Nitrogen, Other Than Nitro Or Nitroso, Bonded Directly To The 2-position Of The Purine Ring System (e.g., Guanosine, Etc.) Patents (Class 536/27.81)
  • Patent number: 9278991
    Abstract: The present invention provides novel anhydrous polymorph forms of 2R,3S,4R,5R)-5-(6-(cyclopentylamino)-9H-purin-9-yl)-3,4-dihydroxytetrahydrofuran-2-yl) methyl nitrate (Compound A), a selective adenosine A1 receptor agonist with a number of therapeutic uses including the treatment of elevated intra-ocular pressure. Also provided are methods for the preparation of the anhydrous polymorphic forms of compound A, pharmaceutical compositions and methods of treatment.
    Type: Grant
    Filed: January 25, 2013
    Date of Patent: March 8, 2016
    Assignee: Inotek Pharmaceuticals Corporation
    Inventor: William K. McVicar
  • Publication number: 20150105341
    Abstract: Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.
    Type: Application
    Filed: October 9, 2014
    Publication date: April 16, 2015
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith, Marija Prhavc, Christian Andreas Jekle, Jerome Deval
  • Publication number: 20150090936
    Abstract: Provided herein are heptamethine cyanine dyes having a large Stokes shift, and the salts and conjugates thereof. Also provided are methods of using and making such large Stokes shift dyes as fluorescence resonance energy transfer (FRET) acceptors or donors.
    Type: Application
    Filed: December 10, 2014
    Publication date: April 2, 2015
    Inventors: Yi-Zhen HU, Hee Chol KANG
  • Patent number: 8957201
    Abstract: A method for the prevention or treatment in a mammal of a disease preventable or treatable by the pharmacologically useful antisense or antigene activity of an oligonucleotide analogue or a pharmacologically acceptable salt thereof in the body of said mammal, which method comprises administering to said mammal in need of such prevention or treatment a pharmaceutically effective amount of an oligonucleotide analogue comprising two or more nucleoside units, wherein at least one of said nucleoside units is a structure of the formula (2): wherein A is methylene; and B is an unsubstituted purin-9-yl, an unsubstituted 2-oxo-pyrimidin-1-yl or a substituted purin-9-yl; or a pharmacologically acceptable salt thereof.
    Type: Grant
    Filed: July 22, 2010
    Date of Patent: February 17, 2015
    Assignee: Daiichi Sankyo Company, Limited
    Inventors: Masakatsu Kaneko, Koji Morita, Takeshi Imanishi
  • Publication number: 20150018297
    Abstract: The present disclosure relates to a pharmaceutical composition, a health functional food composition, and a method for preventing or treating a brain disease or diabetes. The pharmaceutical composition, health functional food composition, and method includes at least one active ingredient that is chlorhexidine, thioguanosine, mebendazole, fenbendazole, colchicine, farnesol, trimethobenzamide hydrochloride, disulfuram, azathioprine, mebeverine hydrochloride, zaprinast, tosufloxacin hydrochloride, efavirenz, thiostrepton, probenecid, entacapone, harmine hydrochloride, flunisolide, thimerosal, hexestrol, sulfaquinoxaline sodium salt, monensin sodium salt, raloxifene hydrochloride, 2-chloropyrazine, or topotecan.
    Type: Application
    Filed: July 14, 2014
    Publication date: January 15, 2015
    Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITY
    Inventors: Dong Gyu JO, Jong Sung PARK, Youngkwang YOUN, Yuri CHOI, Ui Jeong YUN
  • Publication number: 20140377743
    Abstract: This invention provides a nucleotide analogue comprising (i) a base selected from the group consisting of adenine, guanine, cytosine, thymine and uracil, (ii) a deoxyribose, (iii) an allyl moiety bound to the 3?-oxygen of the deoxyribose and (iv) a fluorophore bound to the base via an allyl linker, and methods of nucleic acid sequencing employing the nucleotide analogue.
    Type: Application
    Filed: August 4, 2014
    Publication date: December 25, 2014
    Applicant: The Trustees of Columbia University in the City of New York
    Inventors: Jingyue Ju, Lanrong Bi, Dae Hyun Kim, Qinglin Meng
  • Patent number: 8877731
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof. Examples of viral infections include a respiratory syncytial viral (RSV) and influenza infection.
    Type: Grant
    Filed: September 19, 2011
    Date of Patent: November 4, 2014
    Assignee: Alios Biopharma, Inc.
    Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
  • Patent number: 8846636
    Abstract: The disclosure provides nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moieties with quaternary centers at the 3? position, the pharmaceutical formulations comprising the analogues, and methods of using the analogues and formulations for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses.
    Type: Grant
    Filed: March 18, 2009
    Date of Patent: September 30, 2014
    Assignee: LCB Pharma Inc.
    Inventor: Yvan Guindon
  • Publication number: 20140286903
    Abstract: This invention is directed to compounds of Formula (I) having the structure that are useful in the treatment of viral infections in mammals, particularly in humans, mediated, at least in part, by a virus in the Flaviviridae family of viruses.
    Type: Application
    Filed: November 8, 2012
    Publication date: September 25, 2014
    Applicants: INHIBITEX, INC., UNIVERSITY COLLEGE CARDIFF CONSULTANTS LIMITED
    Inventors: Stanley Chamberlain, John Vernachio, Srinivas K. Battina, Changalvala V.S. Ramamurty, C. Srinivas Rao, Chris McGuigan, Andrea Brancale
  • Publication number: 20140256928
    Abstract: A protecting group for 1-nitrogen atom of an indole group including a sulfonylethyl carbamate group, wherein the protecting group is represented by the following General Formula (I) and capable of being removed from the 1-nitrogen atom of the indole group in an aprotic solvent: where R represents an alkyl group, a derivative of the alkyl group, a phenyl group or a derivative of the phenyl group.
    Type: Application
    Filed: May 9, 2014
    Publication date: September 11, 2014
    Applicant: APTA BIOSCIENCES LTD.
    Inventor: Tsuyoshi FUJIHARA
  • Patent number: 8809520
    Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.
    Type: Grant
    Filed: July 11, 2013
    Date of Patent: August 19, 2014
    Assignee: K.U. Leuven Research & Development
    Inventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
  • Publication number: 20140221304
    Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 10, 2012
    Publication date: August 7, 2014
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
  • Publication number: 20140206640
    Abstract: The present invention relates to 2?-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Azido Substituted Nucleoside Derivative, and methods of using the 2?-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: July 24, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Frank Bennett, Vishal Verma, Ashok Arasappan, Kevin X. Chen, Ying Huang, Angela Kerekes, Latha Nair, Dimitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Publication number: 20140194614
    Abstract: A novel class of pharmaceuticals which comprises a Locked Nucleic Acid (LNA) which can be used in antisense therapy. These novel oligonucleotides have improved antisense properties. The novel oligonucleotides are composed of at least one LNA selected from beta-D-thio/amino-LNA or alpha-L-oxy/thio/amino-LNA. The oligonucleotides comprising LNA may also include DNA and/or RNA nucleotides.
    Type: Application
    Filed: March 15, 2013
    Publication date: July 10, 2014
    Applicant: Santaris Pharma A/S
    Inventors: Signe M. Christensen, Nikolaj Dam Mikkelsen, Miriam Frieden, Henrik Frydenlund Hansen, Troels Koch, Daniel Sejer Pedersen, Christoph Rosenbohm, Charlotte Albaek Thrue, Majken Westergaard
  • Patent number: 8748593
    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: Grant
    Filed: December 22, 2008
    Date of Patent: June 10, 2014
    Assignee: Geron Corporation
    Inventors: Sergei M. Gryaznov, Krisztina Pongracz, Daria Zielinska
  • Publication number: 20140154211
    Abstract: The present invention relates to 2?-Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein A, B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Substituted Nucleoside Derivative, and methods of using the 2?-Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: June 5, 2014
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Vishal Verma, Frank Bennett, Angela Kereles, Ashok Arasappan, Dmitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Patent number: 8658616
    Abstract: Compounds having the general formula (I): are provided which have enhanced inhibitory potency and are thus useful in methods of prophylaxis or treatment of a viral infection such as hepatitis C virus. The compounds are phosphoramidate derivatives of nucleoside compounds derived from bases such as adenine and guanine. The glycoside moiety of the nucleoside compound can be substituted at the ss-2? position with methyl and the phosphoramidate group can be 1-naphthyl linked by —O— to the P atom. These compounds can be administered as pharmaceutical compositions, and methods for their preparation are also provided.
    Type: Grant
    Filed: November 23, 2007
    Date of Patent: February 25, 2014
    Assignees: University College Cardiff Consultants Limited, K.U. Leuven Research and Development
    Inventors: Christopher McGuigan, Plinio Perrone, Johan Neyts
  • Publication number: 20140051848
    Abstract: The present invention relates generally to labeled and unlabeled cleavable terminating groups and methods for DNA sequencing and other types of DNA analysis. More particularly, the invention relates in part to nucleotides and nucleosides with chemically cleavable, photocleavable, enzymatically cleavable, or non-photocleavable groups and methods for their use in DNA sequencing and its application in biomedical research.
    Type: Application
    Filed: June 27, 2013
    Publication date: February 20, 2014
    Inventors: Vladislav A. LITOSH, Megan N. HERSH, Brian P. STUPI, Weidong WU, Michael L. METZKER
  • Publication number: 20140031539
    Abstract: The present invention relates to certain purines, which act as topoisomerase II catalytic inhibitors. These compounds are useful in combination with topoisomerase II poisons, such as anthracyclines and epipodophyllotoxins, in the treatment of proliferative conditions (e.g., cancer). These compounds are useful in the treatment of tissue damage associated with extravasation of a topoisomerase II poison, such as an anthracycline or an epipodophyllotoxin.
    Type: Application
    Filed: July 3, 2013
    Publication date: January 30, 2014
    Applicant: Biocodex, Inc
    Inventors: Lars Hollund JENSEN, Maxwell SEHESTED
  • Publication number: 20140011763
    Abstract: The present invention relates to novel 1,2,3-triazolyl purine derivatives. The invention also relates to using the derivatives to treat cancer and various viral infections.
    Type: Application
    Filed: July 8, 2013
    Publication date: January 9, 2014
    Applicant: RESEARCH FOUNDATION OF THE CITY UNIVERSITY OF NEW YORK
    Inventor: Mahesh K. Lakshman
  • Patent number: 8580949
    Abstract: The disclosure concerns the enzymatic synthesis of stable analogues of nicotinamide adenine dinucleotide NAD/NADH and nicotinamide adenine dinucleotide phosphate NADP/NADPH, the so-called “carba-NADs”, i.e. analogues of NAD/NADH or NADP/NADPH, respectively, comprising a carbacyclic sugar instead of ribose.
    Type: Grant
    Filed: January 25, 2012
    Date of Patent: November 12, 2013
    Assignee: Roche Diagnostics Operations, Inc.
    Inventors: Hartmut Duefel, Dieter Heindl, Carina Horn, Thomas Meier, Rainer Schmuck
  • Patent number: 8575128
    Abstract: The invention relates to methods for transdifferentiation of body tissues which can be used to generate specific cell types needed for regenerating organs or body parts, following cellular degeneration, injury or amputation. The present invention also describes the use of tissue transdifferentiation for treating cancer and autoimmune disease.
    Type: Grant
    Filed: March 6, 2012
    Date of Patent: November 5, 2013
    Inventor: Steven Baranowitz
  • Publication number: 20130237491
    Abstract: The present invention relates to the use of nucleoside derivatives of formula Ia wherein the symbols are as defined in the specification, and of pharmaceutically acceptable salts thereof and to pharmaceutical compositions containing such compounds.
    Type: Application
    Filed: April 12, 2013
    Publication date: September 12, 2013
    Applicant: Roche Palo Alto LLC
    Inventors: Rene Robert Devos, Christopher John Hobbs, Wen-Rong Jiang, Joseph Armstrong Martin, John Herbert Merrett, Isabel Najera, Nobuo Shimma, Takuo Tsukuda
  • Publication number: 20130165400
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a disease and/or a condition, including an infection from a paramyxovirus and/or an orthomyxovirus, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: ALIOS BIOPHARMA, INC.
    Inventor: Alios BioPharma, Inc.
  • Patent number: 8466275
    Abstract: The present invention is a method for preparing 2-halo-6-aminopurines, and more specifically for preparing the clinical agent cladribine (2-chloro-2?-deoxyadenosine, CldAdo, 4), a drug of choice against hairy-cell leukemia and other neoplasms, from 2-amino-6-oxopurines, which are readily obtained from the naturally occurring compound 2?-deoxyguanosine. According to the methods of the present invention, the 6-oxo group of a protected 2?-deoxyguanosine (1) is converted to a 6-(substituted oxy) leaving group, or alternatively to a 6-chloro leaving group, the 2-amino group is replaced with a 2-chloro group, the 6-(substituted oxy) leaving group, or alternatively the 6-chloro leaving group, is replaced with a 6-amino group or, alternatively, a 2,6-dichloro substituted compound is selectively replaced with a 6-amino group, and the protecting groups are removed.
    Type: Grant
    Filed: July 2, 2009
    Date of Patent: June 18, 2013
    Assignee: Brigham Young University
    Inventors: Morris J. Robins, Zlatko Janeba, Paula Francom
  • Patent number: 8461124
    Abstract: Conformationally locked 2?,4?-carbocylic nucleosides with improved thermal and nuclease stability are disclosed. Oligonucleotides incorporating the locked nucleosides, and methods of treating disease states, are also disclosed.
    Type: Grant
    Filed: March 11, 2008
    Date of Patent: June 11, 2013
    Inventor: Jyoti Chattopadhyaya
  • Publication number: 20130144058
    Abstract: Disclosed is a process for preparing a carbonucleoside of formula (1) and intermediates for use therein. The process involves the step of reacting a compound of formula (2) with a compound of formula (3) under Mitsunobu-type reaction conditions to obtain a compound of formula (4), wherein PG1, PG2, PG3 and PG4 are protecting groups. The compound of formula (4) is deprotected to form the compound of formula (1), as shown below.
    Type: Application
    Filed: May 30, 2011
    Publication date: June 6, 2013
    Applicant: ALPHORA RESEARCH INC.
    Inventors: Dino Alberico, Joshua Clayton, Craig Dixon, Boris Gorin
  • Publication number: 20130129651
    Abstract: The present invention has objects to provide an agent for enhancing the effect of skin-whitening ingredients which enhances the skin-whitening action of skin-whitening ingredients and has an improved safeness, and to provide a skin-whitening agent, which contains the above agent and a skin-whitening ingredient(s) and has an improved and enhanced skin-whitening action. The present invention solves the above objects by providing an agent for enhancing the effect of skin-whitening ingredients, which contains one or more members selected from the group consisting of guanine and derivatives thereof as an effective ingredient(s); and a skin-whitening agent which contains the above agent along with a skin-whitening ingredient(s) particularly, members derivatives thereof and/or equol including derivatives thereof.
    Type: Application
    Filed: July 28, 2011
    Publication date: May 23, 2013
    Applicant: HAYASHIBARA CO., LTD.
    Inventors: Masaki Miyake, Osamu Sano, Kanso Iwaki, Takanori Okura, Shigeharu Fukuda
  • Publication number: 20130078217
    Abstract: The present invention relates to 2?-chloroacetylenyl-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.
    Type: Application
    Filed: September 21, 2012
    Publication date: March 28, 2013
    Inventors: Guoqiang Wang, In Jong Kim, Yat Sun Or
  • Publication number: 20130052710
    Abstract: An RNA of the present invention is an RNA containing a 5? cap structure and a coding region having a 5? initiation codon and a 3? stop codon on both ends of the coding region, the RNA having a nucleoside compound introduced at a site selected from among the 5? cap structure and 10 bases from a 5? end of the RNA, wherein the nucleoside compound is such that a group is attached to (i) a carbon atom at position 8 of a purine nucleus or (ii) a carbon atom at position 5 or 6 of a pyrimidine nucleus, the group being represented by formula (I): A-X?X-#??(I) where A represents an aryl group or a heteroaryl group, # represents a site where the group represented by the formula (I) is attached to the carbon atom at the position 8 of the purine nucleus or the carbon atom at the position 5 or 6 of the pyrimidine nucleus, and two Xs, which are identical to or different from each other, each represents a nitrogen atom or CH whose H may be substituted by alkyl.
    Type: Application
    Filed: February 18, 2011
    Publication date: February 28, 2013
    Applicant: RIKEN
    Inventors: Shinji Ogasawara, Mizuo Maeda
  • Publication number: 20130045475
    Abstract: This disclosure provides novel reversibly terminated ribonucleotides which can be used as a reagent for DNA sequencing reactions. Methods of sequencing nucleic acids using the disclosed nucleotides are also provided.
    Type: Application
    Filed: October 23, 2012
    Publication date: February 21, 2013
    Applicant: ALERE SAN DIEGO, INC.
    Inventor: Alere San Diego, Inc.
  • Publication number: 20130017171
    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: Application
    Filed: September 20, 2012
    Publication date: January 17, 2013
    Applicants: UNIVERSITA DEGLI STUDI DI CAGLIARI, IDENIX PHARMACEUTICALS, INC.
    Inventors: Idenix Pharmaceuticals, Inc., Universita Degli Studi di Cagliari
  • Patent number: 8349811
    Abstract: A stable 6-methoxy-2?,3?-dideoxyguanosine comprises 6-30% water content. It is prepared by absorbing water in 6-methoxy-2?,3?-dideoxyguanosine with less than 6% water content at low temperature and certain humidity, or drying 6-methoxy-2?,3?-dideoxyguanosine with more than 30% water content. The stable 6-methoxy-2?,3?-dideoxyguanosine can be used to prepare medicament composition, and be used to manufacture pharmaceutical for fighting hepatitis B virus or HIV.
    Type: Grant
    Filed: October 10, 2008
    Date of Patent: January 8, 2013
    Assignee: Nanjing Changao Pharmaceutical Science & Technology Co., Limited
    Inventors: Zhan Li, Haiyan Huang, Cailian Liu, Lixun Jiang
  • Patent number: 8334364
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a high therapeutic effect at a low dose. [Means For Solving Problems] Disclosed is a high molecular weight derivative of a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the carboxyl group in the side chain is bound to a hydroxyl group in the nucleoside derivative via an ester bond. Also disclosed is a method for producing the high molecular weight derivative.
    Type: Grant
    Filed: November 1, 2007
    Date of Patent: December 18, 2012
    Assignee: Nipon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • 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
  • Publication number: 20120309107
    Abstract: Nucleoside analogs are provided; and fluorescent sensors comprising the nucleoside analogs. The sensors comprise multiple chromophores built on a DNA backbone, in which all the natural DNA bases are replaced by excimeric or exciplex-forming fluorophores, ligands, quenchers and spacers in thousands of combinations. The sensors find use in the detection and identification of target analytes by fluorescence, e.g., detection of metal ions, neutral organic compounds and anions. The sensors find use in the detection and identification of molecular species in the vapor or gaseous phase, or the liquid phase. The sensors find use in qualitative and quantitative screening and detection methods.
    Type: Application
    Filed: December 14, 2010
    Publication date: December 6, 2012
    Inventor: Eric Todd Kool
  • Patent number: 8293215
    Abstract: The present invention relates to the field of improving the flavor of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. More particularly, the present invention provides flavor modulating substances selected from the group represented by formula (I): and edible salts thereof and edible esters thereof, which can advantageously be used for modulating the flavor of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. These flavor modulating substances can be used to impart desirable taste attributes in a wide variety of applications and products. In addition, the present flavor modulating substances are capable of modulating the taste and/or aroma impact of other, flavor imparting, substances contained within these same products, thereby improving the overall flavor quality of these products.
    Type: Grant
    Filed: December 13, 2007
    Date of Patent: October 23, 2012
    Assignee: Givaudan Nederland Services B.V.
    Inventors: Adri De Klerk, Marieke Baalbergen, Harry Renes, Chris Winkel
  • Publication number: 20120245335
    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: Application
    Filed: June 7, 2012
    Publication date: September 27, 2012
    Applicant: GILEAD PHARMASSET LLC
    Inventor: Jeremy Clark
  • Publication number: 20120237480
    Abstract: The present invention relates to 2?-allene-substituted nucleoside derivatives of the general formula (I): As well as pharmaceutical compositions comprising such compounds and methods to treat or prevent an HIV infection, HBV infection, HCV infection or abnormal cellular proliferation, comprising administering said compounds or compositions. In addition, the present invention includes processes for the preparation of such compounds, and the related ?-D and ?-L-nucleoside derivatives.
    Type: Application
    Filed: March 16, 2012
    Publication date: September 20, 2012
    Inventors: YAT SUN OR, Jun Ma, Guoqiang Wang, In Jong Kim, Jiang Long, Yao-Ling Qiu
  • Publication number: 20120232029
    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: December 13, 2011
    Publication date: September 13, 2012
    Applicant: Pharmasset, Inc.
    Inventors: MICHAEL JOSEPH SOFIA, Jinfa Du
  • Patent number: 8252919
    Abstract: The present invention relates to a method for producing a 2?-hydroxy-protected nucleoside derivative by reacting a ribonucleoside with an acylating or a carbamoylating reagent in the presence of a metal complex consisting of a copper compound and an optically active ligand. By the method according to the present invention, a 2?-hydroxy-protected ribonucleoside derivative, which is an important intermediate for producing an oligonucleoside, can be easily produced with good regioselectivity from a nucleoside derivative of which 2?,3?-hydroxy groups are not protected.
    Type: Grant
    Filed: February 26, 2009
    Date of Patent: August 28, 2012
    Assignee: Kaneka Corporation
    Inventors: Hirofumi Maeda, Akio Fujii, Masaru Mitsuda
  • Publication number: 20120142626
    Abstract: Disclosed herein are 2?-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.
    Type: Application
    Filed: November 30, 2011
    Publication date: June 7, 2012
    Applicant: Pharmasset, Inc.
    Inventors: JINFA DU, Michael Joseph Sofia
  • Patent number: 8193339
    Abstract: This invention relates to a process of stereoselectively synthesizing a ?-nucleoside compound of formula (I): wherein R1, R2, and B are as defined in the specification; each of R3 and R4, independently, is H or fluoro. The process includes reacting, in the presence of a transition metal salt, a tetrahydrofuran compound of formula (II): wherein R1, R2, and L are as defined in the specification, with a nucleobase derivative; and each of R3 and R4, independently, is H or fluoro.
    Type: Grant
    Filed: November 6, 2008
    Date of Patent: June 5, 2012
    Assignee: Pharmaessentia Corp.
    Inventors: Chi-Yuan Chu, Wei-Der Lee, Wensen Li, Chan Kou Hwang
  • Patent number: 8188222
    Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose. [Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.
    Type: Grant
    Filed: November 6, 2007
    Date of Patent: May 29, 2012
    Assignee: Nippon Kayaku Kabushiki Kaisha
    Inventors: Keiichiro Yamamoto, Kazutoshi Takashio
  • Patent number: 8173797
    Abstract: The present invention is directed to new therapeutic compounds isolated from spider venom and methods of using these new compounds. The compounds are sulfated nucleoside derivatives including ribonucleoside mono- and disulfates derived from guanine, adenosine, and cytidine. Some of these compounds are glycosylated or fucosylated bearing one or more sugar residues.
    Type: Grant
    Filed: July 21, 2005
    Date of Patent: May 8, 2012
    Assignee: Cornell Research Foundation, Inc.
    Inventors: Jerrold Meinwald, Andrew Edmund Taggi, Frank Clemens Schroeder
  • Publication number: 20120107955
    Abstract: Results of studies of nucleosides in biofluid specimens from patients with esophageal adenocarcinoma and related disorders have identified five biomarkers of the conditions: 1-methyladenosine, N2,N2-dimethylguanosine, N2-methylguanosine, cytidine and uridine. In certain embodiments, methods of measuring these biomarkers and kits for measuring these biomarkers are provided.
    Type: Application
    Filed: September 6, 2011
    Publication date: May 3, 2012
    Applicant: Purdue Research Foundation
    Inventors: M. Daniel Raftery, Danijel Djukovic, Zane Hammoud
  • Patent number: 8163479
    Abstract: The invention relates to substrates for O6-alkylguanine-DNA alkyltransferases (AGT) of formula R1-A-X—CH2—R3—R4-L1, wherein A is a group recognized by AGT as a substrate, X is oxygen or sulfur, R1 is a group —R2-L2 or a group R5, R2 and R4 are, independently of each other, a linker, R3 is an aromatic or a heteroaromatic group, or an optionally substituted unsaturated alkyl, cycloalkyl or heterocyclyl group with the double bond connected to CH2, R5 is arylmethyl or heteroarylmethyl or an optionally substituted cycloalkyl, cycloalkenyl or heterocyclyl group, L1 is a label, a plurality of same or different labels, a bond connecting R4 to A forming a cyclic substrate, or a further group —R3—CH2—X-A-R1, and L2 is a label or a plurality of same or different labels. The invention further relates to methods of transferring a label from these substrates to O6-alkylguanine-DNA alkyltransferases (AGT) and AGT fusion proteins.
    Type: Grant
    Filed: March 1, 2005
    Date of Patent: April 24, 2012
    Assignee: Ecole Polytechnique Federale de Lausanne
    Inventors: Hughes Jaccard, Kai Johnsson, Maik Kindermann, India Christina Sielaff
  • Publication number: 20120095077
    Abstract: Disclosed are compositions and methods related to modified nucleobases. Also disclosed are compositions and methods related to modified interfering RNAs. Also disclosed are compositions and methods related to modified guanine bases for controlling off-target effects in RNA interference.
    Type: Application
    Filed: March 23, 2010
    Publication date: April 19, 2012
    Applicant: UNIVERSITY OF UTAH RESEARCH FOUNDATION
    Inventors: Cynthia J. Burrows, Arunkumar Kannan, Peter A. Beal
  • Publication number: 20120094948
    Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).
    Type: Application
    Filed: December 20, 2011
    Publication date: April 19, 2012
    Inventors: Giancarlo Naccari, Sergio Baroni
  • Publication number: 20120071646
    Abstract: There is a demand for a convenient production method of an NC type purine nucleoside. The present invention relates to a method of producing a purine nucleoside represented the formula (I?) or a salt thereof, which comprising reacting a pyrimidine nucleoside represented by the formula (I) or a salt thereof with a purine nucleobase represented by the formula B?H in the presence of a Lewis acid.
    Type: Application
    Filed: March 30, 2010
    Publication date: March 22, 2012
    Inventors: Tadashi Umemoto, Yoji Hayase, Shumpei Murata, Kenichi Miyata