Abstract: The derivatives of digoxin useful in the radioimmunoassay of digoxin having the following formulae: ##STR1## where R is a carboxylic acid ester. These derivatives are formed by the following process: (1) reacting the carboxylic acid in the presence of trifluoroacetic anhydride with a solution of digoxin in an inert, nonaqueous solvent medium, (2) adding water so as to form the above derivatives, (3) purifying the above derivatives from other constituents of the reaction mixture and (4) radio-labeling these derivatives for use as a labeled hapten in the radioimmunoassay of digoxin.The preferred carboxylic acids are imidazoleacetic acid and p-hydroxyphenylpropionic acid. The preferred radioactive isotope is .sup.125 I.
Abstract: Glucose polymers having an average chain length of 3 - 8 units are added to an electrolyte solution which normally has a saline taste in an amount to substantially disguise the saline taste of the electrolyte solution. Preferably, the polymer is added in an amount in the range of 15% to 50% by weight and the electrolyte solution contains the usual chloride salts of calcium, magnesium and potassium with the solution having a pH in the range of 3 - 6.
Abstract: There is provided, a novel pro-drug form of digoxin having the following formula: ##STR1## wherein R represents a member selected from the group consisting of a hydrogen atom, a residue of any naturally occurring amino acid, and a ##STR2## group, wherein X and Y, which may be the same or different, each represent a member selected from the group consisting of a methyl group and an ethyl group, or wherein X and Y may form a (CH.sub.2).sub.4 or (CH.sub.2).sub.5 heterocyclic ring with the N atom to which each of X and Y are attached, and a non-toxic inorganic or organic pharmaceutically acceptable acid addition salt thereof, with the proviso that:When R is a member other than a hydrogen atom, all of said R's must be the same member.These novel compounds will be cleaved in the bloodstream of a warm-blooded animal, thus delivering digoxin in a cardiotonic effective amount.
Abstract: 2,5-Dimethyl-1-pyrrole-lower-alkanecarboxamides, prepared by reaction of a 3-R.sub.3 -4-R.sub.4 -2,5-hexanedione with either an .omega.-amino-lower-alkanonitrile or an .omega.-amino-lower-alkanecarboxamide, and if appropriate, hydrolysis of the resulting 2,5-dimethyl-3-R.sub.3 -4-R.sub.4 -1-pyrrole-lower-alkano-nitrile, have anti-secretory and anti-ulcer activities.
Abstract: Gas-free paste or gel dentifrices are made by a process which includes producing a degassed gel of a gelling agent in a polyhydric alcohol, and admixing it with other dentifrice constituents, including powdered light weight polishing agent, under vacuum. Preferably, the powdered polishing agent is degassed in a vacuum hopper, before addition to the gel base in a mixer. Where no vacuum hopper or similar facilities are available, however, powdered polishing agent may be added to the gel in a suitable mixer with adequate head space and any gas present is removed from it by vacuum while it is resting on the surface of the gel, after which the polishing agent is mixed in with the gel.
Type:
Grant
Filed:
December 9, 1974
Date of Patent:
April 26, 1977
Assignee:
Colgate-Palmolive Company
Inventors:
Giulio Perla, Giuseppe Mannara, Domenico Milesi
Abstract: This invention relates to highly fluorinated diazides of the formula N.sub.3 CH.sub.2 (CF.sub.2).sub.x CH.sub.2 N.sub.3 wherein x is a positive integer from 2 to 12; to the preparation of these diazides by the reaction of excess sodium azide with a ditosylate of the formula C.sub.7 H.sub.7 SO.sub.3 CH.sub.2 (CF.sub.2).sub.x CH.sub.2 O.sub.3 SC.sub.7 H.sub.7 wherein x has the same meaning given above; and to the synthesis of highly fluorinated primary diamines of the formula H.sub.2 NCH.sub.2 (CF.sub.2).sub.x CH.sub.2 NH.sub.2 wherein x has the same meaning given above by catalytic hydrogenation of said diazides.
Abstract: An aqueous interferon solution wherein the interferon has lost at least part of its initial activity is reactivated by treatment with a combination of (a) an agent for disrupting non-covalent bonds, (b) an agent for reducing disulfide bridges, and (c) an anionic or cationic surface-active agent. A heat-treatment is preferably added. Agent (a) is urea or guanidine-hydrochloride and agent (b) is mercaptoethanol or ethanethiol.
Type:
Grant
Filed:
April 3, 1975
Date of Patent:
April 12, 1977
Inventors:
William Edgar Stewart, Pierre Marie Hendrik Frans DE Somer
Abstract: This patent describes the catalytic promotion of the reaction of oxirane-containing compounds with carboxylic acid compounds at high, ambient, and low temperature. Specifically, this patent describes the method of reacting oxirane-containing compounds with carboxyl-containing compounds, preferably at temperatures at or around ambient, in the presence of active chromium III tricarboxylate salts which have unoccupied coordination sites. More specifically this patent describes the preparation of catalytically active chromium III-tricarboxylates from normally catalytically inactive chromium III tri-carboxylate hydrates. These compounds are powerful catalysts for the reactions of oxirane compounds with both organic carboxylic acids and cyclic primary imides.
Abstract: The invention provides a novel therapeutic composition comprising a pharmaceutically acceptable carrier containing a therapeutically effective amount of an ethereal monosubstitution of a monosaccharide derivative having the general formula S-O-Y, wherein S is the residue of the monosaccharide derivative selected from the group consisting of pentoses, hexoses and heptoses as single or polysubstituted acetals, ketals or esters and Y is selected from the group consisting of cyclic monovalent nitrogen-containing organic radicals and residua and monovalent organic radicals and residua having the general formula ##STR1## wherein R.sub.1 is a divalent organic radical having a linear carbon chain length of about 1-7 carbon atoms and R.sub.2 and R.sub.3 are selected from the group consisting of --H, --OH, --SH; halogen and monovalent organic radicals and residua having a linear carbon chain length of about 1-7 carbon atoms.
Abstract: The invention provides a novel therapeutic composition comprising a pharmaceutically acceptable carrier containing a therapeutically effective amount of an ethereally monosubstituted monosaccharide having the general formula S--O--Y, wherein S is the residue of a monosaccharide selected from the group consisting of pentoses, hexoses and heptoses and Y is selected from the group consisting of cyclic monovalent nitrogen containing organic radicals and residua and monovalent organic radicals and residua having the general formula ##STR1## wherein R.sub.1 is a divalent organic radical having a linear carbon chain length of about 1-7 carbon atoms and R.sub.2 and R.sub.3 are selected from the group consisting of --H, --OH, --SH, halogen and monovalent organic radicals and residua having a linear carbon chain length of about 1-7 carbon atoms. The invention also provides certain novel ethereally monosubstituted monosaccharides, of which 3--O--3'-(N',N'-dimethylamino-n-propyl)-D-glucose is an example.
Abstract: Compounds of the formula ##STR1## wherein E is ##STR2## R.sub.1 is hydrogen; straight or branched alkyl of 1 to 3 carbon atoms; (alkoxy of 1 to 5 carbon atoms)-(alkyl of 1 to 3 carbon atoms); phenyl; or benzyl;R.sub.2 is hydrogen; hydroxyl; straight or branched alkyl of 1 to 3 carbon atoms; or phenyl;R.sub.
Type:
Grant
Filed:
March 29, 1976
Date of Patent:
April 5, 1977
Assignee:
Boehringer Ingelheim GmbH
Inventors:
Bernd Wetzel, Eberhard Woitun, Roland Maier, Wolfgang Reuter, Hanns Goeth, Uwe Lechner
Abstract: Novel compounds, which are useful as additives in lubricating oils, are disclosed. The novel compounds are represented by the formula ##STR1## wherein R is an alkenyl group containing 10 to 100 carbon atoms; R' is an alkylene group containing 1 to 5 carbon atoms; n is an integer of 1 to 4; X is selected from the group consisting of NH.sub.2, NR"R", NHR", and OR"; and Y is selected from the group consisting of NR"R", NHR", OR", and halogen, wherein R" is alkyl, phenyl, alkyl-substituted phenyl, or alkylene polyamino. A process for preparing the novel compounds is disclosed, also.
Abstract: The present invention relates to new 1-(bis-trifluoromethylphenyl)-2-oxo-pyrrolidine-4-carboxylic acid derivatives, to processes for their production, to compositions containing these active substances, as well as to the use of these active substances and compositions for the regulation of plant growth and as herbicides.These derivatives correspond to formula I ##STR1## wherein A represents the nitrile or carboxylic acid group or a derivative of the carboxylic acid.
Abstract: Novel alkylamine fluorophosphates of the formula: ##STR1## wherein R is a linear or branched alkyl group containing 1-20 carbon atoms; R.sub.1 is lower alkyl or hydrogen, R.sub.2 is alkyl or hydrogen; X is 1 or 2; Y is 1 when X=1; Y is 1 or 2 when X=2; m and n are positive whole integers whose sum is 3. When R, R.sub.1 and R.sub.2 are alkyl they can be substituted with an hydroxy group. The novel fluorophosphates have been found to be effective in reducing the acid solubility of tooth enamel.
Type:
Grant
Filed:
October 20, 1975
Date of Patent:
March 8, 1977
Assignee:
Carter-Wallace, Inc.
Inventors:
Gianluigi Soldati, Ralph G. Eilberg, Helga Melger, David A. Schlichting
Abstract: This invention provides novel guar gum formate esters having a degree of substitution between about 0.01 and 3.0, and further provides a process for producing guar gum formate esters by the interaction of guar gum powder or guar gum splits with concentrated formic acid. The invention process represents a general method for formylation of polygalactomannan gums. The polygalactomannan gum formate esters are useful as flocculants, and as sizing agents for paper and textiles.
Abstract: Carbonic acid esters of the formula substituent(s) substituents(s)R'.sub.1 OCOOR'.sub.2wherein R'.sub.1 is lower alkyl which may have substituent)s) selected from the group of halogen, lower alkoxy and aryloxy, or ar(lower)-alkyl which may have substituents)s) selected from the group of lower alkoxy, halogen, nitro and cyano, andR'.sub.2 is benzotriazolyl which may have halogen; or a group represented by the formula: ##STR1## wherein Y' and Z' are each cyano, nitro, carbamoyl, esterified carboxy, lower alkanoyl, aroyl or disubstituted carbamoyl; provided that whenR'.sub.2 is a group represented by the formula: ##STR2## wherein Y' and Z' are each cyano, nitro, carbamoyl or esterified carboxy, R'.sub.1 is ar(lower) alkyl having substituent(s) selected from the group of lower alkoxy, halogen, nitro and cyano.A process for the protection of amino and/or imino groups in compounds containing them by reacting them with the aforementioned esters is also disclosed.
Abstract: An 1-N-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin of the formula ##STR1## wherein R is a hydrogen atom or .beta.-D-ribofuranosyl group of the formula ##STR2## and R.sub.3 is hydroxyl, amino-NH.sub.2 or acylamino group --NHR.sub.4 in which R.sub.4 is an acyl group, and n is a whole number of 1 to 4, may be produced by subjecting the corresponding O-((S)-.alpha.-substituted-.omega.-aminoacyl)-neamine or -ribostamycin of the formula ##STR3## or its hydroxyl-masked and maino-masked form, to the action of a basic medium to produce an acyl-migration product of the formula: ##STR4## and, optionally converting the amino-masking groups into hydrogen atoms and also the hydroxyl-masking group into hydroge atom in a known manner if said amino-masking groups and said hydroxyl-masking groups are present in the acyl-migration product. The 1-N-((S)-.alpha.-substituted-.omega.