Patents Examined by Deepak Rao
  • Patent number: 9845309
    Abstract: PKC inhibitors are disclosed. The PKC inhibitors are useful for treating PKC associated diseases, including certain cancers. The PKC inhibitors have improved efficacy at lower dosage amounts to achieve tumor regression, improved potency, PK profile, absorption, gastrointestinal tolerance and kinase selectivity.
    Type: Grant
    Filed: August 16, 2016
    Date of Patent: December 19, 2017
    Assignee: NOVARTIS AG
    Inventors: Michael Joseph Luzzio, Julien Papillon, Michael Scott Visser
  • Patent number: 9840525
    Abstract: A crystal form of 9-[(R)-2-[[(S)-[[[1-(isopropoxycarbonyl)-1-methyl]ethyl]amino]phenoxyphosphinyl]methoxyl]propyl]adenine fumarate of formula (I) is provided. Also provided is a preparation method and method of using the crystal form. Specifically, a crystal form of 9-[(R)-2-[[(S)-[[[1-(isopropoxycarbonyl)-1-methyl]ethyl]amino]phenoxyphosphinyl]methoxyl]propyl]adenine fumarate of formula (I) having an X-ray powder diffraction (XRPD) spectrum including diffraction peaks at 2?±0.20° of 5.08, 12.44, 13.18, 22.37, 23.37 and 28.56 is provided. The crystal form provided herein has high bioavailability, significant efficacy, good stability, high yield and high purity, and contributes to the selection and design of a drug administration route and the determination of process parameters of a pharmaceutical preparation, thereby improving drug production quality.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: December 12, 2017
    Assignee: JIANGSU HANSOH PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Ming Chen, Chengyao Tian, Mingli Zhao, Jun Yu, Baohai Yang, Aifeng Lu
  • Patent number: 9840512
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
    Type: Grant
    Filed: February 20, 2014
    Date of Patent: December 12, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Linda L. Brockunier, Helen Chen, Harry R. Chobanian, Matthew J. H. Clements, Alejandro Crespo, Duane E. DeMong, Yan Guo, William K. Hagmann, Karen M. Marcantonio, Michael Miller, Barbara Pio, Christopher W. Plummer, Dong Xiao
  • Patent number: 9839664
    Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36), GLP-1(9-36), and oxyntomodulin, or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, R1, R2, R3, R4, R5, n, p and q are as defined herein.
    Type: Grant
    Filed: September 13, 2016
    Date of Patent: December 12, 2017
    Assignee: Celgene International II SÀRL
    Inventors: Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
  • Patent number: 9840477
    Abstract: The present disclosure relates to novel cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, the disclosure relates to novel tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer.
    Type: Grant
    Filed: June 6, 2016
    Date of Patent: December 12, 2017
    Assignee: CB THERAPEUTICS INC.
    Inventor: Deyi Zhang
  • Patent number: 9833452
    Abstract: Compounds of formula (I): are described herein. Compounds of the disclosure are modulators of Kv3 channels and may be used in the prophylaxis or treatment of related disorders.
    Type: Grant
    Filed: July 11, 2016
    Date of Patent: December 5, 2017
    Assignee: AUTIFONY THERAPEUTICS LIMITED
    Inventors: Giuseppe Alvaro, Agostino Marasco
  • Patent number: 9834543
    Abstract: In one aspect, the present disclosure provides indazoles of Formula I: (I) and the pharmaceutically acceptable salts and solvates thereof, wherein R3, R4, R5, R6, Z1, Z2, Z3, and G are defined as set forth in the specification. Further, the present disclosure also provides compounds of Formulae II and IA, and the pharmaceutically acceptable salts and solvates thereof. The present disclosure is also directed to the use of compounds of Formulae I, II, and IA, and the pharmaceutically acceptable salts and solvates thereof, to treat a disorder responsive to the blockade of sodium channels. In one embodiment, compounds of the present disclosure are especially useful for treating pain.
    Type: Grant
    Filed: August 22, 2014
    Date of Patent: December 5, 2017
    Assignee: Purdue Pharma L.P.
    Inventor: Jianming Yu
  • Patent number: 9834521
    Abstract: This invention relates to compounds of the general formula (I): in which the variable groups are as identified herein, and to preparation and use of the compounds.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: December 5, 2017
    Assignee: ARIAD Pharmaceuticals, Inc.
    Inventors: Stephan G. Zech, Anna Kohlmann, Feng Li, Yihan Wang, Tianjun Zhou, David C. Dalgarno, William C. Shakespeare, Xiaotian Zhu
  • Patent number: 9828360
    Abstract: Compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts, or solvates or prodrugs thereof, where R1, R2, Ra, Rb, Rc, Rd, X, Ring B, and Ring C are as defined herein, and wherein Ring B moiety and the NH—C(?X)—NH moiety are in the trans configuration, are inhibitors of TrkA kinase and are useful in the treatment of diseases which can be treated with a TrkA kinase inhibitor such as pain, cancer, inflammation/inflammatory diseases, neurodegenerative diseases, certain infectious diseases, Sjogren's syndrome, endometriosis, diabetic peripheral neuropathy, prostatitis and pelvic pain syndrome.
    Type: Grant
    Filed: November 13, 2013
    Date of Patent: November 28, 2017
    Assignee: Array BioPharma Inc.
    Inventors: Shelley Allen, Steven Wade Andrews, James F. Blake, Barbara J. Brandhuber, Kevin Ronald Condroski, Julia Haas, Yutong Jiang, Timothy Kercher, Gabrielle R. Kolakowski, Shannon L. Winski
  • Patent number: 9828370
    Abstract: The present invention provides compounds for the prevention or treatment of cancer or a bacterial or viral infection. Additionally, the present invention provides compositions and methods for using these compounds and compositions in the prevention or treatment of cancer or a bacterial or viral infection in a subject.
    Type: Grant
    Filed: April 22, 2016
    Date of Patent: November 28, 2017
    Assignee: INHIBIKASE THERAPEUTICS, INC.
    Inventors: Milton H. Werner, Terence A. Kelly
  • Patent number: 9828358
    Abstract: Described herein are amorphous and crystalline forms of pharmaceutically acceptable salts of the lysine specific demethylase-1 inhibitor 4-[2-(4-amino-piperidin-1-yl)-5-(3-fluoro-4-methoxy-phenyl)-1-methyl-6-oxo-1,6-dihydro-pyrimidin-4-yl]-2-fluorobenzonitrile. Also described are pharmaceutical compositions suitable for administration to a mammal that include the lysine specific demethylase-1 inhibitor, and methods of using the lysine specific demethylase-1 inhibitor for treating diseases or conditions that are associated with lysine specific demethylase-1 activity.
    Type: Grant
    Filed: November 4, 2016
    Date of Patent: November 28, 2017
    Assignee: CELGENE QUANTICEL RESEARCH, INC.
    Inventors: Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal, Paula Alessandra Tavares-Greco, Matthew Michael Kreilein
  • Patent number: 9828338
    Abstract: Described herein are compounds and pharmaceutical compositions which inhibit N-acylethanolamine acid amidase (NAAA). Described herein are methods for synthesizing the compounds set forth herein and methods for formulating these compounds as pharmaceutical compositions which include these compounds. Also described herein are methods of inhibiting NAAA in order to sustain the levels of palmitoylethanolamide (PEA) and other N-acylethanolamines (NAE) that are substrates for NAAA, in conditions characterized by reduced concentrations of NAE. Also, described here are methods of treating and ameliorating pain, inflammation, inflammatory diseases, and other disorders in which modulation of fatty acid ethanolamides is clinically or therapeutically relevant or in which decreased levels of NAE are associated with the disorder.
    Type: Grant
    Filed: September 14, 2015
    Date of Patent: November 28, 2017
    Assignees: The Regents of the University of California, Fondazione Istituto Italiano di Technologia, Universita Degli Studi di Urbino “Carlo Bo”, Universita Degli Studi di Parma
    Inventors: Daniele Piomelli, Tiziano Bandiera, Fabio Bertozzi, Andrea Nuzzi, Annalisa Fiasella, Stefano Ponzano, Chiara Pagliuca, Angelo Mario Reggiani, Marco Mor, Giorgio Tarzia
  • Patent number: 9822103
    Abstract: There are disclosed compounds that are inhibitors of EZH2, pharmaceutical compositions containing said compounds and methods of treating hyperproliferative, inflammatory, infectious, and immunoregulatory disorders and diseases utilizing the compounds of the invention.
    Type: Grant
    Filed: November 18, 2014
    Date of Patent: November 21, 2017
    Assignee: Bristol-Myers Squibb Company
    Inventors: Steven P. Seitz, Jay A. Markwalder, Ashok Vinayak Purandare
  • Patent number: 9822141
    Abstract: The present invention provides N-alkyl 2-(disubstituted)alkynyladenosine-5?-uronamides and derivatives thereof and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.
    Type: Grant
    Filed: June 27, 2015
    Date of Patent: November 21, 2017
    Assignee: Lewis and Clark Pharmaceuticals, Inc.
    Inventors: Robert D Thompson, Anthony Beauglehole, Guoquan Wang
  • Patent number: 9822138
    Abstract: Compounds of Formula I: and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: November 21, 2017
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Petr Vachal, Izzat Raheem, Zhiqiang Guo, Timothy John Hartingh
  • Patent number: 9814715
    Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: November 14, 2017
    Assignee: Vitae Pharamceuticals, Inc.
    Inventors: Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
  • Patent number: 9809579
    Abstract: Provided herein are substituted 3-azabicyclo[3.1.0]hexanes as ketohexokinase inhibitors, processes to make said compounds, and methods comprising administering said compounds to a mammal in need thereof.
    Type: Grant
    Filed: December 16, 2016
    Date of Patent: November 7, 2017
    Assignee: Pfizer Inc.
    Inventors: Matthew Dowling, Dilinie Fernando, Kentaro Futatsugi, Kim Huard, Thomas Victor Magee, Brian Raymer, Andre Shavnya, Aaron Smith, Benjamin Thuma, Andy Tsai, Meihua Tu
  • Patent number: 9802946
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: December 23, 2014
    Date of Patent: October 31, 2017
    Assignee: Northwestern University
    Inventors: M. Amin Khan, Joseph R. Moskal, Paul Wood
  • Patent number: 9802891
    Abstract: The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
    Type: Grant
    Filed: December 21, 2016
    Date of Patent: October 31, 2017
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Hongyuan Wei, Chongjun Liu, Xuyang Zhao, Xiaojie Xu, Hua Bai, Yuncai Zhang
  • Patent number: 9801845
    Abstract: Antimicrobial compositions comprising sulfur- or selenium-containing, fatty-acylated alpha-hydroxy acid compounds and methods of using said compounds or compositions to inhibit microbial growth.
    Type: Grant
    Filed: June 29, 2016
    Date of Patent: October 31, 2017
    Assignee: Novus International, Inc.
    Inventors: Graciela B. Arhancet, Matthew Mahoney, Scott Long, Mariya Grega, Drew L. Lichtenstein, Vivek Kuttappan, Jeffery Escobar Monestel, Mercedes Vazquez-Anon