Patents Examined by Emily A Bernhardt
  • Fused pentacyclic imidazole derivatives as modulators of TNF activity
    Patent number: 10980814
    Abstract: Disclosed herein are compounds of formula (I) and pharmaceutically acceptable salt thereof, wherein variables X, R1, R2, and R3 are defined herein. These compounds are potent modulators of human TNF? activity and, accordingly, of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
    Type: Grant
    Filed: April 24, 2018
    Date of Patent: April 20, 2021
    Assignees: UCB Biopharma SRL, Sanofi
    Inventors: Daniel Christopher Brookings, Teresa De Haro Garcia, Yann Foricher, Helen Tracey Horsley, Martin Clive Hutchings, James Andrew Johnson, Malcolm Maccoss, Mengyang Xuan, Zhaoning Zhu
  • Inhibitor of indoleamine-2,3-dioxygenase (IDO)
    Patent number: 10980807
    Abstract: The present disclosure provides compounds of Formula (I). The compounds described herein may be useful in treating a disease associated with IDO, for example, cancer or an infectious disease (e.g., viral or bacterial infectious diseases). Also, provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein.
    Type: Grant
    Filed: February 8, 2017
    Date of Patent: April 20, 2021
    Assignee: InventisBio LLC
    Inventors: Xing Dai, Yaolin Wang
  • Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
    Patent number: 10975069
    Abstract: Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, , wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R2 is H or methyl. At least one described molecular species exhibits an IC50 value below 5 ?M against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.
    Type: Grant
    Filed: May 30, 2019
    Date of Patent: April 13, 2021
    Assignee: WASHINGTON UNIVERSITY
    Inventors: William Hawkins, Robert Mach, Dirk Spitzer, Suwanna Vangveravong, Brian Van Tine
  • Catalyst, method for forming amide bond, and method for producing amide compound
    Patent number: 10974232
    Abstract: A catalyst represented by General Formula (1) below: where in the General Formula (1), R1 to R14 each independently represent a hydrogen atom or a substituent.
    Type: Grant
    Filed: August 14, 2018
    Date of Patent: April 13, 2021
    Assignee: Microbial Chemistry Research Foundation
    Inventors: Naoya Kumagai, Christopher Roderick Opie, Hidetoshi Noda, Masakatsu Shibasaki
  • Phenylsulfonamido-benzofuran derivatives and uses thereof in the treatment of proliferative diseases
    Patent number: 10975051
    Abstract: Described herein are phenylsulfonamido-benzofuran derivatives, and pharmaceutically acceptable salts thereof. Also provided are pharmaceutical compositions, methods, uses, and kits involving compounds of Formulae (I), (II), (III), (IV), (V), or (VI) for treating and/or preventing proliferative diseases (e.g. cancers, inflammatory diseases, and autoimmune diseases) in a subject. The compounds and pharmaceutical compositions as described herein inhibit at least one protein of the BCL-2 family in a biological sample or subject to treat and/or prevent a proliferative disease. In certain embodiments, compounds described herein are selective inhibitors of MCL-1, a BCL-2 family member protein.
    Type: Grant
    Filed: August 12, 2016
    Date of Patent: April 13, 2021
    Assignee: Memorial Sloan Kettering Cancer Center
    Inventors: Emily H. Cheng, Paul Jeng, Ouathek Ouerfelli, James Hsieh, Guangli Yang
  • Small molecule lipid II inhibitors
    Patent number: 10961214
    Abstract: Newly synthesized derivatives of BAS00127538 have been discovered to possess antibiotic activity and to combat resistant bacterial strains. Compounds and pharmaceutical compositions containing these compounds are described, and are based on a generic scaffold structure. Synthetic methods and methods of using the compounds also are described. Preferred compound 6jc48-1 ((E)-2,4-bis(4-bromophenyl)-6-(4-(dimethyl-amino)styryl)pyrylium boron tetrafluoride salt) binds to Lipid II with high affinity, has markedly reduced cytotoxicity than BAS00127538, and retains activity against drug-resistant strains of Enterococci. It is stable in plasma, has dramatically improved pharmacokinetic and pharmacodynamics properties, and possesses in vivo efficacy in a mouse model of sepsis.
    Type: Grant
    Filed: December 20, 2016
    Date of Patent: March 30, 2021
    Assignee: UNIVERSITY OF MARYLAND, BALTIMORE
    Inventors: Erik de Leeuw, Alexander MacKerell, Steven Fletcher, Jamal Chauhan
  • Crystalline forms of an NK-1 antagonist
    Patent number: 10961195
    Abstract: The present invention is related to crystalline forms of 2-(3,5-bis(trifluoromethyl)phenyl)-N,2-dimethyl-N-(6-(4-methylpiperazin-1-yl)-4-(o-tolyl)pyridin-3-yl)propanamide which is an NK-1 antagonist useful in the treatment of induced vomiting and other disorders.
    Type: Grant
    Filed: April 30, 2020
    Date of Patent: March 30, 2021
    Assignee: Helsinn Healthcare SA
    Inventors: Christian Bacilieri, Gionata Frasca
  • Inhibitors of human immunodeficiency virus replication
    Patent number: 10954252
    Abstract: Compounds of Formula I, including pharmaceutically acceptable salts thereof, and compositions and methods for treating human immunodeficiency virus (HIV) infection are set forth.
    Type: Grant
    Filed: May 1, 2018
    Date of Patent: March 23, 2021
    Assignee: ViiV HEALTHCARE UK (NO.5) LIMITED
    Inventors: Suresh Babu, Makonen Belema, John A. Bender, Christiana Iwuagwu, John F. Kadow, Selvakumar Kumaravel, Pulicharla Nagalakshmi, B. Narasimhulu Naidu, Manoj Patel, Kevin M. Peese, Ramkumar Rajamani, Mark Saulnier, Alan Xiangdong Wang
  • Benfotiamine derivatives, method for preparing the same and pharmaceutical composition comprising the same
    Patent number: 10947258
    Abstract: The present disclosure relates to benfotiamine derivatives, a method for preparing the same and a pharmaceutical composition, as indicated below, comprising the same. In the present disclosure, when the ortho position of benzene ring is only a halogen atom or an ethoxy substitution, or the meta position is only a bromine 5 atom, a chlorine atom, a fluorine atom or a nitro substitution, or the para position is only a chlorine atom, a methoxy substitution or a nitro substitution, its compound has a significant inhibition effect on A?40 and A?42. Furthermore, when the ortho position of benzene ring is only a fluorine atom or a bromine atom substitution, the compound has an outstanding inhibition effect on A?40 and A?42.
    Type: Grant
    Filed: August 23, 2019
    Date of Patent: March 16, 2021
    Assignee: SHANGHAI RIXIN BIOTECHNOLOGY CO., LTD.
    Inventors: Chunjiu Zhong, Huan Zhang
  • Phenyl phthalazine derivative, method for the preparation thereof, and pharmaceutical composition comprising the same
    Patent number: 10947241
    Abstract: The present invention relates to a compound represented by Chemical Formula 1, or a pharmaceutically acceptable salt thereof. The compound according to the present invention can be usefully used for the prevention or treatment of cardiovascular diseases.
    Type: Grant
    Filed: October 27, 2017
    Date of Patent: March 16, 2021
    Assignee: Seoul National University Hospital
    Inventors: Ja Kyung Yoo, Nora Lee, Chun Ho Lee, Myunggi Jung, Hyo-Soo Kim
  • Small molecule lipid II inhibitors
    Patent number: 10941114
    Abstract: Newly synthesized derivatives of BAS00127538 have been discovered to possess antibiotic activity and to combat resistant bacterial strains. Compounds and pharmaceutical compositions containing these compounds are described, and are based on a genetic scaffold structure. Synthetic methods and methods of using the compounds also are described. Preferred compounds bind to Lipid II with high affinity, have markedly reduced cytotoxicity compared to BAS00127538, and retain activity against drug-resistant strains of Enterococci. They are stable in plasma, have dramatically improved pharmacokinetic and pharmacodynamics properties, and possess in vivo efficacy in a mouse model of sepsis.
    Type: Grant
    Filed: December 23, 2019
    Date of Patent: March 9, 2021
    Assignee: University Of Maryland, Baltimore
    Inventors: Erik de Leeuw, Alexander MacKerell, Steven Fletcher, Jamal Chauhan
  • Intermediates in the synthesis of cephalosporin compounds
    Patent number: 10941161
    Abstract: Described herein are crystalline forms of a compound of formula (III?), including toluene solvates of TATD-CLE, as well as processes for the preparation thereof and use thereof in the preparation of cephalosporin compounds such as ceftolozane.
    Type: Grant
    Filed: March 4, 2019
    Date of Patent: March 9, 2021
    Assignee: Merck Sharp & Dohme Corp.
    Inventors: Kristos Adrian Moshos, Valdas Jurkauskas, Giovanni Fogliato, Manuel Scanu, You Seok Hwang
  • Bruton's tyrosine kinase inhibitors
    Patent number: 10933063
    Abstract: Bruton's tyrosine kinase (Btk) inhibitors have the following Formula (I):
    Type: Grant
    Filed: May 22, 2019
    Date of Patent: March 2, 2021
    Assignees: Suzhou Baijibugong Pharmaceutical Technology Co., Ltd.
    Inventors: Xibin Liao, Jia Li, Zhijian Lu, Yubo Zhou, Anhui Gao
  • Intermediate compound of novel tetrahydronaphthyl urea derivative
    Patent number: 10927079
    Abstract: An intermediate compound, a pharmaceutically acceptable salt thereof, or a solvate thereof is disclosed wherein the intermediate compound is represented by formula (AM-2-RR)?(D-TA): in which p represents an integer of 0 to 4; R1 each independently represent a halogen atom, a cyano group, a C1-6 alkyl group, a halogenated C1-6 alkyl group, a hydroxy C1-6 alkyl group, a cyanated C1-6 alkyl group, a halogenated C1-6 alkoxy group, a C1-6 alkoxy C1-6 alkyl group, a mono-/di-C2-7 alkanoyl amino group, a carboxamide group, or a C1-6 alkoxy carbonyl group; and R2a and R2b each independently represent a C1-6 alkyl group.
    Type: Grant
    Filed: April 15, 2020
    Date of Patent: February 23, 2021
    Assignee: MOCHIDA PHARMACEUTICAL CO., LTD.
    Inventor: Yuji Kawada
  • Process for the preparation of 4-phenyl-5-alkoxycarbonyl-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-carboxylic acid
    Patent number: 10927116
    Abstract: The present invention relates to a process for synthesizing a compound of formula (I), R1 is phenyl, which is unsubstituted or substituted with one, two or three substituents independently selected from halogen and C1-6alkyl; R2 is C1-6alkyl; R3 is —CxH2x—; x is 1, 2, 3, 4, 5, 6 or 7; or pharmaceutically acceptable salt or diastereomer thereof, which is useful for prophylaxis and treatment of a viral disease in a patient relating to hepatitis B infection or a disease caused by hepatitis B infection.
    Type: Grant
    Filed: August 20, 2018
    Date of Patent: February 23, 2021
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Junli Chen
  • Hetero-halo inhibitors of histone deacetylase
    Patent number: 10919902
    Abstract: This invention provides compounds that are inhibitors of HDAC2. The compounds (e.g., compounds according to Formula I, II or any of Compounds 100-128 or any of those in Tables 2 or 3) accordingly are useful for treating, alleviating, or preventing a condition in a subject such as a neurological disorder, memory or cognitive function disorder or impairment, extinction learning disorder, fungal disease or infection, inflammatory disease, hematological disease, or neoplastic disease, or for improving memory or treating, alleviating, or preventing memory loss or impairment.
    Type: Grant
    Filed: December 26, 2019
    Date of Patent: February 16, 2021
    Assignee: Alkermes, Inc.
    Inventors: Martin R. Jefson, John A. Lowe, III, Fabian Dey, Andreas Bergmann, Andreas Schoop, Nathan Oliver Fuller
  • Substituted tricyclic heterocyclic compounds and use thereof
    Patent number: 10918645
    Abstract: Provided are a substituted tricyclic heterocyclic compound of formula I or a stereoisomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt, ester or a prodrug thereof, a pharmaceutical composition including the same and uses thereof. The substituted tricyclic heterocyclic compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be used for treating a disorder caused by at least one of cancer and neurodegenerative diseases. Further the compounds and the pharmaceutical compositions comprising the compounds disclosed herein can be also used for preventing or treating a disorder caused by, associated with or accompanied by any abnormal kinase activity.
    Type: Grant
    Filed: June 13, 2017
    Date of Patent: February 16, 2021
    Assignees: LIFEARC, SUZHOU YABAO PHARMACEUTICAL R&D CO., LTD.
    Inventors: Yan Xia, Edward Giles McIver, Yang Song, Yuanyuan Xu, Lin Zhu, Chunjun Chu, Ling Wu, Miao Liu, Justin Stephen Bryans
  • Crystalline form of aripiprazole
    Patent number: 10913721
    Abstract: The present invention relates to a crystalline form N of aripiprazole, pharmaceutical compositions thereof and the use of crystalline form N in the preparation of a medicament for the treatment of central nervous system diseases, especially schizophrenia.
    Type: Grant
    Filed: February 19, 2016
    Date of Patent: February 9, 2021
    Assignee: NANJING NORATECH PHARMACEUTICALS CO., LTD
    Inventors: Yun-Zhe Sun, Wei-Ming Jiang, Xin Zhao, Cheng-Gang Lin, Li Gui, Fei Liu
  • Tubulin-binding compounds, compositions and uses related thereto
    Patent number: 10913750
    Abstract: This disclosure relates to methods of treating cancer (e.g., melanoma) with (MI-181).
    Type: Grant
    Filed: September 17, 2019
    Date of Patent: February 9, 2021
    Assignee: The Regents of the University of California
    Inventors: Jorge Torres, Robert Damoiseaux, Todd O. Yeates, Silvia Senese, Dan E. McNamara, Yu-Chen Lo
  • NMDA receptor modulators and uses thereof
    Patent number: 10906913
    Abstract: Disclosed are compounds having enhanced potency in the modulation of NMDA receptor activity. Such compounds are contemplated for use in the treatment of diseases and disorder such as learning, cognitive activities, and analgesia, particularly in alleviating and/or reducing neuropathic pain. Orally available formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
    Type: Grant
    Filed: October 17, 2017
    Date of Patent: February 2, 2021
    Assignee: Northwestern University
    Inventors: M. Amin Khan, Joseph R. Moskal, Paul Wood