Chalcogen Bonded Directly To The Nitrogen By Nonionic Bonding Patents (Class 558/175)
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Publication number: 20150011790Abstract: An emulsifier for emulsion polymerization contains a compound represented by the following general formula (I).Type: ApplicationFiled: January 9, 2013Publication date: January 8, 2015Inventors: Asako Ogasawara, Masayuki Hashimoto
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Publication number: 20140336137Abstract: 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: ApplicationFiled: July 28, 2014Publication date: November 13, 2014Inventors: Lisa Marie Frost, Stephen Martin Courtney, Frederick Arthur Brookfield, Vincent Jacob Kalish
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Patent number: 8859799Abstract: 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: GrantFiled: October 17, 2013Date of Patent: October 14, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Roman B Larichev, Xianjun Meng, Allison Mary Yake
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Publication number: 20140017797Abstract: 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: ApplicationFiled: December 13, 2011Publication date: January 16, 2014Applicant: De Staadt der Nederlanden, vert doorde minister van VWSInventor: Jamila Willhelmina Zomer-Elhadari
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Patent number: 8580995Abstract: 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: GrantFiled: June 19, 2008Date of Patent: November 12, 2013Assignee: TaiMed Biologics, Inc.Inventors: Guy Milot, Stephane Branchaud, Brent R. Stranix
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Publication number: 20130211108Abstract: The present invention relates to a novel process for the preparation of Fosamprenavir or its pharmaceutically acceptable salts thereof by using novel intermediates.Type: ApplicationFiled: June 17, 2011Publication date: August 15, 2013Inventors: Siva Rama Prasad Vellanki, Madhu Murthy Nadella, Rajendra Reddy Mulamalla, Siva Koteswara Rao Prathi, Ravathi Srinivas Rambhotla, Siva Reddy Arumalla, Debashish Datta
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Publication number: 20130204008Abstract: 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: ApplicationFiled: August 9, 2011Publication date: August 8, 2013Applicant: Metabolic Solutions Development Company, LLCInventors: Steven P. Tanis, Timothy Parker, Robert C. Gadwood, Gerald D. Artman, III, James R. Zeller
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Publication number: 20130045951Abstract: 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: ApplicationFiled: October 18, 2012Publication date: February 21, 2013Applicant: CARDIOXYL PHARMACEUTICALS, INC.Inventor: CARDIOXYL PHARMACEUTICALS, INC.
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Patent number: 8163911Abstract: 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: GrantFiled: September 4, 2008Date of Patent: April 24, 2012Assignee: Boehringer Ingelheim International GmbHInventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Patent number: 8022238Abstract: 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: GrantFiled: March 20, 2009Date of Patent: September 20, 2011Assignee: E. I. du Pont de Nemours and CompanyInventors: Sheng Peng, Allison Mary Yake
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Patent number: 7875739Abstract: 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: GrantFiled: March 5, 2007Date of Patent: January 25, 2011Assignee: Queen's University at KingstonInventors: R. Stanley Brown, Alexei A. Neverov, Josephine S. W. Tsang
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Publication number: 20100261677Abstract: 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: ApplicationFiled: September 4, 2008Publication date: October 14, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Elke Langkopf, Alexander Pautsch, Corinna Schoelch, Annette Schuler-Metz, Ruediger Streicher, Holger Wagner
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Publication number: 20100240920Abstract: 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: ApplicationFiled: March 20, 2009Publication date: September 23, 2010Applicant: E. I. du Pont de Nemours and CompanyInventors: Sheng Peng, Allison Mary Yake
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Patent number: 7772340Abstract: 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: GrantFiled: July 23, 2003Date of Patent: August 10, 2010Assignee: Arkema FranceInventors: Jean-Luc Couturier, Olivier Guerret, Denis Bertin, Didier Gigmes, Sylvain Marque, Paul Tordo, Florence Chauvin, Pierre-Emmanuel Dufils
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Patent number: 7301043Abstract: 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: GrantFiled: October 23, 2002Date of Patent: November 27, 2007Assignee: Sirs-Lab GmbHInventors: Hans-Peter Deigner, Stefan Russwurm, Ralf Kinscherf, Wolfgang Lösche
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Publication number: 20040248855Abstract: 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: ApplicationFiled: May 17, 2004Publication date: December 9, 2004Inventors: David George Leppard, Eugen Eichenberger, Rene Kaeser, Gebhard Hug, Urs Schwendimann
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Patent number: 6700007Abstract: 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: GrantFiled: August 8, 2002Date of Patent: March 2, 2004Assignee: AtofinaInventors: Jean-Luc Couturier, Olivier Guerret
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Patent number: 6677374Abstract: 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: GrantFiled: March 29, 2002Date of Patent: January 13, 2004Assignee: Queen's University at KingstonInventors: Gregory R. J. Thatcher, Brian M. Bennett, James N. Reynolds, Roland J. Boegman, Khem Jhamandas
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Patent number: 6569967Abstract: 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: GrantFiled: March 19, 2002Date of Patent: May 27, 2003Assignee: AtofinaInventors: Jean-Luc Couturier, Christiane Henriet-Bernard, Christophe Le Mercier, Paul Tordo, Jean-Francois Lutz
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Patent number: 6534489Abstract: 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: GrantFiled: May 25, 2001Date of Patent: March 18, 2003Assignee: Jomaa Pharmaka GmbHInventor: Hassan Jomaa
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Patent number: 6495720Abstract: 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: GrantFiled: February 23, 2001Date of Patent: December 17, 2002Assignee: AtofinaInventors: Jean-Luc Couturier, Olivier Guerret, Thierry Senninger
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Patent number: 6472406Abstract: 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: GrantFiled: July 5, 2000Date of Patent: October 29, 2002Assignee: MethylGene, Inc.Inventors: Jeffrey M. Besterman, Daniel Delorme, Jubrail Rahil
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Patent number: 5883122Abstract: 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: GrantFiled: June 3, 1997Date of Patent: March 16, 1999Assignee: Queen's University at KingstonInventors: Gregory R. J. Thatcher, Brian M. Bennett, James N. Reynolds, Roland J. Boegman, Khem Jhamandas
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Patent number: 5849771Abstract: 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: GrantFiled: January 26, 1998Date of Patent: December 15, 1998Assignee: Centre National de la Recherche Scientifique (C.N.R.S.)Inventors: Abdelhamid Zeghdaoui, Jean-Pierre Finet, Beatrice Tuccio, Viviane Cerri, Paul Tordo
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Patent number: 5807847Abstract: 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: GrantFiled: June 4, 1996Date of Patent: September 15, 1998Assignee: Queen's University at KingstonInventors: Gregory R. J. Thatcher, Brian M. Bennett
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Patent number: 5792858Abstract: 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: GrantFiled: April 5, 1996Date of Patent: August 11, 1998Assignee: FIDIA S.p.A.Inventors: Francesco Della Valle, Aurelio Romeo
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Patent number: 5714266Abstract: 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: GrantFiled: June 13, 1996Date of Patent: February 3, 1998Assignee: Minnesota Mining and Manufacturing CompanyInventors: Susan S. Harrison, Karlan B. Hunt
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Patent number: 5685880Abstract: 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: GrantFiled: April 21, 1994Date of Patent: November 11, 1997Assignee: Daikin Industries, Ltd.Inventors: Tetsuya Masutani, Masato Kuroi, Yasuo Itami, Masahiko Maeda, Norio Yanagisawa, Yoshihiko Misugi, Maki Yasuhara
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Patent number: 5576308Abstract: 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: GrantFiled: May 27, 1994Date of Patent: November 19, 1996Assignee: Agro-Kanesho Co., Ltd.Inventors: Shinya Henmi, Hideyo Fujii, Akinori Kariya
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Patent number: 5519007Abstract: 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: GrantFiled: July 21, 1992Date of Patent: May 21, 1996Assignee: Fidia, S.p.A.Inventors: Francesco Della Valle, Aurelio Romeo
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Patent number: 5424441Abstract: 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: GrantFiled: May 4, 1994Date of Patent: June 13, 1995Assignee: Ciba-Geigy CorporationInventors: Stuart J. Mickel, Wolfgang Frostl, Pascal Furet
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Patent number: 5414102Abstract: 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: GrantFiled: December 27, 1993Date of Patent: May 9, 1995Assignee: Bayer AktiengesellschaftInventors: Klaus Pohmer, Rainer Weber, Hans-Dieter Block, Hans-Heinrich Moretto
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Patent number: 5247085Abstract: 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: GrantFiled: May 29, 1992Date of Patent: September 21, 1993Assignee: Beecham Group p.l.c.Inventors: Michael R. Harnden, David M. Duckworth
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Patent number: 5166198Abstract: 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: GrantFiled: March 28, 1990Date of Patent: November 24, 1992Assignee: Beecham p.l.c.Inventors: Michael R. Harnden, David M. Duckworth, Halina T. Serafinowska
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Patent number: 5144045Abstract: 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: GrantFiled: November 13, 1990Date of Patent: September 1, 1992Assignee: American Cyanamid CompanyInventors: Allan Wissner, Robert E. Schaub, Kenneth E. Green, Philip R. Hamann
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Patent number: 5091550Abstract: 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: GrantFiled: April 20, 1990Date of Patent: February 25, 1992Assignee: Ciba-Geigy CorporationInventors: Robert A. Falk, Kirtland P. Clark
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Patent number: 5077329Abstract: 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: GrantFiled: April 6, 1990Date of Patent: December 31, 1991Assignee: Ciba-Geigy CorporationInventors: Stephen D. Pastor, Ramanathan Ravichandran
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Patent number: 5055458Abstract: 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: GrantFiled: July 28, 1989Date of Patent: October 8, 1991Assignee: Beecham Group P.l.c.Inventors: Stuart Bailey, Michael R. Harnden
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Patent number: 5051413Abstract: 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: GrantFiled: December 18, 1989Date of Patent: September 24, 1991Assignee: Ciba-Geigy CorporationInventors: Christof Angst, Derek E. Brundish, John G. Dingwall, Graham E. Fagg, Hans Allgeier, Guido Bold, Rudolf Duthaler, Roland Heckendorn, Antonio Togni
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Patent number: 4908465Abstract: 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: GrantFiled: June 7, 1988Date of Patent: March 13, 1990Assignee: Ciba-Geigy CorporationInventors: John G. Dingwall, Josef Ehrenfreund, Roger G. Hall, James Jack
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Patent number: 4898944Abstract: 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: GrantFiled: October 27, 1988Date of Patent: February 6, 1990Assignee: Hoechst AktiengesellschaftInventors: Gunther Schwaiger, Hartmut Springer, Walter Helmling
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Patent number: 4897382Abstract: 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: GrantFiled: June 21, 1988Date of Patent: January 30, 1990Assignee: Fidia S.p.A.Inventors: Francesco della Valle, Aurelio Romeo
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Patent number: 4804654Abstract: Compounds of the formula ##STR1## wherein the symbols have assigned meanings, and their use as insecticides and/or miticides.Type: GrantFiled: March 4, 1987Date of Patent: February 14, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Mohamed A. H. Fahmy
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Patent number: 4772738Abstract: 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: GrantFiled: December 12, 1986Date of Patent: September 20, 1988Assignee: Ciba-Geigy CorporationInventors: John G. Dingwall, Josef Ehrenfreund, Roger G. Hall, James Jack
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Patent number: 4753972Abstract: 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: GrantFiled: July 24, 1987Date of Patent: June 28, 1988Assignee: Ciba-Geigy CorporationInventor: Ramanathan Ravichandran
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Patent number: 4652666Abstract: 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: GrantFiled: July 18, 1985Date of Patent: March 24, 1987Assignee: Hoechst AktiengesellschaftInventors: Heinz Kehne, Hilmar Mildenberger, Klaus Bauer, Hermann Bieringer