Patents Examined by Amanda L Aguirre
  • Lanthanide toolbox for organelle specific molecular imaging
    Patent number: 10183956
    Abstract: The present invention relates to a water-soluble, simple, stable tris(N-(tert-butyl)acetamide) cyclen-based europium complex HGEu001 which exhibits the specific subcellular localization in the primary cilium with a quantum yield as high as 10% in water and a lifetime of 0.56 ms lifetime. In particular, the present invention provides simplicity of the design and synthesis of a complex. Comprehensive studies were performed in numerous cell lines, such as HeLa, SN-K-SH and MRC5; the motif structure, HGEu002, has also been synthesized as the negative control for in vitro imaging studies. The two photon in vitro imaging were done in three dimensions to emphasize on the specific localization in primary cilium of HGEu001. This is one of the very limited examples for direct primary cilium imaging.
    Type: Grant
    Filed: May 25, 2017
    Date of Patent: January 22, 2019
    Assignee: New Life Medicine Technology Company Limited
    Inventors: Ka Leung Wong, Hongguang Li, Chi Fai Chan, Rongfeng Lan
  • 1,3-thiazol-2-yl substituted benzamides
    Patent number: 10183937
    Abstract: The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: January 22, 2019
    Assignee: Bayer Aktiengesellschaft
    Inventors: Adam James Davenport, Nico Bräuer, Oliver Martin Fischer, Andrea Rotgeri, Antje Rottmann, Ioana Neagoe, Jens Nagel, Anne-Marie Godinho-Coelho, Jürgen Klar
  • Isoxazole carboxamides as irreversible SMYD inhibitors
    Patent number: 10179773
    Abstract: The present disclosure provides substituted isoxazole carboxamides having Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2a, R2b, R3a, R3b, X, n, and m are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula I to treat a disorder responsive to the blockade of SMYD proteins such as SMYD3 or SMYD2. Compounds of the present disclosure are especially useful for treating cancer.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: January 15, 2019
    Assignee: EPIZYME, INC.
    Inventors: Richard Chesworth, Megan Alene Cloonan Foley, Kevin Wayne Kuntz, Lorna Helen Mitchell, Jennifer C. Petter, Carl Eric Schwartz
  • Synthesis of chirally purified substituted benzothiazole diamines
    Patent number: 10179774
    Abstract: Methods for preparing chirally purified substituted 4,5,6,7-tetrahydro-benzothiazole diamines such as, for example, (6R)2-amino-4,5,6,7-tetrahydro-6-(propylamino)benzothiazole and purifying a dominant enantiomer of substituted 4,5,6,7-tetrahydro-benzothiazole diamines from entantiomerically enriched mixtures of substituted 4,5,6,7-tetrahydro-benzothiazole diamines are provided herein.
    Type: Grant
    Filed: December 5, 2016
    Date of Patent: January 15, 2019
    Assignee: Knopp Biosciences LLC
    Inventors: Prasad Raje, Rajendrakumar Reddy Gadikota, Jian-Xie Chen, Olga V. Lapina, John M. McCall
  • Heterocyclic compounds, process for preparation of the same and use thereof
    Patent number: 10174011
    Abstract: The present invention provides a heterocyclic compound represented by the formula (I), its stereoisomers, or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and their use in preparing a medicament for the prevention and/or treatment of central nervous system disease.
    Type: Grant
    Filed: March 9, 2015
    Date of Patent: January 8, 2019
    Assignees: SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES, SUZHOU VIGONVITA LIFE SCIENCES CO., LTD., TOPHARMAN SHANDONG CO., LTD.
    Inventors: Hualiang Jiang, Zhen Wang, Jianfeng Li, Rongxia Zhang, Yang He, Yongjian Liu, Minghao Bi, Zheng Liu, Guanghui Tian, Weiming Chen, Feipu Yang, Chunhui Wu, Yu Wang, Xiangrui Jiang, Jingjing Yin, Guan Wang, Jingshan Shen
  • Compound or salt thereof and contrast agent for optical imaging
    Patent number: 10172964
    Abstract: A compound having a high tumor accumulation rate, or a salt thereof, and a contrast agent for optical imaging are provided. A compound having at least one specific organic dye covalently bound to polyethylene glycol, or a salt thereof is provided.
    Type: Grant
    Filed: January 23, 2017
    Date of Patent: January 8, 2019
    Assignee: CANON KABUSHIKI KAISHA
    Inventors: Satoshi Ogawa, Masato Minami, Tatsuki Fukui
  • Natural product-based synthesis of novel anti-infective isothiocyanate- and isoselenocyanate-functionalized amphilectane diterpenes
    Patent number: 10173974
    Abstract: The marine natural product (?)-8,15-diisocyano-11(20)-amphilectene, isolated from the Caribbean sponge Svenzea flava, was used as scaffold to synthesize five new products, all of which were tested against laboratory strains of Plasmodium falciparum and Mycobacterium tuberculosis H37Rv. The scaffold contains two isocyanide units that are amenable to chemical manipulation, enabling them to be elaborated into a small library of sulfur and selenium compounds. The scaffold along with its isothio- and isoselenocyanate analogs has low to sub-micro molar antiplasmodial activity.
    Type: Grant
    Filed: November 7, 2016
    Date of Patent: January 8, 2019
    Assignee: University of Puerto Rico
    Inventors: Abimael D. Rodríguez Pierluissi, Karinel Nieves Merced
  • 1,3-thiazol-2-yl substituted benzamides
    Patent number: 10174016
    Abstract: The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
    Type: Grant
    Filed: December 7, 2015
    Date of Patent: January 8, 2019
    Assignee: BEYER AKTIENGESELLSCHAFT
    Inventors: Adam James Davenport, Nico Bräuer, Oliver Martin Fischer, Andrea Rotgeri, Antje Rottmann, Ioana Neagoe, Jens Nagel, Anne-Marie Godinho-Coelho, Jürgen Klar
  • Synthesis of cyclopropyl indoles and cyclohepta[B]indoles, pharmaceutical compositions containing them and method of using them
    Patent number: 10174008
    Abstract: Methods of making indole analogs using a rhodium-containing catalyst are described, along with methods of using the compounds to treat hyperglycemic, hyperlipidemic, or autoimmune disorders in mammals, and corresponding pharmaceutical compositions. Disclosed herein is a method of making indoles. The method comprises contacting a reactant of formula I wherein E is a protecting group, —SO2-Aryl, or —SO2-substituted-Aryl; and R and R2 are independently selected from the group consisting of hydrogen, halo, C1-C12-alkyl and aryl; with a rhodium(1)-containing catalyst.
    Type: Grant
    Filed: December 3, 2015
    Date of Patent: January 8, 2019
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Weiping Tang, Xiaoxun Li
  • Amide derivatives of N-urea substituted amino acids as formyl peptide receptor like-1 (FPRL-1) receptor modulators
    Patent number: 10172832
    Abstract: The present invention relates to novel amide derivatives of N-urea substituted amino acids, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor like-1 (FPRL-1) receptor.
    Type: Grant
    Filed: April 10, 2018
    Date of Patent: January 8, 2019
    Assignee: ALLERGAN, INC.
    Inventors: Richard L. Beard, Tien T. Duong, John E. Donello, Veena Viswanath, Michael E. Garst
  • Methods for producing viloxazine salts and novel polymorphs thereof
    Patent number: 10160733
    Abstract: Provided here are methods of manufacture of viloxazine and its various salts, as well as viloxazine-related compounds, such as novel intermediate reaction products and polymorphs thereof. In particular, the methods provide a substantially pure API of viloxazine HCl while avoiding undesirable impurities. The methods further provide for separating, identifying, and characterizing novel polymorphs of viloxazine. Further provided are methods for synthesis and identification and characterization of novel intermediates of viloxazine, as well as for some important metabolites and precursors of metabolites of viloxazine.
    Type: Grant
    Filed: May 24, 2018
    Date of Patent: December 25, 2018
    Assignee: Supernus Pharmaceuticals, Inc.
    Inventors: Likan Liang, Padmanabh P. Bhatt, David Dain, Jean-Philippe Taquet, Aleksandr Pechenov, Alexei Tchesnokov, Reynold Mariaux
  • Process for preparing 3-chloro-2-vinylphenol
    Patent number: 10160707
    Abstract: The present invention describes a novel process for preparing 3-chloro-2-vinylphenol which, owing to the chemoselectivity achieved, also allows direct conversion into (3-chloro-2-vinylphenyl)methane-sulphonate.
    Type: Grant
    Filed: June 8, 2015
    Date of Patent: December 25, 2018
    Assignee: Bayer CropScience Aktiengesellschaft
    Inventors: Florian Erver, Mark James Ford
  • Consumer products comprising amino modified hydrocarbons
    Patent number: 10160935
    Abstract: Products selected from the group consisting of: hair conditioners, fabric softeners, skin moisturizers, shampoos, paper product additives, cosmetics, personal cleansing products, shave preparation products, detergents, non-woven additives, oral care products, and assembled products comprising treated paper or non-woven components, and comprising a polyisobutylene composition.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: December 25, 2018
    Assignee: The Procter & Gamble Company
    Inventors: Beth Ann Schubert, Luke Andrew Zannoni, Robert Joseph McChain
  • Methods of preparing tecovirimat
    Patent number: 10155723
    Abstract: Disclosed are methods for the preparation of Tecovirimat for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by the orthopoxvirus.
    Type: Grant
    Filed: June 21, 2018
    Date of Patent: December 18, 2018
    Assignee: Siga Technologies, Inc.
    Inventor: Dongcheng Dai
  • Anti-inflammatory zinc(II) complex
    Patent number: 10144748
    Abstract: The anti-inflammatory zinc(II) complex, viz., crystalline bis(chloro)-(N,N?-(2,2-dimethylpropane-1,3-diyl)bis(1-(2-chlorophenyl)-methanimine))-zinc zinc(II) complex, may be used as an anti-inflammatory. The compound has the formula: This complex is prepared by reaction of a Schiff base, namely, N,N?-bis(2-chlorobenzylidene)-2,2-dimethylpropane-1,3-diamine, with zinc chloride in alcohol to form a precipitate, which is removed by filtration, followed by slow evaporation of the filtrate to obtain the crystalline product. In vivo testing showed that the above zinc(II) complex exhibited good anti-inflammatory effect. It is thought that the present zinc-based anti-inflammatory avoids the gastrointestinal side effects of conventional NSAIDs due to the coordinated zinc complex.
    Type: Grant
    Filed: March 8, 2018
    Date of Patent: December 4, 2018
    Assignee: King Saud University
    Inventors: Mohammad Azam, Saud Ibrahim Al-Resayes, Faiyaz Shakeel, Agata Trzesowska-Kruszynska, Rafal Kruszynski
  • Benzenesulfonamide derivatives of quinoxaline, pharmaceutical compositions thereof, and their use in methods for treating cancer
    Patent number: 10137125
    Abstract: Benzenesulfonamide derivatives of quinoxaline that are kinase inhibitors, pharmaceutical compositions and methods of using these derivatives, e.g., for treatment of cancer are described.
    Type: Grant
    Filed: January 6, 2017
    Date of Patent: November 27, 2018
    Assignee: NEUPHARMA, INC.
    Inventors: Yong-Liang Zhu, Xiangping Qian
  • Aldosterone synthase inhibitors
    Patent number: 10131642
    Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein X, R1, R2 and R3 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: November 20, 2018
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Michael Balestra, Jörg M. Bentzien, Jennifer Burke, Derek Cogan, Xin Guo, Keith R. Hornberger, John Lord, Kenneth M. Meyers, Zhaoming Xiong, Maolin Yu, Zhonghua Zhang
  • Substituted dihydropyrrolopyrazole compound
    Patent number: 10131679
    Abstract: Provided is a compound represented by formula (I) or a pharmacologically acceptable salt thereof: wherein L1 is an optionally substituted C1-6 alkylene group or the like, L2 is a single bond or the like, L3 is a single bond or the like, R1, R2, and R3 are each independently an optionally substituted C1-4 alkyl group or the like, R4 is a hydrogen atom or the like, and R5 is a hydrogen atom or the like.
    Type: Grant
    Filed: October 30, 2015
    Date of Patent: November 20, 2018
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Yasuhiro Aga, Shigeru Ushiyama, Noriaki Iwase, Shigeyuki Kono, Hidetoshi Sunamoto, Takashi Matsushita, Sayaka Ogi, Masayuki Tanaka, Masaaki Matoyama, Satoshi Umezaki, Yusuke Shiraishi, Kazuhiro Onuma, Masahiro Kojima, Hayato Nishiyama, Tomio Kimura
  • Pyrazole derivatives and their uses thereof
    Patent number: 10130609
    Abstract: The present disclosure relates to a compound of formula (I) or a pharmaceutically acceptable salt thereof; wherein U, R1, R2, R3 and Q are as defined herein. The disclosure also provides a method for treating or preventing a method for the prevention, treatment and/or alleviation of one or more autoimmune or alloimmune disease, pharmaceutical compositions and combination comprising a therapeutically effective amount of a compound, as defined herein.
    Type: Grant
    Filed: March 12, 2014
    Date of Patent: November 20, 2018
    Assignees: UNIVERSITY HEALTH NETWORK, CANADIAN BLOOD SERVICES
    Inventors: Donald R. Branch, Lakshmi P. Kotra
  • Method of making cobalt and platinum based surfactants and using for cancer therapy
    Patent number: 10125160
    Abstract: A method of making benzidine hydrogen selenite complex with Cobalt and Platinum as surfactants is discussed. The resultant benzidine hydrogen selenite complex with either Cobalt or Platinum was characterized for its unique and superior properties. The complexes were characterized by elemental analysis, FTIR, and spectroscopy. The critical micelle concentration and thermodynamic parameters were calculated. The Values of IC50 were also calculated for the prepared complexes as well as their parent complex. The method of using the benzidine hydrogen selenite complex with cobalt and platinum as an antitumor agent to treat cancer is also demonstrated.
    Type: Grant
    Filed: January 26, 2015
    Date of Patent: November 13, 2018
    Assignee: Umm-Al-Qura University
    Inventors: Manal Mohamed Khowdiary, Ammona Salem Mohamed, Moshera Zaki Mohamed