Patents Issued in August 21, 2018
  • Monomer and polymer and compensation film and optical film and display device
    Patent number: 10053424
    Abstract: A monomer represented by Chemical Formula 1: wherein in Chemical Formula 1, X1, X2, L1, Y1, Y2, R1 to R9, n1, and n2 are the same as described in the detailed description.
    Type: Grant
    Filed: June 23, 2016
    Date of Patent: August 21, 2018
    Assignee: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Dmitry Androsov, Changki Kim, Masashi Tsuji, Hyunseok Choi
  • Piperidine derivative, liquid crystal composition and liquid crystal display device
    Patent number: 10053425
    Abstract: To provide a compound having an effect for preventing photolysis of a liquid crystal composition, and having a high solubility in the liquid crystal composition, a liquid crystal composition containing the compound, and a liquid crystal display device including the composition. The compound is represented by formula (1), the liquid crystal composition contains the compound, and the liquid crystal display device includes the composition. In formula (1), R1, R2, R3 and R4 are independently hydrogen or alkyl having 1 to 4 carbons; ring A1 and ring A2 are independently 1,4-cyclohexylene, 1,4-phenylene or the like; Z1, Z2 and Z3 are independently a single bond, alkylene or the like; and n is 0, 1 or 2.
    Type: Grant
    Filed: October 29, 2014
    Date of Patent: August 21, 2018
    Assignees: JNC CORPORATION, JNC PETROCHEMICAL CORPORATION
    Inventors: Yasuyuki Gotoh, Kenji Hirata, Maiko Matsukuma, Chikahide Kanadani
  • Process for the synthesis of metyrapone and alkylated metyrapone analogs
    Patent number: 10053426
    Abstract: Process for preparing metyrapone type compounds are generally described herein. In particular, one step process for preparing metyrapone type compounds are described herein. Such processes generally include an alpha-carbon arylation coupling reaction between 3-isobutyrylpyridine and 3-halopyridine compounds in the presence of a palladium catalyst and a phosphine ligand to form the metyrapone-type compounds.
    Type: Grant
    Filed: October 5, 2015
    Date of Patent: August 21, 2018
    Assignee: Albemarle Corporation
    Inventors: Eric L. Williams, James D. Sunderhaus, James J. Springer
  • Crystalline forms of cabozantinib phosphate and cabozantinib hydrochloride
    Patent number: 10053427
    Abstract: The present invention relates to crystalline forms of cabozantinib phosphoric acid salt and cabozantinib hydrochloric acid salt and to a method for their preparation. Furthermore, the invention relates to pharmaceutical compositions comprising said crystalline forms and their use as anti-cancer medicaments. Cabozantinib, i.e. N-{4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl}-N?-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide is represented by the chemical structure: Formula.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: August 21, 2018
    Assignee: Sandoz AG
    Inventors: Marijan Stefinovic, Erwin Paul Schreiner
  • 5-aminotetrahydroquinoline-2-carboxylic acids and their use
    Patent number: 10053428
    Abstract: The present application relates to novel 5-amino-5,6,7,8-tetrahydroquinoline-2-carboxylic acids, to processes for their preparation, to their use for the treatment and/or prevention of diseases, and to their use for producing medicaments for the treatment and/or prevention of diseases, especially for the treatment and/or prevention of cardiovascular and cardiopulmonary disorders.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: August 21, 2018
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Michael Hahn, Markus Follmann, Eva-Maria Becker, Johannes-Peter Stasch, Joerg Keldenich, Martina Delbeck, Hanna Tinel, Frank Wunder, Joachim Mittendorf, Ildiko Terebesi, Dieter Lang, René Martin, Walter Hübsch
  • DGAT2 inhibitors
    Patent number: 10053429
    Abstract: The present invention provides compounds of the Formula below: [Formula should be inserted here] Where A, X, R. and R2-R3 are as described herein; methods of treating patients for hypertriglyceridemia and cardiovascular disease including dyslipidemia and atherosclerosis, and processes for preparing the compounds.
    Type: Grant
    Filed: May 19, 2016
    Date of Patent: August 21, 2018
    Assignee: Eli Lilly and Company
    Inventors: Ana Maria Escribano, Maria Rosario Gonzalez, Celia Lafuente Blanco, Maria Dolores Martin-Ortega Finger, Michael R Wiley
  • RAF kinase modulator compounds and methods of use thereof
    Patent number: 10053430
    Abstract: Compounds, compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: August 21, 2018
    Assignee: AMBIT BIOSCIENCES CORP.
    Inventors: Sunny Abraham, Shripad S. Bhagwat, Brian T. Campbell, Qi Chao, Raffaella Faraoni, Mark W. Holladay, Andiliy G. Lai, Martin W. Rowbottom, Eduardo Setti, Kelly G. Sprankle
  • Tetrahydro-benzodiazepinones
    Patent number: 10053431
    Abstract: Disclosed are compounds of Formula I, or pharmaceutically acceptable salts thereof, wherein W, X, Y, Z, R1, R2, R3, R4 and R5 are as described in this application, and methods of using said compounds in the treatment of cancer.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: August 21, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Shaoqing Chen, Andrew F. Donnell, Robert Francis Kester, Kang Le, Yan Lou, Christophe Michoud, Stacy Remiszewski, Kenneth C. Rupert, Martin Weisel
  • Substituted [1,2,4]triazole and imidazole compounds
    Patent number: 10053432
    Abstract: The present invention relates to compounds of the formula I and the N-oxides and the salts thereof for combating phytopathogenic fungi, and to the use and methods for combating phytopathogenic fungi and to seeds coated with at least one such compound. The invention also relates to processes for preparing these compounds, intermediates, processes for preparing such intermediates, and to compositions comprising at least one compound I.
    Type: Grant
    Filed: December 5, 2014
    Date of Patent: August 21, 2018
    Assignee: BASF SE
    Inventors: Wassilios Grammenos, Nadege Boudet, Bernd Müller, Maria Angelica Quintero Palomar, Ana Escribano Cuesta, Erica May Cambeis, Jan Klaas Lohmann, Thomas Grote, Manuel Kretschmer, Ian Robert Craig
  • Androgen receptor antagonists
    Patent number: 10053433
    Abstract: Disclosed herein are compositions and methods for modulating the androgen receptor.
    Type: Grant
    Filed: December 19, 2016
    Date of Patent: August 21, 2018
    Assignee: The Regents of the University of California
    Inventors: Pamela M. England, Robert J. Fletterick, Kristopher Kuchenbecker, Felipe de Jesus Cortez
  • Histone deacetylase inhibitors and compositions and methods of use thereof
    Patent number: 10053434
    Abstract: Provided are certain histone deacetylase (HDAC) inhibitors of Formula I, compositions thereof, and methods of their use.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: August 21, 2018
    Assignee: CHDI FOUNDATION, INC.
    Inventors: Michel C. Maillard, Perla Breccia, Celia Dominguez, Alan F. Haughan, Amanda Van de Poël, Andrew J. Stott, Christopher A. Luckhurst, Elizabeth A. Saville-Stones, Grant Wishart, Michael Wall, Rebecca E. Jarvis
  • Furoxan compound, and manufacturing method for same
    Patent number: 10053435
    Abstract: The present invention provides: a furoxan compound having a fluorine atom as a substituent group on the ring structure thereof; and a novel nitric oxide donor including the compound. The present invention relates to a fluorofuroxan compound represented by general formula (1) or (2). The compound of formula (1) can be manufactured by reacting a fluoride salt with a nitrofuroxan compound to substitute the nitro group with a fluoro group. The compound of formula (2) can be manufactured by subjecting the compounds of formula (1) to isomerization by irradiation with light.
    Type: Grant
    Filed: December 15, 2015
    Date of Patent: August 21, 2018
    Assignee: NATIONAL UNIVERSITY CORPORATION KOBE UNIVERSITY
    Inventors: Ryosuke Matsubara, Akihiro Ando, Masahiko Hayashi
  • Process for the preparation of substituted oxiranes and triazoles
    Patent number: 10053436
    Abstract: The present invention relates to a process for the preparation of oxirane compounds of formula II from keto compounds III using dimethyl sulfide (CH3)2S and dimethylsulfate (CH3)2SO4, forming the reagent IV, trimethylsulfonium methylsulfate [(CH3)3S+ CH3SO4?], in aqueous solution in the presence of potassium hydroxide (KOH).
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: August 21, 2018
    Assignee: BASF Agro B.V.
    Inventors: Joachim Gebhardt, Manfred Ehresmann, Tiziana Chiodo, Martin Viertelhaus, Roland Goetz
  • Salt of dicarboxylic acid compound
    Patent number: 10053437
    Abstract: It is an object of the present invention to provide a medicament for preventing or treating hyperphosphatemia. The solution is crystals, or hydrate thereof, of a salt of a compound represented by formula (I).
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: August 21, 2018
    Assignee: DAIICHI SANKYO COMPANY, LIMITED
    Inventors: Mizuka Yokoyama, Yasusi Ueda, Daisuke Fukatsu, Yuichi Aki
  • Integrated process for making propene oxide and an alkyl tert-butyl ether
    Patent number: 10053438
    Abstract: An integrated process for making propene oxide and an alkyl tert-butyl ether comprises dehydrogenating a feed stream comprising iso-butane to provide a stream comprising iso-butene and hydrogen and separating this stream into a stream consisting essentially of hydrogen and a stream comprising iso-butene; reacting a part or all of the stream comprising iso-butene with an alkanol in the presence of a solid acid catalyst to provide an alkyl tert-butyl ether; reacting a part or all of the stream consisting essentially of hydrogen with oxygen, providing a stream comprising hydrogen peroxide; and reacting a part or all of the stream comprising hydrogen peroxide with propene in the presence of an epoxidation catalyst to provide propene oxide.
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: August 21, 2018
    Assignees: EVONIK DEGUSSA GMBH, THYSSENKRUPP INDUSTRIAL SOLUTIONS AG
    Inventors: David Bolz, Holger Wiederhold
  • Catalyst system for preparing propylene oxide
    Patent number: 10053439
    Abstract: A catalytic system containing a titanium zeolite of structure type MWW optionally containing zinc and containing at least one of an inorganic potassium salt and an organic potassium salt is provided. The catalyst system is useful in the preparation of propylene oxide.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: August 21, 2018
    Assignees: BASF SE, DOW Global Technologies LLC
    Inventors: Dominic Riedel, Joaquim Henrique Teles, Ulrike Wegerle, Andrei-Nicolae Parvulescu, Alexander Schroeder, Luise Spiske, Daniel Urbanczyk, Ulrich Mueller, Werner Witzl, Meinolf Weidenbach
  • Integrated process for making propene oxide and an alkyl tert-butyl ether
    Patent number: 10053440
    Abstract: An integrated process for making propene oxide and an alkyl tert-butyl ether comprises dehydrogenating a feed stream comprising propane and iso-butane to provide a stream comprising propene, iso-butene and hydrogen; separating this stream into a stream consisting essentially of hydrogen and a stream comprising propene and iso-butene; separating the stream comprising propene and iso-butene into a stream comprising propene and a stream comprising iso-butene; reacting a part or all of the stream comprising iso-butene with an alkanol in the presence of a solid acid catalyst to provide an alkyl tert-butyl ether; and reacting a part or all of the stream comprising propene with hydrogen peroxide in the presence of an epoxidation catalyst to provide propene oxide.
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: August 21, 2018
    Assignees: EVONIK DEGUSSA GMBH, THYSSENKRUPP INDUSTRIAL SOLUTIONS AG
    Inventors: David Bolz, Holger Wiederhold
  • Methods for purifying 5-(halomethyl)furfural
    Patent number: 10053441
    Abstract: The present disclosure provides methods for purifying a 5-(halomethyl)furfural composition, including 5-(chloromethyl)furfural, at operating conditions that decrease or minimize the decomposition or degradation of 5-(chloromethyl)furfural during the process. The methods may employ certain solvents, operating conditions, and/or techniques (e.g., gas stripping). The gaseous 5-(halomethyl)furfural produced from the process can be condensed or deposited to yield 5-(halomethyl)furfural in liquid or solid form. The solid 5-(halomethyl)furfural may be amorphous or crystalline.
    Type: Grant
    Filed: January 27, 2017
    Date of Patent: August 21, 2018
    Assignee: MICROMIDAS, INC.
    Inventors: Alex B. Wood, Shawn M. Browning, Makoto N. Masuno, Ryan L. Smith, John Bissell, II
  • Preparation of dialkyl esters of 2,5-furandicarboxylic acid
    Patent number: 10053442
    Abstract: Dialkyl esters of 2,5-furandicarboxylic acid are prepared from a 2,5-furandicarboxylic acid-containing starting material in a process, which includes: contacting a vaporous stream of an alkanol countercurrently with the at least partially liquid starting material having the 2,5-furandicarboxylic acid, in a reaction zone to conduct an esterification reaction to yield the dialkyl ester of 2,5-furandicarboxylic acid and water; withdrawing a reaction vapor comprising the alkanol and water from the reaction zone; and discharging a liquid phase having at least the dialkyl ester of 2,5-furandicarboxylic acid, from the bottom part of the reaction zone, to obtain the dialkyl ester of 2,5-furandicarboxylic acid.
    Type: Grant
    Filed: November 10, 2015
    Date of Patent: August 21, 2018
    Assignee: Synvina C.V.
    Inventors: Ana Sofia Vagueiro De Sousa Dias, Benjamin McKay, Victor Peter Charles Vreeken, Johannes Maria Franciscus Sijben
  • 2-phenylbenzofuran derivatives, method for preparing the same and use of the same for treating inflammatory disease
    Patent number: 10053443
    Abstract: The present invention relates to a novel 2-phenylbenzofuran derivative or a pharmaceutically acceptable salt thereof, a production method for the same, and a pharmaceutical composition for preventing or treating an inflammatory disease comprising the same as an active ingredient, and the novel 2-phenylbenzofuran derivative or the pharmaceutically acceptable salt thereof according to the present invention is outstandingly effective in suppressing NO, IL-6, and TNF-alpha induced by macrophages, and therefore can advantageously be used in a pharmaceutical composition for preventing or treating an inflammatory disease.
    Type: Grant
    Filed: March 3, 2017
    Date of Patent: August 21, 2018
    Assignees: KOREA RESEARCH INSTITUTE OF BIOSCIENCE AND BIOTECHNOLOGY, DONGGUK UNIVERSITY INDUSTRY—ACADEMIC COOPERATION FOUNDATION
    Inventors: Kyeong Lee, Sei-Ryang Oh, Kyung Seop Ahn, Ok-Kyoung Kwon, Doo-Young Kim, Hyung Won Ryu, Jung Hee Kim, Xuezhen Xu
  • Cannabinergic nitrate esters and related analogs
    Patent number: 10053444
    Abstract: Biologically active cannabinergic nitrate esters and related analogs, process of preparation, pharmaceutical compositions and their methods of use as medicaments, pharmacological tools or biomarkers. Pharmaceutical compositions may include one or more of the nitrate ester compounds. Medicaments include one or more of the cannabinergic nitrate ester compounds and are useful in treating a variety of diseases. A method of treating, preventing or reducing the severity of a condition includes administering at least one of the disclosed nitrate ester compounds to an individual or animal in need thereof.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: August 21, 2018
    Assignee: University of Connecticut
    Inventors: Alexandros Makriyannis, Kiran Vemuri
  • Photocleavable chemical inducers of dimerization (CID) and methods of use
    Patent number: 10053445
    Abstract: The instant invention provides photolysable compounds, and their use in reversible chemical induced dimerization and light-induced regulation of proteins.
    Type: Grant
    Filed: October 24, 2014
    Date of Patent: August 21, 2018
    Assignees: Children's Medical Center Corporation, President and Fellows of Harvard College
    Inventors: Thomas L. Schwarz, Matthew R. Banghart, Amos Gutnick
  • Heterobicyclic compounds and their use for the treatment of tuberculosis
    Patent number: 10053446
    Abstract: It is an object of the present invention to provide a compound having an excellent antibacterial activity against tuberculosis bacteria, multidrug-resistant tuberculosis bacteria and/or non-tuberculous mycobacteria. Disclosed is a compound of the general formula (1): wherein each symbol is defined as described in the attached specification, or a salt thereof.
    Type: Grant
    Filed: August 28, 2015
    Date of Patent: August 21, 2018
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hiroshi Shimizu, Yoshikazu Kawano, Shunpei Ishikawa, Yukitaka Uematsu, Toshio Shinohara, Motohiro Itotani, Yoshikazu Haraguchi, Isao Takemura, Atsunori Kaneshige, Yuya Nakai, Norimitsu Hariguchi, Yohei Hayashi, Makoto Matsumoto
  • Fluorescent compounds
    Patent number: 10053447
    Abstract: Compounds used as labels with properties comparable to known fluorescent compounds. The compounds can be conjugated to proteins and nucleic acids for biological imaging and analysis. Synthesis of the compounds, formation and use of the conjugated compounds, and specific non-limiting examples of each are provided.
    Type: Grant
    Filed: December 20, 2011
    Date of Patent: August 21, 2018
    Assignees: Pierce Biotechnology, Inc, Dyomics GmbH
    Inventors: Greg Hermanson, Peter T. Czerney, Surbhi Desai, Matthias S. Wenzel, Boguslawa Dworecki, Frank G. Lehmann
  • Substituted tetrazolinones for controlling plant diseases
    Patent number: 10053448
    Abstract: A tetrazolinone compound represented by formula (1): wherein R1 represents a hydrogen atom, a C1-C3 alkyl group optionally having one or more halogen atoms, a C1-C3 alkoxy group optionally having one or more halogen atoms, a halogen atom, a cyano group, or a C1-C3 alkylthio group optionally having one or more halogen atoms; and R2 represents a C1-C3 alkyl group optionally having one or more halogen atoms, a C1-C3 alkoxy group optionally having one or more halogen atoms, a hydrogen atom, a halogen atom, or a C3-C4 cycloalkyl group optionally having one or more halogen atoms, has excellent control activity against plant diseases.
    Type: Grant
    Filed: March 28, 2016
    Date of Patent: August 21, 2018
    Assignee: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventors: Nao Maehata, Sadayuki Arimori
  • Quinazoline derivatives, compositions thereof, and use as pharmaceuticals
    Patent number: 10053449
    Abstract: Disclosed herein are protein kinase inhibitors, more particularly novel quinazoline derivatives and pharmaceutical compositions thereof, and method of use thereof.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: August 21, 2018
    Assignee: Shanghai Fochon Pharmaceutical Co., Ltd.
    Inventors: Weibo Wang, Xingdong Zhao, Tongshuang Li, Qiang Tian, Ling Chen, Zuwen Zhou, Zhifu Li, Xianlong Wang, Yue Rong, Lihua Jiang, Yanxin Liu, Jing Sun, Fanxin Zeng
  • Heterocyclic modulators of lipid synthesis
    Patent number: 10053450
    Abstract: 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: Grant
    Filed: July 5, 2016
    Date of Patent: August 21, 2018
    Assignee: 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
  • Heterocyclic estrogen receptor modulators and uses thereof
    Patent number: 10053451
    Abstract: Described herein are compounds that are estrogen receptor modulators. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such estrogen receptor modulators, alone and in combination with other compounds, for treating diseases or conditions that are mediated or dependent upon estrogen receptors.
    Type: Grant
    Filed: May 25, 2016
    Date of Patent: August 21, 2018
    Assignee: Genentech, Inc.
    Inventors: Sharada Labadie, Jun Liang, Daniel Fred Ortwine, Xiaojing Wang, Birong Zhang, Nicholas D. Smith, Steven P. Govek, Mehmet Kahraman, Andiliy G. Lai, Johnny Y. Nagasawa, Simon Charles Goodacre, Nicholas Charles Ray
  • Crystalline forms of N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine salts and uses thereof
    Patent number: 10053452
    Abstract: The present invention relates to crystalline forms and co-crystal forms of pharmaceutically acceptable salts of the compound, N-(4-((3-(2-amino-4-pyrimidinyl)-2-pyridinyl)oxy)phenyl)-4-(4-methyl-2-thienyl)-1-phthalazinamine (AMG 900, and pharmaceutical compositions comprising said crystalline and co-crystal forms thereof. The invention further provides uses of the crystalline forms and compositions, to treat cancer, including various types of solid tumors and hematologic cancer including myeloma and leukemia.
    Type: Grant
    Filed: November 25, 2014
    Date of Patent: August 21, 2018
    Assignee: AMGEN INC.
    Inventors: Mary Chaves, Matthew Bio, Matthew Peterson
  • Compounds and their use as BACE inhibitors
    Patent number: 10053453
    Abstract: The present application relates to compounds of formula (I), (Ia), or (Ib) and their pharmaceutical compositions/preparations. This application further relates to methods of treating or preventing A?-related pathologies such as Down's syndrome, ?-amyloid angiopathy such as but not limited to cerebral amyloid angiopathy or hereditary cerebral hemorrhage, disorders associated with cognitive impairment such as but not limited to MCI (“mild cognitive impairment”), Alzheimer's disease, memory loss, attention deficit symptoms associated with Alzheimer's disease, neurodegeneration associated with diseases such as Alzheimer's disease or dementia, including dementia of mixed vascular and degenerative origin, pre-senile dementia, senile dementia and dementia associated with Parkinson's disease.
    Type: Grant
    Filed: October 7, 2015
    Date of Patent: August 21, 2018
    Assignee: AstraZeneca AB
    Inventors: Roland Bürli, Mark E. Duggan, Jörg Holenz, Patrik Johansson, Karin Kolmodin, Philip Vellacott Thorne, Michael John McKenzie
  • Carbazole compounds useful as bromodomain inhibitors
    Patent number: 10053454
    Abstract: The present invention is directed to carbazole compounds, pharmaceutically acceptable compositions comprising compounds of the invention and methods of using the compositions in the treatment of various disorders.
    Type: Grant
    Filed: February 27, 2014
    Date of Patent: August 21, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Michael A. Poss, David R. Tortolani, Ashok Vinayak Purandare, John S. Tokarski, Christopher P. Mussari, Muthoni G. Kamau, Dharmpal S. Dodd, Ashvinikumar V. Gavai, Daniel O'Malley, Tram N. Huynh, Wayne Vaccaro, Lalgudi S. Harikrishnan
  • Diazaspiroalkaneone-substituted oxazole derivatives as spleen tyrosine kinase inhibitors
    Patent number: 10053455
    Abstract: The present invention is concerned with substituted oxazole derivatives that selectively modulate, regulate, and/or inhibit signal transduction mediated by certain native and/or mutant protein kinases implicated in a variety of human and animal diseases such as cell proliferative, metabolic, autoimmune, allergic, and degenerative disorders. In particular, the presently disclosed compounds are Syk inhibitors.
    Type: Grant
    Filed: March 23, 2015
    Date of Patent: August 21, 2018
    Assignee: AB SCIENCE
    Inventors: Abdellah Benjahad, Jason Martin, Claire Schalon, Didier Pez, Emmanuel Chevenier, Franck Sandrinelli, Willy Picoul, Alain Moussy
  • Cyclopropanamine compound and use thereof
    Patent number: 10053456
    Abstract: The present invention provides a compound having a lysine-specific demethylase-1 inhibitory action, and useful as a medicament such as a prophylactic or therapeutic agent for schizophrenia, developmental disorders, particularly diseases having intellectual disability (e.g., autistic spectrum disorders, Rett syndrome, Down's syndrome, Kabuki syndrome, fragile X syndrome, Kleefstra syndrome, neurofibromatosis type 1, Noonan syndrome, tuberous sclerosis), neurodegenerative diseases (e.g., Alzheimer's disease, Parkinson's disease, spinocerebellar degeneration (e.g., dentatorubural pallidoluysian atrophy) and Huntington's disease), epilepsy (e.g., Dravet syndrome) or drug dependence, and the like. A compound represented by the formula wherein each symbol is as defined in the present specification, or a salt thereof.
    Type: Grant
    Filed: April 9, 2015
    Date of Patent: August 21, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Shigemitsu Matsumoto, Yasushi Hattori, Masashi Toyofuku, Shinji Morimoto, Masaki Daini, Takuto Kojima, Tomohiro Kaku, Mitsuhiro Ito
  • Hydroxyalkyl-piperazine derivatives as CXCR3 receptor modulators
    Patent number: 10053457
    Abstract: The invention relates to compounds of Formula (I) wherein n, X, R1 and R2 are as described in the description; to pharmaceutically acceptable salts thereof, and to the use of such compounds as medicaments, especially as modulators of the CXCR3 receptor.
    Type: Grant
    Filed: January 14, 2016
    Date of Patent: August 21, 2018
    Assignee: IDORSIA PHARMACEUTICALS LTD.
    Inventors: Eva Caroff, Emmanuel Meyer
  • Pyrimidine-2,4-diamine derivative and anticancer pharmaceutical composition comprising same as effective ingredient
    Patent number: 10053458
    Abstract: The present invention relates to a pyrimidine-2,4-diamine derivative or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition for prevention or treatment of cancer comprising the same as an effective ingredient. A compound according to the present invention has the good effect of inhibiting anaplastic lymphoma kinase (ALK) activity, whereby a therapeutic effect on cancer cells having an anaplastic lymphoma kinase (ALK) fusion protein such as EML4-ALK, NPM-ALK, etc. can be enhanced and it is expected that a recurrence of cancer will be effectively inhibited. As such, the compound can be effectively used in a pharmaceutical composition for prevention or treatment of cancer.
    Type: Grant
    Filed: May 21, 2015
    Date of Patent: August 21, 2018
    Assignee: KOREA RESEARCH INSTITUTE OF CHEMICAL TECHNOLOGY
    Inventors: Chang Soo Yun, Hyoung Rae Kim, Sung Yun Cho, Hee Jung Jung, Kwangho Lee, Chong Hak Chae, Chong Ock Lee, Chi Hoon Park, Pilho Kim, Jong Yeon Hwang, Jae Du Ha, Sun Joo Ahn
  • Life-extending agent, life extension method using the life-extending agent, novel dual oxidase activator, method for activating dual oxidase, production of life-extending agent, and production of dual oxidase activator
    Patent number: 10053459
    Abstract: The present invention provides a life-extending agent comprising pyrroloquinoline quinone and/or a derivative of the pyrroloquinoline quinone.
    Type: Grant
    Filed: September 18, 2015
    Date of Patent: August 21, 2018
    Assignees: National University Corporation Nagoya University, Mitsubishi Gas Chemical Company, Inc.
    Inventors: Ikue Mori, Hiroyuki Sasakura, Kazuto Ikemoto, Masahiko Nakano
  • Process for the preparation of tert-butyl 4-((2S ,5R)-6-(benzyloxy)-7-oxo-1,6-diazabicyclo[3.2.1]octane-2-carboxamido)piperidine-1-carboxylate and analogs thereof
    Patent number: 10053460
    Abstract: The present invention relates to processes for preparing compounds of Formula I. Such compounds include interme-diates in the manufacture of 7-oxo-1,6-diazabicyclo[3.2.1 ]octane-2-carboxamide beta-lactamase inhibitors such as (2S,5R)-7-oxo-N-5 piperidin-4-yl-6-(sulfoxy)-1,6-diazabicyclo[3.2.1]octane-2-carboxamide. The present invention also relates to novel intermediates formed i these processes. The present invention relates to a process for preparing a compound of Formula I or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: August 21, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Zhijian Liu, Nobuyoshi Yasuda, Lu Yang, Artis Klapars, Kevin R. Campos, Mikhail Reibarkh
  • Tetracyclic 4-oxo-pyridine-3-carboxylic acid derivatives for the treatment and prophylaxis of hepatitis B virus infection
    Patent number: 10053461
    Abstract: The invention provides novel compounds having the general formula: wherein R1 to R6, V, W, X and Y are as described herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: January 10, 2018
    Date of Patent: August 21, 2018
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Xingchun Han, Min Jiang, Yongguang Wang, Song Yang
  • P2X7 modulators
    Patent number: 10053462
    Abstract: The present invention is directed to a compound of Formula (I): wherein: n is an integer from 0-1; X is CH2 when n is 0, or X is CH2 or oxygen when n is 1; R1 is phenyl or pyridinyl, wherein the phenyl or pyridinyl is optionally substituted with from 1 to 4 substituents independently selected from halogen and alkyl; and R2 is phenyl, pyridinyl, pyrazinyl, pyradizinyl, pyrimidinyl, pyrrolyl, pyrazolyl, thiazolyl or thiophenyl, wherein the phenyl, pyridinyl, pyrazinyl, pyradizinyl, pyrimidinyl, pyrrolyl, pyrazolyl, thiazolyl or thiophenyl is optionally substituted with from 1 to 2 substituents independently selected from the group consisting of halogen, alkyl, hydroxy and alkoxy. The invention also relates to pharmaceutical compositions comprising compounds of Formula (I). Methods of making and using the compounds of Formula (I) are also within the scope of the invention.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: August 21, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael A. Letavic, Dale A. Rudolph
  • Substituted [1,2,4]triazolo[4,3-a]pyrazines as P2X7 modulators
    Patent number: 10053463
    Abstract: The present invention is directed to a compound of Formula (I).
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: August 21, 2018
    Assignee: Janssen Pharmaceutica NV
    Inventors: Michael K. Ameriks, Jason C. Rech, Brad M. Savall, Jessica L. Wall
  • Triazolopyridazine derivatives as modulators of TNF activity
    Patent number: 10053464
    Abstract: A series of substituted [1,2,4]triazolo[4,3-b]pyridazine derivatives of formula (I), being potent modulators of human TNFa activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: December 8, 2014
    Date of Patent: August 21, 2018
    Assignee: UCB BIOPHARMA SPRL
    Inventor: Daniel Christopher Brookings
  • Pyrrolopyrimidine derivatives as TAM inhibitors
    Patent number: 10053465
    Abstract: This application relates to compounds of Formula I: or pharmaceutically acceptable salts thereof, which are inhibitors of TAM kinases which are useful for the treatment of disorders such as cancer.
    Type: Grant
    Filed: August 25, 2016
    Date of Patent: August 21, 2018
    Assignee: Incyte Corporation
    Inventors: Yun-Long Li, David M. Burns, Hao Feng, Joseph Glenn, Chunhong He, Taisheng Huang, Song Mei, Jun Pan, Xiaozhao Wang, Yingda Ye
  • Process for preparing chiral dipeptidyl peptidase-IV inhibitors
    Patent number: 10053466
    Abstract: A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of: ?and reductive amination of:
    Type: Grant
    Filed: December 5, 2017
    Date of Patent: August 21, 2018
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: John Y. L. Chung, Feng Peng, Yonggang Chen, Amude Mahmoud Kassim, Cheng-yi Chen, Mathew Maust, Mark McLaughlin, Michael J. Zacuto, Qinghao Chen, Lushi Tan, Zhiguo Jake Song, Yang Cao, Feng Xu
  • Therapeutic isoxazole compounds
    Patent number: 10053467
    Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.
    Type: Grant
    Filed: April 4, 2017
    Date of Patent: August 21, 2018
    Assignee: Dart NeuroScience (Cayman) Ltd.
    Inventors: Alan Kaplan, Terence Keenan, Andrew McRiner
  • Heterocyclic compound
    Patent number: 10053468
    Abstract: The present invention relates to compound (I) or a salt thereof which has a ROR?t inhibitory action. wherein each symbol is as defined in the specification.
    Type: Grant
    Filed: July 2, 2014
    Date of Patent: August 21, 2018
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Satoshi Yamamoto, Junya Shirai, Hiroyuki Watanabe, Shoji Fukumoto, Tsuneo Oda, Hidekazu Tokuhara, Yoshihide Tomata, Naoki Ishii, Michiko Tawada, Mitsunori Kono, Atsuko Ochida, Takashi Imada, Yoshiyuki Fukase, Tomoya Yukawa
  • Pyridone and aza-pyridone compounds and methods of use
    Patent number: 10053469
    Abstract: Pyridone and aza-pyridone compounds of Formula I are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: September 30, 2016
    Date of Patent: August 21, 2018
    Assignees: GILEAD CONNECTICUT, INC., GENENTECH INC.
    Inventors: Antonio J. M. Barbosa, Peter A. Blomgren, Kevin S. Currie, Ravi Krishnamoorthy, Jeffrey E. Kropf, Seung H. Lee, Scott A. Mitchell, Daniel Ortwine, Aaron C. Schmitt, Xiaojing Wang, Jianjun Xu, Wendy Young, Honglu Zhang, Zhongdong Zhao, Pavel E. Zhichkin
  • Inhibitors of PI3K-delta and methods of their use and manufacture
    Patent number: 10053470
    Abstract: The invention is directed to Compounds of Formula I: and pharmaceutically acceptable salts or solvates thereof as well as methods of making and using the compounds.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: August 21, 2018
    Assignee: Exelixis, Inc.
    Inventor: James William Leahy
  • Azabenzimidazole derivatives
    Patent number: 10053471
    Abstract: The present invention relates to compounds of general formula (I), wherein R1, R2, R3, A1, A2, m and n are defined as in claim 1, which have valuable pharmacological properties, in particular bind to the AMP-activated protein kinase (AMPK) and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: August 21, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Frank Himmelsbach, Elke Langkopf
  • Silicon-based fungicides and process for producing the same
    Patent number: 10053472
    Abstract: The present invention discloses novel antifungal compounds of formula (I), method for preparing these compounds and the use of these compounds as antifungal agents in prevention and treatment of fungal infections, and compositions containing these novel compounds.
    Type: Grant
    Filed: January 5, 2015
    Date of Patent: August 21, 2018
    Assignee: Council of Scientific & Industrial Research
    Inventors: Dumbala Srinivasa Reddy, Gorakhnath Rajaram Jachak, Remya Ramesh, Santosh Genba Tupe, Mukund Vinayak Deshpande
  • Flame retardant filler
    Patent number: 10053473
    Abstract: A flame retardant filler having brominated silica particles, for example, imparts flame retardancy to manufactured articles such as printed circuit boards (PCBs), connectors, and other articles of manufacture that employ thermosetting plastics or thermoplastics. In this example, brominated silica particles serve both as a filler for rheology control (viscosity, flow, etc.) and a flame retardant. In an exemplary application, a PCB laminate stack-up includes conductive planes separated from each other by a dielectric material that includes a flame retardant filler comprised of brominated silica particles. In an exemplary method of synthesizing the brominated silica particles, a monomer having a brominated aromatic functional group is reacted with functionalized silica particles (e.g., isocyanate, vinyl, amine, or epoxy functionalized silica particles).
    Type: Grant
    Filed: December 5, 2017
    Date of Patent: August 21, 2018
    Assignee: International Business Machines Corporation
    Inventors: Dylan J. Boday, Joseph Kuczynski, Robert E. Meyer, III