Patents Examined by Brian E McDowell
  • Patent number: 10738066
    Abstract: The disclosure provides compounds having formula (I): and the pharmaceutically acceptable salts thereof, wherein R1, R2, R2?, and X are as defined as set forth in the specification. Compounds having formula (I) are prodrugs that release glutamine analogs, e.g., 6-diazo-5-oxo-L-norleucine (DON). The disclosure also provides compounds having formula (I) for use in treating cancer.
    Type: Grant
    Filed: June 27, 2019
    Date of Patent: August 11, 2020
    Assignees: The Johns Hopkins University, Ústav organické chemie a biochemie AV {hacek over (C)}R, v.v.i.
    Inventors: Barbara Slusher, Rana Rais, Lukas Tenora, Pavel Majer, Andrej Jancarik
  • Patent number: 10736908
    Abstract: Compounds of Formula (I): (Formula (I)) and their pharmaceutically acceptable salts are useful for the inhibition of HIV reverse transcriptase. The compounds may also be useful for the prophylaxis or treatment of infection by HIV and in the prophylaxis, delay in the onset or progression, and treatment of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antiviral agents, immunomodulators, antibiotics or vaccines.
    Type: Grant
    Filed: October 20, 2017
    Date of Patent: August 11, 2020
    Assignees: MERCK SHARP & DOHME CORP., IDENIX PHARMACEUTICALS LLC
    Inventors: Jean-Laurent Paparin, Houcine Rahali, Aurélien Salanson, Daniel Da Costa, David Dukhan, Timothy J. Hartingh, Izzat Raheem, John Schreier
  • Patent number: 10738033
    Abstract: The present invention relates to the use of substituted pyrimidine derivatives to modulate tropomyosin-related kinase (Trk) family protein kinase, and the use of the substituted pyrimidine derivatives for the treatment of pain, inflammation, cancer, restenosis, atherosclerosis, psoriasis, thrombosis, a disease, disorder, injury, or malfunction relating to dysmyelination or demyelination or a disease or disorder associated with abnormal activities of nerve growth factor (NGF) receptor TrkA. The present invention also provides compounds of the formula: as defined herein.
    Type: Grant
    Filed: May 30, 2018
    Date of Patent: August 11, 2020
    Assignee: NANTBIO, INC.
    Inventors: Chunlin Tao, Qinwei Wang, Sharif Asad, Paul Weingarten, Sherry Ci
  • Patent number: 10730890
    Abstract: There is described a phthalocyanine derivative of formula (I) consisting of 4 isomers wherein the relative isomer B content is less than or equal to 1% by weight.
    Type: Grant
    Filed: January 28, 2016
    Date of Patent: August 4, 2020
    Assignee: MOLTENI THERAPEUTICS S.R.L.
    Inventors: Gabrio Roncucci, Donata Dei, Giacomo Chiti, Daniele Nistri
  • Patent number: 10730851
    Abstract: The application discloses five polymorph forms B, P, F, J, O of (4-((R)-((2S,5R)-4-(3-fluorobenzyl)-(2,5-dimethylpiperazine-1-yl)(3-hydroxyphenyl)methyl)phenyl)(4-methylpiperidine-1-yl)methanone dihydrochloride, preparation methods thereof and application thereof in the manufacture of a medicament for preventing or treating a mood disorder or a disease related to a ? opioid receptor.
    Type: Grant
    Filed: November 21, 2016
    Date of Patent: August 4, 2020
    Assignee: Yunnan Institute of Materia Medica
    Inventors: Jingkun Wang, Zhaoyun Zhu, He Song, Min Sun, Tao Cui, Zeren Wang, Zhi Yang, Min Su, Hongbin Liu, Bing Shi, Yong Mao, Huilang Liu, Zeqian Li, Chunmei Zhao, Mei Su, Fang Yuan, Tiancai Zhang, Yong Liu, Kuanren Zhang, Yunlin Wei, Yuehai Shen
  • Patent number: 10730831
    Abstract: Provided herein are compounds, such as compounds of Formula I, that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: August 4, 2020
    Assignee: Ligand Pharmaceuticals Incorporated
    Inventor: Lin Zhi
  • Patent number: 10723743
    Abstract: Compounds of formula (II) or a pharmaceutically acceptable salt or solvate thereof, the medical uses thereof for diseases or medical conditions where the inhibition of the voltage-gated potassium channel Kv1.3 is beneficial, and methods for their preparation.
    Type: Grant
    Filed: February 13, 2019
    Date of Patent: July 28, 2020
    Assignee: 4SC AG
    Inventors: Stefan Tasler, Ilga Krimmelbein, Juergen Kraus, Mirko Zaja
  • Patent number: 10717749
    Abstract: The present invention relates to novel macrocyclic sulfondiimine compounds of general formula (I) as described and defined herein, and methods for their preparation, their use for the treatment and/or prophylaxis of disorders, in particular of hyper-proliferative disorders and/or virally induced infectious diseases and/or of cardiovascular diseases. The invention further relates to intermediate compounds useful in the preparation of said compounds of general formula (I).
    Type: Grant
    Filed: September 26, 2016
    Date of Patent: July 21, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Ulrich Lücking, Jens Geisler, Daniel Hog, Arne Scholz, Kirstin Petersen, Philip Lienau, Christian Stegmann, Dorothee Andres, Kunzeng Zheng, Ping Gao, Gang Chen, Jiajun Xi, Simon Anthony Herbert, Gerhard Siemeister, Nicolas Werbeck
  • Patent number: 10710997
    Abstract: Compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4) of the following formula: synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.
    Type: Grant
    Filed: September 1, 2017
    Date of Patent: July 14, 2020
    Assignee: Vanderbilt University
    Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Andrew Felts, Aaron M. Bender
  • Patent number: 10696670
    Abstract: A novel class of fluorinated derivatives of Formula I have been prepared and found to be useful in the treatment of cancers and other disorders related mediated by Bromodomain-Containing Proteins.
    Type: Grant
    Filed: March 11, 2019
    Date of Patent: June 30, 2020
    Assignee: Trillium Therapeutics Inc.
    Inventors: Abdelmalik Slassi, Peter Dove
  • Patent number: 10676434
    Abstract: Disclosed are compounds of Formula (I): or a salt thereof, wherein Q, R1a, R1b, R2a, R2b, R3, R4, R5a, R5b, R6a, R6c, R7a, R7b, R7c, and R7d are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bruton's tyrosine kinase (Btk), and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.
    Type: Grant
    Filed: April 10, 2019
    Date of Patent: June 9, 2020
    Assignee: Bristol-Myers Squibb Company
    Inventors: Saleem Ahmad, Douglas G. Batt, Qingjie Liu, John E. Macor, Joseph A. Tino, Scott Hunter Watterson, Satheesh Kesavan Nair, Tarun Kumar Maishal
  • Patent number: 10676424
    Abstract: The present invention provides a process of producing a trifluoromethoxylated aryl or trifluoromethoxylated heteroaryl having the structure: wherein A is an aryl or heteroaryl, each with or without substitution; and R1 is —H, -(alkyl), -(alkenyl), -(alkynyl), -(aryl), -(heteroaryl), -(alkylaryl), -(alkylheteroaryl), —NH-(alkyl), —N(alkyl)2, —NH-(alkenyl), —NH-(alkynyl) —NH-(aryl), —NH-(heteroaryl), —O-(alkyl), —O-(alkenyl), —O-(alkynyl), —O-(aryl), —O-(heteroaryl); —S-(alkyl), —S-(alkenyl), —S-(alkynyl), —S-(aryl), or —S-(heteroaryl), comprising: (a) reacting a compound having the structure: with a trifluoromethylating agent in the presence of a base in a first suitable solvent under conditions to produce a compound having the structure: and (b) maintaining the compound produced in step (a) in a second suitable solvent under conditions sufficient to produce the trifluoromethoxylated aryl or trifluormethoxylated heteroaryl having the structure:
    Type: Grant
    Filed: September 17, 2018
    Date of Patent: June 9, 2020
    Assignee: The Research Foundation for the State University of New York
    Inventors: Ming-Yu Ngai, Katarzyna N. Hojczyk
  • Patent number: 10669246
    Abstract: The present disclosure provides a compound of general Formula (I) having c-abl kinase inhibitory activity or pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the compound, and a method useful to treat or prevent neurodegenerative diseases using the compound.
    Type: Grant
    Filed: October 1, 2018
    Date of Patent: June 2, 2020
    Assignee: 1ST Biotherapeutics, Inc.
    Inventors: Jinhwa Lee, Suyeon Jo, Gwibin Lee, Keonseung Lim, A Yeong Park, Wanjun Li, Mingzhu Fan
  • Patent number: 10669275
    Abstract: The present invention relates to co-crystals of ibrutinib and a pharmaceutical composition comprising the same as well as a method of preparing the same.
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: June 2, 2020
    Assignee: ratiopharm GmbH
    Inventors: Wolfgang Albrecht, Jens Geier, Sebastian Rabe, David Perez Palacios
  • Patent number: 10668065
    Abstract: The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives of Formula I as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 (“mGluR2”). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
    Type: Grant
    Filed: January 31, 2019
    Date of Patent: June 2, 2020
    Assignee: Janssen Pharmaceutica NV
    Inventors: Susana Conde-Ceide, Michiel Luc Maria Van Gool, María Luz Martín-Martín
  • Patent number: 10662178
    Abstract: The present invention provides a novel crystalline form of Olaparib comprising Olaparib and benzyl alcohol, compositions thereof, and the use of this crystalline form in the treatment of cancers, such as germline BRCA-mutated (gBRCAm) advanced ovarian cancer.
    Type: Grant
    Filed: January 30, 2019
    Date of Patent: May 26, 2020
    Assignee: Apotex Inc.
    Inventors: Allan W. Rey, Fabio E. S. Souza, Annyt Bhattacharyya, Bahareh Khalili
  • Patent number: 10662185
    Abstract: The present application relates to novel substituted imidazo[1,2-a]pyridine-3-carboxamides of the general formula (I) to processes for their preparation, to their use alone or in combinations for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular for the treatment and/or prophylaxis of cardiovascular disorders.
    Type: Grant
    Filed: July 2, 2018
    Date of Patent: May 26, 2020
    Assignee: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Alexandros Vakalopoulos, Markus Follman, Ingo Hartung, Philipp Buchgraber, Rolf Jautelat, Jorma Haßfeld, Niels Lindner, Alexey Gromov, Frank Wunder, Johannes-Peter Stasch, Gorden Redlich, Volkhart Min-Jian Li, Eva Maria Becker-Pelster, Andreas Knorr
  • Patent number: 10654836
    Abstract: The present invention relates to a pyrimidine derivative, a method for preparing same and use thereof in medicine. In particular, the present invention relates to a pyrimidine derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as a FGFR4 kinase inhibitor, definitions of each substituent in the general formula (I) being the same as those defined in the description.
    Type: Grant
    Filed: May 19, 2017
    Date of Patent: May 19, 2020
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Lei Chen, Dongliang Guan, Hua Bai, Jun Gou, Weifeng Zhao, Zhongli Wang, Long Ling, Yutao Ma
  • Patent number: 10654839
    Abstract: Provided are compounds of Formula (II) that enhance the efficacy of viruses by increasing spread of the virus in cells, increasing the titer of virus in cells, or increasing the antigen expression from a virus, gene or trans-gene expression from a virus, or virus protein expression in cells. Other uses, compositions and methods of using same are also provided.
    Type: Grant
    Filed: January 26, 2016
    Date of Patent: May 19, 2020
    Assignees: Ottawa Hospital Research Institute, University of Ottawa
    Inventors: Jean-Simon Diallo, Christopher Noyce Boddy, Mark Dornan, Ramya Krishnan, Rozanne Arulanandam, Fabrice Le Boeuf, Jeffrey Smith, Andrew Macklin
  • Patent number: 10654856
    Abstract: The present invention relates to a method for preparing a pyrrolo[3,2-d]pyrimidine compound (the compound represented by formula I), and corresponding intermediates.
    Type: Grant
    Filed: February 4, 2017
    Date of Patent: May 19, 2020
    Assignee: CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.
    Inventors: Zhaozhong Ding, Fei Sun, Yinghu Hu, Yilong Zhou, Rui Zhao, Ling Yang