Patents Examined by Taofiq A. Solola
  • Method to treat lipid dysregulation by modulation of proprotein convertase subtilisin/kexin type 9 (PCSK9) protein activity with small molecule ligands
    Patent number: 11026957
    Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small molecule ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small molecule compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small molecule ligands to PCSK9 alters the conformation of the protein, modifying the interaction between PCSK9 and an endogenous low density lipoprotein receptor, and can lead to reduced or increased levels of circulating LDL-cholesterol. High LDL-cholesterol levels are associated with increased risk for heart disease. Low LDL-cholesterol levels may be problematic in other conditions, such as liver dysfunction; thus, there is also utility for small molecule ligands that can raise LDL levels.
    Type: Grant
    Filed: April 30, 2020
    Date of Patent: June 8, 2021
    Assignee: SRX CARDIO, LLC
    Inventors: Thomas E Barta, Jonathan W Bourne, Kyle D Monroe, Michael M Muehlemann
  • Treating patients harboring an isocitrate dehydrogenase-1 (IDH-1) mutation
    Patent number: 11013734
    Abstract: Methods of treating patients diagnosed with AML or MDS harboring mutant IDH-1 include detecting an IDH1 mutation and the therapeutic administration of an inhibitor of a mutant IDH-1 as a single agent, or in combination with azacitidine (AZA) or cytarabine.
    Type: Grant
    Filed: July 30, 2019
    Date of Patent: May 25, 2021
    Assignee: FORMA Therapeutics, Inc.
    Inventors: Patrick F. Kelly, Alan Collis, Jeff Davis, Duncan Walker, Susan Ashwell, Blythe Thomson, Wei Lu
  • Cyclin-dependent kinase 8 and/or 19 inhibitor
    Patent number: 11013728
    Abstract: The present invention aims to provide a novel cyclin-dependent kinase 8 and/or 19 inhibitor useful as an anti-cancer agent. The present invention relates to a cyclin-dependent kinase 8 and/or 19 inhibitor containing a compound represented by the formula (I): [wherein each symbol is as defined in the DESCRIPTION] or a pharmaceutically acceptable salt thereof as an active ingredient, and use thereof as an agent for preventing and/or treating cancer.
    Type: Grant
    Filed: April 2, 2018
    Date of Patent: May 25, 2021
    Assignee: Kyoto Pharmaceutical Industries, Ltd.
    Inventors: Tatsuya Kitao, Shigemitsu Takeda, Yoshimichi Shoji, Hiroaki Shirahase
  • Methods of drying propylene oxide
    Patent number: 11014899
    Abstract: Methods of drying streams that include propylene oxide. The methods may include contacting a stream that includes propylene oxide with molecular sieves. The molecular sieves may be in a drying unit, and may be regenerated. The streams that include propylene oxide may include one or more other organic compounds.
    Type: Grant
    Filed: May 13, 2020
    Date of Patent: May 25, 2021
    Assignee: Lyondell Chemical Technology, L.P.
    Inventors: Xueyong Yang, Daniel F. White, Ha H. Nguyen, Robert J. Rebman, Chelsee A. Arceneaux
  • TLR 9 inhibitors
    Patent number: 11008303
    Abstract: A method for inhibiting TLR9 includes contacting the TLR9 with compound of general formula (I): wherein the meanings of the variables are explained in the specification, or a stereoisomeric form or a mixture of stereoisomeric forms, or pharmaceutically acceptable salts thereof. A pharmaceutical composition can include compounds of the invention, which can be used in a method for inhibiting TLR9 activity in vitro or in vivo. The method can be performed by administering the compound to a subject to inhibit TLR9 activity, which can be used to treat a disease or disorder associated with TLR9.
    Type: Grant
    Filed: June 1, 2020
    Date of Patent: May 18, 2021
    Assignee: Insilico Medicine IP Limited
    Inventors: Aleksandrs Zavoronkovs, Vladimir Aladinskiy, Aleksandr Aliper
  • Cyclopamine analogs
    Patent number: 11007181
    Abstract: The invention provides derivatives of cyclopamine having the following formula:
    Type: Grant
    Filed: July 24, 2019
    Date of Patent: May 18, 2021
    Assignee: Infinity Pharmaceuticals, Inc.
    Inventors: Brian Austad, Mark L. Behnke, Alfredo C. Castro, Michael J. Grogan, Somarajannair Janardanannair, Andre Lescarbeau, Stephane Peluso, Andre B. Charette, Martin R. Tremblay
  • Stereoselective synthesis of perhydro-3,6-dialkyl-2-benzo[b]furanones and analogs
    Patent number: 10995080
    Abstract: Synthetic methods of preparing perhydro-3,6-dimethyl-2-benzo[b]furanones, in particular dihydromintlactone, and analogs through reaction of dehydrogenation of menthanediols and analogs with a base in the presence of (carbonylchlorohydrido[bis-(2-diphenylphosphinoethyl)amine]ruthenium(II) as catalyst in good stereoselectivity and yields under stereochemistry controlled conditions are disclosed.
    Type: Grant
    Filed: May 28, 2020
    Date of Patent: May 4, 2021
    Assignee: INTERNATIONAL FLAVOR & FRAGRANCES INC.
    Inventors: Yigal Becker, Michael Cheskis
  • Compositions and methods for treatment of lung infections
    Patent number: 10993935
    Abstract: Methods of treating a bacterial lung infection are provided and comprise administering an effective amount of rifaximin to a subject in need thereof. The rifaximin can be delivered by inhalation therapy, such as by delivering the rifaximin in aerosol form. The rifaximin is administered alone or in combination with tobramycin, including in multiple doses. Methods of reducing biofilm formation are also provided and comprise contacting a bacteria with an effective amount of rifaximin. Pharmaceutical composition are also included and comprise rifaximin and a pharmaceutically-acceptable vehicle suitable for administering the rifaximin in aerosol form.
    Type: Grant
    Filed: June 3, 2019
    Date of Patent: May 4, 2021
    Assignee: MARSHALL UNIVERSITY RESEARCH CORPORATION
    Inventors: Hongwei Yu, Thomas Ryan Withers, Brandon Kirby
  • TLR inhibitors
    Patent number: 10988457
    Abstract: A method for inhibiting TLR7 and/or TLR8 receptors includes contacting the receptor with compound of general formula (I): wherein the meanings of the variables are explained in the specification, or a stereoisomeric form or a mixture of stereoisomeric forms, or pharmaceutically acceptable salts thereof. A pharmaceutical composition can include compounds of the invention, which can be used in a method for inhibiting TLR7 receptors and/or TLR8 receptors. The method can be performed by administering the compound to a subject to inhibit TLR7, TLR8, or TLR7/8 activity, which can be used to treat a disease or disorder associated with the receptors.
    Type: Grant
    Filed: April 28, 2020
    Date of Patent: April 27, 2021
    Assignee: INSILICO MEDICINE IP LIMITED
    Inventors: Aleksandrs Zavoronkovs, Vladimir Aladinskiy, Aleksandr Aliper
  • Iloperidone for the treatment of schizophrenia
    Patent number: 10987346
    Abstract: Aspects of the invention relate generally to the treatment of schizophrenia in an individual and, more specifically, to the treatment of an individual with iloperidone, an iloperidone metabolite, or a pharmaceutically-acceptable salt thereof. In one embodiment, the invention provides a method of preventing schizophrenic relapse in an individual diagnosed with schizophrenia, the method comprising: administering to the individual iloperidone, an iloperidone metabolite, or a pharmaceutically-acceptable salt thereof at a daily dose between about 12 mg and about 16 mg following a period in which the individual's schizophrenia was stabilized.
    Type: Grant
    Filed: September 6, 2019
    Date of Patent: April 27, 2021
    Assignee: Vanda Pharmaceuticals Inc.
    Inventors: Mihael H. Polymeropoulos, Curt D. Wolfgang
  • Histone deacetylase inhibitors
    Patent number: 10981933
    Abstract: This invention relates to generally inhibiting histone deacetylase (“HDAC”) enzymes (e.g., HDAC1, HDAC2, and HDAC3).
    Type: Grant
    Filed: March 12, 2019
    Date of Patent: April 20, 2021
    Assignee: BIOMARIN PHARMACEUTICAL INC.
    Inventors: Vincent Jacques, James R. Rusche, Norton P. Peet, Jasbir Singh
  • Compositions and methods comprising a compounded composition
    Patent number: 10973804
    Abstract: The present application relates to compounded compositions, methods of making compounded compositions, kits comprising compounded compositions, containers comprising compounded compositions, and methods of using compounded compositions. For example, disclosed herein are compounded compositions comprising an anti-fungal agent and methods of using a compounded composition to treat or prevent a fungal infection or a suspected fungal infection. 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 5, 2015
    Date of Patent: April 13, 2021
    Assignee: CMPD LICENSING, LLC
    Inventor: Jay Richard Ray, II
  • Urea derivative
    Patent number: 10968169
    Abstract: An object of the present invention is to find a novel pharmaceutical that has an excellent tryptophanase inhibitory effect, and suppresses worsening of renal function to preserve the kidney by reducing production of indoxyl sulfate in the blood. The present invention provides a pharmaceutical composition containing, as an active ingredient, a compound represented by the following formula, or a pharmacologically acceptable salt thereof: wherein R1 and R2 are the same or different, and represent a C1-C6 alkyl group or the like, and Ar represents an optionally substituted phenyl group or an optionally substituted thienyl group.
    Type: Grant
    Filed: October 5, 2017
    Date of Patent: April 6, 2021
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Tsuyoshi Soneda, Yuji Nakamura, Koji Matsumoto, Naomi Tanaka, Taichi Fukunaga
  • Ring-fused thiazolino 2-pyridones, methods for preparation thereof and their use in the treatment and/or prevention of tuberculosis
    Patent number: 10945999
    Abstract: The present disclosure provides a combination comprising: (i) a drug against tuberculosis, or a pharmaceutically acceptable salt thereof, and (ii) a compound of Formula II, or a pharmaceutically acceptable combination thereof. The combination may be used in the treatment and/or prevention of tuberculosis.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: March 16, 2021
    Assignees: QURETECH BIO AB, WASHINGTON UNIVERSITY IN SAINT LOUIS
    Inventors: Christina L. Stallings, Fredrik Almqvist, Kelly Flentie, James Arthur Dudley Good, Fritiof Ponten
  • Small molecule ferroptosis inducers
    Patent number: 10947188
    Abstract: The present invention provides, inter alia, a compound according to formula (I): Also provided are compositions containing a pharmaceutically acceptable carrier and a compound according to the present invention. Further provided are methods for regulating GPX4 in a cell and methods for inducing ferroptosis in a cell.
    Type: Grant
    Filed: June 18, 2019
    Date of Patent: March 16, 2021
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: Brent R. Stockwell, Kenichi Shimada, Rachid Skouta
  • Crystalline form of a 4-[2-(2-fluorophenoxymethyl)phenyl]piperidine compound
    Patent number: 10946006
    Abstract: The invention provides a crystalline hydrochloride salt of 4-[2-(2,4,6-trifluorophenoxymethyl)phenyl]piperidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
    Type: Grant
    Filed: January 16, 2020
    Date of Patent: March 16, 2021
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Lori Jean Patterson, Robert S. Chao, Miroslav Rapta
  • Enantiomerically purified GPER agonist for use in treating disease states and conditions
    Patent number: 10934277
    Abstract: The present disclosure provides 1) an enantiomerically purified compound SRR G-1, or a derivative thereof, including specific crystal forms, salts and co-crystals that modulates G protein-coupled estrogen receptor activity, 2) pharmaceutical and cosmetic compositions comprising an enantiomerically purified SRR G-1, or a derivative thereof, and 3) methods of treating or preventing disease states and conditions and cosmetic conditions mediated through these receptors and related methods thereof in humans and animals.
    Type: Grant
    Filed: November 13, 2019
    Date of Patent: March 2, 2021
    Assignee: LINNAEUS THERAPEUTICS, INC.
    Inventors: Christopher Natale, Patrick T. Mooney, Tina Garyantes, Wayne Luke
  • Process for preparation of boscalid anhydrate form I and boscalid anhydrate form II
    Patent number: 10934259
    Abstract: The present invention relates to a novel process for preparation of boscalid anhydrate form I and boscalid anhydrate form II.
    Type: Grant
    Filed: September 26, 2017
    Date of Patent: March 2, 2021
    Assignee: UPL LIMITED
    Inventors: Digish Manubhai Panchal, Rakesh Bhulabhai Patel, Jaidev Rajnikant Shroff, Vikram Rajnikant Shroff
  • Treating infections with ceftolozane/tazobactam in subjects having impaired renal function
    Patent number: 10933053
    Abstract: Disclosed are methods of administering cephalosporin/tazobactam to human patients with end stage renal disease undergoing hemodialysis and suffering from a complicated intra-abdominal infection or a complicated urinary tract infection.
    Type: Grant
    Filed: July 29, 2019
    Date of Patent: March 2, 2021
    Assignee: MERCK SHARP & DOHME CORP.
    Inventors: Gopal Krishna, Gurudatt Chandorkar, Elham Hershberger, Benjamin Miller, Alan Xiao
  • Methods of treating cochlear synaptopathy
    Patent number: 10925872
    Abstract: The present application describes the use of gamma secretase inhibitors and gamma secretase modulators for the treatment of cochlear synaptopathy.
    Type: Grant
    Filed: December 12, 2017
    Date of Patent: February 23, 2021
    Assignee: Pipeline Therapeutics, Inc.
    Inventors: Daniel Scott Lorrain, Michael Ming-Yuan Poon, Karin Joy Stebbins