Sulfur Attached Indirectly To The Diazine Ring By Nonionic Bonding (e.g., Thiamines, Etc.) Patents (Class 544/327)
  • Patent number: 5500415
    Abstract: A process for the preparation of spherules and emulsions containing such spherules. A primary oil-in-water emulsion is formed containing particles comprising one or more active principles in oily form suspended in water, the water optionally containing at least one protein. Controlled division of the primary emulsion is achieved by combining the primary emulsion with a water-immiscible solvent to create a second emulsion containing spherules of the primary emulsion. Preferably, the particles of the primary emulsion have mean diameters of about 1 .mu.m, and preferably, the spherules contained in the second emulsion have a diameter ranging from 100 .mu.m to 500 .mu.m. If protein is contained in the primary emulsion, the protein can be cross-linked. Further, the spherules can be separated from the water-immiscible solvent.
    Type: Grant
    Filed: March 31, 1994
    Date of Patent: March 19, 1996
    Assignee: Rhone-Poulenc Nutrition Animale
    Inventors: Jean-Marie Dollat, Marc Molin, Pascal Theallier
  • Patent number: 5498612
    Abstract: Disclosed are a 4-phenethylaminopyrimidine compound represented by the formula (I): ##STR1## wherein R.sup.1 represents halogen, hydroxyl, acyloxy, alkoxy, haloalkoxy, alkylthio, benzyloxycarbonyloxy, alkyloxycarbonyloxy, alkylsulfonyloxy, tri(alkyl)silyloxy or alkyloxycarbonylalkyloxy;R.sup.2 represents hydrogen, alkyl, alkoxy, halogen, haloalkyl, haloalkoxy, unsubstituted or substituted benzoyl, hydroxyl, haloalkylcarbonyl, alkylsulfonyloxy, haloalkylsulfonyloxy, alkylsulfonyl, alkylsulfinyl, haloalkylsulfinyl, tri(alkyl)silylalkoxy, alkylthio, unsubstituted or substituted pyridyloxy, unsubstituted or substituted phenoxy, alkenyloxy, haloalkenyloxy, unsubstituted or substituted benzyl, 2-phenyl-2-1,3-dioxolanyl, alkoxyiminobenzyl, nitro, haloalkylthio or alkynyloxy; n is an integer of 1 to 5 and * represents an asymmetric carbon atom.a process for preparing the same and an agricultural and horticultural chemical for controlling noxious organisms which contains the same as an active ingredient.
    Type: Grant
    Filed: January 30, 1995
    Date of Patent: March 12, 1996
    Assignee: Ube Industries, Ltd.
    Inventors: Tokio Obata, Katsutoshi Fujii, Akira Ooka, Yoshinori Yamanaka
  • Patent number: 5468768
    Abstract: A series of novel serotonergic indolyl derivatives of cycloalkanyl- and cycloalkenyl-amines of Formula I are intended for use in the alleviation of vascular headaches.
    Type: Grant
    Filed: January 6, 1994
    Date of Patent: November 21, 1995
    Assignee: Bristol-Myers Squibb Company
    Inventors: Joseph A. Cipollina, Jonas A. Gylys, Ronald J. Mattson, Charles P. Sloan
  • Patent number: 5461026
    Abstract: The present invention relates to novel pyridinesulfonylurea derivatives, having a herbicidal activity, which is described in the following structure of general formula (I) ##STR1## wherein, Q is Q-1, Q-2, Q-3 or Q-4 as follows; ##STR2## E is single bond or CH.sub.2 R.sup.2 is C.sub.1 -C.sub.6 alkyl substituted with 1 to 3 halogens;R.sup.1, R.sup.3, W and A are defined in the claims; and these may be an agriculturally suitable salt.
    Type: Grant
    Filed: November 29, 1993
    Date of Patent: October 24, 1995
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Dae-Whang Kim, Hae Sung Chang, Jae Wook Ryu, In Ho Jo
  • Patent number: 5461025
    Abstract: The present invention relates to novel benzenesulfonylurea derivatives, having a herbicidal activity, which is described in the following structure of general formula (I) ##STR1## wherein R.sup.1 is H,C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 haloalkyl, halogen, CN, NO.sub.2, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 haloalkoxy, SO.sub.2 NR.sup.I R.sup.II, C.sub.1 -C.sub.3 alkylthio, C.sub.1 -C.sub.3 alkylsulfinyl, C.sub.1 -C.sub.3 alkylsulfonyl, SCH.sub.2 F, NH.sub.2, NHCH.sub.3, N(Me).sub.2, C.sub.1 -C.sub.2 alkyl substituted with C.sub.1 -C.sub.2 alkoxy, C.sub.1 -C.sub.2 haloalkoxy, SH, SCH.sub.3, CN or OH, or CO.sub.2 R.sup.III ; and then R.sup.1 is H, C.sub.1 -C.sub.4 alkyl, C.sub.2 -C.sub.3 cyanoalkyl, methoxy or ethoxy; R.sup.II is H, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.4 alkenyl, or when taken together connecting R.sup.I and R.sup.II, --(CH.sub.2).sub.3 --, --(CH.sub.2).sub.4 --, --(CH.sub.2).sub.5 -- or --CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 -- , may be formed;R.sup.III is C.sub.1 -C.sub.
    Type: Grant
    Filed: December 9, 1993
    Date of Patent: October 24, 1995
    Assignee: Korea Research Institute of Chemical Technology
    Inventors: Dae-Whang Kim, Young Kwan Ko, Jin-Seog Kim, Dong Whan Ku
  • Patent number: 5446040
    Abstract: Compounds of the formula ##STR1## wherein the variables R.sub.1 and p and the rings A and B are as defined in claim 1, and, where appropriate, tautomers thereof, in each case in free form or in the form of a salt, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: November 29, 1993
    Date of Patent: August 29, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Harald Walter
  • Patent number: 5444060
    Abstract: The present invention provides an N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring represented by formula [I]: ##STR1## wherein R.sup.1 represents an alkyl group, an alkenyl group, or the like, R.sup.2 represents a hydrogen atom, an alkyl group, or the like, R.sup.3 and R.sup.4 represent independently an alkyl group, alkoxy group, or the like, and X and Y represent independently a methyne group or a nitrogen atom; or the salt of the same, a method for producing the same, and a biocide containing the same as an active ingredient. The N-sulfonyl carboxylic amide derivative including an N-containing 6-membered aromatic ring according to the present invention exhibits superior effects against blight caused by plant pathogenic fungi belonging to Oomycetes such as downy mildew, late blight, or the like in a low concentration as well as controls weeds occurring in paddy fields and plowed fields.
    Type: Grant
    Filed: November 2, 1993
    Date of Patent: August 22, 1995
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Ikumi Urushibata, Takumi Yoshimura, Takeshi Deguchi, Norihasa Yonekura, Junetsu Sakai, Shigeru Hayashi
  • Patent number: 5440040
    Abstract: The present invention is directed to compounds of formula (I), ##STR1## wherein R.sup.1 is OH, NH.sub.2 ; R.sup.2 is a heteroaromatic or aromatic substituent; R.sup.3 is H, OH, F, OCH.sub.3 ; R.sup.4 is H, F, OH or an ether or ester residue thereof, OCH.sub.3, CN, C.dbd.CH, N.sub.3 ; R.sup.5 is OH or an ether or ester residue thereof including mono, di- and triphosphate esters (.alpha.), wherein n is 0 or 1 and M is hydrogen or a pharmaceutically acceptable counterion such as sodium, potassium, ammonium or alkylammonium; and pharmaceutically acceptable salts thereof; and pharmaceutical compositions comprising said compounds can be used for therapeutic treatment of virus infections. The present invention is also directed to compounds of formula (I'), ##STR2## wherein R.sup.1 and R.sup.2 are as defined above, as intermediates.
    Type: Grant
    Filed: January 18, 1991
    Date of Patent: August 8, 1995
    Assignee: Medivir AB
    Inventor: Salo Gronowitz
  • Patent number: 5439911
    Abstract: There is disclosed a novel 4-aminopyrimidine derivative containing an optionally esterified carboxyl group at the 5-position which has potent fungicidal activity as well as insecticidal and miticidal activity. The compound is useful as agricultural fungicides, insecticides and miticides. There are also disclosed a process for producing the above compound and agricultural fungicidal, insecticidal and miticidal compositions.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: August 8, 1995
    Assignee: Shionogi & Co., Ltd.
    Inventors: Toshikazu Ohtsuka, Moriyasu Masui, Takami Takeda, Michio Masuko, Katsuaki Ohba
  • Patent number: 5436324
    Abstract: Improved reactive dyestuffs of the following formula (I) ##STR1## in which the substituents have the meaning given in the description. The improved reactive dyestuffs are highly suitable for the dyeing and printing of natural or synthetic OH-- and/or amido-containing materials, in particular, those made of cellulose and polyamides.
    Type: Grant
    Filed: July 23, 1992
    Date of Patent: July 25, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfram Reddig, Karl-Josef Herd
  • Patent number: 5420255
    Abstract: A process for the continuous reaction of halogenopyrimidines with amines, a halogenopyrimidine and an aqueous amine solution or suspension being passed into a reactor and the reaction product being subsequently conducted away, is described, characterized in that the starting materials are introduced into the reactor simultaneously and continuously with intensive mixing.
    Type: Grant
    Filed: February 22, 1994
    Date of Patent: May 30, 1995
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegbert Arnold, Hans-Georg Frosch, Manfred Hoppe, Wolfgang Mullers, Richard Sommer
  • Patent number: 5420129
    Abstract: The invention is concerned with novel sulphonamides and their use as medicaments. In particular, the invention is concerned with compounds of the formula ##STR1## wherein R.sup.1 is hydrogen, lower-alkyl, lower-alkoxy, lower-alkylthio, halogen or trifluoromethyl;R.sup.2 is hydrogen, lower-alkyl, halogen, lower-alkoxy, trifluoromethyl or --OCH.sub.2 COOR.sup.9 ;R.sup.3 is hydrogen, lower-alkyl, halogen, lower-alkylthio, trifluoromethyl, lower-alkoxy or trifluoromethoxy;R.sup.2 and R.sup.3 together are butadienyl, methylenedioxy, ethylenedioxy or isopropylidenedioxy;R.sup.
    Type: Grant
    Filed: December 8, 1993
    Date of Patent: May 30, 1995
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael Loffler, Marcel Muller, Werner Neidhart, Henri Ramuz
  • Patent number: 5411934
    Abstract: The present invention provides a novel alkanoic acid amide derivative of the formula, ##STR1## (wherein R.sup.1 is a hydrogen atom, an alkyl group or an alkoxyalkoxy group, R.sup.2 is a group of -SO.sub.2 R or a hydroxyl group, R.sup.5 is an alkyl group, R.sup.3 is an alkyl group, a cycloalkyl group, a cycloalkenyl group or a phenyl group, R.sup.4 is a hydrogen atom or an alkyl group, X and Y may be the same or different and are an alkoxy group, an alkylamino group or a dialkylamino group, and Z is a methine group or a nitrogen atom) and its salt, a process for preparing the same and a herbicidal composition containing the same as an effective ingredient.This compound kills annual and perennial weeds grown in paddy fields and upland fields at a small dose, and is safe to a useful crop plant.
    Type: Grant
    Filed: July 30, 1992
    Date of Patent: May 2, 1995
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Takumi Yoshimura, Keiji Toriyabe, Katsumi Masuda, Ryo Hanai
  • Patent number: 5399692
    Abstract: An ultraviolet radiation absorbing agent for bonding to an ocular lens. The agent has the formulaA--NH--Bwherein A is an ultraviolet absorbing compound and B is a specific reactive group or a moiety containing reactive group.
    Type: Grant
    Filed: July 14, 1993
    Date of Patent: March 21, 1995
    Assignee: Ciba-Geigy Corporation
    Inventors: William M. Hung, Kai C. Su
  • Patent number: 5378708
    Abstract: Compounds of the formula: ##STR1## wherein A, Q and R.sup.2 to R.sup.5 are as defined in the text, compositions containing them and methods for using them to control insects, acarids and fungi.
    Type: Grant
    Filed: May 13, 1993
    Date of Patent: January 3, 1995
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Joseph E. Drumm, III, Renee M. Lett, Thomas M. Stevenson
  • Patent number: 5371062
    Abstract: The present invention relates to new substituted azines, of the general formula (I) ##STR1## in which n, Q.sup.1, Q.sup.2, Q.sup.3, R.sup.1, R.sup.2, R.sup.3, X, Y and Z have the meanings given in the description, to a plurality of processes for their preparation, and to their use as herbicides.
    Type: Grant
    Filed: April 1, 1993
    Date of Patent: December 6, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Roland Andreee, Mark W. Drewes, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
  • Patent number: 5362878
    Abstract: Compounds of the formula ##STR1## wherein R.sup.21 and R.sup.22 are as defined in the specification which are intermediates useful in the preparation of compounds of the formula ##STR2## and the pharmaceutically acceptable salts thereof, wherein Q and R.sup.1 are as defined in the specification. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
    Type: Grant
    Filed: July 20, 1992
    Date of Patent: November 8, 1994
    Assignee: Pfizer Inc.
    Inventors: George Chang, Ernest S. Hamanaka, Peter A. McCarthy, Thien Truong, Frederick J. Walker
  • Patent number: 5346902
    Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein Y is a specified small group or single atom and R.sup.1 and R.sup.2 are selected from a wide range of specified substituents.
    Type: Grant
    Filed: May 11, 1993
    Date of Patent: September 13, 1994
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Paul J. de Fraine
  • Patent number: 5340827
    Type: Grant
    Filed: June 14, 1993
    Date of Patent: August 23, 1994
    Assignee: Celltech, Limited
    Inventors: Nigel R. A. Beeley, Thomas A. Millican
  • Patent number: 5336677
    Abstract: This invention relates to substituted 4-aminopyrimidines, which by virtue of their ability to antagonize angiotensin II are useful for the treatment of hypertension, congestive heart failure, and restenosis. The compounds are also useful for reducing lipid levels in the blood plasma and are thus useful for treating hyperlipidemia and hypercholesterolemia. Also disclosed are processes for the production of said compounds and pharmaceutical compositions containing said compounds.
    Type: Grant
    Filed: June 18, 1992
    Date of Patent: August 9, 1994
    Assignee: American Home Products Corporation
    Inventors: Dimitri Sarantakis, James J. Bicksler, John W. Ellingboe, Madelene Nikaido
  • Patent number: 5324710
    Abstract: Compounds of the formula I or their salts ##STR1## in which R.sup.1 to R.sup.6, W, X, a and b are as defined in claim 1 and L is a heterocyclic or isocyclic aromatic radical having 5 to 6 ring atoms, which can be condensed with an aromatic or non-aromatic 5- or 6-membered ring, where the radical can be unsubstituted or substituted, and a, b and c independently of one another are 0 or 1, are suitable as herbicides, plant growth regulators and fungicides. They can be prepared by the processes defined herein, it being possible in some cases to use novel intermediates.
    Type: Grant
    Filed: April 21, 1992
    Date of Patent: June 28, 1994
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz, Burkhard Sachse, Peter Braun
  • Patent number: 5324837
    Abstract: 3,4-Diaryl-4,5-dihydro-1H-pyrazole compounds having a selected 5- or 6-membered aromatic heterocyclic moiety in the 4-position and an optionally substituted phenyl moiety in the 3-position, such as 4,5-dihydro-3-(4-fluorophenyl)-4-(5-trifluoromethyl-2-pyridinyl)-1H-pyrazo le were prepared as intermediates in the preparation of insecticidal 3,4,N-triaryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds. The 3,4-diaryl-4,5-dihydro-1H-pyrazole compounds can be prepared from appropriate 1,2-diarylethanone compounds by successive treatments with N,N,N',N'-tetramethyldiaminomethane in dichloromethane in the presence of acetic anhydride (to form a Mannich adduct) and hydrazine in the presence of a catalytic amount of trifluoroacetic acid.
    Type: Grant
    Filed: August 17, 1992
    Date of Patent: June 28, 1994
    Assignee: DowElanco
    Inventors: James M. Renga, Kevin L. McLaren, James T. Pechacek, Michael J. Ricks, Yulan C. Tong
  • Patent number: 5317005
    Abstract: Herbicidal pyrimidine and triazine derivatives of the formula: ##STR1## and salts thereof, where: X represents --CH.dbd. or --N.dbd.;Y is a substituted or unsubstituted alkyl or amino group;R.sup.1 represents a substituted or unsubstituted alkyl, cycloalkyl, phenyl or heterocyclyl group;R.sup.2 represents hydrogen, halogen or alkyl; andR.sup.4 and R.sup.5, which may be the same or different, each represent hydrogen, alkyl, alkoxy, amino, alkylamino, dialkylamino or halogen.
    Type: Grant
    Filed: January 19, 1993
    Date of Patent: May 31, 1994
    Assignee: Schering Agrochemicals Limited
    Inventor: Graham P. Jones
  • Patent number: 5292740
    Abstract: The novel sulfonamides of formula I, ##STR1## in which the symbols R.sup.1 -R.sup.9, R.sup.a, R.sup.b, X, Y and n have the significance given in the description and salts thereof can be used for the treatment of circulatory disorders, especially hypertension, ischemia, vasopasms and angina pectoris.
    Type: Grant
    Filed: June 9, 1992
    Date of Patent: March 8, 1994
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kaspar Burri, Martine Clozel, Walter Fischli, Georges Hirth, Bernd-Michael Loffler, Werner Neidhart, Henri Ramuz
  • Patent number: 5290773
    Abstract: A sulfonyl compound of the formula ##STR1## The above illuminated formula (I) undergo bimolecular condensation by the condensing agents and easily form simple metal salts especially metal complexes which act as combatting viruses and inhibiting tissue growth.
    Type: Grant
    Filed: March 21, 1990
    Date of Patent: March 1, 1994
    Inventor: Takeo Takayanagi
  • Patent number: 5286709
    Abstract: N-Phenylsulfonyl-N'-pyrimidinylureas and -thioureas of formula I ##STR1## in which X is oxygen, sulfur, SO or SO.sub.2 ; W is oxygen or sulfur; R.sub.1 is hydrogen or methyl; R.sub.2 is hydrogen, fluorine, chlorine, bromine, iodine, (X).sub.n R.sub.3, NO.sub.2, NR.sub.4 R.sub.5,--C.tbd.CR.sub.6, ##STR2## or cyano; n is the number 0 or 1; R.sub.3 is C.sub.1 -C.sub.4 alkyl or C.sub.1 -C.sub.4 alkyl which is substituted by 1-4 halogen atoms, C.sub.1 -C.sub.3 alkoxy or C.sub.1 -C.sub.3 alkylthio; or C.sub.2 -C.sub.4 alkenyl or C.sub.2 -C.sub.4 alkenyl which is substituted by 1-4 halogen atoms; R.sub.4 is hydrogen, CH.sub.3 O, CH.sub.3 CH.sub.2 O or C.sub.1 -C.sub.3 alkyl; R.sub.5 is hydrogen or C.sub.1 -C.sub.3 alkyl; R.sub.6 is hydrogen, methyl or ethyl; R.sub.7 is hydrogen or methyl; Z is ##STR3## R.sub.10 is hydrogen, fluorine, chlorine, methyl, trifluoromethyl, CH.sub.3 O, CH.sub.3 CH.sub.2 O, CH.sub.3 S, CH.sub.3 SO, CH.sub.3 SO.sub.2 or cyano; R.sub.11 is methyl, ethyl, CH.sub.3 O, CH.sub.3 CH.sub.
    Type: Grant
    Filed: February 8, 1993
    Date of Patent: February 15, 1994
    Assignee: Ciba-Geigy Corporation
    Inventor: Willy Meyer
  • Patent number: 5284820
    Abstract: Herbicidal substituted cycloalkenes of the formula ##STR1## in which A is a straight-chain or branched, optionally substituted alkanediyl group,X is O, S, N--R.sup.8 or CR.sup.9 R.sup.10,Y is O, S, NH or N-alkyl,Z is N or R.sup.11, andR.sup.1 to R.sup.11 represent various organic radicals.
    Type: Grant
    Filed: September 2, 1992
    Date of Patent: February 8, 1994
    Assignee: Bayer Aktiengesellschaft
    Inventors: Mark-Wilhelm Drewes, Peter Muller, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
  • Patent number: 5280025
    Abstract: Disclosed are an aralkylaminopyrimidine compound represented by the following formula: ##STR1## wherein R.sup.1 represents a halogen atom, a lower acyloxy group, a hydroxyl group, a lower alkoxy group or a lower alkylthio group; R.sup.2 represents a lower alkyl group, a hydrogen atom or a cycloalkyl group; R.sup.3 may be the same or different and represents a lower haloalkoxy group, a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, a lower alkylthio group, a nitro group, a lower haloalkyl group, a lower alkylsulfinyl group, a lower alkylsulfonyl group, a lower haloalkylthio group or a hydroxyl group; a carbon atom to which * is attached represents an asymmetric carbon atom provided that the case where R.sup.2 is a hydrogen atom is excluded; and n represents an integer of 1 to 5.a method for preparing the same and a chemical for controlling noxious organisms which contains the same as an active ingredient.
    Type: Grant
    Filed: November 17, 1992
    Date of Patent: January 18, 1994
    Assignee: Ube Industries, Ltd.
    Inventors: Tokio Obata, Katsutoshi Fujii, Kiyoshi Tsutsumiuchi, Yasushi Nakamoto
  • Patent number: 5270313
    Abstract: Sulfonamides of formula I, in which the symbols R.sup.1 -R.sup.6, X, Y and n have the significance given in the description and which are in part novel compounds, and salts thereof, which can be used as active ingredients for the manufacture of medicaments for the treatment of circulatory disorders, especially hypertension, ischemia, vasospasms and angina pectoris, are described.
    Type: Grant
    Filed: April 15, 1992
    Date of Patent: December 14, 1993
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Kaspar Burri, Martine Clozel, Walter Fischli, Georges Hirth, Bernd M. Loffler, Henri Ramuz
  • Patent number: 5262385
    Abstract: A compounds represented by the formula ##STR1## wherein X represents a fluorine atom,W represents an oxygen atom, sulfur atom or group --OCH.sub.2 --,Z.sup.1 and Z .sup.2 each represent a nitrogen atom or group CH, but when Z.sup.1 is a nitrogen atom, Z.sup.2 represents a nitrogen atom or group CH and when Z.sup.1 is a group CH, Z.sup.2 represents a nitrogen atom,R.sup.1 and R.sup.2 each independently represent either a hydrogen atom, halogen atom or mono- or dilower alkyl-substituted amino, or a lower alkyl, lower alkoxy or lower alkylthio each of which may be substituted with a halogen atom,R.sup.3 and R.sup.4 form together with the carbon atoms to which they bind respectively a 5- to 8-membered carbon ring.
    Type: Grant
    Filed: July 23, 1991
    Date of Patent: November 16, 1993
    Assignee: Mitsubishi Petrochemical Co., Ltd.
    Inventors: Atsushi Goh, Sachio Kudo, Yorio Kumamoto, Michi Watanabe, Takako Takahashi, Takako Aoki, Norishige Toshima, Keiji Endo, Hideshi Mukaida, Shinji Kawaguchi, Rika Higurashi
  • Patent number: 5252567
    Abstract: This invention concerns compounds of the formula I: ##STR1## wherein R.sup.1 is (1-10C)alkyl, (3-8C)cycloalkyl, (3-8C)cycloalkyl-(1-4C)-alkyl, phenyl or phenyl(1-4C)alkyl, the phenyl moiety of the latter two optionally bearing one or more substituents; R.sup.2 is hydrogen, (1-4C)alkyl, amino or (1-4C)alkylamino; R.sup.6 is (1-4C)alkyl, amino or (1-4C)alkylamino; Q is a group of formula II, in which case R.sup.3 and R.sup.4 are independently hydrogen, (1-4C)alkyl, phenyl or benzyl the phenyl moiety of the latter two optionally bearing one or two substituents; R.sup.5 is hydrogen, (1-4C)alkyl or (2-4C)alkenyl; A and B are independently ethylene or trimethylene; Z is a direct bond between A and B, or an oxy, thio, carbonyl, methylene, ethylenedioxymethylene, ethylidene, or isopropylidene link, or Z is a group of the formula .dbd.N.
    Type: Grant
    Filed: December 18, 1990
    Date of Patent: October 12, 1993
    Assignee: Imperial Chemical Industries PLC
    Inventors: Stuart D. Mills, Rodney B. Hargreaves, Bernard J. McLoughlin
  • Patent number: 5250530
    Abstract: Aminopyrimidine derivatives, their preparation, and agents containing them, and their use as fungicides comprising ##STR1## in which R.sup.1 is alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, substituted aminoalkyl, phenyl, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl or phenoxyphenoxyalkyl, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, or phenyl, R.sup.5 is H, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkoxy, alkylthio, alkoxyalkyl, R.sup.7 R.sup.8 N-,alkylthioalkyl, R.sup.7 R.sup.8 N-alkyl, halogen, alkenyl, alkynyl, phenyl, phenoxy, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl, phenylmercapto, phenylalkoxy or phenylalkylthio, R5 is H, alkyl, alkyloxy, alkenyloxy, alkynyloxy, alkylthio, halogen, or phenyl or R.sup.5 and R.sup.6 together form a chain, and R.sup.7 and R.sup.8 are H, alkyl, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, alkenyl, substituted formyl, phenyl or phenylalkyl, or R.sup.7 or R.sup.
    Type: Grant
    Filed: July 9, 1990
    Date of Patent: October 5, 1993
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Wolfgang Giencke, Burkhard Sachse, Heinrich Wicke
  • Patent number: 5250533
    Abstract: Fungicidal pyridinylpyrimidines of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen, alkoxy, alkylthio, halogenoalkyl, amino or dialkylamino, where, in the case of dialkylamino, the two radicals may, together with the nitrogen to which they are bonded, form a 5- to 7-membered, saturated or unsaturated ring which optionally contains a further hetero atom and which is optionally substituted by 1 or 2 alkyl groups; orR.sup.1 represents in each case optionally substituted aryloxy, arylthio, aralkyloxy or aralkylthio,R.sup.2 and R.sup.3 are independent of one another and are identical or different and in each case represent hydrogen, halogen, alkyl, halogenoalkyl, alkoxy, alkylthio or alkoxycarbonyl,orR.sup.2 and R.sup.3 together represent anaylene chain having 3 to 6 carbon atoms which are linked via the ring positions 3 and 4 or 4 and 5,R.sup.
    Type: Grant
    Filed: March 2, 1992
    Date of Patent: October 5, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Ulrich Heinemann, Alexander Klausener, Dieter Berg, Stefan Dutzmann, Wilhelm Brandes
  • Patent number: 5238907
    Abstract: The invention relates to new 2-pyrimidinyl- and 2-triazinylacetic acid derivatives of general formula I ##STR1## in which A, R.sup.2-5 and X have the meanings given in the description, processes for their preparation and their use as herbicides, fungicides and plant growth regulants.
    Type: Grant
    Filed: January 9, 1992
    Date of Patent: August 24, 1993
    Assignee: Schering Aktiengesellschaft
    Inventors: Gabriele Kruger, Christoph Harde, Nikolaus Heinrich, Anita Kruger, Erhard Nordhoff, Gerhard Tarara, Peter Wegner, Clemens Kotter, Gerhard Johann, Richard Rees, Graham P. Jones
  • Patent number: 5236923
    Abstract: New substituted pyrimidylamide oximes of the general formula (I) ##STR1## in which R.sup.1, R.sup.2, R.sup.3, A and Ar have the meanings given in the description, new intermediates for their preparation, and their use for combating pests.The new compounds of the formula (I) can be prepared by analogous processes, for example by reacting suitable pyrimidylamide oximes with suitable alkylating agents. The starting compounds which are also new, namely the pyrimidylamide oximes of the formula (II) in which --A--Ar represents hydrogen, can be prepared from suitable cynaopyrimidines with hydroxylamine or its acid adducts.
    Type: Grant
    Filed: November 26, 1991
    Date of Patent: August 17, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rolf Kirsten, Hilmar Wolf, Gerd Hanssler, Heinz-Wilhelm Dehne, Stefan Dutzmann
  • Patent number: 5234913
    Abstract: Synergistic combinations of nucleoside derivatives, pharmaceutical formulations containing said combinations and use of the combinations in the treatment of retroviral infections are disclosed.
    Type: Grant
    Filed: March 5, 1992
    Date of Patent: August 10, 1993
    Assignee: Burroughs Wellcome Co.
    Inventors: Phillip A. Furman, Jr., George R. Painter, III
  • Patent number: 5227493
    Abstract: N-fluoro perfluoroheterocyclic sulfonamides of the following Formula I ##STR1## wherein Het.sub.f represents an aromatic perfluoroheterocyclic radical of valency n and each R independently represents a substituted or unsubstituted C.sub.1 -C.sub.30 alkyl, C.sub.6 -C.sub.14 aryl substituted C.sub.1 -C.sub.10 alkyl, C.sub.6 -C.sub.14 aryl, or C.sub.1 -C.sub.10 alkyl substituted C.sub.6 -C.sub.14 aryl group, are novel electrophilic fluorinating agents. Preferably Het.sub.f is a perfluorinated nitrogen-containing aromatic group, especially pyridyl, pyrimidinyl, pyrazinyl or 1,3,5-triazinyl; n is 1; and R is perfluorinated, especially trifluoromethyl.
    Type: Grant
    Filed: August 31, 1990
    Date of Patent: July 13, 1993
    Assignee: Air Products and Chemicals, Inc.
    Inventor: Ronald E. Banks
  • Patent number: 5223505
    Abstract: This invention concerns novel aminopyrimidinium salts of the formula I: ##STR1## in which R.sup.1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R.sup.2 and R.sup.6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperidino and morpholino; and the other of R.sup.2 and R.sup.6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R.sup.2 and R.sup.6 are basic groups as mentioned above; and R.sup.5 is hydrogen, (1-4C)alkyl or (3-6C)alkenyl; or R.sup.2 is a basic group as mentioned above, and R.sup.5 and R.sup.6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R.sup.4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R.sup.4 is an optionally substitutued alkylene or alkenylene linked to the nitrogen atom of the group Q.A.
    Type: Grant
    Filed: April 20, 1990
    Date of Patent: June 29, 1993
    Assignee: Imperial Chemical Industries Plc
    Inventors: Rodney B. Hargreaves, Paul W. Marshall, Bernard J. McLoughlin, Stuart D. Mills
  • Patent number: 5196419
    Abstract: The invention concerns a heterocyclic cyclic ether of the formula I ##STR1## wherein Q is an optionally substituted 6-membered monocyclic or 10-membered bicyclic heterocyclic moiety containing one or two nitrogen atoms;A is (1-6C)alkylene, (3-6C)alkenylene, (3-6C)alkynylene or cyclo(3-6C)alkylene;X is oxy, thio, sulphinyl, sulphonyl or imino;Ar is phenylene which may optionally bear one or two substituents or Ar is an optionally substituted 6-membered heterocyclene moiety containing up to three nitrogen atoms;R.sup.1 and R.sup.2 together form a group of the formula --A.sup.2 --X.sup.2 --A.sup.3 -- which, together with the oxygen atom to which A.sup.2 is attached and with the carbon atom to which A.sup.3 is attached, defines a ring having 5 to 7 ring atoms, wherein A.sup.2 and A.sup.3 each is (1-3C)alkylene and X.sup.2 is oxy, thio, sulphinyl, sulphonyl or imino, and which ring may bear one, two or three substituents; andR.sup.
    Type: Grant
    Filed: November 4, 1991
    Date of Patent: March 23, 1993
    Assignees: Imperial Chemical Industries PLC, ICI Pharma
    Inventors: Graham C. Crawley, Annie Hamon
  • Patent number: 5194612
    Abstract: Reactive dyestuffs of the formula ##STR1## in which the substituents have the meanings given in the description, are highly suitable for the dyeing and printing of hydroxyl- and nitrogen-containing materials, such as cellulose, wool, silk, polyamides, polyurethanes.
    Type: Grant
    Filed: March 23, 1992
    Date of Patent: March 16, 1993
    Assignee: Bayer Aktiengesellschaft
    Inventors: Wolfgang Harms, Frank-Michael Stohr, Karl-Heinz Schundehutte
  • Patent number: 5190945
    Abstract: 2-(Pyrimidyl or pyrazinyl)-imino-1,3-dithietanes ##STR1## wherein Ar is one of the radicals ##STR2## R is unsubstituted C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkyl which is substituted by halogen, C.sub.1 -C.sub.3 alkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylthio or cyano, independently of one another, or is unsubstituted or halo-substituted C.sub.3 -C.sub.7 alkenyl, unsubstituted or halo-substituted C.sub.3 -C.sub.7 alkynyl, or C.sub.3 -C.sub.5 cycloalkyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.3 alkylamino, nitro or halogen,n is a number from 0 to 3,X.sub.1 and X.sub.2 independently of each other are hydrogen or halogen, including the addition salts formed with acids of the formula H.sup..sym. X.sup..crclbar. in which the anion X.sup..crclbar. is Cl.sup..crclbar., Br.sup..crclbar., I.sup..crclbar., HSO.sub.4 -, H.sub.2 PO.sub.4 -, H.sub.2 PO.sub.3 -, NO.sub.3 -, CH.sub.3 COO.sup..crclbar., CH.sub.2 ClCOO-, CF.sub.3 COO-, HOCH.sub.2 COO-, CH.sub.3 CH(OH)COO.sup..crclbar., HOOCCOO.sup..crclbar.
    Type: Grant
    Filed: November 19, 1991
    Date of Patent: March 2, 1993
    Assignee: Ciba-Geigy Corporation
    Inventors: Wolfgang Eckhardt, Urs Muller
  • Patent number: 5169856
    Abstract: The present invention relates to unsaturated carboxylic acid amide derivatives of the formula ##STR1## wherein ring A stands for an optionally substituted aromatic ring; R.sup.1 stands for a hydrogen atom or an optionally substituted hydrocarbon residue or forms an optionally substituted carbocyclic ring with the adjacent group --CH.dbd.C-- together with two carbon atoms constituting the ring A; R.sup.2 stands for a hydrogen atom, an optionally substituted hydrocarbon residue or an optionally substituted acyl group; R.sup.3 stands for an optionally substituted hydrocarbon residue; and n denotes an integer ranging from 2 to 6, and salts thereof, as well as the production thereof.The compounds of the present invention act on the central nervous system of mammals and has a strong anti-cholinesterase activity, which can be used for the prophylaxis and therapy of, for example, senile dementia, Alzheimer's diseases, Huntington's chorea, et., and are useful as medicines.
    Type: Grant
    Filed: February 6, 1989
    Date of Patent: December 8, 1992
    Assignee: Takeda Chemical Industries, Inc.
    Inventors: Giichi Goto, Akinobu Nagaoka
  • Patent number: 5166206
    Abstract: Substituted pyrimidines, pyrimidinones and pyridopyrimidines of formula (I) are as angiotensin II antagonists useful in the treatment of hypertension, ocular hypertension and certain CNS ailments: ##STR1## wherein K is --N(R.sup.8a)--C(.dbd.M) or --N.dbd.C(R.sup.8b) where M is O or NR.sup.22.
    Type: Grant
    Filed: March 27, 1991
    Date of Patent: November 24, 1992
    Assignee: Merck & Co., Inc.
    Inventors: Eric E. Allen, William J. Greenlee, Malcolm MacCoss, Arthur A. Patchett
  • Patent number: 5149357
    Abstract: Compound of the formula ##STR1## in which A is O, S, or NR.sup.3 ; G is CH or N; R and R.sup.1 are independently alkyl, alkoxy, haloalkoxy or alkylamino; R.sup.2 is phenyl, substituted phenyl, alkyl, cycloalkyl, haloalkyl or --CH.sub.2 [(R.sup.4)C(R.sup.5).sub.n --Z; R.sup.3 and R.sup.7 are, independently, hydrogen, alkyl, --C(O)NH.sub.2 or --C(O)alkyl; R.sup.4 and R.sup.5 are independently hydrogen, alkyl, or halogen; R.sup.6 is halogen, alkyl, alkoxy, haloalkoxy, NO.sub.2, amino, alkyl substituted amino, or acyl substituted amino; n is 0 to 5; Z is cyano, amino, alkylamino, dialkylamino, --NHCO.sub.2 alkyl, alkoxy, alkylthio, alkylsulfonyl, alkenyl, alkynyl, phenyl or substituted phenyl; and Q is hydrogen, halogen, alkyl, alkoxy, haloalkoxy, nitro, amino, haloalkyl, alkythio, alkylsulfonyl, phenyl, substituted phenyl or phenoxy; or a 5 or 6 membered aromatic heterocycle having the formula ##STR2## in which "m" is 0 or 1; A' is O, S, or NR.sup.
    Type: Grant
    Filed: June 19, 1990
    Date of Patent: September 22, 1992
    Assignee: FMC Corporation
    Inventors: John A. Dixson, Natesan Murugesan, Keith D. Barnes
  • Patent number: 5138058
    Abstract: Pyrimidine derivatives of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4 and R.sup.5 have the indicated meanings, the salts thereof, and a process for the preparation thereof are described. Because of their sorbitol-accumulating activity, they are suitable as a tool in a pharmacological screening model for aldose reductase inhibitors.
    Type: Grant
    Filed: February 20, 1990
    Date of Patent: August 11, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Karl Geisen, Hans-Jochen Lang, Hildegard Nimmesgern, Klaus Weidmann
  • Patent number: 5129941
    Abstract: Sulfonylureas of the formula ##STR1## where A is a bond or a C.sub.1 -C.sub.10 -hydrocarbon radical,R.sup.1 is an optionally unsaturated hydrocarbon radical which is optionally substituted by halogen, optionally unsaturated alkoxy, alkylthio, alkylsulfonyl or alkylsulfinyl, cycloalkyl, optionally substituted phenyl or a heterocycle, or is optionally substituted phenyl, NRR' with R and R' being alkyl, alkoxy or alkylene (cyclic with N),Y is S, SO or SO.sub.2,R.sup.1 is optionally unsaturated alkoxy which is optionally substituted, or is cycloalkoxy, cycloalkenyloxy, cyclopropylmethyloxy, epoxypropyloxy, furfuryloxy, tetrahydrofurfuryloxy or optionally substituted phenoxyalkoxy or phenoxy,R.sup.3 is alkyl which is optionally unsaturated, or is alkoxy,R.sup.4 is optionally substituted pyrimidinyl, pyrimidinylmethyl, pyrimidinyl with a fused-on cyclopentane, oxolane, oxolene, oxane, pyridine or pyrazine ring or purinyl or triazolyl, andZ is O or S,have herbicidal and/or plant-growth-regulatory properties.
    Type: Grant
    Filed: July 17, 1990
    Date of Patent: July 14, 1992
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heinz-Josef Loher, Lothar Willms, Michael Frey, Klaus Bauer, Hermann Bierigner
  • Patent number: 5126352
    Abstract: Novel polycyclic quinoline, naphthyridine and pyrazinopyridine derivatives are disclosed which are useful for treatment allergic reactions, inflammation, peptic ulcers, hypertension, and hyperproliferative skin diseases and for suppressing the immune response in mammals. Methods for preparing said compounds are also disclosed.
    Type: Grant
    Filed: August 31, 1990
    Date of Patent: June 30, 1992
    Assignee: Schering Corporation
    Inventors: Ashit K. Ganguly, Richard J. Friary, John H. Schwerdt, Marvin I. Siegel, Sidney R. Smith, Vera A. Seidl, Edmund J. Sybertz
  • Patent number: 5126448
    Abstract: This invention relates to novel pyridine derivatives and 1,2,3,4-tetrahydropyridine derivatives shown by following general formula (I) or (II) and salts thereof which are useful as psychotropic medicaments: ##STR1## wherein A is S or O; R.sub.1 represents an unsubstituted or substituted alkoxy, amino, hydrazino, or 6- or 7-membered heterocyclic group having one or two nitrogen atoms with the proviso that R.sub.1 is not an alkoxy group in formula (I); R.sub.2 and R.sub.3 each represents a hydrogen atom or an unsubstituted or substituted alkyl, aryl, alkenyl, acyl, arylcarbonyl group; and m and n each represents an integer of from 0 to 4.
    Type: Grant
    Filed: September 29, 1989
    Date of Patent: June 30, 1992
    Assignee: Asahi Kasei Kogyo K.K.
    Inventors: Showa Ueki, Hiromu Kawakubo, Katsuya Okazaki, Tadashi Nagatani
  • Patent number: 5124333
    Abstract: An aminopyrimidine compound of the formula: ##STR1## wherein R.sup.1 represents a hydrogen atom, an alkyl group, a cycloalkyl group or a halogen atom;R.sup.2 and R.sup.3 each represent an alkyl group or a halogen atom, or R.sup.2 and R.sup.3 represent a saturated or unsaturated 5- or 6-membered ring;R.sup.4 represents a hydrogen atom or --CONR.sup.6 R.sup.7, where R.sup.6 and R.sup.7 represent an unsaturated 5-membered ring; andR.sup.5 represents ##STR2## where m represents an integer of 1 to 10; m' represents an integer of 1 to 15;n represents an integer of 0, 1 or 2;R.sup.8 represents a hydrogen atom, an alkyl group or a cycloalkyl group;R.sup.9 represents an alkyl group, an alkenyl group, an alkynyl group, a substituted or unsubstituted phenyl group, a substituted or unsubstituted aralkyl group or an alkyl group,and acid addition salts thereof. Such compound is useful for combatting insects, acarids, nematodes and fungus.
    Type: Grant
    Filed: July 26, 1990
    Date of Patent: June 23, 1992
    Assignee: Ube Industries, Ltd.
    Inventors: Tokio Obata, Katsutoshi Fujii, Isamu Narita, Shoji Shikita
  • Patent number: 5120843
    Abstract: The aromatic amines (I), alkyl amines (II), bicyclic amines (III). ##STR1## cycloalkyl amines (IV), aromatic bicyclic amines (V), hydroquinone amines (VI), quinone amines (VII), amino-ethers (VIII) and bicyclic amino ethers (IX) are useful as pharmaceutical agents for treating a number of conditions including spinal trauma, mild and/or moderate to severe head injury, etc. Also disclosed is a method of treatment using the 3,4-dihydrobenzopyrans (XI).
    Type: Grant
    Filed: October 23, 1989
    Date of Patent: June 9, 1992
    Assignee: Upjohn
    Inventors: John M. McCall, Donald E. Ayer, E. Jon Jacobsen, Frederick J. VanDoornik, John R. Palmer