Amine Addition Salts Patents (Class 549/316)
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Patent number: 7102019Abstract: An ascorbic acid derivative of the formula Ia: where the variables independently of one another have the following meanings: R1 and R2 independently of one another are hydrogen or C1-C20-acyl; R3 is hydrogen or a cation selected from the group consisting of NH4+, alkali metal and alkaline earth metal cations; R4 is C1-C6-alkoxycarbonyl, and a process for its preparation.Type: GrantFiled: October 1, 2001Date of Patent: September 5, 2006Assignee: BASF AktiengesellschaftInventors: Harald Streicher, Bernd Ostersehlt, Horst Westenfelder
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Publication number: 20040010038Abstract: The subject invention provides derivatives of propargylamino indan (PAI) and propargylamino tetralin that selectively inhibit monoamine oxidase (MAO) in the brain, having the structure: 1Type: ApplicationFiled: February 27, 2003Publication date: January 15, 2004Inventors: Eran Blaugrund, Yaacov Herzig, Jeffrey Sterling
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Publication number: 20020161039Abstract: Crystalline ascorbate, in particular choline ascorbate in the form of crystals free from water of crystallization, processes for its preparation, and its used are described.Type: ApplicationFiled: February 19, 2002Publication date: October 31, 2002Inventors: Ludwig Volkel, Alfred Oftring, Oliver Hasselwander, Ulrike Sindel, Klaus Kramer
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Patent number: 6388098Abstract: A process for preparing a high-purity ascorbic acid-2-monophosphate salt in a convenient manner and in a high yield, comprising hydrolyzing an ascorbic acid-2-polyphosphate or a salt thereof in the presence of magnesium ion at a pH of 7 or more.Type: GrantFiled: March 17, 2000Date of Patent: May 14, 2002Assignee: Showa Denko Kabushiki KaishaInventors: Kazuhiro Ohmori, Yuji Kobayashi, Tomokazu Soda
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Publication number: 20020035273Abstract: A process for preparing a high-purity ascorbic acid-2-monophosphate salt in a convenient manner and in a high yield, comprising hydrolyzing an ascorbic acid-2-polyphosphate or a salt thereof in the presence of magnesium ion at a pH of 7 or more.Type: ApplicationFiled: March 17, 2000Publication date: March 21, 2002Inventors: Kazuhiro Ohmori, Yuji Kobayashi, Tomokazu Soda
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Patent number: 6169187Abstract: The invention provides a process for the recovery of ascorbic acid from a feed containing at least one precursor of ascorbic acid comprising converting the precursor into at least one product, the at least one product being ascorbic acid in an organic extractant composition, the organic extractant composition comprising at least one secondary or tertiary alkyl amine in which the aggregate number of carbon atoms is at least 20, as a primary extractant, and a polar extraction enhancer compound; wherein the extractant composition comprises at least 2 moles of the polar extraction enhancer compound per one mole of primary extractant; and subjecting the ascorbic acid-containing organic extractant composition to a stripping operation with aqueous solution at a temperature of at least 20° C. higher than the temperature at which the conversion is carried out; whereby there is obtained an aqueous solution of ascorbic acid in which the concentration of ascorbic acid is higher than 5%.Type: GrantFiled: August 9, 1999Date of Patent: January 2, 2001Assignee: Yissum Research Development Company of the Hebrew University of JerusalemInventor: Aharon Meir Eyal
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Patent number: 5916915Abstract: Disclosed herein are a L-ascorbic acid derivative having an improved water-in-stability, represented by a following general formula (I): ##STR1## and a method for preparation thereof, and to a skin-whitening cosmetic composition containing the same as an active ingredient.Type: GrantFiled: June 4, 1998Date of Patent: June 29, 1999Assignee: Pacific CorporationInventors: Jong Eon Hong, Ki Hwa Lee, Jun Chul Cho, Jang Sob Lee, Jung No Lee, Ji Min Chun, Dong Il Jang, Ok Sob Lee, Sang Rhin Lee
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Patent number: 5863939Abstract: Creatine ascorbates are described which have the general formula (I)(creatine).sub.z (ascorbate).sub.y (H.sub.2 O).sub.n (I)wherez=1 to 100y=1 to 100 andn=0 to 20.These creatine ascorbates, which can be produced by way of the relatively simple reaction of creatine with ascorbic acid, can be used for enhancing muscular development and strength in the field of sport, as prophylactics against and for the treatment of conditions of oxygen deficit (ischemia) and as immune system stimulants in the field of health, for the treatment of muscular atrophy and as food supplements.Type: GrantFiled: July 22, 1997Date of Patent: January 26, 1999Assignee: SKW Trostberg AktiengesellschaftInventors: Ivo Pischel, Stefan Weiss, Christian Gloxhuber, Bernd Mertschenk
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Patent number: 5679801Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is --CH.sub.2 R;Y is --O-- or --S--;R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl;or a pharmaceutically acceptable salt thereof;which by virtue of their ability to inhibit PLA.sub.2, are of use as antiinflammatory agents and there is also disclosed a method for the treatment of immunoinflammatory conditions, such as allergy, anaphylaxis, asthma and inflammation in mammals.Type: GrantFiled: May 15, 1995Date of Patent: October 21, 1997Assignee: American Home Products CorporationInventors: Craig E. Caufield, James M. Rinker
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Patent number: 5656662Abstract: The present invention relates to a method for synthesis of optically pure 4-alkenyl or 4-alkanyl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase, thus making them useful in the treatment of coronary artery diseases, especially atherosclerosis, and additionally, as inhibitors of various inflammatory cytokines, making them useful in the treatment of both acute and chronic inflammation, as well in the treatment of cachexia, rheumatoid arthritis, multiple sclerosis, Crohn's disease and ulcerative colitis. The invention further relates to pharmaceutical compositions of the instant compounds.Type: GrantFiled: June 7, 1995Date of Patent: August 12, 1997Assignee: The Ohio State University Research FoundationInventors: Padmaja Mantri, Donald T. Witiak
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Patent number: 5516919Abstract: Metal salts or substitutted or non-substituted ammonium salts of ascorbic acid derivatives can be produced in high yield by treating an acidic aqueous solution containing ascorbic acid-2-phosphate or ascorbic acid-2-sulfate with a porous adsorbent such as activated carbon, followed by treating the adsorbent with a basic aqueous solution containing e.g. a metal salt of an organic acid or substituted or non-substituted ammonium salt ion to elute the desired salt of ascorbic acid derivative.Type: GrantFiled: April 18, 1995Date of Patent: May 14, 1996Assignee: Wako Pure Chemical Industries, Ltd.Inventors: Atsunori Sano, Kuniaki Okamoto, Jun Ebashi
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Patent number: 5504108Abstract: The present invention relates to a method for synthesis of optically pure stereogenically labile 4-aryl-2-hydroxytetronic acids from an optically pure aidehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase, and additionally as inhibitors of cyclooxygenase and 5-lipoxygenase. The invention further relates to the pharmaceutical use of such.compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis, and in the treatment of various inflammatory pathologies, especially arthritis.Type: GrantFiled: December 5, 1994Date of Patent: April 2, 1996Assignee: The Ohio State University Research FoundationInventors: Donald T. Witiak, Allen T. Hopper
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Patent number: 5504107Abstract: The present invention relates to a method for synthesis of optically pure 4-alkenyl or 4-alkanyl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. The invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.Type: GrantFiled: May 19, 1994Date of Patent: April 2, 1996Assignee: The Ohio State University Research FoundationInventors: Padmaja Mantri, Donald T. Witiak
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Patent number: 5399721Abstract: The present invention relates to a method for synthesis of optically pure stereogenically labile 4-aryl-2-hydroxytetronic acids from an optically pure aldehyde. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. the invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.Type: GrantFiled: February 25, 1994Date of Patent: March 21, 1995Assignee: The Ohio State University Research FoundationInventors: Allen T. Hopper, Donald T. Witiak
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Patent number: 5359139Abstract: A tert-amine which contains an acid-activated color body precursor is treated to prevent it or a derivative thereof, e.g., an amine oxide, betaine, or quaternary ammonium compound, from turning pink when exposed to acidic conditions by contacting it with ascorbic acid.Type: GrantFiled: March 18, 1991Date of Patent: October 25, 1994Assignee: Albemarle CorporationInventors: Kim R. Smith, James E. Borland, Joe D. Sauer
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Patent number: 5298526Abstract: The present invention relates to a method for synthesis of optically pure stereogenically labile 4-substituted-2-hydroxytetronic acids from an asymmetric .alpha.-hydroxy ester. The chiron approach of the present invention utilizes a non-nucleophilic lithium amide base under kinetically controlled Claisen conditions to produce a 4-substituted-2-pheylmethoxy precursor to the 4-substituted-2-hydroxy tetronic acid. The invention further relates to the use of such optically pure compounds as potent inhibitors of platelet aggregation by working at the level of cyclooxygenase. The invention further relates to the pharmaceutical use of such compounds in the treatment of coronary artery diseases, especially in the treatment and/or prevention of atherosclerosis.Type: GrantFiled: March 6, 1992Date of Patent: March 29, 1994Assignee: The Ohio State University Research FoundationInventors: Donald T. Witiak, Ashok K. Tehim
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Patent number: 5283258Abstract: A procaine acid addition salt, wherein the acid is attached to the diethylamino nitrogen, is complexed with a biologically active organic acid such as a vitamin acid, essential unsaturated fatty acid, C.sub.4 to C.sub.6 hydroxycarboxylic acid or alpha amino acid in stoichiometric ratios of organic acid to procaine acid addition salt to form a double salt complex wherein the organic acid attaches to the p-amino nitrogen. Such double salt complexes protect the procaine molecule from cholinesterase hydrolysis when orally administered to warm blooded animals allowing the complex to be carried intact to the site of damaged cells and across the cell membrane where the double salt complex is disassociated in the cell releasing the organic acid and procaine for cellular repair and regeneration. Procaine hydrochloride is the preferred procaine salt. Preferred acids are citric and vitamin acids including nicotinic acid, ascorbic acid, biotin and folic acid.Type: GrantFiled: September 25, 1992Date of Patent: February 1, 1994Inventor: Robert Koch
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Patent number: 5270336Abstract: Derivatives of 3,4-dihydroxy-2,5-dihydrofuran-5-ones, intermediates and processes useful for their preparation are disclosed. These compounds are useful as free-radical scavengers and exhibit cellular protective properties.Type: GrantFiled: August 26, 1992Date of Patent: December 14, 1993Assignee: Merrell Dow Pharmaceuticals Inc.Inventors: Gilbert Marciniak, J. Martin Grisar
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Patent number: 5242945Abstract: There are disclosed compounds of the formula: ##STR1## wherein X is --CH.sub.2 R;R is ##STR2## and further when Y=S, R may also be --(CH.sub.2).sub.e CH.sub.3 ; Y is --O--or --S--;R.sup.1 and R.sup.2 are each, independently, hydrogen or lower alkyl;R.sup.3 is indolyl, furyl, phenyl or phenyl optionally mono- or disubstituted independently by alkyl of 1-7 carbon atoms, --C(CH.sub.3).sub.3, --C(CH.sub.3).sub.2 CH.sub.2 C(CH.sub.3).sub.3, --C(CH.sub.3).sub.2 CH.sub.2 CH.sub.3, haloloweralkyl, perfluoroalkyl, lower alkoxy, aryl alkoxy, halo or nitro;R.sup.4 and R.sup.5 are, independently, --COCH.sub.2 R.sup.7, --CO.sub.2 R.sup.7, --CONHR.sup.7, geranyl or CH.sub.2 R.sup.3 ;R.sup.6 is hydrogen or lower alkyl;R.sup.7 is geranyl and any moiety selected from R other than ##STR3## A and B are, independently, --O--, --S-- or --NR.sup.6 --; and a is 0-8;b is 1-10 when Y=S, and 2-10 when Y=O;c is 1-3;d is 0-9; ande is 3-18;which by virtue of their ability to inhibit PLA.sub.Type: GrantFiled: April 12, 1991Date of Patent: September 7, 1993Assignee: American Home Products CorporationInventors: Craig E. Caufield, James M. Rinker
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Patent number: 5189057Abstract: A compound of the formula (I): ##STR1## wherein R.sub.1 and R.sub.2 each is a hydrocarbon residue, R.sub.3 is a sulfo group or phosphono group, --CO--R.sub.4 is an esterified carboxyl group, a thiol-esterified carboxyl group or an amidated carboxyl group; and .about. represents the absolute configuration of R or S, or its salt, which is useful for preventing and treating thrombosis.Type: GrantFiled: July 19, 1991Date of Patent: February 23, 1993Assignee: Takeda Chemical Industries, Ltd.Inventors: Koichi Kato, Hirotomo Masuya, Moriya Norihiko
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Patent number: 5180839Abstract: P-carboethoxy ammonium ascorbate as an anti-thrombotic compound and method of making same from ascorbic acid and ethyl p-amino benzoate.Type: GrantFiled: August 30, 1990Date of Patent: January 19, 1993Inventors: Philip N. Sawyer, Leon D. Freeman
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Patent number: 5041563Abstract: A process for the manufacture of ascorbic acid from 2-ketogulonic acid esters (KGAE) utilizing amine salts of the latter is disclosed.Type: GrantFiled: May 22, 1990Date of Patent: August 20, 1991Assignee: Hoffman-La Roche Inc.Inventors: Peter Fahrni, Theodor Siegfried
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Patent number: 5002950Abstract: The present invention is various 7-deazaguanines having activity as immunomodulators. Also included are pharmaceutical compositions and methods of use thereof.Type: GrantFiled: February 1, 1990Date of Patent: March 26, 1991Assignee: Warner-Lambert CO.Inventors: Thomas C. Malone, Jagadish C. Sircar
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Patent number: 4526989Abstract: This disclosure describes symmetrical 1,4-bis (substituted-amino)-5,8-dihydroxyanthraquinones useful as chelating agents and for inhibiting the growth of transplanted mouse tumors.Type: GrantFiled: October 23, 1979Date of Patent: July 2, 1985Assignee: American Cyanamid CompanyInventors: Keith C. Murdock, Frederick E. Durr
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Patent number: 4368330Abstract: 5,6-Anhydro-L-ascorbic acid, 5,6-anhydro-D-erythorbic acid and salts thereof are disclosed. Such compounds are useful intermediates in the preparation of 6-deoxy-6-substituted-L-ascorbic acid and 6-deoxy-6-substituted-D-erythorbic acid, which are useful as antioxidants. Novel 6-deoxy-6-substituted-L-ascorbic and -D-erythorbic acid derivatives are also disclosed.Type: GrantFiled: April 30, 1981Date of Patent: January 11, 1983Assignee: Pfizer Inc.Inventor: Glenn C. Andrews
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Patent number: 4329290Abstract: A solution of L-ascorbic acid and a solution of para amino benzoic acid are mixed and the mixture evaporated to permit recovery of a solid compound. The compound is administered to a host to reduce thrombotic tendencies.Type: GrantFiled: January 31, 1980Date of Patent: May 11, 1982Inventors: Philip N. Sawyer, Leon D. Freeman