Patents Issued in June 25, 2020
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Publication number: 20200199062Abstract: A method for separating one or more amino acids from a whole stillage byproduct produced in a corn dry milling process for making alcohol and system therefore is disclosed. In one embodiment, the method includes separating the whole stillage byproduct into an insoluble solids portion and a thin stillage portion, which include protein and amino acids. Thereafter, the thin stillage portion can be separated into a water soluble solids portion and a protein and amino acids portion. The resulting protein and amino acids portion can be separated into an amino acid(s) portion and a protein portion, both of which may be optionally dried, utilizing microfiltration, ultrafiltration, electrophoresis techniques/devices, or combinations thereof.Type: ApplicationFiled: May 8, 2018Publication date: June 25, 2020Inventors: Michael Franko, Neal Jakel, John Kwik
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Publication number: 20200199063Abstract: The present invention relates to TRPV1 modulator compounds of formula (I) or their pharmaceutically, veterinary or cosmetically acceptable salts, or their stereoisomers or mixtures thereof, wherein m is an integer selected from 1 to 3; R1, R2, R6 and R6? are independently selected from H, (C1-C8)alkyl, unsaturated (C2-C8)hydrocarbon, and (C3-C6)cycloalkyl, being these groups optionally substituted; R3 is hydrogen or halogen; R4 is selected from H, (C1-C8)alkyl, unsaturated (C2-C8)hydrocarbon, (C3-C6)cycloalkyl, (C6-C12)aryl, and (C5-C12)heteroaryl, being these groups optionally substituted; and R5 is selected from (C3-C28)alkyl, unsaturated (C3-C28)hydrocarbon, (C6-C12)aryl, and (C5-C12)heteroaryl, being these groups optionally substituted. It also relates to a process for their preparation, to pharmaceutical, veterinary or cosmetic compositions containing them, and to their pharmaceutical, veterinary and cosmetic applications.Type: ApplicationFiled: May 10, 2018Publication date: June 25, 2020Applicant: ANTALGENICS, S.L.Inventors: Isabel DEVESA GINER, Armando Genazzani, Tracey Pirali, Asia Fernandez Carvajal, Antonio Vicente Ferrer Montiel
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Publication number: 20200199064Abstract: Here described is a composition comprising a compound of formula I: wherein R1 and R2 is independently selected from a group consisting of C10 to C18 alkyl, C12 to C18 alkenyl, and oleoyl group; R3 and R4 are independently selected from a group consisting of C1 to C6 alkyl, and C2 to C6 alkanol; X is selected from a group consisting of —CH2—, —S—, and —O— or absent; Y is selected from —(CH2)n, —S(CH2)n, —O(CH2)n—, thiophene, —SO2(CH2)n—, and ester; n=1-4; a=1-4; b=1-4; c=1-4; and Z? is a counterion.Type: ApplicationFiled: December 2, 2019Publication date: June 25, 2020Inventors: Yoshiro Niitsu, Victor Knopov, Joseph E. Payne, Zheng Hou, John A. Gaudette, Violetta Akopian, Richard P. Witte, Mohammad Ahmadian, Loren A. Perelman, Yasunobu Tanaka, Priya Karmali, Sridhar C. Nagarajan
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Publication number: 20200199065Abstract: The present invention relates to novel functional derivatives of alanine and proline amino acids. The compounds of the present invention were confirmed to have a very superior antifungal or fungicidal effect. In addition, the compounds of the present invention were confirmed to exhibit a synergistic effect when co-administered with an existing antifungal preparation. Moreover, the compounds of the present invention showed activity on a wide range of fungi. Therefore, the compounds of the present invention can be widely used in a field which requires the treatment with an antifungal or fungicidal preparation against human infectious fungi, animal infectious fungi, and phytopathogenic fungi.Type: ApplicationFiled: October 30, 2017Publication date: June 25, 2020Inventors: Ki Duk Park, Yong-Sun Bahn, Jong-Seung Lee, Kyung-Tae Lee, Ae Nim Pae, Seul Ki Yeon, Yong Koo Kang, Jong Hyun Park, Siwon Kim, Bo Ko Jang, Ji Won Choi
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Publication number: 20200199066Abstract: Provided are aromatic oligoamide foldamers and self-assembled compositions of the same. The aromatic oligoamide foldamers and compositions can form tube-like structures that can form pores in membranes. The pores can be used to transport ions and molecules, such as, for example, cryoprotective agents or therapeutic agents, through the membrane. The tube-like structures exhibit desirable stability at low temperatures.Type: ApplicationFiled: February 26, 2020Publication date: June 25, 2020Inventor: Bing GONG
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Publication number: 20200199067Abstract: A hydrogen sulfide donor in an organic salt form and a preparation method thereof. The hydrogen sulfide donor exists as a salt formed by organic compounds with an alkaline motif and hydrogen sulfide with weak acidity. The hydrogen sulfide donor features with a simple structure, and an easy preparation method. Moreover, hydrogen sulfide donors in different forms can be prepared according to research and development needs. After the hydrogen sulfide donor enters an organism, the process of in vivo dissociation and hydrogen sulfide supply is simple, rapid, and effective, and there is no requirement for enzyme or any other complicated condition, and thus, the hydrogen sulfide donor has a great application prospect and value.Type: ApplicationFiled: March 15, 2018Publication date: June 25, 2020Inventors: Hu ZHENG, Lingling WENG
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Publication number: 20200199068Abstract: A continuous flow production process for preparing organic peroxides directly from alcohols or alkanes takes very safe alcohols or alkanes as starting materials, and directly reacts to obtain designated peroxides. The production process is carried out in an integrated continuous flow reactor, and a safe starting source of alcohol or alkane is continuously added at the feed inlet of the integrated continuous flow reactor, and continuously provided with a designated peroxide at the discharge port of the integrated continuous flow reactor.Type: ApplicationFiled: February 11, 2020Publication date: June 25, 2020Inventors: Bing MA, Shuai PAN, Xinlin SHU
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Publication number: 20200199069Abstract: The present invention relates to a solid phase pharmaceutical composition comprising one or more pharmaceutically acceptable excipients and an active pharmaceutical ingredient (“API”) which is a compound of formula A1 or A2 or a pharmacologically acceptable salt, solvate or hydrate thereof, wherein the API is not exposed to a basic compound.Type: ApplicationFiled: February 28, 2020Publication date: June 25, 2020Inventors: Philippe Michel Rene Bouillot, Emeric Reynaud
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Publication number: 20200199070Abstract: The invention relates to crystalline eravacycline bis-hydrochloride and to a process for its preparation. Furthermore, the invention relates to the use of crystalline eravacycline bis-hydrochloride for the preparation of pharmaceutical compositions. The invention further relates to pharmaceutical compositions comprising an effective amount of crystalline eravacycline bis-hydrochloride. The pharmaceutical compositions of the present invention can be used as medicaments, in particular for treatment and/or prevention of bacterial infections e.g. caused by Gram negative pathogens or Gram positive pathogens, in particular caused by multidrug resistant Gram negative pathogens. The pharmaceutical compositions of the present invention can thus be used as medicaments for e.g.Type: ApplicationFiled: January 20, 2017Publication date: June 25, 2020Applicant: Sandoz AGInventor: Hannes Lengauer
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Publication number: 20200199071Abstract: The present disclosure relates to sulfoxide-based reagents suitable in the mass spectrometric determination of analyte molecules such as peptides as well as adducts of such reagents and analyte molecules and applications of the reagents and adducts. Further, the present disclosure relates to methods for the mass spectrometric determination of analyte molecules.Type: ApplicationFiled: March 6, 2020Publication date: June 25, 2020Applicant: Roche Diagnostics Operations, Inc.Inventor: Thomas Carell
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Publication number: 20200199072Abstract: It is described an industrially viable and advantageous process for the preparation of (S)-beta-aminosulfone (1) starting from the corresponding racemic compound, said (S)-beta-aminosulfone being a useful intermediate for the preparation of N-(2-((1S)-1-(3-ethoxy-4-methoxyphenyl)-2-(methylsulfonyl)ethyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl)acetamide, also known as Apremilast, the latter being suitable for use in methods of treating, preventing and/or managing psoriasis or psoriatic arthritis.Type: ApplicationFiled: March 28, 2018Publication date: June 25, 2020Applicant: Quimica Sintetica, S.A.Inventors: Giuseppe Barreca, Giovanni Marras, Bruno Romanò
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Publication number: 20200199073Abstract: Provided herein are piperidine dione compounds having the following structure: wherein RN, R1, R2, R3, R4, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.Type: ApplicationFiled: December 18, 2019Publication date: June 25, 2020Inventors: Massimo Ammirante, Sogole Bahmanyar, Matthew D. Correa, Virginia Grant, Joshua Hansen, Evan J. Horn, Timothy S. Kercher, Christopher Mayne, Mark A. Nagy, Rama Krishna Narla, Surendra Nayak, Stephen Norris, Patrick Papa, Veronique Plantevin-Krenitsky, John J. Sapienza, Brandon W. Whitefield, Shuichan Xu
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Publication number: 20200199074Abstract: Provided herein are piperidine dione compounds having the following structure: wherein RN, R1, R2, R3, R4, X, L, V, m, and n are as defined herein, compositions comprising an effective amount of a piperidine dione compound, and methods for treating or preventing an androgen receptor mediated disease.Type: ApplicationFiled: December 18, 2019Publication date: June 25, 2020Inventors: Massimo Ammirante, Sogole Bahmanyar, Matthew D. Correa, Virginia Grant, Joshua Hansen, Evan J. Horn, Timothy S. Kercher, Christopher Mayne, Mark A. Nagy, Rama Krishna Narla, Surendra Nayak, Stephen Norris, Patrick Papa, Veronique Plantevin-Krenitsky, John J. Sapienza, Brandon W. Whitefield, Shuichan Xu
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Publication number: 20200199075Abstract: The present invention provides for the treatment, prevention, and/or reduction of a risk of a disease, disorder, or condition in which aldehyde toxicity is implicated in the pathogenesis, including ocular disorders, skin disorders, conditions associated with injurious effects from blister agents, and autoimmune, inflammatory, neurological and cardiovascular diseases by the use of a primary amine to scavenge toxic aldehydes, such as MDA and HNE.Type: ApplicationFiled: December 19, 2019Publication date: June 25, 2020Inventors: Todd Brady, Scott Young, William A. Kinney, Susan Macdonald
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Publication number: 20200199076Abstract: The invention provides compounds of formula (I): and salts thereof wherein R1-R5 have any of the meanings described in the specification. The compounds are useful for treating bacterial infections (e.g. tuberculosis).Type: ApplicationFiled: August 29, 2018Publication date: June 25, 2020Applicant: RUTGERS, THE STATE UNIVERSITY OF NEW JERSEYInventors: Joel S. FREUNDLICH, David ALLAND, Matthew B. NEIDITCH, Pradeep KUMAR, Glenn CAPODAGLI, Divya AWASTHI, Sean EKINS
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Publication number: 20200199077Abstract: A process is provided for manufacturing a cyclic urea adduct of an ethyleneamine compound, the ethyleneamine compound having a linear —NH—CH2—CH2—NH— group. The process includes, in an absorption step, contacting a liquid medium comprising an ethyleneamine compound having a linear —NH—CH2—CH2—NH— group with a CO2-containing gas stream at a pressure of from about 1 to about 20 bara, resulting in the formation of a liquid medium into which CO2 has been absorbed. The process further includes bringing the liquid medium to cyclic urea formation conditions, and, in an urea formation step, forming cyclic urea adduct of the ethyleneamine compound, urea formation conditions including a temperature of at least about 120° C., wherein the total pressure at the end of the urea formation step is at most about 20 bara, and wherein the temperature in the absorption step is lower than the temperature in the urea formation step.Type: ApplicationFiled: August 7, 2018Publication date: June 25, 2020Applicant: NOURYON CHEMICALS INTERNATIONAL B.V.Inventors: Rens VENEMAN, Antoon Jacob Berend TEN KATE, Karl Fredrik LAKE, Jenny Valborg Therese ADRIAN MEREDITH, Michiel Jozef Thomas RAAIJMAKERS, Slavisa JOVIC, Rolf Krister EDVINSSON, Hendrik VAN DAM, Eike Nicolas KANTZER, Ina EHLERS
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Publication number: 20200199078Abstract: The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating and/or preventing proliferative diseases (e.g., cancer). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.Type: ApplicationFiled: November 30, 2016Publication date: June 25, 2020Applicants: Children's Medical Center Corporation, Beth Israel Deaconess Medical Center, Inc.Inventors: Bruce R. Zetter, Lijun Sun
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Publication number: 20200199079Abstract: The present disclosure provides pharmaceutical agents of the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents for the treatment of a variety of diseases and disorders are also provided.Type: ApplicationFiled: March 2, 2020Publication date: June 25, 2020Inventors: Peter G. Ruminski, David W. Griggs
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Publication number: 20200199080Abstract: The invention describes the pyrimidine-based compounds of the general formula I. Described compounds lower the production of the prostaglandin E2. In concentrations lowering production of this factor by 50%, these compounds have no negative effect on the cell viability and they are not cytotoxic. Furthermore, the method of production of the compounds of the general formula I is provided. A pharmaceutical composition comprising the polysubstituted pyrimidines according to the invention and the use of these compounds for the treatment of the inflammatory diseases are also provided.Type: ApplicationFiled: May 23, 2018Publication date: June 25, 2020Applicants: USTAV ORGANICKE CHEMIE A BIOCHEMIE AV CR, V.V.I., USTAV EXPERIMENTALNI MEDICINY AV CR, V.V.I.Inventors: VIKTOR KOLMAN, Filip KALCIC, Zlatko JANEBA, Zdenek ZIDEK
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Publication number: 20200199081Abstract: Provided herein are compositions and methods for the treatment and prevention of cancer, including melanoma.Type: ApplicationFiled: December 20, 2019Publication date: June 25, 2020Applicants: TRUSTEES OF BOSTON UNIVERSITY, XIAMEN UNIVERSITYInventors: Rutao CUI, Chengqian YIN, Xianming DENG, Ting ZHANG
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Publication number: 20200199082Abstract: A method for the synthesis of N-protected 3,6-aminoalkyl-2,5-diketopiperazines is provided. The method includes obtaining a cyclic ?-N protected active amino ester and adding it to a mixture of an amine catalyst in an organic solvent.Type: ApplicationFiled: March 2, 2020Publication date: June 25, 2020Inventors: John J. Freeman, Otto Phanstiel, William Elliot Bay, Kelly Sullivan Kraft
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Publication number: 20200199083Abstract: The present invention covers 4-oxo-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-7-carboxamide compounds of general formula (I): in which R1, R2a, R2b, R2c, R3a, R3b, R4a, R4b, R5 and X are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of cancer, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: August 9, 2018Publication date: June 25, 2020Applicants: Bayer Aktiengesellschaft, Bayer Pharma AktiengesellschaftInventors: Jörg WEISKE, Carlo STRESEMANN, Stefan Nikolaus GRADL, Ulrike RÖHN, Clara CHRIST, Holger STEUBER, Manfred HUSEMANN, Norbert SCHMEES, Kai THEDE, Stephan SIEGEL, Antonius TER LAAK
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Publication number: 20200199084Abstract: A reactive UV absorber suitable for polyurethane is provided. The reactive UV absorber is a compound of formula 1: wherein R1 is H or Cl.Type: ApplicationFiled: July 7, 2017Publication date: June 25, 2020Inventors: Chingfan Chris CHIU, Huang-min WU, Wei-chun CHANG, Chi-feng WU, Ching-hao CHENG, Shao-hsuan WU
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Publication number: 20200199085Abstract: The present application relates to functionalized 1,2,4,5-tetrazine compounds. The compounds are useful in compositions and methods using bioorthogonal inverse electron demand Diels-Alder cycloaddition reactions for the rapid and specific covalent delivery of a “payload” to a ligand bound to a biological target.Type: ApplicationFiled: March 2, 2020Publication date: June 25, 2020Inventors: Scott A. Hilderbrand, Neal K. Devaraj, Ralph Weissleder, Mark R. Karver
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Publication number: 20200199086Abstract: The present invention relates to methods of modulating an immune response mediated by a PD-1 signaling pathway and of treating a cancer or an infectious disease. A subject is administered a compound(s) or a pharmaceutically acceptable salt or pharmaceutically acceptable composition thereof of formula (I) In the ring Q is S or O. R1 substituents are an optionally substituted side chain of the amino acid Ser or Thr and R3 substituents are a side chain of the amino acids Asn, Asp, Gln, or Glu. R2 is hydrogen or —CO-Aaa and Aaa is Thr or Ser with a free, amidated or esterified C-terminus. R4 and R5 are independently hydrogen or absent. R6 is hydrogen, alkyl or acyl.Type: ApplicationFiled: March 2, 2020Publication date: June 25, 2020Applicant: Aurigene Discovery Technologies LimitedInventors: Pottayil Govindan Nair Sasikumar, Muralidhara Ramachandra, Seetharamaiah Setty Sudarshan Naremaddepalli
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Publication number: 20200199087Abstract: The present invention relates to the unexpected discovery of novel multi-aromatic, multi-substituted compounds. In certain embodiments, the compounds of the invention are generated by condensing at least two phenolic- and/or aniline-containing monomers and an aromatic, aliphatic or heteroaromatic aldehyde- and/or ketone-containing monomer. In other embodiments, at least one monomer is isolated from a bio-based resource. In yet other embodiments, the compounds of the invention are bis- or poly-phenolic compounds.Type: ApplicationFiled: May 15, 2018Publication date: June 25, 2020Inventors: Alexander W. Bassett, Joseph F. Stanzione, III, John J. La Scala, Joshua M. Sadler, Owen M. Stecca
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Publication number: 20200199088Abstract: The present disclosure includes compositions and methods for improved DNA amplification reactions. In particular, the present disclosure provides compositions and methods for hot-start PCR applications using DNA polymerase inhibitors that minimize non-specific DNA amplification by inactivating DNA polymerase at lower temperatures.Type: ApplicationFiled: December 12, 2019Publication date: June 25, 2020Inventors: Wenhui Zhou, Kimberly K. Knoche, Douglas R. Storts, Min Zhou, Poncho Meisenheimer
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Publication number: 20200199089Abstract: Disclosed are a tetrahydronaphtho[1,2-b]furan-2(3H)-one derivative of formula (I) and a method of making the same, where definitions of R, R1 and R2 herein are the same as those in the specification. It has been demonstrated by animal experiments that the tetrahydronaphtho[1,2-b]furan-2(3H)-one derivative can significantly inhibit the adjuvant-induced in Wistar male rats so that it can alleviate the primary and secondary lesions, showing a preventive activity to some extent. Therefore, the tetrahydronaphtho[1,2-b]furan-2(3H)-one derivative provided herein is applicable to the preparation of a drug for preventing/treating rheumatoid arthritis, and has promising clinical applications.Type: ApplicationFiled: March 13, 2020Publication date: June 25, 2020Inventors: Qingyan SUN, Weidong ZHANG
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Publication number: 20200199090Abstract: An organic compound having a tetraphenyl moiety and at least one fused hetero aryl moiety having at least one oxygen and/or sulfur on a ring and bonded to the tetraphenyl moiety directly or indirectly, and a light emitting diode and a light emitting device having the organic compound are disclosed. The organic compound has excellent thermal resistance property and hole mobility property. The organic compound can be incorporated into a hole transfer layer, an electron blocking layer and/or a charge generation layer of the light emitting diode. Therefore, the light emitting diode and light emitting device according to the present invention have decreased driving voltage and enhanced luminous efficiency.Type: ApplicationFiled: December 18, 2019Publication date: June 25, 2020Applicant: LG Display Co., Ltd.Inventors: So-Young JANG, Hee-Jun PARK, Jeong-Dae SEO, Seon-Keun YOO, Ji-Cheol SHIN, Sang-Beom KIM
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Publication number: 20200199091Abstract: A solvent-free method to extract THCA from cannabis, said method comprising: providing a source of THCA-containing cannabis plant; providing a source of natural oil; combining said source of THCA-containing cannabis and said source of natural oil into a blend; milling said blend; optionally, heating the blend during the milling; and extracting a THCA-containing liquid generated during the milling.Type: ApplicationFiled: May 15, 2018Publication date: June 25, 2020Inventor: Jay Carnahan
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Publication number: 20200199092Abstract: High aldehyde dehydrogenase 1A1 (ALDH1A1) activity has emerged as a reliable marker for the identification of both normal and cancer stem cells. Herein, is presented AlDeSense, a turn-on green fluorescent probe for aldehyde dehydrogenase 1A1 (ALDH1A1) and Ctrl-AlDeSense, a matching non-responsive reagent. AlDeSense exhibits a 20-fold fluorescent enhancement when treated with ALDH1A1. Through the application of surface marker antibody staining, tumorsphere assays, and assessment of tumorigenicity, the disclosed results show that cells exhibiting high AlDeSense signal intensity have properties of cancer stem cells. Herein, is also reported the development of a red congener, red-AlDeSense. Importantly, red-AlDeSense represents one of only a few examples of a turn-on sensor in the red region using the d-PeT quenching mechanism.Type: ApplicationFiled: December 18, 2019Publication date: June 25, 2020Applicant: The Board of Trustees of the University of IllinoisInventors: Thomas Edward BEARROOD, Chelsea Diane ANORMA, Jefferson CHAN
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Publication number: 20200199093Abstract: The composition contains a compound and a solvent. The compound includes a group represented by formula (1). The compound has a molecular weight of no less than 200 and has a percentage content of carbon atoms of no less than 40% by mass. In the formula (1), R1 and R2 each independently represent a hydrogen atom, a fluorine atom, a monovalent hydrocarbon group having 1 to 20 carbon atoms or a monovalent fluorinated hydrocarbon group having 1 to 20 carbon atoms, or R1 and R2 taken together represent a part of an alicyclic structure having 3 to 20 ring atoms constituted together with the carbon atom to which R1 and R2 bond; Ar1 represents a group obtained by removing (n+3) hydrogen atoms from an arene or heteroarene having 6 to 20 ring atoms; and X represents an oxygen atom, —CR3R4—, —CR3R4—O— or —O—CR3R4—.Type: ApplicationFiled: March 5, 2020Publication date: June 25, 2020Applicant: JSR CORPORATIONInventors: Hiroki NAKATSU, Kazunori TAKANASHI, Kazunori SAKAI, Yuushi MATSUMURA, Hiroki NAKAGAWA
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Publication number: 20200199094Abstract: Novel 3-(N-piperidinyl)methyl benzamide derivatives are disclosed. The compounds can be used in treating diseases and conditions which are associated with abnormal cell function related to endoplasmic reticulum (ER) stress. For example, the compounds can be used as suppressors of ER stress-induced pancreatic ?-cell dysfunction and death, for example in the treatment of diabetes.Type: ApplicationFiled: June 15, 2018Publication date: June 25, 2020Inventor: Weidong Wang
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Publication number: 20200199095Abstract: According to the present invention, a cured product obtained by curing a curable composition including a compound represented by General Formula 1, in which a birefringence ?n (587 nm) is 0.00??n (587 nm)?0.01, is provided, and this cured product is suitable for manufacturing an optical member. Pol1-Sp1-L1-Ar-L2-Sp2-Pol2??(General Formula 1) In formula, Ar is an aromatic ring group represented by General Formula 2-2 and the like. In formula, Z1 and Z2 each represent a hydrogen atom, a methyl group, and the like; A1 and A2 each represent —S— and the like; X represents C(Rz)2 and the like (where Rz is a substituent, and two Rz's may form a ring); L1 and L2 each represent a single bond, —O—, —OC(?O)—, —OC(?O)O—, —OC(?O)NH—, and the like; Sp1 and Sp2 each represent a single bond or a divalent linking group; Pol1 and Pol2 each represent a hydrogen atom or a polymerizable group; and a compound represented by General Formula 1 has at least one polymerizable group.Type: ApplicationFiled: February 27, 2020Publication date: June 25, 2020Applicant: FUJIFILM CorporationInventors: Naoyuki MOROOKA, Naozumi SHIRAIWA
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Publication number: 20200199096Abstract: Embodiments provide a harmful organism control agent containing a pyrazole-3-carboxylic acid amide derivative or a salt thereof as an active ingredient, having an excellent harmful organism controlling effect. A pyrazole-3-carboxylic acid amide derivative represented by general formula [I]: (wherein, R1, R2, R3, R4, and R5 represent a hydrogen atom, halogen atom, C1-C6 alkyl group or the like, R6 represents a C1-C12 alkyl group, C1-C12 haloalkyl group or the like, R7 and R8 represent a hydrogen atom, C1-C12 alkyl group or the like) or an agriculturally acceptable salt thereof, and a harmful organism control agent containing the pyrazole-3-carboxylic acid amide derivative or an agriculturally acceptable salt thereof as an active ingredient.Type: ApplicationFiled: May 9, 2018Publication date: June 25, 2020Applicant: KUMIAI CHEMICAL INDUSTRY CO., LTD.Inventors: Akira KINPARA, Ryo ISHIKAWA, Keiji TORIYABE, Katsuya KATO, Masao NAKATANI, Akira TAKANEZAWA, Takeshi MATSUDA
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Publication number: 20200199097Abstract: Disclosed in the present invention are a Pomalidomide derivative and a preparation method therefor. Specifically, the present invention relates to the Pomalidomide derivative and a stereoisomer thereof, or a pharmaceutically acceptable salt, and applications thereof in the preparation of drugs for treating cancers.Type: ApplicationFiled: August 21, 2017Publication date: June 25, 2020Applicant: NANJING NORATECH PHARMACEUTICALS CO., LTDInventors: Fei LIU, Gang WU, Xin ZHAO, Pan CHEN, Yunpeng LIAO, Xiaobo WANG, Zhi QI, Xudong YANG
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Publication number: 20200199098Abstract: The disclosure relates to anti-cancer compounds derived from nuclear steroid receptor binders, to products containing the same, as well as to methods of their use and preparation.Type: ApplicationFiled: November 27, 2019Publication date: June 25, 2020Inventors: Sarvajit Chakravarty, Son Minh Pham, Jiyun Chen, Jayakanth Kankanala, Jeremy D. Pettigrew, Anjan Kumar Nayak, Anup Barde, Brahmam Pujala
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Publication number: 20200199099Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I or their pharmaceutically acceptable salts, and methods of using said compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.Type: ApplicationFiled: July 23, 2019Publication date: June 25, 2020Inventors: Erkan Baloglu, Sharon Shacham, Dilara McCauley, Trinayan Kashyap, William Senapedis, Yosef Landesman, Gali Golan, Ori Kalid, Sharon Shechter
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Publication number: 20200199100Abstract: Disclosed are organic cation transporters (OCTs) inhibitors of Formula (A), as well as their pharmaceutically acceptable tautomers, salts or solvates. Also disclosed are pharmaceutical compositions including such OCTs inhibitor of Formula (A) and their use for treating and/or preventing mood-related disorders such as depressive disorders.Type: ApplicationFiled: July 13, 2018Publication date: June 25, 2020Inventors: Sophie GAUTRON, Nicolas PIETRANCOSTA, Francine ACHER, Laetitia CHAUSSET-BOISSARIE
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Publication number: 20200199101Abstract: Provided are a Syk inhibitor and a use method therefor, and in particular, disclosed are quinolinone represented by formula (I) or quinazoline derivatives or pharmaceutically acceptable salts thereof, a preparation method, a pharmaceutical composition, and uses in preparing a medicament for treatment of Syk receptor related diseases.Type: ApplicationFiled: June 14, 2018Publication date: June 25, 2020Applicant: Chia Tai Tianqing Pharmaceutical Group Co., Ltd.Inventors: Shilan LIU, Guibai LIANG, Hongjian WANG, Ming ZHANG, Shuhui CHEN
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Publication number: 20200199102Abstract: The invention features compounds (e.g., macrocyclic compounds) capable of modulating biological processes, for example through binding to a presenter protein (e.g., a member of the FKBP family, a member of the cyclophilin family, or PIN1) and a target protein (e.g., a eukaryotic target protein such as a mammalian target protein or a fungal target protein or a prokaryotic target protein such as a bacterial target protein). These compounds bind endogenous intracellular presenter proteins, such as the FKBPs or cyclophilins, and the resulting binary complexes selectively bind and modulate the activity of intracellular target proteins. Formation of a tripartite complex among the presenter protein, the compound, and the target protein is driven by both protein-compound and protein-protein interactions, and both are required for modulation of the targeted protein's activity.Type: ApplicationFiled: April 4, 2018Publication date: June 25, 2020Inventors: Mark Joseph MULVIHILL, Meizhong JIN
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Publication number: 20200199103Abstract: This invention is based on the discovery that many lung diseases associated with aging are mediated at least in part by cells bearing a senescent phenotype. Senescent cells accumulate with age, and express factors that contribute to the pathophysiology of age related conditions. The severity of age-related conditions typically correlates with the abundance of senescent cells: thus, clearing senescent cells can help abrogate the condition: providing symptomatic relief, and potentially inhibiting disease progression. In accordance with this invention, a family of Bcl protein inhibitors has been developed for the treatment of lung diseases. These senolytic agents have an appropriate dose and specificity profile to be effective in the clinical management of previously intractable pulmonary diseases.Type: ApplicationFiled: August 13, 2018Publication date: June 25, 2020Inventors: Nick Vlahakis, Scott Armstrong, Jamie Dananberg, Ryan Hudson, Anne-Marie Beausoleil, Nathaniel David, Remi-Martin Laberge
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Publication number: 20200199104Abstract: The present invention relates to novel crystalline polymorphic and amorphous form of 4-(2-(5-chloro-2-fluorophenyl) -5-isopropylpyridin-4-ylamino)-N-(1,3-dihydroxypropan-2-yl) nicotinamide and to methods for their preparation; and the invention is also directed to pharmaceutical compositions containing at least one polymorphic form and to the therapeutic or prophylactic use of such polymorphic forms and compositions.Type: ApplicationFiled: December 17, 2019Publication date: June 25, 2020Applicant: PFIZER INC.Inventors: Anand Venkataramana Sistla, Iain David Roy, Andrew Robbins
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Publication number: 20200199105Abstract: BA-1049 (R) and its active metabolite are disclosed. Also disclosed are pharmaceutical formulations containing BA-1049 (R) or its active metabolite.Type: ApplicationFiled: January 6, 2020Publication date: June 25, 2020Inventors: Kenneth M. ROSEN, Matthew D. ABBINANTI, Joerg RUSCHEL, Lisa MCKERRACHER, Lisa BOND MORITZ
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Publication number: 20200199106Abstract: Provided is a compound for inhibiting and degrading anaplastic lymphoma kinase ALK. Specifically provided is a compound as represented by the following formula I, wherein the definition of each group is as stated in the description. The compound has excellent anaplastic lymphoma kinase (ALK) inhibitory activity, and can be used for preparing drugs for treatment of ALK activity-related diseases.Type: ApplicationFiled: March 3, 2020Publication date: June 25, 2020Inventor: Yongzhi SHU
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Publication number: 20200199107Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.Type: ApplicationFiled: March 5, 2020Publication date: June 25, 2020Inventors: Andrew P. Crew, Keith R. Hornberger, Hanqing Dong, Jing Wang, Yimin Qian, Craig M. Crews
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Publication number: 20200199108Abstract: A compound of Formula (I), pharmaceutically acceptable salts thereof, and individual enantiomers or diastereomers thereof. Compositions and methods useful for treatment or suppression of diseases, developmental delays and symptoms related to oxidative stress.Type: ApplicationFiled: February 26, 2020Publication date: June 25, 2020Inventors: JIA-NING XIANG, ZUDE QI, DEZHENG NING, XIANBO LIU
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Publication number: 20200199109Abstract: The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of inhibiting ROCK1 and/or ROCK2 that are useful for the treatment of disease.Type: ApplicationFiled: June 13, 2018Publication date: June 25, 2020Inventors: Eduardas Skucas, Kevin G. Liu, Ji-In Kim, Masha V. Poyurovsky, Rigen Mo
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Publication number: 20200199110Abstract: A heterocyclic compound represented by Formula 1 and an organic light-emitting device the heterocyclic compound represented by Formula 1: wherein, in Formula 1, Cz1 is a group represented by Formula 1A, Het1 is a group represented by Formula 1B, wherein, R1 to R10, R20, R30, R40, R50, and b10 to b50 are each independently the same as described in the detailed description of the specification.Type: ApplicationFiled: December 17, 2019Publication date: June 25, 2020Inventors: Minsik MIN, Eunsuk Kwon, Kyungdoc Kim, Inkoo KIM, Juhyun KIM, Joonghyuk KIM, Jhunmo SON, Yongsik JUNG
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Publication number: 20200199111Abstract: The present disclosure relates to novel ?-opioid receptor agonists, and the method of making and using the novel ?-opioid receptor agonists. The novel ?-opioid receptor agonists are selective ?-opioid receptor agonists that have substantially no beta-arrestin 2 recruitment or low beta-arrestin 2 recruitment. The novel ?-opioid receptor agonists may be used for the treatment for alcohol use disorders and other co-occurring psychiatric disorders.Type: ApplicationFiled: June 8, 2018Publication date: June 25, 2020Applicant: Purdue Research FoundationInventors: Richard M Van Rijn, Mark S Cushman, Markus Lill, Robert J Cassell, Amr Hamed Mahmoud Abdallah, Mohamed S.A. Elsayed