Pyrimidines (including Hydrogenated) (e.g., Cytosine, Etc.) Patents (Class 514/49)
  • Patent number: 10683320
    Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.
    Type: Grant
    Filed: November 28, 2018
    Date of Patent: June 16, 2020
    Assignee: Janssen BioPharma, Inc.
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
  • Patent number: 10662213
    Abstract: This invention relates to a prodrug of the monophosphate nucleotide of the well-known oncology drug gemcitabine. Specifically, it relates to gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate when present as a single phosphate diastereoisomer and, in particular, it relates to the (S)-phosphate diastereoisomer which offers a remarkable and unexpected increase in solubility relative to the (R)-diastereoisomer. The (S)-phosphate epimer is also preferentially taken up into cyclodextrin solutions over the (R)-diastereoisomer.
    Type: Grant
    Filed: June 25, 2015
    Date of Patent: May 26, 2020
    Assignee: NuCana plc
    Inventors: Hugh Griffith, Christopher McGuigan, Magdalena Slusarczyk, Michaela Serpi, Valentina Ferrari
  • Patent number: 10660912
    Abstract: Disclosed is a combination of gemcitabine-[phenyl-benzoxy-L-alaninyl)]-phosphate (chemical name: 2?-Deoxy-2?,2?-difluoro-D-cytidine-5?-O-[phenyl (benzoxy-L-alaninyl)]phosphate) (NUC-1031) and a platinum-based anticancer agent selected from carboplatin, dicycloplatin, oxaliplatin, satraplatin and nedaplatin. The combinations are useful in the treatment of cancer and particularly ovarian cancer.
    Type: Grant
    Filed: October 5, 2015
    Date of Patent: May 26, 2020
    Assignee: NuCana plc
    Inventor: Hugh Griffith
  • Patent number: 10618927
    Abstract: The invention relates to compounds and compositions for modulation of nicotinamide adenine dinucleotide (NAD+). The invention also relates to methods of making such compounds and compositions. The invention relates to pharmaceutical compositions containing one or more NAD+ modulating compounds as a first ingredient in combination with one or more active pharmaceutical ingredients. Further, the invention relates to methods of using such compounds or compositions to promote the increase of intracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for treating diseases and/or improving cell and tissue survival.
    Type: Grant
    Filed: March 22, 2019
    Date of Patent: April 14, 2020
    Assignee: Metro International Biotech, LLC
    Inventors: Bruce Szczepankiewicz, James M. McKearin
  • Patent number: 10517884
    Abstract: Embodiments of compositions and methods for the treatment of blood disorders and malignancies in a subject are described herein. In one embodiment, a composition for the treatment of a blood disorder or a malignancy in a subject comprises decitabine, tetrahydrouridine, and an excipient. In another embodiment, a method for the treatment of a blood disorder or a malignancy in a subject comprises the oral administration of a composition comprising decitabine and tetrahydrouridine. In some examples, the composition may be administered 1-3 times weekly.
    Type: Grant
    Filed: January 19, 2018
    Date of Patent: December 31, 2019
    Assignee: BOARD OF TRUSTEES OF THE UNIVERSITY OF ILLINOIS
    Inventors: Joseph Desimone, Yogen Saunthararajah
  • Patent number: 10500224
    Abstract: The present invention provides mutual prodrugs comprising anti-cancer nucleosides and short chain fatty acids; methods for production of the mutual prodrugs; methods of treatment comprising administration of the mutual prodrugs; and pharmaceutical compositions comprising the mutual prodrugs. Further, the mutual prodrugs of the present invention can be used as therapeutic agents for the treatment of cancer diseases and conditions.
    Type: Grant
    Filed: November 14, 2014
    Date of Patent: December 10, 2019
    Assignee: KAINOS MEDICINE, INC.
    Inventors: Sunmi Shin, Hyangmi Kim, Su-Sung Oh
  • Patent number: 10485814
    Abstract: Provided herein are stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride, and pharmaceutical compositions and uses thereof. The stereoisomerically pure ester and carbonate analogues of nicotinamide riboside and nicotinamide riboside hydride may be used to treat a disease or disorder that would benefit from increased NAD levels including a mitochondrial disease or disorder, insulin resistance, a metabolic syndrome, diabetes, obesity, for increasing insulin sensitivity in a subject, or to treat or prevent a skin condition. The compounds have general formulas (I) or (II): wherein R1 is —C(?O)—X—(C2-C18 straight chain or branched) alkyl or —C(?O)—X—(C2-C18 straight chain or branched) alkenyl; each R2 is independently selected from hydrogen, and a —C(O)—X—(C1-C18 straight chain or branched) alkyl or a —C(O)—X—(C2-C18 straight chain or branched) alkenyl; and X is a covalent bond or O.
    Type: Grant
    Filed: June 5, 2015
    Date of Patent: November 26, 2019
    Assignee: GlaxoSmithKline Intellectual Property (No. 2) Limited
    Inventors: Bruce G. Szczepankiewicz, Frank Preugschat, Karsten Koppetsch, Robert B. Perni
  • Patent number: 10479820
    Abstract: Rediced genome or native K12 strain E. coli bacteria comprising expression vectors encoding a recombinant CRM197 protein and their use in the production of CRM 197 is provided. The CRM 197 protein may be fused to a signal sequence that directs the expressed CRM197 protein to the periplasm of the E. coli host.
    Type: Grant
    Filed: March 2, 2015
    Date of Patent: November 19, 2019
    Assignee: SCARAB GENOMICS, LLC
    Inventors: Cristopher R. Blattner, David Frisch, Robert E. Novy, Terrance M. Henker, Eric A. Steffen, Frederick R. Blattner, Hyunsic Choi, Gyorgy Posfai, Charles F. Landry
  • Patent number: 10463684
    Abstract: Disclosed herein are derivatives of nucleobase analogs. The disclosed compounds have a nucleobase moiety and an omega-3 polyunsaturated fatty acid moiety, including pharmaceutically acceptable salt or prodrug thereof. Methods of using these compounds for the treatment of cancers such as pancreatic cancer are also disclosed.
    Type: Grant
    Filed: January 29, 2015
    Date of Patent: November 5, 2019
    Assignee: BOARD OF REGENTS, THE UNEVERSETY OF TEXAS SYSTEM
    Inventors: Zhengrong Cui, Dharmika S. P. Lansakara-P.
  • Patent number: 10450325
    Abstract: This invention relates to processes for preparing a JAK1 inhibitor having Formula Ia: as well as new forms of the inhibitor.
    Type: Grant
    Filed: September 22, 2017
    Date of Patent: October 22, 2019
    Assignee: Incyte Corporation
    Inventors: Jiacheng Zhou, Zhongjiang Jia
  • Patent number: 10434094
    Abstract: A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.
    Type: Grant
    Filed: May 31, 2016
    Date of Patent: October 8, 2019
    Assignee: Array BioPharma Inc.
    Inventors: Kurtis D. Davies, Stefan Gross
  • Patent number: 10363265
    Abstract: A method and composition for treating a host infected with hepatitis C comprising administering an effective hepatitis C treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.
    Type: Grant
    Filed: December 28, 2012
    Date of Patent: July 30, 2019
    Assignees: Idenix Pharmaceuticals LLC, Universita Degli Studi di Cagliari
    Inventors: Jean-Pierre Sommadossi, Paolo La Colla
  • Patent number: 10342790
    Abstract: The present invention relates to the use of ceranib-2 molecule in the treatment of lung cancer and breast cancer. At the same time, the present invention also describes the in vitro studies made by the inventors in this direction.
    Type: Grant
    Filed: February 20, 2018
    Date of Patent: July 9, 2019
    Assignee: ANADOLU UNIVERSITESI REKTORLUGU
    Inventors: Hatice Mehtap Kutlu, Gokhan Kus
  • Patent number: 10309957
    Abstract: To provide a marker for determining sensitivity to an anti-cancer agent, which can determine whether or not a patient has a therapeutic response to the anti-cancer agent, and cancer therapeutic means employing the marker.
    Type: Grant
    Filed: September 19, 2017
    Date of Patent: June 4, 2019
    Assignees: KEIO UNIVERSITY, KABUSHIKI KAISHA YAKULT HONSHA
    Inventors: Yusuke Tanigawara, Akito Nishimuta, Yuki Otani, Mitsuhisa Matsuo
  • Patent number: 10287311
    Abstract: The disclosed invention provides compositions and methods of treating a Flaviviridae infection, including hepatitis C virus, West Nile Virus, yellow fever virus, and a rhinovirus infection in a host, including animals, and especially humans, using a (2?R)-2?-deoxy-2?-fluoro-2?-C-methyl nucleosides, or a pharmaceutically acceptable salt or prodrug thereof.
    Type: Grant
    Filed: September 12, 2007
    Date of Patent: May 14, 2019
    Assignee: GILEAD PHARMASSET LLC
    Inventor: Jeremy Clark
  • Patent number: 10053483
    Abstract: Provided in the present invention are novel key intermediates of selamectin and the preparation method thereof. Also provided is a new synthesis process, using doramectin as a starting material, and obtaining selamectin via hydrogenation, oxidation, oximation and desugaring. The new process of the present invention has few steps, and is simple to operate, high in yield, low in cost and causes little pollution, and is more suitable for large scale industrial production.
    Type: Grant
    Filed: April 2, 2013
    Date of Patent: August 21, 2018
    Assignee: Zhejiang Hisun Pharmaceutical Co., Ltd.
    Inventors: Mingxing Yin, Jianchao Wu, Jian Chai
  • Patent number: 10016447
    Abstract: This present invention relates to pharmaceutical compositions comprising cyclophosphamide alone and/or in combination with one or more pharmaceutical active ingredients and one or more pharmaceutically acceptable excipients wherein the cyclophosphamide has D90 particle size less than 100 microns.
    Type: Grant
    Filed: September 25, 2015
    Date of Patent: July 10, 2018
    Assignee: Intas Pharmaceuticals Ltd.
    Inventors: Priyank Patel, Mayur Patel, Mahendra Patel, Balvir Singh, Ashish Sehgal
  • Patent number: 9968627
    Abstract: Provided herein are solid forms comprising (a) 4-amino-1-?-D-ribofuranosyl-1,3,5-triazin-2(1H)-one and (b) a coformer. Pharmaceutical compositions comprising the solid forms (e.g., cocrystals) and methods for treating, preventing and managing various disorders are also disclosed.
    Type: Grant
    Filed: March 25, 2014
    Date of Patent: May 15, 2018
    Assignee: Celgene Corporation
    Inventors: G. Patrick Stahly, David Jonaitis, Ho-Wah Hui, Kevin J. Klopfer
  • Patent number: 9943513
    Abstract: Described herein are oral abuse deterrent pharmaceutical compositions, methods for making the same, and methods for treating pain by administering the pharmaceutical composition to a subject in need thereof. In particular, an oral abuse deterrent pharmaceutical composition comprising a soft capsule and a controlled release matrix comprising oxycodone are described.
    Type: Grant
    Filed: October 5, 2016
    Date of Patent: April 17, 2018
    Assignee: BANNER LIFE SCIENCES LLC
    Inventors: Justin Hughey, Saujanya Gosangari, Chue Hue Yang
  • Patent number: 9895442
    Abstract: The present disclosure relates to the compound of Formula I: Also disclosed are pharmaceutical compositions comprising the compound of Formula I, methods of using the compound of Formula I and/or compositions comprising the compound of Formula I for the treatment of HCV.
    Type: Grant
    Filed: May 15, 2014
    Date of Patent: February 20, 2018
    Assignee: Riboscience LLC
    Inventors: Mark Smith, Klaus G. Klumpp
  • Patent number: 9872873
    Abstract: The present invention relates to a process of preparing a stable pharmaceutical composition of compounds which are susceptible to hydrolysis comprising a. Addition of required quantity of pharmaceutically acceptable lyophilization excipients optionally in Water for Injection in a formulation vessel; b. Addition of organic solvent to form a appropriate proportion of aqueous and organic solvent; c. Maintaining the temperature of the formulation vessel from the range ?5±1° C. to ?5±3° C.; d. Addition of required quantity of compound susceptible to hydrolysis to form a solution and lyophilizing the solution.
    Type: Grant
    Filed: March 29, 2012
    Date of Patent: January 23, 2018
    Assignee: Fresenius Kabi Oncology Limited
    Inventors: Dhiraj Khattar, Rajesh Khanna, Sanjay Motwani, Minakshi Garg, Vikas Chandel, Mukti Yadav, Vijay Kumar Kyama, Vikas Bhandari
  • Patent number: 9862741
    Abstract: The present disclosure provides cytidine derivative dimers, salts and compositions of the cytidine derivative dimers, and methods of making and using the cytidine derivative dimers. The compounds that useful for treating a neoplasm in mammalian subjects. The cytidine derivative dimer has the following general formula (I): where R1 is C1-C10 alkyl, C1-C10 substituted alkyl, —(CH2)n-Ph, or substituted —(CH2)n-Ph; R2 is C1-C10 alkyl, C1-C10 substituted alkyl, —(CH2)n-Ph, or substituted —(CH2)n-Ph; R3 is hydrogen, alkoxycarbonyl or substituted alkoxycarbonyl; R4 is hydrogen, alkoxycarbonyl or substituted alkoxycarbonyl; and R5 is —(CH2)n—, substituted —(CH2)n—, or —(CH2)n—X1—X2—, X1 being O or S, and X2 being —(CH2)n-Ph, pyrimidyl, pyranyl, imidazolyl, pyrazinyl, or pyridyl. The disclosed cytidine derivative dimers/salts provide high anti-tumor activity with low toxicity and are useful for treating cancers.
    Type: Grant
    Filed: February 17, 2015
    Date of Patent: January 9, 2018
    Assignees: CHANGZHOU PANGYUAN PHARMACEUTICAL CO., LTD, INNER MONGOLIA PUYIN PHARMACEUTICAL CO., LTD
    Inventors: Daria Yang, Haidong Wang, Hui-Juan Wang
  • Patent number: 9861629
    Abstract: Described herein are oral abuse deterrent pharmaceutical compositions, methods for making the same, and methods for treating pain by administering the pharmaceutical composition to a subject in need thereof. In particular, an oral abuse deterrent pharmaceutical composition comprising a soft capsule and a controlled release matrix comprising oxycodone are described.
    Type: Grant
    Filed: October 5, 2016
    Date of Patent: January 9, 2018
    Assignee: Banner Life Sciences LLC
    Inventors: Justin Hughey, Saujanya Gosangari, Chue Hue Yang
  • Patent number: 9833515
    Abstract: The present disclosure provides conjugate structures (e.g., polypeptide conjugates) and hydrazinyl-indole compounds used to produce these conjugates. The disclosure also provides methods of production of such conjugates, as well as methods of using the same.
    Type: Grant
    Filed: March 1, 2016
    Date of Patent: December 5, 2017
    Assignee: Redwood Bioscience, Inc.
    Inventors: Romas Alvydas Kudirka, Aaron Edward Albers, Robyn M. Barfield, David Rabuka
  • Patent number: 9834576
    Abstract: The present invention relates to methods and intermediates for synthesizing 2?-deoxy-2?,2?-difluorotetrahydrouridine compounds.
    Type: Grant
    Filed: October 29, 2014
    Date of Patent: December 5, 2017
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Hyeong-wook Choi, Steven Mathieu, Frank Fang, Bryan Matthew Lewis
  • Patent number: 9820998
    Abstract: The present invention relates to use of bisphosphonate formulations for the treatment and management of HIV/AIDS. The method of the invention comprises administering a formulation comprising an effective amount of a bisphosphonate that specifically inhibits the activity and/or decreases the number of monocytes and/or macrophages, thereby reducing or eliminating HIV reservoirs. The invention also provides a method of complementing an HIV antiviral therapy, such as the highly active antiretroviral therapy (HAART), with a bisphosphonate formulation to improve clinical outcome.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: November 21, 2017
    Assignees: BIOREST LTD., OREGON HEALTH & SCIENCE UNIVERSITY
    Inventors: Yoram Richter, Gershon Golomb, Jonah B. Sacha
  • Patent number: 9808460
    Abstract: Disclosed herein are auris acceptable gel compositions containing a multiparticulate glutamate receptor antagonist, and methods for the treatment of otic diseases or conditions through intratympanic administration of the composition to an individual afflicted with an otic disease or condition.
    Type: Grant
    Filed: May 15, 2015
    Date of Patent: November 7, 2017
    Assignees: OTONOMY, INC., THE REGENTS OF THE UNIVERSITY OF CALIFORNIA
    Inventors: Jay Lichter, Andrew M. Trammel, Fabrice Piu, Qiang Ye, Benedikt Vollrath, Luis A. Dellamary, Carl Lebel, Jeffrey P. Harris
  • Patent number: 9802957
    Abstract: This invention relates to processes for preparing a JAK1 inhibitor having Formula Ia: as well as new forms of the inhibitor.
    Type: Grant
    Filed: April 29, 2015
    Date of Patent: October 31, 2017
    Assignee: Incyte Corporation
    Inventors: Jiacheng Zhou, Shili Chen, Yongzhong Wu, Zhongjiang Jia, Yingrui Dai
  • Patent number: 9744186
    Abstract: In accordance with the purpose(s) of the invention, as embodied and broadly described herein, the invention, in one aspect, relates to substituted gemcitabine aryl amide analogs, methods of making the same, pharmaceutical compositions comprising same, methods of treating viral disorders and disorders of uncontrolled cellular proliferation using same.
    Type: Grant
    Filed: August 8, 2016
    Date of Patent: August 29, 2017
    Assignee: NUCORION PHARMACEUTICALS, INC.
    Inventor: Zucai Suo
  • Patent number: 9655905
    Abstract: The present invention includes embodiments for treatment and/or prevention of sickle cell disease that employ Hydroxyfasudil or Isocoronarin D alone or either in conjunction with each other or an inducer of HbF production. The compounds may act synergistically, and the compounds employed circumvent the side effects seen with Hydroxyurea.
    Type: Grant
    Filed: September 13, 2012
    Date of Patent: May 23, 2017
    Assignee: KING ABDULLAH UNIVERSITY OF SCIENCE AND TECHNOLOGY
    Inventors: Magbubah Essack, Vladimir Bajic, Aleksandar Radovanovic
  • Patent number: 9616098
    Abstract: Vancomycin-containing compositions substantially free of precipitation after at least about 12 months of storage at refrigerated or ambient conditions are disclosed. The compositions include vancomycin or a pharmaceutically acceptable salt thereof; a polar solvent including propylene glycol, polyethylene glycol and mixtures thereof; lactic acid, a lactate salt, or mixtures thereof; and optionally, a pH adjuster in an amount sufficient to maintain a pH of the compositions at from about 3 to about 8.
    Type: Grant
    Filed: May 30, 2014
    Date of Patent: April 11, 2017
    Assignee: SciDose, LLC
    Inventor: Nagesh R. Palepu
  • Patent number: 9605031
    Abstract: The invention provides compositions of matter comprising a cowpea chlorotic mottle virus capsid protein (CCMV CP) and a ribonucleic acid, as well as methods for using such compositions. In such compositions, the cowpea chlorotic mottle virus capsid protein envelops the ribonucleic acid so as to for a capsid that can inhibit the degradation of the ribonucleic acid (e.g. by RNAses). A method of delivering a ribonucleic acid into the cytoplasm of a mammalian cell is also provided. Typically, the method comprises the steps of combining the mammalian cell with a composition of matter described herein under conditions selected to allow the cowpea chlorotic mottle virus capsid to contact the mammalian cell and deliver the ribonucleic acid into the cytoplasm of a mammalian cell.
    Type: Grant
    Filed: November 13, 2014
    Date of Patent: March 28, 2017
    Assignee: The Regents of the University of California
    Inventors: William M. Gelbart, Charles M. Knobler, Rees F. Garmann, Odisse Azizgolshani, Ruben D. Cadena-Nava
  • Patent number: 9597344
    Abstract: Provided is a liposome comprising a lipid bilayer and a sonosensitizer that is disposed in and/or on the lipid bilayer, wherein the sonosensitizer self-assembles to form aggregates when exposed to ultrasound; and a method of efficiently delivering an active agent to a target site in the body of a subject using the sonosensitive liposome.
    Type: Grant
    Filed: August 19, 2015
    Date of Patent: March 21, 2017
    Assignee: SAMSUNG ELECTRONICS CO., LTD.
    Inventors: Sun Min Park, Jungyong Nam, Kitae Park, Hyun Ryoung Kim, Eun Sung Park
  • Patent number: 9573971
    Abstract: The invention is directed to processes for synthesizing bicyclic nucleoside antiviral compounds and for synthesizing the intermediates used in the process. The invention is also directed to novel intermediate compounds useful in the process. The antiviral compounds are useful in the treatment of herpes zoster (i.e., varicella zoster virus, VZV, shingles) and for the prevention of post herpetic neuralgia (PHN) resulting from this viral infection.
    Type: Grant
    Filed: January 8, 2016
    Date of Patent: February 21, 2017
    Assignee: ContraVir Pharmaceuticals, Inc.
    Inventors: Yanling Wang, Yuan Wang, Xungui He, Chuanjun Liu, Jirang Zhu, Jie Li, Qingzhong Cheng, Mingyong Yuan
  • Patent number: 9567363
    Abstract: The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.
    Type: Grant
    Filed: December 29, 2014
    Date of Patent: February 14, 2017
    Assignee: OTSUKA PHARMACEUTICAL CO., LTD.
    Inventors: Gregory S. Hamilton, Takashi Tsukamoto, Dana V. Ferraris, Bridget Duvall, Rena Lapidus
  • Patent number: 9480752
    Abstract: The present invention refers to a conjugate comprising at least one polyunsaturated fatty acid residue, particularly an arachidonic acid residue, more particularly an anandamide (arachidonoyl ethanol amide) residue and covalently bound thereto at least one nucleosidic component selected from nucleic acids, nucleosides and nucleotides. This conjugate is suitable for the transfection of cells such as mammalian cells including human cells with high efficacy. Thus, a new delivery vehicle for therapeutic molecules including antisense molecules, siRNA molecules, miRNA molecules, antagomirs or precursors of such molecules, as well as the therapeutic nucleosides or nucleotides, is provided.
    Type: Grant
    Filed: July 10, 2013
    Date of Patent: November 1, 2016
    Assignee: Baseclick GmbH
    Inventor: Thomas Carell
  • Patent number: 9476099
    Abstract: The present invention is a gene expression panel of chemotherapeutic drug-resistant cancer stem cells comprising RIN1, SOX15 and TLR4. In one embodiment the cancer stem cells are testicular cancer germ cells. The present invention provides for a kit and method for determining response to treatment with decitabine at low doses.
    Type: Grant
    Filed: July 31, 2013
    Date of Patent: October 25, 2016
    Assignee: Trustees of Dartmouth College
    Inventors: Michael Spinella, Maroun J. Beyrouthy
  • Patent number: 9457089
    Abstract: In an aqueous solution, a composition includes at least one protein, including at least one antibody fragment, and at least one water-soluble viscosity-reducing agent chosen from the group consisting of cytidine, 2?-deoxycytidine, uridine, 2?-deoxyuridine, thymidine and ribothymidine, alone or as a mixture. The protein includes at least one antibody fragment being at a concentration greater than or equal to 50 mg/ml.
    Type: Grant
    Filed: September 10, 2013
    Date of Patent: October 4, 2016
    Assignee: ADOCIA
    Inventor: Olivier Soula
  • Patent number: 9370567
    Abstract: A combination of a CHK1 inhibitor and a WEE1 inhibitor are provided.
    Type: Grant
    Filed: November 16, 2011
    Date of Patent: June 21, 2016
    Assignee: ARRAY BIOPHARMA INC.
    Inventors: Kurtis D. Davies, Stefan Gross
  • Patent number: 9359451
    Abstract: Disclosed are methods and materials for treating or preventing complications due to traumatic injuries using estrogen or derivatives thereof.
    Type: Grant
    Filed: March 15, 2013
    Date of Patent: June 7, 2016
    Assignee: THE UAB RESEARCH FOUNDATION
    Inventors: Irshad H. Chaudry, William J. Hubbard, Zheng Feng Ba
  • Patent number: 9351989
    Abstract: This invention is directed to phosphoroamidate and phosphorodiamidate derivatives including the compounds of formula (I) having the structure wherein U, V, W, Z, R1, X1, X2, and Y are defined herein. These compounds and pharmaceutical compositions containing these compounds are useful in the treatment of viral infections in mammals infected by a virus in the Flaviviridae family of viruses, in particular hepatitis C virus (HCV). The compounds of this invention may be prepared by various methods known in the art of organic chemistry in general and nucleoside and nucleotide analog synthesis in particular.
    Type: Grant
    Filed: December 29, 2011
    Date of Patent: May 31, 2016
    Assignees: INHIBITEX, INC., UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
    Inventors: Chris McGuigan, Karolina Madela, Claire Bourdin, John Vernachio, Stanley Chamberlain
  • Patent number: 9296741
    Abstract: The present invention provides for compounds of formula (I) wherein A1, A2, A3, A4, X1, X2, Y1, L1, G1, Rx, and Ry have any of the values defined thereof in the specification, and pharmaceutically acceptable salts thereof, that are useful as agents in the treatment of diseases and conditions, including inflammatory diseases, cancer, and AIDS. Also provided are pharmaceutical compositions comprising one or more compounds of formula (I).
    Type: Grant
    Filed: March 14, 2013
    Date of Patent: March 29, 2016
    Assignee: AbbVie Inc.
    Inventors: Le Wang, John K Pratt, Keith F McDaniel, Yujia Dai, Steven D Fidanze, Lisa Hasvold, James H Holms, Warren M Kati, Dachun Liu, Robert A Mantei, William J McClellan, George S Sheppard, Carol K Wada
  • Patent number: 9265785
    Abstract: Embodiments of compositions and methods for the treatment of blood disorders and malignancies in a subject are described herein. In one embodiment, a composition for the treatment of a blood disorder or a malignancy in a subject comprises decitabine, tetrahydrouridine, and an excipient. In another embodiment, a method for the treatment of a blood disorder or a malignancy in a subject comprises the oral administration of a composition comprising decitabine and tetrahydrouridine. In some examples, the composition may be administered 1-3 times weekly.
    Type: Grant
    Filed: March 7, 2012
    Date of Patent: February 23, 2016
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Joseph Desimone, Yogen Saunthararajah
  • Patent number: 9259469
    Abstract: Compositions comprising decitabine and tetrahydrouridine for the treatment of blood disorders and hematological and solid malignancies are described.
    Type: Grant
    Filed: December 21, 2009
    Date of Patent: February 16, 2016
    Assignee: The Board of Trustees of the University of Illinois
    Inventors: Joseph Desimone, Yogen Saunthararajah
  • Patent number: 9145444
    Abstract: The invention relates to compounds and methods useful in detection and therapy of HPV-associated diseases. The invention is based on the elucidation of a mechanism by which replication of HPVs occurs in naturally infected tissues and cells. Moreover it is based on the identification of distinct epigenetic changes of the viral genome in infected cells that allows promotion of the affected cells to precancerous and cancerous cells. The invention therefore provides methods of diagnosing neoplasias and their precursor lesions as well as methods of preventing the development of malignancies or inhibiting tumor growth.
    Type: Grant
    Filed: October 31, 2008
    Date of Patent: September 29, 2015
    Assignee: Ruprecht-Karls-Universität Heidelberg
    Inventors: Magnus Von Knebel Doeberitz, Svetlana Vinokurova
  • Patent number: 9133232
    Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.
    Type: Grant
    Filed: December 16, 2013
    Date of Patent: September 15, 2015
    Assignee: University of North Carolina at Wilmington
    Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
  • Patent number: 9125884
    Abstract: Provided herein are methods for treating subjects having a cancer, such as a relapsed or refractory solid tumor, wherein the method comprises administering to the subject a cytidine analog. In certain of the methods, the cytidine analog is administered alone or in combination with one or more anti-cancer agents. Also provided are methods for using a cytidine analog, to treat diseases and disorders including disorders related to abnormal cell proliferation, hematologic disorders, and immune disorders, among others. In certain of the methods, the cytidine analog is formulated in an oral dosage form and administered orally.
    Type: Grant
    Filed: October 31, 2012
    Date of Patent: September 8, 2015
    Assignee: Celgene Corporation
    Inventors: Kyle J. MacBeth, Aaron N. Nguyen, Jorge DiMartino
  • Patent number: 9126971
    Abstract: The present invention relates to novel compounds according to the general formulas I, II, III, IV or V: wherein B is nucleoside base according to the structure: and the remaining variables as defined in the specification, and pharmaceutical compositions comprising the compounds. The compounds are useful interalia as anti-viral agents in viral therapy.
    Type: Grant
    Filed: May 7, 2012
    Date of Patent: September 8, 2015
    Assignee: YALE UNIVERSITY
    Inventors: Yung-chi Cheng, Hiromichi Tanaka, Masanori Baba
  • Patent number: 9102714
    Abstract: A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: August 11, 2015
    Assignee: Lipoxen Technologies Limited
    Inventors: Dale Howard Hreczuk-Hirst, Sanjay Jain, Peter Laing, Gregory Gregoriadis, Ioannis Papaioannou
  • Patent number: 9078901
    Abstract: Acyclic nucleoside analogs such as acyclovir, ganciclovir, penciclovir and the corresponding pro-drugs, i.e., valacyclovir, valganciclovir and famciclovir, respectively have been identified as inhibitors or antagonists of both telomerase (encoded by TERT) and reverse transcriptase encoded by L-1 (LINE-1) RT, and as useful for treating or preventing cancers induced or mediated by the two enzymes. Method of treating or preventing such cancers in patients involves administration of a therapeutically effective amount of a composition having an inhibitor or antagonist of the reverse transcriptases in cells of the patients. The inhibitor or antagonist blocks lengthening of telomeres in telomerase positive and telomerase negative cells. Methods and kits for detecting pathologically proliferating cells expressing TERT and L1RT are also disclosed.
    Type: Grant
    Filed: December 12, 2013
    Date of Patent: July 14, 2015
    Assignee: ALT Solutions Inc.
    Inventor: Igor E. Bondarev