Phosphorus Containing Patents (Class 554/78)
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Patent number: 6313106Abstract: The present invention relates to compounds, which are phospholipid derivatives of valproic acid, to compositions comprising said compounds and their use for treating epilepsy, migraine, bipolar disorders and pain.Type: GrantFiled: July 12, 2000Date of Patent: November 6, 2001Assignee: D-Pharm Ltd.Inventor: Alexander Kozak
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Patent number: 6303803Abstract: Disclosed is a method for reducing the sterol, for example cholesterol, content of sterol-containing substances such as fats and oils. The method provides an efficient and cost effective process based on the affinity of cholesterol and other sterols for amphipathic molecules that form hydrophobic, fluid bilayers, such as phospholipid bilayers. Aggregates of amphipathic molecules are contacted with, for example, a sterol-containing fat or oil in an aqueous environment and then mixed. Following adequate mixing, the sterol-reduced fat or oil is separated from the aqueous separation mixture. Alternatively, the correspondingly sterol-enriched fraction also may be isolated from the aqueous separation mixture.Type: GrantFiled: April 25, 2000Date of Patent: October 16, 2001Assignee: Cargill, IncorporatedInventor: Dharma R. Kodali
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Patent number: 6258836Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug. In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: November 29, 1999Date of Patent: July 10, 2001Assignee: Protarga, Inc.Inventor: Victor E. Shashoua
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Patent number: 6221856Abstract: Inositol derivatives, compositions comprising inositol derivatives, and methods for using compositions comprising inositol derivatives as agents for inhibiting superoxide anion production are described. The inositol derivatives are obtainable via conventional organic synthesis. The inositol derivatives inhibit superoxide anion produced by neutrophils and macrophages which cause tissue damage.Type: GrantFiled: February 3, 1999Date of Patent: April 24, 2001Assignees: Inologic, Inc., Regents of the University of CaliforniaInventors: Alexis E. Traynor-Kaplan, Carsten Schultz, Marco T. Rudolf
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Patent number: 6107499Abstract: The invention involves the formation of a prodrug from a fatty acid carrier and a neuroactive drug. The prodrug is stable in the environment of both the stomach and the bloodstream and may be delivered by ingestion. The prodrug passes readily through the blood brain barrier. Once in the central nervous system, the prodrug is hydrolyzed into the fatty acid carrier and the drug to release the drug.In a preferred embodiment, the carrier is 4, 7, 10, 13, 16, 19 docosahexa-enoic acid and the drug is dopamine. Both are normal components of the central nervous system. The covalent bond between the drug and the carrier preferably is an amide bond, which bond may survive the conditions in the stomach. Thus, the prodrug may be ingested and will not be hydrolyzed completely into the carrier molecule and drug molecule in the stomach.Type: GrantFiled: June 6, 1995Date of Patent: August 22, 2000Assignee: Neuromedica, Inc.Inventor: Victor E. Shashoua
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Patent number: 6077837Abstract: The invention relates to a pharmaceutically acceptable prodrug which is a covalent conjugate of a pharmacologically active compound and an intracellular transporting adjuvant, characterized by the presence of a covalent bond which is scission-sensitive to intracellular enzyme activity. The prodrug may be used in a technique for treating a condition or disease in a mammal related to supranormal intracellular enzyme activity, whereby on administering it to a human having such condition or disease, the bond is broken in response to such activity, and the pharmacologically active compound is activated selectively within cells having such supranormal intracellular enzyme activity.Type: GrantFiled: October 23, 1998Date of Patent: June 20, 2000Assignee: D-Pharm Ltd.Inventor: Alexander Kozak
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Patent number: 6002029Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.Type: GrantFiled: December 8, 1997Date of Patent: December 14, 1999Inventors: Karl Y. Hostetler, Ganesh D. Kini
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Patent number: 5902802Abstract: Cationic amphiphiles are provided that are alkyl or alkoxyalkyl O-phosphate esters of diacylphosphatidyl zwitterionic compounds such as phosphatidylcholine or phosphatidyl ethanolamine. The amphiphiles can be used as carriers for delivering macromolecules intracellularly.Type: GrantFiled: November 17, 1997Date of Patent: May 11, 1999Assignee: Megabios CorporationInventor: Timothy D. Heath
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Patent number: 5859271Abstract: The present invention provides compositions and methods for protecting cells from injury due to intrinsic membrane lysis, oxidation and/or invasion by destructive agents. Even more particularly, the present invention provides compositions and methods for treating or prophylactically inhibiting phospholipase mediated injury, injury due to oxidation, and inflammation. In a very specific sense, this invention provides compositions and methods of making these compositions that are inhibitors of phospholipase.Type: GrantFiled: April 15, 1996Date of Patent: January 12, 1999Assignee: Virginia Commonwealth UniversityInventors: Richard C. Franson, Raphael M. Ottenbrite
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Patent number: 5846955Abstract: This invention relates to a method for improving the efficiency of a drug containing a free carboxy group, the improvement comprising esterifying said carboxy group to the hydroxy group of the glycerol portion of a glycerolphospholipid ester having the formula: ##STR1## or pharmaceutically acceptable salts thereof wherein one of R.sub.1 and R.sub.2 is hydrogen and the other is hydrogen, a hydrocarbyl fatty acid acyl group having 4-26 carbon atoms or a hydrocarbyl heteroatom fatty acid acyl group having 3-25 carbon atoms, or ##STR2## and R is a naturally occurring polar head group characteristic of a glycerophospholipid isolated from endogenous sources;R.sub.3 is hydrogen or lower alkyl andR.sub.Type: GrantFiled: June 6, 1995Date of Patent: December 8, 1998Assignee: Research Corporation Technologies, Inc.Inventors: Charles Pidgeon, Robert J. Markovich
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Patent number: 5780397Abstract: There is disclosed a lubricant additive ingredient that imparts extreme pressure anti-wear properties to lubricant additive compositions. Specifically, there is disclosed a derivative of a vegetable oil triglyceride, a wax ester or a telomerized oil reacted with phosphorous pentasulfide to produce a phosphorous-sulfur (PS) extreme pressure additive.Type: GrantFiled: September 25, 1996Date of Patent: July 14, 1998Assignee: International Lubricants, Inc.Inventors: Phillip S. Landis, Blaine N. Rhodes, Will F. Williamson
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Patent number: 5744461Abstract: Lipid-containing prodrugs are provided for treating viral infections due to herpes, influenza, hepatitis B, Epstein-Barr, and varicella zoster viruses, as well as cytomegalovirus and derivatives of antiviral agents. The compounds comprise phosphonoacids having antiviral activity which are linked, either through the phosphate group or carboxyl group of the phosphonoacid, to one of a selected group of lipids. Phosphonoacetic acid and phosphonoformic acid are thus linked to phospholipids, glycerolipids, sphingolipids, glycolipids, or fatty acids. The compounds persist, after intracellular hydrolysis, as the antiviral phosphonoacids. The lipid prodrugs are effective in improving the efficacy of antiviral phosphonoacids by prolonging their antiviral activity following administration.Type: GrantFiled: May 26, 1995Date of Patent: April 28, 1998Assignee: NeXstar Pharmaceuticals, Inc.Inventors: Karl Y. Hostetler, Raj Kumar
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Patent number: 5696277Abstract: Lipid prodrugs of phosphonoacids and their analogs that have increased antiviral activity over the parent drugs in inhibiting cytomegalovirus and other susceptible viruses.Type: GrantFiled: November 15, 1994Date of Patent: December 9, 1997Assignee: Karl Y. HostetlerInventors: Karl Y. Hostetler, Ganesh D. Kini
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Patent number: 5677472Abstract: A method for extracting sphingomyelin from a phospho-lipid-containing fat concentrate is described. The method comprises the following steps:A. dissolving the fat concentrate in a solvent mixture of an essentially polar organic solvent and an essentially non-polar organic solvent,B. withdrawing a phase consisting mainly of the non-polar organic solvent and phospholipids dissolved therein,C. adding to the phase withdrawn in step B an organic solvent of intermediate polarity at a temperature of about 13.degree.-25.degree. C., thereby forming a precipitate comprising mainly sphingomyelin, together with a viscous phase and a solvent phase, and thenD. withdrawing the precipitate and the viscous phase, and separating them from one another.Type: GrantFiled: September 21, 1995Date of Patent: October 14, 1997Assignee: Svenska Mejeriernas Riksfoerening Ekonomi ABInventors: Lena Nyberg, Hans Burling
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Patent number: 5643948Abstract: Compounds having anti-inflammatory and other activities are disclosed. The compounds are derived from diterpenes of the phorbol-, resiniferonol- and ingenol-classes.Type: GrantFiled: September 13, 1993Date of Patent: July 1, 1997Assignee: Procyon Pharmaceuticals, Inc.Inventors: Paul E. Driedger, James Quick
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Patent number: 5616745Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6 R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.Type: GrantFiled: June 7, 1995Date of Patent: April 1, 1997Assignee: Centre National de la Recherche ScientifiqueInventors: Jean-Paul Behr, Jean-Philippe Loeffler
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Patent number: 5567597Abstract: The present invention provides compounds that function as hydrolytic enzyme inhibitors (inactivators) and substrates. These compounds are useful in assays to detect and measure levels of hydrolytic enzyme activity and are more particularly useful in treatment regimens for various disease states and conditions implicating the underlying specific hydrolytic enzyme. Examples of hydrolytic enzymes include, but are not limited to, phospholipases, lipases, esterases, proteases, etc.Type: GrantFiled: February 14, 1995Date of Patent: October 22, 1996Assignee: The Regents of the University of CaliforniaInventors: Edward A. Dennis, William N. Washburn
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Patent number: 5552070Abstract: A process for the phosphorylation of epoxides, in particular of epoxidised fatty acid esters, and the use of the phosphorylation products for the production of lubricants.Type: GrantFiled: October 11, 1994Date of Patent: September 3, 1996Assignee: Rhein Chemie Rheinau GmbHInventors: Volker Schafer, Robert Kohler, Gunter Schilling, Alfred Pauli, Ingo Rohrs, Joachim Korff
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Patent number: 5550263Abstract: The present invention refers to a phospholipid-based compound, that is a phospholipid to which an X-ray contrast-giving moiety has been covalently linked, liposomes comprising said compound as well as the use of said liposomes as a diagnostic or contrast agent.Type: GrantFiled: December 30, 1993Date of Patent: August 27, 1996Assignee: Karlshamns LipidTeknik ABInventors: Bengt Hersl of, K.ang.re Larsson, Stig Bengmark
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Patent number: 5523430Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, and inhibition of cholesterol biosynthesis, are effected by compounds of the formula ##STR1## their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:X is --ONR.sup.1 C(O)--, --N(OR.sup.1)C(O)--, --NR.sup.1 C(O)--, --C(O)NR.sup.1 --, --NR.sup.1 S(O.sub.2)--, --C(O)O--, --OC(O)--, --O--, --NR.sup.1 -- or --(S)q;Y and Z are each independently --CO.sub.2 R.sup.2, --SO.sub.3 R.sup.2 or --P(O)(OR.sup.2)(OR.sup.3);R is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkenylene or aryl;R.sup.1, R.sup.2 and R.sup.3 are each independently hydrogen, alkyl, aryl or aralkyl;m and n are each independently 0 or an integer from 1 to 5;p is 0 or 1; andq is an integer from 1 to 2.Type: GrantFiled: May 23, 1994Date of Patent: June 4, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Dinesh V. Patel, Scott A. Biller, Eric M. Gordon
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Patent number: 5463092Abstract: Lipid-containing prodrugs are provided for treating viral infections due to herpes, influenza, hepatitis B, Epstein-Barr, and varicella zoster viruses, as well as cytomegalovirus and derivatives of antiviral agents. The compounds comprise phosphonoacids having antiviral activity which are linked, either through the phosphate group or carboxyl group of the phosphonoacid, to one of a selected group of lipids. Phosphonoacetic acid and phosphonoformic acid are thus linked to phospholipids, glycerolipids, sphingolipids, glycolipids, or fatty acids. The compounds persist, after intracellular hydrolysis, as the antiviral phosphonoacids. The lipid prodrugs are effective in improving the efficacy of antiviral phosphonoacids by prolonging their antiviral activity following administration.Type: GrantFiled: December 18, 1992Date of Patent: October 31, 1995Assignee: Vestar, Inc.Inventors: Karl Y. Hostetler, Raj Kumar
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Patent number: 5453525Abstract: Perhydro-5,5-8a-trimethyl-2-naphthalenone is prepared by acid cyclization of carboxylic esters of formula ##STR1## having a double bond in one of the positions indicated by the dotted lines and wherein symbol R designates a C.sub.1 -C.sub.6 alkyl radical, X stands for a monovalent radical of formula P(O)(OR.sup.1).sub.2 or C(O)R.sup.2, R.sup.1 represents a C.sub.1 -C.sub.6 alkyl group and R.sup.2 is either a linear or branched alkyl group or a substituted or unsubstituted phenyl radical, and wherein the wavy line represents a C--C bond of cis or trans configuration, or of formula ##STR2## wherein the wavy lines and symbol R are defined as above, and R.sup.0 represents a C.sub.3 -C.sub.6 alkyl radical, preferably branched, followed by basic decarboxylation of the obtained product.Type: GrantFiled: July 27, 1994Date of Patent: September 26, 1995Assignee: Firmenich SAInventors: Roger L. Snowden, Cyril Mahaim, Dana P. Simmons
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Patent number: 5352673Abstract: The present invention provides prodrugs that serve as useful therapeutics for various disease states and conditions mediated by underlying specific hydrolytic enzyme activity. The prodrugs hereof (additionally) impart a physiologically bioactive component thus providing prodrug compounds that are capable of imparting dual effect systemically.Type: GrantFiled: June 10, 1991Date of Patent: October 4, 1994Inventor: Edward A. Dennis
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Patent number: 5342978Abstract: Hydrolytically stabilized phosphite compositions are provided. The compositions contain an organic phosphite ester antioxidant and a hindered piperidinyl light stabilizer. The hindered piperidinyl component is not only a light stabilizer but also functions to hydrolitically stabilize the organic phosphite antioxidant. The compositions are useful as stabilizer additives to polymeric compositions.Type: GrantFiled: May 24, 1993Date of Patent: August 30, 1994Assignee: General Electric CompanyInventors: William P. Enlow, Leo L. Valdiserri
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Patent number: 5326690Abstract: Herein described is an ovarian cancer activating factor that has been isolated from ovarian cancer ascites fluid. The factor may be utilized in its isolated form in a screening program aimed at identifying inhibitors of factor-mediated ovarian cancer activation, or as a growth supplement useful for culturing ovarian and other cancer cell lines.Type: GrantFiled: October 1, 1993Date of Patent: July 5, 1994Assignee: Allelix Biopharmaceuticals Inc.Inventors: Yan Xu, Anne E. Goodbody
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Patent number: 5300255Abstract: A surfactant comprising a carboxylic acid ester or amide carrying a terminal strong acid group selected from carboxymethyl, sulphate, sulphonate, phosphate and phosphonate, suitable for stabilising dispersions of solids in organic liquids and oil/water emulsions, processes for the preparation of the surfactant and dispersions and emulsions containing the surfactant. A preferred species of the surfactant is a poly(hydroxyalkanecarboxylic acid) having the strong acid group attached, either directly or through a linking group, to a terminal hydroxy or carboxylic acid group.Type: GrantFiled: July 6, 1987Date of Patent: April 5, 1994Assignee: Imperial Chemical Industries, PLC.Inventors: Frederick Campbell, John D. Schofield, Alan S. Baker
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Patent number: 5273683Abstract: An emulsifier and method for its use in mixing grade emulsion systems of a chemical structure containing a tall oil and/or fatty acid portion, a hydrocarbon oxide portion, and a phosphate functionality. Variations in the components and the order of attachment compensate for variations in field conditions. The newly synthesized molecule may then be used to create mixing grade asphaltic emulsions.Type: GrantFiled: June 26, 1992Date of Patent: December 28, 1993Assignee: Asphalt Technology & Consulting, Inc.Inventor: Dennis Krivohlavek
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Patent number: 5227506Abstract: The invention relates to acyloxymethyl esters of bisphosphonic acids, halo-bisphosphonic acids and hydroxy-bisphosphonic acids which exhibit oral bioavailability and are useful in the treatment of disturbances involving calcium or phosphate metabolism, in particular, the treatment and prevention of diseases involving bone resorption, especially osteoporosis, Paget's disease, malignant hypercalcemia, and metastatic bone disease.Type: GrantFiled: July 12, 1990Date of Patent: July 13, 1993Assignee: Merck & Co., Inc.Inventors: Walfred S. Saari, Paul S. Anderson
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Patent number: 5221796Abstract: A glycerol derivative or a salt thereof is provided and the derivative is represented by the following general formula (I): ##STR1## wherein n is an integer ranging from 1 to 3; R.sup.1 represents a hydrogen atom or a group: --P(O)(OR.sup.2)(OR.sup.3) wherein R.sup.2 represents a hydrogen atom or a protective group for the phosphoric acid residue and R.sup.3 represents a hydrogen atom, a protective group for the phosphoric acid residue or a hydrophilic group; provided that the phosphoric acid residue represented by R.sup.1 may be in the form of a salt wih a proper counter ion; and, in respect of stereochemistry of asymmetric carbon atoms present in the molecule, the derivative or salt may be either an optically active isomer or a racemic isomer.These compounds are excellent in biological compatibility, dispersibility and chemical stability and that they can provide membranes having high flowability and high barrier properties as compared with conventional phospholipids.Type: GrantFiled: February 11, 1992Date of Patent: June 22, 1993Assignee: Fuji Photo Film Co., Ltd.Inventors: Hideto Mori, Naoyuki Nishikawa
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Patent number: 5220043Abstract: A method for making optically pure D-erythro-sphingomyelins which may be labeled for identification and testing purposes is provided.Type: GrantFiled: March 21, 1991Date of Patent: June 15, 1993Assignee: Ohio UniversityInventors: Zhengxin Dong, Jared A. Butcher, Jr.
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Patent number: 5208356Abstract: Substantially pure, non-toxic salts and esters of conjugated linoleic acid (CLA) are useful as antioxidants and as mold growth inhibitors. Methods of making the cis-9, trans-11 isomer of linoleic acid and the compounds are also disclosed.Type: GrantFiled: April 3, 1991Date of Patent: May 4, 1993Assignee: Wisconsin Alumni Research FoundationInventors: Michael W. Pariza, Yeong L. Ha
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Patent number: 5157140Abstract: New derivatives of cyclohexane in substantially pure form suitable as a pharmaceutical, foodstuff or as a stabilizer.Type: GrantFiled: December 29, 1989Date of Patent: October 20, 1992Assignee: Perstorp ABInventor: Matti Siren