Patents Examined by Po-Chih Chen
  • Substituted azaindoline derivatives as NIK inhibitors
    Patent number: 11236084
    Abstract: The present invention relates to pharmaceutical agents useful for therapy and/or prophylaxis in a mammal, and in particular to inhibitors of NF-?B-inducing kinase (NIK—also known as MAP3K14) useful for treating diseases such as cancer, inflammatory disorders, metabolic disorders and autoimmune disorders. The invention is also directed to pharmaceutical compositions comprising such compounds, and to the use of such compounds or pharmaceutical compositions for the prevention or treatment of diseases such as cancer, inflammatory disorders, metabolic disorders including obesity and diabetes, and autoimmune disorders.
    Type: Grant
    Filed: July 4, 2018
    Date of Patent: February 1, 2022
    Assignee: Janssen Pharmaceutica NV
    Inventors: George Hynd, Calum Macleod, Samuel Edward Mann, Janusz Jozef Kulagowski, Ian Stansfield, Olivier Alexis Georges Querolle, Virginie Sophie Poncelet, Gerhard Max Gross, Edgar Jacoby, Lieven Meerpoel
  • Heterocyclic compound
    Patent number: 11236099
    Abstract: The present invention aims to provide a compound that may be useful for the prophylaxis or treatment of constipation and the like. The present invention provides a compound represented by the following formula (I): wherein each symbol is as described in the specification, or a salt thereof.
    Type: Grant
    Filed: June 19, 2018
    Date of Patent: February 1, 2022
    Assignee: Takeda Pharmaceutical Company Limited
    Inventors: Kazuaki Takami, Masaki Seto, Shinobu Sasaki, Haruhi Ando, Masaki Ogino, Tomoko Ohashi, Toshihiro Imaeda, Ikuo Fujimori, Yasuhiro Tsukimi, Masami Yamada, Kenichiro Shimokawa, Takeshi Wakabayashi, Masataka Murakami, Makoto Fushimi, Tomohiro Okawa, Jinichi Yonemori, Tomohiro Ohashi, Hideo Suzuki, Hironobu Maezaki, Ayumu Sato, Yasutomi Asano, Steve Swann
  • Ester compound and PIN1 inhibitor, inflammatory disease therapeutic, and colon cancer therapeutic in which said ester compound is used
    Patent number: 11203565
    Abstract: An object of the present invention is to develop a therapeutic agent for an inflammatory disease such as an inflammatory bowel disease or NASH, which therapeutic agent shows less side effects and high effectiveness. The present invention provides a compound represented by Formula (I) or a salt thereof; and a Pin1 inhibitor, a pharmaceutical composition, a therapeutic agent or a prophylactic agent for an inflammatory disease, and a therapeutic agent or a prophylactic agent for colon cancer, containing the compound.
    Type: Grant
    Filed: November 29, 2017
    Date of Patent: December 21, 2021
    Assignees: Hiroshima University, Tokyo University of Pharmacy & Life Sciences, The University of Tokyo
    Inventors: Tomoichiro Asano, Yusuke Nakatsu, Hisanaka Ito, Takayoshi Okabe
  • 1-heterocyclyl isochromanyl compounds and analogs for treating CNS disorders
    Patent number: 11192885
    Abstract: Disclosed are compounds of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, Ra, R1, R2, R3, R4, R6, w and n1 are defined and described herein; compositions thereof; and methods of use thereof. These compounds are useful for treating a variety of neurological and psychiatric disorders, such as those described herein.
    Type: Grant
    Filed: May 6, 2019
    Date of Patent: December 7, 2021
    Assignees: Sunovion Pharmaceuticals Inc., PGI Drug Discovery LLC
    Inventors: Linghong Xie, Philip Glyn Jones, Kerry L. Spear, Noel Aaron Powell, Taleen G. Hanania, Vadim Alexandrov
  • Derivatives of 1-[(cyclopentyl or 2-pyrrolidinyl)carbonylaminomethyl]-4-(l,3-thiazol-5-yl) benzene which are useful for the treatment of proliferative, autoimmune or inflammatory diseases
    Patent number: 11179373
    Abstract: There is provided novel small molecule E3 ubiquitin ligase protein binding ligand compounds, having utility in PROteolysis Targeted Chimeras (PROTACs), as well as processes for the preparation thereof, and use in medicine. There is particularly provided PROTACs which bind to a protein within the bromo- and Extra-terminal (BET) family of proteins, and especially to PROTACs including novel small molecule E3 ubiquitin ligase protein binding ligand compounds which selectively induce degradation of the BRD4 protein within the bromodomain of the BET family of proteins.
    Type: Grant
    Filed: March 14, 2016
    Date of Patent: November 23, 2021
    Assignee: University of Dundee
    Inventors: Alessio Ciulli, Michael Zengerle, Kwok-Ho Chan
  • Amino sulfonyl compounds
    Patent number: 11168059
    Abstract: Provided herein are dUTPase inhibitors, compositions comprising such compounds and methods of using such compounds and compositions.
    Type: Grant
    Filed: November 21, 2017
    Date of Patent: November 9, 2021
    Assignee: CV6 Therapeutics (NI) Limited
    Inventor: Mark Spyvee
  • Compounds for the treatment of infection
    Patent number: 11168062
    Abstract: Clostridium difficile infection (CDI) is a public health threat that results in 14,000 annual deaths in the United States. Challenges involve the production of CDI spores that can remain dormant for years and the production of toxins that damage the gut. Current therapies for CDI include vancomycin and metronidazole, but neither inhibits spore or toxin production. Thus, recurrence of infection occurs in 25% of patients and there are no antibiotics that are effective for multiple recurrences. We describe oxadiazoles with activity against C. difficile, including the highly virulent NAP1/027 strain with increased production of toxins A and B, as well as the additional binary toxin. Oxadiazole 2 is poorly absorbed, thus advantageously achieving high concentrations in the gut. The compound targets peptidoglycan synthesis and inhibits vegetative cells, spores, and toxin production.
    Type: Grant
    Filed: September 12, 2017
    Date of Patent: November 9, 2021
    Assignee: University of Notre Dame du Lac
    Inventors: Mayland Chang, Shahriar Mobashery, Derong Ding
  • Neuroprotective compounds and methods of use
    Patent number: 11147795
    Abstract: The present invention provides compounds and methods for mitigating a clinical condition associated with a neurodegenerative disease or a locomotor dysfunction in a subject. In one particular aspect, the invention relates to compounds and methods for reducing TDP-43 aggregation or toxicity in a subject.
    Type: Grant
    Filed: July 18, 2019
    Date of Patent: October 19, 2021
    Assignee: Arizona Board of Regents on behalf of the University of Arizona
    Inventors: Jon T. Njardarson, Isaac Chogii, David Townsend Smith, Edon Vitaku, Daniela C. Zarnescu
  • Cell-permeable succinate compounds
    Patent number: 11147789
    Abstract: The present invention provides novel cell-permeable succinates and cell permeable precursors of succinateaimed at increasing ATP-production in mitochondria. The main part of ATP produced and utilized in the eukaryotic cell originates from mitochondrial oxidative phosphorylation, a process to which high-energy electrons are provided by the Kreb's cycle. Not all Kreb's cycle intermediates are readily permeable to the cellular membrane, one of them being succinate. The provision of the novel cell permeable succinates is envisaged to allow passage over the cellular membrane and thus the cell permeable succinates can be used to enhance mitochondrial ATP-output.
    Type: Grant
    Filed: April 8, 2015
    Date of Patent: October 19, 2021
    Assignee: ABLIVA AB
    Inventors: Eskil Elmer, Magnus Joakim Hansson, Karl Henrik Johannes Ehinger, Steven Moss
  • Crystalline forms of a MAGL inhibitor
    Patent number: 11142517
    Abstract: Described herein is the MAGL inhibitor 1,1,1,3,3,3-hexafluoropropan-2-yl 4-(2-(pyrrolidin-1-yl)-4-(trifluoromethyl)benzyl)piperazine-1-carboxylate, including crystalline forms and pharmaceutically acceptable salts and solvates thereof.
    Type: Grant
    Filed: November 15, 2017
    Date of Patent: October 12, 2021
    Assignee: H. LUNDBECK A/S
    Inventors: Cheryl A. Grice, Todd K. Jones, Kurt G. Grimm, Jacqueline Lorayne Blankman, Channing Rodney Beals
  • Heterocyclic ligands of PAR1 and methods of use
    Patent number: 11130743
    Abstract: The present invention provides novel compounds with increased plasma stability that modulate PAR1 signaling, and methods of using them. The present invention provides methods of using the novel PAR1 modulators for the treatment of a number of disorders, including, inflammation, thrombosis, kidney disease, sepsis, stroke, as well as proliferation-related diseases. Furthermore, the PAR1 modulators of the present invention provide cytoprotection for certain cells and tissues, for example, in coronary blood vessels and tissues after a heart attack.
    Type: Grant
    Filed: March 23, 2020
    Date of Patent: September 28, 2021
    Assignee: Marquette University
    Inventors: Christopher Dockendorff, Disha M. Gandhi, Ricardo Rosas, Jr.
  • Human TLR8-selective agonists
    Patent number: 11130736
    Abstract: The disclosure provides human toll-like receptor modulators of general Formula (II), wherein R1, R2, R3, R4, R5, R6, R7, R8 are defined herein.
    Type: Grant
    Filed: August 19, 2016
    Date of Patent: September 28, 2021
    Assignee: University of Kansas
    Inventors: Sunil A. David, Mallesh Beesu, Giuseppe Caruso, Alex Salyer
  • Topical formulations and treatments
    Patent number: 11129896
    Abstract: Provided is a pharmaceutical formulation and a method associated therewith for treating bacterial vaginosis. The pharmaceutical formulation includes from 10 to 25 weight parts of poloxamer F127, from 0.5 to 3.0 weight parts of xanthan gum, from 70 to 90 weight parts of water, and a therapeutically effective amount of a pharmaceutical active ingredient. The pharmaceutical formulation may also include from 0.5 to 1.5 weight parts of benzyl alcohol.
    Type: Grant
    Filed: July 18, 2016
    Date of Patent: September 28, 2021
    Assignee: Trilogic Pharma LLC
    Inventors: Hemant H. Alur, James A. H. Harwick
  • Compounds with circularly polarized luminescence
    Patent number: 11118111
    Abstract: The present subject matter relates to a fluorescent compound having aggregation-induced emission (AIE) characteristics. The compound can be a rod-like chiral luminogen bearing a chiral moiety at one end and long aliphatic chains at an opposing end. The compound emits circularly polarized light or luminescence (CPL) in the aggregate state. For example, the compound does not exhibit a chiroptical signal when dispersed in solution, but demonstrates tunable CPL signals in the aggregate state.
    Type: Grant
    Filed: November 12, 2019
    Date of Patent: September 14, 2021
    Assignee: THE HONG KONG UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Benzhong Tang, Wing Yip Lam, Fengyan Song
  • Solid forms of(Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl) benzoic acid
    Patent number: 11111239
    Abstract: The present invention provides new salts and crystalline forms of leukadherin LA1 [(Z)-4-(5-((3-benzyl-4-oxo-2-thioxothiazolidin-5-ylidene)methyl)furan-2-yl)benzoic acid] according to Formula I. Methods for preparation of the salts and crystalline forms are also described, as well as methods for treating ?2 integrin-mediated diseases and conditions using the salts and crystalline forms.
    Type: Grant
    Filed: November 5, 2019
    Date of Patent: September 7, 2021
    Assignee: GB006, INC.
    Inventor: Antonio J. Barbosa
  • Inhibitors of bruton's tyrosine kinase
    Patent number: 11104668
    Abstract: This application discloses compounds according to generic Formula (I): wherein all variables are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are useful for the treatment of oncological, auto-immune, and inflammatory diseases caused by aberrant B-cell activation. Also disclosed are compositions containing compounds of Formula (I) and at least one carrier, diluent or excipient.
    Type: Grant
    Filed: December 10, 2014
    Date of Patent: August 31, 2021
    Assignees: Hoffmann-La Roche Inc., Chugai Pharmaceutical Co.
    Inventors: Francisco Javier Lopez-Tapia, Sung-Sau So, Qi Qiao, Romyr Dominique
  • Polyamide compound and use thereof
    Patent number: 11084847
    Abstract: The invention relates to a polyamide compound and a use thereof. Specifically, the invention relates to a type of polyamide compound (which preferably comprise one or more amide bonds formed by condensation of same or different L-amino acids or D-amino acids), or stereoisomers, crystalline polymorphs, solvates, metabolites, prodrugs or pharmaceutically acceptable salts or esters thereof, or pharmaceutical compositions thereof, as well as a method for preparing the polyamide compound and a use thereof in the prevention or treatment of diseases associated with ?-opioid receptor. The polyamide compound of the invention has excellent ?-opioid receptor agonistic activity and hydrophilicity, thus having a lesser ability of penetrating the blood-brain barrier and a lower capacity for entering the brain.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: August 10, 2021
    Assignee: SICHUAN KELUN-BIOTECH BIOPHARMACEUTICAL CO., LTD.
    Inventors: Jiaqiang Cai, Qiang Tian, Mingliang Zhao, Hong Zeng, Hongmei Song, Nan Yu, Hua Deng, Wei Zhong, Long Yang, Lei Wu, Haitao Huang, Yongyong Wu, Donghai Su, Xin Zhou, Yuting Tan, Lichun Wang, Jingyi Wang
  • CFTR regulators and methods of use thereof
    Patent number: 11084795
    Abstract: Provided herein are compounds that activate CFTR and methods for treating constipation, dry eye disorders, and other diseases and disorders.
    Type: Grant
    Filed: December 23, 2016
    Date of Patent: August 10, 2021
    Assignee: The Regents of the University of California
    Inventors: Alan S. Verkman, Marc H. Levin, Onur Cil, Mark J. Kurth
  • Bis-phenyl-phenoxy polyolefin catalysts having two methylenetrialkylsilicon ligands on the metal for improved solubility
    Patent number: 11066489
    Abstract: Embodiments are directed to a catalyst system comprising metal ligand complexes and processes for polyolefin polymerization using the metal ligand complex having the following structure: where each X is selected from the group consisting of —(CH2)SiRX3.
    Type: Grant
    Filed: September 19, 2018
    Date of Patent: July 20, 2021
    Assignee: Dow Global Technologies LLC
    Inventors: Arkady L. Krasovskiy, David R. Wilson, Bryan D. Stubbert, Tulaza Vaidya, Jerzy Klosin, Edmund M. Carnahan, Philip P. Fontaine, Mari S. Rosen
  • Bis-phenyl-phenoxy polyolefin catalysts having a methylenetrialkylsilicon ligand on the metal for improved solubility
    Patent number: 11066428
    Abstract: Embodiments are directed to a catalyst system comprising metal-ligand complexes and processes for polyolefin polymerization using the metal-ligand complex having the following structure, Formula (I), where X is selected from the group consisting of —(CH2)SiRX3.
    Type: Grant
    Filed: September 20, 2018
    Date of Patent: July 20, 2021
    Assignee: Dow Global Technologies LLC
    Inventors: Bryan D. Stubbert, Arkady L. Krasovskiy, Tulaza Vaidya, Jerzy Klosin, Edmund M. Carnahan, Philip P. Fontaine, Mari S. Rosen, David R. Wilson