Sulfur Attached Directly To The Phosphorus By Nonionic Bonding Patents (Class 562/9)
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Patent number: 9228142Abstract: The present invention relates to the field of processing hydrocarbons which causes corrosion in the metal surfaces of processing units. The invention addresses the technical problem of high temperature naphthenic acid corrosion and sulphur corrosion and provides a solution to inhibit these types of corrosion. The three combination compositions are formed by three mixtures separately, with one mixture obtained by mixing compound A, which is obtained by reacting high reactive polyisobutylene (HRPIB) with phosphorous pentasulphide in presence of catalytic amount of sulphur with compound B such as trialkyl phosphate and second mixture obtained by mixing compound A with compound C such as phosphite like di-isodecyl phenyl phosphite, and third mixture obtained by mixing compound A with compound D such as a phosphonate, wherein each of these three mixtures independently provide high corrosion inhibition efficiency in case of high temperature naphthenic acid corrosion inhibition and sulphur corrosion inhibition.Type: GrantFiled: April 3, 2008Date of Patent: January 5, 2016Assignee: Dorf Ketal Chemicals (I) Private LimitedInventor: Mahesh Subramaniyam
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Patent number: 9115319Abstract: The present invention relates to the field of processing hydrocarbons which causes corrosion in the metal surfaces of processing units. The invention addresses the technical problem of high temperature naphthenic acid corrosion and sulphur corrosion and provides a solution to inhibit these types of corrosion. The three combination compositions are formed by two mixtures separately, with one mixture obtained by mixing compound A, which is obtained by reacting high reactive polyisobutylene (HRPIB) with phosphorous pentasulphide in presence of catalytic amount of sulphur with compound B which is thiophosphorous compound such as phosphorous thioacid ester of Formula (1) and second mixture obtained by mixing compound A with compound C of Formula (2) which is obtained by reacting compound B with ethylene oxide, wherein each of these two mixtures independently provide high corrosion inhibition efficiency in case of high temperature naphthenic acid corrosion inhibition and sulphur corrosion inhibition.Type: GrantFiled: September 12, 2008Date of Patent: August 25, 2015Assignee: Dorf Ketal Chemicals (I) Private LimitedInventor: Mahesh Subramaniyam
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Patent number: 8940927Abstract: The present invention provides for novel compounds of Formulas I and II and pharmaceutically acceptable salts and co-crystals thereof which have glucokinase activator activity. The present invention further provides for pharmaceutical compositions comprising the same as well as methods of treating, preventing, delaying the time to onset or reducing the risk for the development or progression of a disease or condition for which one or more glucokinase activator is indicated, including Type 1 and 2 diabetes, impaired glucose tolerance, insulin resistance and hyperglycemia. The present invention also provides for processes of making the compounds of Formulas I and II, including salts and co-crystals thereof, and pharmaceutical compositions comprising the same.Type: GrantFiled: May 25, 2011Date of Patent: January 27, 2015Assignee: Metabasis Therapeutics, Inc.Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
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Patent number: 8871693Abstract: A gelling agent for a hydrocarbon fracturing fluid is disclosed, comprising the general formula of: in which X is an OR1, NR1R2, or SR1 group, R1 is an organic group having 2-24 carbon atoms, and R2 is an organic group or a hydrogen. Y is an NR3R4 or SR3 group, R3 is an organic group having 2-24 carbon atoms, and R4 is an organic group or a hydrogen. A method of making a gelling agent for a hydrocarbon fracturing fluid is also disclosed. Phosphorus oxyhalide is reacted with a chemical reagent to produce substantially only diester phosphorus oxyhalide, the chemical reagent comprising at least one of an organic alcohol having 2-24 carbon atoms, an organic amine with an organic group having 2-24 carbon atoms, and an organic sulfide having 2-24 carbon atoms. The diester phosphorus oxyhalide is then hydrolyzed to produce diester phosphoric acid.Type: GrantFiled: August 26, 2009Date of Patent: October 28, 2014Assignee: GasFrac Energy Services Inc.Inventors: Shaun T. Mesher, Chris Collett
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Patent number: 8796487Abstract: An improved process for production of dialkyldithiophosphinic acid including sulfurizing a purified dialkylphosphinic acid by: reacting a hypophosphorous acid or salt with a stoichiometric excess of an alpha olefin in the presence of a free radical initiator to form a reaction product comprising monoalkylphosphinic acid and dialkylphosphinic acid; adding sufficient aqueous base to the reaction product to i) form the salts of the phosphinic acids, and ii) establish an aqueous phase and an organic phase, wherein a monoalkylphosphinic acid solubilizes into an aqueous phase; separating the organic phase from the aqueous phase; acidifying the organic phase and removing the olefin from the organic phase; isolating the purified dialkylphosphinic acid product; and sulfurizing the purified dialkylphosphinic acid product to form a dialkydithiophosphinic acid.Type: GrantFiled: June 8, 2009Date of Patent: August 5, 2014Assignee: Rhodia OperationsInventors: Leo Zhaoqing Liu, Gary Woodward
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Patent number: 8673882Abstract: Stabilized benzyl phosphonic acid and naphthyl phosphonic acid analog compounds are effective in inhibiting the activity of autotaxin.Type: GrantFiled: January 19, 2012Date of Patent: March 18, 2014Assignee: University of Tennessee Research FoundationInventors: Renuka Gupte, Renukadevi Patil, Gabor Tigyi, Duane D. Miller
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Patent number: 8501985Abstract: The object of the present invention is the use of phosphonium salts in coupling reactions, and a method for their preparation.Type: GrantFiled: July 25, 2008Date of Patent: August 6, 2013Assignee: Dynamit Nobel GmbH Explosivstoff-und SystemtechnikInventors: Klemenz Kromm, Jan Haller
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Patent number: 8283453Abstract: The present invention provides a method for selectively placing carbon nanotubes on a substrate surface by using functionalized carbon nanotubes having an organic compound that is covalently bonded to such carbon nanotubes. The organic compound comprises at least two functional groups, the first of which is capable of forming covalent bonds with carbon nanotubes, and the second of which is capable of selectively bonding metal oxides. Such functionalized carbon nanotubes are contacted with a substrate surface that has at least one portion containing a metal oxide. The second functional group of the organic compound selectively bonds to the metal oxide, so as to selectively place the functionalized carbon nanotubes on the at least one portion of the substrate surface that comprises the metal oxide.Type: GrantFiled: August 14, 2009Date of Patent: October 9, 2012Assignee: International Business Machines CorporationInventors: Ali Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
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Publication number: 20110143971Abstract: A gelling agent for a hydrocarbon fracturing fluid is disclosed, comprising the general formula of: in which X is an OR1, NR1R2, or SR1 group, R1 is an organic group having 2-24 carbon atoms, and R2 is an organic group or a hydrogen. Y is an NR3R4 or SR3 group, R3 is an organic group having 2-24 carbon atoms, and R4 is an organic group or a hydrogen. A method of making a gelling agent for a hydrocarbon fracturing fluid is also disclosed. Phosphorus oxyhalide is reacted with a chemical reagent to produce substantially only diester phosphorus oxyhalide, the chemical reagent comprising at least one of an organic alcohol having 2-24 carbon atoms, an organic amine with an organic group having 2-24 carbon atoms, and an organic sulfide having 2-24 carbon atoms. The diester phosphorus oxyhalide is then hydrolyzed to produce diester phosphoric acid.Type: ApplicationFiled: August 26, 2009Publication date: June 16, 2011Applicant: GASFRAC ENERGY SERVICES INC.Inventors: Shaun T. Mesher, Chris Collett
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Publication number: 20100190753Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.Type: ApplicationFiled: August 27, 2009Publication date: July 29, 2010Applicant: BELLUS Health (International) LimitedInventors: Xianqi KONG, Walter A. Szarek, Francine Gervais
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Publication number: 20100145034Abstract: The present invention provides a method for selectively placing carbon nanotubes on a substrate surface by using functionalized carbon nanotubes having an organic compound that is covalently bonded to such carbon nanotubes. The organic compound comprises at least two functional groups, the first of which is capable of forming covalent bonds with carbon nanotubes, and the second of which is capable of selectively bonding metal oxides. Such functionalized carbon nanotubes are contacted with a substrate surface that has at least one portion containing a metal oxide. The second functional group of the organic compound selectively bonds to the metal oxide, so as to selectively place the functionalized carbon nanotubes on the at least one portion of the substrate surface that comprises the metal oxide.Type: ApplicationFiled: August 14, 2009Publication date: June 10, 2010Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATIONInventors: Alina Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
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Publication number: 20100137258Abstract: The invention relates to thiophosphi(o)nic acid derivatives having formula (I) wherein. M is a [C(R3,R4)]n1-C(E,COOR1,N(H,Z)) group, or an optionally substituted Ar—CH(COOR1,N(H,Z)) group (Ar designating an aryl or an heteroaryl group), or an ?, ? cyclic aminoacid group such as, formula (II) or a ?, &ggr;-cyclic aminoacid group such as, formula (III).Type: ApplicationFiled: August 1, 2008Publication date: June 3, 2010Inventors: Francine Acher, Chelliah Selvam, Jean-Philippe Pin
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Publication number: 20100094042Abstract: An extraction agent for the separation of trivalent actinides from lanthanides in an acidic media and a method for forming same are described, and wherein the methodology produces a stable regiospecific and/or stereospecific dithiophosphinic acid that can operate in an acidic media having a pH of less than about 7.Type: ApplicationFiled: September 21, 2005Publication date: April 15, 2010Inventors: John R. Klaehn, Mason K. Harrup, Jack D. Law, Dean R. Peterman
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Publication number: 20090253931Abstract: An improved process for production of dialkyldithiophosphinic acid including sulfurizing a purified dialkylphosphinic acid by: reacting a hypophosphorous acid or salt with a stoichiometric excess of an alpha olefin in the presence of a free radical initiator to form a reaction product comprising monoalkylphosphinic acid and dialkylphosphinic acid; adding sufficient aqueous base to the reaction product to i) form the salts of the phosphinic acids, and ii) establish an aqueous phase and an organic phase, wherein a monoalkylphosphinic acid solubilizes into an aqueous phase; separating the organic phase from the aqueous phase; acidifying the organic phase and removing the olefin from the organic phase; isolating the purified dialkylphosphinic acid product; and sulfurizing the purified dialkylphosphinic acid product to form a dialkyldithiophosphinic acid.Type: ApplicationFiled: June 8, 2009Publication date: October 8, 2009Inventors: Leo Zhaoqing Liu, Gary Woodward
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Publication number: 20090239817Abstract: A method for the prevention or treatment of human immunodeficiency virus infection by administering an effective amount of amifostine, phosphonol, or similar compound to an individual in need is provided.Type: ApplicationFiled: April 16, 2007Publication date: September 24, 2009Applicant: Goverment of the United States of America, as Represented by the Secretary, Dept of HealthInventors: Dale M. Walker, Vernon E. Walker, Miriam C. Poirier, Gene M. Shearer
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Patent number: 7572931Abstract: An improved process for production of dialkyldithiophosphinic acid including sulfurizing a purified dialkylphosphinic acid by: reacting a hypophosphorous acid or salt with a stoichiometric excess of an alpha olefin in the presence of a free radical initiator to form a reaction product comprising monoalkylphosphinic acid and dialkylphosphinic acid; adding sufficient aqueous base to the reaction product to i) form the salts of the phosphinic acids, and ii) establish an aqueous phase and an organic phase, wherein a monoalkylphosphinic acid solubilizes into an aqueous phase; separating the organic phase from the aqueous phase; acidifying the organic phase and removing the olefin from the organic phase; isolating the purified dialkylphosphinic acid product; and sulfurizing the purified dialkylphosphinic acid product to form a dialkydithiophosphinic acid.Type: GrantFiled: October 25, 2007Date of Patent: August 11, 2009Assignee: Rhodia Inc.Inventors: Leo Zhaoqing Liu, Gary Woodward
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Publication number: 20090137531Abstract: The present invention provides compounds that have antagonist activity at the S1P1 and/or S1P3 receptors. These compounds have enhanced selectivity and potency at the S1P1 and/or S1P3 receptors.Type: ApplicationFiled: December 6, 2005Publication date: May 28, 2009Inventors: Kevin R. Lynch, Timothy L. MacDonald, Jeremy J. Clemens, Michael D. Davis
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Publication number: 20080319216Abstract: There is disclosed a salt of a sulfur-containing, phosphorus-containing compound. There is also disclosed a method of making the salt.Type: ApplicationFiled: September 3, 2008Publication date: December 25, 2008Inventors: David J. DeGonia, Roger M. Sheets, Ronald L. Phillips
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Process for producing zinc dialkyldithiophosphates exhibiting improved seal compatibility properties
Patent number: 7368596Abstract: In general terms, the present invention includes a process for producing a new zinc dialkyldithiophosphate (ZDDP) offering improved seal compatibility characteristics in engine and transmission oil packages. The present invention additionally includes zinc dialkyldithiophosphate produced in accordance with the disclosed methodologies, and oil additives, lubricants, and engines and transmission comprising the zinc dialkyldithiophosphate of the present invention.Type: GrantFiled: November 6, 2003Date of Patent: May 6, 2008Assignee: Afton Chemical CorporationInventors: Paul M. Thomson, Peter Growcott, Roger M. Sheets, Abbas Kadkhodayan, Christopher James Dudding -
Publication number: 20080103330Abstract: An improved process for production of dialkyldithiophosphinic acid including sulfurizing a purified dialkylphosphinic acid by: reacting a hypophosphorous acid or salt with a stoichiometric excess of an alpha olefin in the presence of a free radical initiator to form a reaction product comprising monoalkylphosphinic acid and dialkylphosphinic acid; adding sufficient aqueous base to the reaction product to i) form the salts of the phosphinic acids, and ii) establish an aqueous phase and an organic phase, wherein a monoalkylphosphinic acid solubilizes into an aqueous phase; separating the organic phase from the aqueous phase; acidifying the organic phase and removing the olefin from the organic phase; isolating the purified dialkylphosphinic acid product; and sulfurizing the purified dialkylphosphinic acid product to form a dialkydithiophosphinic acid.Type: ApplicationFiled: October 25, 2007Publication date: May 1, 2008Inventors: Leo Zhaoqing Liu, Gary Woodward
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Patent number: 7081544Abstract: The invention relates to novel chiral ligands of formula (I), the production thereof and the use of the same in catalytic reactions.Type: GrantFiled: June 18, 2002Date of Patent: July 25, 2006Assignee: Degussa AGInventors: Matthias Beller, Kathrin Junge, Axel Monsees, Thomas Riermeier, Harald Trauthwein
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Patent number: 6943267Abstract: Compounds of the general formula wherein R is selected from the group consisting essentially of hydrogen, methyl, ethyl, phenyl, a carboxyl, or naphthyl substituted or a carbonyl substituted, alkyl of from 3 to 20 carbon atoms, a mono, bi or tri cyclic aryl or substituted aryl for the inhibition of phosphatase enzymes, including metallophosphatases; and, novel methods for synthesizing such compounds. The methods of use include the administration of an effective amount of the compound to provide effective phosphatase inhibition and therapeutic use to treat or prevent certain diseases, which utilize specific phosphatase enzymes.Type: GrantFiled: January 16, 2003Date of Patent: September 13, 2005Assignee: Utah State UniversityInventors: Alvan Carl Hengge, Krzysztof Jerzy Swierczek
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Publication number: 20040249184Abstract: The invention relates to novel chiral ligands of formula (I), the production thereof and the use of the same in catalytic reactions.Type: ApplicationFiled: April 8, 2004Publication date: December 9, 2004Inventors: Matthias Beller, Kathrin Junge, Axel Monsees, Thomas Riermeier, Harald Trauthwein
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Publication number: 20040133030Abstract: Substituted (Z)-styrylbenzyl sulfones of the formulae (I, II, III, IV), pharmaceutically acceptable salts thereof, and compositions thereof are provided as cell antiproliferative agents, including, for example, anticancer agents.Type: ApplicationFiled: August 21, 2003Publication date: July 8, 2004Inventors: E Premkumar Reddy, M V Ramana Reddy
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Publication number: 20040106823Abstract: 1Type: ApplicationFiled: September 25, 2003Publication date: June 3, 2004Inventors: Allan James Roberstson, Kenneth Richard Seddon
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Publication number: 20030194162Abstract: Compounds of formula (I), methods of making and method of using (including optical compositions and devices) are provided.Type: ApplicationFiled: August 26, 2002Publication date: October 16, 2003Inventors: Robert M. Mininni, Yousef Mohajer, Anthony Garito, Anna A. Panackal, Joseph Virgilo
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Publication number: 20030189193Abstract: Compounds of formula (I), methods of making and method of using (including optical compositions and devices) are provided.Type: ApplicationFiled: August 26, 2002Publication date: October 9, 2003Inventors: Robert M. Mininni, Yousef Mohajer, Anthony Garito, Anna A. Panackal, Joseph A. Virgilio
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Publication number: 20030176721Abstract: The invention relates to a method for the production of trifluoroethoxy-substituted benzoic acids, by reaction of a corresponding halogenated benzoic acid with trifluoroethanol in the solvent tetrahydrofuran, in the presence of a base and a copper salt, followed by an acidic work-up.Type: ApplicationFiled: November 21, 2002Publication date: September 18, 2003Inventors: Kai Fabian, Steffen Enke, Herbert Tilly
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Publication number: 20030153784Abstract: A process is described for the preparation of R or S aminocarnitine, R or S phosphonium aminocarnitine and R and S 3,4 diaminobutanoic acid, and their derivatives with the following formula: 1Type: ApplicationFiled: February 25, 2003Publication date: August 14, 2003Inventors: Fabio Giannessi, Natalina Dell'uomo, Maria Ornella Tinti, Francesco De Angelis
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Patent number: 6291705Abstract: The present invention provides a novel class of extractants and a method of manufacture for the extractants. The extractants are useful for the removal and recovery of metals from waste waters and process streams. The removal process utilizes a combination of a supported liquid membrane (SLM) and a strip dispersion to improve extraction of the target species while increasing membrane stability and reducing processing costs. The new class of extractants include dialkyl phosphoric acids containing alkyl chains of at least 8-12 carbon atoms. The method of manufacture includes mixing phosphorus pentasulfide with an alcohol, followed by hydrolysis of the intermediate reactants with a mineral acid.Type: GrantFiled: March 24, 2000Date of Patent: September 18, 2001Assignee: Commodore Separation Technologies, Inc.Inventors: W. S. Winston Ho, Bing Wang
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Patent number: 6022991Abstract: This is a method of regenerating dithiophosphorus acids from disulfides containing sulfur--sulfur bonds, formed by oxidation of dithiophosphorus acids, such as sulfur--sulfur bonding of dithiophosphoric, dithiophosphonic and dithiophosphinic acids, in a solvent extraction organic phase in which the dithiophosphorus acid is dissolved in a diluent. This process reacts metal directly with the organic solution containing the disulfide to produce a metal loaded complex form of the regenerated dithiophosphorus extractant in the organic solution. This metal complex forms by direct reaction of the metal with the disulfides without requiring the presence or the formation of nascent or gaseous hydrogen. The organic solution containing the regenerated dithiophosphorus extractant can be either directly recycled into a solvent extraction circuit or recycled after the loaded metal is stripped.Type: GrantFiled: December 8, 1998Date of Patent: February 8, 2000Assignees: Cytec Technology Corp., Compagnie des Mines de Xere (CMX)Inventors: Jean-Jacques Robert Perraud, Dennis Frederick Colton, Jean Paul Duterque, Yoshiaki Okita
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Patent number: 5872279Abstract: A bis(1,1,3,3-tetramethylbutyl)phosphinic acid compound represented by the formula (1) and an extracting agent using the same for separating Co from an aged electroless Ni plating solution. A di(1,1,3,3-tetramethylbutyl)phosphine is produced by carrying out a reaction between phosphine and trimethylpentene in the presence of an organic solvent and a catalyst, then said phosphine is reacted with an oxidizing agent or sulfur to obtain the compound (1): ##STR1## (wherein X.sup.1 and X.sup.2 are O or S).Type: GrantFiled: March 19, 1998Date of Patent: February 16, 1999Assignee: Nippon Chemical Industrial Co., Ltd.Inventors: Masashi Sugiya, Tsutomu Watanabe, Kaoru Takeuchi
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Patent number: 5707979Abstract: Compounds of the formula I, ##STR1## in which the symbols or substituents A, B, D, D*, E and E* have the meanings given in the specification, inhibit aspartyl proteases and are suitable for controlling viral diseases.Type: GrantFiled: June 28, 1995Date of Patent: January 13, 1998Assignee: Hoechst AktiengesellschaftInventors: Anuschirwan Peyman, Wilhelm Stahl, Karl-Heinz Budt, Dieter Ruppert, Henning Schussler, Konrad Wagner
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Patent number: 5635608Abstract: The invention relates to caged compounds for the study of biological processes, where the caged compound has a photoremoveable .alpha.-carboxy-substituted o-nitrobenzyl group. Covalent attachment of the substituted o-nitrobenzyl to a parent compound yields a caged compound with biological and/or physical properties that are significantly altered from the original properties of the parent compound. Illumination of the caged compounds to cleave the photoremoveable group yields the parent compound with its original properties restored.Type: GrantFiled: November 8, 1994Date of Patent: June 3, 1997Assignee: Molecular Probes, Inc.Inventors: Richard P. Haugland, Kyle R. Gee
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Patent number: 5571937Abstract: This invention relates to new derivatized solid supports and compounds having the formula: ##STR1## wherein S may be a solid support; L may be a chemical bond or a suitable inorganic or organic linker; Z may be --SO.sub.2 -- or --S--S--; R may be --OH, an H-phosphonate, an alkanephosphonate, a phosphotriester, a phosphite triester, a phosphite diester, a phosphorothioate, a phosphorodithioate, a phosphoroamidate, a phosphoroamidite, --OR.sup.1 --SR.sup.1, a nucleotide, N, which may be substituted or modified in its sugar, phosphate or base or an oligonucleotide of the formula --(N).sub.g, --R.sup.2, wherein N is as defined above which may be the same or different; g is an integer from one to two hundred; R.sup.1 is a suitable protecting group; and R.sup.2 may be an H-phosphonate, an alkane-phosphonate, a phosphotriester, a phosphite triester, a phosphite diester, a phosphorothioate, a phosphorodithioate, a phosphoroamidate, a phosphoroamidite, --OH, --OR.sup.1, --SR.sup.1, or --O--P(OCH.sub.2 CH.sub.Type: GrantFiled: May 13, 1994Date of Patent: November 5, 1996Assignees: Sloan-Kettering Institute for Cancer Research, ZW Biomedical Research AGInventors: Kyoichi A. Watanabe, Wu-Yun Ren, Roger Weil
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Patent number: 5510510Abstract: Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, and inhibition of cholesterol biosynthesis, are effected by compounds of the formula ##STR1## their enantiomers, diastereomers, and pharmaceutically acceptable salts, prodrugs, and solvates, wherein:x is --ONR.sup.1 C(O)--, --N(OR.sup.1)C(O)--, --NR.sup.1 C(O)--, --C(O)NR.sup.1 --, --NR.sup.1 S(O.sub.2)--, --C(O)O--, --OC(O)--, --C(O)--, --O--, --NR.sup.1 -- or --(S).sub.q --;Y is --CO.sub.2 R.sup.2, --SO.sub.3 R.sup.2 or --P(O) (OR.sup.2) (R.sup.3);R is alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkenylene or aryl;R.sup.3 is --(O).sub.t R.sup.4 ;R.sup.1, R.sup.2 and R.sup.4 are each independently hydrogen, alkyl, aryl or aralkyl;m and n are each independently 0 or an integer from 1 to 5;p and t are each independently 0 or 1; andq is an integer from 1 to 2.Type: GrantFiled: June 28, 1994Date of Patent: April 23, 1996Assignee: Bristol-Meyers Squibb CompanyInventors: Dinesh V. Patel, Scott A. Biller
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Patent number: 5434288Abstract: PLA.sub.2 inhibitors selected from the group consisting of ##STR1## wherein A is selected from the group consisting of ##STR2## and Z, W, R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, R.sub.9, X, X' and Y are as defined herein.Type: GrantFiled: June 14, 1994Date of Patent: July 18, 1995Assignee: Monsanto CompanyInventor: Patrick J. Lennon
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Patent number: 5212164Abstract: Compounds which are inhibitors of cholesterol biosynthesis (by inhibiting de novo squalene biosynthesis), and thus are useful as hypocholesterolemic agents and antiatherosclerotic agents are provided which have the structure ##STR1## wherein m is 0, 1, 2 or 3; n is 0, 1, 2, 3 or 4;Y.sup.1 and Y.sup.2 are H or halogen;R.sup.2, R.sup.3 and R.sup.4 may be the same or different and are independently H, metal ion, C.sub.1 to C.sub.8 alkyl or C.sub.3 to C.sub.12 alkenyl;X is O, S, NH or NCH.sub.2 R.sup.15 wherein R.sup.15 is H or C.sub.1 to C.sub.5 alkyl; andR.sup.1 is R.sup.5 --Q.sup.1 --Q.sup.2 --Q.sup.3 -- wherein R.sup.5, Q.sup.1, Q.sup.2 and Q.sup.3 are as defined herein;and when m is o, X is other than S; and if m is o and X is 0, then n is 1, 2, 3 or 4; including all stereoisomers thereof.Type: GrantFiled: March 29, 1990Date of Patent: May 18, 1993Assignee: E. R. Squibb & Sons, Inc.Inventors: Scott A. Biller, Michael J. Sofia
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Patent number: 5177240Abstract: A class of phosphono-hydroisoquinoline compounds is described for treatment to reduce neurotoxic injury associated with anoxia or ischemia which typically follows stroke, cardiac arrest or perinatal asphyxia. The treatment includes administration of a phosphono-hydroisoquinoline compound alone or in a composition in an amount effective as an antagonist to inhibit excitotoxic actions at major neuronal excitatory amino acid receptor sites. Compounds of most interest are those of Formula I: ##STR1## wherein each of R.sup.1 through R.sup.4 is hydrido, wherein each of Z.sup.1 and Z.sup.2 is hydroxyl, wherein W is a single bond connecting the phosphorus atom with the aromatic ring and wherein the A ring is aromatic. Also disclosed are two classes of intermediate compounds having a fully unsaturated A ring, which intermediate compounds are useful in methods to make product compounds of Formula I.Type: GrantFiled: December 31, 1990Date of Patent: January 5, 1993Assignee: G. D. Searle & Co.Inventors: Alexis A. Cordi, Michael L. Vazquez
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Patent number: 5100654Abstract: A phosphorylated derivative of L-dopa of the formula ##STR1## wherein when X is ##STR2## wherein Z is --CH.sub.2, N, S or a linkage other than oxygen which renders the phosphate group resistant to hydrolysis by phosphatase enzymes in tissues and biological fluids,then Y is OQ, wherein Q is H or an alkyl with one to twelve carbon atoms, orwherein X is OQ, then Y is ##STR3## wherein R' is hydrogen or a pharmaceutically acceptable cation and R is a moiety which increases hydropobicity. The phosphorylated derivative of L-dopa is useful as an agent to increase the melanin content in mammalian skin and hair.Type: GrantFiled: April 7, 1989Date of Patent: March 31, 1992Assignee: Yale UniversityInventors: John M. Pawelek, Michael P. Osber
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Patent number: 5072032Abstract: Methods for converting phosphonates into thiophosphonates and specific thiophosphonate compounds so produced are disclosed and claimed. The methods start with a reaction mixture formed of a phosphonate compound, including one or more strong electron-withdrawing groups located adjacent to the phosphorus in the compound, a slight excess of Lawesson's reagent, and a polar aprotic solvent. The reaction mixture is heated until reaction is complete and may be followed with separation or hydrolyzation steps to produce thiophosphonic acids and their addition salts. One of these thio-analogues, thiophosphonoformic acid (TPFA) is particularly effective at inhibiting HIV replication and in treating mammals infected with HIV.Type: GrantFiled: June 21, 1989Date of Patent: December 10, 1991Inventor: Charles E. McKenna