Patents Examined by Rebecca Anderson
  • Benzo-fused heterocyclic derivatives useful as agonists of GPR120
    Patent number: 9562053
    Abstract: The present invention is directed to benzo-fused heterocyclic derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by GPR120. More particularly, the compounds of the present invention are agonists of GPR120, useful in the treatment of, such as for example, Type II diabetes mellitus.
    Type: Grant
    Filed: March 7, 2014
    Date of Patent: February 7, 2017
    Assignee: Janssen Pharmaceutica NV
    Inventors: Zhihua Sui, Nalin Subasinghe
  • (+)-morphinans as antagonists of toll-like receptor 9 and therapeutic uses thereof
    Patent number: 9562014
    Abstract: The present invention provides (+)-morphinans comprising Toll-like receptor 9 (TLR9) antagonist activity, as well as methods for using the (+)-morphinans to treat pain. Also provided are pharmaceutical combination compositions comprising a (+)-morphinan and an opioid agonist/monoamine reuptake inhibitor, as well as methods for using the combination compositions to treat pain.
    Type: Grant
    Filed: December 22, 2010
    Date of Patent: February 7, 2017
    Assignee: Mallinckrodt LLC
    Inventors: Bobby N. Trawick, David W. Berberich, Christopher W. Grote
  • Process for the preparation of a rivaroxaban and intermediates formed in said process
    Patent number: 9556163
    Abstract: The invention relates to a process for the preparation of 5-chloro-N-({(5-S)-2-oxo3-[4-(3-oxo-morj)holine-4-yl)-phenyl]-1,3-oxazolidine-5-yl}-methyl) thiophen-2-carboxamide having the INN rivaroxaban. The invention also relates to intermediates formed in the above process.
    Type: Grant
    Filed: May 4, 2012
    Date of Patent: January 31, 2017
    Assignee: EGIS Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag
    Inventors: Eva Sipos, Gyorgyi Kovanyine Lax, Balazs Havasi, Balazs Volk, Gyorgy Krasznai, Gyorgy Ruzsics, Jozsef Barkoczy, Maria Tothne Lauritz, Gyula Lukacs, Andras Boza, Laszlo Jozsef Hegedus, Maria Julia Taborine Toth, Eva Pecsi
  • Substituted-1-benzo[]imidazole series compounds as lysine-specific demethylase 1 (LSD1) inhibitors
    Patent number: 9556170
    Abstract: The present invention provides compounds which are useful as inhibitors of lysine-specific demethylase 1 (“LSD1”). The present invention also relates to pharmaceutical compositions containing these compounds. The present invention also relates to a method for preparing these compounds. The present invention also relates to a method of treating a mammalian disorder in which LSD1 levels are elevated by administering these compounds and compositions to a patient in need thereof. The present invention also relates to a method for decreasing histone demethylase activity in a mammal comprising administering to the mammal an effective amount of these compounds and compositions.
    Type: Grant
    Filed: August 28, 2014
    Date of Patent: January 31, 2017
    Assignee: University of Utah Research Foundation
    Inventors: Hariprasad Vankayalapati, Sunil Sharma, Venkataswamy Sorna
  • Renin inhibitor
    Patent number: 9556159
    Abstract: The present invention provides a nitrogen-containing saturated heterocyclic compound of the formula [I] which is useful as a renin inhibitor. wherein R1 is a cycloalkyl group or an alkyl, R22 is an optionally substituted aryl and the like, R is a lower alkyl group, R3, R4, R5 and R6 are the same or different, and are a hydrogen atom, an optionally substituted carbamoyl, an optionally substituted alkyl, or alkoxycarbonyl, or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: September 13, 2013
    Date of Patent: January 31, 2017
    Assignees: Mitsubishi Tanabe Pharma Corporation, Shanghai Pharmaceuticals Holding Co., Ltd.
    Inventors: Toru Iijima, Yoichi Takahashi, Miki Hirai, Hiroshi Sugama, Yuko Togashi, Jingkang Shen, Guangxin Xia, Huixin Wan
  • Inhibitors of phosphodiesterase 10 enzyme
    Patent number: 9550784
    Abstract: The present invention relates to novel imidazo[1,2-b]pyridazine and imidazo[1,2-a]-pyrazine derivatives which are inhibitors of the phosphodiesterase 10 enzyme (PDE10) and which may be useful for the treatment or prevention of neurological, psychiatric and metabolic disorders in which the PDE10 enzyme is involved. The invention is also directed to pharmaceutical compositions comprising such compounds, to processes to prepare such compounds and compositions, to the use of such compounds or pharmaceutical compositions for the prevention or treatment of neurological, psychiatric and metabolic disorders and diseases.
    Type: Grant
    Filed: July 8, 2013
    Date of Patent: January 24, 2017
    Assignee: Beerse Pharmaceutica NV
    Inventors: Laurent Christian L. Leclercq, José Manuel Bartolomé-Nebreda, Susana Conde-Ceide, Michiel Luc Maria Van Gool
  • Heterocyclic derivatives and their use in the treatment of neurological disorders
    Patent number: 9550758
    Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.
    Type: Grant
    Filed: September 10, 2014
    Date of Patent: January 24, 2017
    Assignee: NOVARTIS AG
    Inventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sebastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
  • Triazolinthione derivatives
    Patent number: 9550752
    Abstract: The present invention relates to novel triazolinthione derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials and as plant growth regulators.
    Type: Grant
    Filed: April 9, 2014
    Date of Patent: January 24, 2017
    Assignee: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
    Inventors: Sebastian Hoffmann, Alexander Sudau, Peter Dahmen, Ulrike Wachendorff-Neumann, David Bernier, Helene Lachaise, Stephane Brunet, Jacky Vidal, Pierre Genix, Pierre-Yves Coqueron, Julie Geist, Jean-Pierre Vors, Philippe Kennel, Ricarda Miller
  • Synthesis of UDP-glucose: -acylsphingosine glucosyl transferase inhibitors
    Patent number: 9546161
    Abstract: Disclosed is a novel enantiomeric synthesis ceramide-like inhibitors of UDP-glucose: N-acylsphingosine glucosyltransferase. Also disclosed are novel intermediates formed during the synthesis.
    Type: Grant
    Filed: June 26, 2014
    Date of Patent: January 17, 2017
    Assignee: Genzyme Corporation
    Inventors: Bradford H. Hirth, Craig Siegel
  • Benzoxazepin PI3K inhibitor compounds and methods of use
    Patent number: 9546178
    Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
    Type: Grant
    Filed: November 3, 2015
    Date of Patent: January 17, 2017
    Assignee: Genentech, Inc.
    Inventors: Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
  • Modulators of exchange proteins directly activated by cAMP (EPACS)
    Patent number: 9539256
    Abstract: Embodiments of the invention are directed to compounds that inhibit an activity of EP AC proteins and methods of using the same. The inventors have developed a sensitive and robust high throughput screening (HTS) assay for the purpose of identifying EPAC specific inhibitors (Tsalkova et al. (2012) PLOS ONE 7(1):e30441).
    Type: Grant
    Filed: February 8, 2013
    Date of Patent: January 10, 2017
    Assignee: THE BOARD OF REGENTS OF THE UNIVERSITY OF TEXAS SYSTEM
    Inventors: Xiaodong Cheng, Jia Zhou, Tamara Tsalkova, Fang Mei, Haijun Chen
  • Substituted sodium-1H-pyrazole-5-olate
    Patent number: 9533972
    Abstract: The present application relates to sodium 1-[6-(morpholin-4-yl)pyrimidin-4-yl]-4-(1H-1,2,3-triazol-1-yl)-1H-pyrazol-5-olate, to processes for its preparation, to its use for the treatment and/or prophylaxis of diseases and to its use for the preparation of medicaments for the treatment and/or prophylaxis of diseases, in particular cardiovascular and haematological diseases and kidney diseases, and for promoting wound healing.
    Type: Grant
    Filed: November 15, 2011
    Date of Patent: January 3, 2017
    Assignee: Bayer Intellectual Property GmbH
    Inventors: Hans-Christian Militzer, Jörg Gries, Stefan Koep
  • Oxindole compounds carrying a CO-bound spiro substituent and use thereof for treating vasopressin-related diseases
    Patent number: 9527856
    Abstract: The present invention relates to novel substituted oxindole derivatives of formula I wherein the variables are as defined in the claims and the description. The invention further relates to pharmaceutical compositions comprising compounds I and their use for the treatment of vasopressin-related disorders.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: December 27, 2016
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Wilfried Braje, Hervé Geneste, Wilfried Hornberger, Katja Jantos, Andreas Kling, Claudia Krack, Marcel Van Gaalen
  • Hydroxybupropion analogues for treating drug dependence
    Patent number: 9527823
    Abstract: The invention provides hydroxybupropion analogs capable of inhibiting the reuptake of one or more monoamines and/or acting as antagonists at nicotinic acetylcholine receptors. The compounds may selectively bind to one or more monoamine transporters, including those for dopamine, norepinephrine, and serotonin and/or may selectively bind to one or more nicotinic acetylcholine receptor subtypes. Such compounds may be used to treat conditions that are responsive to modification of monoamine levels and/or antagonism of nicotinic acetylcholine receptors, including drug dependency, depression, and obesity.
    Type: Grant
    Filed: November 10, 2014
    Date of Patent: December 27, 2016
    Assignees: Research Triangle Institute, Dignity Health, Virginia Commonwealth University
    Inventors: Frank Ivy Carroll, Bruce E. Blough, Hernan A. Navarro, S. Wayne Mascarella, Ana Zamfira Muresan, M. Imad Damaj, Ronald J. Lukas
  • Crystalline forms of tricyclic compound acid salt or hydrate thereof, and method for making thereof
    Patent number: 9522911
    Abstract: The present invention relates to a novel crystalline acid salt of a tricyclic derivative or a hydrate thereof and a production method thereof. The crystalline acid salt or the hydrate thereof according to the present invention is stable with respect to humidity and stable with respect to hygroscopicity, and the quality control during manufacturing drugs is favorable. In addition, the crystalline acid salt or the hydrate thereof may be used in a pharmaceutical composition for preventing or treating neuropathic pain, epilepsy, stroke, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis (ALS), Huntington's disease, schizophrenia, chronic and acute pain, ischemic brain injury, neuronal loss after hypoxia, trauma and nerve damage, which are medical conditions induced by PARP overactivity.
    Type: Grant
    Filed: July 23, 2014
    Date of Patent: December 20, 2016
    Assignee: JEIL PHARMACEUTICAL CO., LTD.
    Inventors: In-Hae Ye, Chun-Ho Park, Jong-Hee Choi, Dong-il Kang
  • Azole derivative
    Patent number: 9522914
    Abstract: The present invention provides agents for treating or preventing diseases such as mood disorder, anxiety disorder, schizophrenia, Alzheimer's disease, Parkinson's disease, Huntington's chorea, eating disorder, hypertension, gastrointestinal disease, drug addiction, epilepsy, cerebral infarction, cerebral ischemia, cerebral edema, head injury, inflammation, immune-related disease, alopecia, and so forth.
    Type: Grant
    Filed: October 25, 2012
    Date of Patent: December 20, 2016
    Assignee: TAISHO PHARMACEUTICAL CO., LTD
    Inventors: Mitsukane Yoshinaga, Takeshi Kuwada, Naoki Miyakoshi, Tomoko Ishizaka, Daisuke Wakasugi, Shin-ichi Shirokawa, Nobutaka Hattori, Youichi Shimazaki
  • Certain chemical entities, compositions, and methods
    Patent number: 9518029
    Abstract: Chemical entities based on quinoxaline that are kinase inhibitors are described. Specifically quinoxaline derivatives of Formula I, containing a diarylamide or diarylurea substructure that inhibit Braf mutant kinase activity, pharmaceutical compositions containing the inhibitor compounds and methods of treatment of cancer comprising administering an effective amount of the Braf inhibitor compound are described.
    Type: Grant
    Filed: September 14, 2012
    Date of Patent: December 13, 2016
    Assignee: NeuPharma, Inc.
    Inventors: Xiangping Qian, Yong-Liang Zhu
  • Purification of aryltriazoles
    Patent number: 9518030
    Abstract: Impure aryltriazoles such as benzotriazole and tolyltriazole that are contaminated with dark colored impurities can be purified by conversion to an aryltriazole acid salt by treatment with aqueous acid. The aryltriazole acid salt is water soluble whereas the dark colored impurities are not. The aryltriazole acid salt solution is separated from the dark colored impurities and the aryltriazole acid salt is isolated by precipitation. The free aryltriazole may be recovered by neutralization with base.
    Type: Grant
    Filed: November 30, 2015
    Date of Patent: December 13, 2016
    Inventor: Randolph K Belter
  • Synthesis of chiral enaminones, their derivatives, and bioactivity studies thereof
    Patent number: 9518034
    Abstract: This invention provides enantioenriched heterocyclic enaminone compounds with quaternary stereogenic centers and novel methods of preparing the compounds. Methods include the method for the preparation of a compound of formula (I): comprising treating a compound of formula (II): with a transition metal catalyst under alkylation conditions.
    Type: Grant
    Filed: October 14, 2014
    Date of Patent: December 13, 2016
    Assignee: California Institute of Technology
    Inventors: Brian M. Stoltz, Dennis A. Dougherty, Douglas Duquette, Noah Duffy
  • Molecules inhibiting a metabolic pathway involving the Syk protein tyrosine kinase and method for identifying said molecules
    Patent number: 9504676
    Abstract: The present invention relates to the C-13 molecule (methyl 2-{5-[(3-benzyl-4-oxo-2-thioxo-1,3-thiazolidin-5-ylidene)methyl]-2-furyl}-benzoate) and to organic molecules functionally equivalent to the C-13 molecule, capable of inhibiting the binding of an antibody or antibody fragment with the human Syk protein tyrosine kinase, to the use of these molecules for the production of medicaments for the prevention or treatment of diseases dependent on metabolic pathways involving Syk, and also to a method for identifying such molecules.
    Type: Grant
    Filed: October 21, 2013
    Date of Patent: November 29, 2016
    Assignee: CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE
    Inventors: Piona Dariavach, Pierre Emile Ulysse Martineau, Bruno Villoutreix