2,4-diketone Pyrimidine Or Derivative (e.g., Uracil, Etc.) Patents (Class 514/50)
  • Publication number: 20150005251
    Abstract: Disclosed herein are nucleosides, nucleotides and analogs thereof, pharmaceutical compositions that include one or more of nucleosides, nucleotides and analogs thereof, and methods of synthesizing the same. Also disclosed herein are methods of ameliorating and/or treating a paramyxovirus viral infection, with a nucleoside, a nucleotide and an analog thereof.
    Type: Application
    Filed: June 24, 2014
    Publication date: January 1, 2015
    Inventors: Natalia Dyatkina, Guangyi Wang, Leonid Beigelman, Vivek Kumar Rajwanshi
  • Publication number: 20150004225
    Abstract: This invention relates to pharmaceutical dosage forms, particularly to pH dependent pharmaceutical dosage forms with enhanced and/or prolonged distribution of a pharmaceutical compound at a target site. More specifically, this invention relates to a controlled release intravaginal pharmaceutical dosage form and, more particularly, to a pharmaceutical dosage form which comprises microspheres encapsulated and/or embedded within a bioerodible polymeric matrix, together the microspheres and the matrix are formed into a caplet and/or tablet.
    Type: Application
    Filed: February 8, 2013
    Publication date: January 1, 2015
    Inventors: Viness Pillay, Yahya Essop Choonara, Felix Mashingaidse, Pradeep Kumar
  • Patent number: 8916538
    Abstract: The present application relates to solid state forms, for example, crystalline forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, pharmaceutical compositions that can include one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate, and methods of treating or ameliorating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate. Also disclosed herein are methods of treating diseases and/or conditions with one or more solid forms of 2?-C-methyluridine-5?-(O-phenyl-N—(S)-1-(isopropoxycarbonyl)ethyl)thiophosphoramidate in combination with one or more other agents.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: December 23, 2014
    Assignee: Vertex Pharmaceuticals Incorporated
    Inventors: Anuj K. Kuldipkumar, Ales Medek, Lori Ann Ferris, Praveen Mudunuri, Young Chun Jung, David Richard Willcox, Michael Waldo, William Aloysius Nugent
  • Publication number: 20140371167
    Abstract: This disclosure relates to uridine nucleoside derivatives, compositions comprising therapeutically effective amounts of those nucleoside derivatives and methods of using those nucleoside derivatives or compositions in treating disorders that are responsive to ligands, such as agonists, of P2Y6 receptor, e.g., neuronal disorders, including neurodegenerative disorders (e.g., Alzheimer's disease, Parkinson's disease) and traumatic CNS injury, pain, Down Syndrome (DS), glaucoma and inflammatory conditions.
    Type: Application
    Filed: March 13, 2014
    Publication date: December 18, 2014
    Applicant: TUFTS UNIVERSITY
    Inventors: Philip G. Haydon, Jinbo Lee
  • Publication number: 20140370005
    Abstract: The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.
    Type: Application
    Filed: June 26, 2014
    Publication date: December 18, 2014
    Inventors: Gary L. Cantrell, Raghavan Rajagopalan, David W. Berberich, Amolkumar Karwa, Richard B. Dorshow
  • Publication number: 20140370006
    Abstract: The invention relates generally to anti-angiogenesis agents and related methods of using to anti-angiogenesis agents for biomedical applications including direct monotherapy and combination therapy for treatment of an angiogenesis related condition. In an embodiment, the invention provides a class of opioid compounds and structurally related opioid derivatives exhibiting anti-VEGF activity for use in therapeutic procedures, including phototherapy. Opioid compounds and structurally related opioid derivatives of the invention may be administered alone or in combination with administration of a phototherapy agent and/or other therapeutic agent.
    Type: Application
    Filed: June 26, 2014
    Publication date: December 18, 2014
    Inventors: Gary L. Cantrell, Raghavan Rajagopalan, David W. Berberich, Amolkumar Karwa, Richard B. Dorshow
  • Publication number: 20140364389
    Abstract: The present invention relates to a combination therapy for treating an HIV infection or inhibiting integrase comprising (S)-6-(3-Chloro-2-fluorobenzyl)-1-(1-hydroxymethyl-2-methylpropyl)-7-methoxy-4-oxo-1,4-dihydroquinoline-3-carboxylic acid (“Compound A”) or a pharmaceutically acceptable solvate or salt thereof in combination with at least one other anti-HIV agent. In some embodiments of the present invention, the other anti-HIV agents are chosen from reverse transcriptase inhibitors and protease inhibitors. In certain embodiments of the present invention, the other anti-HIV agents are chosen from AZT, 3TC, PMPA, efavirenz, indinavir, nelfinavir, a combination of AZT/3TC, and a combination of PMPA/3TC. Since Compound A has a high inhibitory activity specific for integrases, when used in combinations with other anti-HIV agents it can provide a combination therapy with fewer side effects for humans.
    Type: Application
    Filed: December 12, 2013
    Publication date: December 11, 2014
    Applicant: JAPAN TOBACCO INC.
    Inventors: YUJI MATSUZAKI, WATARU WATANABE, SATORU IKEDA, MITSUKI KANO
  • Publication number: 20140363512
    Abstract: The present invention provides an FTD and TPI-containing oral pharmaceutical composition which can be orally administered and is stable even under high humidity conditions. An oral pharmaceutical composition comprising ?,?,?-trifluorothymidine and 5-chloro-6-(2-iminopyrrolidine-1-yl)methyl-2,4(1H,3H)-pyrimidine dione hydrochloride as an active ingredient; and being substantially free of an additive comprising a metal salt.
    Type: Application
    Filed: February 14, 2013
    Publication date: December 11, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventors: Yoshito Ohnishi, Tetsuo Ogata
  • Patent number: 8906880
    Abstract: 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: Grant
    Filed: April 17, 2014
    Date of Patent: December 9, 2014
    Assignee: Gilead Pharmasset LLC
    Inventors: Jinfa Du, Dhanapalan Nagarathnam, Michael Joseph Sofia, Peiyuan Wang
  • Publication number: 20140356431
    Abstract: The present invention provides an FTD and TPI-containing orally administrable pharmaceutical composition which can be orally administered and is stable even under high-humidity conditions. An orally administrable pharmaceutical composition which comprises ?,?,?-trifluorothymidine and 5-chloro-6-(2-iminopyrrolidine-1-yl)methyl-2,4(1H,3H)-pyrimidine dione hydrochloride as active ingredients and additives having a critical relative humidity of 85% or more at 25° C. as an excipient.
    Type: Application
    Filed: February 14, 2013
    Publication date: December 4, 2014
    Applicant: TAIHO PHARMACEUTICAL CO., LTD.
    Inventor: Yoshito Ohnishi
  • Publication number: 20140343006
    Abstract: 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: Application
    Filed: August 5, 2014
    Publication date: November 20, 2014
    Inventors: 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
  • Publication number: 20140336143
    Abstract: A method and composition for the treatment, prevention and/or prophylaxis of a host, and in particular, a human, infected with Epstein-Barr virus (EBV), is provided that includes administering an effective amount of a 5-substituted uracil nucleoside or its pharmaceutically acceptable salt or prodrug, optionally in a pharmaceutically acceptable diluent or excipient.
    Type: Application
    Filed: December 4, 2013
    Publication date: November 13, 2014
    Applicants: GILEAD PHARMASSET LLC, BETH ISRAEL DEACONESS MEDICAL CENTER, EMORY UNIVERSITY
    Inventors: Raymond F. Schinazi, Junxing Shi, Joyce D. Fingeroth, Erik Gustafson
  • Publication number: 20140335048
    Abstract: This disclosure relates, at least in part, to a method of treatment. In one embodiment, the method of treatment comprises administering to a subject in need of such treatment a first therapeutic agent including compound (1): or a pharmaceutically acceptable salt thereof in combination with a second therapeutic agent, wherein the first therapeutic agent and the second therapeutic agent are administered either simultaneously or sequentially.
    Type: Application
    Filed: July 25, 2014
    Publication date: November 13, 2014
    Applicant: ONCOCEUTICS, INC.
    Inventors: Martin STOGNIEW, Joshua E. ALLEN
  • Patent number: 8883759
    Abstract: There is provided an agent for potentiating the effects of an anti-tumor agent. An anti-tumor effect potentiator containing, as an active ingredient, a uracil compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof: wherein X represents a C1-5 alkylene group and one of methylene groups constituting the alkylene group is optionally substituted with an oxygen atom; R1 represents a hydrogen atom or a C1-6 alkyl group; R2 represents a hydrogen atom or a halogen atom; and R3 represents a C1-6 alkyl group, a C2-6 alkenyl group, a C3-6 cycloalkyl group, a (C3-6 cycloalkyl) C1-6 alkyl group, a halogeno-C1-6 alkyl group or a saturated heterocyclic group.
    Type: Grant
    Filed: November 29, 2010
    Date of Patent: November 11, 2014
    Assignee: Taiho Pharmaceutical Co., Ltd.
    Inventors: Masayoshi Fukuoka, Tatsushi Yokogawa, Seiji Miyahara, Hitoshi Miyakoshi, Wakako Yano, Junko Taguchi, Yayoi Takao
  • Publication number: 20140328793
    Abstract: Compounds, compositions, and methods of treatment and prevention of HIV infection are disclosed. The compounds are pyrrolo[2,3-b]pyridines and pyrrolo[2,3-b]pyrimidine JAK inhibitors. Combinations of these JAK inhibitors and additional antiretroviral compounds, such as NRTI, NNRTI, integrase inhibitors, entry inhibitors, protease inhibitors, and the like, are also disclosed. In one embodiment, the combinations include a combination of adenine, cytosine, thymidine, and guanine nucleoside antiviral agents, optionally in further combination with at least one additional antiviral agent that works via a different mechanism than a nucleoside analog. This combination has the potential to eliminate the presence of HIV in an infected patient.
    Type: Application
    Filed: November 30, 2012
    Publication date: November 6, 2014
    Applicant: Emory University
    Inventors: Christina Gavegnano, Raymond F. Schinazi
  • Patent number: 8877731
    Abstract: 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: Grant
    Filed: September 19, 2011
    Date of Patent: November 4, 2014
    Assignee: Alios Biopharma, Inc.
    Inventors: Leonid Beigelman, Jerome Deval, David Bernard Smith, Guangyi Wang, Vivek Kumar Rajwanshi
  • Patent number: 8877734
    Abstract: Provided are novel selenyl-methyluracil compounds and a pharmaceutical composition for enhancing the effect of radiation treatment. The composition contains at least one compound selected from the group consisting of the selenyl-methyluracil compounds or pharmaceutically acceptable salts thereof, as an active ingredient.
    Type: Grant
    Filed: December 23, 2010
    Date of Patent: November 4, 2014
    Assignee: Kongju National University Industry-University Cooperation Foundation
    Inventors: In Seok Hong, Sung Hee Hong, Marc M. Greenberg
  • Publication number: 20140323427
    Abstract: The present invention relates to the new indications of chronic obstructive pulmonary disease (COPD) and idiophathic lung fibrosis (IPF) for uridine and uridine analogues.
    Type: Application
    Filed: July 24, 2012
    Publication date: October 30, 2014
    Applicant: Universitaetsklinikum Freiburg
    Inventors: Marco Idzko, Stephan Sorichter
  • Publication number: 20140323423
    Abstract: 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: Application
    Filed: May 2, 2014
    Publication date: October 30, 2014
    Applicant: Chrono Therapeutics, Inc.
    Inventors: Guy DiPierro, Steven A. Giannos
  • Publication number: 20140309188
    Abstract: 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: Application
    Filed: April 17, 2014
    Publication date: October 16, 2014
    Inventors: Shizhuang ZHANG, Xin CHENG, Zhiqin GAO, Ming HAN
  • Publication number: 20140301979
    Abstract: Described herein are 4-methyl-piperazine-1-carbothioic acid amide derivatives and analogs, as well as compositions containing the same, for the treatment or prophylaxis of viral infections and diseases associated therewith, particularly those viral infections and associated diseases caused by hemorrhagic fever viruses, such as Arenaviruses.
    Type: Application
    Filed: June 25, 2014
    Publication date: October 9, 2014
    Applicant: SIGA TECHNOLOGIES, INC.,
    Inventors: Sean M. AMBERG, Dongcheng DAI, Tove C. BOLKEN, Dennis E. HRUBY
  • Publication number: 20140303112
    Abstract: The present invention relates to a method for treating disease or condition susceptible to amelioration by AMPK activators and compounds of formula which are useful to activate AMP-activated protein kinase (AMPK) and the use of the compounds in the prevention or treatment of disease, including pre-diabetes, type 2 diabetes, syndrome X, metabolic syndrome and obesity.
    Type: Application
    Filed: April 9, 2013
    Publication date: October 9, 2014
    Inventors: Han-Min CHEN, Cheng-Yi KUO, Chun-Fang HUANG, Jiun-Tsai LIN
  • Publication number: 20140294769
    Abstract: 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: Application
    Filed: April 1, 2014
    Publication date: October 2, 2014
    Inventors: Benjamin Alexander MAYES, Adel M. MOUSSA, Alistair James STEWART
  • Patent number: 8846896
    Abstract: Disclosed herein are methods of preparing a phosphorothioate nucleotide analog, which are useful in treating diseases and/or conditions such as viral infections.
    Type: Grant
    Filed: March 11, 2013
    Date of Patent: September 30, 2014
    Inventors: Vladimir Serebryany, Jyanwei Liu, Leonid Beigelman, Young Chun Jung, Jamison Rose, Shereen Ibrahim, Cavan McKeon, Luigi Anzalone
  • Patent number: 8846639
    Abstract: In certain embodiments, the present invention provides oligomeric compounds having favorable toxicity profiles and therapeutic indexes. Compounds of the present invention comprise bicyclic nucleosides. Certain such bicyclic nucleosides are pyrimidines that do not include a methyl group at the 5-carbon. Oligomeric compounds comprising such nucleosides are less toxic than compounds comprising bicyclic nucleosides that do include a methyl group at the 5-carbon. In certain embodiments, the present invention provides methods of preparing and using such compounds.
    Type: Grant
    Filed: April 3, 2009
    Date of Patent: September 30, 2014
    Assignee: Isis Pharmaceutical, Inc.
    Inventors: Eric E. Swayze, Andrew M. Siwkowski
  • Patent number: 8846636
    Abstract: 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: Grant
    Filed: March 18, 2009
    Date of Patent: September 30, 2014
    Assignee: LCB Pharma Inc.
    Inventor: Yvan Guindon
  • Publication number: 20140287063
    Abstract: Provided are methods of determining a response to a chemotherapeutic agent in a subject with ovarian cancer, comprising: determining a RNA integrity value of a sample comprising ovarian cancer cell RNA from the subject after the subject has received one or more doses of the chemotherapeutic agent; wherein a low RNA integrity value and/or RNA degradation of the cancer cell RNA is indicative that the cancer is responding to the chemotherapeutic agent and/or a high RNA integrity value and/or stable RNA integrity of the ovarian cancer cell RNA is indicative that the cancer is resistant to the chemotherapeutic agent.
    Type: Application
    Filed: August 10, 2011
    Publication date: September 25, 2014
    Applicants: RNA DIAGNOSTICS INC., LAURENTIAN UNIVERSITY OF SUDBURY
    Inventors: Amadeo Mark Parissenti, Baoqing Guo, Kenneth Pritzker, Laura Pritzker
  • Publication number: 20140274939
    Abstract: Kits and methods for treating disordered tissue caused by a virus in a mammal involve co-administration of a systemic anti-virus drug and topically administering an anti-infective composition. The systemic anti-virus drug is internally administered and disrupts or inhibits virus replication systemically within the mammal. Examples include nucleoside analogues, nucleoside analogue precursors, and nucleotide analogues. The topically administered anti-infective composition includes at least one anti-infective agent, such as an organohalide (e.g., benzalkonium chloride), and is formulated to penetrate below the disordered tissue surface and allow the anti-infective agent to kill viruses at the disordered tissue site. The anti-infective composition reduces the time and/or number of dosages required for the systemic anti-virus drug to treat the disordered tissue in the absence of topically administering the anti-infective composition. It also reduces or eliminates incidences of post-treatment neuralgia.
    Type: Application
    Filed: March 14, 2013
    Publication date: September 18, 2014
    Applicant: QUADEX PHARMACEUTICALS, LLC
    Inventor: B. RON JOHNSON
  • Patent number: 8836218
    Abstract: Provided herein are methods of treating a proliferative disease in a subject, comprising administering to the subject a therapeutically effective amount of AC220 and a nucleoside analog, a topoisomerase inhibitor or an anthracycline, or a combination thereof.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: September 16, 2014
    Assignee: Ambit Biosciences Corporation
    Inventors: Robert C. Armstrong, Barbara A. Belli
  • Publication number: 20140255475
    Abstract: Lyophilized liposomal formulations with two or more encapsulated drugs are disclosed. These formulations display superior drug retention profiles and also maintain size distribution following lyophilization and reconstitution.
    Type: Application
    Filed: October 15, 2012
    Publication date: September 11, 2014
    Inventors: Donna Cabral-Lilly, Lawrence Mayer, Paul Tardi, David Watkins, Yi Zeng
  • Publication number: 20140256670
    Abstract: The invention provides Zidovudine conjugated quinoline compound N-((1-(2-(Hydroxy-methyl)-5-(5-methyl-2,4-dioxo-3,4-dihydropyrimidin-1(2H)-yl)-tetrahydrofuran-3-yl)-1H-1,2,3-triazol-4-yl)methyl)-6-(4b,8,8-trimethyl-4b,5,6,7,8,8a-hexahydrodibenzo[a,c]phenazin-2-yloxy)hexanamide. The compound can selectively kills the hepatoma cells especially the hepatoma cells with hepatitis B, and inhibit the growth of subcutaneous tumors in mice, but has no significant toxicity to normal liver cells. Experiments confirm the compound has anti-hepatoma effect, and can be used in preparation of anti-hepatoma drugs.
    Type: Application
    Filed: June 15, 2012
    Publication date: September 11, 2014
    Applicant: Huazhong University of Science and Technology
    Inventor: Qibing Zhou
  • Publication number: 20140248241
    Abstract: Provided herein are compounds, compositions and methods for the treatment of Flaviviridae infections, including HCV infections. In certain embodiments, compounds and compositions of nucleoside derivatives are disclosed, which can be administered either alone or in combination with other anti-viral agents. In certain embodiments, the compounds are 3?-deoxy nucleoside compounds according to Formula 3001a or 3001b: or a pharmaceutically acceptable salts, solvates, stereoisomeric forms, tautomeric forms, or polymorphic forms thereof, wherein PD, Base1 and Base2 are as provided herein.
    Type: Application
    Filed: March 3, 2014
    Publication date: September 4, 2014
    Inventors: Alistair James STEWART, Adel M. MOUSSA, Benjamin Alexander MAYES, Francois-Rene ALEXANDRE, Dominique SURLERAUX, Christophe Claude PARSY, Claire PIERRA, David DUKHAN, Gilles GOSSELIN
  • Patent number: 8815830
    Abstract: 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: Grant
    Filed: March 28, 2014
    Date of Patent: August 26, 2014
    Assignee: Regents of the University of Minnesota
    Inventor: Carston R. Wagner
  • Publication number: 20140234415
    Abstract: The present invention features tablet dosage forms comprising two or more different active ingredients. In one embodiment, a tablet dosage form of the invention comprises a first layer and a second layer, wherein the first layer comprises polymer-based solid dispersion particles having a mean particle size of no more than 200 ?m.
    Type: Application
    Filed: February 19, 2014
    Publication date: August 21, 2014
    Inventors: Todd S. McDermott, Peter T. Mayer, Benjamin M. Collman, Weili Wang, Bei Chen
  • Publication number: 20140235563
    Abstract: 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: Application
    Filed: April 30, 2014
    Publication date: August 21, 2014
    Applicants: Gilead Sciences, Inc., Gilead Pharmasset LLC
    Inventors: Michael Joseph Sofia, Jinfa Du
  • Publication number: 20140228313
    Abstract: Contemplated compositions and methods are directed to prevent and/or treat various autoimmune diseases that are typically associated with glycan dysregulation, and especially autoimmune demyelinating diseases. Further especially contemplated aspects include animal models and systems for screening compounds to treat and/or prevent such diseases.
    Type: Application
    Filed: January 17, 2014
    Publication date: August 14, 2014
    Applicants: The Regents of the University of California, Mount Sinai Hospital
    Inventors: Michael Demetriou, James Dennis, Ken Siu-Kwong Lau
  • Publication number: 20140221304
    Abstract: The present invention relates to 5?-Substituted Nucleoside Analogs of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, Z, R1, R2, R3 and R3? are as defined herein. The present invention also relates to compositions comprising at least one 5?-Substituted Nucleoside Analog, and methods of using the 5?-Substituted Nucleoside Analogs for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: July 10, 2012
    Publication date: August 7, 2014
    Inventors: Vishal A. Verma, Ashok Arasappan, F. George Njoroge, Kevin X. Chen
  • Publication number: 20140219957
    Abstract: The invention features methods of treating an immune disorder characterized by elevated Pin1 marker levels in a subject by administering a retinoic acid compound. Additionally, the invention features methods of treating immune disorders (e.g., immune disorders characterized by elevated Pin1 marker levels) by administering a retinoic acid compound in combination with an anti-inflammatory, anti-viral, or anti-microbial compound.
    Type: Application
    Filed: May 29, 2012
    Publication date: August 7, 2014
    Applicant: Beth Israel Deaconess Medical Center, Inc.
    Inventors: Kun Ping Lu, Adrian Tun-Kyi, Greg Finn
  • Publication number: 20140213540
    Abstract: 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: Application
    Filed: March 20, 2014
    Publication date: July 31, 2014
    Applicants: IDENIX PHARMACEUTICALS, INC., L'UNIVERSITE MONTPELLIER II, CENTRE NATIONAL DE LA RECHERCHE SCIENTIFIQUE, UNIVERSITA DEGLI STUDI DI CAGLIARI
    Inventors: Richard STORER, Gilles GOSSELIN, Jean-Pierre SOMMADOSSI, Paolo LACOLLA
  • Patent number: 8791089
    Abstract: The invention provides a method for supporting operational activities in daily living by providing a combination of (a) long-chain polyunsaturated fatty acids, particularly DHA and/or EPA, and (b) nucleosides or nucleotides, particularly uridine or its equivalent. The operational activities comprise eating; walking; toileting; bathing; grooming; dressing; use of communication equipment; making conversations; keeping appointments; use of household appliances; cleaning dishes; preparation of meal or drink; writing; reading; independent housekeeping; transportation and shopping.
    Type: Grant
    Filed: January 18, 2013
    Date of Patent: July 29, 2014
    Assignee: N.V. Nutricia
    Inventors: Martine Groenendijk, Mattheus Cornelis de Wilde, Robert Johan Joseph Hageman, Patrick Joseph Gerardus Hendrikus Kamphuis
  • Publication number: 20140206639
    Abstract: The present invention provides pharmaceutical compositions comprising a dihydro base described herein (e.g., compound DHdC). The dihydro base may show multiple tautomerism and may increase mutation of an RNA and/or DNA of a virus or cancer cell. The dihydro base may be used to reduce DNA methylation (e.g., in a cancer cell). The present invention also provides kits including the inventive pharmaceutical compositions and methods of treating a viral infection (e.g., influenza, HIV infection, or hepatitis C) or cancer using the pharmaceutical compositions or kits.
    Type: Application
    Filed: January 22, 2014
    Publication date: July 24, 2014
    Applicant: Massachusetts Institute of Technology
    Inventors: John M. Essigmann, Deyu Li, Katherine J. Silvestre
  • Publication number: 20140206640
    Abstract: The present invention relates to 2?-Azido Substituted Nucleoside Derivatives of Formula (I): and pharmaceutically acceptable salts thereof, wherein B, X, R1, R2 and R3 are as defined herein. The present invention also relates to compositions comprising at least one 2?-Azido Substituted Nucleoside Derivative, and methods of using the 2?-Azido Substituted Nucleoside Derivatives for treating or preventing HCV infection in a patient.
    Type: Application
    Filed: April 11, 2012
    Publication date: July 24, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: Vinay Girijavallabhan, F. George Njoroge, Stephane Bogen, Frank Bennett, Vishal Verma, Ashok Arasappan, Kevin X. Chen, Ying Huang, Angela Kerekes, Latha Nair, Dimitri Pissarnitski, Qun Dang, Ian Davies, David B. Olsen, Andrew Stamford, Joseph P. Vacca
  • Publication number: 20140206635
    Abstract: A metal-salen complex compound, which exhibits excellent noninvasiveness and can be efficiently transferred to an affected site, a local anesthetic containing this metal-salen complex compound, and an antineoplastic drug containing this metal-salen complex compound are provided. Regarding the metal-salen complex compound, a metal atom part in each of two molecules of a metal-salen complex or a derivative of the metal-salen complex is dimerized via water, and the metal-salen complex compound is mixed with a base to produce an ointment.
    Type: Application
    Filed: May 10, 2012
    Publication date: July 24, 2014
    Applicants: IHI CORPORATION
    Inventors: Yoshihiro Ishikawa, Haruki Eguchi
  • Publication number: 20140205567
    Abstract: The present invention discloses a class of novel macro-heterocyclic compounds represented by the formula Ia or Ib, and their intermediates, preparation methods and the uses. The macro-heterocyclic compounds of the present invention have good inhibitory activities against hepatitis C virus (HCV), and can be used to treat HCV infection effectively by its excellent inhibition against HCV, low toxicity and side effects.
    Type: Application
    Filed: June 14, 2012
    Publication date: July 24, 2014
    Applicant: AB Pharma Ltd.
    Inventor: Zheng-yun James Zhan
  • Publication number: 20140200516
    Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II; aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.
    Type: Application
    Filed: March 18, 2014
    Publication date: July 17, 2014
    Applicant: ABBOTT LABORATORIES
    Inventor: Harry A. DUGGER, III
  • Publication number: 20140199265
    Abstract: The present disclosure relates to nutritional compositions comprising a neurologic component, wherein, the neurologic component may promote brain and nervous system development and further provide neurological protection and repair. The neurologic component may include phosphatidylethanolamine, sphingomyelin, cytidine diphosphate-choline, ceramide, uridine, at least one ganglioside, and mixtures thereof. The disclosure further relates to methods of promoting brain and nervous system health by providing said nutritional compositions to target subjects, which includes pediatric subjects.
    Type: Application
    Filed: January 11, 2013
    Publication date: July 17, 2014
    Applicant: Mead Johnson Nutrition Company
    Inventors: Chenzhong Kuang, Yan Xiao, Eduard Poels, Zeina Jouni, Dirk Hondmann
  • Publication number: 20140187510
    Abstract: The present invention is directed toward a method of treating a subject for a condition mediated by aberrant Wnt/?-catenin signaling by selecting a subject with a condition mediated by aberrant Wnt/?-catenin signaling and administering to the selected subject a compound selected from the group consisting of those set forth in Table 1, Table 2, and a pharmaceutically acceptable salt thereof. A method of similarly modulating the Wnt/?-catenin pathway in a subject is also discussed.
    Type: Application
    Filed: July 11, 2013
    Publication date: July 3, 2014
    Applicants: THE GENERAL HOSPITAL CORPORATION, MASSACHUSETTS INSTITUTE OF TECHNOLOGY, UNIVERSITY OF WASHINGTON THROUGH ITS CENTER FOR CENTER FOR COMMERCIALIZATION
    Inventors: Randall T. Moon, Travis L. Biechele, Nathan D. Camp, Stephen Haggarty, Daniel Fass
  • Patent number: 8765713
    Abstract: A marker for determining sensitivity of a patient to an anti-cancer agent, and novel cancer therapeutic means employing the marker, wherein the marker for determining sensitivity to an anti-cancer agent is a protein or a fragment, where in the protein or a fragment thereof exhibits a peak at m/z of 5,300 to 5,400, a peak at m/z of 6,130 to 6,230, a peak at m/z of 7,000 to 7,080 a peak at m/z of 7,840 to 7,920, a peak at m/z of 8,920 to 9,000, a peak at m/z of 12,440 to 12,560, a peak at m/z of 17,100 to 17,270, a peak at m/z of 18,290 to 18,470, a peak at m/z of 24,660 to 24,750, a peak at m/z of 35,980 to 36,290, a peak at m/z of 8,650 to 8,750, a peak at m/z of 9,100 to 9,200, a peak at m/z of 11,760 to 11,890, the peaks being determined by means of a mass spectrometer.
    Type: Grant
    Filed: October 29, 2010
    Date of Patent: July 1, 2014
    Assignees: Keio University, Kabushiki Kaisha Yakult Honsha
    Inventors: Yusuke Tanigawara, Sayo Suzuki, Yusuke Ikoma, Akito Nishimuta, Tetsuya Suzuki, Shinji Sugimoto
  • Patent number: 8765712
    Abstract: The present invention concerns an agent for prevention and treatment of pityriasis. The agent according to the present invention comprises at least one transaminase inhibitor effectively inhibiting the transamination process which is of pathogenetic relevance for the disease, prevents a recurrence of the disease and which protects the human skin flora. Upon release into the environment, no resistances are induced in other fungi.
    Type: Grant
    Filed: January 14, 2010
    Date of Patent: July 1, 2014
    Assignee: Justus-Liebig-Universitaet Giessen
    Inventor: Peter Mayser
  • Publication number: 20140179627
    Abstract: Disclosed herein are nucleotide analogs, methods of synthesizing nucleotide analogs and methods of treating diseases and/or conditions such as a HCV infection with one or more nucleotide analogs.
    Type: Application
    Filed: December 19, 2013
    Publication date: June 26, 2014
    Applicant: ALIOS BIOPHARMA, INC.
    Inventors: Leonid Beigelman, Guangyi Wang, David Bernard Smith