Patents Examined by Zinna Northington
  • Acetate salt of buprenorphine and methods for preparing buprenorphine
    Patent number: 10874662
    Abstract: The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further provides method of preparing the acetate salts, buprenorphine free base prepared from the acetate salts, other salts prepared from the free base, and pharmaceutical compositions thereof essentially free of impurities.
    Type: Grant
    Filed: June 19, 2019
    Date of Patent: December 29, 2020
    Assignee: Rhodes Technologies
    Inventors: C. Frederick Huntley, Erik Wayne Kataisto, Helge Alfred Reisch, Archana Sharma
  • Method for manufacturing 1,3-dioxane-5-one
    Patent number: 10870643
    Abstract: The present invention relates to a method for producing a 1,3-dioxan-5-one by a short-step and simple method from raw materials that are procurable easily and inexpensively, using, as a raw material, a 1,3-dioxane that is a mixture containing a 1,3-dioxolane. Provided is a method for producing a 1,3-dioxan-5-one, including using a mixture of a compound represented by the following formula (I) and a compound represented by the following formula (II) as a raw material, the method including a step of oxidizing the mixture under an oxidative esterification condition (step 2): wherein, in the formulae (I) and (II), R1 and R2 each independently represent a hydrogen atom or a monovalent hydrocarbon group, or R1 and R2 are bonded to each other to form a divalent hydrocarbon group for constituting a ring structure.
    Type: Grant
    Filed: December 26, 2017
    Date of Patent: December 22, 2020
    Assignee: KAO CORPORATION
    Inventor: Takashi Aoki
  • Composition and methods of use of tetrahydroisoquinoline small molecules to bind and modulate PCSK9 protein activity
    Patent number: 10865185
    Abstract: This invention is related to the field of PCSK9 biology and the composition and methods of use of small organic compounds as ligands for modulation of PCSK9 biological activity. In particular, the invention provides compositions of small organic compounds that modulate circulating levels of low density lipoproteins by altering the conformation of the protein PCSK9. Binding these small organic compound 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 organic compound ligands that can raise LDL levels.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: December 15, 2020
    Assignee: SRX Cardio, LLC
    Inventors: Thomas E. Barta, Jonathan William Bourne, Kyle D. Monroe, Michael M. Muehlemann, Anjali Pandey, Simeon Bowers
  • Inhibitors for soluble epoxide hydrolase (SEH) and fatty acid amide hydrolase (FAAH)
    Patent number: 10858338
    Abstract: The present invention provides compounds that are dual inhibitors of soluble epoxide hydrolase and fatty acid amide hydrolase. The present invention also provides methods of using the compounds to inhibit soluble epoxide hydrolase and fatty acid amide hydrolase, and to treat cancer.
    Type: Grant
    Filed: March 14, 2017
    Date of Patent: December 8, 2020
    Assignee: The Regents of the University of California
    Inventors: Bruce Hammock, Sean Kodani
  • S1PR2 antagonists and uses therefor
    Patent number: 10858358
    Abstract: Methods and compositions are provided for the treatment of familial exudative vitreoretinopathy (FEVR) through the administration of a therapeutically effective amount of a sphingosine-1-phosphate receptor type 2 (S1PR2) antagonist. Also provided herein are (Z)-2-cyano-1-(2,6-dichloropyridin-4-yl)-3-((4-isopropyl-1,3-dimethyl-1H-pyrazolo[3,4-b]pyridin-6-yl)methyl)guanidine and analogs thereof, and their use in treating retinopathies and diseases characterized by insufficient angiogenesis.
    Type: Grant
    Filed: September 27, 2019
    Date of Patent: December 8, 2020
    Assignee: DALHOUSIE UNIVERSITY
    Inventors: Christopher McMaster, Gordon Simms
  • Ethane-sulfonate salt of quinoline derivative
    Patent number: 10836747
    Abstract: The present invention relates to an ethane-sulfonate salt of N-{5-[(6,7-dimethoxy-4-quinolinyl)oxy]-2-pyridinyl}-2,5-dioxo-1-phenyl-1,2,5,6,7,8-hexahydro-3-quinolinecarboxamide, which has an Axl-inhibiting activity and is useful as a prophylactic and/or therapeutic agent for immune diseases, cancer and the like, a crystal thereof, and a pharmaceutical composition thereof.
    Type: Grant
    Filed: January 25, 2018
    Date of Patent: November 17, 2020
    Assignee: ONO PHARMACEUTICAL CO., LTD.
    Inventors: Takahiro Nekado, Hideomi Kijima, Shizuka Ono, Toshihiko Nishiyama
  • Acetate salt of buprenorphine and methods for preparing buprenorphine
    Patent number: 10835528
    Abstract: The present disclosure provides acetate salts of buprenorphine, and its anhydrates, solvates, hydrates, and crystalline forms thereof, where the acetate salts of buprenorphine are essentially free of impurities. The disclosure further provides method of preparing the acetate salts, buprenorphine free base prepared from the acetate salts, other salts prepared from the free base, and pharmaceutical compositions thereof essentially free of impurities.
    Type: Grant
    Filed: June 19, 2019
    Date of Patent: November 17, 2020
    Assignee: Rhodes Technologies
    Inventors: C. Frederick M. Huntley, Erik Wayne Kataisto, Helge Alfred Reisch, Archana Sharma
  • 5 to 7 membered heterocyclic amides as JAK inhibitors
    Patent number: 10836763
    Abstract: The invention provides compounds of formula (I): where the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are useful as JAK kinase inhibitors. The invention also provides pharmaceutical compositions comprising such compounds and methods of using such compounds to treat respiratory diseases.
    Type: Grant
    Filed: September 3, 2019
    Date of Patent: November 17, 2020
    Assignee: Theravance Biopharma R&D IP, LLC
    Inventors: Daniel D. Long, Cameron Smith, Corbin Thompson
  • Method for producing heterocyclic compound
    Patent number: 10829474
    Abstract: The present invention provides a production method of heterocyclic compound having an excellent CH24H inhibitory action, which is suitable for industrial production. In the present invention, a 2-halogenonicotinic acid or a reactive derivative thereof or a salt thereof is reacted with 4-benzyl-4-hydroxypiperidine acid addition salt to give a (4-benzyl-4-hydroxypiperidin-1-yl) (2-halogenopyridin-3-yl)methanone or a salt thereof, and then the obtained compound is reacted with pyridine-4-boronic acid or a reactive derivative thereof or a salt thereof in the presence of a metal catalyst and a base to give (4-benzyl-4-hydroxypiperidin-1-yl) (2,4?- bipyridin-3-yl)methanone or a salt thereof.
    Type: Grant
    Filed: February 6, 2020
    Date of Patent: November 10, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Fumiya Komura, Yoshihiro Higuchi
  • Substituted pyridinone-containing trycyclic compounds, and methods using same
    Patent number: 10821103
    Abstract: The present invention includes substituted pyridinone-containing tricyclic compounds, and compositions comprising the same, that can be used to treat or prevent hepatitis B virus (HBV) infection in a patient. In certain embodiments, the compounds and compositions of the invention inhibit and/or reduce HBsAg secretion.
    Type: Grant
    Filed: November 3, 2017
    Date of Patent: November 3, 2020
    Assignee: Arbutus Biopharma Corporation
    Inventors: Laurèn Danielle Bailey, Yingzhi Bi, Shuai Chen, Bruce D. Dorsey, Dimitar B. Gotchev, Richard James Holland, Ramesh Kakarla, Duyan Nguyen, Mark Christopher Wood
  • WDR5-MLL1 inhibitors and modulators
    Patent number: 10807959
    Abstract: Benzamides and picolinamides that are meta-substituted with imino-, guanidino-, or heterocycle-containing groups disrupt the WDR5-MLL1 protein-protein interaction, and have use in pharmaceutical compositions and in treating proliferative disorders and conditions in a subject, such as cancer.
    Type: Grant
    Filed: August 16, 2019
    Date of Patent: October 20, 2020
    Assignee: Vanderbilt University
    Inventors: Rocco D. Gogliotti, Shaun R. Stauffer, KyuOk Jeon, James M. Salovich, Jonathan D. Macdonald, Jonathan J. Mills, Kenneth M. Meyers, Joseph R. Alvarado, Changho Han, Stephen W. Fesik, Taekyu Lee
  • Dihydrochromene derivatives
    Patent number: 10807993
    Abstract: The present invention relates to the compound of formula (I) wherein R1A, R1B, R1C, and R1D are hydrogen atom, etc., R2A and R2B are hydrogen atom, etc., R3A, R3B, R3C, and R3D are hydrogen atom, etc., L is bond, etc., V is C1-6 alkylene, Q is optionally-substituted imidazole, or a pharmaceutically acceptable salt thereof, as a novel anti-tumor agent that targets CSCs which are thought to be closely involved in the persistent proliferation of malignant tumor, metastasis or recurrence of cancer, and resistance to anti-tumor agents.
    Type: Grant
    Filed: March 3, 2020
    Date of Patent: October 20, 2020
    Assignee: Sumitomo Dainippon Pharma Co., Ltd.
    Inventors: Hitoshi Ban, Seiji Kamioka, Yusuke Sawayama, Miki Hashizume
  • Carboxamide compounds and uses thereof
    Patent number: 10800761
    Abstract: Disclosed are compounds of Formula (I?) methods of using the compounds for inhibiting HPK1 activity and pharmaceutical compositions comprising such compounds. The compounds are useful in treating, preventing or ameliorating diseases or disorders associated with HPK1 activity such as cancer.
    Type: Grant
    Filed: February 19, 2019
    Date of Patent: October 13, 2020
    Assignee: Incyte Corporation
    Inventors: Oleg Vechorkin, Jun Pan, Alexander Sokolsky, Evan Styduhar, Wenqing Yao
  • Acetophenone compound, preparation method therefor, and application thereof in blood lipid regulation
    Patent number: 10800733
    Abstract: Disclosed are a compound represented by Formula I or a pharmaceutically acceptable salt thereof, a preparation method therefor, the Formula I, and an application thereof in preparing drugs for regulating blood lipids.
    Type: Grant
    Filed: March 15, 2018
    Date of Patent: October 13, 2020
    Assignee: Shanghai Bioenergy Medicine Science & Technology Co., Ltd.
    Inventors: Yuqiong Dong, Quanhai Liu, Yu Shen, Wentao Cai
  • Quinoline compound, preparation method and medical use therefor
    Patent number: 10800741
    Abstract: The present invention relates to a quinoline compound, as well as a preparation method and medical use therefor. Specifically, the present invention relates to a novel quinolone compound represented by the general formula (I) and a method for preparing the same, as well as a use therefor as an inhibitor for a plurality of protein kinases, and a use in the prevention and/or treatment of cancer in particular; the definition of each group in the general formula (I) is the same as the definition in the description.
    Type: Grant
    Filed: February 6, 2018
    Date of Patent: October 13, 2020
    Assignee: Ancureall Pharmaceutical (Shanghai) Co., Ltd.
    Inventors: Jutong Si, Meifeng Jiang, Jiayan Li, Han Zeng, Huabin Yang
  • Abiraterone prodrugs
    Patent number: 10792292
    Abstract: Sustained-release abiraterone prodrug formulations, methods, and kits for parenteral administration to a subject having a sex hormone-dependent benign or malignant disorder such as prostate cancer, a syndrome due to androgen excess, and/or a syndrome due to glucocorticoid excess such as hypercortisolemia.
    Type: Grant
    Filed: March 4, 2020
    Date of Patent: October 6, 2020
    Assignee: Propella Therapeutics, Inc.
    Inventors: Matthew J. Sharp, William R. Moore, Jr.
  • Bicyclic-fused heteroaryl or aryl compounds
    Patent number: 10793579
    Abstract: Compounds, tautomers and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula Ia, as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.
    Type: Grant
    Filed: May 14, 2019
    Date of Patent: October 6, 2020
    Assignee: Pfizer Inc.
    Inventors: John David Trzupek, Katherine Lin Lee, Mark Edward Bunnage, Seungil Han, David Hepworth, Frank Eldridge Lovering, John Paul Mathias, Nikolaos Papaioannou, Betsy Susan Pierce, Joseph Walter Strohbach, Stephen Wayne Wright, Christoph Wolfgang Zapf, Lori Krim Gavrin, Arthur Lee, David Randolph Anderson, Kevin Joseph Curran, Christoph Martin Dehnhardt, Eddine Saiah, Joel Adam Goldberg, Xiaolun Wang, Horng-Chih Huang, Richard Vargas, Michael Dennis Lowe, Akshay Patny
  • TYK2 inhibitors and uses thereof
    Patent number: 10793574
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same for the inhibition of TYK2, and the treatment of TYK2-mediated disorders.
    Type: Grant
    Filed: April 30, 2019
    Date of Patent: October 6, 2020
    Assignee: Nimbus Lakshmi, Inc.
    Inventors: Jeremy Robert Greenwood, Geraldine C. Harriman, Silvana Marcel Leit de Moradei, Craig E. Masse, Thomas H. McLean, Sayan Mondal
  • Prodrugs of pyridone amides useful as modulators of sodium channels
    Patent number: 10787472
    Abstract: The invention relates to prodrug compounds of formula I: wherein R2, R3, R5, R7 and X are as defined herein. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain. The compounds of formula I possess advantageous solubility and physicochemical properties.
    Type: Grant
    Filed: February 25, 2019
    Date of Patent: September 29, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Corey Anderson, Sara Sabina Hadida Ruah, Julian Marian Charles Golec, Beili Zhang, Benjamin Joseph Littler, Ali Keshavarz-Shokri, Tim Edward Alcacio, Daniel T. Belmont
  • Pharmaceutical compounds
    Patent number: 10787447
    Abstract: This invention relates to compounds that are agonists of the muscarinic M1 and/or M4 receptor and which are useful in the treatment of diseases mediated by the muscarinic M1 and M4 receptors. Also provided are pharmaceutical compositions containing the compounds and the therapeutic uses of the compounds. Compounds provided are of formula where Y, R1, R2 and R4 are as defined herein.
    Type: Grant
    Filed: June 24, 2019
    Date of Patent: September 29, 2020
    Assignee: Heptares Therapeutics Limited
    Inventors: Giles Albert Brown, Barry John Teobald, Benjamin Gerald Tehan