Nitrogen, Other Than Nitro Or Nitroso, Bonded Directly To The 4-position, And Chalcogen Bonded Directly To The 2-position Of The Diazine Ring (e.g., Cytidines, Etc.) Patents (Class 536/28.5)
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Patent number: 8461124Abstract: 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: GrantFiled: March 11, 2008Date of Patent: June 11, 2013Inventor: Jyoti Chattopadhyaya
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Publication number: 20130131147Abstract: Provided herein are 2?-amino and 2?-thio bicyclic nucleosides and oligomenc compounds prepared therefrom. The novel bicyclic nucleosides provided herein are expected to be useful for enhancing one or more properties of the oligomeric compounds they are incorporated into such as nuclease resistance.Type: ApplicationFiled: June 2, 2011Publication date: May 23, 2013Applicant: ISIS PHARMACEUTICALS, INC.Inventors: Punit P. Seth, Thazha P. Prakash, Eric E. Swayze
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Publication number: 20130116209Abstract: The subject invention relates to determining the presence and level of hENT1 expression in tumor tissue that is appropriate for gemcitabine therapy, and more importantly, the level of hENT1 expression that signifies that treatment with a gemcitabine derivative is a more appropriate strategy.Type: ApplicationFiled: August 2, 2012Publication date: May 9, 2013Applicants: VENTANA MEDICAL SYSTEMS, INC., CLOVIS ONCOLOGY, INC.Inventors: Jeffrey Dean Isaacson, Mical Raponi, James Ranger-Moore, Eric L. Powell
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Patent number: 8415321Abstract: A method and composition for treating a host infected with a Caliciviridae virus, such as a Norovirus, comprising administering an effective treatment amount of a described modified nucleoside or a pharmaceutically acceptable salt thereof, is provided.Type: GrantFiled: April 9, 2009Date of Patent: April 9, 2013Inventors: Raymond F. Schinazi, Richard Anthony Whitaker, Tamara Rosario McBrayer, Steven J. Coats
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Publication number: 20130072462Abstract: The present invention provides a compound of Formula 1a, wherein R1 is H or phosphate and the double bond is between N? and C? or between N2 and C1; R2 is a mitochondrial targeting moiety; R3 an alkyl, alkylaryl, alkylheteroaryl spacer group, a cleavable linker, or absent; R4 is H or an alkyl, aryl, or heteroaryl group; and R5 is alkyl, aryl, or heteroaryl; or N? C?, and N3 together form a heterocyclic ring containing at least 5 atoms, wherein N1, N3, and R1-R5 are as defined above, or N3 and R5 together form a heterocyclic ring containing at least four atoms; or a pharmaceutically acceptable salt or prodrug thereof.Type: ApplicationFiled: August 17, 2012Publication date: March 21, 2013Applicant: Gencia CorporationInventor: Shaharyar Khan
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Publication number: 20130052710Abstract: 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: ApplicationFiled: February 18, 2011Publication date: February 28, 2013Applicant: RIKENInventors: Shinji Ogasawara, Mizuo Maeda
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Publication number: 20130045475Abstract: 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: October 23, 2012Publication date: February 21, 2013Applicant: ALERE SAN DIEGO, INC.Inventor: Alere San Diego, Inc.
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Patent number: 8377905Abstract: Disclosed is a stable crystal of 1-(2?-cyano-2?-deoxy-?-D-arabinofuranosyl)cytosine monohydrochloride. There is provided a crystal of 1-(2?-cyano-2?-deoxy-?-D-arabinofuranosyl)cytosine monohydrochloride having characteristic peaks at 13.7°, 15.7°, 16.0°, 18.6°, 20.3°, and 22.7° as diffraction angles (2?±0.1°) measured by powder X-ray diffraction, and having a melting point of 192° C. to 197° C.Type: GrantFiled: May 14, 2010Date of Patent: February 19, 2013Assignee: Delta-Fly Pharma, Inc.Inventors: Shotaro Watanabe, Takahiro Hatakeyama
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Publication number: 20130040907Abstract: Described herein are compounds useful in the modulation of blood uric acid levels, formulations containing them and methods of making and using them. In some embodiments, the compounds described herein are used in the treatment or prevention of disorders related to aberrant levels of uric acid.Type: ApplicationFiled: May 4, 2012Publication date: February 14, 2013Applicant: Ardea Biosciences Inc.Inventors: Esmir GUNIC, Jean-Luc GIRARDET, Jean-Michel VERNIER, Martina E. TEDDER, David A. PAISNER
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Publication number: 20130017171Abstract: 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: ApplicationFiled: September 20, 2012Publication date: January 17, 2013Applicants: UNIVERSITA DEGLI STUDI DI CAGLIARI, IDENIX PHARMACEUTICALS, INC.Inventors: Idenix Pharmaceuticals, Inc., Universita Degli Studi di Cagliari
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Patent number: 8350023Abstract: The present application provides several crystalline forms of gemcitabine base and methods of making the same.Type: GrantFiled: June 12, 2009Date of Patent: January 8, 2013Assignee: ScnioPharm Taiwan, Ltd.Inventors: Shu-Ping Chen, Chia-Lin Charlene Shieh
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Publication number: 20120322755Abstract: This invention provides a cytosine analogue, a method of preparation of a cytosine analogue, a DNA rhethyltransferase 1 inhibitor, a method for DNA methylation inhibition, the use of the analogue in the treatment of diseases associated with deviations from normal DNA methylation. More precisely, the invention relates to various derivatives of cytosine, as well as methods of preparation of mono- and multi-1,4,5 and 6-substituted cytosines. In general, the solution relates to providing effective modulators of DNA methylation which could be used in prevention and treatment of diseases associated with DNA methylation level disorders.Type: ApplicationFiled: March 17, 2011Publication date: December 20, 2012Applicant: INSTYTUT CHEMII BIOORGANICZNEJ PANInventors: Jan Barciszewski, Wojciech T. Markiewicz, Ewelina Adamska, Beata Plitta, Malgorzata Giel-Pietraszuk, Eliza Wyszko, Maria Markiewicz, Agnieszka Fedoruk-Wyszomirska, Tadeusz Kulinski, Marcin Chmielewski
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Publication number: 20120309705Abstract: 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: ApplicationFiled: December 14, 2010Publication date: December 6, 2012Applicant: NOVADEX PHARMACEUTICALS ABInventors: Xiao Xiong Zhou, Staffan Torssell, Olov Wallner, Piaoyang Sun
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Patent number: 8324373Abstract: The present invention provides a novel and highly stereoselective process for preparing gemcitabine, which is suitable for industrial production, wherein, it includes the following reactions. Additionally, the invention discloses the key intermediates. The definition for the groups of G1, G2, G3, G4, and G5 are described in the specification.Type: GrantFiled: September 7, 2007Date of Patent: December 4, 2012Assignee: Nanjing Cavendish Bio-Engineering Technology Co., Ltd.Inventors: Yongxiang Xu, Hao Yang, Wen Hou
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Publication number: 20120301902Abstract: The present invention comprises novel conjugates and immunogens derived from gemcitabine and unique antibodies generated by using gemcitabine linked immunogens, which conjugates immunogens and antibodies, are useful in immunoassays for the quantification and monitoring of gemcitabine in biological fluids.Type: ApplicationFiled: June 14, 2011Publication date: November 29, 2012Inventors: Salvatore J. Salamone, Jodi Blake Courtney, Howard Sard, Christopher Spedaliere
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Publication number: 20120301901Abstract: The present invention comprises novel analogs of gemcitabine and novel gemcitabine immunogens leased out of, i.e., derived from, the 5?-hydroxy position of gemcitabine. The invention also comprises unique monoclonal antibodies generated using gemcitabine linked immunogens as well as unique conjugates and tracers which antibodies, conjugates, and tracers are useful in immunoassays for the quantification and monitoring of gemcitabine in biological fluids.Type: ApplicationFiled: May 24, 2011Publication date: November 29, 2012Inventors: Salvatore J. Salamone, Jodi Blake Courtney, Howard Sard, Christopher Spedaliere
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Patent number: 8299239Abstract: Disclosed is the preparation of 2-deoxy-D-erythro-2,2-difluoro-ribofuranose-3,5-dibenzoate, a known intermediate for the preparation of Gemcitabine, by means of a reduction process; further disclosed is the purification of Gemcitabine by chromatography and the purification of Gemcitabine hydrochloride by crystallization techniques from ternary solvent mixtures. The main advantage of the invention is providing Gemcitabine hydrochloride with purity in conformity with the Pharmacopoeia requirements, as well as a process particularly convenient from the industrial point of view.Type: GrantFiled: October 21, 2009Date of Patent: October 30, 2012Assignee: Prime European Therapeucials S.p.A.Inventors: Alberto Varalli, Paolo Anesa, Maria Argese, Giuseppe Guazzi
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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: 20120259106Abstract: A process of stereoselectively synthesizing ?-nucleoside, e.g., 2?-deoxy-2,2?-difluorocytidine, is described. The process includes reacting a tetrahydrofuran compound of the following formula: in which wherein R1, R2, R3, R4, and L as defined in the specification, with a nucleobase derivative in the presence of an oxidizing agent.Type: ApplicationFiled: March 30, 2012Publication date: October 11, 2012Applicant: PharmaEssentia Corp.Inventors: Chungsun Chien, Pin-Shu Chien, Chan-Kou Hwang
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Publication number: 20120252751Abstract: The present invention relates to novel compounds according to the general formulas I, II, III, IV or V: wherein B is nucleoside base according to the structure: and the remaining variables as defined in the specification, and pharmaceutical compositions comprising the compounds. The compounds are useful interalia as anti-viral agents in viral therapy.Type: ApplicationFiled: May 7, 2012Publication date: October 4, 2012Inventors: Yung-chi Cheng, Hiromichi Tanaka, Masanori Baba
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Publication number: 20120245335Abstract: 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: ApplicationFiled: June 7, 2012Publication date: September 27, 2012Applicant: GILEAD PHARMASSET LLCInventor: Jeremy Clark
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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: 20120232029Abstract: 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: ApplicationFiled: December 13, 2011Publication date: September 13, 2012Applicant: Pharmasset, Inc.Inventors: MICHAEL JOSEPH SOFIA, Jinfa Du
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Publication number: 20120220922Abstract: The present invention describes Photolabile Compounds methods for use of the compounds. The Photolabile Compounds have a photoreleasable ligand, which can be biologically active, and which is photoreleased from the compound upon exposure to light. In some embodiments, the Photolabile Compounds comprise a light antenna, such as a labeling molecule or an active derivative thereof. In one embodiment, the light is visible light, which is not detrimental to the viability of biological samples, such as cells and tissues, in which the released organic molecule is bioactive and can have a therapeutic effect. In another embodiment, the photoreleasable ligand can be a labeling molecule, such as a fluorescent molecule.Type: ApplicationFiled: December 23, 2011Publication date: August 30, 2012Applicants: Universidad de Buenos Aires, THE TRUSTEES OF COLUMBIA UNIVERSITY IN THE CITY OF NEW YORKInventors: Rafael YUSTE, Roberto Etchenique, Luis Baraldo
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Patent number: 8252919Abstract: 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: GrantFiled: February 26, 2009Date of Patent: August 28, 2012Assignee: Kaneka CorporationInventors: Hirofumi Maeda, Akio Fujii, Masaru Mitsuda
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Patent number: 8242258Abstract: Aspects of the invention include 2? protected nucleoside monomers that are protected at the 2? site with orthoester-type protecting groups. The 2? protected monomers also include a second, aryl carbonate-type, protecting group. 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: GrantFiled: December 3, 2007Date of Patent: August 14, 2012Assignees: Agilent Technologies, Inc., The Regents of the University of ColoradoInventors: Douglas J. Dellinger, Brian Stell, Marvin H. Caruthers
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Patent number: 8236945Abstract: Process for preparing a compound of the formula (I) R1-S(O)x—S(O)yR2 in which R1 represents a molecular hydrocarbon radical which can be substituted and/or interrupted by one or more atoms and/or by one or more groups containing one or more atoms, said atoms being selected from N, O, P, S, Si and X, where X represents a halogen; R2, independently of R1, represents a carbon-containing group or a molecular hydrocarbon radical which can be substituted and/or interrupted by one or more atoms and/or by one or more groups containing one or more atoms, said atoms being selected from N, O, P, S, Si and X, where X represents a halogen, and x and y are selected from 0 and 1 in such a way that the sum of x and y is not more than 1, characterized in that a compound of formula (II) R1-S(O)x—R3-Si(R4)(R5)(R6) in which R3 represents a hydrocarbon chain of two carbon atoms, which is optionally unsaturated and/or substituted, and R4, R5 and R6, which are identical or different, each represent, independently of one another, aType: GrantFiled: April 24, 2007Date of Patent: August 7, 2012Assignee: Universite Joseph Fourier (Grenoble1)Inventors: Jean-Luc Decout, Beatrice Gerland, Jerome Desire
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Publication number: 20120190838Abstract: The present invention relates to methods and reagents for detecting analytes, e.g. nucleic acids. The new methods and reagents allow a simple and sensitive detection even in complex biological samples.Type: ApplicationFiled: March 2, 2012Publication date: July 26, 2012Applicant: BASECLICK GMBHInventors: Thomas CARELL, Anja SCHWOEGLER, Glenn A. BURLEY, Johannes GIERLICH, Mohammad Reza MOFID
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Publication number: 20120184505Abstract: In its many embodiments, the present invention provides a novel class of pyrimidine analogs as targeted mechanism-based modulators of cell cycle checkpoints. Cancers and/or malignancies can be treated by administration of a cell cycle checkpoint modulator of the invention. Also discussed are suitable combinations of the cell cycle checkpoint modulator with a checkpoint kinase inhibitor to produce synergistic apoptosis in cancer cells. The invention also includes methods of treating cancers by administering the combination of the cell cycle checkpoint modulator and the checkpoint kinase inhibitor, pharmaceutical compositions comprising the cell cycle checkpoint modulator as well as combinations and pharmaceutical kits. An example cell cycle checkpoint modulator is shown below: formula (I).Type: ApplicationFiled: August 27, 2010Publication date: July 19, 2012Inventors: Janeta Popovici-Muller, Timothy J. Guzi, Kristin E. Rosner
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Publication number: 20120178919Abstract: A radiolabeled nucleoside analogue is provided, which includes radioactive iodine 123I/131I, and a nucleoside analogue selected from a group consisting of cytidine, thymidine, uridine, and a derivative thereof. A method for preparing the radiolabeled nucleoside analogue, and a use thereof are further provided. The nucleoside analogue, prepared through the preparation method with a short synthesis time and a high radiochemical yield, has a long in vivo physiological half life and a high stability in serum, and, as a radiopharmaceutical composition, is useful in development of tumor proliferation diagnosis or therapy prognosis evaluation, and further assists in observation of long-time in vivo metabolism of a drug.Type: ApplicationFiled: July 29, 2011Publication date: July 12, 2012Applicants: NATIONAL YANG-MING UNIVERSITY, Institute of Nuclear Energy Research Atomic Energy Council, Executive YuanInventors: HSIN-ELL WANG, CHIH-YUAN LIN, WEI-TI KUO, CHUAN-LIN CHEN, MEI-HUI WANG, HUNG-MAN YU, MAO-CHI WENG, YU CHANG, WUU-JYH LIN
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Publication number: 20120172582Abstract: The present invention relates to methods and reagents for detecting analytes, e.g. nucleic acids. The new methods and reagents allow a simple and sensitive detection even in complex biological samples.Type: ApplicationFiled: March 2, 2012Publication date: July 5, 2012Applicant: BASECLICK GMBHInventors: Thomas CARELL, Anja SCHWÖGLER, Glenn A. BURLEY, Johannes GIERLICH, Mohammad Reza MOFID
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Publication number: 20120149888Abstract: The present invention relates to synthesis, purification and methods to obtain high purity novel 2?-arabino-O-methyl nucleosides and the corresponding phosphoramidites of various arabinonucleoside bases and introduction of such units into defined sequence synthetic DNA and RNA. Various synthetic oligonucleotides, such as HIV integrase inhibitor 14-mer and thrombin binding oligonucleotide, thrombin-1, bearing ara-2?-omethyl modification have been synthesized. It is anticipated the oligonucleotides incorporating these monomers will exhibit biological activities related to antisense approach approach, design of better SiRNA's, diagnostic agents. Similarly, it is anticipated that oligonucleotides incorporating such novel nucleosides will be useful to develop therapeutic candidates designing stable G-quadruplexes and Aptamers for oligonucleotide structure, folding topology, evaluation of biochemical properties and design and develop as therapeutic agents.Type: ApplicationFiled: February 23, 2010Publication date: June 14, 2012Inventors: Suresh C. Srivastava, Divya Pandey, Naveen P. Srivastava, Alok Srivastava
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Publication number: 20120149657Abstract: A method of treating cancer using certain 2?-fluoro arabino nucleosides is provided. Also provided are compounds represented by the formula: (I & A) wherein R is alkyl; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions containing these compounds.Type: ApplicationFiled: May 12, 2010Publication date: June 14, 2012Applicant: Southern Research InstituteInventors: John A. Secrist, III, Anita T. Fowler, Kamal N. Tiwari
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Patent number: 8193354Abstract: A process for isolating ?-anomer enriched Gemcitabine hydrochloride by converting Gemcitabine base into Gemcitabine hydrochloride followed by its purification using solvents from the series of water soluble ethers like 1,4-dioxane or Monoglyme.Type: GrantFiled: April 25, 2006Date of Patent: June 5, 2012Assignee: Arch Pharmalabs LimitedInventors: Ashish Ujagare, Dattatrey Kochrekar, Matthew Uzagare
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Patent number: 8193339Abstract: 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: GrantFiled: November 6, 2008Date of Patent: June 5, 2012Assignee: Pharmaessentia Corp.Inventors: Chi-Yuan Chu, Wei-Der Lee, Wensen Li, Chan Kou Hwang
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Publication number: 20120129799Abstract: The present invention relates to non aqueous pharmaceutical preparations containing gemcitabine or its pharmaceutically, acceptable salts in the form of ready-to-use solutions wherein the concentration of Gemcitabine is in the range of about 16 mg/ml to about 200 mg/ml and a pH of about 3.5 to 10.0. Further, a method for the preparation of non-aqueous Gemcitabine solution of the present invention is also disclosed.Type: ApplicationFiled: July 29, 2010Publication date: May 24, 2012Applicant: ASTRON RESEARCH LIMITEDInventors: Bothra Mukesh, Patel Bhavesh, Sehgal Ashish, Kumar Mandal Jayanta
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Publication number: 20120107955Abstract: 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: ApplicationFiled: September 6, 2011Publication date: May 3, 2012Applicant: Purdue Research FoundationInventors: M. Daniel Raftery, Danijel Djukovic, Zane Hammoud
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Patent number: 8168766Abstract: 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: GrantFiled: August 31, 2009Date of Patent: May 1, 2012Assignee: ScnioPharm Taiwan Ltd.Inventors: Julian Paul Henschke, Yung Fa Chen, George Charles Schloemer
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Publication number: 20120094280Abstract: The present invention relates to a use of non-cofactor compounds, represented by formulas (I) or (II) wherein R and Z are independently selected from H, D, C1-C12-alkyl, preferably C1-C4-alkyl, alkenyl, alkinyl, phenyl or -LX, wherein X represents a functional group or a reporter group attached via a linker group L, and QH is selected from —SH, —SeH, —NHNH2 or —ONH2, for a targeted modification or derivatization of a biomolecule by covalent coupling to the biomolecule in the presence of a directing methyltransferase. Further development of the method of targeted modification and derivatization are the method for targeted labeling a biomolecule and method for detecting unmethylated target sites in a biomolecule comprising modification of the biomolecule according to the present invention.Type: ApplicationFiled: April 1, 2010Publication date: April 19, 2012Applicant: BIOTECHNOLOGIJOS INSTITUTASInventors: Saulius Klimasauskas, Zita Liutkeviciute, Edita Kriukiene
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Publication number: 20120088908Abstract: Prodrugs based on gemcitabine structure shown in formula (I) as well as their synthetic method and application are disclosed in the present invention, wherein the definitions for the groups of a, b, c, d, E, Z and V are described in the specification. By modifying the N4 group, the solubility, the bioavailability and the organ specificity of the prodrugs are improved. Therefore, the fast metabolism problem is overcome for the produced prodrugs compounds. Intestinal toxicity induced by gemcitabine is decreased. Thereby, the prodrugs can be delivered by oral administration in clinics and further improve their anti-tumor, anti-cancer, anti-infection and diffusion preventing capability, and can also specifically act on liver or colon. The synthetic method is simple and adapted to industrial production.Type: ApplicationFiled: March 25, 2010Publication date: April 12, 2012Applicant: SANLUGEN PHARMATECH LTD.Inventors: Xiaoxia Xue, Gang Li, Changjun Sun, Wenbao Li
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Publication number: 20120071641Abstract: The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least one nucleoside of formula (2): Another aspect of the invention relates to a method of inhibiting the expression of a gene in cell, 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: March 2, 2010Publication date: March 22, 2012Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Alexander V. Kelin, Sudhakar Rao Takkellapati, Shigeo Matsuda
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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: 20120064107Abstract: Provided are methods relating to the use of CDP-therapeutic agent conjugates for the treatment of autoimmune disease, inflammatory disease, or cancer. Also provided are CDP-therapeutic agent conjugates, particles comprising CDP-therapeutic agent conjugates, and compositions comprising CDP-therapeutic agent conjugates.Type: ApplicationFiled: August 12, 2011Publication date: March 15, 2012Applicant: CERULEAN PHARMA INC.Inventor: Scott Eliasof
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Publication number: 20120065387Abstract: The present invention provides selenium derivatives of nucleosides, nucleoside phosphoramidites, nucleotides, nucleotide triphosphates, oligonucleotides, polynucleotides, and larger nucleic acids and methods for their synthesis. Selenium derivatives of both ribonucleic acids and deoxyribonucleic acids, as well as methods for their synthesis, crystallization and uses in structural determinations, particularly by X-ray crystallographic techniques are disclosed. The selenium derivatives of the present invention are also useful as food supplements.Type: ApplicationFiled: June 29, 2011Publication date: March 15, 2012Applicant: GEORGIA STATE UNIVERSITY RESEARCH FOUNDATION, INC.Inventor: Zhen Huang
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Patent number: 8114854Abstract: The present invention relates to novel crystal forms of an amide prodrug of gemcitabine, compositions thereof and methods for using.Type: GrantFiled: June 20, 2007Date of Patent: February 14, 2012Assignee: Eli Lilly and CompanyInventor: Alexandr Yevgenyevich Oblezov
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Publication number: 20120029182Abstract: Disclosed is a stable crystal of 1-(2?-cyano-2?-deoxy-?-D-arabinofuranosyl)cytosine monohydrochloride. There is provided a crystal of 1-(2?-cyano-2?-deoxy-?-D-arabinofuranosyl)cytosine monohydrochloride having characteristic peaks at 13.7°, 15.7°, 16.0°, 18.6°, 20.3°, and 22.7° as diffraction angles (2?±0.1°) measured by powder X-ray diffraction, and having a melting point of 192° C. to 197° C.Type: ApplicationFiled: May 14, 2010Publication date: February 2, 2012Applicant: DELTA-FLY PHARMA, INC.Inventors: Shotaro Watanabe, Takahiro Hatakeyama
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Publication number: 20120029167Abstract: A drug using the magnetic properties of a metal salen complex as represented by the following general formula in order to magnetize the intended drug by chemically binding the drug to a metal salen complex so that the drug can be delivered to the target diseased site. The drug can be delivered to the diseased site using the magnetic properties of the drug per se without using a carrier made of a magnetic substance as in the conventional methods.Type: ApplicationFiled: May 20, 2011Publication date: February 2, 2012Applicants: Yoshihiro Ishikawa, IHI CorporationInventors: Yoshihiro ISHIKAWA, Haruki Eguchi
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Publication number: 20110282046Abstract: The present invention relates to a novel and stereoselective synthetic process for the preparation of optically active cis-nucleoside derivatives of compound of Formula (I), wherein R3 represents H, F, Cl, C1-16 alkyl.Type: ApplicationFiled: January 15, 2010Publication date: November 17, 2011Inventors: Rama Shankar, Ravinder Raddy Vennapureddy, Asif Parvez Sayyed, Murali Krishna Ankaraju, Suri Babu Madasu, Janardhan Rao Vascuri, Sivakumaran Meenakshisunderam
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Patent number: 8058260Abstract: The present disclosure provides 2?-C-methyl-ribofuranosyl cytidine prodrugs, methods of making 2?-C-methyl-ribofuranosyl cytidine prodrugs, pharmaceutical compositions of 2?-C-methyl-ribofuranosyl cytidine prodrugs, and methods of using 2?-C-methyl-ribofuranosyl cytidine prodrugs and pharmaceutical compositions thereof to treat viral diseases such as hepatitis C.Type: GrantFiled: May 22, 2007Date of Patent: November 15, 2011Assignee: XenoPort, Inc.Inventor: Mark A. Gallop
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Publication number: 20110257109Abstract: The present invention encompasses compositions and methods that activate P2Y receptors for the increased production of new synapses in the central nervous system. The formulations of the invention may be administered to a healthy subject or to a subject in need thereof to restore synapses.Type: ApplicationFiled: April 19, 2011Publication date: October 20, 2011Inventor: Richard WURTMAN