Additional Nitrogen In Acid Moiety Patents (Class 560/169)
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Patent number: 4601889Abstract: A process for the recovery of a heavy metal which comprises:bringing a polymer having pendant groups of the formula:--CO--NH--NH--CO--COOMin which M is hydrogen, sodium or potassium, into contact with an aqueous solution containing a heavy metal to have the heavy metal adsorbed by said polymer;andhaving said heavy metal desorbed from the said polymer.Type: GrantFiled: October 31, 1983Date of Patent: July 22, 1986Assignee: UBE Industries, Ltd.Inventors: Nagayoshi Sakamoto, Junichi Kugimoto
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Patent number: 4596819Abstract: Modified oxytocin-vasopressin di- or tri-peptides wherein an amide group is replaced by a group selected from ##STR1## --CH.sub.2 NH--, --CH.sub.2 O--, --CH.sub.2 S--, --CH.sub.2 SO--, --CH.sub.2 SO.sub.2 --, --CH.sub.2 CH.sub.2 -- and --CH.dbd.CH-- are described as well as methods for their manufacture, pharmaceutical compositions and methods for treatment, especially of cognitive disorders, depression, morphine dependency and parkinsonism by adjunctive therapy.Type: GrantFiled: January 23, 1984Date of Patent: June 24, 1986Assignee: Warner-Lambert CompanyInventors: Ernest D. Nicolaides, Francis J. Tinney, James S. Kaltenbronn, Dana E. DeJohn, Elizabeth A. Lunney, W. Howard Roark, Joseph T. Repine
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Patent number: 4594188Abstract: An enkephalin-degrading aminopentidase enzyme is inhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salt thereof, wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl, carboxyalkyl, halo substituted alkyl, hydroxyalkyl, aminoalkyl, mercaptoalkyl, alkylthioalkyl, (cycloalkyl)alkyl, (heteroaryl)alkyl, arylalkyl, carbamoylalkyl, guanidinylalkyl, or heteroaryl;R.sub.3 is hydroxy, alkoxy, (substituted alkyl)oxy, arylalkoxy, (heteroaryl)alkoxy or --NY.sub.1 Y.sub.2, wherein Y.sub.1 and Y.sub.2 are each independently hydrogen, alkyl, aryl, or arylalkyl or Y.sub.1 is hydrogen and Y.sub.2 is substituted alkyl or (heteroaryl)alkyl;A.sub.1 is glycyl, alanyl, leucyl, phenylalanyl, arginyl, sarcosyl, seryl, asparagyl, lysyl, glutamyl, histidyl, tryptophyl, cysteinyl, methionyl, threonyl, tyrosyl, leucyl, valyl, aspartyl, prolyl, norleucyl, norvalyl, or ##STR2## wherein n.sub.6 is an integer of 2 to 15; A.sub.2, A.sub.3, A.sub.4 and A.sub.Type: GrantFiled: May 20, 1985Date of Patent: June 10, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Norma G. Delaney, Eric M. Gordon
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Patent number: 4576748Abstract: .beta.-Lactams of the formula: ##STR1## their preparation and use are disclosed.Type: GrantFiled: September 17, 1984Date of Patent: March 18, 1986Assignee: Merck & Co., Inc.Inventors: William J. Greenlee, Arthur A. Patchett
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Patent number: 4563478Abstract: The invention relates to compounds possessing GABA-like sedative and tranquilizing activity, characterized by being of general formula:X.sub.1 OC--(CH.sub.2).sub.2 --NH--(CH.sub.2).sub.3 --CO--X.sub.2whereX.sub.1 and X.sub.2 are hydroxyl, a C.sub.1 -C.sub.6 alkoxy group or a free or substituted amino group, X.sub.1 being the same as or different from X.sub.2.The invention also relates to processes for their preparation, and composition for pharmaceutical and veterinary use which contains them.Type: GrantFiled: May 24, 1985Date of Patent: January 7, 1986Assignee: Hepar Chimie S.A.Inventors: Maria Curti, Fernando Fussi
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Patent number: 4560795Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein Y is F.sub.2 CH--, F.sub.3 C--, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR2## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR3## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.Type: GrantFiled: February 6, 1984Date of Patent: December 24, 1985Assignee: Merrell Dow France et Cie.Inventors: Philippe Bey, Michel Jung
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Patent number: 4558120Abstract: Dense star polymers having terminal group densities greater than conventional star polymers exhibit greater and more uniform reactivity than their corresponding conventional star polymers. For example, a third generation, amine-terminated polyamidoamine dense star polymer prepared from ammonia, methyl acrylate and ethylenediamine has 1.24.times.10.sup.-4 amine moieties per unit volume (cubic Angstrom units) in contrast to the 1.58.times.10.sup.-6 amine moieties per unit volume contained by a conventional star polymer. Such dense star polymers are useful as demulsifiers for oil/water emulsions, wet strength agents in the manufacture of paper, and agents for modifying viscosity in aqueous formulations such as paints.Type: GrantFiled: December 27, 1983Date of Patent: December 10, 1985Assignee: The Dow Chemical CompanyInventors: Donald A. Tomalia, James R. Dewald
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Patent number: 4545804Abstract: Novel N(aminophosphinylmethyl)glycine derivatives are described that show significant herbicidal activity.Type: GrantFiled: November 21, 1983Date of Patent: October 8, 1985Assignee: Monsanto CompanyInventors: John E. Franz, Robert J. Kaufman
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Patent number: 4531010Abstract: A curing agent for fluorocarbon polymer coating compositions having the formula ##STR1## where R is R.sup.1 NH, R.sup.1 is an aliphatic or cycloaliphatic hydrocarbon radical, R.sup.2 is C or an aliphatic hydrocarbon group, R.sup.3 is H or CH.sub.3, where x is 3 when R.sup.2 is a hydrocarbon group and x is 4 when R.sup.2 is C; the curing agents form ambient curing fluorocarbon polymer coating compositions;These compositions are used to provide corrosion and abrasion resistant coatings for large structures in chemical plants, oil refineries, oil drilling platforms, and the interior of smoke stacks of large utility companies.Type: GrantFiled: December 30, 1983Date of Patent: July 23, 1985Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joseph A. Vasta
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Patent number: 4526987Abstract: Lactones of the formula ##STR1## wherein R is hydrogen or a CX.sub.3 group, and each X is a chlorine or bromine atom, are converted to the known cis-3-(2,2-dihalovinyl)-2,2-dimethylcyclopropanecarboxylic acids or lower alkyl esters, from which pyrethroid insecticides are obtained.Type: GrantFiled: January 3, 1979Date of Patent: July 2, 1985Assignee: FMC CorporationInventors: Kiyoshi Kondo, Toshiyuki Takashima, Daiei Tunemoto
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Patent number: 4515803Abstract: Compounds of the formula I ##STR1## in which n denotes 0-3,R.sup.1 and R.sup.1' are the same or different and denote hydrogen, alkyl or alkenyl, phenyl or benzyl, each substituted as desired;R.sup.2 denotes hydrogen, alkyl or alkenyl;R.sup.3 denotes hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl or aminoalkyl, alkanoylaminoalkyl, guanidinoalkyl, imidazolylalkyl, indolylalkyl, mercaptoalkyl or alkylthioalkyl, phenylalkyl, hydroxyphenylalkyl, phenoxyalkyl or phenylthioalkyl, or R.sup.2 and R.sup.3, together with the C and N atoms carrying them, denote a saturated or unsaturated 4- to 8-membered monocyclic or 8- to 10-membered bicyclic isocycle or heterocycle, optionally monosubstituted or disubstituted by hydroxyl, alkoxy having 1 to 3 C atoms or alkyl,R.sup.4 denotes hydrogen, alkyl, alkenyl, alkadienyl, alkinyl, alkeninyl or alkadiinyl, cycloalkyl, phenyl, benzyl, phenethyl or phenylpropyl, each of which can be optionally monosubstituted or disubstituted;R.sup.5 denotes hydrogen or alkyl, hydroxyl or alkoxy andR.Type: GrantFiled: September 1, 1982Date of Patent: May 7, 1985Assignee: Hoechst AktiengesellschafatInventors: Rainer Henning, Hansjorg Urbach, Rolf Geiger, Volker Teetz, Bernward Scholkens
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Patent number: 4496389Abstract: This disclosure relates to alkyl N-trifluoroacetyl-N-phosphonomethylglycine amide and hydrazide derivatives, to herbicidal compositions containing same and to the herbicidal use thereof. These amide and hydrazide derivatives are useful as pre-emergent and/or post-emergent herbicides.Type: GrantFiled: May 11, 1984Date of Patent: January 29, 1985Assignee: Monsanto CompanyInventors: John E. Franz, Robert J. Kaufman
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Patent number: 4491583Abstract: A process for inducing the production of endogenous interferon in a vertebrate animal which comprises parenterally, intranasally or topically adminstering to the animal an interferon-inducing effective amount of composition containing as the essential active ingredient a compound of the formula ##STR1## or a non-toxic acid addition salt thereof wherein R.sub.7 and R.sub.8 are each alkyl of from 12 to 30 carbon atoms and Z is selected from the group consisting of N-(lower alkyl)-piperazino and N-(W-hydroxy-lower alkyl)-piperazino, said lower alkyl groups having from 1 to 4 carbon atoms.Type: GrantFiled: July 18, 1983Date of Patent: January 1, 1985Assignee: Pfizer Inc.Inventors: Timothy H. Cronin, Hermann Faubl, William W. Hoffman, James J. Korst
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Patent number: 4489008Abstract: Hydrolytically stable hydroxyl-terminated liquid polymers that are useful in the preparation of polyurethanes prepared by reacting at least one aminoalcohol with a carboxyl-terminated liquid polymer having a carbon-carbon backbone. The hydroxyl-terminated polymers have the formula ##STR1## wherein B is a carbon-carbon backbone, X is HO-- or HO--Y-- a univalent radical obtained by removing a hydrogen atom from an amine group of aminoalcohol containing one primary or secondary hydroxyl group and one primary or secondary amine group per molecule, and the polymers contain an average of greater than 1.5 terminal hydroxyl groups per molecule.Type: GrantFiled: August 9, 1982Date of Patent: December 18, 1984Assignee: The B. F. Goodrich CompanyInventor: Changkiu K. Riew
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Patent number: 4455308Abstract: This invention relates to novel compounds of the formula ##STR1## wherein R.sup.1 is lower alkenyl or lower alkynyl; R.sup.2 is lower alkenyl, lower alkynyl or cycloalkyl; R.sup.3 is hydrogen; R.sup.4 is alkyl, cycloalkyl or lower alkoxycarbonylalkyl or R.sup.2 and R.sup.3 are joined to form dimethyleneoxy (i.e. --CH.sub.2 OCH.sub.2 --) or R.sup.3 and R.sup.4 taken together with the nitrogen to which they are attached, form a 5- to 6- membered heterocyclic ring, compositions containing said compounds and a method of employing said compounds as arthropod repellents.Type: GrantFiled: September 29, 1982Date of Patent: June 19, 1984Assignee: Rohm and Haas CompanyInventor: Joel R. Smolanoff
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Patent number: 4443475Abstract: Novel amides of acyl-carnitines having general formula ##STR1## wherein R' is acetyl, propionyl, butyryl (unsubstituted or halogen-substituted) isobutyryl, .beta.-hydroxybutyryl, acetoacetyl, pantothenyl, and linoleyl, and R" is either an unsubstituted amino radical (provided that R' is ather than acetyl) or a substituted amino radical, are therapeutically effective in treatment of functional arrythmias or arrhythmias secondary to myocardialsclerotic diseases and as psychosti-mulants.Type: GrantFiled: May 26, 1982Date of Patent: April 17, 1984Inventor: Claudio Cavazza
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Patent number: 4439619Abstract: Fluorinated alkenylene diamine compounds are inhibitors of ornithine decarboxylase enzyme in vivo and have the following formula: ##STR1## wherein: R.sub.a represents hydrogen or R.sub.2, where R.sub.2 is as defined below;R.sub.b represents hydrogen or, when R.sub.a is hydrogen, R.sub.2, where R.sub.2 is as defined below;R.sub.c represents hydrogen or --COR.sub.3, where R.sub.3 is as defined below;R.sub.1 represents hydrogen or C.sub.1 --C.sub.6 alkyl;each R.sub.2, independently, represents C.sub.2 -C.sub.5 alkylcarbonyl, phenylcarbonyl, phenyl-(C.sub.1 -C.sub.4 alkyl) carbonyl, or an aminocarboxylic acid residue derived by removal of an hydroxy group from a carboxy moiety of an L-aminocarboxylic acid;R.sub.3 represents hydroxy, or, when R.sub.a and R.sub.b are both hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.4 R.sub.5, where R.sub.4 and R.sub.5 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;R.sub.4 and R.sub.Type: GrantFiled: August 21, 1981Date of Patent: March 27, 1984Assignee: Merrell Toraude et CompagnieInventors: Philippe Bey, Fritz Gerhart, Michel Jung
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Patent number: 4438270Abstract: Novel halomethyl derivatives of .alpha.-amino acids of the following general structure: wherein Y is ClCH.sub.2, F.sub.2 CH--, F.sub.3 C--, ClCH.sub.2 --, Cl.sub.2 CH--; Z is .beta.-methylthioethyl, .beta.-thioethyl, .beta.-benzylthioethyl; S-(5'-desoxyadenosin-5'-yl)-S-methylthioethyl, .gamma.-guanidinopropyl, R.sub.a HN(CH.sub.2).sub.n -- wherein n is the integer 3 or 4 or ##STR1## wherein Y.sub.2 is F.sub.2 CH--, or F.sub.3 C--; each of R.sub.a and R.sub.b can be the same or different and is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## wherein R.sub.2 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; R.sub.1 is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.Type: GrantFiled: June 25, 1982Date of Patent: March 20, 1984Assignee: Merrell Toraude et CompagnieInventors: Philippe Bey, Michel Jung
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Patent number: 4432907Abstract: Species-linked diamine triacetic acids of the formula ##STR1## wherein T is an organic species containing at least one amine, hydroxyl, or thio functional group, L is the residue of at least one of those functional groups and R is a two or more atom long covalent bridge, are disclosed. Methods for their preparation, for the preparation of metal chelates from them and for the use of the chelates are also disclosed. In a preferred embodiment, the metal ions employed in the formation of the chelates are rare earth metal ions capable of forming fluorescent chelates which can in turn be employed in fluoroassay techniques.Type: GrantFiled: May 5, 1981Date of Patent: February 21, 1984Assignee: Analytical Radiation CorporationInventors: Irwin Wieder, Robert H. Wollenberg
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Patent number: 4431790Abstract: Disclosed are novel curing agents for polyurethanes comprising reaction products of (1) a polyoxy alkylenepolyamine with (2) an alpha-substituted acrylic acid derivative wherein the substituent has a terminal hydroxyl group or (3) with a compound having an oxyrane ring and reaction products of (1) and (2) above, with (3) and (1) and (3) above, with (2). Also disclosed is a process for making polyurethanes by condensing a polyol with an isocyanate in the presence of the present curing agents in an amount ranging from 5 to 100 percent by weight of the polyol.Type: GrantFiled: August 3, 1981Date of Patent: February 14, 1984Assignee: Texaco Inc.Inventors: Arihiko Umeda, Seiichi Ota, Yoshiyuki Iwase
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Patent number: 4423073Abstract: Novel fluorinated alkenylene diamine derivatives are inhibitors of ornithine decarboxylase enzyme and have the following general Formula I: ##STR1## wherein: R.sub.c represents hydrogen or --COR.sub.5, where R.sub.5 is as defined below;R.sub.1 represents hydrogen or C.sub.1 -C.sub.6 alkyl;one of R.sub.2 and R.sub.3 represents hydrogen and the other represents C.sub.1 -C.sub.6 alkyl.R.sub.5 represents hydroxy or C.sub.1 -C.sub.8 alkoxy; andp represents 1 or 2.Type: GrantFiled: August 11, 1982Date of Patent: December 27, 1983Assignee: Merrell Toraude et CompagnieInventors: Fritz Gerhart, Viviane Van Dorsselaer
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Patent number: 4418077Abstract: Fluorinated aminobutyric acid and diaminobutane compounds in vivo are inhibitors of gamma-aminobutyric acid transaminase and have the following formula: ##STR1## wherein: Y represents hydrogen or fluorine;Z represents --CH.sub.2 NR.sub.1 R.sub.2, where R.sub.1 and R.sub.2 are as defined below, or --COR.sub.3 where R.sub.3 is as defined below;R.sub.a represents hydrogen or R.sub.4, where R.sub.4 is as defined below;R.sub.1 represents hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl-(C.sub.1 -C.sub.4 alkyl);R.sub.2 represents hydrogen, C.sub.1 -C.sub.6 alkyl, phenyl-(C.sub.1 -C.sub.4 alkyl) or, when R.sub.a is hydrogen, R.sub.4, where R.sub.4 is as defined below;R.sub.3 represents hydroxy, or when R.sub.a is hydrogen, C.sub.1 -C.sub.8 alkoxy, --NR.sub.5 R.sub.6, where R.sub.5 and R.sub.6 are as defined below, or an aminocarboxylic acid residue derived by removal of an hydrogen atom from the amino moiety of an L-aminocarboxylic acid;each R.sub.4, independently, represents C.sub.2 -C.sub.Type: GrantFiled: August 21, 1981Date of Patent: November 29, 1983Assignee: Merrell Toraude et CompagnieInventors: Philippe Bey, Fritz Gerhart, Michel Jung, Daniel Schirlin
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Patent number: 4414410Abstract: Alkyl esters, such as ethyl acetate, are prepared by contacting the corresponding next lower carbon number alkyl ester, such as methyl acetate, with carbon monoxide and hydrogen in the presence of an iodine or iodide-free catalyst composition comprising a ruthenium-containing compound, a cobalt containing compound and a quaternary phosphonium salt or base, and heating the mixture to an elevated temperature and pressure for sufficient time to produce the desired higher alkyl ester, and then recovering the same from the reaction mixture.Type: GrantFiled: January 13, 1982Date of Patent: November 8, 1983Assignee: Texaco Inc.Inventors: Jiang-Jen Lin, John F. Knifton
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Patent number: 4400529Abstract: Herbicide antidote compounds, compositions, and methods of use are disclosed in which compounds of the formula ##STR1## wherein R can be selected from the group consisting of alkyl groups having from about 1 to about 7 carbon atoms, aryl, and substituted aryl groups in which the substituent group can be lower alkyl having from about 1 to about 3 carbon atoms, substituted lower alkyls of from about 1 to about 3 carbon atoms in which the substituent group is halogen or nitro, lower alkoxy having from about 1 to about 3 carbon atoms; R.sub.1 can be selected from the group consisting of hydrogen or lower alkyl having from about 1 to about 6 carbon atoms; R.sub.2 can be selected from the group consisting of lower alkoxy having from about 1 to about 3 carbon atoms, and X is oxygen or sulfur; are disclosed as suitable for use as suitable for use as herbicide antidotes, when used in conjunction with thiolcarbamate herbicides.Type: GrantFiled: March 22, 1982Date of Patent: August 23, 1983Assignee: Stauffer Chemical CompanyInventor: Hsiao-Ling M. Chin
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Patent number: 4395569Abstract: A sulfonic acid salt of an acyloxyalkylamine is prepared by reaction of an organic acid or amino-acid with a sulfonic acid salt of an alkanolamine. Isocyanates are prepared therefrom by reaction with phosgene.Type: GrantFiled: December 17, 1979Date of Patent: July 26, 1983Assignee: Rohm and Haas CompanyInventors: Sheldon N. Lewis, Jerome F. Levy
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Patent number: 4359332Abstract: This disclosure relates to alkyl N-trifluoroacetyl-N-phosphonomethylglycine amide and hydrazide derivatives, to herbicidal compositions containing same and to the herbicidal use thereof. These amide and hydrazide derivatives are useful as pre-emergent and/or post-emergent herbicides.Type: GrantFiled: July 10, 1978Date of Patent: November 16, 1982Assignee: Monsanto CompanyInventors: John E. Franz, Robert J. Kaufman
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Patent number: 4358606Abstract: Novel esters of phenylalkyloxy- or phenylalkylthioacylamino acids and pyridylalkyloxy- or pyridylalkylthioacylamino acids, synthesis thereof, intermediates therefor, and the use of said esters for the control of weeds.Type: GrantFiled: June 19, 1981Date of Patent: November 9, 1982Assignee: Zoecon CorporationInventors: Shy-Fuh Lee, Clive A. Henrick
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Patent number: 4353731Abstract: This disclosure relates to alkyl N-trifluoroacetyl-N-phosphonomethylglycine amide and hydrazide derivatives, to herbicidal compositions containing same and to the herbicidal use thereof. These amide and hydrazide derivatives are useful as pre-emergent and/or post-emergent herbicides.Type: GrantFiled: April 2, 1981Date of Patent: October 12, 1982Assignee: Monsanto CompanyInventors: John E. Franz, Robert J. Kaufman
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Patent number: 4352751Abstract: Species-linked diamine triacetic acids of the formula ##STR1## wherein T is an organic species containing at least one amine, hydroxyl, or thiol functional group, L is the residue of at least one of those functional groups and R is a two or more atom long covalent bridge, are disclosed. Methods for their preparation, for the preparation of metal chelates from them and for the use of the chelates are also disclosed. In a preferred embodiment, the metal ions employed in the formation of the chelates are rare earth metal ions capable of forming fluorescent chelates which can in turn be employed in fluoroassay techniques.Type: GrantFiled: September 10, 1979Date of Patent: October 5, 1982Assignee: Analytical Radiation CorporationInventors: Irwin Wieder, Robert H. Wollenberg
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Patent number: 4348536Abstract: The instant invention is directed to novel compounds and the use thereof in producing polyurethane resins. The compounds generally correspond to the following formula: ##STR1## wherein n is an integer of from 1 to 5,R is a C.sub.1 -C.sub.5 alkyl groupY is a C.sub.1 -C.sub.5 alkyl group or a ##STR2## and Z is a ##STR3## where n=0 or 1, X is --O-- or ##STR4## and R' is an aliphatic group having from 1 to 15 carbon atoms and may contain ester, ether, or amide groups or tertiary nitrogen and, when m=0, R' may be a hydrogen atom.Type: GrantFiled: February 6, 1978Date of Patent: September 7, 1982Assignee: Bayer AktiengesellschaftInventors: Johannes Blahak, Hans Hubner, Johannes Koster, Hans J. Meiners, Heinz Thomas
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Patent number: 4347375Abstract: A process for preparing .alpha.-amino acids or ester thereof having an .alpha.-vinyl substituent and certain intermediates are disclosed.Type: GrantFiled: December 3, 1980Date of Patent: August 31, 1982Assignee: Merck & Co., Inc.Inventors: Arthur A. Patchett, William J. Greenlee
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Patent number: 4343947Abstract: Amides of carnitine or acyl-carnitines having general formula: ##STR1## wherein X.sup.- is a halogen anion, e.g. the chloride anionR is either hydrogen or an acyl radical, such as acetyl, propionyl or butyryl; andY is the residue of an optically active esterified amino-acid (e.g. the residue of L-phenylglycine methyl ester, ##STR2## are prepared by either (a) directly condensing D,L-carnitine (or acyl-D,L-carnitine) with an ester of an optically active aminoacid, or (b) preparing the acid halogenide of D,L-carnitine or acyl-D,L-carnitine and subsequently condensing it with an ester of an optically active aminoacid.The mixture of the diastereoisomer amides thus obtained is resolved by fractional crystallization from organic solvents into the respective separated diastereoisomers.Type: GrantFiled: December 29, 1980Date of Patent: August 10, 1982Assignee: Sigma-Tau Industrie Farmaceutiche Riunite S.p.A.Inventors: Paolo De Witt, Maria O. Tinti
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Patent number: 4340712Abstract: A process for the preparation of polyisocyanates containing biuret and/or higher polyuret groups by reacting secondary diamines with diisocyanates characterized in that the reaction is carried out in the presence of catalytic quantities of strong acids which form mixed carbamic acid anhydrides with isocyanates. Alternatively, the secondary diamines may be reacted with organic diisocyanates in the absence of catalysts to form a urea diisocyanate which is then reacted in the presence of catalytic quantities of strong acids which form mixed carbamic acid anhydrides either with the same diisocyanate used in the first step or a second diisocyanate. The invention also relates to the polyisocyanates containing biuret and/or higher polyuret groups obtainable by this process.Type: GrantFiled: December 19, 1979Date of Patent: July 20, 1982Assignee: Bayer AktiengesellschaftInventors: Wolfgang Reichmann, Klaus Konig, Manfred Schonfelder
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Patent number: 4337262Abstract: Hydantoins of formula (I) ##STR1## have biological properties related to those of naturally occurring prostaglandins and may be used in medicine, for example in the treatment of thrombosis.Type: GrantFiled: November 30, 1978Date of Patent: June 29, 1982Assignee: Burroughs Wellcome Co.Inventors: Norman Whittaker, Albert G. Caldwell
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Patent number: 4332965Abstract: The invention relates to polyisocyanates which are blocked with an acetoacetic acid alkyl ester.Type: GrantFiled: March 3, 1980Date of Patent: June 1, 1982Assignee: Hoechst AktiengesellschaftInventor: Horst Dalibor
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Patent number: 4328027Abstract: The di-triethylamine salt of N,N'-bis-carboethoxymethyl-N,N'-bis-phosphonomethylurea is disclosed herein, having utility in regulating the natural growth or development of plants.Type: GrantFiled: April 16, 1981Date of Patent: May 4, 1982Assignee: Stauffer Chemical CompanyInventors: Lawrence L. Buren, George B. Large
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Patent number: 4326069Abstract: N-substituted aspartic acid monoesters of the formula I ##STR1## wherein for example R.sub.1 is an alkyl group having 1 to 12 C atoms, cyclohexyl, phenyl, tolyl or benzyl, x is 2 or 3, R.sub.2 and R.sub.3 are each a methyl or ethyl group, or together with the N atom they form an N-heterocyclic ring, are obtained by adding, by means of an addition reaction, to 1 mol of a maleic acid monoester of the formula II ##STR2## 1 mol of an amine of the formula III ##STR3## in the presence of a tertiary amine. The novel N-substituted aspartic acid monoesters are valuable curing accelerators for epoxide resin mixtures containing dicyandiamide or a polycarboxylic acid anhydride as curing agent. They are also suitable alone as catalytically acting curing agents for epoxide resins.Type: GrantFiled: April 28, 1980Date of Patent: April 20, 1982Assignee: Ciba-Geigy CorporationInventors: Friedrich Stockinger, Sameer H. Eldin, Friedrich Lohse
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Patent number: 4325961Abstract: Novel substituted .alpha.-fluoromethyl-.alpha.-amino alkanoic acids and esters thereof are disclosed. The novel compounds have biological activity including decarboxylase inhibition.Type: GrantFiled: June 1, 1977Date of Patent: April 20, 1982Assignee: Merck & Co., Inc.Inventors: Janos Kollonitsch, Arthur A. Patchett
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Patent number: 4323704Abstract: Novel compounds of the formula ##STR1## wherein A is methylene, ethylene or ethylidene; R.sub.1 is --C.tbd.CH or --CH.dbd.CH.sub.2 ; R.sub.2 is hydrogen or COR wherein R is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.4 R.sub.5 wherein each of R.sub.4 and R.sub.5 is hydrogen or a straight or branched lower alkyl group of from 1 to 4 carbon atoms or ##STR2## wherein R.sub.6 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or p-hydroxybenzyl; R.sub.a is hydrogen, ##STR3## alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched or ##STR4## wherein R.sub.7 is selected from hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl and p-hydroxybenzyl; and R.sub.b has the same meaning as defined for R.sub.a except R.sub.b is not ##STR5## and R.sub.a and R.sub.Type: GrantFiled: January 16, 1981Date of Patent: April 6, 1982Assignee: Merrell Toraude et CompagnieInventors: Brian W. Metcalf, Michel Jung, Charles Danzin
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Patent number: 4315022Abstract: Compounds of the formula (I): ##STR1## having pharmacological activities similar to those of natural prostaglandins wherein:n is 0 to 5;X is CO, CS or CH.sub.2 ;Y is --CH.sub.2 --CH.sub.2 --; or, when n is 1 to 5, --CH.dbd.CH-- or --C.tbd.C--;R.sub.1 is either CH.sub.2 NR.sub.5 R.sub.6, wherein R.sub.5 and R.sub.6 are separately hydrogen or C.sub.1-6 alkyl, or R.sub.5 is hydrogen and R.sub.6 is (CH.sub.2).sub.m CO.sub.2 R.sup.1.sub.9 wherein m is 0 to 4 and R.sup.1.sub.9 is optionally substituted C.sub.1-6 alkyl or benzyl, optionally substituted in the phenyl ring by chlorine or bromine atoms or by nitro or CF.sub.3 groups; or R.sub.5 and R.sub.6 are both the same (CH.sub.2).sub.m CO.sub.2 R.sup.1.sub.9 as hereinbefore defined; or C(NH.sub.2).dbd.NOH; or C(OR.sub.7).dbd.NH.sub.2.sup.+ B.sup.- wherein R.sub.7 is C.sub.1-6 alkyl and B.sup.- is a salting ion; or CH.sub.2 NHR.sub.8, wherein R.sub.8 is SO.sub.2 R.sup.1.sub.9, COR.sup.1.sub.9 or CZNHR.sub.9 and R.sup.1.sub.9 is as hereinbefore defined, R.sub.Type: GrantFiled: May 23, 1980Date of Patent: February 9, 1982Assignee: Beecham Group LimitedInventors: Gordon Wootton, Stephen A. Smith
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Patent number: 4314069Abstract: .alpha.-[4-(4-Trifluoromethylphenoxy)phenoxy]alkanecarboxylic acids (the "4-trifluoromethylphenoxy group" of which may contain one chlorine atom as a substituent) and derivatives thereof useful as a herbicide, a herbicidal composition containing the compound, methods of controlling weeds and production thereof.Type: GrantFiled: April 15, 1977Date of Patent: February 2, 1982Assignee: Ishihara Sangyo Kaisha, Ltd.Inventors: Ryohei Takahashi, Kanichi Fujikawa, Isao Yokomichi, Sinzo Someya, Nobuyuki Sakashita
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Patent number: 4313956Abstract: Novel, transient prodrug forms of the phenolic dihydroxy sympathomimetic amines have (i) the structural formula (I): ##STR1## wherein X is O, S or NR.sup.5 ; n is 1 or 2; R.sup.1 is the monodehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 1, and the didehydroxylated residue of a phenolic, nuclear dihydroxy natural sympathetic or sympathomimetic amine when n is 2; R.sup.Type: GrantFiled: December 28, 1979Date of Patent: February 2, 1982Assignee: INTERx Research Corp.Inventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
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Patent number: 4311706Abstract: Novel, transient prodrug forms of dopa and dopamine have (i) the structural formula (I): ##STR1## wherein each R is independently selected from the group consisting of hydrogen, R.sup.3 -CO- and ##STR2## wherein X is O, S or NR.sup.6 ; R.sup.1 is hydrogen or --COOR.sup.8 ; R.sup.2 is hydrogen or OR; R.sup.Type: GrantFiled: January 22, 1980Date of Patent: January 19, 1982Assignee: INTERx Research CorporationInventors: Nicholas S. Bodor, Kenneth B. Sloan, Stefano A. Pogany
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Patent number: 4296095Abstract: A composition is disclosed which is useful in preventing dental plaque and tartar from forming on the teeth. The composition includes compounds which are esters or their mono or double salts derived from lysine in combination with straight chain or branched, saturated or unsaturated, monovalent aliphatic alcohols having 4 to 20 carbon atoms.Type: GrantFiled: September 20, 1978Date of Patent: October 20, 1981Assignee: Beiersdorf AktiengesellschaftInventors: Udo Hoppe, Gerhard Sauermann, Julius Curts, Per-Olof Glantz, Bo Krasse, Kare Larsson, Borje Noren, Goran Odham, Jan Olsson
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Patent number: 4284755Abstract: N-Substituted aspartic acid monoesters of the formula ##STR1## wherein for example R.sub.1 is an alkyl group having 1 to 12 C atoms, a cyclohexyl, phenyl, tolyl or benzyl group, R.sub.2 is an alkyl group having 3 or 4 C atoms, or a cyclohexyl, phenyl, tolyl or methoxyphenyl group, and x is 2 or 3, are obtained by adding, by means of an addition reaction, to 1 mol of a maleic acid monoester of the formula ##STR2## 1 mol of an amine of the formulaH.sub.2 N--(CH.sub.2 ).sub.x NH--R.sub.2in the presence of a tertiary amine. The novel N-substituted aspartic acid monoesters are valuable curing agents for epoxide resins, and are particularly suitable for producing storage-stable B-stage resins.Type: GrantFiled: April 30, 1980Date of Patent: August 18, 1981Assignee: Ciba-Geigy CorporationInventors: Friedrich Lohse, Friedrich Stockinger, Sameer H. Eldin
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Patent number: 4277395Abstract: Compounds of the following general formula are irreversible inhibitors of pancreatic elastase: ##STR1## wherein M is hydroxy, lower alkoxy, benzyloxy or --NY.sub.1 Y.sub.2 wherein each of R.sub.4 and R.sub.5 is hydrogen or lower alkyl; R is CF.sub.3, CHF.sub.2 or CH.sub.2 F; R.sub.1 is straight or branched lower alkyl; R.sub.2 is defined the same as R.sub.1 or is benzyl; R.sub.30 is CHO, carbobenzoxy, tert-butoxycarbonyl, benzoyl or lower alkanoyl; X is pro, ala or leu and Y and Z together form a single bond; or Y-X is ala-pro, ala-ala or ala-leu and Z forms a single bond; and Z-Y-X is ala-ala-pro, ala-ala-ala or pro-ala-leu.Type: GrantFiled: June 16, 1980Date of Patent: July 7, 1981Assignee: Richardson-Merrell Inc.Inventors: Philippe Bey, Brian W. Metcalf, Jeffrey S. Wiseman
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Patent number: 4275217Abstract: A chiral .alpha.-amino acid having a hydrogen substituent in a position alpha to the carboxylic function thereof is prepared by subjecting a corresponding optical antipode with a chiral amino acid to a strong base whereby the proton in a position alpha to the carboxylic function is removed and thereafter reacting the resulting product with a chiral protonation agent.Type: GrantFiled: July 9, 1979Date of Patent: June 23, 1981Assignee: Agence Nationale de Valorisation de la Recherche (ANVAR)Inventors: Lucette Duhamel, Jean-Christophe Plaquevent
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Patent number: 4275220Abstract: A process for preparing .alpha.-amino acids or ester thereof having an .alpha.-vinyl substituent and certain intermediates are disclosed.Type: GrantFiled: August 6, 1979Date of Patent: June 23, 1981Assignee: Merck & Co., Inc.Inventors: Arthur A. Patchett, William J. Greenlee
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Patent number: 4260823Abstract: Novel acetylenic derivatives of .alpha.-amino acids of the following general structure: ##STR1## wherein R is hydrogen, alkylcarbonyl wherein the alkyl moiety has from 1 to 4 carbon atoms and is straight or branched, alkoxycarbonyl wherein the alkoxy moiety has from 1 to 4 carbon atoms and is straight or branched, or ##STR2## is hydrogen, a straight or branched lower alkyl group of 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; each R.sub.1 is the same and is hydroxy, a straight or branched alkoxy group of from 1 to 8 carbon atoms, --NR.sub.3 R.sub.4 wherein each of R.sub.3 and R.sub.4 is hydrogen or a lower alkyl group of from 1 to 4 carbon atoms and can be the same or different, or ##STR3## wherein R.sub.5 is hydrogen, a straight or branched lower alkyl group of from 1 to 4 carbon atoms, benzyl or .rho.-hydroxybenzyl; and pharmaceutically acceptable salts and individual optical isomers thereof.Type: GrantFiled: July 2, 1979Date of Patent: April 7, 1981Assignee: Merrell Toruade et CompagnieInventors: Patrick J. Casara, Michel Jung, Brian W. Metcalf
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Patent number: 4251670Abstract: A glycol polyether-acrylic acid-amine reaction product having detergent and corrosion inhibiting properties for fuels and lubricating oil compositions is provided.Type: GrantFiled: August 13, 1979Date of Patent: February 17, 1981Assignee: Texaco Inc.Inventor: William M. Cummings