Acyclic Patents (Class 564/240)
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Patent number: 9161896Abstract: 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: GrantFiled: December 28, 2011Date of Patent: October 20, 2015Assignee: KAO CORPORATIONInventor: Yumiko Yamamoto
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Publication number: 20150136611Abstract: 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: ApplicationFiled: November 21, 2013Publication date: May 21, 2015Inventors: Julia KOZHUKH, Zuhra I. NIAZIMBETOVA, Maria Anna RZEZNIK
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Publication number: 20140256986Abstract: 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: ApplicationFiled: March 9, 2013Publication date: September 11, 2014Inventor: Guoji Zhang
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Patent number: 8785679Abstract: 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: GrantFiled: December 10, 2012Date of Patent: July 22, 2014Assignee: Empire Technology Development LLCInventors: Glen Leon Brizius, Phillip Kent Montgomery
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Publication number: 20140155654Abstract: 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: ApplicationFiled: March 6, 2013Publication date: June 5, 2014Applicant: Physical Sciences, Inc.Inventor: Physical Sciences, Inc.
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Publication number: 20140051712Abstract: 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: ApplicationFiled: December 16, 2011Publication date: February 20, 2014Inventors: John R. Cashman, Jarosiaw Kalisiak
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Publication number: 20130056676Abstract: 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: ApplicationFiled: September 2, 2011Publication date: March 7, 2013Applicant: BATTELLE MEMORIAL INSTITUTEInventors: David J. Heldebrant, Ward E. Tegrotenhuis, Charles J. Freeman, Michael L. Elliott, Phillip K. Koech, Paul H. Humble, Feng Zheng, Jian Zhang
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Patent number: 8389768Abstract: 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: GrantFiled: May 1, 2009Date of Patent: March 5, 2013Assignee: The University of North Carolina at Chapel HillInventors: Leaf Huang, Yunching Chen, Joyeeta Sen, Surendar Reddy Bathula, Sumio Chono, Shyh-Dar Li, Michael Hackett
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Publication number: 20130046092Abstract: 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: ApplicationFiled: June 29, 2011Publication date: February 21, 2013Applicants: QUEEN'S UNIVERSITY AT KINGSTON, GEORGIA TECH RESEARCH CORPORATIONInventors: Philip JESSOP, Charles ECKERT, Charles LIOTTA, David HELDEBRANT
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Patent number: 8318676Abstract: 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: GrantFiled: August 16, 2007Date of Patent: November 27, 2012Assignee: Wella AGInventors: Rudolf Bimczok, Thomas Kripp, Beate Grasser, Christian Springob
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Publication number: 20120172220Abstract: 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: ApplicationFiled: June 24, 2010Publication date: July 5, 2012Applicants: FLAMEL TECHNOLOGIES S.A., MONSANTO TECHNOLOGY LLCInventors: Ronald J. Brinker, Olivier Soula, Alain Lemercier
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Publication number: 20120134948Abstract: 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: ApplicationFiled: July 19, 2010Publication date: May 31, 2012Applicant: EVONIK GOLDSCHMIDT GMBHInventors: Oliver Springer, Peter Muss, Peter Lersch, Ursula Maczkiewitz, Mike Farwick
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Publication number: 20120116076Abstract: 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: ApplicationFiled: June 29, 2011Publication date: May 10, 2012Applicants: GEORGIA TECH RESEARCH CORPORATION, QUEEN'S UNIVERSITY AT KINGSTONInventors: Philip G. JESSOP, Charles A. ECKERT, Charles L. LIOTTA, David J. HELDEBRANT
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Publication number: 20120035268Abstract: 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: ApplicationFiled: December 28, 2009Publication date: February 9, 2012Inventors: Zdzislaw M. Szulc, Alicja Bielawska, Lina M. Obeld, Yusuf A. Hannun, James Norris, Liu Xiang
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Patent number: 8084502Abstract: 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: GrantFiled: April 3, 2008Date of Patent: December 27, 2011Inventors: Gong Je Seong, Chan Yun Kim, Jong Eun Lee, Samin Hong
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Publication number: 20110311583Abstract: (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: ApplicationFiled: November 10, 2009Publication date: December 22, 2011Applicant: ALNYLAM PHARMACEUTICALS, INC.Inventors: Muthiah Manoharan, kallanthottathil G. Rajeev, Muthusamy Jayaraman, David Butler, Jayaprakash K. Narayanannair, Martin Maier, Laxman Eltepu
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Patent number: 8063106Abstract: 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: GrantFiled: August 9, 2006Date of Patent: November 22, 2011Assignee: TCP Innovations LimitedInventors: David J. Grainger, David John Fox
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Publication number: 20110117219Abstract: 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: ApplicationFiled: May 28, 2009Publication date: May 19, 2011Applicant: EVONIK GOLDSCHMIDT GMBHInventors: Oliver Springer, Peter Muss, Burghard Gruening, Ursula Maczkiewitz, Mike Farwick, Peter Lersch
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Publication number: 20110098392Abstract: 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: ApplicationFiled: March 24, 2009Publication date: April 28, 2011Applicant: BLUESTAR SILICONES FRANCEInventors: Georges Barrandon, Delphine Blanc, Christian Maliverney, Hervé Parisot
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Publication number: 20110034698Abstract: 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: ApplicationFiled: October 20, 2010Publication date: February 10, 2011Inventors: Nikolai(Mykola) Ignatyev, German Bissky, Helge Willner
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Patent number: 7771611Abstract: 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: GrantFiled: July 10, 2006Date of Patent: August 10, 2010Assignee: Air Products and Chemicals, Inc.Inventors: Robert George Syvret, Gauri Sankar Lal, Kristen Elaine Minnich
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Publication number: 20100172890Abstract: 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: ApplicationFiled: February 1, 2010Publication date: July 8, 2010Inventors: Gad Gilad, Varda Gilad
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Publication number: 20100130783Abstract: 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: ApplicationFiled: April 3, 2008Publication date: May 27, 2010Inventors: Gong Je Seong, Chan Yun Kim, Jong Eun Lee, Samin Hong
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Publication number: 20090253912Abstract: 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: ApplicationFiled: November 18, 2005Publication date: October 8, 2009Inventors: Nikolai (Mykola) Ignatyev, Urs Welz-Biermann, Andriy Kucheryna, Helge Willner
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Publication number: 20090076110Abstract: 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: ApplicationFiled: December 4, 2007Publication date: March 19, 2009Inventors: Ronald Kramer, Alexander Nikolaidis
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Patent number: 7470815Abstract: Peptidomimetic compositions for selective inhibition of neuronal nitric oxide synthase.Type: GrantFiled: January 26, 2006Date of Patent: December 30, 2008Assignee: Northwestern UniversityInventors: Richard B. Silverman, Jung-Mi Hah, Jose Antonio Gomez Vidal, Erik Erdal
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Publication number: 20080247991Abstract: 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: ApplicationFiled: February 28, 2005Publication date: October 9, 2008Inventors: Bernhardt L. Trout, Daniel I.C. Wang, Brian M. Baynes
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Patent number: 7078566Abstract: 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: GrantFiled: April 8, 2004Date of Patent: July 18, 2006Assignee: Biosphinks AktiengesellschaftInventor: Eberhard Amtmann
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Patent number: 6960689Abstract: 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: GrantFiled: October 1, 2004Date of Patent: November 1, 2005Assignee: Chugai Seiyaku Kabushiki KaishaInventors: Takashi Emura, Tsuyoshi Haneishi
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Publication number: 20030163000Abstract: 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: ApplicationFiled: August 21, 2002Publication date: August 28, 2003Inventors: Brian Atkinson, Victor Lebedev
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Patent number: 6570038Abstract: 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: GrantFiled: June 9, 2000Date of Patent: May 27, 2003Inventors: Joseph John Caringi, Peter David Phelps, Thomas Link Guggenheim, Daniel Joseph Brunelle
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Patent number: 6492376Abstract: 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: GrantFiled: May 4, 2001Date of Patent: December 10, 2002Assignee: Berlex Laboratories, Inc.Inventor: Gary B. Phillips
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Patent number: 6258976Abstract: 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: GrantFiled: March 19, 1999Date of Patent: July 10, 2001Inventors: Francis Johnson, Ramesh C. Gupta
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Patent number: 6251948Abstract: 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: GrantFiled: June 6, 1995Date of Patent: June 26, 2001Assignee: 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 OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 6235934Abstract: 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: GrantFiled: December 17, 1998Date of Patent: May 22, 2001Assignee: General Electric CompanyInventors: Joseph John Caringi, Gary Ray Faler, Peter David Phelps, Thomas Link Guggenheim, Larry Ivis Flowers, Daniel Joseph Brunelle, Roy Ray Odle
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Patent number: 6187955Abstract: 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: GrantFiled: November 6, 1997Date of Patent: February 13, 2001Assignee: Kao CorporationInventors: Minoru Nagai, Hiromitsu Kawada, Mayumi Tsuchiya, Seiji Yamasaki, Akira Yamamuro, Toshiya Ono
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Patent number: 6162925Abstract: The present invention is directed to anti-bacterial and anti-tumor agents and the synthesis thereof.Type: GrantFiled: November 18, 1999Date of Patent: December 19, 2000Assignee: Research Corporation Tech., Inc.Inventors: Robert M. Williams, Chenguang Yuan
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Patent number: 6147258Abstract: 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: GrantFiled: October 22, 1998Date of Patent: November 14, 2000Assignee: BASF AktiengesellschaftInventors: Thomas Greindl, Gunter Scherr, Rolf Schneider, Klaus Mundinger
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Patent number: 6143932Abstract: 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: GrantFiled: July 1, 1999Date of Patent: November 7, 2000Assignee: Trega Biosciences, Inc.Inventors: Barbara Dorner, John M. Ostresh, Colette T. Dooley, Richard A. Houghten, Jutta Eichler
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Patent number: 6143790Abstract: 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: GrantFiled: September 6, 1996Date of Patent: November 7, 2000Assignee: 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
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Patent number: 6121489Abstract: 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: GrantFiled: March 5, 1997Date of Patent: September 19, 2000Assignee: Trega Biosciences, Inc.Inventors: Barbara Dorner, John M. Ostresh, Colette T. Dooley, Richard A. Houghten, Jutta Eichler
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Patent number: 6118007Abstract: 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: GrantFiled: March 24, 1998Date of Patent: September 12, 2000Assignee: Mitsui Chemicals, Inc.Inventors: Koichi Ebihara, Tatsuo Kaiho, Michihiko Miyamoto, Daisuke Ura
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Patent number: 5872294Abstract: 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: GrantFiled: January 11, 1996Date of Patent: February 16, 1999Assignee: General Electric CompanyInventors: Joseph John Caringi, Gary Ray Faler, Peter David Phelps, Thomas Link Guggenheim, Larry Ivis Flowers, Daniel Joseph Brunelle, Roy Ray Odle
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Patent number: 5852009Abstract: 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: GrantFiled: January 16, 1997Date of Patent: December 22, 1998Assignee: The Rockefeller UniversityInventors: Anthony Cerami, Peter C. Ulrich, Michael A. Brownlee
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Patent number: 5840972Abstract: 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: GrantFiled: February 22, 1995Date of Patent: November 24, 1998Assignee: Glaxo Wellcome Inc.Inventors: Rajnikant Patel, Amrik Singh Mahal, Donald Lloyd Winston Burford
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Patent number: 5830917Abstract: 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: GrantFiled: September 11, 1995Date of Patent: November 3, 1998Assignee: G. D. Searle & Co.Inventors: William M. Moore, E. Ann Hallinan
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Patent number: 5801179Abstract: 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: GrantFiled: June 2, 1997Date of Patent: September 1, 1998Assignee: Janssen Pharmaceutica, NVInventors: Guy Rosalia Eugene Van Lommen, Marcel Frans Leopold De Bruyn, Piet Tom Bert Paul Wigerinck
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Patent number: 5798390Abstract: 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: GrantFiled: May 22, 1995Date of Patent: August 25, 1998Assignee: 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 OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 5767162Abstract: 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: GrantFiled: June 6, 1995Date of Patent: June 16, 1998Assignee: 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 OregonInventors: Eckard Weber, John F. W. Keana
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Patent number: 5756843Abstract: 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: GrantFiled: December 17, 1996Date of Patent: May 26, 1998Assignee: General Electric CompanyInventors: Jimmy Lynn Webb, Matthew Hal Littlejohn, Joseph John Caringi, Thomas Link Guggenheim, Robert Joseph Nick, Patrick Joseph McCloskey, Joseph Anthony King, Jr.