Nitrogen Attached Directly To The Piperidine Ring By Nonionic Bonding Patents (Class 546/244)
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Patent number: 4605743Abstract: 2,2,6,6-tetraalkyl-4-piperidylamines are produced by reacting an amine with a 2,2,6,6-tetraalkyl-4-piperidone in the presence of a palladium catalyst.Type: GrantFiled: April 16, 1985Date of Patent: August 12, 1986Assignee: Uniroyal Chemical Company, Inc.Inventors: Russell E. Malz, Jr., Harold Greenfield
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Patent number: 4599338Abstract: Xanthine compounds of the formula: ##STR1## in which: R.sub.1 is hydrogen or (C.sub.1 -C.sub.5) alkyl;R.sub.2 is hydrogen, (C.sub.1 -C.sub.5) alkyl optionally having a double bond, or benzyl;R.sub.3 is hydrogen or methyl;A is (CH.sub.2).sub.n, in which n is an integer from 1 to 4, optionally substituted, when n is higher than 1, by hydroxy;X is nitrogen or ##STR2## and the substituents R are each (C.sub.1 -C.sub.5) alkyl or they form together a polymethylene chain from C.sub.4 to C.sub.6, optionally containing an oxygen or a sulfur atom.These compounds and physiologically tolerable acid addition salts thereof may be used as medicines especially in the treatment of migraine and asthenia.Type: GrantFiled: January 16, 1985Date of Patent: July 8, 1986Assignee: Adir, S.A.R.L.Inventors: Gilbert Regnier, Claude Guillonneau, Jacques Duhault, Francois Roman
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Patent number: 4588734Abstract: Compounds of the structure: ##STR1## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are hydrogen, alkyl, alkenyl, alkynyl, phenyl-alkyl, or cycloalkyl,n is an integer from 0 to 4 inclusive,M is heterocyclic or heterocyclic alkyl,Y is hydroxy, alkoxy, amino, or substituted amino, amino-alkanoyl, aryloxy, aminoalkoxy, or hydroxyalkoxy, andR.sub.7 is hydrogen, alkanoyl, carboxylalkanoyl, hydroxyalkanoyl, amino-alkanoyl, cyano, amidino, carbalkoxy, ZS, or ##STR2## wherein Z is hydrogen, alkyl, hydroxyalkyl, aminoalkyl or the radical ##STR3## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, n, M and Y are as described above; and where Y is hydroxy their nontoxic, pharmaceutically acceptable alkali metal, alkaline earth metal, and amine salts.These compounds possess antihypertensive and angiotensin converting enzyme inhibitory activity.Type: GrantFiled: November 19, 1984Date of Patent: May 13, 1986Assignee: USV Pharmaceutical Corp.Inventors: John T. Suh, Jerry W. Skiles, Bruce E. Williams, Alfred Schwab
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Patent number: 4564677Abstract: Disclosed is a method of preparing N-amino compounds from corresponding secondary amines by reacting a secondary amine with nitrous acid and zinc in a neutral pH reaction media to form the corresponding N-amine.Type: GrantFiled: January 19, 1984Date of Patent: January 14, 1986Assignee: USV Pharmaceutical Corp.Inventor: Martin L. Kantor
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Patent number: 4544654Abstract: Novel substituted sulfonamidobenzamides are described as useful antiarrhythmic agents. Their use in the treatment of cardiac arrhythmias, especially re-entrant arrhythmias, via the prolongation of the action potential of cardiac tissue is provided. Pharmaceutical formulations containing such compounds are also disclosed.Type: GrantFiled: March 20, 1984Date of Patent: October 1, 1985Assignee: Schering A.G.Inventors: David D. Davey, William C. Lumma, Jr., Ronald A. Wohl
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Patent number: 4529437Abstract: Thiocarbamoyl-guanidine derivatives having herbicide activity are disclosed.The process for their preparation and their use as herbicides are disclosed too.Type: GrantFiled: June 16, 1980Date of Patent: July 16, 1985Assignee: Montedison S.p.A.Inventors: Roberto Colle, Franco Gozzo, Ciro Preziuso, Antony G. M. Barrett, Derek H. R. Barton
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Patent number: 4528374Abstract: Novel oligomer or polymer polyamine-1,3,5-triazines containing at least one polyalkylpiperidine radical, for example that of the formula ##STR1## processes for their production, their use for stabilizing organic material, and the organic material protected therewith against oxidative and light-induced degradation.Type: GrantFiled: November 9, 1981Date of Patent: July 9, 1985Assignee: Ciba-Geigy CorporationInventor: Erwin Nikles
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Patent number: 4496542Abstract: Compounds of the formula ##STR1## wherein R and R.sub.9 are independently hydroxy and lower alkoxy,R.sub.1 and R.sub.2 are independently hydrogen, lower alkyl, aryl-lower alkyl having from 7 to 12 carbon atoms, or heterocyclic-lower alkyl having from 6 to 12 carbon atoms,R.sub.3, R.sub.4, R.sub.5, R.sub.7 and R.sub.8 are hydrogen or lower alkyl,R.sub.6 is heterocyclic and their pharmaceutically acceptable, nontoxic acid addition salts and where R or R.sub.9 or both are hydroxy, their pharmaceutically acceptable, nontoxic basic salts, possess antihypertensive activity.Type: GrantFiled: April 13, 1983Date of Patent: January 29, 1985Assignee: USV Pharmaceutical CorporationInventors: Jerry W. Skiles, Raymond D. Youssefyeh, John T. Suh, Howard Jones
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Patent number: 4487887Abstract: Polymers of diallyl amino-4-(2,2,6,6-tetramethyl piperidyl) carboxylic acid esters and amides are provided, having a molecular weight within the range from about 800 to about 20,000, and derived from a monomer having the formula: ##STR1## wherein: R is alkylene or alkyleneoxy having from one to about six carbon atoms and m is 0 or 1;R.sub.1 is selected from the group consisting of hydrogen; oxyl; alkyl and hydroxyalkyl having from one to about eighteen carbon atoms; alkylaryl having from seven to about eighteen carbon atoms; epoxy alkyl having from three to about eighteen carbon atoms; and acyl having from two to about eighteen carbon atoms; andY is selected from the group consisting of ##STR2## where R.sub.2 and R.sub.3 are hydrogen or alkyl having from one to about eight carbon atoms and n is 0 or 1;Z is selected from the group consisting of ##STR3## in which R.sub.4, R.sub.5 and R.sub.Type: GrantFiled: September 9, 1983Date of Patent: December 11, 1984Assignee: Adeka Argus Chemical Co., Ltd.Inventors: Yutaka Nakahara, Ryoji Kimura
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Patent number: 4487900Abstract: Polymers of diallyl 4-(2,2,6,6-tetramethyl piperidyl) amines are provided, having a molecular weight within the range from about 800 to about 20,000, and derived from the monomer ##STR1## wherein: R is selected from the group consisting of hydrogen, oxyl, alkyl and hydroxyalkyl having from one to about eighteen carbon atoms; alkylaryl having from seven to about eighteen carbon atoms; epoxy alkyl having from three to about eighteen carbon atoms and acyl having from two to about eighteen carbon atoms, as well as stabilized synthetic resin compositions having an improved resistance to deterioration by light and containing such a polymer.Type: GrantFiled: September 9, 1983Date of Patent: December 11, 1984Assignee: Adeka Argus Chemical Co., Ltd.Inventors: Yutaka Nakahara, Ryoji Kimura
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Patent number: 4468403Abstract: Pharmaceutical compounds of the general formula (1) have been prepared ##STR1## and non-toxic pharmaceutically acceptable salts thereof, wherein R.sub.1 is a lower alkyl, phenyl lower alkyl, amino substituted phenyl lower alkyl, nitro substituted phenyl lower alkyl, cycloalkyl lower alkyl or a lower alkenyl substituent, R.sub.2 is a member selected from the group consisting of a cyano, pyridylsulfonyl, lower alkyl substituted sulfonyl, phenylsulfonyl, lower alkyl substituted phenylsulfonyl, lower alkoxy substituted phenylsulfonyl, halogen substituted phenylsulfonyl, nitro substituted phenylsulfonyl, amino substituted phenylsulfonyl and lower alkyl amido substituted phenylsulfonyl; R.sub.3 is a hydrogen or halogen atom; and R.sub.4 is a hydrogen, lower alkyl or lower alkoxy substituent, lower denoting a straight or branched chain having from 1-4 carbon atoms. These compounds exhibit analgesic agonist activity or analgesic agonist-antagonist activities.Type: GrantFiled: July 20, 1982Date of Patent: August 28, 1984Assignee: Canadian Patents & Development LimitedInventors: Edward E. Knaus, Brent K. Warren, Theodore A. Ondrus
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Patent number: 4448975Abstract: Amidines are one of the strongest organic bases and find application where this property is needed, such as in phase transfer catalysis in the form of their substituted derivatives. Their use, however, has been hampered by their expensive nature due to only mediocre yields in their preparation. The present invention provides a process for the preparation of substituted amidines in essentially quantitative yields.Type: GrantFiled: October 15, 1981Date of Patent: May 15, 1984Assignee: General Electric CompanyInventor: Victor Mark
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Patent number: 4429157Abstract: Primary amines and/or diamines can be prepared from oxo compounds, optionally containing additional reducible groups, by a process comprising:(1) reacting the oxo compound with ammonia in the presence of an imine-forming catalyst, preferably an ion exchanger loaded with ammonia ions, at a temperature of 10.degree. to 120.degree. C. and a pressure of 1 to 300 bar, whereby a Schiff base is formed; and(2) reducing the Schiff base by reaction with ammonia and hydrogen in the presence of a hydrogenation catalyst.Type: GrantFiled: June 10, 1981Date of Patent: January 31, 1984Inventors: Josef Disteldorf, Werner Hubel, Lothar Broschinski
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Patent number: 4412021Abstract: Polyalkylpiperidyl-ureas of the formula I ##STR1## in which m is 1-4, X, R.sup.2 and R.sup.3 are monovalent substituents and R.sup.1 is a m-valent radical, can be prepared from the corresponding 4-aminopiperidines by reaction with carbamoyl chlorides. They are outstanding stabilizers for plastics, and especially for polyolefins, to protect them against degradation by the action of light.Type: GrantFiled: February 23, 1982Date of Patent: October 25, 1983Assignee: Ciba-Geigy CorporationInventor: Friedrich Karrer
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Patent number: 4409228Abstract: The present invention relates to novel 4-amino-1-(2-pyridyl)piperidines with anorexiant action, of formula: ##STR1## in which R represents hydrogen, a halogen, a methyl group, a trifluoromethyl group, a lower alkoxy group, a trifluoromethoxy group, a 2,2,2-trifluoroethoxy group, a lower alkylthio group, a trifluoromethylthio group, a possibly substituted phenoxy group or a possibly substituted phenylthio group; to salts thereof; to a process for preparation thereof; to drugs containing same; and to intermediate products in the synthesis thereof.Type: GrantFiled: December 3, 1981Date of Patent: October 11, 1983Assignee: SanofiInventors: Dino Nisato, Paolo Carminati
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Patent number: 4409220Abstract: Compounds of the formula ##STR1## wherein A and B, which may be the same or different, each represent methylene, (alkyl of 1 to 3 carbon atoms)-methylene, ethylene or (alkyl of 1 to 3 carbon atoms)-ethylene;R.sub.1 is hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 7 carbon atoms, alkenyl of 3 to 6 carbon atoms, phenyl-(alkyl of 1 to 3 carbon atoms), halophenyl-(alkyl of 1 to 3 carbon atoms), alkanoyl of 1 to 3 carbon atoms, phenyl-(alkanoyl of 1 to 3 carbon atoms), halophenyl-(alkanoyl of 1 to 3 carbon atoms), alkoxycarbonyl of 2 to 4 carbon atoms, aralkoxycarbonyl of 8 to 10 carbon atoms or phenyl;one of R.sub.2 and R.sub.3 is amino and the other is hydrogen, chlorine, bromine, alkyl of 1 to 3 carbon atoms, alkoxy of 1 to 3 carbon atoms, alkoxycarbonyl of 2 to 4 carbon atoms, phenyl or halophenyl;and non-toxic, pharmacologically acceptable acid addition salts thereof. The compounds as well as their salts are useful as bradycardiacs.Type: GrantFiled: August 27, 1981Date of Patent: October 11, 1983Assignee: Dr. Karl Thomae Gesellschaft mit beschrankter HaftungInventors: Rudolf Hurnaus, Gerhart Griss, Robert Sauter, Wolfgang Grell, Walter Kobinger, Ludwig Pichler
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Patent number: 4377687Abstract: This invention relates to compounds having the formula: ##STR1## wherein R.sub.1 and R.sub.2 are selected from the group consisting of hydrogen, acyl, trifluoroacetyl, straight chained and branched alkyl groups with up to 6 carbon atoms, such alkyl groups with up to 3 substituents selected from the group consisting of OH, OSO.sub.2 CH.sub.3, COOH, COOR, CONH.sub.2 and Hal, where R is an alkyl group with up to 6 carbon atoms, and R.sub.1 and R.sub.2 together form a heterocyclic ring containing 4 to 6 carbon atoms and optionally further heteroatoms and such rings with up to 3 substituents selected from the group consisting of lower alkyl, OH, COOH, COOR, CONH.sub.2, where R has the above meaning, the chloroethyl nitrosoureido group and Hal, and Hal is selected from the group consisting of chlorine and fluorine, which heterocyclic ring is not the para-methyl piperazine group, said nitroso ureas having a tumor inhibiting effect.Type: GrantFiled: April 22, 1981Date of Patent: March 22, 1983Assignee: Stiftung Deutsches KrebsforschungszentrumInventor: Gerhard Eisenbrand
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Patent number: 4348406Abstract: Compounds of the formula: ##STR1## and their pharmaceutically acceptable acid addition salts, useful as anthelmintics are disclosed.Type: GrantFiled: October 20, 1980Date of Patent: September 7, 1982Assignee: Schering CorporationInventor: M. Mehdi Nafissi-Varchei
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Patent number: 4341795Abstract: Asymmetrical N-substituted bis-carbamoyl sulfide compounds exhibit exceptional broad spectrum pesticidal activity coupled with extremely low mammalian toxicity and phytotoxicity.Type: GrantFiled: December 1, 1975Date of Patent: July 27, 1982Assignee: Union Carbide CorporationInventor: Wei C. Liang
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Patent number: 4303588Abstract: Novel farnesylacetic acid amide compounds represented by general formula ##STR1## wherein A is alkylene of at least 2 carbon atoms, R.sup.1 is H or lower alkyl, and R.sup.2 and R.sup.3 are each independently H, alkyl, cycloalkyl, alkenyl, aryl or aralkyl, or either one of R.sup.2 and R.sup.3 is such a group that forms, together with A, a piperidine or pyrrolidine ring which contains as constituent thereof the nitrogen atom lying therebetween, or R.sup.2 and R.sup.3 combinedly represent a group which forms, together with the nitrogen atom to which they are bonded, a piperidine, pyrrolidine or piperazine ring; and salts thereof have antiulcerogenic and antibacterial activities.Type: GrantFiled: March 21, 1980Date of Patent: December 1, 1981Assignee: Kuraray Co., Ltd.Inventors: Susumu Okabe, Yoshiaki Omura, Yoichi Ninagawa, Yoshiji Fujita
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Patent number: 4296033Abstract: 1-Mercaptoacyl proline having an azido group in the 4-position inhibits the conversion of angiotensin I to angiotensin II in mammals and is useful for the treatment of hypertension.Type: GrantFiled: July 23, 1980Date of Patent: October 20, 1981Assignee: E. R. Squibb & Sons, Inc.Inventors: Edward W. Petrillo, Jr., Frank L. Weisenborn
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Patent number: 4256800Abstract: The antistatic composition for application to flat fibrous articles such as textiles, carpets, fabrics and the like which comprises a salt of a polymeric acid with an amine of the general formula ##STR1## wherein A=H, --OR.sub.2, ##STR2## R.sub.1 =H, a lower alkyl radical, a hydroxyalkyl, aminoalkyl, polyalkylene imine or polyalkylene glycol ether radical;R.sub.2 =H, a lower alkyl radical, a hydroxyalkyl, aminoalkyl, polyalkylene imine or polyalkylene glycol ether radical;R.sub.3 =H, a lower alkyl radical, a hydroxyalkyl, aminoalkyl, polyalkylene imine or polyalkylene glycol ether radical;R.sub.Type: GrantFiled: January 18, 1978Date of Patent: March 17, 1981Assignee: Chemische Fabrik Stockhausen & CieInventors: Dolf Stockhausen, Reinmar Peppmoller
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Patent number: 4244963Abstract: 1-[2-(Alkyl and arylsulfonyl)-2-propenyl and propyl] substituted piperidines of the formula: ##STR1## where A is ##STR2## and R.sub.1 -R.sub.5 are various substituents, are useful as antimicrobial and anti-inflammatory agents.Type: GrantFiled: September 27, 1979Date of Patent: January 13, 1981Assignee: Merck & Co., Inc.Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
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Patent number: 4242347Abstract: 1-(Indolyl-3-alkyl)-3 or 4-(ureido or guanidino)-piperidines, e.g. those of the formula ##STR1## R=H; alkyl; free, etherified or esterified OH or SH; CF.sub.3, NO.sub.2 or NH.sub.2m=1-4;n=2 or 3;X=O, S or NHacyl derivatives and salts thereof are antihypertensive agents.Type: GrantFiled: June 18, 1979Date of Patent: December 30, 1980Assignee: Ciba-Geigy CorporationInventor: Charles F. Huebner
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Patent number: 4223147Abstract: The invention relates to new methylol derivatives of 2,2,6,6-tetraalkylpiperidines, to their production and to their use as chemically attached stabilizers for polymers containing reactive OH- and NH-groups.Type: GrantFiled: September 19, 1977Date of Patent: September 16, 1980Assignee: Bayer AktiengesellschaftInventors: Harald Oertel, Paul Uhrhan, Reinhard Lantzsch, Ernst Roos, Hans Schroer, Dieter Arlt
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Patent number: 4177279Abstract: The invention provides compounds of general formula I ##STR1## and pharmaceutically acceptable acid addition and quaternary ammonium salts thereof, wherein R represents hydrogen or lower alkyl, R.sup.1 represents hydrogen or lower alkyl, R.sup.2 represents hydrogen or lower alkyl, R.sup.3 represents hydrogen, halogen, lower alkoxy, hydroxy, or lower alkyl, R.sup.4 represents hydrogen, lower alkyl, cycloalkyl of 5 to 7 carbon atoms, thienyl, furyl, phenyl; phenyl mono- or disubstituted by halogen, lower alkyl, lower alkoxy, hydroxy or trifluoromethyl; or benzoyl, halobenzoyl, lower alkanoyl, cycloalkanoyl of 6 to 8 carbon atoms, or thienoyl, A represents an alkylene, mono- or diketo- or hydroxy-alkylene radical having from 1 to 5 carbon atoms and X is oxygen or sulphur.The compounds exhibit action on the cardiovascular system particularly hypotensive and/or anti-hypertensive activity.Type: GrantFiled: July 21, 1975Date of Patent: December 4, 1979Assignee: John Wyeth & Brother Ltd.Inventors: John L. Archibald, John L. Jackson
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Patent number: 4176135Abstract: Hydrazodicarbonamide is prepared by reacting a compound represented by ##STR1## with urea while the former is being continuously or intermittently introduced into the reaction system and while the carbonyl compound and ammonia produced as by-products are being withdrawn from the system.Type: GrantFiled: January 23, 1978Date of Patent: November 27, 1979Assignee: Otsuka Kagaku Yakuhin Kabushiki KaishaInventors: Shigeaki Ohno, Toshiyuki Kazuta, Takeshi Iwata
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Patent number: 4166813Abstract: New polyalkylated 4-aminopiperidine derivatives contain in their molecule two or three piperidine rings, each having two alkyl substituents at both the 2- and the 6- positions, optionally having substituents at the 1- and 3- positions and having an amino substituent at the 4- position. The piperidine rings are joined together by attachment of the 4-amino substituents through, where there are two piperidine rings, a polyalkylene, polyether or polyester chain, or through, where there are three piperidine rings, an isocyanurate or glycerol system. These compounds and their acid addition salts are useful as stabilizers for synthetic polymers.Type: GrantFiled: May 8, 1978Date of Patent: September 4, 1979Assignee: Sankyo Company Ltd.Inventors: Nobuo Soma, Syoji Morimura, Takao Yoshioka, Tomoyuki Kurumada
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Patent number: 4154934Abstract: New mercaptoacyl derivatives of heterocyclic carboxylic acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: August 11, 1978Date of Patent: May 15, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Jack Bernstein, Kathryn A. Losee
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Patent number: 4145512Abstract: According to the invention there are obtained modified polyurethanes which have a durable, wash-fast, acid-resistant, cleaning-resistant and solvent-resistant stabilization on the basis of 2,2,6,6-tetraalkyl-piperidine light protective agents. The stabilizers are integral constituents of the polyurethanes, that is to say they are built into the polyurethane chain by a chain lengthening reaction in which two H-active reactive groups (preferably from the series of primary or secondary amino groups, carboxylic acid hydrazide, carbazic ester or semicarbazide groups) of a 2,2,6,6-tetraalkyl piperidine derivative react with isocyanate groups of polyisocyanates or isocyanate prepolymers, optionally in the presence of the usual chain lengthening agents.Type: GrantFiled: September 19, 1977Date of Patent: March 20, 1979Assignee: Bayer AktiengesellschaftInventors: Paul Uhrhan, Harald Oertel, Reinhard Lantzsch, Ernst Roos, Dieter Arlt