Chalcogen Bonded Directly To The 2- And 4-positions Of The Diazine Ring (e.g., Uridine, Etc.) Patents (Class 536/28.53)
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Publication number: 20110053154Abstract: 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: ApplicationFiled: June 21, 2010Publication date: March 3, 2011Applicant: TwistDx, Inc.Inventors: Olaf Piepenburg, Derek L. Stemple, Niall A. Armes
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Publication number: 20110039798Abstract: The present invention relates to fatty acid and fatty alcohol substituted nucleoside derivatives and nucleoside and nucleoside derivatives substituted on multivalent scaffolds (e.g., polymers, peptides, polycarboxylic acid substituted compounds, compounds containing polycycloSaligenyl groups) that display potent anti-HIV activity. Furthermore, they show enhanced activity against multi-drug resistant, R5, and cell-associated virus. Some of them also display activity against other sexually transmitted pathogens and sperm. The present invention provides their methods of synthesis, composition of matter, and methods of use. Emphasis is placed on their application as topical microbicides to treat or prevent sexual transmission of disease, especially HIV/AIDS.Type: ApplicationFiled: July 9, 2008Publication date: February 17, 2011Applicant: EASTERN VIRGINIA MEDICAL SCHOOLInventors: Gustavo F. Doncel, Keykavous Parang, Hitesh Kumar Agarwal
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Publication number: 20110040083Abstract: The present invention provides a manufacturing method that can easily manufacture a compound known as photoresponsive (photocoupling) nucleic acids at high yield in a shorter period of time than that of the conventional technology. The present invention relates to a method of manufacturing a photoresponsive nucleic acid which includes a step of reacting a nucleic acid having groups represented by the Formula I, the Formula III, the Formula IV, or the Formula V and a compound represented by the Formula II, or reacting a nucleic acid having groups represented by the Formula VI, the Formula VIII, the Formula IX, or the Formula X and a compound represented by the Formula VII by heating them by microwaves in the presence of a metal catalyst, a basic substance, and a solvent.Type: ApplicationFiled: February 13, 2009Publication date: February 17, 2011Applicant: JAPAN SCIENCE AND TECHNOLOGY AGENCYInventors: Kenzo Fujimoto, Masayuki Ogino, Yoshinaga Yoshimura
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Publication number: 20110021454Abstract: 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: ApplicationFiled: September 26, 2006Publication date: January 27, 2011Applicant: Pharmasset, Inc.Inventors: Jinfa Du, Phillip Furman, Michael Joseph Sofia
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Publication number: 20110015147Abstract: A compound of formula (I) wherein Ar can be one six-membered or two fused six-membered aromatic rings; R8 and R9 can be hydrogen, alkyl, cycloalkyl, halogens, amino, alkylamino, dialkylamino, nitro, cyano, alkyoxy, aryloxy, thiol, alkylthiol, arythiol, or aryl; Q can be O, S or CY2, where Y may be H, alkyl or halogens; X can be O, NH, S, N-alkyl, (CHR2)m where m is 1 to 10, and CY2; Z can be O, S, NH, or N-alkyl; U? is H and U? can be H or CH2; wherein: T can be OH, H, halogens, O-alkyl, O-acyl, O-aryl, CN, NH2. or N3; T? and T? can be H or halogen; and W can be H or a phosphate group. Compounds show anti-viral activity, for example with respect to varicella zoster virus.Type: ApplicationFiled: September 24, 2010Publication date: January 20, 2011Inventors: Christopher MCGUIGAN, Jan BALZARINI
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Publication number: 20110009609Abstract: The present invention relates to a method for producing a 2?-hydroxy-protected nucleoside derivative by reacting a ribonucleoside with an acylating 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: ApplicationFiled: February 26, 2009Publication date: January 13, 2011Inventors: Hirofumi Maeda, Akio Fujii, Masaru Mitsuda
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Publication number: 20100330563Abstract: 1-(2-Fluoro-4-thio-?-D-arabinofuranosyl)-5-methyluracil exhibits an anti-EB virus activity, and is therefore effective as a prophylactic or therapeutic agent for a disease associated with an EB virus. Each of a plasmid capable of expressing EB virus-TK and a plasmid capable of expressing human-TK is introduced into a TK-defect cell, thereby producing two types of cells respectively having the plasmids introduced therein. By using the two types of cells, it is possible to screen a medicinal agent which has cytotoxicity against the cell having the plasmid capable of expressing EB virus-TK introduced therein but has no toxicity against the cell having the plasmid capable of expressing human-TK introduced therein. In this manner, it becomes possible to screen a medicinal agent which specifically exhibits an anti-EB virus activity.Type: ApplicationFiled: September 8, 2008Publication date: December 30, 2010Applicant: YAMASA CORPORATIONInventors: Eiichi Kodama, Masao Matsuoka, Noriyuki Ashida
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Publication number: 20100279968Abstract: The present invention relates to methods of treating viral disease using mutagenic nucleoside analogs.Type: ApplicationFiled: December 27, 2006Publication date: November 4, 2010Applicant: Koronis Pharmaceuticals, Inc.Inventors: Ling Li, Alexander Gall, Richard Daifuku
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Patent number: 7825239Abstract: 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: GrantFiled: January 20, 2010Date of Patent: November 2, 2010Assignee: Medivir ABInventors: Genadiy Kalyanov, Anna Winqvist
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Publication number: 20100272791Abstract: Provided is a composition comprising, as an active ingredient, at least one material selected from the group consisting of uridine and derivatives thereof which promote synthesis of hyaluronic acid in animal and human cell and body, and a pharmaceutical preparation containing the same. The composition and pharmaceutical preparation of the present invention is effective in the treatment and prevention of dry eye syndrome.Type: ApplicationFiled: July 8, 2010Publication date: October 28, 2010Applicant: MD BIOALPHA CO., LTD.Inventors: Myung-Gyu PARK, Min-Kyung KUON
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Patent number: 7803786Abstract: The present invention comprises pharmaceutical compositions comprising a co-crystal of an API and a co-crystal former, and methods of making and using the same.Type: GrantFiled: June 16, 2005Date of Patent: September 28, 2010Assignees: Transform Pharmaceuticals, Inc., University of South FloridaInventors: Jennifer McMahon, Matthew Peterson, Michael J. Zaworotko, Tanise Shattock, Magali Bourghol Hickey
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Patent number: 7776838Abstract: The subject invention discloses compounds, compositions and methods for treatment and prevention of toxicity due to chemotherapeutic agents and antiviral agents. Disclosed are acylated derivatives of non-methylated pyrimidine nucleosides. These compounds are capable of attenuating damage to the hematopoietic system in animals receiving antiviral or antineoplastic chemotherapy.Type: GrantFiled: June 2, 1995Date of Patent: August 17, 2010Assignee: Wellstat Therapeutics CorporationInventors: Reid W. von Borstel, Michael K. Bamat
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Patent number: 7772208Abstract: A method for the treatment or prevention of Flaviviridae infections, in particular, hepatitis C virus infection, in a host, and in particular, a human, is provided that includes administering an effective amount of a ?-L- or ?-D-2?,3?-dideoxynucleoside or a pharmaceutically acceptable salt or prodrug thereof, optionally in a pharmaceutically acceptable diluent or excipient.Type: GrantFiled: January 8, 2008Date of Patent: August 10, 2010Assignees: Pharmasset, Inc., Leland Stanford Junior University, Emory UniversityInventors: Raymond Schinazi, Robert Striker, Junxing Shi
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Publication number: 20100196273Abstract: Compounds for in vivo diagnostic imaging of cellular proliferation are provided. The compounds include L-nucleosides such as a 2?-deoxy-2?-fluoro-L-ara-binofuranosyl pyrimidine nucleoside analogue. These nucleosides are labeled with a positron emitting radioisotope. The present invention also provides a method for in vivo diagnostic imaging of cellular proliferation.Type: ApplicationFiled: February 11, 2008Publication date: August 5, 2010Inventors: Mian M. Alauddin, Uday Mukhopadhyay, Juri Gelovani, Ashutosh Pal, William Bornmann
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Patent number: 7759513Abstract: The present invention discloses novel and improved nucleosidic and nucleotidic compounds that are useful in the light-directed synthesis of oligonucleotides, as well as, methods and reagents for their preparation. These compounds are characterized by novel photolabile protective groups that are attached to either the 5?- or the 3?-hydroxyl group of a nucleoside moiety. The photolabile protective group is comprised of a 2-(2-nitrophenyl)-ethyoxycarbonyl skeleton with at least one substituent on the aromatic ring that is either an aryl, an aroyl, a heteroaryl or an alkoxycarbonyl group. The present invention includes the use of the aforementioned compounds in light-directed oligonucleotide synthesis, the respective assembly of nucleic acid microarrays and their application.Type: GrantFiled: January 26, 2004Date of Patent: July 20, 2010Assignee: NIGU Chemie GmbHInventors: Sigrid Bühler, Markus Ott, Wolfgang Pfleiderer
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Publication number: 20100179312Abstract: The present invention is directed to convertible nucleosides and polymer supported convertible nucleosides for use in SNAP displacement reactions. The convertible nucleosides can be used to synthesize numerous substituted purine and pyrimidine derivatives.Type: ApplicationFiled: October 12, 2007Publication date: July 15, 2010Inventors: Mahesh K. Lakshman, Suyeal Bae
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Publication number: 20100166780Abstract: The invention relates to oligonucleotides including at least one lipophilic substituted nucleotide analog and a pyrimidine-purine dinucleotide. The invention also relates to pharmaceutical compositions and methods of use thereof.Type: ApplicationFiled: September 27, 2007Publication date: July 1, 2010Inventors: Harald Debelak, Eugen Uhlmann, Marion Jurk
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Publication number: 20100160249Abstract: The use of squalenic acid or a derivative thereof in formulating at least one polar active principle with a molecular weight of 100 Da or more, in the form of nanoparticles, and pharmaceutical compositions thereof.Type: ApplicationFiled: March 4, 2010Publication date: June 24, 2010Applicants: Centre National De La Recherche Scientifique, Universite Paris-SudInventors: Patrick Couvreur, Barbara Stella, Luigi Cattel, Flavio Rocco, Jack-Michel Renoir, Véronique Rosilio
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Publication number: 20100143980Abstract: The present invention includes a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, the xyloside having a chemical structure of one of Formula (1), Formula (2), Formula (3), Formula (4), Formula (5), Formula (6), Formula (7), Formula (8), Formula (9), or Formula (10) as shown herein. Also, the present invention includes a method of making a xyloside for use in inducing synthesis of a glycosaminoglycan in a cell, wherein the method is performed with “Click” chemistry. Additionally, the present invention includes a method of administering a xyloside so as to induce synthesis of a glycosaminoglycan in a cell.Type: ApplicationFiled: February 15, 2008Publication date: June 10, 2010Inventors: Kuberan Balagurunathan, Ethirajan Manivannan, V. Victor Xylophone, Vy My Tran, Khiem Nguyen
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Publication number: 20100130735Abstract: 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: ApplicationFiled: January 20, 2010Publication date: May 27, 2010Applicant: Medivir ABInventors: Genadiy Kalyanov, Anna Winqvist
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Publication number: 20100130733Abstract: The present invention provides luminescent metal ion complexes for use in a wide range of biological and chemical studies. The luminescent metal ion complexes of the invention comprise a metal ion chelating component covalently bound to a carrier molecule. Also provided are methods of making and using the luminescent metal ion complexes.Type: ApplicationFiled: December 21, 2009Publication date: May 27, 2010Applicant: BIOSEARCH TECHNOLOGIES, INC.Inventors: RONALD M. COOK, MATT LYTTLE, MARY KATHERINE JOHANNSON
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Publication number: 20100113762Abstract: Methods and apparatus for facilitating the synthesis of compounds in a batch device are presented. Application of the batch type microfluidic devices to the synthesis of radiolabeled compounds is described. These methods and apparatus enable the selective introduction of multiple reagents via an enhanced rotary flow distribution valve through a single inlet port of the synthetic device. The sequential introduction of multiple reagents through a single inlet port allows an optimal delivery of highly concentrated reagents into the reactor and facilitates the synthesis of the desired products with a minimal loss of materials during transfers, which is critical to the synthesis of radiolabeled biomarkers.Type: ApplicationFiled: November 4, 2009Publication date: May 6, 2010Applicant: Siemens Medical Solutions USA, Inc.Inventors: Carroll Edward Ball, Arkadij M. Elizarov, Hartmuth C. Kolb, Reza Miraghaie, Jianzhong Zhang
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Publication number: 20100105888Abstract: The present invention relates to a process for separating a target radiolabelled compound from an impurity, apparatus for performing such a process and a removable cassette for use in such apparatus. Also provided are methods for using the target radiolabelled compound obtained by a method comprising the separating process of the invention.Type: ApplicationFiled: March 7, 2008Publication date: April 29, 2010Inventor: Mette Husbyn
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Patent number: 7704971Abstract: 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: GrantFiled: September 1, 2006Date of Patent: April 27, 2010Assignee: SmithKlineBeecham CorporationInventors: Thomas Spector, David J. T. Porter, Saad G. Rahim
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Patent number: 7691826Abstract: A polysialic acid compound is reacted with a hetero-bifunctional reagent to introduce a pendant functional group for site-specific conjugation to sulfhydryl groups, for instance side chains of cysteine units in drugs, drug delivery systems, proteins or peptides. The functional group is, for instance, an N-maleimide group.Type: GrantFiled: August 12, 2004Date of Patent: April 6, 2010Assignee: Lipoxen Technologies LimitedInventors: Dale Howard Hreczuk-Hirst, Sanjay Jain, Peter Laing, Gregory Gregoriadis, Ioannis Papaioannou
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Publication number: 20100081627Abstract: Disclosed are polymeric compounds which are useful as prodrugs, comprising a chain of monomeric nucleosides, nucleoside analogs or abasic nucleosides, wherein at least one of the nucleosides or nucleoside analogs or a heterocyclic derivative thereof is pharmaceutically active and the nucleosides, nucleoside analogs or abasic nucleosides are linked by a phosphodiester group, a phosphorothioate group or an H—, alkyl or alkenyl phosphonate group.Type: ApplicationFiled: October 2, 2009Publication date: April 1, 2010Applicant: RELIABLE BIOPHARMACEUTICAL, INC.Inventors: UmaShanker Sampath, Joseph A. Toce, Sourena Nadji
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Publication number: 20100056771Abstract: A compound of formula (A) or salt thereof: wherein each of R1, R2, and R3 independently represents hydrogen, alkyl, aryl, acyl, sulfonyl, or silyl; P represents hydrogen or a hydroxy protective group. This compound may be used an intermediate for making a 2-deoxy-2,2-difluoro-D-ribofuranosyl nucleosides, such as gemcitabine.Type: ApplicationFiled: August 31, 2009Publication date: March 4, 2010Applicant: ScinoPharm Taiwan Ltd.Inventors: Julian Paul Henschke, Yung Fa Chen, George Schloemer
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Publication number: 20090318556Abstract: Disclosed herein are biomarkers for determining gamma radiation exposure by an animal or human. The biomarkers include 3-hydroxy-2-methylbenzoic acid 3-O-sulfate, N-hexanoylglycine, ?-thymidine, taurine, xanthine, xanthosine, 2?-deoxyuridine, 2?-deoxycytidine, 2?-deoxyxanthosine, or any salt, ion, or combination thereof. Also disclosed are methods for determining gamma radiation exposure by an animal or human, which include the step of measuring the amount of one or more biomarkers specific to gamma radiation in the biological fluid and correlating the amount of said biomarkers to the amount of gamma radiation exposure by the animal or human. Systems for determining gamma radiation exposure by an animal or human and methods of treating an animal or human for gamma radiation exposure are also disclosed.Type: ApplicationFiled: May 15, 2008Publication date: December 24, 2009Inventors: Jeffrey R. Idle, Frank J. Gonzalez, John B. Tyburski, Kristopher W. Krausz, Andrew David Patterson
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Patent number: 7629447Abstract: The invention provides a 5?-amino-2?-fluoro-2?,5?-dideoxynucleoside compound represented by the formula [1]: wherein R1 represents a nucleic acid base which may have a protecting group; R2 represents a hydrogen atom or an amino protecting group; and R3 represents a hydrogen atom or a hydroxyl protecting group. The invention also provides a dideoxynucleoside-insoluble carrier bound substance and an oligonucleotide analogue involving the dideoxynucleoside compound.Type: GrantFiled: February 26, 2007Date of Patent: December 8, 2009Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Yukio Kitade, Yoshihito Ueno
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Publication number: 20090281054Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis are provided. In particular, methods and compositions comprising substituted derivatives of capuramycin analogs for the treatment of infectious diseases are provided. Also provided are capuramycin analogue formulations comprising PEGylated compounds, including a PEGylated vitamin E derivative, liposomes and nanoparticle carriers. The invention provides methods and compositions comprising a capuramycin analogue and capuramycin analogues in combination with one or more other active agents.Type: ApplicationFiled: December 10, 2008Publication date: November 12, 2009Inventors: Venkata Reddy, Marina Nikolaevna Protopopova, Elena Bogatcheva
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Publication number: 20090281301Abstract: The present invention relates to more improved process for preparing 2?-deoxy-2?,2?-difluoronucleoside and its intermediate. The present invention provide a process for preparing an erythro enantiomer in greater than 98% purity, comprising forming a lactone ring by hydrolyzing ethyl (3RS)-2,2-difluoro-3-hydroxy-3-(2,2-dimethyloxolan-4-yl)propionate is hydrolyzed in the presence of hydrolysis reagents selected from acetic acid or chloroacetic acid, water and a mixture of organic solvents selected from the group comprising acetonilrile, dioxane, tetrahydrofuran or toluene, introducing a substituted benzoyl protecting group at the 3-position and 5-position, and recrys- tallizing said erythro enantiomer. Further, the present invention provides a process for selectively preparing, in greater than 99% purity, a beta-anomer 2?-deoxy-2?,2?-difluoronucleoside at the 3?-position and 5?-position that are protected by a substituted benzoyl in a 2:3 alpha/beta anomeric ratio.Type: ApplicationFiled: December 11, 2006Publication date: November 12, 2009Applicant: DONG-A-PHARM.CO LTDInventors: Moon-Sung Kim, Yong-Jik Kim, Jun-Ho Choi, Hong-Gyu Lim, Dae-Won Cha
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Publication number: 20090258931Abstract: The present invention relates to novel chimeric oligomeric compounds having a plurality of alternating regions having either RNA like having northern or 3?-endo conformational geometry (3?-endo regions) or DNA like having southern or C2?-endo/O4?-endo conformational geometry. The oligomeric compounds of the present invention have shown reduction in mRNA levels in multiple in vitro and in vivo assay systems and are useful, for example, for investigative and therapeutic purposes.Type: ApplicationFiled: February 19, 2009Publication date: October 15, 2009Applicant: ISIS PHARMACEUTICALS, INC.Inventors: Brett P. Monia, Madeline M. Butler, Robert McKay, Brenda F. Baker
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Patent number: 7601702Abstract: Deoxyuridine derivatives of Formula (I?); where A is O, S or CH2; B is O, S or CHR3; R1 is H, or various substituents; R2 is H, F; R3 is H, F, OH, NH2; or R2 and R3 together form a chemical bond; D is —NHCO—, —CONH—, —O—, —C(?O)—, —CH?CH, —C?C—, —NR5—; R4 is hydrogen or various substituents; R5 is H, C1-C4 alkyl, C1-C4 alkanoyl; E is Si or C; R6, R7 and R8 are independently selected from C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, or a stable monocyclic, bicyclic or tricyclic ring system have utility in the prophylaxis of treatment of parasitic diseases such as malaria.Type: GrantFiled: January 6, 2005Date of Patent: October 13, 2009Assignee: Medivir ABInventors: Ian Gilbert, Corinne Nguyen, Gian Filippo Ruda, Alessandro Schipani, Ganasan Kasinathan, Nils-Gunnar Johansson, Dolores Gonzalez Pacanowska
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Patent number: 7598230Abstract: The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.Type: GrantFiled: June 14, 2007Date of Patent: October 6, 2009Assignee: Biota Scientific Management Pty LtdInventors: Phillip D. Cook, Guangyi Wang, Thomas W. Bruice, Nicholas A. Boyle, Janet M. Leeds, Jennifer L. Brooks, Marija Prhavc, Maria Eugenia Ariza, Patrick C. Fagan, Yi Jin, Vivek K. Rajwanshi, Kathleen D. Tucker
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Publication number: 20090233872Abstract: [Problems] To provide a neuronal cell death inhibitor and a therapeutic agent for a neurodegenerative disease, particularly Parkinson's disease. [Means for Solving Problems] It is known that DJ-1 protein is involved in Parkinson's disease and is capable of inhibiting neuronal cell death caused by oxidative stress. Based on this knowledge, screening is made for a low molecular weight molecule capable of binding to an active site of DJ-1 protein (i.e., a region around a cysteine residue at position-106) using an analysis softwear FastDock (Fujitsu Ltd.). When various tests are made using candidate low molecular weight compounds each having a binding energy of ?60 kcal/mol or lower, these compounds show a therapeutic effect on a neurodegenerative disease.Type: ApplicationFiled: November 17, 2006Publication date: September 17, 2009Applicant: National University Corporation Hokkaido UniversityInventor: Hiroyoshi Ariga
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Patent number: 7589078Abstract: The present invention relates to compounds according to the general formula: wherein B is or and the remaining variables are defined in the specification, and compositions comprising the compounds. The compounds are useful as anti-viral agents in viral therapy.Type: GrantFiled: February 18, 2004Date of Patent: September 15, 2009Assignee: Yale UniversityInventors: Yung-chi Cheng, Hiromichi Tanaka, Masanori Baba
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Patent number: 7585851Abstract: The present invention relates to compounds, compositions and methods for the treatment of a host infected with a hepatitis B virus. Specifically, compound and compositions of 3?-esters of 2?-deoxy-?-L-pyrimidine nucleosides are disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents. Compound and compositions of 3?,5?-diesters of 2?-deoxy-?-L-pyrimidine nucleosides are also disclosed, which can be administered either alone or in combination with other anti-hepatitis B agents.Type: GrantFiled: October 25, 2004Date of Patent: September 8, 2009Assignees: Idenix Pharmaceuticals, Inc., Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Martin L. Bryant, Gilles Gosselin, Jean-Louis Imbach
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Publication number: 20090209479Abstract: Aspects of the invention include 2? protected nucleoside monomers that are protected at the 2? site with thiocarbon protecting groups. Thiocarbon protecting groups of interest include thiocarbonate, thionocarbonate, dithiocarbonate groups, as well as thionocarbamate protecting groups. Aspects of the invention further include nucleic acids that include the protecting groups of the invention, as well as methods of synthesizing nucleic acids using the protecting groups of the invention.Type: ApplicationFiled: May 9, 2008Publication date: August 20, 2009Inventors: Douglas J. Dellinger, Agnieszka Sierzchala, John Turner, Joel Myerson, Zoltan Kupihar, Fernando Ferreira, Marvin H. Caruthers
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Patent number: 7560442Abstract: The present invention relates to novel uridine esters of the general formula (I) wherein R represents a carboxylic acid residue, preferably a fatty acid residue and R? represents hydrogen or a hydroxy group, their use as pharmaceutically active agents against a variety of diseases, methods for the preparation of said uridine esters and pharmaceutical compositions containing at least one uridine ester as active ingredient. The present invention relates also to a drug combination comprising free fatty acids and/or fatty acid esters and uridine, deoxyuridine, uridine monophosphate and/or deoxyuridine monophosphate, and to the use of such a drug combination.Type: GrantFiled: April 29, 2002Date of Patent: July 14, 2009Assignee: Trommsdorff GmbH & Co. KG ArzneimittelInventor: Rudy Susilo
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Patent number: 7550442Abstract: Compounds of formula (XXIII), or pharmaceutically acceptable salts or esters thereof, are inhibitors of reverse transcriptase: R4 is a nucleoside with Q substituting a 3? hydroxyl group, and Q is a moiety of formulas (XXIV)-(XXXII):Type: GrantFiled: May 19, 2004Date of Patent: June 23, 2009Assignee: The Board of Trustees of the University of IllinoisInventors: Raven H. Huang, Xianjun Liu
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Patent number: 7544794Abstract: This invention relates to the field of nucleic acid chemistry, more specifically to the field of compositions and processes that are nucleic acid analogs. More specifically, this invention relates to compositions that allow the sequencing of oligonucleotides by synthesis, and processes for sequencing by synthesis that exploit these compositions. Most specifically, the instant invention discloses compositions of matter that are 5?-triphosphates of ribo- and 2?-deoxyribonucleosides wherein the 3?-OH group is replaced by a 3?-ONHR group in the alpha configuration, wherein R is either a H or CH3 group. Also disclosed are these triphosphates where the nucleobase carries, via a linker, a reporter groups, such as a fluorescent species that can be used in single- or multi-copy DNA sequencing, or a tag that can be visualized by ultramicroscopy. Also disclosed are processes that use these compositions to do sequencing by synthesis.Type: GrantFiled: March 11, 2006Date of Patent: June 9, 2009Inventor: Steven Albert Benner
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Publication number: 20090137521Abstract: The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.Type: ApplicationFiled: October 16, 2008Publication date: May 28, 2009Inventors: Gregory S. Hamilton, Takashi Tsukamoto, Dana V. Ferraris, Bridget Duvall, Rena Lapidus
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Publication number: 20090130214Abstract: The invention concerns a 2?,2?-difluoro-2?-deoxycytidine derivative of general formula (I), wherein: R1, R2 and R3, identical or different, represent independently of one another, a hydrogen atom or an at least C18 hydrocarbon acyl radical and of such conformation that it is capable of providing the compound of general formula (I), a compacted form in a polar solvent medium, at least one of groups R1, R2 and R3 being other than a hydrogen atom.Type: ApplicationFiled: June 23, 2005Publication date: May 21, 2009Inventors: Patrick Couvreur, Barbara Stella, Luigi Cattel, Flavio Rocco, Jack-Michel Renoir, Veronique Rosilio
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Publication number: 20090124796Abstract: Provided is a simple and efficient production process of a nucleobase having a perfluoroalkyl group. A nucleobase (for example, uracils, cytosines, adenines, guanines, hypoxanthines, xanthines, or the like) is reacted with a perfluoroalkyl halide in the presence of a sulfoxide, a peroxide and an iron compound to produce a perfluoroalkyl-substituted nucleobase, which is useful as an intermediate for medical drugs, economically.Type: ApplicationFiled: November 6, 2006Publication date: May 14, 2009Inventors: Tetsu Yamakawa, Kyoko Yamamoto, Daisuke Uraguchi, Kenji Tokuhisa
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Publication number: 20090118224Abstract: To provide a novel anti-psychosocial stress agent which is highly safety and can be continuously taken, more particularly, a novel anti-psychosocial stress agent which prevents or alleviates psychosocial stress. The invention provides an anti-psychosocial stress agent containing, as an active ingredient, uridylic acid, uridine, or uracil. Since uridylic acid, uridine, or uracil, which is an active ingredient of the anti-psychosocial stress agent of the present invention, is inexpensively available and is a biological component, the agent exhibits high safety and can be continuously taken. Therefore, the anti-psychosocial stress agent of the present invention is effective for mitigating, alleviating, or relieving psychosocial stress, which is an issue in modern society. When the anti-psychosocial stress agent is taken before development of symptoms associated with psychosocial stress, the symptoms can be prevented.Type: ApplicationFiled: June 26, 2007Publication date: May 7, 2009Applicant: YAMASA CORPORATIONInventors: Kazuki Endo, Noriyuki Ashida
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Publication number: 20090099105Abstract: This invention relates to cytidine deaminase inhibitors (Cytidine deaminase inhibitors) of cytidine deaminases and uses thereof.Type: ApplicationFiled: May 6, 2005Publication date: April 16, 2009Inventors: Joseph E. Wedekind, Harold C. Smith
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Publication number: 20090068751Abstract: Dibenzorhodamine compounds having the structure are disclosed, including nitrogen- and aryl-substituted forms thereof. In addition, two intermediates useful for synthesizing such compounds are disclosed, a first intermediate having the structure including nitrogen- and aryl-substituted forms thereof, and a second intermediate having the structure including nitrogen- and aryl-substituted forms thereof, wherein substituents at positions C-14 to C18 taken separately are selected from the group consisting of hydrogen, chlorine, fluorine, lower alkyl, carboxylic acid, sulfonic acid, —CH2OH, alkoxy, phenoxy, linking group, and substituted forms thereof. The invention further includes energy transfer dyes comprising the dibenzorhodamine compounds, nucleosides labeled with the dibenzorhodamine compounds, and nucleic acid analysis methods employing the dibenzorhodamine compounds.Type: ApplicationFiled: July 8, 2008Publication date: March 12, 2009Applicant: Applied Biosystems Inc.Inventors: Scott C. BENSON, Joe Y.L. Lam, Steven Michael Menchen
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Publication number: 20090036659Abstract: To provide a method for efficiently and industrially deuterating the benzyl position of a —O-benzyl group formed by introducing a benzyl group, a benzyloxymethyl group and the like as a protecting group. The deuteration method for the benzyl position of a —O-benzyl group of a compound having the —O-benzyl group which may have a substituent, comprising reacting the compound with a heavy hydrogen source in the coexistence of a palladium/carbon-ethylenediamine complex and hydrogen.Type: ApplicationFiled: March 2, 2007Publication date: February 5, 2009Applicant: WAKO PURE CHEMICAL INDUSTRIES, LTD.Inventors: Hironao Sajiki, Tomohiro Maegawa, Takanori Kurita
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Publication number: 20090004137Abstract: The invention relates to the use of an uridine derivative of formula (I); wherein —R1 represents monohalogenated alkynyl or dihalogenated alkenyl; —R2 is chosen from among hydrogen, hydroxyl, O-alkyl, O—CO alkyl and halogen; —R3 is chosen from among hydrogen, hydroxyl, O-alkyl, O—CO alkyl, halogen, SH, S-alkyl and N3; and —R4 is chosen from among hydroxyl, O-alkyl, O—CO alkyl, O-phosphate, O-diphosphate, O-triphosphate and O phosphonate, as well as its possible tautomers, its possible pharmaceutically acceptable addition salts with an acid or a base, and its N-oxide forms, for the preparation of a drug having antiviral activity against a Flaviviridae.Type: ApplicationFiled: December 22, 2005Publication date: January 1, 2009Applicants: Institute National De La Sainte Et De La Rechderche Medicale, Centre National De La Recherche SceintifiqueInventors: Vincent Aucagne, Vanessa Escuret, Fabien Zoulim, David Durantel, Christian Trepo, Luigi Agrofoglio, Nicolas Joubert, Franck Amelard
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Publication number: 20080311186Abstract: Provided is a composition comprising, as an active ingredient, at least one material selected from the group consisting of uridine and derivatives thereof which promote synthesis of hyaluronic acid in animal and human cell and body, and a pharmaceutical preparation containing the same. The composition and pharmaceutical preparation of the present invention is effective in the treatment and prevention of dry eye syndrome.Type: ApplicationFiled: November 18, 2006Publication date: December 18, 2008Applicant: MD BIOALPHA CO., LTD.Inventors: Myung-Gyu Park, Min-Kyung Kuon