Purines (including Hydrogenated) (e.g., Adenine, Guanine, Etc.) Patents (Class 514/45)
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Patent number: 9387220Abstract: The present application provides methods and compositions for inducing hepatocyte proliferation and liver regeneration, the latter being mainly dependent on hepatocyte proliferation even if all the other cell types divide to reconstitute the organ specific-lobular-architecture. The methods and compositions provided herein make use of an A3AR agonist. A preferred A3AR agonist disclosed herein is Cl-IB-MECA.Type: GrantFiled: August 21, 2014Date of Patent: July 12, 2016Assignee: CAN-FITE BIOPHARMA LTD.Inventors: Pnina Fishman, Shira Cohen
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Patent number: 9315535Abstract: The present invention provides compounds shown by the formula: wherein Y1 is CR6 or N, Y2 is CR7 or N, Y3 is CR8 or N, R6, R7 and R8 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, Bx is a nucleic acid base moiety, Z1 and Z2 are each independently, a hydrogen atom, a hydroxyl protecting group or a reactive phosphorus group, R1 to R5 are each independently, a hydrogen atom, halogen, cyano, substituted or unsubstituted alkyl or the like, and n is an integer of 0 to 3, or salts thereof, that are novel nucleosides or nucleotides that can be useful as materials for synthesizing nucleic acid pharmaceuticals.Type: GrantFiled: February 17, 2014Date of Patent: April 19, 2016Assignee: SHIONOGI & CO., LTD.Inventors: Yasunori Mitsuoka, Akira Kugimiya, Aiko Yamashita
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Patent number: 9315545Abstract: Compounds and methods are described herein that can be used to treat subjects for conditions related to hepcidin activity, such as but not limited diseases of iron metabolism, beta thalassemia, hemochromatosis, iron-loading anemias, alcoholic liver disease, or chronic hepatitis C.Type: GrantFiled: April 7, 2015Date of Patent: April 19, 2016Assignee: MERGANSER BIOTECH, INC.Inventor: Gene Scott Merutka
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Patent number: 9301960Abstract: The invention provides compositions for inhibiting a redox-sensitive GTPase protein, including a Rho or Rab family GTPase, comprising an effective amount of a redox-sensitive purine compound and an effective amount of a redox agent. The invention further provides methods of inhibiting a redox-sensitive GTPase protein, including a Rho or Rab family GTPase, by administering compositions of the invention. Methods of screening for compounds that inhibit a redox-sensitive GTPase protein, including compounds that target and inhibit Rho or Rab family GTPases, are further provided.Type: GrantFiled: March 27, 2014Date of Patent: April 5, 2016Assignee: Board of Regents, The University of Texas SystemsInventor: Jongyun Heo
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Patent number: 9290533Abstract: 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: GrantFiled: March 22, 2013Date of Patent: March 22, 2016Assignees: Novartis AG, Centre National de la Recherche Scientifique, L'Universite Montpellier IIInventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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Patent number: 9249409Abstract: A method for detecting a cancer(s) based on an expression of prescribed polypeptides is disclosed. These polypeptides were isolated, by the SEREX method using a cDNA library derived from canine testis and serum from a cancer-bearing dog, as a polypeptide which binds to an antibody existing in serum derived from cancer-bearing living body. Because these polypeptides react with antibodies specifically existing in serum of a cancer patient, cancers in a living body can be detected by measuring the antibody in a sample. Cancers in a living body can also be detected by measuring the antigen protein of the antibody per se or mRNA encoding it.Type: GrantFiled: October 23, 2008Date of Patent: February 2, 2016Assignee: TORAY INDUSTRIES, INC.Inventors: Fumiyoshi Okano, Kana Suzuki
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Patent number: 9247875Abstract: A method of diagnosing a patient with age-related macular degeneration (AMD), by detecting biomarkers in the patient's Bruch's membrane, and diagnosing the patient with AMD. A method of detecting the presence of AMD in a patient, by detecting biomarkers in the patient's Bruch's membrane. A method of detecting inflammation in a patient, by detecting biomarkers in the patient's Bruch's membrane. A method of determining the progression of AMD in a patient. A method of determining efficacy of a treatment for AMD in a patient. A method of determining the presence of AMD in an animal model. A kit for detecting the presence of disease in a patient, including an assay for biomarkers 3-nitrotyrosine and nitro-A2E. An assay of the biomarkers.Type: GrantFiled: April 2, 2010Date of Patent: February 2, 2016Assignee: Board of Trustees of Northern Illinois UniversityInventors: Elizabeth R. Gaillard, James P. Dillon
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Patent number: 9221864Abstract: The present disclosure provides tricyclic nucleosides and oligomeric compounds prepared therefrom. The tricyclic nucleosides each have a tricyclic ribosyl sugar moiety wherein a bridge between the 2? and 4? ribosyl ring carbon atoms further comprises a fused carbocyclic or heterocyclic ring. The tricyclic nucleosides are expected to be useful for enhancing properties of oligomeric compounds including for example binding affinity and nuclease resistance.Type: GrantFiled: March 20, 2013Date of Patent: December 29, 2015Assignee: Isis Pharmaceuticals, Inc.Inventors: Punit P. Seth, Eric E. Swayze, Stephen Hanessian, Benjamin R. Schroeder, Robert D. Giacometti, Bradley L. Merner
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Patent number: 9134313Abstract: A tumor marker comprising diacetylspermine, and a method of evaluating the state of a tumor, comprising reacting an antibody to diacetylspermine with a biological sample to thereby detect diacetylspermine and evaluating the state of the tumor using the obtained detection results as an indicator.Type: GrantFiled: June 9, 2009Date of Patent: September 15, 2015Assignees: Tokyo Metropolitan Organization For Medical Research, CRC Inc., Tokyo Metropolitan Government, Trans Genic Inc.Inventors: Masao Kawakita, Kyoko Hiramatsu, Keiichi Takahashi, Naotaka Hamasaki, Koji Yamaguchi, Tsunehisa Kaku, Koichiro Muta, Munechika Enjoji, Seiji Naito, Jun Hayashi, Shoshu Mitsuyama, Hiroyuki Yamashita, Toru Inoue, Masato Kato
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Patent number: 9090646Abstract: The invention provides new biotinylated compounds and methods for their use.Type: GrantFiled: December 4, 2013Date of Patent: July 28, 2015Assignee: Rutgers, The State University of New JerseyInventors: Roger A. Jones, Barbara L. Gaffney
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Patent number: 9078910Abstract: The present invention relates to compositions comprising spicamycin derivatives, methods of making such compositions, and their use in the treatment and/or prevention of pain, including neuropathic pain.Type: GrantFiled: August 8, 2013Date of Patent: July 14, 2015Assignee: DARA BIOSCIENCES, INC.Inventors: Michael Radomsky, Mary Katherine Delmedico, Linda Jett
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Patent number: 9062046Abstract: The present invention relates to substituted imidazo[4,5-c]quinoline derivatives, the compounds of formula (I), wherein R1, R2, R3, R4, R5, R6 and R7 are as defined in the specification, processes for their preparation, pharmaceutical compositions comprising compounds of formula (I), and their use in the treatment of diseases or disorders mediated by one or more kinases, particularly proliferative diseases or disorders such as cancer. These compounds can also be used in the treatment of inflammatory diseases and angiogenesis related disorders.Type: GrantFiled: July 15, 2011Date of Patent: June 23, 2015Assignee: Piramal Enterprises LimitedInventors: Sanjay Kumar, Rajiv Sharma, Robert Zahler, Bichismita Sahu, Veena R. Agarwal, Nishigandha Naik
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Patent number: 9040498Abstract: The present invention relates to novel 1,2,3-triazolyl purine derivatives. The invention also relates to using the derivatives to treat cancer and various viral infections.Type: GrantFiled: July 8, 2013Date of Patent: May 26, 2015Assignee: Research Foundation of the City University of New YorkInventor: Mahesh K. Lakshman
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Publication number: 20150141362Abstract: The invention relates to inhibition of wild-type and certain mutant forms of human histone methyltransferase EZH2, the catalytic subunit of the PRC2 complex which catalyzes the mono- through tri-methylation of lysine 27 on histone H3 (H3-K27). In one embodiment the inhibition is selective for the mutant form of the EZH2, such that trimethylation of H3-K27, which is associated with certain cancers, is inhibited. The methods can be used to treat cancers including follicular lymphoma and diffuse large B-cell lymphoma (DLBCL). Also provided are methods for identifying small molecule selective inhibitors of the mutant forms of EZH2 and also methods for determining responsiveness to an EZH2 inhibitor in a subject.Type: ApplicationFiled: November 13, 2014Publication date: May 21, 2015Inventors: Robert A. Copeland, Victoria M. Richon, Margaret D. Scott, Christopher J. Sneeringer, Kevin W. Kuntz, Sarah K. Knutson, Roy M. Pollock
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Publication number: 20150132258Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.Type: ApplicationFiled: November 14, 2014Publication date: May 14, 2015Inventor: George D. Hartman
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Patent number: 9029345Abstract: An agent for inhibiting P-glycoproteins comprises a non-natural adenine ribose analog.Type: GrantFiled: November 16, 2007Date of Patent: May 12, 2015Assignee: Case Western Reserve UniversityInventors: Anthony J. Berdis, Irene Lee
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Patent number: 9029335Abstract: Provided herein are novel bicyclic nucleosides, oligomeric compounds that include such bicyclic nucleosides and methods of using the oligomeric compounds. More particularly, the novel bicyclic nucleosides comprise a furanose ring system having a bridge comprising a 4?-methylene group attached to a 2?-sulfoxide or sulfone group and optionally including one or more substituent groups attached to the 4?-methylene and or the 5?-position. In certain embodiments, the oligomeric compounds provided herein are expected to hybridize to a portion of a target RNA resulting in loss of normal function of the target RNA.Type: GrantFiled: October 9, 2013Date of Patent: May 12, 2015Assignee: Isis Pharmaceuticals, Inc.Inventors: Thazha P. Prakash, Eric E. Swayze
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Patent number: 9029343Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, and the uses of the compounds and compositions as modulators of histone methyltransferases, and for treating diseases influenced by modulation of histone methyltransferase activity.Type: GrantFiled: December 5, 2011Date of Patent: May 12, 2015Assignee: Epizyme, Inc.Inventors: Richard Chesworth, Kevin W. Kuntz, Edward J. Olhava, Michael A. Patane
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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: 9006207Abstract: Compounds and compositions for treating disorders related to TRPA1 are described herein.Type: GrantFiled: January 8, 2013Date of Patent: April 14, 2015Assignee: Hydra Biosciences, Inc.Inventors: Howard Ng, Jianfeng Hang
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Publication number: 20150087613Abstract: The invention provides methods and compositions for inhibiting opioid tolerance by administering an A3AR agonist to a subject receiving opiate therapy for nociceptive pain. Also provided are methods of treating opiate withdrawal using an A3AR agonist.Type: ApplicationFiled: September 25, 2014Publication date: March 26, 2015Inventor: Daniela SALVEMINI
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Publication number: 20150079107Abstract: Provided herein are methods and assays for isolating and culturing seborrheic keratosis cells ex vivo. Also provided herein are screening assays using cultured seborrheic keratosis cells and methods for treating seborrheic keratosis in a subject.Type: ApplicationFiled: April 26, 2013Publication date: March 19, 2015Applicant: THE GENERAL HOSPITAL CORPORATIONInventors: Anna I. Mandinova, Sam W. Lee, Victor A. Neel
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Patent number: 8980850Abstract: The present disclosure relates to methods for the treatment of cancer in patients in recognized need of such treatment. The methods comprise administering to such a patient an NAE inhibitor or a pharmaceutically acceptable salt thereof, such as ((1S,2S,4R)-4-(4-((1S)-2,3-dihydro-1H-inden-1-ylamino)-7H-pyrrolo[2,3-d]pyrimidin-7-yl)-2-hydroxycyclopentyl)methyl sulfamate (MLN4924) or {(1S,2S,4R)-4-[(6-{[(1R,2S)-5-chloro-2-methoxy-2,3-dihydro-1H-inden-1-yl]amino}pyrimidin-4-yl)oxy]-2-hydroxycyclopentyl}methyl sulfamate (I-216), and a hypomethylating agent or a pharmaceutically acceptable salt thereof, such as azacitidine or decitabine. Also disclosed are medicaments for use in the treatment of cancer.Type: GrantFiled: November 2, 2012Date of Patent: March 17, 2015Assignee: Millennium Pharmaceuticals, Inc.Inventor: Peter G. Smith
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Publication number: 20150057243Abstract: Methods and compositions disclosed herein relate to detecting, analyzing, isolating and inhibiting methyltransferases, methyltransferase substrates, S-adenosyl-methionine-binding proteins and RNA, including for the treatment of disease.Type: ApplicationFiled: April 2, 2013Publication date: February 26, 2015Applicant: Northern UniversityInventors: Zhaohui Sunny Zhou, Wanlu Qu, Tianyi Bai
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Publication number: 20150051167Abstract: 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: March 19, 2013Publication date: February 19, 2015Inventors: Guangyi Wang, David Bernard Smith, Leonid Beigelman, Jerome Deval, Marija Prhavc
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Patent number: 8951985Abstract: Provided herein are compounds, compositions and methods for the treatment of liver disorders, including HCV infections. In one embodiment, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents.Type: GrantFiled: September 11, 2012Date of Patent: February 10, 2015Assignee: Idenix Pharmaceuticals, Inc.Inventors: Dominique Surleraux, Cyril B. Dousson, David Dukhan, Claire Pierra
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Patent number: 8946188Abstract: Many pathogens, including Mycobacterium tuberculosis and Yersinia pestis, rely on an iron acquisition system based on siderophores, secreted iron-chelating compounds with extremely high Fe(III) affinity. The compounds of the invention are inhibitors of domain salicylation enzymes, which catalyze the salicylation of an aroyl carrier protein (ArCP) domain to form a salicyl-ArCP domain thioester intermediate via a two-step reaction. The compounds include the intermediate mimic 5?-O—[N-(salicyl)sulfamoyl]-adenosine (salicyl-AMS) and analogs thereof. These compounds are inhibitors of the salicylate activity of MbtA, YbtE, PchD, and other domain salicylation enzymes involved in the biosynthesis of siderophores. Therefore, these compounds may be used in the treatment of infection caused by microorganisms which rely on siderphore-based iron acquisition systems.Type: GrantFiled: May 20, 2013Date of Patent: February 3, 2015Assignees: Sloan-Kettering Institute for Cancer Research, Cornell Research Foundation, Inc.Inventors: Derek Shieh Tan, Luis E. N. Quadri, Jae-Sang Ryu, Justin Scott Cisar, Julian Alberto Ferreras, Xuequan Lu
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Publication number: 20150025031Abstract: The present invention provides a system and method of maintaining and/or increasing cell viability by downregulating cellular metabolic rate under hypoxic conditions, wherein the availability of adenosine or derivatives thereof in the cell is increased and/or prolonged. The present invention also relates to a system and method of prolonging the survival of implanted cells that are under hypoxic condition until host neovascularization is achieved, wherein the availability of adenosine or derivatives thereof in the cell is increased and/or prolonged. The present invention also provides a system and method of maintaining and/or increasing cell viability by downregulating cellular metabolic rate under hypoxic conditions, wherein at least one purine metabolism enzyme inhibitor is applied to the cell.Type: ApplicationFiled: March 5, 2013Publication date: January 22, 2015Inventors: James Yoo, Sang Jin Lee, Jachyun Kim, Anthony Atala
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Publication number: 20150018297Abstract: The present disclosure relates to a pharmaceutical composition, a health functional food composition, and a method for preventing or treating a brain disease or diabetes. The pharmaceutical composition, health functional food composition, and method includes at least one active ingredient that is chlorhexidine, thioguanosine, mebendazole, fenbendazole, colchicine, farnesol, trimethobenzamide hydrochloride, disulfuram, azathioprine, mebeverine hydrochloride, zaprinast, tosufloxacin hydrochloride, efavirenz, thiostrepton, probenecid, entacapone, harmine hydrochloride, flunisolide, thimerosal, hexestrol, sulfaquinoxaline sodium salt, monensin sodium salt, raloxifene hydrochloride, 2-chloropyrazine, or topotecan.Type: ApplicationFiled: July 14, 2014Publication date: January 15, 2015Applicant: RESEARCH & BUSINESS FOUNDATION SUNGKYUNKWAN UNIVERSITYInventors: Dong Gyu JO, Jong Sung PARK, Youngkwang YOUN, Yuri CHOI, Ui Jeong YUN
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Publication number: 20150011496Abstract: The invention provides methods and compositions for stimulating or promoting bone regeneration or repairing bone fracture or for stimulating or increasing differentiation or activation of osteoblasts by administering to a subject a therapeutically effective amount of an adenosine receptor agonist, or an analog, derivative or combination thereof, an adenosine receptor antagonist, or an analog, derivative or combination thereof, or adenosine or a compound that upregulates, increases the amount of or increases the biological activity of adenosine. The invention also extends to pharmaceutical compositions such as those comprising an agent that modulates an adenosine receptor such as an adenosine A2A agonist or A1 antagonist.Type: ApplicationFiled: February 21, 2013Publication date: January 8, 2015Inventors: Bruce Cronstein, Aranzazu Mediero Munoz
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Publication number: 20150011497Abstract: 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 norovirus, with a nucleoside, a nucleotide and an analog thereof.Type: ApplicationFiled: June 24, 2014Publication date: January 8, 2015Inventors: Leonid Beigelman, Jerome Deval, Zhinan Jin
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Patent number: 8927520Abstract: The present invention relates to compounds of formula (I): wherein Rj, R2, R3, R4, Xi, X2, X3 and Z are as defined in claim 1. The compounds are useful in the prevention and/or treatment of bacterial infections.Type: GrantFiled: December 22, 2011Date of Patent: January 6, 2015Assignees: Institut Pasteur, Institut CurieInventors: Sylvie Pochet, Gilles Labesse, Muriel Gelin, Liliane Assairi, Olivier Dussurget, Guillaume Poncet-Montange
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Patent number: 8916535Abstract: The invention relates to the therapeutic uses of 2?,5?-oligoadenylate derivative compounds, more particularly for the treatment of chronic fatigue syndrome (CFS) and in the treatment of infection by a gamma-retrovirus.Type: GrantFiled: November 10, 2011Date of Patent: December 23, 2014Assignee: Protea Biopharma N.V.Inventors: Christiaan Roelant, Kenny De Meirleir
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Patent number: 8916204Abstract: The invention provides methods for predicting or determining the response of a mammalian tumor to a chemotherapeutic agent and for treating a mammalian tumor comprising detecting and quantifying the SPARC protein or RNA in a sample isolated from the mammal. The invention further provides kit for predicting the response of a mammalian tumor to a chemotherapeutic agent, comprising a means for the isolation of protein or RNA from the tumor, a SPARC protein or RNA detection and quantification means, control RNAs, and rules for predicting the response of the tumor based on the level of SPARC protein or RNA in tumor.Type: GrantFiled: March 13, 2013Date of Patent: December 23, 2014Assignee: Abraxis BioSciences, LLCInventors: Vuong Trieu, Neil P. Desai, Patrick Soon-Shiong
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Publication number: 20140364388Abstract: The present application provides methods and compositions for inducing hepatocyte proliferation and liver regeneration, the latter being mainly dependent on hepatocyte proliferation even if all the other cell types divide to reconstitute the organ specific-lobular-architecture. The methods and compositions provided herein make use of an A3AR agonist. A preferred A3AR agonist disclosed herein is Cl-IB-MECA.Type: ApplicationFiled: August 21, 2014Publication date: December 11, 2014Inventors: Pnina FISHMAN, Shira COHEN
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Publication number: 20140357594Abstract: This invention relates to heteroaryl compounds, containing a purinyl moiety, that inhibit DNA methyltransferase (DNMT) activity—including DNMT1, DNMT3a, or DNMT3b—useful in the treatment of cancer and hyperproliferative diseases.Type: ApplicationFiled: October 23, 2012Publication date: December 4, 2014Applicant: GlaxoSmithkline Intellectual Property (No.2) LimitedInventors: Thomas Francis Hendrickson, Koc-Kan Ho, Michael David Saunders, Brian John Stevens, Krzysztof Swierczek, Kevin Bret Wright
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Patent number: 8901092Abstract: Embodiments of the invention include functionalized polysaccharides and compositions and structures including the same. In an embodiment, the invention includes an active agent delivery composition including a polysaccharide functionalized with a coupling group, wherein the polysaccharide lacks charged groups at a pH of between 6 and 8; and a complex comprising a nucleic acid and a transfection agent. In an embodiment, the invention includes an active agent delivery structure including a matrix comprising a polysaccharide covalently cross-linked through the residue of a coupling group on the polysaccharide, the polysaccharide lacking charged groups at a pH of between 6 and 8; and a nucleic acid delivery complex disposed within the active agent delivery structure. In an embodiment, the invention includes a material for medical applications including glycogen functionalized with coupling groups at a degree of substitution of between about 0.01 and 0.5. Other embodiments are also included herein.Type: GrantFiled: December 22, 2011Date of Patent: December 2, 2014Assignee: SurModics, Inc.Inventor: Joram Slager
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Patent number: 8901102Abstract: Compounds containing nucleic acid bases or their precursors modified by enrichment at specific sites with heavy stable isotopes of elements naturally present at those sites in minute amount are useful for the treatment of diseases characterized by altered gene expression and altered pattern of epigenomic control. These compounds, when used as nutrients or in other medicinal application methods, can alter the DNA methylation pattern in a simple way through the well-understood mechanism of kinetic isotope effect (KIE). This effect could also be useful for modifying methylation kinetics in stem cell technology, cloning and as disease therapeutics.Type: GrantFiled: January 27, 2014Date of Patent: December 2, 2014Assignee: Retrotope, Inc.Inventor: Mikhail S. Shchepinov
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Publication number: 20140343006Abstract: This invention concerns HIV replication inhibitors of formula the N-oxides, the pharmaceutically acceptable addition salts, the quaternary amines and the stereochemically isomeric forms thereof, wherein the ring containing -a1=a2-a3=a4- and -b1=b2-b3=b4- represents phenyl, pyridyl, pyrimidinyl, pirazinyl, pyridazinyl; n is 0 to 5; m is 1 to 4; R1 is hydrogen; aryl; formyl; C1-6alkylcarbonyl; C1-6alkyl; C1-6alkyloxycarbonyl; substituted C1-6alkyl, C1-6alkylcarbonyl, C1-6alkyloxycarbonyl, C1-6alkylcarbonyloxy; substituted C1-6alkyloxyC1-6alkylcarbonyl; R2 is hydroxy, halo, optionally substituted C1-6alkyl, C3-7cycloalkyl, optionally substituted C2-6alkenyl, optionally substituted C2-6alkynyl, C1-6alkyloxy, C1-6alkyloxycarbonyl, carboxyl, cyano, nitro, amino, mono- or di(C1-6alkyl)amino, polyhalomethyl, polyhalomethyloxy, polyhalomethylthio, —S(?O)pR6, —NH—S(?O)pR6, —C(?O)R6, —NHC(?O)H, —C(?O)NHNH2, —NHC(?O)R6, —C(?NH)R6 or a 5-membered heterocycle; X1 is —NR5—, —NH—NH—, —N?N—, —O—, —C(?O)—, C1-4alkanediyl,Type: ApplicationFiled: August 5, 2014Publication date: November 20, 2014Inventors: Jerome Emile Georges Guillemont, Patrice Palandijian, Marc Rene DeJonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desire Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Frank Xavier Jozef Herwig Arts
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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: 20140323423Abstract: Systems and methods for longevity, anti-aging, fatigue management, obesity, weight loss, weight management, delivery of nutraceuticals, and treating hyperglycemia, Alzheimer's disease, sleep disorders, Parkinson's disease, Attention Deficit Disorder and nicotine addiction involve synchronizing and tailoring the administration of nutraceuticals, medications and other substances (for example, stimulants) in accordance with the body's natural circadian rhythms, meal times and other factors. Improved control of blood glucose levels, extended alertness, and weight control, and counteracting of disease symptoms when they are at their worst are possible.Type: ApplicationFiled: May 2, 2014Publication date: October 30, 2014Applicant: Chrono Therapeutics, Inc.Inventors: Guy DiPierro, Steven A. Giannos
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Patent number: 8871735Abstract: The invention provides a method of reducing infarct size and/or limiting, decreasing and/or inhibiting reperfusion injury and/or ameliorating heart failure in a patient comprising administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to the patient. The compound capable of inhibiting AC5 is particularly effective when administered during or after reperfusion in patients suffering from an ischemic injury.Type: GrantFiled: November 5, 2012Date of Patent: October 28, 2014Assignee: Rutgers, The State University of New JerseyInventors: Stephen F. Vatner, Dorothy E. Vatner
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Publication number: 20140309188Abstract: A method for treatment of a tumor including administering to a patient in need thereof a pharmaceutical preparation including a combination of a deoxynucleoside and a nucleoside. The deoxynucleoside is selected from deoxyadenosine, deoxyguanosine, deoxycytidine, thymidine, or a mixture thereof. The nucleoside is selected from adenosine, guanosine, cytidine, uridine, deoxyadenosine, deoxyguanosine, deoxycytidine, thymidine, or a mixture thereof.Type: ApplicationFiled: April 17, 2014Publication date: October 16, 2014Inventors: Shizhuang ZHANG, Xin CHENG, Zhiqin GAO, Ming HAN
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Patent number: 8859512Abstract: 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: November 30, 2012Date of Patent: October 14, 2014Assignees: University College Cardiff Consultants Limited, K.U. Leuven Research and DevelopmentInventors: Christopher McGuigan, Jan Balzarini, Marco Migliore
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Patent number: 8859513Abstract: The invention relates to the novel use of 1-beta-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide for the treatment of infectious salmon anaemia caused by the infectious salmon anaemia or ISA virus in salmonids.Type: GrantFiled: June 8, 2010Date of Patent: October 14, 2014Assignee: Laboratorio de Diagnostico Gam, S.A.Inventors: Ana Maria Sandino, Geraldine Mlynarz Zylberberg, Matilde Jashes Morgues, Eugenio Spencer Ossa
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Publication number: 20140303239Abstract: The present disclosure is directed toward pharmaceutical compositions and methods of using 6-mercaptopurine ribosides and analogs thereof for the treatment of cancer and other hyperproliferative diseases. The described compounds can be converted into telomere substrates in vivo and can be recognized by telomerase for incorporation into telomeres of telomerase active cells, leading to induction of cell death of the telomerase active cells.Type: ApplicationFiled: April 8, 2014Publication date: October 9, 2014Applicant: The Board of Regents of The University of Texas SystemInventors: Jerry W. Shay, Sergei M. Gryaznov
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Publication number: 20140294769Abstract: Provided herein are compounds, methods and pharmaceutical compositions for use in treatment of viral infections, including hepatitis C virus (HCV) infections, in hosts in need thereof. In certain embodiments, the compounds are 2?,4?-fluoro nucleosides according to Formula 1001: or a pharmaceutically acceptable salt, solvate, stereoisomeric form, tautomeric form, or polymorphic form thereof, wherein Base, RA, and PD are as described herein. In certain embodiments, 2?,4?-fluoro nucleosides are provided which display remarkable efficacy and bioavailability for the treatment of, for example, HCV infection in a human.Type: ApplicationFiled: April 1, 2014Publication date: October 2, 2014Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART
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Publication number: 20140296176Abstract: The invention provides a method of treating a subject with cancer, particularly leukemia, lymphoma, solid cancer such as colorectal cancer, gastric cancer, bladder cancer, non-small cell lung cancer, and breast cancer, comprising administering to the subject a compound of formulae (I) 40 or (Ia) in combination with an antimetabolite such as methotrexate, pemetrexed, cytarabine or nelarabine, or 5-fluorouracil, or capecitabine or their derivatives.Type: ApplicationFiled: August 17, 2012Publication date: October 2, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: David Proia, Julie Friedland
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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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Patent number: 8846635Abstract: The present application provides methods and compositions for inducing hepatocyte proliferation and liver regeneration, the latter being mainly dependent on hepatocyte proliferation even if all the other cell types divide to reconstitute the organ specific-lobular-architecture. The methods and compositions provided herein make use of an A3AR agonist. A preferred A3AR agonist disclosed herein is Cl-IB-MECA.Type: GrantFiled: October 22, 2008Date of Patent: September 30, 2014Assignee: Can-Fite Biopharma Ltd.Inventors: Pnina Fishman, Shira Cohen