Patents Examined by Rebecca L. Anderson
  • Patent number: 10738004
    Abstract: Provided is a compound, such as ethyl 6-((2-chloro-4-fluorobenzyl)sulfonyl) -3-hydroxycyclohex-1-ene-1-carboxylate or an optical isomer thereof, having a superior Toll-like receptor 4 (TLR4) signaling inhibitory action, which may be useful as a prophylactic or therapeutic drug for diseases such as autoimmune diseases and/or inflammatory diseases, or chemotherapy-induced peripheral neuropathy (CIPN), chemotherapy-induced neuropathic pain (CINP), liver failure, and ischemia reperfusion injury (IRI).
    Type: Grant
    Filed: September 7, 2017
    Date of Patent: August 11, 2020
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Toshitake Kobayashi, Morihisa Saitoh, Yasufumi Wada, Nobuyuki Negoro, Masashi Yamasaki, Takahiro Tanaka, Naomi Kitamoto
  • Patent number: 10738017
    Abstract: Substituted 1,2,3-triazole compounds are disclosed which have utility in the treatment of a variety of neurological disorders. The compounds provided herein have the general structure: wherein R1, R2, R3 and n are as defined herein, including stereoisomers, esters, solvates and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound provided herein in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for treating neurological disorders in a subject in need thereof.
    Type: Grant
    Filed: October 29, 2018
    Date of Patent: August 11, 2020
    Assignee: Neurocrine Biosciences, Inc.
    Inventors: Neil J. Ashweek, John P. Williams, Deborah Slee, Manisha Moorjani
  • Patent number: 10722593
    Abstract: Disclosed are compounds based on dolastatins, drug-conjugates, methods of preparing drug-conjugates, and uses thereof. Also disclosed are pharmaceutical compositions and methods of treatment. The compounds and drug-conjugates disclosed herein can be used to treat diseases such as bladder cancer, breast cancer, colon cancer, rectal cancer, endometrial cancer, kidney cancer, lung cancer, melanoma, non-Hodgkin lymphoma, glioblastoma, pancreatic cancer, prostate cancer, and thyroid cancer.
    Type: Grant
    Filed: September 27, 2016
    Date of Patent: July 28, 2020
    Assignee: SIRENAS LLC
    Inventors: Oliver Booth Vining, Venkata Rami Reddy Macherla, Alexander Wayne Schammel, Ippei Usui, Jacob Neal Beverage, Elizabeth Paige Stout, Bryan Junn Lee, Steven Bruce Cohen, Eduardo Esquenazi
  • Patent number: 10722497
    Abstract: Compounds of formula I: and pharmaceutically acceptable salts, hydrates, or solvates thereof, pharmaceutical compositions comprising the compounds of formula I, and methods of using such compounds and compositions to treat various disorders associated with CRM1 activity.
    Type: Grant
    Filed: May 16, 2019
    Date of Patent: July 28, 2020
    Assignee: Biogen MA Inc.
    Inventors: Vincent Sandanayaka, Sharon Shechter, Sharon Shacham, Dilara McCauley, Erkan Baloglu
  • Patent number: 10717716
    Abstract: The present invention relates to novel compounds having histone deacetylase 6 (HDAC6) in-hibitory activity, stereoisomers thereof or pharmaceutically acceptable salts thereof the use thereof for the preparation of therapeutic medicaments, pharmaceutical compositions containing the same, a method for treating diseases using the composition, and methods for preparing the novel compounds.
    Type: Grant
    Filed: August 4, 2016
    Date of Patent: July 21, 2020
    Assignee: Chong Kun Dang Pharmaceutical Corp.
    Inventors: Jaekwang Lee, Yuntae Kim, Chang Sik Lee, Hyeseung Song, Dal-Yong Gwak, Jaeyoung Lee, Jung Taek Oh, Chang Gon Lee, Il Hyang Kim
  • 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
  • Patent number: 10709712
    Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
    Type: Grant
    Filed: February 12, 2019
    Date of Patent: July 14, 2020
    Assignee: NOVARTIS AG
    Inventors: Robert John Aversa, Paul Andrew Barsanti, Matthew T. Burger, Michael Patrick Dillon, Alan Dipesa, Cheng Hu, Yan Lou, Gisele A. Nishiguchi, Yue Pan, Valery Rostislavovich Polyakov, Savithri Ramurthy, Alice C. Rico, Lina Quattrocchio Setti, Aaron Smith, Sharadha Subramanian, Benjamin R. Taft, Huw Roland Tanner, Lifeng Wan, Naeem Yusuff
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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
  • 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