Purines (including Hydrogenated) (e.g., Adenine, Guanine, Etc.) Patents (Class 514/45)
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Patent number: 8329664Abstract: A compound for use in the treatment or prophylaxis of viral infections such, for example as chicken pox or shingles caused by the Varicella Zoster virus, said compound having the general formula (II): wherein X is O, S, NH or CH2, Y is O, S or NH, Z is O, S or CH2, R1 is C1-6 alkyl, preferably n-alkyl, e.g., n-pentyl or n-hexyl, and one of R2 and R3 is OH, and the other of R3 and R2 is a neutral, non-polar amino acid moiety, or a pharmaceutically acceptable salt or hydrate thereof. Said neutral, non-polar amino acid moiety R2 or R3 may be (IV): in which R4, R5, R6 and R7 are each independently H or C1-2 alkyl. In preferred embodiments, one of R2 or R3 is valine, leucine, isoleucine or alanine, particularly valine.Type: GrantFiled: May 9, 2007Date of Patent: December 11, 2012Assignees: University College Cardiff Consultants Limited, K.U. Leuven Research and DevelopmentInventors: Christopher McGuigan, Jan Balzarini, Marco Migliore
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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: 8324179Abstract: The invention provides unsaturated phosphonates of Formula I or a tautomer or pharmaceutically acceptable 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: GrantFiled: February 8, 2008Date of Patent: December 4, 2012Assignee: 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: 20120302518Abstract: Disclosed herein, in certain embodiments, is a crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide. Further disclosed herein, in certain embodiments, are pharmaceutical compositions comprising the crystalline polymorph form A of N—(S)-(3,4-difluoro-2-(2-fluoro-4-iodophenylamino)-6-methoxyphenyl)-1-(2,3-dihydroxypropyl)cyclopropane-1-sulfonamide.Type: ApplicationFiled: July 24, 2012Publication date: November 29, 2012Applicant: ARDEA BIOSCIENCES, INC.Inventor: Stuart DIMOCK
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Publication number: 20120282218Abstract: New chiral and achiral oxy-substituted cyclopentyl pyridinone diketocarboxamides and their derivatives and methods for their preparations are disclosed. The compounds include tautomers, regioisomers and geometric isomers. These complex carboxamides are designed as inhibitors of HIV replication through inhibition of HIV integrase. The compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS and ARC, either as the compounds, or as pharmaceutically acceptable salts, with pharmaceutically acceptable carriers, used alone or in combination with antivirals, immunomodulators, antibiotics, vaccines, and other therapeutic agents, especially other anti-HIV compounds (including other anti-HIV integrase agents), which can be used to create combination anti-HIV cocktails. Methods of treating AIDS and ARC and methods of treating or preventing infection by HIV are also described.Type: ApplicationFiled: December 7, 2010Publication date: November 8, 2012Applicant: University of Georgia Research Foundation Inc.Inventors: Vasu Nair, Maurice O. Okello, Abdumalik A. Nishonov, Sanjaykumar Mishra
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Publication number: 20120283177Abstract: The invention relates to a pharmaceutical composition for treating the human immunodeficiency virus (HIV) in humans, including three or four active principles selected as: a nucleoside reverse transcriptase inhibitor (NARTI) selected from lamivudine and emtricitabine; a nucleoside or nucleotide reverse transcriptase inhibitor (NARTI) selected from didanosine, abacavir and tenofovir; and the combination of ritonavir with a protease inhibitor (PI) selected from lopinavir, fosamprenavir, atazanavir and darunavir; or an non-nucleoside reverse transcriptase inhibitor (NNRTI) selected from efavirenz and etravirine; for daily administration to said human being one to four days per week.Type: ApplicationFiled: November 19, 2010Publication date: November 8, 2012Inventor: Jacques Leibowitch
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Publication number: 20120282261Abstract: The present invention discloses: (i) two novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (ii) methods of synthesis of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, and/or derivatives thereof; (iii) pharmaceutically-acceptable formulations comprising said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents; and (iv) methods of administration of said novel deuterated Karenitecin® analogs, pharmaceutically-acceptable salts, derivatives thereof; and/or, optionally, one or more additional chemotherapeutic agents, to subjects in need thereof.Type: ApplicationFiled: May 6, 2011Publication date: November 8, 2012Inventors: Xinghai Chen, Qiuli Huang, Harry Kochat, Andrey Malakhov, Frederick H. Hausheer
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Publication number: 20120283211Abstract: The invention provides methods and compositions for reducing or inhibiting bone resorption, osteoclast differentiation and stimulation and the loosening of medical prostheses by administering a compound or agent that modulates an adenosine receptor such as the adenosine A2A receptor, in particular, an agonist of an adenosine A2A receptor. The invention also extends to pharmaceutical compositions comprising such an agent that modulates an adenosine receptor such as an adenosine A2A agonist and to prosthetic devices containing such an agent that modulates an adenosine receptor such as an A2A agonist on one or more surfaces or within the prosthetic device such as, for example, suspended in the cement forming the prosthetic device.Type: ApplicationFiled: May 18, 2012Publication date: November 8, 2012Inventors: Bruce N. Cronstein, Aranzazu Mediero Munoz
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Publication number: 20120282172Abstract: The present invention provides a system presenting site-specific accumulation through a ligand that specifically targets a receptor overexpressed on the surface of specific cells within a target organ, like, for example, tumor cells and/or vascular cells of tumor blood vessels. Moreover, this invention provides a method where, upon internalization of the previous-mentioned system by the target cells, triggered release at a high rate of the associated agent takes place, permitting efficient intracellular delivery and, thus, increased concentration of the transported cargo at the target site. Overall, this invention provides a method for the diagnosis, prevention and treatment of human diseases and disorders.Type: ApplicationFiled: May 9, 2012Publication date: November 8, 2012Applicants: Centro de Neurociencias e Biologia Celular, Universidade de CoimbraInventors: João Nuno Sereno de Almeida Moreira, Vera Lúcia Dantas Nunes Caldeira de Moura, Sérgio Paulo de Magalhães Simões, Maria da Conceição Monteiro Pedroso de Lima
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Patent number: 8304529Abstract: Novel cap analogs which are easily synthesized, resulting in high levels of capping efficiency and transcription and improved translation efficiencies are provided. Such caps are methylated at the N7 position of one or both guanosines of the dinucleotide cap as well as at the 3? position on the ribose ring. Substituent groups on the ribose ring also result in the cap being incorporated in the forward orientation. Also provided are methods useful for preparing capped analogs and using mRNA species containing such analogs are also contemplated herein, as well as kits containing the novel cap analogs.Type: GrantFiled: July 10, 2007Date of Patent: November 6, 2012Assignee: Life Technologies CorporationInventors: Anilkumar R. Kore, Muthian Shanmugasundaram
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Patent number: 8299038Abstract: 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: July 16, 2009Date of Patent: October 30, 2012Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi di CagliariInventors: Jean-Pierre Sommadossi, Paulo LaColla
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Publication number: 20120270828Abstract: The present invention relates to a pharmaceutical composition for treating the human immunodeficiency virus (HIV) in a human being, comprising four active principles selected as being: a non-nucleoside inhibitor of reverse transcriptase (NNRTI) selected from nevirapine, efavirenz and etravirine; a nucleoside inhibitor of reverse transcriptase (NRTI) selected from lamivudine and emtricitabine; and two different nucleoside or nucleotide inhibitors of reverse transcriptase (NRTI) selected from didanosine, abacavir and tenofovir.Type: ApplicationFiled: November 19, 2010Publication date: October 25, 2012Inventor: Jacques Leibowitch
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Publication number: 20120269865Abstract: The present disclosure relates to nutritional compositions comprising a fructo-oligosaccharide (FOS) in an amount of 35 to 44% by weight; a polysaccharide that is not a partially hydrolyzed guar gum such as, for example, an arabinogalactan in an amount of 50% to 38% by weight; and inulin in an amount of 12% to 24% by weight. The FOS and the polysaccharide may be present in a weight ratio of about 1:1. More specifically, the FOS and inulin may be present in a weight ratio of about 7:3. Also provided are methods of promoting gut microbiota balance and health. The methods include administering an effective amount of the nutritional composition to patients in need of same.Type: ApplicationFiled: November 11, 2010Publication date: October 25, 2012Applicant: NESTEC S.A.Inventors: Zamzam (Fariba) Roughead, Jalil Benyacoub, Claudia Roessle, Jennifer Rae Mager, Julie Ann Swanson, Norman Alan Greenberg, Douglas Richard Bolster, Clara Lucia Garcia Rodenas, Florence Rochat
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Patent number: 8293778Abstract: The present invention relates to a method of treating an HIV-I infection with a compound according to formula I where R1, R2, R3, R4, R5, are as defined herein.Type: GrantFiled: February 20, 2010Date of Patent: October 23, 2012Assignee: Roche Palo Alto LLCInventors: James Patrick Dunn, Todd Richard Elworthy, Dimitrios Stefanidis, Zachary Kevin Sweeney
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Patent number: 8293720Abstract: The present invention provides substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: December 18, 2008Date of Patent: October 23, 2012Assignee: Dogwood Pharmaceuticals, Inc.Inventors: Robert D Thompson, Anthony Beauglehole, Frank Schmidtmann, Jayson M. Rieger
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Publication number: 20120264707Abstract: 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: May 4, 2012Publication date: October 18, 2012Applicants: 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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Patent number: 8288526Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).Type: GrantFiled: July 30, 2010Date of Patent: October 16, 2012Assignee: Ajinomoto Co., Inc.Inventors: Takayoshi Torii, Kunisuke Izawa, Doo Ok Jang, Dae Hyan Cho
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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: 20120232028Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.Type: ApplicationFiled: May 21, 2012Publication date: September 13, 2012Applicant: Tobira Therapeutics, Inc.Inventors: Mitsuru SHIRAISHI, Masanori BABA, Katsuji AIKAWA, Naoyuki KANZAKI, Masaki SETO, Yuji IIZAWA
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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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Patent number: 8263574Abstract: Disclosed herein are topical formulations for treating depression with S adenosyl methionine (SAM-e) The topical formulations contain at least 35% wt/wt of SAM-e partially dissolved in aqueous and lipophilic phases of an emulsion and the emulsion is stable from separation of phases for a period of at least 30 days despite the high concentration of SAM-e. Also provided are methods for making such compositions and methods of treating depression using the same.Type: GrantFiled: September 29, 2004Date of Patent: September 11, 2012Inventors: James L. Schaller, Ben Briggs
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Patent number: 8258115Abstract: The present invention refers to new salts of S-adenosyknethionine (SAMe) with improved stability and containing at least 70% by weight of SAMe.Type: GrantFiled: October 22, 2007Date of Patent: September 4, 2012Assignee: Gnosis SpAInventors: Ermanno Valoti, Daniele Giovannone, Marco Berna
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Patent number: 8252767Abstract: The present invention provides substituted 4-{3-[6-amino-9-(3,4-dihydroxy-tetrahydro-furan-2-yl)-9H-purin-2-yl]-prop-2-ynyl}-piperidine-1-carboxylic acid esters and pharmaceutical compositions containing the same that are selective agonists of A2A adenosine receptors (ARs). These compounds and compositions are useful as pharmaceutical agents.Type: GrantFiled: December 20, 2008Date of Patent: August 28, 2012Assignee: Dogwood Pharmaceuticals, Inc.Inventors: Robert Thompson, Anthony Beauglehole, Frank Schmidtmann, Jayson Rieger
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Patent number: 8252920Abstract: The present invention provides a method for producing an inosine derivative represented by the following general formula (1) including the steps of subjecting an inosine derivative of general formula (3) to dithiocarbonylation and carrying out radical reduction of the obtained compound. According to the present invention there can be produced compounds useful as anti-AIDS drugs on industrial scale. wherein R1 may be the same or different and are each benzyl group, benzhydryl group or trityl group, each of which may have a substituent in general formulas (1) and (3).Type: GrantFiled: July 30, 2010Date of Patent: August 28, 2012Assignee: Ajinomoto Co., Inc.Inventors: Takayoshi Torii, Kunisuke Izawa, Doo Ok Jang, Dae Hyan Cho
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Patent number: 8247382Abstract: A method for increasing oxytocin release through direct action on the epidermal keratinocytes is provided. The method for increasing oxytocin release in the epidermis includes increasing the calcium ion concentration in the epidermal cells. In the method of the present invention, the increase of the calcium ion concentration in the epidermal cells may be achieved by physically stimulating the skin. The physical stimulation may be achieved by applying a heat stimulus and/or a massage. The increase of the calcium ion concentration in the epidermal cells may be achieved by stimulating the epidermal cells by at least one agent selected from the group consisting of ATP, UTP, 4 alpha-phorbol 12,13-didecanoate, and pharmaceutically acceptable salts thereof.Type: GrantFiled: November 12, 2009Date of Patent: August 21, 2012Assignee: Shiseido Company, Ltd.Inventors: Sumiko Denda, Mitsuhiro Denda, Kazuyuki Ikeyama
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Patent number: 8242087Abstract: 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: GrantFiled: August 27, 2009Date of Patent: August 14, 2012Assignee: K.U.Leuven Research & DevelopmentInventors: Olga Adelfinskaya, Piet Herdewijn
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Publication number: 20120196826Abstract: 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 disease.Type: ApplicationFiled: March 6, 2012Publication date: August 2, 2012Inventor: Steven Baranowitz
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Patent number: 8227431Abstract: The present patent application relates to the novel nucleoside derivatives and novel intermediates, which are useful to antiviral, anti tumor and immunomodulatory activity, method of treating diseases, conditions and/or disorders modulated by viral infections with them, and processes for preparing them.Type: GrantFiled: March 12, 2009Date of Patent: July 24, 2012Assignee: Hetero Drugs LimitedInventors: Bandi Parthasaradhi Reddy, Vedula Manohar Sharma, Kura Rathnakar Reddy, Musku Madhanmohan Reddy, Jennepalli Sreenu, Aryasomayajula Ratnakar
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Publication number: 20120177601Abstract: This present invention provides for a new class of HCV NS3/4A protease inhibitors as additional therapeutics for hepatitis C virus. The proposed compounds, biliverdin, bilirubin, and derivatives thereof, are based on natural enzymatic products of heme metabolism that may be more stable, better tolerated, and more resistant to mutations than present prototypic protease inhibitors.Type: ApplicationFiled: June 9, 2010Publication date: July 12, 2012Applicants: THE USA AS REPRESENTED BY THE SECRETARY OF THE DEPARTMENT OF VETERANS AFFAIRS, THE UNIVERSITY OF IOWA RESEARCH FOUNDATIONInventor: Warren Schmidt
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Patent number: 8217014Abstract: Disclosed is a pharmaceutical composition for the prevention or treatment of blood clotting disorder which can reduce a burden on a patient. The pharmaceutical composition comprises an effective amount of ribavirin or a derivative thereof or a pharmaceutically acceptable salt of ribavirin or the derivative.Type: GrantFiled: March 9, 2006Date of Patent: July 10, 2012Assignee: National University Corporation Nagoya UniversityInventors: Takashi Honda, Junki Takamatsu, Hidenori Toyoda, Koji Yamamoto, Hidemi Goto
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Patent number: 8211863Abstract: This invention relates to methods for treating or preventing hepatitis C virus infections in mammals using Toll-Like Receptor (TLR)7 ligands and prodrugs thereof. More particularly, this invention relates to methods of orally administering a therapeutically effective amount of one or more prodrugs of TLR7 ligands for the treatment or prevention of hepatitis C viral infection. Oral administration of these TLR7 immunomodulating ligands and prodrugs thereof to a mammal provides therapeutically effective amounts and reduced undesirable side effects.Type: GrantFiled: October 7, 2011Date of Patent: July 3, 2012Assignee: Anadys Pharmaceuticals, Inc.Inventor: Devron R. Averett
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Patent number: 8211466Abstract: A mucosal bioadhesive slow release carrier comprising an active principle and devoid of starch, lactose, which can release the active principal for a duration of longer than 20 hours. This bioadhesive carrier contains a diluent, an alkali metal alkylsulfate, a binding agent, at least one bioadhesive polymer and at least one sustained release polymer, as well as a method for its preparation.Type: GrantFiled: February 17, 2010Date of Patent: July 3, 2012Assignee: Bioalliance PharmaInventors: Dominique Costantini, Caroline Lemarchand
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Patent number: 8211869Abstract: The present invention relates to a method of modulating pluripotency and/or self-renewing characteristics of a stem/progenitor cell. The method comprises administering to the respective cell a compound of the general formula (I) In the general formula A is C or N. R1, R4 and R5 are, independently selected, H or aliphatic, cycloaliphatic, aromatic, arylaliphatic, or arylcycloaliphatic hydrocarbyl groups, that comprise 0-3 heteroatoms being N, O, S, or Si. R4 and R5 may optionally be linked so as to define an aliphatic hydrocarbyl bridge. R2 is H or a halogen. R3 is H, or an aliphatic or arylaliphatic hydrocarbyl group comprising 1-8 main chain carbon atoms and 0-3 heteroatoms being N, O, S, Si, or a halogen.Type: GrantFiled: September 26, 2011Date of Patent: July 3, 2012Assignee: Agency for Science, Technology and ResearchInventors: Qiang Yu, Jing Tan, Xiao Jing Yang
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Publication number: 20120165284Abstract: The present invention is based on the clinical finding that twice daily administrations of 2 mg of 1-[N6-(3-iodobenzyl)-adenin-9-yl]-?-D-ribofuronamide (IB-MECA) (total daily administration of 4 mg) to subjects having moderate to severe psoriasis, was significantly more effective in treatment of the psoriatic plaques than treatment of psoriasis at two administration doses of 1 mg or 4 mg (total daily doses of 2 or 8 mg, respectively). Thus, the present invention provides a pharmaceutical composition for the treatment of psoriasis comprising as the active ingredient IB-MECA in an amount suitable for a total daily dose administration of about 4 mg. In one preferred embodiment IB-MECA is administered twice a day to a subject in need of psoriasis treatment, the pharmaceutical composition comprising an administration dose of 2 mg.Type: ApplicationFiled: September 6, 2010Publication date: June 28, 2012Applicant: Can-Fite Biopharma Ltd.Inventor: Pnina Fishman
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Publication number: 20120165251Abstract: The present invention relates to methods for treating and/or preventing metabolic diseases comprising the combined administration of a DPP-4 inhibitor and a long-acting insulin. The invention further relates to a DPP-4 inhibitor for subcutaneous or transdermal use.Type: ApplicationFiled: June 23, 2011Publication date: June 28, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Thomas KLEIN, Michael MARK, Leo THOMAS
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Publication number: 20120165286Abstract: Disclosed herein are cyclic nucleotide analogs, methods of synthesizing cyclic nucleotide analogs and methods of treating diseases and/or conditions such as viral infections, cancer, and/or parasitic diseases with cyclic nucleotide analogs.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: ALIOS BIOPHARMA, INC.Inventors: Leonid Beigelman, David Bernard Smith, Jerome Deval, Vivek Kumar Rajwanshi
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Patent number: 8202850Abstract: 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: December 1, 2010Date of Patent: June 19, 2012Assignee: Idera Pharmaceuticals, Inc.Inventors: Sudhir Agrawal, Ekambar R. Kandimalla, Dong Yu, Lakshmi Bhagat
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Patent number: 8197807Abstract: The present invention relates to isolated nicotinamide riboside kinase (Nrk) nucleic acid sequences, vectors and cultured cells containing the same, and Nrk polypeptides encoded thereby. Methods for identifying individuals or tumors susceptible to nicotinamide riboside-related prodrug treatment and methods for treating cancer by administering an Nrk nucleic acid sequence or polypeptide in combination with a nicotinamide riboside-related prodrug are also provided. The present invention further provides screening methods for isolating a nicotinamide riboside-related prodrug and identifying a natural source of nicotinamide riboside.Type: GrantFiled: April 20, 2006Date of Patent: June 12, 2012Assignee: Trustees of Dartmouth CollegeInventor: Charles M. Brenner
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Publication number: 20120142626Abstract: Disclosed herein are 2?-spiro-nucleosides and derivatives thereof useful for treating a subject infected by hepatitis C virus or dengue virus.Type: ApplicationFiled: November 30, 2011Publication date: June 7, 2012Applicant: Pharmasset, Inc.Inventors: JINFA DU, Michael Joseph Sofia
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Publication number: 20120135950Abstract: Compositions and methods to treat lymphoma and cancer are disclosed. In particular, the method teaches treatment of lymphoma and cancer using anti-HERV-K(HML-2) therapies. Further taught are compositions and methods for characterizing patient samples to, for example, select or identify therapeutic options or assess the impact of therapies.Type: ApplicationFiled: May 21, 2010Publication date: May 31, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF MICHIGANInventors: Mark H. Kaplan, Rafael Contreras-Galindo, David Markovitz
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Patent number: 8188222Abstract: [Problems] A derivative of a nucleic acid antimetabolite is demanded which can show a higher therapeutic effect at a lower dose. [Means for Solving Problems] Disclosed is a high molecular weight derivative a nucleic acid antimetabolite, which is characterized by comprising a high molecular weight compound comprising a polyethylene glycol moiety and a polymer moiety having a carboxyl group in a side chain and a nucleoside derivative which can act as a nucleic acid antimetabolite, wherein the nucleoside derivative is bound to the carboxyl group in the side chain of the high molecular weight compound via a highly hydrophobic linker.Type: GrantFiled: November 6, 2007Date of Patent: May 29, 2012Assignee: Nippon Kayaku Kabushiki KaishaInventors: Keiichiro Yamamoto, Kazutoshi Takashio
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Patent number: 8188055Abstract: Disclosed are compounds that are AGT inactivators that include a folate residue, e.g., a compound of formula (I), wherein X1, X2, R1, and R2 are as described herein. Also disclosed is a pharmaceutical composition comprising a compound of the invention and a pharmaceutically acceptable carrier. Also disclosed are methods of enhancing the chemotherapeutic treatment of tumor cells and inactivating AGT in a tumor cell. The methods comprise, inter alia, administering a compound or pharmaceutically acceptable salt of formula (I).Type: GrantFiled: March 12, 2008Date of Patent: May 29, 2012Assignees: The United States of America, as represented by the Secretary, Department of Health and Human Services, The Penn State Research FoundationInventors: Robert C. Moschel, Matthew Karl Moschel, legal representative, Anthony E. Pegg, Sahar Javanmard, Natalia Loktionova, Gary Pauly
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Publication number: 20120115805Abstract: A method for influencing the natural pigmentation process of skin or appendages thereof, includes the step of topically contacting the skin or appendages thereof with at least one nucleic acid containing at least 55% guanine nucleotide.Type: ApplicationFiled: January 20, 2012Publication date: May 10, 2012Applicant: Henkel AG & Co. KGaAInventors: Melanie Giesen, Andreas Bock, Erik Schulze zur Wiesche
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Patent number: 8173621Abstract: 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: GrantFiled: June 5, 2009Date of Patent: May 8, 2012Assignee: Gilead Pharmasset LLCInventors: Jinfa Du, Dhanapalan Nagarathnam, Ganapati Reddy Pamulapati, Bruce S. Ross, Michael Joseph Sofia
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Patent number: 8173620Abstract: The disclosure encompasses caged compounds such as caged nucleoside phosphoesters (caged nucleotides). In an embodiment, the caged nucleotides include compounds corresponding to those described by formula (I) that may be activated by two-photon excitation, and methods of synthesis of such compounds. 8-Bromo-7-hydroxyquinoline-caged ATP was synthesized and examined for its photochemistry as a biologically useful, temporally and spatially controlled ATP-releasing reagent. The combination of two-photon excitation hydrolysis and activation of caged ATP enables methods for finely focusing ATP activation at the sub-cellular level or to a greater depth of activation, thereby providing improved resolution of ATP-dependent processes at the cellular level.Type: GrantFiled: August 20, 2009Date of Patent: May 8, 2012Assignee: University of Georgia Research Foundation, Inc.Inventors: Timothy M. Dore, Yue Zhu, Khalilah G. Reddie, James D. Lauderdale
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Publication number: 20120093738Abstract: The present invention relates to taste-masked oral formulations of influenza antivirals. The taste-masked pharmaceutical formulations for oral administration comprise one or more influenza antivirals, at least one taste-masking agent and at least one pharmaceutically acceptable excipient. Further, the taste-masked influenza antiviral formulations of the present invention are provided in the form of dispersible tablets, effervescent tablets, orally disintegrating tablets, chewable tablets, bite-dispersion tablets or the like, wherein the bitter taste of influenza antivirals is masked thereby providing palatable formulations.Type: ApplicationFiled: June 10, 2010Publication date: April 19, 2012Applicant: Rubicon Research Private LimitedInventors: Pratibha Sudhir Pilgaonkar, Maharukh Tehmasp Rustomjee, Anilkumar Surendrakumar Gandhi
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Publication number: 20120094948Abstract: 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: December 20, 2011Publication date: April 19, 2012Inventors: Giancarlo Naccari, Sergio Baroni
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Patent number: 8153608Abstract: The invention relates to the therapeutic use of oligonucleotides as immunostimulatory agents in immunotherapy applications. More particularly, the invention provides immunomers and an immunostimulatory oligonucleotides for use in methods for generating an immune response or for treating a patient in need of immunostimulation. The immunomers and an immunostimulatory oligonucleotides of the invention preferably comprise novel purines. The immunomers according to the invention further 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 immunomodulatory oligonucleotide and having an accessible 5? end.Type: GrantFiled: November 23, 2010Date of Patent: April 10, 2012Assignee: Idera Pharmaceuticals, Inc.Inventors: Sudhir Agrawal, Lakshmi Bhagat, Dong Yu, Ekambar R. Kandimalla
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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: 20120064127Abstract: It has now been found that after administration to a diseased person or person that is at risk for developing such disease of a neutraceutical or pharmaceutical composition that comprises a) a lipid fraction comprising at least one of docosahexaenoic acid (DHA), docosapentaenoic acid (DPA) and eicosapentaenoic acid (EPA); b) a protein fraction comprising proteinaceous material from non-human origin which provide at least cysteine and/or taurine; and c) a mineral fraction comprising at least one of manganese and molybdenum, the health of these persons improves. Membrane function of several types of mammalian cells improves, which allows efficient treatment of immune related disorders, such as allergy, autoimmune diseases, cancer, cognitive dysfunction and other diseases of the nervous system, neuropathies, such as diabetic neuropathies and neuropathic pains, neuronal damage during insulin resistance, and gut diseases and support of the development of gut and lung function during growth or recovery.Type: ApplicationFiled: November 11, 2011Publication date: March 15, 2012Applicant: N.V.NUTRICIAInventor: Robert J.J. Hageman