Abstract: The present invention concerns novel C2,5?-disubstituted and N6,C2,5?-trisubstituted adenosine derivatives and their different uses. These adenosine derivatives were found to be potent adenosine receptor agonists and thus are of a therapeutic value in the treatment and prophylaxis of diseases and disorders affected by adenosine receptor agonists.
Abstract: A reduction inhibitory agent for active-oxygen eliminating activity comprises trehalose as an effective ingredient. A method for inhibiting the reduction of active-oxygen eliminating activity comprises incorporating either trehalose or the reduction inhibitory agent into plant edible products and/or plant antioxidants. A composition is provided that reduces the active-oxygen eliminating activity of plant edible products and/or plant antioxidants.
Abstract: The present invention relates to processes for the preparation of any of the intermediate 1,3-substituted indenes of the formulae (Ia), (Ib) and (Ic) or a mixture thereof: wherein R1, R2, R3, R4, and R5 are defined herein. Compounds of formulae (Ia), (Ib) and (Ic) or mixtures thereof are useful in the preparation of compounds of formula (II): wherein R2, R3 and R6 are also defined herein.
Abstract: Synthetic processes are provided wherein oligomeric compounds are prepared having phosphodiester, phosphorothioate, phosphorodithioate, or other covalent linkages. The oligomers have substantially reduced exocyclic adducts deriving from acrylonitrile or related contaminants.
Type:
Grant
Filed:
December 28, 2004
Date of Patent:
March 6, 2007
Assignee:
Isis Pharmaceuticals, Inc.
Inventors:
Vasulinga Ravikumar, Muthiah Manoharan, Daniel C. Capaldi, Achim Krotz, Douglas L. Cole, Andrei P. Guzaev
Abstract: 2-adenosine N-pyrazole compounds having the following formula: and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart are disclosed.
Type:
Grant
Filed:
August 29, 2003
Date of Patent:
February 27, 2007
Assignee:
CV Therapeutics, Inc.
Inventors:
Jeff Zablocki, Elfatih O. Elzein, Venkata P. Palle, Luiz Belardinelli
Abstract: Disclosed are methods and intermediates for the preparation of 7-(2?-R1-substituted-?-D-ribofuranosyl)-4-amino-5-(optionally substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine compounds. These compounds are useful in treating viral infections caused by a flaviviridae family virus, such as hepatitis C virus. Such 7-(2?-substituted-?-D-ribofuranosyl)-4-amino-5-(optionally substituted ethyn-1-yl)-pyrrolo[2,3-d]pyrimidine compounds are represented by Formula I as follows: wherein, each of R1, R2, and R3 are as defined herein.
Type:
Grant
Filed:
October 20, 2004
Date of Patent:
January 30, 2007
Assignee:
Genelabs Technologies, Inc.
Inventors:
Christopher D. Roberts, Jesse D. Keicher, Natalia B. Dyatkina
Abstract: A process of manufacturing oligonucleotides includes a 5?-deblocking step in which the 5-blocking group is removed with dichloroacetic acid that is essentially free of chloral. The process is useful for making oligonucleotides that are substantially free of chloral adducts.
Type:
Grant
Filed:
March 31, 2003
Date of Patent:
January 30, 2007
Assignee:
Isis Pharmaceuticals, Inc.
Inventors:
Achim Krotz, Daniel Capaldi, Hans Gaus, Brett Turney
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 I as follows: wherein, Y, W, W1 and W2 are as defined herein.
Type:
Grant
Filed:
October 20, 2004
Date of Patent:
January 2, 2007
Assignee:
Genelabs Technologies, Inc.
Inventors:
Jesse D. Keicher, Christopher D. Roberts, Natalia B. Dyatkina
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 I as follows: wherein, R, Y, W, W1 and W2 are as defined herein.
Type:
Grant
Filed:
June 4, 2004
Date of Patent:
December 19, 2006
Assignee:
Genelabs Technologies, Inc.
Inventors:
Christopher D. Roberts, Jesse D. Keicher
Abstract: A method for treating a cancer. The cancer excluding an adenocarcinoma and being epithelioma, glioma, sarcoma, melanoma, lymphoma or leukemia; or the cancer is an adenocarcinoma cancer excluding colon cancer, lung cancer and gastric cancer. The method comprises administering to a subject in need thereof and suffering from cancer, a pharmaceutically effective amount of at least one sulfoquinovosylacylglycerol compound represented by formula (1): wherein R101 represents an acyl residue of an unsaturated fatty acid and R102 represents a hydrogen atom and/or at least one pharmaceutically acceptable salt thereof.
Abstract: Disclosed are novel compounds that are partial and full A1 adenosine receptor agonists, useful for treating various disease states, in particular tachycardia and atrial flutter, angina, myocardial infarction and hyperlipidemia.
Type:
Grant
Filed:
February 19, 2003
Date of Patent:
December 5, 2006
Assignee:
CV Therapeutics, Inc.
Inventors:
Prabha Ibrahim, Elfatih Elzein, Kevin Shenk, Robert Jiang, Jeff Zablocki, Xiaofen Li, Christopher Morrison, Thao Perry, Dengming Xiao
Abstract: This specification discloses 2-adenosine N-pyrazole compounds having the following formula: and methods for using the compounds as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.
Type:
Grant
Filed:
October 18, 2005
Date of Patent:
December 5, 2006
Assignee:
CV Therapeutics, Inc.
Inventors:
Jeff A. Zablocki, Elfatih O. Elzein, Venkata Palle, Luiz Belardinelli
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 I as follows: wherein, each of R, Y, W, W1 and W2 is as defined herein.
Type:
Grant
Filed:
June 4, 2004
Date of Patent:
December 5, 2006
Assignee:
Genelabs Technologies, Inc.
Inventors:
Christopher D. Roberts, Jesse D. Keicher
Abstract: Oligonucleotides with a novel sugar-phosphate backbone containing at least one internucleoside 3?-NHP(O)(S?)O-5? linkage, and methods of synthesizing and using the inventive oligonucleotides are provided. The inventive thiophosphoramidate oligonucleotides were found to retain the high RNA binding affinity of the parent oligonucleotide N3??P5? phosphoramidates and to exhibit a much higher acid stability.
Type:
Grant
Filed:
October 18, 2004
Date of Patent:
November 21, 2006
Assignee:
Geron Corporation
Inventors:
Sergei Gryaznov, Krisztina Pongracz, Tracy Matray
Abstract: A reusable linker arm for solid support oligonucleotide synthesis, the linker arm comprising formula (a) wherein Z is a linker moiety and T is an organic radical.
Type:
Grant
Filed:
June 30, 1999
Date of Patent:
November 14, 2006
Assignee:
University Technologies International Inc.
Abstract: The present invention provides nucleoside compounds and certain derivatives thereof which are inhibitors of RNA-dependent RNA viral polymerase. These compounds are inhibitors of RNA-dependent RNA viral replication and are useful for the treatment of RNA-dependent RNA viral infection. They are particularly useful as inhibitors of hepatitis C virus (HCV) NS5B polymerase, as inhibitors of HCV replication, and/or for the treatment of hepatitis C infection. The invention also describes pharmaceutical compositions containing such nucleoside compounds alone or in combination with other agents active against RNA-dependent RNA viral infection, in particular HCV infection. Also disclosed are methods of inhibiting RNA-dependent RNA polymerase, inhibiting RNA-dependent RNA viral replication, and/or treating RNA-dependent RNA viral infection with the nucleoside compounds of the present invention.
Type:
Grant
Filed:
October 17, 2003
Date of Patent:
October 24, 2006
Assignee:
Merck & Co., Inc.
Inventors:
Balkrishen Bhat, Neelima Bhat, Anne B. Eldrup, Thazha P. Prakash, Marija Prhavc, Quanlai Song, Phillip Dan Cook, Steven S. Carroll, Malcolm Maccoss, David B. Olsen
Abstract: The present invention discloses a method for treating HIV that includes administering ?-D-D4FC or its pharmaceutically acceptable salt or prodrug to a human in need of therapy in combination or alternation with a drug that induces a mutation in HIV-1 at a location other than the 70(K to N), 90 or the 172 codons of the reverse transcriptase region. Also disclosed is a method for using ?-D-D4FC as “salvage therapy” to patients which exhibit drug resistance to other anti-HIV agents. ?-D-D4FC can be used generally as salvage therapy for any patient which exhibits resistance to a drug that induces a mutation at other than the 70(K to N), 90 or the 172 codons.
Type:
Grant
Filed:
January 23, 2003
Date of Patent:
October 3, 2006
Assignee:
Emory University
Inventors:
Raymond F. Schinazi, Jennifer L. Hammond, John W. Mellors, Dennis C. Liotta
Abstract: Compositions comprising the nucleotides adenosine diphosphate and adenosine monophosphate, and their use for neutralizing effects of excess incident energy on the human body, particularly effects of ionizing radiation from nuclear or radiological energy sources, are disclosed and claimed.
Abstract: Novel C2,8-disubstituted adenosine derivatives disclosed herein have been found to be potent adenosine receptor agonists, in particular for the A2A receptor. The said compounds have biological activity against conditions such as hypertension, ischemic heart disease, ischemic brain disease, psychosis and wound healing. Further, the invention also discloses a process for the preparation of such compounds and pharmaceutical compositions comprising them.
Abstract: The invention provides compounds comprising at least one phosphohalohydrin group of the formula: where X is a halogen selected from among I, Br, Cl, R1 is selected from among —CH3 and —CH2—CH3, Cat+ is an organic or inorganic cation, and n is an integer between 2 and 20, processes for the production thereof and uses thereof, in particular therapeutic uses and for activating primate T?9?2 lymphocytes.
Type:
Grant
Filed:
October 14, 2003
Date of Patent:
September 19, 2006
Assignee:
Institut National de la Sante et de la Recherchik Medicale
Inventors:
Christian Belmant, Jean-Jacques Fournie, Marc Bonneville, Marie-Alix Peyrat