ACIDS - Objects of the present invention are novel ureido derivatives of naphthalensulfonic acids, pharmaceutical compositions comprising such derivatives, a process for the preparation thereof and the use of said derivatives as medications, in particular in the treatment of HIV infections. Formula (I): | 2016-06-09 |
| 20160159779 | CO-CRYSTAL OF THE PAR-1 RECEPTOR ANTAGONISTS VORAPAXAR AND ASPRIN - This invention relates to a co-crystal of vorapaxar and aspirin. The inventive co-crystal antagonizes the PAR-1 receptor. This invention also provides for pharmaceutical compositions comprising the inventive co-crystal as well as potentially to methods for the treatment, amelioration or prevention of conditions that could be treated by antagonizing the PAR-1 receptor. | 2016-06-09 |
| 20160159780 | STRIGOLACTONE FORMULATIONS AND USES THEREOF - Disclosed herein plant propagation materials, methods of manufacturing, formulations and uses thereof. The plant propagation materials disclosed herein may comprise a strigolactone obtained by a biosynthetic process. The plant propagation material may comprise a chemical mimic of a strigolactone. The strigolactone may be 5-deoxystrigol. Methods of manufacturing the plant propagation materials may comprise a chemical process. Alternatively, methods of manufacturing the plant propagation material may comprise a biosynthetic process. The methods may comprise use of one or more polynucleotides. The polynucleotides may encode a metabolite. The polynucleotides may comprise one or more genes encoding one or more components of a strigolactone pathway. | 2016-06-09 |
| 20160159781 | CHEMICAL COMPOUNDS - The invention relates to pyrrolone compounds of the formula (I) wherein X, R | 2016-06-09 |
| 20160159782 | INHIBITORS OF EZH2 - The present invention relates to compounds that inhibit activity of the histone lysine N-methyltransferase, Enhancer of Zeste Homolog 2 (EZH2), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, such as hematologic and solid tumors. | 2016-06-09 |
| 20160159783 | PDE4 Inhibitor - Provided is a compound represented by formula (1a) or a pharmacologically acceptable salt thereof. However, R | 2016-06-09 |
| 20160159784 | N-CYCLOPROPYL-N-PIPERIDINYL-AMIDES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND USES THEREOF - Compounds of formula I | 2016-06-09 |
| 20160159785 | SUBSTITUTED-QUINOXALINE-TYPE PIPERIDINE COMPOUNDS AND THE USES THEREOF - The invention relates to Substituted-Quinoxaline-Type Piperidine Compounds, compositions comprising an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted-Quinoxaline-Type Piperidine Compound. | 2016-06-09 |
| 20160159786 | CHEMICAL PROCESS - The present invention relates to a process for the preparation of umeclidinium bromide, and to processes for preparing intermediates used in the preparation of umeclidinium bromide. | 2016-06-09 |
| 20160159787 | Cis-tetrahydro-spiro(cyclohexane-1, 1' -pyrido[3,4-b]indole)-4-amine Compounds - Cis-tetrahydro-spiro(cyclohexane-1,1′-pyrido[3,4-b]indole)-4-amine compounds which act on the nociceptin/ORL-1 receptor system as well as on the μ-opioid receptor system and which are distinguished in particular by selective effectiveness in the treatment of chronic pain, such as inflammatory pain, visceral pain, tumour pain, and neuropathic pain, without at the same time developing pronounced effectiveness against acute, nociceptive pain. | 2016-06-09 |
| 20160159788 | METHOD FOR PREPARATION OF 1-CYCLOPROPYL-6-FLUORO-1,4-DIHYDRO-8-METHOXY-7-[(4AS,7AS)-OCTAHYDRO-6H-PY- RROLO[3,4-B]PYRIDIN-6-YL]-4-OXO-3-QUINOLINECARBOXYLIC ACID - This invention relates to methods for preparation of chemical compound 1-cyclopropyl-6-fluoro-1,4-dihydro-8-methoxy-7-[(4a8,7aS)-octahydro-6H-pyrrolo[3,4-b]pyridin-6-yl]-4-oxo-3-quinolinecarboxylic acid, which comprise addition of heterocyclic amine containing protecting group, to ethyl-3-oxo-3-(2,4,5-trifluoro-3-methoxyphenyl)propanoate, followed by interaction with triethyl orthoformate, addition of cyclic amine, subsequent cyclization and formation of target product. The method for preparation claimed is technologically simple in comparison with analogue and requires no special complex technical operations, which in its turn simplifies method for preparation of this chemical compound, and reduces cost of the final product, while the commercial production utilizing the mehod claimed has low degree of environmental threat. | 2016-06-09 |
| 20160159789 | SUBSTITUTED PYRAZOLOPYRIDINES - The present invention relates to substituted pyrazolopyridine compounds of general formula I as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyperproliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 2016-06-09 |
| 20160159790 | Pyrroloquinoline Derivatives as 5-HT6 Antagonists, Preparation Method and Use Thereof - This invention concerns pyrroloquinoline derivatives as antagonists of 5-HT6 receptors, to methods for the preparation of these compounds and to novel intermediates useful for their synthesis. The invention also relates to the uses of such compounds and compositions, particularly their use in administering them to patients to achieve a therapeutic effect in schizophrenia, anxiety, depression, maniac depression, epilepsy, obsessive compulsive disorders, mood disorders, migraine, Alzheimer's disease, age related cognitive decline, mild cognitive impairment, sleep disorders, eating disorders, anorexia, bulimia, panic attacks, attention deficit hyperactivity disorder, attention deficit disorder, Parkinson's disease, Huntington's disease, withdrawal from abuse of cocaine, ethanol, nicotine or benzodiazepines, pain, obesity and type-2 diabetes, functional bowel disorder, Irritable Bowel Syndrome. The compounds have the general formula (XIV), wherein the symbols have the meanings given in the description. | 2016-06-09 |
| 20160159791 | COMPOUNDS AS MODULATORS OF RORC - The present invention encompasses compounds of the formula (I), wherein the variables are defined herein which are suitable for the modulation of RORC and the treatment of diseases related to the modulation of RORC. The present invention also encompasses processes of making compounds of formula (I) and pharmaceutical preparations containing them. | 2016-06-09 |
| 20160159792 | PROCESS FOR PREPARATION OF INDOLIZINE BASED DERIVATIVES AS POTENTIAL PHOSPHODIESTRASE 3 (PDE3) INHIBITORS - The present invention provides compounds of general formula 1 useful as potential phosphodiesterase3 (PDE3) inhibitory agents and a process for the preparation thereof. The derivatives of formula 1 can be employed as therapeutics in human and veterinary medicine, where they can be used, for example, for the treatment and prophylaxis of the following diseases: heart failure, dilated cardiomyopathy, platelet inhibitors, cancer and obstructive pulmonary diseases. | 2016-06-09 |
| 20160159793 | Fused Pyrroledicarboxamides and Their Use as Pharmaceuticals - The present invention relates in fused pyrroledicarboxamides of the formula (I), in which R1 to R9, X, m and n are as defined in claims. The compounds of the formula (I) are inhibitors of the acid-sensitive potassium channel TASK-1 and suitable for the treatment of TASK-1 channel-mediated diseases such as arrhythmias, in particular atrial arrhythmias like atrial fibrillation or atrial flutter, and respiratory disorders, in particular sleep-related respiratory disorders like sleep apnea, for example. | 2016-06-09 |
| 20160159794 | NOVEL AZA-OXO-INDOLES FOR THE TREATMENT AND PROPHYLAXIS OF RESPIRATORY SYNCYTIAL VIRUS INFECTION - The invention provides novel compounds having the general formula: | 2016-06-09 |
| 20160159795 | DIAZEPINONE DERIVATIVES - The invention relates to compound of the formula I | 2016-06-09 |
| 20160159796 | NAPHTHYRIDINE DERIVATIVES AS INHIBITORS OF HYPOXIA INDUCIBLE FACTOR (HIF) HYDROXYLASE - The present disclosure relates to novel compounds, methods, and compositions capable of inhibiting HIF hydroxylase enzyme activity, thereby increasing the stability and/or activity of hypoxia inducible factor (HIF). | 2016-06-09 |
| 20160159797 | PYRAZOLO[3,4-c]PYRIDINE COMPOUNDS AND METHODS OF USE - Pyrazolo[3,4-c]pyridine compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R | 2016-06-09 |
| 20160159798 | (1-AZINONE)-SUBSTITUTED PYRIDOINDOLES - Substituted pyridoindoles for incorporation in pharmaceutical compositions employed in the treatment of various diseases correspond to formula (I) | 2016-06-09 |
| 20160159799 | NOVEL PROCESS FOR THE PREPARATION OF SPIROHETEROCYCLIC PYRROLIDINE DIONES - A process for making certain spiroheterocyclic pyrrolidine dione derivatives. | 2016-06-09 |
| 20160159800 | MK2 INHIBITORS - The present invention relates to compounds of general Formula I | 2016-06-09 |
| 20160159801 | NOVEL BICYCLIC BROMODOMAIN INHIBITORS - The invention relates to substituted bicyclic compounds, which are useful for inhibition of BET protein function by binding to bromodomains, pharmaceutical compositions comprising these compounds, and use of the compounds and compositions in therapy. | 2016-06-09 |
| 20160159802 | 18F-LABELLED FOLATES - The present invention is directed towards new | 2016-06-09 |
| 20160159803 | 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. | 2016-06-09 |
| 20160159804 | PYRIDINES, PYRIMIDINES, AND PYRAZINES, AS BTK INHIBITORS AND USES THEREOF - The present invention relates to pyridine, pyrimidine, and pyrazene compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors. | 2016-06-09 |
| 20160159805 | Heterocyclic sulfonylamino(thio)carbonyl-derivatives with nematicidal properties - Disclosed are compounds of formula (I) which possess nematicidal properties | 2016-06-09 |
| 20160159806 | SUBSTITUTED PYRAZOLYLPYRAZOLE DERIVATIVE AND USE OF SAME AS HERBICIDE - Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (1) is disclosed that is able to solve the above-mentioned problems. | 2016-06-09 |
| 20160159807 | SUBSTITUTED PYRAZOLYLPYRAZOLE DERIVATIVE AND USE OF SAME AS HERBICIDE - Provided is a compound capable of effectively control worst weeds of higher leaf stages that present practical problems. A specific pyrazolylpyrazole derivative of formula (1) is disclosed that is able to solve the above-mentioned problems. | 2016-06-09 |
| 20160159808 | HETEROCYCLIC COMPOUND - A compound represented by the formula (I): | 2016-06-09 |
| 20160159809 | HETEROCYCLIC COMPOUNDS AS BIOGENIC AMINE TRANSPORT MODULATORS - The present disclosure relates to certain amine derivatives of fused bicyclic heterocycles that inhibit the amine reuptake function of the biogenic amine transporters, dopamine transporter (DAT), serotonin transporter (SERT) and norepinephrine transporter (NET). Compounds of the present disclosure are potent inhibitors of the reuptake of dopamine (DA), serotonin (5-hydroxytryptamine, 5-HT) and norepinephrine (NE) with full or partial maximal efficacy. The compounds with partial maximal efficacy in inhibiting reuptake of all three biogenic amines are herein referred to as partial triple uptake inhibitors (PTRIs). Compounds of the present disclosure are useful for treating depression, pain and substance abuse and relapse to substance abuse and addiction to substances such as cocaine, methamphetamine, nicotine and alcohol. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention. | 2016-06-09 |
| 20160159810 | 4-IMIDAZOPYRIDAZIN-1-YL-BENZAMIDES AND 4-IMIDAZOTRIAZIN-1-YL-BENZAMIDES AS BTK INHIBITORS - The present invention relates to 6-5 membered fused pyridine ring compounds according to Formula (I) | 2016-06-09 |
| 20160159811 | FUSED TETRA OR PENTA-CYCLIC DIHYDRODIAZEPINOCARBAZOLONES AS PARP INHIBITORS - Provided are certain fused tetra or penta-cyclic compounds and salts thereof, compositions thereof, and methods of use thereof. | 2016-06-09 |
| 20160159812 | NOVEL SYNTHESIS OF NOROXYMORPHONE FROM MORPHINE - The present invention is directed to an improved process to convert morphine into noroxymorphone having economic and ecological advantages. | 2016-06-09 |
| 20160159813 | PROCESS FOR N-DEALKYLATION OF TERTIARY AMINES - The present disclosure provides improved methods for N-dealkylation of tertiary amines, including methods for N-demethylation of alkaloids and opioids, in which the dealkylation reaction is carried out in a solvent comprising a tertiary alcohol. The present disclosure also provides improved processes for preparing semi-synthetic opioids that incorporate the disclosed methods for N-dealkylation of tertiary amines. | 2016-06-09 |
| 20160159814 | GLYCINE TRANSPORTER INHIBITOR - The present invention provides novel compounds of formula [I] or pharmaceutically acceptable salts thereof: | 2016-06-09 |
| 20160159815 | Fused Piperidine Amides as Modulators of Ion Channels - The invention relates to fused piperidine amides useful as inhibitors of ion channels for the treatment of pain. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders. | 2016-06-09 |
| 20160159816 | SUBSTITUTED THIENOPYRIMIDINES AND PHARMACEUTICAL USE THEREOF - The present invention relates to substituted thienopyrimidine compounds of general formula (I) as described and defined herein, to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients. | 2016-06-09 |
| 20160159817 | TRICYCLIC HETEROCYCLES AS BET PROTEIN INHIBITORS - The present invention relates to tricyclic heterocycles of Formula (I), which are inhibitors of BET proteins such as BRD2, BRD3, BRD4, and BRD-t and are useful in the treatment of diseases such as cancer. | 2016-06-09 |
| 20160159818 | Amino-Oxazine and Amino-Dihydrothiazine Compounds as Beta-Secretase Modulators and Methods of Use - The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A | 2016-06-09 |
