Phosphorus Containing Patents (Class 536/117)
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Patent number: 5401647Abstract: Disclosed is a method of preparing limulus amoebocyte lysate substantially free from factor G which comprises bringing limulus amoebocyte lysate into contact with an insoluble carrier on which a (1.fwdarw.3)-.beta.-D-glucoside structural portion represented by the following formula [I] produced by depolymerizing and/or fractionating a carbohydrate chain is immobilized: ##STR1## wherein n represents an integer of 2 to 370.Type: GrantFiled: May 27, 1992Date of Patent: March 28, 1995Assignee: Seikagaku Kogyo Kabushiki Kaisha (Seikagaku Corporation)Inventors: Shigenori Tanaka, Jun Aketagawa, Yuko Shibata
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Patent number: 5393744Abstract: A compound having the following formula I: ##STR1## in which: R' represents a hydrogen atom or an azido group,alc represents an alkyl group of 1 to 4 carbon atoms, an alkoxy group of 1 to 4 carbon atoms or an amino group.Type: GrantFiled: January 29, 1990Date of Patent: February 28, 1995Assignee: Institut PasteurInventors: Tam Huynh Dinh, Catherine Gouyette, Bernadette Dupraz, Jean Igolen, Nathalie Savatier, Jean-Francois Nicolas, Francoise Barre-Sinoussi
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Patent number: 5384311Abstract: This invention relates to liquid sucralose concentrate compositions comprising sucralose, a preservative system, a buffering system and a liquid.Type: GrantFiled: August 18, 1992Date of Patent: January 24, 1995Assignee: McNeil-PPC, Inc.Inventors: Robert N. Antenucci, Richard L. Barndt, Kas Mohammed
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Patent number: 5371203Abstract: The invention relates to a process for the stereoselective preparation of .beta.-L-fucopyranosyl phosphates via the trichloroacetimidates of protected L-fucose and the synthesis and purification of very pure GDP-fucose from the .beta.-L-fucopyranosyl phosphates.Type: GrantFiled: January 31, 1992Date of Patent: December 6, 1994Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Richard R. Schmidt, Karl-Heinz Jung, Barbara Spahngehl, Willy Kinzy, Jurgen Hemberger
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Patent number: 5367068Abstract: The present invention relates to a method for treating, and in particular for abrading surfaces, utilizing glass-like polysaccharide grits. The invention also extends to novel glass-like polysaccharide products, especially starches, and to processes for the production thereof. Additionally, there is disclosed cross-linked polysaccharide materials and glass-like starches having a substantially occluded water component. Combinations of these various polysaccharide grits and other abrasive grit materials are also disclosed.Type: GrantFiled: November 25, 1992Date of Patent: November 22, 1994Assignee: ADM Agri-Industries, Ltd.Inventors: Christopher C. Lane, Ruben P. Lenz, Costa Athanassoulias
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Patent number: 5360903Abstract: The present invention relates to a method for treating, and in particular for abrading surfaces, utilizing glass-like polysaccharide grits. The invention also extends to novel glass-like polysaccharide products, especially starches, and to processes for the production thereof. Additionally, there is disclosed cross-linked polysaccharide materials and glass-like starches having a substantially occluded water component. Combinations of these various polysaccharide grits and other abrasive grit materials are also disclosed.Type: GrantFiled: November 25, 1992Date of Patent: November 1, 1994Assignee: ADM Agri-Industries, Ltd.Inventors: Christopher C. Lane, Ruben P. Lenz, Costa Athanassoulias
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Patent number: 5358936Abstract: A glucofuranose derivative substituted at the 3,5,6- or 3,6-positions with a radical that provides an anionic charge at physiological pH values is disclosed, as are pharmaceutical compositions, and methods of making and using the same. The compounds are useful in treating inflammation, and particularly conditions that involve neutrophil influx; they are also useful in inhibiting gastric ulcer formation.Type: GrantFiled: July 31, 1991Date of Patent: October 25, 1994Assignee: Paul GordonInventors: Paul Gordon, Edward P. Gamson
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Patent number: 5314811Abstract: A process for converting lipid-containing bacterial capsular polysaccharide, such as lipo-polyribosyl ribitol phosphate, lipo-PRP, into lipid-free, endotoxin-free polysaccharide, such as polyribosyl ribitol phosphate, PRP, by solubilizing polysaccharide-containing powder derived from culture media of bacteria, such as Haemophilus influenzae type b, cleaving covalently bound fatty acids from the polysaccharide, and removing the lipids, and endotoxin.Type: GrantFiled: July 13, 1992Date of Patent: May 24, 1994Assignee: Merck & Co., Inc.Inventors: Ann L. Lee, Mark S. Rienstra, Walter E. Manger, Robert D. Sitrin
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Patent number: 5288859Abstract: A process for stereospecific preparation of glycosyl azides by reacting a metal azide with a glycosyl phosphate triester having the phosphate group cis to the adjacent C-2 substituent is disclosed.Type: GrantFiled: January 22, 1991Date of Patent: February 22, 1994Assignee: E. I. Du Pont de Nemours and CompanyInventor: Subramaniam Sabesan
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Patent number: 5278300Abstract: 4,6-O-hydroxyphosphoryl-glucosamine derivatives as shown in the following formula [I] and their pharmaceutically-acceptable salts: ##STR1## wherein R.sub.1 and R.sub.2 represent a hydrogen atom or a hydroxy group; one of R.sub.3 and R.sub.4 represents --OCO(CH.sub.2).sub.n CH.sub.3, --CH.sub.2 (CH.sub.2).sub.n CH.sub.3, or --O--CH.sub.2 (CH.sub.2).sub.n CH.sub.3, and the other represents a hydrogen atom; l is an integer of 4-16; m is an integer of 4-16; and n is an integer of 6-18.Type: GrantFiled: December 12, 1991Date of Patent: January 11, 1994Assignees: Japan Tobacco, Inc., Akira HasegawaInventors: Akira Hasegawa, Shinichi Uesato, Tomio Ishida, Tomio Ishida
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Patent number: 5219843Abstract: The saccharides of formula I, ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 independently are optionally substituted acyl, are novel. They possess interesting pharmacological, especially immunostimulant, antiinflammatory and antitumor properties. They may be obtained by deprotection of a corresponding compound in protected form.Type: GrantFiled: November 22, 1991Date of Patent: June 15, 1993Assignee: Sandoz Ltd.Inventor: Ingolf Macher
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Patent number: 5191072Abstract: Lipid A monosaccharide analogues of the following general formula: ##STR1## wherein R.sub.1 is a hydrogen atom or a hydroxyl group, 1 is an integer of 8-14, m is an integer of 11-17 integer, and n is 8-14 integer.Type: GrantFiled: July 17, 1991Date of Patent: March 2, 1993Assignees: Japan Tobacco Inc., Akira HasegawaInventors: Akira Hasegawa, Makoto Kiso, Shinichi Uesato, Masanobu Suzuki, Tomio Ishida, Yutaka Saito
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Patent number: 5166139Abstract: Complexes of saponins from Centella asiatica, terminalia sp. and Terminalia sericea and relevant aglycons with phospholipids are described. The saponins may be asiaticoside, madecassicoside and sericoside. The molar ratio of phospholipids to saponins is from 0.5 to 2. The phospholipids are selected from the group consisting of soy lecithins, phospholipids from bovine or swine brain or cutis, phosphatidylcholine, phosphatidylserine, phosphatidylethanolamine in which the acyl groups can be the same or different and are mostly derived from palmitic, stearic, oleic, linoleic, linolenic acids. Pharmaceutical compositions and the method of treatment are also described.Type: GrantFiled: January 18, 1991Date of Patent: November 24, 1992Assignee: Indena, S.p.A.Inventors: Ezio Bombardelli, Gianfranco Patri, Roberto Pozzi
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Patent number: 5164375Abstract: A phospholipid having the formula ##STR1## is described. The compound has antifungal properties.Type: GrantFiled: September 27, 1991Date of Patent: November 17, 1992Assignee: Merck & Company, Inc.Inventors: Frank VanMiddlesworth, Kenneth E. Wilson, Otto D. Hensens, Deborah Zink, Maria B. Lopez
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Patent number: 5158941Abstract: This invention concerns the use of synthetic Lipid A analog P9132 to activate human monocytes, and inhibit growth of tumor cells.Type: GrantFiled: June 8, 1990Date of Patent: October 27, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventors: Prabhakar K. Jadhav, Mary E. Neville, Robert C. Newton, Subramaniam Sabesan
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Patent number: 5158939Abstract: A method is disclosed for stimulating the immune systems of animals with non-toxic lipid A derivatives. The derivatives include the lipopolysaccharide (LPS) and diphosphoryl lipid A (DPLA) for Rhodopsuedomonas.Type: GrantFiled: May 11, 1990Date of Patent: October 27, 1992Assignee: Wisconsin Alumni Research FoundationInventors: Kuni K. Takayama, Nilofer Qureshi
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Patent number: 5152928Abstract: Surfactant containing one or more of lysophospholipid represented by general formula; ##STR1## [wherein R.sup.1 and R.sup.2 represent hydrogen atom or the acyl residue of fatty acid, but either one of R.sup.1 and R.sup.2 is hydrogen atom, the other being acyl group. X represents an organic group remaining after removing one hydrogen atom of an optional hydroxyl group of polyhydric alcohol therefrom] and the method for producing the same are described.Type: GrantFiled: December 12, 1990Date of Patent: October 6, 1992Assignee: Kabushiki Kaisha Yakult HonshaInventors: Satoshi Kudo, Eriko Nishi
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Patent number: 5143831Abstract: A method for preparing optically pure N-containing sugars is disclosed wherein an optically impure chiral aldehyde acceptor is enzymatically condensed with dihydroxyacetone phosphate or dihydroxyacetone with a catalytic amount of inorganic arsenate in the presence of an aldolase to form an N-containing sugar.Type: GrantFiled: August 30, 1988Date of Patent: September 1, 1992Assignee: G. D. Searle & Co.Inventors: Chi-Huey Wong, John R. Durrwachter, Richard L. Pederson
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Patent number: 5137876Abstract: The compound having the formula: ##STR1## has antiviral activity, specifically in the prevention or treatment of infection by retroviruses, including HIV, and immunosuppressive activity, either as a compound, pharmaceutically acceptable salt, or a pharmaceutical composition ingredient, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of preventing or treating viral infections and modulating immune responses in vivo are also described.Type: GrantFiled: October 12, 1990Date of Patent: August 11, 1992Assignee: Merck & Co., Inc.Inventors: Malcolm MacCoss, Laura C. Meurer, Richard L. Tolman
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Patent number: 5134230Abstract: A disaccharide compound represented by formula (I): ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined in the specification and a salt thereof are disclosed. The compound exhibits excellent antitumor activity and low toxicity and is useful as an antitumor agent.Type: GrantFiled: January 18, 1991Date of Patent: July 28, 1992Assignee: Daiichi Pharmaceutical Co., Ltd.Inventors: Tsuneo Kusama, Tsunehiko Soga, Tetsuo Shiba
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Patent number: 5132416Abstract: Compounds of the formula (I) ##STR1## wherein R.sup.1 represents a pyranosyl radical and R.sup.4, R.sup.2, and R.sup.3 are as specified herein, compositions containing the compounds, methods of using the compounds to selectively kill tumor cells, and a process for the preparation of the compounds.Type: GrantFiled: August 20, 1990Date of Patent: July 21, 1992Assignee: Bayer AktiengesellschaftInventors: Lutz F. Tietze, Roland Fischer, Matthias Beller
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Patent number: 5118671Abstract: Complexes formed between aescin, cholesterol or .beta.-sitosterol and phospholipids are described. The molar ratio of phospholipids to aescin/.beta.-sitosterol or cholesterol is from 0.5 to 2. The phospholipids are selected from the group of soy or egg lecithins, phospholipids from bovine or swine brain or cutis, phosphatidylcholine, phospatidylserine, phosphatidylethanolamine in which the acyl groups may be the same or different and are mostly derived from palmitic, stearic, oleic, linoleic, linolenic acids, for instance, pharmaceutical compositions and a method for producing an anti-inflammatory effect in an animal are also described.Type: GrantFiled: December 19, 1990Date of Patent: June 2, 1992Assignee: Indena S.p.A.Inventors: Ezio Bombardelli, Gianfranco Patri, Roberto Pozzi
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Patent number: 5095104Abstract: A glucofuranose derivative substituted at the 3,5,6- or 3,6-positions with a radical that provides an anionic charge at physiological pH values is disclosed, as are pharmaceutical compositions, and methods of making and using the same. The compounds are useful in treating inflammation, and particularly conditions that involve neutrophil influx; they are also useful in inhibiting peptic ulcer formation.Type: GrantFiled: August 3, 1990Date of Patent: March 10, 1992Inventor: Paul Gordon
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Patent number: 5094947Abstract: A process for producing fructose-1,6-diphosphate comprising the steps of: (a) enzymatically converting adenosine 5'-diphosphate to adenosine 5'-triphosphate using an acetate kinase-containing microorganism or an extract of the microorganism and phosphate donor; and (b) enzymatically converting a substrate capable of being converted to glucose or fructose to fructose-1,6-diphosphate using the adenosine 5'-triphosphate resulting from step (a) and the acetate kinase-containing microorganism or the extract of the microorganism.Type: GrantFiled: September 9, 1991Date of Patent: March 10, 1992Assignee: Unitika, Ltd.Inventors: Hiroshi Nakajima, Masaaki Onda, Ryoichi Turutani, Hayato Ishihara
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Patent number: 5095123Abstract: Glycosyl phosphate triesters are prepared by reacting an anomeric mixture of a substituted hexopyranose with 4-N,N-dimethylaminopyridine and diphenyl chlorophosphate wherein using a specific order of addition determines the stereochemistry of the product.Type: GrantFiled: November 30, 1990Date of Patent: March 10, 1992Assignee: E. I. Du Pont de Nemours and CompanyInventor: Subramaniam Sabesan
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Patent number: 5066794Abstract: Disaccharide derivatives represented by the formula (I): ##STR1## wherein R.sup.1 CO-- and R.sup.2 CO-- each represents a residue of a straight chain fatty acid having from 8 to 20 carbon atoms and having a hydroxyl group at the 3-position thereof; R.sup.3 CO-- and R.sup.4 CO-- each represents a residue of a straight chain fatty acid having from 8 to 20 carbon atoms; and m and n each represents an integer of from 8 to 12, and the salts thereof. The compounds exhibit biological activities equal to or higher than those of natural lipid A. Also, the compounds of this invention are very useful as standard reagent for determination of endotoxin in the samples to be tested.Type: GrantFiled: January 29, 1990Date of Patent: November 19, 1991Assignee: Daiichi Pharmaceutical Co., Ltd.Inventor: Tetsuo Shiba
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Patent number: 5045593Abstract: Organophilic polymer adducts which are effective fluid loss control additives for oil base well-working fluids are prepared from an anionic or cationic water soluble polymer and one or more phosphatides. Preferred phosphatides are phosphoglycerides obtained from vegetable oils, most preferably commercial lecithin. Preferred polymers comprise polysaccharides or derivatives thereof and synthetic polymers.Type: GrantFiled: July 2, 1990Date of Patent: September 3, 1991Assignee: Venture Chemicals, Inc.Inventors: Jack C. Cowan, Roy F. House, Victor M. Granquist
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Patent number: 5043436Abstract: A substrate for measurement of .alpha.-amylase activity comprising a malto-oligo saccharide respresented by general formula (I) or (V) described below:A--Gn--B (I)A--Gn--I (V)wherein A represents: ##STR1## B represents a monosaccharide or a derivative thereof other than glucose; I represents inositol or a derivative thereof; G represents glucose; and n represents an integer of 3 to 15; in formula (II) or (III), R.sub.1 to R.sub.4 each represents a hydrogen atom, a lower alkyl group or (CH.sub.2)yCOOM (wherein y is 0, 1 or 2 and M represents a hydrogen atom or an alkali metal); and X.sub.1 to X.sub.4 each represents an oxygen atom or a sulfur atom.Type: GrantFiled: November 3, 1987Date of Patent: August 27, 1991Assignees: Kurita Water Ind., Ltd., Zensuke OgawaInventor: Zensuke Ogawa
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Patent number: 5041427Abstract: Compounds are disclosed which are useful in a method of treating animals to protect them from the toxic effects of Gram negative endotoxin. They include the diphosphoryl lipid A (DPLA) which can be obtained from R. sphaeroides ATCC 17023 grown at about 26.degree. C.Type: GrantFiled: January 19, 1990Date of Patent: August 20, 1991Assignee: Wisconsin Alumni Research FoundationInventors: Kuni K. Takayama, Nilofer Qureshi
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Patent number: 5039330Abstract: The invention concerns the use of fructose-1,6-diphosphate in botany for the formulations of compositions suited for the stimulation of the germination of dormant seeds and of the growth of stem tissues of growing plants.Type: GrantFiled: March 6, 1990Date of Patent: August 13, 1991Assignee: Biomedica Foscama Industria Chimico-Farmaceutica S.p.A.Inventors: Guillermo M. Bisso, Franco Gitti
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Patent number: 5039665Abstract: The invention relates to methods of treatment of patients with heat disorders using fructose-1,6-diphosphate.Type: GrantFiled: August 29, 1990Date of Patent: August 13, 1991Inventor: Angel K. Markov
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Patent number: 5034519Abstract: The invention relates to new oligosaccharides comprising the structure (D-ribose-D-ribitol-phosphate).sub.m, (D-ribitol-phosphate-D-ribose).sub.m or (phosphate-D-ribose-D-ribitol).sub.m, m being 2,3,4 . . . 19 or 20, to immunogens containing such oligosaccharide, to vaccines containing such immunogens and to methods for preparing such oligosaccharides, immunogens and vaccines. The vaccine is very suitable for treating infections caused by Haemophilus influenzae type b.Type: GrantFiled: December 29, 1987Date of Patent: July 23, 1991Assignee: De Staat Der NederlandenInventors: Eduard C. Beuvery, Adolf Evenberg, Jan T. Poolman, Jacobus H. van Boom, Peter Hoogerhout, Constant A. A. van Boeckel
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Patent number: 5026834Abstract: A modified cellulose has a structure represented by the formula ##STR1## Cell is the framework of the unmodified cellulose molecule or of the chitin molecule, in each case without hydroxyl groups. Z is a nitrogen or sulfur atom. In the case where Z is a nitrogen atom, T and Z together are an acylamide or urea group and Q is (X'-Y') and/or together with the O an ester group and/or together with the O a carbamate group. In the case where Z is a sulfur atom, T is omitted and Q together with the O is an ester group and/or together with the O a carbamate group and, as desired, (X'--Y'). The relationships 0<n<m and 0.ltoreq.s<m are obeyed and (n+s) indicates the mean degree of substitution. m=3 in the case of the unmodified cellulose molecule and m=2 in the case of the chitin molecule.Type: GrantFiled: December 9, 1988Date of Patent: June 25, 1991Assignee: Akzo N.V.Inventors: Michael Diamantoglou, Helmut Kuhne
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Patent number: 5013724Abstract: According to the process of the invention, a glycosaminoglycan is used in the form of a salt soluble in an organic medium and is subjected to the action of a given sulfation agent.Type: GrantFiled: July 11, 1986Date of Patent: May 7, 1991Assignee: Sanofi Societe AnonymeInventors: Maurice Petitou, Jean Choay
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Patent number: 5006647Abstract: A disaccharide compound represented by formula (I): ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, and R.sup.5 are as defined in the specification and a salt thereof are disclosed. The compound exhibits excellent antitumor activity and low toxicity and is useful as an antitumor agent.Type: GrantFiled: March 2, 1988Date of Patent: April 9, 1991Assignee: Daiichi Seiyaku Co., Ltd.Inventors: Tsuneo Kusama, Tsunehiko Soga, Tetsuo Shiba
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Patent number: 5001114Abstract: New alkyl mono and polyglycoside phosphate esters and anionic derivatives thereof are described which compounds have the general formulaRO(G).sub.x Z.sub.ywhereinG is a glycosyl moiety which is selected from the group consisting of fructose, glucose, mannose, galactose, talose, gulose, allose, altrose, idose, arabinose, xylose, lyxose, ribose or mixtures thereof,R is an aliphatic or aromatic hydrocarbon group substituted on the glycosyl moiety which aliphatic or aromatic group is a straight chain or is branched, or is cyclic, saturated or unsaturated and has 6 to 30 carbon atoms;x=1 to 10;y=1 to 3.times.+1;at least one of the hydroxyl groups at the hydroxyl position of at least one of the glycosyl moieties is substituted with Z which is ##STR1## wherein A=R.sub.1, H.sup.+ or (G).sub.x ORB=R.sub.2, M.sup.+ or (G).sub.x ORexcept that when B--R.sub.2 or (G).sub.x OR, A.noteq.H, when A or B=(G).sub.x OR, Z substitutes one of the hydroxyl groups of the glycosyl moieties of A or B, and R.sub.1 and R.sub.Type: GrantFiled: October 27, 1989Date of Patent: March 19, 1991Assignee: Henkel Kommanditgesellschaft auf AktienInventor: Robert S. McDaniel, Jr.
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Patent number: 4987237Abstract: Novel derivatives of monophosphoryl lipid A and a process for their preparation are provided. The derivatives contain one or more free groups, such as an amine, on a side chain attached to the primary hydroxyl groups of the monophosphoryl lipid A nucleus through an ester group. The derivatives provide a convenient method for coupling the lipid A through coupling agents to various biologically active materials, substrates, and the like, wherein the immunostimulant properties of lipid A are desired.Type: GrantFiled: October 22, 1987Date of Patent: January 22, 1991Assignee: Ribi ImmunoChem Research, Inc.Inventors: Kent R. Myers, Edgar F. Ribi, deceased
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Patent number: 4983582Abstract: A preventive and therapeutic method for hypertension by dosing hexose phosphate calcium which produces an immediate effect without having any undesirable side-effects to control a rise in the blood pressure, and is efficacious also for various diseases of which onset can be ascribed to hypertension, such as myocardial infarction, cerebral apoplexy, cirrhosis of livers, billiary stasis, and others.Type: GrantFiled: February 12, 1988Date of Patent: January 8, 1991Assignee: Kao CorporationInventors: Masakazu Murata, Yoshinao Nagashima, Kenji Hara, Shigeto Kayane, Takashi Imamura
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Patent number: 4968790Abstract: Phosphates are disclosed which stimulate the enzyme fructose-1,6-bisphosphatase and inhibit the enzyme 6-phosphofructo-1-kinase, thereby lowering glucose levels in mammals. These phosphates may thus be used to treat hyperglycemia and/or diabetes. Processes for the synthesis of the phosphates are also disclosed.Type: GrantFiled: October 28, 1988Date of Patent: November 6, 1990Assignee: American Cyanamid CompanyInventors: Vern G. DeVries, Thomas H. Claus, Middleton B. Floyd, Jr., Semiramis Ayral-Kaloustian
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Patent number: 4948883Abstract: Bismuth salts of phosphorylated and/or sulfonated saccharides are prepared from a corresponding metal salt reactant, a water soluble organic acid, and a bismuth substance. For example, a complex salt of bismuth hydroxide sucrose octasulfate can be prepared in high yield and good purity from potassium sucrose octasulfate, trichloroacetic acid, trifluoracetic acid or 4-methylbenzenesulfonic acid, and bismuth hydroxide. Corresponding hydrogen phosphorylated and/or sulfonated saccharides may be intermediate products.Type: GrantFiled: October 31, 1989Date of Patent: August 14, 1990Assignee: Marion Laboratories, Inc.Inventor: Steven R. Duff
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Patent number: 4945158Abstract: Phosphonates are disclosed which stimulate the enzyme fructose-1,6-bisphosphatase and inhibit the enzyme 6-phosphofructo-1-kinase, thereby lowering glucose levels in mammals. These phosphonates may thus be used to treat hyperglycemia and/or diabetes. Processes for the synthesis of the phosphonates are also disclosed.Type: GrantFiled: August 12, 1988Date of Patent: July 31, 1990Assignee: American Cyanamid CompanyInventors: Vern G. DeVries, Thomas H. Claus, Middleton B. Floyd, Jr., Semiramis Ayral-Kaloustian
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Patent number: 4943629Abstract: Alpha-substituted phosphonates are disclosed which stimulate the enzyme fructose-1,6-bisphosphatase and inhibit the enzyme 6-phosphofructo-1-kinase, thereby lowering glucose levels in mammals. These alpha-substituted phosphonates may thus be used to treat hyperglycemia and/or diabetes. Processes for the synthesis of the alpha-substituted phosphonates are also disclosed.Type: GrantFiled: August 12, 1988Date of Patent: July 24, 1990Assignee: American Cyanamid CompanyInventors: Vern G. DeVries, Thomas H. Claus, Middleton B. Floyd, Jr., Semiramis Ayral-Kaloustian
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Patent number: 4940786Abstract: Bismuth salts of phosphorylated and/or sulfonated saccharides can be prepared in one reaction vessel from a corresponding metal salt reactant, a water soluble organic acid, and a bismuth substance. For example, a complex salt of bismuth hydroxide sucrose octasulfate can be prepared in high yield and good purity from potassium sucrose octasulfate, trifluoracetic acid, and bismuth hydroxide.Type: GrantFiled: October 31, 1989Date of Patent: July 10, 1990Assignee: Marion Laboratories, Inc.Inventor: Steven R. Duff
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Patent number: 4935406Abstract: Bismuth (phosph/sulf)ated saccharides are useful in ameliorating gastrointestinal disorders associated with Campylobacter-like organisms such as, for example, Campylobacter pylori. For example, compositions containing a complex salt of bismuth hydroxide sucrose octasulfate can be thus employed to treat Type B gastritis.Type: GrantFiled: September 20, 1988Date of Patent: June 19, 1990Assignee: Marion Laboratories, Inc.Inventors: James C. Coleman, Douglas L. Cole
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Patent number: 4918175Abstract: The titled compositions are useful as pharmaceuticals in ameliorating disorders associated with gastric mucosal damage. For example, compositions containing a complex salt of bismuth hydroxide sucrose octasulfate can be thus employed.Type: GrantFiled: June 21, 1988Date of Patent: April 17, 1990Assignee: Marion Laboratories, Inc.Inventors: S. Marc Bowen, Richard S. Bodine, James C. Coleman
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Patent number: 4916220Abstract: A pharmaceutical preparation containing a carrier with palmitoyl-fructose-1,6- diphosphate as the active drug, for use in the therapy of hypophosphatemias, of cardiopathies, and of alcoholism and relevant methods for producing said preparation.Type: GrantFiled: April 18, 1989Date of Patent: April 10, 1990Assignee: Biomedica Foscama Industria Chimico-FarmaceuticaInventors: Lauro Galzigna, Franco Gritti
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Patent number: 4916217Abstract: Etoposide-3',4'-quinone is converted into a phosphorane or phosphate ester by reaction with an organic phosphine or phosphite. The resulting phosphoranes and phosphates have anti-tumor activity in animals.Type: GrantFiled: January 8, 1987Date of Patent: April 10, 1990Assignee: Bristol-Myers CompanyInventor: Mark G. Saulnier
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Patent number: 4914197Abstract: Novel phosphoric diesters of general formula: ##STR1## wherein R.sub.1 and R.sub.2 are the same or different and each means a methyl group or a hydrogen atom, provided that at least one of R.sub.1 and R.sub.2 is a hydrogen atom, or a salt thereof which can be produced by reacting .beta., .gamma. or .delta.-tocopherol with a halophosphorylating agent such as phosphorus oxychloride, reacting the resultant product with ascorbic acid whereof hydroxyl groups at 5- and 6-positions are protected, and then removing protected groups from the hydroxyl groups. The phosphoric diester has antiinflammatory activity.Type: GrantFiled: March 4, 1987Date of Patent: April 3, 1990Assignee: Senju Pharmaceutical Co., Ltd.Inventors: Itaru Yamamoto, Kazumi Ogata
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Patent number: 4912094Abstract: Modified lipopolysaccharides, particularly de-3-0-acylated monophosphoryl lipid A and de-3-0-acylated diphosphoryl lipid A, are provided by an alkaline hydrolysis under controlled conditions which removes only the .beta.-hydroxymyristic acyl residue that is ester-linked to the reducing-end glucosamine at position 3. The modified products are less endotoxic and maintain their antigenic and immuno-stimulating properties.Type: GrantFiled: June 29, 1988Date of Patent: March 27, 1990Assignee: Ribi ImmunoChem Research, Inc.Inventors: Kent R. Myers, Alex T. Truchot
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Patent number: 4904768Abstract: Phosphate derivatives of 4'-demethylepipodophyllotoxin glucosides are novel antitumor agents and the salts thereof offer the pharmaceutical advantage of high water solubility.Type: GrantFiled: May 27, 1988Date of Patent: February 27, 1990Assignee: Bristol-Myers CompanyInventors: Mark G. Saulnier, Peter D. Senter, John F. Kadow