Patents Examined by Amanda L Aguirre
  • Imidazole derivatives as formyl peptide receptor modulators
    Patent number: 10301269
    Abstract: The present invention relates to imidazole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of the N-formyl peptide receptor.
    Type: Grant
    Filed: May 21, 2015
    Date of Patent: May 28, 2019
    Assignee: ALLERGAN, INC.
    Inventors: Richard L. Beard, Tien T. Duong, Michael E. Garst
  • Myricanol derivatives and uses thereof for treatment of neurodegenerative diseases
    Patent number: 10287227
    Abstract: The subject invention pertains to myricanol derivatives, therapeutic compositions, and methods for treatment of neurodegenerative diseases, in particular, neurodegenerative diseases associated with abnormal accumulation of protein tau.
    Type: Grant
    Filed: January 24, 2017
    Date of Patent: May 14, 2019
    Assignees: UNIVERSITY OF SOUTH FLORIDA, The Department of Veterans Affairs
    Inventors: Chad Dickey, Umesh Jinwal, Laurent Calcul, Bill J. Baker, Matthew Lebar
  • Salts of a dihydroquinazoline derivative
    Patent number: 10287254
    Abstract: The invention relates to besylate and tosylate salts of {8-fluoro-2-[4-(3-methoxyphenyl)piperazin-1-yl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-3,4-dihydroquinazolin-4-yl} acetic acid and solvates thereof, to the use thereof in a method of treating and/or preventing virus infections, and to the use thereof to produce drugs for use in treating and/or preventing diseases, in particular use as antiviral agents, in particular against cytomegaloviruses (FIG. 1).
    Type: Grant
    Filed: October 31, 2016
    Date of Patent: May 14, 2019
    Assignee: AiCuris GmbH & Co. KG
    Inventors: Welljanne Maertens, Christian Schickaneder
  • Substituted dihydropyrrolopyrazole derivative
    Patent number: 10273252
    Abstract: The present invention provides a compound represented by the general formula (Ia) or a pharmacologically acceptable salt thereof. In the general formula (Ia), two R moieties each independently represent a C1-3 alkyl group or the like; and R1, R2 and R3 each independently represent an optionally substituted linear or branched C1-4 alkyl group.
    Type: Grant
    Filed: June 14, 2016
    Date of Patent: April 30, 2019
    Assignee: UBE INDUSTRIES, LTD.
    Inventors: Noriaki Iwase, Yasuhiro Aga, Shigeru Ushiyama, Shigeyuki Kono, Hidetoshi Sunamoto, Takashi Matsushita, Sayaka Ogi, Satoshi Umezaki, Masahiro Kojima, Kazuhiro Onuma, Yusuke Shiraishi, Makoto Okudo, Tomio Kimura
  • Screening methods for the binding affinity of chemical entities to biological molecules and NEDD4-1 inhibitors identified by the screening methods
    Patent number: 10273208
    Abstract: Disclosed are methods for preparing and screening for an inhibitor of the activity of a biological molecule having a catalytic or non-catalytic cysteine residue. The methods including preparing a library of candidate inhibitor molecules by conjugating an electrophile to a plurality of drug molecules where the library of candidate inhibitor molecules thus formed react with cysteine residues. The library of candidate inhibitor molecules then may be reacted with the biological molecule to identify those inhibitor molecule that react with the catalytic or non-catalytic cysteine residue of the biological molecule in order to identify an inhibitor of the biological molecule.
    Type: Grant
    Filed: February 9, 2017
    Date of Patent: April 30, 2019
    Assignee: Northwestern University
    Inventors: Alexander V. Statsyuk, Stefan G. Kathman
  • Substituted heteroaryl compounds and methods of use
    Patent number: 10266521
    Abstract: The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof. They are useful in preventing, managing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.
    Type: Grant
    Filed: January 4, 2018
    Date of Patent: April 23, 2019
    Assignees: CALITOR SCIENCES, LLC, SUNSHINE LAKE PHARMA CO., LTD.
    Inventors: Ning Xi, Minxiong Li, Xiaobo Li, Wuhong Chen, Tao Zhang, Haiyang Hu, Weilong Dai, Yanjun Wu
  • Thieno[2,3-e]indole derivatives as new antitumor agents
    Patent number: 10266547
    Abstract: The present invention relates to a novel class of alkylating agents comprising a thieno[2,3-e]indole moiety tethered to a DNA-binding moiety, which have cytotoxic activity and are useful in treating diseases such as cancer, cellular proliferation disorders and viral infections. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising them and methods of treating diseases utilizing such compounds or the pharmaceutical composition containing them. The invention also relates to the use of this novel class of alkylating agents in the preparation of conjugates.
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: April 23, 2019
    Assignee: NERVIANO MEDICAL SCIENCES S.R.L.
    Inventors: Marina Caldarelli, Michele Caruso, Paolo Orsini
  • N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides
    Patent number: 10265411
    Abstract: The invention relates to (among other things) N-optionally substituted aryl-2-oligomer-3-alkoxypropionamides and compositions comprising the same. A compound of the invention, when administered by any of a number of administration routes, exhibits one or more advantages over corresponding compounds lacking the oligomer.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: April 23, 2019
    Assignee: Nektar Therapeutics
    Inventors: Jennifer Riggs-Sauthier, Wen Zhang
  • Organocatalytic asymmetric synthesis of antidepressants
    Patent number: 10266481
    Abstract: The present invention relates to a short enantioselective synthesis of 1-amino aryl tetraline compounds of Formula 1 via nucleophilic enamine catalysis using organocatalyst such as proline. wherein R1 and R2 represent independent of each other hydrogen, (un)substituted or substituted amine; R3 and R4 represent independent of each other hydrogen or halogen.
    Type: Grant
    Filed: June 22, 2015
    Date of Patent: April 23, 2019
    Assignee: Council of Scientific & Industrial Research
    Inventors: Venkataramasubramanian Vaithiyanathan, Rupali Gundappa Kalshetti, Sudalai Arumugam
  • Indazolyl- and indolyl-benzamide derivatives
    Patent number: 10246421
    Abstract: The invention relates to indazolylbenzamide, indolylbenzamide, benzo[d]imidazolyl-benzamide, and benzo[d]triazolylbenzamide derivatives of formula useful in the treatment and/or prevention of diseases and/or conditions related to cell proliferation, such as cancer, infection, inflammation and inflammation-associated disorders, and conditions associated with angiogenesis.
    Type: Grant
    Filed: September 11, 2015
    Date of Patent: April 2, 2019
    Assignee: Esanex, Inc.
    Inventor: Philip F. Hughes
  • Cyclopropylamine compounds as histone demethylase inhibitors
    Patent number: 10233165
    Abstract: The present disclosure relates to cyclopropyl compounds of general formula (I), wherein R1, and R2 are as defined in the specification. The present application also relates to pharmaceutical compositions containing such compounds and to their use in therapy.
    Type: Grant
    Filed: May 29, 2015
    Date of Patent: March 19, 2019
    Assignee: Istituto Europeo di Oncologia S.r.l.
    Inventors: Paola Vianello, Mario Varasi, Ciro Mercurio, Anna Cappa, Giuseppe Meroni, Manuela Villa, Antonello Mai, Sergio Valente
  • Hydroxyalkylamine- and hydroxycycloalkylamine-substituted diamine-arylsulfonamide compounds with selective activity in voltage-gated sodium channels
    Patent number: 10221167
    Abstract: Disclosed are compounds of Formula A, or a salt thereof: wherein R1, R2, and E are defined herein, which compounds have properties for inhibiting Nav 1.7 ion channels found in peripheral and sympathetic neurons. Also described are pharmaceutical formulations comprising the compounds of Formula A or their salts, and methods of treating pain disorders, cough, and itch using the same.
    Type: Grant
    Filed: December 14, 2016
    Date of Patent: March 5, 2019
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Thomas J. Greshock, James Mulhearn, Junying Zheng, Ronald M. Kim, Ting Zhang, Anthony J. Roecker, Walter Won, Philippe Nantermet, Rajan Anand, Gang Zhou, Deping Wang, Liangqin Guo
  • Compounds as opioid receptor modulators
    Patent number: 10213415
    Abstract: The present invention is directed to novel opioid receptor modulators of Formula (I). The invention further relates to methods for preparing such compounds, pharmaceutical compositions containing them, and their use in the treatment of disorders that may be ameliorated or treated by the modulation of opioid receptors.
    Type: Grant
    Filed: June 7, 2017
    Date of Patent: February 26, 2019
    Assignee: Janssen Pharmaceutica NV
    Inventors: Henry J. Breslin, Chaozhong Cai, Wei He, Robert W. Kavash
  • Bicyclic heteroaryl amine compounds
    Patent number: 10214537
    Abstract: Disclosed are compounds of Formula (I) or a salt thereof; wherein: X is N or CH; Q1 is: (i) Cl, Br, I, —CN, —CH3, or —CF3; (ii) a 5-membered heteroaryl selected from pyrrolyl, pyrazolyl, imidazolyl, oxazolyl, thiazolyl, triazolyl, oxadiazolyl, and thiadiazolyl; (iii) a 6?membered heteroaryl selected from pyridinyl, pyridazinyl, and pyrimidinyl; or (iv) a bicyclic heteroaryl selected from indolyl, pyrrolopyridinyl, pyrazolopyridinyl and benzo[d]oxazolyl; wherein each of said 5-membered, 6-membered, and bicyclic heteroaryl is substituted with zero to 1 Ra and zero to 1 Rb; and R1, R2, R3, R4, R5, R6, Ra, and Rb are defined herein. Also disclosed are methods of using such compounds as modulators of PI3K, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing inflammatory and autoimmune diseases.
    Type: Grant
    Filed: October 21, 2015
    Date of Patent: February 26, 2019
    Assignee: Bristol-Myers Squibb Company
    Inventors: Rajeev S. Bhide, Douglas G. Batt, Robert J. Cherney, Lyndon A. M. Cornelius, Qingjie Liu, David Marcoux, James Neels, Michael A. Poss, Zheming Ruan, Qing Shi, Anurag S. Srivastava, Lan-ying Qin, Joseph A. Tino, Scott Hunter Watterson
  • PKM2 modulators and methods for their use
    Patent number: 10207996
    Abstract: Compounds having activity as PKM2 activators are disclosed. The compounds have the following structure (I): including stereoisomers, tautomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, R5 and R6 are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: February 19, 2019
    Assignee: Tolero Pharmaceuticals, Inc.
    Inventors: Koc-Kan Ho, Yong Xu, Michael David Saunders, Xiaohui Liu, Scott Albert Pearce, Kevin Bret Wright, Jason Marc Foulks, Kenneth Mark Parnell, Steven Brian Kanner, David Lee Vollmer, Jihua Liu
  • Substituted alkyl diaryl derivatives, methods of preparation and uses
    Patent number: 10207989
    Abstract: Compounds according to Formula I are provided: and salts thereof, wherein Q1, Q2, R3, R4, X, and Y are as defined herein. Methods for preparing compounds of Formula I are also provided, as well as methods of treating cellular proliferative disorders, such as cancer, using compounds of Formula (I).
    Type: Grant
    Filed: September 18, 2013
    Date of Patent: February 19, 2019
    Assignee: TEMPLE UNIVERSITY—Of The Commonwealth System of Higher Education
    Inventors: M. V. Ramana Reddy, E. Premkumar Reddy
  • Hydantoins that modulate bace-mediated app processing
    Patent number: 10202355
    Abstract: In certain embodiments hydantoin compounds are provided herein that are effective to inhibit BACE activity against APP. Without being bound to a particular theory, it is believed the activity of the hydantoins identified herein appears to be associated with binding to BACE and/or to APP particularly when these moieties form a BACE/APP complex. Accordingly, it is believed the compounds described herein represent a new class of compounds designated herein as APP-Binding-BACE Inhibitors (ABBIs) and provide a new mechanism to modulate APP processing. The hydantoins described herein appear to show improved brain permeability and functional BACE inhibition.
    Type: Grant
    Filed: February 12, 2014
    Date of Patent: February 12, 2019
    Assignee: BUCK INSTITUTE FOR RESEARCH ON AGING
    Inventors: Varghese John, Dale E. Bredesen
  • Spiro-lactam NMDA receptor modulators and uses thereof
    Patent number: 10195179
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: December 4, 2017
    Date of Patent: February 5, 2019
    Assignee: Aptinyx Inc.
    Inventor: M. Amin Khan
  • Spiro-lactam NMDA receptor modulators and uses thereof
    Patent number: 10196401
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: December 4, 2017
    Date of Patent: February 5, 2019
    Assignee: Aptinyx Inc.
    Inventor: M. Amin Khan
  • Aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amides as somatostatin receptor subtype 4 (SSTR4) agonists
    Patent number: 10183940
    Abstract: The invention relates to aryl and heteroaryl-fused tetrahydro-1,4-oxazepine amide derivatives of general formula (1), which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4. In addition, the invention relates processes for manufacture of the compounds according to the invention.
    Type: Grant
    Filed: November 12, 2015
    Date of Patent: January 22, 2019
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Rocco Mazzaferro, Marco Ferrara, Riccardo Giovannini, Iain Lingard