Plural Phosphori Attached Indirectly To Each Other By Nonionic Bonding Patents (Class 562/20)
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Patent number: 6600068Abstract: The invention relates to a process for preparing ethanebis(methylphosphinic) acid which comprises reacting ethyne (acetylene) with methyl phophonous acid. The invention further relates to the use of the ethanebis(methylphosphinic) acid prepared by this process for preparing flame retardants or preparing other phosphorus-containing products.Type: GrantFiled: December 19, 2001Date of Patent: July 29, 2003Assignee: Clariant GmbHInventors: Martin Sicken, Hans-Peter Schmitz
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Patent number: 6593376Abstract: A process for preparing amphiphilic compounds having at least two hydrophilic and at least two hydrophobic groups by reacting an olefinic substrate having at least two double bonds with an organic hydroperoxide to form an oxirane ring, opening, the oxirane ring with an alcohol in the presence of a catalyst system comprising a molybdenum compound as a first catalyst component and a second catalyst component selected from the group consisting of boron trifluoride, alumina, 1,8-diazzabicyclo-(5.4.0)-undec-7-ene, 1,4-diazabicyclo-(2,2,2)-octane.Type: GrantFiled: December 30, 1999Date of Patent: July 15, 2003Assignee: SASOL Germany GmbHInventors: Mark Rüsch gen. Klaas, Klaus Kwetkat, Siegfried Warwel
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Patent number: 6583315Abstract: The invention relates to a process for preparing ethanebis(alkylphosphinic) acids by a) reacting elemental yellow phosphorus with alkyl halides in the presence of alkali metal hydroxide or of alkaline earth metal hydroxide to give a mixture whose main constituents are the alkali metal salts and/or alkaline earth metal salts of alkylphosphonous, phosphorous, and hypophosphorous acid, b) liberating alkylphosphonous, phosphorous, and hypophosphorous acid by adding mineral acids, and also at the same time precipitating the alkali metal ions and, respectively, alkaline earth metal ions in the form of their salt of the mineral acids, and then c) esterifying the alkylphosphonous acid from the mixture of the alkylphosphonous, phosphorous, and hypophosphorous acid, d) isolating the ester of alkylphosphonous acid from the mixture and hydrolyzing the same to give alkylphosphonous acid, and e) preparing, from the alkylphosphonous acid, the corresponding ethanebis(alkylphosphinic) acid of the general formula (I) wherType: GrantFiled: December 19, 2001Date of Patent: June 24, 2003Assignee: Clariant GmbHInventors: Martin Sicken, Norbert Weferling, Hans-Peter Schmitz
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Publication number: 20030073865Abstract: The invention relates to a process for preparing ethanebis(alkylphosphinic) acids byType: ApplicationFiled: December 19, 2001Publication date: April 17, 2003Applicant: Clariant GmbHInventors: Martin Sicken, Norbert Weferling, Hans-Peter Schmitz
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Patent number: 6504049Abstract: A process for synthesizing pharmaceutically active disulfides, particularly Dimesna and certain derivatives thereof. The process includes reacting an alkylene salt with a sulfurating reagent, then alkalizing the intermediate and flowing oxygen through the mixture to produce the final compound in high yield.Type: GrantFiled: April 30, 2002Date of Patent: January 7, 2003Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Harry Kochat
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Patent number: 6465444Abstract: The invention encompasses the novel class of compounds represented by the formula below, which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases, including diabetes.Type: GrantFiled: March 21, 2001Date of Patent: October 15, 2002Assignees: Merck Frosst Canada & Co., Banyu Pharmaceutical Co., Ltd.Inventors: Christopher Bayly, Mitsuru Ohkubo
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Patent number: 6444701Abstract: Compounds of formula (I) wherein the groups are as defined in the description are disclosed. The compounds of formula (I) are endowed with reversible inhibiting activity of carnitine palmitoyl-transferase and are useful in the preparation of medicaments useful in the pathologies related to a hyperactivity of carnitine palmitoyl-transferase, such as hyperglycemia, diabetes and pathologies related thereto, heart failure, ischemia.Type: GrantFiled: November 8, 2001Date of Patent: September 3, 2002Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Fabio Giannessi, Mauro Marzi, Patrizia Minetti, Francesco De Angelis, Maria Ornella Tinti, Piero Chiodi, Arduino Arduini
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Patent number: 6414185Abstract: Aluminum salts of phosphinic acid or diphosphinic acids having alkyl and/or aryl substitutes, obtainable by heating an ester of the corresponding phosphinic acids or diphosphinic acids with aluminum hydroxide at a temperature of more than 150° C. under pressure in the presence of water, are distinguished by a particular crystal structure and are suitable as flameproofing agents for plastics.Type: GrantFiled: April 2, 2001Date of Patent: July 2, 2002Assignee: Ticona GmbHInventor: Hans-Jerg Kleiner
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Publication number: 20020082447Abstract: The invention relates to a process for preparing ethylenediphosphonic acids of the formula I, 1Type: ApplicationFiled: December 19, 2001Publication date: June 27, 2002Applicant: Clariant GmbHInventors: Martin Sicken, Hans-Peter Schmitz
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Publication number: 20020052347Abstract: The invention encompasses the novel class of compounds represented by formula I, which are inhibitors of the PTP-1B enzyme.Type: ApplicationFiled: December 21, 2000Publication date: May 2, 2002Inventors: Yves Leblanc, Claude Dufresne, Jacques Yves Gauthier, Robert Young
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Patent number: 6380439Abstract: A single-stage method for producing &agr;-hydroxy ethers by oxidizing olefinic substrates with organic hydroperoxides and opening the resultant oxirane ring by means of monovalent or polyvalent alcohols wherein a molybdenum compound in combination with a compound selected from the group consisting of boron trifluoride, aluminum oxides, 1,8-diazabicyclo-[5.4.0]-undec-7-ene or 1,4-diazabicyclo-[2.2.2]-octane, and mixtures thereof is used as a catalyst system.Type: GrantFiled: January 25, 2000Date of Patent: April 30, 2002Assignee: RWE-DEA Aktiengesellschaft fur Mineraloel und ChemieInventors: Mark Rüsch gen. Klaas, Siegfried Warwel, Hans-Martin Zillmann, Klaus Kwetkat
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Patent number: 6355833Abstract: A catalyst comprising at least one nickel(O) complex which comprises at least one mono-, bi- or multidentate phosphonite ligand of the formula I or salts and mixtures thereof, is prepared as described, and the catalysts are used to prepare mixtures of monoolefinic C5 mononitriles with nonconjugated C═C and C≡N bonds by catalytic hydrocyanation of butadiene or of a 1,3-butadiene-containing hydrocarbon mixture in the presence of a catalyst of this type.Type: GrantFiled: February 14, 2001Date of Patent: March 12, 2002Assignee: BASF AktiengesellschaftInventors: Jakob Fischer, Wolfgang Siegel
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Patent number: 6316396Abstract: The invention relates to amphiphilic compounds of the general formula (I) with at least two hydrophilic and at least two hydrophobic groups based on di, oligo or polyolethers. The amphiphilic compounds of this invention are highly surface active and are suitable as emulsifiers, demulsifiers, detergents, dispersants and hydrotropes for industrial and domestic purposes, e.g. in the fields of metalworking, ore separation, surface treatment, washing and cleaning, cosmetics, medicine and food processing and preparation.Type: GrantFiled: April 9, 1999Date of Patent: November 13, 2001Assignee: RWE-DEA Aktiengesellschaft fuer Mineraloel und ChemieInventors: Klaus Kwetkat, Wolfgang Schröder
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Patent number: 6307098Abstract: This invention relates to water soluble phosphines of the following structural formula and method of preparing these phosphines: Wherein A is a moiety which is stable to the reaction conditions and does not interfere with solubility of the compound in the preparation reaction. R1 and R2 are selected from hydroxyl groups, dialkylamino group, and alkoxide groups.Type: GrantFiled: June 9, 2000Date of Patent: October 23, 2001Assignee: The United States of America as represented by the Secretary of the NavyInventors: Terrence L. Schull, Walter J. Dressick
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Patent number: 6245754Abstract: The present invention relates to the preparation and biological activity of 3-deoxy-D-myo-inositol ether lipid analogs as inhibitors of phosphatidylinositol-3-kinase signaling and cancer cell growth. The compounds of the present invention are useful as anti-tumor agents which effectively inhibit the growth of mammalian cells.Type: GrantFiled: June 25, 1999Date of Patent: June 12, 2001Inventors: Alan P. Kozikowski, Lixin Qioa, Garth Powis
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Patent number: 6211402Abstract: Aluminum salts of phosphinic acid or diphosphinic acids having alkyl and/or aryl substitutes, obtainable by heating an ester of the corresponding phosphinic acids or diphosphinic acids with aluminum hydroxide at a temperature of more than 150° C. under pressure in the presence of water, are distinguished by a particular crystal structure and are suitable as flameproofing agents for plastics.Type: GrantFiled: February 16, 1999Date of Patent: April 3, 2001Assignee: Ticona GmbHInventor: Hans-Jerg Kleiner
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Patent number: 6174874Abstract: The invention encompasses the novel class of compounds represented by formula I which are inhibitors of the PTP-1B enzyme. The invention also encompasses pharmaceutical compositions and methods of treating or preventing PTP-1B mediated diseases.Type: GrantFiled: September 17, 1999Date of Patent: January 16, 2001Assignee: Merck Frosst Canada & Co.Inventors: Zhaoyin Wang, Claude Dufresne, Yves Leblanc, Chun Sing Li, Jacques Y. Gauthier, Cheuk K. Lau, Michel Therien, Patrick Roy
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Patent number: 6172131Abstract: Hydrolysis-stable and polymerizable acrylphosphonic acids are described which are particularly suitable as a component of dental adhesives owing to their adhesion-promoting properties.Type: GrantFiled: October 9, 1998Date of Patent: January 9, 2001Assignee: Ivoclar AGInventors: Norbert Moszner, Frank Zeuner, Volker Rheinberger
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Patent number: 6160167Abstract: This invention relates to novel compositions of matter which either terminate in a sulfhydryl moiety or are disulfides. The compounds also include a terminal sulfonate or phosphonate moiety, and have many uses, such as toxicity reducing agents when administered with many antineoplastic agents.Type: GrantFiled: September 1, 1998Date of Patent: December 12, 2000Assignee: BioNumerik Pharmaceuticals, Inc.Inventors: Frederick H. Hausheer, Kochat Haridas, Qiuli Huang
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Patent number: 6160166Abstract: Phosphonic acid agents are synthesized and characterized which are potent inhibitors of angiogenesis, tumorigenesis and metalloproteinase activity. Their method of use for the inhibition of angiogenesis and metalloproteinase and the treatment of tumors is also shown.Type: GrantFiled: July 21, 1999Date of Patent: December 12, 2000Assignee: The University of Kentucky Research FoundationInventors: Delwood C. Collins, Antonio R. Gagliardi, Peter Nickel
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Patent number: 6121253Abstract: This invention relates to prostaglandin-bisphosphonate conjugates. These conjugates are effective for treating or preventing bone diseases such as osteoporosis. These conjugates simultaneously deliver a prostaglandin agent for increasing bone formation and a bisphosphonate agent for inhibiting bone resorption.Type: GrantFiled: November 15, 1999Date of Patent: September 19, 2000Assignee: Merck Frosst Canada & Co.Inventors: Yongxin Han, Robert N. Young, Laurent Gil, Rejean Ruel
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Patent number: 6090345Abstract: The present invention relates to phosphorus-containing compounds based on 1-hydroxypropane-1,3-diphosphonic acid and to the acid itself of general formula (I) ##STR1## in which M.sup.1, M.sup.2, M.sup.3, M.sup.4 and M.sup.5, independently of one another, each denote a radical from the series hydrogen, alkali metal, an equivalent of ammonium, alkyl- or hydroxyalkyl-substituted ammonium,a process for the preparation thereof, novel intermediates and the use thereof as a corrosion inhibitor, scale inhibitor and as a flame retardant.Type: GrantFiled: January 29, 1999Date of Patent: July 18, 2000Assignee: Bayer AGInventors: Christoph Holzner, Armin Spaniol, Hans Dahmen
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Patent number: 5977404Abstract: The invention relates to amphiphilic compounds of the general formula (I) with at least two hydrophilic and at least two hydrophobic groups based on di, oligo or polyolethers. The amphiphilic compounds of this invention are highly surface active and are suitable as emulsifiers, demulsifiers, detergents, dispersants and hydrotropes for industrial and domestic purposes, e.g. in the fields of metalworking, ore separation, surface treatment, washing and cleaning, cosmetics, medicine and food processing and preparation.Type: GrantFiled: June 26, 1997Date of Patent: November 2, 1999Assignee: Huels AktiengesellschaftInventors: Klaus Kwetkat, Wolfgang Schroder
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Patent number: 5922902Abstract: A process for synthesizing disulfides and sulfhydryl compounds which are useful pharmaceuticals. The process includes a two step, single pot process for preparing disulfides from an alkenyl sulfonate salt. The disulfides are useful as toxicity mitigating agents of chemotherapeutic drugs, such as certain platinum complexes, and as use therapeutic drugs for a variety of conditions in mammals.The two step process involves first the conversion of the starting reagent to a mercaptane sulfonate, then an oxidation to the desired disulfide.Type: GrantFiled: June 30, 1998Date of Patent: July 13, 1999Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Kochat Haridas
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Patent number: 5847200Abstract: New diphosphines in the form of ammonium carboxylates, sulfonates or phosphonates having a singly or multiply charged diphosphine anion and the corresponding number of ammonium cations as counter ions, and a process for their preparation useful as ligand in rhodium catalyst systems for hydroformylation of olefins.Type: GrantFiled: April 17, 1997Date of Patent: December 8, 1998Assignee: Hoechst AktiengesellschaftInventors: Helmut Bahrmann, Peter Lappe, Thomas Muller
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Patent number: 5811575Abstract: The present invention relates to a process for preparing vinylphosphonic acids of the formula ##STR1## in which m is an integer from 1 to 20 by heating 2-chloroethylphosphonic acids of the formula ##STR2## in which n is an integer equal to or smaller than m, if desired in the form of a solution, in the absence or presence of a catalyst to a temperature of 180 to 350.degree. C. and eliminating hydrogen chloride and, where appropriate, water under atmospheric pressure or reduced pressure and, if desired, hydrolysing the vinylphosphonic acids of the formula (I).Type: GrantFiled: May 16, 1997Date of Patent: September 22, 1998Assignee: Clariant GmbHInventors: Hans-Jerg Kleiner, Gunter Roscher
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Patent number: 5808140Abstract: A process for synthesizing disulfides and sulfhydryl compounds which are useful pharmaceuticals. The process includes a two step, single pot process for preparing disulfides from an alkenyl sulfonate salt. The disulfides are useful as toxicity mitigating agents of chemotherapeutic drugs, such as certain platinum complexes, and as use therapeutic drugs for a variety of conditions in mammals.The two step process involves first the conversion of the starting reagent to a mercaptane sulfonate, then an oxidation to the desired disulfide.Type: GrantFiled: September 24, 1997Date of Patent: September 15, 1998Assignee: BioNumerik Pharmaceuticals, Inc.Inventor: Kochat Haridas
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Patent number: 5801263Abstract: Tertiary phosphines of the formula (I) ##STR1## in which X is a phosphinate or phosphonate group, are prepared by a palladium-catalyzed coupling of p-, m- or o-bromofluorobenzenes with alkyl akylphosphonous acid ester or alkyl alkylphosphite ester and reacting the resulting alkyl fluorophenylphosphinates or alkyl fluorophenylphosphonates with a metal phosphide.Type: GrantFiled: May 15, 1997Date of Patent: September 1, 1998Assignee: Hoechst AktiengesellschaftInventors: Thomas Seitz, Steffen Haber, Hans-Jerg Kleiner
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Patent number: 5783728Abstract: An improved method is disclosed for the preparation of novel alkali metal diphosphinate salts by the reaction of an acetylenic compound with an alkali metal hypophosphite in the presence of a free radical source, the use of these novel compounds in further reactions to prepare diphosphonate compounds and diphosphinate containing adducts, oligomers and polymers and utilization of these compounds, polymers and oligomers to control calcium carbonate scale and mild steel corrosion in cooling water.Type: GrantFiled: January 7, 1997Date of Patent: July 21, 1998Assignee: Nalco Chemical CompanyInventors: James F. Kneller, Donald A. Johnson, Vytas Narutis, Binaifer S. Khambatta
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Patent number: 5698541Abstract: The invention concerns compounds of the general formula I ##STR1## in which R denotes a lower alkyl which can be substituted if desired by hydroxy, alkoxy, amino, dialkylamino, alkylmercapto, alkylsulfinyl, alkanesulfonyl, cycloalkyl, aryl or a heterocyclic ring, or it denotes lower alkenyl, cycloalkyl, cycloalkenyl, aryl or a heterocyclic ring andR.sub.1 and R.sub.2 can be, independently of one another, hydrogen, lower alkyl, cycloalkyl, aryl or arylmethyl,their optically active salts as well as their pharmacologically acceptable salts, processes for their production as well as pharmaceutical agents which contain these compounds for treating diseases of calcium metabolism. Moreover the invention concerns compounds of formula II as intermediate products for the production of compounds of formula I.Type: GrantFiled: September 25, 1996Date of Patent: December 16, 1997Assignee: Boehringer Mannheim GmbHInventors: Gerd Zimmermann, Angelika Esswein, Christos Tsaklakidis, Frieder Bauss
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Patent number: 5574025Abstract: The compounds disclosed inhibit the prenylation of several proteins. These compounds are potent inhibitors of famesyl-protein transferase and geranylgeranyl-protein transferase. Further contained in this invention are chemotherapeutic compositions containing these prenyl-transferase inhibitors and methods for their production.Type: GrantFiled: October 26, 1994Date of Patent: November 12, 1996Assignee: Merck & Co., Inc.Inventors: Neville J. Anthony, Robert P. Gomez, Charles A. Omer
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Patent number: 5519102Abstract: A method of preparing poly(isopropenylphosphonic acid) is disclosed, which provides a high yield with low initiator charge. The method comprises preparing poly(isopropenylphosphonic acid) by polymerizing a mixture of isopropenylphosphonic acid and isopropenylphosphonic acid anhydride, preferably in an aqueous solution.Type: GrantFiled: May 9, 1995Date of Patent: May 21, 1996Assignee: Betz Laboratories, Inc.Inventors: Michael A. Cady, William S. Carey, Andrew Solov
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Patent number: 5405598Abstract: Compounds of formula I and II ##STR1## in which B contains a carboranyl group and one of R.sub.3 and R.sub.4 is a carboranyl group or a boronic acid or ester are useful sensitizing agents for boron neutron capture therapy.Type: GrantFiled: February 24, 1992Date of Patent: April 11, 1995Inventors: Raymond F. Schinazi, Dennis C. Liotta
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Patent number: 5405601Abstract: The present invention provides new and structurally diverse compositions for diagnostic imaging comprising compounds of the general formula: ##STR1## wherein A is N or CR.sub.1, R.sub.1 is hydrogen, C.sub.1 -C.sub.8 alkyl, or C.sub.6 -C.sub.10 aryl, where the alkyl or aryl group may be optionally substituted with one or more hydroxy, C.sub.1 -C.sub.8 alkyl, C.sub.1 -C.sub.8 hydroxyalkyl, C.sub.1 -C.sub.8 alkoxy, C.sub.6 -C.sub.10 aryl, C.sub.6 -C.sub.10 hydroxyaryl, C.sub.6 -C.sub.10 aryloxy, --CO.sub.2 R.sub.2, --CONR.sub.3 R.sub.4, or NR.sub.3 R.sub.4 ; D is O, --O(CH.sub.2).sub.2 O--, --O(CH.sub.2).sub.3 O--, or NR.sub.5 ; E is O, --O(CH.sub.2).sub.2 O--, --O(CH.sub.2).sub.3 O-- or NR.sub.6 ; F is O, --O(CH.sub.2).sub.2 O--, --O(CH.sub.2).sub.3 O-- or NR.sub.7 ; R.sub.2 -R.sub.7 are as defined within; g, h, i, j, k and m may be the same or different and are an integer from one to about six; X is --CO.sub.2 H, --PO.sub.3 H.sub.2, --SO.sub.3 H or --CONHOH.Type: GrantFiled: July 2, 1993Date of Patent: April 11, 1995Assignee: Mallinckrodt Medical Inc.Inventors: T. Jeffrey Dunn, Dennis A. Moore, Muthanadar Periasamy, Milorad M. Rogic, Rebecca A. Wallace, David H. White, Steven R. Woulfe
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Patent number: 5386038Abstract: Unsaturated compounds which can be dissolved in aqueous based solvents, such as ethylenic or acetylenic carboxylate or alcohols with less than 10 carbon atoms, especially maleic and/or acrylic acid or propargyl alcohol, are reacted with alkali metal phosphite in aqueous solution at neutral or alkaline pH in the presence of free radical initiators such as persulphate to form threshold scale and corrosion inhibitors.Type: GrantFiled: September 17, 1992Date of Patent: January 31, 1995Assignee: Albright & Wilson LimitedInventors: Keith P. Davis, Peter A. T. Hoye, Michael J. Williams, Gary Woodward, Martin P. Greenhall
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Patent number: 5338731Abstract: Bisphosphonate compounds are of the Formula (I): ##STR1## wherein Y is .dbd.O or .dbd.N--OH and n is from 3 to 24, and further wherein when Y is .dbd.O, (i) R.sub.1 is hydrogen and R.sub.2 is sodium, or (ii) R.sub.1 is sodium and R.sub.2 is methyl, and when Y is .dbd.N--OH, R.sub.1 is sodium and R.sub.2 is methyl.Type: GrantFiled: March 8, 1993Date of Patent: August 16, 1994Assignee: Yissum, Research Development Company of the Hebrew University of JerusalemInventors: Eli Breuer, Gershon Golomb
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Patent number: 5324843Abstract: 3-(3,4,5,6-tetrahydrophthalimido)cinnamic esters I ##STR1## (R.sup.1 =H, halogen; R.sup.2, R.sup.3 =halogen; R.sup.4 =C-organic radical, R.sup.5 =H, CH.sub.3) are prepared by reducing 3-nitrocinnamic esters II ##STR2## with hydrogen in the presence of a catalyst and condensing the resulting 3-aminocinnamic esters III ##STR3## with a 3,4,5,6-tetrahydrophthalic anhydride IV ##STR4## and are valuable active ingredients in crop protection.Type: GrantFiled: April 29, 1993Date of Patent: June 28, 1994Assignee: BASF AktiengesellschaftInventors: Lothar Rueb, Karl Eicken, Bernd Schaefer, Gernot Reissenweber, Peter Schaefer
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Patent number: 5312954Abstract: Novel bisphosphonates comprise compounds of the formula (I) ##STR1## wherein m and l are independently 1 or 2; R.sub.1 represents hydrogen, a lower alkyl group, or an alkali metal cation; R.sub.2 represents hydrogen, a lower alkyl group or an alkali metal cation; Y represents .dbd.0 or .dbd.N--OH, or --OH and X represents --(CH.sub.2).sub.n --, a branched alkylene group, or a branched or straight alkenylene or alkynylene chain optionally substituted by one or more oxygen or nitrogen atoms, wherein n is an integer from 3 to 24. Further definitions of X are included in the description.Type: GrantFiled: May 13, 1992Date of Patent: May 17, 1994Assignee: Yissum, Research Development Company of the Hebrew University of JerusalemInventors: Eli Breuer, Gershon Golomb
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Patent number: 5266722Abstract: Polyether bis-phosphonic acid compounds are disclosed which have the formula (HO).sub.2 OP--R--(OR').sub.n --OR--PO(OH).sub.2 where R is selected from the group consisting of methylene and ethylene, R' is selected from the group consisting of ethylene and ethylene substituted with one or more methyl groups, and n is an integer from 1 to 4, water soluble salts thereof, and esters thereof with alkyl groups having from 1 to 6 carbon atoms.Type: GrantFiled: November 9, 1988Date of Patent: November 30, 1993Assignee: W. R. Grace & Co.-Conn.Inventors: Charles G. Carter, Ranjit Kumar
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Patent number: 5242908Abstract: The use of a compound of the formula I ##STR1## in which V is an alkyl group, fluorine, chlorine, bromine, or iodine, n is an integer from 1 to 5, W is an alkyl, alkenyl, alkynyl or alkoxy group, cyanide, nitro, carboxyl, hydrogen or a cycloalkyl, aryl, aralkyl or carboalkoxy group, R.sup.1 and R.sup.2 are an alkyl, alkenyl, alkynyl, cycloalkyl or halogenoalkyl group, sodium, potassium, calcium, magnesium, aluminum, lithium, ammonium, triethylammonium or hydrogen, R.sup.1 and R.sup.2 together form a cyclic diester, R.sup.3 and R.sup.4 are an alkyl, alkenyl, alkynyl, carboalkoxy, cycloalkyl or alkoxy group, hydrogen, fluorine, chlorine, bromine or iodine and X, Y and Z are oxygen or sulfur, for the treatment of diseases caused by DNA viruses or RNA viruses is described.Type: GrantFiled: February 1, 1991Date of Patent: September 7, 1993Assignee: Hoechst AktiengesellschaftInventors: Anuschirwan Peyman, Eugen Uhlmann, Karlheinz Budt, Jochen Knolle, Irvin Winkler, Matthias Helsberg
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Patent number: 5196409Abstract: Novel bisphosphonates comprise compounds of the formula (I) ##STR1## wherein m and l are independently 1 or 2; R.sub.1 represents hydrogen, a lower alkyl group, or an alkali metal cation; R.sub.2 represents hydrogen, a lower alkyl group or an alkali metal cation; Y represents .dbd.0 or .dbd.N--OH, or --OH; and X represents --(CH.sub.2).sub.n --, a branched alkylene group, or a branched or straight alkenylene or alkynylene chain optionally substituted by one or more oxygen or nitrogen atoms, wherein n is an integer from 3 to 24; with the provision that when l.dbd.m.dbd.1, Y is .dbd.0, and R.sub.1 and R.sub.2 denote a lower alkyl group, n represents an integer from 9 to 20; and with the provision that when l.dbd.m.dbd.2, Y is --OH and R.sub.1 and R.sub.2 are methyl groups, n represents an integer from 9-24; and with the further provision that when l.dbd.m.dbd.2, Y is --OH and R.sub.1 and R.sub.2 are hydrogen, n represents 3, 5 or an integer from 7 to 24; or X is--(CH.sub.2).sub.p --(OCH.sub.2 CH.sub.2).sub.Type: GrantFiled: September 23, 1991Date of Patent: March 23, 1993Assignee: Yissum, Research Development Company of the Hebrew University of JerusalemInventors: Eli Breuer, Gershon Golomb
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Patent number: 5159097Abstract: An alkenoic acid derivative of the formula ##STR1## in which X and Y are identical or different and represent sulfur, sulfoxide, sulfone, an alkylene chain, --SCH.sub.2 --, or oxygen or a direct bond,W represents --CH.dbd.CH--or --CH.sub.2 --CH.sub.2 --,o represents a number 1 to 5,A and B are identical or different and represent carboxyl, carboxymethylene, tetrazolyl or tetrazolylmethylene, or --CO.sub.2 R.sup.9 or --CH.sub.2 CO.sub.2 R.sup.9 or --CONR.sup.10 R.sup.11 or nitrilen represents a number 1 to 10,m represents a number 0 to 7,T and Z are identical or different and represent oxygen or a direct bond andR.sup.2, R.sup.3, R.sup.8 are identical or different and represent hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano or nitro andR.sup.9 is lower alkyl and R.sup.10 and R.sup.11 are hydrogen, lower alkyl, alkylsulfonyl or arylsulfonyl or together are an alkylene chain to form a ringand pharmaceutically acceptable salts thereof.Type: GrantFiled: November 26, 1990Date of Patent: October 27, 1992Assignee: Bayer AktiengesellschaftInventors: Ulrich Rosentreter, Harold C. Kluender, Trevor S. Abram, Peter Norman, Steven R. Tudhope
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Patent number: 5017306Abstract: A method of preparing phosphonate compositions comprising di-(phosphonomethyl) formal is disclosed which comprises (a) forming an intimate mixture of hydroxymethylphosphonic acid and formaldehyde or its condensates, said mixture having a least about 0.5 equivalents of formaldehyde per equivalent of hydroxymethylphosphonic acid; and (b) subjecting said intimate mixture to a temperature of between about 100.degree. C. and 180.degree. C. for a time sufficient to allow the components to react to form a reacted mixture comprising di-(phosphonomethyl) formal.Type: GrantFiled: November 9, 1988Date of Patent: May 21, 1991Assignee: W. R. Grace & Co.-Conn.Inventors: Donald A. Bansleben, Charles G. Carter, Ranjit Kumar