Patents Issued in January 30, 2018
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Patent number: 9878964Abstract: A process for producing olefins from oxygenates comprises the following steps: (i) heterogeneously catalyzed conversion of at least one oxygenate to an entire stream containing propylene, aromatics and cyclic olefins; (ii) olefin interconversion of at least a part of the entire stream; (iii) separation of a stream rich in aromatics from the reaction product of the olefin interconversion; and (iv) hydrogenation of the stream rich in aromatics.Type: GrantFiled: February 4, 2014Date of Patent: January 30, 2018Assignee: L'AIR LIQUIDE SOCIÉTÉ ANONYME POUR L'ÉTUDE ET L'EXPLOITATION DES PROCEDES GEORGES CLAUDEInventors: Martin Rothaemel, Roberta Olindo, Stephane Haag, Thomas Renner, Frank Castillo-Welter
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Patent number: 9878965Abstract: The present invention relates to a gas-phase process for the preparation of butadiene comprising (i) providing a gas stream G-1 comprising ethanol; (ii) contacting the gas stream G-1 comprising ethanol with a catalyst, thereby obtaining a gas stream G-2 comprising butadiene, wherein the catalyst comprises a zeolitic material having a framework structure comprising YO2, Y standing for one or more tetravalent elements, wherein at least a portion of Y comprised in the framework structure is isomorphously substituted by one or more elements X, as well as to a zeolitic material having a framework structure comprising YO2, Y standing for one or more tetravalent elements, wherein at least a portion of Y comprised in the framework structure is isomorphously substituted by one or more elements X, wherein the zeolitic material displays a specific X-ray powder diffraction pattern, and to its use.Type: GrantFiled: June 13, 2014Date of Patent: January 30, 2018Assignee: BASF SEInventors: Kirsten Spannhoff, Andrei-Nicolae Parvulescu, Armin Lange de Oliveira, Stefan Marx, Mathias Feyen, Ulrich Müller, Ekkehard Schwab
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Patent number: 9878966Abstract: The present invention provides methods, reactor systems, and catalysts for increasing the yield of aromatic hydrocarbons produced while converting alkanols to hydrocarbons. The invention includes methods of using catalysts to increase the yield of benzene, toluene, and mixed xylenes in the hydrocarbon product.Type: GrantFiled: January 2, 2015Date of Patent: January 30, 2018Assignee: Virent, Inc.Inventors: Paul G. Blommel, Li Yuan, Matthew Van Straten, Warren Lyman, Randy D. Cortright
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Patent number: 9878967Abstract: The present invention relates to a method of converting levulinic acid or a derivative thereof to hydrocarbons and hydrogen by providing a source of levulinic acid or a derivative thereof and converting the levulinic acid or a derivative thereof in the source to hydrocarbons and hydrogen, where converting is carried out in a single reactor. The present invention also relates to methods for producing hydrocarbons and hydrogen.Type: GrantFiled: December 22, 2016Date of Patent: January 30, 2018Assignee: Iowa State University Research Foundation, Inc.Inventors: Wenyu Huang, Chaoxian Xiao
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Patent number: 9878968Abstract: A process is described for separating paraxylene from a multicomponent fluid mixture of C8 aromatics. A mixture of C8 aromatics is fed to a simulated moving bed adsorptive apparatus having at least two sieve chambers and at least two rotary valves. Each sieve chamber may be operated individually using the PowerFeed process. The flow rates of the streams to or from the individual sieve chambers may be varied during the step time in an inverse manner such that a substantially constant flow to and from the apparatus is achieved. Alternatively, the flow rates to each sieve chamber may vary during the step time according to the same profile, but the rotary valves may be off-set and step independently in a staggered manner to achieve a substantially constant flow of a stream to or from the apparatus.Type: GrantFiled: March 10, 2017Date of Patent: January 30, 2018Assignee: ExxonMobil Chemical Patents Inc.Inventors: John R. Porter, Michael W. Weber, Gaurav Agrawal
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Patent number: 9878969Abstract: Disclosed is a process for the preparation of 1,3,3,3-tetrafluoropropene, comprising: (a) a compound having the formula CF3-xClxCHClCHF2-yCly and in the presence of a compound catalyst, undergoes, through n serially-connected reactors, gas-phase fluorination with hydrogen fluoride, producing 1,2,3-trichloro-1,1,3-trifluoropropane, and 1,2-dichloro-1,1,3,3-tetrafluoropropane; in said formula, x=1, 2 or 3; y=1 or 2, and 3?x+y?5; (b) 1,2,3-trichloro-1,1,3-trifluoropropane, and 1,2-dichloro-1,1,3,3-tetrafluoropropane undergo, in the presence of a dehalogenation catalyst, gas-phase dehalogenation with hydrogen, producing 3-chloro-1,3,3-trifluoropropene, and 1,1,3,3-tetrafluoropropene; (c) 3-chloro-1,3,3-trifluoropropene and 1,1,3,3-tetrafluoropropene undergo, in the presence of a fluorination catalyst, gas-phase fluorination with hydrogen fluoride, producing 1,3,3,3-tetrafluoropropene. The present invention is primarily used to produce 1,3,3,3-tetrafluoropropene.Type: GrantFiled: February 5, 2015Date of Patent: January 30, 2018Assignee: Xi'an Modern Chemistry Research InstituteInventors: Jian Lv, Hui Ma, Yujie Gu, Bo Wang, Yue Qin, Zhenhua Zhang, Zhijun Hao, Chunying Li, Fengxian Li, Jing Lv, Yanbo Bai
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Patent number: 9878970Abstract: The present invention relates to a novel a process for the preparation of 9-dichloromethylene-1,2,3,4-tetrahydro-1,4-methano-naphthalen-5-ylamine which process comprises a) reacting cyclopentadiene in the presence of a radical initiator and CXCl3, wherein X is chloro or bromo, to a compound of formula I1, or aa) reacting cyclopentadiene with CXCl3, wherein X is chloro, in the presence of a metal catalyst to a compound of formula I1, wherein X is chloro, b) reacting the compound of formula I1 with a base in the presence of an appropriate solvent to the compound of formula III, c) and converting the compound of formula III in the presence of 1,2-dehydro-6-nitrobenzene to the compound of formula IV, and d) hydrogenating the compound of formula IV in the presence of a metal catalyst.Type: GrantFiled: September 27, 2017Date of Patent: January 30, 2018Assignee: Syngenta Crop Protection, LLCInventors: Denis Gribkov, Bjorn Antelmann, Fanny Bois, Harald Walter, Alain De Mesmaeker
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Patent number: 9878971Abstract: The present invention relates to methods of making fused ring compounds, such as indeno-fused naphthols, and fused ring indenopyran compounds, such as indeno-fused naphthopyrans, that each employ an unsaturated compound represented by the following Formula II. Referring to the unsaturated compound of Formula II: Ring-A can be selected from optionally substituted aryl (e.g., phenyl); m can be, for example, from 0 to 4; R1 for each m can be selected from optionally substituted hydrocarbyl (e.g., C1-C6 alkyl) optionally interrupted with at least one linking group (e.g., —O—); and R3 and R16 can each be independently selected from, for example, hydrogen or optionally substituted hydrocarbyl, such as C1-C8 alkyl. When Ring-A is a phenyl group, the unsaturated compound represented by Formula II can be referred to as an unsaturated indanone acid/ester compound, or an indenone acid/ester compound (depending on whether R16 is hydrogen, or an optionally substituted hydrocarbyl group).Type: GrantFiled: November 7, 2016Date of Patent: January 30, 2018Assignee: Transitions Optical, Inc.Inventors: Meng He, Anil Kumar
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Patent number: 9878972Abstract: This invention pertains generally to prostacyclin formulations and methods for their use in promoting vasodilation, inhibiting platelet aggregation and thrombus formation, stimulating thrombolysis, inhibiting cell proliferation (including vascular remodeling), providing cytoprotection, preventing atherogenesis and inducing angiogenesis.Type: GrantFiled: August 17, 2016Date of Patent: January 30, 2018Assignee: United Therapeutics CorporationInventors: Ken Phares, David Mottola
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Patent number: 9878973Abstract: Provided herein are processes for preparing estolides and estolide base oils from fatty acid reactants utilizing catalysts. Further provided herein are processes for preparing carboxylic esters from at least one carboxylic acid reactant and at least one olefin.Type: GrantFiled: May 2, 2016Date of Patent: January 30, 2018Assignee: Biosynthetic Technologies, LLCInventors: Jakob Bredsguard, Jeremy Forest, Travis Thompson
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Patent number: 9878974Abstract: Provided are an ester of isotridecanoic acid and pentaerythritol, etc., wherein (i) the kinematic viscosity at 40° C. is in the range of 80-140 mm2/sec. and (ii) the number of terminal methyl groups per molecule of isotridecanoic acid in the isotridecanoic acid obtained by 1H-NMR measurement is in the range of 2.6-3.4 on average.Type: GrantFiled: February 6, 2015Date of Patent: January 30, 2018Assignee: KH NEOCHEM CO., LTD.Inventors: Junya Kishi, Shinji Tanaka
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Patent number: 9878975Abstract: The present invention relates to a process for the preparation of amines, comprising the following steps: a. reaction of a (i) carboxylic acid amide of the general formula (I), or (ii) carboxylic acid diamide of the general formula (II), or (iii) di-, tri- or polypeptide, or (iv) peptide amide with carboxy-terminal amide function with an alkylating agent, b. addition of a hydrogenation catalyst to the reaction mixture in a molar ratio of from 1:10 to 1:100 000, based on carboxylic acid amide, carboxylic acid diamide, di-, tri- or polypeptide or peptide amide, c. reaction of the reaction mixture with hydrogen, where a hydrogen pressure of from 0.1 bar to 200 bar is established and where a temperature in a range of from 0° C. to 250° C. is established.Type: GrantFiled: October 16, 2014Date of Patent: January 30, 2018Assignee: Evonik Degussa GmbHInventor: Renat Kadyrov
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Patent number: 9878976Abstract: The present invention provides a method for producing a high quality cationic surfactant, which is prevented from smelling and coloring, and has favorable storage stability. The production method includes the following step 1, step 2, step 3, and step 4: step 1: a step of obtaining an alkanolamine ester by reacting an alkanolamine with a fatty acid or a fatty acid alkyl ester without using hypophosphoric acid or a salt thereof; step 2: a step of obtaining a cationic surfactant by quaternizing the alkanolamine ester obtained in the step 1 with a dialkyl sulfate; step 3: a step of performing an oxidation treatment of the cationic surfactant obtained in the step 2; and step 4: a step of performing a reduction treatment of the cationic surfactant subjected to the oxidation treatment obtained in the step 3.Type: GrantFiled: October 28, 2015Date of Patent: January 30, 2018Assignee: KAO CORPORATIONInventors: Katsuhisa Inoue, Haruka Yoshida
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Patent number: 9878977Abstract: The present invention provides a compound of general formula A, useful as potential anticancer agents against human cancer cell lines and process for the preparation thereof. [Formula should be entered here] General formula A where in B selected from aryl, heteroaryl and fused heteroaryl ring R and X selected from H, hydroxy, alkyl, alkoxy, prop-2-ynyloxy, allyloxy, halo, alkylhalides, alkoxy halides, nitro, amine.Type: GrantFiled: August 18, 2015Date of Patent: January 30, 2018Assignee: COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCHInventors: Ahmed Kamal, Shaik Bajee, Challa Ratna Reddy, Mohammed Shaheer Malik, Vadithe Lakshma Nayak
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Patent number: 9878978Abstract: The present disclosure relates, in general, to processes for converting 2,5-dichloroaniline compounds to the corresponding 2,5-dichlorobenzenediazonium compounds, and further relates to processes for the preparation of 2,5-dichlorophenol which is a key intermediate used in the manufacture of dicamba.Type: GrantFiled: June 12, 2017Date of Patent: January 30, 2018Assignee: Monsanto Technology LLCInventors: Bruno De Kort, Matthew D. McReynolds, John J. Parlow, Rhonda S. Woerndle
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Patent number: 9878979Abstract: The present invention relates to the fine purification of isophoronenitrile (IPN) by melt crystallization.Type: GrantFiled: November 25, 2016Date of Patent: January 30, 2018Assignee: Evonik Degussa GmbHInventors: Joerg-Joachim Nitz, Stephan Kohlstruk, Robert Jansen, Anja Mueller, Jan Cassens, Axel Hengstermann
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Patent number: 9878980Abstract: Compounds of Formula (Ia) wherein R is a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl, a C1-C6 substituted or unsubstituted alkyl or —NR?R?, Q is C(O), O, NR?, S, S(O)2, C(O)2(CH2)p Y is C(O), O, NR?, S, S(O)2, C(O)2(CH2)p Z is H or C1-C4 alkyl, R? is H, C(O), S(O)2, C(O)2, a C6-C12 substituted or unsubstituted aryl, a C6-C12 substituted or unsubstituted heteroaryl or a C1-C6 substituted or unsubstituted alkyl, when substituted, aryl, heteroaryl and alkyl are substituted with halogen, C6-C12 heteroaryl, —NR?R? or COOZ, which have diagnostic and therapeutic properties, such as the treatment and management of prostate cancer and other diseases related to NAALADase inhibition, Radiolabels can be incorporated into the structure through a variety of prosthetic groups attached at the X amino acid side chain via a carbon or hetero atom linkage.Type: GrantFiled: October 28, 2016Date of Patent: January 30, 2018Assignee: Molecular Insight Pharmaceuticals, Inc.Inventors: John W. Babich, Craig N. Zimmerman, Kevin P. Maresca
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Patent number: 9878981Abstract: Provided is a production method of a synthetic intermediate for a heterocyclic compound having a renin inhibitory activity and useful as a prophylactic or therapeutic drug for diabetic nephropathy, hypertension and the like. A production method of a compound represented by the formula (III-1a), the formula (III-1b), the formula (III-1c) and/or the formula (III-1d); wherein each symbol is as described in DESCRIPTION, or a salt thereof, including reacting a compound represented by the formula (Ia) or (Ib): wherein each symbol is as described in DESCRIPTION, or a salt thereof with a compound represented by the formula (II): wherein each symbol is as described in DESCRIPTION, or a salt thereof, in the presence of an aluminum compound and a chiral amine compound.Type: GrantFiled: April 9, 2015Date of Patent: January 30, 2018Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Hironori Yamashita, Kazuhiro Miwa
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Patent number: 9878982Abstract: Disclosed are a method for preparing a series of novel pyridine derivatives and a use thereof. Such derivatives can be used in the treatment of related diseases caused by mycobacteria, in particular diseases caused by pathogenic mycobacteria, such as Mycobacterium tuberculosis, Mycobacterium bovis, Mycobacterium avium and Mycobacterium marinum.Type: GrantFiled: July 9, 2015Date of Patent: January 30, 2018Assignee: CISEN PHARMACEUTICAL CO., LTD.Inventors: Zhaozhong Ding, Shuhui Chen, Zhigang Huang, Wei Luo, Zhe Cai, Yepeng Wang, Dongdong Tang
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Patent number: 9878983Abstract: Disclosed are mild temperature (e.g., from 0 to 80° C.) SNAr fluorinations of a variety of halide and sulfonate substituted aryl and heteroaryl substrates using NMe4F.Type: GrantFiled: August 4, 2016Date of Patent: January 30, 2018Assignees: Dow AgroSciences LLC, The Regents of the University of MichiganInventors: Melanie Sanford, Sarah Ryan, Sydonie Schimler, Yang Cheng, Douglas Bland
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Patent number: 9878984Abstract: The present invention relates to anti-cancer compounds, methods for their discovery, and their therapeutic use. In particular, the present invention provides analogs of the known anti-cancer compound amonafide, and structurally and functionally related compounds, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with hyperproliferation.Type: GrantFiled: September 8, 2014Date of Patent: January 30, 2018Assignee: NORTHWESTERN UNIVERSITYInventors: Sui Huang, John Norton, Daniel Appella, Mark Witschi
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Patent number: 9878985Abstract: The present invention relates to novel benzocyclobutane(thio) carboxamides, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.Type: GrantFiled: October 28, 2014Date of Patent: January 30, 2018Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFTInventors: Christophe Dubost, Ulrike Wachendorff-Neumann, Philipp Winter, Stephane Brunet, Jean-Pierre Vors, Cyril Montagne
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Patent number: 9878986Abstract: Provided are urea derivatives of Formula I: with histone deacetylase (HDAC) inhibitory activity, optical isomers thereof, pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising the same. The provided urea derivatives of Formula I are selective histone deacetylase (HDAC) inhibitors and are effective for the treatment of histone deacetylase-mediated diseases such as malignant tumors, inflammatory diseases, rheumatoid arthritis, and neurodegeneration.Type: GrantFiled: April 29, 2014Date of Patent: January 30, 2018Assignee: Chong Kun Dang Pharmaceutical Corp.Inventors: Changsik Lee, Hyun-Mo Yang, Hojin Choi, Dohoon Kim, Soyoung Kim, Nina Ha, Hyojin Lim, Eunhee Ko, Seongae Yoon, Daekwon Bae
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Patent number: 9878987Abstract: The present invention provides compounds I and II and compositions thereof for use in the modulation of Hsp70. In some embodiments, the present invention provides a method for inhibiting Hsp70 activity. In some embodiments, the present invention provides a method of treating a subject suffering from or susceptible to a disease, disorder, or condition responsive to Hsp70 inhibition comprising administering to the subject a therapeutically effective amount of a provided compound. In some embodiments, the present invention provides a method for treating or preventing cancer in a subject suffering therefrom, comprising administering to a patient in need thereof a therapeutically effective amount of a provided compound.Type: GrantFiled: May 13, 2015Date of Patent: January 30, 2018Assignee: Memorial Sloan Kettering Cancer CenterInventors: Gabriela Chiosis, Yanlong Kang, Hardik J. Patel, Maulik Patel, Stefan Ochiana, Anna Rodina, Tony Taldone, Liza Shrestha
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Patent number: 9878988Abstract: Sodium channel blockers represented by the formula: are provided where the structural variables are defined herein. The invention also includes a variety of compositions, combinations and methods of treatment using these inventive sodium channel blockers.Type: GrantFiled: January 5, 2016Date of Patent: January 30, 2018Assignee: PARION SCIENCES, INC.Inventors: Michael Ross Johnson, William Robert Thelin, Richard C. Boucher
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Patent number: 9878989Abstract: The present invention provides a compound having a cholinergic muscarinic M1 receptor positive allosteric modulator activity, which may be useful as a prophylactic or therapeutic drug for Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, dementia with Lewy bodies and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof: wherein each symbol is as defined in the attached DESCRIPTION.Type: GrantFiled: June 23, 2016Date of Patent: January 30, 2018Assignee: Takeda Pharmaceutical Company LimitedInventors: Takahiro Sugimoto, Shinkichi Suzuki, Hiroki Sakamoto, Masami Yamada, Minoru Nakamura, Makoto Kamata, Kenichiro Shimokawa, Masataka Murakami, Jinichi Yonemori, Takuto Kojima
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Patent number: 9878990Abstract: The invention relates to benzylhydroxyde derivatives of formula (I): The invention also relates to the preparation and the therapeutic use of the compounds of formula (I).Type: GrantFiled: October 29, 2015Date of Patent: January 30, 2018Assignee: SANOFIInventors: Jérôme Meneyrol, Nathalie Alet, Guillaume Barre, Tristan Rousseaux, Valérie Vin
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Patent number: 9878991Abstract: The invention relates to compounds of formula IA and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: June 10, 2016Date of Patent: January 30, 2018Assignee: Purdue Pharma L.P.Inventor: Laykea Tafesse
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Patent number: 9878992Abstract: Described are GCF-8 inhibitors of the formula (I), and pharmaceutically acceptable salts thereof, wherein n, R1, R2, R5, R6, X and Z are defined herein. Also provided are pharmaceutical compositions comprising the same. Such compounds and compositions are useful in methods for inhibiting GDF-8 in a cell and methods for treating a patient suffering from a disease or disorder, wherein the patient would therapeutically benefit from an increase in mass or strength of muscle tissue.Type: GrantFiled: July 13, 2017Date of Patent: January 30, 2018Assignee: RIGEL PHARMACEUTICALS, INC.Inventors: Somasekhar Bhamidipati, Marina Gelman, Pingyu Ding, Rajinder Singh, Jeffrey Clough, Todd Kinsella, Donald Payan
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Patent number: 9878993Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. 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 19, 2016Date of Patent: January 30, 2018Assignee: Vertex Pharmaceuticals IncorporatedInventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
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Patent number: 9878994Abstract: Indazole compounds of formula (I) as cyclin-dependent kinase (CDK) and cell-proliferation inhibitors, and therapeutic uses and methods of preparation thereof, are disclosed. These compounds, and pharmaceutically acceptable salts, solvates, prodrugs, and pharmaceutical compositions thereof, are useful for treating diseases and disorders associated with activity of cyclin-dependent kinases, in particular CDK4/6, including but not limited to various cancers and inflammation-related diseases or conditions.Type: GrantFiled: July 24, 2015Date of Patent: January 30, 2018Assignee: Beta Pharma Inc.Inventors: Michael Nicholas Greco, Michael John Costanzo, Jirong Peng, Victoria Lynn Wilde, Don Zhang
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Patent number: 9878995Abstract: The present disclosure relates generally to modulators of Cot (cancer Osaka thyroid) and methods of use and manufacture thereof.Type: GrantFiled: February 9, 2017Date of Patent: January 30, 2018Assignee: GILEAD SCIENCES, INC.Inventors: Elizabeth M. Bacon, Gayatri Balan, Chien-Hung Chou, Christopher T. Clark, Jeromy J. Cottell, Musong Kim, Thorsten A. Kirschberg, John O. Link, Gary Phillips, Scott D. Schroeder, Neil H. Squires, Kirk L. Stevens, James G. Taylor, William J. Watkins, Nathan E. Wright, Sheila M. Zipfel
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Patent number: 9878996Abstract: Imidazolyl-pyrimidine and related compounds, as can utilize heme-iron coordination in the selective inhibition of neuronal nitric oxide synthase.Type: GrantFiled: May 23, 2017Date of Patent: January 30, 2018Assignee: Northwestern UniversityInventors: Richard B. Silverman, Paramita Mukherjee, Hien M. Nguyen
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Patent number: 9878997Abstract: Compounds of Formula I: or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Y, B, and Ring C are as defined herein, and wherein the Y—B moiety and the NH—C(?X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation, neurodegenerative diseases and certain infectious diseases.Type: GrantFiled: December 16, 2016Date of Patent: January 30, 2018Assignee: Array BioPharma Inc.Inventors: Shelley Allen, Steven W. Andrews, James F. Blake, Kevin R. Condroski, Julia Haas, Lily Huang, Yutong Jiang, Timothy Kercher, Gabrielle R. Kolakowski, Jeongbeob Seo
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Patent number: 9878998Abstract: Provided are methods and compositions for use in therapy, and in particular for treating cancer, preferably drug-resistant cancer, and/or radiation resistant cancer. The compounds may be used for reducing tumor size in a mammalian subject and for inducing apoptosis in a tumor cell. The methods are effective on tumor cells that are resistant to drugs such as temozolomide, doxorubicin, and geldanamycin, as well as non-resistant tumor cells. Further provided are barbiturate and thiobarbiturates diene compounds for use in treating cancer, and uses, methods and compositions relating to these compounds.Type: GrantFiled: August 15, 2012Date of Patent: January 30, 2018Assignee: NUHOPE LLCInventors: James R. Connor, Sang Yong Lee
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Patent number: 9878999Abstract: Focused library synthesis and medicinal chemistry on an oxadiazole-isopropylamide core proteasome inhibitor provided the lead compound that strongly inhibits CT-L activity. Structure activity relationship studies indicate the amide moiety and two phenyl rings are sensitive toward synthetic modifications. Only para-substitution in the A-ring was important to maintain potent CT-L inhibitory activity. Hydrophobic residues in the A-ring's para-position and meta-pyridyl group at the B-ring significantly improved inhibition. The meta-pyridyl moiety improved cell permeability. The length of the aliphatic chain at the para position of the A-ring is critical with propyl yielding the most potent inhibitor, whereas shorter (i.e. ethyl, methyl or hydrogen) or longer (i.e. butyl, propyl and hexyl) chains demonstrating progressively less potency. Introduction of a stereogenic center next to the ether moiety (i.e.Type: GrantFiled: September 24, 2013Date of Patent: January 30, 2018Assignee: H. Lee Moffitt Cancer Center and Research Institute, Inc.Inventors: Harshani R. Lawrence, Said M. Sebti, Sevil Ozcan
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Patent number: 9879000Abstract: The invention relates to aryl substituted heterocyclyl sulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.Type: GrantFiled: April 14, 2015Date of Patent: January 30, 2018Assignee: GRÜNENTHAL GMBHInventors: Stefan Schunk, Melanie Reich, Florian Jakob, Nils Damann, Michael Haurand, Achim Kless, Marc Rogers, Kathy MacKenzie
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Patent number: 9879001Abstract: Compounds of formula (I) wherein X1, X2, W, R1 to R5, L and m have the meaning according to the claims, are glucosidase inhibitors, and can be employed, inter alia, for the treatment of Alzheimer's disease.Type: GrantFiled: March 10, 2014Date of Patent: January 30, 2018Assignee: Merck Patent GmbHInventors: Henry Yu, Lesley Liu-Bujalski, Theresa L. Johnson
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Patent number: 9879002Abstract: Isolated or pure compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including but not limited to psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing an isolated or pure compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: GrantFiled: April 22, 2016Date of Patent: January 30, 2018Assignee: Omeros CorporationInventors: Jennifer Lynn Gage, Kevin L. Harbol, Raghuram Bommagani, Durga Varaprasad Botla, Laxma Reddy Karnati, Satyamurthi Narayanan
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Patent number: 9879003Abstract: Novel antiviral compounds of Formulae (I)-(III) are provided: (I) (II) (III) The inventive compounds, pharmaceutical compositions thereof, and kits including the inventive compounds are useful for the prevention and treatment of infectious diseases caused by viruses, for example, by Flaviviridae virus (e.g., Dengue virus (DENY)), Kunjin virus, Japanese encephalitis virus, vesicular stomatitis virus (VSV), herpes simplex virus 1 (HSV-1), human cytomegalovirus (HCMV), poliovirus, Junin virus, Ebola virus, Marburg virus (MARV), Lassa fever virus (LASV), Venezuelan equine encephalitis virus (VEEV), or Rift Valley Fever virus (RVFV).Type: GrantFiled: March 15, 2013Date of Patent: January 30, 2018Assignees: Dana-Farber Cancer Institute, Inc., President and Fellows of Harvard CollegeInventors: Nathanael Gray, Priscilla Yang, Qingsong Liu, Mélissanne de Wispelaere
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Patent number: 9879004Abstract: The present invention relates to novel acetylene derivatives as positive allosteric modulators for modulating metabotropic glutamate receptor subtype 4 (mGluR4) and/or altering glutamate level or glutamatergic signalling.Type: GrantFiled: January 15, 2014Date of Patent: January 30, 2018Assignee: Merck Patent GMBHInventors: Thomas E. Richardson, Nadia Brugger, Justin Potnick
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Patent number: 9879005Abstract: The present disclosure provides compositions and methods for treating ocular disorders in mammals especially in and not limited to humans and mice. The present disclosure further provides methods of treating cancer and appetite suppression using the compositions which are novel small molecule inhibitors of CaMKK2. In addition, these derived compositions can regulate non-ocular disorders, such as cancer and appetite suppression by modulating and inhibiting CaMKK2 and the regulation of the macrophage mediated diseases.Type: GrantFiled: February 5, 2016Date of Patent: January 30, 2018Assignee: Duke UniversityInventors: Scott W. Cousins, David M. Gooden, Priyatham S. Mettu
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Patent number: 9879006Abstract: The present invention relates to azaindole acetic acid derivatives of formula (I), wherein R1 and R2 are as described in the description, and their use as prostaglandin receptor modulators, most particularly as prostaglandin D2 receptor modulators, in the treatment of various prostaglandin-mediated diseases and disorders, to pharmaceutical compositions containing these compounds and to processes for their preparation.Type: GrantFiled: March 16, 2015Date of Patent: January 30, 2018Assignee: IDORSIA PHARMACEUTICALS LTDInventors: Hamed Aissaoui, Christoph Boss, Patrick Bouis, Julien Hazemann, Romain Siegrist
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Patent number: 9879007Abstract: Provided herein are compounds of Formula (I): and forms thereof, including compositions thereof and uses therewith for treating spinal muscular atrophy.Type: GrantFiled: August 26, 2016Date of Patent: January 30, 2018Assignees: PTC Therapeutics, Inc., F. Hoffmann-La Roche AGInventors: Hongyan Qi, Soongyu Choi, Amal Dakka, Gary Mitchell Karp, Jana Narasimhan, Nikolai Naryshkin, Anthony A. Turpoff, Marla L. Weetall, Ellen Welch, Matthew G. Woll, Tianle Yang, Nanjing Zhang, Xiaoyan Zhang, Xin Zhao, Luke Green, Emmanuel Pinard, Hasane Ratni
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Patent number: 9879008Abstract: The present invention relates to 2,3,4,6-tetra-substituted benzene-1,5-diamine derivatives, a preparation method therefor and a medicinal use thereof. Specifically, disclosed are compounds of formula (I) or pharmaceutically acceptable salts, stereoisomers, solvates or prodrugs, preparation method therefor and application thereof. Definition of each group in the formula can be found in the specification for details.Type: GrantFiled: April 13, 2015Date of Patent: January 30, 2018Assignees: SHANGHAI HAIYAN PHARMACEUTICAL TECHNOLOGY CO., LTD., YANGTZE RIVER PHARMACEUTICAL GROUP CO., LTD.Inventors: Jiong Lan, Yunzhou Jin, Fusheng Zhou, Qi He, Xiangyu He, Qiang Lv
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Patent number: 9879009Abstract: The present invention provides a method for manufacturing a compound represented by formula (I). With this method, provided are a method for manufacturing a 4-heteroaryl-N-(2-phenyl-[1,2,4]triazolo[1,5-a]pyridin-7-yl)-1H-pyrazole-5-carboxylic acid amide derivative; and an intermediate for this manufacturing method.Type: GrantFiled: July 29, 2015Date of Patent: January 30, 2018Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Tsutomu Satoh, Takashi Kudoh, Tetsuo Iwama
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Patent number: 9879010Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: GrantFiled: January 18, 2017Date of Patent: January 30, 2018Assignees: Incyte Holdings Corporation, Incyte CorporationInventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks
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Patent number: 9879011Abstract: The present invention relates to an amorphous form of linagliptin and processes for the preparation thereof. The invention also relates to a pharmaceutical composition comprising a therapeutically effective amount of an amorphous form of linagliptin and use of the composition for treatment of diabetes especially type-I or type-II, prediabetes or reduction of glucose tolerance.Type: GrantFiled: March 12, 2013Date of Patent: January 30, 2018Assignee: Cadila Healthcare LimitedInventors: Shriprakash Dhar Dwivedi, Ashok Prasad, Kuldeep Natwarlal Jain, Kumar Kamlesh Singh, Jitendra Maganbhai Gajera
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Patent number: 9879012Abstract: Click nucleic acid monomers and polymers containing such monomers are disclosed. The click nucleic acid monomers include an optionally protected thiol moiety, an optionally protected thiol-click acceptor moiety, and an optionally protected nucleobase (NB), which in some examples is an A, G, T, U, or C nucleobase. In some examples, the click nucleic acid monomer includes a N-vinyl thiol acetamide (VTA) backbone. In other examples the click nucleic acid monomer includes a N-vinyl thiol ethylamine (VTE) backbone. Methods of using such polymers, for example in place of naturally occurring nucleic acid polymer applications, such as DNA or RNA, and synthetic nucleic acid polymer applications, such as PNA or morpholino nucleic acids, are also disclosed.Type: GrantFiled: March 12, 2013Date of Patent: January 30, 2018Assignee: REGENTS OF THE UNIVERSITY OF COLORADO, A BODY CORPORATEInventors: Christopher N. Bowman, Christopher J. Kloxin, Weixian Xi
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Patent number: 9879013Abstract: Compounds represented by general formula (I) (all of the symbols in the formula conform to the definitions in the Description) are compounds that, in addition to having a Btk-selective inhibitory activity, exhibit an excellent metabolic stability and can avoid hepatotoxicity or the like, and as a consequence can provide safe therapeutic agents for diseases in which B cells or mast cells participate.Type: GrantFiled: December 9, 2014Date of Patent: January 30, 2018Assignee: ONO PHARMACEUTICAL CO., LTD.Inventors: Shingo Yamamoto, Toshio Yoshizawa