Nitrogen Containing Hetero Ring Patents (Class 514/43)
  • Publication number: 20130190263
    Abstract: The invention relates to a novel oral veterinary composition for salmonids, comprising 1-beta-D-ribofuranosyl-1H-1,2,4-triazole-3-carboxamide and to the use thereof for the treatment of infectious salmon anaemia (USA) caused by the infectious salmon anaemia or ISA virus in salmonids.
    Type: Application
    Filed: June 8, 2010
    Publication date: July 25, 2013
    Applicant: LABORATORIO DE DIAGNOSTICO GAM, S.A.
    Inventors: Ana Sandino, Geraldine Mlynarz Zylberberg, Matilde Jashes Morgues, Eugenio Spencer Ossa
  • Publication number: 20130189333
    Abstract: An oral product includes a body that is wholly receivable in an oral cavity. The body includes a mouth-stable polymer matrix, cellulosic fibers embedded in the mouth-stable polymer matrix, and an additive dispersed in the mouth-stable polymer matrix. The oral product is adapted to release the additive from the body when the body is received within the oral cavity and exposed to saliva.
    Type: Application
    Filed: January 18, 2013
    Publication date: July 25, 2013
    Applicant: ALTRIA CLIENT SERVICES INC.
    Inventor: Altria Client Services Inc.
  • Patent number: 8492362
    Abstract: The present invention relates to prodrug forms of ?-L-1-[5-(E-2-Bromovinyl)-2-(hydroxymethyl)-1,3-dioxolan-4-yl)]uracil (L-BHDU) and their use to treat viral infections of Varicella Zoster Virus, including recurrent VZV (shingles), especially including drug resistant Varicella Zoster Virus and related complications of this viral infection such as rash or post-herpetic neuralgia.
    Type: Grant
    Filed: November 8, 2011
    Date of Patent: July 23, 2013
    Assignee: University of Georgia Research Foundation, Inc.
    Inventor: Chung K. Chu
  • Patent number: 8492361
    Abstract: The present disclosure provides methods for treating subjects having non-small cell lung cancer, wherein the methods comprise administering to the subject a cytidine analog, such as 5-azacytidine. Also provided are methods relating to identification and treatment of particular non-small cell lung cancer types sensitive to particular cytidine analogs.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: July 23, 2013
    Assignee: Celgene Corporation
    Inventors: Aaron N. Nguyen, Kyle J. MacBeth
  • Publication number: 20130183266
    Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof, wherein the variables of Structural Formula (I) are as described in the specification and the claims. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutically acceptable carrier of excipient. A biological probe comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a HCV infection in a subject comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: December 21, 2012
    Publication date: July 18, 2013
    Applicant: Vertex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated
  • Publication number: 20130183269
    Abstract: The present disclosure is generally directed to antiviral compounds, and more specifically directed to combinations of compounds which can inhibit the function of the NS5A protein encoded by Hepatitis C virus (HCV), compositions comprising such combinations, and methods for inhibiting the function of the NS5A protein.
    Type: Application
    Filed: January 7, 2013
    Publication date: July 18, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Patent number: 8486957
    Abstract: A method of treating cancer in a subject in need thereof comprises administering said subject reserpine, yohimbine, an analog thereof, or a pharmaceutically acceptable salt or prodrug thereof, in an amount effective to treat the cancer. Compounds and compositions useful for carrying out the method are also described.
    Type: Grant
    Filed: February 24, 2010
    Date of Patent: July 16, 2013
    Assignee: Wake Forest University Health Sciences
    Inventors: Freddie R. Salsbury, Jr., Karin D. Scarpinato, S. Bruce King
  • Publication number: 20130178428
    Abstract: Long noncoding RNAs (lncRNAs) that may be used as cancer biomarkers and methods of diagnosing, prognosing and monitoring cancer including, but not limited to, cutaneous melanoma using said lncRNAs are provided herein. In some embodiments, the methods include steps of isolating one or more lncRNA transcripts in a biological sample from the subject; measuring a test level of the one or more isolated lncRNA transcripts; comparing the test level to a control level of the one or more lncRNA transcripts; and diagnosing or making a prognosis based on the lncRNA level. In some embodiments, the lncRNA transcript is an linc00340 transcript or variant thereof. These lncRNA transcripts may also be used as a therapeutic target in the treatment of cancer.
    Type: Application
    Filed: November 30, 2012
    Publication date: July 11, 2013
    Inventors: Dave S.B. Hoon, Laurent Lessard
  • Publication number: 20130177529
    Abstract: Aryl substituted pyrazole derivatives are provided, as well as processes for their preparation. The invention also provides compositions and methods for the treatment of HCV by administering a compound of the present invention, alone or in combination with additional antiviral agents, in a therapeutically effective amount.
    Type: Application
    Filed: November 15, 2012
    Publication date: July 11, 2013
    Inventors: Youhong Hu, Bin Xu, Yun Liao, Kenneth Nawoschik, Yixin Liu, Anthony Sandrasagra, Reza Fathi, Zhen Yang
  • Publication number: 20130178439
    Abstract: The invention relates to pharmaceutical compositions and methods of treating inflammatory-related diseases associated with pro-inflammatory cytokine expression and/or reduced expression of anti-inflammatory cytokines. The method typically comprises administration of one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, such as, Meisoindigo and NATURA. Preferably the pharmaceutical composition comprises one or more compounds selected from isoindigo, indigo, indirubin, or derivatives thereof, an anti-inflammatory agent, and a pharmaceutically acceptable carrier.
    Type: Application
    Filed: March 8, 2013
    Publication date: July 11, 2013
    Applicant: NATROGEN THERAPEUTICS INTERNATIONAL INC.
    Inventor: NATROGEN THERAPEUTICS INTERNATIONAL INC.
  • Publication number: 20130177530
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: March 1, 2013
    Publication date: July 11, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Patent number: 8481503
    Abstract: The invention relates to combination anticancer therapy with certain Akt inhibitor and other anticancer agents such as anticancer antimetabolites, anticancer antibiotics, plant-derived anticancer agents, anticancer platinum-coordinated complex compounds, anticancer camptothecin derivatives and anticancer tyrosine kinase inhibitors.
    Type: Grant
    Filed: February 23, 2010
    Date of Patent: July 9, 2013
    Assignees: Merck Sharp & Dohme Corp., MSD K.K.
    Inventors: Mark E. Layton, Hiroshi Hirai, Hidehito Kotani
  • Publication number: 20130172284
    Abstract: 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: Application
    Filed: June 8, 2010
    Publication date: July 4, 2013
    Applicant: LABORATORIO DE DIAGNOSTICO GAM, S.A.
    Inventors: Ana Maria Sandino, Geraldine Mlynarz Zylberberg, Matilde Jashes Morgues, Eugenio Spencer Ossa
  • Publication number: 20130171101
    Abstract: Surprising antiviral activity of 3-amino-2-(4-nitrophenyl)-4-(3H)-quinazolinone (Compound 1) was reported in the treatment or prevention of viral infections, particularly in combination with other antiviral agents such as interferon and/or ribavarin.
    Type: Application
    Filed: December 31, 2011
    Publication date: July 4, 2013
    Inventors: Sheikh Riazuddin, Osman Ali, Usman Ashfaq, Shaheen N. Khan, Javed Akram, Atta-ur Rahman, M. Iqbal Choudhary, Khalid M. Khan, Zulfiqa Ali Khan
  • Publication number: 20130171103
    Abstract: Compounds that selectively inhibit viral replication or the production of viral RNA or DNA, viral protein or virus induced cytopathic effects and compositions comprising such Compounds are described. Also described are methods of inhibiting viral replication or the production of viral RNA or DNA, viral protein or virus induced cytopathic effects using such Compounds and methods for treating viral infections involving the administration of such Compounds. The Compounds may be administered as a single agent therapy or in combination with one or more additional therapies to a human in need of such treatments.
    Type: Application
    Filed: May 26, 2011
    Publication date: July 4, 2013
    Applicant: PTC Therapeutics, Inc.
    Inventors: Thomas Davis, Jason D. Graci, Zhengxian Gu, Christopher Trotta
  • Patent number: 8476241
    Abstract: The inventors have determined, contrary to the prior art and experience, how to successfully use triciribine to treat esophogeal adenocarcinoma by one or a combination of (i) administering triciribine only to patients which according to a diagnostic test described below, exhibit enhanced sensitivity to the drug; (ii) use of a described dosage level that minimizes the toxicity of the drug but yet still exhibits efficacy; or (iii) use of a described dosage regimen that minimizes the toxicity of the drug.
    Type: Grant
    Filed: June 17, 2011
    Date of Patent: July 2, 2013
    Assignee: University of South Florida
    Inventor: Jin Q. Cheng
  • Patent number: 8476254
    Abstract: The present invention relates to the treatment of psychosis associated with interferon-? therapy by administering an amount of a glucocorticoid receptor antagonist effective to ameliorate the symptoms of psychosis in the patient, wherein the patient is not otherwise in need of treatment with a glucocorticoid receptor antagonist. The present invention further relates to kits for the treatment of Hepatitis C infection in a patient.
    Type: Grant
    Filed: July 2, 2003
    Date of Patent: July 2, 2013
    Assignee: Corcept Therapeutics, Inc.
    Inventor: Joseph K. Belanoff
  • Publication number: 20130165400
    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.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: ALIOS BIOPHARMA, INC.
    Inventor: Alios BioPharma, Inc.
  • Publication number: 20130164280
    Abstract: The invention provides compounds and pharmaceutically acceptable salts and esters and compositions thereof, for treating viral infections. The compounds and compositions are useful for treating Pneumovirinae virus infection including Human respiratory syncytial virus infections.
    Type: Application
    Filed: December 20, 2012
    Publication date: June 27, 2013
    Applicant: GILEAD SCIENCES, INC.
    Inventor: Gilead Sciences, Inc.
  • Publication number: 20130165398
    Abstract: A concentration-enhancing drink contains, in each case independently of one another, per liter: 1 mg to 10 g, preferably 1 to 1000 mg, still more preferably 10 to 500 mg, in particular 50 to 300 mg, of epigallocatechin gallate; 1 to 500 mg, preferably 10 to 100 mg, in particular 20 to 80 mg, of nicotinamide ribose; and/or 0.05 to 10 g, preferably 0.1 to 5 g, in particular 0.5 to 3 g of tryptophan.
    Type: Application
    Filed: March 29, 2011
    Publication date: June 27, 2013
    Inventor: Johannes Huber
  • Publication number: 20130164260
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: November 16, 2012
    Publication date: June 27, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Patent number: 8470826
    Abstract: The present invention relates to an episomal structure expressing a functional oncogene, whereby said oncogene is a fusion gene of two chromosomal gene fragments. More specifically, the invention relates to a NUP214-ABL1 fusion product, important in the development of T-cell acute lymphoblastic leukemia, to methods to detect the fusion and to methods to prevent the oncogenic activity of said fusion product.
    Type: Grant
    Filed: June 15, 2010
    Date of Patent: June 25, 2013
    Assignees: VIB VZW, K.U. Leuven Research and Development
    Inventors: Jan Cools, Anne Hagemeijer, Peter Marynen
  • Publication number: 20130156727
    Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which inhibit the activity of histone deacetylase 8 (HDAC8). Also described herein are methods of using such HDAC8 inhibitors, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of HDAC8 activity.
    Type: Application
    Filed: November 21, 2012
    Publication date: June 20, 2013
    Applicant: Pharmacyclics, Inc.
    Inventor: Pharmacyclics, Inc.
  • Publication number: 20130157971
    Abstract: 2?-Fluoro-nucleoside compounds are disclosed which are useful in the treatment of hepatitis B infection, hepatitis C infection, HIV and abnormal cellular proliferation, including tumors and cancer. The compounds have the general formulae: wherein Base is a purine or pyrimidine base; R1 is OH, H, OR3, N3, CN, halogen, CF3, lower alkyl, amino, loweralkylamino, di(lower)alkylamino, or alkoxy; R2 is H, phosphate, or a stabilized phosphate prodrug; acyl, or other pharmaceutically acceptable leaving benzyl, a lipid, an amino acid, peptide, or cholesterol; and R3 is acyl, alkyl, phosphate, or other pharmaceutically acceptable leaving group; or a pharmaceutically acceptable salt thereof.
    Type: Application
    Filed: April 2, 2012
    Publication date: June 20, 2013
    Inventors: RAYMOND F. SCHINAZI, Dennis C. Liotta, Chung K. Chu, J. Jeffrey McAtee
  • Publication number: 20130156732
    Abstract: The disclosure is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: November 16, 2012
    Publication date: June 20, 2013
    Applicant: Gilead Sciences, Inc.
    Inventor: Gilead Sciences, Inc.
  • Publication number: 20130157970
    Abstract: Compounds of formula (I): wherein X, Y, and Z are defined herein. Also disclosed are pharmaceutical compositions and therapeutical methods related to these compounds.
    Type: Application
    Filed: December 13, 2012
    Publication date: June 20, 2013
    Applicant: National Health Research Institutes
    Inventor: National Health Research Institutes
  • Patent number: 8466276
    Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water-soluble oligomer.
    Type: Grant
    Filed: February 20, 2009
    Date of Patent: June 18, 2013
    Assignee: Nektar Therapeutics
    Inventors: Bo-Liang Deng, Timothy A. Riley, Jennifer Riggs-Sauthier
  • Patent number: 8461128
    Abstract: 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: Grant
    Filed: April 14, 2006
    Date of Patent: June 11, 2013
    Assignees: 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
  • Patent number: 8461123
    Abstract: Oligonucleotide analogues are provided that incorporate 5-aza-cytosine in the oligonucleotide sequence, e.g., in the form of 5-aza-2?-deoxycytidine (decitabine) or 5-aza-cytidine. In particular, oligonucleotide analogues rich in decitabine-deoxyguanosine islets (DpG and GpD) are provided to target the CpG islets in the human genome, especially in the promoter regions of genes susceptible to aberrant hypermethylation. Such analogues can be used for modulation of DNA methylation, such as effective inhibition of methylation of cytosine at the C-5 position. Methods for synthesizing these oligonucleotide analogues and for modulating nucleic acid methylation are provided. Also provided are phosphoramidite building blocks for synthesizing the oligonucleotide analogues, methods for synthesizing, formulating and administering these compounds or compositions to treat conditions, such as cancer and hematological disorders.
    Type: Grant
    Filed: February 9, 2010
    Date of Patent: June 11, 2013
    Assignee: Astex Pharmaceuticals, Inc.
    Inventors: Pasit Phiasivongsa, Sanjeev Redkar
  • Publication number: 20130143833
    Abstract: The present invention relates to a method of reducing injury to cells, a tissue or organ to be explanted from a body and upon implantation into a body by administering a composition to the cell, tissue or organ, including: (i) a potassium channel opener or agonist and/or an adenosine receptor agonist; and (ii) an antiarrhythmic agent. The invention also provides a composition for reducing injury to vasculature ex vivo including: (i) a potassium channel opener or agonist and/or an adenosine receptor agonist; and (ii) an antiarrhythmic agent.
    Type: Application
    Filed: November 13, 2012
    Publication date: June 6, 2013
    Applicant: Hibernation Therapeutics Limited
    Inventor: Hibernation Therapeutics Limited
  • Publication number: 20130143827
    Abstract: A method of generating synthetic metabolites of tanaproget derivatives thereof is provided. These compounds and methods of using these derivatives for detecting tanaproget metabolites in samples are provided.
    Type: Application
    Filed: January 28, 2013
    Publication date: June 6, 2013
    Applicant: Wyeth LLC
    Inventor: Wyeth LLC
  • Publication number: 20130136804
    Abstract: N-(4-{4-amino-7-[1-(2-hydroxyethyl)-1H-pyrazol-4-yl]thieno[3,2-c]pyridin-3-yl}phenyl)-N?-(3-fluorophenyl)urea free base and crystallines form thereof are suitable pharmaceutical ingredients for pharmaceutical compositions useful in the treatment of disease, for example, cancer.
    Type: Application
    Filed: December 17, 2012
    Publication date: May 30, 2013
    Applicant: AbbVie Inc.
    Inventor: AbbVie Inc.
  • Patent number: 8450293
    Abstract: The invention provides analogs cyclic diguanosine monophosphate (c-di-GMP) having different substituents at the guanine C8 position.
    Type: Grant
    Filed: August 10, 2011
    Date of Patent: May 28, 2013
    Assignee: Rutgers, The State University of New Jersey
    Inventors: Roger A. Jones, Elizabeth Veliath
  • Patent number: 8450467
    Abstract: The present invention provides iRNA agents comprising at least one subunit of the formula (I): wherein: A and B are each independently for each occurrence O, N(RN) or S; X and Y are each independently for each occurrence H, OH, a hydroxyl protecting group, a phosphate group, a phosphodiester group, an activated phosphate group, an activated phosphite group, a phosphoramidite, a solid support, —P(Z?)(Z?)O-nucleoside, —P(Z?)(Z?)O-oligonucleotide, a lipid, a PEG, a steroid, a lipophile, a polymer, —P(Z?)(Z?)O-Linker-OP(Z??)(Z??)O-oligonucleotide, a nucleotide, an oligonucleotide, —P(Z?)(Z?)-formula (I), —P(Z?)(Z?)— or -Linker-R; R is LG, -Linker-LG, or has the structure shown below: LG is independently for each occurrence a carbohydrate, e.g.
    Type: Grant
    Filed: December 14, 2011
    Date of Patent: May 28, 2013
    Assignee: Alnylam Pharmaceuticals, Inc.
    Inventors: Muthiah Manoharan, Kallanthottathil G. Rajeev, Narayanannair K. Jayaprakash, Martin Maier
  • Publication number: 20130129680
    Abstract: A method for treating hepatitis C virus infection with a composition containing quercetin, together with one or more of vitamin B3, vitamin C, a folate compound. Also disclosed is a method for treating conditions associated with an elevated level of heat shock proteins, including liver cancer, using the above-mentioned composition.
    Type: Application
    Filed: November 23, 2011
    Publication date: May 23, 2013
    Inventor: Thomas Christian Lines
  • Patent number: 8445458
    Abstract: A composition comprising (a) one or more ?-3 fatty acids selected from DHA, DPA and EPA, (b) uridine or its equivalent, and (c) a methyl donor, useful in the treatment of a person having characteristics of a prodromal dementia patient. The characteristics include e.g. a level of more than 350 ng Total-tau per liter cerebrospinal fluid (CSF), and a weight ratio of abeta-42/Phospho-tau-181 of less than 6.5 in CSF.
    Type: Grant
    Filed: June 20, 2008
    Date of Patent: May 21, 2013
    Assignee: N. V. Nutricia
    Inventors: Robert Johan Joseph Hageman, Patrick Joseph Gerardus Hendrikus Kamphuis, Ladislaus Maria Broersen
  • Patent number: 8445457
    Abstract: A pharmaceutical solution suitable for oral administration comprising ?-L-thymidine/2?-deoxy-L-thymidine (telbivudine), a pharmaceutically suitable solvent system, one or more taste-enhancing/masking agents, a preservative system, and a buffer system suitable to allow both drug stability and preservation.
    Type: Grant
    Filed: July 10, 2008
    Date of Patent: May 21, 2013
    Assignee: Novartis AG
    Inventor: Nabila Sekkat
  • Publication number: 20130121965
    Abstract: Methods of treating a hepatitis C virus (HCV) related disease, such as HCV infections in subjects non-responsive to anti-HCV therapy, are described herein, comprising administering to the subject a therapeutically effective amount of hydroxychloroquine. An antiviral agent may be co-administered with the hydroxychloroquine. Methods utilizing synergistic combinations of hydroxychloroquine and an antiviral agent are disclosed. Further disclosed are compositions comprising hydroxychloroquine and an antiviral agent, as well as hydroxychloroquine and uses thereof for the treatment of a hepatitis C virus (HCV) related disease.
    Type: Application
    Filed: December 26, 2012
    Publication date: May 16, 2013
    Applicants: Genoscience Pharma SAS, Panmed Ltd.
    Inventors: Panmed Ltd., Genoscience Pharma SAS
  • Publication number: 20130121986
    Abstract: The present invention concerns nitrogenated derivatives of narciclasine and pancratistatin of the following general formula (I) as well as their pharmaceutically acceptable salts. The present invention also concerns the use of these compounds in cancer therapy as well as a method for their preparation.
    Type: Application
    Filed: December 26, 2012
    Publication date: May 16, 2013
    Inventors: Frederic MARION, Jean-Philippe ANNEREAU, Jacques FAHY
  • Publication number: 20130121957
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: May 7, 2012
    Publication date: May 16, 2013
    Inventors: Qi Chen, Omar D. Lopez, John A. Bender, Gan Wang, Van N. Nguyen, John F. Kadow, Nicholas A. Meanwell, Makonen Belema
  • Publication number: 20130123345
    Abstract: Described herein is a method of treating a viral infection such as an influenza infection, in a subject comprising administering an effective amount of a pharmaceutical composition to disrupt a adenosine receptor pathway, such as the Aradenosine receptor pathway, in a subject. The adenosine receptor pathway includes the steps of 1) producing the adenosine precursor adenosine triphosphate (ATP), 2) releasing ATP into the extracel lular space, 3) enzymatic conversion of ATP to adenosine, 4) activation of the adenosine receptor and the adenosine receptor cascade, and 5) clearance of adenosine from the extracellular space by degradation or uptake into a cell. The method includes affecting at least one of these steps so as to decrease the activation of the adenosine receptor pathway. This may be accomplished by decreasing the production, release, or conversion of ATP to adenosine, decreasing the expression of the adenosine receptor, antagonizing adenosine receptor activation, and/or increasing adenosine clearance.
    Type: Application
    Filed: July 22, 2011
    Publication date: May 16, 2013
    Applicant: THE OHIO STATE UNIVERSITY
    Inventor: Ian C. Davis
  • Publication number: 20130123328
    Abstract: We describe a method of determining whether a cancer cell is likely to be resistant to treatment by an mTOR inhibitor. The method may comprise detecting PPP2R2B (GenBank Accession Number: NM_18167) in or of the cell. It may, alter-natively, or in addition, comprise detecting PDK1 (GenBank Accession Number: NM_002613), in or of the cell. The method may comprise detecting methylation of the PPP2R2B promoter in or of the cell. It may comprise detecting the expression and/or activity of PPP2R2B in or of the cell. It may comprise detecting PDK1 mediated Myc phosphorylation activity.
    Type: Application
    Filed: January 10, 2011
    Publication date: May 16, 2013
    Applicant: AGENCY FOR SCIENCE, TECHNOLOGY AND RESEARCH
    Inventors: Qiang Yu, Jing Tan
  • Publication number: 20130123207
    Abstract: A resveratrol-containing composition capable of providing a therapeutic benefit to a subject such as modulation of a biological activity, improving cell transplantation therapy, or improving macular degeneration or dystrophy treatments. The compositions comprise trans-resveratrol, a metal chelator, one or more additional antioxidants such as quercetin, gamma-tocotrienol, or apple polyphenols, allicin, and nucleotides.
    Type: Application
    Filed: November 16, 2012
    Publication date: May 16, 2013
    Applicant: RESVERATROL PARTNERS, LLC
    Inventor: Resveratrol Partners, LLC
  • Patent number: 8440640
    Abstract: The invention provides methods for, and compositions effective for, treating obesity, inhibiting weight gain, treating diabetes mellitus, inhibiting atherosclerosis and treating related disorders and conditions comprising administering a pharmaceutically effective amount of at least one compound capable of inhibiting AC5 to a patient. The compound capable of inhibiting AC5 may be administered singly or in combination with another agent. In some embodiments, the AC5 inhibiting compound is 9-?-D-arabinofuranosyladenine (AraAde). The compounds may be administered in an amount of about 1 to about 200 mg/kg/day, about 1 to about 100 mg/kg/day, about 10 to about 80 mg/kg/day, about 12 to about 40 mg/kg/day or about 15 to about 25 mg/kg/day. In some embodiments, the compound is administered orally.
    Type: Grant
    Filed: November 18, 2009
    Date of Patent: May 14, 2013
    Assignee: University of Medicine and Dentistry of New Jersey
    Inventor: Stephen F. Vatner
  • Publication number: 20130116207
    Abstract: Provided herein are compounds used to inhibit the deamination enzyme responsible for the inactivation of therapeutic compounds, and methods of using them.
    Type: Application
    Filed: October 31, 2012
    Publication date: May 9, 2013
    Applicant: Eisai Inc.
    Inventor: Eisai Inc.
  • Publication number: 20130116206
    Abstract: There is provided compounds of formula (I), wherein R1, R2, X1, X2, and X3 have meanings given in the description, and pharmaceutically-acceptable salts thereof, which compounds are useful as positron emission tomography (PET) imaging agents, useful in the treatment of diseases in which inhibition of epidermal growth factor receptor tyrosine kinase activity or the inhibition of HER2 activity is desired and/or required, and useful in the treatment of cancer.
    Type: Application
    Filed: December 22, 2010
    Publication date: May 9, 2013
    Applicant: IMPERIAL INNOVATIONS LIMITED
    Inventors: Federica Pisaneschi, Alan Spivey, Graham Smith, Eric Aboagye
  • Publication number: 20130116208
    Abstract: 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: Application
    Filed: November 2, 2012
    Publication date: May 9, 2013
    Applicant: MILLENNIUM PHARMACEUTICALS, INC.
    Inventor: Millennium Pharmaceuticals, Inc.
  • Publication number: 20130116204
    Abstract: Provided are (methylsulfonyl)ethyl benzene isoindoline compounds, and pharmaceutically acceptable salts, solvates, or stereoisomers thereof. Methods of use and pharmaceutical compositions of these compounds are also disclosed.
    Type: Application
    Filed: December 21, 2010
    Publication date: May 9, 2013
    Applicant: Celgene Corporation
    Inventors: Peter H. Schafer, Anthony J. Frank, Hon-Wah Man, Sai L. Shankar
  • Publication number: 20130115193
    Abstract: The present disclosure relates to compounds, compositions and methods for the treatment of Hepatitis C virus (HCV) infection. Also disclosed are pharmaceutical compositions containing such compounds and methods for using these compounds in the treatment of HCV infection.
    Type: Application
    Filed: November 8, 2012
    Publication date: May 9, 2013
    Applicant: Bristol-Myers Squibb Company
    Inventor: Bristol-Myers Squibb Company
  • Publication number: 20130115194
    Abstract: The invention provides compounds of formula (I): wherein the variables are defined in the specification, or a pharmaceutically-acceptable salt thereof, that are inhibitors of replication of the hepatitis C virus. The invention also provides pharmaceutical compositions comprising such compounds, methods of using such compounds to treat hepatitis C viral infections, and processes and intermediates useful for preparing such compounds.
    Type: Application
    Filed: November 2, 2012
    Publication date: May 9, 2013
    Inventors: Daniel D. LONG, Robert Murray MCKINNELL, Lan JIANG, Mandy LOO, Kassandra LEPACK, Lori Jean VAN ORDEN, Gavin OGAWA, Xiaojun HUANG, Weijiang ZHANG