Halogen Or Nitrogen Attached Directly To Diazine Ring Carbon By Nonionic Bonding Patents (Class 544/356)
  • Patent number: 4977155
    Abstract: Heterocyclic dihydroxyquinoxaline compounds having the formula ##STR1## wherein R.sup.2 is hydrogen, NO.sub.2, NH.sub.2, CN, halogen, or SO.sub.2 NH.sub.2 ; --X--Y--Z-- is selected from --N.dbd.N--N.sup.3 --,--NR.sup.3 --N.dbd.N--,.dbd.N--NR.sup.3 --N.dbd., wherein R.sup.3 is hydrogen, lower alkyl, or CF.sub.3.The invention also relates to a method of preparing the compounds, pharmaceutical compositions thereof, and their use.The compounds are useful in the treatment of indications caused by hyperactivity of the excitatory neurotransmitters.
    Type: Grant
    Filed: June 22, 1989
    Date of Patent: December 11, 1990
    Assignee: A/S Ferrosan
    Inventors: Poul Jacobsen, Flemming E. Nielsen, Tage Honore, Jorgen Drejer
  • Patent number: 4968681
    Abstract: Substituted hydroxylamines of the formula ##STR1## in which R.sup.1 stands for an aromatic or heterocyclic radical, are especially useful in the treatment of hyperlipoproteinaemia, lipoproteinaemia and atherosclerosis.
    Type: Grant
    Filed: November 15, 1988
    Date of Patent: November 6, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
  • Patent number: 4943576
    Abstract: Substituted quinoxalyl-imidazolidine-2,4-diones, processes for their preparation, their use as medicaments and pharmaceutical preparations 5-Quinoxalyl-imidazolidine-2,4-diones 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 meanings given, and physiologically tolerated salts thereof and processes for their preparation are described. The compounds inhibit aldose reductase and can be used as medicaments.
    Type: Grant
    Filed: April 22, 1988
    Date of Patent: July 24, 1990
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Heiner Glombik, Roland Utz, Hans-Jochen Lang, Karl Geisen, Friedrich E. Beyhl
  • Patent number: 4942234
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; or ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is ##STR4## X is lower alkylene, vinylene, O or NH; m is 1-5;n is 0-4;p is 1-4;q is 1-2;and the pharmaceutically acceptable salts thereof, and their use as antipsychotic/anxiolytic agents having a low liability for extrapyramidal side effects.
    Type: Grant
    Filed: February 28, 1989
    Date of Patent: July 17, 1990
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Guy A. Schiehser, Usha R. Patel
  • Patent number: 4937255
    Abstract: For inhibiting 3-hydroxy-3-methylglutaryl coenzyme A and cholesterol biosynthesis, the novel disubstituted pyrroles of the formula ##STR1## in which R.sup.1 is aryl or heteroaryl,R.sup.2 is cycloalkyl or optionally substituted alkyl,R.sup.3 is hydrogen or cycloalkyl, or optionally substituted alkyl, aryl or heteroaryl,X is --CH.sub.2 --CH.sub.2 -- or --CH.dbd.CH--,A is ##STR2## R.sup.6 is hydrogen or alkyl, and R.sup.7 is hydrogen, a cation or alkyl, aryl or aralkyl.
    Type: Grant
    Filed: March 16, 1989
    Date of Patent: June 26, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
  • Patent number: 4925861
    Abstract: According to the present invention, there are provided novel carboxystyrene derivatives of the general formula (I): wherein the symbols are as defined hereinabove. Also provided herein are leukotriene antagonists and phospholipase inhibitors containing the carboxystyrene derivative or pharmaceutically acceptable salt thereof as an effective ingredient.
    Type: Grant
    Filed: April 13, 1988
    Date of Patent: May 15, 1990
    Assignee: Mitsubishi Kasei Corporation
    Inventors: Yoshio Hayashi, Oguri Tomei, Masaki Shinoda, Kazuo Takahashi, Munehiro Hashimoto
  • Patent number: 4902800
    Abstract: There are disclosed compounds of the formula: ##STR1## wherein R is phenyl, naphthyl, pyridyl, quinolinyl, pyrazinyl, pyrimidinyl, quinoxalinyl quinazolinyl or any of the foregoing substituted with halo, lower alkyl, lower alkenyl, lower alkoxy, carboxy, lower alkoxycarbonyl, hydroxy, amino, mono- or diloweralkylamino, mercapto, lower alkylthio, lower alkylsulfonyl, cyano, nitro or trifluoromethyl; which, by virtue of their ability to inhibit interleukin 1, are of use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction.
    Type: Grant
    Filed: August 17, 1988
    Date of Patent: February 20, 1990
    Assignee: American Home Products Corporation
    Inventor: Jerauld S. Skotnicki
  • Patent number: 4863945
    Abstract: Pyrrolobenzimidazoles of the formula: ##STR1## are useful for treatment of heart and circulatory diseases. R.sub.1 is substituted phenyl; or optionally substituted naphthyl or a five- or six-membered heterocyclic group which can be condensed with a phenyl ring to form a bicyclic radical. R.sub.2 is hydrogen, alkyl, alkenyl or cycloalkenyl; R.sub.3 is alkyl, alkenyl or hydroxyalkyl or with R.sub.2 together forms cycloakylene; or R.sub.2 and R.sub.3 together form alkylidene or cycloalkylidene. R.sub.4 is hydrogen or lower alkanoyl. X is a valency bond, alkylene, vinylene, imino or carbonylamino. T stands for two hydrogen atoms. When X is a valency bond, R.sub.1 can also be hydrogen, hydrocarbyl which may also contain oxygen, amino, sulfur, carbonyl and sulfonyl groups. When X is imino or carbonylamino or when R.sub.1 is a bicyclic radical, T can also be oxygen. The compounds also include the tautomers and physiologically acceptable salts with inorganic and organic acids.
    Type: Grant
    Filed: December 10, 1987
    Date of Patent: September 5, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Walter-Gunar Friebe, Alfred Mertens, Klaus Strein, Erwin Boehm
  • Patent number: 4853400
    Abstract: Compounds of any one of formulae I-VII ##STR1## where is a single or double bond;A is oxygen or sulphurR.sup.1 is aryl;R.sup.2 is 1-imidazolyl or 1,2,4-triazol-1-yl andR.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are each hydrogen, halo, alkyl or alkoxy, have fungicidal activity.
    Type: Grant
    Filed: May 16, 1988
    Date of Patent: August 1, 1989
    Assignee: Schering Agrochemicals Limited
    Inventors: John H. Parsons, Russell G. Hunt, Susan E. Leach, Anthony D. Buss, David E. Green, Michael Mellor, Albert Percival
  • Patent number: 4833142
    Abstract: Blood-pressure lowering compounds having a structure as shown in the accompanying formula sheets.
    Type: Grant
    Filed: November 9, 1987
    Date of Patent: May 23, 1989
    Assignee: Duphar International Research B.V.
    Inventors: Jan Hartog, Wouter Wouters, Lneke van Wijngaarden
  • Patent number: 4833249
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are each, independently, hydrogen, lower alkyl, aryl or halo, or R.sup.1 and R.sup.2 taken together represent ##STR2## where the dotted lines represent optional double bonds; R.sup.3, R.sup.4 and R.sup.5 are each, independently, hydrogen, lower alkyl, aryl or halo;R.sup.6 is 2-pyridinyl, 2-pyrazinyl, 2-quinolyl, 2-quinoxalinyl or any of the foregoing R.sup.6 moieties substituted by lower alkyl, lower alkoxy, trifluoromethyl, cyano, nitro or halo; orR.sup.6 is ##STR3## wherein R.sup.7 is phenyl, 2-pyridinyl, 2-pyrimidinyl, 3-pyridazinyl or 2-pyrazinyl or any of the foregoing R.sup.7 moieties substituted by lower alkyl, lower alkoxy, halo, cyano, trifluoromethyl or nitro;Z is --(CH.sub.2).sub.
    Type: Grant
    Filed: March 5, 1987
    Date of Patent: May 23, 1989
    Assignee: American Home Products Corporation
    Inventors: Magid A. Abou-Gharbia, Guy A. Schiehser, Usha R. Patel
  • Patent number: 4812161
    Abstract: Thia-diazole derivatives having the following partial structural formula had selective herbicidal activity on some crops.
    Type: Grant
    Filed: July 29, 1985
    Date of Patent: March 14, 1989
    Assignee: Nippon Soda Co., Ltd.
    Inventors: Kenji Hagiwara, Hisao Ishikawa, Hideo Hosaka, Hideo Inaba
  • Patent number: 4790868
    Abstract: This invention relates to herbicidally active substituted benzoxazolone (or benzthiazolone) compounds and to the use of such compounds to control the growth of noxious plants, i.e., weeds.
    Type: Grant
    Filed: January 7, 1987
    Date of Patent: December 13, 1988
    Assignee: PPG Industries, Inc.
    Inventor: Donald R. Nielsen
  • Patent number: 4772613
    Abstract: Compounds of any of one of formulae I-VII ##STR1## where is a single or double bond;A is oxygen or sulphur;R.sup.1 is aryl;R.sup.2 is 1-imidazolyl or 1,2,4-triazol-1-yl; andR.sup.3, R.sup.4, R.sup.5 and R.sup.6, which may be the same or different, are each hydrogen, halo, alkyl or alkoxy, have fungicidal activity.
    Type: Grant
    Filed: May 26, 1987
    Date of Patent: September 20, 1988
    Assignee: Schering Agrochemicals Ltd.
    Inventors: John H. Parsons, Russell G. Hunt, Susan E. Leach, Anthony D. Buss, David E. Green, Michael Mellor, Albert Percival
  • Patent number: 4750931
    Abstract: Certain novel fluorophenoxy compounds, principally aryloxyfluorophenoxyalkanoic acids and derivatives thereof, are described. More specifically, these novel compounds bear 1 to 4 fluorine substituents on the phenyl ring. These novel compounds exhibit surprising preemergent and postemergent activity when used according to the method of the invention in the control of grassy weeds.
    Type: Grant
    Filed: October 15, 1985
    Date of Patent: June 14, 1988
    Assignee: The Dow Chemical Company
    Inventor: Richard B. Rogers
  • Patent number: 4751305
    Abstract: There are disclosed compounds of the formula ##STR1## wherein R.sup.1 is pyridl, quinolinyl, pyrazinyl, pyridinyl, pyridazinyl, pyrimidinyl, quinoxalinyl, quinazolinyl or any of the foregoing substituted with halo, lower alkyl, lower alkyl carbonyl, benzoyl, carboxy, lower alkoxycarbonyl, OR.sup.2, N(R.sup.2).sub.2, CON(R.sup.2).sub.2, SO.sub.3 R.sup.2, SO.sub.2 N(R.sup.2).sub.2, phenylsulfonyl, lower alkylsulfonyl, cyano, nitro or trifluoromethyl;R.sup.2 is hydrogen, lower alkyl or phenyl;R.sup.3 is halo, morpholino, 4-methylpiperazino, R.sup.4 NNHR.sup.5, NR.sup.4 R.sup.5, OR.sup.5, SR.sup.5, R.sup.4 NCH.sub.2 CH.sub.2 OCH.sub.3, SCH.sub.2 CH.sub.2 CH.sub.2 NH.sub.2, or ##STR2## R.sup.4 is hydrogen or lower alkyl; R.sup.5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkylor phenyl; andR.sup.6 and R.sup.
    Type: Grant
    Filed: May 7, 1987
    Date of Patent: June 14, 1988
    Assignee: American Home Products Corporation
    Inventors: Jerauld S. Skotnicki, Steven C. Gillman
  • Patent number: 4748246
    Abstract: There are disclosed compounds of the formula ##STR1## wherein the various substituents are defined hereinbelow, and, by virtue of their ability to inhibit interleukin 1, their use as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction.
    Type: Grant
    Filed: May 7, 1987
    Date of Patent: May 31, 1988
    Assignee: American Home Products Corporation
    Inventors: Jerauld S. Skotnicki, Steven C. Gilman, Bruce A. Steinbaugh, John H. Musser
  • Patent number: 4642310
    Abstract: Tetrahydrothienopyridines of the formula ##STR1## in which R is optionally substituted aryl or heterocyclyl,R.sup.1 is an organic radical, andR.sup.2, R.sup.3 and R.sup.4 each independently is hydrogen or an organic radical, or pharmaceutically acceptable salts thereof, which are coronary active, hypotensive, anti-diabetic and salt balance restoring.
    Type: Grant
    Filed: March 28, 1985
    Date of Patent: February 10, 1987
    Assignee: Bayer Aktiengesellschaft
    Inventors: Siegfried Goldmann, Matthias Schramm, Gunter Thomas, Rainer Gross
  • Patent number: 4636562
    Abstract: A process for the preparation of 2-chloro-6-haloquinoxaline compounds from the corresponding 4-halo-2-nitroaniline utilizing four reaction steps with generally compatible solvents and reagents with volatile by-products to minimize the isolation and purification of intermediates has been developed.
    Type: Grant
    Filed: November 1, 1984
    Date of Patent: January 13, 1987
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Richard F. Davis
  • Patent number: 4623725
    Abstract: A series of novel [1,2,4]triazolo[4,3-a]quinoxaline-4-amine derivatives wherein the amine group is optionally substituted with lower alkyl, phenylalkyl having up to three carbon atoms in the alkyl moiety or alkanoyl having from two to five carbon atoms, or the amine group alternatively completes a piperazino ring, the quinoxaline ring is optionally substituted with fluorine, chlorine, bromine or methoxy, and the triazolo ring is optionally substituted with lower alkyl, lower perfluoroalkyl or phenyl are disclosed. These novel compounds are useful for treatment of symptoms associated with depression. Also disclosed are pharmaceutical compositions containing the novel compounds of this invention.
    Type: Grant
    Filed: November 8, 1985
    Date of Patent: November 18, 1986
    Assignee: Pfizer Inc.
    Inventors: Saul B. Kadin, Reinhard Sarges
  • Patent number: 4507294
    Abstract: There are disclosed herein certain substituted imidazo[1,2-a]pyrazine compounds which are useful in the treatment of peptic ulcer diseases.
    Type: Grant
    Filed: March 8, 1982
    Date of Patent: March 26, 1985
    Assignee: Schering Corp.
    Inventors: James A. Bristol, Raymond G. Lovey
  • Patent number: 4474784
    Abstract: Novel compounds of the formula ##STR1## wherein A is selected from the group consisting of nitrogen and .dbd.CH--, G is selected from the group consisting of --0--, ##STR2## Z is selected from the group consisting of hydrogen and alkyl of 1 to 5 carbon atoms or taken with Y forms a carbon-nitrogen or carbon-carbon bond, Z' is selected from the group consisting of hydrogen and halogen, Y is hydrogen, or taken with Z is a carbon-nitrogen or carbon-carbon bond or taken with X is .dbd.0 and X is hydrogen or taken with Y is .dbd.0, R is selected from the group consisting of hydroxymethyl, formyl, tetrazol-5-yl, N-(tetrazol-5-yl) carbamoyl, aminomethyl and carbamoyl, R.sub.1 is selected from the group consisting of hydrogen, halogen and alkoxy of 1 to 5 carbon atoms and its non-toxic, pharmaceutically acceptable acid addition salts having anti-allergic activity and their preparation.
    Type: Grant
    Filed: March 1, 1982
    Date of Patent: October 2, 1984
    Assignee: Roussel Uclaf
    Inventors: Alan C. Barnes, David A. Rowlands
  • Patent number: 4439606
    Abstract: This disclosure describes 4-aryl, -heteroaryl and -heteroarylmethyl-1-piperazinecarbonyl compounds which are capable of ameliorating atherosclerosis in mammals.
    Type: Grant
    Filed: May 6, 1982
    Date of Patent: March 27, 1984
    Assignee: American Cyanamid Company
    Inventors: Mila T. Du, Robert G. Shepherd
  • Patent number: 4358307
    Abstract: The invention concerns novel compounds of the formula I ##STR1## The compounds are herbicides and in further embodiments the invention provides processes for the preparation of compounds of formula I, intermediates useful in the preparation of compounds of formula I, herbicidal composition containing as active ingredient a compound of formula I, and processes for severely damaging or killing unwanted plants by applying to the plants or to the growth medium of the plants an effective amount of a compound of formula I.
    Type: Grant
    Filed: September 8, 1980
    Date of Patent: November 9, 1982
    Assignee: ICI Australia Limited
    Inventors: Alexander Serban, Keith G. Watson, Graeme J. Farquharson
  • Patent number: 4352804
    Abstract: Oxime ether derivatives of the formula (I): ##STR1## wherein Het is a monocyclic heteroaromatic group containing two hetero atoms at least one of which is nitrogen, or a bicyclic heteroaromatic group containing one or two hetero atoms at least one of which is nitrogen, Ar is a phenyl or a 5- or 6-membered monocyclic heteroaromatic group, and R is an alkyl, alkenyl, alkynyl, cyanoalkyl, carbamidoalkyl or aminoalkyl group, or N-oxides thereof, have anti-ulcer activity in the gastro-intestinal tract of mammals.
    Type: Grant
    Filed: July 11, 1979
    Date of Patent: October 5, 1982
    Assignee: ACF Chemiefarma NV
    Inventor: Jacob A. van Zorge
  • Patent number: 4343942
    Abstract: The synthesis of quinoxaline and benzimidazole-N-oxides and of ester and amide derivatives of 3-hydroxy-2-quinoxalinecarboxylic acid by a novel process consisting of the reaction between a benzofuroxan and an activated methylene-containing compound under basic conditions.
    Type: Grant
    Filed: December 9, 1969
    Date of Patent: August 10, 1982
    Assignee: Research Corporation
    Inventors: Costas H. Issidorides, Makhluf J. Haddadin
  • Patent number: 4338316
    Abstract: The disclosure relates to 9.beta.-aryloxy prostane derivatives, for example 16-(3-chlorophenoxy)-11.alpha.,15.alpha.-dihydroxy-16-methyl-9.beta.-pheno xy-18,19,20-trinor-5-cis,13-trans-prostadienoic acid, which possess high activity as abortifacients, cervical softeners, inducers of parturition or inhibitors of gastric acid production in mammals. These properties are typical of prostaglandin analogues of the E series, but chemically the new 9.beta.-aryloxy prostane derivatives are prostaglandin F series analogues and are therefore more stable than the E series analogues previously used for the above purposes. The new derivatives are manufactured by known analogy processes, and are formulated in conventional manner.
    Type: Grant
    Filed: September 26, 1979
    Date of Patent: July 6, 1982
    Assignee: Imperial Chemical Industries Limited
    Inventor: Peter R. Marsham
  • Patent number: 4328228
    Abstract: 2,3-Dihalo-6-quinoxalinesulfonyl fluoride compounds are useful as fungicides and insecticides.
    Type: Grant
    Filed: July 8, 1980
    Date of Patent: May 4, 1982
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: John B. Adams, Jr.
  • Patent number: 4309182
    Abstract: Liquid finished formulations which are stable to storage and hydrolysis and are based on the lyotropic liquid crystal aqueous phase of the dyestuff of the formula ##STR1## which is present in water in a concentration of 23-35% at room temperature, are outstandingly suitable for the preparation of dyebaths and printing pastes for dyeing cotton, wool, regenerated cellulose, paper and leather.
    Type: Grant
    Filed: November 19, 1980
    Date of Patent: January 5, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jochen Koll, Volker Paulat, Reinhold Hornle, Hans-Heinz Molls, Konrad Nonn
  • Patent number: 4309183
    Abstract: Liquid finished formulations which are stable to storage and hydrolysis and are based on the lyotropic liquid crystal aqueous phase of the dyestuff of the formula ##STR1## in water in a concentration of 12-35% at room temperature are outstandingly suitable for the preparation of dyebaths and printing pastes for dyeing cotton, wool, regenerated cellulose, paper and leather.
    Type: Grant
    Filed: November 19, 1980
    Date of Patent: January 5, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jochen Koll, Volker Paulat, Reinhold Hornle, Hans-Heinz Molls, Konrad Nonn
  • Patent number: 4294772
    Abstract: Tin-containing oxime derivatives of the formula ##STR1## wherein n is 0, 1 or 2,m is 0 or 1,Ar is an optionally substituted phenyl radical or an optionally substituted naphthyl radical, or when m is 0, Ar may also be an ester group,X is hydrogen, --CN, halogen, lower alkyl, lower alkanoyl, --COOH, a carboxylic acid ester radical, a carbamoyl radical andR.sub.8, R.sub.9 and R.sub.10, each independently of the other, are alkyl, aryl, aralkyl or C.sub.3 -C.sub.7 cycloalkyl, are suitable for protecting cultivated plants from the phytotoxic action of aggressive agrochemicals, in particular herbicides preferred are compounds of the above formula in whichAr is alkylphenyl, alkoxyphenyl, halophenyl, naphthyl or amido,X is cyano or a carboxylic acid ester radical, andR.sub.8, R.sub.9 and R.sub.10 are the same and are C.sub.1 -C.sub.4 alkyl, benzyl or phenyl.
    Type: Grant
    Filed: August 20, 1979
    Date of Patent: October 13, 1981
    Assignee: Ciba-Geigy Corporation
    Inventor: Henry Martin
  • Patent number: 4258044
    Abstract: Haloalkyl polyhaloquinoxaline sulfonate compounds of the formula ##STR1## are useful as fungicides.
    Type: Grant
    Filed: May 25, 1979
    Date of Patent: March 24, 1981
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Thomas S. Woods
  • Patent number: 4256882
    Abstract: Reactive dyestuffs which in form of the free acid correspond to the following formula ##STR1## wherein R.sub.1, R.sub.2, W.sub.1, Y, Z, Q, as well as A, B and C have the meaning given in claim 1, and their use for the dyeing and printing of fibre material made of polyamide, for example natural and, in particular, synthetic polyamides, and natural and regenerated cellulose in red and bluish-tinged red fluorescent color.
    Type: Grant
    Filed: August 3, 1976
    Date of Patent: March 17, 1981
    Assignee: Bayer Aktiengesellschaft
    Inventors: Adolf Friedrich, Horst Harnisch, Roderich Raue
  • Patent number: 4200748
    Abstract: This disclosure describes substituted 2,3,3a,4-tetrahydro-1H-pyrrolo[1',2':4,5][1,4]oxazino[2,3-b]quinoxalines and 1,2,3,4,4a,5-hexahydropyrido[1',2':4,5][1,4]oxazino[2,3-b]quinoxalines which possess anxioyltic activity.
    Type: Grant
    Filed: January 22, 1979
    Date of Patent: April 29, 1980
    Assignee: American Cyanamid Company
    Inventors: William B. Wright, Jr., Andrew S. Tomcufcik
  • Patent number: 4189580
    Abstract: A process for the preparation of a nitrile of the formulaR--(CN).sub.n'wherein R represents an optionally substituted alkyl, cycloalkyl or aryl radical or an optionally substituted 5- or 6-membered heterocyclic radical which may additionally be fused with a benzene ring and n' represents 1 to 6 which comprises contacting a carboxylic acid of the formulaR--(COOH).sub.n'wherein R and n' have the meanings given above with cyanogen chloride and/or cyanogen bromide at a temperature in the range of 100.degree. to 300.degree. C.
    Type: Grant
    Filed: August 10, 1978
    Date of Patent: February 19, 1980
    Assignee: Bayer Aktiengesellschaft
    Inventor: Kurt Findeisen
  • Patent number: 4150230
    Abstract: 1,4-Diaminoanthraquinone derivatives containing a halopyrimidinyl or haloquinoxaline-6-carbonyl reactive group are useful as reactive dyestuffs for the dyeing or printing of leather and textile materials.
    Type: Grant
    Filed: March 23, 1978
    Date of Patent: April 17, 1979
    Assignee: Sandoz Ltd.
    Inventors: Roland Mislin, Wolfgang Schoenauer, Karl U. Steiner
  • Patent number: 4138243
    Abstract: The present invention relates to novel 3,4-dimethyl-2-hydroxy-5-oxo-2,5-dihydropyrrole compounds substituted on the nitrogen atom, to processes for producing them, to their use in agriculture for combating animal and plant pests and also for regulating plant growth, and to compositions containing these novel pyrrole compounds.The novel 3,4-dimethyl-2-hydroxy-5-oxo-2,5-dihydropyrrole compounds substituted on the nitrogen atom correspond to the formula ##STR1## where A represents the hydroxyl group, a halogen atom or an O-acyl radical, andR represents an aryl radical, an aralkyl radical, or an heteroaromatic radical which has 5-6 ring members and which is bound by way of a carbon atom.
    Type: Grant
    Filed: August 8, 1977
    Date of Patent: February 6, 1979
    Assignee: Ciba-Geigy Corporation
    Inventors: Beat Bohner, Marcus Baumann
  • Patent number: 4133956
    Abstract: Benzoylureas are prepared from a benzamide, an alkyllithium, a phenyl chloroformate, and an amine. Two reaction sequences are described. The benzoylureas obtained by the process are useful as insecticides.
    Type: Grant
    Filed: July 27, 1977
    Date of Patent: January 9, 1979
    Assignee: Eli Lilly and Company
    Inventors: Riaz F. Abdulla, Norman H. Terando
  • Patent number: 4125724
    Abstract: An improved and novel process is provided for the reduction of isocyanate groups in organic compounds to formamide groups by catalytic hydrogenation with a noble metal catalyst. The process allows preparation of formamides in consistently high yields from all types of isocyanates.
    Type: Grant
    Filed: October 6, 1977
    Date of Patent: November 14, 1978
    Assignee: Bristol-Myers Company
    Inventor: Henry G. Howell
  • Patent number: 4101547
    Abstract: 1,4-Diaminoanthraquinone derivatives containing a halopyrimidinyl or haloquinoxaline-6-carbonyl reactive group are useful as reactive dyestuffs for the dyeing or printing of leather and textile materials.
    Type: Grant
    Filed: June 25, 1976
    Date of Patent: July 18, 1978
    Assignee: Sandoz Ltd.
    Inventors: Roland Mislin, Wolfgang Schoenauer, Karl Ulrich Steiner
  • Patent number: 4096152
    Abstract: Pyrazole derivatives of the formula: ##STR1## and pharmaceutically acceptable nontoxic salts thereof wherein R is hydrogen, trifluoromethyl or alkyl;R.sup.1 is hydrogen or alkyl;R.sup.2 is alkyl;R.sup.3 is mono- or di-substituted aryl, naphthyl, or pyridyl;R.sup.4 is R.sup.5 CO wherein R.sup.5 is alkyl unsubstituted or substituted by 1, 2 or 3 halogen moieties, by alkoxy, or by mono- or dialkylamino; lower alkoxy; dialkylamino; thiophene; phenyl unsubstituted or substituted by 1 or 2 alkyl, trifluoromethyl, alkoxy, nitro or halogen moieties; or a 5- to 7-membered heterocycle unsubstituted or substituted by 1 or 2 halogen, alkyl or nitro moieties; orR.sup.4 is Z--SO.sub.2 wherein Z is alkyl, phenyl or phenyl substituted by 1 or 2 alkyl, halogen, nitro, trifluoromethyl or trifluoromethylsulphonyl moieties; or dichloroquinoxalinyl.The pyrazole derivatives and their salts are useful as diuretics, saluretics and antihypertensives.
    Type: Grant
    Filed: October 6, 1975
    Date of Patent: June 20, 1978
    Assignee: Bayer Aktiengesellschaft
    Inventors: Eike Moller, Karl Meng, Egbert Wehinger, Harald Horstmann
  • Patent number: 4093712
    Abstract: N.sup.2 -arylsulfonyl-L-argininamides and the pharmaceutically acceptable salts thereof have been found to be effective as pharmaceutical agents for the inhibition and suppression of thrombosis in mammals.
    Type: Grant
    Filed: January 19, 1977
    Date of Patent: June 6, 1978
    Assignees: Mitsubishi Chemical Industries Limited, Shosuke Okamoto
    Inventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuno Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
  • Patent number: 4089858
    Abstract: The present invention is concerned with the preparation of chemical intermediates, namely, beta-amino-acrylic acid ester derivatives of nitrogen heterocycles, i.e. pyridine, quinoline, quinoxaline, pyrazine, pyrimidine and the like. Said intermediates are cyclized to form pyrido-pyrimidine type final products possessing analgesic activity.
    Type: Grant
    Filed: September 17, 1975
    Date of Patent: May 16, 1978
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Zoltan Meszaros, Jozsef Knoll, Istvan Hermecz, Piroska Simon, Peter Szentmiklosy, Lelle Vasvari, Agnes Horvath, Gabor Horvath, Peter Dvortsak