Sulfur Attached Directly To The Phosphorus By Nonionic Bonding Patents (Class 562/9)
  • Patent number: 9228142
    Abstract: 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: Grant
    Filed: April 3, 2008
    Date of Patent: January 5, 2016
    Assignee: Dorf Ketal Chemicals (I) Private Limited
    Inventor: Mahesh Subramaniyam
  • Patent number: 9115319
    Abstract: 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: Grant
    Filed: September 12, 2008
    Date of Patent: August 25, 2015
    Assignee: Dorf Ketal Chemicals (I) Private Limited
    Inventor: Mahesh Subramaniyam
  • Patent number: 8940927
    Abstract: 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: Grant
    Filed: May 25, 2011
    Date of Patent: January 27, 2015
    Assignee: Metabasis Therapeutics, Inc.
    Inventors: Feng Tian, Qun Dang, G. Sridhar Prasad, Wenyu Li, Brett C. Bookser, Nicholas Brian Raffaele, Mark D. Erion
  • Patent number: 8871693
    Abstract: 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: Grant
    Filed: August 26, 2009
    Date of Patent: October 28, 2014
    Assignee: GasFrac Energy Services Inc.
    Inventors: Shaun T. Mesher, Chris Collett
  • Patent number: 8796487
    Abstract: 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: Grant
    Filed: June 8, 2009
    Date of Patent: August 5, 2014
    Assignee: Rhodia Operations
    Inventors: Leo Zhaoqing Liu, Gary Woodward
  • Patent number: 8673882
    Abstract: Stabilized benzyl phosphonic acid and naphthyl phosphonic acid analog compounds are effective in inhibiting the activity of autotaxin.
    Type: Grant
    Filed: January 19, 2012
    Date of Patent: March 18, 2014
    Assignee: University of Tennessee Research Foundation
    Inventors: Renuka Gupte, Renukadevi Patil, Gabor Tigyi, Duane D. Miller
  • Patent number: 8501985
    Abstract: The object of the present invention is the use of phosphonium salts in coupling reactions, and a method for their preparation.
    Type: Grant
    Filed: July 25, 2008
    Date of Patent: August 6, 2013
    Assignee: Dynamit Nobel GmbH Explosivstoff-und Systemtechnik
    Inventors: Klemenz Kromm, Jan Haller
  • Patent number: 8283453
    Abstract: 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: Grant
    Filed: August 14, 2009
    Date of Patent: October 9, 2012
    Assignee: International Business Machines Corporation
    Inventors: Ali Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
  • Publication number: 20110143971
    Abstract: 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: Application
    Filed: August 26, 2009
    Publication date: June 16, 2011
    Applicant: GASFRAC ENERGY SERVICES INC.
    Inventors: Shaun T. Mesher, Chris Collett
  • Publication number: 20100190753
    Abstract: Methods, compounds, pharmaceutical compositions and kits are described for treating or preventing amyloid-+related disease.
    Type: Application
    Filed: August 27, 2009
    Publication date: July 29, 2010
    Applicant: BELLUS Health (International) Limited
    Inventors: Xianqi KONG, Walter A. Szarek, Francine Gervais
  • Publication number: 20100145034
    Abstract: 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: Application
    Filed: August 14, 2009
    Publication date: June 10, 2010
    Applicant: INTERNATIONAL BUSINESS MACHINES CORPORATION
    Inventors: Alina Afzali-Ardakani, Phaedon Avouris, James B. Hannon, Christian Klinke
  • Publication number: 20100137258
    Abstract: 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: Application
    Filed: August 1, 2008
    Publication date: June 3, 2010
    Inventors: Francine Acher, Chelliah Selvam, Jean-Philippe Pin
  • Publication number: 20100094042
    Abstract: 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: Application
    Filed: September 21, 2005
    Publication date: April 15, 2010
    Inventors: John R. Klaehn, Mason K. Harrup, Jack D. Law, Dean R. Peterman
  • Publication number: 20090253931
    Abstract: 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: Application
    Filed: June 8, 2009
    Publication date: October 8, 2009
    Inventors: Leo Zhaoqing Liu, Gary Woodward
  • Publication number: 20090239817
    Abstract: 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: Application
    Filed: April 16, 2007
    Publication date: September 24, 2009
    Applicant: Goverment of the United States of America, as Represented by the Secretary, Dept of Health
    Inventors: Dale M. Walker, Vernon E. Walker, Miriam C. Poirier, Gene M. Shearer
  • Patent number: 7572931
    Abstract: 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: Grant
    Filed: October 25, 2007
    Date of Patent: August 11, 2009
    Assignee: Rhodia Inc.
    Inventors: Leo Zhaoqing Liu, Gary Woodward
  • Publication number: 20090137531
    Abstract: 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: Application
    Filed: December 6, 2005
    Publication date: May 28, 2009
    Inventors: Kevin R. Lynch, Timothy L. MacDonald, Jeremy J. Clemens, Michael D. Davis
  • Publication number: 20080319216
    Abstract: There is disclosed a salt of a sulfur-containing, phosphorus-containing compound. There is also disclosed a method of making the salt.
    Type: Application
    Filed: September 3, 2008
    Publication date: December 25, 2008
    Inventors: David J. DeGonia, Roger M. Sheets, Ronald L. Phillips
  • Patent number: 7368596
    Abstract: 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: Grant
    Filed: November 6, 2003
    Date of Patent: May 6, 2008
    Assignee: Afton Chemical Corporation
    Inventors: Paul M. Thomson, Peter Growcott, Roger M. Sheets, Abbas Kadkhodayan, Christopher James Dudding
  • Publication number: 20080103330
    Abstract: 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: Application
    Filed: October 25, 2007
    Publication date: May 1, 2008
    Inventors: Leo Zhaoqing Liu, Gary Woodward
  • Patent number: 7081544
    Abstract: The invention relates to novel chiral ligands of formula (I), the production thereof and the use of the same in catalytic reactions.
    Type: Grant
    Filed: June 18, 2002
    Date of Patent: July 25, 2006
    Assignee: Degussa AG
    Inventors: Matthias Beller, Kathrin Junge, Axel Monsees, Thomas Riermeier, Harald Trauthwein
  • Patent number: 6943267
    Abstract: 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: Grant
    Filed: January 16, 2003
    Date of Patent: September 13, 2005
    Assignee: Utah State University
    Inventors: Alvan Carl Hengge, Krzysztof Jerzy Swierczek
  • Publication number: 20040249184
    Abstract: The invention relates to novel chiral ligands of formula (I), the production thereof and the use of the same in catalytic reactions.
    Type: Application
    Filed: April 8, 2004
    Publication date: December 9, 2004
    Inventors: Matthias Beller, Kathrin Junge, Axel Monsees, Thomas Riermeier, Harald Trauthwein
  • Publication number: 20040133030
    Abstract: 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: Application
    Filed: August 21, 2003
    Publication date: July 8, 2004
    Inventors: E Premkumar Reddy, M V Ramana Reddy
  • Publication number: 20040106823
    Abstract: 1
    Type: Application
    Filed: September 25, 2003
    Publication date: June 3, 2004
    Inventors: Allan James Roberstson, Kenneth Richard Seddon
  • Publication number: 20030194162
    Abstract: Compounds of formula (I), methods of making and method of using (including optical compositions and devices) are provided.
    Type: Application
    Filed: August 26, 2002
    Publication date: October 16, 2003
    Inventors: Robert M. Mininni, Yousef Mohajer, Anthony Garito, Anna A. Panackal, Joseph Virgilo
  • Publication number: 20030189193
    Abstract: Compounds of formula (I), methods of making and method of using (including optical compositions and devices) are provided.
    Type: Application
    Filed: August 26, 2002
    Publication date: October 9, 2003
    Inventors: Robert M. Mininni, Yousef Mohajer, Anthony Garito, Anna A. Panackal, Joseph A. Virgilio
  • Publication number: 20030176721
    Abstract: 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: Application
    Filed: November 21, 2002
    Publication date: September 18, 2003
    Inventors: Kai Fabian, Steffen Enke, Herbert Tilly
  • Publication number: 20030153784
    Abstract: 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: 1
    Type: Application
    Filed: February 25, 2003
    Publication date: August 14, 2003
    Inventors: Fabio Giannessi, Natalina Dell'uomo, Maria Ornella Tinti, Francesco De Angelis
  • Patent number: 6291705
    Abstract: 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: Grant
    Filed: March 24, 2000
    Date of Patent: September 18, 2001
    Assignee: Commodore Separation Technologies, Inc.
    Inventors: W. S. Winston Ho, Bing Wang
  • Patent number: 6022991
    Abstract: 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: Grant
    Filed: December 8, 1998
    Date of Patent: February 8, 2000
    Assignees: Cytec Technology Corp., Compagnie des Mines de Xere (CMX)
    Inventors: Jean-Jacques Robert Perraud, Dennis Frederick Colton, Jean Paul Duterque, Yoshiaki Okita
  • Patent number: 5872279
    Abstract: 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: Grant
    Filed: March 19, 1998
    Date of Patent: February 16, 1999
    Assignee: Nippon Chemical Industrial Co., Ltd.
    Inventors: Masashi Sugiya, Tsutomu Watanabe, Kaoru Takeuchi
  • Patent number: 5707979
    Abstract: 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: Grant
    Filed: June 28, 1995
    Date of Patent: January 13, 1998
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Anuschirwan Peyman, Wilhelm Stahl, Karl-Heinz Budt, Dieter Ruppert, Henning Schussler, Konrad Wagner
  • Patent number: 5635608
    Abstract: 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: Grant
    Filed: November 8, 1994
    Date of Patent: June 3, 1997
    Assignee: Molecular Probes, Inc.
    Inventors: Richard P. Haugland, Kyle R. Gee
  • Patent number: 5571937
    Abstract: 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: Grant
    Filed: May 13, 1994
    Date of Patent: November 5, 1996
    Assignees: Sloan-Kettering Institute for Cancer Research, ZW Biomedical Research AG
    Inventors: Kyoichi A. Watanabe, Wu-Yun Ren, Roger Weil
  • Patent number: 5510510
    Abstract: 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: Grant
    Filed: June 28, 1994
    Date of Patent: April 23, 1996
    Assignee: Bristol-Meyers Squibb Company
    Inventors: Dinesh V. Patel, Scott A. Biller
  • Patent number: 5434288
    Abstract: 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: Grant
    Filed: June 14, 1994
    Date of Patent: July 18, 1995
    Assignee: Monsanto Company
    Inventor: Patrick J. Lennon
  • Patent number: 5212164
    Abstract: 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: Grant
    Filed: March 29, 1990
    Date of Patent: May 18, 1993
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Scott A. Biller, Michael J. Sofia
  • Patent number: 5177240
    Abstract: 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: Grant
    Filed: December 31, 1990
    Date of Patent: January 5, 1993
    Assignee: G. D. Searle & Co.
    Inventors: Alexis A. Cordi, Michael L. Vazquez
  • Patent number: 5100654
    Abstract: 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: Grant
    Filed: April 7, 1989
    Date of Patent: March 31, 1992
    Assignee: Yale University
    Inventors: John M. Pawelek, Michael P. Osber
  • Patent number: 5072032
    Abstract: 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: Grant
    Filed: June 21, 1989
    Date of Patent: December 10, 1991
    Inventor: Charles E. McKenna