Patents Examined by Janet L Coppins
  • Pyridic ketone derivatives, method of preparing same, and pharmaceutical application thereof
    Patent number: 10064848
    Abstract: Compounds for the preparation of pyridone derivatives are provided. In particular, compounds of formula (IA) are provided, wherein the variable groups are as defined in the specification. The compounds of formula (IA) can be used as intermediates in the preparation of pyridone derivatives useful as mitogen-activated protein kinase kinase (MEK) inhibitors and therapeutic agents for treating cancer.
    Type: Grant
    Filed: September 28, 2017
    Date of Patent: September 4, 2018
    Assignees: Shanghai Hengrui Pharmaceutical Co., Ltd., Jiangsu Hengrui Medicine Co., Ltd.
    Inventors: Wangyang Tu, Haitang Zhang, Guoji Xu, Jiangtao Chi
  • Separase inhibitors and uses thereof
    Patent number: 10052310
    Abstract: In some embodiments, the present disclosure pertains to compositions with compounds that inhibit Separase activity. In additional embodiments, the present disclosure pertains to methods of treating a tumor in a subject by administering one or more compositions of the present disclosure to the subject.
    Type: Grant
    Filed: October 20, 2014
    Date of Patent: August 21, 2018
    Assignee: BAYLOR COLLEGE OF MEDICINE
    Inventors: Debananda Pati, Nenggang Zhang
  • Spiro-lactam NMDA receptor modulators and uses thereof
    Patent number: 10052308
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: August 21, 2018
    Assignee: Aptinyx Inc.
    Inventors: John A. Lowe, III, M. Amin Khan
  • Heteroaryl compounds as BTK inhibitors and uses thereof
    Patent number: 10045985
    Abstract: The present invention relates to pyrimidine compounds, and pharmaceutically acceptable compositions thereof, useful as BTK inhibitors.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: August 14, 2018
    Assignee: Merck Patent GmbH
    Inventors: Hui Qiu, Richard D. Caldwell, Lesley Liu-Bujalski
  • Polymorphic forms of ST-246 and methods of preparation
    Patent number: 10045964
    Abstract: Polymorph forms of 4-trifluoromethyl-N-(3,3a,4,4a,5,5a,6,6a-octahydro-1,3-dioxo-4,6-ethenocycloprop[f]isoindol-2(1H)-yl)-benzamide are disclosed as well as their methods of synthesis and pharmaceutical compositions.
    Type: Grant
    Filed: July 27, 2017
    Date of Patent: August 14, 2018
    Assignee: Siga Technologies Inc.
    Inventors: Shanthakumar R. Tyavanagimatt, Melialani A. C. L. S. Anderson, William C. Weimers, Dylan Nelson, Tove' C. Bolken, Dennis E. Hruby, Michael H. O'Neill, Gary Sweetapple, Kelley A. McCloughan
  • Imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives as LRRK2 inhibitors
    Patent number: 10039753
    Abstract: The present invention provides novel imidazo[4,5-c]quinoline and imidazo[4,5-c][1,5]naphthyridine derivatives of Formula (I), and the pharmaceutically acceptable salts thereof wherein R1, R1a, R1b, R2, R4, R5, R6, X and Z are as defined in the specification. The invention is also directed to pharmaceutical compositions comprising the compounds of Formula (I) and to use of the compounds in the treatment of diseases associated with LRRK2, such as neurodegenerative diseases including Parkinson's disease or Alzheimer's disease, cancer, Crohn's disease or leprosy.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: August 7, 2018
    Assignee: Pfizer Inc.
    Inventors: Karen Jean Coffman, Paul Galatsis, Michelle Renee Garnsey, Jaclyn Louise Henderson, Bethany Lyn Kormos, Ravi G. Kurumbail, Martin Youngjin Pettersson, Matthew Richard Reese, Antonia Friederike Stepan, Patrick Robert Verhoest, Travis T. Wager
  • Methods for the treatment of HER2 amplified cancer
    Patent number: 10016434
    Abstract: Described herein are methods and compositions for treating HER2-amplified cancer. The methods include administering to an individual in need thereof ibrutinib.
    Type: Grant
    Filed: July 18, 2017
    Date of Patent: July 10, 2018
    Assignee: Pharmacyclics LLC
    Inventors: Jun Chen, Joseph J. Buggy, Laurence Elias
  • 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-ones as inhibitors of myeloperoxidase
    Patent number: 10016430
    Abstract: There are disclosed certain 1-[2-(aminomethyl)benzyl]-2-thioxo-1,2,3,5-tetrahydro-4H-pyrrolo[3,2-d]pyrimidin-4-one compounds of formula (I), and pharmaceutically acceptable salts thereof, together with compositions containing them and their use in therapy. The compounds are inhibitors of the enzyme MPO and are thereby particularly useful in the treatment or prophylaxis of cardiovascular disorders such as heart failure and coronary artery disease related conditions.
    Type: Grant
    Filed: March 9, 2017
    Date of Patent: July 10, 2018
    Assignee: AstraZeneca AB
    Inventors: Tord Bertil Inghardt, Petra Johannesson, Ulrik Jurva, Erik Michaelsson, Eva-Lotte Lindstedt-Alstermark, Nicholas Tomkinson, Jeffrey Paul Stonehouse, Li-Ming Gan
  • Desferrithiocin analogs and uses thereof
    Patent number: 10010535
    Abstract: Iron overload is associated with pathological conditions such as oxidative stress, transfusional iron overload, thalassemia, primary hemochromatosis, secondary hemochromatosis, diabetes, liver disease, heart disease, cancer, radiation injury, neurological or neurodegenerative disorder, Friedreich's ataxia (FRDA), macular degeneration, closed head injury, irritable bowel disease, and reperfusion injury. The present invention provides methods and pharmaceutical compositions using desferrithiocin analogs of Formulae (A) and (J) for treating and/or preventing these pathological conditions, metal (e.g., iron, aluminum, a lanthanide, or an actinide (e.g., uranium)) overload conditions, and infectious diseases (e.g., malaria).
    Type: Grant
    Filed: November 21, 2014
    Date of Patent: July 3, 2018
    Assignee: University of Florida Research Foundation, Incorporated
    Inventor: Raymond J. Bergeron, Jr.
  • METAP2 inhibitors and methods of treating obesity
    Patent number: 10010544
    Abstract: The present invention relates to modified or polymer conjugated MetAP2 inhibitors. The present invention also relates to methods of preventing, inducing, causing or increasing weight loss, treating obesity and/or treating metabolic syndrome utilizing the modified or polymer conjugated MetAP2 inhibitors. The present invention also relates to methods of improving insulin sensitivity and glycemic control, reducing insulin levels and/or improving leptin sensitivity utilizing the modified or polymer conjugated MetAP2 inhibitors.
    Type: Grant
    Filed: August 1, 2017
    Date of Patent: July 3, 2018
    Assignee: SynDevRx, Inc.
    Inventors: John S. Petersen, James Shanahan
  • Pyrrolobenzodiazepine compounds
    Patent number: 9999625
    Abstract: The invention relates to pyrrolo[2,1-c][1,4]benzodiazepines (PBDs) of formula (I) and in particular to PBD dimers linked through the C1 position, and PBD monomers linked through the C1 position to aromatic groups, and pharmaceutically acceptable salts thereof, which are useful as medicaments, in particular as anti-proliferative agents.
    Type: Grant
    Filed: May 1, 2015
    Date of Patent: June 19, 2018
    Assignee: Femtogenix Limited
    Inventors: David Edwin Thurston, Khondaker Mirazur Rahman, Paul Joseph Mark Jackson
  • Benzothiophene derivatives as estrogen receptor inhibitors
    Patent number: 9988376
    Abstract: A compound of formula (I): or a pharmaceutically acceptable salt thereof, compositions, combinations and medicaments containing said compounds and processes for their preparation. The invention also relates to the use of said compounds, combinations, compositions and medicaments, for example as inhibitors of the activity of the estrogen receptor, including degrading the estrogen receptor, the treatment of diseases and conditions mediated by the estrogen receptor.
    Type: Grant
    Filed: July 1, 2014
    Date of Patent: June 5, 2018
    Assignee: GLAXOSMITHKLINE INTELLECTUAL PROPERTY DEVELOPMENT LIMITED
    Inventors: Sebastien Andre Campos, John David Harling, Afjal Hussain Miah, Ian Edward David Smith
  • ERK inhibitors and uses thereof
    Patent number: 9980964
    Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.
    Type: Grant
    Filed: February 2, 2017
    Date of Patent: May 29, 2018
    Assignee: CELGENE CAR LLC
    Inventors: Nadia Haq, Deqiang Niu, Russell C. Petter, Lixin Qiao, Juswinder Singh, Zhendong Zhu
  • Aromatic heterocyclic derivatives and pharmaceutical applications thereof
    Patent number: 9974785
    Abstract: Provided herein are aromatic heterocyclic derivatives or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof used for treating Alzheimer's disease. Also provided herein are pharmaceutical compositions containing such compounds, and use of such compounds or pharmaceutical compositions thereof for managing or treating 5-HT6 receptor-mediated diseases, especially in the manufacture of a medicament for managing or treating Alzheimer's disease.
    Type: Grant
    Filed: July 8, 2015
    Date of Patent: May 22, 2018
    Assignee: Sunshine Lake Pharma Co., Ltd.
    Inventors: Yingjun Zhang, Chuanfei Jin, Wenhe Zhong, Kangzhi Chen, Li Gao, Runzhi Liu, Ji Zhang
  • Aldehyde oxidation processes
    Patent number: 9975840
    Abstract: The oxidation of isobutyraldehyde produces isobutyric acid and byproducts, such as isopropyl formate. A process of reducing the isopropyl formate byproduct and other byproducts in the oxidation of isobutyraldehyde is described. The process uses a carbonyl compound, such as acetone, to reduce byproduct levels in the resulting product. Process for use of static mixers in oxidation reactions of aldehydes are also provided.
    Type: Grant
    Filed: July 20, 2016
    Date of Patent: May 22, 2018
    Assignee: Eastman Chemical Company
    Inventors: Damon Ray Billodeaux, Kenneth Wayne Hampton, Jr., Chad A. Johnson
  • Substituted pyridinones as MGAT2 inhibitors
    Patent number: 9974778
    Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a polymorph, or a solvate thereof, wherein all of the variables are as defined herein. These compounds are monoacylglycerol acyltransferase type 2 (MGAT2) inhibitors which may be used as medicaments.
    Type: Grant
    Filed: June 10, 2015
    Date of Patent: May 22, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Pratik Devasthale, Fang Moore, James Mignone, Wei Wang
  • Medications for deposition on biological surfaces
    Patent number: 9974761
    Abstract: Personal care compositions, such as oral medication compositions containing a flavor system comprising one or more coolants. The pleasant cool sensation provided by a coolant is enhanced in terms of quicker onset, greater intensity, impact or longer duration, which improves appeal and acceptability of the compositions to consumers.
    Type: Grant
    Filed: September 12, 2016
    Date of Patent: May 22, 2018
    Assignee: The Procter & Gamble Company
    Inventors: John Christian Haught, Michael Reilly, Steven Hamilton Hoke, Qingxin Lei, Yakang Lin, Koti Tatachar Sreekrishna, Ashraf Traboulsi
  • Use of a benzoate containing composition in urea cycle disorders and neurodegenerative disorders
    Patent number: 9968582
    Abstract: This disclosure relates to pharmaceutical compositions useful for inhibiting the progression of urea cycle disorders and neurodegenerative disorders, such as Parkinson's disease, Alzheimer's disease, and multiple sclerosis. The pharmaceutical compositions may include glyceryl tribenzoate and glyceryl dibenzoate. The pharmaceutical compositions may be orally administered to the patient one time per day.
    Type: Grant
    Filed: January 16, 2015
    Date of Patent: May 15, 2018
    Assignee: Rush University Medical Center
    Inventor: Kalipada Pahan
  • Antiproliferative compounds and methods of use thereof
    Patent number: 9968596
    Abstract: Compounds of formula I for treating, preventing or managing cancer are disclosed. Also disclosed are methods of treating, preventing or managing cancer, such as leukemia, comprising administering the compounds. In certain embodiments, the method of treatment comprise administering a compound provided herein in combination with a second agent. Pharmaceutical compositions and single unit dosage forms comprising the compounds are also disclosed.
    Type: Grant
    Filed: October 2, 2017
    Date of Patent: May 15, 2018
    Assignee: Celgene Corporation
    Inventors: Brian E. Cathers, Matthew Daniel Correa, Joshua Hansen, Antonia Lopez-Girona, Ehab M. Khalil, Kyle MacBeth, Hon-Wah Man, George W. Muller, Michael Pourdehnad, Raj Raheja
  • Imidazo-pyridazine derivatives as casein kinase 1 ?/? inhibitors
    Patent number: 9956220
    Abstract: The invention provides compounds of Formula (I) and pharmaceutically-acceptable salts thereof. The compounds of Formula (I) inhibit protein kinase activity thereby making them useful as anticancer agents.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: May 1, 2018
    Assignee: Bristol-Myers Squibb Company
    Inventors: Upender Velaparthi, Selvakumar Kumaravel, Arul Mozhi Selvan Subbiah Karupplah, Shilpa Holehatti Maheshwarappa, Chandrasekhar Reddy Rachamreddy, Mark D. Wittman