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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Patent number: 11306091Abstract: The present invention relates to a process for producing an organofluoro compound including [18F]fluorine, and by using a solvent represented by Formula 1 in nucleophilic fluorination reaction, an organofluoro compound may be prepared at a high yield. In addition, since the solvent has very excellent solubility for a precursor compound, the solvent is suitable for the automated synthesis of 18F-labeled radiopharmaceuticals.Type: GrantFiled: May 29, 2020Date of Patent: April 19, 2022Assignee: FUTURECHEM CO., LTDInventors: Dae Yoon Chi, Byoung Se Lee, So Young Chu, Hyeon Jin Jeong, Hyeon Seok Kim
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Patent number: 11124536Abstract: This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.Type: GrantFiled: January 27, 2020Date of Patent: September 21, 2021Assignee: Tufts UniversityInventors: Philip G. Haydon, Jinbo Lee
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Patent number: 10544183Abstract: This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.Type: GrantFiled: March 13, 2014Date of Patent: January 28, 2020Assignee: TUFTS UNIVERSITYInventors: Philip G. Haydon, Jinbo Lee
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Patent number: 9885352Abstract: A delivery system for a sensor chip includes a plurality of selectable ports arranged on a first assembly. Each of the selectable ports is in communication with a separate channel. The delivery system includes a second assembly movable in relation to the first assembly. The second assembly has a channel that is mechanically connectable to different ones of the plurality of selectable ports on the first assembly by motion of the second assembly relative to the first assembly. The delivery system includes a mechanical interface configured to engage a separate actuator so that relative motion of the first assembly and the second assembly is affected by the actuator.Type: GrantFiled: September 28, 2015Date of Patent: February 6, 2018Assignee: Genia Technologies, Inc.Inventor: Robert A. Yuan
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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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Patent number: 9012428Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate useful in the treatment of patients infected with the hepatitis C virus (HCV).Type: GrantFiled: November 10, 2011Date of Patent: April 21, 2015Assignees: Janssen Products, LP, Medivir ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
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Publication number: 20150105341Abstract: Disclosed herein are nucleosides, nucleotides and nucleotide analogs, methods of synthesizing the same and methods of treating diseases and/or conditions such as a Picornavirus and/or Flaviviridae infection with one or more nucleosides, nucleotides and nucleotide analogs.Type: ApplicationFiled: October 9, 2014Publication date: April 16, 2015Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith, Marija Prhavc, Christian Andreas Jekle, Jerome Deval
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Patent number: 9006209Abstract: This invention relates to a stereochemically pure uracyl spirooxetane nucleoside phosphoramidate which inhibits the hepatitis C virus (HCV).Type: GrantFiled: November 10, 2011Date of Patent: April 14, 2015Assignees: Janssen Products, LP, Medivir ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Bernard Raboisson, Koen Vandyck, Steven Maurice Paula Van Hoof, Lili Hu, Abdellah Tahri
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Publication number: 20150094462Abstract: A novel method of simultaneously protecting two functions which are same or different, namely hydroxyl, amine, or thiol ones, particularly in sugars, polyalcohols, nucleosides, nucleotides, peptides, and nucleic acids during an organic synthesis, and to novel compounds for implementing this method, as well as to the method of obtaining these compounds. Method of simultaneously protecting two hydroxyl, amine, or thiol functions according to the invention by carrying out a protecting reaction between a compound having at least two free hydroxyl, amine, or thiol groups, and the disilane of formula 1, where R stands for Cl or Br, or I, or a substituent of formula 2, where X1, X2, X3, X4 are the same or different.Type: ApplicationFiled: April 23, 2013Publication date: April 2, 2015Inventors: Wojciech Tadeusz Markiewicz, Marcin Krzysztof Chmielewski, Sylwia Maria Musial, Hieronim Franciszek Maciejewski, Grzegorz Hreczycho
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Patent number: 8951988Abstract: The invention provides the Zidovudine-conjugated quinoline compound N-((1-(2-(hydroxy-methyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-tetrahydrofuran-3-yl)-1H-1,2,3-triazol-4-yl)methyl)-6-(4b,8,8-trimethyl-4b,5,6,7,8,8a-hexahydrodibenzo[a,c]phenazin-2-yloxy)hexanamide. The compound can selectively kill hepatoma cells, especially hepatoma cells with hepatitis B, and inhibit the growth of subcutaneous tumors in mice, but has no significant toxicity to normal liver cells. Experiments confirm that the compound has an anti-hepatoma effect and can be used in preparation of anti-hepatoma drugs.Type: GrantFiled: June 15, 2012Date of Patent: February 10, 2015Assignee: Huazhong University of Science and TechnologyInventor: Qibing Zhou
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Publication number: 20150005251Abstract: 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 paramyxovirus viral infection, with a nucleoside, a nucleotide and an analog thereof.Type: ApplicationFiled: June 24, 2014Publication date: January 1, 2015Inventors: Natalia Dyatkina, Guangyi Wang, Leonid Beigelman, Vivek Kumar Rajwanshi
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Publication number: 20140377743Abstract: This invention provides a nucleotide analogue comprising (i) a base selected from the group consisting of adenine, guanine, cytosine, thymine and uracil, (ii) a deoxyribose, (iii) an allyl moiety bound to the 3?-oxygen of the deoxyribose and (iv) a fluorophore bound to the base via an allyl linker, and methods of nucleic acid sequencing employing the nucleotide analogue.Type: ApplicationFiled: August 4, 2014Publication date: December 25, 2014Applicant: The Trustees of Columbia University in the City of New YorkInventors: Jingyue Ju, Lanrong Bi, Dae Hyun Kim, Qinglin Meng
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Patent number: 8916538Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.Type: GrantFiled: March 11, 2013Date of Patent: December 23, 2014Assignee: Vertex Pharmaceuticals IncorporatedInventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
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Patent number: 8912319Abstract: The present invention relates to methods of synthesizing 18F-FMAU. In particular, 18F-FMAU is synthesized using one-pot reaction conditions in the presence of Friedel-Crafts catalysts. The one-pot reaction conditions are incorporated into a fully automated cGMP-compliant radiosynthesis module, which results in a reduction in synthesis time and simplifies reaction conditions. The one-pot reaction conditions are also suitable for the production of 5-substituted thymidine or cytidine analogs. The products from the one-pot reaction (e.g. the labeled thymidine or cytidine analogs) can be used as probes for imaging tumor proliferative activity. More specifically, these [18F]-labeled thymidine or cytidine analogs can be used as a PET tracer for certain medical conditions, including, but not limited to, cancer disease, autoimmunity inflammation, and bone marrow transplant.Type: GrantFiled: July 15, 2011Date of Patent: December 16, 2014Assignee: University of Southern CaliforniaInventors: Zibo Li, Hancheng Cai, Peter S. Conti
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Patent number: 8877731Abstract: 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: GrantFiled: September 19, 2011Date of Patent: November 4, 2014Assignee: Alios Biopharma, Inc.Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
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Publication number: 20140323427Abstract: The present invention relates to the new indications of chronic obstructive pulmonary disease (COPD) and idiophathic lung fibrosis (IPF) for uridine and uridine analogues.Type: ApplicationFiled: July 24, 2012Publication date: October 30, 2014Applicant: Universitaetsklinikum FreiburgInventors: Marco Idzko, Stephan Sorichter
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Publication number: 20140309412Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds 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 compounds of the present invention.Type: ApplicationFiled: June 12, 2013Publication date: October 16, 2014Inventors: Balkrishen Bhat, Anne B. El drup, Thazha P. Prakash, Phillip Dan Cook, Robert L. LaFemina, Amy L. Simcoe, Carrie A. Rutkowski, Mario A. Valenciano
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Patent number: 8846636Abstract: The disclosure provides nucleotide analogues that comprise tetrahydrofuranyl or tetrahydrothienyl moieties with quaternary centers at the 3? position, the pharmaceutical formulations comprising the analogues, and methods of using the analogues and formulations for treating, preventing, and/or inhibiting diseases or conditions associated with cancers and viruses.Type: GrantFiled: March 18, 2009Date of Patent: September 30, 2014Assignee: LCB Pharma Inc.Inventor: Yvan Guindon
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Publication number: 20140275511Abstract: This invention relates to an improved method of purifying Nikkomycin Z, an antifungal compound shown to be particularly useful in treating Valley Fever, coccidioidomycosis. The improvement of this invention lies in the choice of resins and elution conditions, chosen to minimize handling of the material.Type: ApplicationFiled: March 15, 2013Publication date: September 18, 2014Inventor: David J. Larwood
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Publication number: 20140256670Abstract: The invention provides Zidovudine conjugated quinoline compound N-((1-(2-(Hydroxy-methyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-tetrahydrofuran-3-yl)-1H-1,2,3-triazol-4-yl)methyl)-6-(4b,8,8-trimethyl-4b,5,6,7,8,8a-hexahydrodibenzo[a,c]phenazin-2-yloxy)hexanamide. The compound can selectively kills the hepatoma cells especially the hepatoma cells with hepatitis B, and inhibit the growth of subcutaneous tumors in mice, but has no significant toxicity to normal liver cells. Experiments confirm the compound has anti-hepatoma effect, and can be used in preparation of anti-hepatoma drugs.Type: ApplicationFiled: June 15, 2012Publication date: September 11, 2014Applicant: Huazhong University of Science and TechnologyInventor: Qibing Zhou
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Publication number: 20140248241Abstract: 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 3?-deoxy nucleoside compounds according to Formula 3001a or 3001b: or a pharmaceutically acceptable salts, solvates, stereoisomeric forms, tautomeric forms, or polymorphic forms thereof, wherein PD, Base1 and Base2 are as provided herein.Type: ApplicationFiled: March 3, 2014Publication date: September 4, 2014Inventors: Alistair James STEWART, Adel M. MOUSSA, Benjamin Alexander MAYES, Francois-Rene ALEXANDRE, Dominique SURLERAUX, Christophe Claude PARSY, Claire PIERRA, David DUKHAN, Gilles GOSSELIN
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Publication number: 20140235563Abstract: 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: April 30, 2014Publication date: August 21, 2014Applicants: Gilead Sciences, Inc., Gilead Pharmasset LLCInventors: Michael Joseph Sofia, Jinfa Du
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Patent number: 8809520Abstract: The invention is directed to processes of preparing phosphonate nucleosides comprising a phosphonalkoxy-substituted five-membered, saturated or unsaturated, oxygen-containing ring coupled to a heterocyclic nucleobase such as a pyrimidine or purine base.Type: GrantFiled: July 11, 2013Date of Patent: August 19, 2014Assignee: K.U. Leuven Research & DevelopmentInventors: Piet Herdewijn, Christophe Pannecouque, Tongfei Wu, Erik De Clercq
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Publication number: 20140219958Abstract: In one aspect, the invention provides compounds represented by Formula I, and pharmaceutically acceptable salts, esters, stereoisomers, tautomers, solvates, and combinations thereof, pharmaceutical compositions comprising these compounds and the use of these compounds for treating a viral infection in a subject.Type: ApplicationFiled: January 31, 2014Publication date: August 7, 2014Applicant: ENANTA PHARMACEUTICALS, INC.Inventors: Jay R. Luly, Jun Ma, Guoqiang Wang, Yat Sun Or
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Publication number: 20140221304Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.Type: ApplicationFiled: July 10, 2012Publication date: August 7, 2014Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
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Publication number: 20140221639Abstract: 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: April 8, 2014Publication date: August 7, 2014Applicants: Institute of Nuclear Energy Research Atomic Energy Council, Executive Yuan, NATIONAL YANG-MING UNIVERSITYInventors: 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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Patent number: 8785620Abstract: This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g. neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.Type: GrantFiled: November 6, 2013Date of Patent: July 22, 2014Assignee: Tufts UniversityInventors: Philip Haydon, Jinbo Lee
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Publication number: 20140179627Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.Type: ApplicationFiled: December 19, 2013Publication date: June 26, 2014Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
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Publication number: 20140179910Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.Type: ApplicationFiled: December 19, 2013Publication date: June 26, 2014Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith
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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 -
Publication number: 20140128339Abstract: The present invention relates to 2?-Methyl Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein R, R1, R2 and R3, are as defined herein. The present invention also relates to compositions comprising at least one 2?-Methyl Substituted Nucleoside Derivative, and methods of using the 2?-Methyl Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.Type: ApplicationFiled: October 15, 2013Publication date: May 8, 2014Inventors: Vinay Girijavallabhan, Stephane Bogen, Quang T. Truong, Ping Chen, Angela Kerekes, Frank Bennett, Sara Esposite, Qingmei Hong, Ian Davies
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Patent number: 8710198Abstract: Caprazene is provided which is the compound represented by the following formula (I) wherein Me stands for methyl group, and a 5?-N-alkoxycarbonyl or 5?-N-aralkyloxycarbonyl derivative thereof, and wherein said compound has the 1H-NMR and 13C-NMR data as set forth in Table 15.Type: GrantFiled: December 29, 2008Date of Patent: April 29, 2014Assignee: Meiji Seika Pharma Co., Ltd.Inventors: Toshiaki Miyake, Masayuki Igarashi, Tetsuo Shitara, Yoshiaki Takahashi, Masa Hamada
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Publication number: 20140066613Abstract: This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.Type: ApplicationFiled: November 6, 2013Publication date: March 6, 2014Applicant: TUFTS UNIVERSITYInventors: Philip Haydon, Jinbo Lee
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Publication number: 20140051846Abstract: Disclosed are O-protected compounds of the formula (I): wherein B is an optionally protected nucleobase, and R1-R3 are as described herein, a method of preparing such compounds, and a method of preparing oligonucleotides such as RNA starting from such compounds. The O-protected compounds have one or more advantages, for example, the 2?-O-protected compound is stable during the various reaction steps involved in oligonucleotide synthesis; the protecting group can be easily removed after the synthesis of the oligonucleotide, for example, by reaction with tetrabutylammonium fluoride; and/or the O-protected groups do not generate DNA/RNA alkylating side products, which have been reported during removal of 2?-O-(2-cyanoethyl)oxymethyl or 2?-O-[2-(4-tolylsulfonyl)ethoxymethyl groups under similar conditions.Type: ApplicationFiled: March 29, 2012Publication date: February 20, 2014Applicant: TheUnited ofAmerica,asrepresentedbythe Secre -tary,Department ofHealthand Human ServiceInventors: Serge L. Beaucage, Jacek Cieslak
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Publication number: 20140045798Abstract: The present invention provides a compound of Formula Ia, wherein R1 is H or phosphate and the double bond is between N1 and C1 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 N1 C1, 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: October 18, 2013Publication date: February 13, 2014Applicant: Gencia CorporationInventor: Shaharyar Khan
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Patent number: 8633309Abstract: Disclosed herein are nucleoside phosphoramidates and their use as agents for treating viral diseases. These compounds are inhibitors of RNA-dependent 5 RNA viral replication and are useful as inhibitors of HCV NS5B polymerase, as inhibitors of HCV replication and for treatment of hepatitis C infection in mammals.Type: GrantFiled: January 10, 2013Date of Patent: January 21, 2014Assignee: Gilead Pharmasset LLCInventors: Bruce Ross, Michael Joseph Sofia, Ganapati Reddy Pamulapati, Suguna Rachakonda, Hai-Ren Zhang, Byoung-Kwon Chun, Peiyuan Wang
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Patent number: 8633308Abstract: Described herein are compounds and methods that prevent the viral infection of cells. The compounds and methods described herein minimize viral resistance and maximize the number of targeted viruses. Additionally, the compounds and methods minimize the toxicity toward uninfected cells.Type: GrantFiled: February 27, 2008Date of Patent: January 21, 2014Assignee: The Governors of The University of AlbertaInventors: Luis M. Schang, Mireilli R. St. Vincent, Alexey V. Ustinov
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Publication number: 20140005369Abstract: The present invention relates to a new uridine nucleoside-based amphiphilic gadolinium complex and a magnetic resonance imaging (MRI) contrast agent including the gadolinium complex. The MRI contrast agent has high relaxivity, high binding affinity for and stability in human serum albumin, pH response, and high liver specificity.Type: ApplicationFiled: March 15, 2012Publication date: January 2, 2014Applicants: KOREA BASIC SCIENCE INSTITUTE, KOREA UNIVERSITY RESEARCH AND BUSINESS FOUNDATIONInventors: Jong-Seung Kim, Sankarprasad Bhuniya, Sumin Lee, Kwan Soo Hong, Hyunseung Lee, Hyeyoung Moon
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Patent number: 8618075Abstract: The present invention provides certain tetrahydrouridine derivative compounds, pharmaceutical compositions and kits comprising such compounds, and methods of making and using such compounds.Type: GrantFiled: July 24, 2012Date of Patent: December 31, 2013Assignee: Eisai Inc.Inventors: Gregory S. Hamilton, Takashi Tsukamoto, Dana V. Ferraris, Bridget Duvall, Rena Lapidus
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Patent number: 8603999Abstract: Amphiphilic prodrugs of general formula A-X are disclosed, wherein A is a biologically active agent or may be metabolised to a biologically active agent; and X is selected from the group consisting of R, or up to three R moieties attached to a linker, Y1, Y2 or Y3, wherein R is selected from a group consisting of alkyl, alkenyl, alkynyl, branched alkyl, branched alkenyl, branched alkynyl, substituted alkyl, substituted alkenyl and substituted alkynyl groups and their analogues; Y1 is a linker group which covalently attached to an R group at one site and is attached to A at a further independent site; Y2 is a linker group which is covalently attached to two R groups at two independent sites and is attached to A at a further independent site; and Y3 is a linker group which is covalently attached to three R groups at three independent sites and is attached to A at a further independent site.Type: GrantFiled: December 4, 2009Date of Patent: December 10, 2013Assignee: Commonwealth Scientific and Industrial Research OrganisationInventors: Calum John Drummond, Sharon Marie Sagnella, Minoo Jalili Moghaddam, Xiaojuan Gong
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Publication number: 20130324491Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2?-deoxy-?-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted. The 2?-deoxy-?-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof may be administered either alone or in combination with another 2?-deoxy-?-L-erythro-pentofuranonucleoside or in combination with another anti-hepatitis B agent.Type: ApplicationFiled: March 22, 2013Publication date: December 5, 2013Applicants: Idenix Pharmaceuticals, Inc., L'Universite Montpellier II, Centre National de la Recherche ScientifiqueInventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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Publication number: 20130323836Abstract: The present invention provides compounds of formula (1). 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: April 22, 2011Publication date: December 5, 2013Applicant: Isis Pharmaceuticals, Inc.Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Ivan Zlatev, Eric E. Swayze, Thazha P. Prakash, Walter F. Lima
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Patent number: 8598141Abstract: This disclosure relates to uridine diphosphate (UDP) derivatives, compositions comprising therapeutically effective amounts of those UDP derivatives and methods of using those derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease) and traumatic CNS injury, as well as pain.Type: GrantFiled: March 8, 2013Date of Patent: December 3, 2013Assignee: Tufts UniversityInventors: Philip Haydon, Jinbo Lee, Jinghui Dong, Stephen Moss, Raquel Revilla-Sanchez
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Publication number: 20130303747Abstract: The present invention relates to the field of pharmacochemistry. Disclosed are fluorinated and azido-substituted pyrimidine nucleoside derivatives, and preparation methods and uses thereof. The structural formula is as shown (I). These compounds can be used for preparing medicaments for treating diseases such as tumors and viral infections, and can be used separately or in combination with other medicaments. The compounds also have effective activity against diseases such as tumors and viral infections, while having few side effects, and thus have potential application value.Type: ApplicationFiled: September 2, 2011Publication date: November 14, 2013Inventors: Junbiao Chang, Haoyun An, Xuejun Yu, Xiaohe Guo
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Publication number: 20130289266Abstract: We claim a simple strategy for the synthesis of a collection of C(3?)-spirodihydroisobenzo- furannulated and C(3?)-spirodihydroisobenzo-furannulated nucleosides featuring a [2+2+2]-cyclotrimerization as the key reaction. The cyclotrimerization reactions are facile with the unprotected nucleosides having a diyne unit. When both alkynes of the diyne are terminal, the regioselectivity is poor. However, when one of the terminal alkynes is additionally substituted, the cyclotrimerizations are highly diaste reoselective. Since the key bicycloannulation is the final step, this strategy provides flexibility in terms of the alkynes and is thus amenable for the synthesis of a focussed small molecule library.Type: ApplicationFiled: December 27, 2011Publication date: October 31, 2013Applicant: Council of Scientific & Industrial ResearchInventors: Venkata Ramana Chepuri, Mangesh Pandurang Dushing
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Publication number: 20130281687Abstract: Disclosed herein are methods of preparing a phosphorothioate nucleotide analog, which are useful in treating diseases and/or conditions such as viral infections.Type: ApplicationFiled: March 18, 2013Publication date: October 24, 2013Inventors: ALIOS BIOPHARMA, INC., VERTEX PHARMACEUTICALS INC.
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Publication number: 20130203836Abstract: The present invention provides nucleosides of formula (1) and oligonucleotides comprising at least on nucleoside of formula (2):Formula (1) and Formula (2). 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: March 31, 2011Publication date: August 8, 2013Applicants: ISIS PHARMACEUTICALS, INC., ALNYLAM PHARMACEUTICALS, INC.Inventors: Kallanthottathil G. Rajeev, Muthiah Manoharan, Eric E. Swayze, Thazha P. Prakash
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Patent number: 8492362Abstract: The present invention relates to prodrug forms of ?-L-1-[5-(E-2-Bromovinyl)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)]uracil (L-BHDU) and their use to treat viral infections of Varicella Zoster Virus, including recurrent VZV (shingles), especially including drug resistant Varicella Zoster Virus and related complications of this viral infection such as rash or post-herpetic neuralgia.Type: GrantFiled: November 8, 2011Date of Patent: July 23, 2013Assignee: University of Georgia Research Foundation, Inc.Inventor: Chung K. Chu
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Patent number: 8481510Abstract: Compounds of the formula I: including any possible stereoisomers thereof, wherein: R4 is a monophosphate, diphosphate or triphosphate ester; or R4 is R7 is optionally substituted phenyl, optionally substituted naphthyl, or optionally substituted indolyl; R8 and R8? are hydrogen, C1-C6alkyl, benzyl, or phenyl; or R8 and R8? form C3-C7cycloalkyl; R9 is C1-C10alkyl, C3-C7cycloalkyl, phenyl or phenyl-C1-C6alkyl, wherein the phenyl moiety in phenyl or phenyl-C1-C6alkyl is optionally substituted; or a pharmaceutically acceptable salt or solvate thereof; pharmaceutical formulations and the use of compounds I as HCV inhibitors.Type: GrantFiled: May 11, 2010Date of Patent: July 9, 2013Assignees: Janssen Products, LP, Medivir ABInventors: Tim Hugo Maria Jonckers, Pierre Jean-Marie Raboisson, Koen Vandyck, Steven Maurice Van Hoof, Lili Hu, Abdellah Tahri
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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.