Lysine Per Se Or Salt Thereof Patents (Class 562/562)
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Patent number: 6756510Abstract: Liquid lysine can be made with almost any particular specification that may be reasonably expected. A multistep process for producing lysine includes at least: fermentation, ultrafiltration, evaporation, and mixing. Depending upon the particular specifications that are to be met, at least two liquids may be taken from selected points in the multistep process. The lysine in these two liquids is concentrated to a desired level and then the liquids are mixed together and returned to the processing feed stream. The process may be applied to any amino acid which can be produced by fermentation.Type: GrantFiled: January 20, 2000Date of Patent: June 29, 2004Assignee: Archer Daniels Midland CompanyInventors: Thomas Binder, Thomas Wiegand, Kevin Moore
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Patent number: 6703042Abstract: The present invention relates to stable, non-hygroscopic salts of L-carnitine and lower alkanoyl L-carnitine endowed with enhanced nutritional and /or therapeutical efficacy with respect to their inner salts congeners and tom solid compositions containing such salts particularly suited to oral administration.Type: GrantFiled: November 27, 2001Date of Patent: March 9, 2004Assignee: Sigma-Tau Industries Farmaceutiche Riunite S.p.A.Inventor: Atonietta Buononato
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Patent number: 6699869Abstract: There are disclosed &bgr;-sheet mimetics and methods relating to the same for imparting or stabilizing the &bgr;-sheet structure of a peptide, protein or molecule. In one aspect, &bgr;-sheet mimetics are disclosed having utility as protease inhibitors in general and, more specifically, as serine protease inhibitors such as thrombin, elastase and Factor X inhibitors. In one embodiment, the &bgr;-sheet mimetic is a thrombin inhibitor.Type: GrantFiled: April 28, 2000Date of Patent: March 2, 2004Assignee: Myriad Genetics Inc.Inventors: Michael Kahn, Cyprian O. Ogbu, Masakatsu Eguchi, Hwa-Ok Kim, Patrick Douglas Boatman, Jr.
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Patent number: 6696611Abstract: The present invention provides a method for enantioselectively reducing a prochiral carbon centered radical having one or more electron donator groups attached directly to the central prochiral carbon atom of the radical, and/or attached to a carbon atom within 1 to 4 atoms of the central prochiral carbon atom, comprising treating said radical with a chiral non-racemic organotin hydride in the presence of a Lewis acid.Type: GrantFiled: July 27, 2001Date of Patent: February 24, 2004Assignee: Chirogen Pty. LimitedInventors: Dainis Dakternieks, Carl H. Schiesser, Tamara Perchyonok
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Patent number: 6632921Abstract: Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula: wherein R1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C.Type: GrantFiled: March 26, 1999Date of Patent: October 14, 2003Assignee: G. D Searle & CoInventors: James A. Sikorski, Devadas Balekudru, Daniel P. Getman, David L. Brown, Srinivasan Nagarajan, Mark E. Zupec, Jeffrey I. Gordon
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Patent number: 6632961Abstract: Compounds having Formula I or pharmaceutically acceptable salts or prodrugs thereof, are useful for treating pathological states which arise from or are exacerbated by angiogenesis. The invention also relates to pharmaceutical compositions comprising these compounds and to methods of inhibiting angiogenesis in a mammal.Type: GrantFiled: May 21, 1999Date of Patent: October 14, 2003Assignee: Abbott LaboratoriesInventors: Megumi Kawai, Jack Henkin, George S. Sheppard, Richard A. Craig
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Publication number: 20030049284Abstract: Method of increasing the solubility of salts of alpha hydroxy carboxylic acids, preferably used in the field of nutrition and feeding of living matter, and products obtained by the method, the products enhancing and increasing the bio-availability of macro and micro essential elements contained in the products.Type: ApplicationFiled: September 5, 2001Publication date: March 13, 2003Inventors: Jose Ruben Boccio, Adrian Tomas De Paoli, Eduardo Walter Ettlin, Edgardo Adrian Hager
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Patent number: 6495716Abstract: Crystals of [S,S]-ethylenediamine-N,N′-disuccinic acid which have a bulk density of 0.45 to 1.2 g/cm3, and a process for obtaining these crystals comprising the steps of adjusting an aqueous solution of an [S,S]-ethylenediamine-N,N′-disuccinic acid metal salt to a temperature of 40 to 80° C. and a pH of 1.9 to 4.5, and cooling the solution to a temperature below 40° C. over a period of 0.2 to 10 hours while supplying a mineral acid so as to maintain the pH at 1.9 to 4.5 to precipitate [S,S]-ethylenediamine-N,N′-disuccinic acid in a high yield.Type: GrantFiled: February 27, 2002Date of Patent: December 17, 2002Assignee: Mitsubishi Rayon Co., Ltd.Inventors: Hiroyasu Banba, Shigeho Tanaka, Kiyonobu Niwa, Takakazu Endo
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Patent number: 6492489Abstract: The invention relates to novel peptides synthesized according a method utilizing the hypusine reagent: wherein: Q1 Q2 and Q3 may be the same or different and are amino protective groups, provided that Q3 is orthogonal to Q1 and Q2; and Z is a hydroxy protective group, as well as improved methods of peptide synthesis wherein the above-described hypusine reagent is employed to prepare novel hypusine-containing peptides.Type: GrantFiled: March 7, 2000Date of Patent: December 10, 2002Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Publication number: 20020123648Abstract: Herein is disclosed an aqueous stable lysine solution containing an acid radical in such amount that the solubility of lysine therein has been increased than in the corresponding aqueous lysine base solution, whereby during storage of lysine in the form of a free-lysine solution (liquid composition), the precipitation of lysine base crystals due to the drop in temperature is prevented thereby improving the handling thereof during transportation (transfer) etc.Type: ApplicationFiled: February 27, 2002Publication date: September 5, 2002Applicant: AJINOMOTO CO., INC.Inventors: Kazuhiro Hasegawa, Toshiya Tanabe, Keita Minami
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Patent number: 6414189Abstract: Crystals of [S,S]-ethylenediamine-N,N′-disuccinic acid which have a bulk density of 0.45 to 1.2 g/cm3, and a process for obtaining these crystals comprising the steps of adjusting an aqueous solution of an [S,S]-ethylenediamine-N,N′-disuccinic acid metal salt to a temperature of 40 to 80° C. and a pH of 1.9 to 4.5, and cooling the solution to a temperature below 40° C. over a period of 0.2 to 10 hours while supplying a mineral acid so as to maintain the pH at 1.9 to 4.5 to precipitate [S,S]-ethylenediamine-N,N′-disuccinic acid in a high yield.Type: GrantFiled: May 18, 2000Date of Patent: July 2, 2002Assignee: Mitsubishi Rayon Co., Ltd.Inventors: Hiroyasu Banba, Shigeho Tanaka, Kiyonobu Niwa, Takakazu Endo
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Patent number: 6392094Abstract: A method for recovering amino acids, which comprises supplying a mixed solution containing inorganic acid salts, amino acids and non-electrolytes such as saccharides to a first-step resin layer comprising an Na type or K type strongly acidic ion exchange resin; separating an effluent into at least a first fraction containing coloring matters, acidic amino acids and ashes, a second fraction containing neutral amino acids and saccharides, and a third fraction containing betaines; supplying the second fraction to a second-step resin layer comprising at least one resin selected from the group consisting of NH4 type, Ca type and Mg type strongly acidic ion exchange resins, and optionally further supplying it to a third-step resin layer comprising an Mg type or Ca type strongly acidic ion exchange resin different from the resin of the second-step resin layer, thereby recovering various kinds of amino acids contained in an effluent.Type: GrantFiled: June 19, 2001Date of Patent: May 21, 2002Assignee: Nippon Beet Sugar Mfg. Co., Ltd.Inventors: Takashi Kanno, Koji Sayama, Tsutomu Aritsuka, Hiroto Kikuchi
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Publication number: 20020051849Abstract: A cell adhesion solution of a cross-linked polymer for substrates includes an amino acid polymer, a buffered cross-linking agent, and deionized water (DI H2O). In one example, the amino acid polymer is selected from a neutral or basic amino acid, such as poly 1-lysine or poly 1-arginine. In another example, the amino acid polymer includes poly 1-1sine. In another example, the amino acid polymer includes poly 1-1sine of molecular weight of 100,000 or higher. The cross-linking agent can be selected from an aldehyde functional group, a buffered formaldehyde solution or a 10% neutral buffered formalin solution.Type: ApplicationFiled: August 7, 2001Publication date: May 2, 2002Inventor: Willaim Alan Fox
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Patent number: 6376544Abstract: L-arginine found essential to enhance the glomerular function of the kidneys is used &phgr; formulate a low viscosity, calorie-dense, nutritional product for a person having renal failure. In a product free of citric acid or citrates, for oral ingestion, the taste of arginine is counteracted by lactic, malic or adipic acid; in a formulation for tube-feeding, citric acid and citrates in a specified ratio controls the product's stability. The ratio of calcium to phosphorus is controlled, as is the caloric distribution and water content; the amounts of vitamins and minerals included provide a nutritionally complete formulation.Type: GrantFiled: February 2, 2001Date of Patent: April 23, 2002Assignee: Novartis Nutrition AGInventors: Carol Jo Lowry, Kathy Marie Sass
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Publication number: 20020042536Abstract: The invention relates to novel processes for preparing differentially protected lysine derivatives via a novel p-anisaldehyde Schiff base intermediate and the intermediate prepared therein.Type: ApplicationFiled: October 8, 1999Publication date: April 11, 2002Inventor: PRASAD S. RAJE
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Patent number: 6364914Abstract: Herein is disclosed a method of crystallization with the particle size distribution being controlled, characterized in that while crystals are being precipitated by vacuum concentration crystallization, the temperature of the slurry is periodically varied up and down during the concentration of the crystallization mother liquor (i.e., the slurry), which method is an excellent one free from the defects of the conventional methods.Type: GrantFiled: March 19, 1999Date of Patent: April 2, 2002Assignee: Ajinomoto Co., Inc.Inventors: Hiroshi Ueda, Hiroshi Fukushi, Muneyuki Ozawa
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Patent number: 6344483Abstract: The current invention discloses halogenated amidino amino acid derivatives useful as nitric oxide synthase inhibitors, and pharmaceutically acceptable salts thereof.Type: GrantFiled: January 31, 2000Date of Patent: February 5, 2002Assignee: G. D. Searle & Co.Inventors: E. Ann Hallinan, Barnett S. Pitzele, Dale P. Spangler, Mihaly V. Toth, R. Keith Webber, Arija A. Bergmanis, Timothy J. Hagen, Sofya Tsymbalov
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Patent number: 6329548Abstract: Herein is disclosed an aqueous stable lysine solution containing an acid radical in such amount that the solubility of lysine therein has been increased than in the corresponding aqueous lysine base solution, whereby during storage of lysine in the form of a free-lysine solution (liquid composition), the precipitation of lysine base crystals due to the drop in temperature is prevented thereby improving the handling thereof during transportation (transfer) etc.Type: GrantFiled: March 3, 2000Date of Patent: December 11, 2001Assignee: Ajinomoto Co., Inc.Inventors: Kazuhiro Hasegawa, Toshiya Tanabe, Keita Minami
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Publication number: 20010025110Abstract: Methods, compositions, and devices for alleviating the problems of toxic discharge of aldehydes present in waste streams are disclosed. The methods relate to reducing neutralized aldehydes wherein the neutalized aldehydes are formed by treating aldehydes with amino acids and thereinafter are reduced. These reduced, neutralized aldehydes do not revert back to toxic aldehydes, but form amino acids and thus allow waste containing aldehyde to be more environmentally safely disposed.Type: ApplicationFiled: December 22, 2000Publication date: September 27, 2001Inventors: Peter Zhu, Xiaolan Chen, Charles G. Roberts
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Patent number: 6288116Abstract: L-arginine found essential to enhance the glomerular function of the kidneys is used to formulate a low viscosity, calorie-dense, nutritional product for a person having renal failure. In a product free of citric acid or citrates, for oral ingestion, the taste of arginine is counteracted by lactic, malic or adipic acid; in a formulation for tube-feeding, citric acid and citrates in a specified ratio controls the product's stability. The ratio of calcium to phosphorus is controlled, as is the caloric distribution and water content; the amounts of vitamins and minerals included provide a nutritionally complete formulation.Type: GrantFiled: May 13, 1998Date of Patent: September 11, 2001Assignee: Novartis Nutrition AGInventors: Carol Jo Lowry, Kathy Marie Sass
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Patent number: 6255503Abstract: Water-soluble dodecandioates wherein the cationic moiety is selected from the group comprising the cations of basic aminoacids (e.g. lysine) and choline and orally or parenterally administrable compositions containing same, are disclosed.Type: GrantFiled: November 30, 1999Date of Patent: July 3, 2001Assignee: Sigma-Tau Healthscience S.p.A.Inventors: Mosé Santaniello, Nazareno Scafetta, Maria Ornella Tinti
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Patent number: 6248866Abstract: A derivative of hypusine useful as a reagent for synthesizing peptides containing hypusine, as well as an improved method for synthesizing the same, the derivative having the formula: wherein: Q1 and Q2 may be the same or different and are amino protective groups; Q3 is an amino protective group which is orthogonal to Q1 and Q2; and Z is a hydroxy protective group.Type: GrantFiled: August 19, 1998Date of Patent: June 19, 2001Assignee: University of Florida Research Foundation, IncorporatedInventor: Raymond J. Bergeron, Jr.
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Patent number: 6069172Abstract: A new use of the enantiomer (R)-ketoprofen and of its salts with suitable organic and inorganic bases in the therapy of neutrophil-dependent diseases and phlogistic processes is described as well as pharmaceutical preparations containing such compounds and useful for oral, parenteral or topical administration.Type: GrantFiled: January 27, 1999Date of Patent: May 30, 2000Assignee: Dompe' SpAInventors: Riccardo Bertini, Cinzia Bizzarri, Laura Brandolini, Gabriella Melillo, Gianfranco Caselli, Gaetano Clavenna
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Patent number: 6060586Abstract: Ureins are obtained by reaction, in basic medium, between an N.sup..omega. -(aryloxycarbonyl)diamino acid and a compound containing a free amino group. The chirality of the compounds is outstandingly well preserved.Type: GrantFiled: June 17, 1997Date of Patent: May 9, 2000Assignee: Solvay (Societe Anonyme)Inventors: Roland Callens, Georges Blondeel, Marc Anteunis, Frank Becu
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Patent number: 6057297Abstract: Peptidomimetic compounds capable of inhibiting zinc-dependent metalloproteinases to treat pathological conditions associated with activation of endogenous metalloproteinases in mammals.Type: GrantFiled: March 18, 1998Date of Patent: May 2, 2000Assignee: Polifarma S.p.A.Inventors: Vincenzo Politi, Silvana D'Alessio, Giovanni Di Stazio, Giovanna De Luca, Mario Materazzi
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Patent number: 6020331Abstract: There are disclosed .beta.-sheet mimetics and methods relating to the same for imparting or stabilizing the .beta.-sheet structure of a peptide, protein or molecule. In one aspect, the .beta.-sheet mimetics are covalently attached at the end or within the length of the peptide or protein. The .beta.-sheet mimetics have utility as protease inhibitors generally, including activity as serine protease inhibitors such as thrombin, elastase and Factor X.Type: GrantFiled: January 20, 1998Date of Patent: February 1, 2000Assignee: Molecumetics, Ltd.Inventor: Michael Kahn
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Patent number: 6017555Abstract: A process produces an L-Lysine feed supplement with a final L-Lysine purity in the range theoretically between about 35% and 80%, measured as a percent of free-base per kg, and more preferably between about 50% and 80% L-Lysine. The process comprises adding a material containing L-Lysine to an L-Lysine fermentation broth or a fraction of an L-Lysine fermentation broth. The added material being an amount which brings a final L-Lysine feed supplement with an L-Lysine purity into a range theoretically between about 35% and 80%, measured as a percent of free-base per kg, and more preferably between about 50% and 80% L-Lysine. The fraction of L-Lysine fermentation broth is obtained by any suitable separating means such as ultrafiltration or centrifugation. The process also comprises a drying step which may involve any suitable drying means such as a spray granulator, spray dryer, tray dryer, drum dryer, rotary dryer, and tunnel dryer.Type: GrantFiled: June 17, 1998Date of Patent: January 25, 2000Assignee: Archer Daniels Midland CompanyInventors: Joseph Michael Stevens, Thomas P. Binder
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Patent number: 6015792Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.Type: GrantFiled: March 13, 1998Date of Patent: January 18, 2000Assignee: Bioresearch, Inc.Inventors: Robert J. Kurtz, William D. Fuller
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Patent number: 6008250Abstract: Ingestible compounds which are substantially tasteless and which have been found to be effective reducers or eliminators of undesirable tastes for eatables.Type: GrantFiled: March 13, 1998Date of Patent: December 28, 1999Assignee: Bioresearch, Inc.Inventors: Robert J. Kurtz, William D. Fuller
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Patent number: 5998594Abstract: A chromogenic receptor comprises a self-assembled chromogenic compound having at least one intrinsic binding site. The chromogenic compound is characterized by the property of producing a reversible color change responsive to binding a target substrate to the receptor. The chromogenic compound has a transition metal ion and at least one ligand bound to the transition metal ion. The ligand is selected from the group consisting of substituted phenanthroline, substituted 2,2'-bipyridine and substituted 2,2':6',2"-terpyridine. The transition metal is selected from the group consisting of Cu(I), Cu(II), Ag(I), Ni(II), Fe(II), Fe(III), Ru(II), Co(III), and Os(II). Self-assembly can be effected in the presence of Cu(I) to form receptors for dicarboxylic acids, carbohydrate, amino acids, steroids and pyrophosphates. The receptors are characterized by the formation of a 2:1 complex of the target substrate with the receptor producing a visible color change from orange to red and a measurable change in its luminescence.Type: GrantFiled: December 30, 1994Date of Patent: December 7, 1999Assignee: University of Pittsburgh of the Commonwealth System of Higher EducationInventors: M. Scott Goodman, Andrew D. Hamilton
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Patent number: 5990350Abstract: Process for the efficient production of a substantially dust-free, free flowing granular L-Lysine in which the L-Lysine content is adjustable. Cells are removed from a fermentation broth containing L-Lysine to make a substantially cell free L-Lysine broth. Water is removed from the L-Lysine broth to form a concentrated L-Lysine broth. The L-Lysine content of the concentrated L-Lysine broth may be adjusted to be between about 35% and 76%, measured as a percent of freebase per kg, by adding material containing L-Lysine to provide an enriched L-Lysine broth. The enriched L-Lysine broth is agglomerated by means of an atomized spray of the enriched L-Lysine broth directed onto a fluidized bed of percolating L-Lysine particles. The L-Lysine particulates act as seeds for the agglomeration process wherein the L-Lysine particulates grow in size to provide a substantially dust-free, free flowing granular L-Lysine.Type: GrantFiled: December 16, 1997Date of Patent: November 23, 1999Assignee: Archer Midland CompanyInventors: Joseph Michael Stevens, Thomas P. Binder
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Patent number: 5981564Abstract: The invention relates to new paclitaxel derivatives showing an increased solubility in water. More particularly, the invention relates to glutarylpaclitaxel, glutarylpaclitaxel 6-aminohexanol glucuronide and to different amino acid derivatives of the glutarylpaclitaxel, all of which possess the cytotoxicity activity of the parent compound, paclitaxel. Also disclosed are fluorescent derivatives of paclitaxel for determining a concentration of paclitaxel in a medium or for detecting apoptotic cancer cells.Type: GrantFiled: July 1, 1998Date of Patent: November 9, 1999Assignee: Universite LavalInventors: Michel Page, Renee Paradis, Cyrille Bicamumpaka
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Patent number: 5973113Abstract: A derivative of hypusine useful as a reagent for synthesizing peptides containing hypusine, as well as a method for synthesizing the same, the derivative having the formula: ##STR1## wherein: Q.sub.1 and Q.sub.2 may be the same or different and are amino protective groups;Q.sub.3 is an amino protective group which is orthogonal to Q.sub.1 and Q.sub.2 ; andZ is a hydroxy protective group.Type: GrantFiled: October 31, 1997Date of Patent: October 26, 1999Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 5965770Abstract: Compounds having the general formula: ##STR1## in which R3 represents an aryl group which is unsubstituted or substituted by one or more alkyl groups containing 1 to 4 carbon atoms; R4 represents a hydrogen atom, a group for protecting the amino functional group, an amino acid or a peptide some of whose functional groups are optionally substituted by a protecting group or by an activating group; R5 represents a hydroxy group, a halogen atom, a group for protecting the carboxyl functional group, an activating group, an amino group, an amino acid or a peptide some of whose functional groups are optionally substituted by a protecting group or by an activating group; and n is an integer from 1 to 10.Type: GrantFiled: October 31, 1997Date of Patent: October 12, 1999Assignee: SolvayInventors: Marc Anteunis, Frank Becu, Roland Callens, Georges Blondeel
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Patent number: 5958977Abstract: A novel phosphoric acid-amino acid complex salt is provided which manifests insolubility in a neutral or alkaline aqueous solution and solubility in an acidic aqueous solution and has a basic amino acid, an alkaline earth metal, and phosphoric acid as main components thereof. An additive composition containing the complex salt and used in a feed for ruminant mammals excels in protection in the first compartment of the stomach of a ruminant mammal and solubility in the fourth compartment of the stomach. This additive composition improves the nutrition of the feed with respect to such a basic amino acid as lysine, a substance frequently missing in the feed for ruminant mammals.Type: GrantFiled: August 9, 1996Date of Patent: September 28, 1999Assignee: Ajinomoto Co., Inc.Inventors: Toru Ikeda, Toshihide Yukawa
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Patent number: 5948415Abstract: The present invention relates to new compounds, which are N.sup..delta. -substituted ornithine derivatives, having the formula (I)HOOC--CH(NH.sub.2)--(CH.sub.2).sub.3 --NH--(X).sub.h --(CH.sub.2).sub.j --(CHOH).sub.k --(CH.sub.2).sub.m --(O).sub.n --(CH.sub.2).sub.p --Rin which R represents a hydrocarbon alkyl radical or a perfluorinated alkyl radical, X is a divalent radical chosen from --CO--O--, --CO--NH-- and --SO.sub.2 --, h, j, k, m and n are, independently, zero or 1 and p is zero to 4, a salt of a compound of formula (I), an optical isomer of D or L configuration thereof or a mixture thereof. The invention also relates to a process for the preparation of these compounds, to their use, especially in cosmetics, and to compositions, especially cosmetic compositions, comprising them.Type: GrantFiled: April 17, 1996Date of Patent: September 7, 1999Assignee: L'OrealInventors: Michel Philippe, Thierry Bordier
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Patent number: 5948939Abstract: An .omega.-guanidino-.alpha.-amino-acid (or its functional derivative) or a compound containing it may be prepared by the reaction of the .omega.-amino group of an .alpha.,.omega.-diamino acid (or its functional derivative) or a compound containing it with a formamidinesulfonic acid.Type: GrantFiled: April 20, 1992Date of Patent: September 7, 1999Assignee: Syntex (U.S.A.) Inc.Inventors: Humberto B. Arzeno, David J. Morgans, Jr.
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Patent number: 5942600Abstract: Seryl-lysyl-based peptide and peptidomimetic compounds are described as inhibitors of the enzyme N-myristoyl transferase to provide selective control of the fungal organism Candida albicans. Peptidomimetic compounds of particular interest are those of the formula: ##STR1## wherein R.sup.1 is selected form aminoalkyl, p-aminoalkylphenylalkyl, imidazolylalkylphenylalkyl, 2-alkylimidazolylalkylphenylalkyl, benzimidazolylalkylphenylalkyl and 2-alkylbenzimidazolylalkylphenylalkyl; wherein R.sup.2 is selected from hydrido, alkyl, cycloalkyl, akenyl, alkynyl, haloalkyl, benzyl, alkylphenylalkyl, alkoxyphenylalkyl, halophenylalkyl, phenethyl, cycloalkylalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, alkoxycycloalkylalkyl and naphthylalkyl; wherein Y is selected from carboxylic acid, hydroxamic acid, phosphonic acid and tetrazolyl; or a pharmaceutically-acceptable salt, amide or ester thereof. Compounds of the formula are species-specific inhibitors of C.Type: GrantFiled: March 24, 1997Date of Patent: August 24, 1999Assignee: G. D. Searle & Co.Inventors: James A. Sikorski, Balekudru Devadas, Daniel P. Getman, David L. Brown, Srinivasan Nagarajan, Mark E. Zupec, Jeffrey I. Gordon
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Patent number: 5888518Abstract: A method for preventing and treating parasitic infections in animals by administering a lysine analog, such as EACA, to the animals on a continuous basis. In the preferred embodiment, the method of the present invention is directed to preventing and treating coccidial infections in poultry by adding EACA to the daily diet of a poultry flock. EACA may also be administered in ovo before hatching. The administration of EACA enhances the natural immune response of the poultry to the invading coccidial organisms and enables the poultry to combat the parasites without the need for antibiotics. Another aspect of the present invention involves preventing parasitic diseases in humans and animals by prophylactically administering a serine protease inhibitor, such as EACA, as an adjuvant in conjunction with a conventional vaccine effective against the target parasite.Type: GrantFiled: October 6, 1995Date of Patent: March 30, 1999Inventors: Guy R. Beretich, Sr., Louis D. Beretich
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Patent number: 5872101Abstract: Methods of use of compounds and compounds for the treatment of disorders characterized by the cerebral deposition of amyloid are provided. Among the compounds are those of formulae (I), (II) and (III): ##STR1## in which R.sub.1 is preferably 2-methyl propene, 2-butene, norleucine; R.sub.2, R.sub.4, and R.sub.8 are each independently methyl or ethyl; R.sub.3 is preferably iso-butyl or phenyl; R.sub.5 is preferably iso-butyl; R.sub.6 is H or methyl; R.sub.7 --(Q).sub.n is preferably benzyloxycarbonyl or acetyl; Q is preferably --C(O)--; R.sub.8 is preferbly iso-butyl; R.sub.A =--(T).sub.m --(D).sub.m --R.sub.1, is which T is preferably oxygen or carbon, and D is preferably a mono-unsaturated C.sub.3-4 alkenyl being more preferred; and X is an alcohol, particularly a secondary alcohol.Type: GrantFiled: May 18, 1995Date of Patent: February 16, 1999Assignee: Sibia Neurosciences, Inc.Inventors: Benito Munoz, Ian A. McDonald, Elisabeth Albrecht
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Patent number: 5863931Abstract: Amidino derivatives of formula (I) and salts, and pharmaceutically acceptable esters and amides thereof, in which: R.sup.1 is a C.sub.1-6 straight or branched chain alkyl group, a C.sub.2-6 alkenyl group, a C.sub.2-6 alkynyl group, a C.sub.3-6 cycloalkyl group or a C.sub.3-6 cycloalkylC.sub.1-6 alkyl group; Q is an alkylene, alkenylene or alkynylene group having 3 to 6 carbon atoms and which may optionally be substituted by one or more C.sub.1-3 alkyl groups; a group of formula --(CH.sub.2).sub.p X(CH.sub.2).sub.q -- where p is 2 or 3, q is 1 or 2 and X is S(O).sub.x where x is 0, 1 or 2, O or NR.sup.2 where R.sup.2 is H or C.sub.1-6 alkyl; or a group of formula --(CH.sub.2).sub.r A(CH.sub.2).sub.s -- where r is 0, 1 or 2, s is 0, 1 or 2 and A is a 3 to 6 membered carbocyclic or heterocyclic ring which may optionally be substituted by one or more suitable substituents such as C.sub.1-6 alkyl, C.sub.1-6 alkoxy, hydroxy, halo, nitro, cyano, trifluoro C.sub.1-6 alkyl, amino, C.sub.1-6 alkylamino or diC.sub.Type: GrantFiled: June 22, 1994Date of Patent: January 26, 1999Assignee: Glaxo Wellcome Inc.Inventors: Richard Mansfield Beams, Harold Francis Hodson, Richard Michael John Palmer
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Patent number: 5847206Abstract: New fluorinated derivatives useful as surfactants or in the transport of drug or markers, or in drug targeting, and preparations containing the derivatives, for medical, cosmetic and veterinary uses, having the formula: ##STR1## wherein R.sub.F is a fluorinated radical, X is a linear or branched alkylene, R.sup.1 is H or CH.sub.3, R.sup.2 is a radical having at least one OH group, R.sup.3 is a radical derived from an amino acid or a peptide, 1.ltoreq.n.ltoreq.50 and 0.ltoreq.m.ltoreq.200 with 0.2.ltoreq.n/n+m.ltoreq.1.These derivatives can be used as prodrugs or in formulating pharmaceutical, cosmetic and veterinary preparations, in biology and medicine, notably in compositions acting as carriers of oxygen and other gases, of contrast agents, or as carriers of substances used in therapy, or as carriers of markers.Type: GrantFiled: June 7, 1995Date of Patent: December 8, 1998Assignee: Alliance Pharmaceutical Corp.Inventors: Andre Pavia, Bernard Pucci, Jean G. Riess, Leila Zarif
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Patent number: 5811401Abstract: The present invention relates to advaced glycosylation endproducts formed by the reaction of arginine-lysine or lysine-arginine dipeptides, optionally as part of a larger protein or amino-containing-biomolecule, with reducing sugars. These AGEs can be used in various diagnostic and therapeutic methods.Type: GrantFiled: November 27, 1996Date of Patent: September 22, 1998Assignee: The Picower Institute for Medical ResearchInventors: Richard J. Bucala, Yousef Al-Abed
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Patent number: 5811398Abstract: This invention relates to compounds having the following formula ##STR1## or pharmaceutically acceptable salt thereof which are useful in the inhibition of platelet aggregation, to pharmaceutical compositions containing such compounds, and to a method of inhibiting platelet aggregation in mammals by administering such compounds and compositions.Type: GrantFiled: April 11, 1995Date of Patent: September 22, 1998Assignee: G. D. Searle & Co.Inventors: Norman Anthony Abood, Philippe Roger Bovy, Daniel Lee Flynn, Joseph Gerace Rico, Thomas Edward Rogers
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Patent number: 5807555Abstract: The present invention relates to a method and composition for topically administering a Smelophyllum capense extract as a cosmetic, dermatologic, or pharmaceutical composition to promote collagen synthesis. Administration of the composition results in the firming of the skin, improves healing and is suitable for treating various pathologies accompanied with a deficiency in collagen. The extract can also be added to cell culture medium used in the culture of skin cells, particularly skin fibroblasts. The composition can contain between 0.0001% and 1% by weight of the Smelophyllum capense extract, and the extract can be obtained by extraction with a polar solvent. The composition can contain other ingredients including ascorbic acid, madecassic acid, asiatic acid, madecassoside, asiaticoside, alpha-1-protease inhibitor, collagenase inhibitors, elastase inhibitors, lysine, proline, 2-oxoglutarate and ginsenoside Ro.Type: GrantFiled: June 18, 1997Date of Patent: September 15, 1998Assignee: LVMH RechercheInventors: Frederic Bonte, Marc Dumas, Catherine Lavaud, Georges Massiot
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Patent number: 5808069Abstract: The salts of S(+) 2-(3-benzoylphenyl)propionic acid and of R(-) 2-(3-benzoylphenyl)propionic acid with an organic base such as D-lysine, L-lysine, L-arginine, (R) 3-(4-phenylpiperazin-1-yl)propane-1,2-diol and (S) 3-(4-phenylpiperazin-1-yl)propane-1,2-diol, the process for their preparation and the corresponding pharmaceutical compositions containing said salts are described.Type: GrantFiled: October 31, 1995Date of Patent: September 15, 1998Assignees: Dompe' Farmaceutici SpA, Dimpe' SpAInventors: Enrico Bosone, Gaetano Clavenna, Carmelo Gandolfi, Marco Mantovanini, Roberto Curti
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Patent number: 5770574Abstract: Long-chain, unbranched alkylamides of the general formulaCH.sub.3 --(CH.sub.2).sub.n N--NH--Rin which n=11-20 and R=amino acid, its D- and L-enantiomers, di- and tripeptides, forms derived by N-protective groups, and terminal ethyl esters as well as its physiologically compatible salt forms as active pharmaceutical substances with anti-proliferative and anti-inflammatory properties.Type: GrantFiled: June 19, 1997Date of Patent: June 23, 1998Assignee: ASTA Medica AktiengesellschaftInventors: Bernhard Kutscher, Michael Bernd, Heinz Grossmann, Maria Kick, Jurgen Arp, Manfred Lieflander, Jurgen Engel, Rainer Voegeli
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Patent number: 5763657Abstract: The present specification discloses a ruminant feed additive composition which contains as an active ingredient a phosphoric acid-amino acid-polyvalent metal composite salt (final composite salt) which is insoluble in neutral or alkaline water and is soluble in acidic water and which can be obtained by treating a composite salt composed of a basic amino acid, magnesium and phosphoric acid with a salt of a divalent or trivalent (polyvalent) metal other than magnesium, or by treating the above-mentioned composite salt with the polyvalent metal salt and a condensed phosphoric acid component (alone) or the condensed phosphoric acid component and a phosphoric acid component (in combination), this composition taking the form of a powder or granules.Type: GrantFiled: August 28, 1997Date of Patent: June 9, 1998Assignee: Ajinomoto Co., Inc.Inventors: Toyoto Hijiya, Toru Ikeda, Kenichi Mori, Toshihide Yukawa, Tadashi Takemoto, Hajime Kamada
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Patent number: 5756761Abstract: A process for improving the solubility of hydrophobic amino acids in which hot saturated aqueous solutions of at least two different amino acids are first combined. A first step includes making a hot saturated aqueous solution of a first and hydrophobic amino acid having a low solubility in water. A second step includes making a hot saturated aqueous solution of a second and hydrophilic amino acid having a high solubility in water. Then the two hot saturated aqueous solutions are mixed to prepare a combined hot solution mixture, and dried. The resulting product is an amino acid food supplement which is blended into animal feed. The preferred amino acids are tryptophan and lysine, when the animal is a domestic farm animal. A preferred ratio is where the concentration of tryptophan is greater than 50 grams per liter and the concentration of lysine is greater than 300 grams per liter.Type: GrantFiled: June 5, 1995Date of Patent: May 26, 1998Assignee: Archer Daniels Midland CompanyInventors: Daniel Dueppen, Thomas Binder, Mark Matlock
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Patent number: 5750572Abstract: 4,7,10,13,16,19-cis-Docosahexaenoic acid (DHA) salts with basic amino acids, in particular arginine and lysine, have favorable therapeutic and technological characteristics compared with the acid.Type: GrantFiled: July 5, 1996Date of Patent: May 12, 1998Assignee: Prospa B.V.Inventor: Tiberio Bruzzese