Multideoxy Or Didehydro Patents (Class 536/28.2)
  • Patent number: 9865368
    Abstract: A computer-implemented method for determining optimized amount of radiopharmaceutical to be produced at a production facility, the radiopharmaceutical being for use in nuclear imaging at customer sites, in order to meet aggregate demands of orders placed by the customer sites (e.g. medical imaging centers, hospitals, etc.), wherein the quantity of radiopharmaceutical is sufficient to meet the aggregate demand while minimizing any overproduction of the radiopharmaceutical.
    Type: Grant
    Filed: March 10, 2017
    Date of Patent: January 9, 2018
    Assignee: Siemens Medical Solutions USA, Inc.
    Inventors: Ioannis Akrotirianakis, Amit Chakraborty, Todd Putvinski, Eric Greaser, Steven Zigler
  • Publication number: 20150140610
    Abstract: A process for making the compound of Formula I utilizes the starting compound, together with sulfilimine and sulfoxide process steps later on.
    Type: Application
    Filed: May 22, 2013
    Publication date: May 21, 2015
    Inventors: Adrian Ortiz, Tamas Benkovics, Zhongping Shi, Prashant P. Deshpande, Zhiwei Guo, David R. Kronenthal, Chris Sfouggatakis
  • Publication number: 20150104818
    Abstract: The present invention comprises novel conjugates and immunogens derived from gemcitabine and unique antibodies generated by using gemcitabine linked immunogens, which conjugates immunogens and antibodies, are useful in immunoassays for the quantification and monitoring of gemcitabine in biological fluids.
    Type: Application
    Filed: December 19, 2014
    Publication date: April 16, 2015
    Inventors: Salvatore J. Salamone, Jodi Blake Courtney, Howard Sard, Christopher Spedaliere
  • Publication number: 20150045548
    Abstract: The present invention relates to a method for labelling fluorine-18, which is a radioisotope, and more specifically, to a method for labelling a [18F]fluoride in a method for preparing an organic [18F]fluoro compound by reacting an alkyl halide or an alkyl sulfonate with a [18F]fluoride, wherein a [18F]fluoride supported on a quaternary alkyl ammonium polymer support is eluted using a solution containing a metal salt or a quaternary ammonium salt with an adjusted pH, and a base is not additionally used. The present invention enables a labeling reaction without an additional base after precisely reflecting the concentration of a base absolutely necessary for the nucleophilic substitution of a [18F]fluoride or eluting a [18F]fluoride using a [18F]fluoride eluent with an adjusted pH, thereby stably obtaining a [18F]fluoride-labelled compound in a high yield, and is thus useful for production of fluorine-18-labelled radioactive medical supplies.
    Type: Application
    Filed: December 21, 2012
    Publication date: February 12, 2015
    Inventors: Sang Ju Lee, Seung Jun Oh, Dae Hyuk Moon, Jin Sook Ryu, Jae Seung Kim, Jong Jin Lee
  • Publication number: 20150038692
    Abstract: Orthogonally protected 3?-amino nucleoside monomers and efficient methods for their synthesis are described. The methods employ selective protection of the 3?-amino group in the presence of the unprotected nucleoside base.
    Type: Application
    Filed: May 13, 2014
    Publication date: February 5, 2015
    Applicant: Geron Corporation
    Inventors: Sergei M. Gryaznov, Krisztina Pongracz, Daria Zielinska
  • Patent number: 8916538
    Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: December 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
  • Patent number: 8884001
    Abstract: The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2? into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
    Type: Grant
    Filed: May 8, 2009
    Date of Patent: November 11, 2014
    Assignee: Cyclacel Limited
    Inventors: Gavin Wood, Robert Westwood, Tsuyoshi Murofushi, Eiji Numagami, Takashi Takita
  • Publication number: 20140294769
    Abstract: Provided herein are compounds, methods and pharmaceutical compositions for use in treatment of viral infections, including hepatitis C virus (HCV) infections, in hosts in need thereof. In certain embodiments, the compounds are 2?,4?-fluoro nucleosides according to Formula 1001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, RA, and PD are as described herein. In certain embodiments, 2?,4?-fluoro nucleosides are provided which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human.
    Type: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART
  • Publication number: 20140273023
    Abstract: The present invention comprises novel analogs of gemcitabine and novel gemcitabine immunogens teased out of, i.e., derived from, the 5?-hydroxy position of gemcitabine. The invention also comprises unique monoclonal antibodies generated using gemcitabine linked immunogens as well as unique conjugates and tracers which antibodies, conjugates, and tracers are useful in immunoassays for the quantification and monitoring of gemcitabine in biological fluids.
    Type: Application
    Filed: March 15, 2013
    Publication date: September 18, 2014
    Applicant: Saladax Biomedical Inc.
    Inventors: Salvatore J. Salamone, Jodi Blake Courtney, Howard Sard, Christopher Spedaliere
  • Patent number: 8691972
    Abstract: Disclosed are compounds of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Also disclosed are methods of preparing compound of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Further disclosed are methods of counducting drug discovery and research comprises applying the compound of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer in an investigation.
    Type: Grant
    Filed: July 20, 2012
    Date of Patent: April 8, 2014
    Inventor: Zhen Huang
  • Patent number: 8653048
    Abstract: Prodrugs based on gemcitabine structure shown in formula (I) as well as their synthetic method and application are disclosed in the present invention, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N4 group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is overcome for the produced prodrugs compounds. Intestinal toxicity induced by gemcitabine is decreased. Thereby, the prodrugs can be delivered by oral administration in clinics and further improve their anti-tumor, anti-cancer, anti-infection and diffusion preventing capability, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.
    Type: Grant
    Filed: March 25, 2010
    Date of Patent: February 18, 2014
    Assignee: Sanlugen Pharmatech Ltd.
    Inventors: Xiaoxia Xue, Gang Li, Changjun Sun, Wenbao Li
  • Patent number: 8642756
    Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.
    Type: Grant
    Filed: May 20, 2010
    Date of Patent: February 4, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
  • Patent number: 8569478
    Abstract: Compounds, methods and compositions for treating a host infected with human immunodeficiency virus and hepatitis B virus comprising administering an effective amount of a described 4?-C-substituted ?-D- and ?-L-nucleoside or a pharmaceutically acceptable salt or prodrug thereof, are provided.
    Type: Grant
    Filed: September 26, 2006
    Date of Patent: October 29, 2013
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Phillip Furman, Michael Joseph Sofia
  • Patent number: 8492537
    Abstract: The invention relates to special nucleosides, for example, a nucleoside of the formula I, wherein R1-R5 are as described herein, and also to drugs which contain these nucleosides. Furthermore, the invention relates to the use of such nucleosides in a method for suppressing or reducing the formation of resistance in the case of cytotstatic treatment of a cancer patient.
    Type: Grant
    Filed: August 13, 2007
    Date of Patent: July 23, 2013
    Assignee: RESprotect GmbH
    Inventors: Rudolf Fahrig, Dieter Lohmann, Andreas Rolfs, Henrik Dieks, Janek Teubner, Jorg-Christian Heinrich
  • Publication number: 20130137861
    Abstract: A reagent for oligonucleotide synthesis or purification, wherein the reagent has a structure of: X—C-L-H??(Formula A) wherein X is a phosphoramidite group, an H-phosphonate group, an acetal group, or an isocyanate; C is a direct bond or a cleavable adaptor represented by —Ca-Cb—; L is a hydrocarbyl chain; and H is a terminal alkyne or an activated cyclooctyne. The reagent of Formula (A) can be used in the synthesis and purification of oligonucleotides.
    Type: Application
    Filed: November 6, 2012
    Publication date: May 30, 2013
    Applicant: AGILENT TECHNOLOGIES, INC.
    Inventor: Agilent Technologies, Inc.
  • Patent number: 8445669
    Abstract: The present invention provides a process for producing 2?,3?-didehydro-3?-deoxy-4?-ethynylthymidine, which is useful as a medicine, in an efficient and industrially advantageous manner, and more specifically, provides a process for producing 2?,3?-didehydro-3?-deoxy-4?-ethynylthymidine as shown below. (wherein R1 and R2 independently represent a protective group for a hydroxy group, or R1 and R2 together form a protective group for two hydroxy groups, R3 and R4 independently represent a protective group for a hydroxy group, R5 represents a protective group for a hydroxy group, R6 represents a protective group for a hydroxy group, X represents a leaving group, and Y represents a halogen atom.
    Type: Grant
    Filed: April 10, 2009
    Date of Patent: May 21, 2013
    Assignee: Hamari Chemicals, Ltd.
    Inventors: Tatsunori Sato, Tetsuya Kawashima, Toshio Miwa, Kazutoyo Dokei, Chikoto Fujimoto
  • Patent number: 8435960
    Abstract: The present invention provides devices and compositions for the management of infection of topical lesions, each of the devices and compositions containing protonated/acidified nucleic acids either on its surface, or integrated into the device. These modified nucleic acids are effective as bactericidal and/or bacteriostatic agents without regard to the class of bacteria, so are especially useful when diagnosis is difficult or when multiple infectious organisms are present. The antibiotic activity of nucleic acids of the invention is not dependent on either the specific sequence of the nucleic acid or the length of the nucleic acid molecule. The nucleic acids used in the invention are protonated/acidified to give a pH when dissolved in water of less than pH 7 to about 1, more preferably less than pH 4.5 to about 1, and even more preferably less than pH 2 to about 1.
    Type: Grant
    Filed: May 30, 2008
    Date of Patent: May 7, 2013
    Assignee: Lakewood-Amedex, Inc.
    Inventors: Roderic M. K. Dale, Steven L. Gatton, Amy Arrow
  • Publication number: 20130102772
    Abstract: Systems, methods, and devices for generating radionuclides for use in production of radiopharmaceuticals; synthesizing the radionuclides generated and removing any unwanted products; measuring the quantity and activity level of the synthesized radionuclides; distributively delivering the radionuclides in appropriate quantities to modular cassette synthesis units in a modular cassette subsystem for contemporaneous/parallel production of radiopharmaceutical output and that allow reuse and/or quick, safe, and disposable replacement of portions of the subsystem; delivering non-radionuclide components to the modular cassette synthesis units as part of production of radiopharmaceutical output; measuring the quantity and activity level of each stream of radiopharmaceutical output; purifying the radiopharmaceutical output; dispensing individual doses in sterile vial(s); automatically producing labeling and dose related information; performing automated quality control on extracted samples of produced radiopharmaceuti
    Type: Application
    Filed: July 16, 2012
    Publication date: April 25, 2013
    Applicant: CARDINAL HEALTH 414, LLC
    Inventors: Dennis ESHIMA, Mehmet Husnu, Jim Stone, Derrick Alcaide, Henry Padgett, Joseph E. Zambanini, Thomas A. Klausing, Chad E. Bouton, Brian C. Kelley, Scott N. Danhof, David A. Holley, Jeffrey T. Stroup, James B. Gleeson, Eric Hassenpflug, James A. Prescott, Herman Benecke, Daniel B. Garbark
  • Patent number: 8394934
    Abstract: A method is disclosed for synthesizing 2?,3?-didehydro-2?,3?-dideoxynucleosides (d4Ns) from a nucleophile-mediated elimination, such as a telluride-mediated elimination reaction. After substitution of 2,2?-anhydronucleosides with a nucleophile, such as a telluride monoanion, a telluride intermediate is formed, and its elimination leads to formation of the olefin products (d4Ns). This disclosure describes this telluride-assisted (or nucleophile-assisted) reaction and how to facilitate the substitution and elimination in order to form d4Ns.
    Type: Grant
    Filed: March 20, 2009
    Date of Patent: March 12, 2013
    Inventors: Zhen Huang, Jia Sheng
  • Publication number: 20130041144
    Abstract: Provided herein are novel 5?-(S)—CH3 substituted bicyclic nucleosides, oligomeric compounds prepared therefrom and methods of using the oligomeric compounds. More particularly, the furanose ring of each of the novel 5?-(S)—CH3 substituted bicyclic nucleosides includes a 2? to 4? bridging group. The 5?-(S)—CH3 substituted bicyclic nucleosides are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as for example increasing the binding affinity. In certain 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: March 10, 2011
    Publication date: February 14, 2013
    Applicant: Isis Pharmaceuticals, Inc.
    Inventors: Michael T. Migawa, Thazha P. Prakash, Charles Allerson, Balkrishen Bhat, Punit P. Seth, Eric E. Swayze
  • Publication number: 20130023657
    Abstract: A system and method for radiopharmaceutical production involving solid and liquid phase interactions are provided, the system including a module for facilitating solid and liquid phase interactions by performing techniques including high pressure, low pressure, and solid phase extraction. The system includes various modular components, each of which performs steps in the process of preparing radiopharmaceuticals, and one or more radiation detectors monitor the radiation level and path of various products. The modular components may be added to and removed from the system easily to allow for flexibility in the operation of the system. An HPLC module may be included to purify radiopharmaceuticals.
    Type: Application
    Filed: July 16, 2012
    Publication date: January 24, 2013
    Applicant: CARDINAL HEALTH 414, LLC
    Inventors: Thomas A. KLAUSING, Jeffery T. STROUP, Jason T. HOLDRIDGE
  • Publication number: 20130005956
    Abstract: A method for synthesizing an 18F-labeled probe. The method includes a step of eluting an amount of 18F with a first solvent which includes a predetermined amount of water and at least one organic solvent. In this step, the 18F elutes as an 18F solution. The method also includes a step of using the 18F solution to perform 18F-labeling in the presence of at least one labeling reagent and at least one phase transfer catalyst so as to generate the 18F-labeled probe. In the method, there is no step of drying the 18F starting from a time when the eluting step is performed and ending at a time when the 18F-labeling step is performed.
    Type: Application
    Filed: April 8, 2011
    Publication date: January 3, 2013
    Applicant: SIEMENS MEDICAL SOLUTIONS USA, INC.
    Inventors: Umesh Gangadharmath, Joseph Walsh, Hartmuth Kolb
  • Patent number: 8343478
    Abstract: The present invention relates to the use of Parapoxviruses in combination with other agents for the treatment of viral diseases, and in particular HIV infections and AIDS. The invention also relates to methods for producing medicaments based on combinations of Parapoxviruses and other antiviral agents, and to such medicaments. In particular, the invention relates to the use of Parapoxviruses in combination with agents of the kind used for antiretroviral therapy and highly active antiretroviral therapy (HAART).
    Type: Grant
    Filed: January 11, 2007
    Date of Patent: January 1, 2013
    Assignee: AiCuris GmbH & Co. KG
    Inventors: Daniela Paulsen, Helga Ruebsamen-Schaeff, Amar Kureishi, Gerhard Hunsmann, Christiane Stahl-Hennig, Andreas Meyerhans, Alexandra Schuetz, Olaf Weber
  • Publication number: 20120322995
    Abstract: The invention provides a process for producing a ?-dihydrofuran derivative represented by formula (1) or a ?-tetrahydrofuran derivative represented by formula (4), characterized in that the process includes causing a dialkyl dicarbonate, a diaralkyl dicarbonate, or a halide to act on a diol compound represented by formula (2) or (3). The invention also provides a process for producing 4?-ethynyl-2?,3?-didehydro-3?-deoxythymidine or an analog thereof, the process including glycosylation and deprotection.
    Type: Application
    Filed: February 7, 2011
    Publication date: December 20, 2012
    Inventors: Yusuke Iriyama, Tsutomu Higashiyama
  • Publication number: 20120309705
    Abstract: The present invention includes novel 3?-deoxy-3?-methylidene-?-L-nucleosides, pharmaceutical composition comprising such compounds, as well as the methods to treat or to prevent viral infections and in particular HBV and/or HIV infections.
    Type: Application
    Filed: December 14, 2010
    Publication date: December 6, 2012
    Applicant: NOVADEX PHARMACEUTICALS AB
    Inventors: Xiao Xiong Zhou, Staffan Torssell, Olov Wallner, Piaoyang Sun
  • Patent number: 8318756
    Abstract: Methods for improved administration and dosing of DPD inhibitors in combination with 5-FU and/or 5-FU prodrugs are provided, comprising first administering to a patient in need thereof a DPD inhibitor that substantially eliminates activity of the enzyme and thereafter administering 5-FU or a 5-FU prodrug, wherein the level of 5-FU or 5-FU prodrug is in substantial excess of DPD inhibitor in the patient.
    Type: Grant
    Filed: December 5, 2005
    Date of Patent: November 27, 2012
    Assignee: Adherex Technologies, Inc.
    Inventors: Thomas Spector, William Paul Peters, Donald W. Kufe, Brian Huber
  • Publication number: 20120282702
    Abstract: Disclosed are compounds of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Also disclosed are methods of preparing compound of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer. Further disclosed are methods of conducting drug discovery and research comprises applying the compound of formula (I), a derivative, or a tautomer thereof, or a pharmaceutically acceptable salt of said compound or said tautomer in an investigation.
    Type: Application
    Filed: July 20, 2012
    Publication date: November 8, 2012
    Inventor: Zhen Huang
  • Publication number: 20120238740
    Abstract: The present invention provides novel and advantageous processes for preparing and purifying pharmaceuticals The processes comprise a nucleophilic reaction wherein a modified leaving group LM, which has increased lipophilicity, of a vector in a nucleophilic reaction which offers a convenient and time-saving way to purify the product from non-reacted precursors vector-LM and by-products LM.
    Type: Application
    Filed: July 6, 2010
    Publication date: September 20, 2012
    Applicant: BAYER PHARMA AKTIENGESELLSCHAFT
    Inventors: Keith Graham, Mathias Berndt, Dae Yoon Chi, Byoung Se Lee, Sandip S. Shinde, Hee Seup Kil, Sang Ju Lee, Jin-Sook Ryu, Seung Jun Oh
  • Publication number: 20120202766
    Abstract: The present invention is directed to a method and composition of treating or preventing viral infections, in particular, human immunodeficiency virus (HIV) and hepatitis B virus (HBV) infections, in human patients or other animal hosts, comprising the administration of N.sup.4-acyl-2?,3?-dideoxy-5-fluorocytidine or N.sup.4-acyl-2?,3?-didehyd-ro-2?,3?-dideoxy-5-fluorocytidine, and pharmaceutically acceptable salts, prodrugs, and other derivatives thereof.
    Type: Application
    Filed: February 13, 2012
    Publication date: August 9, 2012
    Applicant: Pharmasset, Inc.
    Inventors: Michael J. Otto, Junxing Shi, Kyoichi A. Watanabe
  • Patent number: 8193165
    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: August 17, 2009
    Date of Patent: June 5, 2012
    Assignee: Yale University
    Inventors: Yung-chi Cheng, Hiromichi Tanaka, Masanori Baba
  • Publication number: 20120135954
    Abstract: Described herein are compounds and methods that prevent the viral infection of cells. The compounds and methods described herein minimize viral resistance and maximize the number of targeted viruses. Additionally, the compounds and methods minimize the toxicity toward uninfected cells.
    Type: Application
    Filed: February 27, 2008
    Publication date: May 31, 2012
    Inventors: Luis M. Schang, Mireilli R. St. Vincent, Alexey V. Ustinov
  • Publication number: 20110312880
    Abstract: The present invention relates to compounds, in particular, dual antagonists comprising a nucleoside reverse transcriptase inhibitor (NRTI) or a nucleoside competititive reverse transcriptase inhibitor and a non-nucleoside reverse transcriptase inhibitor (NNRTI), linked together using a chemical linker, which may be used to inhibit HIV (HIV-1) reverse transcriptase and in the treatment of HIV infections, more severe cases of HIV infections, including ARC and AIDS, including reducing the likelihood of these infections and disease states.
    Type: Application
    Filed: April 9, 2009
    Publication date: December 22, 2011
    Inventors: Karen S. Anderson, Roger Hunter
  • Publication number: 20110294213
    Abstract: Oligonucleotides with a novel sugar-phosphate backbone containing at least one 2?-arabino-fluoronucleoside and an internucleoside 3?-NH—P(?O)(OR)—O-5? linkage, where R is a positively charged counter ion or hydrogen, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive phosphoramidate 2?-aribino-fluorooligonucleotides have a high RNA binding affinity to complementary nucleic acids and are base and acid stable.
    Type: Application
    Filed: July 27, 2011
    Publication date: December 1, 2011
    Inventors: Sergei Gryaznov, Ronald G. Schultz
  • Patent number: 8058424
    Abstract: The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylated 5-azacytosine to a protected ?-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).
    Type: Grant
    Filed: December 20, 2010
    Date of Patent: November 15, 2011
    Assignee: Pharmion LLC
    Inventors: Dumitru Ionescu, Peter Blumbergs
  • Patent number: 8026356
    Abstract: The present invention provides a method for preparing pure Stavudine having purity more than 99.5% comprises: i) Converting 3?,5?-anhydrothymidine to crude Stavudine, ii) Converting crude Stavudine to stable solvates of Stavudine, iii) Desolvation of the solvates to give pure Stavudine. The present invention also disclosed novel solvates of Stavudine and conversion of novel Stavudine solvates to Stavudine.
    Type: Grant
    Filed: November 17, 2006
    Date of Patent: September 27, 2011
    Assignee: Matrix Laboratories, Ltd.
    Inventors: Purna Chandra Ray, Jagan Mohana Chary Tummanapalli, Seeta Ramanjaneyulu Gorantla
  • Publication number: 20110224421
    Abstract: The present invention relates to a process for preparing a compound of formula 682-4, said process comprising the steps of: (i) converting a compound of formula 682-1 into a compound of formula 682-2; (ii) converting said compound of formula 682-2? into a compound of formula 682-3; and (iii) converting said compound of formula 682-3 into a compound of formula 682-4. Further aspects of the invention relate to the use of the above process in the preparation of 2?-cyano-2?-deoxy-N4-palmitoyl-1-?-D-arabmofuranosylcytosine, a pyrimidine nucleoside which is therapeutically useful in the treatment and/or prevention of cancer.
    Type: Application
    Filed: May 8, 2009
    Publication date: September 15, 2011
    Applicant: CYCLACEL LIMITED
    Inventors: Gavin Wood, Robert Westwood
  • Publication number: 20110183933
    Abstract: In its many embodiments, the present invention provides a novel class of pyrimidine analogs of formula (V) as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the activator as well as the combination and pharmaceutical kits.
    Type: Application
    Filed: November 5, 2008
    Publication date: July 28, 2011
    Inventors: Timothy J. Guzi, David A. Parry, Marc A. Labroli, Michael P. Dwyer, Kamil Paruch
  • Publication number: 20110172410
    Abstract: 4-Amino-1-((2R,3S,4S,5R)-5-azido-4-hydroxy-5-hydroxymethyl-3-methyl-tetrahydro-furan-2-yl)-1H-pyrimidin-2-one (22) and prodrugs thereof are hepatitis C(HCV) polymerase inhibitors. Also disclosed are compositions and methods for inhibiting HCV and treating HCV-mediated diseases, processes for making the compounds and synthetic intermediates employed in the process.
    Type: Application
    Filed: March 28, 2011
    Publication date: July 14, 2011
    Applicant: Medivir AB
    Inventors: Nils-Gunnar JOHANSSON, Genadiy Kalyanov, Joseph Armstrong Martin, David Bernard Smith, Anna Winqvist
  • Publication number: 20110054164
    Abstract: The present invention provides a process for producing 2?,3?-didehydro-3?-deoxy-4?-ethynylthymidine, which is useful as a medicine, in an efficient and industrially advantageous manner, and more specifically, provides a process for producing 2?,3?-didehydro-3?-deoxy-4?-ethynylthymidine as shown below. (wherein R1 and R2 independently represent a protective group for a hydroxy group, or R1 and R2 together form a protective group for two hydroxy groups, R3 and R4 independently represent a protective group for a hydroxy group, R5 represents a protective group for a hydroxy group, R6 represents a protective group for a hydroxy group, X represents a leaving group, and Y represents a halogen atom.
    Type: Application
    Filed: April 10, 2009
    Publication date: March 3, 2011
    Inventors: Tatsunori Sato, Tetsuya Kawashima, Toshio Miwa, Kazutoyo Dokei, Chikoto Fujimoto
  • Patent number: 7858774
    Abstract: The present invention provides a method for the preparation of 5-azacytidine, wherein 5-azacytidine is represented by the structure: The method involves the silylation of 5-azacytosine, followed by the coupling of silylated 5-azacytosine to a protected ?-D-ribofuranose derivative. The coupling reaction is catalyzed by trimethylsilyl trifluoromethanesulfonate (TMS-Triflate).
    Type: Grant
    Filed: September 10, 2008
    Date of Patent: December 28, 2010
    Assignee: Pharmion LLC
    Inventors: Dumitru Ionescu, Peter Blumbergs
  • Publication number: 20100298257
    Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.
    Type: Application
    Filed: May 20, 2010
    Publication date: November 25, 2010
    Applicant: PHARMASSET, INC.
    Inventors: BRUCE ROSS, MICHAEL JOSEPH SOFIA, GANAPATI REDDY PAMULAPATI, SUGUNA RACHAKONDA, HAI-REN ZHANG, BYOUNG-KWON CHUN, PEIYUAN WANG
  • Patent number: 7824851
    Abstract: The present invention discloses a method for the treatment of Flaviviridae infection that includes the administration of a 2?-branched nucleoside, or a pharmaceutically acceptable prodrug and/or salt thereof, to a human in need of therapy in combination or alternation with a drug that directly or indirectly induces a mutation in the viral genome at a location other than a mutation of a nucleotide that results in a change from seine to a different amino acid in the highly conserved consensus sequence, XRXSGXXXT (Sequence ID No. 63), of domain B of the RNA polymerase region, or is associated with such a mutation. The invention also includes a method to detect a mutant strain of Flaviviridae and a method for its treatment.
    Type: Grant
    Filed: November 17, 2003
    Date of Patent: November 2, 2010
    Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi Di Cagliari
    Inventors: Jean-Pierre Sommadossi, Paolo LaColla, David Standring, Vadim Bichko, Lin Qu
  • Publication number: 20100234584
    Abstract: The present invention provides 2?-fluorine-4?-substituted-nucleoside analogues or their pro-drugs or 5?-phosphate esters (including the pro-drugs of the 5?-phosphate esters), preparation methods and uses thereof. The compounds have the general formula as follows: wherein B= R=CH3, CN, N3, C?CH; R?=H, F; X=F, OH, NH2; Y=H, CH3, F, OH, NH2 The compounds are used in the synthesis of drugs for the treatment of virus infection, especially for the treatment of HBV, HCV or HIV infection.
    Type: Application
    Filed: June 27, 2008
    Publication date: September 16, 2010
    Inventor: Junbiao Chang
  • Publication number: 20100227834
    Abstract: The invention relates to special nucleosides, for example, a nucleoside of the formula I, wherein R1-R5 are as described herein, and also to drugs which contain these nucleosides. Furthermore, the invention relates to the use of such nucleosides in a method for suppressing or reducing the formation of resistance in the case of cytostatic treatment of a cancer patient.
    Type: Application
    Filed: August 13, 2007
    Publication date: September 9, 2010
    Applicant: RESprotech GmbH
    Inventors: Rudolf Fahrig, Dieter Lohmann, Andreas Rolfs, Henrik Dieks, Janek Teubner, Jörg-Christian Heinrich
  • Patent number: 7759481
    Abstract: The present invention provides novel crystalline forms of 5-deazacytidine, and pharmaceutical compositions comprising these novel forms. The invention also provides methods for the preparation of the novel forms and compositions.
    Type: Grant
    Filed: January 11, 2008
    Date of Patent: July 20, 2010
    Assignee: Ivax Corporation
    Inventors: Ales Gavenda, Alexandr Jegorov
  • Publication number: 20100179314
    Abstract: The present invention provides a novel and highly stereoselective process for preparing gemcitabine, which is suitable for industrial production, wherein, it includes the following reactions. Additionally, the invention discloses the key intermediates. The definition for the groups of G1, G2, G3, G4, and G5 are described in the specification.
    Type: Application
    Filed: September 7, 2007
    Publication date: July 15, 2010
    Applicant: NANJING CAVENDISH BIO-ENGINEERING TECHNOLOGY CO.,
    Inventors: Yongxiang Xu, Hao Yang, Wen Hou
  • Publication number: 20100105887
    Abstract: Disclosed is the preparation of 2-deoxy-D-erythro-2,2-difluoro-ribofuranose-3,5-dibenzoate: a known intermediate for the preparation of Gemcitabine, by means of a reduction process; further disclosed is the purification of Gemcitabine by chromatography and the purification of Gemcitabine hydrochloride by crystallization techniques from ternary solvent mixtures. The main advantage of the invention is providing Gemcitabine hydrochloride with purity in conformity with the Pharmacopoeia requirements, as well as a process particularly convenient from the industrial point of view.
    Type: Application
    Filed: October 21, 2009
    Publication date: April 29, 2010
    Applicant: PRIME EUROPEAN THERAPEUTICALS S.P.A.
    Inventors: Alberto Varalli, Paolo Anesa, Maria Argese, Giuseppe Guazzi
  • Patent number: 7704971
    Abstract: Uracil reductase inactivators, notably a 5-substituted uracil or 5,6-dihydro-5-substituted uracil, potentiate 5-flourouracil and find use particularly in the treatment of cancer. The 5-substituent is selected from bromo, ido, cyano, halo-substituted C1-4 alkyl, C2-6 alkenyl, 1-halo-C2-6 alkenyl and halo-substituted C2-6 alkynyl.
    Type: Grant
    Filed: September 1, 2006
    Date of Patent: April 27, 2010
    Assignee: SmithKlineBeecham Corporation
    Inventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
  • Publication number: 20100075917
    Abstract: The invention relates to a pharmaceutical composition containing as an active ingredient at least one compound selected from the compounds of the formula (II), in which the S atom is bonded to the nucleoside carbon at T or to the nucleoside carbon at 3?, and from the compounds of the following formula (III): formulae in which B is a nucleotide natural or modified base, x is 0, 1 or 2, and R1 and R represent a carbonated group or a molecular hydrocarbon remnant that can be substituted and/or interrupted by one or more atoms and/or by one or more groups containing one or more atoms, said atoms being selected from N, O, P, S, Si, X where X is halogen. The invention also relates to pharmaceutically acceptable carrier.
    Type: Application
    Filed: October 29, 2007
    Publication date: March 25, 2010
    Applicant: UNIVERSITE JOSEPH FOURIER (GRENOBLE 1)
    Inventors: Jean-Luc Decout, Beatrice Gerland, Jerome Desire, Michel Lepoivre, Jan Balzarini
  • Publication number: 20090318380
    Abstract: Embodiments of the invention are to compounds, methods, and compositions for use in the treatment of viral infections. More specifically embodiments of the invention are 2?,4?-substituted nucleoside compounds useful for the treatment of viral infections, such as HIV, HCV, and HBV infections.
    Type: Application
    Filed: November 14, 2008
    Publication date: December 24, 2009
    Applicant: PHARMASSET, INC.
    Inventors: MICHAEL JOSEPH SOFIA, JINFA DU