Boron Containing Doai Patents (Class 514/64)
  • Patent number: 11147802
    Abstract: Provided are a substituted oxadiazole chemical compound and composition containing said chemical compound and use thereof; said substituted oxadiazole chemical compound is the oxadiazole chemical compound as represented by formula (I), or its crystalline form, pharmaceutically acceptable salt, prodrug, stereoisomer, hydrate, or solvent compound. The disclosed substituted oxadiazole chemical compound and composition containing said chemical compound are capable of inhibiting indoleamine 2,3-dioxygenase; it also has better pharmacokinetic parameter attributes and is capable of improving the drug concentration of the chemical compound in an animal body, thus improving the therapeutic efficacy and safety of the drug.
    Type: Grant
    Filed: January 5, 2017
    Date of Patent: October 19, 2021
    Assignee: Shenzhen TargetRx, Inc.
    Inventors: Yihan Wang, Huanyin Li
  • Patent number: 11137400
    Abstract: The present disclosure relates to methods for predicting and/or determining responsiveness to an activator of JNK kinase activity. The present disclosure further relates to improved methods for treating a cancer patient with an activator of JNK kinase activity. The present disclosure also relates to methods for screening for a modulator of XBP1s protein phosphorylation.
    Type: Grant
    Filed: June 29, 2018
    Date of Patent: October 5, 2021
    Assignee: UNIVERSITY OF PITTSBURGH-OF THE COMMONWEALTH SYSTEM OF HIGHER EDUCATION
    Inventor: Hongjiao Ouyang
  • Patent number: 11091505
    Abstract: Described herein are crystalline forms of (R)-3-(2-(trans-4-(2-aminoethylamino)cyclohexyl)acetamido)-2-hydroxy-3,4-dihydro-2H-benzo[e][1,2]oxaborinine-8-carboxylic acid. In some embodiments, the crystalline forms are formulated for treating a subject in need thereof with a bacterial infection.
    Type: Grant
    Filed: March 5, 2018
    Date of Patent: August 17, 2021
    Assignee: VenatoRx Pharmaceuticals, Inc.
    Inventors: Christopher J. Burns, Daniel C. Pevear, Luigi Xerri, Timothy Henkel, Daniel McGarry, Lawrence Rosen, Gerald Brenner, Jean-Baptiste Arlin, Ana Fernandez Casares
  • Patent number: 11066425
    Abstract: Provided is a novel compound that has an excellent ?-lactamase inhibitory effect. More specifically, provided is a compound represented by formula (1a), (1b) or (11) having an excellent ?-lactamase inhibitory effect or a pharmaceutically acceptable salt thereof. By using this compound either in combination with a ?-lactam drug or alone, a useful preventive or therapeutic agent for bacterial infections is provided. Also provided are useful preventive or therapeutic agents for treating various diseases with the combined use of the aforesaid compound and ?-lactam drugs.
    Type: Grant
    Filed: December 29, 2020
    Date of Patent: July 20, 2021
    Assignees: SUMITOMO DAINIPPON PHARMA CO., LTD., THE KITASATO INSTITUTE
    Inventors: Toshio Kanai, Sachiko Koike, Takayuki Fukaya, Shunichiro Uesugi, Shingo Mizushima, Hitoshi Suda, Yuki Mizukami, Yohei Ikuma, Toshiaki Sunazuka, Yoshihiko Noguchi
  • Patent number: 11046715
    Abstract: The present disclosure relates to boronic derivatives of hydroxamate compounds, methods for making the same, methods for use as a monotherapy or in combination with one or more other therapeutic agents, for treatment of proliferative diseases such as cancer. The present disclosure also teaches the utilization of said boronic derivatives of hydroxamates as epigenetic therapy medications with enhanced bioavailability, lower-toxicity, and longer-lasting efficacy.
    Type: Grant
    Filed: November 27, 2017
    Date of Patent: June 29, 2021
    Assignee: Xavier University of Louisiana
    Inventors: Guangdi Wang, Shilong Zheng, Jiawang Liu, Qiu Zhong, Shanchun Guo
  • Patent number: 11028050
    Abstract: Provided herein are free base crystalline forms and crystalline salts of Compound 1.
    Type: Grant
    Filed: April 17, 2020
    Date of Patent: June 8, 2021
    Assignee: TETRA DISCOVERY PARTNERS, INC.
    Inventors: Mark E. Gurney, Jon P. Lawson, Stephan D. Parent, Richard James Ely
  • Patent number: 11007206
    Abstract: Method of treating or ameliorating a bacterial infection comprising administering a composition comprising a cyclic boronic acid ester compound in combination with a carbapenem antibacterial agent such as Biapenem, and the pharmacokinetics studies thereof are provided.
    Type: Grant
    Filed: January 17, 2020
    Date of Patent: May 18, 2021
    Assignee: MELINTA SUBSIDIARY CORP.
    Inventors: David C. Griffith, Michael N. Dudley, Olga Lomovskaya
  • Patent number: 10973835
    Abstract: A method is disclosed for altering the redox equilibrium of a transmembrane receptor-like protein tyrosine phosphatase (RPTP), particularly a type IIa RPTP, by chemically modulating the activity through contact of such an enzyme with a diaryl boron compound that preferentially reacts with an RPTP in an oxidized state (CyS-OH). This redox modulation is most readily observed and put to use by assaying the inhibition of the phosphatase activity of the RPTP. Such an assay can be carried out on an enzyme in vitro or by contacting the enzyme in a living organism (in vivo). A useful diaryl boron compound corresponds in structure to Formula I in which Ar-1, Ar-2, R1, R2, R3 and R4 are defined within. A pharmaceutical composition containing a useful diaryl boron compound is also disclosed, as are particularly preferred diaryl boron compounds.
    Type: Grant
    Filed: March 2, 2018
    Date of Patent: April 13, 2021
    Assignees: The Penn State Research Foundation, Cold Spring Harbor Laboratory
    Inventors: Stephen J. Benkovic, Nicholas K. Tonks, Chun Yu Liu, Navasona Krishnan, Chunliang Liu
  • Patent number: 10959993
    Abstract: The present invention is directed to a combination therapy involving a selective Bcl-2 inhibitor and a MEK inhibitor for the treatment of a patient in need of such a therapy. The patient in need of the combination therapy is suffering from cancer, such as acute myeloid leukemia.
    Type: Grant
    Filed: November 3, 2016
    Date of Patent: March 30, 2021
    Assignee: Genentech, Inc.
    Inventors: Mark Merchant, Deepak Sampath, Marina Konopleva, Lina Han
  • Patent number: 10851118
    Abstract: The invention relates to a novel class of compounds that exhibit activity inhibitory activity toward arginase, and pharmaceutical compositions comprising the compounds of the invention. Also provided herein are methods of treating cancer with the arginase inhibitors of the invention.
    Type: Grant
    Filed: August 10, 2018
    Date of Patent: December 1, 2020
    Assignee: CALITHERA BIOSCIENCES, INC.
    Inventors: Eric B. Sjogren, Jim Li, Michael Van Zandt, Darren Whitehouse
  • Patent number: 10690675
    Abstract: Compositions and methods for enriching glycocompounds are disclosed which can comprise a glycocompound bound to a boronic acid compound which can be conjugated to a dendrimer.
    Type: Grant
    Filed: April 13, 2018
    Date of Patent: June 23, 2020
    Assignee: Georgia Tech Research Corporation
    Inventors: Ronghu Wu, Weixuan Chen
  • Patent number: 10689403
    Abstract: The present invention relates to a method for preparing a four-coordinated organic boron compound, and more specifically, to a method for preparing various and widespread four-coordinated organic boron compounds by directly using an aryl, heteroaryl, or vinyl-functional boronic acid, boroxine, or borate compound as a starting material and adding the compound to any bidentate N,O-ligand, O,O-ligand, or N,N-ligand.
    Type: Grant
    Filed: March 10, 2016
    Date of Patent: June 23, 2020
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Kee In Lee, Venkata Subbaiah Sadu, In Taek Hwang
  • Patent number: 10669287
    Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to A? peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: June 2, 2020
    Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCY
    Inventors: Motomu Kanai, Yohei Soma, Jizhi Ni, Atsuhiko Taniguchi
  • Patent number: 10669290
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: January 2, 2019
    Date of Patent: June 2, 2020
    Assignee: VENATORX PHARMACEUTICALS, INC.
    Inventors: Christopher J. Burns, Denis Daigle, Bin Liu, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout
  • Patent number: 10660909
    Abstract: What is described is a method for treating cancer in a patient in need of such treatment through the use of an antagonist to CXCR1 and/or CXCR2 receptors by administering a therapeutically effective amount of an antagonist of CXCR1 and/or CXCR2, or pharmaceutical compositions thereof, either alone as monotherapy, or in combination with at least one other anticancer therapy.
    Type: Grant
    Filed: February 23, 2018
    Date of Patent: May 26, 2020
    Assignee: Syntrix Biosystems Inc.
    Inventors: John A. Zebala, Dean Y. Maeda, Aaron D. Schuler
  • Patent number: 10662140
    Abstract: The present invention relates to a method for skin-whitening using a composition containing resveratryl triglycolate as an active ingredient, and more specifically, relates to a composition for skin-whitening containing resveratryl triglycolate or a cosmetically or pharmaceutically acceptable salt thereof as an active ingredient, a method for skin-whitening including applying or administering a composition containing resveratryl triglycolate or an acceptable salt thereof as an active ingredient to a subject, and a resveratryl triglycolate compound which has a skin-whitening effect, since the resveratryl triglycolate can inhibit melanin synthesis and brighten skin tone.
    Type: Grant
    Filed: November 9, 2016
    Date of Patent: May 26, 2020
    Assignee: KYUNGPOOK NATIONAL UNIVERSITY INDUSTRY-ACADEMIC COOPERATION FOUNDATION
    Inventors: Yong Chool Boo, Won Choul Park
  • Patent number: 10640520
    Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: May 5, 2020
    Assignee: MERCK PATENT GMBH
    Inventors: Markus Klein, Oliver Schadt, Philipp Haselmayer, Michael Busch
  • Patent number: 10633399
    Abstract: Disclosed are functionalized aminobenzoboroxoles compounds, method for preparing these compounds, and methods for treating cancers.
    Type: Grant
    Filed: August 15, 2016
    Date of Patent: April 28, 2020
    Assignee: Channel Therapeutics, Inc.
    Inventors: Kandalam V. Ramanujachary, Subash C. Jonnalagadda
  • Patent number: 10626128
    Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to A? peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: April 21, 2020
    Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCY
    Inventors: Motomu Kanai, Yohei Soma, Jizhi Ni, Atsuhiko Taniguchi
  • Patent number: 10618918
    Abstract: Disclosed herein are antimicrobial compounds having the structure of the formula III? pharmaceutical compositions, the use and preparation thereof. The compounds are of the class of boronic acid derivatives, useful for antimicrobial treatment.
    Type: Grant
    Filed: March 14, 2019
    Date of Patent: April 14, 2020
    Assignee: QPEX BIOPHARMA, INC.
    Inventors: Scott Hecker, Raja K. Reddy
  • Patent number: 10526348
    Abstract: Provided is a compound which is bioapplicable and amyloid-selective, and is useful as an amyloid oxygenation catalyst applicable not only to A? peptides but also to other amyloids, and a preventive/therapeutic drug for an amyloid-related disease using the same.
    Type: Grant
    Filed: March 21, 2017
    Date of Patent: January 7, 2020
    Assignee: JAPAN SCIENCE AND TECHNOLOGY AGENCY
    Inventors: Motomu Kanai, Yohei Soma, Jizhi Ni, Atsuhiko Taniguchi
  • Patent number: 10479805
    Abstract: A beta-lactamase inhibitor having a formula (I). Also provided is a method of using the beta-lactamase inhibitor for prevention or treatment of diseases.
    Type: Grant
    Filed: October 19, 2018
    Date of Patent: November 19, 2019
    Assignee: WUHAN VISION PHARMACEUTICAL TECHNOLOGY CO., LTD.
    Inventors: Shiping Wu, Hongyu Xu, Xiangdong Hu
  • Patent number: 10464952
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: June 7, 2018
    Date of Patent: November 5, 2019
    Assignee: VENATORX PHARMACEUTICALS, INC.
    Inventors: Christopher J. Burns, Daniel C. Pevear, Robert E. Lee Trout, Randy W. Jackson, Jodie Hamrick, Allison L. Zulli, Eugen F. Mesaros, Steven A. Boyd
  • Patent number: 10449226
    Abstract: The present invention relates to a method of treating cancer in a human and to pharmaceutical combinations useful in such treatment. In particular, the method relates to a cancer treatment method that includes administering a proteasome inhibiting compound, and N-{(1S)-2-amino-1-[(3-fluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-thiophenecarboxamide, or a pharmaceutically acceptable salt thereof, and optional additional antineoplastic agents, to a human in need thereof.
    Type: Grant
    Filed: December 20, 2016
    Date of Patent: October 22, 2019
    Assignee: Novartis AG
    Inventor: Rakesh Kumar
  • Patent number: 10435418
    Abstract: A reaction method comprising combining a carbonyl-substituted arylboronic acid or ester and an ?-effect amine in aqueous solution at a temperature between about ?5 C to 55 C, and a pH between 2 and 8 to produce an adduct. A process is also provided comprising: contacting a boron compound having a boron atom bonded to a sp2 hybridized carbon conjugated with a cis-carbonyl, the boron having at least one labile substituent, with an ?-effect amine, in a solvent for a time sufficient to form an adduct, which may proceed to further products.
    Type: Grant
    Filed: September 11, 2017
    Date of Patent: October 8, 2019
    Assignee: The Research Foundation for the State University o
    Inventors: Susan Bane Tuttle, Ozlem Dilek, Kamalika Mukherjee
  • Patent number: 10421870
    Abstract: A method to prepare a self-decontaminating surface, where that method includes dissolving tartaric acid in water, adding titanium (IV) isopropoxide to the tartaric acid solution to form a coating composition in water, and casting that coating composition onto a surface to form a coating having anti-microbial function.
    Type: Grant
    Filed: December 8, 2016
    Date of Patent: September 24, 2019
    Assignee: ALLIED BIOSCIENCE, INC.
    Inventors: Craig Grossman, Mai Ngo, Ronald Wysocki
  • Patent number: 10413549
    Abstract: The present invention relates to a compositions for and methods for cancer treatment, for example, hematopoietic cancers (e.g. B-cell Lymphoma). In other aspects, the invention provides methods for treating particular types of hematopoietic cancers, such as B-cell lymphoma, using a combination of one or more of the disclosed compounds and, for example, 26S proteasome inhibitors, such as, for example, Bortezomib. In another aspect the present invention relates to autoimmune treatment with the disclosed compounds. In another aspect, this invention relates to methods for identifying compounds, for example, compounds of the BH3 mimic class, that have unique in vitro properties that predict in vivo efficacy against B-cell lymphoma tumors and other cancers as well as autoimmune disease.
    Type: Grant
    Filed: October 24, 2017
    Date of Patent: September 17, 2019
    Assignee: Eutropics Pharmaceuticals, Inc.
    Inventors: David Richard, Michael H. Cardone
  • Patent number: 10352931
    Abstract: The present invention provides a diagnostic device allowing highly specific and efficient in vivo and/or in vitro detection of a bio marker in a broad range of bodily fluids or tissues. The diagnostic device is composed of a binding agent that specifically binds a bio marker present in the bodily fluid linked by a linker compound or layer to the substrate, which includes a metallic, a semiconductor, or a polymeric carrier. The present invention further provides methods using said device for the detection of bio markers, as well as kits comprising said device and suitable ingredients for the detections of bio markers in a bodily fluid. Furthermore, the invention provides suitable in vivo and in vitro applications of said binding agent for the detection of specific disease-related target structures.
    Type: Grant
    Filed: August 27, 2014
    Date of Patent: July 16, 2019
    Assignee: GILUPI GMBH
    Inventor: Björn Nowack
  • Patent number: 10314795
    Abstract: The present invention includes compounds useful in preventing, treating or ameliorating Sigma-related disorders or diseases. The compounds of the invention may modulate cellular protein homeostasis, which includes: translation initiation, folding, processing, transport, and degradation (including ubiquitin selective autophagy) of proteins. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound. The present invention also includes methods of preventing, treating or ameliorating a Sigma-related disorder or disease in a subject in need thereof, the method comprising administering to the subject an effective amount of a Sigma-modulating compound, further comprising administering an effective amount of a compound that inhibits the ubiquitin proteasome system (UPS) and/or autophagic survival pathways.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: June 11, 2019
    Assignee: Drexel University
    Inventors: Felix J. Kim, Joseph M. Salvino
  • Patent number: 10314308
    Abstract: Compounds of formula (I) are as defined in the claims, and their use in compositions and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.
    Type: Grant
    Filed: January 13, 2016
    Date of Patent: June 11, 2019
    Assignee: SYNGENTA PARTICIPATIONS AG
    Inventors: Ramya Rajan, Daniel Stierli, Renaud Beaudegnies, Peter Renold
  • Patent number: 10294246
    Abstract: Compounds of formula (I) are inhibitors of LMP7 and can be employed, inter alia, for the treatment of an autoimmune disorder or hematological malignancies.
    Type: Grant
    Filed: October 1, 2015
    Date of Patent: May 21, 2019
    Assignee: MERCK PATENT GMBH
    Inventors: Markus Klein, Oliver Schadt, Philipp Haselmayer, Michael Busch
  • Patent number: 10292976
    Abstract: The present invention aims to prevent and/or treat malaria using an antimalarial drug comprising, as an active ingredient, a metal chelator represented by the following formula (I), (III), (IV), (V), (VI), or (VII), such as tris(2-pyridylmethyl)amine.
    Type: Grant
    Filed: October 23, 2018
    Date of Patent: May 21, 2019
    Assignee: RIKEN
    Inventors: Akira Wada, Hiroki Hayase, Nobumoto Watanabe, Hiroyuki Osada, Takeshi Shimizu, Konstanty Wierzba
  • Patent number: 10293048
    Abstract: A pharmaceutical composition and preparing processes thereof. The composition comprises bortezomib or pharmaceutically acceptable salt or solvate thereof, tromethamine and an organic carboxylic acid, and the pH of the composition is from about 3.0 to 6.0.
    Type: Grant
    Filed: March 1, 2013
    Date of Patent: May 21, 2019
    Assignee: DR. REDDY'S LABORATORIES LIMITED
    Inventors: Navin Vaya, Harshal Prabhakar Bhagwatwar, Rakeshwar Bandichhor, Nirmal Khati, Riyaz Ahmed Shaik, Rahul Bhise, Yakaswamy Asalla, Rajkumar Bhimrao Shinde
  • Patent number: 10214547
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: October 18, 2017
    Date of Patent: February 26, 2019
    Assignee: VENATORX PHARMACEUTICALS, INC.
    Inventors: Christopher J. Burns, Denis Daigle, Bin Liu, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout
  • Patent number: 10183908
    Abstract: The present invention relates to novel compounds and their use in the prophylactic and/or therapeutic treatment of kidney and/or liver disease.
    Type: Grant
    Filed: March 18, 2016
    Date of Patent: January 22, 2019
    Assignee: VECTUS BIOSYSTEMS LIMITED
    Inventor: Karen Annette Duggan
  • Patent number: 10125152
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: November 13, 2018
    Assignee: VENATORX PHARMACEUTICALS, INC.
    Inventors: Christopher J. Burns, Denis Daigle, Bin Liu, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout, Randy W. Jackson
  • Patent number: 10117944
    Abstract: The present invention provides pharmacological compounds including an effector moiety conjugated to a binding moiety that directs the effector moiety to a biological target of interest. Likewise, the present invention provides compositions, kits, and methods (e.g., therapeutic, diagnostic, and imaging) including the compounds. The compounds can be described as a protein interacting binding moiety-drug conjugate (SDC-TRAP) compounds, which include a protein interacting binding moiety and an effector moiety. For example, in certain embodiments directed to treating cancer, the SDC-TRAP can include an Hsp90 inhibitor conjugated to a cytotoxic agent as the effector moiety.
    Type: Grant
    Filed: July 28, 2016
    Date of Patent: November 6, 2018
    Assignee: MADRIGAL PHARMACEUTICALS, INC.
    Inventors: Dinesh U. Chimmanamada, Weiwen Ying
  • Patent number: 10118936
    Abstract: The present invention is directed to arginase inhibitor compounds of formula IA or formula IB: or a pharmaceutically acceptable salt thereof, compositions containing these compounds, and methods of their use for the treatment and diagnosis of conditions characterized by upregulation of arginase, abnormally high arginase activity, or by abnormally low nitric oxide synthase activity.
    Type: Grant
    Filed: December 4, 2015
    Date of Patent: November 6, 2018
    Assignees: The Trustees of the University of Pennsylvania, AstraZeneca AB
    Inventors: David W. Christianson, Bruce Edward Tomczuk, Richard Scott Pottorf, Andrew Vargha Colasanti, Gary Lee Olson
  • Patent number: 10093685
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: August 11, 2017
    Date of Patent: October 9, 2018
    Assignee: VENATORX PHARMACEUTICALS, INC.
    Inventors: Christopher J. Burns, Denis Daigle, Bin Liu, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout, Randy W. Jackson
  • Patent number: 10085452
    Abstract: An anti-fungal composition for the control of one or more target fungi (or a similar heterotrophic, hyphae-producing organism) that infect plant materials and are(is) separately controllable by a benzoxaborole and an anti-fungal compound of a preselected FRAC Target Site Code is disclosed, as is a method of its use. A composition contains a diluent medium having dissolved or dispersed therein a synergistic effective amount of each of a first and a second anti-fungal compound. The first anti-fungal compound is a benzoxaborole of Formula I. The second anti-fungal compound is other than a benzoxaborole and is known to control said one or more target species of fungus when utilized as the sole anti-fungal compound at a concentration greater than the synergistic effective amount and has a preselected FRAC Target Site Code of B, C, D, E, G, H, or M.
    Type: Grant
    Filed: July 7, 2017
    Date of Patent: October 2, 2018
    Assignee: The Penn State Research Foundation
    Inventors: Stephen Benkovic, Chunyu Liu
  • Patent number: 10072029
    Abstract: The present disclosure relates to a novel crystalline form of a proteasome inhibitor, and to the processes for the preparation thereof. The novel crystalline form according to the disclosure may be used in the preparation of pharmaceutical compositions for the treatment of cancer.
    Type: Grant
    Filed: February 10, 2016
    Date of Patent: September 11, 2018
    Assignee: Millennium Pharmaceuticals, Inc.
    Inventors: Marianne Langston, Debra Mazaik, Eric Elliott, Anton Peterson, Patricia Andres, Jing Teng
  • Patent number: 10065974
    Abstract: The invention relates to a novel class of compounds that exhibit activity inhibitory activity toward arginase, and pharmaceutical compositions comprising the compounds of the invention. Also provided herein are methods of treating cancer with the arginase inhibitors of the invention.
    Type: Grant
    Filed: October 28, 2016
    Date of Patent: September 4, 2018
    Inventors: Eric B. Sjogren, Jim Li, Michael Van Zandt, Darren Whitehouse
  • Patent number: 10011616
    Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
    Type: Grant
    Filed: April 8, 2016
    Date of Patent: July 3, 2018
    Assignee: MMV MEDICINES FOR MALARIA VENTURE
    Inventors: Yong-Kang Zhang, Jacob J. Plattner, Robert T. Jacobs
  • Patent number: 10004730
    Abstract: A method for treating prostate cancer in a subject, comprising administering a therapeutically effective amount of at least one agent to the subject, wherein the agent is selected from: (a) a phenyl-substituted imidazole, or a pharmaceutically acceptable salt or ester thereof; or (b) a compound, or a pharmaceutically acceptable salt or ester thereof, having a formula I of: ?wherein R20 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing group, a boryl-containing group, a phosphine-containing group, amino, a thio-containing group, a seleno-containing group, halide, or a nitro-containing group; R21 is an alkanediyl or a substituted alkanediyl; a is 0 or 1; c is 0 or 1; X is C or S; R22 is a moiety that includes at least one divalent amino radical; and R23 is an aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocycloalkyl, substituted heterocycloalkyl, alkoxy, aryloxy, a silyl-containing
    Type: Grant
    Filed: March 13, 2017
    Date of Patent: June 26, 2018
    Assignee: University of Pittsburgh—Of the Commonwealth System of Higher Education
    Inventors: Zhou Wang, Joel Byron Nelson, Minh Bao Nguyen, John S. Lazo, Paul A. Johnston, Peter Wipf
  • Patent number: 9949995
    Abstract: A method of treating a bacterial infection in a subject in need thereof includes administering to the subject therapeutically effective amounts of at least one ?-lactam antibiotic and at least one triazolylmethyl boronic acid.
    Type: Grant
    Filed: September 6, 2016
    Date of Patent: April 24, 2018
    Assignee: Case Western Reserve University
    Inventors: Robert Bonomo, Fabio Prati, Emilia Caselli, Chiara Romagnoli
  • Patent number: 9944658
    Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
    Type: Grant
    Filed: March 13, 2014
    Date of Patent: April 17, 2018
    Assignee: VENATORX PHARMACEUTICALS, INC.
    Inventors: Christopher J. Burns, Denis Daigle, Bin Liu, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout
  • Patent number: 9944660
    Abstract: The present invention provides a tricyclic compound represented by general formula (I), a pharmaceutical salt thereof, or a stereoisomer thereof exhibits excellent antibacterial activity against Gram-negative bacteria resistant bacteria thereof, and also being excellent in terms of safety. Furthermore, the present invention provides production processes, pharmaceutical compositions comprising a tricyclic compound, a pharmaceutically acceptable salt thereof, or a stereoisomer thereof as an active ingredient and use thereof as a pharmaceutical agent. The compounds of the present invention are useful for the treatment and/or prevention of disease such as complicated urinary tract infections (cUTIs), nosocomial pneumonia, intra-abdominal infections (IAIs) or bacteremia.
    Type: Grant
    Filed: December 29, 2016
    Date of Patent: April 17, 2018
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Ajay Soni, Aditi Agarwal, Sangram Shesharao Deshmukh, Kedar Padmakar Purnapatre, Shinji Marumoto
  • Patent number: 9937154
    Abstract: The described invention relates to methods for preventing or treating graft-versus-host disease while preserving a graft-versus-tumor effect, increasing survival of, preserving alloreactivity, or a combination thereof in a patient with a tumor receiving a transplant. The described methods comprise administering to the patient a therapeutic amount of a pharmaceutical composition comprising a Rho kinase inhibitor compound, e.g., telmisartan or related angiotensin receptor blockers, and a pharmaceutically acceptable excipient. The therapeutic amount may be effective to attenuate graft-versus-host disease and to preserve the graft-versus-tumor effect of the transplant.
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: April 10, 2018
    Assignee: Hackensak University Medical Center
    Inventors: David Schwartz, Sujatha Iyengar
  • Patent number: 9889146
    Abstract: Norvaline and/or other amino acids that are capable of being acylated onto tRNALeu by LeuRS, in combination with substituted benzoxaboroles, such as a compound having a structure according to formula III: and methods for decreasing the frequency of resistance and/or reducing the rate of resistance and/or suppressing the emergence of resistance that develops in bacteria exposed to a substituted benzoxaborole or salt thereof by administering a combination of a substituted benzoxaborole such as a compound of formula III or salt thereof and an amino acid or a salt thereof.
    Type: Grant
    Filed: May 23, 2016
    Date of Patent: February 13, 2018
    Assignee: Anacor Pharmaceuticals, Inc.
    Inventors: Michael Richard Kevin Alley, Katherine Widdowson
  • Patent number: 9861626
    Abstract: The present invention aims to prevent and/or treat malaria using an antimalarial drug comprising, as an active ingredient, a metal chelator represented by the following formula (I), (III), (IV), (V), (VI), or (VII), such as tris(2-pyridylmethyl)amine.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: January 9, 2018
    Assignee: RIKEN
    Inventors: Akira Wada, Hiroki Hayase, Nobumoto Watanabe, Hiroyuki Osada, Takeshi Shimizu, Konstanty Wierzba