Patents Examined by Kahsay Habte
  • Tetracyclic heteroaryl compounds
    Patent number: 11407765
    Abstract: The specification relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
    Type: Grant
    Filed: May 7, 2019
    Date of Patent: August 9, 2022
    Assignee: AstraZeneca, AB
    Inventors: Jason Grant Kettle, Sharanjeet Kaur Bagal, Andrew John Eatherton, Shaun Michael Fillery, Graeme Richard Robb, Scott Gibson Lamont, Paul David Kemmitt, Frederick Woolf Goldberg
  • Materials and methods useful to induce cancer cell death via methuosis or autophagy or a combination thereof
    Patent number: 11406626
    Abstract: Compounds, compositions, and methods useful for inducing cancer cell death via methuosis, autophagy, or a combination thereof, are described. The compounds have a 4-pyridyl group linked by a heterocyclic group to an aryl, heteroaryl, aralkyl, or heteroaryl alkyl.
    Type: Grant
    Filed: September 26, 2018
    Date of Patent: August 9, 2022
    Assignee: The University of Toledo
    Inventors: Amit K. Tiwari, Chandrabose Karthikeyan, Haneen Amawi, Paul W. Erhardt, Piyush Trivedi
  • Alkoxybenzo-five-membered (six-membered) heterocyclic amine compound and pharmaceutical use thereof
    Patent number: 11396504
    Abstract: Alkoxybenzeno five- or six-member heterocyclic amines compounds, their pharmaceutically acceptable salts, and pharmaceutical compositions are used as the active ingredients, and their application in drugs which can prevent and cure diseases caused by abnormal increasing of SM. These diseases caused by abnormal increasing of SM include atherosclerosis, type II diabetes, fatty liver, obesity, metabolic syndromes, enteritis and other inflammatory diseases.
    Type: Grant
    Filed: January 21, 2019
    Date of Patent: July 26, 2022
    Assignee: FUDAN UNIVERSITY
    Inventors: Deyong Ye, Mingguang Mo, Jintong Yang, Lu Zhou, Yong Chu, Jinyu Fei, Xiangyu Qi
  • Modulators of estrogen receptor proteolysis and associated methods of use
    Patent number: 11384063
    Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of estrogen receptor (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a cereblon, Von Hippel-Lindau ligase-binding moiety, Inhibitors of Apotosis Proteins, or mouse double-minute homolog 2 ligand, which binds to the respective E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.
    Type: Grant
    Filed: March 5, 2020
    Date of Patent: July 12, 2022
    Assignee: ARVINAS OPERATIONS, INC.
    Inventors: Andrew P. Crew, Hanqing Dong, Jing Wang, Yimin Qian
  • Tetrahydroisoquinoline derivative, preparation method therefor and use thereof
    Patent number: 11384097
    Abstract: Provided are a tetrahydroisoquinoline derivative, a preparation method therefor and an application thereof in medicine. In particular, provided are a tetrahydroisoquinoline derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as an angiotensin II type 2 receptor (AT2R) antagonist, wherein definitions of substituent groups in the general formula (I) are the same as definitions in the description.
    Type: Grant
    Filed: June 18, 2019
    Date of Patent: July 12, 2022
    Assignee: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.
    Inventors: Yanghui Guo, Xiangui Huang, Weiwei Liao, Lichen Meng, Taishan Hu, Lei Chen, Guoping Jiang
  • Quinolinone compounds
    Patent number: 11384075
    Abstract: The invention relates to new quinolinone compounds, to pharmaceutical compositions comprising said compounds, to processes for the preparation of said compounds and to the use of said compounds as FGFR (fibroblast growth factor receptor) inhibitors and to their use in the treatment of diseases, e.g. cancer.
    Type: Grant
    Filed: June 26, 2018
    Date of Patent: July 12, 2022
    Assignee: Janssen Pharmaceutica NV
    Inventors: Haibing Guo, Zhao-Kui Wan, Luoheng Qin, Qian Liu, Wing Shun Cheung
  • 2-amino-n-heteroaryl-nicotinamides as Na1.8 inhibitors
    Patent number: 11377438
    Abstract: Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are inhibitors of Nav1.8 channel activity and may be useful in the treatment, prevention, management, amelioration, control and suppression of diseases mediated by Nav1.8 channel activity. The compounds of the present invention may be useful in the treatment, prevention or management of pain disorders, cough disorders, acute itch disorders, and chronic itch disorders.
    Type: Grant
    Filed: October 31, 2019
    Date of Patent: July 5, 2022
    Assignee: Merck Sharp & Dohme LLC
    Inventors: Ashok Arasappan, Ian M. Bell, Michael J. Breslin, Christopher James Bungard, Christopher S. Burgey, Harry R. Chobanian, Jason M. Cox, Anthony T. Ginnetti, Deodial Guy Guiadeen, Kristen L. G. Jones, Mark E. Layton, Hong Liu, Jian Liu, James J. Perkins, Shawn J. Stachel, Linda M. Suen-Lai, Zhe Wu
  • Inhibitors of RAF kinases
    Patent number: 11377431
    Abstract: Provided herein are inhibitors of receptor tyrosine kinase effector, RAF, pharmaceutical compositions comprising said compounds, and methods for using said compounds for the treatment of diseases.
    Type: Grant
    Filed: October 11, 2021
    Date of Patent: July 5, 2022
    Assignee: KINNATE BIOPHARMA INC.
    Inventors: Stephen W. Kaldor, Toufike Kanouni, Eric Murphy, Jason Cox, Robert Kania
  • Lanthionine C-like protein 2 ligands, cells prepared therewith, and therapies using same
    Patent number: 11377437
    Abstract: Provided are compounds that target the lanthionine synthetase C-like protein 2 pathway. The compounds can be used to treat a number of conditions, including autoimmune diseases, inflammatory diseases, chronic inflammatory diseases, diabetes, and infectious diseases, such as lupus, Sjögren's syndrome, rheumatoid arthritis, type 1 diabetes, inflammatory bowel disease, viral diseases, and nonalcoholic steatohepatitis. The compounds can also be used to generate cells, such as immune cells, for treating the conditions.
    Type: Grant
    Filed: August 2, 2021
    Date of Patent: July 5, 2022
    Assignee: LANDOS BIOPHARMA, INC.
    Inventors: Josep Bassaganya-Riera, Andrew Leber, Raquel Hontecillas
  • Crystalline solid forms of a BET inhibitor
    Patent number: 11377446
    Abstract: The present application relates to crystalline solid forms of an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of diseases such as cancer.
    Type: Grant
    Filed: December 18, 2020
    Date of Patent: July 5, 2022
    Assignee: Incyte Corporation
    Inventors: Shili Chen, Zhongjiang Jia, Pingli Liu, Lei Qiao, Yongzhong Wu, Jiacheng Zhou, Qun Li
  • Modulators of stimulator of interferon genes (STING)
    Patent number: 11377440
    Abstract: Disclosed are compounds having the formula: (I) wherein q, r, s, A, B, C, RA1, RA2, RB1, RB2, RC1, RC2, R3, R4, R5, R6, R14, R15, R16, R17, Rx, and Ry are as defined herein, or a tautomer thereof, or a salt, particularly a pharmaceutically acceptable salt, thereof.
    Type: Grant
    Filed: October 4, 2018
    Date of Patent: July 5, 2022
    Assignee: GlaxoSmithKline Intellectual Property Development Limited
    Inventors: David T. Fosbenner, Todd L. Graybill, Jianxing Kang, Bryan W. King, Yunfeng Lan, Lara Kathryn Leister, Mukesh K. Mahajan, John F. Mehlmann, Angel I. Morales-Ramos, George Scott Pesiridis, Joshi M. Ramanjulu, Joseph J. Romano, Stuart Paul Romeril, Mark J. Schulz, Huiqiang Zhou, Junya Qu
  • Small molecule Wnt inhibitor as treatment for dyslipidemia
    Patent number: 11369609
    Abstract: Compositions and methods for treating cardiovascular diseases and dyslipidemias are provided. The compositions can inhibit Wnt signaling and can reduce inflammation. The levels of cholesterol can be reduced when the compositions are administered to a subject, such as a human.
    Type: Grant
    Filed: May 1, 2020
    Date of Patent: June 28, 2022
    Assignee: YALE UNIVERSITY
    Inventor: Julie Goodwin
  • Pyrazole compounds, formulations thereof, and a method for using the compounds and/or formulations
    Patent number: 11370787
    Abstract: Disclosed herein are embodiments of a pyrazole compound according to formula I. Compositions comprising the compound, and a method for making the composition also are disclosed. The composition may comprise a carrier, such as a polymer and/or the composition may be a spray-dried formulation. Also disclosed is a method for using the compound and/or composition. The compound and/or composition may be useful to inhibit an IRAK protein and/or to ameliorate, treat and/or prevent an IRAK-associated disease or condition in a subject.
    Type: Grant
    Filed: August 28, 2020
    Date of Patent: June 28, 2022
    Assignee: Rigel Pharmaceuticals, Inc.
    Inventors: Lu Chou, Matt Duan, Ihab Darwish, Simon Shaw, Somasekhar Bhamidipati, Vanessa Taylor, Yan Chen, Dazhong Fan, Zhushou Luo
  • Heteroaryl plasma kallikrein inhibitors
    Patent number: 11370803
    Abstract: The present invention provides compounds and compositions thereof which are useful as inhibitors of plasma kallikrein and which exhibit desirable characteristics for the same.
    Type: Grant
    Filed: September 17, 2020
    Date of Patent: June 28, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Nikolaos Papaioannou, Jeremy Mark Travins, Sarah Jocelyn Fink, John Mark Ellard, Alastair Rae
  • Triazolo-azepine derivatives
    Patent number: 11370802
    Abstract: The present invention relates to a compound of formula (I) wherein Ar is (II) or (II); R is CH3 or OCH3; or a pharmaceutically acceptable acid addition salt or a corresponding enantiomer thereof. The compounds are modulators of ?-secretase (A ?42) and may be useful for the treatment of Alzheimer's disease, cerebral amyloid angiopathy, hereditary cerebral hemorrhage with amyloidosis-Dutch type (HCHWA-D), multi-infarct dementia, dementia pugilistica or Down syndrome.
    Type: Grant
    Filed: January 21, 2019
    Date of Patent: June 28, 2022
    Assignee: Hoffmann-La Roche, Inc.
    Inventor: Hasane Ratni
  • Pyridine compound substituted with azole
    Patent number: 11365192
    Abstract: The present invention provides a compound represented by formula [I] shown below or a pharmaceutically acceptable salt thereof that has an inhibitory effect on 20-HETE producing enzyme.
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: June 21, 2022
    Assignee: TAISHO PHARMACEUTICAL CO., LTD.
    Inventors: Hiroaki Tanaka, Madoka Kawamura, Makoto Hamada, Yohei Kobashi, Yuji Ito, Kazuaki Suzuki, Ayako Bohno, Kosuke Funayama
  • Non-catalytic substrate-selective, p38?-specific MAPK inhibitors with endothelial-stabilizing and anti-inflammatory activity, and methods of use thereof
    Patent number: 11357781
    Abstract: Compounds that inhibit p38? MAPK protein, and methods of using the same, are provided for treating or preventing diseases such as cancer or inflammatory diseases.
    Type: Grant
    Filed: April 15, 2021
    Date of Patent: June 14, 2022
    Assignees: University of Maryland, Baltimore, The United States of America as represented by The Department of Veterans Affairs
    Inventors: Paul S. Shapiro, Alexander D. MacKerell, Jr., Jeffrey D. Hasday
  • Thienopyrimidine derivatives as ACC inhibitors and uses thereof
    Patent number: 11352371
    Abstract: The present disclosure relates generally to thienopyrimidine compounds that bind to Acetyl-CoA Carboxylase (ACC) and act as inhibitors of ACC. The disclosure further relates to the use of the thienopyrimidine compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of ACC, including liver diseases such as non-alcoholic fatty liver disease (NAFLD) and non-alcoholic steatohepatitis (NASH).
    Type: Grant
    Filed: August 6, 2020
    Date of Patent: June 7, 2022
    Assignee: Gilead Sciences, Inc.
    Inventors: Jamie G. Bates, Ana Z. Gonzalez Buenrostro, Hongyan Guo, Xiaochun Han, Brian J. Kirby, Yurong Lai, Michael L. Mitchell, Gregg M. Schwarzwalder, James G. Taylor, Ting Wang
  • Methods of preparing inhibitors of influenza viruses replication
    Patent number: 11345700
    Abstract: A method of preparing Compound (1) or a pharmaceutically acceptable salt thereof: comprises: (a) reacting Compound (X): or a pharmaceutically acceptable salt thereof with Compound (Y): in the presence of a palladium catalyst and a carbonate or phosphate base to form compound (Z): or a pharmaceutically acceptable salt thereof; and (b) deprotecting the Ts group of Compound (Z) to form Compound (1) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: March 9, 2020
    Date of Patent: May 31, 2022
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Gerald J. Tanoury, William Aloysius Nugent, Vadims Dvornikovs, Peter Jamison Rose
  • Quaternary lactam compound and pharmaceutical use thereof
    Patent number: 11345679
    Abstract: A quaternary lactam compound of formula (I). The compound is used in the manufacture of a medicament for the treatment and/or prevention of thrombotic or thromboembolic disorders.
    Type: Grant
    Filed: March 29, 2019
    Date of Patent: May 31, 2022
    Assignee: SHANGHAI MEIYUE BIOTECH DEVELOPMENT CO., LTD.
    Inventors: Shanghai Yu, Yan Feng, Shiqiang Li, Xiaolin Wang, Zhilong Hu, Yawen Ding, Feihong Dai, Qian He, Chaodong Wang