Patents Issued in August 27, 2019
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Patent number: 10392359Abstract: Provided are a compound represented by Formula 1, and an organic electric element comprising a first electrode, a second electrode, and an organic material layer formed between the first electrode and the second electrode, wherein the organic material layer comprised the compound represented by Formula 1, and the driving voltage of an organic electronic device can be lowered, and the luminous efficiency, color purity and life time of an organic electronic device can be improved by comprising the compound represented by Formula 1 in the organic material layer.Type: GrantFiled: March 8, 2016Date of Patent: August 27, 2019Assignee: DUK SAN NEOLUX CO., LTD.Inventors: Yun-Sun Byun, Jung Cheol Park, Jinho Yun, Seung-Won Choi, Hyojin Kim, Yeon Hee Choi, Gyumin Lee
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Patent number: 10392360Abstract: This disclosure is related to methods for producing anhydroryanodol, ryanodol, or analogs thereof and novel compounds prepared thereby.Type: GrantFiled: December 20, 2017Date of Patent: August 27, 2019Assignee: California Institute of TechnologyInventors: Sarah Reisman, Kangway V. Chuang, Chen Xu
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Patent number: 10392361Abstract: The present invention relates to a novel process for the synthesis of the intermediate compounds constituted by chromanyl haloketones of formula III and 6-fluoro-2-(oxiran-2-yl)chromans of formula I. The intermediates thus obtained can be used for the synthesis of Nebivolol.Type: GrantFiled: January 23, 2017Date of Patent: August 27, 2019Assignee: Menarini International Operations Luxembourg S.A.Inventors: Sandra Bartoli, Serena Mannucci, Alessio Griselli, Alessio Stefanini
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Patent number: 10392362Abstract: The present invention relates to a method for the catalytic synthesis of lactide from lactic acid. The method relates to the synthesis of lactide from lactic acid under the catalysis of a zinc oxide nanoparticle aqueous dispersion as a catalyst. The present invention has four technical characteristics: I. the zinc oxide nanoparticle aqueous dispersion catalyst has a sufficient surface area, and the size of nanoparticles is merely 30-40 nm, providing a sufficient contact area between the substrate (lactic acid) and the catalyst; II. the new catalyst has a milder catalytic effect on polymerization, allowing the molecular weight distribution of a prepolymer within a range of 400-1500 g/mol, which is advantageous for depolymerization to proceed; III. the new catalyst is stable, thus avoiding oxidation or carbonization in a high temperature reaction; and IV. the new catalyst has a low toxicity and a small threat to human health.Type: GrantFiled: March 1, 2016Date of Patent: August 27, 2019Assignee: The Hong Kong Research Institute of Textiles and Apparel LimitedInventors: Yunzi Hu, Carol Sze Ki Lin, Walid Daoud
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Patent number: 10392363Abstract: The invention provides compounds of Formula (I), and their use in methods for treating or preventing a protozoan infection in a subject using a compound of Formula (I). The invention also provides the use of a compound of Formula (I) in the manufacture of a medicament for the treatment of a protozoan infection in a subject. The invention further provides a medical device when used in a method of treating or preventing a protozoan infection in a subject and to a medical device comprising the composition of the invention.Type: GrantFiled: August 28, 2015Date of Patent: August 27, 2019Assignee: Neoculi Pty Ltd.Inventors: Stephen Page, Andrew Stevens, Adam McCluskey, Martine Keenan, Rebecca Abraham
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Patent number: 10392364Abstract: Disclosed herein is an improved process for preparation of Lenalidomide and crystalline polymorphic forms thereof.Type: GrantFiled: August 11, 2015Date of Patent: August 27, 2019Assignee: AVRA LABORATORIES PVT. LTD.Inventors: Ramakrishna Rao, Ramadevi Nandipati, Ravi Gooda, Mukesh Padmakar Shewalkar, Venkat Vasantrao Bhadke
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Patent number: 10392365Abstract: The present invention relates to a process for preparing compound 1 that is useful as an antifungal agent. In particular, the invention seeks to provide new methodology for preparing compound 1 and substituted derivatives thereof.Type: GrantFiled: January 7, 2019Date of Patent: August 27, 2019Assignees: Mycovia Pharmaceuticals, Inc., The United States of America, as represented by the Secretary, Department of Health and Human ServicesInventors: William J. Hoekstra, Christopher M. Yates, Mark Behnke, Asaf Alimardanov, Scott A. David, Douglas Franklin Fry
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Patent number: 10392366Abstract: The present disclosure relates to azetidine compounds. The azetidine compounds are GPR119 modulators and useful for the prevention and/or treatment of diabetes, obesity, dyslipidemia and related disorders. The present disclosure furthermore relates to the use of azetidine compounds as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: GrantFiled: February 20, 2018Date of Patent: August 27, 2019Assignee: SANOFIInventors: Lothar Schwink, Christian Buning, Heiner Glombik, Christoph Pöverlein, Kurt Ritter, Nis Halland, Matthias Lohmann
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Patent number: 10392367Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.Type: GrantFiled: May 31, 2018Date of Patent: August 27, 2019Assignee: Quentis Therapeutics, Inc.Inventors: Joseph P. Vacca, Dansu Li, Sarah Bettigole
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Patent number: 10392368Abstract: The invention provides compounds of formula (I): or a pharmaceutically-acceptable salt thereof, wherein the variables are defined in the specification, that are inhibitors of JAK kinases, particularly JAK3. The invention also provides crystalline forms, pharmaceutical compositions comprising such compounds, methods of using such compounds to treat gastrointestinal and other inflammatory diseases, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: July 31, 2018Date of Patent: August 27, 2019Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Erik Fenster, Tom M. Lam, Mandy Loo, Robert Murray McKinnell, Anthony Francesco Palermo, Diana Jin Wang, Breena Fraga, Jerry Nzerem, Marta Dabros, Venkat R. Thalladi, Miroslav Rapta
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Patent number: 10392369Abstract: This invention relates to compounds of formula (I), a process for their preparation, pharmaceutical compositions containing them and their use in the treatment of conditions having an association with the orexin sub-type 1 receptor. Ar, R1, R2, R3, R4, R5 have meanings given in the description.Type: GrantFiled: April 17, 2017Date of Patent: August 27, 2019Assignee: Boehringer Ingelheim International GmbHInventors: Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec
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Patent number: 10392370Abstract: The present invention relates to an improved process for the preparation of Daclatasvir dihydrochloride by using compound salt of formula (VIIc).Type: GrantFiled: May 19, 2017Date of Patent: August 27, 2019Assignee: OPTIMUS DRUGS PVT LTDInventors: Desi Reddy Srinivas Reddy, Peketi Subba Reddy
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Patent number: 10392371Abstract: Provided herein are compounds which are useful as cooling sensation compounds.Type: GrantFiled: September 21, 2016Date of Patent: August 27, 2019Assignee: Senomyx, Inc.Inventors: Andrew P. Patron, Alain Noncovich, Timothy Davis, Chad Priest, Joseph R. Fotsing, Jane Ung, Catherine Tachdjian
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Patent number: 10392372Abstract: The present disclosure is directed to disclosed compounds that increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.Type: GrantFiled: December 23, 2015Date of Patent: August 27, 2019Assignee: Proteostasis Therapeutics, Inc.Inventors: Cecilia M. Bastos, Benito Munoz, Bradley Tait
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Patent number: 10392373Abstract: The present invention is concerned with substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, autoimmune, allergic, hematological, inflammatory and degenerative disorders. In particular, the compounds of the invention are Syk inhibitors. The invention also relates to a process for manufacturing the compounds of the invention.Type: GrantFiled: September 16, 2016Date of Patent: August 27, 2019Assignee: AB ScienceInventors: Alain Moussy, Abdellah Benjahad, Didier Pez, Claire Schalon, Franck Sandrinelli, Jason Martin, Willy Picoul, Emmanuel Chevenier
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Patent number: 10392374Abstract: A fumarate salt and a maleate salt of compound (I) represented by the following structural formula, as well as their corresponding pharmaceutical compositions, are disclosed. Particular single crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are characterized by a variety of properties and physical measurements. Methods of preparing specific crystalline forms of 1:1 compound (I) fumarate and 1:1 compound (I) maleate are also disclosed. The present invention also provides methods of treating a subject with a cancer.Type: GrantFiled: February 1, 2018Date of Patent: August 27, 2019Assignee: University Health NetworkInventors: Peter Brent Sampson, Miklos Feher, Heinz W. Pauls
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Patent number: 10392375Abstract: The present invention relates to compounds of Formula I and pharmaceutically acceptable compositions thereof, useful as IRAK inhibitors.Type: GrantFiled: April 23, 2018Date of Patent: August 27, 2019Assignee: Merck Patent GmbHInventors: Catherine Jorand-Lebrun, Ruoxi Lan, Austin Chen, Ryan C. Clark
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Patent number: 10392376Abstract: The present disclosure relates to heterocyclic compounds and methods which may be useful as inhibitors of ATR kinase for the treatment or prevention of cancer.Type: GrantFiled: July 13, 2018Date of Patent: August 27, 2019Assignees: Board of Regents, The University of Texas System, ChemPartner CorporationInventors: Maria Emilia Di Francesco, Philip Jones, Christopher Lawrence Carroll, Jason Bryant Cross, Suyambu Kesava Vijayan Ramaswamy, Michael Garrett Johnson, Sarah Lively, David Lapointe
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Patent number: 10392377Abstract: The invention relates to a compound comprising the following general formula (1): and said compound for use as a medicament, in particular for use in the treatment psychiatric or neurological disorders and inflammation, in particular neuroinflammation: (formula 1) wherein each of R1, R2 and R3 are selected independently from each other from alkyl, alkoxy, alkenyl, alkynyl, cycloalkyl, aryl, heterocycle, or heteroaryl.Type: GrantFiled: December 17, 2018Date of Patent: August 27, 2019Assignee: UNIVERSITAT BERNInventors: Jean-Louis Reymond, Simon Nicolussi, Jurg Gertsch
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Patent number: 10392378Abstract: The present disclosure is based, in part, on the discovery that disclosed compounds such as those having Formula (IIIa), (III), or (IV) can increase cystic fibrosis transmembrane conductance regulator (CFTR) activity as measured in human bronchial epithelial (hBE) cells.Type: GrantFiled: December 23, 2015Date of Patent: August 27, 2019Assignee: Proteostasis Therapeutics, Inc.Inventors: Cecilia M. Bastos, Benito Munoz, Bradley Tait
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Patent number: 10392379Abstract: The present disclosure provides, in part, compounds having allosteric effector properties against Hepatitis B virus Cp. Also provided herein are methods of treating viral infections, such as hepatitis B, comprising administering to a patient in need thereof a disclosed compound.Type: GrantFiled: September 15, 2016Date of Patent: August 27, 2019Assignees: Assembly Biosciences, Inc., Indiana University Research And Technology CorporationInventors: William Turner, Lee Daniel Arnold, Hans Maag, Mark Bures
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Patent number: 10392380Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of ubiquitin C-terminal hydrolase L1 (UCHL1). The invention further relates to the use of DUB inhibitors in the treatment of cancer and other indications. Compounds of the invention include compounds having the formula (I) or a pharmaceutically acceptable salt thereof, wherein R1 to R8 are as defined herein.Type: GrantFiled: February 12, 2018Date of Patent: August 27, 2019Assignee: MISSION THERAPEUTICS LIMITEDInventors: Alison Jones, Mark Ian Kemp, Martin Lee Stockley, Karl Gibson, Gavin Alistair Whitlock, Andrew Madin
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Patent number: 10392381Abstract: Methods for preventing, treating, and/or reducing the risk of developing non-alcoholic fatty liver disease in a subject in need thereof and pharmaceutical compositions for the prevention or treatment of non-alcoholic fatty liver disease. Methods for inhibiting excessive accumulation of fat in liver tissue. The methods include administering to the subject or contacting the liver tissue with a therapeutically effective amount of at least one compound of General Formula (I) or General Formula (II): or pharmaceutically-acceptable salts or solvates thereof. The pharmaceutical composition includes at least one compound of the General Formula (I) or the General Formula (II) for administration to a subject for the prevention or treatment of non-alcoholic fatty liver disease.Type: GrantFiled: May 6, 2015Date of Patent: August 27, 2019Assignee: Ohio UniversityInventors: Kelly D. McCall, Frank L. Schwartz, Douglas J. Goetz
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Patent number: 10392382Abstract: The present invention provides a compound, that is a 1-({halo-2-[(2-hydrocarbyl or substituted hydrocarbyl)oxy]phenyl}methyl)-(fused bicyclic nitrogen heteroaryl) carboxylic acid or an ester or sulfonamide thereof. The compound may be represented by the following formula Wherein R1, R2, R3, R4 A, X, W, Z and Y are as defined in the specification. The compounds may be administered to treat DP, FP, EP1, TP and/or EP4 receptor-mediated diseases or conditions.Type: GrantFiled: January 13, 2017Date of Patent: August 27, 2019Assignee: ALLERGAN, INC.Inventors: William R. Carling, Jose L. Martos, Jussi J. Kangasmetsa, Jenny W. Wang, David F. Woodward
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Patent number: 10392383Abstract: 4-Azaindazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of a 4-azaindazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.Type: GrantFiled: August 3, 2016Date of Patent: August 27, 2019Assignee: Samumed, LLCInventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, Joseph Timothy Marakovits, Venkataiah Bollu, John Hood
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Patent number: 10392384Abstract: The present invention relates to a novel process for preparing (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) and recovering (4S)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula (I) proceeding from (4R)-4-(4-cyano-2-methoxyphenyl)-5-ethoxy-2,8-dimethyl-1,4-dihydro-1,6-naphthyridine-3-carboxamide of the formula ent-(I)Type: GrantFiled: August 18, 2016Date of Patent: August 27, 2019Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Johannes Platzek, Kathrin Gottfried, Jens Assmann, Giulio Lolli
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Patent number: 10392385Abstract: A compound of general formula A, useful as potential anticancer agents against human cancer cell lines and process for the preparation thereof. General formula A R1=3-F, 3,4,5-OMe, 4-OMe, H, 4-CF3, 4-Cl, 4-OH-3-OMe, 3,4-CH2—O—CH2, 3,5-F, 4-OH, 1-napthyl, 9-phenanthryl, 4-Me. R2=3,4,5-OMe, 3,4-Cl, 4-F, 3,5-F, 2,5-OMe, 4-Cl, 4-OH-3-OMe, 3-OH, 3,4,5-OH, 4-CF3, 4-OMe, 4-NH2.Type: GrantFiled: January 20, 2017Date of Patent: August 27, 2019Assignee: Council of Scientific & Industrial ResearchInventors: Ahmed Kamal, Sathish Manda, Nagesh Narayana, Shankaraiah Nagula, Chetan Dushantrao Sabanis, Hari Krishna Namballa
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Patent number: 10392386Abstract: The invention provides compounds of formula (I): which contain a 4-membered heterocyclic amide, where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat respiratory diseases, and processes and intermediates useful for preparing such compounds.Type: GrantFiled: December 17, 2018Date of Patent: August 27, 2019Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Paul R. Fatheree, Gary E. L. Brandt, Cameron Smith, Steven D. E. Sullivan, Lori Jean Van Orden, Melanie A. Kleinschek, Glenn D. Crater
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Patent number: 10392387Abstract: Thermally assisted delayed fluorescent materials with triad-type materials for use in full color displays and lighting applications with the following generic structures are provided:Type: GrantFiled: May 18, 2018Date of Patent: August 27, 2019Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITYInventor: Jian Li
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Patent number: 10392388Abstract: The present invention provides novel derivative of ?-lactam antibiotics, such as meropenem. The inventive compounds include compounds of Formula (I), and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, and prodrugs thereof. Also provided are particles (e.g., nanoparticles) and pharmaceutical compositions thereof that are mucus penetrating. The inventive particles and pharmaceutical compositions may be useful in delivering an inventive compound to the respiratory tract of a subject. The invention further provides methods of using and kits including the inventive compounds, particles thereof, and/or pharmaceutical compositions thereof for treating and/or preventing a pulmonary disease (e.g., a respiratory tract infection).Type: GrantFiled: July 14, 2017Date of Patent: August 27, 2019Assignee: kala pharmaceuticals, Inc.Inventors: Winston Zapanta Ong, Pawel Wojciech Nowak, Jinsoo Kim, Elizabeth M. Enlow, James Bourassa, Yen Cu, Alexey Popov, Hongming Chen
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Patent number: 10392389Abstract: Disclosed herein are new heterocyclic compounds and compositions and their application as pharmaceuticals for the treatment of disease. Methods of inhibiting PAS Kinase (PASK) activity in a human or animal subject are also provided for the treatment of diseases such as diabetes mellitus.Type: GrantFiled: October 25, 2013Date of Patent: August 27, 2019Assignee: BioEnergenix LLCInventors: John McCall, Robert C. Kelly, Donna L. Romero
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Patent number: 10392390Abstract: Provided in some embodiments are compounds herein. Also provided in some embodiments are methods for weight management, inducing satiety, and decreasing food intake, and for preventing and treating obesity, antipsychotic-induced weight gain, type 2 diabetes, Prader-Willi syndrome, tobacco/nicotine dependence, drug addiction, alcohol addiction, pathological gambling, reward deficiency syndrome, and sex addiction), obsessive-compulsive spectrum disorders and impulse control disorders (including nail-biting and onychophagia), sleep disorders (including insomnia, fragmented sleep architecture, and disturbances of slow-wave sleep), urinary incontinence, psychiatric disorders (including schizophrenia, anorexia nervosa, and bulimia nervosa), Alzheimer disease, sexual dysfunction, erectile dysfunction, epilepsy, movement disorders (including parkinsonism and antipsychotic-induced movement disorder), hypertension, dyslipidemia, nonalcoholic fatty liver disease, obesity-related renal disease, and sleep apnea.Type: GrantFiled: April 26, 2016Date of Patent: August 27, 2019Assignee: Arena Pharmaceuticals, Inc.Inventors: Albert S. Ren, Graeme Semple, Xiuwen Zhu, Carleton R. Sage
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Patent number: 10392391Abstract: The present invention relates to compounds useful as inhibitors of ATR protein kinase. The invention also relates to pharmaceutically acceptable compositions comprising the compounds of this invention; methods of treating of various diseases, disorders, and conditions using the compounds of this invention; processes for preparing the compounds of this invention; intermediates for the preparation of the compounds of this invention; and methods of using the compounds in in vitro applications, such as the study of kinases in biological and pathological phenomena; the study of intracellular signal transduction pathways mediated by such kinases; and the comparative evaluation of new kinase inhibitors. The compounds of this invention have formula I: or a pharmaceutically acceptable salt, wherein the variables are as devined herein. Moreover, The compounds of this invention have formula I-A: or a pharmaceutically acceptable salt, wherein the variables are as defined herein.Type: GrantFiled: June 26, 2017Date of Patent: August 27, 2019Assignee: Vertex Pharmaceuticals IncorporatedInventors: Nadia Ahmad, Dean Boyall, Jean-Damien Charrier, Chris Davis, Rebecca Davis, Steven Durrant, Gorka Etxebarria I Jardi, Damien Fraysse, Juan-Miguel Jimenez, David Kay, Ronald Knegtel, Donald Middleton, Michael O'Donnell, Maninder Panesar, Francoise Pierard, Joanne Pinder, David Shaw, Pierre-Henri Storck, John Studley, Heather Twin
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Patent number: 10392392Abstract: The present invention provides substituted imidazo[1,2-b]pyridazines that are useful as protein kinase inhibitors and have one of the following structures (I), (II) or (III): or a stereoisomer, prodrug, tautomer or pharmaceutically acceptable salt thereof, wherein R, R1, R2 and X are as defined herein. For example, a compound having the following structure: Compositions and methods for using the same in the treatment of cancer, autoimmune, inflammatory and other Pim kinase-associated conditions are also disclosed.Type: GrantFiled: July 11, 2018Date of Patent: August 27, 2019Assignee: Tolero Pharmaceuticals, Inc.Inventors: Yong Xu, Benjamin Gary Brenning, Steven G. Kultgen, Xiaohui Liu, Michael David Saunders, Koc-Kan Ho
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Patent number: 10392393Abstract: A compound with the formula I, wherein R2 is of formula II, where A is a C5-7 aryl group, X is selected from the group consisting of: OH, SH, CO2H, COH, N?C?O, NHNH2, CONHNH2, (III), (IV), and NHRN, wherein RN is selected from H and C1-4 alkyl, and either: (i) Q1 is a single bond, and Q2 is selected from a single bond and —Z—(CH2)n—, where Z is selected from a single bond, O, S and NH and n is from 1 to 3; or (ii) Q1 is —CH?CH—, and Q2 is a single bond; and its conjugates.Type: GrantFiled: January 26, 2017Date of Patent: August 27, 2019Assignee: Medimmune LimitedInventors: Philip Wilson Howard, Thaïs Cailleau
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Patent number: 10392394Abstract: Antimicrobial compounds are provided that are polymerizable. The compounds include monomers with antimicrobial properties. The compounds have cross-linking properties. The compounds may be utilized in dental and/or medical applications, including dental composites, dentures, bonding agents, sealants, resins and medical devices.Type: GrantFiled: February 1, 2018Date of Patent: August 27, 2019Assignee: Board of Supervisors of Louisiana State University and Agricultural and Mechanical CollegeInventor: Xiaoming Xu
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Patent number: 10392395Abstract: To provide nitrogen-containing aromatic compounds with excellent oxygen reduction activity, metal complexes containing them, and catalysts and electrodes employing the same, the present invention provides an aromatic compound satisfying the following conditions (a) and (b): (a) It has 2 or more structures surrounded by at least 4 coordinatable nitrogen atoms (which structures may be the same or different), (b) At least one of the nitrogen atoms composing the structure is a nitrogen atom in a 6-membered nitrogen-containing heterocyclic ring.Type: GrantFiled: October 29, 2010Date of Patent: August 27, 2019Assignees: SUMITOMO CHEMICAL COMPANY, LIMITED, MAX PLANCK GESELLSCHAFT ZUR FOERDERUNG DER WISSENSCHAFTEN E.V.Inventors: Nobuyoshi Koshino, Hideyuki Higashimura, Klaus Muellen, Christian von Malotki, Qi Su, Martin Baumgarten, Hassan Norouzi-Arasi, Lena Arnold, Ruili Liu
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Patent number: 10392396Abstract: Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases. Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.Type: GrantFiled: May 3, 2018Date of Patent: August 27, 2019Assignee: University of Puerto RicoInventors: Cornelis P. Vlaar, Suranganie Dharmawardhane Flanagan, Eliud Hernandez-O'Farrill, Linette Castillo-Pichardo
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Patent number: 10392397Abstract: Pharmaceutical compounds, compositions, and methods are presented in which various heterocyclic thiosemicarbazone derivatives are prepared. Contemplated compounds will be suitable to inhibit or reduce cellular growth or proliferation and are thus beneficial in the manufacture of drugs to treat neoplastic diseases.Type: GrantFiled: August 8, 2016Date of Patent: August 27, 2019Assignees: NantBio, Inc., Nant Holdings IP, LLCInventors: Chunlin Tao, Qinwei Wang, Patrick Soon-Shiong
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Patent number: 10392398Abstract: The present invention is directed to methods, compositions and kits for treatment of cancer, e.g. heptacellular carcinoma. In some embodiments, the present invention discloses the use of a small-molecule compound of formula (I)-(XXVI) and (III?) as disclosed herein to inhibit transcription factor Late SV40 Factor (LSF) for treatment of cancer, e.g., HCC.Type: GrantFiled: September 25, 2017Date of Patent: August 27, 2019Assignee: TRUSTEES OF BOSTON UNIVERSITYInventors: Ulla Hansen, Scott Schaus, Trevor Grant, Joshua Bishop, John Kavouris, Lisa M. Christadore
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Patent number: 10392399Abstract: Described herein are crystalline forms of Compound 1 useful for the prevention and treatment of angiogenic ocular conditions; methods of treating a disease comprising; processes for preparing; and kits comprising, the same.Type: GrantFiled: September 1, 2017Date of Patent: August 27, 2019Assignee: kala pharmaceuticals, Inc.Inventors: Minh Ngoc Nguyen, Winston Zapanta Ong
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Patent number: 10392400Abstract: Provided herein are palladium-mediated coupling reactions useful in the preparation of ketone-containing organic molecules. The provided methods can be used for the preparation of natural products and pharmaceutical agents, including Eribulin, halichondrins, and analogs thereof. The present invention also provides novel halichondrin analogs which can be prepared via the palladium-mediated coupling reactions. The novel halichondrin analogs can be used in the prevention and/or treatment of diseases or conditions (e.g., proliferative diseases such as cancer).Type: GrantFiled: November 10, 2017Date of Patent: August 27, 2019Assignee: President and Fellows of Harvard CollegeInventors: Jung Hwa Lee, Yoshito Kishi, Ayumi Osawa, Zhanjie Li
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Patent number: 10392401Abstract: The present invention relates to crystal form A of a compound. The present invention also discloses a preparation method and a pharmaceutical composition of the crystal form A. The crystal form A has strong hypoglycemic activity in vivo and is expected to be a novel pharmaceutically active ingredient for treating or preventing type II diabetes and/or complications of type II diabetes.Type: GrantFiled: February 3, 2016Date of Patent: August 27, 2019Assignee: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCESInventors: Hong Liu, Jiang Wang, Jian Li, Jia Li, Jingya Li, Shengbin Zhou, Mingbo Su, Hualiang Jiang, Xiaomin Luo, Kaixian Chen
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Patent number: 10392402Abstract: The present invention is directed to certain amides and heterocyclic compounds. The present invention also relates to uses of these compounds to treat several diseases including autoimmune disorders, cardiovascular disorders, inflammation, central nervous system disorders, arterial thrombotic disorders, fibrotic disorders, glaucoma, and neoplastic disorders.Type: GrantFiled: May 18, 2016Date of Patent: August 27, 2019Assignee: Translational Drug Development, LLCInventors: Tong Wang, Stephen Gately
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Patent number: 10392403Abstract: The present invention relates to a novel method for preparing thienopyrimidine compound having an activity of selectively inhibiting tyrosine kinase, specifically the mutant epidermal growth factor receptor tyrosine kinase; and a novel intermediate used therein. According to the method of the present invention, the industrial mass-production of the compound of Formula 1, which is useful as a therapeutic agent for non-small cell lung cancer induced by the mutant epidermal growth factor receptor tyrosine kinase, can be implemented more conveniently and efficiently than the conventional technology.Type: GrantFiled: October 31, 2016Date of Patent: August 27, 2019Assignee: HANMI PHARM. CO., LTD.Inventors: Wook Jang, Young Ho Moon, Tae Hee Ha, Kwee Hyun Suh
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Patent number: 10392404Abstract: The present invention provides compounds of Formula (I) and (II) as described herein, and salts thereof and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.Type: GrantFiled: September 11, 2015Date of Patent: August 27, 2019Assignee: Novartis AGInventors: Paul Andrew Barsanti, Matthew T. Burger, Yan Lou, Gisele A. Nishiguchi, Valery Rostislavovich Polyakov, Savithri Ramurthy, Sharadha Subramanian, Benjamin R. Taft, Huw Rowland Tanner, Lifeng Wan
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Patent number: 10392405Abstract: Compounds are provided that are useful as immunomodulators. The compounds have the following Formula (I) or (II): including stereoisomers and pharmaceutically acceptable salts thereof, wherein R, R1, R2a, R2b, R2c, R3, R4, R5, R6a, R6b, R6c, m and n are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.Type: GrantFiled: August 7, 2018Date of Patent: August 27, 2019Assignee: ChemoCentryx, Inc.Inventors: Viengkham Malathong, Jeffrey McMahon, Darren J. McMurtrie, Sreenivas Punna, Howard S. Roth, Rajinder Singh, Penglie Zhang
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Patent number: 10392406Abstract: The present invention provides the following compounds having anti-viral activity. A1 is CR1AR1B, S or O; A2 is CR2AR2B, S or O; A3 is CR3AR3B, S or O; A4 is CR4AR4B, S or O; the number of hetero atoms among atoms constituting the ring which consists of A1, A2, A3, A4, nitrogen atom adjacent to A1 and carbon atom adjacent to A1, is 1 or 2; R1A and R1B are each independently hydrogen, halogen, alkyl, or the like; R2A and R2B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B are each independently hydrogen, halogen, alkyl, or the like; R4A and R4B are each independently hydrogen, halogen, alkyl, or the like; R3A and R3B may be taken together to form non-aromatic carbocycle or non-aromatic heterocycle; X is CH2, S or O; R1 is each independently halogen, hydroxy, or the like; m is any integer of 0 to 2; and n is any integer of 1 to 2.Type: GrantFiled: April 27, 2016Date of Patent: August 27, 2019Assignee: SHIONOGI & CO., LTD.Inventor: Makoto Kawai
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Patent number: 10392407Abstract: The invention relates to novel methods for preparing indolinobenzodiazepine dimer compounds and their synthetic precursors.Type: GrantFiled: January 3, 2018Date of Patent: August 27, 2019Assignee: IMMUNOGEN, INC.Inventors: Baudouin Gérard, Manami Shizuka, Michael Louis Miller, Richard A. Silva
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Patent number: 10392408Abstract: A siloxane oligomer of the following formula is provided. This siloxane can increase the hydrophobicity and/or the lipophobicity of a surface of a solid substrate and/or self-propel when deposited in solution on a surface of a solid substrate.Type: GrantFiled: June 26, 2018Date of Patent: August 27, 2019Assignee: AVMOR LTDInventor: Mitra Vasei