Patents Examined by Valerie Rodriguez-Garcia
  • Substituted 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-A]pyridine-3(2H)-ones and 2,5,6,7-tetrahydro-3H-pyrrolo[2,1-C][1,2,4]triazol-3-ones, and use thereof
    Patent number: 10722501
    Abstract: The present application relates to novel substituted 5,6,7,8-tetrahydro[1,2,4]triazolo[4,3-a]pyridin-3(2H)-ones and 2,5,6,7-tetrahydro-3H-pyrrolo[2,1-c][1,2,4]triazol-3-ones of formula (I), to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of lung inflammation disorders.
    Type: Grant
    Filed: May 8, 2017
    Date of Patent: July 28, 2020
    Assignees: BAYER AKTIENGESELLSCHAFT, BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Nicole Biber, Damian Brockschnieder, Kersten Matthias Gericke, Florian Kölling, Klemens Lustig, Jörg Meding, Heinrich Meier, Thomas Neubauer, Martina Schäfer, Andreas Timmermann, Dmitry Zubov, Carsten Terjung, Niels Lindner, Volker Badock, Dieter Moosmayer, Hideki Miyatake Ondozabal, Stephen Moore, Alexander Schulz
  • N-[(Pyrimidinylamino)propanyl]-and N-[(Pyridinylamino)-propanyl]arylcarboxamides
    Patent number: 10710984
    Abstract: The present invention relates to novel N-[(Pyrimidinylamino)propanyl]- and N-[(Pyridinylamino)propanyl]arylcarboxamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the orexin sub-type 1 receptor.
    Type: Grant
    Filed: April 7, 2017
    Date of Patent: July 14, 2020
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Doris Riether, Marco Ferrara, Niklas Heine, Uta Lessel, Janet Rachel Nicholson, Anton Pekcec, Stefan Scheuerer
  • HDAC inhibitors and uses thereof
    Patent number: 10703737
    Abstract: The present invention relates to histone deacetylase inhibitors, and to pharmaceutical compositions comprising the compounds, useful for the treatment of ischemia-reperfusion injury and for cardioprotection.
    Type: Grant
    Filed: March 13, 2019
    Date of Patent: July 7, 2020
    Assignee: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT
    Inventors: Donald R. Menick, Chung-Jen James Chou, Daniel Herr, Xiaoyang Li
  • Imidazo[1,2-A]pyridine derivatives, methods for preparing the same and use thereof
    Patent number: 10696671
    Abstract: The present disclosure relates to novel imidazo[1,2-a]pyridine derivatives, and more particularly to imidazo[1,2-a]pyridine derivatives of Formula 1 wherein Y1, Y2 and Y3 are each independently H, halogen, a C1-C6 straight chain alkyl unsubstituted or substituted with R1, or hydroxy; R1 is hydroxy; Y4 is H, C1-C6 straight chain alkyl, or C1-C6 alkoxy; and X is H or halogen, and having an excellent activity of inhibiting gastric acid secretion, methods for preparing the same, and the use thereof. The imidazo[1,2-a]pyridine derivatives according to the present disclosure have gastric acid secretion inhibitory activity, and thus may be effectively used for the prevention or treatment of gastrointestinal inflammatory diseases or gastric acid-related diseases.
    Type: Grant
    Filed: July 4, 2017
    Date of Patent: June 30, 2020
    Assignee: Jeil Pharmaceutical Co., Ltd.
    Inventors: Jeongmin Kim, Hyunho Lee, Kwangwoo Chun, Chun-Ho Park, Eunsung Jang, Yoonsun Park, Joseph Kim
  • Imidazopyridopyrimidine derivative compound and use thereof
    Patent number: 10696675
    Abstract: A novel imidazopyridine derivative compound and uses thereof are disclosed.
    Type: Grant
    Filed: June 28, 2017
    Date of Patent: June 30, 2020
    Assignee: HANMI PHARMACEUTICAL CO., LTD.
    Inventors: Moon Sub Lee, Eun Young Byun, Ji Sook Kim, Won Jeoung Kim, Nam Du Kim, Seung Hyun Jung, Young Gil Ahn
  • Composition for inhibiting formation of SNARE complex, containing myricetin derivatives
    Patent number: 10682333
    Abstract: The present invention relates to a composition for inhibiting the formation of a SNARE complex, containing myricetin derivatives, and having novel structures and obtained by the acylation of myricetin, laricitrin, combretol, or syringetin. The myricetin derivatives are considered to exhibit an effect of being bioconverted into myricetin in a cell. The myricetin derivatives lost the dark color of conventional myricetin and properties thereof were changed such that the myricetin derivatives have properties of photostability and fat solubility. Therefore, since stable form myricetin derivatives are absorbed into a cell such that an activity, possessed by normal myricetin, of inhibiting the formation of a SNARE complex are exhibited, the present invention can exhibit an excellent function as a SNARE targeting prodrug, and as a composition for inhibiting the formation of a SNARE complex, containing the same.
    Type: Grant
    Filed: July 29, 2016
    Date of Patent: June 16, 2020
    Assignee: Research & Business Foundation Sungkyunkwan University
    Inventors: Dae Hyuk Kweon, Joon Bum Park, Young Hun Jung, Woo Jae Chung, Pa Ul Heo
  • Epothilone B and dictyostatin analogs, their preparation and use
    Patent number: 10683288
    Abstract: A compound having the structure:
    Type: Grant
    Filed: July 22, 2016
    Date of Patent: June 16, 2020
    Assignee: The Trustees of Columbia University in the City of New York
    Inventors: James Leighton, Stephen Ho, Corinne Foley
  • Spiro-condensed pyrrolidine derivatives as deubiquitylating enzymes (DUB) inhibitors
    Patent number: 10654853
    Abstract: The present invention relates to novel compounds and methods for the manufacture of inhibitors of deubiquitylating enzymes (DUBs). In particular, the invention relates to the inhibition of Cezanne 1. The invention further relates to the use of DUB inhibitors in the treatment of cancer.
    Type: Grant
    Filed: March 2, 2017
    Date of Patent: May 19, 2020
    Assignee: MISSION THERAPEUTICS LIMITED
    Inventors: Mark Ian Kemp, Martin Lee Stockley, Michael David Woodrow, Alison Jones
  • Podophyllotoxin derivative with 4-position nitrogen substitution and preparation method and application thereof
    Patent number: 10639295
    Abstract: A compound represented by formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable formulation prepared using the compound and the salt. The compound represented by formula (I) or the pharmaceutically acceptable salt exhibits significantly higher buildup and concentration in the lungs compared to other tissues, a longer dwell time in the lungs, and/or elevated pharmaceutical efficacy.
    Type: Grant
    Filed: August 2, 2016
    Date of Patent: May 5, 2020
    Assignee: YAOPHARMA CO., LTD.
    Inventors: Zhirong Zhang, Meiling Zhou, Yan Zhang
  • Hepatitis C virus inhibitor and uses thereof
    Patent number: 10640515
    Abstract: Disclosed is a compound of formula (I-a) as an inhibitor of hepatitis C virus (HCV), or an optical isomer, a pharmaceutically acceptable salt, a hydrate or a solvate thereof, usable to treat HCV infections or hepatitis C diseases and also usable as an inhibitor of HCV non-structural protein 5A (NS5A) In the formula (I-a), A and A? are independently each R1, R4 and R6 are independently selected from the group consisting of fluorine, chlorine, bromine and iodine; R2 and R2? are independently selected from substituted or unsubstituted C1-C6 alkyl; R3 and R3? are independently selected from substituted or unsubstituted C1-C6 alkyl; R5 is selected from the group consisting of hydrogen, fluorine, chlorine, bromine and iodine; n is 2, 3, 4 or 5; m is 0, 1, 2 or 3; and p is 0, 1, 2 or 3.
    Type: Grant
    Filed: December 21, 2018
    Date of Patent: May 5, 2020
    Assignee: ZHEJIANG PALO ALTO PHARMACEUTICALS, INC
    Inventors: Zhijian Xi, Huaqiang Xu, Chunping Lu
  • Simplified structural mimetics of AIPS as quorum sensing inhibitors
    Patent number: 10597372
    Abstract: Compounds that regulate quorum sensing in Staphylococcal bacteria and in particular in Staphylococcus aureus are provided. Compounds are described in formulas I, II, III, IV, V and VI herein. One or more compounds herein can be employed to inhibit QS and to thus inhibit virulence in Staphylococcus bacteria and in particular in Staphylococcus aureus. Compounds herein and pharmaceutical compositions containing one or more of these compounds are useful, for example, in treating infections of Staphylococcus bacteria and in particular of Staphylococcus aureus. Methods for treating such bacterial infections are provided.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: March 24, 2020
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Helen Blackwell, Joseph Vasquez, Yiftah Tal Gan
  • Alcohol derivatives of carboxamides as Kv7 potassium channel openers
    Patent number: 10590067
    Abstract: The present invention provides novel compounds which activate the Kv7 potassium channels. Exemplary compounds of the invention have the structure of Formula 1. Separate aspects of the invention are directed to pharmaceutical compositions comprising said compounds and uses of the compounds to treat disorders responsive to the activation of Kv7 potassium channels.
    Type: Grant
    Filed: February 20, 2018
    Date of Patent: March 17, 2020
    Assignee: H. Lundbeck A/S
    Inventors: Mario Rottlander, Anette Graven Sams, Xiaofang Wang, Debasis Das, Jian Hong, Shu Hui Chen
  • 4-(benzimidazol-2-ylamino)benzamide derivatives and methods of synthesis thereof
    Patent number: 10590088
    Abstract: Disclosed are 4-(benzimidazol-2-ylamino)benzamide derivatives useful in slowing the expansion of cancer cells and methods of synthesizing derivatives of formula 5 or formula 7: wherein R and R? are defined herein.
    Type: Grant
    Filed: October 16, 2018
    Date of Patent: March 17, 2020
    Assignee: Translational Drug Development, LLC
    Inventors: Tong Wang, Stephen Gately
  • Aminonapthoquinone compounds and pharmaceutical composition for blocking ubiquitination-proteasome system in diseases
    Patent number: 10577328
    Abstract: The invention relates to a compound of formula (I) with low cytotoxicity for blocking the ubiquitination-proteasome system in diseases. Accordingly, these compounds can be used in treatment of disorders including, but not limited to, multiple myeloma, cancers, neurodegenerative diseases, inflammatory disorders, autoimmune disorders and metabolic disorders.
    Type: Grant
    Filed: July 23, 2015
    Date of Patent: March 3, 2020
    Assignee: Taipei Medical University
    Inventors: Yun Yen, Jing-ping Liou, Shiow-lin Pan
  • Cycloartane tetracyclic triterpenoid compound, preparation method therefor and use thereof
    Patent number: 10568892
    Abstract: The present invention relates to the field of natural medicine and pharmaceutical chemistry, and in particular relates to a cycloartane tetracyclic triterpenoid compound (I), a preparation method thereof and the medical use thereof. The pharmacodynamic tests demonstrate that the compound of the present invention has a pharmacodynamic activity on heart and cerebral vessels and can be used to prevent or treat cardiovascular and/or cerebrovascular diseases such as arrhythmia, myocardial infarction, and coronary heart disease or the like.
    Type: Grant
    Filed: February 3, 2017
    Date of Patent: February 25, 2020
    Assignees: Hefei Cosource Pharmaceuticals Inc., Hefei Blooming Drug Safety Evaluation Co., Ltd.
    Inventors: Shanchun Zhang, Shu Gao, Xiaorong Lu, Hongzhang Sun, Yijun Bao, Bin Yang, Jiashi Peng
  • Synthesis of sulfur containing ammonium and phosphonium borates
    Patent number: 10562871
    Abstract: The present disclosure relates to the preparation of sulfur containing ammonium and phosphonium borates KA, wherein K is a compound of formula (I), and A is an anion of formulae (IIa) or (IIb) by bringing into contact ammonium borates with sulfur containing ammonium or phosphonium halides or sulfonates.
    Type: Grant
    Filed: August 31, 2018
    Date of Patent: February 18, 2020
    Assignee: Gotion Inc.
    Inventors: Nicole Holub, Juergen Herbel
  • Phosphorus-containing heterocycles and a method for making and using
    Patent number: 10556920
    Abstract: Disclosed embodiments concern a phosphorus-containing heterocyclic compound according to the formula One exemplary compound is Certain embodiments fluoresce with excitation by light. The compounds are useful as fluorescent probes and as bioisosteres. In some embodiments, the compounds are bioisosteres of alpha-quinolones. Also disclosed is a method for making the compounds.
    Type: Grant
    Filed: December 21, 2017
    Date of Patent: February 11, 2020
    Assignee: University of Oregon
    Inventors: Chris Vonnegut, Airlia Shonkwiler, Michael Haley, Darren Johnson
  • NLRP3 modulators
    Patent number: 10556903
    Abstract: This disclosure features compounds of Formula I, or a pharmaceutically acceptable salt thereof: in which R1, R2, R3, and R4 are as defined herein. These compounds are modulators of NLRP3, which are useful, e.g., for treating a condition, disease or disorder in which a decrease in NLRP3 activity (e.g., a condition, disease or disorder associated with repressed or impaired NLRP3 signaling) contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., cancer) in a subject (e.g., a human). This disclosure also features compositions as well as other methods of using and making the same.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: February 11, 2020
    Assignee: Innate Tumor Immunity, Inc.
    Inventors: Gary D. Glick, Shomir Ghosh, William R. Roush, Edward James Olhava
  • Quinazolinone and benzotriazinone compounds with cholinergic muscarinin M1 receptor positive allosteric modulator activity
    Patent number: 10548899
    Abstract: The present invention provides a compound which has a cholinergic muscarinic M1 receptor positive allosteric modulator activity and may be useful as a medicament such as an agent for the prophylaxis or treatment of Alzheimer's disease, schizophrenia, pain, sleep disorder, Parkinson's disease dementia, Lewy body dementia and the like. The present invention relates to a compound represented by the formula (I) or a salt thereof. In the formula (I), each symbol is as described in the attached specification.
    Type: Grant
    Filed: October 19, 2016
    Date of Patent: February 4, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Takahiro Sugimoto, Shinkichi Suzuki, Hiroki Sakamoto, Masami Yamada, Minoru Nakamura, Makoto Kamata, Kenichiro Shimokawa, Masaki Ogino, Eiji Kimura, Masataka Murakami, Takuto Kojima, Jinichi Yonemori
  • 4,5-substituted picolinamide and picolinonitrile metabotropic glutamate receptor 2 negative allosteric modulators
    Patent number: 10538491
    Abstract: 4,5-Substituted Picolinamide and picolinonitrile compounds of formula (I), where R4 is CONH2 or CN and R1 is an optionally substituted aryl or heteroaryl, are negative allosteric modulators of the metabotropic glutamate receptor 2 (mGlu2). The compounds and pharmaceutical compositions including the compounds may be useful for treating depression, anxiety, obsessive-compulsive disorder, cognitive disorders, Alzheimer's disease, or autism spectrum disorders in a subject.
    Type: Grant
    Filed: March 16, 2016
    Date of Patent: January 21, 2020
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Kyle A. Emmitte, Andrew S. Felts, Katrina A. Bollinger