Patents Examined by Rebecca L. Anderson
  • Patent number: 10308668
    Abstract: Compounds of Formula II, wherein X is selected from chloro, fluoro, bromo and iodo, R1 and R2 are each independently selected from H, —CH3, —CH2CH3, —CH2CH2CH3, or —CH(CH3)2; compositions containing them, their use in therapy, including their use as anti-mycobacterial agents, for example in the treatment of a mycobacterial infection in a mammal, and methods for the preparation of such compounds, are provided.
    Type: Grant
    Filed: October 24, 2017
    Date of Patent: June 4, 2019
    Assignees: GlaxoSmithKline Intellectual Property (No. 2) Limited, Anacor Pharmaceuticals, Inc.
    Inventors: Michael Richard Kevin Alley, Vincent Hernandez, Jacob J. Plattner, Xianfeng Li, David Barros-Aguirre, Ilaria Giordano
  • Patent number: 10301291
    Abstract: The present invention relates to a novel imidazole derivative having a C-Jun N-terminal kinase (JNK) inhibitory activity and a use thereof. A novel imidazole derivative or a pharmaceutically acceptable salt thereof according to the present invention exhibits an excellent inhibitory activity against C-Jun N-terminal kinase (JNK), and thus it is anticipated that a more fundamental approach and target treatment will be possible in the prevention or treatment of degenerative brain nervous system diseases.
    Type: Grant
    Filed: January 25, 2017
    Date of Patent: May 28, 2019
    Inventors: Jung-Mi Hah, Song I Yang, Jung Hun Lee
  • Patent number: 10300061
    Abstract: Aminothiazole compounds of Formula (I) shown below and pharmaceutical compositions containing one of such compounds: Also disclosed are methods of inhibiting a tyrosine kinase and treating cancer associated with a tyrosine kinase with one of the aminothiazole compounds.
    Type: Grant
    Filed: June 13, 2018
    Date of Patent: May 28, 2019
    Assignee: National Health Research Institutes
    Inventors: Weir-Torn Jiaang, Chuan Shih, Hui-Jen Tsai
  • Patent number: 10301296
    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: June 27, 2018
    Date of Patent: May 28, 2019
    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
  • Patent number: 10301319
    Abstract: The invention provides novel cytotoxic compounds and cytotoxic conjugates comprising these cytotoxic compounds and cell-binding agents. More specifically, this invention relates to novel thailanstatin A analogs, useful as cytotoxic small molecule toxins in antibody-drug conjugates (ADCs). The present invention further relates to compositions including these cytotoxic compounds and ADCs, and methods for using these toxins and ADCs to treat pathological conditions including cancer.
    Type: Grant
    Filed: September 19, 2018
    Date of Patent: May 28, 2019
    Assignee: pH Pharma Co., Ltd.
    Inventors: Vasu Jammalamadaka, Sanjeev Satyal, Hoyoung Huh
  • Patent number: 10294207
    Abstract: Provided is pyrazole derivatives as a TNIK (Traf2- and NCK-interacting kinase), IKK? (I-kappa-B kinase epsilon) and TBK1 (TANK-binding kinase 1) inhibitor; the pyrazole derivative according to the present invention effectively inhibits TNIK, IKK? and TBK1, and thus is useful not only as an anticancer agent for the treatment of various cancers including colorectal cancer, breast cancer, CNS cancer, colon cancer, non-small cell lung cancer, kidney cancer, prostate cancer, ovarian cancer, uterus cancer, stomach cancer, liver cancer, skin cancer, lung cancer, brain cancer, bladder cancer, esophageal cancer, pancreatic cancer, thyroid cancer, head and neck cancer, squamous cell carcinoma, osteosarcoma, B-cell or T-cell lymphoma, acute or chronic leukemia and multiple myeloma, but as a therapeutic agent for chronic inflammation.
    Type: Grant
    Filed: March 29, 2016
    Date of Patent: May 21, 2019
    Inventors: Soongyu Choi, Kisoo Park, Hee Jeong Seo, Eun-Jung Park, Younggyu Kong, Ickhwan Son, Sang-ho Ma, Kwang-Seop Song, Min Ju Kim, So Ok Park, Man-Young Cha, Mi-Soon Kim, Sang Mi Kang, Dong Hyuk Jang, Jangwon Hong
  • Patent number: 10287240
    Abstract: Provided is a method for resolution of formula 4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxy-methyl benzonitrile as an enantiomer thereof, comprising the following steps: a salt of (S)-4-[4-dimethylamino-1-(4-fluorophenyl)-1-hydroxylbutyl]-3-hydroxymethyl benzonitrile with a resolving agent D-(+)di-p-toluoyl tartaric acid was crystallized in a resolving solvent; the method is characterized in that the resolving solvent is an ether solvent. Also provided is a new crystal form of the resolved intermediate.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: May 14, 2019
    Assignee: Zhejiang Hushai Pharmaceuticals Co., Ltd.
    Inventors: Zunjun Liang, Siqi Hu, Caihua Peng, Wenfeng Huang, Qifeng Lu, Guoliang Tu
  • Patent number: 10280161
    Abstract: Disclosed herein are aztreonam derivatives, therapeutic methods of using the aztreonam derivatives, particularly in combination with ?-lactamase inhibitors, and pharmaceutical compositions thereof. The aztreonam derivatives can be administered orally to provide orally bioavailable aztreonam.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: May 7, 2019
    Inventors: Eric M. Gordon, Matthew A. J. Duncton, John Freund
  • Patent number: 10280166
    Abstract: Indazole compounds for treating various diseases and pathologies are disclosed. More particularly, the present invention concerns the use of an indazole compound or analogs thereof, in the treatment of disorders characterized by the activation of Wnt pathway signaling (e.g., cancer, abnormal cellular proliferation, angiogenesis, fibrotic disorders, bone or cartilage diseases, and osteoarthritis), the modulation of cellular events mediated by Wnt pathway signaling, as well as genetic diseases and neurological conditions/disorders/diseases due to mutations or dysregulation of the Wnt pathway and/or of one or more of Wnt signaling components. Also provided are methods for treating Wnt-related disease states.
    Type: Grant
    Filed: June 22, 2018
    Date of Patent: May 7, 2019
    Assignee: Samumed, LLC
    Inventors: Sunil Kumar KC, David Mark Wallace, Jianguo Cao, Chandramouli Chiruta, John Hood
  • Patent number: 10273218
    Abstract: The present application relates to compounds of any one of Formulae I, Ia, Ib, Ic, Id, Ie, and If. Compounds of Formula (I) have the structure: wherein A, B, W, Y, Z, R2, R4, R5, R6, Rq and q are as defined herein. The compounds can be used as inhibitors of Bcl-3 and can be used for the treatment of cancer, particularly metastatic cancer.
    Type: Grant
    Filed: July 31, 2015
    Date of Patent: April 30, 2019
    Assignee: University College Cardiff Consultants Limited
    Inventors: Andrew David Westwell, Andrea Brancale, Richard William Ernest Clarkson
  • 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
  • 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
    Inventors: Yuk-Ching Tse-Dinh, Dianqing Sun
  • 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
  • Patent number: 10259811
    Abstract: Compounds having the following formula (I) and methods of their use and preparation are disclosed:
    Type: Grant
    Filed: July 24, 2018
    Date of Patent: April 16, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Zhimin Du, Juan Arnaldo Guerrero, Joshua Aaron Kaplan, John Edward Knox, Jr., Devan Naduthambi, Barton W. Phillips, Chandrasekar Venkataramani, Peiyuan Wang, William J. Watkins, Jeff Zablocki
  • 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
  • Patent number: 10253019
    Abstract: Compounds having the following formula (I) and methods of their use and preparation are disclosed:
    Type: Grant
    Filed: June 27, 2018
    Date of Patent: April 9, 2019
    Assignee: Gilead Sciences, Inc.
    Inventors: Zhimin Du, Juan A. Guerrero, Joshua A. Kaplan, John E. Knox, Jr., Jennifer R. Lo, Scott A. Mitchell, Devan Naduthambi, Barton W. Phillips, Chandrasekar Venkataramani, Peiyuan Wang, William J. Watkins, Zhongdong Zhao
  • 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
  • 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
  • Patent number: 10251847
    Abstract: Disclosed herein are polymorphic and amorphous forms of anhydrate, hydrate, and solvates of (R)-2-hydroxy-2-methyl-4-(2,4,5-trimethyl-3,6-dioxocyclohexa-1,4-dienyl)butanamide and methods of using such compositions for treating or suppressing oxidative stress disorders, including mitochondrial disorders, impaired energy processing disorders, neurodegenerative diseases and diseases of aging. Further disclosed are methods of making such polymorphic and amorphous forms.
    Type: Grant
    Filed: December 16, 2015
    Date of Patent: April 9, 2019
    Inventors: Paul Mollard, Christopher R. Cornell, Kieron E. Wesson, Peter Giannousis, Shazad Suchit, Mahmoud Mirmehrabi
  • Patent number: 10253043
    Abstract: The invention relates to the novel products of formula (I) with p, q=0, 1 or 2; R1=phenyl, pyridyl; —(CH2)m—Ra; alkylene; cycloalkyl; heterocycloalkyl; alkyl; —SO2 —Rb; —CO—Re; m=1 or 2; Ra=aryl, heteroaryl, —CO-cycloalkyl, —CO-heterocycloalkyl, —CO—Rb, —C(Rb)?N—ORc, —CO 2 Rd, —CONRxRy; Rb=alkyl, aryl, heteroaryl; Rc=H, alkyl; Rd=alkyl, cycloalkyl; Re=alkyl, cycloalkyl, aryl, heteroaryl; NRxRy with Rx,Ry=H, alkyl, cycloalkyl, alkoxy, phenyl, or form with N a ring with optionally O, N; R2, R3=H, alkyl, CF 3, or form with C a ring with optionally O, S and N; R4=H, F, Cl, CH3 or CN; the morpholine is substituted with Me, and optionally substituted with F, OH; or is (Formula 1a) and the isomer of configuration R,R (Formula 1b) these products being in all the isomer forms and the salts, as medicaments, in particular as anticancer medicaments.
    Type: Grant
    Filed: June 21, 2013
    Date of Patent: April 9, 2019
    Assignee: SANOFI
    Inventors: Youssef El-Ahmad, Bruno Filoche-Romme, Jean-Philippe Letallec, Gilbert Marciniak, Baptiste Ronan, Bertrand Vivet, Maurice Brollo