Patents Examined by Rebecca L. Anderson
  • Sulfide alkyl compounds for HBV treatment
    Patent number: 10710959
    Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
    Type: Grant
    Filed: December 28, 2018
    Date of Patent: July 14, 2020
    Assignee: NOVIRA THERAPEUTICS, INC.
    Inventors: Austin Chen, Yalda Bravo, Nicholas Stock, Bijan Pedram, Jason Jacintho, Ryan C. Clark
  • Acyl phosphonamidates and acyl benzylamines that are Bcl family antagonists for use in clinical management of conditions caused or mediated by senescent cells and for treating cancer
    Patent number: 10703745
    Abstract: This disclosure provides compounds with Bcl inhibitory activity based on a new chemical scaffold. Acyl phosphonamidate compounds may include a P-phenyl phosphonamidate moiety which is N-acylated with an aroyl or heteroaroyl group. The P-phenyl phosphonamidate moiety can be optionally substituted at phosphorus with thio (?S) instead of oxo (?O), and/or with a thioxy group or a second amino group instead of an oxy group. One of the heteroatoms attached to phosphorus can be cyclically linked to a carbon atom of the adjacent phenyl ring attached to the phosphorus to provide, together with the phosphorus atom through which they are connected, a heterocyclic ring. By incorporating such a cyclic constraint between two phosphorus substituents of the core linking moiety a favorable binding conformation can be promoted in the compounds.
    Type: Grant
    Filed: May 29, 2019
    Date of Patent: July 7, 2020
    Assignee: Unity Biotechnology, Inc.
    Inventors: Anne-Marie Beausoleil, Ryan Hudson
  • Mono- or di-substituted indole derivatives as dengue viral replication inhibitors
    Patent number: 10696632
    Abstract: The present invention relates to mono- or di-substituted indole compounds, methods to prevent or treat dengue viral infections by using the compounds and also relates to use of the compounds as a medicine, more preferably for use as a medicine to treat or prevent dengue viral infections. The present invention furthermore relates to pharmaceutical compositions or combination preparations of the compounds, to the compositions or preparations for use as a medicine, more preferably for the prevention or treatment of dengue viral infections. The invention also relates to processes for preparation of the compounds.
    Type: Grant
    Filed: May 4, 2016
    Date of Patent: June 30, 2020
    Assignees: Janssen Pharmaceuticals, Inc., Katholieke Universiteit Leuven
    Inventors: Bart Rudolf Romanie Kesteleyn, Jean-François Bonfanti, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Dorothée Alice Marie-Eve Bardiot, Arnaud Didier M Marchand
  • C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker as BACE inhibitors, compositions, and their use
    Patent number: 10689401
    Abstract: In its many embodiments, the present invention provides certain C5-C6-oxacyclic fused iminothiazine dioxide compounds bearing an ether linker, including compounds Formula (I) or a tautomer thereof and pharmaceutically acceptable salts of said compounds and said tautomers, wherein R1, R2, R3, RA, ring A, m, n, -L1-, ring B, RB, and p are as defined herein. The novel compounds of the invention are useful as BACE inhibitors and/or for the treatment and prevention of various pathologies related thereto. Pharmaceutical compositions comprising one or more such compounds (alone and in combination with one or more other active agents), and methods for their preparation and use, including for the possible treatment of Alzheimer's disease, are also disclosed.
    Type: Grant
    Filed: February 6, 2017
    Date of Patent: June 23, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Wen-Lian Wu, Jared N. Cumming, Brandon M. Taoka, Xing Dai
  • Substituted 2, 3-dihydro-1H-inden-1-one retinoic acid-related orphan nuclear receptor antagonists for treating multiple sclerosis
    Patent number: 10682358
    Abstract: The present invention is directed to compounds, their synthesis, and their use as antagonists, inverse agonists, modulators and or inhibitors of the Retinoic acid-related orphan nuclear receptor ?t (ROR?t)/ROR?. The compounds of the present invention are useful for modulating ROR?t)/ROR? activity and for treating diseases or conditions mediated by ROR?t)/ROR? such as for example, disease states associated with immunopathology of human autoimmune diseases such as Multiple Sclerosis (MS), Rheumatoid Arthritis (RA), Inflammatory Colitis, Psoriasis, COPD, Pain, Obesity, Diabetes, Dyslipidemia, Osteoporosis, Asthma, Neurodegenerative diseases and Cancer.
    Type: Grant
    Filed: January 4, 2019
    Date of Patent: June 16, 2020
    Assignee: Arrien Pharmaceuticals LLC
    Inventors: Hariprasad Vankayalapati, Venkatakrishnareddy Yerramreddy
  • Heterocyclic derivatives and their use in the treatment of neurological disorders
    Patent number: 10683287
    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: April 9, 2019
    Date of Patent: June 16, 2020
    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
  • Phosphoinositide 3-kinase inhibitors with a zinc binding moiety
    Patent number: 10676482
    Abstract: The instant application relates to deazapurines, thienopyrimidines and furopyrimidines with zinc-binding moiety based derivatives and their use in the treatment of phosphoinositide 3-kinase related diseases and disorders such as cancer. The instant application further relates to the treatment of histone deacetylase related disorders and diseases related to both histone deacetylase and phosphoinositide 3-kinase.
    Type: Grant
    Filed: May 29, 2019
    Date of Patent: June 9, 2020
    Assignee: CURIS, INC.
    Inventors: Xiong Cai, Haixiao Zhai, Chengjung Lai, Changgeng Qian
  • Pegylated carfilzomib compounds
    Patent number: 10675353
    Abstract: The present invention provides a method of treating multiple myeloma using polymeric pegylated carfilzomib compounds, and pharmaceutically acceptable salts thereof, of Formula I wherein R1, R2, linker, PEG, n and o are as defined herein.
    Type: Grant
    Filed: November 5, 2019
    Date of Patent: June 9, 2020
    Assignee: AMGEN INC.
    Inventors: Gary Luehr, Shabbir T. Anik, Ge Peng, Irina Dotsenko, Pasit Phiasivongsa, Dante Romanini
  • Compounds for improving mRNA splicing
    Patent number: 10676475
    Abstract: Provided herein are compounds useful for improving mRNA splicing in a cell. Exemplary compounds provided herein are useful for improving mRNA splicing in genes comprising at least one exon ending in the nucleotide sequence CAA. Methods for preparing the compounds and methods of treating diseases of the central nervous system are also provided.
    Type: Grant
    Filed: January 15, 2016
    Date of Patent: June 9, 2020
    Assignees: The General Hospital Corporation, The United States of America, as Represented by the Secretary, Department of Health and Human Services
    Inventors: Susan A. Slaugenhaupt, Graham Johnson, William D. Paquette, Wei Zhang, Juan Marugan
  • Irreversible bruton's tyrosine kinase inhibitor
    Patent number: 10669238
    Abstract: The present invention provides an inhibitor of Bruton's tyrosine kinase, which is a compound of formula (I), or its pharmaceutically acceptable salt, solvate, ester, acid, metabolite or prodrug. The present invention also provides a pharmaceutical composition comprising the compound. The present invention also provides a method for inhibiting the activity of tyrosine kinase activity or for treating a disease, disorder, or condition, which would benefit from the inhibition of Bruton's tyrosine kinase(s), by using the Bruton's tyrosine kinase inhibitor, as well application of the Bruton's tyrosine kinase inhibitor for the same.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: June 2, 2020
    Assignee: HEFEI INSTITUTES OF PHYSICAL SCIENCE, CHINESE ACADEMY OF SCIENCES
    Inventors: Jing Liu, Qingsong Liu, Qianmao Liang, Yongfei Chen, Cheng Chen, Aoli Wang, Hong Wu, Kailin Yu, Wei Wang, Chen Hu, Wenchao Wang, Shuang Qi, Beilei Wang, Li Wang
  • Curcumin conjugates and methods of use thereof
    Patent number: 10660967
    Abstract: Curcumin-based conjugates and methods of use thereof are provided. Pharmaceutical compositions including an effective amount of one or more curcumin conjugates are also provided. In particular embodiments, the compositions are formulated for oral delivery. The conjugates and pharmaceutical compositions thereof can be administered to a subject in need thereof to treat a host of diseases and disorders including but not limited to, cancer, inflammation, and microbial growth.
    Type: Grant
    Filed: October 23, 2017
    Date of Patent: May 26, 2020
    Assignee: AUGUSTA UNIVERSITY RESEARCH INSTITUTE, INC.
    Inventor: Siva Panda
  • Nicotinic acetylcholine receptor silent agonists
    Patent number: 10662191
    Abstract: Derivatives of N,N-diethyl-N?-phenyl-piperazine, a silent agonist of the mammalian ?7 nicotinic acetylcholine receptor, are provided. These silent agonists control the desensitization state of the receptor. Further provided are pharmaceutical compositions that allow the administration of the silent agonists of the disclosure to a subject animal or human in need of treatment for a pathological condition arising from such as inflammation. The novel silent agonists also may be co-administered to a patient simultaneously or consecutively with a type II positive allosteric modulator to modulate the activity of the receptor.
    Type: Grant
    Filed: October 14, 2016
    Date of Patent: May 26, 2020
    Assignee: UNIVERSITY OF FLORIDA RESEARCH FOUNDATION INC.
    Inventors: Nicole Alana Horenstein, Roger Lee Papke, Marta Quadri
  • Benzimidazole derivatives as PI3 kinase inhibitors
    Patent number: 10660898
    Abstract: This invention relates to the use of benzimidazole derivatives for the modulation, notably the inhibition of the activity or function of the phosphoinositide 3? OH kinase family (hereinafter PI3 kinases), suitably, PI3K?, PI3K?, PI3K?, and/or PI3K?. Suitably, the present invention relates to the use of benzimidazoles in the treatment of one or more disease states selected from: autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, allergy, asthma, pancreatitis, multiorgan failure, kidney diseases, platelet aggregation, cancer, sperm motility, transplantation rejection, graft rejection and lung injuries. More suitably, the present invention relates to PI3K? selective benzimidazoles compounds for treating cancer.
    Type: Grant
    Filed: April 24, 2019
    Date of Patent: May 26, 2020
    Assignee: GLAXOSMITHKLINE LLC
    Inventors: Rosanna Tedesco, Junya Qu, Robert Sanchez, Ralph A. Rivero
  • Carboxamides as modulators of sodium channels
    Patent number: 10647661
    Abstract: Compounds, and pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels are provided. Also provided are pharmaceutical compositions comprising the compounds or pharmaceutically acceptable salts and methods of using the compounds, pharmaceutically acceptable salts, and pharmaceutical compositions in the treatment of various disorders, including pain.
    Type: Grant
    Filed: July 11, 2018
    Date of Patent: May 12, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Nadia Ahmad, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Joanne Louise Camp, Lev Tyler Dewey Fanning, Sara Sabina Hadida Ruah, Dennis Hurley, Yvonne Schmidt, David Shaw, Urvi Patel, Stephen Andrew Thomson, Lidio Marx Carvalho Meireles
  • Crystal form of imidazolone type compounds, and preparation method, pharmaceutical composition and use thereof
    Patent number: 10646483
    Abstract: The present invention relates to the crystal form of imidazolone type compounds, and a preparation method, pharmaceutical composition and use thereof, and falls within the field of pharmaceutical compound crystals. The crystal form provided by the present invention has a good stability, comprising good stability under the three extreme conditions of high temperature, high humidity and strong illumination, and can also maintain a good stability during the tablet compressing process. The crystal form provided by the present invention has good absorption and metabolism properties in vivo, comprising the drug concentration of blood, the drug concentration-time curve AUC, the half-life period, etc. In addition, the dissolving rate of the crystal form of the present invention is improved, wherein same is beneficial for the applications thereof in preparations.
    Type: Grant
    Filed: January 26, 2016
    Date of Patent: May 12, 2020
    Assignee: Foreland Pharma Co., Ltd.
    Inventors: Qi Ji, Zhenjian Du, Xingmin Zhang, Lei Wang, Congmin Gao, Longlong Gong
  • Bicyclic heterocyclyl derivatives as IRAK4 inhibitors
    Patent number: 10640517
    Abstract: The present invention provides bicyclic heterocyclyl kinase enzyme inhibitor compounds of formula (I), which are therapeutically useful as kinase inhibitors, particularly IRAK4 inhibitors. wherein A, Y, Z, X1, X2, X3, R1, R3, ‘m’, ‘n’ and ‘p’ have the meanings given in the specification and pharmaceutically acceptable salt or stereoisomer thereof that are useful in the treatment and prevention of diseases or disorder, in particular their use in diseases or disorder mediated by kinase enzyme, particularly IRAK4 enzyme. The present invention also provides pharmaceutical composition comprising at least one of the compounds of compound of formula (I) together with a pharmaceutically acceptable carrier, diluent or excipient therefor.
    Type: Grant
    Filed: August 3, 2018
    Date of Patent: May 5, 2020
    Assignee: Aurigene Discovery Technologies Limited
    Inventors: Venkateshwar Rao Gummadi, Susanta Samajdar
  • Compounds
    Patent number: 10624898
    Abstract: The invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.
    Type: Grant
    Filed: July 9, 2019
    Date of Patent: April 21, 2020
    Assignee: Glaxo Group Limited
    Inventors: Julie Nicole Hamblin, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Charlotte Jane Mitchell, Nigel James Parr
  • Nuclear transport modulators and uses thereof
    Patent number: 10617677
    Abstract: The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using the compounds, salts and compositions in the treatment of various disorders associated with CRM1 activity.
    Type: Grant
    Filed: July 17, 2018
    Date of Patent: April 14, 2020
    Assignee: Biogen MA Inc.
    Inventors: Vincent P. Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
  • Bicyclic heterocycle compounds and their uses in therapy
    Patent number: 10618895
    Abstract: The invention relates to new bicyclic heterocycle compounds, to pharmaceutical compositions comprising the compounds and to the use of the compounds in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: April 14, 2020
    Assignee: ASTEX THERAPEUTICS LIMITED
    Inventors: Gianni Chessari, Christopher Norbert Johnson, Steven Howard, James Edward Harvey Day, Ildiko Maria Buck, Charlotte Mary Griffiths-Jones, Gordon Saxty, Emiliano Tamanini, Nicola Elizabeth Wilsher
  • Solid forms of cannabidiol and uses thereof
    Patent number: 10604467
    Abstract: Disclosed herein are cocrystals of cannabidiol and a coformer containing 5-6 membered rings comprised of carbon and nitrogen atoms, wherein the 5-6 membered rings can be unsaturated or saturated and the rings contain 1 to 2 nitrogen atoms. Cocrystals of cannabidiol and a coformer selected from L-proline, D-proline, tetramethylpyrazine, and 4,4?-dipyridyl are also disclosed herein.
    Type: Grant
    Filed: April 26, 2019
    Date of Patent: March 31, 2020
    Assignee: Artelo Biosciences, Inc.
    Inventors: R. Martin Emanuele, Tanise Shattock-Gordon, Tabitha Williford, Mark Andres, Patricia Andres