Having -c(=x)-, Wherein X Is Chalcogen, Attached Indirectly To A Piperdine Ring By Nonionic Bonding Patents (Class 546/190)
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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: 4238613Abstract: Polyalkylpiperidinylesters and N-polyalkylpiperidinylamides of substituted malonic acids, methane tricarboxylic acids, .beta.-keto-, .alpha.-cyano-, .alpha.-phosphono- or .alpha.-sulfonocarboxylic acids are excellent stabilizers for polymers, especially against photochemical degradation. Polymers which can be stabilized in this way very effectively are polyolefins, styrene homo- and copolymers, polyamides and polyurethanes.Type: GrantFiled: October 13, 1978Date of Patent: December 9, 1980Assignee: Ciba-Geigy CorporationInventors: Michael Rasberger, Friedrich Karrer
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Patent number: 4237297Abstract: Malonic acid derivatives of the formula ##STR1## wherein Z contain sterically hindered piperidines as stabilizers against light-induced degradation for organic material.Type: GrantFiled: November 5, 1979Date of Patent: December 2, 1980Assignee: Ciba-Geigy CorporationInventors: Jean Rody, Friedrich Karrer
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Patent number: 4234471Abstract: By reacting polyalkyl-piperidones-4 with the 0.5- to 1.1-molar amount of formaldehyde in the presence of an aliphatic monoalcohol at 50.degree. to 180.degree. C., polymers of a polymerization degree of from 2 to about 200 are obtained, which may be hydrogenated or partially hydrogenated. Especially in this form, they are suitable as light stabilizers for synthetic polymers and as intermediate products for the preparation of other stabilizers for plastic materials.Type: GrantFiled: September 7, 1979Date of Patent: November 18, 1980Assignee: Hoechst AktiengesellschaftInventors: Hartmut Wiezer, Helmut Korbanka, Gerhard Pfahler
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Patent number: 4226999Abstract: A compound of the formula I ##STR1## in which R.sub.2 is an optionally substituted 4-piperidinyl bonded via oxy or imino, or an optionally substituted 2-(piperidino)-ethoxy, n is 1 or 2, R.sub.7 and R.sub.8 are hydrocarbon radicals, R.sub.9 is hydrogen or methyl, R.sub.14 is cyano, --CH.sub.2 OH, a hydroxymethyl which is C-substituted by an optionally substituted 4-piperidinyl bonded via oxy or imino, or by an optionally substituted 2-(piperidino)-ethoxy, or R.sub.14 is also acyl or nitro, and, when n=1, R.sub.15 is hydrogen, a substituted hydroxybenzyl, an optionally substituted hydrocarbon radical, an optionally substituted 4-piperidinyl, or alkylene which is optionally linked to R.sub.14 and optionally substituted, or, when n=2, R.sub.15 is a direct bond or an optionally interrupted hydrocarbon radical, and its salts as stabilizers for organic material.Type: GrantFiled: January 5, 1979Date of Patent: October 7, 1980Assignee: Ciba-Geigy CorporationInventors: Roger Malherbe, Michael Rasberger
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Patent number: 4224244Abstract: Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid, tetraenal or tetraenol derivatives useful as anti-tumor agents.Type: GrantFiled: May 9, 1979Date of Patent: September 23, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Werner Bollag, Rudolf Ruegg, Gottlieb Ryser
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Patent number: 4223139Abstract: Amine salts of tertiary amino acids have been found to be effective as catalysts for polyurethane synthesis and they have been found to exhibit delayed action, in many instances, in the polymerization of urethanes. Typically, the amine salts of tertiary amino acids are formed by initially reacting a primary or secondary amine with an aldehyde and disubstituted acid to form a Mannich adduct and then reacting the resulting Mannich acid adduct with an amine.Type: GrantFiled: October 23, 1978Date of Patent: September 16, 1980Assignee: Air Products and Chemicals, Inc.Inventors: Ibrahim S. Bechara, Rocco L. Mascioli, Philip J. Zaluska
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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: 4215215Abstract: Novel 9-phenyl 5,6-dimethyl-nona-2,4,6,8-tetraenoic acid, tetraenal or tetraenol derivatives useful as anti-tumor agents.Type: GrantFiled: July 6, 1979Date of Patent: July 29, 1980Assignee: Hoffmann-La Roche Inc.Inventors: Werner Bollag, Rudolf Ruegg, Gottlieb Ryser
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Patent number: 4210576Abstract: New derivatives of N,N'-4-piperidyl-tetralkyl-substituted alkylene diamines are disclosed. These new compounds are useful for stabilizing thermoplastic polymers, in particular polyolefins, against sunlight, heat and oxidation. A process for producing the new compounds is also disclosed, as well as the use thereof as stabilizers of polymers and polymeric compositions.Type: GrantFiled: November 28, 1978Date of Patent: July 1, 1980Assignee: Montedison S.p.A.Inventors: Piero Di Battista, Renzo Fontanelli, Francesco Gratani, Giuseppe Nelli
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Patent number: 4209516Abstract: The present invention relates to new triazole derivatives of the formula ##STR1## wherein R.sub.1 represents hydrogen, lower alkyl, optionally esterified or etherified hydroxymethyl, formyl, optionally functionally modified carboxy, or optionally mono- or disubstituted aminomethyl,R.sub.2 represents lower alkyl, and R.sub.3 represents hydrogen or lower alkyl, whereby R.sub.2 and R.sub.3 as lower alkyl can be bound directly, or in .beta.- or .gamma.-position also by way of oxygen, sulphur or the imino radical or a lower alkylimino radical, and the rings A and B independently of each other can be unsubstituted or substituted, and to their addition salts with inorganic and organic acids, in particular the pharmaceutically acceptable acid addition salts. These new compounds possess valuable pharmacological properties. In particular they have an anti-convulsive activity and are useful for the treatment of epilepsy and of conditions of tension and of agitation.Type: GrantFiled: August 31, 1978Date of Patent: June 24, 1980Assignee: Ciba-Geigy CorporationInventors: Roland Heckendorn, Rene Meier
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Patent number: 4204064Abstract: A method, composition and compounds useful in said compositions for treating the skin and scalp characterized by an excessive secretion of sebum to improve the condition thereof by reducing said excessive secretion of sebum includes topically applying to a human having skin and/or a scalp so characterized a cosmetic composition containing as an active ingredient a derivative of cysteine or cysteamine. The composition contains about 0.1-5 weight percent of said derivative and also contains as a carrier for the active ingredient, water, a mixture of water and a lower alkanol, a lower alkanol, a mixture of a lower alkanol and a cosmetic resin, a reducing agent, a neutralizing agent or a vegetable oil.Type: GrantFiled: January 24, 1978Date of Patent: May 20, 1980Assignee: L'OrealInventor: Gregoire Kalopissis
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Patent number: 4198334Abstract: Esters and amides from 4-hydroxy-and 4-amino-polyalkylpiperidines and hydroxybenzylmalonic acids substituted at the central carbon atom with an organic residue, preferably alkyl-, esteralkyl- or phosphonoalkyl-groups, are excellent stabilizers for organic polymers, especially for polyolefins. They protect the polymers as well against light degradation as against thermo-oxidative degradation. The compounds can be prepared by hydroxybenzylation of the corresponding derivatives of substituted malonic acids. Bis-malonic acid derivatives may be obtained from the monomalonics by reaction with formaldehyde.Type: GrantFiled: December 15, 1977Date of Patent: April 15, 1980Assignee: Ciba-Geigy CorporationInventor: Michael Rasberger
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Patent number: 4198306Abstract: Hydrocarbylpoly(oxyalkylene) aminoesters which are monoesters of a hydrocarbyl-terminated poly(oxyalkylene) alcohol and a monocarboxylic C.sub.2 -C.sub.20 (amino-substituted) alkanoic acid find use as fuel and lubricating oil additives.Type: GrantFiled: July 3, 1978Date of Patent: April 15, 1980Assignee: Chevron Research CompanyInventor: Robert A. Lewis
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Patent number: 4191683Abstract: Derivatives of sterically hindered 4-aminopiperidines are effective as light-stabilizers for organic polymers, especially for polyolefins. The piperidine ring is substituted with at least five alkyl groups, preferably methyl and ethyl groups. The 4-amino group is substituted with mono- or divalent acyl groups. The nitrogen in 1-position may also be substituted with a monovalent organic substituent. The compounds can be synthesized starting from higher homologs of acetone in sequence of several reaction steps.Type: GrantFiled: November 21, 1977Date of Patent: March 4, 1980Assignees: Ciba-Geigy Corporation, Sankyo Company LimitedInventors: Heimo Brunetti, Jean Rody, Nobuo Soma, Tomoyuki Kurumada
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Patent number: 4188495Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.Type: GrantFiled: November 14, 1977Date of Patent: February 12, 1980Assignee: Pfizer Inc.Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
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Patent number: 4186127Abstract: Compounds represented below ##STR1## and pharmaceutical compositions thereof, the compositions including the non-substituted phenylene dioxamates are useful in the prophylactic treatment of sensitized mammals for allergy and all anaphylactic reactions of a reagin or non-reagin mediated nature.Type: GrantFiled: July 27, 1977Date of Patent: January 29, 1980Assignee: The Upjohn CompanyInventors: Charles M. Hall, John B. Wright
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Patent number: 4172945Abstract: Compounds are provided having the structure ##STR1## wherein n is 1, 2 or 3, m is 0, 1 or 2, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 may be the same or different and can be hydrogen, lower alkyl, halo-lower alkyl, acyl, lower alkoxy-carbonyl ##STR2## amido ##STR3## or lower alkoxyalkylene, X is a straight or branched bivalent aliphatic radical and Y is ##STR4## These compounds are useful in the treatment of hypertension.Type: GrantFiled: July 27, 1978Date of Patent: October 30, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Frederic P. Hauck, Joseph E. Sundeen, Joyce Reid
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Patent number: 4169897Abstract: Novel bis-basic ethers of 9-substituted phenanthrene and related 10-oxa and 10-aza derivatives, their method of preparation and their use as pharmaceutical agents for the prevention and inhibition of viral infections are disclosed.Type: GrantFiled: November 11, 1976Date of Patent: October 2, 1979Assignee: Richardson-Merrell Inc.Inventors: Donald R. Meyer, Arthur D. Sill, Paul L. Tiernan
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Patent number: 4154722Abstract: Polyalkylpiperidinyl esters of diazocarboxylic acids are prepared, which compounds protect organic polymers against UV light degradation. The light stabilizers have the ability to react with the organic polymeric substrates thus making the piperidinyl esters migration and extraction resistant. Polymers which may be stabilized with the compounds of this invention include polypropylene, polyethylene, polystyrene and polyamides.Type: GrantFiled: June 20, 1977Date of Patent: May 15, 1979Assignee: Ciba-Geigy CorporationInventors: Roger Malherbe, Michael Rasberger
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Patent number: 4154946Abstract: New substituted acyl derivatives of amino acids which have the general formula ##STR1## are useful as angiotensin converting enzyme inhibitors.Type: GrantFiled: June 28, 1978Date of Patent: May 15, 1979Assignee: E. R. Squibb & Sons, Inc.Inventors: Miguel A. Ondetti, Michael E. Condon
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Patent number: 4153702Abstract: The invention provides novel antithrombotics diphenyl-disulphide-2,2'-bis-carboxylic acid amides of the general formula ##STR1## in which R.sup.1 represents a hydrogen or halogen atom or an optionally substituted alkyl, alkoxy or aralkoxy group,R.sup.2 represents a hydrogen or halogen atom or an optionally substituted alkyl or alkoxy group, or together with R.sup.1, and adjacent carbon atoms of the benzenoid nucleus, forms an optionally substituted aliphatic or carbocyclic aromatic ring,R.sup.3 represents an optionally substituted alkyl group,A represents a single bond or an optionally substituted alkylene chain andM and n each represents 0 or a number from 1 to 5, m and n together having a value of 2-5, and acid addition salts thereof.Also included in the invention are compositions containing said antithrombotic compounds and methods for using said compounds or compositions for combating thrombo-embolic illness. In addition, the invention includes methods for the preparation of the antithrombotic compounds.Type: GrantFiled: November 21, 1977Date of Patent: May 8, 1979Assignee: Bayer AktiengesellschaftInventors: Ulrich Horlein, Horst Boshagen, Friedel Seuter
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Patent number: 4145426Abstract: Compounds of the structure: ##STR1## where A is either ##STR2## where R.sub.1 to R.sub.4 are various substituents are active as antibacterials and antifungals.Type: GrantFiled: July 18, 1977Date of Patent: March 20, 1979Assignee: Merck & Co., Inc.Inventors: Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
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Patent number: 4141992Abstract: 2,6 Anthraquinonylene cycloalkylcarboxamidines and halobenzamidines that are effective against cecal and hepatic amebic infestations in warm-blooded animals, methods of treatment therewith and therapeutic compositions thereof.Type: GrantFiled: July 13, 1977Date of Patent: February 27, 1979Assignee: American Cyanamid CompanyInventors: Stanley A. Lang, Jr., Yang-I Lin, Thomas L. Fields, Paul F. Fabio, Keith C. Murdock
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Patent number: 4138492Abstract: The invention relates to aromatic amides N-substituted by heterocyclic groups. More particularly, the invention relates to substituted benzoic acid amides of 1-arylalkylamino or aminoalkyl-N-heterocyclic rings and to pharmaceutical compositions thereof, which have the ability to antagonize the effects of dopamine or dopaminergic agents of endogenous or exogenous origin and which may be used for the treatment of nausea and vomiting resulting from gastrointestinal disorders, congestive heart failure, post operative conditions, etc., other gastrointestinal disorders such as dyspepsia, flatulence, bile regurgitations, hiatus hernia, peptic ulcer, reflux aerophagitis, gastritis, duodenitis, and cholethiasis, and a variety of conditions affecting the central nervous system such as acute and chronic psychoses, maniacal psychosis, schizophrenias, serious disturbances of behavior and non-melancholic depressive state and migraine.Type: GrantFiled: March 17, 1975Date of Patent: February 6, 1979Assignee: Anphar, S.A.Inventors: Armando V. Noverola, Jose P. Soto, R. G. W. Spickett
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Patent number: 4134994Abstract: Amine salts of tertiary amino acids have been found to be effective as catalysts for polyurethane synthesis and they have been found to exhibit delayed action, in many instances, in the polymerization of urethanes. Typically, the amine salts of tertiary amino acids are formed by initially reacting a primary or secondary amine with an aldehyde and disubstituted acid to form a Mannich adduct and then reacting the resulting Mannich acid adduct with an amine.Type: GrantFiled: December 1, 1976Date of Patent: January 16, 1979Assignee: Air Products and Chemicals, Inc.Inventors: Ibrahim S. Bechara, Philip J. Zaluska, Rocco L. Mascioli
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Patent number: 4133957Abstract: Amine-terminated liquid polymers are prepared by reacting a carboxyl-terminated, ester-terminated or acid chloride-terminated liquid polymer having a carbon-carbon backbone with at least one aliphatic, alicyclic, heterocyclic or aromatic amine containing at least two secondary or mixed primary/secondary amine groups, but no more than one primary amine group per molecule. The novel amine-terminated polymers are useful as elastic vulcanizates, polymeric cure agents, tougheners and flexibilizers for epoxy resins, in paints and coatings, in sealants and adhesives, and the like.Type: GrantFiled: December 20, 1976Date of Patent: January 9, 1979Assignee: The B. F. Goodrich CompanyInventor: Changkiu K. Riew
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Patent number: 4130710Abstract: New piperidine derivatives and in particular esters and amides of substituted (piperidinylidene-4) acetic acid are used as stabilizers for polymers, especially for polyolefines.Type: GrantFiled: April 23, 1976Date of Patent: December 19, 1978Assignee: Ciba-Geigy CorporationInventor: Barry Cook