Patents Examined by Eric Crane
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Patent number: 6444652Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted.Type: GrantFiled: December 10, 1999Date of Patent: September 3, 2002Assignees: Novirio Pharmaceuticals Limited, Centre National da la Recherche ScientifiqueInventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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Patent number: 6440948Abstract: 2-(3-,4-(substituted)-5-alkylthienyl)adenosines and the 5′-uronic acid amide analogues thereof having the following formula: are disclosed herein. Additionally disclosed are medicinal methods of treatment wherein the adenosine A2A agonist activity of the noted compounds stimulates mammalian coronary vasodilation for therapeutic purposes and for purposes of imaging the heart.Type: GrantFiled: June 20, 2000Date of Patent: August 27, 2002Assignee: CV Therapeutics, Inc.Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
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Patent number: 6437118Abstract: The invention relates to a process for the preparation of vinyl pyrimidines of the formula I wherein R1 is hydrogen or a carboxylic ester group, and R2 is hydrogen or a group of the formula (a) wherein Ra is hydrogen, a protecting group or a group easily hydrolyzable under physiological conditions, by reacting a compound of the formula II wherein R21 is hydrogen or a group (a) wherein hydroxy groups are optionally protected, R3 is bromo, chloro or iodo, and R1 is as above, with a vinyl borane compound in the presence of a Pd complex and a base, and optionally, further reacting a product of formula I wherein R2 is hydrogen with a compound of the formula IV wherein Rb is a hydroxy protecting group and Z is a leaving group, in the presence of a Lewis acid catalyst.Type: GrantFiled: May 23, 2000Date of Patent: August 20, 2002Assignee: Hoffmann-La Roche Inc.Inventors: Kurt Püntener, Michelangelo Scalone
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Patent number: 6429315Abstract: This invention is directed to a process for preparing N6-substituted adenosine derivatives, to intermediates useful therefor and to methods of preparing these intermediates.Type: GrantFiled: January 21, 2000Date of Patent: August 6, 2002Assignee: Aventis Pharmaceuticals Inc.Inventors: Adam W. Sledeski, Luc Grondard, Matthew R. Powers, Tory H. Powner, Michael K. O'Brien, Ching T. Tsuei, Patrick Leon, Gregory G. Kubiak, Laurence Pailleres-Hubert, Benoit Viguier
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Patent number: 6407076Abstract: A compound of formula (I) wherein R2 represents C1-3 alkyl, halogen or hydrogen; R3 represents a fluorinated straight or branched alkyl group of 1-6 carbon atoms; and salts and solvates thereof, in particular, physiologically acceptable solvates and salts thereof. These compounds are agonists of the Adenosine A1 receptor.Type: GrantFiled: June 27, 2000Date of Patent: June 18, 2002Assignee: SmithKline Beecham CorporationInventors: Philip Charles Box, Brian David Judkins, Andrew Michael Kenneth Pennell
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Patent number: 6403567Abstract: 2-adenosine N-pyrazole compositions having the following formula: and methods for using the compositions as A2A receptor agonists to stimulate mammalian coronary vasodilatation for therapeutic purposes and for purposes of imaging the heart.Type: GrantFiled: June 22, 1999Date of Patent: June 11, 2002Assignee: CV Therapeutics, Inc.Inventors: Jeff A. Zablocki, Elfatih O. Elzein, Venkata P. Palle
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Patent number: 6395716Abstract: This invention is directed to a method for treating a host infected with hepatitis B comprising administering an effective amount of an anti-HBV biologically active 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof, wherein the 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside has the formula: wherein R is selected from the group consisting of H, straight chained, branched or cyclic alkyl, CO-alkyl, CO-aryl, CO-alkoxyalkyl, CO-aryloxyalkyl, CO-substituted aryl, alkylsulfonyl, arylsulfonyl, aralkylsulfonyl, amino acid residue, mono, di, or triphosphate, or a phosphate derivative; and BASE is a purine or pyrimidine base which may be optionally substituted.Type: GrantFiled: August 10, 1999Date of Patent: May 28, 2002Assignees: Novirio Pharmaceuticals Limited, Centre National da la Recherche ScientifiqueInventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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Patent number: 6384209Abstract: The invention relates to the chemical synthesis of oligonucleotides and to chemical entities useful in such synthesis. More particularly, the invention relates to sulfurization of the internucleoside linkages of oligonucleotides. The invention provides new sulfur transfer reagents and processes for their use in sulfurizing oligonucleotides. The sulfur transfer reagents according to the invention are inexpensive to make, stable in storage and highly efficient in sulfurization.Type: GrantFiled: November 26, 1997Date of Patent: May 7, 2002Assignee: Avecia Biotechnology, Inc.Inventors: Jin-Yan Tang, Zhaoda Zhang
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Patent number: 6350736Abstract: Aryl phosphate derivatives of d4T with para-bromo substitution on the aryl group show markedly increased potency as anti-HIV agents without undesirable levels of cytotoxic activity. In particular, these derivatives are potent inhibitors of HIV reverse transcriptase. In a preferred aspect of the present invention, the phosphorus of the aryl phosphate group is further substituted with an amino acid residue that may be esterified or substituted, such as a methoxy alaninyl group.Type: GrantFiled: December 15, 1999Date of Patent: February 26, 2002Assignee: Parker Hughes InstituteInventors: Faith M. Uckun, Rakesh Vig
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Patent number: 6339074Abstract: Hyaluronic acid, hyaluronate esters and salts thereof are sulfated such that the number of sulfate groups per monomeric unit is in the range of from 0.5 to 3.5. The sulfated derivatives exhibit anticoagulant and cell adhesion reduction properties, and may be used to prepare biomaterials.Type: GrantFiled: November 23, 1999Date of Patent: January 15, 2002Assignee: Fidia Advanced Biopolymers, SrlInventors: Gloria Cialdi, Agnese Magnani
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Patent number: 6323185Abstract: A method and compositions for treating viral infection in vitro and in vivo using a guanosine-rich oligonucleotide. The oligonucleotides have sufficient guanosine to form a guanosine tetrad. Also provided are oligonucleotides of at least two runs of at least two guanosines. Also provided are guanosine-rich oligonucleotides and methods for treating viral infections in humans, and a method for designing guanosine-rich oligonucleotides having anti-viral activity and integrase inhibition activity.Type: GrantFiled: July 17, 1996Date of Patent: November 27, 2001Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Robert F. Rando, Susan Fennewald, Joseph G. Zendegui, Joshua O. Ojwang, Michael E. Hogan
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Patent number: 6294522Abstract: N6 heterocyclic 8 modified adenosine derivatives that are selective, partial or full adenosine A1 receptor partial or full agonists, and as such, are useful for modifying cardiac activity, modifying adipocyte function, treating central nervous system disorders, and treating diabetic disorders and obesity in mammals, and especially in humans.Type: GrantFiled: December 3, 1999Date of Patent: September 25, 2001Assignee: CV Therapeutics, Inc.Inventors: Jeff A. Zablocki, Venkata P. Palle, Prabha N. Ibrahim, Luiz Belardenelli
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Patent number: 6291670Abstract: The invention provides 4′-C-ethynyl pyrimidine nucleosides (other than 4′-C-ethynylthymidine) represented by formula [I]: wherein B represents a base selected from the group consisting of pyrimidine and derivatives thereof; X represents a hydrogen atom or a hydroxyl group; and R represents a hydrogen atom or a phosphate residue; and a pharmaceutical composition containing any one of the compounds and a pharmaceutically acceptable carrier. Preferably, the composition is used as an anti-HIV agent or a drug for treating AIDS.Type: GrantFiled: May 12, 2000Date of Patent: September 18, 2001Assignee: Yamasa CorporationInventors: Hiroshi Ohrui, Shiro Shigeta, Eiichi Kodama, Haruhiko Machida, Satoru Kohgo, Hiroaki Mitsuya
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Patent number: 6288042Abstract: Guanosine-rich oligonucleotides having sequences that favor the formation under physiological conditions of a stable four-stranded structure containing two stacked guanosine quartets (G4s) are disclosed. These oligonucleotides demonstrate enhanced nuclease resistance, cellular uptake and biological efficacy. Methods and composition for treating viral infection using these guanosine-rich oligonucleotides are also disclosed. Certain embodiments of the new oligonucleotides are 16-17 nucleotides long and contain at least one C-5 propynyl dU substitution. A method for designing anti-viral oligonucleotides is also disclosed.Type: GrantFiled: February 3, 1998Date of Patent: September 11, 2001Assignees: Aronex Pharmaceuticals, Inc., Baylor College of MedicineInventors: Robert F. Rando, Joshua O. Ojwaug, Michael E. Hogan, Thomas L. Wallace, Paul A. Cossum
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Patent number: 6271212Abstract: Pharmaceutical prodrug compositions are provided comprising azide derivatives of drugs which are capable of being converted to the drug in vivo. Azide derivatives of drugs having amine, ketone and hydroxy substituents are converted in vivo to the corresponding drugs, increasing the half-life of the drugs. In addition azide prodrugs are often better able to penetrate the blood-brain barrier than the corresponding drugs. Especially useful are azide derivatives of cordycepin, 2′-F-ara-ddI, AraA, acyclovir, penciclovir and related drugs. Useful azide prodrugs are azide derivatives of therapeutic alicyclic amines, ketones, and hydroxy-substituted compounds, including aralkyl, heterocyclic aralkyl, and cyclic aliphatic compounds, where the amine or oxygen moiety is on the ring, or where the amine or oxygen moiety is on an aliphatic side chain, as well as therapeutic purines and pyrimidines, nucleoside analogs and phosphorylated nucleoside analogs.Type: GrantFiled: March 3, 1998Date of Patent: August 7, 2001Assignees: University of Georgia Research Foundation Inc., Emory UniversityInventors: Chung K. Chu, Lakshimi Kotra, Kostantine K. Manouilov, Jinfa Du, Raymond Schinazi
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Patent number: 6271370Abstract: The present invention relates to an improved method for synthesizing nucleosides with a low &agr;:&bgr; anomeric ratio. The method comprises coupling a protected furanosyl halide and an appropriately protected heterocycle in the presence of a nucleophilic polar solvent and a strong base.Type: GrantFiled: May 8, 2000Date of Patent: August 7, 2001Assignee: Pfizer INCInventor: Robert W. Scott
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Patent number: 6262254Abstract: An efficient, regiocontrolled approach to the synthesis of 8-fluoropurines by direct fluorination of purines with dilute elemental fluorine, or acetyl hypofluorite, is provided. In a preferred embodiment, a purine compound is dissolved in a polar solvent and reacted with a dilute mixture of F2 in He or other inert gas.Type: GrantFiled: November 25, 1998Date of Patent: July 17, 2001Assignee: The Regents of Univ. of CaliforniaInventors: Jorge R. Barrio, Nagichettiar Satyamurthy, Mohammad Namavari, Michael E. Phelps
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Patent number: 6248905Abstract: Acyl derivatives of glycosyl-L-ascorbic acids which have a higher oil-solubility than L-ascorbic acid, glycosyl-L-ascorbic acids, and inorganic esters of L-ascorbic acid such as phosphates and sulfates of L-ascorbic acid. When administered to living bodies, the acyl derivatives easily permeate into living tissues to release L-ascorbic acid, resulting in an exertion of the physiological action inherent to L-ascorbic acid. Thus, the derivatives can be arbitrarily used in food products, cosmetics, and pharmaceuticals.Type: GrantFiled: March 3, 1999Date of Patent: June 19, 2001Assignees: Kabushiki Kaisha Hayashibara Seibutsu Kagaku KenkyujoInventors: Yoshihito Fujinami, Shino Okazaki, Akihiro Tai, Kenji Sasaki, Itaru Yamamoto
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Patent number: 6232464Abstract: The invention relates to an apparatus for isolating nucleic acids from biological fluids and suspensions containing nucleic acids, a reaction compartment 17 for receiving an adsorption medium 100 being connected to a removal compartment 50, and the nucleic acids being able to be moved and enriched from the reaction compartment 17 into the removal compartment 50 by an electrophoresis apparatus 20a, 20b.Type: GrantFiled: August 27, 1999Date of Patent: May 15, 2001Inventor: Hans Lange
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Patent number: 6229008Abstract: &agr;-D-pentofuranoside derivatives have the general formula (D), in which R stands for (C1-C4)alkyl that is non-substituted or substituted one or several times by halogen, (C1-C4)alkyl, (C1-C4)alkoxy and/or phenyl, and R1 stands for [(C6-C20)aryl]k−[(C1-C4)alkyl or [(C6-C20)]aryl]k−[(C1-C12)alkyl)(3-k)Si in which k=0 to 3, that are non-substituted or substituted one or several times by halogen, (C1-C4)alkyl, (C1-C4)alkoxy and/or (C6-C20) aryl, or preferably a benzyl that is non-substituted or substituted one or several times by the above substituents. Also disclosed are starting and intermediary compounds, up to furanosides (D) having an analogous structure, processes for preparing said furanosides and their precursors, and their use.Type: GrantFiled: April 18, 1997Date of Patent: May 8, 2001Inventors: Jörn Saischek, Berndt Stadelmann