Patents Issued in August 27, 2020
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Publication number: 20200270182Abstract: A method for producing a coating system includes depositing a first slurry on a composite substrate, the first slurry including a first carrier fluid and boron-containing powder, removing the first carrier fluid and consolidating the boron-containing powder to form a boron-containing layer on the composite substrate, depositing a silicon-containing coating on the boron-containing layer and consolidating the silicon-containing coating to form a silicon-containing layer, and depositing at least one layer of phosphate on the silicon-containing layer.Type: ApplicationFiled: February 27, 2019Publication date: August 27, 2020Inventors: Steven Poteet, Gavin Charles Richards, Zachary Cohen
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Publication number: 20200270183Abstract: A potassium humate, rock phosphorous, sulfur granule: a fully soluble potassium humate component comprising about 3% of the composite granule; a sulfur component comprising about 15% of the composite granule; and a rock phosphate powder component comprising about 82% of the composite granule. The composite granule is semi-soluble and has a pH of 2.5 to about 12.Type: ApplicationFiled: April 17, 2019Publication date: August 27, 2020Inventor: Kevin Merritt
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Publication number: 20200270184Abstract: The present invention relates to a controlled-release type fertilizer with outstandingly decreased floating property, comprising a granular fertilize core; a coating layer (shell) formed on the surface of the granular fertilizer core, and comprising olefin-based resin; and additives attached on the coating layer, and comprising ethylene oxide-propylene oxide-ethylene oxide(EO-PO-EO) or propylene oxide-ethylene oxide-propylene oxide(PO-EO-PO) tri-block copolymer.Type: ApplicationFiled: September 13, 2018Publication date: August 27, 2020Applicants: LG CHEM, LTD., FarmHannong Co., Ltd.Inventors: Mihee KIM, Hyosook JOO, Eun Kyoung PARK, Hyeon CHOI, Kiyoul YOON, Joon Seok LEE
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Publication number: 20200270185Abstract: The present invention relates to a controlled-release type fertilizer with remarkably decreased floating property, comprising a granular fertilizer core; a coating layer (shell) formed on the surface of the granular fertilizer core, and comprising olefin-based resin; and additives attached on the coating layer, and comprising polyoxyethylene alkyl(-aryl)ether.Type: ApplicationFiled: September 13, 2018Publication date: August 27, 2020Applicants: LG CHEM, LTD., FarmHannong Co., Ltd.Inventors: Mihee KIM, Hyosook JOO, Eun Kyoung PARK, Hyeon CHOI, Kiyoul YOON, Joon Seok LEE
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Publication number: 20200270186Abstract: The present invention relates to a method for producing an aldehyde by a hydroformylation reaction of reacting an olefin with hydrogen and carbon monoxide in the presence of a Group 8 to 10 metal-phosphine complex catalyst, including the following steps (1) and (2): (1) a step of oxidizing by withdrawing a reaction solution having accumulated therein a high-boiling-point byproduct from a reaction zone and bringing the withdrawn reaction solution into contact with an oxygen-containing gas, and (2) a step of, after the step (1), mixing a poor solvent and hydrogen with the reaction solution, then crystallizing the Group 8 to 10 metal-phosphine complex catalyst by crystallization, and recovering the crystallized complex catalyst from the reaction solution.Type: ApplicationFiled: May 11, 2020Publication date: August 27, 2020Applicant: Mitsubishi Chemical CorporationInventors: Takashi Sato, Yoshiyuki Tanaka
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Publication number: 20200270187Abstract: A method for preparing aromatics from syngas, which includes a) contacting a raw material stream containing syngas with a catalyst in a reaction zone under reaction conditions sufficient to convert at least part of the raw material to obtain a reaction effluent; b) separating the reaction effluent to obtain at least a recycle stream containing gas-phase hydrocarbons having 1 to 4 carbon atoms and unconverted syngas and a liquid stream containing hydrocarbons having 5 or more carbon atoms; c) returning the recycle stream to the reaction zone; and d) separating aromatic products from the liquid stream, wherein the catalyst includes at least one of an inert carrier-confined highly dispersed metal oxide material, an acidic molecular sieve, and, optionally, graphite powder and a dispersant.Type: ApplicationFiled: October 29, 2018Publication date: August 27, 2020Applicant: DALIAN INSTITUTE OF CHEMICAL PHYSICS, CHINESE ACADEMY OF SCIENCESInventors: Youming NI, Wenliang ZHU, Zhongmin LIU, Yong LIU, Zhiyang CHEN, Hongchao LIU, Xiangang MA, Shiping LIU
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Publication number: 20200270188Abstract: A method for directly preparing p-xylene from synthetic gas and aromatic hydrocarbon. The method includes contacting the feedstock containing synthetic gas and aromatic hydrocarbon excluding p-xylene with the catalyst in the reaction zone under reaction conditions sufficient to convert at least part of the feedstock to obtain a reaction effluent containing p-xylene; and separating p-xylene from the reaction effluent, where the catalyst includes a highly dispersed metal oxide material confined by an inert carrier, an acidic molecular sieve, and optionally at least one of graphite powder and dispersant, where in the highly dispersed metal oxide material confined by the inert carrier, the inert carrier is at least one of silicon oxide and alumina, and the content of the metal oxide in terms of metal is less than or equal to 10% by mass calculated based on the weight of the highly dispersed metal oxide material confined by the inert carrier.Type: ApplicationFiled: November 21, 2017Publication date: August 27, 2020Applicant: DALIAN INSTITUTE OF CHEMICAL PHYSICS, CHINESE ACADEMY OF SCIENCESInventors: Youming NI, Wenliang ZHU, Zhongmin LIU, Yong LIU, Zhiyang CHEN, Hongchao LIU, Xiangang MA, Shiping LIU
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Publication number: 20200270189Abstract: A method for producing para-xylene (PX) includes introducing a C8 aromatic-containing composition to a xylene rerun column to separate the C8 aromatic-containing composition into a xylene-containing effluent and a heavy effluent and passing the xylene-containing effluent to a PX processing loop that includes a PX recovery unit operable to separate a PX product from the xylene-containing effluent, a membrane isomerization unit operable to convert a portion of the MX, OX, or both from the xylene-containing effluent to PX, an EB dealkylation unit operable to dealkylate EB from the xylene-containing effluent to produce benzene, toluene, and other C7? compounds, and a membrane separation unit operable to produce a permeate that is PX-rich and a retentate that is PX-lean. The permeate is passed to the PX recovery unit for recovery of PX, which the retentate is bypassed around the PX recovery unit circulated through the xylene processing loop.Type: ApplicationFiled: February 22, 2019Publication date: August 27, 2020Applicant: Saudi Arabian Oil CompanyInventors: Zhonglin Zhang, Sohel K. Shaikh, Veera Venkata R. Tammana, Raed H. Abudawoud, Bruce Richard Beadle, Hisham Tawfiq Bassam, Rakan Sulaiman Bilaus
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Publication number: 20200270190Abstract: A process for the hydrogenation or hydrogenolysis of an oxygenate is disclosed. The process takes place in a reactor in the presence of a catalyst, hydrogen and liquid water and the catalyst comprises one or more elements from Groups 8 to 11 of the periodic table dispersed on a hydrothermally stable oxide support.Type: ApplicationFiled: December 15, 2016Publication date: August 27, 2020Inventors: Dionysius Jacobus Maria DE VLIEGER, Jean Paul Andre Marie Joseph Ghislain LANGE, Smita EDULJI, Hendrik Albertus COLIJN
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Publication number: 20200270191Abstract: Provided is a process for the preparation of certain 1,4-bicyclo[2.2.2]octane derivatives. The new synthetic procedure involves treating 1,4-dimethylene cyclohexane with an oxidizing agent in the presence of a transition metal catalyst to afford an oxo-substituted bicyclo[2.2.2]octane species. This intermediate structure can then be further derivatized. The processes of this disclosure thus affords a novel and simplified means for the commercial production of a wide variety of bicyclo[2.2.2]octane derivatives.Type: ApplicationFiled: October 10, 2018Publication date: August 27, 2020Applicant: Eastman Chemical CompanyInventors: Yue Rachel HU, Robert Thomas HEMBRE, Gerald Charles TUSTIN, Zhufang LIU, Steven J. ADAMS
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Publication number: 20200270192Abstract: A process of purification of a homoallylic alcohol by distillation in the presence of a base, wherein the homoallylic alcohol is E,E-homofarnesol.Type: ApplicationFiled: October 30, 2018Publication date: August 27, 2020Inventors: Alain BRINGHEN, Jacques MEMBREZ
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Publication number: 20200270193Abstract: Described herein are polymorphic forms of 1,6-dibromo-1,6-dideoxy-dulcitol (dibromo dulcitol or DBD), which is a known antitumor agent. Also described are methods of making these new crystalline polymorphic forms as well as methods of using these polymorphic forms to treat cancer.Type: ApplicationFiled: May 12, 2020Publication date: August 27, 2020Applicant: Targent, LLCInventors: Stefano Luca Giaffreda, Elena Dichiarante
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Publication number: 20200270194Abstract: Method of forming a trisubstituted ethylene compound, the method comprising: (A) providing a trisubstituted ethylene compound bearing a first, a second and a third substituent, in which the first and the second substituent are bound to the one olefinic carbon atom and are different from one another; (B) providing a monosubstituted ethylene compound or a disubstituted ethylene compound in which the substituents are vicinally bound to the olefinic carbon atoms, bearing at least a fourth substituent, respectively; (C) subjecting the trisubstituted ethylene compound provided in step (A) to a cross-metathesis reaction with olefin provided in step (B) to form said trisubstituted ethylene, wherein the cross-metathesis reaction is catalysed by a transition metal complex bearing ligands from which one ligand is a carbene ligand, wherein the carbene complex is characterized by a M?C moiety, wherein M is the transition metal; and wherein the reaction proceeds stereoselectively.Type: ApplicationFiled: September 21, 2018Publication date: August 27, 2020Inventors: Amir H. Hoveyda, Thach T. Nguyen, Ming Joo Koh, Chaofan Xu, Sebastian Torker, Richard Royce Schrock
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Publication number: 20200270195Abstract: The invention relates to an esterification unit (150) and esterification process for producing crude methyl methacrylate (MMA) from methacrylamide (MAM), which enable particularly to improve the yield, meaning that the organics spent acids are low; and at the same time, providing crude MMA with rather good quality, meaning that MMA concentration in crude MMA is rather high and preferably from 50 wt % to 80 wt %. According to the invention, the esterification unit comprises esterification reactors (1, . . . , 5 (or 6) set up in a serial way so that there is a counter current flow between gaseous phase and liquid phase, the liquid phase flowing from first reactor (1) of the series to last reactor (5 (or 6)), and the gaseous phase flowing from reactor to first reactor (1).Type: ApplicationFiled: October 15, 2018Publication date: August 27, 2020Inventors: Yves Bernardin, Romain Billon, Xavier Marcarian, Florent Vallet
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Publication number: 20200270196Abstract: Provided is a citrate-based plasticizer and a resin composition including the same. The citrate-based plasticizer includes one or more citrates having alkyl groups with 7 carbon atoms. The citrate-based plasticizer can solve limitations on migration and volatile loss inherent in the conventional plasticizer and limitations on characteristics of processing such as plasticizing efficiency and absorption rate.Type: ApplicationFiled: May 21, 2018Publication date: August 27, 2020Inventors: Hyun Kyu KIM, Yun Ki CHO, Joo Ho KIM, Jeong Ju MOON
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Publication number: 20200270197Abstract: The present invention relates to a process for continuous hydrogenation of a nitro compound to the corresponding amine in a liquid reaction mixture comprising the nitro compound in a reaction chamber in the presence of a supported catalyst which comprises as the active component at least one element from groups 7 to 12 of the periodic table of the elements, wherein ammonia is added to the reaction chamber during the hydrogenation.Type: ApplicationFiled: October 8, 2018Publication date: August 27, 2020Applicant: BASF SEInventors: Barbara WUCHER, Thomas HEIDEMANN, Michael FRIKO, Christian BECHTOLD
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Publication number: 20200270198Abstract: Provided is a method of refining 1,5-diaminopentane, the method including preparing a fermented broth including a carbonate salt of 1,5-diaminopentane; preparing a first composition by heating the fermented broth; preparing a second composition and an evaporation residue by evaporating the first composition; preparing a third composition by adding water to the evaporation residue and evaporating the water; and recovering 1,5-diaminopentane by distilling the second composition and the third composition.Type: ApplicationFiled: October 8, 2018Publication date: August 27, 2020Inventors: Seok Hyun KANG, Won Sik GWAK, Chang Yub OH, Jin Tae HONG
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Publication number: 20200270199Abstract: A preparation method for a racemic adrenaline as represented by formula II. The method may comprise the following steps: compound 1 is directly racemized in an acidic solution to produce compound 2, the acid solution comprising neither sodium bisulfite nor salicylic acid; and specifically comprises (a), in the acid solution of which the pH is 0.5-1.5, compound 1 is placed under the protection of nitrogen gas and, with the reaction temperature being controlled at 75-95ยฐ C., stirred and reacted for 1-3 hours; (b) the reaction solution is controlled at a temperature of 5-20ยฐ C., into which an activated carbon is added, under the protection of nitrogen gas, stirred for 20-40 minutes, and filtered, then a filtrate is collected; the filtrate is controlled at a temperature of 5-20ยฐ C., the pH thereof is adjusted using ammonia to 8.5-9.5, and is filtered when the pH is stabilized, and a filter cake is washed and dried to produce a high purity racemic adrenaline white powder.Type: ApplicationFiled: March 5, 2019Publication date: August 27, 2020Inventors: Yin WANG, Aoxiang ZHANG, Yonggang XU, Song CHEN, Haoning ZHANG
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Publication number: 20200270200Abstract: An anthraquinone compound of formula I (such as the compounds of formulae II to X) and processes for making the same are provided. Pharmaceutical compositions for use in the treatment of cancer, optionally in combination with an agent capable of reducing the level of oxygenation of a tumour, are also provided. Additionally, an option for combination with chemotherapeutic and radiotherapeutic modalities to enhance overall tumour cell kill is provided. Methods for the detection of cellular hypoxia, both in vivo and in vitro, are additionally provided.Type: ApplicationFiled: August 19, 2019Publication date: August 27, 2020Inventors: Stefan OGRODZINSKI, Paul SMITH, Stephanie MCKEOWN, Laurence PATTERSON, Rachel Jane ERRINGTON
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Publication number: 20200270201Abstract: Provided herein are compounds of the formulas: wherein: n, X2, R3, R3?, R4, R4?, R5, R5?, R6, and R6? are as defined herein. Pharmaceutical compositions of the compounds are also provided. In some aspects, these compounds may be used for the treatment of diseases, including diabetic peripheral neuropathy or cancer.Type: ApplicationFiled: January 29, 2020Publication date: August 27, 2020Inventors: Brian S.J. BLAGG, Rick T. DOBROWSKY, Mercy ANYIKA
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Publication number: 20200270202Abstract: Compounds, compositions, and methods for the treatment of Canavan disease are described.Type: ApplicationFiled: March 23, 2017Publication date: August 27, 2020Applicant: The University of ToledoInventors: Ronald E. Viola, Bharani Thangavelu, Vinay Mutthamsetty, Qinzhe Wang
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Publication number: 20200270203Abstract: A novel branched fluorine-containing compound represented by formula (1): (RfโY?n1L?X-A)n2??(1) wherein L represents a predetermined carbon-containing linker moiety; Rf, in each occurrence, is the same or different and represents fluoroalkyl optionally having at least one ether bond; Y, in each occurrence, is the same or different and represents a predetermined divalent linking group or a bond; RY, in each occurrence, is the same or different and represents hydrogen or an organic group; L represents an (n1+n2)-valent carbon-containing linker moiety having at least one carbon atom; n1 represents a number greater than or equal to 1; n2 represents a number greater than or equal to 1; n1+n2 is a number from 3 to 6; X, in each occurrence, is the same or different and represents a divalent linking group or a bond; A, in each occurrence, is the same or different and represents โArSO3M or the like; M, in each occurrence, is the same or different and represents hydrogen, โNR4, or a metal salt; and R represents hydrType: ApplicationFiled: September 13, 2017Publication date: August 27, 2020Applicant: DAIKIN INDUSTRIES, LTD.Inventors: Masahiro HIGASHI, Moe HOSOKAWA, Akiyoshi YAMAUCHI, Sumi ISHIHARA, Yosuke KISHIKAWA
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Publication number: 20200270204Abstract: An exemplary embodiment of the present invention provides a urea water manufacturing device which can reduce the time for producing urea water by forming a vibrating atmosphere using an ultrasonic wave generator when stirring urea and pure water supplied inside a stirring tank, and can produce urea water with high purity by real-time feedback control of specific gravity of urea water, and a method thereof. The urea water manufacturing device according to an exemplary embodiment of the present invention includes a pure water supply unit, a urea supply unit, a stirring unit, a specific gravity detection unit, a control unit, and a urea water discharge unit.Type: ApplicationFiled: February 7, 2020Publication date: August 27, 2020Inventors: Woo-Sik JEONG, Hyun BONG, Sung Wook Lee
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Publication number: 20200270205Abstract: Disclosed herein are novel cannabionid receptor-2 (CB2) agonists and inverse agonists represented by Formula (I), and method of modulating the activity of CB2 by contacting the CB-2 receptor with a compound of Formula (I). Also, disclosed are methods for treating multiple myeloma or osteoporosis in a mammal in need thereof by modulating the activity of a cannabinoid receptor-2 (CB2).Type: ApplicationFiled: May 11, 2020Publication date: August 27, 2020Applicant: UNIVERSITY OF PITTSBURGH - OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATIONInventors: Xiang-Qun XIE, Abdulrahman Almehizia, Peng Yang
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Publication number: 20200270206Abstract: The invention relates to a novel process for preparing a-carboxamide pyrrolidine derivatives, in particular (2S, 5R)-5-(4-((2-fluorobenzyl)oxy)phenyl)pyrrolidine-2-carboxamide, and to novel intermediates for use in said process along with processes for preparing said intermediates.Type: ApplicationFiled: October 5, 2018Publication date: August 27, 2020Inventors: Weirong Chen, Vinny Couming, Erwin Irdam, William F. Kiesman, Daw-long A. Kwok, Tamera L. Mack, Suzanne M. Opalka, Daniel B. Patience, Donald G. Walker, Wenli Liang
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Publication number: 20200270207Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.Type: ApplicationFiled: March 2, 2020Publication date: August 27, 2020Inventors: Robert D. Ladner, Mark Spyvee, Pravin S. Shirude
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Publication number: 20200270208Abstract: A method for producing dihydroxyindoles includes: a step 1 of obtaining an aqueous first solution including dihydroxyindoles obtained by causing at least a material selected from the group consisting of 3-(3,4-dihydroxyphenyl)alanine and a derivative of 3-(3,4-dihydroxyphenyl)alanine to react with an oxidizing agent; and a step 2 of obtaining an oleaginous second solution in which the dihydroxyindoles are extracted in an extraction solvent by mixing the first solution obtained in the step 1 with the extraction solvent. Before the first solution obtained in the step 1 is mixed with the extraction solvent in the step 2, a water-insoluble by-product is removed from the first solution.Type: ApplicationFiled: October 31, 2018Publication date: August 27, 2020Applicant: Kao CorporationInventors: Masayoshi NAKAMOTO, Norihiro ITO
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Publication number: 20200270209Abstract: The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using the compounds and also relates to use of the compounds as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.Type: ApplicationFiled: May 13, 2020Publication date: August 27, 2020Applicants: Janssen Pharmaceuticals, Inc., Katholieke Universiteit LeuvenInventors: Bart Rudolf Romanie KESTELEYN, Jean-Franรงois BONFANTI, Tim Hugo Maria JONCKERS, Pierre Jean-Marie Bernard RABOISSON, Dorothรฉe Alice Marie-Eve BARDIOT, Arnaud Didier M MARCHAND
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Publication number: 20200270210Abstract: This invention relates to non-steroidal compounds that are modulators of androgen receptor, and also to the methods for the making and use of such compounds.Type: ApplicationFiled: May 12, 2020Publication date: August 27, 2020Inventors: Philip Stewart TURNBULL, Rodolfo Cadilla
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Publication number: 20200270211Abstract: Herein, compounds, compositions and methods for modulating inclusion formation and stress granules in cells related to the onset of neurodegenerative diseases, musculoskeletal diseases, cancer, ophthalmological diseases, and viral infections are described.Type: ApplicationFiled: December 22, 2017Publication date: August 27, 2020Inventors: Duane A. Burnett, Joseph P. Vacca
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Publication number: 20200270212Abstract: Provided are an electron donor that is easy to handle and can be used to carry out a coupling reaction economically and efficiently through simple operations under mild conditions in a short period of time, and a method for synthesizing 4,4?-bipyridine using the electron donor. The electron donor includes a mixture of a dispersion product obtained by dispersing sodium in a dispersion solvent and 1,3-dimethyl-2-imidazolidinone, and this electron donor is used in the method for synthesizing 4,4?-bipyridine.Type: ApplicationFiled: September 27, 2018Publication date: August 27, 2020Inventors: Yoshiaki MURAKAMI, Miyuki FUKUSHIMA, Kazuhiko TAKAI, Sobi ASAKO
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Publication number: 20200270213Abstract: The present invention relates to a compound formed by entinostat as shown in formula (I) and acidic counterion. Compared with the known solid form of entinostat, the compound involved has advantages in terms of solubility, stability, etc. The present invention also relates to a crystalline form of the compound and a preparation method therefor, a pharmaceutical composition thereof and the use thereof in the preparation of a drug for preventing and/or treating a disease associated with differentiation or proliferation.Type: ApplicationFiled: July 28, 2017Publication date: August 27, 2020Inventors: Xiaohong SHENG, Xiaoxia SHENG
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Publication number: 20200270214Abstract: This disclosure relates to compounds and methods of treating or preventing a Nox related disease or condition comprising administering to a subject in need thereof a Nox inhibitor or pharmaceutical compositions comprising a Nox inhibitor disclosed herein, derivatives, or compounds disclosed herein optionally substituted with one or more substitutes including optional salt and prodrug forms. In certain embodiments, this disclosure relates to sulfonylurea compounds and uses reported herein.Type: ApplicationFiled: July 26, 2019Publication date: August 27, 2020Inventors: Osman Gรผner, Bernard Lassegue, Kathy Griendling, Qian Xu, David Brown, J. Phillip Bowen, Amol Kulkarni, E. Blake Watkins
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Publication number: 20200270215Abstract: Provided herein are isotopologues of Compound A, which are enriched with isotopes such as, for example, deuterium. Pharmaceutical compositions comprising the isotope-enriched compounds, and methods of using such compounds are also provided.Type: ApplicationFiled: May 11, 2020Publication date: August 27, 2020Inventors: Hon-Wah MAN, Mohit Atul KOTHARE
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Publication number: 20200270216Abstract: Provided herein are compounds of Formula (I) and (II) and their salts, and compositions comprising such compounds that are useful for useful for modulating neutral sphingomyelinase 2 (n-SMase2) in cells. Also disclosed herein are methods of using the disclosed compounds and compositions for inhibiting the spread of Tau seeds from donor cells to recipient cells. Moreover, disclosed herein are methods of using the disclosed compounds and compositions for treating or preventing a neurodegenerative disorder, such as a tauopathy, Alzheimer's disease (AD), Parkinson's disease (PD), Huntington's disease (HD), Lewy body dementia, frontotemporal dementia, and amyotrophic lateral sclerosis (ALS).Type: ApplicationFiled: September 14, 2018Publication date: August 27, 2020Inventors: Tina Bilousova, Barbara Jagodzinska, Varghese John
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Publication number: 20200270217Abstract: The present embodiment provides a compound represented by the formula (1): Q-CHR2??(1) (Q is a nitrogen-containing aliphatic group containing two or more tertiary nitrogens but no oxygen, and R is an aliphatic group containing a biodegradable group). From the compound in combination with other lipids such as a lipid capable of reducing aggregation, lipid particles can be formed. Further, the compound can be used for a pharmaceutical composition to deliver an activator into cells.Type: ApplicationFiled: March 9, 2020Publication date: August 27, 2020Applicant: KABUSHIKI KAISHA TOSHIBAInventors: Mitsuko ISHIHARA, Eiichi Akahoshi, Katsuyuki Naito, Emi Nozaki, Saeko Saruwatari
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Publication number: 20200270218Abstract: This application relates to a method of detecting negatively charged phosphate-containing membranes and membrane components, such as in cell membranes or artificial lipid vesicles, and its use, for example, in detecting apoptosis and bacterial infection.Type: ApplicationFiled: October 1, 2018Publication date: August 27, 2020Inventors: Patrick Thomas Gunning, Dzlyana Kraskouskaya, Aaron Cabral, Bronte Murcar-Evans, Krlmo Toutah, Elvln De Araujo
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Publication number: 20200270219Abstract: The present invention provides crystalline forms of compound of formula (Ia) and processes of making the crystalline forms. Also provided are compositions comprising the crystalline forms and methods of use of the crystalline forms.Type: ApplicationFiled: March 20, 2020Publication date: August 27, 2020Applicant: BOEHRINGER INGELHEIM ANIMAL HEALTH USA INC.Inventors: Roelof Johannes Gorter de Vries, Bruno Baillon, Sylvaine Lafont, Myriam Gay de Saint Michel, Stephane Kozlovic
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Publication number: 20200270220Abstract: An object of the present invention is to provide a novel ascochlorin derivative which activates adenosine monophosphate-activated protein kinase (AMPK), and is useful in the treatment or prevention of diseases or conditions that involve AMPK dysregulation. The present invention provides a compound presented by formula I, a pharmaceutically acceptable salt or a solvate thereof.Type: ApplicationFiled: January 4, 2017Publication date: August 27, 2020Inventors: Nobuo SHIMMA, Tatsuo HOSHINO
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Publication number: 20200270221Abstract: Disclosed herein are compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), methods of synthesizing compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It), and methods of using compounds of Formulae (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih), (Ik), (Im), (In), (Io), (Ip), (Iq), (Ir), (Is) and (It) as an analgesic.Type: ApplicationFiled: May 11, 2018Publication date: August 27, 2020Inventors: Chad Daniel Hopkins, Joseph Robert Pinchman, Kevin Duane Bunker, Deborah Helen Slee, Brant Clayton Boren, Mehmet Kahraman
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Publication number: 20200270222Abstract: The present disclosure provides a compound of general Formula (I) having c-abl kinase inhibitory activity or pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the compound, and a method useful to treat or prevent neurodegenerative diseases using the compound.Type: ApplicationFiled: May 14, 2020Publication date: August 27, 2020Inventors: Jinhwa LEE, Suyeon JO, A Yeong PARK, Gwibin LEE, Jae Eun KIM, Misoon KIM, Gyooseung JUNG, Seung Mook LIM, Keonseung LIM, Minwoo LEE, Heekyoung YANG, Hyonam KIM, Hyeongjun KIM, Wanjun LI, Mingzhu FAN
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Publication number: 20200270223Abstract: This disclosure provides compounds and compositions which may be modulators of MAGL and/or ABHD6 and their use as medicinal agents, processes for their preparation, and pharmaceutical compositions that include disclosed compounds as at least one active agent. The disclosure also provides for method of treating a patient in need thereof, where the patient is suffering from indications such as pain, solid tumor cancer and/or obesity comprising administering a disclosed compound or composition.Type: ApplicationFiled: December 17, 2019Publication date: August 27, 2020Inventors: Justin S. CISAR, Cheryl A. GRICE, Todd K. JONES, Micah J. NIPHAKIS, Jae Won CHANG, Kenneth M. LUM, Benjamin F. CRAVATT
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Publication number: 20200270224Abstract: The present invention provides novel compounds with increased plasma stability that modulate PAR1 signaling, and methods of using them. The present invention provides methods of using the novel PAR1 modulators for the treatment of a number of disorders, including, inflammation, thrombosis, kidney disease, sepsis, stroke, as well as proliferation-related diseases. Furthermore, the PAR1 modulators of the present invention provide cytoprotection for certain cells and tissues, for example, in coronary blood vessels and tissues after a heart attack.Type: ApplicationFiled: March 23, 2020Publication date: August 27, 2020Inventors: Christopher Dockendorff, Disha M. Gandhi, Ricardo Rosas, JR.
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Publication number: 20200270225Abstract: The present invention provides diacylhydrazine ligands and chiral diacylhydrazine ligands for use with ecdysone receptor-based inducible gene expression systems. Thus, the present invention is useful for applications such as gene therapy, large scale production of proteins and antibodies, cell-based screening assays, functional genomics, proteomics, metabolomics, and regulation of traits in transgenic organisms, where control of gene expression levels is desirable. An advantage of the present invention is that it provides a means to regulate gene expression and to tailor expression levels to suit the user's requirements.Type: ApplicationFiled: April 16, 2020Publication date: August 27, 2020Applicant: Intrexon CorporationInventors: Robert Eugene Hormann, Bing Li
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Publication number: 20200270226Abstract: The present disclosure relates to novel crystalline forms of ARN-509 (structure shown in formula I), processes for preparation of the novel crystalline forms, pharmaceutical composition of the novel crystalline forms, and uses of the novel crystalline forms for preparing drug products of androgen receptor antagonists and for treating prostate cancer. The crystalline forms of ARN-509 provided by the present disclosure have one or more improved properties compared with the prior art, and is of great value to the future optimization and development of drugs.Type: ApplicationFiled: May 16, 2019Publication date: August 27, 2020Inventors: Minhua Chen, Yanfeng Zhang, Xiaoting Zhai, Jiale Qian, Yuhao Chen, Chaohui Yang
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Publication number: 20200270227Abstract: The present invention relates to compounds of formula (I): wherein Q is O or S, R1 is a 6-membered heteroaryl group containing at least one nitrogen atom in the 6-membered ring structure, wherein R1 may optionally be substituted, and R2 is a cyclic group substituted at the ?-position, wherein R2 may optionally be further substituted. The present invention further relates to salts, solvates and prodrugs of such compounds, to pharmaceutical compositions comprising such compounds, and to the use of such compounds in the treatment and prevention of medical disorders and diseases, most especially by the inhibition of NLRP3.Type: ApplicationFiled: July 4, 2018Publication date: August 27, 2020Inventors: Matthew COOPER, David MILLER, Angus MACLEOD, Jimmy VAN WILTENBURG, Stephen THOM, Stephen ST-GALLAY, Jonathan SHANNON
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Publication number: 20200270228Abstract: A process for manufacturing 2-isobutyl-6-(3-(methylamino)azetidin-l-yl)pyrimidin-4-amine of Formula (I): including starting from 6-chloro-2-isobutylpyrimidin-4-amine and tert-butyl azetidin-3-yl(methyl)carbamate, or another N-protected N-methylazetidin-3-amine, and performing the following steps: (a) coupling reaction of both compounds in dimethylsulfoxide in presence of potassium carbonate to afford an intermediate protected compound; and (b) deprotection of the protected compound to afford 2-isobutyl-6-(3-(methylamino)azetidin-1-yl)pyrimidin-4-amine. Also, a process for manufacturing the intermediate protected compound, wherein deprotection step (b) is omitted, and the compounds obtained from the processes.Type: ApplicationFiled: October 17, 2018Publication date: August 27, 2020Applicant: SENSORIONInventors: Daan COPMANS, Amandine MOHR, Maurice Hubert BONTEN, Dawn TORONTO
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Publication number: 20200270229Abstract: The present invention relates to a pharmaceutical composition for preventing or treating acute myeloid leukemia or metastatic breast cancer, comprising, as an active ingredient, an indirubin derivative. When the compound of the present invention is used, it can effectively inhibit the activity of FLT3 kinase and can be usefully used to prevent or treat acute myeloid leukemia or metastatic breast cancer.Type: ApplicationFiled: April 30, 2020Publication date: August 27, 2020Applicant: PELEMED CO., LTD.Inventors: Yong Chul Kim, Pyeong-Hwa Jeong
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Publication number: 20200270230Abstract: Disclosed are a class of ?-opioid receptor agonists and a preparation method therefor and the use thereof in the field of medicine, belonging to the field of medicinal chemistry. The ?-opioid receptor agonists significantly increase the selectivity for a G protein signaling pathway, and not only can exhibit excellent pharmacodynamic effects, but also significantly improve safety.Type: ApplicationFiled: September 17, 2018Publication date: August 27, 2020Inventors: Xin Xu, Zhen Zhang, Yunfei Li, Liming Zhang, Fengying Guo, Qingyun Jiang, Dongsheng Li, Linli Zhang, Jinqian Song, Lei Liu, Qiang Liu, Jing Su, Yijin Wang, Jian Ge
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Publication number: 20200270231Abstract: A method of inhibiting TNIK and/or MAP4K4 kinase can include: contacting the kinase with a compound of Formula A, wherein: ring 1 is an aromatic ring with or without hetero atoms; ring 2 is a hetero aromatic ring; ring 3 includes at least one hetero aromatic ring and optionally at least one cycloaliphatic ring fused with the at least one hetero aromatic ring; ring 4 is an aromatic ring with or without hetero atoms; Y is a bond or a linker; Y1 is a linker; each n is independently 0, 1, or 2; each o is independently 0, 1, 2, 3, 4, or 5; each R1, R6, R11, and R12 is independently a substituent; and RA is a ring structure, straight aliphatics, or branched aliphatics, which can be substituted or unsubstituted, any with or without hetero atoms.Type: ApplicationFiled: February 20, 2020Publication date: August 27, 2020Inventors: Aleksandr Aliper, Vladimir Aladinskiy, Aleksandrs Zavoronkovs