21st week of 2016 patent applcation highlights part 21 |
Patent application number | Title | Published |
20160145215 | PROCESS FOR PREPARING A PYRIMIDINE INTERMEDIATE - The present invention relates to a process for preparing a pyrimidine intermediate, namely the compound of formula I-2 or a salt thereof. Said compound of formula I-2 or its salt can be used to prepare macitentan. Macitentan (chemical names: N-[5-(4-bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidinyl]-N′-propylsulfamide or N-[5-(4-bromophenyl)-6-{2-[(5-bromopyrimidin-2-yl)oxy]ethoxy}pyrimidin-4-yl]-N′-propylsulfuric diamide) is an endothelin receptor antagonist that has notably been approved by the US Food and Drug Administration and the European Commission for the treatment of pulmonary arterial hypertension. It has been first disclosed in WO 02/053557. The last step of one of the potential preparation routes described in WO 02/053557, called “Possibility A” and “Possibility B”, can be summarised as shown in Scheme A1 hereafter. | 2016-05-26 |
20160145216 | AMORPHOUS LETERMOVIR AND SOLID PHARMACEUTICAL FORMULATIONS THEREOF FOR ORAL ADMINISTRATION - The present invention provides for amorphous Letermovir and orally administrable solid pharmaceutical formulations thereof (immediate release formulation). Said amorphous Letermovir is suitable for immediate release formulations when isolated out of an organic solution by either roller-drying said organic solution in a volatile organic solvent, in particular acetone, at a temperature of 30° C. to 60° C., and subsequently drying the amorphous Letermovir obtained, or isolating said amorphous Letermovir by precipitation from water miscible solvents selected from acetone or acetonitrile into excess water as anti-solvent, and subsequently filtrating or centrifuging the amorphous Letermovir obtained. | 2016-05-26 |
20160145217 | METHOD FOR PREPARING NITROGEN-CONTAINING AROMATIC COMPOUND BY CATALYTIC PYROLYSIS OF ORGANIC MATERIAL - Provided is a method for preparing a nitrogen-containing aromatic compound through catalytic pyrolysis from organic materials. The method comprises: feeding organic materials and a catalyst into a reactor, to enable the organic material to undergo reactions in the presence of nitrogen and under heating conditions, so as to generate a reaction system flow containing one or more nitrogen-containing aromatic compounds. | 2016-05-26 |
20160145218 | 4-OXO-3,4-DIHYDRO-1,2,3-BENZOTRIAZINE MODULATORS OF GPR139 - The present invention provides a method for treating a disease, disorder or condition associated with GPR139 using compounds of formula 1: | 2016-05-26 |
20160145219 | STROBILURIN TYPE COMPOUNDS FOR COMBATING PHYTOPATHOGENIC FUNGI - The present invention relates to novel strobilurine type compounds, to compositions comprising at least one such compound, to methods for combating phytopathogenic fungi, to the use of such compounds and to seeds coated with at least one such compound. | 2016-05-26 |
20160145220 | NITROGEN-CONTAINING SATURATED HETEROCYCLIC COMPOUND - The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I]: | 2016-05-26 |
20160145221 | METHOD FOR PRODUCING POLYISOCYANATES COMPRISING IMINOOXADIAZINEDIONE GROUPS AND USE OF THESE - The present invention relates to a method for producing polyisocyanates comprising iminooxadiazinedione groups, wherein at least one monomeric di- and/or tri-isocyanate is oligomerised in the presence of a) at least one catalyst, b) at least one additive (A) having a relative permittivity at 18° C. to 30° C. of less than 4.0, c) optionally further additives other than A. The invention relates further to a reaction system for producing polyisocyanates comprising iminooxadiazinedione groups, and to the use of an additive (A) having a relative permittivity at 18° C. to 30° C. of less than 4.0 for producing polyisocyanates comprising iminooxadiazinedione groups by catalysed modification of monomeric di- and/or tri-isocyanates. | 2016-05-26 |
20160145222 | Methods for Controlling Pests in Soybean - The present invention relates to agricultural methods for controlling pests on soybean plants and soybean crops and the general use of isothiazoline compounds of formula (I) | 2016-05-26 |
20160145223 | Bicyclyl-Substituted Isothiazoline Compounds - The present invention relates to bicyclyl-substituted isothiazoline compounds of formula I | 2016-05-26 |
20160145224 | PROCESS FOR THE PREPARATION OF AN ANTIDEPRESSANT AND THE INTERMEDIATES THEREOF - The present invention relates to a process for the preparation of 1-[2-(2,4-dimethylphenylsulphanyl)phenyl]piperazine of formula (I), also known as vortioxetine, salts thereof, and intermediates useful for its synthesis. | 2016-05-26 |
20160145225 | PRODRUGS OF PHENOLIC TRPV1 AGONISTS - Described herein are compounds, pharmaceutical compositions and medicaments that include such compounds, and methods of using such compounds to modulate transient receptor potential vanilloid 1 receptor (TRPV1) activity. | 2016-05-26 |
20160145226 | PROCESS FOR PREPARING PHTHALIC ANHYDRIDE - The present invention relates to a process for preparing phthalic anhydride by gas phase oxidation of aromatic hydrocarbons, in which a gas stream comprising at least one aromatic hydrocarbon and molecular oxygen is passed continuously over a thermostatted catalyst and the supply of the at least one aromatic hydrocarbon to the catalyst is temporarily interrupted after putting the catalyst on stream. | 2016-05-26 |
20160145227 | PROCESSES FOR CONVERSION OF BIOLOGICALLY DERIVED MEVALONIC ACID - The invention relates to a process comprising reacting mevalonic acid, or a solution comprising mevalonic acid, to yield a first product or first product mixture, optionally in the presence of a solid catalyst and/or at elevated temperature and/or pressure. The invention further relates to a process comprising: (a) providing a microbial organism that expresses a biosynthetic mevalonic acid pathway; (b) growing the microbial organism in fermentation medium comprising suitable carbon substrates, whereby biobased mevalonic acid is produced; and (c) reacting said biobased mevalonic acid to yield a first product or first product mixture. | 2016-05-26 |
20160145228 | FORMATION OF CHIRAL 4-CHROMANONES USING CHIRAL PYRROLIDINES IN THE PRESENCE OF UREAS OR THIOUREAS - The present invention relates to a synthesis of chromanones or chromanes in a stereospecific matter in view of the 2-position in the chromanone or chromane ring. It has been found that this synthesis is particularly possible in the presence of a chiral compound of formula of a specific type and of at least one urea or thiourea. | 2016-05-26 |
20160145229 | EXTRACTION SEPARATION METHOD OF A FLAVONE COMPONENT BASED ON GRAPHENE - The present invention refers to the technical field of flavone component extraction, and provides an extraction separation method of a flavone component based on amination graphene. The flavone components comprise flavones, flavanols, isoflavones, flavanones, flavanonols, flavanones, anthocyanidins, chalcones, and chromones etc. The extraction separation method is adsorption extraction, and amination graphene is taken as a medium of adsorption extraction. The extraction separation method of the flavone components based on amination graphene is superior in separation speed and product purity, low cost and convenient operation. | 2016-05-26 |
20160145230 | AGENT CONTAINING FLAVONOID DERIVATIVES FOR TREATING CANCER AND INFLAMMATION - A pharmaceutical composition for the prevention and treatment of cancer with specific flavanoid-based compounds selected from among the groups of Flavone, Flavanone and Flavanol, a method for the prevention and treatment of cancer and inflammation using the specific flavonoid-based pharmaceutical compositions, a method for isolating the flavonoid-based pharmaceutical compositions from raw plant material, and a method for synthesizing said specific flavonoid-based pharmaceutical compositions. | 2016-05-26 |
20160145231 | RESIST COMPOSITION, METHOD FOR FORMING RESIST PATTERN, POLYPHENOLIC COMPOUND FOR USE IN THE COMPOSITION, AND ALCOHOLIC COMPOUND THAT CAN BE DERIVED THEREFROM - A resist composition containing a compound represented by the general formula (1) or (2), a method for forming a resist pattern using the composition, a polyphenolic compound for use in the composition, and an alcoholic compound that can be derived therefrom are described. | 2016-05-26 |
20160145232 | 2-OXO-1,3-DIOXOLANE-4-ACYL HALIDES, THEIR PREPARATION AND USE - The present invention suggests 2-oxo-1,3-dioxolane-4-acyl halides of formula (I), | 2016-05-26 |
20160145233 | METHODS OF MAKING ALKYLENE CARBONATES AND METHODS OF CONVERTING CO2 - Embodiments of the present disclosure provide for a method of making an alkylene carbonate, catalysts, methods of converting CO | 2016-05-26 |
20160145234 | METHOD FOR PRODUCING CYCLIC CARBONATE - Provided is a method for producing a cyclic carbonate obtained by reacting epoxide and carbon dioxide, the method being capable of efficiently producing a cyclic carbonate at a high conversion rate and a high yield, in which degradation of the catalyst over time is suppressed and catalytic activity hardly decreases. | 2016-05-26 |
20160145235 | ARYL SULFIDE DERIVATIVES AND ARYL SULFOXIDE DERIVATIVES AS ACARICIDES AND INSECTICIDES - The present invention relates to aryl sulphide and aryl sulphoxide derivatives, to the use thereof as acaricides and insecticides for controlling animal pests and to processes and intermediates for preparation thereof. The aryl sulphide and aryl sulphoxide derivatives have the general structure (I) | 2016-05-26 |
20160145236 | 4-(3-CYANOPHENYL)-6-PYRIDINYLPYRIMIDINE MGLU5 MODULATORS - The disclosures herein relate to novel compounds of formula wherein R | 2016-05-26 |
20160145237 | PROTEIN TYROSINE KINASE MODULATORS AND METHODS OF USE - Heterocyclic pyrimidine compounds that modulate mutant-selective epidermal growth factor receptor (EGFR) and ALK kinase activity are disclosed. More specifically, the invention provides pyrimidines which inhibit, regulate and/or modulate kinase receptor, particularly in selectively modulation of various EGFR mutant activity and ALK kinase activity have been disclosed. Pharmaceutical compositions comprising the pyrimidine derivative, and methods of treatment for diseases associated with protein kinase enzymatic activity, particularly EGFR or ALK kinase activity including non-small cell lung cancer comprising administration of the pyrimidine derivative are disclosed. | 2016-05-26 |
20160145238 | HETEROARYL SUBSTITUTED PYRAZOLES - Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals. | 2016-05-26 |
20160145239 | DIAMINOHETEROARYL SUBSTITUTED PYRAZOLES - Compounds of formula (I), and their use as pharmaceuticals. | 2016-05-26 |
20160145240 | HETEROARYLAMINE DERIVATIVES AS PROTEIN KINASE INHIBITORS - A heteroarylamine compound includes protein kinase inhibition activity, a pharmaceutically acceptable salt thereof and a pharmaceutical composition for preventing and treating a disease caused by abnormal cell growth, which contains the compound as an active ingredient. | 2016-05-26 |
20160145241 | STABLE CRYSTAL FORM OF TIPIRACIL HYDROCHLORIDE AND CRYSTALLIZATION METHOD FOR THE SAME - An objective of the present invention is to obtain a stable crystal form of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride. The present invention provides a crystal of 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione hydrochloride exhibiting characteristic peaks at angles of 11.6°, 17.2°, 17.8°, 23.3°, 27.1°, and 29.3° as a diffraction angle (2θ±0.1°) in powder X-ray diffraction. | 2016-05-26 |
20160145242 | PHENYLIMIDAZOLE DERIVATIVE, AND THERAPEUTIC MEDICINE OR PREVENTIVE MEDICINE FOR INFLAMMATORY DISEASE, ETC. - A medicinal active ingredient is provided which is useful for the treatment or prevention of inflammatory diseases, diseases caused by lipid oxidation, retinochoroidal disorders. A phenylimidazole derivative represented by Formula (IB) or a salt thereof is provided. A therapeutic medicine or preventive medicine is provided for inflammatory diseases, diseases caused by lipid oxidation, or retinochoroidal disorders, the medicine including at least one selected from the phenylimidazole derivative, a salt thereof, and metabolites thereof as an active ingredient. In Formula (IB), R | 2016-05-26 |
20160145243 | Novel Anti-Cancer Agents - The present invention provides a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is a method of treatment of cancer in a subject comprising administering to said subject an effective amount of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. Further provided is the use of a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof in the preparation of a medicament for the treatment of cancer. In addition, the present invention also provides a pharmaceutical composition comprising a compound of Formula (I), or a pharmaceutical acceptable derivative, salt or prodrug thereof. | 2016-05-26 |
20160145244 | CERTAIN PROTEIN KINASE INHIBITORS - Provided are certain ALK inhibitors, pharmaceutical compositions thereof, and methods of use therefor. | 2016-05-26 |
20160145246 | NUCLEAR TRANSPORT MODULATORS AND USES THEREOF - The present invention relates to compounds of formula I: | 2016-05-26 |
20160145247 | Aminomethyl-Biaryl Derivatives Complement Factor D inhibitors and uses thereof - The present invention provides a compound of formula (I), a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 2016-05-26 |
20160145248 | NOVEL SUBSTITUTED BICYCLIC COMPOUNDS AS 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. | 2016-05-26 |
20160145249 | ALXR AGONIST COMPOUND - The present invention provides a compound having ALXR agonist activity. Specifically, the invention provides a compound having ALXR agonist activity represented by general formula (I) wherein all the symbols are as defined in the specification, a salt thereof, a solvate thereof, or a prodrug thereof as well as an agent containing the same as an active ingredient for preventing and/or treating an ALXR-associated disease, such as an inflammatory bowel disease, an autoimmune disease, a chronic inflammatory disease, asthma, pulmonary fibrosis, atopic dermatitis, ischemia-reperfusion injury, myocardial infarction, or Alzheimer's disease. | 2016-05-26 |
20160145250 | ANTI-CANCER COMPOUNDS - Provided are methods and compositions for the treatment of diseases such as cancer. In certain aspects, compounds which can inhibit Skp2 are provided. Specifically chromenone derivatives are disclosed that have the capability toward reducing differentiation of pluripotent, multipotent or totipotent cells and thus have therapeutic utility in the treatment of a proliferative disease such as cancer. | 2016-05-26 |
20160145251 | INHIBITORS OF MYOCARDIN-RELATED TRANSCRIPTION FACTOR AND SERUM RESPONSE FACTOR (MRTF/SRF)-MEDIATED GENE TRANSCRIPTION AND METHODS FOR USE OF THE SAME - Disclosed herein are inhibitors of gene transcription mediated by myocardin-related transcription factor and serum response factor, or both myocardin-related transcription factor and serum response factor (“MRTF/SRF”), and methods for their use in treating or preventing cancer and fibrosis. In particular, disclosed herein are compounds of Formula (I) and Formula (II), and pharmaceutically acceptable salts thereof: | 2016-05-26 |
20160145252 | HETEROARYL COMPOUNDS AS IRAK INHIBITORS AND USES THEREOF - The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors. | 2016-05-26 |
20160145253 | SALTS OF AZA-BICYCLIC DI-ARYL ETHERS AND METHODS TO MAKE THEM OR THEIR PRECURSORS - The present invention relates to salts of (R)-3-(6-(4-methylphenyl)-pyridin-3-yloxy)-1-aza-bicyclo[2.2.2]octane, to methods for making them or their precursors, to pharmaceutical compositions comprising them, and to their use as medicaments. | 2016-05-26 |
20160145254 | TRIAZOLOPYRIDINE COMPOUND, AND ACTION THEREOF AS PROLYL HYDROXYLASE INHIBITOR OR ERYTHROPOIETIN PRODUCTION-INDUCING AGENT - The present invention provides a triazolopyridine compound having a prolyl hydroxylase inhibitory action and an erythropoietin production-inducing ability. The present invention relates to a compound represented by the following formula [I]: | 2016-05-26 |
20160145255 | NON-NUCLEOSIDE REVERSE TRANSCRIPTASE INHIBITORS - Compounds of Formula I: | 2016-05-26 |
20160145256 | PROCESS AND INTERMEDIATES FOR THE SYNTHESIS OF 8-[-METHYL]-8-PHENYL-1,7-DIAZA-SPIRO[4.5]DECAN-2-ONE COMPOUNDS - This application discloses a novel process to synthesize 8-[{1-(3,5-Bis-(trifluoromethyl)phenyl)-ethoxy}-methyl]-8-phenyl-1,7-diaza-spiro[4.5]decan-2-one compounds, which may be used, for example, as NK-1 inhibitor compounds in pharmaceutical preparations, intermediates useful in said process, and processes for preparing said intermediates; also disclosed is a process for removal of metals from N-heterocyclic carbine metal complexes. | 2016-05-26 |
20160145257 | SUBSTITUTED XANTHINES AND METHODS OF USE THEREOF - Compounds, compositions and methods are described for inhibiting the TRPC5 ion channel and disorders related to TRPC5. | 2016-05-26 |
20160145258 | Inhibitor Crystalline Form and Preparation Method and Use Thereof - The present invention relates to a new crystalline forms of the inhibitor, 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazoline-4-one; the new crystalline form, compared to known forms, has one or more improved properties. The present invention also relates to a method for preparing a new crystalline form of 5-fluoro-3-phenyl-2-[(S)-1-(9H-purin-6-ylamino)-propyl]-3H-quinazolin-4-one, a pharmaceutical composition thereof and a use thereof in preparation of a pharmaceutical for the treatment and/or prevention of diseases such as chronic lymphocytic leukemia and indolent non-Hodgkin's lymphoma. | 2016-05-26 |
20160145259 | CXCR7 ANTAGONISTS - Compounds having formula I, | 2016-05-26 |
20160145260 | STABLE PEMETREXED ARGININE SALT AND COMPOSITIONS COMPRISING IT - The present invention relates to arginine salt of pemetrexed of formula (1), particularly to a stable solid form thereof, and to pharmaceutical compositions comprising such salt. | 2016-05-26 |
20160145261 | FREE BASE CRYSTALS - The present invention relates to crystals of (6aR,9aS)-5,6a,7,8,9,9a-hexahydro-5-methyl-3-(phenylamino)-2-((4-(6-fluoropyridin-2-yl)phenyl)methyl)-cyclopent[4,5]imidazo[1,2-a]pyrazolo[4,3-e]pyrimidin-4(2H)-one, and methods of making and using such crystals. | 2016-05-26 |
20160145262 | NEW POLYMORPHIC FORMS OF ICOTINIB PHOSPHATE AND USES THEREOF - Disclosed is Icotinib phosphate (i.e., the compound of Formula (I)) and polymorph forms thereof, and methods of preparing and using them. | 2016-05-26 |
20160145263 | TETRAHYDROISOQUINOLINES CONTAINING SUBSTITUTED AZOLES AS FACTOR XIA INHIBITORS - The present invention provides compounds of Formula (I), or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein all the variables are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of FXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same. | 2016-05-26 |
20160145264 | NOVEL LIPOPHILIC N-SUBSTITUTED NORCANTHARIMIDE DERIVATIVES AND USES THEREOF - Novel N-substituted norcantharimide derivatives are disclosed herein. The novel N-substituted norcantharimide derivatives are useful as lead compounds for manufacturing a medicament or a pharmaceutical composition for treating cancer, particularly for treating leukemia. | 2016-05-26 |
20160145265 | METHOD AND APPARATUS FOR THE SYNTHESIS OF DIHYDROARTEMISININ AND ARTEMISININ DERIVATIVES - The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C | 2016-05-26 |
20160145266 | COMPOUNDS FOR THE TREATMENT OF CLOSTRIDIUM DIFFICILE ASSOCIATED DISEASE - Disclosed are compounds of formula (I): | 2016-05-26 |
20160145267 | HETEROARYL SUBSTITUTED PYRAZOLES - Compounds of formula (I), which are inhibitors of Bub1 kinase, processes for their production and their use as pharmaceuticals. | 2016-05-26 |
20160145268 | SUBSTITUTED HETEROCYCLIC COMPOUNDS AS CRAC MODULATORS - The invention relates to compounds of Formula (I) and their pharmaceutically acceptable salts, wherein the substituents are as described herein, and their use in medicine for the treatment of diseases, disorders associated with the modulation of calcium release-activated calcium (CRAC) channel. The invention also relates to pharmaceutical compositions containing such compounds in treating diseases disorders associated with calcium release-activated calcium (CRAC) channel modulators. wherein, ring D is Formula (a) or Formula (b): A and B, which may be same or different, are independently CR | 2016-05-26 |
20160145269 | DOLUTEGRAVIR SALTS - Dolutegravir potassium salt and solid state forms thereof are provided, as well as methods of making and interconverting these forms. The Dolutegravir potassium forms, and pharmaceutical compositions containing them, may be used to treat subjects in need of medical treatment, such as for HIV infection. | 2016-05-26 |
20160145270 | COMPOUNDS FOR TREATING SPINAL MUSCULAR ATROPHY - The present invention provides compounds of formula (I) wherein A, B, X, Y, R1 and R2 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments. | 2016-05-26 |
20160145271 | BENZYL-1H-PYRAZOLO[3,4-B]PYRIDINES AND USE THEREOF - The present application relates to novel benzyl-1H-pyrazolo[3,4-b]pyridines, to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases, and to their use for producing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders. | 2016-05-26 |
20160145272 | TRIAZOLO-PYRAZINYL DERIVATIVES USEFUL AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS - A compound of Formula I | 2016-05-26 |
20160145273 | PRECATALYST FOR SHIBASAKI'S RARE EARTH METAL BINOLATE CATALYSTS - Disclosed herein are schemes for the synthesis of novel hydrogen-bonded rare earth-BINOLate precatalyst complexes, the precatalysts, per se, and their application for the generation of anhydrous REMB catalysts by cation-exchange from metal halides. | 2016-05-26 |
20160145274 | REAGENT FOR ENHANCING GENERATION OF CHEMICAL SPECIES - A reagent that enhances acid generation of a photoacid generator and composition containing such reagent is disclosed. | 2016-05-26 |
20160145275 | FLAME RETARDANT FILLER - A flame retardant filler having brominated silica particles, for example, imparts flame retardancy to manufactured articles such as printed circuit boards (PCBs), connectors, and other articles of manufacture that employ thermosetting plastics or thermoplastics. In this example, brominated silica particles serve both as a filler for rheology control (viscosity, flow, etc.) and a flame retardant. In an exemplary application, a PCB laminate stack-up includes conductive planes separated from each other by a dielectric material that includes a flame retardant filler comprised of brominated silica particles. In an exemplary method of synthesizing the brominated silica particles, a monomer having a brominated aromatic functional group is reacted with functionalized silica particles (e.g., isocyanate, vinyl, amine, or epoxy functionalized silica particles). Alternatively, a monomer having a brominated aromatic functional group may be reacted with a silane to produce a brominated alkoxysilane monomer, which is then reacted with the surface of silica particles. | 2016-05-26 |
20160145276 | TRACELESS DIRECTING GROUPS IN RADICAL CASCADES: FROM OLIGOALKYNES TO FUSED HELICENES WITHOUT TETHERED INITATORS - The present disclosure is directed to a traceless directing group in a radical cascade. The chemo- and regioselectivity of the initial attack in skipped oligoalkynes is controlled by a propargyl alkoxy moiety. Radical translocations lead to the boomerang return of radical center to the site of initial attack where it assists to the elimination of the directing functionality via β-scission in the last step of the cascade. In some aspects, the reaction of the present invention is catalyzed by a stannane moiety, which allows further via facile reactions with electrophiles as well as Stille and Suzuki cross-coupling reactions. This selective radical transformation opens a new approach for the controlled transformation of skipped oligoalkynes into polycyclic ribbons of tunable dimensions. | 2016-05-26 |
20160145277 | B-Ketophosphonic Acids And Dental Materials Based Thereon - β-Ketophosphonic acid according to general formula I: | 2016-05-26 |
20160145278 | Compound, Manufacturing Method Therefor, and Method for Manufacturing Optically Active alpha-Aminophosphonate Derivative - A method for producing a compound represented by General Formula (1), the method including:
| 2016-05-26 |
20160145279 | STAT6 INHIBITORS - The present disclosure provides compounds that are useful for inhibiting the STAT6 pathway. Also provided are related pharmaceutical compositions and methods of using the compounds. In some embodiments, the compounds may be used to treat a disease such as, e.g., an allergic lung disease, allergic rhinitis, chronic pulmonary obstructive disease, or a cancer. | 2016-05-26 |
20160145280 | TUNABLE FLUORESCENCE USING CLEAVABLE LINKERS - The invention relates to cleavable chemistry in general, and in particular, to tunable fluorescence using cleavable linkers present in fluorochrome-quencher conjugates. | 2016-05-26 |
20160145281 | NEW IRIDIUM-BASED COMPLEXES FOR ECL - Novel iridium-based Ir(III) luminescent complexes, conjugates comprising these complexes as a label and their application, for example in the electrochemiluminescence based detection of an analyte. | 2016-05-26 |
20160145282 | METAL COMPLEX INCLUDING TRIDENTATE AMINODICARBENE LIGAND AND HYDROGENATION REDUCTION METHOD USING SAME - The use of a metal complex containing a ruthenium ion or an osmium ion, and a tridentate aminodicarbene ligand, the tridentate aminodicarbene ligand having one secondary amino group and two specific heterocyclic carbene groups sandwiching the amino group, enables hydrogenation reduction of carbonyl compounds, such as ketones, carboxylic acid esters, lactones, carboxylic acid amides, and lactams, and imine compounds under relatively mild conditions to produce corresponding alcohols, amines, and the like in a high yield with high catalytic efficiency. The metal complex is obtained by a method comprising steps of reacting a specific metal compound with a specific aminodicarbene precursor and subsequently reacting a specific compound. Reduction of a carbonyl compound or an imine compound in the presence of this metal complex using a hydrogen donor makes it possible to reduce the carbonyl compound or imine compound by hydrogenation. | 2016-05-26 |
20160145283 | NOVEL CATALYSTS HAVING A SILENE LIGAND - A subject matter of the present invention is the use as catalyst, in particular in hydrosilylation, of a metal complex including at least one metal atom chosen from the metals of Groups 8, 9 and 10 of the Periodic Table of the Elements and one or more ligands, characterized in that at least one ligand includes a silene structure. | 2016-05-26 |
20160145284 | LIPID-BASED PLATINUM COMPOUNDS AND NANOPARTICLES - The present disclosure is in relation to the field of nanotechnology and cancer therapeutics. In particular, the present disclosure relates to platinum based compounds comprising platinum moiety, linker moiety and lipid moiety and corresponding nanoparticles thereof. The disclosure further relates to synthesis of said platinum based compounds, nanoparticles and compositions comprising said platinum based compounds/nanoparticles. The disclosure also relates to methods of managing cancer by employing aforesaid carbene compounds, platinum based compounds, nanoparticles and compositions thereof. | 2016-05-26 |
20160145285 | Bio-Oil Polyols, Alkoxylated Bio-Oil Polyols and Bio-Oil Phenolic Resins - Methods are provided for producing bio-oil polyols, alkoxylating bio-oil polyols to provide polyols, and for employing the alkoxylated bio-oil polyols for making polymers or copolymers of polyesters or polyurethanes. Compositions and methods are provided for incorporating bio-oils into phenolic resins such as phenol-formaldehyde resin and phenol-formaldehyde-urea resin, as well as hot melt adhesive compositions. | 2016-05-26 |
20160145286 | Novel Crystalline Hydrates of 1-(Beta-D-Glucopyranosyl)-4-Methyl-3-[5-(4-Fluorophenyl)-2-Thienylmethyl]- Benzene - The present invention relates to non-stoichiometric crystalline hydrates of 1-(β-D-glucopyranosyl)-4-methyl-3-[5-(4-fluorophenyl)-2-thienylmethyl]benzene, processes for their preparation, and their use as medicaments. In addition the present invention relates to pharmaceutical compositions comprising an effective amount of the novel crystalline hydrates. | 2016-05-26 |
20160145287 | Dendrimer Scaffolds for Pharmaceutical Use - This invention relates to certain dendrimer compounds. In particular, this invention relates to novel dendrimer compounds that can be elaborated to give increasingly large and complex compounds. These elaborated compounds can be attached to, or can encapsulate within, active agent(s) so as to beneficially modify the characteristics of that active agent. Alternatively, the elaborated compounds can themselves be beneficially modified into therapeutic agents by the attachment of inactive agents. | 2016-05-26 |
20160145288 | EDIBLE PLASTICIZERS FOR FOOD AND FOOD PACKAGING FILMS - Disclosed are plasticizers, salts thereof, chelates thereof and cleavage derivatives thereof, that exhibit a superior combination of properties. The plasticizers can be used for a variety of purposes, including food preparation, cosmetics, beverages and polymeric matrices. The plasticizers can be prepared by esterifying gallic acid, fulvic acid, or tannic acid. | 2016-05-26 |
20160145289 | COMPOUNDS AND METHODS FOR TREATING BACTERIAL INFECTIONS - The present invention encompasses compounds and methods for treating and preventing bacterial infections specifically urinary tract infections and those caused by bacteria containing type 1 pili and FimH. The present invention also encompasses compounds and methods for treating inflammatory bowel disease specifically Crohn's Disease. | 2016-05-26 |
20160145290 | E-SELECTIN ANTAGONIST COMPOUNDS, COMPOSITIONS, AND METHODS OF USE - Methods and compositions using E-selectin antagonists are provided for the treatment and prevention of diseases and disorders treatable by inhibiting binding of E-selectin to an E-selectin ligand. Described herein are E-selection antagonists including, for example, glycomimetic compounds, antibodies, aptamers and peptides that are useful in methods for treatment of cancers, and treatment and prevention of metastasis, inhibiting infiltration of the cancer cells into bone marrow, reducing or inhibiting adhesion of the cancer cells to endothelial cells including cells in bone marrow, and inhibiting thrombus formation. | 2016-05-26 |
20160145291 | Therapeutic Monosaccharide-Based Inhibitors of Hexokinase and Glucokinase for Parasitic Diseases, Along with Methods of their Formation and Use - Methods for treating a mammal that is infected by a parasitic organism are provided, along with pharmaceutical compositions and compounds. The method includes administering to the mammal the pharmaceutical composition of FIG. | 2016-05-26 |
20160145292 | PHOSPHOROAMIDATE ESTERS, AND USE AND SYNTHESIS THEREOF - Phosphoramidate esters and related nucleotide analogs useful in polynucleotide sequencing techniques, and synthetic methods for preparing those compounds, are disclosed. These compounds include nucleotide phosphoramidates analogs that are modified on the alpha-phosphate to enable attachment of a variety of application-specific substituents such as tether molecules. | 2016-05-26 |
20160145293 | OLIGONUCLEOTIDES CONTAINING HIGH CONCENTRATIONS OF GUANINE MONOMERS - This invention pertains to methods for oligonucleotide synthesis, specifically the synthesis of oligonucleotides that contain a high content of guanine monomers. In more detail, the invention relates to a method for coupling a nucleoside phosphoramidite during the synthesis of an oligonucleotide to a universal support, to a first nucleoside, or to an extending oligonucleotide. The invention further relates to oligonucleotides obtainable by the methods of the invention. | 2016-05-26 |
20160145294 | Antagonists of CB1 Receptor - The invention relates to an antagonist of CB1 receptor for use in the treatment of a pathologic condition or disorder selected from the group consisting of bladder and gastrointestinal disorders; inflammatory diseases; cardiovascular diseases; nephropathies; glaucoma; spasticity; cancer; osteoporosis; metabolic disorders; obesity; addiction, dependence, abuse and relapse related disorders; psychiatric and neurological disorders; neurodegenerative disorders; autoimmune hepatitis and encephalitis; pain; reproductive disorders and skin inflammatory and fibrotic diseases. | 2016-05-26 |
20160145295 | TETRAZOLE DERIVATIVES OF BILE ACIDS AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF - The present invention provides compounds of Formula I: | 2016-05-26 |
20160145296 | BILE ACID ANALOGS AS FXR/TGR5 AGONISTS AND METHODS OF USE THEREOF - The present invention relates to compounds of Formula (IA) and Formula (IB), | 2016-05-26 |
20160145297 | HYDROXY-ETHYLENE DERIVATIVES FOR THE TREATMENT OF ARTHROSIS - The present invention relates to compounds of the formula I and in particular medicaments comprising at least one compound of the formula I for use in the treatment and/or prophylaxis of physiological and/or pathophysiological conditions in the triggering of which cathepsin D is involved, in particular for use in the treatment and/or prophylaxis of arthrosis, traumatic cartilage injuries, arthritis, pain, allodynia or hyperalgesia. | 2016-05-26 |
20160145298 | MACROCYCLIC PROLINE DERIVED HCV SERINE PROTEASE INHIBITORS - The present invention discloses compounds of Formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof: | 2016-05-26 |
20160145299 | Cell Penetrating Peptides for Intracellular Delivery of Molecules - A cell-penetrating peptide characterized in that it comprises an amino acid sequence consisting of a beta-alanine or a serine in N-terminal position, linked to a sequence consisting of 9 consecutive amino acids from the sequence RXWXRLWXRLR (SEQ ID NO:7), wherein X in position 2 is R or S and X in positions 4 and 8 are, independently from each other, W or F. | 2016-05-26 |
20160145300 | ARTIFICIAL DECAPEPTIDE, MEDICATION AND METHOD OF INDUCING BREEDING OF CRUSTACEANS - The present invention provides an artificial decapeptide for inducing the development of gonad in crustacean, a medication including the artificial decapeptide and a method of inducing the gonad development of crustacean. The method includes administrating an effective amount of an artificial decapeptide to a crustacean, thereby promoting gonad development of crustaceans, wherein the artificial decapeptide includes a sequence set forth in SEQ ID NO: 2. | 2016-05-26 |
20160145301 | PROCESS FOR THE MANUFACTURE OF DEGARELIX AND ITS INTERMEDIATES - The present invention relates to a liquid (or solution)-phase manufacturing process for preparing the decapeptide Degarelix, its protected precursor, and other useful intermediates. The invention further relates to polypeptides useful in the solution-phase manufacturing process and to the purification of Degarelix itself. Degarelix can be obtained by subjecting a Degarelix precursor according to formula II: (P | 2016-05-26 |
20160145302 | A SHORT PEPTIDE TARGETING EPS8 BINDING WITH EGFR AND USE THEREOF - The present invention discloses a short peptide targeting EPS8 binding with EGFR and use thereof, and sequence of the short peptide is N′-Arg-Lys-Lys-Asn-Lys-Pro-Pro-Pro-Pro-Lys-Lys-C′. The short peptide can effectively inhibit proliferation of EPS8 positive tumors, and can also be used to make a pharmaceutical preparation for treating EPS8 positive tumors, which has the potential of being developed into anti-cancer peptide inhibitor drugs. | 2016-05-26 |
20160145303 | Strong Secretory Signal Peptide Enhancing Small Peptide Motifs and the Use Thereof - The present invention belongs to protein engineering and genetic engineering fields, relating to a strong secretory signal peptide enhancing small peptide motifs and the use thereof. The strong secretory signal peptide enhancing small peptide motifs of the present invention have the amino acid sequence of the following formula: M (αXβYγ/αYβXγ) | 2016-05-26 |
20160145304 | CYSTOBACTAMIDES - The present invention provides cystobactamides of formula (I) and the use thereof for the treatment or prophylaxis of bacterial infections: | 2016-05-26 |
20160145305 | ENERGY TRANSFER WITHIN PI-CONJUGATED PEPTIDE HETEROSTRUCTURES IN AQUEOUS ENVIRONMENTS - Nanostructures comprising Π-conjugated peptides for energy migration in aqueous environments are disclosed. Conductive material comprising these nanostructures, and supramolecular assemblies comprising covalently-bound electron donor-acceptor chromophores for photoinduced electron transfer also are disclosed. | 2016-05-26 |
20160145306 | ORAL PEPTIDE INHIBITORS OF INTERLEUKIN-23 RECEPTOR AND THEIR USE TO TREAT INFLAMMATORY BOWEL DISEASES - The present invention provides novel peptide inhibitors of the interleukin-23 receptor, and related compositions and methods of using these peptide inhibitors to treat or prevent a variety of diseases and disorders, including inflammatory bowel disease. | 2016-05-26 |
20160145307 | ULTRA-PURE AGONISTS OF GUANYLATE CYCLASE C, METHOD OF MAKING AND USING SAME - The invention provides processes of purifying a peptide including a GCC agonist sequence selected from the group consisting of SEQ ID NOs: 1-251 described herein. The processes include a solvent exchange step before a freeze-drying (lyophilization) step. | 2016-05-26 |
20160145308 | Compositions and Methods for Targeted Endometriosis Treatment - Disclosed are compositions and methods for selectively targeting an endometriosis cell. Also disclosed are compositions and methods for treating endometriosis. | 2016-05-26 |
20160145309 | DISULFIDE CYCLIC POLYPEPTIDES FOR THE TREATMENT OF HEART FAILURE - The invention provides a synthetic polypeptide of Formula I′: X1-R-P-R-X5-X6-X7-K-X9-P-X11-X12-X13 or an amide, an ester, a salt or a bioconjugate thereof, wherein X1, X5, X6, X7, X9 and X11 to X13 are defined herein. The polypeptides and bioconjugates are agonist of the APJ receptor. The invention also relates to a method for manufacturing the polypeptides or bioconjugates of the invention, and its therapeutic uses such as treatment or prevention of acute decompensated heart failure (ADHF), chronic heart failure, pulmonary hypertension, atrial fibrillation, Brugada syndrome, ventricular tachycardia, atherosclerosis, hypertension, restenosis, ischemic cardiovascular diseases, cardiomyopathy, cardiac fibrosis, arrhythmia, water retention, diabetes (including gestational diabetes), obesity, peripheral arterial disease, cerebrovascular accidents, transient ischemic attacks, traumatic brain injuries, amyotrophic lateral sclerosis, burn injuries (including sunburn) and preeclampsia. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition. | 2016-05-26 |
20160145310 | HYPERSENSITIVE RESPONSE ELICITOR PEPTIDES AND USE THEREOF - Disclosed are hypersensitive-response eliciting peptides that exhibit improved solubility, stability, resistance to chemical degradation, or a combination of these properties. Use of these peptides or fusion polypeptides, or DNA constructs encoding the same, for modulating plant biochemical signaling, imparting disease resistance to plants, enhancing plant growth, imparting tolerance to biotic stress, imparting tolerance and resistance to abiotic stress, imparting desiccation resistance to cuttings removed from ornamental plants, imparting post-harvest disease or post-harvest desiccation resistance to a fruit or vegetable, or enhancing the longevity of fruit or vegetable ripeness are also disclosed. | 2016-05-26 |
20160145311 | COMPOSITIONS COMPRISING FIBROUS POLYPEPTIDES AND POLYSACCHARIDES - Isolated polypeptides are disclosed comprising an amino acid sequence encoding a monomer of a fibrous polypeptide attached to a heterologous polysaccharide binding domain. Composites comprising same, methods of generating same and uses thereof are all disclosed. | 2016-05-26 |
20160145312 | CETP ANTIGENIC PEPTIDE AND FUSION PROTEIN AND THEIR COMPOSITION AND APPLICATIONS - The disclosure provides an antigenic peptide targeting the extracellular, but not the intracellular, form of CETP to reduce the level of LDL (including oxLDL and other derivatives of LDL) and increase the level of HDL. Accordingly, the disclosure provides a CETP vaccine to overcome the low immunogenicity of CETP and for long-term inhibition of CETP activity to prevent or treat oxLDL or other LDL derivative-related diseases/symptoms. | 2016-05-26 |
20160145313 | COMPOSITIONS AND METHODS FOR TREATING CANCER - The present invention provides compositions and methods of treating MUC16 expressing cancer. | 2016-05-26 |
20160145314 | COMPOSITIONS AND METHODS OF USING THERAPEUTIC p53 PEPTIDES AND ANALOGUES - The present invention relates to compositions useful in inhibiting Bcl-XL or MCL-1 and disrupting p53-MDM2 and p53-MDMX interactions, and methods of using those compositions for treating a subject for conditions responsive to increasing p53 mediated activity or promoting p53 independent apoptosis, such as treating cancer. In some aspects, the compositions of this invention relate to fusion polypeptides comprising a human serum polypeptide and a p53-peptide, which can be, in some aspects, a p53 derived peptide and/or a p53 activating peptide. | 2016-05-26 |
20160145315 | PEPTIDE ANTAGONISTS OF THE CALCITONIN CGRP FAMILY OF PEPTIDE HORMONES AND THEIR USE - The embodiments provide a modified calcitonin gene-related peptide antagonist including an N-terminal fragment of modified calcitonin gene-related peptide or related protein family member where at least two residues of the N-terminal fragment are cysteine (Cys) and at least one amino acid comprises a non-threonine substitution of a threonine (Thr) residue; a central core where the central core comprises an a-helix; and a C-terminal fragment of modified calcitonin gene-related peptide or related protein family member comprising a C-terminal amide and where at least one amino acid of the C-terminal fragment is phenylalanine (Phe), proline (Pro), tyrosine (Tyr) or hydroxyproline (Hyp) or pharmaceutically acceptable salt thereof, as well as compositions, including pharmaceutical compositions, comprising a subject peptide. The embodiments further provide treatment methods, including methods of treating a migraine, the methods generally involving administering to an individual in need thereof an effective amount of a subject peptide or composition. | 2016-05-26 |