Halogen Or Nitrogen Attached Directly To Diazine Ring Carbon By Nonionic Bonding Patents (Class 544/356)
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Patent number: 4977155Abstract: 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: GrantFiled: June 22, 1989Date of Patent: December 11, 1990Assignee: A/S FerrosanInventors: Poul Jacobsen, Flemming E. Nielsen, Tage Honore, Jorgen Drejer
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Patent number: 4968681Abstract: 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: GrantFiled: November 15, 1988Date of Patent: November 6, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt
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Patent number: 4943576Abstract: 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: GrantFiled: April 22, 1988Date of Patent: July 24, 1990Assignee: Hoechst AktiengesellschaftInventors: Heiner Glombik, Roland Utz, Hans-Jochen Lang, Karl Geisen, Friedrich E. Beyhl
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Patent number: 4942234Abstract: 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: GrantFiled: February 28, 1989Date of Patent: July 17, 1990Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Guy A. Schiehser, Usha R. Patel
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Patent number: 4937255Abstract: 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: GrantFiled: March 16, 1989Date of Patent: June 26, 1990Assignee: Bayer AktiengesellschaftInventors: Walter Hubsch, Rolf Angerbauer, Peter Fey, Hilmar Bischoff, Dieter Petzinna, Delf Schmidt, Gunter Thomas
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Patent number: 4925861Abstract: 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: GrantFiled: April 13, 1988Date of Patent: May 15, 1990Assignee: Mitsubishi Kasei CorporationInventors: Yoshio Hayashi, Oguri Tomei, Masaki Shinoda, Kazuo Takahashi, Munehiro Hashimoto
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Patent number: 4902800Abstract: 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: GrantFiled: August 17, 1988Date of Patent: February 20, 1990Assignee: American Home Products CorporationInventor: Jerauld S. Skotnicki
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Patent number: 4863945Abstract: 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: GrantFiled: December 10, 1987Date of Patent: September 5, 1989Assignee: Boehringer Mannheim GmbHInventors: Walter-Gunar Friebe, Alfred Mertens, Klaus Strein, Erwin Boehm
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Patent number: 4853400Abstract: 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: GrantFiled: May 16, 1988Date of Patent: August 1, 1989Assignee: Schering Agrochemicals LimitedInventors: John H. Parsons, Russell G. Hunt, Susan E. Leach, Anthony D. Buss, David E. Green, Michael Mellor, Albert Percival
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Patent number: 4833142Abstract: Blood-pressure lowering compounds having a structure as shown in the accompanying formula sheets.Type: GrantFiled: November 9, 1987Date of Patent: May 23, 1989Assignee: Duphar International Research B.V.Inventors: Jan Hartog, Wouter Wouters, Lneke van Wijngaarden
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Patent number: 4833249Abstract: 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: GrantFiled: March 5, 1987Date of Patent: May 23, 1989Assignee: American Home Products CorporationInventors: Magid A. Abou-Gharbia, Guy A. Schiehser, Usha R. Patel
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Patent number: 4812161Abstract: Thia-diazole derivatives having the following partial structural formula had selective herbicidal activity on some crops.Type: GrantFiled: July 29, 1985Date of Patent: March 14, 1989Assignee: Nippon Soda Co., Ltd.Inventors: Kenji Hagiwara, Hisao Ishikawa, Hideo Hosaka, Hideo Inaba
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Patent number: 4790868Abstract: 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: GrantFiled: January 7, 1987Date of Patent: December 13, 1988Assignee: PPG Industries, Inc.Inventor: Donald R. Nielsen
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Patent number: 4772613Abstract: 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: GrantFiled: May 26, 1987Date of Patent: September 20, 1988Assignee: Schering Agrochemicals Ltd.Inventors: John H. Parsons, Russell G. Hunt, Susan E. Leach, Anthony D. Buss, David E. Green, Michael Mellor, Albert Percival
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Patent number: 4750931Abstract: 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: GrantFiled: October 15, 1985Date of Patent: June 14, 1988Assignee: The Dow Chemical CompanyInventor: Richard B. Rogers
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Patent number: 4751305Abstract: 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: GrantFiled: May 7, 1987Date of Patent: June 14, 1988Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gillman
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Patent number: 4748246Abstract: 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: GrantFiled: May 7, 1987Date of Patent: May 31, 1988Assignee: American Home Products CorporationInventors: Jerauld S. Skotnicki, Steven C. Gilman, Bruce A. Steinbaugh, John H. Musser
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Patent number: 4642310Abstract: 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: GrantFiled: March 28, 1985Date of Patent: February 10, 1987Assignee: Bayer AktiengesellschaftInventors: Siegfried Goldmann, Matthias Schramm, Gunter Thomas, Rainer Gross
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Patent number: 4636562Abstract: 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: GrantFiled: November 1, 1984Date of Patent: January 13, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Richard F. Davis
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Patent number: 4623725Abstract: 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: GrantFiled: November 8, 1985Date of Patent: November 18, 1986Assignee: Pfizer Inc.Inventors: Saul B. Kadin, Reinhard Sarges
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Patent number: 4507294Abstract: There are disclosed herein certain substituted imidazo[1,2-a]pyrazine compounds which are useful in the treatment of peptic ulcer diseases.Type: GrantFiled: March 8, 1982Date of Patent: March 26, 1985Assignee: Schering Corp.Inventors: James A. Bristol, Raymond G. Lovey
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Patent number: 4474784Abstract: 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: GrantFiled: March 1, 1982Date of Patent: October 2, 1984Assignee: Roussel UclafInventors: Alan C. Barnes, David A. Rowlands
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Patent number: 4439606Abstract: This disclosure describes 4-aryl, -heteroaryl and -heteroarylmethyl-1-piperazinecarbonyl compounds which are capable of ameliorating atherosclerosis in mammals.Type: GrantFiled: May 6, 1982Date of Patent: March 27, 1984Assignee: American Cyanamid CompanyInventors: Mila T. Du, Robert G. Shepherd
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Patent number: 4358307Abstract: 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: GrantFiled: September 8, 1980Date of Patent: November 9, 1982Assignee: ICI Australia LimitedInventors: Alexander Serban, Keith G. Watson, Graeme J. Farquharson
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Patent number: 4352804Abstract: 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: GrantFiled: July 11, 1979Date of Patent: October 5, 1982Assignee: ACF Chemiefarma NVInventor: Jacob A. van Zorge
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Patent number: 4343942Abstract: 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: GrantFiled: December 9, 1969Date of Patent: August 10, 1982Assignee: Research CorporationInventors: Costas H. Issidorides, Makhluf J. Haddadin
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Patent number: 4338316Abstract: 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: GrantFiled: September 26, 1979Date of Patent: July 6, 1982Assignee: Imperial Chemical Industries LimitedInventor: Peter R. Marsham
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Patent number: 4328228Abstract: 2,3-Dihalo-6-quinoxalinesulfonyl fluoride compounds are useful as fungicides and insecticides.Type: GrantFiled: July 8, 1980Date of Patent: May 4, 1982Assignee: E. I. Du Pont de Nemours and CompanyInventor: John B. Adams, Jr.
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Patent number: 4309182Abstract: 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: GrantFiled: November 19, 1980Date of Patent: January 5, 1982Assignee: Bayer AktiengesellschaftInventors: Jochen Koll, Volker Paulat, Reinhold Hornle, Hans-Heinz Molls, Konrad Nonn
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Patent number: 4309183Abstract: 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: GrantFiled: November 19, 1980Date of Patent: January 5, 1982Assignee: Bayer AktiengesellschaftInventors: Jochen Koll, Volker Paulat, Reinhold Hornle, Hans-Heinz Molls, Konrad Nonn
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Patent number: 4294772Abstract: 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: GrantFiled: August 20, 1979Date of Patent: October 13, 1981Assignee: Ciba-Geigy CorporationInventor: Henry Martin
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Patent number: 4258044Abstract: Haloalkyl polyhaloquinoxaline sulfonate compounds of the formula ##STR1## are useful as fungicides.Type: GrantFiled: May 25, 1979Date of Patent: March 24, 1981Assignee: E. I. Du Pont de Nemours and CompanyInventor: Thomas S. Woods
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Patent number: 4256882Abstract: 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: GrantFiled: August 3, 1976Date of Patent: March 17, 1981Assignee: Bayer AktiengesellschaftInventors: Adolf Friedrich, Horst Harnisch, Roderich Raue
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Patent number: 4200748Abstract: 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: GrantFiled: January 22, 1979Date of Patent: April 29, 1980Assignee: American Cyanamid CompanyInventors: William B. Wright, Jr., Andrew S. Tomcufcik
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Patent number: 4189580Abstract: 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: GrantFiled: August 10, 1978Date of Patent: February 19, 1980Assignee: Bayer AktiengesellschaftInventor: Kurt Findeisen
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Patent number: 4150230Abstract: 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: GrantFiled: March 23, 1978Date of Patent: April 17, 1979Assignee: Sandoz Ltd.Inventors: Roland Mislin, Wolfgang Schoenauer, Karl U. Steiner
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Patent number: 4138243Abstract: 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: GrantFiled: August 8, 1977Date of Patent: February 6, 1979Assignee: Ciba-Geigy CorporationInventors: Beat Bohner, Marcus Baumann
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Patent number: 4133956Abstract: 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: GrantFiled: July 27, 1977Date of Patent: January 9, 1979Assignee: Eli Lilly and CompanyInventors: Riaz F. Abdulla, Norman H. Terando
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Patent number: 4125724Abstract: 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: GrantFiled: October 6, 1977Date of Patent: November 14, 1978Assignee: Bristol-Myers CompanyInventor: Henry G. Howell
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Patent number: 4101547Abstract: 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: GrantFiled: June 25, 1976Date of Patent: July 18, 1978Assignee: Sandoz Ltd.Inventors: Roland Mislin, Wolfgang Schoenauer, Karl Ulrich Steiner
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Patent number: 4096152Abstract: 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: GrantFiled: October 6, 1975Date of Patent: June 20, 1978Assignee: Bayer AktiengesellschaftInventors: Eike Moller, Karl Meng, Egbert Wehinger, Harald Horstmann
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Patent number: 4093712Abstract: 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: GrantFiled: January 19, 1977Date of Patent: June 6, 1978Assignees: Mitsubishi Chemical Industries Limited, Shosuke OkamotoInventors: Shosuke Okamoto, Akiko Hijikata, Ryoji Kikumoto, Yoshikuno Tamao, Kazuo Ohkubo, Tohru Tezuka, Shinji Tonomura
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Patent number: 4089858Abstract: 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: GrantFiled: September 17, 1975Date of Patent: May 16, 1978Assignee: 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