Chalcogen Bonded Directly To The Nitrogen By Nonionic Bonding Patents (Class 558/175)
  • Publication number: 20150011790
    Abstract: An emulsifier for emulsion polymerization contains a compound represented by the following general formula (I).
    Type: Application
    Filed: January 9, 2013
    Publication date: January 8, 2015
    Inventors: Asako Ogasawara, Masayuki Hashimoto
  • Publication number: 20140336137
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: July 28, 2014
    Publication date: November 13, 2014
    Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
  • Patent number: 8859799
    Abstract: The present invention relates to a compound of formula (1), or mixtures thereof: wherein Rf, X, Y, A, p, m, n, r, q, x, M, R1, R2, Z, a, and R6 are defined herein; wherein at least one of p or m is a positive integer; provided that, when q is 0, r is (3?x), and when q is 1, r and x are each 1; provided that, if n is greater than 2, then p is 1; provided that, if m is 0 then Y is a single bond, and if m is a positive integer then Y is 0; and provided that when R1 is greater than 8 carbons, the ratio of hetero atoms to carbon atoms is at least 1:2.
    Type: Grant
    Filed: October 17, 2013
    Date of Patent: October 14, 2014
    Assignee: E I du Pont de Nemours and Company
    Inventors: Roman B Larichev, Xianjun Meng, Allison Mary Yake
  • Publication number: 20140017797
    Abstract: This invention concerns isotopically coded or non-isotopically coded affinity-tags for analysis of certain target molecules in complex samples, in particular for mass spectrometric analysis of proteomic samples. The affinity-tags have the following general formula X-SPACER-OPO3H2, wherein X is a functional group or moiety capable of reacting with a functional group of a protein, peptide, DNA, lipid, sugar and/or steroid. These phosphate affinity tags (‘PTAG’) are capable of high but reversible binding to metal-oxides like TiO2. Due to this property, tagged sample fractions can be isolated from non-tagged sample fraction by affinity chromatography. The binding of organophosphate to metal-oxides remains intact during multiple washings of preferably acidic solutions to remove non-specifically bound components. PTAG's are also envisaged wherein X is selected such that it is capable of binding proteins, peptides, nucleic acid molecules, lipids, carbohydrates, steroids and the like.
    Type: Application
    Filed: December 13, 2011
    Publication date: January 16, 2014
    Applicant: De Staadt der Nederlanden, vert doorde minister van VWS
    Inventor: Jamila Willhelmina Zomer-Elhadari
  • Patent number: 8580995
    Abstract: The present invention provides processes for synthesizing lysine based compounds of the formula; wherein R1 may be, for example, (HO)2P(O)—, (NaO)2P(O)—, wherein X may be, for example, NH2, Y may be H, F, Cl, or Br, and wherein n, X?, Y?, R2, R3, R4, R5 and R6 are as defined herein.
    Type: Grant
    Filed: June 19, 2008
    Date of Patent: November 12, 2013
    Assignee: TaiMed Biologics, Inc.
    Inventors: Guy Milot, Stephane Branchaud, Brent R. Stranix
  • Publication number: 20130211108
    Abstract: The present invention relates to a novel process for the preparation of Fosamprenavir or its pharmaceutically acceptable salts thereof by using novel intermediates.
    Type: Application
    Filed: June 17, 2011
    Publication date: August 15, 2013
    Inventors: Siva Rama Prasad Vellanki, Madhu Murthy Nadella, Rajendra Reddy Mulamalla, Siva Koteswara Rao Prathi, Ravathi Srinivas Rambhotla, Siva Reddy Arumalla, Debashish Datta
  • Publication number: 20130204008
    Abstract: The present invention provides novel methods for synthesizing PPAR? sparing compounds, e.g., thiazolidinediones, that are useful for preventing and/or treating metabolic disorders such as diabetes, obesity, hypertension, and inflammatory diseases.
    Type: Application
    Filed: August 9, 2011
    Publication date: August 8, 2013
    Applicant: Metabolic Solutions Development Company, LLC
    Inventors: Steven P. Tanis, Timothy Parker, Robert C. Gadwood, Gerald D. Artman, III, James R. Zeller
  • Publication number: 20130045951
    Abstract: The invention relates to nitroso derivatives including carboxylic acid and phosphoric acid esters of hydroxy nitroso compounds that donate nitroxyl (HNO) under physiological conditions. The compounds and compositions of the invention are useful in treating and/or preventing the onset and/or development of diseases or conditions that are responsive to nitroxyl therapy, including heart failure, ischemia/reperfusion injury and cancer.
    Type: Application
    Filed: October 18, 2012
    Publication date: February 21, 2013
    Applicant: CARDIOXYL PHARMACEUTICALS, INC.
    Inventor: CARDIOXYL PHARMACEUTICALS, INC.
  • Patent number: 8163911
    Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
    Type: Grant
    Filed: September 4, 2008
    Date of Patent: April 24, 2012
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
  • Patent number: 8022238
    Abstract: A compound of Formula 1 Rf-A-OP(O)(O?M+)(OROH)??Formula 1 wherein Rf is a C2 to C6 linear or branched perfluoroalkyl optionally interrupted by one, two or three ether oxygen atoms; A is (CH2CF2)m(CH2)n—, (CH2)oSO2N(CH3)(CH2)p—, O(CF2)q(CH2)r—, or OCHFCF2OE-; m is 0 to 4; n, o, p, and r are each independently 2 to 20; q is 2; E is a C2 to C20 linear or branched alkyl group optionally interrupted by oxygen, sulfur, or nitrogen atoms; a cyclic alkyl group, or a C6 to C10 aryl group; M is H or a Group I metal or an ammonium cation (NHxR2y)+ wherein R2 is a C1 to C4 alkyl, x is 0 to 4, y is 0 to 4 and x+y is 4; and R is a C2 to C60 linear or branched alkyl group optionally interrupted by hetero atoms selected from the group consisting of an oxygen, sulfur, or nitrogen atom; a cyclic alkyl; or a C6 to C10 aryl; provided that when R is greater than 8 carbons, the ratio of hetero atoms to carbon atoms is at least 1:2.
    Type: Grant
    Filed: March 20, 2009
    Date of Patent: September 20, 2011
    Assignee: E. I. du Pont de Nemours and Company
    Inventors: Sheng Peng, Allison Mary Yake
  • Patent number: 7875739
    Abstract: Methods and kits for decomposing organophosphorus compounds in non-aqueous media at ambient conditions are described. Insecticides, pesticides, and chemical warfare agents can be quickly decomposed to non-toxic products. The method comprises combining the organophosphorus compound with a non-aqueous solution, preferably an alcohol, comprising metal ions and at least a trace amount of alkoxide ions. In a first preferred embodiment, the metal ion is a lanthanum ion. In a second preferred embodiment, the metal ion is a transition metal.
    Type: Grant
    Filed: March 5, 2007
    Date of Patent: January 25, 2011
    Assignee: Queen's University at Kingston
    Inventors: R. Stanley Brown, Alexei A. Neverov, Josephine S. W. Tsang
  • Publication number: 20100261677
    Abstract: The invention relates to substituted arylsulphonylaminomethylphosphonic acid derivatives of general formula (I) wherein the groups Ra to Rf, A and Z are defined as mentioned in the specification and claims, which are suitable for preparing a medicament for the treatment of metabolic disorders, particularly type 1 or type 2 diabetes mellitus.
    Type: Application
    Filed: September 4, 2008
    Publication date: October 14, 2010
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
  • Publication number: 20100240920
    Abstract: A compound of Formula 1 Rf-A-OP(O)(O?M+)(OROH) ??Formula 1 wherein Rf is a C2 to C6 linear or branched perfluoroalkyl optionally interrupted by one, two or three ether oxygen atoms; A is (CH2CF2)m(CH2)n—, (CH2)oSO2N(CH3)(CH2)p—, O(CF2)q(CH2)r—, or OCHFCF2OE-; m is 0 to 4; n, o, p, and r are each independently 2 to 20; q is 2; E is a C2 to C20 linear or branched alkyl group optionally interrupted by oxygen, sulfur, or nitrogen atoms; a cyclic alkyl group, or a C6 to C10 aryl group; M is H or a Group I metal or an ammonium cation (NHxR2y)+ wherein R2 is a C1 to C4 alkyl, x is 0 to 4, y is 0 to 4 and x+y is 4; and R is a C2 to C60 linear or branched alkyl group optionally interrupted by hetero atoms selected from the group consisting of an oxygen, sulfur, or nitrogen atom; a cyclic alkyl; or a C6 to C10 aryl; provided that when R is greater than 8 carbons, the ratio of hetero atoms to carbon atoms is at least 1:2.
    Type: Application
    Filed: March 20, 2009
    Publication date: September 23, 2010
    Applicant: E. I. du Pont de Nemours and Company
    Inventors: Sheng Peng, Allison Mary Yake
  • Patent number: 7772340
    Abstract: A subject-matter of the invention is alkoxyamines resulting from ?-phosphorated nitroxides corresponding to the formula: in which R represents an alkyl radical having a number of carbon atoms ranging from 1 to 3, R1 represents a hydrogen atom or a residue: in which R3 represents an alkyl radical having a number of carbon atoms ranging from 1 to 20, and R2 represents a hydrogen atom, an alkyl radical having a number of carbon atoms ranging from 1 to 8, a phenyl radical, an alkali metal, such as Li, Na or K, H4N+, Bu4N+ or Bu3HN+, exhibiting a kinetic dissociation constant kd, measured at 120° C. by EPR, of greater than 0.05 s?1. These compounds can be used as initiators for the (co)polymerizations of at least one monomer which can be polymerized by the radical route.
    Type: Grant
    Filed: July 23, 2003
    Date of Patent: August 10, 2010
    Assignee: Arkema France
    Inventors: Jean-Luc Couturier, Olivier Guerret, Denis Bertin, Didier Gigmes, Sylvain Marque, Paul Tordo, Florence Chauvin, Pierre-Emmanuel Dufils
  • Patent number: 7301043
    Abstract: Compounds for determining the activity of phospholipase A2, are described herein, and include embodiments having formula (1) wherein L1 is derived from an ether (R1—OR2)m, wherein R1 and R2 are independently selected and are derived from a hydrocarbon having 1 to 12 carbon atoms, with m being an integer from 1 to 4, or from a hydrocarbon R having 1 to 20 carbon atoms; F is unsubstituted or substituted pyrene as a flouraphore; Q is a quencher, and L2 is C(O)-L1 or C(O)-L1-NH, wherein L1 is as defined above. These compounds may be used to determine the activity of phospholipase A2, in particular PAF-AH.
    Type: Grant
    Filed: October 23, 2002
    Date of Patent: November 27, 2007
    Assignee: Sirs-Lab GmbH
    Inventors: Hans-Peter Deigner, Stefan Russwurm, Ralf Kinscherf, Wolfgang Lösche
  • Publication number: 20040248855
    Abstract: A description is given of processes for the preparation of mono- and bisacylphosphines and of mono- and bisacylphosphine oxides and mono- and bisacylphosphine sulfides, which comprises first reacting organic P-monohalogenophosphines or P,P-dihalogenophosphines, or mixtures thereof, with an alkali metal or magnesium in combination with lithium, where appropriate in the presence of a catalyst, and then carrying out the reaction with acid halides and, in the case of the process for the preparation of oxides, carrying out an oxidation step and, in the case of the preparation of sulfides, reacting the phosphines so obtained with sulfur. It is characteristic, Inter alia, that the processes are carried out without isolation of the intermediates.
    Type: Application
    Filed: May 17, 2004
    Publication date: December 9, 2004
    Inventors: David George Leppard, Eugen Eichenberger, Rene Kaeser, Gebhard Hug, Urs Schwendimann
  • Patent number: 6700007
    Abstract: A process for preparing alkoxyamines in a biphasic medium comprises mixing an ionic liquid, an organic solvent, a metal salt, a ligand for the metal, a halocarbon compound ZX and a nitroxide, keeping the reaction medium stirring at a temperature of between 20° C. and 90° C. until the nitroxide has disappeared, separating the mixture by decantation, recovering the organic phase, and optionally washing it with water and then isolating the alkoxyamine by evaporating the organic solvent under reduced pressure.
    Type: Grant
    Filed: August 8, 2002
    Date of Patent: March 2, 2004
    Assignee: Atofina
    Inventors: Jean-Luc Couturier, Olivier Guerret
  • Patent number: 6677374
    Abstract: Compounds and methods for mitigating neurodegeneration, effecting neuroprotection and/or effecting cognition enhancement in a subject are described. Neurological or cognitive conditions are treated by administering to a subject an effective amount of a therapeutic compound comprising a nitrate ester, or a pharmaceutically acceptable salt or ester thereof.
    Type: Grant
    Filed: March 29, 2002
    Date of Patent: January 13, 2004
    Assignee: Queen's University at Kingston
    Inventors: Gregory R. J. Thatcher, Brian M. Bennett, James N. Reynolds, Roland J. Boegman, Khem Jhamandas
  • Patent number: 6569967
    Abstract: The invention concerns alkoxyamines derived from &bgr;-phosphorous nitroxides corresponding to formula (I). Said compounds can be used as (co)polymerization initiators of at least a monomer polymerizable by radical polymerization.
    Type: Grant
    Filed: March 19, 2002
    Date of Patent: May 27, 2003
    Assignee: Atofina
    Inventors: Jean-Luc Couturier, Christiane Henriet-Bernard, Christophe Le Mercier, Paul Tordo, Jean-Francois Lutz
  • Patent number: 6534489
    Abstract: The invention relates to organophosphorus compounds of general formula (I) wherein A corresponds to general formula (II), wherein one or more of the carbon atoms, selected from the group C3, C4, C5 and their respective substituents can be omitted, and at least one substituent of B1 to B10 is a C3-8 cycloalkyl (C0-9) alkyl group, wherein both the C3-8 cycloalkyl group and the C0-9 alkyl group can have one or more double bonds and one or two carbon atoms of the cycloalkyl group can be substituted by nitrogen, oxygen or sulfur atoms, and wherein both the cycloalkyl group and the alkyl group can be substituted by hydrogen, halogen amine, oxo groups with branched or unbranched C1-9 alkyl groups and C2-9 alkenyl groups, wherein the C1-9 alkyl groups and C2-9 alkenyl groups can be substituted by hydrogen, hydroxy, amine, halogen, and oxo groups.
    Type: Grant
    Filed: May 25, 2001
    Date of Patent: March 18, 2003
    Assignee: Jomaa Pharmaka GmbH
    Inventor: Hassan Jomaa
  • Patent number: 6495720
    Abstract: The invention relates to a process for preparing alkoxyamines. This process consists in mixing, in an organic solvent, a metal salt, a ligand for the metal, a halocarbon compound ZX and a nitroxide, in keeping the reaction medium stirring at a temperature of between 20° C. and 90° C. until the nitroxide has disappeared, in recovering the organic phase, in washing it with water and then in isolating the alkoxyamine by evaporating the organic solvent under reduced pressure.
    Type: Grant
    Filed: February 23, 2001
    Date of Patent: December 17, 2002
    Assignee: Atofina
    Inventors: Jean-Luc Couturier, Olivier Guerret, Thierry Senninger
  • Patent number: 6472406
    Abstract: The intention relates to bacterial antibiotic resistance and, in particular, to compositions and methods for overcoming bacterial antibiotic resistance. The invention provides novel &bgr;-lactamase inhibitors, which are structurally unrelated to the natural product and semi-synthetic &bgr;-lactamase inhibitors presently available, and which do not require a &bgr;-lactam pharmacophore. The invention also provides pharmaceutical compositions and methods for inhibiting bacterial growth.
    Type: Grant
    Filed: July 5, 2000
    Date of Patent: October 29, 2002
    Assignee: MethylGene, Inc.
    Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
  • Patent number: 5883122
    Abstract: Aliphatic nitrate esters having a sulfur or phosphorus atom .beta. or .gamma. to a nitrate group and their congeners having efficacy as neuroprotective agents are described. Preferred nitrate esters may be synthesized by nitration of a 3-bromo-1,2-propanediol, and subsequent reaction to yield the desired mono-, di- or tetra-nitrate ester.
    Type: Grant
    Filed: June 3, 1997
    Date of Patent: March 16, 1999
    Assignee: Queen's University at Kingston
    Inventors: Gregory R. J. Thatcher, Brian M. Bennett, James N. Reynolds, Roland J. Boegman, Khem Jhamandas
  • Patent number: 5849771
    Abstract: Compounds of formula (I), wherein Ar, R.sub.1, R.sub.2, Y and R are as defined in claim 1, are effective as traps for free radicals.
    Type: Grant
    Filed: January 26, 1998
    Date of Patent: December 15, 1998
    Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)
    Inventors: Abdelhamid Zeghdaoui, Jean-Pierre Finet, Beatrice Tuccio, Viviane Cerri, Paul Tordo
  • Patent number: 5807847
    Abstract: Aliphatic Nitrate esters having a sulfur or phosphorus atom .beta. or .gamma. to a nitrate group having efficacy as vasodilators are described. Preferred nitrate esters may be synthesized by nitration of a 3-bromo-1,2-propanediol, and subsequent reaction to yield the desired mono, di or tetra nitrate ester.
    Type: Grant
    Filed: June 4, 1996
    Date of Patent: September 15, 1998
    Assignee: Queen's University at Kingston
    Inventors: Gregory R. J. Thatcher, Brian M. Bennett
  • Patent number: 5792858
    Abstract: Novel derivatives of lysophingolipids free from sialic acids which are N-acyllysosphingolipids having one of the two formulae: ##STR1## in which -A- stands for the group --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, n.sub.1 is a whole number of between 6 and 18, n.sub.2 is a whole number of between 11 and 15, X is a hydrogen atom or the residue of a monosaccharide or a disaccharide or phosphorylcholine and R represents an alkyl radical derived from a saturated or unsaturated aliphatic carboxylic acid having from 2 to 24 carbon atoms substituted by one or more polar groups. The lysosphingolipid derivatives of the invention exhibit an inhibiting action on protein-kinase C activation and, thus, can be utilized in therapies for various pathologies of the nervous system.
    Type: Grant
    Filed: April 5, 1996
    Date of Patent: August 11, 1998
    Assignee: FIDIA S.p.A.
    Inventors: Francesco Della Valle, Aurelio Romeo
  • Patent number: 5714266
    Abstract: Compositions for treating pulp slurry in the wet end comprising (A) a mixture of fluoroaliphatic radical-containing phosphate esters comprising at least 70% of a phosphate monoester, e.g., C.sub.8 F.sub.17 SO.sub.2 N(C.sub.2 H.sub.5)C.sub.2 H.sub.4 OP(O) (OH) (O.sup.- NH.sub.4.sup.+) and (B) an alkyl ketene dimer are disclosed. Methods for using such compositions and the resulting treated products are also disclosed.
    Type: Grant
    Filed: June 13, 1996
    Date of Patent: February 3, 1998
    Assignee: Minnesota Mining and Manufacturing Company
    Inventors: Susan S. Harrison, Karlan B. Hunt
  • Patent number: 5685880
    Abstract: A leather modifier containing a compound which is obtainable through a reaction of an ethylene oxide derivative having a fluorine-containing group with a phosphorus compound is disclosed. A leather treated with the modifier has much improved properties.
    Type: Grant
    Filed: April 21, 1994
    Date of Patent: November 11, 1997
    Assignee: Daikin Industries, Ltd.
    Inventors: Tetsuya Masutani, Masato Kuroi, Yasuo Itami, Masahiko Maeda, Norio Yanagisawa, Yoshihiko Misugi, Maki Yasuhara
  • Patent number: 5576308
    Abstract: An insecticidal, acaricidal or nematocidal composition which comprises an organophosphorus compound represented by formula (I): ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each represents C.sub.1 to C.sub.4 alkyl; A represents H, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 alkylthio or N(R.sup.4)R.sup.5 ; Z represents C(CN)R.sup.4 or N-R.sup.7 and an inert carrier show excellent effect for controlling harmful insects, mites and nematodes, do not give off a bad or irritating odor and exhibit very low toxicity to warm-blooded animals. R.sup.4, R.sup.5, R.sup.6, and R.sup.7 are defined in the specification.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: November 19, 1996
    Assignee: Agro-Kanesho Co., Ltd.
    Inventors: Shinya Henmi, Hideyo Fujii, Akinori Kariya
  • Patent number: 5519007
    Abstract: Novel derivatives of lysophingolipids free from sialic acids which are N-acyllysosphingolipids having one of the two formulae: ##STR1## in which --A-- stands for the group --CH.dbd.CH-- or --CH.sub.2 --CH.sub.2 --, n.sub.1 is a whole number of between 6 and 18, n.sub.2 is a whole number of between 11 and 15, X is a hydrogen atom or the residue of a monosaccharide or a disaccharide or phosphorylcholine and R represents an alkyl radical derived from a saturated or unsaturated aliphatic carboxylic acid having from 2 to 24 carbon atoms substituted by one or more polar groups. The lysosphingolipid derivatives of the invention exhibit an inhibiting action on protein-kinase C activation and, thus, can be utilized in therapies for various pathologies of the nervous system.
    Type: Grant
    Filed: July 21, 1992
    Date of Patent: May 21, 1996
    Assignee: Fidia, S.p.A.
    Inventors: Francesco Della Valle, Aurelio Romeo
  • Patent number: 5424441
    Abstract: N-aralkyl- and N-heteroaralkyl-aminoalkanephosphinic acids of formula I ##STR1## wherein R is an aliphatic, cycloaliphatic, cycloaliphatic-aliphatic, araliphatic or heteroarylaliphatic radical having at least 2 carbon atoms, R.sub.1 is hydrogen or hydroxy, R.sub.2 is an araliphatic or heteroarylaliphatic radical substituted by free or functionally modified carboxy that is bonded directly or by way of a spacer, and R.sub.3 is hydrogen, lower alkyl or a group R.sub.2, and the salts thereof have valuable nootropic and anti-epileptic properties and can be used in the preparation of a nootropic or anti-epileptic medicament.
    Type: Grant
    Filed: May 4, 1994
    Date of Patent: June 13, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: Stuart J. Mickel, Wolfgang Frostl, Pascal Furet
  • Patent number: 5414102
    Abstract: The present invention relates to fluorinated carboxylic acid esters of phosphonocarboxylic acids containing acrylate and/or methacrylate groups, their use as waterproofing or oil-repellency agents, and a method for their preparation.
    Type: Grant
    Filed: December 27, 1993
    Date of Patent: May 9, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Klaus Pohmer, Rainer Weber, Hans-Dieter Block, Hans-Heinrich Moretto
  • Patent number: 5247085
    Abstract: Compounds of formula (I), and pharmaceutically acceptable salts thereof ##STR1## wherein R.sub.1 is hydroxy, amino, chloro or OR.sub.7 whereinR.sub.7 is C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-2 alkyl either of which phenyl moieties may be substituted by one or two substituents selected from halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;R.sub.2 is amino or, when R.sub.1 is hydroxy or amino, R.sub.2 may also be hydrogen;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl;R.sub.4 is a group of formula: ##STR2## R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-6 alkyl and optionally substituted phenyl; orR.sub.3 and R.sub.4 together are: ##STR3## wherein R.sub.6 is as defined above;having antiviral activity, to processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: May 29, 1992
    Date of Patent: September 21, 1993
    Assignee: Beecham Group p.l.c.
    Inventors: Michael R. Harnden, David M. Duckworth
  • Patent number: 5166198
    Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof: ##STR1## wherein R.sub.1 is hydroxy or amino;R.sub.2 is hydrogen or amino;R.sub.3 is hydrogen, hydroxymethyl or acyloxymethyl;R.sub.4 is hydrogen or (when R.sub.3 =H and Z is a bond or CH.sub.2) hydroxy, acyloxy, hydroxymethyl or acyloxymethyl;Z is a bond, or a group CHR.sub.8 wherein R.sub.8 is hydrogen, or (when R.sub.3 =R.sub.4 =H), R.sub.8 is hydroxy, acyloxy, hydroxymethyl or acyloxymethyl;R.sub.5 is a group of formula: ##STR2## wherein R.sub.6 and R.sub.7 are independently selected from hydrogen,C.sub.1-6 alkyl and optionally substituted phenyl.
    Type: Grant
    Filed: March 28, 1990
    Date of Patent: November 24, 1992
    Assignee: Beecham p.l.c.
    Inventors: Michael R. Harnden, David M. Duckworth, Halina T. Serafinowska
  • Patent number: 5144045
    Abstract: Phospocholine derivatives having the formula: ##STR1## in which W, Z, Q and R are described in the specification are disclosed as useful for inhibiting the enzyme phospholipase A.sub.2. Methods of making and using the compounds are also disclosed.
    Type: Grant
    Filed: November 13, 1990
    Date of Patent: September 1, 1992
    Assignee: American Cyanamid Company
    Inventors: Allan Wissner, Robert E. Schaub, Kenneth E. Green, Philip R. Hamann
  • Patent number: 5091550
    Abstract: 5,5-Bis(perfluoroalkylheteromethyl)-2-hydroxy-2-oxo-1,3,2-dioxaphosphorinan es, derived acyclic phosphorus and phosphoric acids obtained by ring-opening, and salts or esters thereof are prepared from heteroatom containing perfluoroalkyl terminated neopentyl glycols of the formula: HO[CH.sub.2 C(CH.sub.2 --X--E.sub.n --R.sub.f).sub.2 CH.sub.2 O]H by cyclization with appropriate phosphorus containing esters or acids, or hydrolysis. These compositions provide improved thermal stability, and useful low surface energy oil and water repellent coatings for textiles, glass, paper, leather and other materials.Another aspect of this invention relates to the use of the phosphite group containing products as polymer stabilizers.
    Type: Grant
    Filed: April 20, 1990
    Date of Patent: February 25, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Robert A. Falk, Kirtland P. Clark
  • Patent number: 5077329
    Abstract: Hydroxyaminomethylphosphonates of formula I ##STR1## where R.sub.1 to R.sub.5 are independently hydrogen, alkyl, cycloalkyl, aryl or phenylalkyl, R.sub.6 has the same meanings except for hydrogen, and R.sub.1 can also be trialkylsilyl, are useful stabilizers for organic materials subject to oxidative, thermal or actinic induced degradation.
    Type: Grant
    Filed: April 6, 1990
    Date of Patent: December 31, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Stephen D. Pastor, Ramanathan Ravichandran
  • Patent number: 5055458
    Abstract: Compounds of formula (I) and pharmaceutically acceptable salts thereof: ##STR1## wherein R.sub.1 is hydroxy, amino, chloro or OR.sub.7 whereinR.sub.7 is C.sub.1-6 alkyl, phenyl or phenyl C.sub.1-2 alkyl either of which phenyl moieties may be substituted by one or two substituents selected from halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy;R.sub.2 amino or, when R.sub.1 is hydroxy or amino, R.sub.2 may also be hydrogen;X is --CH.sub.2 CH.sub.2 -- or a moiety of structure (a), (b) or (c): ##STR2## wherein n is 1 or 2;m is 0, 1 or 2; andR.sub.3 is hydrogen or acyl;R.sub.4 is a group of formula: ##STR3## wherein R.sub.5 and R.sub.6 are independently selected from hydrogen, C.sub.1-6 alkyl and optionally substituted phenyl; having antiviral activity, processes for their preparation and their use as pharmaceuticals.
    Type: Grant
    Filed: July 28, 1989
    Date of Patent: October 8, 1991
    Assignee: Beecham Group P.l.c.
    Inventors: Stuart Bailey, Michael R. Harnden
  • Patent number: 5051413
    Abstract: The invention relates to unsaturated amino acids of the formula I ##STR1## in which R.sup.1 represents hydroxy or etherified hydroxy, R.sup.2 represents hydrogen, alkyl, hydroxy or etherified hydroxy, R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxyalkyl, lower alkoxyalkyl, arylalkyl, lower alkenyl, halogen or aryl, R.sup.4 represents hydrogen, alkyl or aryl, R.sup.5 represents hydrogen or alkyl, R.sup.6 represents carboxy or esterified or amidated carboxy, R.sup.7 represents amino or amino substituted by alkyl or acyl, A represents unsubstituted or alkyl-substituted .alpha.,.omega.-alkylene having from 1 to 3 carbon atoms or represents a bond, and B represents methylene or a bond, with the proviso that A is other than a bond when B represents a bond, and salts thereof. They can be manufactured, for example, in accordance with the Michaelis-Arbuzov reaction and can be used as pharmacologically active substances.
    Type: Grant
    Filed: December 18, 1989
    Date of Patent: September 24, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Christof Angst, Derek E. Brundish, John G. Dingwall, Graham E. Fagg, Hans Allgeier, Guido Bold, Rudolf Duthaler, Roland Heckendorn, Antonio Togni
  • Patent number: 4908465
    Abstract: The compounds of the formula ##STR1## in which one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen, C.sub.1 -.sub.8 -alkyl, C.sub.3 -.sub.6 -cycloalkyl, phenyl optionally substituted by halogeno, C.sub.1 -.sub.4 -alkyl, C.sub.1 -.sub.4 -alkoxy and/or trifluoromethyl, or C.sub.7 -.sub.10 -phenylalkyl optionally substituted in the phenyl moiety by halogeno, C.sub.1 -.sub.4 -alkyl, C.sub.1 -.sub.4 -alkoxy and/or trifluoromethyl, and the other two are hydrogen, or salts thereof.These compounds have valuable pharmaceutical properties.
    Type: Grant
    Filed: June 7, 1988
    Date of Patent: March 13, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: John G. Dingwall, Josef Ehrenfreund, Roger G. Hall, James Jack
  • Patent number: 4898944
    Abstract: Precursors for the preparation of fiber-reactive triphendioxazine dyestuffs correspond to the general formulas: ##STR1## in which Y' is a vinyl, a beta-hydroxyethyl or an ethyl group which contains in the beta-position a substituent which can be eliminated by an alkali;T is an optionally substituted alkyl (e.g.
    Type: Grant
    Filed: October 27, 1988
    Date of Patent: February 6, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Gunther Schwaiger, Hartmut Springer, Walter Helmling
  • Patent number: 4897382
    Abstract: Organic amide compounds of the formula ##STR1## wherein R.sub.1 --CO is a residue of a carboxylic acid with the proviso that the carboxylic acid is not a natural fatty acid normally bound to nitrogen of nitrogenous lipids, R.sub.2 is a hydrogen atom, a C.sub.1-7 alkyl group, or a C.sub.4-7 cycloalkyl group, and R.sub.3-N is a residue of a nitrogenous lipid. The compounds are useful in increasing or stimulating the in vivo biological activity of in vitro biologically active carboxylic acids.
    Type: Grant
    Filed: June 21, 1988
    Date of Patent: January 30, 1990
    Assignee: Fidia S.p.A.
    Inventors: Francesco della Valle, Aurelio Romeo
  • Patent number: 4804654
    Abstract: Compounds of the formula ##STR1## wherein the symbols have assigned meanings, and their use as insecticides and/or miticides.
    Type: Grant
    Filed: March 4, 1987
    Date of Patent: February 14, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Mohamed A. H. Fahmy
  • Patent number: 4772738
    Abstract: The compounds of the formula ##STR1## in which one of the groups R.sup.1, R.sup.2 and R.sup.3 represents hydrogen, C.sub.1-8 -alkyl, C.sub.3-6 -cycloalkyl, phenyl optionally substituted by halogeno, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy and/or trifluoromethyl, or C.sub.7-10 -phenylalkyl optionally substituted in the phenyl moiety by halogeno, C.sub.1-4 -alkyl, C.sub.1-4 -alkoxy and/or trifluormethyl, and the other two are hydrogen, or salts thereof.These compounds have valuable pharmaceutical properties.
    Type: Grant
    Filed: December 12, 1986
    Date of Patent: September 20, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: John G. Dingwall, Josef Ehrenfreund, Roger G. Hall, James Jack
  • Patent number: 4753972
    Abstract: Substituted aminoxyethyl phosphonates of the formula ##STR1## and various metal salts thereof are prepared by the reaction of the appropriate hydroxylamine and vinylphosphonate compounds and are useful as color improvers and stabilizers of organic materials.
    Type: Grant
    Filed: July 24, 1987
    Date of Patent: June 28, 1988
    Assignee: Ciba-Geigy Corporation
    Inventor: Ramanathan Ravichandran
  • Patent number: 4652666
    Abstract: The novel compounds of the formula I ##STR1## in which R.sup.1 denotes (subst.) alkyl, (subst.) alkenyl, (subst.) alkinyl, (subst.) cycloalkyl, phenyl, naphthyl or alkoxycarbonyl, R.sup.2 denotes alkyl, alkoxy or phenyl, R.sup.3 denotes alkyl, R.sup.4 denotes H or alkyl, Ar denotes (subst.) phenyl, (subst.) naphthyl or (subst.) quinolyl and n denotes 1, 2, 3 or 4, have interesting safener properties, i.e. they reduce the phytotoxic side effects of herbicides.
    Type: Grant
    Filed: July 18, 1985
    Date of Patent: March 24, 1987
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz Kehne, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer