Abstract: 1-Substituted-3-aminoethoxypyrrolidines having the formula ##STR1## WHEREIN R is benzyl, 2-ethoxyphenoxylower-alkyl, 2-propionyloxy-ethyl, 2-methoxy-4-acetylphenoxylower-alkyl, 4-fluorophenoxy lower alkyl, benzoyloxylower-alkyl, 3,4,5-trimethoxybenzoyloxylower-alkyl, 3,4,5-trimethoxybenzoyl, N-(4-methoxyphenyl) carbamoyl, 2-methoxyphenoxylower-alkyl, 3,4,5-trimethoxyphenyl-acetyl, 2-piperidinoethyl or carbamoyl, and Am is dilower-alkylamino, morpholino or piperidino having hypotensive properties are disclosed.
Type:
Grant
Filed:
December 5, 1977
Date of Patent:
February 13, 1979
Assignee:
A. H. Robins Company, Inc.
Inventors:
Robert F. Boswell, Jr., Robert L. Duncan, Jr.
Abstract: Cyclic and acyclic amides, substituted ureas and sulphonamides are disclosed having the property of stimulating the cold receptors of the nervous system of the body to produce a cold sensation and are used for this purpose in a variety of edible and topical preparations.
Abstract: Compounds of the formula ##STR1## wherein K.sup..sym. is a cationic group, preferably heterocyclic,R is hydrogen or an organic radical, preferably alkyl, phenyl or acyl,R.sub.1 is hydrogen, hydrocarbyl, substituted hydrocarbyl, heterocyclyl, substituted heterocyclyl, amino or substituted amino, andA.sup..crclbar. is an anion,Are useful as intermediates in the synthesis of azo dyes of the formula ##STR2## wherein D is an aromatic carbocyclic or heterocyclic diazo component radical, andK.sup..sym., r, r.sub.1 and A.sup..crclbar. are as defined above.
Abstract: New piperidine derivatives and in particular esters and amides of substituted (piperidinylidene-4) acetic acid are used as stabilizers for polymers, especially for polyolefines.
Abstract: 2,4,5,6-Tetrahydrocyclopenta[c]pyrrole-4-carboxamide and 4-thiocarboxamide derivatives useful as antisecretory and anti-ulcer agents are prepared by hydrolysis or thiohydrolysis of the corresponding 2,4,5,6-tetrahydrocyclopenta[c]pyrrole-4-carbonitriles or, in the case of the thiocarboxamides, by reaction of the 4-carboxamide with phosphorus pentasulfide.
Abstract: Novel (2-amino-2-oxoethoxy)acetic acid compounds and antisecretory compositions and methods employing (2-amino-2-oxoethoxy)acetic acid compounds are disclosed. The (2-amino-2-oxoethoxy)acetic acid compounds are also useful as cardiotonic agents and as calcium binding agents; certain of the compounds are also useful for their calcium transport properties. Novel 4-substituted 3,5-morpholinediones intermediates in the preparation of certain of the (2-amino-2-oxoethoxy)acetic acid compounds and further useful as antisecretory agents are also disclosed.
Abstract: Derivatives of 2H, 3H-benzimidazo (1,2-b) oxazole have the property of inhibiting the beta-lactamase produced by many germs resistant to penicillins and cephalosporins, and may be used in mixture with these antibiotics to increase their activity.
Abstract: New 3-amino-phenylacetic acid compounds of the formula: ##STR1## wherein X is hydrocarbyloxy or hydrocarbylthio optionally substituted by halogen, alkoxy, aryloxy, alkylmercapto or arylmercapto, or X is mono- or disubstituted amino, or represent a 5- to 8-membered heterocyclic ring;Y is oxygen or sulfur;Z is optionally substituted hydrocarbyl or hydrocarbyloxy or -thio, or Z can represent mono- or disubstituted amino, or a closed heterocyclic ring;Possess outstanding herbicidal activity, both pre-emergence and post-emergence.
Abstract: 1-heterocyclic alkyl-1,2,3,4-tetrahydroquinazolinones, acid addition salts thereof, and intermediate compounds having analgesic properties. A representative quinazolinone compound is 1-[2-(1-phenyl-4-piperazinyl)-ethyl]-2-phenyl-1,2,3,4-tetrahydro-4-quinazo linone. A representative analgesic intermediate is 2-[2-(4-[1-phenyl]piperazinyl)ethylamino]benzamide.
Abstract: Substituted 2-(carbamoyl)oxyimino-3-iminobutyramides and 2-(carbamoyl)oxyimino-3-iminobutyrates of the formula ##STR1## where Q is --OR.sub.4 or --NR.sub.5 R.sub.6, and A, R, R.sub.2, R.sub.3, R.sub.4, R.sub.5, and R.sub.6 are as hereinafter defined are useful as aphicides. The compounds are made by reacting an amine with a substituted 2-hydroxyiminoacetoacetamide (or 2-hydroxyiminopropionylacetamide) or an alkyl 2-hydroxyiminoacetoacetate (or 2-hydroxyiminopropionylacetate), then carbamylating the resulting substituted 2-hydroxyimino-3-iminobutyramide (or 2-hydroxyimino-3-iminovaleramide) or 2-hydroxyimino-3-iminobutyrate (or 2-hydroxyimino)-3-iminovalerate).
Abstract: Pyranoindole and thiopyranoindole derivatives characterized by having an amino(lower)alkyl radical attached to either or both the 1 and 9 position of a pyrano[3,4-b]indole or thiopyrano[3,4-b]indole nucleus are disclosed. The amino portion of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated into a heterocyclic amine radical. The derivatives having the amino(lower)alkyl radical only at position 1 are further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7, 8, and 9. The derivatives having the amino(lower)alkyl radical only at position 9 possess two substituents at position 1 and may be optionally substituted at position 3, 4, 5, 6, 7, and 8. The derivatives having an amino(lower)alkyl radical at both positions 1 and 9 are further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7 and 8.
Type:
Grant
Filed:
October 18, 1976
Date of Patent:
November 1, 1977
Assignee:
Ayerst McKenna and Harrison Ltd.
Inventors:
Christopher A. Demerson, Leslie G. Humber, Andre A. Asselin, Ivo Jirkovsky, Thomas A. Dobson
Abstract: Pyranoindole and thiopyranoindole derivatives characterized by having an amino(lower)alkyl radical attached to either or both the 1 and 9 position of a pyrano[ 3,4-b]indole or thiopyrano[3,4-b]indole nucleus are disclosed. The amino position of the amino(lower)alkyl radical may be further substituted with one or two lower alkyl groups or incorporated into a heterocyclic amine radical. The derivatives having the amino(lower)alkyl radical only at position 1 are further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7, 8, and 9. The derivatives having the amino(lower)alkyl radical only at position 9 posses two substituents at position 1 and may be optionally substituted at position 3, 4, 5, 6, 7, and 8. The derivatives having an amino(lower)alkyl radical at both positions 1 and 9 are further substituted at position 1 and may be optionally substituted at positions 3, 4, 5, 6, 7 and 8.
Type:
Grant
Filed:
October 18, 1976
Date of Patent:
November 1, 1977
Assignee:
Ayerst, McKenna & Harrison Limited
Inventors:
Christopher A. Demerson, Leslie G. Humber, Andre A. Asselin, Ivo Jirkovsky, Thomas A. Dobson
Abstract: The present invention is concerned with novel 4-aryl-3/4-amino/hydroxy-piperidine derivatives of the general formula I: ##STR1## wherein R.sub.1 represents hydrogen; lower alkyl; lower aralkyl; lower acyl; aminoalkyl, wherein the alkyl moiety contains 2 to 6 carbon atoms and the amino moiety may be mono- or dialkyl substituted --(CH.sub.2).sub.n --COOH; --(CH.sub.2).sub.n --OH; ##STR2## wherein X is hydrogen or halogen and n is 1, 2, 3 or 4; one of R.sub.2 and R.sub.3 represents a cyano, or a free amino group or a derivative thereof and the other represents a free or protected hydroxyl group; or R.sub.2 represents an azido group when R.sub.3 represents a free or protected hydroxyl group, or R.sub.2 and R.sub.3 together with their associated ring carbons represent an oxazepine ring, and Ar represents an aryl group which may be substituted by lower alkyl, lower alkoxy, halogen or CF.sub.3, as well as addition salts thereof with organic or inorganic acids.
Type:
Grant
Filed:
December 17, 1974
Date of Patent:
September 13, 1977
Assignee:
Delmar Chemicals Limited
Inventors:
Rudolph Kubela, Jose Maria Do Nascimento
Abstract: This application relates to benzenesulphonamides and more specifically to 1-acylamino 2- alcoxy or alcenyloxy 5-morpholinylsulfonyl benzenes and their salts with a mineral or organic acid. It also relates to processes for producing these compounds.The disclosed compounds are useful for stimulating gastric evacuation while inhibiting emisis and gastric secretion in warm-blooded animals.
Type:
Grant
Filed:
January 9, 1975
Date of Patent:
September 13, 1977
Assignee:
Science Union et Cie
Inventors:
Michel Vincent, Georges Remond, Xavier Pascaud, Jean-Claude Poignant
Abstract: Indoaniline of the formula ##STR1## wherein R.sub.1 represents hydrogen, halogen, alkyl or alkoxy;R.sub.2 represents alkyl, hydroxyalkyl, carbamylalkyl, piperidinoalkyl, morpholinoalkyl, sulfoalkyl, dialkylaminoalkyl, acylaminoalkyl, (preferably acetylaminoalkyl or benzoylaminoalkyl) and mesylaminoalkyl;R.sub.3 represents hydroxyalkyl, carbamylalkyl, piperidinoalkyl, morpholinoalkyl, sulfoalkyl, dialkylaminoalkyl, acylaminoalkyl, (preferably acetylaminoalkyl or benzoylaminoalkyl), mesylaminoalkyl; or R.sub.2 and R.sub.3 together form with the nitrogen atom to which they are attached a heterocycle selected from piperidino or morpholino;R.sub.4, r.sub.5 and R.sub.6 each independently represents hydrogen, halogen, alkyl, alkoxy, acylamino, ureido or carbalkoxyamino, and R.sub.5 can also represent amino, alkylamino, hydroxyalkylamino or carbamylalkylamino. The alkyl and alkoxy groups above can contain from 1 to 6 carbon atoms and the acyl group can contain from 2 to 7 carbon atoms.