Patents Examined by Sagar Patel
  • Analogs of celastrol
    Patent number: 10662218
    Abstract: Described herein, inter alia, are compositions and methods for treating or preventing obesity and using the same.
    Type: Grant
    Filed: October 21, 2016
    Date of Patent: May 26, 2020
    Inventors: Ralph Mazitschek, Yanbing Ding, Kaisheng Shen
  • Crystalline polymorphs of 1,6-dibromo-1,6-dideoxy-dulcitol
    Patent number: 10654783
    Abstract: Described herein are polymorphic forms of 1,6-dibromo-1,6-dideoxy-dulcitol (dibromo dulcitol or DBD), which is a known antitumor agent. Also described are methods of making these new crystalline polymorphic forms as well as methods of using these polymorphic forms to treat cancer.
    Type: Grant
    Filed: June 15, 2016
    Date of Patent: May 19, 2020
    Assignee: Targent, LLC
    Inventors: Stefano Luca Giaffreda, Elena Dichiarante
  • Substituted hydroxamic acid compounds
    Patent number: 10647664
    Abstract: Disclosed are compounds of formulae: (I), and (II) and pharmaceutically acceptable salts thereof, wherein the variables, R, R1, R2, R3, R21, R22, R23, R34, R37, R33, R39, D, Q, Y, X, X1, X3, and X4 are defined herein. These compounds are useful for treating Gram-negative bacteria infections.
    Type: Grant
    Filed: August 18, 2014
    Date of Patent: May 12, 2020
    Assignees: Duke University, University of North Carolina
    Inventors: Pei Zhou, Eric J. Toone, Robert A. Nicholas
  • Phenoxymethyl derivatives
    Patent number: 10640472
    Abstract: The invention provides novel compounds having the general formula (I) wherein RA, RB, RC, RC1 and W are as defined herein, compositions including the compounds and methods of using the compounds.
    Type: Grant
    Filed: March 2, 2018
    Date of Patent: May 5, 2020
    Assignee: Hoffman-La Roche Inc.
    Inventors: Jerome Hert, Daniel Hunziker, Holger Kuehne, Thomas Luebbers, Rainer E. Martin, Patrizio Mattei, Werner Neidhart, Hans Richter, Markus Rudolph, Emmanuel Pinard
  • Manufacture of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol
    Patent number: 10626123
    Abstract: The present invention relates to a process for synthesis of 4,5,6,7-tetrahydroisoxazolo[5,4-c]pyridin-3-ol abbreviated THIP, having the INN name gaboxadol, starting from pyrrolidin-2-one. The process comprises a new direct process to obtain the intermediate dimethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-5 dicarboxylate or the intermediate diethyl 5-hydroxy-3,6-dihydropyridine-1,4(2H)-dicarboxylate.
    Type: Grant
    Filed: March 22, 2016
    Date of Patent: April 21, 2020
    Assignee: H. Lundbeck A/S
    Inventors: Carla De Faveri, Florian Anton Martin Huber
  • Method for producing kakeromycin and derivatives thereof
    Patent number: 10618876
    Abstract: Provided is a production method of kakeromycin and a derivative thereof showing an antifungal activity and cytotoxicity and expected as a new antifungal agent or anticancer agent, by chemical synthesis. A production method of a compound represented by the formula (1): wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group; and n is 0 or 1, or a salt thereof, including a step of subjecting a compound represented by the formula (2): wherein R and n are as defined above, or a salt thereof, to an oxidation reaction.
    Type: Grant
    Filed: September 21, 2018
    Date of Patent: April 14, 2020
    Assignees: OP BIO FACTORY CO., LTD., SEED RESEARCH INSTITUTE CO., LTD.
    Inventors: Teruhiko Ishikawa, Morita Iwami
  • 2,3-dihydro-isoindole-1-one derivative as BTK kinase suppressant, and pharmaceutical composition including same
    Patent number: 10604508
    Abstract: The present invention provides a compound selected from the group consisting of a compound of formula (I), pharmaceutically acceptable salts, esters, prodrugs, hydrates, solvates and isomers thereof; a use of the compound for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase, and a use of the compound for the manufacture of a medicament for the treatment, relief or prevention of the diseases; a pharmaceutical composition comprising the compound as an active ingredient; and a method for the treatment, relief or prevention of the diseases using the compound. The inventive compound is useful for the treatment, relief or prevention of diseases caused by abnormal or uncontrolled activation of protein kinase.
    Type: Grant
    Filed: August 30, 2017
    Date of Patent: March 31, 2020
    Assignee: CrystalGenomics, Inc.
    Inventors: Yong Rae Hong, Jeong Eun Na, Im Sook Min, Hyun Ju Cha, Sool Ki Kwon, Seonggu Ro, Joong Myung Cho
  • Salts and solid forms of (S)-3-(4-((4-(morpholinomethyl)benzyl) oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione and compositions comprising and methods of using the same
    Patent number: 10596180
    Abstract: Salts and solid forms of 3-(4-((4-(morpholinomethyl)benzyl)oxy)-1-oxoisoindolin-2-yl)piperidine-2,6-dione, or a stereoisomer thereof, are disclosed. Compositions comprising and methods of using the salts and solid forms are also disclosed.
    Type: Grant
    Filed: June 17, 2019
    Date of Patent: March 24, 2020
    Assignee: Celgene Corporation
    Inventors: Benjamin M. Cohen, John F. Traverse, Jean Xu, Ying Li
  • Syringolin analogues and methods of making and using same
    Patent number: 10597368
    Abstract: The present invention provides, in certain aspects, novel syringolin analogues, In certain embodiments, the compounds of the invention are proteasome inhibitors, In other embodiments, the compounds treat or prevent a cancer such as, but not limited to, leukemia in a subject.
    Type: Grant
    Filed: May 7, 2016
    Date of Patent: March 24, 2020
    Assignee: BROWN UNIVERSITY
    Inventors: Jason K. Sello, Kyle A. Totaro
  • Benzofuran derivatives for the treatment of CNS and other disorders
    Patent number: 10590100
    Abstract: The present application discloses 2-phenyl benzofuran derivative compounds and compositions, and methods for treating ocular diseases, neurological disorders and protein aggregation-related disorders in patients using the compounds and compositions as disclosed herein.
    Type: Grant
    Filed: November 10, 2016
    Date of Patent: March 17, 2020
    Assignee: AMBIENT PHOTONICS, INC.
    Inventors: John C. Warner, Srinivasa R. Cheruku, Jeffery A. Gladding
  • Substituted 6,7-dihydro-5H-benzo[7]annulene compounds, processes for their preparation and therapeutic uses thereof
    Patent number: 10570090
    Abstract: Compounds of formula (I): wherein R1 and R2 represent hydrogen or deuterium atoms; R3 represents a hydrogen atom or a —COOH, a —OH or a —OPO(OH)2 group; R4 represents a hydrogen atom or a fluorine atom; R5 represents a hydrogen atom or a —OH group; wherein at least one of R3 or R5 is different from a hydrogen atom; when R3 represents a —COOH, —OH or —OPO(OH)2 group, then R5 represents a hydrogen atom; when R5 represents a —OH group, then R3 and R4 represent hydrogen atoms; and R6 is selected from an optionally substituted phenyl, heteroaryl, cycloalkyl and heterocycloalkyl group; and the preparation and the therapeutic uses of the compounds of formula (I) as inhibitors and degraders of estrogen receptors, useful especially in the treatment of cancer.
    Type: Grant
    Filed: June 5, 2017
    Date of Patent: February 25, 2020
    Assignee: SANOFI
    Inventors: Monsif Bouaboula, Maurice Brollo, Victor Certal, Youssef El-Ahmad, Bruno Filoche-Romme, Frank Halley, Gary McCort, Laurent Schio, Michel Tabart, Corinne Terrier, Fabienne Thompson
  • Modulator of cystic fibrosis transmembrane conductance regulator, pharmaceutical compositions, methods of treatment, and process for making the modulator
    Patent number: 10570115
    Abstract: Compounds of Formula I: pharmaceutically acceptable salts thereof, deuterated derivatives of any of the foregoing, and metabolites of any of the foregoing are disclosed. Pharmaceutical compositions comprising the same, methods of treating cystic fibrosis using the same, and methods for making the same are also disclosed.
    Type: Grant
    Filed: September 29, 2017
    Date of Patent: February 25, 2020
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Timothy Alcacio, Minson Baek, Peter Grootenhuis, Sara Sabina Hadida Ruah, Robert M. Hughes, Ali Keshavarz-Shokri, Rachel McAuley-Aoki, Jason McCartney, Mark Thomas Miller, Fredrick Van Goor, Beili Zhang, Corey Anderson, Thomas Cleveland, Bryan A. Frieman, Haripada Khatuya, Pramod Virupax Joshi, Paul John Krenitsky, Vito Melillo, Fabrice Jean Denis Pierre, Andreas P. Termin, Johnny Uy, Jinglan Zhou, Alexander Russell Abela, Brett Bradley Busch, Prasuna Paraselli, David Andrew Siesel
  • Bicyclic compounds and methods of use
    Patent number: 10570147
    Abstract: The present invention provides compounds that modulate protein function, specifically phosphodiesterase 4 (PDE4). The invention provides methods of treating, ameliorating, and/or preventing diseases, disorders, and conditions associated with PDE4. Compositions, including in combination with other inflammatory mediators, are also provided.
    Type: Grant
    Filed: June 5, 2018
    Date of Patent: February 25, 2020
    Assignee: BioTheryX, Inc.
    Inventors: Robert Sullivan, Paul E. Erdman, Eduardo Torres, Leah Fung, Kyle W. H. Chan, Frank Mercurio
  • Aryl sulfonamide compounds as carbonic anhydrase inhibitors and their therapeutic use
    Patent number: 10562859
    Abstract: Disclosed herein are compounds having the following structure useful as inhibitors of carbonic anhydrase IX (CAIX) and XII, and particularly useful for reducing or eliminating metastases see Formula (I).
    Type: Grant
    Filed: July 1, 2016
    Date of Patent: February 18, 2020
    Assignee: SIGNALCHEM LIFESCIENCES CORPORATION
    Inventor: Zaihui Zhang
  • Cancer therapeutics
    Patent number: 10562890
    Abstract: This invention relates to compounds that bind to wild-type CBF? and inhibit CBF? binding to RUNX proteins. The potent compounds of the invention inhibit this protein-protein interaction at low micromolar concentrations, using allosteric mechanism to achieve inhibition, displace wild-type CBF? from RUNX1 in cells, change occupancy of RUNX1 on target genes, and alter gene expression of RUNX1 target genes. These inhibitors show clear biological effects consistent with on-target RUNX protein activity. Pharmaceutical compositions containing a compound of the invention and a pharmaceutically acceptable carrier represent a separate embodiment of the invention. Another embodiment of the invention are methods of treating a RUNX-signaling-dependent cancer that expresses wild-type CBF? in a subject in need thereof by administering to the subject a therapeutically effective amount of a compound of the invention.
    Type: Grant
    Filed: August 13, 2015
    Date of Patent: February 18, 2020
    Assignee: UNIVERSITY OF VIRGINIA PATENT FOUNDATION
    Inventors: John H. Bushweller, Anuradha Illendula
  • Bis-diazeniumdiolate compounds as anti-cancer agents
    Patent number: 10556875
    Abstract: A series of double-component, bis O2-aryl diazeniumdiolate derivatives are provided, of which each molecule can release up to four nitric oxide molecules. These compounds show cytotoxic activities to cancer cells, such as human leukemia, breast cancer and lung cancer. Among them, the compound 3 showed the highest specific activity against human leukemia cells.
    Type: Grant
    Filed: October 9, 2018
    Date of Patent: February 11, 2020
    Assignee: ARIZONA BOARD OF REGENTS ON BEHALF OF ARIZONA STATE UNIVERSITY
    Inventor: Shengxi Chen
  • Acyl sulfonamide NaV1.7 inhibitors
    Patent number: 10550080
    Abstract: The present disclosure relates to compounds of formula I which inhibit NaV1.7, and include pharmaceutically acceptable salts, compositions comprising such compounds, and methods using and making such compounds and compositions.
    Type: Grant
    Filed: April 19, 2017
    Date of Patent: February 4, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Guanglin Luo, Ling Chen
  • Spirocyclic quinolizine derivatives useful as HIV integrase inhibitors
    Patent number: 10544155
    Abstract: The present invention relates to spirocyclic quinolizine derivatives and pharmaceutically acceptable salts or prodrug thereof, compositions comprising at least one spirocyclic quinolizine derivative, and methods of using the spirocyclic quinolizine derivatives for treating or preventing HIV infection in a subject.
    Type: Grant
    Filed: December 12, 2016
    Date of Patent: January 28, 2020
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Yonglian Zhang, Sherman T. Waddell, Tao Yu, John A. McCauley, Andrew Stamford
  • Malononitrile oxime ether compound and use thereof
    Patent number: 10544092
    Abstract: Disclosed is a malononitrile oxime ether compound having a novel structure as shown in the general formula I. Respective substituents in the general formula I as defined in the specification. The compound of the general formula I exhibits an excellent microbicidal activity, and can effectively prevent and treat plant diseases caused by bacteria and fungi. Also provided is a use of the compound of the general formula I as a microbicide in the agricultural and other fields.
    Type: Grant
    Filed: December 22, 2016
    Date of Patent: January 28, 2020
    Assignee: SHENYANG SINOCHEM AGROCHEMICALS R&D CO., LTD.
    Inventors: Xueming Cheng, Lixin Zhang, Liang Chen, Qin Sun, Junli Liu, Zhinian Li, Jie Zhao, Jingbo Xu, Hongfei Wu
  • Method for preparing 3-((2S, 5S)-4-methylene-5-(3-oxopropyl)tetrahydrofurane-2-yl) propanol derivative, and intermediate therefor
    Patent number: 10538539
    Abstract: A method for preparing a 3-((2S,5S)-4-methylene-5-(3-oxopropyl)tetrahydrofuran-2-yl)propanol derivative by a simple process with high yields, and an intermediate useful for the method.
    Type: Grant
    Filed: January 13, 2017
    Date of Patent: January 21, 2020
    Assignee: YONSUNG FINE CHEMICAL CO., LTD.
    Inventors: Hyun Ik Shin, Kee Young Lee, Changyoung Oh