The N-hetero Ring Is A Diazine Or A Diazole Ring, Including Hydrogenated Patents (Class 536/26.14)
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Publication number: 20150141365Abstract: The present invention relates to compounds of the formula I: including any possible stereoisomers thereof, wherein R9 has the meaning as defined herein, or a pharmaceutically acceptable salt or solvate thereof. The present invention also relates to processes for preparing said compounds, pharmaceutical compositions containing them and their use, alone or in combination with other HCV inhibitors, in HCV therapy.Type: ApplicationFiled: May 24, 2013Publication date: May 21, 2015Applicant: Janssen R&D IrelandInventors: Ioannis Nicolaos Houpis, Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Abdellah Tahri
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Publication number: 20140356325Abstract: Compositions and methods relating to 2?-C-methyl nucleoside 5?-monophosphate derivative compounds are provided. In some embodiments, the novel compounds are useful to treat viral infections. In particular, 2?-C-methyl nucleoside 5?-monophosphate derivative compounds, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of viral infection are described.Type: ApplicationFiled: January 8, 2013Publication date: December 4, 2014Applicant: Ligand Pharmaceuticals IncorporatedInventors: Lin Zhi, K. Raja Reddy, Mark David Erion, Scott Hecker
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Publication number: 20140303108Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.Type: ApplicationFiled: June 23, 2014Publication date: October 9, 2014Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
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Publication number: 20140206640Abstract: 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: ApplicationFiled: April 11, 2012Publication date: July 24, 2014Applicant: 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
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Patent number: 8772474Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.Type: GrantFiled: December 20, 2011Date of Patent: July 8, 2014Assignee: Alios BioPharma, Inc.Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
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Publication number: 20140161770Abstract: The present invention relates to 2?-Cyano 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?-Cyano Substituted Nucleoside Derivative, and methods of using the 2?-Cyano Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: April 11, 2012Publication date: June 12, 2014Applicant: MERCK SHARP & DOHME CORP.Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Angela Kerekes, Frank Bennett, Ying Huang, Latha Nair, Dmitri Pissarnitski, Vishal Verma, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
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Publication number: 20140155345Abstract: The invention provides new biotinylated compounds and methods for their use.Type: ApplicationFiled: December 4, 2013Publication date: June 5, 2014Applicant: Rutgers, the State University of New JerseyInventors: Roger A. Jones, Barbara L. Gaffney
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2'-SUBSTITUTED NUCLEOSIDE DERIVATIVES AND METHODS OF USE THEREOF FOR THE TREATMENT OF VIRAL DISEASES
Publication number: 20140154211Abstract: 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: ApplicationFiled: April 11, 2012Publication date: June 5, 2014Inventors: 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: 8742094Abstract: The invention relates to a method for producing phosphate-bridged nucleoside conjugates. In the method, a cyclosaligenyl nucleotide is produced first, to which a linker is added, which is used to perform the immobilization on a solid phase. A subsequent reaction with corresponding nucleophiles results in the desired phosphate-bridged nucleoside conjugates, which can then again be cleaved from the solid phase-bound linker.Type: GrantFiled: May 6, 2010Date of Patent: June 3, 2014Assignee: Universitaet HamburgInventors: Chris Meier, Viktoria Caroline Tonn
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Publication number: 20140099283Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 2?-chloro nucleosides according to Formula 2001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form or polymorphic form thereof, wherein B, Z and PD are as described herein.Type: ApplicationFiled: October 7, 2013Publication date: April 10, 2014Inventors: Gilles GOSSELIN, Christophe Claude PARSY, Francois-Rene ALEXANDRE, Houcine RAHALI, Jean-Francois GRIFFON, Julien MILHAU, Dominique SURLERAUX, Cyril B. DOUSSON, Claire PIERRA, Adel M. MOUSSA, Benjamin Alexander MAYES
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Publication number: 20130315864Abstract: The present invention provides nucleoside phosphoramidate compounds of Formula I, where R1, R2a, R2b, R3, R4, R5a, R5b, R6, R7, R8a, R8b, M and W are as defined herein. The invention further includes pharmaceutical compositions comprising a compound of Formula I, methods of use of these compounds for treating a viral infection, and methods of producing these compounds.Type: ApplicationFiled: May 17, 2013Publication date: November 28, 2013Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Yat Sun Or, Jun Ma, Guoqiang Wang
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Publication number: 20130315867Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: ApplicationFiled: May 21, 2013Publication date: November 28, 2013Inventors: Christophe Claude PARSY, Francois-Rene ALEXANDRE, Cyril B. DOUSSON, David DUKHAN, Gilles GOSSELIN, Houcine RAHALI, Dominique SURLERAUX
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Publication number: 20130178612Abstract: Chiral auxiliaries useful for efficiently producing a phosphorus atom-modified nucleic acid derivative with high stereoregularity, and compounds represented by the following the general formula (I) or the general formula (XI) for introducing the chiral auxiliaries.Type: ApplicationFiled: September 22, 2011Publication date: July 11, 2013Applicant: CHIRALGEN, LTD.Inventors: Takeshi Wada, Mamoru Shimizu
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Publication number: 20130165400Abstract: 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: ApplicationFiled: December 20, 2012Publication date: June 27, 2013Applicant: ALIOS BIOPHARMA, INC.Inventor: Alios BioPharma, Inc.
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Publication number: 20120269725Abstract: Method of using androgen receptor and/or butyrylcholinesterase targeted radiolabeled compounds, e.g., cycloSalingenyl pyrimidine nucleoside monophosphates, for the treatment and diagnosis of cancer.Type: ApplicationFiled: December 23, 2010Publication date: October 25, 2012Inventors: Janine Baranowska-Kortylewicz, Zbigniew P. Kortylewicz
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Publication number: 20120263678Abstract: Provided are compounds of Formula I: nucleosides, nucleoside phosphates and prodrugs thereof, wherein R6 is CN, ethenyl, 2-haloethen-1-yl, or (C2-C8)-alkyn-1-yl. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections.Type: ApplicationFiled: April 13, 2012Publication date: October 18, 2012Applicant: GILEAD SCIENCES, INC.Inventors: Aesop Cho, Choung U. Kim, Thorsten A. Kirschberg, Michael R. Mish, Neil Squires
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Publication number: 20120258928Abstract: Cyclic phosphate of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof, represented by the following structure:Type: ApplicationFiled: April 5, 2012Publication date: October 11, 2012Applicant: GILEAD PHARMASSET LLCInventors: JINFA DU, DHANAPALAN NAGARATHNAM, GANAPATI REDDY PAMULAPATI, BRUCE S. ROSS, MICHAEL JOSEPH SOFIA
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Publication number: 20120237480Abstract: 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: ApplicationFiled: March 16, 2012Publication date: September 20, 2012Inventors: YAT SUN OR, Jun Ma, Guoqiang Wang, In Jong Kim, Jiang Long, Yao-Ling Qiu
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Publication number: 20120157511Abstract: The present invention provides nucleosides and oligonucleotides comprising a 5? phosphate mimics of formula (IVc) or (Vc). One aspect of the present invention relates to modified nucleosides and oligonucleotides comprising such dinucleotide of formula (Ia). Another aspect of the invention relates to a method of inhibiting the expression of a gene in call, the method comprising (a) contacting an oligonucleotide of the invention with the cell; and (b) maintaining the cell from step (a) for a time sufficient to obtain degradation of the mRNA of the target gene.Type: ApplicationFiled: July 7, 2010Publication date: June 21, 2012Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Marija Prhavc, Ivan Zlatev
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Publication number: 20120116067Abstract: The invention relates to a method for producing phosphate-bridged nucleoside conjugates. In the method, a cyclosaligenyl nucleotide is produced first, to which a linker is added, which is used to perform the immobilization on a solid phase. A subsequent reaction with corresponding nucleophiles results in the desired phosphate-bridged nucleoside conjugates, which can then again be cleaved from the solid phase-bound linker.Type: ApplicationFiled: May 6, 2010Publication date: May 10, 2012Applicant: UNIVERSITAET HAMBURGInventors: Chris Meier, Viktoria Caroline Tonn
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Patent number: 8148349Abstract: The present invention provides nucleoside cyclic phosphoramidates of formula (I), pharmaceutical compositions comprising the compounds of formula (I) and methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection using the compounds of formula (I).Type: GrantFiled: December 14, 2007Date of Patent: April 3, 2012Assignees: Istituto di Ricerche di Biologia Molecolare P. Angeletti S.P.A., Merck Sharp & Dohme Corp.Inventors: Malte Meppen, Frank Narjes, Barbara Pacini, Cristina Gardelli, Philippe L. Durette
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Publication number: 20120070415Abstract: 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: ApplicationFiled: September 19, 2011Publication date: March 22, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
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Publication number: 20120039845Abstract: Compounds having the formula I or II, wherein R1, R2, B, and V are as defined herein, are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: October 26, 2011Publication date: February 16, 2012Applicant: METABASIS THERAPEUTICS, INC.Inventors: Scott J. HECKER, K. Raja REDDY, Zhili SUN, Brett C. BOOKSER, David Bernard SMITH
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Publication number: 20110028705Abstract: The present invention relates to a method for stereoselective synthesis of phosphorus compounds, whereby in the first reaction step a chiral auxiliary on the phosphorus atom of phosphoryl chloride, thiophosphoryl chloride or phosphorus trichloride is covalently bonded, the product from the first reaction step is reacted in the following step with an alcohol, thiol, or amine as the nucleophile in the presence of a base, and in the last step the chiral auxiliary is displaced from the product of the following step by a nucleophile.Type: ApplicationFiled: April 3, 2009Publication date: February 3, 2011Applicant: UNIVERSITAET HAMBURGInventors: Chris Meier, Jens O. Thomann
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Publication number: 20100305060Abstract: This application provides compositions or compounds as disclosed herein that are suitable for treating hepatic viral diseases, such as hepatitis C(HCV).Type: ApplicationFiled: November 26, 2008Publication date: December 2, 2010Applicant: Ligand Pharmaceuticals IncorporatedInventors: Scott J. Hecker, K. Raja Reddy
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Publication number: 20100297079Abstract: The present invention describes compounds of formulae I and II and methods for treating viral infection, such as Flaviviridae virus infection, including Hepatitis C infection (HCV).Type: ApplicationFiled: May 20, 2010Publication date: November 25, 2010Applicant: Chimerix, Inc.Inventors: Merrick Almond, Ernest R. Lanier, David L. Musso, Roy Ware
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Publication number: 20100068179Abstract: The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, and n is an integer between 2 and 20, processes for the production thereof and uses theroef, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.Type: ApplicationFiled: November 24, 2009Publication date: March 18, 2010Applicant: Institut National de la Sante et de la Recherche MedicaleInventors: Christian Belmant, Jean-Jacques Fournie, Marc Bonneville, Marie-Alix Peyrat
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Publication number: 20100022468Abstract: The present invention provides nucleoside cyclic phosphoramidates of structural formula (I) which are precursors to inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors to inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as pre-cursors to inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors to inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside cyclic phosphoramidates alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside cyclic phosphoramidates of the present invention.Type: ApplicationFiled: December 14, 2007Publication date: January 28, 2010Inventors: Malte Meppen, Frank Narjes, Barbara Pacini, Cristina Gardelli, Philippe L. Durette
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Publication number: 20090317361Abstract: Provided are imidazo[1,5-f][1,2,4]triazinyl, imidazo[1,2-f][1,2,4]triazinyl, and [1,2,4]triazolo[4,3-f][1,2,4]triazinyl nucleosides, nucleoside phosphates and prodrugs thereof. The compounds, compositions, and methods provided are useful for the treatment of Flaviviridae virus infections, particularly hepatitis C infections.Type: ApplicationFiled: April 22, 2009Publication date: December 24, 2009Applicant: Gilead Sciences, Inc.Inventors: Aesop Cho, Choung U. Kim, Jay Parrish, Jie Xu
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Publication number: 20090209481Abstract: Compounds having the formula I or II wherein R1, R2, B, and V are as defined herein are Hepatitis C virus NS5b polymerase inhibitors. Also disclosed are compositions and methods for treating an HCV infection and inhibiting HCV replication.Type: ApplicationFiled: November 26, 2008Publication date: August 20, 2009Inventors: Scott J. Hecker, K. Raja Reddy, Zhili Sun, Brett C. Bookser, David Bernard Smith
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Publication number: 20090118223Abstract: Novel 2?-C-methyl nucleoside 5?-monophosphate and 4?-C-methyl nucleoside 5?-monophosphate derivatives, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described.Type: ApplicationFiled: August 14, 2006Publication date: May 7, 2009Inventors: Mark D. Erion, K. Raja Reddy, Malcolm MacCoss, David B. Olsen
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Publication number: 20090117041Abstract: Disclosed are certain cycloSalingenyl pyrimidine nucleoside monophosphates comprising positron emitters or gamma-emitting radiohalides, uses thereof for monitoring Alzheimer's disease progression and evaluating response to therapy and process for their preparation.Type: ApplicationFiled: August 8, 2008Publication date: May 7, 2009Inventors: Zbigniew P. Kortylewicz, Janina Baranowska-Kortylewicz
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Publication number: 20030176392Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.Type: ApplicationFiled: December 19, 2002Publication date: September 18, 2003Inventors: Raymond F. Schinazi, Junxing Shi, Joyce D. Fingeroth, Erik Gustafson
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Publication number: 20030130213Abstract: Pyrazine derivatives represented by general formula [1]: 1Type: ApplicationFiled: August 16, 2002Publication date: July 10, 2003Applicant: Toyama Chemical Co., Ltd.Inventors: Hiroyuki Egawa, Yousuke Furuta, Jun Sugita, Sayuri Uehara, Shoichi Hamamoto, Kenji Yonezawa
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Publication number: 20030040502Abstract: Inosine compounds, compositions comprising an inosine compound and methods for treating or preventing an inflammation disease or a reperfusion disease comprising administering an effective amount of an inosine compound to a patient in need thereof are disclosed.Type: ApplicationFiled: March 26, 2002Publication date: February 27, 2003Applicant: Inotek Pharmaceuticals CorporationInventors: Andrew L. Salzman, Csaba Szabo
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Publication number: 20020160980Abstract: A method for the treatment for hepatitis delta infection in a host, that includes administering an effective amount of a nucleoside or a nucleoside analog that suppresses the expression of the hepatitis B surface or preS1 antigen in the host 100-fold or more relative to pretreatment values in vivo; or to not more than 1 microgram per milliliter in vivo. In a preferred embodiment, the nucleoside is L-FMAU, or a pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: March 29, 2001Publication date: October 31, 2002Inventors: John L. Casey, Brent E. Korba, Paul J. Cote, John L. Gerin, Bud C. Tennant, Chung K. Chu
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Publication number: 20020102590Abstract: Provided are nucleotide-dye conjugates and related compounds in which a dye is linked to a nucleobase directly or indirectly by an anionic linker. The anionic character of the linker is provided by one or more anionic moieties which are present in the linker, such as phosphate, phosphonate, sulfonate, and carboxylate groups. When the dye is a provided as a donor/acceptor dye pair, the anionic linker can be located between the donor and the acceptor, or between the nucleobase and either the donor or acceptor, or both. In one embodiment, conjugates of the invention provide enhanced electrophoretic mobility characteristics to sequencing fragments, e.g., for dideoxy sequencing using labeled terminators.Type: ApplicationFiled: October 11, 2001Publication date: August 1, 2002Applicant: PE Corporation (NY)Inventors: Meng Taing, Shaheer H. Khan, Steven M. Menchen, Barnett B. Rosenblum
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Publication number: 20020025922Abstract: Contraceptive activity as well as anti-viral protection can be provided by contraceptive compositions containing a pyrimidine-based nucleoside or nucleotide exhibiting spermicidal or sperm-immobilizing activity. In one example, the active ingredient contains a thymine ring (e.g. AZT) that has 5-halo, 6-alkoxy substitution. Additional improvements in anti-HIV activity for certain AZT derivatives are seen by providing the pentose ring of AZT with aryl phosphate substitution.Type: ApplicationFiled: December 1, 2000Publication date: February 28, 2002Inventors: Osmond D'Cruz, Fatih M. Uckun, Taracad Venkatachalam
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Patent number: RE38416Abstract: This invention is directed to novel substituted nucleotide bases with a crosslinking arm which accomplish crosslinking between specific sites on adjoining strands of oligonucleotides a oligodeoxynucleotides. The invention is also directed to oligonucleotides comprising at least one of these crosslinking agents and to the use of the resulting novel oligonucleotides for diagnostic and therapeutic purposes.Type: GrantFiled: October 19, 2000Date of Patent: February 3, 2004Assignee: Epoch Biosciences, Inc.Inventors: Charles R. Petrie, Rich B. Meyer, John C. Tabone, Gerald D. Hurst