Patents Examined by Valerie Rodriguez-Garcia
  • Process for preparing electron deficient olefins
    Patent number: 10889542
    Abstract: This invention relates to a process for preparing electron deficient olefins, such as 2-cyanoacrylates, using an acid catalyzed two-step process including a transesterification reaction followed by a Knoevenagel condensation reaction.
    Type: Grant
    Filed: June 12, 2019
    Date of Patent: January 12, 2021
    Assignee: Henkel IP & Holding GmbH
    Inventors: Cormac Duffy, Marisa Phelan, Barry Burns
  • Azetidine derivatives useful as modulators of cortical catecholaminergic neurotransmission
    Patent number: 10875829
    Abstract: The disclosure provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of Formula (I): (I) or an isotope labelled analog thereof, or a pharmaceutically acceptable salt thereof, wherein: each of R1, R2, R3, R6 and R7 represents H or F, R4 represents H or CH3 R5 represents H or C1-C4alkyl, wherein at least two of R1, R2, R3, R6 and R7 represent F, together with at least one pharmaceutically acceptable carrier, excipient and/or diluent.
    Type: Grant
    Filed: November 17, 2017
    Date of Patent: December 29, 2020
    Assignee: INTEGRATIVE RESEARCH LABORATORIES SWEDEN AB
    Inventors: Clas Sonesson, Fredrik Pettersson
  • Aryl and heteroaryl amides for use as anti-proliferative, anti-thrombotic, and anti-viral agents
    Patent number: 10851096
    Abstract: Certain compounds of formula I: I and salts including pharmaceutically acceptable salts thereof are disclosed. Also disclosed are pharmaceutical compositions comprising a compound of formula I, processes for preparing compounds of formula I, intermediates useful for preparing compounds of formula I and therapeutic methods using a compound of formula I.
    Type: Grant
    Filed: June 16, 2017
    Date of Patent: December 1, 2020
    Assignees: Rutgers, The State University of New Jersey, The Curators of the University of Missouri
    Inventors: William J. Welsh, Raymond Birge, Vladyslav Kholodovych, Youyi Peng, Thomas Walter Comollo, Stanley G. Kimani, Kamlendra Singh
  • Process for the production of cannabidiol and delta-9-tetrahydrocannabinol
    Patent number: 10844035
    Abstract: The present disclosure relates to a cannabidiol compound and compositions thereof and processes for preparing the compound and compositions. The processes include an acid-catalyzed reaction of a suitably selected and substituted di-bromo-olivetol or derivative thereof with a suitably selected and substituted cyclic alkene to produce a dibromo-cannabidiol compound or derivative thereof. The dibromo-cannabidiol compound or derivative thereof can be produced in high yield, high stereospecificity, or both. It can then be converted under reducing conditions to a cannabidiol compound or derivatives thereof.
    Type: Grant
    Filed: July 13, 2018
    Date of Patent: November 24, 2020
    Assignee: PURISYS LLC
    Inventors: Lukas Dialer, Denis Petrovic, Ulrich Weigl
  • Methods for preparing antibody-drug conjugates
    Patent number: 10815309
    Abstract: This invention describes a method of conjugating a cell binding agent such as an antibody with an effector group (e.g., a cytotoxic agent) or a reporter group (e.g., a radionuclide), whereby the reporter or effector group is first reacted with a bifunctional linker and the mixture is then used without purification for the conjugation reaction with the cell binding agent. The method described in this invention is advantageous for preparation of stably-linked conjugates of cell binding agents, such as antibodies with effector or reporter groups. This conjugation method provides in high yields conjugates of high purity and homogeneity that are without inter-chain cross-linking and inactivated linker residues.
    Type: Grant
    Filed: February 1, 2019
    Date of Patent: October 27, 2020
    Assignee: IMMUNOGEN, INC.
    Inventors: Brenda A. Kellogg, Rajeeva Singh, Ravi V. Chari
  • [F]-labelled lactate derivative as pet radiotracer
    Patent number: 10799470
    Abstract: A positron emission tomography (PET) radiotracer for imaging lactate uptake, wherein the tracer is a [18F]-labelled lactate derivative which is [18F]-3-fluoro-2-hydroxypropionic acid: Also, a process for the radiosynthesis of the [18F]-labelled lactate derivative. Further, the use of the [18F]-labelled lactate derivative for imaging lactate uptake in living cells, especially in humans.
    Type: Grant
    Filed: September 8, 2017
    Date of Patent: October 13, 2020
    Assignee: GRANDIS
    Inventors: Pierre Sonveaux, Daniel Labar, Vincent Van Hée, Gwenaël Dehon, Raphaël Frédérick
  • Triazole derivatives and their use as PDE4 activators
    Patent number: 10793531
    Abstract: Compounds of Formula (I), which are activators of long form cyclic nucleotide phosphodiesterase-4 (PDE4) enzymes, are provided. Methods and uses of these compounds for the treatment or prevention of disorders requiring a reduction of second messenger responses mediated by cyclic 3?,5?-adenosine monophosphate (cAMP) are also described.
    Type: Grant
    Filed: July 10, 2019
    Date of Patent: October 6, 2020
    Assignee: Mironid Limited
    Inventor: Julia Adam
  • Pyridazine derivatives as EAAT2 activators
    Patent number: 10787433
    Abstract: Pyradizine derivatives that activity the excitatory amino acid transporter 2 (EAAT2) of the formula: and methods of use thereof for treating or preventing diseases, disorders, and conditions with glutamate toxicity.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: September 29, 2020
    Assignees: THE BRIGHAM AND WOMEN'S HOSPITAL, INC., OHIO STATE UNIVERSITY
    Inventors: Kevin Hodgetts, Chien-Liang Glenn Lin
  • Antimicrobial composition for protecting wood
    Patent number: 10779538
    Abstract: A multifunctional broad spectrum antimicrobial composition is described. The composition can be incorporated into a wood preservative, or used as an additive to provide antimicrobial properties to water-based wood coatings. The composition is a concentrated water-miscible emulsion containing 3-iodo-2-propynyl N-butylcarbamate (IPBC), carbendazim (BCM) and propiconazole (PPCZ), and has antimicrobial activity against a wide variety of fungal organisms, including surface molds, blue stain fungi and wood rotting fungi. The composition can act as an in-can preservative and is useful for antimicrobial protection of wood and wood-based substrates.
    Type: Grant
    Filed: December 20, 2018
    Date of Patent: September 22, 2020
    Assignee: Boss Holdings Inc.
    Inventors: Eric Bos, Nenad Vidovic
  • Separating a solvent from a nickel catalyst by distillation
    Patent number: 10759741
    Abstract: A solvent is at least partially separated from a catalyst. The catalyst comprises nickel and a bidentate phosphorus-containing ligand. The method for separation involves distilling a catalyst solution. The ratio of 2-pentenenitrile to 3-pentenenitrile in distillation column bottoms is controlled to reduce the amount of 3-pentenenitrile which is isomerized to form 2-methyl-3-butenenitrile. Isomerization of 3-pentenenitrile to 2-methyl-3-butenenitrile and subsequent isomerization of 2-methyl-3-butenenitrile to 2-methyl-2-butenenitrile, and/or hydrocyanation of 2-methyl-3-butenenitrile to methylglutaronitrile represents a loss in adiponitrile yield in a process for making adiponitrile.
    Type: Grant
    Filed: July 16, 2014
    Date of Patent: September 1, 2020
    Assignee: INVISTA North America S.a r.l.
    Inventors: Sudhir N. V. K. Aki, James M. Garner, William J. Tenn, III, Thomas E. Vos
  • Hydrogenation reaction catalyst for 1,4-anhydroerythritol, method for producing 3-hydroxytetrahydrofuran, and method for producing 1,3-butane diol
    Patent number: 10751704
    Abstract: A hydrogenation reaction catalyst used for a reaction of 1,4-anhydroerythritol and hydrogen to produce 3-hydroxytetrahydrofuran includes a carrier, at least one oxide selected from the group consisting of an oxide of a Group 6 element and an oxide of a Group 7 element, the oxide being supported on the carrier, and a metal other than a Group 6 element and a Group 7 element, the other metal being supported on the carrier. The amount of the oxide supported on the carrier in terms of a metal atom forming the oxide is 0.01 to 10% by weight based on the total amount of the oxide and the carrier being 100% by weight. The molar ratio in terms of metal of the other metal to the Group 6 element and Group 7 element forming the oxide [other metal/Group 6 element and Group 7 element] is 50/1 to 1/4.
    Type: Grant
    Filed: May 10, 2019
    Date of Patent: August 25, 2020
    Assignee: DAICEL CORPORATION
    Inventors: Keiichi Tomishige, Yoshinao Nakagawa, Yasuteru Kajikawa, Yuuichirou Hirai
  • Derivatives of korormicin useful as antibiotics
    Patent number: 10744111
    Abstract: An antibiotic compound of formula (III): or a salt or stereoisomer thereof; wherein R1-R3 and R5-R10 are independently selected from the group consisting of H, alkyl group, substituted alkyl group, halogen, OH, NH2 and SH; R4 is H, alkyl group or substituted alkyl group; X1-X2 are independently selected from the group consisting of ?O, ?S, NH, H, alkyl, halogen, OH, SH and NH2; W is a saturated acyclic hydrocarbon chain of 1 to 15 carbon atoms; and Z is a neutral or positively charged organic group. The compounds are useful in treating bacterial diseases.
    Type: Grant
    Filed: November 15, 2018
    Date of Patent: August 18, 2020
    Inventors: Pavel Dibrov, Elena Dibrov, Grant Pierce
  • Crystal forms of valsartan disodium salt
    Patent number: 10745363
    Abstract: Provided are crystal forms A, B, D, E, F, G and H of valsartan disodium salt and a preparation method therefor.
    Type: Grant
    Filed: September 2, 2016
    Date of Patent: August 18, 2020
    Assignee: NANJING NORATECH PHARMACEUTICALS CO., LTD
    Inventors: Fei Liu, Gang Wu, Weiming Jiang, Cheng-Gang Lin, Xuan Cai, Ping Lin, Yuling Lu, Lixiang Liu
  • Halogenated benzotropolones as ATG4B inhibitors
    Patent number: 10738002
    Abstract: The present invention relates to compounds having a benzotropolone core, and compositions containing said compounds acting as ATG4B inhibitors, thereby inhibiting autophagy. Moreover, the present invention provides processes for the preparation of the disclosed compounds, as well as methods of using them, for instance as a medicine, in particular for the treatment of cell proliferative disorders, such as cancer.
    Type: Grant
    Filed: November 24, 2017
    Date of Patent: August 11, 2020
    Assignees: UNIVERSITAIR ZIEKENHUIS ANTWERPEN, UNIVERSITEIT ANTWERPEN
    Inventors: Koen Augustyns, Matthias Cleenewerck, Guido R. Y. De Meyer, Jurgen Joossens, Ammar Kurdi, Pieter Van Der Veken, Christel Vangestel, Sigrid Stroobants, Wim Martinet
  • Spiro three-membered ring, spiro five-membered ring peptide deformylase inhibitor and use thereof in antibacteria and anti-tumor
    Patent number: 10738028
    Abstract: Disclosed are the anti-bacterial activity and the anti-tumor activity of a class of new spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor. The spiro three-membered ring and spiro five-membered ring peptide deformylase inhibitor of the present invention, as a class of new anti-bacterial agent, are effective against many antibiotic-resistant Gram-positive strains by inhibiting the activity of the peptide deformylase required in the synthesis of bacterial proteins, and do not affect the synthetic process of the main proteins of the human body, thus selectively killing bacteria.
    Type: Grant
    Filed: May 10, 2017
    Date of Patent: August 11, 2020
    Assignee: RUDONG RUIEN PHARMACEUTICAL TECHNOLOGY CO. LTD
    Inventors: Wenhao Hu, Fengping Lv, Yang Tang, Ziyan Li, Chen Chen, Jianhai Wei, Suzhen Dong, Yu Qian
  • Carbazole EHop-016 derivatives as anti-cancer and anti-migratory agents
    Patent number: 10729689
    Abstract: A series of novel EHop-016 derivatives is presented herein via designing and synthesizing compounds that mimics its more favorable “U-shaped” conformation that appears to be critical for inhibitory activity against Rac. Based on modeling studies on EHop-016, compounds with a more rigid structural conformation can mimic this “U-shaped” conformation would improve the anti-migration activity against metastatic cells. Compounds are disclosed that inhibit RhoGTPases that are useful for inhibiting hyperprofilerative and neoplastic diseases, for instance compounds of formula (I) Specifically, the compounds inhibit the GTPases Rac and Cdc42 that are overactive or overexpressed in signaling pathways in cancer and metastasis. Methods for treatment of cancer and hyperproliferative diseases are disclosed.
    Type: Grant
    Filed: October 23, 2018
    Date of Patent: August 4, 2020
    Assignee: UNIVERSITY OF PUERTO RICO
    Inventors: Eliud Hernandez-O'Farrill, Cornelis P. Vlaar, Suranganie Dharmawardhane Flanagan, Linette Castillo-Pichardo
  • N-hydroxylsulfonamide derivatives as nitroxyl donors
    Patent number: 10730828
    Abstract: The disclosed subject matter provides N-hydroxylsulfonamide derivative compounds of formulae (I), (II) or (III) as drawn below, pharmaceutical compositions comprising such compounds, kits comprising such compounds, and methods of using such compounds or pharmaceutical compositions. In particular, the disclosed subject matter provides methods of using such compounds or pharmaceutical compositions for treating heart failure.
    Type: Grant
    Filed: October 18, 2016
    Date of Patent: August 4, 2020
    Assignees: Cardioxyl Pharmaceuticals, Inc., The Johns Hopkins University
    Inventors: Vincent Jacob Kalish, Lisa Marie Frost, Frederick Arthur Brookfield, Stephen Martin Courtney, John P. Toscano
  • 5-substituted 2-(morpholin-4-yl)-1,7-naphthyridines
    Patent number: 10729680
    Abstract: The present invention relates to 5-substituted 2-(morpholin-4-yl)-1,7-naphthyridine compounds of general formula (I) or (Ib), to methods of preparing said compounds, to intermediate compounds useful for preparing said compounds, 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 a hyperproliferative disease as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: August 4, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Lücking, Marcus Koppitz, Julien Lefranc, Lars Wortmann, Antje Margret Wengner, Gerhard Siemeister, Ulf Bömer, Benjamin Bader, Philip Lienau, Hans Schick
  • Substituted 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-A]pyridine-3(2H)-ones and 2,5,6,7-tetrahydro-3H-pyrrolo[2,1-C][1,2,4]triazol-3-ones, and use thereof
    Patent number: 10722501
    Abstract: The present application relates to novel substituted 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-3(2H)-ones and 2,5,6,7-tetrahydro-3H-pyrrolo[2,1-c][1,2,4]triazol-3-ones of formula (I), to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of lung inflammation disorders.
    Type: Grant
    Filed: May 8, 2017
    Date of Patent: July 28, 2020
    Assignees: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Nicole Biber, Damian Brockschnieder, Kersten Matthias Gericke, Florian Kölling, Klemens Lustig, Jörg Meding, Heinrich Meier, Thomas Neubauer, Martina Schäfer, Andreas Timmermann, Dmitry Zubov, Carsten Terjung, Niels Lindner, Volker Badock, Dieter Moosmayer, Hideki Miyatake Ondozabal, Stephen Moore, Alexander Schulz
  • N-[(Pyrimidinylamino)propanyl]-and N-[(Pyridinylamino)-propanyl]arylcarboxamides
    Patent number: 10710984
    Abstract: The present invention relates to novel N-[(Pyrimidinylamino)propanyl]- and N-[(Pyridinylamino)propanyl]arylcarboxamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the orexin sub-type 1 receptor.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: July 14, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec, Stefan Scheuerer