Divalent Chalcogen Or Acyclic Nitrogen Double Bonded Directly At Both 2- And 4- Positions, Or Tautomeric Equivalent (e.g., Hydantoin, Etc.) Patents (Class 514/389)
Abstract: A spiro-3-heteroazolidine compound and agents comprising that compound which have special utility as an antidiabetic composition and as a substance to inhibit aldose reductase enzyme activity.
Abstract: Novel bioactive metabolites from the Caribbean sponge Agelas coniferin are disclosed. These compounds are generically referred to as halopyrroles. They exhibit antiviral and antibacterial properties, and, thus, are useful for various non-therapeutic and therapeutic purposes.
Type:
Grant
Filed:
September 30, 1986
Date of Patent:
April 12, 1988
Assignee:
The Board of Trustees of The University of Illinois
Abstract: Method of promoting healing of ocular wounds comprising the topical application of an aldose reductase inhibitor; compositions comprising such inhibitors are also disclosed.
Abstract: A product and process for treating allergy are described. An immunotoxin specific for the IgE isotype is used to eliminate the IgE producing B-lymphocytes responsible for allergy.
Abstract: Spiro-imidazolones are disclosed which are useful as aldose reductase inhibitors and as therapeutic agents for the treatment of complications arising from diabetes. Pharmaceutical compositions containing the spiro compounds and a method of treating diabetic complications are also disclosed.
Abstract: The present invention is directed to a novel process for manufacturing tablets of N-halohydantoin compounds. In the process, at least one dry, particulate N-halohydantoin compound is blended with a dry, particulate alkali metal or alkaline earth salt to form a dry mixture, and the mixture is compacted into densified forms such as tablets. Dry particulate alkali metal or alkaline earth salts consist of a cation selected from among the group comprising lithium, sodium, potassium, magnesium and calcium and an anion selected from among the group comprising carbonate, bicarbonate, borate, silicate, phosphate, percarbonate, and perphosphate, to form a dry mixture and compressing the mixture.The invention is further directed to tablets produced by this process. The invention is also directed to mixtures comprising N-halohydantoin, one-half to three percent by weight alkali metal or alkaline earth salt, minor components and less than about five percent water.
Abstract: A benzofuran derivative having the general formula (I): ##STR1## wherein R.sup.1 is hydrogen atom, a benzyl group, unsubstituted or substituted with a halogen atom or an alkyloxy group, or an alkyl group having 1 to 3 carbon atoms, R.sup.2 is hydrogen atom or an alkyl group having 1 to 3 carbon atoms, R.sup.3 is acetyl group, ethyl group, carboxyl group or 4-methyl-2,5-dioxoimidazolidine-4-yl group, R.sup.4 is hydrogen atom, hydroxyl group, an alkyl group having 1 to 6 carbon atoms, an alkoxy group having 1 to 9 carbon atoms, carboxymethoxy group, nitro group, acetoamino group, a benzylozy group unsubstituted or substituted with a halogen atom, nitro group or an alkyloxy group or a group having the formula: --OR.sup.6, wherein R.sup.6 is an alkenyl group having 2 to 4 carbon atoms or an alkyl group having 2 to 3 carbon atoms having a halogen atom, cyano group or oxo group, R.sup.5 is hydrogen atom or methylenedioxy group together with R.sup.
Abstract: This invention relates to a method for treating human beings and animals suffering from mental disorders comprising administering to said human beings and animals an effective amount of a compound for the treatment of such mental disorders comprising a compound having the formula ##STR1## wherein R is alkyl straight or branch chained having from 1 to 10 carbon atoms, cycloalkyl having from 3 to 8 carbon atoms, aralkyl having from 7 to 9 carbon atoms or phenyl unsubstituted or substituted by one to three F, Cl, Br, lower alkyl having from 1 to 5 carbon atoms, lower alkoxy having from 1 to 5 carbon atoms, alkylenedioxy having from 1 to 3 carbon atoms, --CF.sub.3 or --CN substituents, R.sub.1 -R.sub.4 are independently H, CH.sub.3, C.sub.2 H.sub.5 with cis or trans configuration provided that only two of them are other than hydrogen, and pharmaceutically acceptable salts thereof.
Abstract: The present invention is directed to a synergistic antimicrobial admixture comprising 2-bromo-2-bromomethylglutaronitrile and a formaldehyde donor.
Abstract: The present invention relates to novel hydantoin derivatives represented by the general formula (I) and pharmaceutical compositions containing them as an active ingredient. ##STR1## In the formula (I), X is hydrogen or a group having the formula --OR.sub.4, and each of R.sub.1, R.sub.2, R.sub.3 and R.sub.4, which may be the same or different, is hydrogen, an alkyl group or a cycloalkyl group.Hydantoin derivatives and pharmaceutically acceptable salts thereof of the present invention have excellent hypoglycemic, hypolipidemic and diuretic effects, as well as low toxicity and great safety. Therefore, the compounds of the present invention are not only useful as antidiabetics but also as drugs for hyperlipidemia.
Abstract: Halogenated dimethylhydantoins are intimately mixed with calcium chloride and water and compressed to provide a densified particulate solid that is capable of withstanding the stresses of automatic packaging, conveying and handling.
Abstract: This invention relates to stereoisomeric forms and mixtures thereof of compounds of the formula ##STR1## having insecticidal, nematocidal, and acaricidal properties.
Abstract: Method of promoting healing of ocular wounds comprising the topical application of an aldose reductase inhibitor; compositions comprising such inhibitors are also disclosed.
Abstract: The invention concerns 1'-(4-bromo-2-fluorobenzyl)-7'-chloro-spiro[imidazolidine-4,3'-indoline]-2 ,2',5-trione in racemic or dextrorotatory form; pharmaceutical compositions thereof for use in the treatment or prophylaxis of certain complications of diabetes; and processes for its manufacture.
Abstract: Compounds related to 3',4'-dihydrospiro[imidazolidine-4,1'(2'H)-naphthalene]2,3',5-trione, spiro[chroman-4,4'-imidazolidine]2,2',5'-trione and 1',2'-dihydrospiro[imidazolidine-4,4'-(3'H)-quinoline 2,2'5-trione and reduced products thereof as aldose reductase inhibitors.
Abstract: Novel esters in all possible isomeric forms and mixtures thereof of the formula ##STR1## wherein R is selected from the group consisting of (a) optionally unsaturated alkyl of 1 to 18 carbon atoms and optionally unsaturated cycloalkyl or cycloalkylalkyl of 3 to 8 carbon atoms optionally substituted with at least one member of the group consisting of halogen, --OH, --SH, --OR', --SR', --NO.sub.2, ##STR2## --SO.sub.2 AlK.sub.2, --SO.sub.3 AlK.sub.3, aryl optionally substituted with at least one member of the group consisting of --OH, alkoxy of 1 to 8 carbon atoms, alkyl of 1 to 8 carbon atoms, halogen, --CF.sub.3, --OCF.sub.3, --SCF.sub.3 and ##STR3## R' is alkyl of 1 to 8 carbon atoms, R" and R'" are individually selected from the group consisting of hydrogen and alkyl of 1 to 8 carbon atoms, AlK.sub.1, AlK.sub.2 and AlK.sub.
Type:
Grant
Filed:
October 28, 1983
Date of Patent:
February 11, 1986
Assignee:
Roussel Uclaf
Inventors:
Jean Tessier, Andre Teche, Jean-Pierre Demoute
Abstract: This invention relates to Mannich-furyl(thienyl, pyridyl or phenyl) alkylaminoimidazolinones which have histamine H.sub.2 -antagonist activity. A specific compound of this invention is 2-[2-(5-dimethylaminomethylfuran-2-ylmethylthio)-ethylamino]-1-methyl-imid azolin-4-one.
Type:
Grant
Filed:
April 18, 1984
Date of Patent:
January 28, 1986
Assignee:
Smith Kline & French Laboratories Limited
Abstract: All stereoisomeric forms and mixtures of stereoisomers of compounds of the formula ##STR1## wherein X is selected from the group consisting of oxygen, sulfur, sulfoxide and sulfone, R.sub.1 and R.sub.3 are individually selected from the group consisting of optionally unsaturated alkyl of 1 to 7 carbon atoms and optionally unsaturated cycloalkyl of 3 to 7 carbon atoms optionally substituted with at least one halogen and optionally interrupted with at least one heteroatom and aryl and aralkyl of 6 to 18 carbon atoms and R.sub.2 is the residue of a R.sub.2 OH alcohol used in pyrethrinoids synthesis having pesticidal activity and their preparation and novel intermediates.
Type:
Grant
Filed:
October 12, 1983
Date of Patent:
December 3, 1985
Assignee:
Roussel Uclaf
Inventors:
Jean Tessier, Jean-Pierre Demoute, Joseph Cadiergue
Abstract: Novel hydantoin derivatives and salts thereof, the process for the preparation thereof, and medicines containing the same, wherein the hydantoin derivatives are represented by the general formula: ##STR1## wherein X.sub.1 and X.sub.2, which may be the same or different, independently represent a hydrogen atom, a halogen atom, a lower alkyl group or a lower alkoxy group; Y represents an oxygen atom or sulfur atom, R.sub.1 and R.sub.2, which may be the same or different, independently represent a hydrogen atom, a lower alkyl group or phenyl group, or both may form a ring with carbon atoms, excluding the case wherein both R.sub.1 and R.sub.2 are hydrogen atom, and n represents 0 or 1. The novel hydantoin derivatives and salts thereof have excellent effects for the treatment of the complications of diabetes mellitus.
Abstract: Inhibition of aldose reductase activity with tetracyclic spiro-hydantoins, new tetracyclic spirohydantoin derivatives useful in the treatment of complications arising from diabetes mellitus, and a process for preparing spiro-imidazolidine-diones by reacting a mono- or di-fluorofluorene with an excess of oxygen and a tetralkyl- or arylalkyl-trialkyl-ammonium hydroxide are disclosed.
Abstract: The invention concerns novel trifluoromethyl derivatives of 1'-halogenobenzyl-spiro[imidazolidine-4,3'-indoline]-2,2',5-trione (I), their pharmaceutically acceptable salts, and non-toxic, biodegradable precursors thereof. The derivatives are potent inhibitors of the enzyme aldose reductase and are useful in treating or preventing certain complications of diabetes. The invention also provides pharmaceutical compositions and processes for the manufacture of the derivatives.
Type:
Grant
Filed:
May 6, 1983
Date of Patent:
September 3, 1985
Assignee:
Imperial Chemical Industries, plc
Inventors:
David R. Brittain, David Brown, Robin Wood
Abstract: Novel 3-(1,2-propadienyl)-cyclopropane-carboxylates of the formula ##STR1## wherein R is alcohol used in pyrethrinoid synthesis, X and Y are both hydrogen or individually halogen or X is hydrogen or halogen and Y is alkyl of 1 to 18 carbon atoms or halogen or X is hydrogen or halogen or alkyl of 1 to 18 carbon atoms and Y is --COOR' or --CN or ##STR2## R' is alkyl of 1 to 18 carbon atoms, R.sub.2 and R.sub.3 are individually hydrogen or alkyl of 1 to 18 carbon atoms or R.sub.2 and R.sub.3 together with the nitrogen atom form a heterocycle having pesticidal properties.
Type:
Grant
Filed:
September 15, 1983
Date of Patent:
August 27, 1985
Assignee:
Roussel Uclaf
Inventors:
Jean Tessier, Jean-Pierre Demoute, Joseph Cadiergue
Abstract: A composition having broad spectrum antimicrobial activity and being freeze and heat stable is comprised of a clear solution containing up to approximately 90% by weight of a eutectic mixture of three or more lower alkyl esters of p-hydroxybenzoic acid such as isopropyl p-hydroxybenzoate, isobutyl p-hydroxybenzoate and n-butyl p-hydroxybenzoate in a ratio between approximately 1:1:1 to 4:2:2, respectively, approximately 10% to 90% by weight of a "Glydant" solution (composed of 55% 1,3-bis(hydroxymethyl)-5,5-dimethylhydantoin and 45% water) and at least approximately 0.5% by weight based on the weight of the eutectic mixture and the "Glydant" solution of an anionic surfactant. The latter, for example, may be dioctyl sodium sulfosuccinate, sodium lauryl sulfate or the ammonium or sodium salt of sulfated nonylphenoxypoly(ethyleneoxy) ethanol.
Type:
Grant
Filed:
September 12, 1983
Date of Patent:
January 29, 1985
Assignee:
Mallinckrodt, Inc.
Inventors:
Donald F. Loncrini, Thomas E. Haag, Steven R. Freebersyser