Patents Examined by Karen Cheng
  • Plasmodial surface anion channel inhibitors for the treatment or prevention of malaria
    Patent number: 10265313
    Abstract: The invention provides methods of treating or preventing malaria comprising administering to an animal an effective amount of a compound of formula I: Q-Y—R1—R2??(I), wherein Q, Y, R1, and R2 are as described herein. Methods of inhibiting a plasmodial surface anion channel of a parasite in an animal are also provided. The invention also provides pharmaceutical compositions comprising a compound represented by formula I in combination with any one or more compounds represented by formulas II, V, and VI. Use of the pharmaceutical compositions for treating or preventing malaria or for inhibiting a plasmodial surface anion channel in animals including humans are also provided. Also provided by the invention are clag3 amino acid sequences and related nucleic acids, vectors, host cells, populations of cells, antibodies, and pharmaceutical compositions.
    Type: Grant
    Filed: October 3, 2017
    Date of Patent: April 23, 2019
    Assignee: The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventor: Sanjay A. Desai
  • 3-acetylenyl-pyrazole-pyrimidine derivative, and preparation method therefor and uses thereof
    Patent number: 10266537
    Abstract: The present invention relates to the field of chemical and medicine, more particularly, 3-ethynylpyrazolopyrimidine derivatives and their preparation methods and uses. The invention provides a 3-ethynylpyrazolopyrimidine derivative, and the structure is shown in formula I. The present invention also provides preparation methods and use of 3-ethynylpyrazolopyrimidine derivatives, comprising the compounds and derivatives, and their pharmaceutical compositions for the use of the treatment and prevention of tumors.
    Type: Grant
    Filed: July 12, 2017
    Date of Patent: April 23, 2019
    Assignee: St. Chuan University
    Inventors: Shengyong Yang, Yuquan Wei
  • Olefin metathesis catalysts
    Patent number: 10265691
    Abstract: The present invention refers to novel ruthenium-based catalysts for olefin metathesis reactions, particularly to fast initiating catalysts having stereoselective properties. In olefin metathesis reactions, the disclosed catalysts provide a high catalytic activity combined with the capability to generate higher yields of the olefin metathesis product.
    Type: Grant
    Filed: July 8, 2016
    Date of Patent: April 23, 2019
    Assignee: Bergen Teknologioverforing AS
    Inventors: Vidar R. Jensen, Giovanni Occhipinti
  • Bacterial topoisomerase I inhibitors with antibacterial activity
    Patent number: 10266550
    Abstract: The present invention provides compounds as bacterial topoisomerase inhibitors with antibacterial activity. The present invention also provides pharmaceutical compositions comprising at least one of the compounds and methods of using the compounds and pharmaceutical compositions as antibacterial agents for treating infectious diseases.
    Type: Grant
    Filed: September 18, 2017
    Date of Patent: April 23, 2019
    Assignees: THE FLORIDA INTERNATIONAL UNIVERSITY BOARD OF TRUSTEES, UNIVERSITY OF HAWAII
    Inventors: Yuk-Ching Tse-Dinh, Dianqing Sun
  • Oxysterols and methods of use thereof
    Patent number: 10259840
    Abstract: Compounds are provided according to Formula (I) and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, Y, R1, R2a, R2b, R4a, R4b, R5a, R5b, R6a, R6b, R7, and R8 are as defined herein. Compounds of the present invention are contemplated useful for the prevention and treatment of a variety of conditions.
    Type: Grant
    Filed: June 18, 2015
    Date of Patent: April 16, 2019
    Assignee: Sage Therapeutics, Inc.
    Inventors: Boyd L. Harrison, Gabriel Martinez Botella, Albert Jean Robichaud, Francesco G. Salituro
  • Drug with antiviral activity (variants)
    Patent number: 10253037
    Abstract: The invention relates to the field of organic chemistry and medicine, and more particularly to synthetic substances of the pyrimidine series, namely 2-chloro-5-phenyl-5H-pyrimido[5?,4?:5,6]pyrano[2,3-d]pyrimidine-4-ol derivatives, having antiviral activity.
    Type: Grant
    Filed: April 6, 2016
    Date of Patent: April 9, 2019
    Inventors: Viktor Veniaminovich Tets, Georgy Viktorovich Tets
  • Amide compound and use of same for noxious arthropod control
    Patent number: 10251396
    Abstract: There is provided a noxious arthropod controlling agent containing an amide compound of formula (I): wherein R1 represents a C1-C8 chain hydrocarbon group optionally having one or more groups selected from Group A, R2 represents a hydrogen atom or the like, R3 represents a hydrogen atom or the like, R5 and R6 are the same or different, and independently represent a hydrogen atom or the like, Y represents an oxygen atom or the like, m represents 0, 1, 2, 3, 4, 5, 6 or 7, and Q represents a C1-C8 chain hydrocarbon group optionally having one or more atoms or groups selected from Group D.
    Type: Grant
    Filed: July 21, 2015
    Date of Patent: April 9, 2019
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hiromasa Mitsudera, Mayumi Okajima, Ayano Kowata, Kenichiro Awasaguchi, Kazuya Ujihara
  • Indanylaminopyrazinylcyclopropanecarboxylic acids, pharmaceutical compositions and uses thereof
    Patent number: 10253004
    Abstract: The present invention relates to compounds of formula I, wherein the groups R, R1, R2, R3, m and n are defined herein, which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
    Type: Grant
    Filed: January 22, 2018
    Date of Patent: April 9, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Matthias Eckhardt, Holger Wagner, Stefan Peters
  • Salt form of a human histone methyltransferase EZH2 inhibitor
    Patent number: 10245269
    Abstract: Provided herein is N-((4,6-dimethyl-2-oxo-1,2-dihydropyridin-3-yl)methyl)-5-(ethyl (tetrahydro-2H-pyran-4-yl)amino)-4-methyl-4?-(morpholinomethyl)-[1,1?-biphenyl]-3-carboxamide hydrobromide. Also provided herein is a particular polymorph form of this compound.
    Type: Grant
    Filed: December 11, 2017
    Date of Patent: April 2, 2019
    Assignees: Epizyme, Inc., Eisai R&D Management Co., Ltd.
    Inventors: Kevin Wayne Kuntz, Kuan-Chun Huang, Hyeong Wook Choi, Kristen Sanders, Steven Mathieu, Arani Chanda, Francis Fang
  • Carboxylic acid derivatives and use thereof in the preparation of prodrugs
    Patent number: 10239851
    Abstract: The present invention discloses a class of carboxylic acid derivatives and use thereof in preparation of prodrugs. The carboxylic acid derivatives have the general formula (I), wherein R1 is H or alkyl; X is H or F; Y is F or fluoroalkyl; n is 0, 1, 2, 3, 4, 5, or 6; W is W1 or W2; W1 is NR2R3, NR2R3.A, R2 and R3 are each independently H, alkyl, cycloalkyl, or a protecting group for amino; m is 0, 1, 2, or 3; A is an acid; W2 is COOR4, OPO(OR4)2, or PO(OR)2; R4 is H, or a protecting group for carboxyl or hydroxyl in phosphoric acid.
    Type: Grant
    Filed: February 16, 2015
    Date of Patent: March 26, 2019
    Inventor: Qingeng Li
  • Fused tricyclic heterocyclic compounds useful for treating HIV infection
    Patent number: 10233193
    Abstract: The present invention relates to Fused Tricyclic Heterocycle Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, Y, m, R1, R2, R3, R3, R3, R4, R5 and R9 are as defined herein. The present invention also relates to compositions comprising at least one Fused Tricyclic Heterocycle Derivative, and methods of using the Fused Tricyclic Heterocycle Derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: May 20, 2016
    Date of Patent: March 19, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Tao Yu, Thomas H. Graham, Sherman T. Waddell, John A. McCauley, Andrew W. Stamford, John M. Sanders, Lihong Hu, Jiaqiang Cai, Lianyun Zhao
  • Compounds for treating parasitic infections
    Patent number: 10227320
    Abstract: Compounds and compositions comprising them are provided. The compounds and compositions are useful for inhibiting transport of heme across membranes in parasitic heme auxotrophic organisms, thereby limiting their growth or killing the parasites.
    Type: Grant
    Filed: May 6, 2016
    Date of Patent: March 12, 2019
    Assignees: University of Maryland, College Park, University of Maryland, Baltimore
    Inventors: Iqbal Hamza, Fengtian Xue
  • Chiral dihydrobenzooxaphosphole ligands and synthesis thereof
    Patent number: 10221203
    Abstract: This invention relates to novel phosphorous ligands useful for organic transformations. Methods of making and using the ligands in organic synthesis are described. The invention also relates to processes for preparing the novel ligands.
    Type: Grant
    Filed: December 6, 2017
    Date of Patent: March 5, 2019
    Assignee: Boehringer Ingelheim International Gmbh
    Inventors: Jean-Nicolas Desrosiers, Daniel Robert Fandrick, Nizar Haddad, Guisheng Li, Nitinchandra D. Patel, Bo Qu, Sonia Rodriguez, Chris Hugh Senanayake, Joshua Daniel Sieber, Zhulin Tan, Xiao-Jun Wang, Nathan K. Yee, Li Zhang, Yongda Zhang
  • Processes to produce brivaracetam
    Patent number: 10221134
    Abstract: The present invention provides a scalable synthesis of enantiomerically pure brivaracetam, and related derivatives.
    Type: Grant
    Filed: May 24, 2016
    Date of Patent: March 5, 2019
    Assignee: Esteve Quimica S.A.
    Inventors: Peng Wang, Pixu Li, Qiang Wei, Yuanhua Liu
  • Fused heterocyclic compounds as GPR120 agonists
    Patent number: 10214521
    Abstract: The present invention relates to fused heterocyclic compound of Formula (I), a stereoisomer, a tautomer, a pharmaceutically acceptable salt, a pharmaceutically acceptable solvate, a prodrug, a polymorph, N-oxide, S-oxide, or a carboxylic acid isostere thereof; processes for their preparation; pharmaceutical compositions comprising said compounds; and their use for the treatment of the diseases or disorders mediated by GPR120 receptor.
    Type: Grant
    Filed: September 9, 2015
    Date of Patent: February 26, 2019
    Assignee: Piramal Enterprises Limited
    Inventors: Sanjay Kumar, Rajiv Sharma, Sangameshwar Prabhakar Sawargave, Vishal Mahajan
  • Compounds for treating spinal muscular atrophy
    Patent number: 10208067
    Abstract: The present invention provides compounds of formula (I) wherein A, X, Y, R1 and R2 are as described herein, as well as pharmaceutically acceptable salts thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as medicaments.
    Type: Grant
    Filed: November 16, 2017
    Date of Patent: February 19, 2019
    Assignee: HOFFMANN-LA ROCHE INC.
    Inventors: Robert Jack Gillespie, Hasane Ratni, Jerome Charles Sarie
  • Isoindoline compositions and methods for treating neurodegenerative disease
    Patent number: 10207991
    Abstract: Isoindoline sigma-2 receptor antagonist compounds, pharmaceutical compositions comprising such compounds, and methods for inhibiting Abeta-associated synapse loss or synaptic dysfunction in neuronal cells, modulating an Abeta-associated membrane trafficking change in neuronal cells, and treating cognitive decline associated with Abeta pathology are provided.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: February 19, 2019
    Assignee: COGNITION THERAPEUTICS, INC.
    Inventors: Gilbert M. Rishton, Susan M. Catalano, Gary C. Look
  • Alkyne-, azide- and triazole-containing flavonoids as modulators for multidrug resistance in cancers
    Patent number: 10208025
    Abstract: A triazole bridged flavonoid dimer compound library was efficiently constructed via the cycloaddition reaction of a series of flavonoid-containing azides (Az 1-15) and alkynes (Ac 1-17). These triazole bridged flavonoid dimers and their precursor alkyne- and azide-containing flavonoids were screened for their ability to modulate multidrug resistance (MDR) in P-gp-overexpressed cell line (LCC6MDR), MRP1-overexpressed cell line (2008/MRP1) and BCRP-overexpressed cell line (HEK293/R2 and MCF7-MX100). Generally, they displayed very promising MDR reversal activity against P-gp-, MRP1- and BCRP-mediated drug resistance. Moreover, they showed different levels of selectivity for various transporters. Overall, they can be divided into mono-selective, dual-selective and multi-selective modulators for the P-gp, MRP1 and BCRP transporters.
    Type: Grant
    Filed: October 18, 2016
    Date of Patent: February 19, 2019
    Assignees: The Hong Kong Polytechnic University, The Royal Institution for the Advancement of Learning/McGill University
    Inventors: Larry Ming Cheung Chow, Tak Hang Chan, Kin Fai Chan, Iris Lai King Wong, Man Chun Law
  • N-pyridinyl acetamide derivatives as Wnt signalling pathway inhibitors
    Patent number: 10202375
    Abstract: Disclosed are compounds useful as inhibitors of the Wnt signalling pathway. Specifically, inhibitors of Porcupine (Porcn) are contemplated by the invention. In addition, the invention contemplates processes to prepare the compounds and uses of the compounds. The compounds of the invention may therefore be used in treating conditions mediated by the Wnt signalling pathway, for example, in treating cancer, sarcoma, melanoma, skin cancer, haematological tumors, lymphoma, carcinoma, and leukemia; or enhancing the effectiveness of an anti-cancer treatment.
    Type: Grant
    Filed: October 8, 2015
    Date of Patent: February 12, 2019
    Assignee: Redx Pharma PLC
    Inventors: Inder Bhamra, Michael Mathieson, Craig Donoghue, Richard Testar
  • Compounds and their use
    Patent number: 10201532
    Abstract: Described herein are compounds and their use in the treatment of infections. The compound of formula (I), their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, solvates, pharmaceutically acceptable salts and pharmaceutical compositions described herein are also useful as ?-lactamase inhibitors, which restore or enhance the antibiotic spectrum of a suitable antibiotic agent. The compounds of formula (I) act as inhibitors of ?-lactamases. These compounds restore/potentiate the activities of ?-lactam antibiotics against carbapenemases. These compounds find use in diagnostic method for detecting ?-lactamases.
    Type: Grant
    Filed: November 25, 2011
    Date of Patent: February 12, 2019
    Assignee: ALLECRA THERAPEUTICS GMBH
    Inventors: Senthilkumar Udayampalayam Palanisamy, Maneesh Paul-Satyaseela, Shridhar Narayanan, Gopalan Balasubramanian, Aravind Appu, Senthilnathan Manickam, Hariharan Periasamy