Patents Examined by Timothy R Rozof
  • Patent number: 10350210
    Abstract: The present application provides a compound of formula I, which is a EGFR and ALK dual inhibitor and can be used alone or in combination with other therapeutic agents to treat diseases such as non-small cell lung cancer. The compounds of the present application are useful in the treatment of diseases carrying the EGFR wild-type gene, or carrying the EGFR T790M mutant gene and/or the EGFR L858R mutant gene and/or the EGFR delE746_A750 mutant gene, or in the treatment of diseases carrying the ALK wild-type gene, ALK F1174L mutant gene and/or ALK F1196M gene and/or EML4-ALK mutant gene and/or NPM-ALK mutant gene, and can be used in the first-line treatment of anaplastic lymphoma kinase (ALK) positive late-stage non-small cell Lung cancer.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: July 16, 2019
    Assignee: PRECEDO PHARMACEUTICALS CO., LTD
    Inventors: Jing Liu, Qingsong Liu, Taoshan Jiang, Aoli Wang, Jiaxin Wu, Hong Wu, Ziping Qi, Yongfei Chen, Fengming Zou, Wenchao Wang, Zheng Zhao, Li Wang, Beilei Wang
  • Patent number: 10351532
    Abstract: Provided is a compound of formula (I), in which Ar1, R1, U, V, W, X, and p are as described herein. Also provided are methods of using a compound of formula (I), including a method of treating cancer, a method of treating a patient with cancer cells resistant to an anti-cancer agent, and a method of inhibiting lactate dehydrogenase A (LDHA) and/or lactate dehydrogenase B (LDHB) activity in a cell.
    Type: Grant
    Filed: December 29, 2015
    Date of Patent: July 16, 2019
    Assignees: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES, VANDERBILT UNIVERSITY, THE UAB RESEARCH FOUNDATION, THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA
    Inventors: David J. Maloney, Alex Gregory Waterson, Ganesh Rai Bantukallu, Kyle Ryan Brimacombe, Plamen Christov, Chi V. Dang, Victor Darley-Usmar, Xin Hu, Ajit Jadhav, Somnath Jana, Kwangho Kim, Jennifer L. Kouznetsova, William J. Moore, Bryan T. Mott, Leonard M. Neckers, Anton Simeonov, Gary Allen Sulikowski, Daniel Jason Urban, Shyh Ming Yang
  • Patent number: 10343996
    Abstract: The invention provides heterocyclic compounds with quaternary centers and methods of preparing compounds. Methods include the method for the preparation of a compound of Formula (II): comprising treating a compound of Formula (I): with a transition metal catalyst and under alkylation conditions as valence and stability permit.
    Type: Grant
    Filed: July 30, 2018
    Date of Patent: July 9, 2019
    Assignee: California Institute of Technology
    Inventors: Brian M. Stoltz, Scott C. Virgil, David E. White, Taiga Yurino, Yiyang Liu, Douglas C. Behenna, Douglas Duquette, Christian Eidamshaus
  • Patent number: 10344038
    Abstract: The present invention provides unified synthesis of the CI-CI 9 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hydridized carbon. The provided efficient selective coupling reactions can allow easy access to the CI-CI 9 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.
    Type: Grant
    Filed: April 29, 2016
    Date of Patent: July 9, 2019
    Assignee: President and Fellows of Harvard College
    Inventors: Yoshito Kishi, Wuming Yan, Jingwei Li, Zhanjie Li, Kenzo Yahata
  • Patent number: 10343966
    Abstract: The invention relates to a process for producing 17-oxabicyclo[14.1.0]heptadec-8-ene comprising a reaction with the reactants cyclohexadeca-1,9-diene and hydrogen peroxide.
    Type: Grant
    Filed: October 23, 2017
    Date of Patent: July 9, 2019
    Assignee: SYMRISE AG
    Inventors: Peter Esser, Angela Köckritz, Andreas Martin, Diego Jaime
  • Patent number: 10336701
    Abstract: The present invention is directed to pyridin-2-one derivatives, pharmaceutical compositions containing them and their use as antagonists of the EP3 receptor, for the treatment of for example, impaired oral glucose tolerance, elevated fasting glucose, Type II Diabetes Mellitus, Syndrome X (also known as Metabolic Syndrome) and related disorders and complications thereof.
    Type: Grant
    Filed: August 9, 2018
    Date of Patent: July 2, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Xuqing Zhang, Mark J. Macielag
  • Patent number: 10323054
    Abstract: Metal coordination complexes comprising a metal atom coordinated to at least one aza-allyl ligand having the structure represented by: where each R1-R4 are independently selected from the group consisting of H, branched or unbranched C1-C6 alkyl, branched or unbranched C1-C6 alkenyl, branched or unbranched C1-C6 alkynyl, cycloalkyl groups having in the range of 1 to 6 carbon atoms, silyl groups and halogens. Methods of depositing a film using the metal coordination complex and a suitable reactant are also described.
    Type: Grant
    Filed: November 28, 2017
    Date of Patent: June 18, 2019
    Assignee: Applied Materials, Inc.
    Inventors: Benjamin Schmiege, Jeffrey W. Anthis, David Thompson
  • Patent number: 10322996
    Abstract: A method for producing derivatives of N-retinoylaminoalkane sulfonic acid, the method comprising providing retinoic acid, chloroformate, aminoalkanesulfonic acid selected from the group consisting of cysteic acid and alkyl ester thereof, cysteinesulfinic acid and alkyl ester thereof, homocysteic acid and alkyl ester thereof, homocysteinesulfinic acid and alkyl esters thereof, taurine and derivatives thereof, and an organic solvent, and a base, mixing said components under substantial absence of oxidizing compounds thereby forming a reaction mixture comprising a liquid phase, wherein the liquid phase is one phase and the derivatives of N-retinoylaminoalkane sulfonic acid are formed in said liquid phase.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: June 18, 2019
    Assignee: ARDENIA INVESTMENTS, LTD
    Inventors: Dzianis Babrou, Maryna Budnikava, Mikael Björklund, Julian Aleksov
  • Patent number: 10316012
    Abstract: Disclosed is a method of synthesizing a series of compounds with the structure of (1S, 5R)-lactone. In the method, under the catalysis of a chiral phosphonic acid, substituted bicyclo[3.2.0]-hept-2-en-6-one (II) as a substrate is reacted with hydrogen peroxide for enantioselective Baeyer-Villiger oxidation to produce a chiral lactone (I). This method involves mild reaction conditions, simple operation, quantitatively recyclable catalyst and high reaction selectivity and stereoselectivity, which is suitable for industrial production.
    Type: Grant
    Filed: January 13, 2019
    Date of Patent: June 11, 2019
    Assignee: FUDAN UNIVERSITY
    Inventors: Fener Chen, Haihui Peng, Sha Hu, Ge Meng, Yan Wu, Dang Cheng, Zedu Huang, Guanfeng Liang
  • Patent number: 10308661
    Abstract: The invention provides methods for the synthesis of a halichondrin macrolides through a macrocyclization strategy. The macrocyclization strategy of the present invention involves subjecting a non-macrocyclic intermediate to a carbon-carbon bond-forming reaction (e.g., an olefination reaction (e.g., Homer-Wadsworth-Emmons olefination), catalytic Ring-Closing Olefin Metathesis, or Nozaki-Hiyama-Kishi reaction) to afford a macrocyclic macrolide. The invention also provides compounds useful as intermediates in the synthesis of a halichondrin macrolides and methods for preparing the same.
    Type: Grant
    Filed: May 9, 2016
    Date of Patent: June 4, 2019
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase
  • Patent number: 10300471
    Abstract: Using a [RuCl2(arene)]2 complex and a formate source, a directed ortho C—H insertion and aryl-aryl coupling sequence in water provides biaryl compounds useful in the preparation of biologically active molecules and intermediates. Reactions may be conducted in the ambient atmosphere. Ruthenium catalysts prepared from [RuCl2(arene)]2 and a formate source may be prepared in situ or isolated for later use.
    Type: Grant
    Filed: October 6, 2014
    Date of Patent: May 28, 2019
    Inventors: Ali Aiden Koohang, Anita Mehta
  • Patent number: 10278965
    Abstract: An object of the present invention is to provide a cancer cell inhibitory drug, particularly a cancer stem-cell inhibitory drug, or a cancer stem-cell detection probe.
    Type: Grant
    Filed: August 16, 2017
    Date of Patent: May 7, 2019
    Assignee: CANON KABUSHIKI KAISHA
    Inventors: Taichi Shintou, Tsuyoshi Nomoto, Kohei Watanabe, Takeshi Miyazaki, Toshio Tanaka, Yasuhito Shimada, Yuhei Nishimura
  • Patent number: 10273258
    Abstract: The present invention provides a process for the preparation of mono- and bisacylphosphanes based on formula (I): as well as for their corresponding oxides or sulfides. The present invention further relates to photoinitiators obtainable by said process.
    Type: Grant
    Filed: May 24, 2017
    Date of Patent: April 30, 2019
    Assignee: ETH ZUERICH
    Inventors: Hansjoerg Gruetzmacher, Georgina Mueller
  • Patent number: 10273245
    Abstract: The present invention provides a compound useful as an agent for the prophylaxis or treatment of neurodegenerative disease and the like, or a salt thereof. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
    Type: Grant
    Filed: November 19, 2018
    Date of Patent: April 30, 2019
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Tatsuki Koike, Masato Yoshikawa, Haruhi Ando, William John Farnaby
  • Patent number: 10276806
    Abstract: Provided are a coating solution for a non-light-emitting organic semiconductor device having high carrier mobility that contains a compound represented by Formula (2) and a solvent having a boiling point of equal to or higher than 100° C., an organic transistor, a compound, an organic semiconductor material for a non-light-emitting organic semiconductor device, a material for an organic transistor, a method for manufacturing an organic transistor, and a method for manufacturing an organic semiconductor film. (In Formula (2), R11 and R12 each independently represent a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, or an alkoxy group and may have a substituent, and an aromatic portion in Formula (2) may be substituted with a halogen atom.
    Type: Grant
    Filed: April 3, 2018
    Date of Patent: April 30, 2019
    Assignees: FUJIFILM Corporation, The University of Tokyo
    Inventors: Hiroaki Tsuyama, Kimiatsu Nomura, Yoshihisa Usami, Masatoshi Yumoto, Tetsu Kitamura, Masashi Koyanagi, Tetsuya Watanabe, Toshihiro Okamoto, Junichi Takeya
  • Patent number: 10270044
    Abstract: Provided are a coating solution for a non-light-emitting organic semiconductor device having high carrier mobility that contains a compound represented by Formula (2) and a solvent having a boiling point of equal to or higher than 100° C., an organic transistor, a compound, an organic semiconductor material for a non-light-emitting organic semiconductor device, a material for an organic transistor, a method for manufacturing an organic transistor, and a method for manufacturing an organic semiconductor film. (In Formula (2), R11 and R12 each independently represent a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, or an alkoxy group and may have a substituent, and an aromatic portion in Formula (2) may be substituted with a halogen atom.
    Type: Grant
    Filed: November 5, 2018
    Date of Patent: April 23, 2019
    Assignees: FUJIFILM Corporation, The University of Tokyo
    Inventors: Hiroaki Tsuyama, Kimiatsu Nomura, Yoshihisa Usami, Masatoshi Yumoto, Tetsu Kitamura, Masashi Koyanagi, Tetsuya Watanabe, Toshihiro Okamoto, Junichi Takeya
  • Patent number: 10266494
    Abstract: The invention relates to a novel process for preparing polyfluoroalkylated quinolines from ketimines in the presence of fluoroalkylamino reagents.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: April 23, 2019
    Assignees: Bayer CropScience Aktiengesellschaft, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Sergii Pazenok, Jean-Pierre Vors, Frédéric R Leroux, Fallia Aribi, Etienne Schmitt, Armen Panossian
  • Patent number: 10259824
    Abstract: The disclosure provides for compounds that bind with a high affinity to the C3d component of complement. The disclosure further provides for the use of the C3d-binding compounds as therapeutic and/or diagnostic agents for complement-mediated diseases or disorders.
    Type: Grant
    Filed: May 1, 2016
    Date of Patent: April 16, 2019
    Assignee: The Regents of the University of California
    Inventors: Dimitrios Morikis, Ronald D. Gorham, Jr.
  • Patent number: 10259797
    Abstract: Provided herein is a process for preparing a mixture including 5-(hydroxy-methyl)furfural (HMF) and one or more HMF esters of formula (I), the process including the following steps: (A-1) preparing or providing a starting mixture which includes one, two or more carbohydrate compounds and as the solvent or as a co-solvent for the carbohydrate compounds an amount of one or more carboxylic acid esters of formula (II); (A-2) subjecting the starting mixture to reaction conditions so that at least one of the one, two or more carbohydrate compounds reacts, and a fraction of the amount of one or more carboxylic acid esters of formula (II) is hydrolyzed, so that a mixture results that includes 5-(hydroxy-methyl)furfural and/or the one or more HMF esters of formula (I), one or more carboxylic acids of formula (III) and a remaining fraction of the amount of one or more carboxylic acid esters of formula (II).
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: April 16, 2019
    Assignee: BASF SE
    Inventors: Alvaro Gordillo, Martin Alexander Bohn, Stephan A Schunk, Ivana Jevtovikj, Holger Werhan, Svenia Duefert, Markus Piepenbrink, Rene Backes, Richard Dehn
  • Patent number: 10252978
    Abstract: An N-substituted triacetonediamine compound is produced by reacting 4-amino-2,2,6,6-tetramethylpiperidine or a derivative thereof with a carbonyl compound in a reductive amination.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: April 9, 2019
    Assignee: Evonik Degussa GmbH
    Inventors: Katharina Minke, Benjamin Willy