Patents Examined by Patricia L. Morris
  • N3,N6-bis(2-(5-methoxy-1H-indole-3-yl)ethyl)-2,6-dimethyl-4-(2-nitrophenyl)pyridine-3,5-dicarboxamide and use thereof in the field of neurotoxicity
    Patent number: 10758521
    Abstract: The invention relates to a molecule enabling removal of neurotoxicity observed in neuron cells due to various reasons.
    Type: Grant
    Filed: June 10, 2019
    Date of Patent: September 1, 2020
    Inventors: Ahmet Hacimuftuoglu, Orhan Ates, Nurullah Saracoglu, Ali Taghizadehghalehjoughi, Farrokh Lafzi
  • Synthesis and resolution of nicotine
    Patent number: 10759776
    Abstract: The present disclosure generally relates to methods of preparing nicotine and resolving R,S nicotine to enrich the (S)(?) enantiomer. The method may comprise combining N-methyl-2-pyrrolidone or a salt thereof with a nicotinate compound in the presence of a solvent and a strong base to form 1-methyl-3-nicotinoyl-2-pyrrolidone or a salt thereof; and reducing the 1-methyl-3-nicotinoyl-2-pyrrolidone or salt thereof in solution with Na2S2O4 to produce racemic nicotine or salt thereof. Resolving the racemic nicotine (or other enantiomeric mixture) may comprise combining the nicotine with (?)-O,O?-di-p-toluoyl-L-tartaric acid (L-PTTA).
    Type: Grant
    Filed: May 15, 2019
    Date of Patent: September 1, 2020
    Assignee: NJOY, LLC
    Inventors: Bert Willis, Mohammed Moinuddin Ahmed, Wesley Freund, Douglas Sawyer
  • Monofunctional intermediates for ligand-dependent target protein degradation
    Patent number: 10759808
    Abstract: The present disclosure provides compounds represented by Formula I: and the salts or solvates thereof, wherein X, L, Y, and B are as defined in the specification. Compounds having Formula I are immunomodulators and/or monofunctional synthetic intermediates that can be used to prepare small-molecule drug conjugates.
    Type: Grant
    Filed: April 6, 2017
    Date of Patent: September 1, 2020
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Shaomeng Wang, Yangbing Li, Angelo Aguilar, Bing Zhou, Jiantao Hu, Fuming Xu, Chong Qin, Yang Hu, Weiguo Xiang, Rohan Rej, Jiuling Yang, Xin Han, Longchuan Bai, Chao-Yie Yang
  • N-phosphonoxymethyl prodrugs of hydroxyalkyl thiadiazole derivatives
    Patent number: 10752647
    Abstract: There is a need for a new antibiotic having a novel mechanism of action, which exhibits strong antibacterial activity not only against sensitive bacteria, but also against resistant bacteria thereof, and at the same time possess excellent solubility and safety profile amenable to human use. As a result of intensive research, the present inventors have found that N-phosphonoxymethyl prodrugs of hydroxyalkyl thiadiazole derivatives represented by general formula (I), a regioisomer, a stereoisomer, or a pharmaceutically acceptable salt thereof possess excellent solubility and safety profile for use in human for the treatment of bacterial infectious diseases.
    Type: Grant
    Filed: March 13, 2018
    Date of Patent: August 25, 2020
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Manoj Kumar Khera, Naresh Chintaman Dumbre, Pasha Khan
  • 1-Substituted 1,2,3,4-tetrahydro-1,7-naphthyridin-8-amine derivatives and their use as EP4 receptor antagonists
    Patent number: 10745397
    Abstract: The present invention provides a compound represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof has an EP4 receptor antagonistic action, and is useful as an agent for the prophylaxis or treatment of EP4 receptor associated diseases (e.g., rheumatoid arthritis, aortic aneurysm (e.g. abdominal aortic aneurysm, thoracic aortic aneurysm, thoracoabdominal aortic aneurysm etc.), endometriosis, ankylosing spondylitis, inflammatory breast cancer etc.) and the like.
    Type: Grant
    Filed: July 26, 2016
    Date of Patent: August 18, 2020
    Assignee: TAKEDA PHARMACEUTICAL COMPANY LIMITED
    Inventors: Dinesh Barawkar, Anil M Deshpande, Santosh Patil, Yogesh Waman, Anil Panmand, Dilip Jadhav, Bheemashankar Kulkarni
  • Isoquinoline derivatives and use thereof
    Patent number: 10738026
    Abstract: The Invention provides compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof: wherein W1, W2, W3, J1, J2, A, R1, R2, R3, R4, R5, a, and b are defined as set forth in the specification. The Invention also provides uses of the compounds of any one of Formulae (I)-(VIII) and the pharmaceutically acceptable salts, solvates, hydrates, N-oxides, or diastereomers thereof. Compounds of the Invention are useful for treating a disorder responsive to blockade of one or more sodium channels. In certain embodiments, Compounds of the Invention are useful for treating pain.
    Type: Grant
    Filed: February 12, 2015
    Date of Patent: August 11, 2020
    Assignee: Purdue Pharma L.P.
    Inventors: Laykea Tafesse, Jae Hyun Park
  • Process for preparing [(3-hydroxypyridine-2-carbonyl)amino] alkanoic acids, esters and amides
    Patent number: 10738010
    Abstract: Disclosed are processes for preparing [(3-hydroxypyridine-2-carbonyl)amino]-alkanoic acids, derivatives, inter alia, 5-aryl substituted and 5-heteroaryl substituted [(3-hydroxypyridine-2-carbonyl]amino}acetic acids. Further disclosed are methods for making prodrugs of [(3-hydroxypyridine-2-carbonyl)-amino]acetic acids, for example, [(3-hydroxypyridine-2-carbonyl]amino}acetic acid esters and {[3-hydroxypyridine-2-carbonyl]amino}acetic acid amides. The disclosed compounds are useful as prolyl hydroxylase inhibitors or for treating conditions wherein prolyl hydroxylase inhibition is desired.
    Type: Grant
    Filed: March 13, 2019
    Date of Patent: August 11, 2020
    Assignee: Akebia Therapeutics, Inc.
    Inventors: Christopher M. Lanthier, Boris Gorin, Jan Oudenes, Craig Edward Dixon, Alan Quigbo Lu, James Densmore Copp, John Michael Janusz
  • Methods for the synthesis of deuterated dextromethorphan
    Patent number: 10730841
    Abstract: The application describes methods for making a deuterated dextromethorphan of Formula (I), deuterated dextromethorphan produced by these methods, and pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: July 3, 2017
    Date of Patent: August 4, 2020
    Assignee: Avanir Pharmaceuticals, Inc.
    Inventors: Matt Johnson, Cunxiang Zhao, Weihua Meng, Zhijun Lu, Yan Li
  • Crystalline polymorphs of the free base of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde
    Patent number: 10722502
    Abstract: Disclosed are crystalline free base an solvate forms of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1), such as the free base Form I, Form II and Material N. Also disclosed are crystalline free base solvates of 2-hydroxy-6-((2-(1-isopropyl-1H-pyrazol-5-yl)pyridin-3-yl)methoxy)benzaldehyde (or Compound 1).
    Type: Grant
    Filed: October 18, 2018
    Date of Patent: July 28, 2020
    Assignee: Global Blood Therapeutics, Inc.
    Inventors: Zhe Li, Stephan D. Parent, Travis Houston
  • Aminopyridine derivatives as TAM family kinase inhibitors
    Patent number: 10723725
    Abstract: Provided herein are aminopyridine derivatives and pharmaceutical compositions that are useful as TAM family kinase inhibitors.
    Type: Grant
    Filed: January 22, 2019
    Date of Patent: July 28, 2020
    Assignee: SignalChem Lifesciences Corporation
    Inventor: Zaihui Zhang
  • Compounds useful for treating cancer
    Patent number: 10717724
    Abstract: The present invention relates to a compound of formula (I): wherein A and A? independently represent a phenylene group or a pyridylene group; R2 is a hydrogen atom or a (C1-C4)alkyl group; R3 is a 2-pyridyl group, 3-pyridyl group, a 4-pyridyl group, a 2-pyrimidinyl group, a 4-pyrimidinyl group or a 5-pyrimidinyl group; R4 is a carbonyl group or a sulfonyl group; and R5 is a —NH—(CH2)a—NR6R7 group or a 4-methylpiperazinyl group, with a being an integer from 1 to 4, R6 and R7 representing independently a (C1-C4)alkyl group, or R6 and R7 together with the nitrogen atom to which they are linked forming a heterocycle group which is chosen among a 4-methylpiperazinyl group, a morpholino group, a pyrrolidinyl group and a piperidino group; or any one of its pharmaceutically acceptable salt.
    Type: Grant
    Filed: April 5, 2018
    Date of Patent: July 21, 2020
    Assignees: ABIVAX, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, INSTITUT CURIE, UNIVERSITE DE MONTPELLIER
    Inventors: Pierre Roux, Florence Mahuteau, Romain Najman, Gilles Gadea, Jamal Tazi, Didier Scherrer, Carsten Brock, Nathalie Cahuzac
  • Piperidinone formyl peptide 2 receptor and formyl peptide 1 receptor agonists
    Patent number: 10717708
    Abstract: The disclosure relates to compounds of formula I, which are formyl peptide 2 (FPR2) receptor agonists and/or formyl peptide 1 (FPR1) receptor agonists. The disclosure also provides compositions and methods of using the compounds, for example, for the treatment of atherosclerosis, heart failure, chronic obstructive pulmonary disease (COPD), and related diseases.
    Type: Grant
    Filed: December 8, 2016
    Date of Patent: July 21, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Nicholas R. Wurtz, Pravin Sudhakar Shirude
  • Modified compound of andrographolide
    Patent number: 10717720
    Abstract: The present disclosure discloses a modified compound of andrographolide, and particularly discloses a compound shown in formula (I) and (II) or a pharmaceutically acceptable salt thereof.
    Type: Grant
    Filed: November 22, 2016
    Date of Patent: July 21, 2020
    Assignees: Heilongjiang Zhenbaodao Pharmaceutical Co., Ltd., Medshine Discovery Inc.
    Inventors: Haiying He, Zhigan Jiang, Jianhua Xia, Jing Wang, Lixia Han, Lihong Lan, Hui Zhou, Kunmin Lai, Shuhui Chen
  • Aminopyridine derivatives and their use as selective ALK-2 inhibitors
    Patent number: 10710980
    Abstract: The invention relates to a compound of formula (I) in free form or in pharmaceutically acceptable salt form (I) to pharmaceutical compositions comprising said compound and to the use of said compound in the treatment of heterotopic ossification and fibrodysplasia ossificans progressiva.
    Type: Grant
    Filed: July 18, 2017
    Date of Patent: July 14, 2020
    Assignee: Novartis AG
    Inventors: Luca Arista, Sreehari Babu, Jianwei Bian, Kai Cui, Michael Patrick Dillon, Rene Lattmann, Jialiang Li, Lv Liao, Dimitrios Lizos, Rita Ramos, Nikolaus Johannes Stiefl, Thomas Ullrich, Peggy Usselmann, Xiaoyang Wang, Liladhar Murlidhar Waykole, Sven Weiler, Yubo Zhang, Yizong Zhou, Tingying Zhu
  • Substituted pyridinones as bromodomain inhibitors
    Patent number: 10710992
    Abstract: The present disclosure relates to substituted pyridinones, which are useful for inhibition of BET protein function by binding to bromodomains, and their use in therapy.
    Type: Grant
    Filed: December 1, 2015
    Date of Patent: July 14, 2020
    Assignee: Zenith Epigenetics Ltd.
    Inventors: May Xiaowu Jiang, Bruce Francis Molino, Shuang Liu, Ruifang Wang, Bryan Cordell Duffy, John Frederick Quinn, Gregory Steven Wagner
  • (S)-N-(3-6-isopropoxypyridin-3-3YL)-1H-indazol-5-yl)-1-(2-(4-4(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H-yl)-2-oxoethyl)-3(methylthio)pyrrolidine-3-carboxamide compositions for pharmaceutical preparations
    Patent number: 10710982
    Abstract: A composition comprising (S)—N-(3-(6-isopropoxypyridin-3-yl)-1H-indazol-5-yl)-1-(2-(4-(4-(1-methyl-1H-1,2,4-triazol-3-yl)phenyl)-3,6-dihydropyridin-1(2H)-yl)-2-oxoethyl)-3-(methylthio)pyrrolidine-3-carboxamide and hypromellose acetate succinate for pharmaceutical preparations, especially capsule preparations.
    Type: Grant
    Filed: February 12, 2020
    Date of Patent: July 14, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Pranav Gupta, Jiansheng Wan
  • Substituted benzimidazoles, their preparation and their use as pharmaceuticals
    Patent number: 10703740
    Abstract: This application relates to substituted benzimidazoles, compositions comprising them and their uses in the treatment of diseases and conditions in which inhibition of a bromodomain is indicated. For example, the application relates to substituted benzimidazoles and to their use as bromodomain inhibitors. The present application is also related to the treatment or prevention of proliferative disorders, auto-immune disorders, inflammatory disorders, dermal disorders, and neoplasms, including tumors and/or cancers.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: July 7, 2020
    Assignee: Neomed Institute
    Inventors: Mehrnaz Pourashraf, Guillaume Jacquemot, Stephen Claridge, Malken Bayrakdarian, Shawn Johnstone, Jeffrey S. Albert, Andrew Griffin
  • Integrin antagonists
    Patent number: 10703752
    Abstract: The present invention relates to novel integrin antagonists of Formula I and their use as a medicament, in particular for inhibiting neovascularization.
    Type: Grant
    Filed: August 19, 2019
    Date of Patent: July 7, 2020
    Assignee: OXURION NV
    Inventors: Ove Pedersen, Elke Vermassen
  • Imidazo-oxadiazole and imidazo-thiadiazole derivatives
    Patent number: 10696690
    Abstract: The present invention provides compounds of Formula (I) used as Amyloid beta lowering agent for the treatment of neurodegenerative diseases.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: June 30, 2020
    Assignee: Ares Trading S.A.
    Inventors: Anna Quattropani, Dominique Swinnen
  • Heterocyclic compounds as pesticides
    Patent number: 10689348
    Abstract: The present application relates to the use of heterocyclic compounds for controlling animal pests including arthropods, insects and nematodes, to novel heterocyclic compounds, to processes for their preparation and to intermediates for preparing the heterocyclic compounds.
    Type: Grant
    Filed: August 9, 2019
    Date of Patent: June 23, 2020
    Assignee: Bayer Cropscience AG
    Inventors: Eike Kevin Heilmann, Joerg Greul, Axel Trautwein, Hans-Georg Schwarz, Isabelle Adelt, Roland Andree, Peter Luemmen, Maike Hink, Martin Adamczewski, Mark Drewes, Angela Becker, Arnd Voerste, Ulrich Goergens, Kerstin Ilg, Johannes-Rudolf Jansen, Daniela Portz