Patents Examined by Laura L. Stockton
  • IRE1 small molecule inhibitors
    Patent number: 11021466
    Abstract: Provided herein are small molecule inhibitors for the targeting or IRE1 protein family members. Binding may be direct or indirect. Further provided herein are methods of using IRE1 small molecule inhibitors for use in treating or ameliorating cancer in a subject. Moreover, IRE1 small molecule inhibitors described herein are for the treatment of cancer, where the cancer is a solid or hematologic cancer.
    Type: Grant
    Filed: August 16, 2019
    Date of Patent: June 1, 2021
    Assignee: Cornell University
    Inventors: Joseph P. Vacca, Dansu Li, Sarah Bettigole
  • Azetidine derivative
    Patent number: 11014943
    Abstract: Disclosed in the present application are a compound represented by formula (I), or a pharmaceutically acceptable salt, a tautomer thereof, a stereoisomer thereof, or a geometrical isomer thereof, and uses thereof in the preparation of drugs for treating or preventing multiple myeloma.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: May 25, 2021
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP GO., LTD.
    Inventors: Jian Xiong, Cheng Xie, Kevin X Chen, Xiongbin Xu, Xuejin Zhang, Zhen Gong, Jian Li, Shuhui Chen, Aiming Zhang, Zhulian Jiang, Xiquan Zhang, Xin Tian
  • LSD1 inhibitors and medical uses thereof
    Patent number: 11013718
    Abstract: Provided are novel compounds of Formula (I or Ia?): and pharmaceutically acceptable salts thereof, which are useful for treating a variety of diseases, disorders or conditions, associated with LSD1. Also provided are pharmaceutical compositions comprising the novel compounds of Formula (I or Ia?), pharmaceutically acceptable salts thereof, and methods for their use in treating one or more diseases, disorders or conditions, associated with LSD1.
    Type: Grant
    Filed: November 1, 2019
    Date of Patent: May 25, 2021
    Assignee: Constellation Pharmaceuticals, Inc.
    Inventors: Francois Brucelle, Victor S. Gehling, Avinash Khanna
  • Hepatitis B capsid assembly modulators
    Patent number: 11014881
    Abstract: Described herein are hepatitis B capsid assembly modulators and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for the treatment of hepatitis B.
    Type: Grant
    Filed: November 1, 2019
    Date of Patent: May 25, 2021
    Assignee: VENATORX PHARMACEUTICALS, INC.
    Inventors: Christopher J. Burns, Glen Coburn, Bin Liu, Jiangchao Yao, Christopher Benetatos, Steven A. Boyd, Stephen M. Condon, Thomas Haimowitz
  • Potassium salt of benzimidazole compound and preparation method therefor, composition and application thereof
    Patent number: 11008311
    Abstract: The preparation method for the compound, composition and application thereof in preparing an angiotensin II receptor antagonist or application in preparing medicine for preventing and/or treating hypertension, chronic heart failure and diabetic nephropathy. After entering a human body, when releasing azilsartan, the compound releases hydroxyligustrazine or NO at the same time, thus generating a synergistic effect with azilsartan. The compound therefore has stronger and longer blood pressure lowering effect, more obvious and longer lasting heart rate lowering effect and high safety, and achieves ideal protective effect for heart and kidney functions.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: May 18, 2021
    Assignee: WUHAN LL SCIENCE AND TECHNOLOGY DEVELOPMENT CO., LTD.
    Inventors: Sijun Lei, Xiang Fang, Yongkai Chen, Wei Feng, Chaodong Wang
  • Crystal form of URAT1 inhibitor, and preparation method therefor
    Patent number: 10995087
    Abstract: Disclosed are a crystal form of a URAT1 inhibitor, and a preparation method therefor.
    Type: Grant
    Filed: November 20, 2018
    Date of Patent: May 4, 2021
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Jianfei Wang, Yang Zhang, Wenyuan Zhu, Jian Li, Shuhui Chen
  • Zaindole derivatives and their use as ERK kinase inhibitors
    Patent number: 10995089
    Abstract: The present invention concerns a compound of formula (I): H or one of its pharmaceutically acceptable salts, especially for use as inhibitors of the ERK kinase activity in particular ERK2 activity, it also concerns prodrugs of these compounds.
    Type: Grant
    Filed: November 17, 2016
    Date of Patent: May 4, 2021
    Assignees: AGV DISCOVERY, INSTITUT NATIONAL DE LA SANTE ET DE LA RECHERCHE MEDICALE (INSERM), CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE MONTPELLIER
    Inventors: Jean-François Guichou, Cédric Bories, Clément Geoffroy, Charline Duquenne, Muriel Gelin, Gilles Labesse, Yannick Bessin, Loic Mathieu
  • Treatment of Fabry disease
    Patent number: 10995067
    Abstract: Disclosed herein are novel uses of a polyhydroxylated pyrrolidine for the manufacture of a medicament for treating Fabry disease (FD). Accordingly, the present disclosure provides a method of treating a subject having or suspected of having FD. The method includes the step of, administering to the subject a therapeutically effective amount of a compound of formula (I), a salt, an ester or a solvate thereof, wherein: R1 is H, or C1-3 amine optionally substituted with —COR2; R2 is alkyl or alkene optionally substituted with cycloalkyl or phenyl having at least one substituent selected from the group consisting of, halo, alkyl, haloalkyl, and alkoxyl; so as to ameliorate, alleviate mitigate and/or prevent symptoms associated with the FD. According to preferred embodiments of the present disclosure, the compound of formula (I) is a chaperon of a mutated human lysosomal ?-galactosidase A (?-Gal A).
    Type: Grant
    Filed: June 14, 2017
    Date of Patent: May 4, 2021
    Assignee: ACADEMIA SINICA
    Inventor: Wei-Chieh Cheng
  • Glucose uptake inhibitors
    Patent number: 10988484
    Abstract: Provided herein are compounds that modulate glucose uptake activity and are useful for treating cancer, autoimmune diseases, inflammation, infectious diseases, and metabolic diseases. In certain embodiments, the compounds modulate glucose uptake activity by modulating cellular components, including, but not limited to those related to glycolysis and the known transporters/co-transporters of glucose such as GLUT1 and other GLUT family members/alternative hexose transporters. In certain embodiments, the compounds have the structure of formula I: wherein the variables have the values disclosed herein.
    Type: Grant
    Filed: April 29, 2019
    Date of Patent: April 27, 2021
    Assignee: Kadmon Corporation, LLC
    Inventors: Kellen L. Olszewski, Ji-In Kim, Masha V. Poyurovsky, Kevin G. Liu, Anthony Barsotti, Koi Morris
  • CXCR4 inhibitors and uses thereof
    Patent number: 10988465
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: June 21, 2017
    Date of Patent: April 27, 2021
    Assignee: X4 PHARMACEUTICALS, INC.
    Inventors: Elyse Marie Josee Bourque, Renato Skerlj
  • Heterocyclic derivatives useful as SHP2 inhibitors
    Patent number: 10988466
    Abstract: This invention relates to certain novel pyrazine derivatives (Formula I) as SHP2 inhibitors which is shown as formula I, their synthesis and their use for treating a SHP2 mediated disorder. More particularly, this invention is directed to fused heterocyclic group derivatives useful as inhibitors of SHP2, methods for producing such compounds and methods for treating a SHP2-mediated disorder.
    Type: Grant
    Filed: March 23, 2018
    Date of Patent: April 27, 2021
    Assignee: Jacobio Pharmaceuticals Co., Ltd.
    Inventors: Cunbo Ma, Panliang Gao, Shaojing Hu, Zilong Xu, Huifeng Han, Xinping Wu, Di Kang
  • Spiro compound and use thereof
    Patent number: 10981900
    Abstract: The present disclosure relates to a series of tricyclic compounds and the use thereof as receptor agonists of sphingosine-1-phosphate subtype 1 (S1P1), and in particular relates to compounds as shown in formula (I) or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: February 28, 2018
    Date of Patent: April 20, 2021
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Peng Zhang, Lingyun Wu, Jun Yin, Jian Li, Shuhui Chen
  • Heterocyclic amides useful as protein modulators
    Patent number: 10975287
    Abstract: Disclosed are compounds having the formula: wherein Ra, R1, R2, R3, R4, R5, R6, R7, and R8, are as defined herein, or a salt, particularly a pharmaceutically acceptable salt, thereof.
    Type: Grant
    Filed: April 5, 2017
    Date of Patent: April 13, 2021
    Inventors: Adam Kenneth Charnley, Michael G. Darcy, Jason W. Dodson, Terry V. Hughes, Yue Li, Yiqian Lian, Neysa Nevins, Joshi M. Ramanjulu
  • Fused indazole pyridone compounds as antivirals
    Patent number: 10975078
    Abstract: The invention provides compounds of Formula (I) as described herein, along with pharmaceutically acceptable salts, pharmaceutical compositions containing such compounds, and methods to use these compounds, salts and compositions for treating viral infections, particularly infections caused by hepatitis B virus, and reducing the occurrence of serious conditions associated with HBV.
    Type: Grant
    Filed: March 4, 2020
    Date of Patent: April 13, 2021
    Assignee: NOVARTIS AG
    Inventors: Jiping Fu, Wooseok Han, Subramanian Karur, Peichao Lu, Keith Bruce Pfister, Joseph Michael Young
  • Diamino-alkylamino-linked arylsulfonamide compounds with selective activity in voltage-gated sodium channels
    Patent number: 10968210
    Abstract: Disclosed are compounds of Formula A, or a salt thereof: Formula (A), wherein: Het, Q and R1A to R4A are defined herein, which compounds have properties for blocking Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating cough, itch, acute pain and neuropathic pain disorders using the same.
    Type: Grant
    Filed: November 13, 2017
    Date of Patent: April 6, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas J. Greshock, James Mulhearn, Anthony J. Roecker, Tianying Jian, Gang Zhou, Liangqin Guo, Walter Won, Ting Zhang, Rajan Anand, John E. Stelmach, Deping Wang, Ronald M. Kim, Mark E. Layton, Christopher S. Burgey, Philippe G. Nantermet
  • Oxazole derivatives for use in the treatment of cancer
    Patent number: 10961234
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, wherein: •B is an aryl or heteroaryl group optionally substituted by one or more R10 groups; and *X is selected from 0, (CR11R12)p and (CR11R12)p CO. Said compounds are capable of inhibiting PAICS and are useful in the treatment of proliferative disorders. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (I).
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: March 30, 2021
    Assignee: LIFEARC
    Inventors: Simon Osborne, Jonathan Large
  • TGF beta receptor antagonists
    Patent number: 10961239
    Abstract: The invention relates generally to compounds of formula (I) that modulate the activity of TGF?R-1 and TGF?R-2, pharmaceutical compositions containing said compounds and methods of treating proliferative disorders and disorders of dysregulated apoptosis, such as cancer, utilizing the compounds of the invention.
    Type: Grant
    Filed: January 3, 2018
    Date of Patent: March 30, 2021
    Assignee: Bristol-Myers Squibb Company
    Inventors: Robert M. Borzilleri, Upender Velaparthi, Chetan Padmakar Darne, Peiying Liu, Manjunatha Narayana Rao Kamble, Balaji Seshadri, Raju Mannoori, Hasibur Rahaman, Jayakumar Sankara Warrier
  • Oxazole derivatives for use in the treatment of cancer
    Patent number: 10961233
    Abstract: A first aspect of the invention relates to a compound of formula (I), or a pharmaceutically acceptable salt or ester thereof, • B is a saturated or partially unsaturated monocyclic or bicyclic, heterocyclic group optionally substituted by one or more R 10 groups; *X is selected from SO2, CO2, CO, CONR11 and (CR12R13) p. Said compounds are capable of inhibiting PAICS and are useful in the treatment of proliferative disorders. Further aspects relate to pharmaceutical compositions, therapeutic uses and process for preparing compounds of formula (I).
    Type: Grant
    Filed: December 19, 2017
    Date of Patent: March 30, 2021
    Assignee: LIFEARC
    Inventors: Simon Osborne, Jonathan Large
  • 1 H-pyrazol-1-yl-thiazoles as inhibitors of lactate dehydrogenase and methods of use thereof
    Patent number: 10954228
    Abstract: The disclosure provides a compound of the formula (II) and pharmaceutically acceptable salts thereof. The variables, e.g. n, R, R3, R10, X, Y, and Z are defined herein. These compounds act as lactate dehydrogenase inhibitors and are useful for treating cancer and fibrosis. The compounds may be particularly useful for treating forms of cancer in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred. The disclosure also provides pharmaceutical compositions containing a compound of this formula and method for treating patients having cancer, fibrosis, or other conditions in which a metabolic switch from oxidative phosphorylation to glycolysis has occurred.
    Type: Grant
    Filed: June 29, 2017
    Date of Patent: March 23, 2021
    Assignees: THE TRUSTEES OF THE UNIVERSITY OF PENNSYLVANIA, THE UAB RESEARCH FOUNDATION, VANDERBILT UNIVERSITY, NATIONAL INSTITUTES OF HEALTH, UNITED STATES DEPT. OF HEALTH AND HUMAN SERVICES
    Inventors: David J. Maloney, Alex Gregory Waterson, Ganesha Rai Bantukallu, Kyle Ryan Brimacombe, Plamen Christov, Chi V. Dang, Victor M. Darley-Usmar, Matthew Hall, Xin Hu, Ajit Jadhav, Somnath Jana, Kwangho Kim, William J. Moore, Bryan T. Mott, Leonard M. Neckers, Anton Simeonov, Gary Allen Sulikowski, Daniel Jason Urban, Shyh Ming Yang
  • Anti-angiogenesis compound
    Patent number: 10954200
    Abstract: An anti-angiogenic compound includes 4-Benzyl-N?-(2-(o-tolyloxy) acetyl) morpholine-2-carbohydrazide (BAMC), having the following structural formula: or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: October 24, 2019
    Date of Patent: March 23, 2021
    Assignee: KING SAUD UNIVERSITY
    Inventors: Yasser Hussein Issa Mohammed, Nabil Ahmed Qassim Al-Zeqri, Ali Mohammed Alsalme, Fahed Ahmed Ali Alharthi, Ismail Khalil Warad, Anas Khaled Alali, Abdelkader M. Zarrouk