Abstract: The invention relates to compounds of the general formula (I) ##STR1## and physiologically acceptable salts, N-oxides, hydrates and bioprecursors thereof, in which Y represents .dbd.O, .dbd.S, .dbd.CHNO.sub.2 or .dbd.NR.sub.3 where R.sub.3 represents hydrogen, nitro, cyano, lower alkyl, aryl, lower alkylsulphonyl or arylsulphonyl; R.sub.1 and R.sub.2, which may be the same or different, each represent hydrogen lower alkyl, cycloalkyl, lower alkenyl, aralkyl, hydroxy, lower trifluoroalkyl, lower alkyl substituted by hydroxy, lower alkoxy, amine, lower alkylamino or dialkylamino, or R.sub.1 and R.sub.2 together with the nitrogen atom to which they are attached form a 5 to 7 membered heterocyclic ring which may contain other heteroatoms or the group ##STR2## where R.sub.
Type:
Grant
Filed:
June 6, 1980
Date of Patent:
July 21, 1981
Assignee:
Glaxo Group Limited
Inventors:
Michael Martin-Smith, Barry J. Price, John Bradshaw, John W. Clitherow
Abstract: New piperidine compounds of the formula ##STR1## in which the radicals have the meanings indicated in the specification and which are stabilizers against light, heat and oxidation for synthetic polymers.
Abstract: The invention entitled "Polymers containing polyalkylpiperidines and use thereof as stabilizers" provides a class of polymers in which groups containing sterically hindered polyalkylpiperidines are linked in the main chain of the polymers via bridging members containing 2-hydroxy-1,3-trimethylene groups.The polymers show superior stabilizing effects for various synthetic polymers such as polyolefins against degradation thereof induced by light and/or heat. The polymers have advantages, as compared with known stabilizer compounds, that they hardly volatile upon processing with heating or during storage of articles containing thereof, and that they are resistant to extraction with solvents from articles containing thereof.
Abstract: Covers a process for the preparation of a .beta.-aminopropionanide of the formula ##STR1## wherein R.sub.1 is H or methyl, n is an integer of 2 to 6 and R.sub.2 and R.sub.3, taken singly are hydrogen or lower alkyl groups containing 1 to 4 carbon atoms or R.sub.2 and R.sub.3, taken jointly are combined with the nitrogen atom to form a heterocyclic group selected from the groups consisting of morpholine, pyrrolidine and piperidine ring groups; which process comprises reacting in the presence of an alkali or alkaline earth metal salt of a strong acid having a pK.sub.a of less than about 2.0 acting as a catalyst a tertiaryaminoalkyl amine of the formula: where R.sub.2, R.sub.3 and n are as above with an acrylic or methacrylic compound of the formula: ##STR2## where R.sub.1 is as above and R.sub.4 is lower alkyl and recovering said .beta.-aminopropionamide.
Abstract: Covers a process for the preparation of a .beta.-aminopropionamide of the formula ##STR1## wherein R.sub.1 is H or methyl, n is an integer of 2 to 6 and R.sub.2 and R.sub.3, taken singly are hydrogen or lower alkyl groups containing 1 to 4 carbon atoms or R.sub.2 and R.sub.3, taken jointly are combined with the nitrogen atom to form a heterocyclic group selected from the groups consisting of morpholine, pyrrollidine and piperidine ring groups; which process comprises reacting in the presence of carbon dioxide acting as a catalyst a tertiaryaminoalkyl amine of the formula. ##STR2## where R.sub.2, R.sub.3 and n are as above with an acrylic or methacrylic compound of the formula: ##STR3## where R.sub.1 is as above and R.sub.4 is lower alkyl and recovering said .beta.-aminopropionamide.
Abstract: Covers a process for the preparation of a .beta.-aminopropionamide of the formula ##STR1## wherein R.sub.1 is H or methyl, n is an integer of 2 to 6 and R.sub.2 and R.sub.3, taken singly are hydrogen or lower alkyl groups containing 1 to 4 carbon atoms or R.sub.2 and R.sub.3, taken jointly are combined with the nitrogen atom to form a heterocyclic group selected from the groups consisting of morpholine, pyrrolidine and piperidine ring groups; which process comprises reacting in the presence of a Lanthanide salt having an anion derivative from a strong acid having a pK.sub.a of about 5 or less acting as a catalyst, a tertiaryaminoalkyl amine of the formula: ##STR2## where R.sub.2, R.sub.3 and n are as above with an acrylic or methacrylic compound of the formula: ##STR3## where R.sub.1 is as above and R.sub.4 is lower alkyl and recovering said .beta.-aminopropionamide.
Abstract: A non-catalytic process for the preparation of N-(tertiaryaminoalkyl)acrylamides is disclosed which comprises subjecting a corresponding .beta.-aminopropionamide to a pyrolysis temperature of about 180.degree. to 300.degree. C. after storage of the .beta.-aminopropionamide in an atmospheric holding tank at a temperature of about 150.degree. to 220.degree. C. from eight to seventy-two hours prior to pyrolysis. The corresponding .beta.-aminopropionamide compounds can be prepared by mixing and reacting at least two moles of a tertiaryaminoalkyl amine with an acrylic acid or ester compound. The inventive process provides the production of the N-(tertiaryaminoalkyl)acrylamides in high yields with minimal back addition or polymerization and greatly reduced acid impurity levels.
Abstract: Antimicrobial agents suitable for use in aqueous systems for their preservation against biodeterioration include substitutedpiperidinomethyl-propenenitriles and propanenitriles. The unsaturated compounds are prepared by reaction of a suitable piperidine with cyano acetic acid and formaldehyde: the propane derivatives therefrom by nucleophilic addition. spThis application is a continuation-in-part of Ser. No. 795,693, filed May 11, 1977, now abandoned.
Type:
Grant
Filed:
February 5, 1979
Date of Patent:
January 27, 1981
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
Abstract: Disclosed are novel polymeric quaternary ammonium salts containing specific di-tertiary amino substituted cationic recurring units. Said salts are useful as dyeing and finishing agents, especially for dyeing textile materials, such as polyacrylonitrile fiber materials, as dispersing agents and emulsifiers, as antistatic, antimicrobial and flocculating agents and as precipitants.
Type:
Grant
Filed:
June 1, 1978
Date of Patent:
January 27, 1981
Assignee:
Ciba-Geigy Corporation
Inventors:
Jaroslav Haase, Ulrich Horn, Hans-Ulrich Berendt
Abstract: A process is provided for producing bis-(N,N-dialkylamino)alkyl ethers of the formula (R.sub.2 NR').sub.2 O, wherein R is a methyl or ethyl group and R' is a bivalent alkylene group having from 2 to 3 carbon atoms. The novel process is effected by a two-step, preferably "one pot," reaction that utilizes SO.sub.3 vapor and R.sub.2 NR'ONa as reactants, wherein R and R' are defined above. The resulting bis-ethers are useful as catalysts in the production of polyurethanes, especially cellular polyurethanes.
Abstract: Compounds of the formula ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 are the same or different and are hydrogen, C.sub.1 to C.sub.6 alkyl, C.sub.6 to C.sub.14 carbocyclic aryl or aralkyl of 1 to 6 carbon atoms in the alkyl moiety and 6 to 12 carbon atoms in the carbocyclic aryl moiety and R.sup.4 is selected from the group having the formula ##STR2## where R is C.sub.1 to C.sub.8 alkyl, C.sub.1 to C.sub.8 alkoxy, halo, cyano, AlkNHC(O)-- or AlkC(O)NH-- and R' is Alk NHC(O) or Alk C(O)NH where Alk is C.sub.1 to C.sub.6 alkyl or the group 2-(endobicyclo[3.1.0]hexyl)ethyl. Methods for preparing the compounds are disclosed. The compounds are useful for the treatment of hypertension and cardiac disorders.
Abstract: 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:
Grant
Filed:
September 27, 1979
Date of Patent:
January 13, 1981
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
Abstract: 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:
Grant
Filed:
September 24, 1979
Date of Patent:
December 2, 1980
Assignee:
Pfizer Inc.
Inventors:
Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
Abstract: Compounds of the general formula I ##STR1## where B is a bridge member,the radicals R independently of one another are hydrogen or substituted or unsubstituted alkyl, or two radicals R together with the nitrogen are a heterocyclic saturated 5-membered or 6-membered ring,the radicals R.sup.1 independently of one another are hydrogen or C.sub.1 -C.sub.4 -alkyl,the radicals R.sup.2 independently of one another are hydrogen, C.sub.1 -C.sub.4 -alkyl or halogen,the radicals R.sup.3 independently of one another are hydrogen or substituted or unsubstituted alkyl or together are an alkylene group, and X.crclbar. is an anion. The compounds of the formula I are particularly suitable for dyeing paper.
Type:
Grant
Filed:
September 5, 1978
Date of Patent:
September 16, 1980
Assignee:
BASF Aktiengesellschaft
Inventors:
Hellmut Kast, Klaus Grychtol, Franz Feichtmayr
Abstract: This disclosure describes novel compounds of the formula: ##STR1## where A is --CH.sub.2 OH or ##STR2## wherein R.sub.4 and R.sub.5 each independently represent hydrogen or lower alkyl having 1 to 2 carbon atoms or together with N represent ##STR3## and, R.sub.1 is hydrogen or lower alkyl having 1 to 2 carbon atoms, andR.sub.2 and R.sub.3 each independently represent hydrogen, chloro, fluoro, methyl, methoxy or together, represent methylenedioxy, andn is 1 or 2, provided that one of R.sub.2 and R.sub.3 is other than hydrogen which are useful as hypolipidemic agents.
Abstract: 5-, 6- or 7-Membered fully saturated 1-azacarbocyclic-2-ylidene derivatives of guanidine having anti-secretory and hypoglycemic activities, and further useful for treatment of cardiovascular disease states.
Abstract: 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.
Abstract: 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.
Abstract: Chelated lithium aluminum compounds are prepared by mixing a lithium aluminum compound such as a lithium aluminum hydride with a chelating agent wherein the agent contains at least one nitrogen atom. The chelating agent is a tertiary polyamine or aminoether. The resultant chelate is used for a variety of processes such as separations, catalytic reactions, substitution reactions, reductions, electrochemical reactions, and also as an oil and fuel additive.
Type:
Grant
Filed:
February 13, 1978
Date of Patent:
May 1, 1979
Assignee:
Exxon Research & Engineering Co.
Inventors:
Arthur W. Langer, Jr., Thomas A. Whitney
Abstract: 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:
Grant
Filed:
July 18, 1977
Date of Patent:
March 20, 1979
Assignee:
Merck & Co., Inc.
Inventors:
Nathaniel Grier, Richard A. Dybas, Bruce E. Witzel
Abstract: Piperidine derivatives of formula ##STR1## can be prepared by reacting 4-amino-piperidine with for example enolic ethers. The compounds obtained may be used as stabilizers.
Type:
Grant
Filed:
March 17, 1977
Date of Patent:
February 20, 1979
Assignee:
Bayer Aktiengesellschaft
Inventors:
Burkhard Lachmann, Hans J. Rosenkranz, Harald Oertel, Alfred Pischtschan, Aziz El-Sayed