Patents Examined by D Margaret M Seaman
  • Patent number: 10774068
    Abstract: Disclosed herein are compounds, compositions, and methods of their use for the treatment of diabetes.
    Type: Grant
    Filed: June 24, 2016
    Date of Patent: September 15, 2020
    Assignees: THE SCRIPPS RESEARCH INSTITUTE, UNIVERSITÄT BREMEN
    Inventors: Hank Michael James Petrassi, Murali Mohan Reddy Peram Surakattula, Kathrin Maedler, Amin Ardestani, Jason T. Roland, Tyler D. Baguley, Matthew S. Tremblay, Weijun Shen, Peter G. Schultz, Arnab K. Chatterjee
  • Patent number: 10766925
    Abstract: The present invention provides compounds that can modulate opioid receptors. Some compounds of the invention are modulators of ?- and/or ?-opioid receptors. Still other compounds of the invention are opioid receptor antagonists. Some compounds of the invention can modulate opioid receptors with a significantly less likelihood of developing addiction or abuse compared to conventional opioid ligands, such as morphine. In particular, compounds of the invention are of the formula: wherein Ar1 is H, optionally substituted aryl or optionally substituted heteroaryl; R1 is a heteroalkyl; R2 is alkyl; R3 is an oligopeptide or a moiety of the formula —R4—Y; R4 is alkylene; Y is optionally substituted heteroaryl, optionally substituted aryl or a moiety of the formula —C(?X2)—X3—R5; each of X1, X2 and X3 is independently O, NR6 or S; and each of R5 and R6 is independently H or alkyl.
    Type: Grant
    Filed: April 11, 2017
    Date of Patent: September 8, 2020
    Assignee: Arizona Board of Regents on behalf of the University of Arizona
    Inventors: Ruben Vardanyan, Victor Hruby
  • Patent number: 10766862
    Abstract: Disclosed are a crystal form and a salt form of and a preparation method for a tyrosine kinase inhibitor.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: September 8, 2020
    Assignee: Guangdong Raynovent Biotech Co., Ltd.
    Inventors: Chaofeng Long, Zhengxia Chen, Xiaoxin Chen, Yang Zhang, Zhuowei Liu, Shuhui Chen, Jian Li
  • Patent number: 10759762
    Abstract: There are described novel compounds of formula I: which R1, R2, R3, R4, R5, R6, R7, R8, R9 and R10 are each as herein defined.
    Type: Grant
    Filed: October 9, 2015
    Date of Patent: September 1, 2020
    Assignee: HIGH FORCE RESEARCH LIMITED
    Inventors: Andrew Whiting, Todd Marder
  • Patent number: 10738009
    Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: 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.
    Type: Grant
    Filed: August 21, 2018
    Date of Patent: August 11, 2020
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Sabina Hadida Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
  • Patent number: 10730852
    Abstract: To provide an industrial method for producing a 5-alkynyl pyridine compound at a high yield. A method for producing a compound represented by the formula (3), which comprises reacting a 5-chloropyridine compound represented by the formula (1) and an alkyne compound represented by the formula (2) by using sodium carbonate or sodium hydrogen carbonate in the presence of a palladium catalyst having phosphine ligands: (in the formula (2), R is a hydrogen atom, a C1-C6 alkyl or a C3-C7 cycloalkyl).
    Type: Grant
    Filed: June 14, 2019
    Date of Patent: August 4, 2020
    Assignee: Nissan Chemical Corporation
    Inventors: Hirohisa Saito, Shinji Iba, Yukiko Ebihara
  • Patent number: 10730864
    Abstract: The present invention includes novel RAD51 inhibitors. The compounds of the invention may be useful in preventing or treating cancer in a subject in need thereof. The present invention also includes methods of preventing or treating cancer in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.
    Type: Grant
    Filed: August 20, 2019
    Date of Patent: August 4, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Jiewen Zhu, Wen-Hwa Lee, Hongyuan Chen, Xuning Guo, Xiao-Long Qiu
  • Patent number: 10703748
    Abstract: Diazanaphthalene compounds for treating various diseases and pathologies are disclosed. More particularly, the present disclosure concerns the use of a diazanaphthalene compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, Alzheimer's disease, lung disease, inflammation, auto-immune diseases and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as neurological conditions/disorders/diseases linked to overexpression of DYRK1A.
    Type: Grant
    Filed: October 31, 2018
    Date of Patent: July 7, 2020
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar Kc, Chi Ching Mak, Jianguo Cao, Venkataiah Bollu, Chandramouli Chiruta, Gopi Kumar Mittapalli, Brian Walter Eastman, Brian Joseph Hofilena
  • Patent number: 10703764
    Abstract: The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein X, Y, Z, R1, R2, R4 and R7 are defined herein.
    Type: Grant
    Filed: June 18, 2019
    Date of Patent: July 7, 2020
    Assignee: Forma Therapeutics, Inc.
    Inventors: Kenneth W. Bair, Torsten Herbertz, Goss S. Kauffman, Katherine J. Kayser-Bricker, George P. Luke, Matthew W. Martin, David S. Millan, Shawn E. R. Schiller, Adam C. Talbot, Mark J. Tebbe
  • Patent number: 10696662
    Abstract: The present invention is directed to 5-fluoro-C-(aryl or hetercyclyl)-glycoside derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by SGLT activity, more particularly dual SGLT1/2 activity.
    Type: Grant
    Filed: August 21, 2018
    Date of Patent: June 30, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Guozhang Xu, Gee-Hong Kuo, Micheal Gaul
  • Patent number: 10689356
    Abstract: Compounds having activity as inhibitors of G12C mutant KRAS protein are provided. The compounds have the following structure (I): or a pharmaceutically acceptable salt, tautomer, stereoisomer or prodrug thereof, wherein A, R1, R3a, R3b, R4a, R4b, G2, G3, G4, m1, m2, m3, m4, L1, L2 and E are as defined herein. Methods associated with preparation and use of such compounds, pharmaceutical compositions comprising such compounds and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, are also provided.
    Type: Grant
    Filed: September 28, 2016
    Date of Patent: June 23, 2020
    Assignee: ARAXES PHARMA LLC
    Inventors: Liansheng Li, Jun Feng, Yun Oliver Long, Yuan Liu, Pingda Ren, Yi Liu
  • Patent number: 10675268
    Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
    Type: Grant
    Filed: November 2, 2018
    Date of Patent: June 9, 2020
    Assignee: Centrexion Therapeutics Corporation
    Inventors: Riccardo Giovannini, Yunhai Cui, Henri Doods, Marco Ferrara, Stefan Just, Raimund Kuelzer, Iain Lingard, Rocco Mazzaferro, Klaus Rudolf
  • Patent number: 10676454
    Abstract: A process produces a (meth)acrylate ester mixture. The process includes reacting a glycerol formal isomer mixture with an alkyl (meth)acrylate in the presence of a catalyst.
    Type: Grant
    Filed: January 30, 2017
    Date of Patent: June 9, 2020
    Assignee: Evonik Operations GmbH
    Inventors: Silvia Beyer, Gaurang Dave, Hans-Jürgen Dillmann, Volker Herzog, Joachim Knebel, Ralf Merbach, Thorben Schütz, Martin Trocha, Sabine Kömmelt, Patrik Hartmann
  • Patent number: 10669291
    Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
    Type: Grant
    Filed: January 7, 2019
    Date of Patent: June 2, 2020
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventors: Tsutomu Akama, Eric Easom, Yvonne Freund, Jacob J. Plattner, Jessica Sligar, Daitao Chen, Jennifer Freeman, Joe Perales
  • Patent number: 10660884
    Abstract: The present invention provides compositions and methods for providing controllable local delivery of a conjugate of chloroquine (CQ) and a bisphosphonate to treat diseases characterized by abnormal bone metabolism. In certain embodiments, the invention is used as a treatment for a subject with diseases and disorders characterized by bone loss.
    Type: Grant
    Filed: November 2, 2016
    Date of Patent: May 26, 2020
    Assignee: University of Rochester
    Inventors: Robert Boeckman, Brendan Boyce, Lifeng Xiao, Zhenqiang Yao, Frank H. Ebetino
  • Patent number: 10662200
    Abstract: The present invention relates to compounds of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the beta-3 adrenergic receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of a beta-3 adrenergic receptor-mediated disorder, such as, heart failure; cardiac performance in heart failure; mortality, reinfarction, and/or hospitalization in connection with heart failure; acute heart failure; acute decompensated heart failure; congestive heart failure; severe congestive heart failure; organ damage associated with heart failure (e.g.
    Type: Grant
    Filed: September 6, 2019
    Date of Patent: May 26, 2020
    Assignee: Arena Pharmaceuticals, Inc.
    Inventors: Thuy-Anh Tran, Quyen-Quyen Do, Brett Ullman, Anthony C. Blackburn, Maiko Nagura
  • Patent number: 10662192
    Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator, compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.
    Type: Grant
    Filed: June 12, 2018
    Date of Patent: May 26, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Sara Hadida-Ruah, Anna Hazlewood, Peter Grootenhuis, Fredrick Van Goor, Ashvani Singh, Jinglan Zhou, Jason McCartney
  • Patent number: 10654866
    Abstract: Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, wherein either R1 or R2 is independently selected from Cl, F, —CF3, or —CH3, and the other is hydrogen, and methods for their use are provided.
    Type: Grant
    Filed: July 11, 2019
    Date of Patent: May 19, 2020
    Assignee: Eli Lilly and Company
    Inventors: Jolie Anne Bastian, Jeffrey Daniel Cohen, Almudena Rubio, Daniel Jon Sall
  • Patent number: 10654844
    Abstract: Provided are compounds that are inhibitors of both rho kinase and of a monoamine transporter (MAT) act to improve the disease state or condition. Further provided are compositions comprising the compounds. Further provided are methods for treating diseases or conditions, the methods comprising administering compounds according to the invention. One such disease may be glaucoma for which, among other beneficial effects, a marked reduction in intraocular pressure (IOP) may be achieved.
    Type: Grant
    Filed: June 7, 2019
    Date of Patent: May 19, 2020
    Assignee: Aerie Pharmaceuticals, Inc.
    Inventors: Mitchell A. deLong, Jill Marie Sturdivant, Susan M. Royalty
  • Patent number: 10646494
    Abstract: The present invention relates to novel Heterocycle-Substituted Tetracyclic Compounds of Formula (I): (I) and pharmaceutically acceptable salts thereof, wherein A, A?, R2 R3 and R5 are as defined herein. The present invention also relates to compositions comprising at least one Heterocycle-Substituted Tetracyclic Compound, and methods of using the Heterocycle-Substituted Tetracyclic Compounds for treating or preventing HCV infection in a patient.
    Type: Grant
    Filed: August 14, 2017
    Date of Patent: May 12, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wensheng Yu, Ling Tong, Joseph A. Kozlowski, Craig A. Coburn, De-Yi Yang, Deyou Sha, Jae-Hun Kim, Michael Dwyer, Kartik M Keertikar, Bin Hu, Bin Zhong, Jinglai Hao, Dahai Wang