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.
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.
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.
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.
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.
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.
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
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.
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
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.
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.
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
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
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
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
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.
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.
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.
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.
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.
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.
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
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.
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
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.
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.
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
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.
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.
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.
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.
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
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.
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
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.
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.
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
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
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.
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
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.
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
Abstract: Provided herein are compounds used to inhibit the deamination enzyme responsible for the inactivation of therapeutic compounds, and methods of using them.
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
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.
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
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.
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