Phosphorus Containing Patents (Class 514/48)
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Publication number: 20100323980Abstract: The invention relates to analogous compounds of 6-thioguanosine triphosphate of general formula (I). A compound of the general formula (I); wherein the dashed bond in the sugar moiety can be either single or double and wherein R1, R2, R3, R4 or R5, equal or different between each other, have general formula -(Int)m-Ter, wherein m is between 0 and 12 and Int and Ter are Internal and Terminal building blocks, wherein Int is selected from the group consisting of formula (II); and Ter is selected from the group consisting of formula (III).Type: ApplicationFiled: July 24, 2006Publication date: December 23, 2010Inventors: Giancarlo Naccari, Sergio Baroni
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Publication number: 20100316594Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.Type: ApplicationFiled: June 2, 2008Publication date: December 16, 2010Inventors: Jean-Pierre Sommadossi, Paolo LaColla, Richard Storer, Gilles Gosselin
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Patent number: 7846912Abstract: The present application describes deuterium-enriched nelarabine, pharmaceutically acceptable salt forms thereof, and methods of treating using the same.Type: GrantFiled: September 5, 2008Date of Patent: December 7, 2010Assignee: Protia, LLCInventor: Anthony W. Czarnik
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Patent number: 7842672Abstract: A compound of Formula I, Formula II, Formula III, or Formula IV: or a pharmaceutically acceptable salt, solvate, and/or ester thereof, therapeutic compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: GrantFiled: July 6, 2007Date of Patent: November 30, 2010Assignee: Gilead Sciences, Inc.Inventors: Constantine G. Boojamra, James M. Chen, Alan X. Huang, Choung U. Kim, Kuei-Ying Lin, Richard L. Mackman, David A. Oare, Jason K. Perry, Oliver L. Saunders, Sundaramoorthi Swaminathan, Lijun Zhang
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Publication number: 20100298255Abstract: Described herein are methods, devices, and compositions for providing personalized medicine tests for hematological neoplasms. In some embodiments, the methods comprise measuring the efficacy of inducing apoptosis selectively in malignant cells using any number of potential alternative combination drug treatments. In some embodiments, the ex vivo testing is measured using a recently extracted patient hematological samples. In other embodiments, the efficacy is measured ex vivo using an automated flow cytometry platform. For example, by using an automated flow cytometry platform, the evaluation of hundreds, or even thousands of drugs and compositions, can be made ex vivo. Thus, alternative polytherapy treatments can be explored. Non-cytotoxic drugs surprisingly induce apoptosis selectively in malignant cells ex vivo. In some embodiments, the methods described herein comprise evaluating non-cytotoxic drugs.Type: ApplicationFiled: May 19, 2010Publication date: November 25, 2010Applicant: Vivia Biotech S.L.Inventors: Juan Ballesteros, Teresa Bennett, Daniel Primo, Alberto Orfao, Coyt Jackson, Santiago Lago, Maria Matoses, Lilia Suarez, Sandra Sapia, Andrew Bosanquet, Julian Gorrochategui, Consuelo Tudela, Pilar Hernandez, Luis Ignacio Caveda
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Publication number: 20100291236Abstract: The present invention relates to osmium compounds of formula (I), their preparation and use in methods of treatment, particularly for cancer treatment.Type: ApplicationFiled: August 10, 2007Publication date: November 18, 2010Applicant: THE UNIVERSITY OF WARWICKInventors: Peter John Sadler, Anna Frances Acushla Peacock, Sabine Helena Van Rijt, Abraha Habtemariam
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Publication number: 20100286082Abstract: Riboswitches are targets for antibiotics and other small molecule therapies. Riboswitches and portions thereof can be used to regulate the expression or function of RNA molecules and other elements and molecules. Riboswitches and portions thereof can be used in a variety of other methods to, for example, identify or detect compounds. Compounds can be used to stimulate, active, inhibit and/or inactivate the riboswitch. Riboswitches and portions thereof, both alone and in combination with other nucleic acids, can be used in a variety of constructs and RNA molecules and can be encoded by nucleic acids.Type: ApplicationFiled: May 29, 2008Publication date: November 11, 2010Applicant: Yale UniversityInventors: Ronald R. Breaker, Zasha Weinberg, Narasimhan Sudarsan, Joy Xin Wang, Michelle M. Meyer, Adam Roth, Elizabeth E. Regulski
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Publication number: 20100279973Abstract: A process for preparing phosphoramidate prodrugs or cyclic phosphate prodrugs of nucleoside derivatives, which is a compound, its stereoisomers, salts (acid or basic addition salts), hydrates, solvates, or crystalline forms thereof.Type: ApplicationFiled: December 23, 2009Publication date: November 4, 2010Applicant: PHARMASSET, INC.Inventors: BYOUNG-KWON CHUN, JINFA DU, SUGUNA RACHAKONDA, BRUCE ROSS, MICHAEL JOSEPH SOFIA, GANAPATI REDDY PAMULAPATI, WONSUK CHANG, HAI-REN ZHANG, DHANAPALAN NAGARATHNAM
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Publication number: 20100267656Abstract: Myeloid differentiating agents can be used in the treatment of myeloid disorders.Type: ApplicationFiled: June 12, 2008Publication date: October 21, 2010Inventor: David Wald
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Publication number: 20100266674Abstract: The main drawback in the use of most nucleoside anticancer agents originates from their hydrophilic nature, of which property requires a high and frequent dosage for an intravenous administration. Unlike other nucleoside anti-tumor agents, troxacitabine appears to predominantly enter tumor cells by passive diffusion rather then by using nucleoside transporters, although this may be model dependent. Accordingly, in the present work, a small library of twenty troxacitabine prodrugs has been synthesized using a parallel approach in order to evaluate the relationship between the lipophilicity of the prodrugs and their antitumor activity. Biological evaluation of the prodrugs on two non-small cell lung cancer cell lines (A549 and SW1573) and in pancreatic cell lines clearly showed better antitumor activity than that of troxacitabine, with IC50 values in the nanomolar range.Type: ApplicationFiled: August 30, 2007Publication date: October 21, 2010Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.Inventor: David C.K. Chu
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Patent number: 7812000Abstract: The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers of the invention comprise at least two oligonucleotides linked at their 3? ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunostimulatory oligonucleotide and having an accessible 5? end.Type: GrantFiled: October 3, 2007Date of Patent: October 12, 2010Assignee: Idera Pharmaceuticals, Inc.Inventors: Sudhir Agrawal, Ekambar R. Kandimalla, Dong Yu, Lakshmi Bhagat
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Patent number: 7807653Abstract: The present invention relates to nucleoside diphosphate mimics and nucleoside triphosphate mimics, which contain diphosphate or triphosphate moiety mimics and optionally sugar-modifications and/or base-modifications. The nucleotide mimics of the present invention, in a form of a pharmaceutically acceptable salt, a pharmaceutically acceptable prodrug, or a pharmaceutical formulation, are useful as antiviral, antimicrobial, and anticancer agents. The present invention provides a method for the treatment of viral infections, microbial infections, and proliferative disorders. The present invention also relates to pharmaceutical compositions comprising the compounds of the present invention optionally in combination with other pharmaceutically active agents.Type: GrantFiled: June 14, 2007Date of Patent: October 5, 2010Assignee: Biota Scientific Management Pty LtdInventors: Phillip D. Cook, Guangyi Wang, Thomas W. Bruice, Nicholas A. Boyle, Janet M. Leeds, Jennifer L. Brooks, Marija Prhavc, Maria Eugenia Ariza, Patrick C. Fagan, Yi Jin, Vivek K. Rajwanshi, Kathleen D. Tucker
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Publication number: 20100222292Abstract: The invention relates to methods for transdifferentiation of body tissues which can be used to generate specific cell types needed for regenerating organs or body parts, following cellular degeneration, injury or amputation. The present invention also describes the use of tissue transdifferentiation for treating cancer and autoimmune diseases.Type: ApplicationFiled: May 7, 2010Publication date: September 2, 2010Inventor: Steven Baranowitz
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Publication number: 20100204162Abstract: The present invention provides a compound which is an inhibitor of sphingolipid biosynthesis for use in the treatment of a disease which has a secondary Niemann-Pick type C disease like cellular phenotype.Type: ApplicationFiled: June 26, 2008Publication date: August 12, 2010Inventors: Mary Frances Platt, Emyr Lloyd-Evans, Forbes Dennison Porter
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Patent number: 7772206Abstract: This invention relates to methods of treating or preventing an autoimmune disorder comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate, clathrate, prodrug or metabolite thereof to a patient in need of such treatment. The invention further relates to methods of treating or preventing an autoimmune disorder comprising the administration of clofarabine or a pharmaceutically acceptable salt, hydrate, solvate, clathrate, prodrug or metabolite thereof and an additional therapeutic agent to a patient in need of such treatment.Type: GrantFiled: February 27, 2009Date of Patent: August 10, 2010Assignee: Genzyme CorporationInventors: Christopher B. Wood, Stuart W. Smith
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Publication number: 20100173013Abstract: The present application is generally directed to compounds, compositions and methods of combination therapy for the treatment of neoplastic disorders.Type: ApplicationFiled: January 7, 2010Publication date: July 8, 2010Inventors: Denis Drygin, Kenna Anderes, Caroline B. Ho, Joshua R. Bliesath, Christopher B. Proffitt, Sean O'Brien, William G. Rice
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Patent number: 7749975Abstract: The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers of the invention comprise at least two oligonucleotides linked at their 3? ends, internucleoside linkages or functionalized nucleobase or sugar to a non-nucleotidic linker, at least one of the oligonucleotides being an immunostimulatory oligonucleotide and having an accessible 5? end.Type: GrantFiled: July 1, 2005Date of Patent: July 6, 2010Assignee: Idera Pharmaceuticals, Inc.Inventors: Sudhir Agrawal, Ekambar R. Kandimalla, Dong Yu, Lakshmi Bhagat
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Publication number: 20100136136Abstract: This invention relates to the field of protein tyrosine kinases and inhibitors thereof. In particular, the invention relates to inhibitors of JAK-2, pharmaceutical compositions of the compounds for inhibiting JAK-2, methods of inhibiting JAK-2 in a cell, comprising contacting a cell in which inhibition of JAK-2 is desired with a compound or pharmaceutical composition comprising a compound according to the invention. The also comprises methods of treating a disease or condition that involves JAK-2 comprising administering to a patient a pharmaceutical composition comprising a compound according to the invention.Type: ApplicationFiled: September 28, 2007Publication date: June 3, 2010Applicant: EXELIXIS, INC.Inventors: Adam Antoni Galan, Jeff Chen, Hongwang Du, Timothy Forsyth, Tai Phat Huynh, Henry William Beecroft Johnson, Patrick Kearney, James W. Leahy, Matthew Sangyup Lee, Grace Mann, Brian Hugh Ridgway, Craig Stacy Takeuchi, Peiwen Zhou
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Publication number: 20100119479Abstract: Disclosed herein are compounds represented by a formula: Therapeutic methods, compositions, medicaments, and dosage forms related thereto are also disclosed.Type: ApplicationFiled: October 14, 2009Publication date: May 13, 2010Applicant: INTERMUNE, INC.Inventors: BRAD BUCKMAN, VLADIMIR SEREBRYANY, SCOTT SEIWERT, LEONID BEIGELMAN, ANTITSA STOYCHEVA
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Patent number: 7709449Abstract: The invention provides compounds capable of treating against hepatitis infections, particularly hepatitis B viral infections. Compounds of the invention are nucleic acid-based and preferably comprise 2, 3, 4, 5 or 6 nucleoside units.Type: GrantFiled: July 10, 2007Date of Patent: May 4, 2010Assignee: Migenix, Inc.Inventors: Radhakrishnan P. Iyer, Yi Jin, Arlene Roland, Wenqiang Zhou
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Publication number: 20100104532Abstract: The invention provides unsaturated phosphonates of Formula I or a tautomer or pharmaceutically accepatble salt thereof, as described herein, as well as pharmaceutical compositions comprising the compounds, and therapeutic methods comprising administering the compounds. The compounds have anti-viral properties and are useful for treating viral infections (e.g. HCV) in animals (e.g. humans).Type: ApplicationFiled: February 8, 2008Publication date: April 29, 2010Applicant: GILEAD SCIENCES, INC.Inventors: James M. Chen, Alan X. Huang, Richard L. Mackman, Jay Parrish, Jason K. Perry, Oliver L. Saunders, David Sperandio
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Publication number: 20100099643Abstract: Disclosed are polycyclic polyether compounds of formula I and pharmaceutical compositions comprising such compounds. wherein R, OR1, and R2 are as defined herein. Also disclosed are methods of regulating mucus clearance in a cell, and methods of treating decreased mucus clearance or mucociliary dysfunction.Type: ApplicationFiled: December 22, 2009Publication date: April 22, 2010Inventors: Daniel G. Baden, William M. Abraham, Andrea J. Bourdelais, Sophie Michelliza
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Patent number: 7700567Abstract: Oligonucleotide analogues are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2?-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogues rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogues can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogues and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogues, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.Type: GrantFiled: September 29, 2005Date of Patent: April 20, 2010Assignee: Supergen, Inc.Inventors: Pasit Phiasivongsa, Sanjeev Redkar
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Patent number: 7700576Abstract: Novel pharmaceutical compositions which contain one of the reverse transcriptase inhibitors, viz., Zidovudine, Lamivudine or Stavudine in clinically efficacious amount and Meldonium as well as pharmaceutically applicable excipients. It has been proved that inclusion of Meldonium in these pharmaceutical compositions essentially diminishes the cardio- and neuro-toxicity of the reverse transcriptase inhibitor.Type: GrantFiled: August 8, 2006Date of Patent: April 20, 2010Assignee: Latvian Institute of Organic SynthesisInventors: Vija Klusha, Sergejs Isajevs, Jolanta Pupure, Juris Rumaks, Valentina Gordjushina, Immanuels Taivans, Ivars Kalvinsh
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Publication number: 20100093656Abstract: This invention relates to novel phosphate-modified nucleosides, and methods for producing them, being useful for the prevention or treatment of a viral infection in a mammal, and for preparing oligonucleotides by DNA/RNA polymerase-dependent amplification, e.g. PCR.Type: ApplicationFiled: August 27, 2009Publication date: April 15, 2010Inventors: Olga ADELFINSKAYA, Piet HERDEWIJN
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Publication number: 20100081628Abstract: 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: June 5, 2009Publication date: April 1, 2010Applicant: PHARMASSET, INC.Inventors: Jinfa DU, Dhanapalan NAGARATHNAM, Ganapati REDDY PAMULAPATI, Bruce S. ROSS, Michael Joseph SOFIA
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Publication number: 20100081627Abstract: Disclosed are polymeric compounds which are useful as prodrugs, comprising a chain of monomeric nucleosides, nucleoside analogs or abasic nucleosides, wherein at least one of the nucleosides or nucleoside analogs or a heterocyclic derivative thereof is pharmaceutically active and the nucleosides, nucleoside analogs or abasic nucleosides are linked by a phosphodiester group, a phosphorothioate group or an H—, alkyl or alkenyl phosphonate group.Type: ApplicationFiled: October 2, 2009Publication date: April 1, 2010Applicant: RELIABLE BIOPHARMACEUTICAL, INC.Inventors: UmaShanker Sampath, Joseph A. Toce, Sourena Nadji
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Publication number: 20100074850Abstract: The present invention relates to the field of improving the flavour of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. More particularly, the present invention provides flavour modulating substances selected from the group represented by formula (1): and edible salts thereof and edible esters thereof, which can advantageously be used for modulating the flavour of foodstuffs, beverages, tobacco products, pharmaceutics and oral care products. These flavour modulating substances can be used to impart desirable taste attributes in a wide variety of applications and products. In addition, the present flavour modulating substances are capable of modulating the taste and/or aroma impact of other, flavour imparting, substances contained within these same products, thereby improving the overall flavour quality of these products.Type: ApplicationFiled: December 13, 2007Publication date: March 25, 2010Applicant: GIVAUDAN NEDERLAND SERVICES B.V.Inventors: Adri De Klerk, Marieke Baalbergen, Harry Renes, Chris Winkel
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Publication number: 20100062995Abstract: Provided are methods of designing a putative inhibitor of a human 5?-methylthioadenosine phosphorylase (MTAP). Also provided are methods of inhibiting a human MTAP.Type: ApplicationFiled: September 18, 2007Publication date: March 11, 2010Inventor: Vern L. Schramm
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Patent number: 7666855Abstract: Compounds of Formula I, stereoisomers, and pharmaceutically acceptable salts or prodrugs thereof, their preparation, and their uses for the treatment of hepatitis C viral infection are described:Type: GrantFiled: October 30, 2006Date of Patent: February 23, 2010Assignee: Metabasis Therapeutics, Inc.Inventors: K. Raja Reddy, Mark D. Erion
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Patent number: 7662361Abstract: The invention provides methods and compositions for modulating the activity of therapeutic agents for the treatment of a cancer by administering one or more agents that (either alone or in combination) induces telomere damage and inhibits telomerase activity in the cancer cell. The method initially uses, e.g., a telomere damage-inducing agent such as paclitaxel, and a telomerase inhibitory agent such as AZT. The invention also provides methods for identifying other agents with telomere damage-inducing activity and/or telomerase inhibitory activity (as well as and compositions having such activity), for use in the treatment of cancer.Type: GrantFiled: February 2, 2006Date of Patent: February 16, 2010Inventors: Jessie L.-S. Au, M. Guillaume Wientjes
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Publication number: 20100022467Abstract: The invention is related to phosphorus substituted anti-cancer compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: September 2, 2008Publication date: January 28, 2010Inventors: Constantine G. Boojamra, Carina Cannizzaro, James M. Chen, Xiaowu Chen, Aesop Cho, Lee S. Chong, Maria Fardis, Alan X. Huang, Choung U. Kim, Thorsten Kirschberg, Steven Krawczyk, Christopher P. Lee, Kuei-Ying Lin, Richard L. Mackman, David Y. Markevitch, Peter H. Nelson, David A. Oare, Vidya K. Prasad, Hyung-Jung Pyun, Adrian S. Ray, Sundaramoorthi Swaminathan, William J. Watkins, Jennifer R. Zhang, Lijun Zhang
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Publication number: 20100016252Abstract: Disclosed are Mannich base N-oxides of drugs containing acidic N—H groups. Pharmaceutical compositions comprising a therapeutically effective amount of Mannich base N-oxides, or a N-oxide rearrangement product, pharmaceutically acceptable salt or prodrug thereof, are also disclosed. Further, disclosed are methods of using the compounds, alone or in combination with one or more other active agents or treatments.Type: ApplicationFiled: September 21, 2009Publication date: January 21, 2010Applicant: State of Oregon Acting By and Through The Oregon State Board of Higher Education On Behalf of The UInventors: John F.W. Keana, Paul Westberg, John Curd, Alshad S. Lalani
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Publication number: 20100016250Abstract: The present invention provides TLR9 agonists comprising, as an active ingredient, a compound represented by formula (I): (wherein a represents 0 or 1; n represents an integer of 0 to 2; m represents an integer of 0 to 5; X1 and X2 each independently represent a hydrogen atom or hydroxy; Y represents an oxygen atom or a sulfur atom; -Q1-represents —O— or the like; -Q2- represents —O— or the like; -Z- represents —O— or the like; R1, R3 and R4 each independently represent hydroxy or the like; R2 and R5 each independently represent a hydrogen atom, hydroxy or the like; and A represents 6-aminopurin-9-yl or the like) or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: April 13, 2007Publication date: January 21, 2010Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Hiroyuki Nagata, Michio Ichimura, Rieko Nakatsu, Shun-Ichi Ikeda, Ayako Kawabata, Toshio Ota, Masayuki Abe, Michio Takashima, Makoto Suzuki
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Publication number: 20100016251Abstract: Disclosed herein are phosphoramidate prodrugs of nucleoside derivatives for the treatment of viral infections in mammals, which is a compound, its stereoisomer, salt (acid or basic addition salt), hydrate, solvate, or crystalline form thereof, represented by the following structure: Also disclosed are methods of treatment, uses, and processes for preparing each of which utilize the compound represented by formula I.Type: ApplicationFiled: March 21, 2008Publication date: January 21, 2010Applicant: PHARMASSET, INC.Inventors: MICHAEL JOSEPH SOFIA, JINFA DU, PEIYUAN WANG, DHANAPALAN NAGARATHNAM
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Patent number: 7648967Abstract: The present invention relates to methods of treating viral disease using mutagenic nucleoside analogs. In particular, the invention provides isoguanosine nucleosides and derivatives thereof as well a method of increasing the mutation rate of a virus such as bovine viral diarrhea virus (BVDV) and hepatitis C virus (HCV).Type: GrantFiled: February 13, 2006Date of Patent: January 19, 2010Assignee: Koronis Pharmaceuticals, IncorporatedInventors: Ling Li, Alexander Gall, Richard Daifuku
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Publication number: 20100004161Abstract: The present invention relates to an in vitro method of assessing the sensitivity of a subject to a treatment of cancer, which method comprises detecting the presence of a mutated Toll Like Receptor 4 (TLR4) nucleic acid or an abnormal TLR4 protein expression or activity in a sample from the subject, the presence of said mutated TLR4 nucleic acid or abnormal TLR4 expression or activity being indicative of a resistance to said treatment. The invention further provides compounds for treating or preventing a cancer in a subject having a mutated TLR4 nucleic acid or an abnormal TLR4 protein expression or activity.Type: ApplicationFiled: July 17, 2007Publication date: January 7, 2010Inventors: Lionel Apetoh, Guido Kroemer, Laurence Zitvogel
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Patent number: 7635690Abstract: The present invention discloses a method for treating HIV that includes administering ?-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using ?-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. ?-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.Type: GrantFiled: October 3, 2006Date of Patent: December 22, 2009Assignee: Emory UniversityInventors: Raymond F. Schinazi, Jennifer L. Hammond, John W. Mellors, Dennis C. Liotta
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Patent number: 7635689Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.Type: GrantFiled: December 6, 2004Date of Patent: December 22, 2009Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi di Cagliari, Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Paola LaColla, Richard Storer, Gilles Gosselin, Jean-Pierre Sommadossi
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Patent number: 7632821Abstract: The present invention provides ribonucleoside 2?,3?-cyclic acetals of structural formula I which are precursors or prodrugs of inhibitors of RNA-dependent RNA viral polymerase. These compounds are precursors of inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as precursors or prodrugs of inhibitors of hepatitis C virus (HCV) NS5B polymerase, as precursors or prodrugs of inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such ribonucleoside 2?,3?-cyclic acetals alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection.Type: GrantFiled: August 4, 2006Date of Patent: December 15, 2009Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Kenneth Alan Koeplinger, Malcolm MacCoss, Daniel R. McMasters, David B. Olsen, Lihu Yang
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Publication number: 20090306007Abstract: The invention provides a compound of formula (I), wherein R1-R6 and X have any of the values described, as well as pharmaceutical compositions comprising such compounds and therapeutic methods comprising the administration of such compounds.Type: ApplicationFiled: December 8, 2005Publication date: December 10, 2009Applicant: Regents of the University of MinnesotaInventor: Carston R. Wagner
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Patent number: 7625876Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.Type: GrantFiled: August 20, 2007Date of Patent: December 1, 2009Assignee: Hopital-Sainte-JustineInventors: Ernest G. Seidman, Yves Theoret
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Patent number: 7625872Abstract: The invention provides immunomodulatory compounds and methods for immunomodulation of cells and individuals using the immunomodulatory compounds.Type: GrantFiled: December 17, 2003Date of Patent: December 1, 2009Assignee: Dynavax Technologies CorporationInventor: Karen L. Fearon
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Patent number: 7625875Abstract: 2? and 3?-Prodrugs of 1?, 2?, 3? or 4?-branched ?-D or ?-L nucleosides, or their pharmaceutically acceptable salts and derivatives are described, which are useful in the prevention and treatment of Flaviviridae infections and other related conditions. These modified nucleosides provide superior results against flaviviruses and pestiviruses, including hepatitis C virus and viruses generally that replicate through an RNA dependent RNA reverse transcriptase. Compounds, compositions, methods and uses are provided for the treatment of Flaviviridae infection, including HCV infection, that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.Type: GrantFiled: December 6, 2004Date of Patent: December 1, 2009Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi di Cagliari, Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Gilles Gosselin, Richard Storer, Paola LaColla, Jean-Pierre Sommadossi
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Patent number: 7618949Abstract: The present invention provides a P2Y12 receptor antagonist compound-eluting stent, wherein the stent is coated with one or more P2Y12 receptor antagonist compounds or a pharmaceutically acceptable salt, solvate, or hydrate thereof. When the stent is placed in a narrowed or damaged arterial vessel, a therapeutically effective amount of the P2Y12 receptor antagonist compound is eluted continuously from the stent to the local environment of the stent. The P2Y12 receptor antagonist compound-eluting stents are useful in preventing thrombosis and restenosis, and are effective in inhibiting the contraction of vascular smooth muscle cells, inhibiting cell proliferation, and reducing inflammation.Type: GrantFiled: July 30, 2008Date of Patent: November 17, 2009Assignees: Inspire Pharmaceuticals, Inc., University of North Carolina at Chapel HillInventors: José L. Boyer, James G. Douglass, III, Sammy R. Shaver
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Publication number: 20090274686Abstract: The present invention discloses compounds of formula (I) or (II), or pharmaceutically acceptable salts, esters, or prodrugs thereof: which inhibit, preventing or treating abnormal cellular proliferation and/or a viral infection, particularly by HIV, HCV or HBV. Consequently, the compounds of the present invention interfere with the replication cycle of a virus and are also useful as antiviral agents, or interfere with host cellular biochemical process and are also useful as antiproliferative agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from viral infection and/or cell proliferation. The invention also relates to methods of treating a viral infection and/or cell proliferation in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.Type: ApplicationFiled: May 1, 2009Publication date: November 5, 2009Inventors: Yat Sun Or, Lu Ying, Xiaowen Peng, Ce Wang, Yao-Ling Qiu
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Patent number: 7612047Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation-resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation-resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides. The mononucleoside phosphate compounds of the present invention are useful in preventing and treating epithelial tissue diseases or diseases or disorders associated with platelet aggregation.Type: GrantFiled: September 10, 2008Date of Patent: November 3, 2009Assignee: Inspire Pharmaceuticals, Inc.Inventors: James G. Douglass, III, Benjamin R. Yerxa, Sammy R. Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean, José L. Boyer
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Patent number: 7608599Abstract: The invention provides novel nucleoside compounds of formula I wherein R1, R2a, R2b, R3, R4, R5 R6, R8a, R9 and R10 are as defined herein which are useful for the treatment of Hepatitis C Virus (HCV) mediated diseases.Type: GrantFiled: August 11, 2006Date of Patent: October 27, 2009Assignee: Roche Palo Alto LLCInventors: Klaus Klumpp, Joseph Armstrong Martin, Christopher McGuigan, David Bernard Smith
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Patent number: 7608600Abstract: 2? and/or 3? prodrugs of 1?, 2?, 3? or 4?-branched nucleosides, and their pharmaceutically acceptable salts and derivatives are described. These prodrugs are useful in the prevention and treatment of Flaviviridae infections, including HCV infection, and other related conditions. Compounds and compositions of the prodrugs of the present invention are described. Methods and uses are also provided that include the administration of an effective amount of the prodrugs of the present invention, or their pharmaceutically acceptable salts or derivatives. These drugs may optionally be administered in combination or alteration with further anti-viral agents to prevent or treat Flaviviridae infections and other related conditions.Type: GrantFiled: June 27, 2003Date of Patent: October 27, 2009Assignees: Idenix Pharmaceuticals, Inc., University of Cagliari, Centre National de la Recherche Scientifique, L'Universite Montfellier IIInventors: Richard Storer, Gilles Gosselin, Jean-Pierre Sommadossi, Paola LaColla
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Patent number: 7608597Abstract: 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: GrantFiled: June 20, 2003Date of Patent: October 27, 2009Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi Di CagliariInventors: Jean-Pierre Sommadossi, Paulo LaColla