Patents Examined by Timothy R Rozof
  • Ingenol compounds and use thereof in anti-HIV latency treatment
    Patent number: 10959974
    Abstract: Provided in the present invention are ingenol compounds and a use thereof in preparing an anti-HIV latency drug. In particular, provided in the present invention is a use of ingenol compounds and pharmaceutically acceptable salts thereof for preparing a drug for: (a) intervening with HIV viral latency; (b) activating an HIV virus that has been integrated into mammalian genomes; and/or (c) inducing the expression of the dormant HIV provirus in infected cells. The compounds of the present invention may also be used in combination with antiretroviral drugs to accelerate the removal of latent viral reservoirs.
    Type: Grant
    Filed: February 22, 2016
    Date of Patent: March 30, 2021
    Assignee: SHANGHAI XIN HAO BIOLOGICAL TECHNOLOGY COMPANY
    Inventors: Longfei Zhang, Pengfei Wang, Zhongjun Ma, Huanzhang Zhu
  • Acetylation of cannabinoids using sulfuric acid catalyst
    Patent number: 10954209
    Abstract: A process for producing THC-O-acetate using a succession of distillation, salting-out assisted liquid-liquid extractions (SALLEs), and solvent recovery techniques. Tetrahydrocannabinol (THC) in Cannabis oil reacts with acetic anhydride with hexane and under reflux to produce THC-O-acetate and acetic acid using sulfuric acid as a catalyst. The resulting crude product is distilled and subjected to a SALLE with hexane followed by a SALLE with petroleum ether, before being distilled again in order to obtain a refined, THC-O-acetate product.
    Type: Grant
    Filed: September 15, 2019
    Date of Patent: March 23, 2021
    Assignee: Nextleaf Solutions Ltd.
    Inventor: David Novitski
  • Water soluble fluorescent or colored dyes and methods for their use
    Patent number: 10954391
    Abstract: Compounds useful as fluorescent or colored dyes are disclosed. The compounds have the following structure (I): including stereoisomers, salts and tautomers thereof, wherein R1, R2, R3, L1, L2, L3, L4, L5, L6, M1, M2, A, q, w and n are as defined herein. Methods associated with preparation and use of such compounds are also provided.
    Type: Grant
    Filed: June 13, 2019
    Date of Patent: March 23, 2021
    Assignee: Sony Corporation
    Inventors: Tracy Matray, Hesham Sherif, C. Frederick Battrell
  • Organotin catalysts in esterification processes of furan-2,5-dicarboxylic acid (FDCA)
    Patent number: 10947208
    Abstract: A method for preparing sugar-based mono and diesters is described. The process entails the esterification of 2,5-furan-dicarboxylic acid (FDCA) with an alcohol in the presence of low loadings of a homogeneous organotin (IV) catalyst.
    Type: Grant
    Filed: May 11, 2017
    Date of Patent: March 16, 2021
    Assignees: ARCHER DANIELS MIDLAND COMPANY, DUPONT INDUSTRIAL BIOSCIENCES USA, LLC
    Inventors: Kenneth Stensrud, Stuart Fergusson
  • Formulations for intravenous administration
    Patent number: 10945947
    Abstract: The present invention relates to an improved formulation of danirixin in its hydrobromide salt form. This improved formulation can be an aqueous intravenous formulation containing danirixin or a lyophilized pharmaceutical solid composition containing danirixin to be reconstituted to provide a solution for intravenous administration.
    Type: Grant
    Filed: December 3, 2019
    Date of Patent: March 16, 2021
    Inventors: Rachel Apfelbaum, Andrew James Peat, Yoon Oh
  • Fused polycyclic dimers
    Patent number: 10947253
    Abstract: Novel fused tricyclic or bicyclic dimers, such as ?-carboline and quinoline moieties with a central linker, exhibit anti-cancer activities against a variety of human cancer cell lines. The dimer compounds can be used in anti-cancer therapeutic compositions useful in the treatment of human cancers.
    Type: Grant
    Filed: August 5, 2019
    Date of Patent: March 16, 2021
    Assignee: Ankh Life Sciences Limited
    Inventors: Brian Scott Johnathan Blagg, Vishal Chandrakumar Birar, Gene H. Zaid
  • Furo[2,3-b]pyran-2-one compounds and process for preparation thereof
    Patent number: 10941155
    Abstract: The present invention discloses a novel furo[2,3-b]pyran-2-one compound of formula (I) and a single step process for the preparation of furo[2,3-b]pyran-2-ones using Lewis acid-promoted cascade annulation of alkynols and ?-ketoesters.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: March 9, 2021
    Assignee: Council of Scientific & Industrial Research
    Inventors: Ravindar Kontham, Sagar Sudam Thorat
  • Compounds and methods for inhibiting fascin
    Patent number: 10941141
    Abstract: Provided are compounds, compositions and methods for inhibiting fascin activity or treating a condition or disorder mediated by fascin activity in a subject in need thereof.
    Type: Grant
    Filed: March 11, 2019
    Date of Patent: March 9, 2021
    Assignees: NOVITA PHARMACEUTICALS, INC., CORNELL UNIVERSITY
    Inventors: Xin-Yun Huang, Christy Young Shue
  • Quinoline and isoquinoline derivatives for treating pain and pain related conditions
    Patent number: 10941138
    Abstract: The present invention relates to new compounds of formula (I): showing great affinity and activity towards the subunit ?2? of voltage-gated calcium channels (VGCC), especially the ?2?-1 subunit of voltage-gated calcium channels or dual activity towards subunit ?2? of voltage-gated calcium channels (VGCC), especially the ?2?-1 subunit of voltage-gated calcium channels, and the noradrenaline transporter (NET).
    Type: Grant
    Filed: December 20, 2017
    Date of Patent: March 9, 2021
    Assignee: ESTEVE PHARMACEUTICALS, S.A.
    Inventors: Carmen Almansa-Rosales, Susana Yenes-Mínguez, Marina Virgili-Bernado, Monica Alonso-Xalma
  • Pyrazole MAGL inhibitors
    Patent number: 10927105
    Abstract: Provided herein are pyrazole compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful as modulators of monoacylglycerol lipase (MAGL). Furthermore, the subject compounds and compositions are useful for the treatment of pain.
    Type: Grant
    Filed: June 12, 2020
    Date of Patent: February 23, 2021
    Assignee: LUNDBECK LA JOLLA RESEARCH CENTER, INC.
    Inventors: Cheryl A. Grice, John J. M. Wiener, Olivia D. Weber, Katharine K. Duncan
  • Modulators of indoleamine 2,3-dioxygenase
    Patent number: 10927078
    Abstract: Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: February 23, 2021
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Martha Alicia De La Rosa, Wieslaw Mieczyslaw Kazmierski, Yoshiaki Washio
  • Process for preparing intermediate of anti-tumor drug niraparib and intermediate thereof
    Patent number: 10927077
    Abstract: Disclosed is a process for preparing an intermediate of anti-tumor drug niraparib and an intermediate thereof. The present invention discloses a process for preparing compound f, which comprises conducting a cyclization reaction of compound e in a solvent and in the presence of a base to give compound f. The process of the present invention does not involve the steps of catalytic reduction or catalytic coupling reaction of precious metals and chiral separation, which has advantages such as low equipment requirements, simple operation, favorable industrial production, avoiding waste liquid containing heavy metals and phosphorus, low cost and high product ee value.
    Type: Grant
    Filed: October 12, 2018
    Date of Patent: February 23, 2021
    Assignee: ZAI LAB (SHANGHAI) CO., LTD.
    Inventor: Tianhao Wang
  • Metal-free direct arylation of dialkyl phosphonates for the synthesis of mixed alkyl aryl phosphonates
    Patent number: 10927135
    Abstract: Provided herein are phosphates, thiophosphates, phosphonates, and phosphinates, methods of making same, and methods of using these compounds and methods for the generation of pharmaceutically relevant phosphate, phosphonate, and phosphinate analogs. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: February 23, 2021
    Assignee: THE BOARD OF REGENTS OF THE NEVADA SYSTEM OF HIGHER EDUCATION ON BEHALF OF THE UNIVERSITY OF NEVADA, LAS VEGAS
    Inventors: Jun Yong Kang, Hai Huang
  • Phenyl [a]indole[2,3-g]quinolizine compounds, preparation method therefor, pharmaceutical composition, and applications thereof
    Patent number: 10927107
    Abstract: The present invention relates to phenyl [a]indole[2,3-g]quinolizine compounds represented by formula (I), a preparation method therefor, a pharmaceutical composition, and applications thereof. Specific applications are applications in the preparation of drugs for treating diseases related to a proprotein convertase subtilisin Kexin-9 (PCSK9), comprising the applications in the preparation of drugs for treating hyperlipemia, hypercholesterolemia, hypertriglyceridemia, fatty liver deformation, atherosclerosis, obesity and other metabolic diseases.
    Type: Grant
    Filed: March 29, 2017
    Date of Patent: February 23, 2021
    Assignee: Shanghai Institute of Materia Medica, Chinese Academy of Sciences
    Inventors: Hong Liu, Yiping Wang, Fei Zhao, Jing Zhao, Jiang Wang, Cong Xi, Chenglin Wu, Hao Shen, Xu Han, Hualiang Jiang, Kaixian Chen
  • Silylations of aromatic substrates with base-activated organosilanes
    Patent number: 10927065
    Abstract: The present disclosure describes methods for silylating aromatic organic substrates, and associated chemical systems, said methods comprising or consisting essentially of contacting the aromatic organic substrate with a mixture of (a) at least one organosilane and (b) at least one strong base, under conditions sufficient to silylate the aromatic substrate.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: February 23, 2021
    Assignee: California Institute of Technology
    Inventors: Robert H. Grubbs, Alexey Fedorov, Anton Toutov, Kerry N. Betz
  • Macrocyclization reactions and intermediates and other fragments useful in the synthesis of halichondrin macrolides
    Patent number: 10913749
    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., Horner-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: April 18, 2019
    Date of Patent: February 9, 2021
    Assignee: EISAI R&D MANAGEMENT CO., LTD.
    Inventors: Francis G. Fang, Dae-Shik Kim, Hyeong-Wook Choi, Charles E. Chase
  • Thienopyridine carboxamides as ubiquitin-specific protease inhibitors
    Patent number: 10913753
    Abstract: The disclosure relates to inhibitors of USP28 and/or USP25 useful in the treatment of cancers, inflammation, autoimmune diseases, and infectious diseases, having the Formula: where R1, R2, R3, R4, R5, R5?, R6, R7, X, m, and n are described herein.
    Type: Grant
    Filed: February 13, 2017
    Date of Patent: February 9, 2021
    Assignee: VALO EARLY DISCOVERY, INC.
    Inventors: David Joseph Guerin, Kenneth W. Bair, Justin A. Caravella, Stephanos Ioannidis, Jr., David R. Lancia, Jr., Hongbin Li, Steven Mischke, Pui Yee Ng, David Richard, Shawn E. R. Schiller, Tatiana Shelekhin, Zhongguo Wang
  • Modulators of indoleamine 2,3-dioxygenase
    Patent number: 10906924
    Abstract: Provided are IDO inhibitor compounds of Formula I and pharmaceutically acceptable salts thereof, their pharmaceutical compositions, their methods of preparation, and methods for their use in the prevention and/or treatment of diseases.
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: February 2, 2021
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Martha Alicia De La Rosa, Hongfeng Deng, Ghotas Evindar, Wieslaw Mieczyslaw Kazmierski, John Franklin Miller, Vicente Samano, Yoshiaki Washio, Bing Xia
  • Quaternary heteroatom containing compounds
    Patent number: 10906875
    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: May 31, 2019
    Date of Patent: February 2, 2021
    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
  • Process for the preparation of quinolone based compounds
    Patent number: 10899713
    Abstract: The present invention relates to an improved process for the preparation of quinolone based compounds of general formula (I) using intermediate compound of general formula (XII). Invention also provides an improved process for the preparation of compound of formula (I-a) using intermediate compound of formula (XII-a) and some novel impurities generated during process. Compounds prepared using this process can be used to treat anemia.
    Type: Grant
    Filed: May 24, 2019
    Date of Patent: January 26, 2021
    Assignee: CADILA HEALTHCARE LIMITED
    Inventors: Ranjit C. Desai, Rajiv Sharma, Vrajesh Pandya, Kalpesh Shah, Sunil Patel, Rakesh Chauhan, Ranjeet Nair, Vivek Joshi, Manoj Patel, Mrigendra Shukla