Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
  • Patent number: 10328079
    Abstract: The present invention relates to the treatment of solid tumors in humans such as cancer, especially colorectal cancer (CRC), which involves administering multiple boluses of the diastereomerically pure folate adjuvant [6R]-5,10-methylenetetrahydrofolate in 5-fluorouracil (5-FU) based chemotherapy.
    Type: Grant
    Filed: January 9, 2018
    Date of Patent: June 25, 2019
    Assignee: Isofol Medical AB
    Inventors: Per L. Lindberg, Anders Vedin, Gunnel E. Sundén, Bengt Gustavsson
  • Patent number: 10292984
    Abstract: The present invention provides methods for increasing plasma dUrd levels comprising the administration of 6R-MTHF. The methods of increasing plasma dUrd increase dUrd levels compared to equimolar concentrations of LV. The present invention also provides methods for increasing TS inhibition comprising the administration of 6R-MTHF. The present invention also provides methods for increasing TS inhibition comprising the administration of 6R-MTHF.
    Type: Grant
    Filed: February 9, 2018
    Date of Patent: May 21, 2019
    Assignee: Isofol Medical AB
    Inventors: Göran U. Carlsson, Bengt Gustavsson, Elisabeth Odin, Yvonne Wettergren, Anders Vedin
  • Patent number: 10266558
    Abstract: Nucleosides and nucleotides (nucleos(t)ides) have been in clinical use for almost 50 years and have become cornerstones of treatment for patients with viral infections or cancer. The approval of several additional drugs over the past decade demonstrates that this family still possesses strong potential. Therefore nucleos(t)ide are of great interest as promising chemotherapeutic agents, including: 2?-deoxy-L-uridine (CAS 31501-19-6), 2?-deoxy-D-uridine (CAS 951-78-0), telbivudine (CAS 3424-98-4), zidovudine (AZT, CAS 30516-87-1), trifluridine (CAS 70-00-8), clevudine (CAS 163252-36-6), PSI-6206 (CAS 863329-66-2), 2?-(S)-2?-chloro-2?-deoxy-2?-fluorouridine (CAS 1673560-41-2), ND06954 (CAS 114248-23-6), stavudine (CAS 3056-17-5), 5-ethynyltavudine (Festinavir, CAS 634907-30-5), torcitabine (CAS 40093-94-5), (?)-beta-D-(2R,4R)-dioxolane-thymine (DOT, 1-((2R,4R)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)-5-methyl-2,4(1H,3H)-pyrimidinedione, CAS No.
    Type: Grant
    Filed: October 7, 2016
    Date of Patent: April 23, 2019
    Inventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Andrey Alexandrovich Ivashchenko, Alena Alexandrovna Ivachtchenko, Nikolay Filippovich Savchuk
  • Patent number: 10259792
    Abstract: The present invention provides a crystal that has preferable oral absorption and can be obtained with particularly preferable reproducibility. Provided is a crystal of (R)—N-(1-(3-(cyclopentyloxy)phenyl)ethyl)-3-((2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)methoxy)propane-1-sulfonamide.
    Type: Grant
    Filed: April 28, 2016
    Date of Patent: April 16, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Masayoshi Fukuoka
  • Patent number: 10251884
    Abstract: Disclosed herein are compositions comprising lopinavir alone or in combination with ritonavir for use as a medicament in the treatment of cancer or benign proliferative disorders (warts) or in the prevention of the development of cancer. Pharmaceutical compositions formulated for topical application comprising a therapeutically effective amount of lopinavir or a therapeutically effective amount lopinavir and ritonavir in a pharmaceutically acceptable vehicle are also provided. Also disclosed are methods of treating a patient having an HPV related dysplasia of the cervix comprising administering to said patient a therapeutically effective dose of the disclosed pharmaceutical compositions.
    Type: Grant
    Filed: September 5, 2017
    Date of Patent: April 9, 2019
    Assignee: The University of Manchester
    Inventors: Ian Hampson, Lynne Hampson
  • Patent number: 10172354
    Abstract: A fungicidal composition containing a fungicidally effective amount of (a) the compound of Formula I, (3S,6S,7R,8R)-8-benzyl-3-(3-((isobutyryloxy)methoxy)-4-methoxypicolinamido)-6-methyl-4,9-dioxo-1,5-dioxonan-7-yl isobutyrate, and (b) fluxapyroxad, provides synergistic control of selected fungi.
    Type: Grant
    Filed: December 27, 2013
    Date of Patent: January 8, 2019
    Assignee: Dow AgroSciences LLC
    Inventors: David G. Ouimette, J. Todd Mathieson, Gregory M. Kemmitt
  • Patent number: 10143680
    Abstract: The present invention relates to pharmaceutical dosage forms for oral administration comprising the drug substance 4-[(5R)-6,7-dihydro-5H-pyrrolo[1,2-c]imidazol-5-yl]-3-fluorobenzonitrile or any pharmaceutically acceptable salt thereof and to processes of making said solid pharmaceutical dosage forms.
    Type: Grant
    Filed: July 6, 2015
    Date of Patent: December 4, 2018
    Assignee: Novartis AG
    Inventors: Stefania Beato, Peggy Quinton
  • Patent number: 10118910
    Abstract: This invention is benzothiophene-based estrogen receptor downregulators and their compositions and uses to treat estrogen-related medical disorders.
    Type: Grant
    Filed: December 9, 2016
    Date of Patent: November 6, 2018
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Gregory R. Thatcher, Rui Xiong, Jiong Zhao, Debra A. Tonetti
  • Patent number: 10112909
    Abstract: The disclosure describes methods of synthesis of phosphonate ester compounds. The methods according to the disclosure allow for large-scale preparation of phosphonate ester compounds having high purity and stability. Also disclosed are morphic forms of phosphonate ester compounds.
    Type: Grant
    Filed: December 1, 2017
    Date of Patent: October 30, 2018
    Assignee: Chimerix, Inc.
    Inventors: Roy Wendell Ware, Aaron Leigh Downey
  • Patent number: 10105365
    Abstract: The present disclosure relates to solid dosage forms comprising antiviral compounds and methods of using such dosage forms to treat antiviral infection.
    Type: Grant
    Filed: June 30, 2017
    Date of Patent: October 23, 2018
    Assignee: AbbVie Inc.
    Inventors: Jonathan M. Miller, John B. Morris, Nancy E. Sever, Eric A. Schmitt, Ping X. Gao, Yi Shi, Yi Gao, Bernd Liepold, Anna Moosmann, Mirko Pauli, Fatih Durak, Thomas Kessler, Peter Hoelig, Karin Rosenblatt, Drazen Kostelac, Rajeev Gokhale, Mark Costello, Carl Knable, Susan George
  • Patent number: 10058551
    Abstract: The invention provides a compound of formula (Ia), and pharmaceutically acceptable salts thereof. The invention also provides use of the compounds or salts as modulators of Kv3.1 and/or Kv3.2, and in the treatment of diseases or disorders where a modulator of Kv3.1 and/or Kv3.2 is required, such as depression and mood disorders, hearing disorders, schizopherenea, substance abuse disorders, sleep disorders or epilepsy.
    Type: Grant
    Filed: October 2, 2017
    Date of Patent: August 28, 2018
    Assignee: Autifony Therapeutics Limited
    Inventors: Giuseppe Alvaro, Anne Decor, Stefano Fontana, Dieter Hamprecht, Charles Large, Agostino Marasco
  • Patent number: 10051862
    Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi wherein the at least one fungicide is a multi-site inhibitor or a strobilurin inhibitor.
    Type: Grant
    Filed: December 13, 2016
    Date of Patent: August 21, 2018
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
  • Patent number: 10045534
    Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi, wherein the at least one fungicide is a succinate dehydrogenase-inhibitor.
    Type: Grant
    Filed: December 13, 2016
    Date of Patent: August 14, 2018
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
  • Patent number: 10045533
    Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide to provide synergistic control of selected fungi wherein the at least one fungicide is a fungicidal sterol biosynthesis-inhibitor.
    Type: Grant
    Filed: December 13, 2016
    Date of Patent: August 14, 2018
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
  • Patent number: 10023564
    Abstract: Disclosed herein are novel GRK2 inhibitors and methods for their use in treating or preventing heart disease, such as cardiac failure, cardiac hypertrophy, and hypertension. In particular, disclosed herein are compounds of Formula (I) and pharmaceutically acceptable salt thereof: wherein the substituents are as described.
    Type: Grant
    Filed: August 10, 2015
    Date of Patent: July 17, 2018
    Assignee: THE REGENTS OF THE UNIVERSITY OF MICHIGAN
    Inventors: Scott D. Larsen, Kristoff Homan, Helen Waldschmidt, John J. G. Tesmer
  • Patent number: 10016424
    Abstract: The present invention relates to a compound which is an antagonist of the GluK2/GluK5 receptor or an inhibitor of the GluK2/GluK5 receptor expression for use in the treatment or the prevention of epilepsy.
    Type: Grant
    Filed: September 16, 2014
    Date of Patent: July 10, 2018
    Assignees: INSERM (INSTITUT NATIONAL DE LA SANTÉ ET DE LA RECHERCHE MÉDICALE, UNIVERSITÉ D'AIX MARSEILLE, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE (CNRS), UNIVERSITE DE BORDEAUX
    Inventors: Valerie Crepel, Christophe Mulle, Angelique Peret
  • Patent number: 10015964
    Abstract: The present invention provides a fungicidal composition useful as an agricultural and horticultural fungicide having remarkably improved controlling effects against plant diseases, and a method for controlling plant diseases using the composition. A fungicidal composition comprising, as active ingredients, (a) 3-(2,3,4-trimethoxy-6-methylbenzoyl)-5-chloro-2-methoxy-4-methylpyridine (pyriofenone) or its salt and (b) at least one fungicide selected from the group consisting of bixafen, fluxapyroxad, penflufen, isopyrazam, fluopyram, ametoctradin, fenpyrazamine and sedaxane, and a method for controlling plant diseases, which comprises applying the fungicidal composition to plants.
    Type: Grant
    Filed: June 15, 2012
    Date of Patent: July 10, 2018
    Assignee: Ishihara Sangyo Kaisha, Ltd.
    Inventors: Munekazu Ogawa, Yuzuka Kawai
  • Patent number: 9988687
    Abstract: A method of classifying a patient for eligibility for cancer therapy based on the presence or absence of splicing variants in a sample of the patient's cancer tissue. Also, a method of screening cancer therapies for efficacy against splicing variants. More specifically, the methods relate to novel splicing variants of genes associated with cancer risk and survival, particularly splicing variants of PIK3CD, FGFR3, TSC2, RASGRP2, ITGA4, MET, NF1 and BAK1. Also more specifically, the methods relate to classifying a patient for eligibility for cancer therapy involving the use of GS-1101.
    Type: Grant
    Filed: March 5, 2015
    Date of Patent: June 5, 2018
    Assignee: THE GEORGE WASHINGTON UNIVERISTY
    Inventors: Norman Lee, Bi-Dar Wang
  • Patent number: 9987280
    Abstract: Provided herein are, inter alia, methods and compositions for treating or preventing diseases using SIRT1 inhibitors. The methods provided herein are particularly useful for treating or preventing age-related hematological diseases as well as cancerous hematological diseases. Further provided herein are hematopoietic cells useful for treating or preventing hematological diseases.
    Type: Grant
    Filed: August 11, 2014
    Date of Patent: June 5, 2018
    Assignee: City of Hope
    Inventors: WenYong Chen, Zhiqiang Wang
  • Patent number: 9877966
    Abstract: The invention provides therapeutic compositions and methods for the inhibition of metastasis and for treatment of cancers in human and non-human mammals that are directed to the coformulation and/or coadministration of a dehydropyrimidine dehydrogenase inhibitor such as gimeracil and a pyrrolopyrimidine compound.
    Type: Grant
    Filed: August 10, 2016
    Date of Patent: January 30, 2018
    Inventors: Eugene J. Oliva, Paul Diamond
  • Patent number: 9850215
    Abstract: Provided herein are 5-fluoro-4-imino-3-(alkyl/substituted alkyl)-1-(arylsulfonyl)-3,4-dihydropyrimidin-2(1H)-one and processes for their preparation which may include the use of an alkali carbonate and an alkylating agent
    Type: Grant
    Filed: June 3, 2016
    Date of Patent: December 26, 2017
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: Nakyen Choy, Ronald Ross, Jr.
  • Patent number: 9802933
    Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Grant
    Filed: December 15, 2016
    Date of Patent: October 31, 2017
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
  • Patent number: 9776985
    Abstract: Provided is a novel process for the preparation of alogliptin.
    Type: Grant
    Filed: May 20, 2014
    Date of Patent: October 3, 2017
    Assignee: GLENMARK PHARMACEUTICALS LIMITED
    Inventors: Navin Ganesh Bhatt, Samir Naik, Ajay Kumar Sharma, Mahendra Joma Choraghe, Shekhar Bhaskar Bhirud
  • Patent number: 9770406
    Abstract: The invention relates to a medicament containing a compound of general formula (I), where R1=independently, a straight or branched, saturated, singly- or multiply-unsaturated, optionally substituted C11-C21 alkyl, alkylene or alkinyl group, preferably a C11-C15 alkyl, alkylene or alkinyl group, particularly a C11-C13 alkyl, alkylene or alkinyl group, most preferably a C13 alkyl group, R2=independently, a straight or branched C1-C8 alkyl, alkylene or alkinyl group, preferably a C1-C6 alkyl, alkylene or alkinyl group, in particular a C2-C4 alkyl, alkylene or alkinyl group, most preferably a C3 alkyl group, a —[CH2—(CH2)m-O]nH group with n=1 to 10, preferably n=1 to 5, to m=1 to 5, preferably m=1 to 3, a —CH2—[CH—(OH)]p[CH2—R3]- group, where R3=independently H or OH, p=1 to 7, preferably p=1 to 4, a pentose group or a hexose group, as therapeutically active agent, alone or in combination with one or several further pharmaceutical agents as a combination preparation for the treatment of viral skin diseases and/or
    Type: Grant
    Filed: September 21, 2010
    Date of Patent: September 26, 2017
    Assignee: Medigene AG
    Inventors: Yunik Chang, Robert Lathrop, Erwin Böhm, Irene Gander-Meisterernst, Regina Greger, Johanna Holldack, Ulrich Moebius
  • Patent number: 9676714
    Abstract: Disclosed are a sulfonylindole derivative useful for the prevention or treatment of peptic ulcer, gastritis or reflux esophagitis, a method of preparing the same, and a pharmaceutical composition containing the same.
    Type: Grant
    Filed: October 2, 2014
    Date of Patent: June 13, 2017
    Assignee: Daewoong Pharmaceutical Co., Ltd.
    Inventors: Kyung A Yu, Ji Sung Yoon, Deok Ki Eom, Yeon Im Lee, Hye Ryun Shin, Jun Hee Lee, Ha Nee Seo, Ji Duck Kim, Sang Ho Lee, Chun Ho Lee
  • Patent number: 9669030
    Abstract: The present invention relates to the prophylaxis of acute noise-induced hearing loss by administering a compound of formula (I): wherein: W is group (Wa), group (Wb) or group (Wc):
    Type: Grant
    Filed: May 22, 2013
    Date of Patent: June 6, 2017
    Assignee: AUTIFONY THERAPEUTICS LIMITED
    Inventor: Charles Large
  • Patent number: 9642373
    Abstract: The present invention provides novel insecticidal formulations comprising an effective concentration of: 1) at least one or more essential oils and an insecticidal soap; 2) at least one or more essential oils, an insecticidal soap, and pyrethrins; 3) at least one or more essential oils and pyrethrins; 4) at least one or more essential oils, an insecticidal soap and a synergist, such as sodium lauryl sulfate, sodium dodecyl sulfate or lecithin; 5) at least one or more essential oils, an insecticidal soap, a synergist, and pyrethrins; and 6) at least one or more essential oils, a synergist, and pyrethrins. A carrier oil, such as mineral oil, may be added to any of the foregoing formulations.
    Type: Grant
    Filed: March 20, 2014
    Date of Patent: May 9, 2017
    Assignee: WOODSTREAM CORPORATION
    Inventor: David L. Anderson
  • Patent number: 9642808
    Abstract: Extended release pharmaceutical compositions comprising mycophenolate sodium as the active agent, wherein the said composition exhibits a characteristic release profile when subjected to in-vitro dissolution study, and wherein said mycophenolate sodium is released in a sustained manner in-vivo for a prolonged duration in such quantities that substantially alleviates or at least reduces the chances of causing any associated gastrointestinal side effect(s) without compromising the bioavailability of the said active agent are provided. The present invention also provides process of preparing dosage form compositions and prophylactic and/or therapeutic methods of using such dosage form. The compositions of the present invention are useful for the management such as prophylaxis, amelioration and/or treatment of immunosuppressant indicated disease(s)/disorder(s) especially for the treatment or prevention of organ, tissue or cellular allograft or xenograft rejection, e.g.
    Type: Grant
    Filed: August 11, 2008
    Date of Patent: May 9, 2017
    Assignee: PANACEA BIOTECH LIMITED
    Inventors: Rajesh Jain, Sukhjeet Singh, Sampath Kumar Devarajan
  • Patent number: 9642368
    Abstract: This present disclosure is related to the field of 3-alkyl-5-fluoro-4-substituted-imino-3,4-5 dihydropyrimidin-2(1H)-ones and their derivatives and to the use of these compounds as fungicides. Also provided are methods of controlling a fungal disease such as Septoria tritici, comprising administering an effective amount of the fungicide compound to at lease one surface associated with the plant, seed or soil.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: May 9, 2017
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: Beth Lorsbach, Ronald Ross, W. John Owen, Jeffery D. Webster, Lindsay Stelzer, Chenglin Yao, Paul R. LePlae, Jr., Chris V. Galliford
  • Patent number: 9624213
    Abstract: Compounds active on protein kinases are described, as well as methods of making and using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.
    Type: Grant
    Filed: February 1, 2012
    Date of Patent: April 18, 2017
    Assignee: Plexxikon Inc.
    Inventors: Prabha Ibrahim, Chao Zhang, Wayne Spevak, Jiazhong Zhang, Guoxian Wu, Jack Lin, Hanna Cho, Marika Nespi, Songyuan Shi, Todd Ewing, Ying Zhang
  • Patent number: 9597316
    Abstract: Provided herein are compounds, comprising Formula (I) or Formula (II), and their pharmaceutically acceptable salts. Also provided are pharmaceutical compositions comprising a pharmaceutically acceptable excipient and at least one compound of Formula (I) and (II), singly or in combination with other pharmaceutically active ingredients, such as anti-inflammatory agents or anticancer agents. These compounds and pharmaceutical compositions are useful for treating inflammation or an inflammation related disorder in a subject via administration to the subject. These compounds and pharmaceutical compositions are also useful for inhibiting COX-2, for treating cancer, for reducing the size of a neoplasm, and for inhibiting tubulin polymerization in a cell.
    Type: Grant
    Filed: December 26, 2013
    Date of Patent: March 21, 2017
    Assignee: BIOVENTURES LLC
    Inventors: Narsimha Reddy Penthala, Peter Crooks
  • Patent number: 9593114
    Abstract: The invention relates to fluorinated compounds and their use as integrin receptor antagonists. Novel fluorinated 3-(2-oxo-3-(3-arylpropyl)imidazolidin-1-yl)-3-arylpropanoic acid derivatives and pharmaceutically acceptable salts or solvates thereof and their use are described.
    Type: Grant
    Filed: January 19, 2016
    Date of Patent: March 14, 2017
    Assignee: SciFluor Life Sciences, Inc.
    Inventors: Ben C. Askew, Richard W. Heidebrecht, Takeru Furuya, Mark E. Duggan
  • Patent number: 9592231
    Abstract: A method for enhancing glycemic control and/or insulin sensitivity in a human subject having diabetic nephropathy and/or metabolic syndrome comprises administering to the subject a selective endothelia A (ETA) receptor antagonist in a glycemic control and/or insulin sensitivity enhancing effective amount. A method for treating a complex of comorbidities in an elderly diabetic human subject comprises administering to the subject a selective ETA receptor antagonist in combination or as adjunctive therapy with at least one additional agent that is (i) other than a selective ETA receptor antagonist and (ii) effective in treatment of diabetes and/or at least one of said comorbidities other than hypertension. A therapeutic combination useful in such a method comprises a selective ETA receptor antagonist and at least one antidiabetic, anti-obesity or antidyslipidemic agent other than a selective ETA receptor antagonist.
    Type: Grant
    Filed: September 19, 2014
    Date of Patent: March 14, 2017
    Assignee: AbbVie Deutschland GmbH & Co. KG
    Inventors: Robert L. Roden, Richard J. Gorczynski, Michael J. Gerber
  • Patent number: 9538753
    Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide selected from the group consisting of mancozeb, chlorothalonil, pyraclostrobin, fluoxastrobin, azoxystrobin, trifloxystrobin, picoxystrobin, and kresoxim-methyl provides synergistic control of selected fungi.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: January 10, 2017
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
  • Patent number: 9532570
    Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide selected from the group consisting of fluxapyroxad, benzovindiflupyr, penthiopyrad, isopyrazam, boscalid, and fluopyram provides synergistic control of selected fungi.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: January 3, 2017
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
  • Patent number: 9526245
    Abstract: A fungicidal composition containing a fungicidally effective amount of the compound of Formula I: 5-fluoro-4-imino-3-methyl-1-tosyl-3,4-dihydropyrimidin-2(1H)-one, and at least one fungicide selected from the group consisting of: prothioconazole, epoxiconazole, cyproconazole, myclobutanil, metconazole, difenoconazole, propiconazole, fluquinconazole, and flutriafol provides synergistic control.
    Type: Grant
    Filed: December 30, 2014
    Date of Patent: December 27, 2016
    Assignee: ADAMA MAKHTESHIM LTD.
    Inventors: W. John Owen, Chenglin Yao, Beth Lorsbach
  • Patent number: 9487534
    Abstract: In addition to containing and protecting the viral genome, the capsid (protein shell) of hepatitis B virus (HBV) plays critical roles in the viral life cycle including regulation of intracellular trafficking and nucleic acid metabolism. Substituted pyrimidine modulators of the assembly of the HBV capsid structure and methods for their use are described.
    Type: Grant
    Filed: August 2, 2012
    Date of Patent: November 8, 2016
    Assignees: Scripps Research Institute, A Not-for-Profit Public Benefit Corporation of California, Indiana University Research and Technology Corporation
    Inventors: Adam Zlotnick, M. G. Finn
  • Patent number: 9399626
    Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
    Type: Grant
    Filed: June 9, 2014
    Date of Patent: July 26, 2016
    Assignee: Pfizer Inc.
    Inventors: Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
  • Patent number: 9382204
    Abstract: The present invention provides STAT3 inhibitors which preferentially suppress proliferation of cancer over non-cancer cells and inhibit migration and invasion of malignant cells. The inhibitors of the present invention selectively inhibit STAT3 binding to DNA without affecting the activation and dimerization of STAT3. Furthermore, the inhibitors of the present invention inhibit expression of STAT3 downstream target genes and STAT3 binding to chromatin in situ.
    Type: Grant
    Filed: September 25, 2014
    Date of Patent: July 5, 2016
    Assignee: Indiana University Research and Technology Corporation
    Inventor: Jian-Ting Zhang
  • Patent number: 9382286
    Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.
    Type: Grant
    Filed: December 4, 2013
    Date of Patent: July 5, 2016
    Assignees: EMORY UNIVERSITY, BETH ISRAEL DEACONESS MEDICAL CENTER, INC.
    Inventors: Raymond F. Schinazi, Junxing Shi, Joyce D. Fingeroth, Erik Gustafson
  • Patent number: 9345709
    Abstract: The present invention directs a compound represented by formula (I).
    Type: Grant
    Filed: May 21, 2015
    Date of Patent: May 24, 2016
    Assignee: OncoTherapy Science, Inc.
    Inventors: Yo Matsuo, Shoji Hisada, Yusuke Nakamura, Feryan Ahmed, Joel R. Walker, Raymond Huntley
  • Patent number: 9271496
    Abstract: A fungicidal composition containing a fungicidally effective amount of a compound of Formula I: (3S,6S,7R,8R)-8-benzyl-3-(3-((isobutyryloxy)methoxy)-4-methoxypicolinamido)-6-methyl-4,9-dioxo-1,5-dioxonan-7-yl isobutyrate, and at least one fungicide selected from the group consisting of: benzovindiflupyr and penthiopyrad provides synergistic control of selected fungi.
    Type: Grant
    Filed: December 29, 2014
    Date of Patent: March 1, 2016
    Assignee: Dow AgroSciences LLC
    Inventor: Greg Kemmitt
  • Patent number: 9271497
    Abstract: This present disclosure is related to the field of 1-(substituted-benzoyl)-5-fluoro-4-imino-3-methyl-3,4-dihydropyrimidin-2(1H)-ones and their derivatives and to the use of these compounds as fungicides. Fungicides are compounds, of natural or synthetic origin, which act to protect and/or cure plants against damage caused by agriculturally relevant fungi. Generally, no single fungicide is useful in all situations. Consequently, research is ongoing to produce fungicides that may have better performance, are easier to use, and cost less. The present disclosure relates to 1-(substituted-benzoyl)-5-fluoro-4-imino-3-methyl-3,4-dihydropyrimidin-2(1H)-one compounds and their use as fungicides. The compounds of the present disclosure may offer protection against fungi and fungi like organisms including ascomycetes, basidiomycetes, deuteromycetes, and oomycetes.
    Type: Grant
    Filed: December 23, 2013
    Date of Patent: March 1, 2016
    Assignee: Dow AgroSciences LLC
    Inventors: Beth Lorsbach, W. John Owen, Lindsay Stelzer, Chenglin Yao
  • Patent number: 9249107
    Abstract: The invention relates to a compound of the formula wherein the substituents are as defined herein, and a pharmaceutically acceptable salt of the compound of formula (1). The compounds of formula (1) and their salts possess inflammation inhibiting properties and are therefore useful in the treatment and prevention of conditions related to inflammations such as inflammatory joint diseases. The compounds of formula (1) are also useful for the treatment of diseases where chronic inflammation is the underlying cause. This application relates to compounds of formula (1), methods for their preparation, pharmaceutical compositions comprising these compounds, and their use for the preparation of a medicament for the treatment of humans and animals.
    Type: Grant
    Filed: September 20, 2013
    Date of Patent: February 2, 2016
    Inventor: Hubert Maehr
  • Patent number: 9221782
    Abstract: There is provided a compound which is (a) a pyrimidine sulfonamide of formula (I) or (b) a pharmaceutically acceptable salt thereof, crystalline forms of the compound, processes for obtaining the compound, pharmaceutical intermediates used in the manufacture of the compound, and pharmaceutical compositions containing the compound. The compound is useful in the treatment of a disease/condition in which modulation of chemokine receptor activity is beneficial.
    Type: Grant
    Filed: April 15, 2014
    Date of Patent: December 29, 2015
    Assignee: AstraZeneca AB
    Inventors: Stephen Connolly, Mark Richard Ebden, Iain Alastair Stewart Walters, Thomas Langer, Alan Robert Steven, Craig Robert Stewart, Paula Margaret Tomlin, Andrew John Williams
  • Patent number: 9204653
    Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.
    Type: Grant
    Filed: September 19, 2013
    Date of Patent: December 8, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Timothy Boebel, Kristy Bryan, Carla J. R. Klittich, Beth Lorsbach, Timothy P. Martin, Mark A. Pobanz, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, W. John Owen
  • Patent number: 9199946
    Abstract: The present invention provides compounds of Formula (I), as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.
    Type: Grant
    Filed: March 29, 2013
    Date of Patent: December 1, 2015
    Assignee: Bristol-Myers Squibb Company
    Inventors: Jennifer X. Qiao, Carol Hui Hu, Tammy C. Wang, Ji Jiang
  • Patent number: 9174970
    Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.
    Type: Grant
    Filed: January 22, 2009
    Date of Patent: November 3, 2015
    Assignee: Dow AgroSciences LLC
    Inventors: Zoltan L. Benko, Timothy Boebel, Nneka T. Breaux, Kristy Bryan, George E. Davis, Jeffrey B. Epp, Beth Lorsbach, Timothy P. Martin, Kevin G. Meyer, Bassam S. Nader, W. John Owen, Mark A. Pobanz, James M. Ruiz, Frisby D. Smith, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, David H. Young
  • Patent number: 9174968
    Abstract: The present invention relates to novel compounds that inhibit Lp-PLA2 activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases associated with the activity of Lp-PLA2, for example atherosclerosis, Alzheimer's disease, and/or diabetic macular edema.
    Type: Grant
    Filed: December 15, 2014
    Date of Patent: November 3, 2015
    Assignee: Glaxo Group Limited
    Inventors: Yun Jin, Zehong Wan, Qing Zhang
  • Patent number: RE47388
    Abstract: The present invention provides an agent for alleviating side effects caused by use of an anti-tumor agent, which contains 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H-pyrimidi nedione (1) represented by formula (1): or a pharmaceutically acceptable salt thereof. The 5-chloro-6-(2-iminopyrrolidin-1-yl)methyl-2,4(1H,3H)-pyrimidinedione or a pharmaceutically acceptable salt thereof exhibit an inflammatory-suppressing action in the digestive tract and advantageously alleviate diarrhea and loss of body weight concomitant with administration of a chemical for treating cancer without suppressing the anti-tumor effect. Thus, the compounds of the present invention are of great value as agents for alleviating side effects caused by use of an anti-tumor agent, which enable not only the chemotherapy to be continuedly carried out, but also the body exhaustion to be effectively prevented.
    Type: Grant
    Filed: August 23, 2017
    Date of Patent: May 14, 2019
    Assignee: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Masakazu Fukushima, Noriyuki Yamamoto, Norihiko Suzuki