Patents Examined by Ebenezer O. Sackey
  • Pyrazolopyrimidine compounds
    Patent number: 10570143
    Abstract: The present teachings provide a compound represented by structural formula (1-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
    Type: Grant
    Filed: October 9, 2018
    Date of Patent: February 25, 2020
    Assignee: UNIVERSITY HEALTH NETWORK
    Inventors: Yong Liu, Heinz W. Pauls, Radoslaw Laufer, Sze-Wan Li, Peter Brent Sampson, Miklos Feher, Grace Ng, Narendra Kumar B. Patel, Yunhui Lang
  • Blood brain barrier-penetrating oximes for cholinesterase reactivation
    Patent number: 10570088
    Abstract: The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.
    Type: Grant
    Filed: August 22, 2017
    Date of Patent: February 25, 2020
    Inventors: John R. Cashman, Jaroslaw Kalisiak
  • Synthesis of 1-[2-(2,4-dimethyl-phenylsulfanyl)-phenyl]piperazine
    Patent number: 10562872
    Abstract: The invention relates to a method for synthesis of 1-[2-(2,4-Dimethyl-phenylsulfanyl)-phenyl]piperazine in the presence of a strong base.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: February 18, 2020
    Assignee: H. Lundbeck A/S
    Inventors: Frederik Diness, Morten Meldal, Christian Borch Jacobsen
  • Prolyl hydroxylase inhibitors
    Patent number: 10562854
    Abstract: Disclosed herein are prolyl hydroxylase inhibitors that can stabilize hypoxia inducible factor-1 alpha (HIF-1?), as well as hypoxia inducible factor-2 (HIF-2). Also disclosed herein are pharmaceutical compositions comprising one or more of the disclosed compounds. Yet further disclosed are methods for stimulating the cellular immune response in a mammal such as increasing phagocytosis, for example, prolonging the life of phagocytes, inter alia, kerotyiocytes, neutrophils. As such the disclosed compounds provide methods for treating diseases that relate to the body's immune response.
    Type: Grant
    Filed: February 20, 2018
    Date of Patent: February 18, 2020
    Assignee: AERPIO THERAPEUTICS, INC.
    Inventors: Joseph H. Gardner, Robert Shalwitz, Shengde Wu
  • Process for the preparation of 2-{4-[(5,6-diphenyl pyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide and novel polymorphs thereof
    Patent number: 10544107
    Abstract: The present invention relates to a processes for the preparation of 2-{4-[(5,6-diphenyl pyrazin-2-yl)(isopropyl)amino]butoxy}-N-(methylsulfonyl)acetamide compound of formula-1 and novel polymorphs thereof.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: January 28, 2020
    Assignee: MAITHRI DRUGS PRIVATE LIMITED
    Inventors: Nagaraju Chakilam, Kondana Ramprasad Achampeta, Pradeep Rebelli, Tavitayya Kondaka
  • Adamantane and memantine derivatives as peripheral NMDA receptor antagonists
    Patent number: 10538482
    Abstract: The present invention relates to cationic compounds of formula (I) for use as peripheral NMDA receptor antagonists.
    Type: Grant
    Filed: July 26, 2016
    Date of Patent: January 21, 2020
    Assignees: Institut National de la Santé et de la Recherche Médicale (INSERM), Assistance Publique-Hopitaux de Paris, Centre National de la Recherche Scientifique (CNRS), Université Paris-Sud
    Inventors: Marc Humbert, Sylvia Cohen-Kaminsky, Sébastien Dumas, Gilles Bru-Mercier, Mouad Alami, Jean-Daniel Brion, Samir Messaoudi, Gilles Galvani
  • Pharmaceutical salts, physical forms, and compositions of pyrrolopyrimidine kinase inhibitors, and methods of making same
    Patent number: 10533011
    Abstract: Provided are methods of making certain pyrrolopyrimidine derivatives, which are useful in the treatment of proliferation disorders and other diseases related to the dysregulation of kinase (such as, but not limited to, EGFR (including HER), Alk, PDGFR, BLK, BMX/ETK, BTK, FLT3 (D835Y), ITK, JAK1, JAK2, JAK3, TEC and TXK) and/or the respective pathways, salts, polymorphs, and amorphous forms of said compounds, synthetic intermediates for preparing said compounds, and pharmaceutical compositions comprising said compounds and methods for making such compositions.
    Type: Grant
    Filed: June 30, 2016
    Date of Patent: January 14, 2020
    Assignee: ACEA THERAPEUTICS, INC.
    Inventors: Long Mao, Jia Liu, Yile Chen, Yuning Hua, Kongen Dai, Yimei Bao, Bojie Weng, Xiaopeng Mo, Jian Wu, Xiao Xu, Wanhong Xu, Xiaobo Wang
  • Methods of preparing inhibitors of influenza viruses replication
    Patent number: 10533004
    Abstract: A method of preparing a compound of Formula (I) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (1): or a pharmaceutically acceptable salt thereof with Compound (2): in the presence of water, an organic solvent, a base, and a transition metal catalyst to generate a compound of Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 9, 2017
    Date of Patent: January 14, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Luc J. Farmer, Michael John Boyd, David B. Miller, Jr., Valerie Ann Cwynar
  • Rutaecarpine analogs and applications thereof
    Patent number: 10526333
    Abstract: The present invention provides RUT analogs with various biological activities. In particular, the biological activities comprise anti-inflammatory activity, vasodilator effects, migration/invasion-suppressive activities, ability against damage due to remodeling between the epithelium and endothelium, collagen deposition and cardiac fibrosis suppress, Snail protein inhibitory effect, etc., which may improve cardiac, vasodilation, and lung functions. The RUT analogs disclosed herein also exhibit a lower cytotoxicity comparing to RUT.
    Type: Grant
    Filed: April 13, 2018
    Date of Patent: January 7, 2020
    Assignees: TAIPEI MEDICAL UNIVERSITY, NATIONAL TAIPEI UNIVERSITY OF TECHNOLOGY
    Inventors: Chun-Mao Lin, Chi-Ming Lee, Chi Wang, Sheng-Tung Huang, Jiun-An Gu, Tin-An Rau
  • Amide-substituted heterocyclic compounds useful as modulators of IL-12, IL-23 and/or IFN alpha responses
    Patent number: 10526321
    Abstract: Compounds having the following formula I: or a stereoisomer or pharmaceutically-acceptable salt thereof, where R1, R2, R3, R4, and R5 are as defined herein, are useful in the modulation of IL-12, IL-23 and/or IFN?, by acting on Tyk-2 to cause signal transduction inhibition.
    Type: Grant
    Filed: May 15, 2018
    Date of Patent: January 7, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Stephen T. Wrobleski, Shuqun Lin
  • Vinyl compounds as FGFR and VEGFR inhibitors
    Patent number: 10519133
    Abstract: FGFR and VEGFR inhibitors are provided, and compounds represented by formula (1) or formula (II) as FGFR and VEGFR inhibitors, pharmaceutically acceptable salts or tautomers thereof are specifically disclosed.
    Type: Grant
    Filed: August 3, 2016
    Date of Patent: December 31, 2019
    Assignees: MEDSHINE DISCOVERY INC., HARBIN ZHENBAO PHARMACEUTICAL CO., LTD.
    Inventors: Shuhui Chen, Zhengxia Chen, Meibi Dai, Cheng Xie, Peng Li, Yang Zhang, Guibai Liang, Qiang Wang, Jiangpeng Liao, Fei Sun, Guoping Hu, Jian Li
  • Benzimidazole-linked indole compound acting as novel divalent IAP antagonist
    Patent number: 10508103
    Abstract: The present invention discloses a benzimidazole-linked indole compound acting as novel divalent IAP antagonist, specifically disclosing the compound shown in formulas (I) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: April 27, 2017
    Date of Patent: December 17, 2019
    Assignee: MEDSHINE DISCOVERY INC.
    Inventors: Fei Sun, Charles Z. Ding, Zhe Cai, Wenyuan Qian, Guoping Hu, Jian Li, Shuhui Chen
  • DNA-PK inhibitors
    Patent number: 10501439
    Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders.
    Type: Grant
    Filed: March 5, 2018
    Date of Patent: December 10, 2019
    Assignee: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
  • Processes for the preparation of uracil derivatives
    Patent number: 10494347
    Abstract: The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: December 6, 2017
    Date of Patent: December 3, 2019
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Donald J. Gallagher, Laszlo R. Treiber, Robert Michael Hughes, Onorato Campopiano, Peng Wang, Yuxin Zhao, Shine K. Chou, Michael Allen Ouellette, Donald Nicholas Hettinger
  • Compositions and methods for inhibition of the JAK pathway
    Patent number: 10479783
    Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.
    Type: Grant
    Filed: February 8, 2018
    Date of Patent: November 19, 2019
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Crystallization process of aripiprazole derivatives in extended release formulations for treatment of schizophrenia
    Patent number: 10478434
    Abstract: Processes for providing depot injections of recrystallized aripiprazole lauroxil in which particles of the aripiprazole lauroxil have a surface area of about 0.50 to about 3.3 m2/g; and crystals of aripiprazole lauroxil produced by such processes.
    Type: Grant
    Filed: July 24, 2018
    Date of Patent: November 19, 2019
    Assignee: ALKERMES PHARMA IRELAND LIMITED
    Inventors: Wilfredo Morales, Tarek A. Zeidan, Renato A. Chiarella, Steven G. Wright, Jason M. Perry
  • Derivatives of pyrrole-2,5-diones having a fungicidal activity, their agronomical compositions and use thereof
    Patent number: 10464893
    Abstract: Derivatives of pyrrole-2,5-diones having formula (I): (I) are described, together with agronomic compositions containing said derivatives having formula (I) and the use thereof for the control of phytopathogenic fungi in agricultural crops.
    Type: Grant
    Filed: March 30, 2017
    Date of Patent: November 5, 2019
    Assignee: ISAGRO S.P.A
    Inventors: Paolo Bellandi, Marilena Gusmeroli, Silvia Mormile, Christian Badaracco, Matteo Vazzola
  • Process for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds
    Patent number: 10457648
    Abstract: The present disclosure relates to processes for preparing (cyclopentyl[d]pyrimidin-4-yl)piperazine compounds, and more particularly relates to processes for preparing (R)-4-(5-methyl-7-oxo-6,7-dihydro-5H-cyclopenta[d] pyrimidin-4-yl)piperazine and N-protected derivatives thereof, which may be used as an intermediate in the synthesis of Ipatasertib (i.e., (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)-propan-1-one). The present disclosure additionally relates to various compounds that are intermediates employed in these processes.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: October 29, 2019
    Assignees: GENENTECH INC., F. HOFFMANN-LA ROCHE AG
    Inventors: Francis Gosselin, Chong Han, Hans Iding, Reinhard Reents, Scott Savage, Beat Wirz
  • Substituted 2-thioxo-imidazolidin-4-ones and spiro analogues thereof, active anticancer ingredient, pharmaceutical composition, medicinal preparation, method for treating prostate cancer
    Patent number: 10450278
    Abstract: Novel (R)-stereoisomers of substituted 2-thioxo-imidazolidin-4-ones of formula 1, or spiro analogues thereof, which exhibit androgen receptor antagonist properties. Also provided are variants of a method for producing the same, intermediate compounds for producing compounds of formula 1, and pharmaceutical compositions containing compounds of formula 1 in the form of tablets, capsules, and/or injections. Compounds of formula 1 can be used to produce a medicinal agent suitable for treating cancers, such as prostate cancer and breast cancer. The compounds of formula 1 may have the structure: wherein R1 is OH, NH2, or an OR4 group; R2 and R3 are methyl, or R2 and R3 are a CH2—CH2 group; and R4 is C1-C4 alkyl or cyclopropyl.
    Type: Grant
    Filed: June 26, 2015
    Date of Patent: October 22, 2019
    Assignee: R-Pharm Overseas Inc.
    Inventor: Alexandre Vasilievich Ivachtchenko
  • Process for the preparation of dipeptidyl peptidase-4 (DPP-4) enzyme inhibitor
    Patent number: 10450315
    Abstract: The present invention relates to a novel and improved process for the preparation of Sitagliptin of Formula (I) and its pharmaceutically acceptable salts. The present invention also relates to novel intermediates and process for the preparation of intermediates used in the preparation of Sitagliptin.
    Type: Grant
    Filed: February 20, 2015
    Date of Patent: October 22, 2019
    Assignee: Lee Pharma Limited
    Inventors: Venkat Reddy Alla, Raghumitra Alla, Srinivas Reddy Mallepalli, Suresh Babu Nandam, Madhukar Reddy Guda, Raja Reddy Alluri