At 2-position Patents (Class 546/243)
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Patent number: 5041546Abstract: Heterocyclic (poly)peroxycarboxylic acids having a N-amidic heteroatom, which have the formula:R--(CH.sub.2).sub.m --R' (I)wherein:R and R', alike or different from each other, represent hydrogen atoms or a group: ##STR1## with the proviso that at least one of R and R' shall be different from H, and wherein the other symbols have the following meaning:R" represents a hydrogen atom or any other substituent non-reactive in the presence of the active oxygen of the peroxycarboxylic group and/or under the preparation conditions;m represents a number between 1 to 12;n represents a number selected from 0, 1 and 2;p represents a number between 1 and 3;their process of preparation and their use as bleaching agents.Type: GrantFiled: June 14, 1989Date of Patent: August 20, 1991Assignee: Ausimont S.r.l.Inventors: Carlo Venturello, Claudio Cavallotti
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Patent number: 5037822Abstract: The invention relates to the products of formula ##STR1## in which R represents the radical ##STR2## in which R.sub.1 at any position on the benzene ring represents a linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, which may be identical or different, represent a hydrogen atom or a linear alkyl, alkenyl or alkynyl containing up to 8 carbon atoms or form, together with the nitrogen atom to which they are attached, a carbonaceous heterocyclic radical optionally containing another hetero form, or the radical OR', R' representing hydrogen, a linear, branched or cyclic alkyl radical containing up to 8 carbon atoms or an aryl radical containing up to 14 carbon atoms, or the radical SR.sub.4 or S(O)R.sub.5, R.sub.4 and R.sub.5 representing a linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or R represents naphthyl optionally substituted with a radical R'.sub.1, R'.sub.Type: GrantFiled: February 21, 1990Date of Patent: August 6, 1991Assignee: Roussel-UclafInventors: Emilio Toja, Fernando Barzaghi, Giulio Galliani
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Patent number: 5021439Abstract: A compound having the formula (I) or (II) ##STR1## wherein R.sup.1 is a hydrogen atom or an organic residue bonded via a carbon atom, R.sup.2 is a hydrogen atom or a N-protecting group, --COR.sup.3 is an optionally esterified or amidated carboxyl group, R.sup.4 and R.sup.5 are the same or different and respectively a hydrogen atom or an acyl group or a chain or alicyclic hydrocarbon group optionally having an aryl substituent, R.sup.6 is NOH or O, n is an integer of 0 to 3, or R.sup.4 and R.sup.5 together with the adjacent nitrogen atom may form a ring or an optionally substituted benzylidene amino group, which is useful therapeutics of brain dysfunction.Type: GrantFiled: September 18, 1989Date of Patent: June 4, 1991Assignee: Takeda Chemical Industries, Ltd.Inventors: Setsuo Harada, Akinobu Nagaoka, Katsumi Itoh, Shinji Terao
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Patent number: 5011941Abstract: The invention relates primarily to quaternized compounds having the formula ##STR1## wherein n and n' are each independently integers having a value of from 1 to 25; p is an integer having a value of from 1 to 4; Y and Y' are each independently H or CH.sub.3 ; R is linear alkyl, alkenyl, or amidoalkyl having from 8 to 22 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; Z is linear alkylene having from 3 to 8 carbon atoms and is optionally substituted with lower alkyl and A.sup.- is an anion.Type: GrantFiled: September 14, 1990Date of Patent: April 30, 1991Assignee: GAF Chemicals CorporationInventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login
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Patent number: 5008391Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.Type: GrantFiled: July 7, 1989Date of Patent: April 16, 1991Assignee: Eli Lilly and CompanyInventors: Charles J. Barnett, Thomas M. Wilson
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Patent number: 5008104Abstract: The invention relates primarily to quaternized compounds having the formula ##STR1## wherein n and n' are each independently integers having a value of from 1 to 25; p is an integer having a value of from 1 to 4; Y and Y' are each independently H or CH.sub.3 ; R is linear alkyl, alkenyl, or amidoalkyl having from 8 to 22 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; Z is linear alkylene having from 3 to 8 carbon atoms and is optionally substituted with lower alkyl and A.sup.- is an anion.Type: GrantFiled: June 22, 1989Date of Patent: April 16, 1991Assignee: GAF Chemicals CorporationInventors: Ratan K. Chaudhuri, David J. Tracy, Robert B. Login
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Patent number: 5003072Abstract: O-acylated derivatives of 1,5-dideoxy-1,5-imino-D-glucitol and their N-alkyl, N-acyl and N-aryl derivatives in which from one to four of the free hydroxyl groups are acylated with acyl groups having from one to eight carbon atoms and in which the N-alkyl and N-acyl substituents contain from four to fourteen carbon atoms and the N-aryl substituents contain from seven to fourteen carbon atoms are disclosed, provided that when N-aryl is benzyloxycarbonyl, the O-acyl groups contain four to eight carbon atoms.Type: GrantFiled: October 12, 1989Date of Patent: March 26, 1991Assignee: G. D. Searle & Co.Inventors: Richard A. Partis, Francis J. Koszyk, Richard A. Mueller
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Patent number: 5001113Abstract: Enzyme di- or tripeptides of the formula: ##STR1## and analogs thereof which inhibit renin and are useful for treating various forms of renin-associated hypertension, hyperaldosteronism and congestive heart failure; compositions containing these renin-inhibitory peptides, optionally with other antihypertensive agents; and methods of treating hypertension, hyperaldosteronism or congestive heart failure or of establishing renin as a causative factor in these problems which employ these novel peptides.Type: GrantFiled: March 7, 1990Date of Patent: March 19, 1991Assignee: Merck & Co., Inc.Inventors: Peter D. Williams, Daniel E. Veber
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Patent number: 4990628Abstract: The reaction of lactams (preferably N-methyl-2-pyrrolidone) with hydrogen sulfide to thiolactams (preferably N-methyl-2-thiopyrrolidone) is conducted in the presence of a catalyst comprising an alumina-supported Group VIII metal or Group VIII metal compound (preferably palladium metal/oxide and/or iron oxide).Type: GrantFiled: March 1, 1990Date of Patent: February 5, 1991Assignee: Phillips Petroleum CompanyInventor: Alan D. Eastman
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Patent number: 4985445Abstract: Sugar lactams such as N-(3-phenylpropyl)-1-deoxynojirimycin, 1-deoxynojirimycin, D-glucaro-.delta.-lactam, 6-O-triphenylmethyl-D-gluco-.delta.-lactam, etc. and new derivatives thereof which markedly inhibit metastasis of cancer cells.Type: GrantFiled: February 6, 1989Date of Patent: January 15, 1991Assignee: Meiji Seika Kaisha, Ltd.Inventors: Tsutomu Tsuruoka, Satoru Nakabayashi, Harumi Fukuyasu, Yuuko Ishii, Takashi Tsuruoka, Haruo Yamamoto, Shigeharu Inouye, Shinichi Kondo
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Patent number: 4959482Abstract: A novel class of pyrrolidin-2-one and piperidin-2-one compounds in which the nitrogen atom is bonded to an oxyphenyl radical haivng tertiary-alkyl and tri-methylsilyl substituents. The compounds posses anti-inflammatory, immunomodulatory, analgesic and anti-pyretic activity and they may be combined with excipients to provide formulations which are useful in treating arthritis and conditions associated with that disease.Type: GrantFiled: September 26, 1988Date of Patent: September 25, 1990Assignee: Biofor, Ltd.Inventor: Sung J. Lee
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Patent number: 4956476Abstract: The reaction of lactams (preferably N-methyl-2-pyrrolidone) with hydrogen sulfide to thiolactams (preferably N-methyl-2-thiopyrrolidone) is conducted in the presence of a catalyst consisting essentially of alumina.Type: GrantFiled: March 1, 1990Date of Patent: September 11, 1990Assignee: Phillips Petroleum CompanyInventors: Alan D. Eastman, Marvin M. Johnson, Richard D. Skinner
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Patent number: 4950429Abstract: 6-Aminocaproic acid is prepared by(a) reacting a 5-formylvaleric acid ester with water in the presence of an acid agent at 30.degree.-200.degree. C. and(b) reacting the 5-formylvaleric acid thus obtained with excess ammonia and hydrogen in the presence of a hydrogenation catalyst and of a solvent which is inert under the reaction conditions at 50.degree.-150.degree. C. under superatmospheric pressure.Type: GrantFiled: March 23, 1989Date of Patent: August 21, 1990Assignee: BASF AktiengesellschaftInventors: Uwe Vagt, Rolf Fischer, Franz Merger, Hans-Martin Hutmacher
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Patent number: 4943633Abstract: This invention relates to an improved process for the preparation of cyanoalkyl lactams by the reaction of an unsaturated nitrile with a lactam, said cyanoalkyl lactam of the formula ##STR1## wherein R is H, or methyl, R.sub.1 is H, methyl or ethyl and n is a number ranging from 2-11 and wherein each of the methylene groups may carry a lower alkyl substituent as shown. The improvement comprises: reacting said lactam with an alpha-beta unsaturated nitrile having from 3-6 carbon atoms in the presence of a catalytic amount of a diazabicycloalkene of the formula ##STR2## wherein R, R.sub.1 and n have the above meaning. Typically, acrylonitrile is reacted with .epsilon.-caprolactam in the presence of diazabicycloundecene.Type: GrantFiled: June 22, 1988Date of Patent: July 24, 1990Assignee: Air Products and Chemicals, Inc.Inventors: Richard V. C. Carr, Thomas A. Johnson
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Patent number: 4929736Abstract: Certain amino-acid derivatives are disclosed as effective inhibitors of human leukocyte elastase and therefore useful in preventing the imbalance of this proteolytic enzyme in vivo. The compounds specifically are derivatives L-valine, L-norvaline, L-norleucine, and L-methionine methyl ester azolides succinimides or pyridones and sulfonate salts, and related compounds such as L-leucine and L-phenylalanine methyl ester derivatives. The compounds were found to be excellent inhibitors in that they embody both inhibitory and anti-oxidant or anti-inflammatory activity.Type: GrantFiled: November 6, 1987Date of Patent: May 29, 1990Assignee: Board of Trustees of the Wichita State UniversityInventor: William C. Groutas
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Patent number: 4908445Abstract: A new class of novel, biologically active sesquiterpene compounds, pharmaceutical compositions containing them, methods of producing the compounds and compositions and methods of using them are disclosed. This new class of compounds have the generic formulae: ##STR1## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7 =H or lower alkyl.Type: GrantFiled: January 9, 1989Date of Patent: March 13, 1990Assignee: Harbor Branch Oceanographic Institution, Inc.Inventors: Kenneth L. Rinehart, Ashok D. Patil
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Patent number: 4889953Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is a higher alkyl group which may be substituted; R.sup.2 is a hydrogen, a lower alkyl group which may be substituted, a lower alkanoyl group which may be substituted or a lower alkylthiocarbamoyl group; R.sup.3 is a primary to tertiary amino group or a quaternary ammonium group; and n is 2 or 3, and salts thereof, have antitumor activity and platelet activating factor inhibitory activity.Type: GrantFiled: July 22, 1987Date of Patent: December 26, 1989Assignee: Takeda Chemical Industries, Ltd.Inventors: Keizo Inoue, Hiroaki Nomura, Tetsuya Okutani
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Patent number: 4886911Abstract: The invention concerns compounds of formula I ##STR1## wherein: X and Y are independently selected from the group consisting of hydrogen, C.sub.1 to C.sub.4 alkyl, C.sub.1 to C.sub.4 haloalkyl, and the group wherein X and Y together from a three or four-membered carbon bridge the bridge optionally comprising one or both of a double bond and a carbonyl group;Z is selected from the group consisting of hydrogen, halogen, C.sub.1 to C.sub.4 alkyl and C.sub.1 to C.sub.4 alkanoyl;R.sup.1 is selected from the group consisting of: hydrogen; an acyl group; and an inorganic or organic cation;R.sup.2 is selected from the group consisting of: C.sub.1 to c.sub.6 alkyl; C.sub.2 to C.sub.6 alkenyl; C.sub.2 to C.sub.6 haloakenyl; C.sub.2 to C.sub.6 alkynyl; and substituted C.sub.1 to C.sub.Type: GrantFiled: June 12, 1987Date of Patent: December 12, 1989Assignee: ICI Australia LimitedInventors: Keith G. Watson, Craig G. Lovel
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Patent number: 4885158Abstract: The invention relates primarily to quaternized compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.1, R.sub.2 and R.sub.3 are each independently selected from the group of alkyl, alkyloxyalkyl, alkyloxyalkenyl, hydroxyalkyl, aryl, aralkyl, alkaryl, alkyl amidoalkyl, alkyl carbamoylalkyl, aryl amido alkyl and aryl carbamoyalkyl radicals, and R.sub.2 and R.sub.3, together with the quaternized nitrogen atom can form a heterocyclic radical containing from 1 to 2 heteroatoms selected from the group of nitrogen, sulfur and oxygen, in which case R.sub.1 can represent a double bond in the heterocyclic structure or can be any of the aforementioned groups for R.sub.1, R.sub.2 and R.sub.3 ; said groups R.sub.1, R.sub.2 and R.sub.3 each having from 1 to 30 carbon atoms and at least one of R.sub.1, R.sub.2 and R.sub.3 is a radical having from 8 to 30 carbon atoms when R.Type: GrantFiled: April 29, 1988Date of Patent: December 5, 1989Assignee: GAF CorporationInventors: David J. Tracy, Thomas Rizzo, Robert B. Login
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Patent number: 4874865Abstract: Preparation of substituted lactams Ia to Ic ##STR1## where n is 0 or 1, X is --O--CO--R.sup.1, --O--SO.sub.2 --R.sup.1, --CO--R.sup.2, --CO--O--R.sup.3 or --CO--NR.sup.4 R.sup.5, R.sup.1 is a C.sub.1 -C.sub.8 -radical of a carboxylic or sulfonic acid, R.sup.2 is C.sub.1 -C.sub.8 -alkyl, R.sup.3 is H or alkyl, aryl or aralkyl of not more than 8 carbon atoms, R.sup.4 and R.sup.5 are each H or C.sub.1 -C.sub.4 -alkyl or together form a 5-membered or 6-membered ring, by reacting a lactam II ##STR2## with a vinyl compound IIICH.sub.2 .dbd.CH-Xand a compound IV which forms free radicals to give Ia, and preparation of Ib by hydrolysis of a compound Ia in which X is (--O--CO--R.sup.1) or (--O--SO.sub.2 --R.sup.1), and preparation of Ic by thermolysis of Ib or of a compound Ia in which X is (--O--CO--R.sup.1) or (--O--SO.sub.2 --R.sup.1), and the novel substituted lactams Ia and Ib where X is (--O--CO--R.sup.1) and (--O--SO.sub.2 --R.sup.1).Type: GrantFiled: June 2, 1988Date of Patent: October 17, 1989Assignee: BASF AktiengesellschaftInventors: Ludwig Wambach, Martin Fischer
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Patent number: 4873336Abstract: The invention relates to the preparation of N-vinyl lactams having the formula ##STR1## wherein n is an integer having an value of from 1 to 3 in a one-stage, non-aqueous process which comprises reacting a lactam having the formula ##STR2## with acetylene under an acetylene partial pressure of from about 25 to about 125 psig. in the presence of an inert gas diluent and a catalyst having the formula ##STR3## wherein R.sub.1, R.sub.2 and R.sub.3 are all lower alkyl or alyl or one of R.sub.1, R.sub.2 and R.sub.3 can also be hydrogen and M is a metal selected from the group of cesium, potassium, sodium and lithium.Type: GrantFiled: March 28, 1988Date of Patent: October 10, 1989Assignee: GAF CorporationInventors: Kou-Chang Liu, Paul D. Taylor
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Patent number: 4873329Abstract: A compound of the formula ##STR1## wherein X has the formula ##STR2## wherein ring A is phenyl, naphthyl or heterocyclic; wherein R.sup.1 is hydrogen, alkyl, alkanoyl or aroyl; wherein R.sup.2, R.sup.3 and R.sup.4, which may be the same or different, each is an electron withdrawing substituent selected from halogeno, nitro, cyano, trifluoromethyl, alkylthio, alkylsulphinyl and alkylsulphonyl or each is hydrogen, alkyl, alkoxy or dialkylamino provided that when ring A is phenyl or naphthyl at least one of R.sup.2, R.sup.3 and R.sup.4 is an electron-withdrawing substituent; wherein R.sup.5 and R.sup.6, which may be the same or different, each is hydrogen, halogeno or alkyl; wherein R.sup.7 is alkyl or halogenoalkyl; and wherein R.sup.8 is carbamoyl, alkyl, cycloalkyl, alkenyl, alkynyl, halogenoalkyl, halogenoalkenyl, halogenoalkynyl, alkanoyl, alkylcarbamoyl, dialkylcarbamoyl or aroyl; or wherein R.sup.Type: GrantFiled: February 21, 1985Date of Patent: October 10, 1989Assignee: Imperial Chemical Industries PLCInventors: Leslie R. Hughes, John Oldfield, Howard Tucker
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Patent number: 4870173Abstract: This invention provides a process for preparing lactams, by selectively reacting a novel 1-hydrocarbyl-amino (or heteroatom-substituted hydrocarbylamino); 1,1-dicarboxylic acid, alkylesters; 1-hydrocarbyl (or heteroatom-substituted hydrocarbyl) carboxylic acid, alkyl ester methane, as the salt of an acid having a pKa of 0 or more, in the absence or presence of a base, whereby novel lactams wherein one or both hydrocarbyl moieties are incorporated into the lactam ring are obtained. That is, the acid moiety of said novel salt promotes the reaction whereby both hydrocarbyl moieties are incorporated into the ring, while the presence of a base, in an amount substantially equivalent to said acid promotes the reaction whereby only one hydrocarbyl is incorporated into the ring.Type: GrantFiled: April 3, 1986Date of Patent: September 26, 1989Assignee: Nelson Research & Development Co.Inventors: Gevork Minaskanian, James V. Peck
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Patent number: 4864017Abstract: The present invention provides novel renin-inhibiting peptides of the formula X-A.sub.6 -B.sub.7 -C.sub.8 -D.sub.9 -E.sub.10 -F.sub.11 -G.sub.12 -H.sub.13 - I.sub.14 -Z, wherein the E.sub.10 -F.sub.11 moiety is a dihydroxyethylene isostere, X and Z are terminal groups, and the remaining variables are absent or are amino acid residues. Such inhibitors are useful for the control of hypertension.Type: GrantFiled: August 23, 1988Date of Patent: September 5, 1989Assignee: The Upjohn CompanyInventor: Suvit Thaisrivongs
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Patent number: 4864055Abstract: A compound represented by the following formula: ##STR1## wherein R is a C.sub.3 -C.sub.24 olefinically unsaturated organic radical having functionality which renders the nitrogen atom electron deficient, the olefinic unsaturation functionality being polymerizable,R.sup.1 is hydrogen or a C.sub.1 -C.sub.4 alkyl radical, orR and R.sup.1 together with the nitrogen atom can form an olefinically unsaturated 5 to 7-member ring which has functionality that renders the nitrogen atom electron deficient and the olefinic unsaturation functionality is polymerizable,R.sup.2 and R.sup.3 are hydrogen, a C.sub.1 -C.sub.4 alkyl or acyl radical, orR.sup.2 and R.sup.3 together are a C.sub.1 -C.sub.4 alkylene group,R.sup.4 is hydrogen or a C.sub.1 -C.sub.4 alkyl, acyl, ester, amide or acid group, andn is an integer from 1 to 10, provided n is not 1 when R is (meth)acryloyl, R.sup.2 and R.sup.3 are methyl and R.sup.1 and R.sup.4 are hydrogen.Type: GrantFiled: September 3, 1987Date of Patent: September 5, 1989Assignee: Air Products and Chemicals, Inc.Inventors: Robert K. Pinschmidt, Jr., Dale D. Dixon, William F. Burgoyne, Jr.
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Patent number: 4859780Abstract: Hydrophilic modifier monomers of the formula [X-T].sub.z 'G are disclosed wherein X is a reactive group, G is a hydrophilic group and T is a divalent linking group, z' being a number up to the available valence of G, excess G valences being taken up by hydrogen. The monomers of the invention can be used to boost the hydrophilic nature of a wide variety of polymeric materials or be polymerized themselves with varying degrees of copolymerizable monomers. They are particularly suited for making hydrophilic contact lens materials.Type: GrantFiled: February 26, 1988Date of Patent: August 22, 1989Assignee: Ciba-Geigy CorporationInventors: Frank Molock, J. Richard Robertson, Jr., Kai C. Su
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Patent number: 4837013Abstract: The invention relates primarily to quaternized compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.4 is alkylene having from 1 to 4 carbon atoms, phenyl or naphthyl optionally substituted with lower alkyl; Y is ##STR2## wherein R.sub.6 is hydrogen or lower alkyl; R.sub.7 is alkyl of from 1 to 30 carbon atoms; R.sub.2 and R.sub.3 are each independently selected from the group of --R.sub.4 --Y--R.sub.7 alkyl, alkyleneoxyalkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, and alkyleneamidoalkyl radicals, said groups each having from 1 to 30 carbon atoms and at least one of R.sub.7, R.sub.2 and R.sub.3 having at least 8 carbon atoms and X.sup.-- is a chloride, bromide or iodide anion. The invention also relates to the preparation and use of said quaternized compounds.Type: GrantFiled: August 28, 1987Date of Patent: June 6, 1989Assignee: GAF CorporationInventors: Robert B. Login, Ratan K. Chaudhuri, David J. Tracy, Michael W. Helioff
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Patent number: 4831161Abstract: Prepare N-(amidoalkyl)imides by contacting an imide with a 2-oxazoline under reaction conditions, optionally in the presence of a solvent.Type: GrantFiled: June 24, 1987Date of Patent: May 16, 1989Assignee: The Dow Chemical CompanyInventors: Pen-Chung Wang, Steven P. Crain
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Patent number: 4830851Abstract: A stable iodine complex formed from the association of iodine with a pyrrolidonyl surfactant and its use in therapeutic, environmental and industrial applications and particularly as low foaming disinfectants for gradual release of iodine over significantly extended periods.Type: GrantFiled: March 3, 1987Date of Patent: May 16, 1989Assignee: GAF CorporationInventors: David J. Tracy, Mohamed M. Hashem, Robert B. Login
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Patent number: 4830850Abstract: The invention relates primarily to quaternized compounds having the formula ##STR1## wherein m and p are each integers having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.1 is alkyl or alkenyl having from 1 to 30 carbon atoms; R.sub.2 and R.sub.3 are each independently selected from the group of --(CH.sub.2).sub.p OR.sub.1, alkyl, alkylhydroxy, aryl, aralkyl, aralkenyl, alkaryl, and alkylene amidoalkyl radicals, said R.sub.2 and R.sub.3 groups having from 1 to 30 carbon atoms and at least one of R.sub.1, R.sub.2 and R.sub.3 is a radical having from 8 to 30 carbon atoms; and X.sup.- is a chloride, bromide or iodide anion. The invention also relates to the preparation and use of said quaternized compounds.Type: GrantFiled: August 28, 1987Date of Patent: May 16, 1989Assignee: GAF CorporationInventors: Robert B. Login, Ratan K. Chaudhuri, David J. Tracy, Michael W. Helioff
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Patent number: 4822886Abstract: Cyclic N-hydroxyimide compounds are disclosed which show strong metal ion chelating properties and are useful as detergent additives. Detergent compositions containing the N-hydroxyimides improve the stain removing effectiveness of detergents and are biodegradable.Type: GrantFiled: August 12, 1987Date of Patent: April 18, 1989Assignee: American Cyanamid CompanyInventor: Stephen F. Donovan
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Patent number: 4800212Abstract: Compounds of formula (I) or when a compound of formula (I) contain a salifiable group, a pharmaceutically acceptable salt thereof: ##STR1## wherein: R.sub.1 -R.sub.7 and X are as defined, are useful as anti-hypertensive agents.Type: GrantFiled: June 10, 1985Date of Patent: January 24, 1989Assignee: Beecham Group p.l.c.Inventors: John M. Evans, Geoffrey Stemp
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Patent number: 4797491Abstract: Bifunctional chemicals useful for linking aldehyde containing moieties to moieties containing functionalities which are or can be reactive with sulfhydryl are claimed and have the formula:L--S--(CH.sub.2).sub.n1 --CONH--SPACER--NH--Xwherein L is a leaving group selected from --H or --S--Ar, wherein Ar represents optionally substituted phenyl or pyridyl;n.sub.1 =2-4;X is selected from:--CO--Y--CONHNH.sub.2, a hydrazide; ##STR1## a hydrazine; ##STR2## a hydrazine; --CO--Y--NH--CONHNH.sub.2, a semicarbazide; and--CO--Z--NH--CSNHNH.sub.2, a thiosemicarbazide;wherein Y is alkylene or oxaalkylene and Z is alkylene or a polypeptide residue bridging the N-terminal amino group and C-terminal carboxy group thereof;the SPACER is oxaalkylene or oxaalkylene substituted with hydroxyl and specifically includes residues having formulas selected from--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --O--(CH.sub.2).sub.n2 --(a)wherein each n2 is independently 2-4 and ##STR3## wherein n3 is 2-6.Type: GrantFiled: March 17, 1986Date of Patent: January 10, 1989Assignee: Cetus CorporationInventors: Danute E. Nitecki, Margaret Moreland
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Patent number: 4792604Abstract: A process for the manufacture of haloalkyl lactams having the formula ##STR1## wherein n is an integer having a value of from 1 to 3; m is an integer having a value of 1 or 2 and X is chlorine or bromine in the absence of an inert solvent by reacting a hydroxyalkyl lactam of the formula ##STR2## with a thionyl chloride or bromide in the liquid phase under anhydrous conditions, vaporizing and removing any excess thionyl halide along with SO.sub.2 by-product from the liquid reaction mixture under vacuum followed by vacuum distillation of the remaining liquid product mixture at a temperature below its decomposition and recovering said product.The product of this process can be obtained in greater than 90% yield and 99% purity.Type: GrantFiled: March 20, 1987Date of Patent: December 20, 1988Assignee: GAF CorporationInventors: David J. Tracy, Thomas Rizzo
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Patent number: 4760152Abstract: (1) Pyrrolidonyl acrylate block polymers having the formula ##STR1## wherein n has a value of 1 to 3; X and X' are dissimilar and each is hydrogen or methyl; y and z each have a value of from 1 to 40, except that at least one of y and z is greater than 1 and R is hydrogen or methyl;(2) preparation of said polymers and(3) uses of said polymers.Type: GrantFiled: March 2, 1987Date of Patent: July 26, 1988Assignee: GAF CorporationInventors: David J. Tracy, Mohamed M. Hashem, Fulvio J. Vara
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Patent number: 4743691Abstract: 2-(Fluoromethyl or chloromethyl)-2,5-diaminopentanoic acid, 2-(fluoromethyl or chloromethyl)-2,6-diaminohexanoic acid, and 2-fluoromethyl-2-amino-5-guanidinopentanoic acid, and certain derivatives thereof, are inhibitors of ornithine decarboxylase. Methods of preparing the compounds and derivatives are also described.Type: GrantFiled: June 25, 1982Date of Patent: May 10, 1988Assignee: Merrell Dow France et CieInventors: Philippe Bey, Michel Jung
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Patent number: 4732990Abstract: The invention relates primarily to quaternized compounds having the formula ##STR1## wherein m is an integer having a value of from 1 to 4; R is alkylene having from 3 to 8 carbon atoms and is optionally substituted with C.sub.1 to C.sub.4 alkyl; R.sub.1, R.sub.2 and R.sub.3 are each independently selected from the group of alkyl, alkyl oxide, alkylhydroxy, alkoxy, aryl, aralkyl, alkaryl, and alkyl amidoalkyl radicals, said groups each having from 1 to 30 carbon atoms and at least one of R.sub.1, R.sub.2 and R.sub.3 is radical having from 8 to 30 carbon atoms; and X.sup.- is a chloride, bromide or iodide anion. The invention also relates to the preparation and use of said quaternized compounds.Type: GrantFiled: October 24, 1986Date of Patent: March 22, 1988Assignee: GAF CorporationInventors: Robert B. Login, Ratan K. Chaudhuri, David J. Tracy, Michael W. Helioff
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Patent number: 4731454Abstract: A method for producing a lactam having the formula: ##STR1## wherein R.sup.1 is a hydrogen atom, or a straight chain or branched chain alkyl group having from 1 to 5 carbon atoms, and R.sup.2 is an organic group having at least 2 carbon atoms, and connected at both ends to the cyclic acid imide group, which comprises reducing a cyclic acid imide having the formula: ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, or its precursor, with hydrogen by means of a cobalt-based catalyst comprising (a) cobalt and (b) at least one modifier component selected from the group consisting of molybdenum, tungsten and rhenium.Type: GrantFiled: May 29, 1987Date of Patent: March 15, 1988Assignee: Mitsubishi Chemical Industries LimitedInventors: Masayuki Otake, Isamu Fukushima
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Patent number: 4692523Abstract: A process for the preparation of 1-substituted azacycloalkan-2-ones of the formula I ##STR1## in which R, m and n have the meanings indicated by reaction of corresponding 1-trimethylsilylazacycloalkan-2-ones with alkali metal alcoholate or alkali metal oxide and then alkylation of the alkali metal salts which are formed.Type: GrantFiled: October 7, 1986Date of Patent: September 8, 1987Assignee: Hoechst AktiengesellschaftInventors: Manfred Schorr, Wilfried Schmitt
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Patent number: 4692533Abstract: Prepare N-(amidoalkyl)imides by contacting an imide with a 2-oxazoline under reaction conditions, optionally in the presence of a solvent.Type: GrantFiled: September 9, 1985Date of Patent: September 8, 1987Assignee: The Dow Chemical CompanyInventors: Pen-Chung Wang, Steven P. Crain
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Patent number: 4692520Abstract: The invention relates to the N-substituted acyl-lactam compound of the formula: ##STR1## where R' is a bivalent cyclic or non-cyclic alkyl, aralkyl, alkaryl or aryl radicalR" a bivalent radical having the following general formula ##STR2## wherein R'" is H, alkyl, cycloalkyl, aryl, alkaryl or aralkyl,R.sup.iv is H, alkyl, cycloalkyl, aryl, alkaryl or aralkyl whereR'" and R.sup.iv may jointly form a substituted or non-substituted cycloalkyl residuen is 0 or 1(-L) represents a non-opened lactam ring andx a number>1.It has been found that this group of compounds is very suitable as activator in the preparation of nylon polymers, more specifically in the so-called RIM (Reaction Injection Moulding) or RRIM (reinforced RIM) systems, in which it is highly essential for the polymerization to take effect within a very short time.Type: GrantFiled: December 13, 1985Date of Patent: September 8, 1987Assignee: Stamicarbon B.V. (Subsidiary of DSM)Inventors: Albert A. Van Geenen, Jozef J. M. Bongers
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Patent number: 4692521Abstract: The invention relates to N-substitutecd acyl lactam compounds of the formula ##STR1## where R is a polyol residue originating from a polyol with the formula R-(OH).sub.x where x is a number.ltoreq.2R' a bivalent cyclic or non-cyclic alkyl, aralkyl, alkaryl or aryl radicalR" a bivalent radical having the following general formula ##STR2## wherein R'" is H, alkyl, cycloalkyl, aryl, alkaryl or aralkyl,R.sup.iv is H, alkyl, cycloalkyl, aryl, alkaryl or aralkyl whereR"' and R.sup.iv may jointly form a substituted or non-substituted cycloalkyl residuen is 0 or 1 and(-L) represents a non-opened lactam ring of the formula ##STR3## wherein Y is hydrocarbon residue with 3-11 carbon atoms. It has been found that this group of compounds is very suitable as activator in the preparation of nylon block copolymers, more specifically in the RIM or RRIM systems.Type: GrantFiled: December 13, 1985Date of Patent: September 8, 1987Assignee: Stamicarbon B.V.Inventors: Jozef J. M. Bongers, Albert A. Van Geenen
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Patent number: 4683304Abstract: The invention relates to a process for preparing an acyl-lactam compound characterized in that the reaction product of a lactam with a dicarboxylic acid anhydride is reacted with a polyol at a temperature of 150.degree. C. at most. These acyl-lactam compounds are very suitable as activator in the preparation of nylon block copolymers, more specifically in the RIM or RRIM systems.Type: GrantFiled: December 13, 1985Date of Patent: July 28, 1987Assignee: Stamicarbon B.V.Inventors: Albert A. Van Geenen, Jozef J. M. Bongers
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Patent number: 4680410Abstract: The invention is a process for the preparation of a N- or S-1,2-ethylenically unsaturated organic compound which comprises(a) contacting a N- or S-silylated organic compound with an aldehyde, wherein the aldehyde has a hydrogen atom bonded to the carbon adjacent to the carbonyl moiety, at elevated temperatures under conditions such that a N- or S-1-siloxyalkyl-substituted organic compound is prepared; and(b) pyrolyzing the N- or S-1-siloxyalkyl-substituted organic compound under conditions such that the siloxy moiety is elminated to prepare a N- or S-1,2-ethylenically unsaturated compound.Type: GrantFiled: March 2, 1984Date of Patent: July 14, 1987Assignee: The Dow Chemical CompanyInventor: Pen C. Wang
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Patent number: 4668703Abstract: This invention is for .gamma.-allenyl-.gamma.-aminobutyric acid derivatives which are .gamma.-aminobutyric acid transaminase inhibitors.Type: GrantFiled: July 1, 1985Date of Patent: May 26, 1987Assignee: Syntex (U.S.A.) Inc.Inventors: Alexander Krantz, Arlindo L. Castelhano, Diana H. Pliura
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Patent number: 4666967Abstract: The invention provides polyurethanes and polyisocyanurate having incorporated therein a flame retardant amount of a salt formed by reaction between dimethyl methyl phosphonate, monomethyl methyl phosphonate or methyl phosphonic acid, and a compound of the general formula (I). ##STR1## in which X is O, S or NH, R.sup.1 is H, alkyl with 1 to 4 carbon atoms, alkenyl of up to 4 carbon atoms, CN, CONH.sub.2 or NH.sub.2, R.sup.2 is H, alkyl with 1 to 4 carbon atoms or alkenyl of up to 4 carbon atoms or R.sup.1 and R.sup.2 together with the nitrogen atom to which they are attached form a heterocyclic ring of up to 6 carbon atoms which may optionally contain another hetero atom and R is H, an alkyl group with 1 to 8 carbon atoms, an aryl group with 6 to 10 carbon atoms, a cycloalkyl group with 5 to 12 carbon atoms or a heterocyclic group with up to 9 ring carbon atoms, or, together with R.sup.1 forms an alkylene chain of 3 to 10 carbon atoms, or R is a group NHR.sup.3 wherein R.sup.Type: GrantFiled: January 22, 1986Date of Patent: May 19, 1987Assignee: Ciba-Geigy CorporationInventors: Norman Richardson, deceased, Brian G. Clubley, Richard J. Dellar
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Patent number: 4663319Abstract: Novel thioketene derivatives of the formula: ##STR1## wherein R.sup.1 is hydrogen atom, an alkyl group, a lower alkenyl group, a phenyl group or a group of the formula: --B--Y;Y is a nitrogen-containing monocyclic heterocyclic group or a substituted or unsubstituted phenyl group;B is a straight or branched lower alkylene group;R.sup.2 and R.sup.3 are both a lower alkyl group or are combined together to form a group of the formula: --CH.sub.2 CH.sub.2 -- or --CH.dbd.CH--;R.sup.4 is hydrogen atom, a lower alkyl group or a (lower alkoxy)carbonyl group;A is a group of the formula: --(CH.sub.2).sub.n -- or --CH(COOR.sup.5)--;n is an integer of 0, 1 or 2 andR.sup.5 is a lower alkyl group,are disclosed. The compound (I) is useful as an agent for treating and protecting various liver diseases.Type: GrantFiled: January 7, 1985Date of Patent: May 5, 1987Assignee: Tanabe Seiysku Co., Ltd.Inventors: Ikuo Iijima, Koichi Homma, Yutaka Saiga, Yuzo Matsuoka, Mamoru Matsumoto
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Patent number: 4650608Abstract: A novel star block copolymer represented by the general formula as shown below and a process for the production thereof are described. The copolymer has superior physical properties, particularly impact strength and, furthermore, is reduced in coloration. Thus the copolymer can find numerous uses; for example, it can be used in preparation of fibers, foams, automotive parts, and electrical components. The copolymer is produced by copolymerizing a star-shaped polyether prepolymer and a lactam, said prepolymer being prepared by reacting a star-shaped polyoxyalkylene having at least 3 terminal hydroxy groups and an N-chlorocarbonyl lactam, in the presence of an anionic polymerization catalyst. ##STR1## In this formula, all the symbols are as defined hereinbefore.Type: GrantFiled: August 6, 1985Date of Patent: March 17, 1987Assignee: Sumitomo Chemical Company, LimitedInventors: Saegusa Takeo, Jiro Horikawa, Masahiro Niwano, Takenobu Kanazawa
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Patent number: 4647661Abstract: A method of preparing .omega.-lactams, in particular caprolactam, comprising: a step of premixing cycloaliphatic acids having the formula ##STR1## where n=3-13, with a dehydrating agent; the first step of reaction with a nitrosating agent; the second step of reaction with the addition of a very small amount of water corresponding to a molar ratio U=H.sub.2 O/SO.sub.3 within the 0.1 to 0.9 range; and the step of reclaiming the unreacted cycloaliphatic acid. The method affords improved output from the lactamization reaction and reduced byproducts.Type: GrantFiled: March 27, 1986Date of Patent: March 3, 1987Assignee: Chimica del Friuli S.p.A.Inventors: Paolo Senni, Leandro Zuliani, Sergio Ferruzzi
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Patent number: 4639436Abstract: The invention includes certain 3,4,5-trihydroxypiperidine compounds, methods for their preparation, compositions containing said 3,4,5-trihydroxypiperidine compounds and methods for the use of said compounds and compositions.The subject matter of the invention is useful against diabetes, hyperlipaemia and adiposity as well as in animal nutrition.Type: GrantFiled: August 23, 1978Date of Patent: January 27, 1987Assignee: Bayer AktiengesellschaftInventors: Bodo Junge, Hans P. Krause, Lutz Muller, Walter Puls