Patents Issued in January 22, 2019
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Patent number: 10183903Abstract: The present invention discloses a method for preparing 2,3,3,3-tetrafluoropropene using methylmagnesium chloride, comprising the following steps: 1) preparing 1,1,2-trifluoropropene (CH3CF?CF2); 2) preparing 1,1,1,2,2-pentafluoropane (CF3CF2CH3); 3) preparing 2,3,3,3-tetrafluoropropene (CF3CF?CH2). In the present invention, using a Grignard reagent, namely methylmagnesium chloride, and tetrafluoroethylene as starting raw materials, 2,3,3,3-tetrafluoropropene is prepared by three steps of nucleophilic addition-elimination, fluorine addition, and dehydrofluorination in sequence. The process flow is relatively short, and the product yield is high.Type: GrantFiled: December 24, 2015Date of Patent: January 22, 2019Assignee: JUHUA GROUP TECHNOLOGY CENTERInventors: Hongfeng Li, Shuhua Wang, Xiaobo Xu, Liyong Ma
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Patent number: 10183904Abstract: A method of making 1,5-pentanediol from tetrahydrofurfural alcohol. The method includes the steps of dehydrating tetrahydrofurfural alcohol (THFA) to dihydropyran (DHP); hydrating at least a portion of the DHP to 2-hydroxy-tetrahydropyran (2-HY-THP) in the absence of homogeneous acid; and hydrogenating at least a portion of the 2-HY-THP to 1,5-pentanediol. The method can be conducted entirely in the absence of noble metal catalysts.Type: GrantFiled: January 22, 2016Date of Patent: January 22, 2019Assignee: Wisconsin Alumni Research FoundationInventors: George Willis Huber, James A. Dumesic, Kevin J. Barnett, Zach J. Brentzel
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Patent number: 10183905Abstract: A method produces acetic acid and includes a reaction step, a first purification step, a second purification step, and a third purification step. In the reaction step, a material mixture including methanol, carbon monoxide, a catalyst, and an iodide is subjected to a methanol carbonylation reaction in a reactor (1) to form acetic acid. In the first purification step, a crude acetic acid stream including acetic acid formed in the reaction step is subjected to distillation in a distillation column (3) to give a first acetic acid stream enriched with acetic acid. In the second purification step, the first acetic acid stream is subjected to distillation in a distillation column (5) to give a second acetic acid stream further enriched with acetic acid. In the third purification step, an acetic acid stream is subjected to purification in an additional purification unit (e.g.Type: GrantFiled: September 20, 2016Date of Patent: January 22, 2019Assignee: DAICEL CORPORATIONInventors: Masahiko Shimizu, Nobuyuki Hirabayashi, Yoshihisa Mizutani
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Patent number: 10183906Abstract: Process for the hydrolysis of a methyl acetate with at least one of water and methanol in the presence of at least one Brønsted acid catalyst to produce acetic acid. The process employs a methyl acetate feed in which the total amount of acetaldehyde and 1,1 dimethoxyethane impurities is maintained at 100 pm wt or less calculated as mass equivalents of acetaldehyde.Type: GrantFiled: June 12, 2015Date of Patent: January 22, 2019Assignee: BP CHEMICALS LIMITEDInventors: Berian John Daniel, John Glenn Sunley, Russell Alan Taylor, Gareth Gerald Armitage
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Patent number: 10183907Abstract: A process for the synthesis of acrylic acid oligomer represented by formula (I): in which n is an integer ranging from 1 to 10, wherein the process comprises the step of heating acrylic acid at a temperature from 50° C. to 200° C. in the presence of a catalyst, water and at least one polymerization inhibitor. Formula (I) where n=0 is acrylic acid, the precursor for preparing the acrylic acid oligomer.Type: GrantFiled: September 7, 2016Date of Patent: January 22, 2019Assignee: Arkema FranceInventors: Reinhard Linemann, Benoit Riflade, Serge Tretjak, Andre Levray, Patrice Defer
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Patent number: 10183908Abstract: The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of kidney and/or liver disease.Type: GrantFiled: March 18, 2016Date of Patent: January 22, 2019Assignee: VECTUS BIOSYSTEMS LIMITEDInventor: Karen Annette Duggan
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Patent number: 10183909Abstract: A process is provided for preparation of (R)-N-Boc biphenyl alaninol. It provides a preparation process for a compound outlined as compound 4, which includes these operations: in one of the alcohol solvents, asymmetric hydrogenation of 5 in the presence of [Rh(Duanphos)(X)]Y and hydrogen to provide compound 4. Here “Duanphos” is (Rc,Sp)-Duanphos or (Sc,Rp)-Duanphos; X is NBD or/and COD; Y is one or more of BF4, PF6, SbF6. This process has a lot of advantages, such as low cost, safe operation, less pollution and high yield. The product was obtained in >99% purity and ee which is suitable to scale up in industrial scale.Type: GrantFiled: September 9, 2016Date of Patent: January 22, 2019Assignees: CHIRAL QUEST (SUZHOU) CO., LTD., JIANGXI LONG LIFE BIO-PHARMACEUTICAL CO., LTD.Inventors: Shengwen Wu, Wenge Li, Lei Wu, Li Zou, Siming Hu, Tengyue Xu, Hongfeng Liu, Yi Tao, Yongxiang Chi
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Patent number: 10183910Abstract: A process for producing ammonia and a derivative of ammonia from a natural gas feed comprising conversion of natural gas into a make-up synthesis gas; synthesis of ammonia; use of said ammonia to produce said derivative of ammonia, wherein a portion of the natural gas feed is used to fuel a gas turbine; power produced by said gas turbine is transferred to at least one power user of the process, such as a compressor; heat is recovered from exhaust gas of said gas turbine, and at least part of said heat is recovered as low-grade heat available at a temperature not greater than 200° C., to provide process heating to at least one thermal user of the process, such as CO2 removal unit or absorption chiller; a corresponding plant and method of modernization are also disclosed.Type: GrantFiled: June 3, 2015Date of Patent: January 22, 2019Assignee: Casale SAInventors: Raffaele Ostuni, Geoffrey Frederick Skinner
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Patent number: 10183911Abstract: A process for the preparation of a polyunsaturated thiol comprising: (1) reacting a polyunsaturated alcohol in the presence of a compound of formula R2—SO2Hal wherein R2 is a C1-20 hydrocarbyl group, such an C1-10 alkyl group, to form a polyunsaturated sulphonyl ester; (2) converting the polyunsaturated sulphonyl ester to a polyunsaturated thioester by reacting with an anion of formula ?SC(?O)R4 wherein R4 is a C1-20 hydrocarbyl group; (3) converting the polyunsaturated thioester to form a polyunsaturated thiol optionally in the presence of an antioxidant, e.g. using a metal carbonate. (4) reacting said polyunsaturated thiol with a compound (LG)R3COX wherein X is an electron withdrawing group and R3 is an alkylene group carrying a leaving group (LG), such as LG-CH2— forming where X is an electron withdrawing group and LG is a leaving group; optionally in the presence of an antioxidant, so as to form a polyunsaturated ketone compound.Type: GrantFiled: January 25, 2016Date of Patent: January 22, 2019Assignee: Avexxin ASInventors: Marcel Sanderberg, Inger-Reidun Aukrust
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Patent number: 10183912Abstract: The present invention provides for novel acridine-like class of compounds that have demonstrated efficiency in treating cancer. The compounds of the present invention have demonstrated efficacy in binding to and antagonizing the activity of the p53 repressor, HDMX. Once administered to a cell, the compounds of the present invention bind HDMX, thereby allowing p53 to induce apoptosis of the cancerous cell. A combination of this class of compounds along with Nutlin3 provides a novel approach to treat cancers.Type: GrantFiled: March 31, 2015Date of Patent: January 22, 2019Assignee: MIRX PHARMACEUTICALS, LLCInventors: David Wald, Mukesh Agarwal, Zhiqing Xia, Goutam Karan, Mahesh Gundluru
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Patent number: 10183913Abstract: The present invention relates to a novel serotonin reuptake inhibitor which also exhibits 5-HT2C antagonistic action (antidepressive and anxiolytic effects), in particular, 5-HT2C inverse agonistic action comprising Compound (1): or a pharmaceutically acceptable salt thereof wherein R1, R2, R3 and R4 are independently hydrogen or C1-6 alkyl etc.; R5 is C4-7 alkyl or —(CR8R9)r-E; R6, R7, R8 and R9 are independently hydrogen, fluorine or C1-6 alkyl; A is C6-10 aryl or heteroaryl etc.; r is 1, 2, 3 or 4; E is C3-8 cycloalkyl or C6-10 aryl etc.; L is oxygen, sulfur or —NR10—; n is 1, 2 or 3; R10 is hydrogen or C1-6 alkyl etc.; and X is hydrogen or halogen etc.Type: GrantFiled: May 25, 2018Date of Patent: January 22, 2019Assignee: SUMITOMO DAINIPPON PHARMA CO., LTD.Inventors: Izumi Sasaki, Tomohiro Toyoda, Hidefumi Yoshinaga, Itaru Natsutani, Yoko Takahashi
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Patent number: 10183914Abstract: What are described are compounds of the general formula (I) and agrochemically acceptable salts thereof and the use thereof in the crop protection sector.Type: GrantFiled: June 29, 2015Date of Patent: January 22, 2019Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Klemens Minn, Hansjoerg Dietrich, Elmar Gatzweiler, Christopher Hugh Rosinger, Dirk Schmutzler, Estella Buscató Arsequell
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Patent number: 10183915Abstract: Disclosed are two axially chiral isomers and pharmaceutically available salts thereof, preparation method therefor, and pharmaceutical use of the two axially chiral isomers or pharmaceutical compositions thereof.Type: GrantFiled: April 1, 2016Date of Patent: January 22, 2019Assignee: MEDSHINE DISCOVERY INC.Inventors: Jianfei Wang, Jing Zhang, Long Zhang, Yang Zhang, Jian Li, Shuhui Chen
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Patent number: 10183916Abstract: The invention relates to an improved process for the manufacture of bis-resorcinyl triazines of formula (I) wherein R1 is a C1C18alkyl group or C2-C18alkenyl group as well as the respective alkyl substituted bis-resorcinyl derivatives of formula (II) wherein R1 is a C1-C18alkyl group or C2-C18alkenyl group and R2 and R3 are independently of each other a C1-C18alkyl group or a C2-C18alkenyl group.Type: GrantFiled: May 12, 2016Date of Patent: January 22, 2019Assignee: DSM IP ASSETS B.V.Inventors: Nadine Greiner, Sandro Schmid, René Tobias Stemmler
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Patent number: 10183917Abstract: The present invention relates to novel tricyclic compounds which can bind to FXR and act as modulators of the FXR, or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and the uses of the compounds for the treatment of diseases and/or conditions mediated by FXR. The invention further provides a pharmaceutical composition containing the compound disclosed herein and a method of treatment of diseases and/or conditions mediated by FXR comprising administering the compound or the pharmaceutical composition.Type: GrantFiled: February 5, 2016Date of Patent: January 22, 2019Assignee: SUNSHINE LAKE PHARMA CO., LTD.Inventors: Xiaojun Wang, Xinye Yang, Shengqiang Pan, Rui Guo, Junwen Wu, Yingjun Zhang, Changchung Cheng
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Patent number: 10183918Abstract: The present invention relates to oxa-azaspiro compounds having pharmacological activity towards the sigma (?) receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use in therapy, in particular for the treatment of pain.Type: GrantFiled: October 21, 2016Date of Patent: January 22, 2019Assignee: LABORATORIOS DEL DR. ESTEVE S.A.Inventors: Carmen Almansa-Rosales, Carlos Alegret-Molina
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Patent number: 10183919Abstract: The present invention provides a compound having the structure: or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: March 12, 2015Date of Patent: January 22, 2019Assignee: THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Andrew C. Kruegel, Adam Henke, Madalee M. Gassaway, Marie-Laure Rives, Jonathan A. Javitch, Dalibor Sames
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Patent number: 10183920Abstract: The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methylthio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat).Type: GrantFiled: October 23, 2015Date of Patent: January 22, 2019Assignee: Elobix ABInventors: Ingvar Ymén, Martin Bohlin, Thomas Larsson, Helena Nicklasson
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Patent number: 10183921Abstract: The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described.Type: GrantFiled: April 17, 2014Date of Patent: January 22, 2019Assignee: QBiotics LimitedInventors: Paul Warren Reddell, Victoria Anne Gordon, Ryan Moseley, Robert Steadman, Rachael Louise Moses, Glen Mathew Boyle, Peter Gordon Parsons
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Patent number: 10183922Abstract: The present invention relates to epoxy-tigliane compounds and their use in promoting wound healing. In particular embodiments, the epoxy-tigliane compounds are epoxy-tigliaen-3-one compounds. Methods of inducing or promoting wound healing as well as methods of reducing scarring and improving cosmetic outcomes upon healing of a wound are described. Compounds and compositions for use in wound healing are also described.Type: GrantFiled: February 6, 2017Date of Patent: January 22, 2019Assignee: QBiotics LimitedInventors: Paul Warren Reddell, Victoria Anne Gordon, Ryan Moseley, Robert Steadman, Rachael Louise Moses, Glen Mathew Boyle, Peter Gordon Parsons
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Patent number: 10183923Abstract: This disclosure provides a method for preparing a precursor of a single dairy-lactone isomer, methods of preparing a single dairy-lactone isomer, and to the organoleptic uses thereof.Type: GrantFiled: April 8, 2016Date of Patent: January 22, 2019Assignees: INSTITUT DES SCIENCES ET INDUSTRIES DU VIVANT ET DE L'ENVIRONNEMENT—AGROPARIS TECH, UNIVERSITY OF NEW ENGLAND, CIRCA GROUP PTY LTDInventors: Florent Allais, Amandine Flourat, Aurélien Peru, Ben Greatrex, Warwick Raverty, Anthony Duncan
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Patent number: 10183924Abstract: The present disclosure provides a composition. In an embodiment, a composition is provided and includes an ethylene/?-olefin/diene terpolymer and a polar component. The composition also includes a sulfonamide phthalic anhydride linkage (SPA) bonding the ethylene/?-olefin/diene terpolymer to the polar component.Type: GrantFiled: December 19, 2016Date of Patent: January 22, 2019Assignee: Dow Global Technologies LLCInventors: Jerzy Klosin, Adriana I. Moncada, Brian W. Walther, Michael D. Read
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Patent number: 10183925Abstract: The present invention provides compounds represented by formula (1A), or pharmaceutically acceptable salts. Compounds represented by formula (1A), or pharmaceutically acceptable salts thereof, wherein A1 and A2 are identical or different, and each independently —C(?O) B, —C(?O)CR3AR3BB, —CO2B, —C(?S)OB, —CONR3CB, —C(?S)NR3CB, a hydrogen atom, or the like, wherein A1 and A2 are not both hydrogen atoms, wherein B is an optionally substituted 3- to 12-membered monocyclic or polycyclic heterocyclic group, an optionally substituted 3- to 12-membered cyclic amino group, or a group represented by the following formula (B), wherein the 3- to 12-membered monocyclic or polycyclic heterocyclic group and the 3- to 12-membered cyclic amino group have at least one or more secondary nitrogen atoms in the ring; R1 is a hydrogen atom or the like; R2A, R2B, R2C, and R2D are identical or different, and each independently a hydrogen atom or the like; and R8 is alkyl. wherein * denotes a bonding position.Type: GrantFiled: March 25, 2016Date of Patent: January 22, 2019Assignees: BOSTON BIOMEDICAL, INC., SUMITOMO DAINIPPON PHARMA CO., LTD.Inventors: Hitoshi Ban, Seiji Kamioka, Yusuke Sawayama, Chiang Jia Li
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Patent number: 10183926Abstract: The present invention relates to a pseudo-ceramide compound and a method for preparing the same. The pseudo-ceramide compound of the present invention may provide antioxidant effects, and exhibits improved properties such as high solubility compared to existing natural ceramides and pseudo-ceramide compounds, and therefore, may be included in large quantities in the formulation. Accordingly, the pseudo-ceramide compound may be used in various fields such as cosmetics, medicinal substances, external preparations and foods.Type: GrantFiled: December 15, 2016Date of Patent: January 22, 2019Assignee: AMOREPACIFIC CORPORATIONInventors: Yung Hyup Joo, Jae Won Yoo, Yong Jin Kim, Ho Sik Rho, John Hwan Lee
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Patent number: 10183927Abstract: The present invention provides crystalline forms of a compound of formula (I): Also provided are pharmaceutical compositions that include the provided crystalline forms and methods of using the provided crystalline forms and pharmaceutical compositions for the treatment of cancer.Type: GrantFiled: May 17, 2017Date of Patent: January 22, 2019Assignees: Biomed Valley Discoveries, Inc., Vertex Pharmaceuticals IncorporatedInventors: Gary DeCrescenzo, Dean Welsch, Petinka I. Vlahova, Stephan X. M. Boerrigter, Alexander Aronov, Ali Keshavarz-Shokri, Alexander N. Scangas, Kathy Stavropoulos, Benjamin Littler, Irina Nikolaevna Kadiyala, Rossitza Gueorguieva Alargova
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Patent number: 10183928Abstract: Described herein are compounds that inhibit wild-type RET and its resistant mutants, pharmaceutical compositions including such compounds, and methods of using such compounds and compositions.Type: GrantFiled: March 17, 2017Date of Patent: January 22, 2019Assignee: BLUEPRINT MEDICINES CORPORATIONInventors: Joseph L. Kim, Kevin J. Wilson, Jason D. Brubaker
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3-(benzoimidazol-2-yl)-indazole inhibitors of the Wnt signaling pathway and therapeutic uses thereof
Patent number: 10183929Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease 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: February 6, 2018Date of Patent: January 22, 2019Assignee: Samumed, LLCInventors: Sunil Kumar K C, John Hood -
Patent number: 10183930Abstract: The present invention relates to crystalline forms of (1aS,5aS)-2-(4-oxy-pyrazin-2-yl)-1a,2,5,5a-tetrahydro-1H-2,3-diaza-cyclopropa[a]pentalene-4-carboxylic acid ((S)-1-hydroxymethyl-2,2-dimethyl-propyl)-amide (Compound 1) and pharmaceutical compositions thereof that modulate the activity of the cannabinoid CB2 receptor and are therefore useful in the treatment of CB2 receptor-mediated disorders, for example, osteoarthritis; pain; hyperalgesia; allodynia; inflammatory hyperalgesia; neuropathic hyperalgesia; acute nociception; osteoporosis; multiple sclerosis-associated spasticity; autoimmune disorders; allergic reactions; CNS inflammation for example; atherosclerosis; undesired immune cell activity, and inflammation associated with a disorder selected from: osteoarthritis, anaphylaxis, Behcet's disease, graft rejection, vasculitis, gout, spondylitis, viral disease, bacterial disease, lupus, inflammatory bowel disease, autoimmune hepatitis, and type 1 diabetes mellitus; age-related macular degeneration; cough;Type: GrantFiled: August 26, 2016Date of Patent: January 22, 2019Assignee: Arena Pharmaceuticals, Inc.Inventors: Anthony C. Blackburn, Sangdon Han, Robert M. Jones, Antonio Garrido Montalban, Biman B. Pal, Jaimie Karyn Rueter
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Patent number: 10183931Abstract: The invention relates to inhibitors of ROCK1 and/or ROCK2. Also provided are methods of treating diseases and disorders involving inhibiting ROCK1 and/or ROCK2.Type: GrantFiled: November 10, 2017Date of Patent: January 22, 2019Assignee: Kadmon Corporation, LLCInventors: Masha Poyurovsky, Ji-In Kim, Kevin Liu, Alexandra Zanin-Zhorov
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Patent number: 10183932Abstract: The invention relates to substituted oxopyridine derivatives and to processes for their preparation, and also to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular disorders, preferably thrombotic or thromboembolic disorders, and oedemas, and also ophthalmic disorders.Type: GrantFiled: October 17, 2017Date of Patent: January 22, 2019Assignee: Bayer Pharma AktiengesellschaftInventors: Susanne Röhrig, Alexander Hillisch, Julia Strassburger, Stefan Heitmeier, Martina Victoria Schmidt, Karl-Heinz Schlemmer, Adrian Tersteegen, Anja Buchmüller, Christoph Gerdes, Martina Schäfer, Tom Kinzel, Henrik Teller, Hartmut Schirok, Jürgen Klar, Eloisa Jimenez Nunez
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Patent number: 10183933Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.Type: GrantFiled: May 23, 2017Date of Patent: January 22, 2019Assignee: Vertex Pharmaceuticals IncorporatedInventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
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Patent number: 10183934Abstract: The present invention relates to inhibitors of zinc-dependent histone deacetylases (HDACs) useful in the treatment of diseases or disorders associated with HDAC6, having a Formulae I or Formula II: where R, L, X1, X2, X3, X4, X5, Y1, Y2, Y3, and Y4 are described herein.Type: GrantFiled: February 2, 2016Date of Patent: January 22, 2019Assignee: Forma Therapeutics, Inc.Inventors: Xiaozhang Zheng, Pui Yee Ng, Aleksandra Rudnitskaya, David R. Lancia, Jr.
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Patent number: 10183935Abstract: Novel benzamide derivatives of formula (I) wherein W1, W2, R1 to R10 and X have the meaning according to the claims, are positive allosteric modulators of the FSH receptor, and can be employed, inter alia, for the treatment of fertility disorders.Type: GrantFiled: April 26, 2017Date of Patent: January 22, 2019Assignee: Merck Patent GmbHInventors: Henry Yu, Thomas E. Richardson, Pandi Bharathi, Brian H. Heasley, Matthew G. Jenks, Robert J. Foglesong
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Patent number: 10183936Abstract: 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: March 13, 2015Date of Patent: January 22, 2019Assignees: Indiana University Research and Technology Corporation, Assembly Biosciences, Inc.Inventors: William W. Turner, Jr., Lee Daniel Arnold, Hans Maag, Adam Zlotnick
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Patent number: 10183937Abstract: The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.Type: GrantFiled: November 21, 2017Date of Patent: January 22, 2019Assignee: Bayer AktiengesellschaftInventors: Adam James Davenport, Nico Bräuer, Oliver Martin Fischer, Andrea Rotgeri, Antje Rottmann, Ioana Neagoe, Jens Nagel, Anne-Marie Godinho-Coelho, Jürgen Klar
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Patent number: 10183938Abstract: The present invention relates to novel geminal substituted quinuclidine amide compounds, and pharmaceutical compositions of the same, that are suitable as agonists or partial agonists of ?7-nAChR, and methods of preparing these compounds and compositions, and the use of these compounds and compositions in methods of maintaining, treating and/or improving cognitive function. In particular, methods of administering the compound or composition to a patient in need thereof, for example a patient with a cognitive deficiency and/or a desire to enhance cognitive function, that may derive a benefit therefrom.Type: GrantFiled: December 14, 2015Date of Patent: January 22, 2019Assignee: Axovant Sciences GmbHInventors: Raksha Acharya, Duane A. Burnett, Matthew Gregory Bursavich, Andrew Simon Cook, Bryce Alden Harrison, Gerhard Koenig, Andrew J. Mcriner
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Patent number: 10183939Abstract: This invention relates to novel compounds. The compounds of the invention are kinase inhibitors. Specifically, the compounds of the invention are useful as inhibitors of Raf kinases, e.g., B-Raf and C-Raf. The invention also contemplates the use of the compounds for treating conditions treatable by the inhibition of Raf kinases, for example, cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia.Type: GrantFiled: September 11, 2015Date of Patent: January 22, 2019Assignee: Redx Pharma PLCInventors: Matilda Bingham, Richard Testar, Camille Gignoux
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Patent number: 10183940Abstract: The invention relates to aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amide derivatives of general formula (1), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates processes for manufacture of the compounds according to the invention.Type: GrantFiled: November 12, 2015Date of Patent: January 22, 2019Assignee: Boehringer Ingelheim International GmbHInventors: Rocco Mazzaferro, Marco Ferrara, Riccardo Giovannini, Iain Lingard
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Patent number: 10183941Abstract: The present invention discloses a pyrimidine or pyridopyridone compound as shown in formula (I) and an application thereof relating to the technical field of medicament preparation. The compound can selectively suppress cyclin-dependent kinases (Cdks) CDK4 and CDK6 with almost no suppression of the activity of the kinase CDK2. Thus, the compound can be used for various diseases caused by cell cycle control disorders involving CDK4 and CDK6, and particularly in the treatment of malignant tumors.Type: GrantFiled: May 31, 2016Date of Patent: January 22, 2019Assignee: GUANGZHOU BEBETTER MEDICINE TECHNOLOGY CO., LTD.Inventors: Xiong Cai, Changgeng Qian, Junqi Li, Yuanhui Qing, Yanyan Wang, Weicai Xue, Huajin You
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Patent number: 10183942Abstract: The invention provides compounds of formula (I): wherein X is and 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: July 18, 2018Date of Patent: January 22, 2019Assignee: THERAVANCE BIOPHARMA R&D IP, LLCInventors: Noah Benjamin, Marta Dabros, Venkat R. Thalladi
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Patent number: 10183943Abstract: The present invention relates to heterocyclic compounds, their process of preparation, pharmaceutical compositions comprising these compounds and use thereof, optionally in combination with other antibacterial agents and/or beta-lactam compounds, for the prevention or treatment of bacterial infections. The present invention also relates to the use of these compounds as ?-lactamase inhibitors and/or as antibacterial agents.Type: GrantFiled: May 6, 2016Date of Patent: January 22, 2019Assignee: MUTABILISInventors: Julien Barbion, Audrey Caravano, Sophie Chasset, Francis Chevreuil, Nicolas Lecointe, Benoît Ledoussal, Frédéric Le Strat, Sébastien Richard, Christophe Simon, Sophie Vomscheid, Julie Brias, Sophie Briet, Fabien Faivre, Géraldine Le Fralliec, Chrystelle Oliveira
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Patent number: 10183944Abstract: The present application provides novel pyrimido-pyridazinone compounds and methods for preparing and using these compounds. These compounds are useful in treating inflammation in patients by administering one or more of the compounds to a patient. In one embodiment, the novel pyrimido-pyridazinone compound is of Formula (I) and R1 and R2 are defined herein.Type: GrantFiled: April 25, 2016Date of Patent: January 22, 2019Assignee: Asana BioSciences, LLCInventors: Aranapakam Venkatesan, Roger Astbury Smith, Hosahalli Subramanya, Vijay Potluri, Sunil Kumar Panigrahi, Vishnu Basetti, Karunasree Kunta
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Patent number: 10183945Abstract: Disclosed herein are methods for obtaining aza-pyridone compounds, which can be useful for ameliorating and/or treating a disease and/or a condition, including an orthomyxovirus infection.Type: GrantFiled: March 10, 2017Date of Patent: January 22, 2019Assignee: ALIOS BIOPHARMA, INC.Inventors: Michael Hunter Welch, Leonid Beigelman, Robert Than Hendricks, Andras Horvath, Gareth Brown, Prasad Ganji, Stefan Mix
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Patent number: 10183946Abstract: The invention relates to a compound of formula (I) wherein R1 to R4 and n are defined as in the description and in the claims. The compound of formula (I) can be for treating.Type: GrantFiled: April 4, 2017Date of Patent: January 22, 2019Assignee: HOFFMANN-LA ROCHE INC.Inventors: Uwe Grether, Matthias Nettekoven, Mark Rogers-Evans, Sebastien Schmitt, Benjamin James Stenton
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Patent number: 10183947Abstract: The present application relates to novel compounds of formula (I) to their utility in treating and/or preventing clinical conditions including cardiovascular diseases (CVD), to methods for their therapeutic use, to pharmaceutical compositions containing them and to processes for preparing such compounds.Type: GrantFiled: May 3, 2016Date of Patent: January 22, 2019Assignee: ASTRAZENECA ABInventors: Johan Olof Broddefalk, Hans Fredrik Emtenäs, Kenneth Lars Granberg, Malin Anita Lemurell, Daniel Tor Pettersen, Alleyn Thomas Plowright, Lars Johan Andreas Ulander
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Patent number: 10183948Abstract: A method for treating and/or preventing polycystic ovary syndrome (PCOS) including the administration, to a patient in need thereof, of a pharmaceutically effective amount of a compound of Formula I or a pharmaceutically acceptable solvate thereof.Type: GrantFiled: October 27, 2017Date of Patent: January 22, 2019Assignee: OGEDA SAInventors: Hamid Hoveyda, Guillaume Dutheuil, Graeme Fraser
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Patent number: 10183949Abstract: A compound according to any one of formula (Ia) to (Ic), or its pharmaceutically acceptable salt: wherein R1, R2, R3, R4a, R4c, R5 are as defined in the description.Type: GrantFiled: February 24, 2017Date of Patent: January 22, 2019Assignees: THE UNIVERSITY OF TOKYO, TOHOKU UNIVERSITY, SHIONOGI & CO., LTD.Inventors: Tetsuo Nagano, Takayoshi Okabe, Hirotatsu Kojima, Mitsuyasu Kawaguchi, Osamu Nureki, Ryuichiro Ishitani, Hiroshi Nishimasu, Junken Aoki, Nobuyuki Tanaka, Yasuhiko Kanda, Yoshiyuki Kioi, Yusuke Tateno, Shiro Kida, Junji Yamane
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Patent number: 10183950Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R1, R2, R3, R4, R5, R6, A, G, M, Q and X are as defined herein. A compound of formula (I) and its salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.Type: GrantFiled: January 26, 2017Date of Patent: January 22, 2019Assignee: Cancer Research Technology LimitedInventors: Bruce D. Dorsey, Keith S. Learn, Emma L. Morris, Gregory R. Ott, Jonathan R. A. Roffey, Christelle N. Soudy, Jason C. Wagner
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Patent number: 10183951Abstract: The present invention provides solid forms of compounds useful as inhibitors of Acetyl CoA Carboxylase (ACC), compositions thereof, methods of producing the same, and methods of using the same in the treatment of ACC-mediated diseases.Type: GrantFiled: March 1, 2017Date of Patent: January 22, 2019Assignee: Gilead Apollo, LLCInventors: John C. Amedio, Jr., Sijun Hu, Henry Morrison
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Patent number: 10183952Abstract: The present application relates to thienopyrrole derivatives, compounds of Formulas (I) and (Ia), wherein R, R1, R2 and R3 are as defined in the specification, pharmaceutical compositions containing such compounds and to their use in therapy. The compounds of the application can be useful for inhibiting KDM1 and the prevention and/or treatment of cancer, infectious disease, or a disease characterized by aberration of cellular energy metabolism, e.g., obesity.Type: GrantFiled: September 4, 2015Date of Patent: January 22, 2019Assignee: Istituto Europeo di Oncologia S.r.l.Inventors: Paola Vianello, Luca Sartori, Mario Varasi, Ciro Mercurio, Elisa Zagarri, Anna Cappa, Alessia Romussi, Manuela Villa, Giuseppe Meroni, Loris Moretti