Phosphorus Containing Patents (Class 514/51)
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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: 6852688Abstract: The subject invention provides novel methods and materials for treating diabetic retinopathy. One embodiment of the subject invention involves the co-administration of a somatostatin, or analogue thereof, and a thryoid-related substance such as thyroxine. Somatostatin or thyroid-related substance can be administered in combination, or separately through the same or different modes of administration.Type: GrantFiled: March 12, 2001Date of Patent: February 8, 2005Assignee: University of FloridaInventor: Maria Grant
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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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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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Patent number: 6825177Abstract: Methods for increasing the elimination half-life of key metabolites such as d4T by administering an aryl phosphate derivative of d4T having an electron withdrawing substituent on the aryl group and an amino acid substituent on the phosphate group are described. A preferred aryl phosphate derivative of d4T is HI-113 (d4T-5′-[p-bromophenyl methoxyalaninyl phosphate]). The administration of HI-113 results in more prolonged systemic exposure to the key metabolites, Ala-d4T-MP and d4T, than administration of an equimolar dose of either metabolite. Each metabolite has a significantly longer elimination half life when formed in vivo from the administration of HI-113 than when the metabolite is administered directly.Type: GrantFiled: October 19, 2001Date of Patent: November 30, 2004Assignee: Parker Hughes InstituteInventors: Fatih Uckun, Chun-Lin Chen, Taracad K. Venkatachalam, Zhoa-Hai Zhu
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Patent number: 6818629Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The pharmaceutical formulation useful in this invention comprises a P2Y receptor agonist with enhanced resistance to extracellular hydrolysis, such as dinucleoside polyphosphate compounds, or hydrolysis-resistant mononucleoside triphosphates.Type: GrantFiled: March 25, 2003Date of Patent: November 16, 2004Assignee: Inspire Pharmaceuticals, Inc.Inventors: Ward M. Peterson, Benjamin R. Yerxa
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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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Patent number: 6787525Abstract: The invention relates to glyceryl nucleotides of the formula Ia in which a) one of the radicals A1, A2 and A3 is a hydrogen atom or a radical selected from hydroxyl, mercapto, alkyl, alkenyl, polyoxyalkenyl, aryl, acyl, alkyloxy, alkenyloxy, polyoxyalkenyloxy, acyloxy, aryloxy, alkylthio, alkenylthio, acylthio and arylthio, where the alkyl, alkenyl and acyl radicals are optionally substituted by from 1 to 3 aryl radicals; and b1) two of the remaining radicals A1, A2 and A3 are two nucleoside groups which are different from each other; or b2) one of the remaining radicals A1, A2 and A3 is a nucleoside group and the other of the remaining radicals is a hydroxycarbonyl group, where at least one of the nucleoside groups is not a naturally occurring nucleoside group; to processes for preparing these compounds, to pharmaceutical remedies which comprise these compounds, and to the use of these compounds for treating cancer diseases and infectious diseases.Type: GrantFiled: September 12, 2001Date of Patent: September 7, 2004Inventors: Herbert Schott, Peter Stephan Ludwig
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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: 6774121Abstract: The invention discloses prodrugs comprising anti-proliferative drugs covalently linked, via bridging group, to a phospholipid moiety such that the active species is preferentially released, preferably by enzymatic cleavage, at the required site of action. The invention further discloses pharmaceutical compositions said prodrugs and the uses thereof for the treatment of diseases and disorders related to inflammatory, to degenerative or atrophic conditions, and to uncontrolled cell growth. FIG. 1 depicts a graph of animal survival during the course of an experiment wherein mice were i.p. transplanted with 11210 mouse leukemia cells and then treated with vehicle only (squares), MTX (triangles) or molar equivalent dose of DP-MTX071 (circles) according to the regiment described example in Example 11.Type: GrantFiled: March 13, 2002Date of Patent: August 10, 2004Assignee: D-Pharm, Ltd.Inventors: Alexander Kozak, Israel Shapiro, Marina Vinnikova, Leonid Ershov, Alexander Senderikhin, Oran Ayalon
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Publication number: 20040116359Abstract: The invention provides compositions comprising formula 1 steroids, e.g., 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one hemihydrate and one or more excipients, typically wherein the composition comprises less than about 3% water. The compositions are useful to make improved pharmaceutical formulations. The invention also provides methods of intermittent dosing of steroid compounds such as analogs of 16&agr;-bromo-3&bgr;-hydroxy-5&agr;-androstan-17-one and compositions useful in such dosing regimens. The invention further provides compositions and methods to inhibit pathogen (viral) replication, ameliorate symptoms associated with immune dysregulation and to modulate immune responses in a subject using certain steroids and steroid analogs. The invention also provides methods to make and use these immunomodulatory compositions and formulations.Type: ApplicationFiled: December 21, 2002Publication date: June 17, 2004Inventors: Clarence Nathaniel Ahlem, James Martin Frincke, Luis Daniel dos Anjos de Carvalho, William Heggie, Patrick T. Prendergast, Christopher L. Reading, Krupakar Paul Thadikonda, Russell Neil Vernon
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Publication number: 20040092476Abstract: Compounds of Formula I, their preparation and uses are described: 1Type: ApplicationFiled: October 31, 2003Publication date: May 13, 2004Inventors: Serge Boyer, Mark D. Erion
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Publication number: 20040077585Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The pharmaceutical formulation useful in this invention comprises a P2Y receptor agonist with enhanced resistance to extracellular hydrolysis, such as dinucleoside polyphosphate compounds, or hydrolysis-resistant mononucleoside triphosphates.Type: ApplicationFiled: October 8, 2003Publication date: April 22, 2004Inventors: Ward M. Peterson, Benjamin R. Yerra
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Publication number: 20040063651Abstract: Excellent remedies for hepatitis C which contain as the active ingredients a 3′-deoxy-3′-fluorouridine derivatives and a 1-(3′-deoxy-fluoro-&bgr;-L-ribofuranosyl)uracil derivative and show little side effects.Type: ApplicationFiled: July 31, 2003Publication date: April 1, 2004Inventors: Masahiko Morioka, Masaru Ubasawa, Masaaki Arai
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Patent number: 6713458Abstract: The present invention provides new methods for the synthesis of the therapeutic dinucleotide, P1,P4-di(uridine 5′-tetraphosphate), and demonstrates applicability to the production of large quantities. The methods of the present invention substantially reduce the time period required to synthesize diuridine tetraphosphate, preferably to three days or less. The novel tetrammonium and tetrasodium salts of P1,P4-di(uridine 5′-tetraphosphate) (Formula I) prepared by these methods are stable, soluble, nontoxic, and easy to handle during manufacture. Therapeutic uses of Formula I include treatment of sinusitis, otitis media, dry eye, retinal detachment, nasolacrimal duct obstruction, female infertility and irritation due to vaginal dryness, via increased mucus secretions and hydration of the epithelial surface. wherein: X is Na, NH4 or H, provided that all X groups are not H.Type: GrantFiled: November 24, 1999Date of Patent: March 30, 2004Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, William Pendergast
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Patent number: 6706876Abstract: The present invention is directed to a pulp useful for making lyocell fibers. The pulp has a degree of polymerization from about 300 to about 1000; an alpha cellulose content of less than about 90% and in one instance can be made in a roll form. The degree of polymerization can be modified by acid hydrolysis, steam explosion; or alkaline enzymate degradation.Type: GrantFiled: September 18, 2001Date of Patent: March 16, 2004Assignee: Weyerhaeuser CompanyInventors: Mengkui Luo, Vincent A. Roscelli, Amar N. Neogi
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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: 6696425Abstract: This invention is directed to a method of stimulating tear secretion and mucin production in eyes. The method comprises the step of administering to the eyes of a subject a composition comprising a compound of Formula I, II, III, or IV and its pharmaceutically acceptable salts, in an amount effective to stimulate tear fluid secretion. The method of the present invention may be used to increase tear production for any reason, including, but not limited to, treatment of dry eye disease and corneal injury. Pharmaceutical formulations and methods of making the same are also disclosed. Methods of administering the same would include: topical administration via a liquid, gel, cream, or as part of a contact lens or selective release membrane; or systemic administration via nasal drops or spray, inhalation by nebulizer or other device, oral form (liquid or pill), injectable, intra-operative instillation or suppository form.Type: GrantFiled: December 19, 2001Date of Patent: February 24, 2004Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Karla Jacobus, William Pendergast, Janet L. Rideout
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Patent number: 6689762Abstract: Method of inhibiting or treating Human Immunodeficiency Virus (HIV) infection, comprising administering to a patient in need thereof an effective amount of a pharmaceutically acceptable composition comprising a PEG-ASNase compound or asparaginase, and optionally at least one compound selected from the group consisting of protease inhibitor compounds, ribonucleotide reductase inhibitor compounds and HIV reverse transcriptase inhibitor compounds.Type: GrantFiled: August 6, 1999Date of Patent: February 10, 2004Assignee: Enzon Pharmaceuticals, Inc.Inventors: Vassilios I. Avramis, Lewis Cohen
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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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Patent number: 6683061Abstract: This invention provides novel substrate compounds that selectively inhibit the proliferation of pathological cells, for example, pathological calls that endogenously overexpress a target enzyme that confers resistance to biologic and chemotherapeutic agents. The enzyme acts on a substrate compound to 1) convert it to a cellular toxin and/or 2) release a toxic byproduct. In one embodiment, the activity of the target enzyme has been greatly enhanced in a target cell as a result of loss of tumor suppressor function and/or selection resulting from previous exposure to chemotherapy. In another embodiment, the pathological cell contains a target enzyme that is an expression product of an infectious agent in the cell. Further provided by this invention is a method for treating a subject by delivering to the subject a prodrug as described herein. The prodrugs of this invention may be used alone or in combination with other chemotherapeutics or alternative anti-cancer therapies such as radiation.Type: GrantFiled: October 10, 2001Date of Patent: January 27, 2004Assignee: NewBiotics, Inc.Inventors: H. Michael Shepard, Ming Fai Chan, Michael P. Groziak
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Publication number: 20040014713Abstract: The present invention are directed to P1, P4-di(uridine 5′)-tetraphosphate, tetra-alkali metal salts such as tetrasodium, tetralithium, tetrapotassium, and mixed tetra-alkali metal cations thereof. The tetra alkali metal salts of P1, P4-di(uridine 5′)-tetraphosphate are water-soluble, nontoxic, and easy to handle during manufacture. These tetra-monovalent alkali metal salts are more resistant to hydrolysis than the mono-, di-, or tri-acid salts, therefore, they provide an improved stability and a longer shelf life for storage. The present invention also provides methods for the synthesis of P1, P4-di(uridine 5′)-tetraphosphate, and its pharmaceutically acceptably acceptable salts thereof, and demonstrates the applicability to the production of large quantities. The methods substantially reduce the time required to synthesize diuridine tetraphosphate, for example, to three days or less.Type: ApplicationFiled: April 14, 2003Publication date: January 22, 2004Inventors: Benjamin R. Yerxa, Edward G. Brown
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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: 6673779Abstract: The present invention is directed to a method of stimulating ciliary beat frequency to promote mucociliary or cough clearance of retained mucus secretions from the lungs, sinuses, upper airways, ears, eyes, genito-urinary tract, spermatozoa, ovaries, fallopian tubes, neutrophils, and macrophages of a patient. The method comprises administering uridine triphosphates, adenosine triphosphates, cytidine triphosphates, or dinucleoside tetraphosphates and the derivatives thereof to an affected body of a patient, to treat dysfunction of the mucociliary clearance system as a result of impaired ciliary movement in the patient.Type: GrantFiled: June 5, 2002Date of Patent: January 6, 2004Assignees: Inspire Pharmaceuticals, Inc., The University of North Carolina at Chapel HillInventors: Karla M. Jacobus, Benjamin R. Yerxa, William Pendergast, Richard C. Boucher, Jr., Janet L. Rideout, David J. Drutz, Michael K. James, Monroe Jackson Stutts, Cara Geary, Eduardo R. Lazarowski
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Patent number: 6670336Abstract: 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: April 13, 2000Date of Patent: December 30, 2003Assignee: Parker Hughes InstituteInventors: Fatih M. Uckun, Rakesh Vig
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Publication number: 20030236217Abstract: Disclosed are compositions and methods for alleviating mucositis, wherein said methods and compositions are directed to the formulation or use of selected nucleoside derivatives, especially ADP-ribose, that conform to the general formula A-B-X and pharmaceutically acceptable salts thereof, wherein “A” is a nucleoside structure selected from adenosine, guanosine, and uridine; “B” is a diphosphate linkage attached to the 5′ carbon of the nucleoside ribose moiety; and “X” is attached to B an is a moiety selected from hydrogen, furanose, or pyranose. Also disclosed are pharmaceuticals and nutritional liquid embodiments thereof, including lozenges, mouthwashes, or other product forms that effectively coat the oral, laryngeal or other mucosal areas.Type: ApplicationFiled: April 18, 2003Publication date: December 25, 2003Inventors: Robert A. Shalwitz, Tapas Das, Paul W. Johns, James L. Leach
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Patent number: 6663859Abstract: D-Ribose and methods for using D-Ribose are provided for enhancing the immune response in mammals. Those with a less than optimal immune response will benefit from oral or parenteral administration of D-Ribose. Methods are also provided for the enhancement of the immune response in isolated leukocytes. Leukocytes are cultured ex vivo in the presence of D-Ribose and transfused into a patient in need of leukocyte augmentation.Type: GrantFiled: January 8, 2001Date of Patent: December 16, 2003Assignees: Bioenergy, Inc., University of FloridaInventors: Susan S. Percival, Robin J. Henken, John St. Cyr, Clarence A. Johnson, Terri L. Butler
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Patent number: 6660723Abstract: 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&ggr;9&dgr;2 lymphocytes.Type: GrantFiled: March 1, 2001Date of Patent: December 9, 2003Assignee: Institut National de la Sante et de la Recherche MedicaleInventors: Christian Belmant, Jean-Jacques Fournie, Marc Bonneville, Marie-Alix Peyrat
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Publication number: 20030220290Abstract: 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: 1Type: ApplicationFiled: May 13, 2003Publication date: November 27, 2003Applicants: Centre National da la Reserche Scientifique, L'Universite Montpellier II, Idenix Pharmaceuticals Inc.Inventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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Method and pharmaceutical composition for inhibiting invasion and/or metastasis of ovarian carcinoma
Publication number: 20030199474Abstract: The invention discloses a compound of the general formula (I) 1Type: ApplicationFiled: April 25, 2003Publication date: October 23, 2003Inventors: Li-Wei Hsu, Su-Chen Chang -
Publication number: 20030186917Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a pharmaceutical formulation comprising a hydrolysis-resistant P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist can be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The pharmaceutical formulation useful in this invention comprises a P2Y receptor agonist with enhanced resistance to extracellular hydrolysis, such as dinucleoside polyphosphate compounds, or hydrolysis-resistant mononucleoside triphosphates.Type: ApplicationFiled: March 25, 2003Publication date: October 2, 2003Inventors: Ward M. Peterson, Benjamin R. Yerxa
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Publication number: 20030186927Abstract: Based on research for compounds that can display a corneal epithelial migration promoting effect in ophthalmology, the present invention provides P2Y receptor agonist corneal epithelial migration promoters, such as phosphoric acid compounds having an adenosyl group, uridyl group, xanthosyl group, guanosyl group, or thymidyl group, or their salts, with excellent corneal epithelial migration promoting effects.Type: ApplicationFiled: May 20, 2003Publication date: October 2, 2003Inventors: Katsuhiko Nakata, Masatsugu Nakamura, Tsutomu Fujihara, Hiromi Fujita
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Publication number: 20030186930Abstract: Uridine analogs and techniques for making and using uridine analogs are disclosed in this invention. These uridine analogs include nucleoside phosphates having a 5-aminouracil group. These nucleotides can be incorporated into a nucleic acid as an unnatural base, as a substitute for uridine or thymine. The nucleic acid can then be treated with an oxidizing agent and an alkaline solution, which causes cleavage of the nucleic acid at the position of the unnatural base. The nucleoside phosphate analogs can be used in many ways, including measuring chemical interactions between nucleic acids and other compounds, or sequencing nucleic acids. Additional compounds can also be derivitized onto the amino group, allowing other functionalities to be added to the nucleoside phosphate, or to the nucleic acid incorporating the nucleoside phosphate.Type: ApplicationFiled: February 7, 2002Publication date: October 2, 2003Inventors: Gregory L. Verdine, Michael Storek
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Patent number: 6624150Abstract: The invention provides a method of regulating water and mucin secretions and fluid transport in the gastrointestinal tract. The invention also provides a method for treating a gastrointestinal disease in which the mucosal barrier of the gastrointestinal system is impaired. The invention additionally provides a method for correcting disorders of fluid secretion or absorption in the gastrointestinal system. The method comprises administering to a patient a pharmaceutical composition comprising a purinergic P2Y receptor agonist, in an amount effective to regulate water and mucin secretions or to correct abnormal fluid transport in the gastrointestinal tract.Type: GrantFiled: December 22, 2000Date of Patent: September 23, 2003Assignee: Inspire Pharmaceuticals, Inc.Inventors: Benjamin R. Yerxa, Janet L. Rideout, William Pendergast, Sammy Ray Shaver, Zhen Zhang, Ward M. Peterson, Matthew Cowlen
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Patent number: 6620796Abstract: The invention provides new methods for synthesis of nucleotide-based compounds and new libraries of such compounds. Compounds of the invention are useful for a variety of therapeutic applications, including treatment of viral or bacterial infections and associated diseases and disorders.Type: GrantFiled: November 8, 2000Date of Patent: September 16, 2003Assignee: Micrologix Biotech Inc.Inventors: Wenqiang Zhou, Yi Jin, Arlene Roland, Radhakrishnan Iyer
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Patent number: 6617444Abstract: The present invention is directed to crystals of P1-(2′-deoxycytidine 5′-)P4-(uridine 5′-)tetraphosphate (dCP4U) or a salt thereof and to a process for producing the crystals. The present invention also provides a process for producing dCP4U involving reacting uridine 5′-monophosphate (UMP), 2′-deoxycytidine 5′-monophosphate (dCMP), diphenyl phosphorochloridate (DPC), and pyrophosphate (PPi). The crystals of dCP4U obtained through the process according to the present invention have high purity and high stability and no hygroscopicity as compared with a freeze-dried product, and thereby serve as a useful raw material for preparing a pharmaceutical. The process for producing dCP4U according to the present invention permits use of inexpensive UMP as a raw material and realizes high yield. Thus, the process is suitable for large-scale synthesis of dCP4U.Type: GrantFiled: November 30, 2000Date of Patent: September 9, 2003Assignee: Yamasa CorporationInventors: Kenya Mori, Takanori Miyashita, Hideaki Maeda, Hiroshi Sato, Yutaka Noda
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Patent number: 6610841Abstract: This invention relates to nucleotide-based prodrugs and their drug-delivery applications. The nucleotide-based prodrugs of the present invention comprise a drug component covalently attached via junctional ester bond(s) to one or more nucleotide components. Release and activation of the drug component of a nucleotide-based prodrug arises from hydrolysis of the junctional ester bond joining the nucleotide component to the drug component. The active drug component may be a nucleoside analog, a nucleic acid ligand, or a non-nucleoside drug. The nucleotide component provides a means of targeting and/or anchoring the nucleotide-based prodrug to the desired tissue compartment and/or a mechanism of sustained release of the active drug, thereby providing for a more effective drug delivery system with reduced toxicity.Type: GrantFiled: December 18, 1997Date of Patent: August 26, 2003Assignee: Gilead Sciences, Inc.Inventor: Stephen Warren
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Publication number: 20030158147Abstract: The present invention is directed to a method of treating pain. The method comprises administering to a subject a pharmaceutical composition comprising an effective amount of a P2X receptor antagonist. The methods of the present invention are useful in reducing pain, such as traumatic pain, neuropathic pain, organ pain and pain associated with diseases. The P2X receptor antagonists particularly useful for this invention are mononucleoside polyphosphate derivatives or dinucleoside polyphosphate derivatives of general Formula I. The compounds of the present method can be used alone to treat pain. The compounds of the present method can also be used in conjunction with other therapeutic agents or adjunctive therapies commonly used to treat pain, thus enhancing the overall pain-reducing effect in a subject in need of such treatment.Type: ApplicationFiled: January 31, 2003Publication date: August 21, 2003Inventors: Benjamin R. Yerxa, Ward M. Peterson, Christopher S. Crean
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Patent number: 6602664Abstract: It has been discovered that 3′-azido-2′,3′-dideoxyuridine (CS-87) induces a transient mutation in HIV-1 at the 70th codon (K to R, i.e., lysine to arginine) of the reverse transcriptase region of the virus. Based on this discovery, a method and composition for treating HIV is provided that includes administering CS-87 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 70th codon of the reverse transcriptase region. This invention can be practiced by referring to the published mutation patterns for known anti-HIV drugs, or by determining the mutation pattern for a new drug.Type: GrantFiled: February 26, 2001Date of Patent: August 5, 2003Assignees: Emory University, Idenix Pharmaceuticals, Inc.Inventors: Raymond F. Schinazi, Martin L. Bryant, Maureen W. Myers
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Patent number: 6599887Abstract: Compounds are disclosed for treating AIDS, herpes, and other viral infections by means of lipid derivatives of antiviral agents. The compounds consist of nucleoside analogues having antiviral activity which are linked, commonly through a phosphate group at the 5′ position of the pentose residue, to one of a selected group of lipids. The lipophilic nature of these compounds provide advantages over the use of the nucleoside analogue alone. It also makes it possible to incorporate them into the lamellar structure of liposomes, either alone or combined with similar molecules. In the form of liposomes, these antiviral agents are preferentially taken up by macrophages and monocytes, cells which have been found to harbor the target HIV virus. Additional site specificity may be incorporated into the liposomes with the addition of ligands, such as monoclonal antibodies or other peptides or proteins which bind to viral proteins.Type: GrantFiled: May 1, 2001Date of Patent: July 29, 2003Assignee: Chimerix, Inc.Inventors: Karl Y. Hostetler, Raj Kumar, Louise M. Stuhmiller
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Patent number: 6596725Abstract: The present invention provides a method of treating edematous retinal disorders. The method comprises administration of a P2Y receptor agonist to stimulate the removal of pathological extraneous fluid from the subretinal and retinal spaces and thereby reduce the accumulation of said fluid associated with retinal detachment and retinal edema. The P2Y receptor agonist may be administered with therapeutic and adjuvant agents commonly used to treat edematous retinal disorders. The pharmaceutical composition useful in this invention comprises a P2Y receptor agonist with enhanced resistance to extracellular hydrolysis, such as dinucleoside polyphosphate compounds.Type: GrantFiled: January 30, 2001Date of Patent: July 22, 2003Assignee: Inspire Pharmaceuticals, Inc.Inventors: Ward M. Peterson, Benjamin R. Yerxa
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Patent number: 6589941Abstract: The invention relates to a method of producing a composition and to a composition for preventing or reducing formation of resistance in cytostatic treatment comprising combining BVDU, a salt thereof or BVDU in protected form or in prodrug form with at least one cytostatic agent in order to prevent or reduce the formation of resistance during cytostatic treatment. The present invention is also directed to a method of reducing resistance in cytostatic treatment comprising delivering therapeutically-effective amount of at least one cytostatic agent and a therapeutically effective amount of BVDU, a salt thereof, or BVDU in protected form or in prodrug form.Type: GrantFiled: March 7, 2000Date of Patent: July 8, 2003Assignee: Resprotect GmbHInventors: Rudolf Fahrig, Angela Steinkamp-Zucht
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Publication number: 20030125299Abstract: The present invention provides a method of preventing or treating an inflammatory disease, including but not limited to, sinusitis, rhinitis, conjunctivitis, asthma, dermatitis, inflammatory bowel disease, inflammatory collagen vascular diseases, glomerulonephritis, inflammatory skin diseases, and sarcoidosis. The method comprises administrating to a subject a pharmaceutical formulation comprising a nucleotide receptor agonist, such as nucleoside diphosphate, nucleoside triphosphate, or dinucleoside polyphosphate, according to general formula Ia, Ib, IIa, IIb, or III. Preferred indications of the present invention are perennial allergic rhinitis, seasonal allergic rhinitis, infectious allergic rhinitis, and allergic conjunctivitis.Type: ApplicationFiled: November 6, 2002Publication date: July 3, 2003Inventors: Ward M. Peterson, Benjamin R. Yerxa
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Publication number: 20030114415Abstract: This invention relates to compositions and methods for preventing and treating cognitive dysfunction or memory impairment. The compositions include an effective amount of citicoline, or pharmaceutically-acceptable salts thereof, and one or more of the compounds selected from the group consisting of linoleic acid and linolenic acid. Other compositions of this invention include an effective amount of citicoline, or pharmaceutically-acceptable salt thereof, wherein said citicoline is metabolized to form at least one of cytidine, uridine, and choline. Still other compositions of this invention include effective amounts of choline, cytidine, and/or uridine, or their pharmaceutically-acceptable salts. This invention also encompasses methods for preparing these compositions.Type: ApplicationFiled: February 13, 2002Publication date: June 19, 2003Inventors: Richard J. Wurtman, Lisa Teather
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Publication number: 20030109697Abstract: This invention provides compounds, compositions and methods for treating cancer, infectious disease, an autoimmune disorder or an inflammatory condition.Type: ApplicationFiled: April 9, 2002Publication date: June 12, 2003Inventors: H. Michael Shepard, Andrew Rein Vaino, Danielle M. Lehsten
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Patent number: 6576622Abstract: This invention pertains to a method for treating a human with human immunodeficiency virus infection which comprises administering to the human a therapeutically effective amount of a thymidine analog, which analog acts as an inhibitor of viral reverse transcriptase necessary for viral replication of human immunodeficiency virus, and a thymidylate synthase inhibitor, or pharmaceutically acceptable salts thereof.Type: GrantFiled: September 10, 1997Date of Patent: June 10, 2003Assignee: University of Medicine & Dentistry of New JerseyInventors: Roger Strair, Daniel Medina, Peter Tung
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Publication number: 20030105026Abstract: The invention relates to new compositions and medical uses, such as anti-infectious pharmacology. The compositions include salts and compounds of GSSG including at least one counterion comprising a nitrogenous base. Examples of such nitrogenous bases include DNA bases, nucleosides of DNA bases, nucleotides of DNA bases, RNA bases, nucleosides of RNA bases, nucleotides of RNA bases, inosine, nucleotides of inosine, and homologues, analogues and derivatives thereof. The invention is also directed to methods for treatment and prevention of infectious diseases such as viral hepatitis B and C, AIDS and herpes.Type: ApplicationFiled: February 7, 2002Publication date: June 5, 2003Inventors: Leonid A. Kozhemyakin, Andrew L. Kozhemyakin
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Patent number: 6569837Abstract: 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 14, 2001Date of Patent: May 27, 2003Assignee: Idenix Pharmaceuticals Inc.Inventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant
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Patent number: 6566344Abstract: 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-pentoftiranonucleoside 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 14, 2001Date of Patent: May 20, 2003Assignee: Idenix Pharmaceuticals, Inc.Inventors: Gilles Gosselin, Jean-Louis Imbach, Martin L. Bryant