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)
  • Patent number: 4744990
    Abstract: Substituted hydantoin analogues of essential amino acids are used as nutritive supplements in animal feed compositions.
    Type: Grant
    Filed: September 25, 1986
    Date of Patent: May 17, 1988
    Assignee: W. R. Grace & Co.
    Inventors: Robert W. Bragdon, Roger R. Gaudette
  • Patent number: 4740517
    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.
    Type: Grant
    Filed: March 3, 1986
    Date of Patent: April 26, 1988
    Assignee: Sanwa Kagaku Kenyusho Co., Ltd.
    Inventors: Masayasu Kurono, Takuji Yamaguchi, Toshinao Usui, Masato Fukushima, Kuniharu Mizuno, Akira Matsubara
  • Patent number: 4737510
    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
    Inventor: Kenneth L. Rinehart, Jr.
  • Patent number: 4717725
    Abstract: Method of promoting healing of ocular wounds comprising the topical application of an aldose reductase inhibitor; compositions comprising such inhibitors are also disclosed.
    Type: Grant
    Filed: January 7, 1986
    Date of Patent: January 5, 1988
    Assignee: Alcon Laboratories, Inc.
    Inventor: Billie M. York, Jr.
  • Patent number: 4714759
    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.
    Type: Grant
    Filed: December 2, 1985
    Date of Patent: December 22, 1987
    Inventor: Robert B. Whitaker, Jr.
  • Patent number: 4713390
    Abstract: 5-(2-methyl-2-thiol ethyl) hydantoin and derivatives thereof are useful in the treatment of evolutive chronic polyarthritis.
    Type: Grant
    Filed: December 20, 1985
    Date of Patent: December 15, 1987
    Assignee: Region Wallonne
    Inventors: Pierre Dumont, Jacques Poupaert
  • Patent number: 4694010
    Abstract: Diphenylhydantoin and for dextromethorphan to control seizures.
    Type: Grant
    Filed: August 16, 1985
    Date of Patent: September 15, 1987
    Assignee: New York University
    Inventors: Jose M. Musacchio, Frank C. Tortella
  • Patent number: 4680306
    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.
    Type: Grant
    Filed: March 14, 1986
    Date of Patent: July 14, 1987
    Assignee: Pfizer Inc.
    Inventor: Christopher A. Lipinski
  • Patent number: 4677130
    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.
    Type: Grant
    Filed: October 7, 1985
    Date of Patent: June 30, 1987
    Assignee: Great Lakes Chemical Corporation
    Inventor: Edward H. Puzig
  • Patent number: 4666931
    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.
    Type: Grant
    Filed: December 27, 1985
    Date of Patent: May 19, 1987
    Assignee: Kaken Pharmaceutical Co., Ltd.
    Inventors: Yoshitaka Ohishi, Michiko Nagahara, Norio Kajikawa, Motoyuki Yajima, Katsumi Nogimori, Shigeki Kurokawa
  • Patent number: 4656175
    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.
    Type: Grant
    Filed: July 11, 1985
    Date of Patent: April 7, 1987
    Assignee: AB Ferrosan
    Inventors: Anders K. Bjork, Erik G. Christensson
  • Patent number: 4655815
    Abstract: The present invention is directed to a synergistic antimicrobial admixture comprising 2-bromo-2-bromomethylglutaronitrile and a formaldehyde donor.
    Type: Grant
    Filed: March 27, 1985
    Date of Patent: April 7, 1987
    Assignee: Calgon Corporation
    Inventor: John A. Jakubowski
  • Patent number: 4650798
    Abstract: 1-Substituted-spiro[chroman-4,4'-imidazolidine]-2',5'-dione compounds are useful for treating arrhythmia.
    Type: Grant
    Filed: January 25, 1985
    Date of Patent: March 17, 1987
    Assignee: Eisai Co., Ltd.
    Inventors: Norio Minami, Masayuki Mathukura, Koichiro Ueda, Satoru Tanaka, Toshiji Igarashi
  • Patent number: 4647574
    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.
    Type: Grant
    Filed: March 8, 1985
    Date of Patent: March 3, 1987
    Assignee: Nippon Zoki Pharmaceutical Co., Ltd.
    Inventors: Kazuharu Ienaga, Ko Nakamura
  • Patent number: 4631282
    Abstract: Antihypertensive compounds of formula (I): ##STR1## wherein the various substituents are defined hereinbelow.
    Type: Grant
    Filed: June 20, 1985
    Date of Patent: December 23, 1986
    Assignee: Beecham Group Plc
    Inventor: Frederick Cassidy
  • Patent number: 4621096
    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.
    Type: Grant
    Filed: March 26, 1985
    Date of Patent: November 4, 1986
    Assignee: Great Lakes Chemical Corporation
    Inventor: Leon M. Cole
  • Patent number: 4607026
    Abstract: This invention relates to stereoisomeric forms and mixtures thereof of compounds of the formula ##STR1## having insecticidal, nematocidal, and acaricidal properties.
    Type: Grant
    Filed: September 29, 1982
    Date of Patent: August 19, 1986
    Assignee: Roussel Uclaf
    Inventors: Jean Tessier, Andre Teche
  • Patent number: 4600717
    Abstract: Method of promoting healing of ocular wounds comprising the topical application of an aldose reductase inhibitor; compositions comprising such inhibitors are also disclosed.
    Type: Grant
    Filed: April 11, 1984
    Date of Patent: July 15, 1986
    Assignee: Alcon Laboratories, Inc.
    Inventor: Billie M. York, Jr.
  • Patent number: 4581366
    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.
    Type: Grant
    Filed: March 19, 1984
    Date of Patent: April 8, 1986
    Assignee: Imperial Chemical Industries PLC
    Inventors: David R. Brittain, Robin Wood
  • Patent number: 4575507
    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.
    Type: Grant
    Filed: May 29, 1985
    Date of Patent: March 11, 1986
    Assignee: Pfizer Inc.
    Inventor: Christopher A. Lipinski
  • Patent number: 4569928
    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
  • Patent number: 4567176
    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
    Inventor: Thomas H. Brown
  • Patent number: 4560553
    Abstract: Eucalyptol is used to enhance skin permeation of bio-affecting agents.
    Type: Grant
    Filed: November 21, 1983
    Date of Patent: December 24, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Jacob A. Zupan
  • Patent number: 4560678
    Abstract: A therapeutic composition containing allantoin and desoxyribonycleic acid is useful for the healing of wounds.
    Type: Grant
    Filed: November 7, 1983
    Date of Patent: December 24, 1985
    Inventor: Michele Ranson
  • Patent number: 4556666
    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
  • Patent number: 4540704
    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.
    Type: Grant
    Filed: June 7, 1983
    Date of Patent: September 10, 1985
    Assignee: Eisai Co., Ltd.
    Inventors: Kouichiro Ueda, Satoru Tanaka, Toshinobu Kunii, Kengo Kagei, Tadashi Sato, Ono Hideki, Issei Ohtsuka, Mayumi Kawase, Toshiharu Ohgoh, Tsuneo Wakabayashi
  • Patent number: 4540700
    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.
    Type: Grant
    Filed: February 7, 1984
    Date of Patent: September 10, 1985
    Assignee: Alcon Laboratories, Inc.
    Inventor: Billie M. York, Jr.
  • Patent number: 4539329
    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
  • Patent number: 4537897
    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
  • Patent number: 4496576
    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