Acyclic Patents (Class 564/240)
  • Patent number: 9161896
    Abstract: A cosmetic comprising the following components (A), (B), (C) and (D): (A) 0.001 to 50% by weight of an organic acid represented by a general formula (1), wherein R1 denotes a residue derived from a natural sterin having one hydroxy group or a hydrogenated product thereof, or a residue derived from bile acid in which the hydroxyl hydrogen atom is removed; R2 denotes a divalent hydrocarbon group having 1 to 24 carbon atoms; and M denotes a hydrogen atom, an alkali metal, an alkaline earth metal, ammonium, alkanolammonium having 2 to 9 carbon atoms in total, alkylammonium or alkenylammonium having 1 to 22 carbon atoms in total, a pyridinium substituted with an alkyl group or an alkenyl group having 1 to 18 carbon atoms, or a basic amino acid; (B) 0.001 to 20% by weight of a base; (C) 0.0001 to 50% by weight of a ceramide; and (D) water, and comprising, as a component (E), an acid other than the component (A) in a content satisfying a relationship: 0?(E)/(A)<0.2, and having pH of 6 to 11.
    Type: Grant
    Filed: December 28, 2011
    Date of Patent: October 20, 2015
    Assignee: KAO CORPORATION
    Inventor: Yumiko Yamamoto
  • Publication number: 20150136611
    Abstract: Reaction products of guanidine compounds or salts thereof, polyepoxide compounds and polyhalogen compounds may be used as levelers in metal electroplating baths, such as copper electroplating baths, to provide good throwing power. Such reaction products may plate with good surface properties of the metal deposits and good physical reliability.
    Type: Application
    Filed: November 21, 2013
    Publication date: May 21, 2015
    Inventors: Julia KOZHUKH, Zuhra I. NIAZIMBETOVA, Maria Anna RZEZNIK
  • Publication number: 20140256986
    Abstract: A chemical compound of creatinol sulfate is formed by chemically reacting N-methyl-amino-ethanol, cyanamide, with sulfuric acid to produce the creatinol sulfate with relatively higher yield rate and purity, wherein the mol ratio of N-methyl-amino-ethanol, sulfuric acid, and cyanamide is approximately 2:1:2.
    Type: Application
    Filed: March 9, 2013
    Publication date: September 11, 2014
    Inventor: Guoji Zhang
  • Patent number: 8785679
    Abstract: Hydrophilic, biocidal coating compositions and methods to make and use the compositions are disclosed. The coatings include compounds with quaternary amine polyethylene glycol groups and polyaminoalkyl biguanide groups as substituents. The compounds when incorporated in paints provide hydrophilic, self-cleaning and biocidal property to the coating.
    Type: Grant
    Filed: December 10, 2012
    Date of Patent: July 22, 2014
    Assignee: Empire Technology Development LLC
    Inventors: Glen Leon Brizius, Phillip Kent Montgomery
  • Publication number: 20140155654
    Abstract: Methods for forming spherical crystal habit are shown. A needle-shaped crystal habit, a solvent, and a surfactant are combined and dissolved forming a first solution. The first solution and an anti-solvent are combined forming a second solution. The second solution is cooled. Spherical crystal habit is formed.
    Type: Application
    Filed: March 6, 2013
    Publication date: June 5, 2014
    Applicant: Physical Sciences, Inc.
    Inventor: Physical Sciences, Inc.
  • Publication number: 20140051712
    Abstract: The invention describes pharmaceutical agents capable of crossing the blood brain barrier to protect against organophosphate pesticides and nerve agents or other electrophiles by reactivating inhibited cholinesterase (i.e., acetylcholinesterase and butyrylcholinesterase) and other proteins in the peripheral and central nervous system.
    Type: Application
    Filed: December 16, 2011
    Publication date: February 20, 2014
    Inventors: John R. Cashman, Jarosiaw Kalisiak
  • Publication number: 20130056676
    Abstract: A polarity swing-assisted regeneration (PSAR) process is disclosed for improving the efficiency of releasing gases chemically bound to switchable ionic liquids. Regeneration of the SWIL involves addition of a quantity of non-polar organic compound as an anti-solvent to destabilize the SWIL, which aids in release of the chemically bound gas. The PSAR decreases gas loading of a SWIL at a given temperature and increases the rate of gas release compared to heating in the absence of anti-solvent.
    Type: Application
    Filed: September 2, 2011
    Publication date: March 7, 2013
    Applicant: BATTELLE MEMORIAL INSTITUTE
    Inventors: David J. Heldebrant, Ward E. Tegrotenhuis, Charles J. Freeman, Michael L. Elliott, Phillip K. Koech, Paul H. Humble, Feng Zheng, Jian Zhang
  • Patent number: 8389768
    Abstract: Provided herein are novel cationic lipids, compositions comprising the cationic lipids, and methods of using the cationic lipids. In some claims, the cationic lipids have cytotoxic activity and can be used alone or in combination with a cytotoxic bioactive compound to kill a cell. In some of these claims, the cationic lipid enhances the cytotoxic activity of the cytotoxic bioactive compound. Methods for treating a subject afflicted with a disease or unwanted condition are provided, wherein the method comprises administering a delivery system comprising a novel cationic lipid to the subject. The invention further provides methods for making delivery systems comprising the novel cationic lipids of the invention.
    Type: Grant
    Filed: May 1, 2009
    Date of Patent: March 5, 2013
    Assignee: The University of North Carolina at Chapel Hill
    Inventors: Leaf Huang, Yunching Chen, Joyeeta Sen, Surendar Reddy Bathula, Sumio Chono, Shyh-Dar Li, Michael Hackett
  • Publication number: 20130046092
    Abstract: A solvent that reversibly converts from a nonionic liquid mixture to an ionic liquid upon contact with a selected trigger, e.g., contact with CO2, is described. In preferred embodiments, the ionic solvent is readily converted back to the nonionic liquid mixture. The nonionic liquid mixture includes an amidine or guanidine or both, and water, alcohol, or a combination thereof. Single component amine solvents that reversibly convert between ionic and non-ionic states are also described. Some embodiments require increased pressure to convert; others convert at 1 atmosphere.
    Type: Application
    Filed: June 29, 2011
    Publication date: February 21, 2013
    Applicants: QUEEN'S UNIVERSITY AT KINGSTON, GEORGIA TECH RESEARCH CORPORATION
    Inventors: Philip JESSOP, Charles ECKERT, Charles LIOTTA, David HELDEBRANT
  • Patent number: 8318676
    Abstract: The invention relates to the use of creatine, creatinine and/or derivatives thereof and/or their salts in an agent for hardening, strengthening, restructuring or increasing the shine, volume or combability of keratin fibers, particularly of human hair.
    Type: Grant
    Filed: August 16, 2007
    Date of Patent: November 27, 2012
    Assignee: Wella AG
    Inventors: Rudolf Bimczok, Thomas Kripp, Beate Grasser, Christian Springob
  • Publication number: 20120172220
    Abstract: The present invention provides N-phosphonomethylglycine guanidine salts. The N-phosphonomethylglycine guanidine salts have improved herbicidal efficacy over glyphosate alone. The present invention also provides guanidine compounds and salts thereof.
    Type: Application
    Filed: June 24, 2010
    Publication date: July 5, 2012
    Applicants: FLAMEL TECHNOLOGIES S.A., MONSANTO TECHNOLOGY LLC
    Inventors: Ronald J. Brinker, Olivier Soula, Alain Lemercier
  • Publication number: 20120134948
    Abstract: The present invention relates to the use of at least one ether guanidine of the general formula (I) and/or of a salt or hydrate thereof, in which R1?—CH2—CH2—CH2—O—R3, where R3 is a linear or branched hydrocarbon radical having 6 to 22 carbon atoms, and R2?H or an optionally branched hydrocarbon radical which has 1 to 22 C atoms and which optionally comprises double bonds, for reducing the growth of microorganisms, and to cosmetic and pharmaceutical formulations comprising at least one ether guanidine of the general formulae (I).
    Type: Application
    Filed: July 19, 2010
    Publication date: May 31, 2012
    Applicant: EVONIK GOLDSCHMIDT GMBH
    Inventors: Oliver Springer, Peter Muss, Peter Lersch, Ursula Maczkiewitz, Mike Farwick
  • Publication number: 20120116076
    Abstract: A solvent that reversibly converts from a nonionic liquid mixture to an ionic liquid upon contact with a selected trigger, e.g., contact with CO2, is described. In preferred embodiments, the ionic solvent is readily converted back to the nonionic liquid mixture. The nonionic liquid mixture includes an amidine or guanidine or both, and water, alcohol, or a combination thereof. Single component amine solvents that reversibly convert between ionic and non-ionic states are also described. Some embodiments require increased pressure to convert; others convert at 1 atmosphere.
    Type: Application
    Filed: June 29, 2011
    Publication date: May 10, 2012
    Applicants: GEORGIA TECH RESEARCH CORPORATION, QUEEN'S UNIVERSITY AT KINGSTON
    Inventors: Philip G. JESSOP, Charles A. ECKERT, Charles L. LIOTTA, David J. HELDEBRANT
  • Publication number: 20120035268
    Abstract: The presently disclosed subject matter provides compounds of the formula: (1) and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, and R8 are as defined herein. Also disclosed are methods for making the compounds of the formula as set forth hereinabove, their use in inhibiting sphingosine kinase, and their use in the treatment and/or prevention of diseases and/or conditions associated with undesirable ceramidase or sphingosine kinase activity, including, but not limit cancer, cancer metastasis, atherosclerosis, stenosis, inflammation, immunological disorders, asthma, atopic dermatitis, wound healing, and other proliferative diseases.
    Type: Application
    Filed: December 28, 2009
    Publication date: February 9, 2012
    Inventors: Zdzislaw M. Szulc, Alicja Bielawska, Lina M. Obeld, Yusuf A. Hannun, James Norris, Liu Xiang
  • Patent number: 8084502
    Abstract: A use method of agmatine or a pharmaceutically allowable salt thereof, and a pharmaceutical composition comprising the same are disclosed. The method and pharmaceutical composition of the present invention can effectively cure or prevent eye diseases preferably including glaucoma, retinopathy, and optic neuropathy associated with apoptosis in retinal ganglion cells (RGCs), particularly hypoxia-induced or tumor necrosis factor-? (TNF-?)-induced apoptosis.
    Type: Grant
    Filed: April 3, 2008
    Date of Patent: December 27, 2011
    Inventors: Gong Je Seong, Chan Yun Kim, Jong Eun Lee, Samin Hong
  • Publication number: 20110311583
    Abstract: (A1) Translate this text The present invention provides lipids that are advantageously used in lipid particles for the in vivo delivery of therapeutic agents to cells.
    Type: Application
    Filed: November 10, 2009
    Publication date: December 22, 2011
    Applicant: ALNYLAM PHARMACEUTICALS, INC.
    Inventors: Muthiah Manoharan, kallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Jayaprakash K. Narayanannair, Martin Maier, Laxman Eltepu
  • Patent number: 8063106
    Abstract: The invention provides low molecular weight apoE mimetic agents suitable for preparing a medicament to treat autoimmune, inflammatory or neurodegenerative disease, (X)a-L-(X)b(Formula (I)) wherein each X is a (potentially different) chemical moiety bearing a positive charge at physiological pH a and b are, independently, numbers between 3 and 6; and L is a linker.
    Type: Grant
    Filed: August 9, 2006
    Date of Patent: November 22, 2011
    Assignee: TCP Innovations Limited
    Inventors: David J. Grainger, David John Fox
  • Publication number: 20110117219
    Abstract: The invention relates to ether guanidines of the general formulae (I) and/or salts or hydrates thereof, in which R1=—CH2—CH2—CH2—O—R3 where R3 is, independently of the others, hydrocarbon radicals having greater than or equal to 10 carbon atoms, where part of the ether guanidines has radicals R3 which are branched and part of the ether guanidines has radicals R3 which are unbranched, and R2=independently of the others H or an optionally branched, optionally double-bond-containing hydrocarbon radical having 1 to 30 carbon atoms, and use thereof in hair treatment compositions and hair aftertreatment compositions, in particular for preventing damage by chemical treatment compositions and for repairing hair which is already damaged.
    Type: Application
    Filed: May 28, 2009
    Publication date: May 19, 2011
    Applicant: EVONIK GOLDSCHMIDT GMBH
    Inventors: Oliver Springer, Peter Muss, Burghard Gruening, Ursula Maczkiewitz, Mike Farwick, Peter Lersch
  • Publication number: 20110098392
    Abstract: The present invention relates to an organopolysiloxane composition that can be vulcanized at room temperature into an elastomer that is crosslinked by polycondensation and that does not contain alkyltin-based catalysts which exhibit toxicity problems. The invention also relates to novel polycondensation catalysts having a guanidine structure, in silicone chemistry, and to the uses thereof as catalysts for the organopolysiloxane polycondensation reaction.
    Type: Application
    Filed: March 24, 2009
    Publication date: April 28, 2011
    Applicant: BLUESTAR SILICONES FRANCE
    Inventors: Georges Barrandon, Delphine Blanc, Christian Maliverney, Hervé Parisot
  • Publication number: 20110034698
    Abstract: The present invention relates to oxonium salts having [(Ro)3O]+ cations and sulfonium salts having [(Ro)3S]+ cations, where Ro denotes straight-chain or branched alkyl groups having 1-8 C atoms or phenyl which is unsubstituted or substituted by Ro, ORo, N(Ro)2, CN or halogen, and anions selected from the group of [PFx(CyF2y+1?xHz)6?x]? anions, where 2?x?5, 1?y?8 and 0?z?2y+1, or anions selected from the group of [BFn(CN)4?n]? anions, where n=0, 1, 2 or 3, or anions selected from the group of [(Rf1SO2)2N]9? anions or anions selected from the group of [BFWRf24?w]? anions, to processes for the preparation thereof, and to the use thereof, in particular for the preparation of ionic liquids.
    Type: Application
    Filed: October 20, 2010
    Publication date: February 10, 2011
    Inventors: Nikolai(Mykola) Ignatyev, German Bissky, Helge Willner
  • Patent number: 7771611
    Abstract: Novel compositions are provided containing a compound represented by the formula YOSF5 or ZOSF5, where: (a) Y is: (i) an organic cation other than (Me2N)3S+ or (ii) an inorganic cation, provided that when Y is the inorganic cation, the composition further includes a complexing agent; and (b) Z is C1-20 alkyl, aryl, cycloalkyl, combinations thereof, or analogues thereof containing at least one heteroatom, provided that the compound represented by the formula ZOSF5 is a molecular compound. Processes of making the cationic compounds are disclosed as are processes for using the compositions containing cationic compounds in nucleophilic replacement reactions to prepare the compositions containing molecular compounds including the OSF5 group.
    Type: Grant
    Filed: July 10, 2006
    Date of Patent: August 10, 2010
    Assignee: Air Products and Chemicals, Inc.
    Inventors: Robert George Syvret, Gauri Sankar Lal, Kristen Elaine Minnich
  • Publication number: 20100172890
    Abstract: The invention is dietary supplements, nutraceutical compositions, medical foods, and animal feeds that have cytoprotective (cell and tissue protection) and health promoting effects. The compositions contain a high dose range of agmatine and nutraceutical acceptable salts thereof as dietary fortification for providing effective long-term cytoprotection and affording for soft stool. The compositions may contain agmatine alone or in combination with other dietary ingredients having health promoting effects. The compositions can be prepared with dietary accepted excipients and compatible forms of carriers, including but not limited to, powders, tablets, capsules, controlled release carriers, lozenges and chewable preparations, liquid suspensions, suspensions in an edible supporting matrix or foodstuff and oral rehydration solutions, to enable consumption of said compositions.
    Type: Application
    Filed: February 1, 2010
    Publication date: July 8, 2010
    Inventors: Gad Gilad, Varda Gilad
  • Publication number: 20100130783
    Abstract: A use method of agmatine or a pharmaceutically allowable salt thereof, and a pharmaceutical composition comprising the same are disclosed. The method and pharmaceutical composition of the present invention can effectively cure or prevent eye diseases preferably including glaucoma, retinopathy, and optic neuropathy associated with apoptosis in retinal ganglion cells (RGCs), particularly hypoxia-induced or tumor necrosis factor-? (TNF-?)-induced apoptosis.
    Type: Application
    Filed: April 3, 2008
    Publication date: May 27, 2010
    Inventors: Gong Je Seong, Chan Yun Kim, Jong Eun Lee, Samin Hong
  • Publication number: 20090253912
    Abstract: The invention relates to a method for producing onium salts with tetrafluoroborate anion by reacting an onium halide with an oxonium tetrafluoroborate, sulfonium tetrafluoroborate, or triphenylcarbonium tetrafluoroborate.
    Type: Application
    Filed: November 18, 2005
    Publication date: October 8, 2009
    Inventors: Nikolai (Mykola) Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
  • Publication number: 20090076110
    Abstract: An Amino Acid Compound is described. The Amino Acid Compound may comprise an Amino Acid and one of a Nitrate and a Nitrite. The Amino Acid may be one of Agmatine, Arginine, Beta Alanine, Citrulline, Creatine, Glutamine, L-Histidine, Isoleucine, Leucine, Norvaline, Ornithine, and Valine.
    Type: Application
    Filed: December 4, 2007
    Publication date: March 19, 2009
    Inventors: Ronald Kramer, Alexander Nikolaidis
  • Patent number: 7470815
    Abstract: Peptidomimetic compositions for selective inhibition of neuronal nitric oxide synthase.
    Type: Grant
    Filed: January 26, 2006
    Date of Patent: December 30, 2008
    Assignee: Northwestern University
    Inventors: Richard B. Silverman, Jung-Mi Hah, Jose Antonio Gomez Vidal, Erik Erdal
  • Publication number: 20080247991
    Abstract: In part, the present invention relates to a compound or polymer comprising a non-protein-binding moiety and at least one protein-binding group. The present invention relates to a method of screening compounds or polymers for the property of inhibiting protein aggregation in solution, a method of preparing a compound or polymer having the property of protein aggregation inhibition in solution, a method of classifying a compound or polymer as either inhibitory of protein aggregation in solution or not inhibitory of protein aggregation in solution, and to a method of determining the preferential binding coefficient, ?XP, of an additive in a protein solution. The present invention also relates to a method of suppressing or preventing aggregation of a protein in solution, a method of decreasing the toxicological risk associated with administering a protein to a mammal in need thereof, and a method of facilitating native folding of a recombinant protein in solution.
    Type: Application
    Filed: February 28, 2005
    Publication date: October 9, 2008
    Inventors: Bernhardt L. Trout, Daniel I.C. Wang, Brian M. Baynes
  • Patent number: 7078566
    Abstract: This invention relates to salts of guanidine derivatives of formula R—X—C(?NH)NH3+Z?, wherein X represents a valence bond, —CH2—NH—, —CH2—NH—NH— or —CH?N—NH—; R represents a linear or branched C1–C30 alkyl, C3–C20 cycloalkyl, adamantyl, norbornyl, tricyclodecyl, benzyl, furyl, pyridyl, anthracyl, naphthyl, phenanthryl, perinaphthyl or quinuclidinyl residue, which can be substituted by one or more hydroxyl groups, C1–C4 alkoxy groups, C1–C4 alkyl groups and/or one or more halogen atoms or one or more amino groups; Z represents O—CO—Y, O—S(O)2—Y, or O—P(O)(OH)—Y; and Y represents a linear or branched C1–C12 alkyl, C3–C8 cycloalkyl, benzyl, furyl or pyridyl residue, which can be substituted by one or more hydroxyl groups, carboxylic acid groups, C1–C4 alkoxy groups, C1–C4 alkyl groups and/or one or more halogen atoms or one or more amino groups. These compounds are useful for treating tumor diseases, autoimmune diseases, cardiovascular diseases, infections, and viral diseases.
    Type: Grant
    Filed: April 8, 2004
    Date of Patent: July 18, 2006
    Assignee: Biosphinks Aktiengesellschaft
    Inventor: Eberhard Amtmann
  • Patent number: 6960689
    Abstract: A synthesis method which comprises reacting NH group-containing compounds with thiocyanates, cyanamides, nitrites or esters in the presence of a silylating agent to synthesize the corresponding nitrogen-containing addition or substitution products. This method not only enables the direct and efficient synthesis of nitrogen-containing compounds including isothioureas, guanidines, amidines and amides, but it also has a wide range of applications and is suitable for large-scale synthesis.
    Type: Grant
    Filed: October 1, 2004
    Date of Patent: November 1, 2005
    Assignee: Chugai Seiyaku Kabushiki Kaisha
    Inventors: Takashi Emura, Tsuyoshi Haneishi
  • Publication number: 20030163000
    Abstract: An essentially anhydrous agitated mixture of (i) finely-divided essentially anhydrous alkali metal fluoride (e.g., KF), (ii) haloaromatic compound having at least one halogen atom of atomic number greater than 9 on an aromatic ring (e.g., C6Cl6), and (iii) an organo guanidinium salt catalyst (e.g., [(Et2N)2CNEt2]Br), is heated at a temperature at which fluorine replaces one or more of the ring halogen atoms of the haloaromatic compound. A new synthetic route to hexahydrocarbyl guanidinium salts is also described.
    Type: Application
    Filed: August 21, 2002
    Publication date: August 28, 2003
    Inventors: Brian Atkinson, Victor Lebedev
  • Patent number: 6570038
    Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts for the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.
    Type: Grant
    Filed: June 9, 2000
    Date of Patent: May 27, 2003
    Inventors: Joseph John Caringi, Peter David Phelps, Thomas Link Guggenheim, Daniel Joseph Brunelle
  • Patent number: 6492376
    Abstract: This invention is directed to poly-hydroxylated monocyclic N-heterocyclic derivatives selected from the following formulae: wherein Z1, Z2, R1, R2, R3, R4, R5, R6, and R7 are defined herein. These compounds are useful as anti-coagulants.
    Type: Grant
    Filed: May 4, 2001
    Date of Patent: December 10, 2002
    Assignee: Berlex Laboratories, Inc.
    Inventor: Gary B. Phillips
  • Patent number: 6258976
    Abstract: Disclosed are processes for the preparation of compounds of the formula (I): H2N—(CH2)n—A—(CH2)m—NH2, or (II): H2N—(CH2)n—NH—C(═NR1)—NH—(CH2)m—NH2, wherein n and m are each independently an integer from 2 to 8; A is selected from the group consisting of —NR1—, —NR1—(CH2)r—NR1— and —NR1—(CH2)r—NR1—(CH2)z—NR1—, wherein r and z are an integer ranging from 2 to 8; and R1 is hydrogen or a protecting group having a carbonyl group.
    Type: Grant
    Filed: March 19, 1999
    Date of Patent: July 10, 2001
    Inventors: Francis Johnson, Ramesh C. Gupta
  • Patent number: 6251948
    Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 26, 2001
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 6235934
    Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts for the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.
    Type: Grant
    Filed: December 17, 1998
    Date of Patent: May 22, 2001
    Assignee: General Electric Company
    Inventors: Joseph John Caringi, Gary Ray Faler, Peter David Phelps, Thomas Link Guggenheim, Larry Ivis Flowers, Daniel Joseph Brunelle, Roy Ray Odle
  • Patent number: 6187955
    Abstract: A guanidine derivative represented by formula (1), (2), (3) or its acid addition salt and a production process thereof wherein each of A and B is a C2-C8 alkylene, D is a single bond, —CO— or a C1-C6 alkylene, E is H, a lower alkyl or the like, m is 1 to 6, n is 0 to 6 and R1 is H, a lower alkyl or the like, 1 is 1 to 10 and G is H, —OH or the like and a skin cosmetic containing the same. It can exert excellent keratin layer softening effect continuously for a long period of time.
    Type: Grant
    Filed: November 6, 1997
    Date of Patent: February 13, 2001
    Assignee: Kao Corporation
    Inventors: Minoru Nagai, Hiromitsu Kawada, Mayumi Tsuchiya, Seiji Yamasaki, Akira Yamamuro, Toshiya Ono
  • Patent number: 6162925
    Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.
    Type: Grant
    Filed: November 18, 1999
    Date of Patent: December 19, 2000
    Assignee: Research Corporation Tech., Inc.
    Inventors: Robert M. Williams, Chenguang Yuan
  • Patent number: 6147258
    Abstract: Substituted guanidine derivatives of the formula I ##STR1## are prepared by reacting calcium cyanamide with a primary or secondary amino carboxylic acid or a primary or secondary amino sulfonic acid or their derivatives of the formula II ##STR2## where the substituents R.sup.1 and R.sup.2 have the meanings explained in the description.
    Type: Grant
    Filed: October 22, 1998
    Date of Patent: November 14, 2000
    Assignee: BASF Aktiengesellschaft
    Inventors: Thomas Greindl, Gunter Scherr, Rolf Schneider, Klaus Mundinger
  • Patent number: 6143932
    Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.
    Type: Grant
    Filed: July 1, 1999
    Date of Patent: November 7, 2000
    Assignee: Trega Biosciences, Inc.
    Inventors: Barbara Dorner, John M. Ostresh, Colette T. Dooley, Richard A. Houghten, Jutta Eichler
  • Patent number: 6143790
    Abstract: There is disclosed a novel amino glycol derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: September 6, 1996
    Date of Patent: November 7, 2000
    Assignee: G.D. Searle & Co.
    Inventors: E. Ann Hallinan, Foe S. Tjoeng, Kam F. Fok, Timothy J. Hagen, Mihaly V. Toth, Sofya Tsymbalov, Barnett S. Pitzele
  • Patent number: 6121489
    Abstract: The instant invention is directed to a single, selectively N-alkylated compound and libraries of such compounds as set forth in Formula I. Furthermore, the instant invention is directed to methods of effecting analgesia, a decrease in the postprandial rise in the blood glucose levels of a mammal after ingestion of a carbohydrate load by said mammal, and treating microbial infections, utilizing such a single compound of Formula I in conjunction with a pharmaceutically-acceptable carrier. Also, the instant invention is directed to methods for selective alkylation, positional scanning and iterative synthetic and screening technologies.
    Type: Grant
    Filed: March 5, 1997
    Date of Patent: September 19, 2000
    Assignee: Trega Biosciences, Inc.
    Inventors: Barbara Dorner, John M. Ostresh, Colette T. Dooley, Richard A. Houghten, Jutta Eichler
  • Patent number: 6118007
    Abstract: A process, as a substitute for hydrolysis, for preparing a nitroguanidine derivative represented by the following formula (2): ##STR1## wherein A represents a substituted or unsubstituted aromatic or non-aromatic hydrocarbon ring, a substituted or unsubstituted aromatic or non-aromatic heterocycle, a hydrogen atom or a substituted or unsubstituted alkyl, alkenyl or alkynyl group; and R.sub.2 represents a hydrogen atom, a substituted or unsubstituted C.sub.1-6 alkyl, alkenyl or alkynyl group, which comprises reacting a compound represented by the following formula (1): ##STR2## wherein R.sub.1 represents a substituted or unsubstituted, linear or cyclic C.sub.1-10 alkyl group and A and R.sub.2 have the same meanings as defined above, with ammonia, a primary amine or a secondary amine, or a salt thereof.
    Type: Grant
    Filed: March 24, 1998
    Date of Patent: September 12, 2000
    Assignee: Mitsui Chemicals, Inc.
    Inventors: Koichi Ebihara, Tatsuo Kaiho, Michihiko Miyamoto, Daisuke Ura
  • Patent number: 5872294
    Abstract: Hexasubstituted guanidinium chlorides are prepared by a method which affords them in high yield as aqueous solutions, optionally also containing alkali metal chlorides. The solutions may be employed as sources of hexasubstituted guanidinium salts useful as phase transfer catalysts and the reaction of alkali metal salts of dihydroxyaromatic compounds with substituted imides to form polyetherimides or their intermediates.
    Type: Grant
    Filed: January 11, 1996
    Date of Patent: February 16, 1999
    Assignee: General Electric Company
    Inventors: Joseph John Caringi, Gary Ray Faler, Peter David Phelps, Thomas Link Guggenheim, Larry Ivis Flowers, Daniel Joseph Brunelle, Roy Ray Odle
  • Patent number: 5852009
    Abstract: The present invention relates to compositions and methods for inhibiting protein aging. Accordingly, a composition is disclosed which comprises an agent or compound capable of inhibiting the formation of advanced glycosylation end products of target proteins by reacting with the carbonyl moiety of the early glycosylation product of such target proteins formed by their initial glycosylation. Suitable agents may contain an active nitrogen-containing group, such as a hydrazine group. Particular agents comprise aminoguanidine, .alpha.-hydrazinohistidine and mixtures thereof. The method comprises contacting the target protein with the composition. Both industrial and therapeutic applications for the invention are envisioned, as food spoilage and animal protein aging can be treated.
    Type: Grant
    Filed: January 16, 1997
    Date of Patent: December 22, 1998
    Assignee: The Rockefeller University
    Inventors: Anthony Cerami, Peter C. Ulrich, Michael A. Brownlee
  • Patent number: 5840972
    Abstract: A process is disclosed for the preparation of N.sup.G -monoalkyl-L-arginine and related compounds and salts thereof, for example N.sup.G -monomethyl-L-arginine by reacting N-alkylaminoiminomethane sulphonic acid of formula (II) with an amino acid of formula (III).
    Type: Grant
    Filed: February 22, 1995
    Date of Patent: November 24, 1998
    Assignee: Glaxo Wellcome Inc.
    Inventors: Rajnikant Patel, Amrik Singh Mahal, Donald Lloyd Winston Burford
  • Patent number: 5830917
    Abstract: There is disclosed a novel amino alcohol amine derivatives of L-N.sup.6 -(1-iminoethyl)lysine, pharmaceutical compositions containing these novel compounds, and to their use in therapy, in particular their use as nitric oxide synthase inhibitors.
    Type: Grant
    Filed: September 11, 1995
    Date of Patent: November 3, 1998
    Assignee: G. D. Searle & Co.
    Inventors: William M. Moore, E. Ann Hallinan
  • Patent number: 5801179
    Abstract: The present invention is concerned with compounds having the formula ##STR1## the pharmaceutically acceptable acid addition salts thereof, and the stereochemically isomeric forms thereof, wherein R.sup.1 is hydrogen or C.sub.1--6 alkyl; R.sup.2 is hydrogen or C.sub.1- 6 alkyl; R.sup.3 is C.sub.1-6 alkyl, hydroxy, cyano, halo, C.sub.1-6 alkyloxy, aryloxy, arylmethoxy, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, C.sub.1-6 alkyl--S--, C.sub.1-6 alkyl(S.dbd.O)--, C.sub.1-6 alkylcarbonyl; R.sup.4 is hydrogen, halo, hydroxy, C.sub.1-6 alkyl, or C.sub.1-6 alkyloxy; or R.sup.3 and R.sup.4 taken together form a bivalent radical; R.sup.5 and R.sup.6 each independently are hydrogen, halo, hydroxy, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, aryloxy or arylmethoxy; R.sup.7 is hydrogen; Alk.sup.1 is C.sub.2-5 alkanediyl; Alk.sup.2 is C.sub.2-15 alkanediyl; Q is a heterocyclic ring containing at least one nitrogen atom or a radical of formula ##STR2## Pharmaceutical compositions, preparations and use as a medicine are described.
    Type: Grant
    Filed: June 2, 1997
    Date of Patent: September 1, 1998
    Assignee: Janssen Pharmaceutica, NV
    Inventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Piet Tom Bert Paul Wigerinck
  • Patent number: 5798390
    Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
    Type: Grant
    Filed: May 22, 1995
    Date of Patent: August 25, 1998
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 5767162
    Abstract: Tri- and tetra-substituted guanidines which exhibit a high binding affinity to phencyclidine (PCP) receptors and, more preferably, low affinity to the brain sigma receptors. These guanidine derivatives act as non-competitive inhibitors of glutamate induced responses of the NMDA receptor by acting as blockers for the ion channel of the NMDA receptor-ion channel complex. These compounds thus exert neuroprotective activity and are useful in the therapeutic treatment of neuronal loss in hypoxia, hypoglycemia, brain or spinal cord ischemia, and brain or spinal chord trauma as well as being useful for the treatment of epilepsy, Alzheimer's disease, Amyotrophic Lateral Sclerosis, Parkinson's disease, Huntington's disease, Down's Syndrome, Korsakoff's disease and other neurodegenerative disorders.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: June 16, 1998
    Assignee: State of Oregon, acting by and through the Oregon State Board of Higher Education, acting for and on behalf of the Oregon Health Sciences University and the University of Oregon
    Inventors: Eckard Weber, John F. W. Keana
  • Patent number: 5756843
    Abstract: Quaternary salts having a double helix structure are prepared by the reaction of dihydroxyaromatic compound, preferably a bisphenol, with an alkali metal hydroxide and a quaternary salt, such as a tetraalkylammonium or hexaalkylguanidinium chloride. The quaternary salts and their alkaline hydrolysis products are useful as catalysts in various reactions, including imide formation from bisphenol salts and halo- or nitro-substituted phthalimides and redistribution and equilibration of polycarbonates.
    Type: Grant
    Filed: December 17, 1996
    Date of Patent: May 26, 1998
    Assignee: General Electric Company
    Inventors: Jimmy Lynn Webb, Matthew Hal Littlejohn, Joseph John Caringi, Thomas Link Guggenheim, Robert Joseph Nick, Patrick Joseph McCloskey, Joseph Anthony King, Jr.