Abstract: The invention relates to a process for deblocking substantially a blocked, detectably labeled oligonucleotide by contacting the blocked detectably labeled oligonucleotide with an effective amount of a nucleophilic amino compound under conditions that result in substantial deblocking of the oligonucleotide, thereby giving the substantially deblocked oligonucleotide.
Abstract: This invention provides novel compounds selected from the group consisting of a 1,5-substituted pyrimidine derivative or analog and substituted furano-pyrimidone analogs. The compounds are useful to treat or prevent diseases such as cancer.
Type:
Grant
Filed:
October 7, 2003
Date of Patent:
October 20, 2009
Assignee:
Celmed Oncology (USA), Inc.
Inventors:
H. Michael Shepard, Ming Fai Chan, Michael P. Groziak
Abstract: Disclosed are hydrophilic choline/N-heterocycle ester compounds containing single amino acids, peptides, or derivatives thereof which have the potential to express anti-oxidant activity capable of reducing reactive oxygen species in cells. These compounds may be used to inhibit oxidative stress-induced cell injury or death both in vivo and ex vivo. In addition, methods for the synthesis of these compounds are disclosed.
Type:
Grant
Filed:
November 26, 2004
Date of Patent:
September 8, 2009
Assignee:
University of Rochester
Inventors:
Shey-Shing Sheu, Marion W. Anders, Lin Xu, Virendra K. Sharma
Abstract: New pharmaceutical compositions for oral use containing diclofenac together with alkali metal bicarbonates in amounts of from 20 to 80 by weight with respect to diclofenac are described. These compositions are entirely palatable and free from any unpleasant taste or other, side effects; in particular, these formulations permit to obtain in human patients higher Cmax of the active principle and shorter Tmax together with a lower coefficient of variation.
Abstract: Individuals suffering from multiple sclerosis may be treated by administration of an A3 adenosine receptor agonist (A3RAg), such as APNEA, AB-MECA, IB-MECA or Cl-IB-MECA. The A3RAg is preferably administered orally with a pharmaceutically acceptable carrier.
Type:
Grant
Filed:
December 23, 2004
Date of Patent:
December 16, 2008
Assignee:
Can-Fite Biopharma, Ltd.
Inventors:
Pnina Fishman, Sara Bar Yehuda, Lea Madi
Abstract: The present invention discloses compounds and methods used to specifically target substrates of methylation by S-adenosyl-L-methionine (SAM)-dependent methyltransferases. The substrates can be peptides, single stranded nucleic acids or double stranded nucleic acids, including RNA, DNA and PNA or phospholipids. The compounds disclosed are SAM analogs that are ligated to a methylation site by the methyltransferase. Also disclosed, are reacting groups that are ligatable to the cofactor analogs and can also be used as detectable labels. The reacting group can be used to cleave the substrate providing a methylation footprint. The invention can be used clinically to determine methylation state of a gene or gene promoter such as those involved in imprinting and transcription. In some preferred embodiments, the invention includes a kit, which can include one or more suitable SAM analogs and may include one or more detectable labels. In other preferred embodiments, the invention includes a pharmaceutical composition.
Type:
Grant
Filed:
January 11, 2006
Date of Patent:
December 16, 2008
Assignee:
Wisconsin Alumni Research Foundation
Inventors:
Scott R. Rajski, Lindsay R. Comstock, Rachel L. Weller
Abstract: The invention provides methods for removing a contaminant or inhibitor from a nucleic acid-comprising sample, wherein the contaminant or inhibitor inhibits the amplification or hybridization of the nucleic acid in the sample, or inhibits an enzymatic reaction utilizing the nucleic acid in the sample, the method comprising the steps of: (a) providing a reaction mixture comprising the sample, a chaotropic agent, ammonium acetate or an equivalent, and a detergent, (b) isolating the nucleic acid and remaining contaminants and inhibitors from the reaction mixture in a supernatant; and (c) contacting the nucleic acid supernantant with a flocculant resulting in the further removal of the contaminant or the inhibitor from the supernatant. The invention also provides kits that comprise the components necessary to carry out the method.
Type:
Grant
Filed:
May 20, 2005
Date of Patent:
December 2, 2008
Assignee:
Mo Bio Laboratories, Inc.
Inventors:
Mark N. Brolaski, Raveendran J. Venugopal, David Stolow
Abstract: Method for the sterospecific preparation of 2? or 3? deoxy and 2?,3?-dideoxy-?-L-pentafuranonucleoside compounds. 2? or 3? deoxy and 2?,3?-dideoxy-?-L-pentofuranonucleoside compounds are also described. Finally, the invention concerns the use of these compounds, and particularly 2?,3?dideoxy-?-L-fluorocytidine, as drugs, and especially as anti-viral agents.
Type:
Grant
Filed:
September 26, 2003
Date of Patent:
October 21, 2008
Assignees:
The UAB Research Foundation, Emory University, Centre National de la Recherche Scientifique (CNSR)
Inventors:
Gilles Gosselin, Jean-Louis Imbach, Anne-Marie Aubertin, Jean-Pierre Sommmadossi, Raymond F. Schinazi
Abstract: The invention relates to conjugates including at least one linker, a biomolecule coupled to the linker, and cyclohexane derivatives of the following formula: and oligomers thereof.
Type:
Grant
Filed:
December 23, 2003
Date of Patent:
October 21, 2008
Assignee:
Nanogen Recognomics GmbH
Inventors:
Christian Miculka, Norbert Windhab, Albert Eschenmoser, Stefan Scherer, Gerhard Quinkert
Abstract: The present invention provides a method of stimulating cervical and vaginal secretions in a mammal by treatment with P2Y2 and/or P2Y4 purinergic receptor agonists. Treatment of vaginal dryness associated with menopause, chemotherapy, and various disease states as well as the treatment of vulvar pain is discussed. Suitable agonists such as UTP, CTP, ATP, dinucleotides and analogs thereof are disclosed.
Type:
Grant
Filed:
March 20, 2000
Date of Patent:
October 7, 2008
Assignee:
Inspire Pharmaceuticals, Inc.
Inventors:
William Pendergast, Sammy Ray Shaver, David J. Drutz, Janet L. Rideout, Benjamin R. Yerxa
Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.
Abstract: The present invention provides a therapeutic method for treating biological diseases that includes the administration of an effective amount of a suitable antibiotic agent, antifungal agent or antiviral agent in conjunction with an A2A adenosine receptor agonist. If no anti-pathogenic agent is known the A2A agonist can be used alone to reduce inflammation, as may occur during infection with antibiotic resistant bacteria, or certain viruses such as those that cause SARS or Ebola. Optionally, the method includes administration of a type IV PDE inhibitor.
Type:
Grant
Filed:
December 2, 2004
Date of Patent:
September 23, 2008
Assignee:
University of Virginia Patent Foundation
Inventors:
Joel M. Linden, Kenneth Brayman, Gail W. Sullivan
Abstract: Precursors for use in the synthesis of polynucleotides are disclosed. The precursors include a heterocyclic base having an exocyclic amine group and a substituted or unsubstituted triaryl methyl protecting group bound to the exocyclic amine group.
Type:
Grant
Filed:
August 30, 2003
Date of Patent:
September 23, 2008
Assignee:
Agilent Technologies, Inc.
Inventors:
Douglas J. Dellinger, Agnieszka B. Sierzchala, Marvin H. Caruthers
Abstract: The present invention provides a method of optimizing therapeutic efficacy and reducing toxicity associated with 6-mercaptopurine drug treatment of an immune-mediated gastrointestinal disorder such as inflammatory bowel disease. The method of the invention includes the step of determining the level of one or more 6-mercaptopurine metabolites in the patient having an immune-mediated gastrointestinal disorder.
Abstract: Disclosed are compounds, compositions and methods for treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such compounds are represented by Formula IB as follows: and pharmaceutically acceptable prodrugs and salts thereof, where R, R1, R13, R14, W, W2, W3, Y and Z are as defined herein.
Type:
Grant
Filed:
September 30, 2003
Date of Patent:
September 16, 2008
Assignee:
Genelabs Technologies, Inc.
Inventors:
Christopher Don Roberts, Natalia B. Dyatkina
Abstract: Disclosed herein are compounds having Formula I, which are non-natural L-adenosine analogs. Also disclosed are their methods of making. Still further, disclosed are the uses of the disclosed compounds to treat cardiovascular disease, ischemia related injuries; and neurodegenerative diseases. The compounds disclosed herein have the formula: wherein R1 and R2 are, independently, H, branched or straight-chain, substituted or unsubstituted alkyl, alkenyl, alkynyl, or aryl; R3 is branched or straight-chain, substituted or unsubstituted alkyl, hydroxy-alkyl, or —C(?O)NR6R7; and R4 and R5 are, independently, H, hydroxy, halogen, and NR8R9, wherein R6, R7, R8, and R9 are, independently, H, branched or straight-chain, substituted or unsubstituted alkyl, alkenyl, alkynyl, or aryl.
Type:
Grant
Filed:
September 8, 2006
Date of Patent:
September 9, 2008
Assignee:
MUSC Foundation for Research Development
Inventors:
Giuseppe Gumina, Craig C. Beeson, Gary L. Wright
Abstract: The present invention provides novel chemical compounds, and methods for their use. In particular, the present invention provides indole derivatives (e.g. as shown in Formula (I)) and related compounds and methods of using indole derivatives and related compounds as therapeutic agents to treat a number of conditions, including those associated with viral infection and cardiovascular diseases.
Abstract: A method and composition for the treatment of HIV and HBV infections in humans and other host animals is disclosed that includes the administration of an effective amount of a [5-carboxamido or 5-fluoro]-2?,3?-dideoxy-2?,3?-didehydro-pyrimidine nucleoside or a [5-carboxamido or 5-fluoro]-3?-modified-pyrimidine nucleoside, or a mixture or a pharmaceutically acceptable derivative thereof, including a 5? or N4 alkylated or acylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.
Abstract: The subject of the present invention is specific lipidesters of halogenated nucleotides of the following formula wherein R1, R2, R3, X and Y are defined as described herein and salts thereof, said compounds have anti-cancer properties; pharmaceutical compositions containing the compounds, a method of synthesizing the compounds, and a method of using the compounds for treating malignant tumors.
Type:
Grant
Filed:
March 18, 2004
Date of Patent:
September 2, 2008
Assignee:
Heidelberg Pharma AG
Inventors:
Dieter Herrmann, Brigitte Heckl-Oestreicher, Christoph Mueller, Christian Lutz, Robert Voigt, William E. Bauta
Abstract: Methods of forming an internucleotide bond are disclosed. Such methods find use in synthesis of polynucleotides. The method involves contacting a functionalized support with a precursor having an exocyclic amine triaryl methyl protecting group under conditions and for a time sufficient to result in internucleotide bond formation. The functionalized support includes a solid support, a triaryl methyl linker group, and a nucleoside moiety having a reactive site hydroxyl, the nucleoside moiety attached to the solid support via the triaryl methyl linker group.
Type:
Grant
Filed:
August 30, 2003
Date of Patent:
August 26, 2008
Assignee:
Agilent Technologies, Inc.
Inventors:
Douglas J Dellinger, Agnieszka B. Sierzchala, Marvin H Caruthers, Geraldine F Dellinger