Phosphorus Containing Patents (Class 514/48)
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Patent number: 7148206Abstract: A method and composition for treating a host infected with flavivirus or pestivirus comprising administering an effective flavivirus or pestivirus treatment amount of a described 1?, 2? or 3?-modified nucleoside or a pharmaceutically acceptable salt or prodrug thereof, is provided.Type: GrantFiled: June 20, 2003Date of Patent: December 12, 2006Assignees: Idenix Pharmaceuticals, Inc., Universita Degli Studi Di CagliariInventors: Jean-Pierre Sommadossi, Paulo LaColla
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Patent number: 7148207Abstract: This invention relates to a quick-release tablet formulation with >99.19% pure fludara (high-purity fludara) as an active ingredient in a defined composition of residual contaminants.Type: GrantFiled: December 20, 2002Date of Patent: December 12, 2006Assignee: Schering AktiengesellschaftInventors: Wolfgang Heil, Ulf Tistam, Ralph Lipp, Johannes-Wilhelm Tack
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Patent number: 7132408Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutic effective amount of P2Y12 receptor antagonist compound, wherein said amount is effective to bind the P2Y12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y12 receptor antagonist compounds useful for this invention include mononucleoside 5?-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates of general Formula I, or salts thereof. The present invention also provides novel compounds of mononucleoside 5?-monophosphates, mononucleoside polyphosphates, and dinucleoside polyphosphates. The present invention further provides pharmaceutical formulations comprising mononucleoside 5?-monophosphates, mononucleoside polyphosphates, or dinucleoside polyphosphates.Type: GrantFiled: March 30, 2004Date of Patent: November 7, 2006Assignees: Inspire Pharmaceuticals, Inc., University of North CarolinaInventors: José L. Boyer, James G. Douglass, III, Sammy R. Shaver, Krzysztof Bednarski, Benjamin R. Yerxa, Gillian M. Olins
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Patent number: 7119110Abstract: A method for preventing and or reducing the symptoms of insulin resistance and a related syndrome in persons comprises identifying persons having or at risk for having such symptoms, and administering to them an effective amount of a composition comprising niacin-bound chromium that prevents or reduces the symptoms. Compositions incorporating niacin-bound chromium and additional compounds also are disclosed that are particularly effective in synergistically preventing or reducing these symptoms.Type: GrantFiled: October 4, 2002Date of Patent: October 10, 2006Assignee: Interhealth Nutraceuticals IncorporatedInventors: Debasis Bagchi, Harry G. Preuss, Shil C. Kothari
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Patent number: 7115585Abstract: The present invention relates to mononucleoside phosphate compounds that have the benefits of a dinucleotide pharmaceutical. These mononucleoside phosphates can be made from a mononucleotide that has been modified by attaching a degradation resistant substituent on the terminal phosphate of a polyphosphate mononucleotide. By attaching this degradation resistant substituent, the stability from degradation matches or exceeds those of certain dinucleotides.Type: GrantFiled: February 27, 2002Date of Patent: October 3, 2006Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, James G. Douglass, III, Sammy Ray Shaver, Ward M. Peterson, Edward G. Brown, Christopher S. Crean
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Patent number: 7115579Abstract: The invention provides methods for modulating the immune response caused by CpG dinucleotide-containing compounds. The methods according to the invention enables both decreasing the immunostimulatory effect for antisense applications, as well as increasing the immunostimulatory effect for immunotherapy applications.Type: GrantFiled: April 30, 2001Date of Patent: October 3, 2006Assignee: Idera Pharmaceuticals, Inc.Inventors: Sudhir Agrawal, Ekambar Kandimalla
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Patent number: 7109181Abstract: The present invention is directed to a method of altering the amount or composition of synovial fluids secreted from joints in a subject in need of such treatment. The method comprises administering to a subject a pharmaceutical composition comprising a P2Y purinergic receptor agonist in an amount effective to alter the amount or composition of synovial fluids. The P2Y purinergic receptor agonist is administered in an amount effective to stimulate secretion of synovial fluid, lubricin, hyaluronic acid, or surface-active phospholipids; to enhance joint lubrication; or to treat osteoarthritis. The pharmaceutical compositions useful in the present invention comprise a P2Y purinergic receptor agonist of Formula I and include, but are not limited to: uridine-, adenosine-, cytidine-5?-di- or triphosphates, dinucleoside polyphosphates, and analogs thereof. The invention is useful for treating conditions associated with reduced joint lubrication and joint stiffness, such as osteoarthritis.Type: GrantFiled: June 25, 2002Date of Patent: September 19, 2006Assignee: Inspire Pharmaceuticals, Inc.Inventors: Matthew S. Cowlen, Benjamin R. Yerxa, Arthur C. Jones, Edward G. Brown
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Patent number: 7105495Abstract: The invention provides methods for modulating the immune response caused by CpG dinucleotide-containing compounds. The methods according to the invention enables both decreasing the immunostimulatory effect for antisense applications, as well as increasing the immunostimulatory effect for immunotherapy applications.Type: GrantFiled: April 3, 2003Date of Patent: September 12, 2006Assignee: Idera Pharmaceuticals, Inc.Inventors: Sudhir Agrawal, Ekambar R. Kandimalla
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Patent number: 7105497Abstract: 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.Type: GrantFiled: June 14, 2005Date of Patent: September 12, 2006Assignee: Hôpital Sainte-JustineInventors: Ernest G. Seidman, Yves Theoret
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Patent number: 7101860Abstract: This invention is directed to a method of preventing or treating diseases or conditions associated with platelet aggregation. The method is also directed to a method of treating thrombosis. The method comprises administering to a subject a pharmaceutical composition comprising a therapeutically effective amount of P2Y12 receptor antagonist compound, wherein said amount is effective to bind the P2Y12 receptors on platelets and inhibit ADP-induced platelet aggregation. The P2Y12 receptor antagonist compounds useful for this invention include mononucleoside polyphosphates and dinucleoside polyphosphates of general Formula I, or salts thereof The present invention also provides compositions comprising mononucleoside polyphosphates and dinucleoside polyphosphates according to Formula Ia and Ib.Type: GrantFiled: August 21, 2001Date of Patent: September 5, 2006Assignees: Inspire Pharmaceuticals, Inc., University of North CarolinaInventors: Jose L. Boyer, Gillian M. Olins, Benjamin R. Yerxa, James G. Douglass
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Patent number: 7091190Abstract: The present invention is related to antiviral compositions comprising long-chain aliphatic compounds in combination with a nucleoside analog or phosphonoformic acid, in a pharmaceutically acceptable carrier. Methods for treating viral infections using such compositions are also disclosed.Type: GrantFiled: July 16, 2002Date of Patent: August 15, 2006Assignee: Avanir PharmaceuticalsInventors: John F. Marcelletti, Laura E. Pope, Mohammed H. Khalil, David H. Katz, Lee R. Katz
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Patent number: 7084128Abstract: The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a purinerginic receptor ligand, which is a mononucleoside polyphosphate or dinucleoside polyphosphate defined by general Formula I. The method of the present invention is useful in the treatment or prevention of ocular hypertension, such as glaucoma, including primary and secondary glaucoma. The method can be used alone to reduce intraocular pressure. The method can also be used in conjunction with other therapeutic agents or adjunctive therapy commonly used to treat glaucoma to enhance the therapeutic effect of reducing the intraocular pressure.Type: GrantFiled: January 15, 2003Date of Patent: August 1, 2006Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Robert Plourde, Jr., Edward G. Brown, Ward M. Peterson
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Patent number: 7084126Abstract: Methods and composisions for enhancing cellular function through protection of a tissue components such receptors, proteins, lipids, nucleic acids, carbohydrates, hormones, vitamins, and cofactors, by administering pyrophosphate analogs or related compounds.Type: GrantFiled: April 27, 2001Date of Patent: August 1, 2006Assignee: HealthPartners Research FoundationInventors: William H. Frey, II, John Randall Fawcett
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Patent number: 7081449Abstract: A purine nucleoside analog includes a pyrido[2,3-d]pyrimidine or a pyrimido[4,5-d]pyrimidine and further has a sugar moiety that is optionally modified at the C2?, C3?, C4? and/or C5? position. Particularly contemplated compounds also include prodrug forms of the purine nucleoside analogs, and both purine nucleoside analogs and the corresponding prodrugs are employed in the reduction of growth of neoplastic cells.Type: GrantFiled: July 3, 2001Date of Patent: July 25, 2006Assignee: Valeant Research & DevelopmentInventors: Zbigniew Pietrzkowski, Guangyi Wang, Johnson Lau, Zhi Hong, Jean-Luc Girardet, Esmir Gunic
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Patent number: 7071173Abstract: A method for treatment of HBV and HIV infections comprising administering the compound or salt of formula IgType: GrantFiled: August 12, 2005Date of Patent: July 4, 2006Assignee: Medivir ABInventors: Xiao-Xiong Zhou, Horst Wahling
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Patent number: 7056894Abstract: The present invention provides compounds having the formula: wherein A is chosen from a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group; both B and C are hydrogen, or either B or C is a halogen, amino, or thiol group and the other of B or C is hydrogen; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds.Type: GrantFiled: January 4, 2002Date of Patent: June 6, 2006Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Anthony A. Sauve, Vern L. Schramm
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Patent number: 7053064Abstract: The invention provides methods for treating or suppressing tobacco or nicotine usage or dependence involving administration of a therapeutically-effective amount of a cytosine-containing or cytidine-containing compound, creatine-containing compound, adenosine-containing, or adenosine-elevating compound to a mammal.Type: GrantFiled: November 6, 2003Date of Patent: May 30, 2006Assignee: The McLean Hospital CorporationInventor: Scott Lukas
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Patent number: 7049303Abstract: Disclosed is a pharmaceutical composition comprising a ribonucleoside analogue in accordance with general formula I or II as herein defined, in admixture with a physiologically acceptable excipient diluent or carrier.Type: GrantFiled: July 30, 2002Date of Patent: May 23, 2006Assignee: Medical Research CouncilInventors: David Loakes, Daniel M. Brown, Kazuo Negishi, Kei Moriyama, Jan Balzarini
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Patent number: 7045309Abstract: The present invention relates to 9-substituted adenine derivatives represented by formula (I) wherein W is selected from the group consisting of H, halogen, azido and amino group; X is selected from the group consisting of O, S, N(H), CH2, CH and C; Y is selected from the group consisting of H, hydroxy, C1-4 alkyl, C1-4 alkoxy and halogen; R is selected from the group consisting of H, hydroxymethyl, C1-4 alkyl, and C1-4 alkoxy; R1is selected from the group consisting of O, NH and CH2; R2represents a radical selected from the group consisting of —(CH2)n—S—C(O)—R4 and —(CH2)n—S—S—R4, where n=1-4 and R4is a C1-4-alkyl or aryl group and R4 is optionally substituted with a halogen, amino, N-alkylamino, N, N-dialkylamino or C1-4 alkoxy group and wherein each of the R2radicals may be the same or different; and R3is O or S. The derivatives are useful as prodrugs for inhibiting adenylyl cyclase and lowering 3?:5?-cAMP in cells, thereby inhibiting adenylyl cyclase dependent effects within cells.Type: GrantFiled: July 6, 2001Date of Patent: May 16, 2006Assignee: The Research Foundation of State University of New YorkInventors: Roger A. Johnson, Praveen Pande, Wolfgang Laux, Gilles Gosselin
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Patent number: 7030100Abstract: Several lines of evidence have shown a role for the nitric oxide (NO)/cyclic guanosine monophosphate (cGMP) signaling pathway in the development of spinal hyperalgesia. However, the roles of effectors for cGMP are not fully understood in the processing of pain in the spinal cord. cGMP-dependent protein kinase (PKG) I? but not PKGI? was localized in the neuronal bodies and processes, and was distributed primarily in the superficial laminae of the spinal cord. Intrathecal administration of an inhibitor of PKGI?, Rp-8-[(4-Chlorophenyl)thio]-cGMPS triethylamine, produces significant antinociception. Moreover, PKGI? protein expression was dramatically increased in the lumbar spinal cord after noxious stimulation. This upregulation of PKGI? expression was completely blocked not only by a neuronal NO synthase inhibitor, and a soluble guanylate cyclase inhibitor, but also by an N-methyl-D-aspartate (NMDA) receptor antagonist, MK-801.Type: GrantFiled: June 28, 2002Date of Patent: April 18, 2006Assignee: Johns Hopkins UniversityInventors: Yuanxiang Tao, Roger A. Johns
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Patent number: 7022680Abstract: The present invention provides compounds having the formula: wherein A is a nitrogen-, oxygen-, or sulfur-linked aryl, alkyl, cyclic, or heterocyclic group, the group being further substituted with an electron contributing moiety; B is hydrogen, or a halogen, amino, or thiol group; C is hydrogen, or a halogen, amino, or thiol group; and D is a primary alcohol, a hydrogen, or an oxygen, nitrogen, carbon, or sulfur linked to phosphate, a phosphoryl group, a pyrophosphoryl group, or adenosine monophosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted phosphodiester bridge, or to adenosine diphosphate through a phosphodiester or carbon-, nitrogen-, or sulfur-substituted pyrophosphodiester bridge. The present invention also provides pharmaceutical compositions containing the above compounds, methods of using the above compounds as pharmaceuticals, and processes for preparing the above compounds.Type: GrantFiled: May 30, 2002Date of Patent: April 4, 2006Assignee: Albert Einstein College of Medicine of Yeshiva UniversityInventors: Anthony A. Sauvé, Vern L. Schramm
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Patent number: 7018985Abstract: The present invention provides novel compounds of dinucleotide polyphosphates and the method of preventing or treating diseases or conditions associated with platelet aggregation. The method comprises administering systemically to a patient a pharmaceutical comprising a purinergic P2? receptor antagonist, in an amount effective to elevate its extracellular concentration to bind to P2? receptors and inhibit P2? receptor-mediated platelet aggregation. Methods of systemic administration include injection by intravenous, intramuscular, intrasternal and intravitreal routes, infusion, transdermal administration, oral administration, rectal administration and intra-operative instillation.Type: GrantFiled: August 21, 2000Date of Patent: March 28, 2006Assignees: Inspire Pharmaceuticals, Inc., University of North Carolina at Chapel HillInventors: José L. Boyer, Gillian M. Olins, Benjamin R. Yerxa, James G. Douglass, III
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Patent number: 6995145Abstract: The invention provides methods and compositions for modulating the activity of therapeutic agents for the treatment of a cancer by administering one or more agents that (either alone or in combination) induces telomere damage and inhibits telomerase activity in the cancer cell. The method initially uses, e.g., a telomere damage-inducing agent such as paclitaxel, and a telomerase inhibitory agent such as AZT. The invention also provides methods for identifying other agents with telomere damage-inducing activity and/or telomerase inhibitory activity (as well as and compositions having such activity), for use in the treatment of cancer.Type: GrantFiled: June 5, 2000Date of Patent: February 7, 2006Inventors: Jessie L.-S. Au, M. Guillaume Wientjes
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Patent number: 6987095Abstract: The present invention provides for the improved uptake of feed additives, pigments for use in coloring the flesh and the like. This improved intestinal uptake of foodstuffs and additives is effected through enhancing the development of the intestinal tract. Specifically the present method comprises of feeding fish with a diet which has an augmented level of nucleotides present therein. The nucleotides may be selected from the group consisting of nucleotides of uridine, guanosine, cytidine, thymindine, adenosine and mixtures thereof. The resultant improvement in the development of the intestinal tract leads to an improvement of the intestinal surfaces to absorb nutrients and/or dietary additives, this increase being at least partly due to an increase in gut surface area, for example through an increase in villus height.Type: GrantFiled: October 11, 2000Date of Patent: January 17, 2006Assignee: Ewos LimitedInventors: Charles Burrells, Paul David Williams
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Patent number: 6987097Abstract: 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.Type: GrantFiled: November 6, 2003Date of Patent: January 17, 2006Assignee: Hospital Sainte-JustineInventors: Ernest G. Seidman, Yves Théorêt
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Patent number: 6977246Abstract: The present invention relates to certain novel dinucleotides and formulations thereof which are highly selective agonists of the P2Y2 and/or P2Y4 purinergic receptor. They are useful in the treatment of chronic obstructive pulmonary diseases such as chronic bronchitis, PCD, cystic fibrosis, as well as prevention of pneumonia due to immobility. Furthermore, because of their general ability to clear retained mucus secretions and stimulate ciliary beat frequency, the compounds of the present invention are also useful in the treatment of sinusitis, otitis media and nasolacrimal duct obstruction. They are also useful for treatment of dry eye disease and retinal detachment as well as facilitating sputum induction and expectoration.Type: GrantFiled: November 6, 2001Date of Patent: December 20, 2005Assignee: Inspire Pharmaceuticals, Inc.Inventors: William Pendergast, Benjamin R. Yerxa, Janet L. Rideout, Suhaib M. Siddiqi
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Patent number: 6974802Abstract: A method of treating HBV or HIV infections comprising administering to an individual an effective amount of the compound of formula IId?: wherein R2 is the residue of an aliphatic L-amino acid, p is 0, 1, or 2-20, and q is 0, or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 16, 2001Date of Patent: December 13, 2005Assignee: Medivir ABInventors: Xiao-Xiong Zhou, Nils Gunnar Johansson, Horst Wahling
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Patent number: 6958324Abstract: Inosine compounds, compositions comprising an inosine compound and methods for treating or preventing an inflammation disease or a reperfusion disease comprising administering an effective amount of an inosine compound to a patient in need thereof are disclosed.Type: GrantFiled: March 26, 2002Date of Patent: October 25, 2005Assignee: Inotek Pharmaceuticals CorporationInventors: Andrew L. Salzman, Csaba Szabo
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Patent number: 6949522Abstract: The present invention includes compounds and compositions of ?-halonucleosides, as well as methods to treat HIV, HBV or abnormal cellular proliferation comprising administering said compounds or compositions.Type: GrantFiled: June 24, 2002Date of Patent: September 27, 2005Assignees: Pharmasset, Inc., The University of Georgia Research Foundation, Inc., Emory UniversityInventors: Michael J. Otto, Junxing Shi, Chung K. Chu, Raymond F. Schinazi, Giuseppe Gumina, Youhoon Chong, Yongseok Choi
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Patent number: 6919320Abstract: The invention relates to compositions comprising 2?-deoxyribonucleosides. The invention also relates to methods of accelerating the healing of wounds, abrasions, cuts, incisions, and superficial burns induced by heat, sunlight, chemical agents, or infections, and methods for ameliorating the effects of aging of the epidermal tissues comprising administering the compositions of the present invention to an animal.Type: GrantFiled: June 7, 1995Date of Patent: July 19, 2005Assignee: Wellstat Therapeutics CorporationInventors: Reid Warren von Borstel, Michael Kevin Bamat
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Patent number: 6897201Abstract: The present invention is directed to a method of reducing intraocular pressure. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a nucleoside 5?-pyrophosphate pyranoside or analogue, which is defined by general Formula I. The method of the present invention is useful in the treatment or prevention of ocular hypertension, such as found in glaucoma, including primary and secondary glaucoma. The method can be used alone to reduce intraocular pressure. The method can also be used in conjunction with another therapeutic agent or adjunctive therapy commonly used to treat glaucoma to enhance the therapeutic effect of reducing the intraocular pressure. The present invention also provides a novel composition comprising a nucleoside 5?-pyrophosphate pyranoside or analogues.Type: GrantFiled: February 27, 2002Date of Patent: May 24, 2005Assignee: Inspire Pharmaceuticals, Inc.Inventors: Jose L. Boyer, Benjamin R. Yerxa, Robert Plourde, Jr., Edward G. Brown
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Patent number: 6881831Abstract: The invention provides compounds capable of treating against hepatitis infections, particularly hepatitis B viral infections. Compounds of the invention are nucleic acid-based and preferably comprise 2, 3, 4, 5 or 6 nucleoside units.Type: GrantFiled: May 15, 2002Date of Patent: April 19, 2005Assignee: Migenix Inc.Inventors: Radhakrishnan P. Iyer, Yi Jin, Arlene Roland, Wenqiang Zhou
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Patent number: 6858591Abstract: The invention provides compounds of the Formula 1 wherein the definitions of m, n, R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12 and R13 are in the specification. These compounds are useful as antibacterial agents.Type: GrantFiled: April 25, 2002Date of Patent: February 22, 2005Assignee: Wyeth Holdings CorporationInventors: Ayako Yamashita, Emily Boucher Norton
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Patent number: 6838447Abstract: Disclosed are compositions that include triboelectrically chargeable nucleotide particles of less than 50 ?m diameter and carrier particles. In one example, a substrate is selectively patterned with the compositions, e.g., by transfer from a selectively charged surface. The compositions can be used to synthesize nucleic acid arrays.Type: GrantFiled: March 26, 2002Date of Patent: January 4, 2005Assignee: Linden Technologies, Inc.Inventor: Tai-Nang Huang
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Publication number: 20040266723Abstract: The disclosed invention is a composition for and a method of treating Flaviviridae (Hepacivirus, Flavivirus, Pestivirus) infections, including BVDV and HCV, in a host, including animals, and especially humans, using a small molecule or its pharmaceutically acceptable salt or prodrug.Type: ApplicationFiled: December 17, 2001Publication date: December 30, 2004Inventors: Michael J. Otto, Kyoichi A. Watanabe, Steve Patterson, Krysztof W. Pankiewicz, Lieven Stuyver
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Patent number: 6833362Abstract: A composition for accelerating the disposal of ethanol from bodily fluid. Certain additives can accelerate the metabolic oxidation of ethanol, and others in addition act as catalysts or “pseudo” enzymes for the oxidation. Additives include the oxidant Nicotinamide Adenine Dinucleotide and a variety of other additives such as transition metal ions and complexes thereof which favor the oxidation reaction. The compositions described can act as a sobriety inducer and/or as an effective palliative for the unpleasant effects of overuse of ethanol.Type: GrantFiled: June 7, 2001Date of Patent: December 21, 2004Inventors: Ward Beryl Bowen, Jr., Daniel Salman Daniel
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Patent number: 6833361Abstract: Conformationally restricted 2′, 4′-bridged nucleoside analogues are described herein. The compounds can be prepared by cyclization at C2′ and C4′ of nucleosides through a linker or linking molecule. These novel nucleosides have a desired, locked sugar pucker and are potentially useful as pharmaceutical ingredients, and especially for use in treatment of HCV.Type: GrantFiled: April 30, 2002Date of Patent: December 21, 2004Assignee: Ribapharm, Inc.Inventors: Zhi Hong, Haoyun An
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Publication number: 20040242465Abstract: Nucleotide analogs characterized by the presence of an amidate linked amino acid or an ester linked group which is bonded to the phosphorus atom of phosphonate nucleotide analogs are disclosed. The analogs comprise a phosphoamidate or ester bond that is hydrolyzed in vivo to yield a corresponding phosphonate nucleotide analog. Methods and intermediates for their synthesis and use are described.Type: ApplicationFiled: June 29, 2004Publication date: December 2, 2004Inventors: Norbert W. Bischofberger, Robert J. Jones, Murty N. Arimilli, Kuei-Ying Lin, Michael S. Louie, Lawrence R. McGee, Ernest J. Prisbe, William A. Lee, Kenneth C. Cundy
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Patent number: 6800616Abstract: Disclosed is a method of treating an HIV-infected host including administering to the host a therapeutic agent that is cytotoxic or cytostatic with respect to CD4+ T cells, but has reduced cytotoxic or cytostatic activity with respect to T lymphocyte stem cells, in a CD4+ T cell cytotoxic or cytostatic effective amount. Also disclosed is a method of treating an HIV-infected host including administering highly active antiretroviral therapy; and coadministering to the host a therapeutic agent that is cytotoxic or cytostatic with respect to CD4+ T cells, but has reduced cytotoxic or cytostatic activity with respect to T lymphocyte stem cells, in a CD4+ T cell cytotoxic or cytostatic effective amount.Type: GrantFiled: February 26, 1998Date of Patent: October 5, 2004Assignee: SuperGen, Inc.Inventor: Simeon M. Wrenn, Jr.
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Publication number: 20040192638Abstract: The present invention provides methods and compositions for slowing the transit time of foodstuffs, pharmaceutical compounds, nutritional supplements, and vitamins through the gastrointestinal tract using cyclic GMP (cGMP) alone and cGMP in combination with succinate. The method and corresponding compositions prolong residence time of such compounds, and thereby increase absorption through the small intestine, increase bioavailability, and improve feed conversion ratios.Type: ApplicationFiled: April 7, 2004Publication date: September 30, 2004Inventors: John A. Oaks, Paul Bass, David M. Barnes, Noah P. Zimmerman
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Patent number: 6787526Abstract: A method and composition for treating a host infected with hepatitis D comprising administering an effective hepatitis D treatment amount of a described 2′-deoxy-&bgr;-L-erythro-pentofuranonucleoside or a pharmaceutically acceptable salt or prodrug thereof.Type: GrantFiled: December 26, 2002Date of Patent: September 7, 2004Assignee: Idenix Pharmaceuticals, Inc.Inventors: Martin L. Bryant, Jean-Pierre Sommadossi
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Patent number: 6784161Abstract: The present invention relates to a method for the treatment or prevention of Flavivirus infections using nucleoside analogues in a host comprising administering a therapeutically effective amount of a compound having the formula I or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 20, 2001Date of Patent: August 31, 2004Assignee: BioChem Pharma, Inc.Inventors: Hicham Moulay Alaoui Ismaili, Yun-Xing Cheng, Jean-François Lavallée, Arshad Siddiqui, Richard Storer
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Patent number: 6762170Abstract: There are provided according to the invention, novel compounds of formula (I) wherein R1, R2 and R3 are as described in the specification, processes for preparing them, formulations containing them and their use in therapy for the treatment of inflammatory disease.Type: GrantFiled: July 31, 2000Date of Patent: July 13, 2004Assignee: SmithKlineBeecham CorporationInventors: Chuen Chan, Richard Charles Peter Cousins, Brian Cox
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Patent number: 6703376Abstract: A method of promoting drainage of mucous secretions in the congested airways of a bedridden/immobilized patient or an intubated/mechanically-ventilated patient is disclosed. The method comprises administering to the airways of the patient a uridine phosphate such as uridine 5′-triphsophate(UTP) or P1,P4-di(uridine-5′) tetraphosphate, an analog of UTP, or any other analog, in an amount effective to promote drainage of fluid in the congested airways, including sinuses, to create the ciliary beat frequency of cilia on the surface lumina epithelia cells, to increase the secretions of mucous by goblet cells and to promote the clearance of retained secretions by hydrating mucous secretions, by stimulating ciliary beat frequency in the airways and by stimulating surfactant production. Pharmaceutical formulations and methods of making the same are also disclosed.Type: GrantFiled: December 22, 1998Date of Patent: March 9, 2004Assignee: Inspire Pharmaceuticals, Inc.Inventors: Karla M. Jacobus, H. Jeff Leighton
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Patent number: 6689759Abstract: Provided are methods and compositions for treating hepatitis virus infections in mammals, especially humans. The methods comprise (1) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antiviral agents, nucleotide antiviral agents, mixtures thereof, or immunomodulating/immunostimulating agents, or (2) administering N-substituted-1,5-dideoxy-1,5-imino-D-glucitol compounds in combination with nucleoside antivirals agents, nucleotide antiviral agents, or mixtures thereof, and immunomodulating/immunostimulating agents.Type: GrantFiled: January 19, 2000Date of Patent: February 10, 2004Assignee: G. D. Searle & Co.Inventors: Gary S. Jacob, Timothy M. Block, Raymond A. Dwek
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Publication number: 20040023921Abstract: Pharmaceutical compositions comprise a nucleotide analog with a phosphonate group at a concentration effective to act as a substrate and/or inhibitor of a viral polymerase, and especially of the HCV RNA dependent RNA polymerase.Type: ApplicationFiled: April 29, 2003Publication date: February 5, 2004Inventors: Zhi Hong, Yung-hyo Koh, Jae Hoon Shim, Jean-Luc Girardet
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Patent number: 6680303Abstract: 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 acrylated derivative, or a pharmaceutically acceptable salt thereof, in a pharmaceutically acceptable carrier.Type: GrantFiled: May 15, 2002Date of Patent: January 20, 2004Assignee: Emory UniversityInventors: Raymond F. Schinazi, Dennis C. Liotta
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Patent number: 6680302Abstract: 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.Type: GrantFiled: December 27, 2001Date of Patent: January 20, 2004Assignee: Hospital Sainte-JustineInventors: Ernest G. Seidman, Yves Théorêt
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Patent number: 6677310Abstract: The present invention relates to compositions comprising analogues of purine nucleosides containing a ring-expanded (“fat”) heterocyclic ring, in place of purine, and an unmodified or modified sugar residue, pharmaceutically acceptable derivatives of such compositions, as well as methods of use thereof. In particular, these compositions may be utilized in the treatment of certain cancers, bacterial, fungal, parasitic, and viral infections, including, but not limited to, Acquired Immunodeficiency Syndrome (AIDS), hepatitis, Epstein-Barr and cytomegalovirus.Type: GrantFiled: April 21, 1999Date of Patent: January 13, 2004Assignees: Nabi, University of Maryland Baltimore CountyInventors: Ramachandra S. Hosmane, Ramesh K. Sood
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Patent number: RE38385Abstract: A material or mixture of materials which is not itself storage stable is rendered storage stable by incorporation into a water-soluble or swellable glassy or rubbery composition which can then be stored at ambient temperature. Recovery is by adding aqueous solution to the composition.Type: GrantFiled: August 28, 2001Date of Patent: January 13, 2004Assignee: Nektar TherapeuticsInventors: Felix Franks, Ross H. M. Hatley