Patents Issued in November 6, 2018
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Patent number: 10118885Abstract: A carbonylation process for producing acetic acid including: (a) carbonylating methanol or its reactive derivatives in the presence of a Group VIII metal catalyst and methyl iodide promoter to produce a liquid reaction mixture including acetic acid, water, methyl acetate and methyl iodide; and (b) feeding the liquid reaction mixture at a feed temperature to a flash vessel which is maintained at a reduced pressure.Type: GrantFiled: November 9, 2017Date of Patent: November 6, 2018Assignee: CELANESE INTERNATIONAL CORPORATIONInventor: Jeremy J. Patt
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Patent number: 10118886Abstract: A process for producing biofuels compounds directly from carboxylic acid esters recovered from a fermentation system is described. The process involves taking a fermentation broth that has been reduced to a dry powder containing free organic acids; reacting the carboxylic acid in the powder with an alcohol solvent under a CO2-containing atmosphere in substantial absence of any other acid catalyst at a reaction temperature and pressure that corresponds to supercritical, critical or near critical conditions for at least one of the alcohol or CO2 to synthesize an ester, then subjecting the ester to either hydrogenolysis or hydrogenation to form a biofuel.Type: GrantFiled: October 19, 2016Date of Patent: November 6, 2018Assignee: Archer Daniels Midland CompanyInventors: Kenneth Stensrud, Padmesh Venkitasubramanian
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Patent number: 10118887Abstract: Polymers including ?-hydroxymethylacrylate units and methods of preparing polymers from ?-hydroxymethylacrylates are provided. Advantageously, ?-hydroxymethylacrylates may be used in an emulsion polymerization and function as a polymerizable surfactant. The ability of the ?-hydroxymethylacrylates to be used as a polymerizable surfactant allows for emulsion polymerization systems to be prepared without other surfactants.Type: GrantFiled: August 21, 2015Date of Patent: November 6, 2018Assignee: The University of AkronInventors: Abraham Joy, Chao Peng
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Patent number: 10118888Abstract: A method for isomerizing a bis(aminomethyl)cyclohexane, including isomerizing a bis(aminomethyl)cyclohexane while introducing an inert gas in a reaction solution containing a bis(aminomethyl)cyclohexane, at least one selected from the group consisting of an alkali metal, an alkali metal-containing compound, an alkaline earth metal and an alkaline earth metal-containing compound, and a benzylamine compound.Type: GrantFiled: February 25, 2016Date of Patent: November 6, 2018Assignee: Mitsubishi Gas Chemical Company, Inc.Inventors: Yuko Shimizu, Yoshiaki Yamamoto
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Patent number: 10118889Abstract: A compound is represented by the following formula (1). In the formula (1), Ar is a substituted or unsubstituted aryl group including 6 to 30 ring carbon atoms, Ra are independently a substituted or unsubstituted alkyl group including 1 to 15 carbon atoms, or a substituted or unsubstituted cycloalkyl group including 3 to 15 carbon atoms, Rb1 to Rb4 are independently a halogen atom, a cyano group, a substituted or unsubstituted alkyl group including 1 to 15 carbon atoms, or the like, Rc1 to Rc10 are independently a hydrogen atom, a halogen atom, a cyano group, a substituted or unsubstituted alkyl group including 1 to 15 carbon atoms, or the like, * is a bonding position at which one of Rc1 to Rc10 is bonded to either nitrogen atom, x is an integer from 0 to 3, y is an integer from 0 to 4, and z are independently an integer from 0 to 5.Type: GrantFiled: January 5, 2017Date of Patent: November 6, 2018Assignee: IDEMITSU KOSAN CO., LTD.Inventors: Hirokatsu Ito, Masahiro Kawamura, Yumiko Mizuki, Tasuku Haketa, Tomoharu Hayama, Ryota Takahashi
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Patent number: 10118890Abstract: The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: wherein A is an aryl or heteroaryl, each with or without subsutitution; and R1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl)2, —NH-(alkenyl), —NH-(alkynyl)—NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl), —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure: with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure: and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:Type: GrantFiled: October 9, 2015Date of Patent: November 6, 2018Assignee: THE RESEARCH FOUNDATION FOR THE STATE UNIVERSITY OF NEW YORKInventors: Ming-Yu Ngai, Katarzyna N. Hojczyk
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Patent number: 10118891Abstract: Organosulfur compounds and compositions are disclosed which can be administered in order to provide protection from the formation of aldehyde-protein adducts, protein aggregates, and the resulting neuroinflammation. Various neurodegenerative diseases which are suitable for treatment using these compositions include Alzheimer's disease, senile dementia, Parkinson's disease, multiple sclerosis, Lewy body disease, peripheral neuropathy, spinal cord injury, traumatic brain injury, stroke and cerebral ischemia.Type: GrantFiled: March 1, 2017Date of Patent: November 6, 2018Assignee: Allium Vitalis, Inc.Inventor: David Michael Ott
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Patent number: 10118892Abstract: The present invention relates to sulfonium salts of formula (I): (I), their preparation, and utility as precursors for preparing functionalized organic compounds, wherein R1 and R2 are the same or different and each is independently selected from an optionally substituted aryl group, an optionally substituted alkynyl group, an optionally substituted alkenyl group, an optionally substituted alkyl group, an optionally substituted cycloalkyl group, an optionally substituted cycloalkenyl group, an optionally substituted aralkyl group, an optionally substituted arylalkenyl group, an optionally substituted heteroaryl group, an optionally substituted heterocyclyl group, an optionally substituted amine, an optionally substituted alkoxy group, an optionally substituted thioether group, an optionally substituted phosphine group, an optionally substituted boron species, an optionally substituted carbene, an organometallic moiety, and a halide, or R1 and R2 are joined together to form an optionally substituted sulfur-conType: GrantFiled: October 14, 2013Date of Patent: November 6, 2018Assignee: UCL BUSINESS PLCInventors: Erik Arstad, Kerstin Sander, Thibault Gendron
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Patent number: 10118893Abstract: The development of anticancer metal-based drugs was done by reacting oyelamine with selenous acid to produce a quaternary ammonium salt which consequently converted to platinum and cobalt cationic complexes via complexing the first compounds with platinum (II) or cobalt (II) ions. The surface properties studies that were conducted included critical micelle concentration (CMC), maximum surface excess (?max) and minimum surface area (Amin). Free energy of micellization (?G° mic) and adsorption (?G° ads) were calculated. Antitumor activities were tested by using Ehrlich Acites Carcinoma (EAC) as a model system of mice cell tumor. These compounds were also tested in vitro on human five monolayer tumor cell lines: MCF7 (Breast carcinoma), HEPG2 (liver carcinoma), and HCT116 (colon carcinoma), etc. FTIR spectra, elemental analysis and H1 NMR spectrum were performed to insure the purity of the prepared compounds.Type: GrantFiled: September 29, 2014Date of Patent: November 6, 2018Assignee: Umm-Al-Qura UniversityInventor: Manal Mohamed Khowdairy
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Patent number: 10118894Abstract: Compounds of Formula I are disclosed and methods of treating viral infections with compositions comprising such compounds.Type: GrantFiled: July 20, 2015Date of Patent: November 6, 2018Assignee: ViiV HEALTHCARE UK LIMITEDInventors: Brian Alvin Johns, Emile Johann Velthuisen, Jason Gordon Weatherhead
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Patent number: 10118895Abstract: Novel compounds according to Formula I Meta or para or a pharmaceutically acceptable salt thereof wherein: A11-A14 are N or CR11, CR12, CR13, CR14, respectively, with the proviso that no more than two of the four positions A in A11-A14 can be simultaneously N; A6, A7, A8, A9, A10 are N or CR6, CR7, CR8, CR9, CR10, respectively, with the proviso that at least one but no more than two of the five positions A in A6, A7, A8, A9, A10 is N; R1 is C(2-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, (di)C(3-6)cycloalkylamino or (di)(C(3-6)cycloalkylC(1-3)alkyl)amino; R5 is H, hydroxyethyl, methoxyethyl, C(1-6)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroarylC(1-3)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(2-5)heterocycloalkyl or C(2-5)heterocycloalkylC(1-3)alkyl; the sulfonyl group with R1 is represented by one of R7, R8 or R9; R15 is H, C(1-6)alkyl, C(3-6)cycloalkyl, C(3-6)cycloalkylC(1-3)alkyl, C(6-10)aryl, C(6-10)arylC(1-3)alkyl, C(1-9)heteroaryl, C(1-9)heteroType: GrantFiled: June 3, 2016Date of Patent: November 6, 2018Assignees: LEAD PHARMA HOLDING B.V., SANOFIInventors: Joseph Maria Gerardus Barbara Cals, David Machnik, Sander Bernardus Nabuurs, Jean-Francois Sabuco, Laurent Schio
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Patent number: 10118896Abstract: The present technology is directed to compounds, compositions, and methods related to non-morphinan-like kappa opioid receptor (KOR) antagonists. The technology is suited to treat addiction, diuresis, depression, post traumatic stress disorder, an eating disorder, panic disorder, social anxiety disorder, general anxiety disorder, obsessive compulsive disorders, excessive or unreasonable specific phobias, and/or other conditions related to anxiety or aversion-reward responses.Type: GrantFiled: November 25, 2015Date of Patent: November 6, 2018Assignees: UNIVERSITY OF KANSAS, THE SCRIPPS RESEARCH INSTITUTEInventors: Jeffrey Aube, Kevin Frankowski, Thomas Prisinzano, Laura Bohn
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Patent number: 10118897Abstract: The present disclosure relates to crystalline solid forms of [(4-hydroxy-1-methyl-7-phenoxy-isoquinoline-3-carbonyl)-amino]-acetic acid, the process of preparing the forms, and pharmaceutical compositions and methods of use thereof.Type: GrantFiled: March 17, 2017Date of Patent: November 6, 2018Assignee: FibroGen, Inc.Inventors: Claudia Witschi, Jung Min Park, Michael D. Thompson, Michael John Martinelli, David A. Yeowell, Michael P. Arend
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Patent number: 10118898Abstract: The present application provides methods for decarboxylation of amino acids via imine formation with a catalyst under pressurized, heated, conditions in either a microwave or oil bath, with optional recovery of the catalyst and/or catalyst byproduct.Type: GrantFiled: August 29, 2016Date of Patent: November 6, 2018Assignee: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.Inventors: Richard W. Morrison, Douglas Michael Jackson, Daniel Richard Morrison
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Patent number: 10118899Abstract: The present invention aims to provided a novel production method of an enzalutamide crystal form in which wet crystals of enzalutamide are obtained in a step of crystallizing in the production process of the enzalutamide crystal form, and then 2-propanol which is solvated with enzalutamide and the B-type crystals are reduced. The present invention relates to a production method of an enzalutamide crystal form, which comprises a step of crystallizing for obtaining wet crystals of enzalutamide, and a step of drying the wet crystals, and comprises a step of washing using a mixed solvent of a good solvent and a poor solvent after the step of crystallizing.Type: GrantFiled: May 27, 2016Date of Patent: November 6, 2018Assignee: Astellas Pharma, Inc.Inventors: Yusuke Suzuki, Shuichi Nakagawa, Tsuyoshi Kitamura
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Patent number: 10118900Abstract: The present invention is directed to benzimidazole derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions mediated by the CB-1 receptor; more particularly, use in the treatment of disorders and conditions responsive to inverse agonism of the CB-1 receptor. More particularly, the compounds of the present invention are useful in the treatment of metabolic disorders.Type: GrantFiled: August 23, 2016Date of Patent: November 6, 2018Assignee: Janssen Pharmaceutica NVInventors: Mark J. Macielag, Rui Zhang, Yue-Mei Zhang, Bin Zhu, Michael H. Parker, Donald W. Ludovici, Daniel J. Parks, Bart L. DeCorte, Michael N. Greco
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Patent number: 10118901Abstract: The present invention relates to a class of hydroxamic acid compounds of Formula (I), which act as alkylating agents and/or inhibitors of the HDAC pathway, having potential utility in the treatment of a neoplastic disease and immune diseases.Type: GrantFiled: January 31, 2013Date of Patent: November 6, 2018Assignee: Purdue Pharmaceutical Products L.P.Inventors: Yu Chen, Yi Chen
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Patent number: 10118902Abstract: Provided herein are small molecule neurotensin receptor agonists, compositions comprising the compounds, and methods of using the compounds and compositions comprising the compounds.Type: GrantFiled: June 24, 2015Date of Patent: November 6, 2018Assignee: SANFORD BURNHAM PREBYS MEDICAL DISCOVERY INSTITUTEInventors: Anthony B. Pinkerton, Paul M. Hershberger, Satyamaheshwar Peddibhotla, Patrick R. Maloney, Michael P. Hedrick
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Patent number: 10118903Abstract: In some aspects, the present invention provides compounds of the formula (IV), wherein the variables are as defined herein, which may be used as inhibitors of histone demethylase or spermine oxidase. Also provided herein are pharmaceutical compositions of the compounds and methods using the compounds in the treatment of diseases such as cancer and cardiovascular disease.Type: GrantFiled: February 6, 2015Date of Patent: November 6, 2018Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENTInventors: Patrick M. Woster, Craig J. Kutz
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Patent number: 10118904Abstract: The invention relates to triazole compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as modulators of demyelinating diseases: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention, methods of using the compositions and kits thereof in the treatment of various demyelinating and neurodegenerative diseases, including multiple sclerosis.Type: GrantFiled: June 3, 2016Date of Patent: November 6, 2018Assignee: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Robert J. Davies, Jingrong Cao, Meghan Elise Cockerill, Philip Noel Collier, Elisabeth Doyle, James Daniel Frantz, Huai Gao, Brian Anthony Goldman, Ronald Lee Grey, Jr., Anne-Laure Grillot, Wenxin Gu, James A. Henderson, Raul Eduardo Krauss Irarrazaval, Adrianne Lynn Kolpak, Yusheng Liao, Sanjay Shivayogi Magavi, David Messersmith, Albert Charles Pierce, Emanuele Perola, Elizabeth Jin-Sun Ryu, Joshua Syken, Jian Wang, Michael Paul DeNinno, Francois Maltais
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Patent number: 10118905Abstract: Triazine-arylhydroxy-aldehyde condensates are reacted with at least one alkylene carbonate to form alkoxylated triazine-arylhydroxy-aldehyde condensates.Type: GrantFiled: September 22, 2017Date of Patent: November 6, 2018Assignee: Hexion Inc.Inventors: Ganapathy Viswanathan, Anthony Maiorana, Stephan Schröter, Pravin Kukkala
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Patent number: 10118906Abstract: The present invention relates to the use of novel oxadiazoles of the formula I or an N-oxide and/or their agriculturally useful salts for controlling phytopathogenic fungi, or to a method for combating phytopathogenic harmful fungi, which process comprises treating the fungi or the materials, plants, the soil or seeds to be protected against fungal attack, with an effective amount of at least one compound of formula I or an N-oxide or an agriculturally acceptable salt thereof; and to agrochemical compositions comprising at least one such compound and to agrochemical compositions further comprising seeds.Type: GrantFiled: June 1, 2015Date of Patent: November 6, 2018Assignee: BASF SEInventors: Andy Wieja, Christian Winter, Claudia Rosenbaum, Doris Kremzow-Graw, Franz Roehl, Joachim Rheinheimer, Manojkumar Poonoth, Violeta Terteryan, Egon Haden, Ana Escribano Cuesta, Janosch Harald Achenbach, Tobias Mentzel, Christine Wiebe
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Patent number: 10118907Abstract: The present invention relates to deuterated 1-piperazino-3-phenyl-indanes and salts thereof with activity at dopamine receptors D1 and D2 as well as the 5HT2 receptors in the central nervous system, to medicaments comprising such compounds as active ingredients, to the use of such compounds in the treatment of diseases in the central nervous system, and to methods of treatment comprising administration of such compounds.Type: GrantFiled: February 17, 2017Date of Patent: November 6, 2018Assignee: H. LUNDBECK A/SInventors: Morten Jorgensen, Peter Hongaard Andersen, Klaus Gjervig Jensen
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Patent number: 10118908Abstract: A method for manufacturing furan-2,5-dicarboxylic acid (FDCA) by converting a furan-2,5-dicarboxylate salt (MFDC) into furan-2,5-dicarboxylic acid (FDCA), includes the steps of combining solid MFDC with an inorganic acid (HY), to form a reaction mixture having solid FDCA in a concentration of 1-15 wt. % in a solution of a salt resulting from the cation of the furan-2,5-dicarboxylate salt and the anion of the inorganic acid (MY solution), removing solid FDCA from the reaction mixture in a solid/liquid separation step, and providing at least 40 vol. % of the MY solution resulting from the solid/liquid separation step to the step of combining MFDC with HY. The step of providing part of the MY salt solution resulting from the solid/liquid separation step to the step of combining MFDC with HY makes it possible to obtain a stable and economic process which results in an FDCA product with good quality, and obtained in high yield.Type: GrantFiled: March 17, 2016Date of Patent: November 6, 2018Assignee: PURAC BIOCHEM B.V.Inventors: Jan Van Krieken, Andre Banier De Haan
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Patent number: 10118909Abstract: The present invention relates to a monascuspurpurone compound of formula (I): or a pharmaceutically acceptable derivative thereof as described in the specification, the process for preparation of the same, and the composition comprising the same. The uses of a monascuspurpurone compound for promoting adipocyte differentiation, for increasing the activity of PPAR? and/or C/EBP?, for lowering blood glucose, for preventing and/or treating a disease or disorder related to insulin resistance, and for preventing and/or treating metabolic syndrome or its complications are also provided.Type: GrantFiled: October 9, 2014Date of Patent: November 6, 2018Inventors: Ming-Jen Cheng, Ping-Hsun Yang, Ming-Der Wu, Shie-Jea Lin, Gwo-Fang Yuan, Yen-Lin Chen, Hsuen-Chun Liao, Kai-Ping Chen
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Patent number: 10118910Abstract: This invention is benzothiophene-based estrogen receptor downregulators and their compositions and uses to treat estrogen-related medical disorders.Type: GrantFiled: December 9, 2016Date of Patent: November 6, 2018Assignee: The Board of Trustees of the University of IllinoisInventors: Gregory R. Thatcher, Rui Xiong, Jiong Zhao, Debra A. Tonetti
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Patent number: 10118911Abstract: Disclosed are a p-toluenesulfonate of a MEK kinase inhibitor, and a crystal form thereof and a preparation method thereof. Specifically disclosed are a 2-((2-fluorine-4-iodophenyl)amino)-1-methyl-4-((6-methylpyridine-3-group)oxygroup)-6-carbonyl-1,6-dihydropyridine-3-formamide p-toluenesulfonate (a compound represented by formula (I)), a crystal form I, and a preparation method thereof. The obtained crystal form I of the compound of formula (I) has good crystal form stability and chemical stability, and the crystallization solvent used has low toxicity and low residue, and is more suitable for use in clinical treatment.Type: GrantFiled: March 8, 2016Date of Patent: November 6, 2018Assignee: Jiangsu Hengrui Medicine Co., Ltd.Inventors: Guaili Wu, Xiaohui Gao, Lin Bian, Junlei Jia
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Patent number: 10118912Abstract: An improved process is provided for the preparation of Ledipasvir and its pharmaceutically acceptable salts or solvates thereof, which is useful as an antiviral agent. This disclosure also provides a process for the preparation of key intermediates of Ledipasvir.Type: GrantFiled: June 29, 2016Date of Patent: November 6, 2018Assignee: Optimus Drugs Private Ltd.Inventors: Dnyandev Ragho Rane, Srinivas Reddy Desi Reddy, Subbareddy Peketi, Srinivas Rao Velivela
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Patent number: 10118913Abstract: Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.Type: GrantFiled: March 30, 2018Date of Patent: November 6, 2018Assignee: 3-V Biosciences, Inc.Inventors: Johan D. Oslob, Robert S. McDowell, Russell Johnson, Hanbiao Yang, Marc Evanchik, Cristiana A. Zaharia, Haiying Cai, Lily W. Hu, Allan S. Wagman
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Patent number: 10118914Abstract: The present invention provides compounds having a CB1 receptor-binding moiety and a directing moiety. In related aspects, the invention provides pharmaceutical compositions containing compounds of the invention, methods for inhibiting a pathway modulated in part by the CB1 receptor activity, and methods for treating a condition or disorder mediated in part by CB1 receptor activity. In certain embodiments, the compounds are compounds of Formula I. Methods of preparing compounds of Formula I are also described. In another aspect, the invention provides methods of identifying a selective agonist of the beta-arrestin pathway over the G-protein pathway.Type: GrantFiled: December 19, 2016Date of Patent: November 6, 2018Assignee: The University of North Carolina at GreensboroInventors: Patricia H. Reggio, Derek M. Shore, Dow P. Hurst
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Patent number: 10118915Abstract: The invention provides novel ligands of Kappa (?) opioid receptors, such as can be used to modulate a Kappa opioid receptor. Methods of synthesis and methods of use are also provided. Compounds of the invention can be used therapeutically in the treatment of dissociative disorders or pain, or to provide neuroprotection, or to induce diuresis, or to modulate the immune system, or for treatment of one or more of an affective disorders comprising depression or stress/anxiety; an addictive disorder; alcoholism, epilepsy; a cognition deficiency; schizophrenia; Alzheimer's disease; or pain.Type: GrantFiled: May 15, 2017Date of Patent: November 6, 2018Assignee: The Scripps Research InstituteInventors: Edward Roberts, Miguel A. Guerrero, Mariangela Urbano, Hugh Rosen
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Patent number: 10118916Abstract: The present invention provides for compounds of formula (I) wherein R1, m, Z, G1, R2, and R3 have any of the values defined in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions mediated and modulated by CFTR, including cystic fibrosis, Sjögren's syndrome, pancreatic insufficiency, chronic obstructive lung disease, and chronic obstructive airway disease. Also provided are pharmaceutical compositions comprised of one or more compounds of formula (I).Type: GrantFiled: April 25, 2017Date of Patent: November 6, 2018Assignees: AbbVie S.á.r.l., Galapagos NVInventors: Robert J. Altenbach, Andrew Bogdan, Vincent Chan, Timothy A. Grieme, John R. Koenig, Philip R. Kym, Bo Liu, Karine Fabienne Malagu, Sachin V. Patel, Marc Scanio, Xenia B. Searle, Shashank Shekhar, Xueqing Wang, Ming C. Yeung
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Patent number: 10118917Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein X is O, S or NR5; or X is —C(R6)?C(R7)—, wherein the carbon atom bonded to R6 is also bonded to the carbon atom bonded to R4, and the carbon atom bonded to R7 is also bonded to the phenyl ring moiety in Formula 1; and R1, R2, R3, R4, R5, R6, R7, G and W are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling undesired vegetation comprising contacting the undesired vegetation or its environment with an effective amount of a compound or a composition of the invention.Type: GrantFiled: April 27, 2015Date of Patent: November 6, 2018Inventors: Thomas Paul Selby, Nicholas Ryan Deprez, Thomas Martin Stevenson, Andrew Edmund Taggi, John Robbins DeBergh
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Patent number: 10118918Abstract: Described herein are compounds of formula (A), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting PRMT5 activity. Methods of using the compounds for treating PRMT5-mediated disorders are also described.Type: GrantFiled: December 20, 2013Date of Patent: November 6, 2018Assignee: Epizyme, Inc.Inventors: Kenneth W. Duncan, Richard Chesworth, Paula Ann Boriack-Sjodin, Michael John Munchhof
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Patent number: 10118919Abstract: Compounds of the formula I in which R, W, R1, R4, X1, X2, X3, X4 and q have the meanings indicated in Claim 1, are inhibitors of fatty acid synthase, and can be employed, inter alia, for the treatment of diseases such as cancer, cardiovascular diseases, central nervous system injury and different forms of inflammation.Type: GrantFiled: September 6, 2017Date of Patent: November 6, 2018Assignee: Merck Patent GmbHInventors: Christos Tsaklakidis, Wolfgang Staehle, Birgitta Leuthner
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Patent number: 10118920Abstract: A compound which is a benzimidazolyl isoxazole of formula (I): wherein: R0 and R, which are the same or different, are each H or C1-6 alkyl; R9, R9 and R9, which are the same or different, are each H or F; X is -(alkn-, -alk-C(?O)—NR—, -alk-NR—C(?O)— or -alk-C(?O)—; R1 is selected from —S(?O)2R?; a 4- to 6-membered, C-linked heterocyclic group which is unsubstituted or substituted; and an N-linked spiro group of the following formula: R2 and R2?, which are the same or different, are each H or C1-6 alkyl, or R2 and R2? form, together with the C atom to which they are attached, a C3-6 cycloalkyl group; R3 and R3, which are the same or different, are each H, C1-6 alkyl, OH or F; R4 is phenyl or a 5- to 12-membered, N-containing heteroaryl group and is unsubstituted or substituted; alk is C1-6 alkylene; R? is C1-6 alkyl; and n is 0 or 1; or a pharmaceutically acceptable salt thereof. The compound has activity in modulating the activity of p300 and/or CBP and is used to treat cancer, particularly prostate cancer.Type: GrantFiled: April 20, 2016Date of Patent: November 6, 2018Assignee: CELLCENTRIC LTDInventors: Neil Anthony Pegg, David Michel Adrien Taddei, Stuart Thomas Onions, Eric Sing Yuen Tse, Richard James Brown, David Kenneth Mycock, David Cousin, Anil Patel
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Patent number: 10118921Abstract: A compound of formula I, for use in pain therapy and a pharmaceutical composition comprising said compound.Type: GrantFiled: December 17, 2015Date of Patent: November 6, 2018Assignee: PHARMNOVO ABInventors: Bengt Von Mentzer, Ingemar Starke, Peter Brandt
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Patent number: 10118922Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.Type: GrantFiled: March 7, 2014Date of Patent: November 6, 2018Assignee: JANSSEN PHARMACEUTICA NVInventors: Zhihua Sui, Chaozhong Cai, Xuqing Zhang
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Patent number: 10118923Abstract: The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.Type: GrantFiled: November 7, 2017Date of Patent: November 6, 2018Assignee: Inhibikase Therapeutics, Inc.Inventors: Milton H. Werner, Terence A. Kelly
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Patent number: 10118924Abstract: The present invention refers to novel process for the preparation of Apixaban. Further, the invention also related to a process for the preparation of intermediate of Apixaban from very basic and cheap row material i.e. Aniline which is widely commercially available. The present invention provides process for preparation of Apixaban using a different sequence of synthetic steps and does not involve use of Ullmann reaction.Type: GrantFiled: September 6, 2017Date of Patent: November 6, 2018Assignee: Unichem Laboratories LimitedInventors: Dhananjay G. Sathe, Arijit Das, Yashwant Surve, Ramdas N. Ahire
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Patent number: 10118925Abstract: Imidazo[4,5-c] ring compounds, (particularly imidzao[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridine compounds) having a substituted guanidine substituent at the 1-position, pharmaceutical compositions containing the compounds, and methods of making the compounds are disclosed. Methods of use of the compounds as immune response modifiers, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are also disclosed.Type: GrantFiled: August 26, 2016Date of Patent: November 6, 2018Assignee: 3M Innovative Properties CompanyInventor: George W. Griesgraber
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Patent number: 10118926Abstract: The present invention relates to tricyclic quinoline and quinoxaline derivatives, to a pharmaceutical composition containing such compounds, to their use as modulators, especially agonists or partial agonists, of the 5-HT2C receptor, their use for preparing a medicament for the prevention or treatment of conditions and disorders which respond to the modulation of 5-HT2C receptor, and to a method for preventing or treating conditions and disorders which respond to the modulation of 5-HT2C receptor.Type: GrantFiled: September 13, 2013Date of Patent: November 6, 2018Assignees: ABBVIE DEUTSCHLAND GMBH & CO. KG, ABBVIE INC.Inventors: Hannes Koolman, Wilfried Braje, Helmut Mack, Andreas Haupt, Ana Lucia Relo, Karla Drescher, Margaretha Henrica Maria Bakker, Viktor Lakics, Carolin Hoft, Ruxu Xu, Xiaona Zhao
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Patent number: 10118927Abstract: The disclosure relates to Substituted Piperidin-4-amino-Type Compounds of Formula (I) and pharmaceutically acceptable salts and solvates thereof wherein R1, R2, R3, Q1, Q2, E1, E2, A, B, D, W, Z, a, b, n, and x are as defined herein, compositions comprising an effective amount of a Substituted Piperidin-4-amino-Type Compound, and methods to treat or prevent a condition, such as pain, comprising administering to an animal in need thereof an effective amount of a Substituted Piperidin-4-amino-Type Compound.Type: GrantFiled: December 23, 2013Date of Patent: November 6, 2018Assignee: Purdue Pharma L.P.Inventors: Kevin Brown, Dawit Tadesse, Nobuyuki Tanaka, Naoki Tsuno, Xiaoming Zhou
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Patent number: 10118928Abstract: Methods of treating infections due to Helicobacter pylori (H. pylori), in particular in subjects having a peptic ulcer, are disclosed where the methods comprise administering inhibitors of H.Type: GrantFiled: February 6, 2015Date of Patent: November 6, 2018Assignees: Albert Einstein College of Medicine, Inc., Victoria Link LimitedInventors: Vern L. Schramm, Keith Clinch, Shivali Ashwin Gulab
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Patent number: 10118929Abstract: The present disclosure relates to fluorinated compounds of formula I and methods of synthesizing these compounds. The present disclosure also relates to pharmaceutical compositions containing the fluorinated compounds of the disclosure, and methods of treating fibrosis, macular degeneration, diabetic retinopathy (DR), macular edema, diabetic macular edema (DME), and macular edema following retinal vein occlusion (RVO), by administering these compounds and pharmaceutical compositions to subjects in need thereof.Type: GrantFiled: April 27, 2017Date of Patent: November 6, 2018Assignee: SciFluor Life Sciences, Inc.Inventors: Takeru Furuya, Ben C. Askew
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Patent number: 10118930Abstract: The present application relates to novel substituted piperidinylpyrazolopyrimidinones, to processes for their preparation, the compounds for use alone or in combinations in a method for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of acute and recurrent bleeding in patients with or without underlying hereditary or acquired hemostatic disorders, wherein the bleeding is associated with a disease or medical intervention selected from the group consisting of heavy menstrual bleeding, postpartum hemorrhage, hemorrhagic shock, hemorrhagic cystitis, gastrointestinal hemorrhage, trauma, surgery, transplantation, stroke, liver diseases, hereditary angioedema, nosebleed, and synovitis and cartilage damage following hemarthrosis.Type: GrantFiled: October 30, 2015Date of Patent: November 6, 2018Assignee: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Manuel Ellermann, Gaelle Valot, Yolanda Cancho Grande, Jorma Haßfeld, Tom Kinzel, Johannes Köbberling, Kristin Beyer, Susanne Röhrig, Michael Sperzel, Jan Stampfuß, Imke Meyer, Maria Köllnberger, Nils Burkhardt, Karl-Heinz Schlemmer, Christian Stegmann, Joachim Schuhmacher, Matthias Werner, Jörg Heiermann, Willem Jan Hengeveld
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Patent number: 10118931Abstract: Provided herein are compounds of Formula (I): and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula: wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.Type: GrantFiled: December 8, 2017Date of Patent: November 6, 2018Assignee: Epizyme, Inc.Inventors: Richard Chesworth, Oscar Miguel Moradei, Gideon Shapiro, Lei Jin, Robert E. Babine
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Patent number: 10118932Abstract: The present invention provides solid state forms of certain spiro-oxindole compounds, such as funapide and the racemic mixture of funapide and its corresponding (R) enantiomer, pharmaceutical compositions comprising the solid state forms and processes for preparing the solid state forms and the pharmaceutical compositions.Type: GrantFiled: June 16, 2017Date of Patent: November 6, 2018Assignee: Xenon Pharmaceuticals Inc.Inventors: Ronen Ben-David, Stephen Bierlmaier, Ralph Curtis Haltiwanger, Alexandr Jegorov, Raeann Ruiyun Wu, Mehran Yazdanian
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Patent number: 10118933Abstract: The present disclosure relates to compounds of formula (I), and pharmaceutically acceptable salts thereof. The present disclosure also relates to compositions and methods of treating comprising compounds of formula (I), and pharmaceutically acceptable salts thereof.Type: GrantFiled: April 13, 2017Date of Patent: November 6, 2018Assignee: ORION CORPORATIONInventors: Gerd Wohlfahrt, Olli Törmäkangas, Harri Salo, Iisa Höglund, Arja Karjalainen, Pia Koivikko, Patrik Holm, Sirpa Rasku, Anniina Vesalainen
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Patent number: 10118934Abstract: Compounds and salts thereof which inhibit microbial growth or attenuate the virulence of pathogenic microorganisms and which inhibit UDP-galactopyranose mutase (UGM). Compounds of the invention include triazolothiadiazines, particularly 3, 6, 7-substituted-7H-[1,2,4]triazolo[3,4-b][1,3,4]thiadiazines, and 4-(1H-pyrrol-3-yl) thiazoles, particularly 4-(1,2,5-substituted-1H-pyrrol-3-yl)-2-substituted thiazoles, and salts thereof. Methods for inhibiting growth or attenuating virulence of microbial pathogens including mycobacterium, for example, M. tuberculosis and M. smegmatis and Klebsiella, for example, Klebsiella pneumoniae. Methods for inhibiting eukaryotic human and animal pathogens, and fungi and nematodes in particular. Methods for treatment of infections by prokaryotic and eukaryotic pathogens employing compounds of the invention.Type: GrantFiled: June 14, 2017Date of Patent: November 6, 2018Assignee: Wisconsin Alumni Research FoundationInventors: Laura L. Kiessling, Virginia A. Kincaid, Nir London, Brian K. Shoichet