Polycyclo Ring System Having The Diazine Ring As One Of The Cyclos Patents (Class 544/244)
  • Patent number: 10561614
    Abstract: The present invention relates to a granular composition comprising essentially Tenofovir, wherein the composition is devoid of an excipient. Tenofovir granules of the present invention are prepared in twin-screw processor such that the content of total impurities in the prepared granules is less than 2.0%.
    Type: Grant
    Filed: January 26, 2018
    Date of Patent: February 18, 2020
    Assignee: STEERLIFE INDIA PRIVATE LIMITED
    Inventors: Indu Bhushan, Vinay Rao, Radhika Ghike
  • Patent number: 9775842
    Abstract: The compositions and methods of the invention provide compositions and methods for preferential targeting of tissues to delivery therapeutic or diagnostic agents. For example, such compounds are useful in the treatment of joint disorders those affecting articulating joints, e.g., injury-induced osteoarthritis as well as autoimmune diseases affecting joint tissue such as rheumatoid arthritis.
    Type: Grant
    Filed: March 16, 2015
    Date of Patent: October 3, 2017
    Assignee: Rhode Island Hospital
    Inventors: Qian Chen, Yupeng Chen, Hongchuan Yu, Michael G. Ehrlich
  • Patent number: 9487546
    Abstract: The present invention relates to solid forms of tenofovir and methods for preparation, use and isolation of such forms.
    Type: Grant
    Filed: January 9, 2015
    Date of Patent: November 8, 2016
    Assignee: GILEAD SCIENCES, INC.
    Inventors: Paul Bernard Hurley, Olga Viktorovna Lapina, Bing Shi, Fang Wang, Zhi Xian Wang, Jacqueline Ching-See Woo
  • Patent number: 9370587
    Abstract: The present invention relates to a substance selected from the group consisting of riboflavin, its esters, salts and hydrates thereof, for use in an ophthalmic diagnostic method. In preferred aspects of the invention, the riboflavin is applied into the eye as part of a solution having a concentration from about 0.01 and 0.5% riboflavin or acceptable salt, ester, hydrate thereof.
    Type: Grant
    Filed: September 3, 2014
    Date of Patent: June 21, 2016
    Assignees: IROS R.C. S.R.L
    Inventors: Ciro Caruso, Salvatore Troisi
  • Patent number: 9187508
    Abstract: The present invention relates to a crystalline form of tenofovir dipivoxil fumarate, a crystalline composition and a pharmaceutical composition comprising the crystalline form, and also to a process for preparing the same and the use for prophylaxis or treatment of a disease associated with a viral infection. The crystalline form has an X-ray powder diffraction pattern using Cu-K? radiation, expressed in terms of lattice spacing “d” comprising peaks at about 18.4714 ?, 5.0350 ?, 4.6380 ?, 4.5347 ?, 4.3838 ?, 4.2874 ? and 3.6304 ?.
    Type: Grant
    Filed: August 1, 2011
    Date of Patent: November 17, 2015
    Assignee: Jiangsu Chiatai Tianqing Pharmaceutical Co., LTD.
    Inventors: Aiming Zhang, Qide Li, Chunguang Xia, Xiquan Zhang
  • Patent number: 9029534
    Abstract: Methods for isolating 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.
    Type: Grant
    Filed: January 14, 2014
    Date of Patent: May 12, 2015
    Assignee: Gilead Sciences, Inc.
    Inventors: Denise A. Colby, Andrew Anthony Martins, Benjamin James Roberts, Robert William Scott, Nicole S. White
  • Publication number: 20150119352
    Abstract: The invention provides a dinucleoside polyphosphate analogue, or a pharmaceutically acceptable salt thereof, for use in the inhibition (or down-regulation) of a pain, via a transducing ATP-gated P2X3 receptor, often by means of high-affinity desensitisation (HAD) mechanism.
    Type: Application
    Filed: May 24, 2013
    Publication date: April 30, 2015
    Applicant: GlobalAcornLtd.
    Inventors: Andrew David Miller, Natalya Lozovaya, Nail Burnashev, Rashid Giniatullin
  • Patent number: 9006218
    Abstract: The present invention relates to compounds and methods for treating viral diseases. Some compounds of the invention are described by Formula I: (I), wherein M+ is Na+, Li+, K+, Ca2+, Mg2+, or NRcRdReRf+ and Rc, Rd, Re and Rf are each independently hydrogen or C1-5 alkyl, or a stereoisomer, a diastereomer, an enantiomer or racemate thereof.
    Type: Grant
    Filed: February 14, 2011
    Date of Patent: April 14, 2015
    Assignee: Chimerix Inc.
    Inventors: Merrick Almond, Bernhard Lampert, Ernest Randall Lanier, Roy W. Ware
  • Publication number: 20150099722
    Abstract: The invention relates to compounds which are useful as inhibitors of 6-oxopurine phosphoribosyltransferases such as hypoxanthine-guanine-(xanthine) phosphoribosyltransferase (HG(X)PRT).
    Type: Application
    Filed: May 7, 2013
    Publication date: April 9, 2015
    Inventors: John De Jersey, Luke William Guddat, Dana Hockova, Dianne Therese Keough
  • Publication number: 20150051174
    Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
    Type: Application
    Filed: October 29, 2014
    Publication date: February 19, 2015
    Inventors: Karl Y. Hostetler, James R. Beadle
  • Publication number: 20150045324
    Abstract: The present invention relates to a novel fused pyrimidine derivative having an inhibitory activity for tyrosine kinases, and a pharmaceutical composition for preventing or treating cancers, tumors, inflammatory diseases, autoimmune diseases, or immunologically mediated diseases comprising same as an active ingredient.
    Type: Application
    Filed: October 23, 2014
    Publication date: February 12, 2015
    Applicant: HANMI SCIENCE CO., LTD
    Inventors: Mi Young CHA, Seok Jong KANG, Mi Ra KIM, Ju Yeon LEE, Ji Young JEON, Myoung Gi JO, Eun Joo KWAK, Kwang Ok LEE, Tae Hee HA, Kwee Hyun SUH, Maeng Sup KIM
  • Publication number: 20150045323
    Abstract: Disclosed are compounds having the formula: wherein X is as defined herein, and methods of making and using the same.
    Type: Application
    Filed: September 13, 2013
    Publication date: February 12, 2015
    Inventors: Linda N. Casillas, Pamela A. Haile, Robert W. Marquis, JR., Gren Wang
  • Patent number: 8946244
    Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Hepatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses.
    Type: Grant
    Filed: November 16, 2010
    Date of Patent: February 3, 2015
    Assignee: University of Georgia Research Foundation, Inc.
    Inventors: Chung K. Chu, Jianing Wang
  • Publication number: 20150025039
    Abstract: The invention is related to phosphorus substituted compounds with antiviral activity, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: June 19, 2014
    Publication date: January 22, 2015
    Inventors: Constantine G. BOOJAMRA, Carina E. CANNIZZARO, James M. CHEN, Xiaowu CHEN, Aesop CHO, Lee S. CHONG, Maria FARDIS, Haolun JIN, Ralph HIRSCHMANN, Alan X. HUANG, Choung U. KIM, Thorsten A. KIRSCHBERG, Christopher P. LEE, William A. LEE, Richard L. MACKMAN, David Y. MARKEVITCH, David A. OARE, Vidya K. PRASAD, Hyung-Jung PYUN, Adrian S. RAY, Rosemarie O'SHEA, Sundaramoorthi SWAMINATHAN, William J. WATKINS, Jennifer R. ZHANG
  • Patent number: 8884011
    Abstract: This invention relates to a purine or pyrimidine phosphonate compound of formula (I) or pharmaceutically acceptable salt thereof; wherein B, X, and R1-R3 are as defined in classes and subclasses herein. These compounds may be used as antiviral precursors. The invention also relates to therapeutic compositions of these compounds and their use for the preparation of a medication for testing and/or preventing a viral infection in a patient. The invention also provides methods for making these compounds. In particular, the invention provides an H-phosphinate precursor intermediate of formula (II) wherein B is a purine or pyrimidine base as defined herein and R1 is selected from the group comprising a hydrogen atom, and a methyl, ethyl, hydroxymethyl, hydroxyethyl and C1-6haloalkyl group.
    Type: Grant
    Filed: November 8, 2007
    Date of Patent: November 11, 2014
    Assignees: Centre National de la Recherche Scientifique-CNRS, Universite d'Aix-Marseille, K.U. Leuven Research & Development
    Inventors: Bruno Canard, Karine Alvarez, Karine Barral, Jean-Louis Romette, Johan Neyts, Jan Balzarini
  • Publication number: 20140323441
    Abstract: The present invention relates to purine derivatives of formula (I), processes for their preparation, pharmaceutical compositions, and their use in treating viral infections.
    Type: Application
    Filed: November 8, 2012
    Publication date: October 30, 2014
    Inventors: Jean-François Bonfanti, Frédéric Marc Maurice Doublet, Werner Embrechts, Jérôme Michel Claude Fortin, David Craig Mc Gowan, Philippe Muller, Piere Jean-Marie Bernand Raboisson
  • Publication number: 20140323726
    Abstract: Provided herein are synthetic methods for preparing a compound of formula (I): Also provided herein are synthetic methods for preparing a compound of formula (XIII): The disclosure also provides useful intermediates, derivatives, prodrugs, and pharmaceutically acceptable salts, solvates and hydrates of the formula (I) and formula (XIII) compounds. These compounds are useful for treating diseases associated with molybdenum cofactor deficiency.
    Type: Application
    Filed: February 17, 2012
    Publication date: October 30, 2014
    Applicant: ALEXION PHARMA INTERNATIONAL SÀRL
    Inventors: Xiangtian Long, Danmei Dai, Andreas Brunner, Derek Kevin Watt, Keith Clinch, Sylvia Myrna Baars, Rachel Anne Dixon, Gillian Mary Little, Cyrille Abel Sébastien Landreau, Nicolas Georges Rene Proisy
  • Patent number: 8871520
    Abstract: The invention provides a method of detecting uracil. The method comprises reacting uracil with a compound represented by the formula (I) in the presence of an oxidant and a base to produce a fluorescent compound represented by the formula (II).
    Type: Grant
    Filed: March 1, 2011
    Date of Patent: October 28, 2014
    Assignee: Nagasaki University
    Inventors: Masaaki Kai, Takayuki Shibata
  • Publication number: 20140303368
    Abstract: The present invention provides a process for preparation of tenofovir by dealkylation of its phosphonate ester using Ionic complexes. The present invention also provides a process for preparation of tenofovir disoproxil or a salt thereof using the tenofovir of the present invention.
    Type: Application
    Filed: November 15, 2012
    Publication date: October 9, 2014
    Applicant: Laurus Labs Private Limited
    Inventors: Venkata Sunil Kumar Indukuri, Sree Rambabu Joga, Seeta Ramanjaneyulu Gorantla, Satyanarayana Chava
  • Publication number: 20140302120
    Abstract: The invention provides TLR agonists and conjugates thereof useful in vaccines and to prevent, inhibit or treat a variety of disorders including pathogen infection and asthma.
    Type: Application
    Filed: June 19, 2014
    Publication date: October 9, 2014
    Inventors: Dennis A. Carson, Howard B. Cottam, Wolfgang Wrasidlo, Christina C.N. Wu, Gregory A. Daniels
  • Publication number: 20140303367
    Abstract: Provided herein are synthetic methods for preparing a compound of formula (I): Also provided herein are synthetic methods for preparing a compound of formula (XIII): The disclosure also provides useful intermediates, derivatives, prodrugs, and pharmaceutically acceptable salts, solvates and hydrates of the formula (I) and formula (XIII) compounds. These compounds are useful for treating diseases associated with molybdenum cofactor deficiency.
    Type: Application
    Filed: March 7, 2014
    Publication date: October 9, 2014
    Applicant: Alexion Pharma International Sàrl
    Inventors: Xiangtian Long, Danmei Dai, Andreas Brunner, Derek Kevin Watt, Keith Clinch, Sylvia Myrna Baars, Rachel Anne Dixon, Gillian Mary Little, Cyrille Abel Sébastien Landreau, Nicolas George Rene Proisy
  • Patent number: 8846643
    Abstract: There are provided, inter alia, acyclic nucleoside phosphonate compounds having reduced toxicity and enhanced antiviral activity, and pharmaceutically accepted salts and solvates thereof. There are also provided methods of using the disclosed compounds for inhibiting viral RNA-dependent RNA polymerase, inhibiting viral reverse transcriptase, inhibiting replication of virus, including hepatitis C virus or a human retrovirus, and treating a subject infected with a virus, including hepatitis C virus or a human retrovirus.
    Type: Grant
    Filed: October 11, 2012
    Date of Patent: September 30, 2014
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Publication number: 20140288025
    Abstract: The invention relates to fatty acid antiviral conjugates; compositions comprising an effective amount of a fatty acid antiviral conjugate; and methods for treating or preventing a viral infection comprising the administration of an effective amount of a fatty acid antiviral conjugate.
    Type: Application
    Filed: March 12, 2014
    Publication date: September 25, 2014
    Applicant: Catabasis Pharmaceuticals, Inc.
    Inventors: Jill C. MILNE, Michael R. JIROUSEK, Chi B. VU, Allison WENSLEY, Amal TING
  • Publication number: 20140274959
    Abstract: The present disclosure relates, inter alia, to compositions and methods for treating viral diseases and cancer. There are disclosed lipophilic antiviral and anticancer acyclic nucleoside phosphonate diesters, preparation thereof, and methods of using the compounds to treat viral diseases and cancer.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: The Regents of the University of California, a California corporation
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Publication number: 20140275532
    Abstract: The present disclosure relates, inter alia, to compositions and methods for treating viral diseases and cancer. There are disclosed lipophilic antiviral and anticancer acyclic nucleoside phosphonate diesters, preparation thereof, and methods of using the compounds to treat viral diseases and cancer.
    Type: Application
    Filed: March 14, 2014
    Publication date: September 18, 2014
    Applicant: The Regents of the University of California, a California Corporation
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Patent number: 8835630
    Abstract: The present disclosure relates, inter alia, to compositions and methods for treating viral diseases and cancer. There are disclosed lipophilic antiviral and anticancer acyclic nucleoside phosphonate diesters, preparation thereof, and methods of using the compounds to treat viral diseases and cancer.
    Type: Grant
    Filed: March 14, 2014
    Date of Patent: September 16, 2014
    Assignee: The Regents of the University of California, a California corporation
    Inventors: Karl Y. Hostetler, James R. Beadle, Nadejda Valiaeva
  • Patent number: 8822434
    Abstract: Phosphonate and phosphinate N-methanocarba derivatives of AMP including their prodrug analogs are described. MRS2339, a 2-chloro-AMP derivative containing a (N)-methanocarba (bicyclo[3.1.0]hexane) ring system in place of ribose, activates P2X receptors, ligand-gated ion channels. Phosphonate analogs of MRS2339 were synthesized using Michaelis-Arbuzov and Wittig reactions, based on the expectation of increased half-life in vivo due to the stability of the C—P bond. When administered to calsequestrin-overexpressing mice (a genetic model of heart failure) via a mini-osmotic pump (Alzet), some analogs significantly increased intact heart contractile function in vivo, as assessed by echocardiography-derived fractional shortening (FS) as compared to vehicle-infused mice. The range of carbocyclic nucleotide analogs for treatment of heart failure has been expanded.
    Type: Grant
    Filed: February 22, 2011
    Date of Patent: September 2, 2014
    Assignees: The University of Connecticut, The United States of America, as represented by the Secretary, Department of Health and Human Services
    Inventors: Bruce Liang, Kenneth A. Jacobson, Bhalchandra V. Joshi, Thatikonda Santhosh Kumar
  • Publication number: 20140206650
    Abstract: This disclosure describes novel compounds and pharmaceutical compositions for inhibiting the TRPA1 ion channel and/or medical conditions related to TRPA1, such as pain and respiratory conditions.
    Type: Application
    Filed: January 21, 2014
    Publication date: July 24, 2014
    Inventors: Blaise S. Lippa, Qingyi Li, Lily Cheng, Christopher M. Liu, Iwona E. Wrona, Chester A. Metcalf, III, Andrew J. Jackson
  • Publication number: 20140187773
    Abstract: A hemifumarate form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine (tenofovir alafenamide), and antiviral therapy using tenofovir alafenamide hemifumarate (e.g., anti-HIV and anti-HBV therapies).
    Type: Application
    Filed: March 5, 2014
    Publication date: July 3, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Dazhan Liu, Bing Shi, Fang Wang, Richard Hung Chiu Yu
  • Patent number: 8765722
    Abstract: Provided are compounds of Formula I: and pharmaceutically acceptable salts and esters thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.
    Type: Grant
    Filed: June 26, 2013
    Date of Patent: July 1, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Aesop Cho, Lee S. Chong, Michael O'Neil Hanrahan Clarke, Edward Doerffler, Choung U. Kim, Qi Liu, William J. Watkins, Jennifer R. Zhang
  • Patent number: 8759515
    Abstract: The present invention relates to an improved process for the preparation of Tenofovir Disoproxil and its pharmaceutically acceptable salts comprising the steps of: a) esterifying Tenofovir with chloromethyl isopropyl carbonate in presence of a base, phase transfer catalyst and optionally dehydrating agent, in a suitable solvent; b) optionally purifying Tenofovir Disoproxil; and c) converting of Tenofovir Disoproxil into its pharmaceutically acceptable salts. The present invention further relates to a process for the preparation of Tenofovir by reacting 1-(6-amino-purin-9-yl)-propan-2-ol with toluene-4-sulfonic acid diethoxy phosphoryl methyl ester in presence of a base in a non-polar solvent medium followed by hydrolysis.
    Type: Grant
    Filed: March 11, 2011
    Date of Patent: June 24, 2014
    Assignee: Mylan Laboratories Limited
    Inventors: Debashish Datta, Siva Rama Prasad Vellanki, Arabinda Sahu, Raja Babu Balusu, Mastan Rao Ravi, Hari Babu Nandipati, Shankar Rama, Lakshmana Rao Vadali, Srikanth Sarat Chandra Gorantla, Srinivasa Rao Dasari, Nagaraju Mittapelly
  • Patent number: 8754065
    Abstract: A hemifumarate form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine (tenofovir alafenamide), and antiviral therapy using tenofovir alafenamide hemifumarate (e.g., anti-HIV and anti-HBV therapies).
    Type: Grant
    Filed: August 15, 2012
    Date of Patent: June 17, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Dazhan Liu, Bing Shi, Fang Wang, Richard Hung Chiu Yu
  • Publication number: 20140162984
    Abstract: Quinazoline derivatives of formula (I): wherein A is 5-membered heteroaryl containing a nitrogen atom and one or two further nitrogen atoms; compositions containing them, processes for their preparation and their use in therapy.
    Type: Application
    Filed: August 21, 2012
    Publication date: June 12, 2014
    Applicant: ASTRAZENECA AB
    Inventors: Nicola Murdoch HERON, Andrew Austen MORTLOCK, Frederic Henri JUNG, Georges Rene PASQUET
  • Publication number: 20140154240
    Abstract: The invention provides compounds of Formula I or Formula II: or a pharmaceutically acceptable salt or ester, thereof, as described herein. The compounds and compositions thereof are useful for treating Pneumovirinae virus infections. The compounds, compositions, and methods provided are particularly useful for the treatment of Human respiratory syncytial virus infections.
    Type: Application
    Filed: May 30, 2013
    Publication date: June 5, 2014
    Inventors: Kerim Babaoglu, Constantine G. Boojamra, Eugene J. Eisenberg, Hon Chung Hui, Richard L. Mackman, Jay P. Parrish, Michael Sangi, Oliver L. Saunders, Dustin Siegel, David Sperandio, Hai Yang
  • Publication number: 20140148410
    Abstract: Disclosed are nucleopeptide compounds that include a nucleobase, and an amino acid. Certain compounds further comprise a glycoside. The compounds may self-assemble to form supramolecular hydrogels. Also, the compounds may be used as a platform to examine specific biological functions (e.g., binding to DNA and RNA) of a dynamic supramolecular system that is able to interact with both proteins and nucleic acids. Other uses include: methods of growing cells and methods of delivering a substance to a cell.
    Type: Application
    Filed: December 2, 2013
    Publication date: May 29, 2014
    Applicant: Brandeis University
    Inventor: Bing Xu
  • Publication number: 20140138659
    Abstract: The present invention provides a new compound and an organic electronic device using the same. The compound according to the present invention may serve as hole injection, hole transporting, electron injection and transporting, and light emitting materials and the like in an organic electronic device comprising an organic light emitting device, and the organic electronic device according to the present invention shows excellent properties in terms of efficiency, driving voltage and service life.
    Type: Application
    Filed: June 12, 2012
    Publication date: May 22, 2014
    Applicant: LG CHEM, LTD.
    Inventors: Changhwan Shin, Kongkyeom Kim, Dong Hoon Lee, Jungi Jang, Minseung Chun
  • Publication number: 20140128347
    Abstract: An oligonucleotide derivative comprises repeating structural units represented by the following general formula (wherein B represents adenine, guanine, cytosine, or uracil; X represents a sulfur atom or an oxygen atom; n represents an integer of 6 to 60; and B and X are independently represented in each of the repeating structural units), wherein X is a sulfur atom in at least one of the repeating structural units represented by the general formula:
    Type: Application
    Filed: June 1, 2012
    Publication date: May 8, 2014
    Inventors: Akira Matsuda, Mayumi Takahashi
  • Publication number: 20140128602
    Abstract: Methods for isolating 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)—{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.
    Type: Application
    Filed: January 14, 2014
    Publication date: May 8, 2014
    Applicant: GILEAD SCIENCES, INC.
    Inventors: Denise A. Colby, Andrew Anthony Martins, Benjamin James Roberts, Robert William Scott, Nicole S. White
  • Publication number: 20140121186
    Abstract: The present invention provides methods of treating viral infection of the eye or posterior ocular condition including administering a pharmaceutical composition comprising a compound described in the present application. In some embodiments, the pharmaceutical composition is topically administered. In another embodiment, the pharmaceutical composition is orally administered or intraocularly administered.
    Type: Application
    Filed: December 23, 2013
    Publication date: May 1, 2014
    Applicant: Chimerix, Inc.
    Inventors: George R. Painter, Merrick R. Almond
  • Patent number: 8710030
    Abstract: The present invention relates to phosphonate compounds, compositions containing them, processes for obtaining them, and their use for treating a variety of medical disorders, e.g., osteoporosis and other disorders of bone metabolism, cancer, viral infections, and the like.
    Type: Grant
    Filed: October 4, 2012
    Date of Patent: April 29, 2014
    Assignee: The Regents of the University of California
    Inventors: Karl Y. Hostetler, James R. Beadle
  • Publication number: 20140113882
    Abstract: The present application provides a compound of formula (I) or a salt thereof, wherein R7, R8, R9, G, and X are as defined herein. This application further describes compositions comprising the same. Compounds of formula (I) and their salts have aPKC inhibitory activity, and may be used to treat proliferative disorders.
    Type: Application
    Filed: September 27, 2013
    Publication date: April 24, 2014
    Applicants: Cancer Research Technology Limited, Cephalon, Inc.
    Inventors: Henry J. Breslin, Bruce D. Dorsey, Benjamin J. Dugan, Katherine M. Fowler, Robert L. Hudkins, Eugen F. Mesaros, Nathaniel J.T. Monck, Emma L. Morris, Ikeoluwa Olowoye, Gregory R. Ott, Gregoire A. Pave, Jonathan R. Roffey, Christelle N. Soudy, Ming Tao, Craig A. Zificsak, Allison L. Zulli
  • Patent number: 8697675
    Abstract: A hemifumarate form of 9-[(R)-2-[[(S)-[[(S)-1-(isopropoxycarbonyl)ethyl]amino]phenoxyphosphinyl]methoxy]propyl]adenine (tenofovir alafenamide), and antiviral therapy using tenofovir alafenamide hemifumarate (e.g., anti-HIV and anti-HBV therapies).
    Type: Grant
    Filed: August 15, 2012
    Date of Patent: April 15, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Dazhan Liu, Bing Shi, Fang Wang, Richard Hung Chiu Yu
  • Publication number: 20140100195
    Abstract: Compounds that have agonist activity at one or more of the S1P receptors are provided. The compounds are sphingosine analogs that, after phosphorylation, can behave as agonists at S1P receptors.
    Type: Application
    Filed: October 5, 2012
    Publication date: April 10, 2014
    Inventors: Richard D. Caldwell, Kevin M. GUCKIAN, Gnanasambandam KUMARA VEL, Wen-Cherng LEE, Edward Yin-Shiang LIN, Xiaogao LlU, Bin MA, Daniel M. SCOTT, Zhan SHl, Jermaine THOMAS, Arthur G. TAVERAS, Guo Zhu ZHENG
  • Patent number: 8691830
    Abstract: Compounds of formulae I, II or III, and pharmaceutically acceptable salts thereof, are useful as CDK inhibitors.
    Type: Grant
    Filed: April 24, 2013
    Date of Patent: April 8, 2014
    Assignee: G1 Therapeutics, Inc.
    Inventors: Francis X. Tavares, Jay C. Strum
  • Publication number: 20140086843
    Abstract: The present invention relates to a bifunctional hydroxy-bisphosphonic acid derivative of formula (I) below: or a pharmaceutically-acceptable salt thereof, a method for producing the same, pharmaceutical compositions containing the same, and the use thereof as a medicament, as well as a compound of formula (II) below: or a pharmaceutically-acceptable salt thereof, and the use thereof for producing a vectorized molecule of therapeutic or diagnostic purpose.
    Type: Application
    Filed: March 28, 2012
    Publication date: March 27, 2014
    Applicant: ATLANTHERA
    Inventors: Maxim Egorov, Jean-Yves Goujon, Ronan Le Bot
  • Patent number: 8674094
    Abstract: The present invention provides a new class of solids supports for synthesis of modified oligomers of nucleic acids, and nucleic acid probes that have a format expediently synthesized on the new supports. Exemplary solid supports include at least one quencher bound through a linker to the solid support. Various exemplary embodiments include a moiety that stabilizes a duplex, triplex or higher order aggregation (e.g., hybridization) of nucleic acids of which the oligomer of the invention is a component. Other components of the solid support include moieties that stabilize aggregations of nucleic acids, e.g., intercalators, minor groove binding moieties, bases modified with a stabilizing moiety (e.g., alkynyl moieties, and fluoroalkyl moieties), and conformational stabilizing moieties, such as those described in commonly owned U.S. Patent Application Publication No. 2007/0059752.
    Type: Grant
    Filed: July 28, 2011
    Date of Patent: March 18, 2014
    Assignee: Biosearch Technologies, Inc.
    Inventors: Ronald M. Cook, Matt Lyttle
  • Publication number: 20140073786
    Abstract: The present disclosure describes cyclohexenyl nucleic acid analogs, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, cyclohexenyl nucleic acid analogs are provided, having one or more chiral substituents, that are expected to be useful for enhancing properties of oligomeric compounds including nuclease resistance and binding affinity. In some embodiments, the oligomeric compounds provided herein hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.
    Type: Application
    Filed: November 1, 2013
    Publication date: March 13, 2014
    Applicant: Isis Pharmaceuticals, Inc.
    Inventors: Punit P. Seth, Eric E. Swayze
  • Publication number: 20140073606
    Abstract: The present invention relates to 2?-Fluoro-6?-methylene carbocyclic nucleosides, pharmaceutical compositions containing these nucleosides and their use in the treatment or prophylaxis of a number of viral infections and secondary disease states and conditions thereof, especially including Hepatitis B virus (HBV) and secondary disease states and conditions thereof (cirrhosis and liver cancer), Heptatitis C virus (HCV), Herpes Simplex virus I and II (HSV-1 and HSV-2), cytomegalovirus (CMV), Varicella-Zoster Virus (VZV) and Epstein Barr virus (EBV) and secondary cancers which occur thereof (lymphoma, nasopharyngeal cancer, including drug resistant (especially including lamivudine and/or adefovir resistant) and other mutant forms of these viruses, especially HBV.
    Type: Application
    Filed: November 13, 2013
    Publication date: March 13, 2014
    Inventors: Chung K. Chu, Jianing Wang
  • Publication number: 20140066406
    Abstract: The invention features compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
    Type: Application
    Filed: March 15, 2013
    Publication date: March 6, 2014
    Applicant: ARIAD PHARMACEUTICALS, INC.
    Inventor: ARIAD PHARMACEUTICALS, INC.
  • Patent number: 8664386
    Abstract: Methods for isolating 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine (compound 16): a method for preparing, in high diastereomeric purity, intermediate compounds 13 and 15: and a method for preparing intermediate compound 12: 9-{(R)-2-[((S)-{[(S)-1-(isopropoxycarbonyl)ethyl]amino}phenoxyphosphinyl)methoxy]propyl}adenine has anti-viral properties.
    Type: Grant
    Filed: October 3, 2012
    Date of Patent: March 4, 2014
    Assignee: Gilead Sciences, Inc.
    Inventors: Denise A. Colby, Andrew Anthony Martins, Benjamin James Roberts, Robert William Scott, Nicole S. White