Sulfur Attached Indirectly To The Diazine Ring By Nonionic Bonding (e.g., Thiamines, Etc.) Patents (Class 544/327)
-
Patent number: 4791112Abstract: N-heterocyclic-4-piperidyl-amides as analgesics and antagonists of opioids with respect to such undesirable side effects as respiratory depression.Exemplary compounds have the formula ##STR1## in which formula R is a heterocyclic group, and R.sup.1 is a furanyl, thienyl, or lower alkoxy lower alkyl group, and R.sup.2 is a lower alkyl phenyl group.Type: GrantFiled: February 2, 1987Date of Patent: December 13, 1988Assignee: The BOC Group, Inc.Inventors: Jerome R. Bagley, H. Kenneth Spencer
-
Patent number: 4777172Abstract: This invention relates to 2- and 4-pyrimidinylmethylsulphinyl(and thio)benzimidazoles in which the pyrimidyl group is substituted by an optionally substituted amino group. These compounds inhibit exogenously and endogenously stimulated gastric acid secretion.Type: GrantFiled: February 14, 1986Date of Patent: October 11, 1988Assignee: Smith Kline & French Laboratories LimitedInventors: Robert J. Ife, Thomas H. Brown
-
Patent number: 4770689Abstract: A method for controlling weeds preferably in the crops of useful plants by using a 1-methyl-1H-imidazole-5-carboxylic acid derivative; herbicidal compositions containing the same; 1-methyl-1H-imidazole-5-carboxylic acid derivatives.Type: GrantFiled: December 19, 1986Date of Patent: September 13, 1988Assignee: Janssen Pharmaceutica N.V.Inventors: Jozef F. E. Van Gestel, William R. Lutz, Guy R. E. Van Lommen, Hanspeter Fischer, Marc F. J. Schroven, Rudolph C. Thummel
-
Patent number: 4769060Abstract: The invention relates to certain sulfonylurea compounds having an ester group ortho to the sulfonylurea linkage which have been found to be excellent preemergent and postemergent herbicides or plant growth regulators.Type: GrantFiled: February 18, 1987Date of Patent: September 6, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Donald J. Dumas
-
Patent number: 4762550Abstract: This invention relates to novel pyrazolesulfonamides, agricultural compositions thereof and the methods of their use as general and/or selective herbicides and/or plant growth regulants.Type: GrantFiled: August 13, 1987Date of Patent: August 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Stephen L. Hartzell
-
Patent number: 4762932Abstract: Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof.Type: GrantFiled: June 2, 1986Date of Patent: August 9, 1988Assignees: Imperial Chemical Industries, Ltd., ICI Americas, Inc.Inventors: Tobias O. Yellin, Philip N. Edwards, Michael S. Large
-
Patent number: 4759791Abstract: N-(3,4-Dihydro-2,2-dioxo-1,2-benzoxathiin-8-ylsulfonyl)-N'-pyrimidinylureas , N-(3,4-dihydro-2,2-dioxo-1,2-benzoxathiin-8-yl-sulfonyl)-N'-triazolylurea s and N-(3,4-dihydro-2,2-dioxo-1,2-benzoxathiin-8-ylsulfonyl)-N'-triazinylureas of the formula ##STR1## wherein R.sup.1 is hydrogen, halogen, nitro, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 haloalkoxy, C.sub.1 -C.sub.4 alkoxycarbonyl, C.sub.1 -C.sub.4 alkylthio, C.sub.1 -C.sub.4 alkylsulfinyl, C.sub.1 -C.sub.4 alkylsulfonyl or C.sub.2 -C.sub.5 alkoxyalkoxy,R.sup.2 and R.sup.3 are each independently of the other hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.4 is hydrogen, methyl or ethyl,W is oxygen or sulfur, andA is a radical ##STR2## in which formulae the substituents E.sup.1, E.sup.2, X.sup.1, X.sup.2, X.sup.3, X.sup.4, X.sup.5, X.sup.6, X.sup.7, X.sup.8, Y.sup.1, Y.sup.2, Y.sup.3, Y.sup.4, Y.sup.6, Y.sup.61, Y.sup.8, Y.sup.81, Z.sup.3 and Z.sup.Type: GrantFiled: June 11, 1986Date of Patent: July 26, 1988Assignee: Ciba-Geigy CorporationInventors: Werner Fory, Willy Meyer
-
Patent number: 4748165Abstract: This invention relates to amidine derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention there is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 is hydrogen or a 1-10C alkyl, 3-8C cycloalkyl, 4-14C cycloalkylalkyl, 3-6C alkenyl, 3-6C alkynyl, 1-6C alkanoyl, 6-10C aryl, 7-11C aralkyl or 7-11C aroyl radical, the latter three being optionally substituted; ring X is a heterocyclic ring as defined in the specification; A is phenylene or 5-7C cycloalkylene or a 1-8C alkylene chain into which is optionally inserted one or two groups; and R.sup.2 and R.sup.3 are a variety of radicals described in the specification: and the pharmaceutically-acceptable acid-addition salts thereof. Manufacturing processes and pharmaceutical compositions are also described.Type: GrantFiled: May 11, 1982Date of Patent: May 31, 1988Assignee: Imperial Chemical Industries PLCInventors: Derrick F. Jones, Keith Oldham
-
Patent number: 4746353Abstract: Tetrazole-substituted benzenesulfonamides are useful as agricultural chemicals and, in particular, as growth regulants and herbicides.Type: GrantFiled: November 24, 1986Date of Patent: May 24, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: George Levitt
-
Patent number: 4741760Abstract: N-Pyrimidin-4-yl-N'-sulfonylureas of the formula I and the basic addition salts thereof have herbicidal properties and properties for regulating, especially inhibiting, plant growth: ##STR1## the symbols in this formula having the following meanings: Q is halogen, lower alkyl, lower haloalkyl, lower alkoxy, lower haloalkoxy, nitro, amino, lower alkyl or dialkylamino, lower alkoxycarbonyl, formyl, lower alkoxyalkyl, lower alkoxyalkoxy, lower alkylthio, lower alkylsulfinyl or alkylsulfonyl, C.sub.1 -C.sub.4 -alkenyl or C.sub.1 -C.sub.4 -alkynyl,R.sub.1 is hydrogen, halogen, nitro, a ketal radical, a carbonyl radical substituted by allyl, haloalkyl, alkoxy or cycloalkyl, or is an oxime radical, a lower alkoxy, lower alkylthio, lower alkyl, lower alkylsulfinyl or sulfonyl group,R.sub.2 and R.sub.Type: GrantFiled: December 5, 1986Date of Patent: May 3, 1988Assignee: Ciba-Geigy CorporationInventors: Willy Meyer, Karl Hoegerle, Rudolph C. Thummel, Hans Tobler, Beat Bohner
-
Patent number: 4737184Abstract: Novel N-(heterocyclicaminocarbonyl) substituted thiophene-, furan- and pyrrolesulfonamides, such as N-[(4-methoxy-6-methylpyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno- [3,2-b]thiopyran-3-sulfonamide, 4,4-dioxide and N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-6,7-dihydro-5H-thieno[3,2-b ]thiopyran-3-sulfonamide, 4,4-dioxide and their method-of-use as herbicides are described.Type: GrantFiled: May 10, 1985Date of Patent: April 12, 1988Assignee: E. I. Du Pont De Nemours and CompanyInventor: Robert J. Pasteris
-
Patent number: 4723987Abstract: Sulfonamides such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-1,3-dihydro-6-methyl-3-oxof uro[3,4-c]pyridine-4-sulfonamide are useful as herbicides and plant growth regulants.Type: GrantFiled: April 22, 1986Date of Patent: February 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Mary A. Hanagan
-
Patent number: 4721520Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substituted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-2-methoxycarbonylbenzenesulf onamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.Type: GrantFiled: March 27, 1986Date of Patent: January 26, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: George Levitt
-
Patent number: 4708732Abstract: Herbicidal compounds having the formula ##STR1## wherein R.sup.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or substituted phenyl;R.sup.2 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.1 and R.sup.2 together are C.sub.2 -C.sub.5 alkylene;R.sup.3 is hydrogen, C.sub.1 -C.sub.4 alkyl, phenyl or substituted phenyl, with the proviso that R.sup.1 and R.sup.3 are not both phenyl or substituted phenyl;R.sup.4 is hydrogen or C.sub.1 -C.sub.4 alkyl; orR.sup.3 and R.sup.4 together are oxo;R.sup.5 is hydrogen or C.sub.1 -C.sub.4 alkyl;R.sup.6 is hydrogen or C.sub.1 -C.sub.4 alkyl; andR.sup.7 and R.sup.8 independently are (1) hydrogen; (2) halogen; (3) C.sub.1 -C.sub.4 alkyl; (4) C.sub.1 -C.sub.4 alkoxy; (5) trifluoromethoxy; (6) cyano; (7) nitro; (8) C.sub.1 -C.sub.4 haloalkyl; (9) R.sup.b SO.sub.n -- wherein n is the integer 0, 1 or 2; and R.sup.b is (a) C.sub.1 -C.sub.4 alkyl; (b) C.sub.1 -C.sub.4 alkyl substituted with halogen or cyano; (c) phenyl; or (d) benzyl; (10) --NR.sup.c R.sup.d wherein R.sup.c and R.sup.Type: GrantFiled: October 24, 1986Date of Patent: November 24, 1987Assignee: Stauffer Chemical CompanyInventor: Charles G. Carter
-
Patent number: 4699647Abstract: This invention relates to herbicidal benzene sulfonamides containing a five or six membered heterocyclic ring consisting of 2-3 heteroatoms and 1-2 carbonyl groups as a substituent on benzene.Type: GrantFiled: March 27, 1986Date of Patent: October 13, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
-
Patent number: 4683228Abstract: A guanidine derivative of the formula I: ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, ring X and D are a variety of radicals defined in the specification and A is a 3-8C alkylene chain which is substituted by a hydroxy radical and into which is optionally inserted, as part of the backbone of the chain, one or two groups selected from oxygen and sulphur atoms and NH and 1-6C N-alkyl radicals; and the pharmaceutically-acceptable acid additions salts thereof. Pharmaceutical compositions and methods of manufacture are also described. The compound of the formula I is a histamine H-2 antagonist and is therefore useful in ulcer therapy.Type: GrantFiled: January 22, 1985Date of Patent: July 28, 1987Assignees: ICI Americas Inc., Imperial Chemical Industries PLCInventors: Karin M. Kirkland, Derrick M. Mant
-
Patent number: 4680395Abstract: Pyrimidyl-sulfonyl isoureas of the formula ##STR1## in which R.sub.a is the difluoromethoxy group,R.sub.b is hydrogen, halogen, C.sub.1 -C.sub.5 -alkyl, C.sub.1 l-C.sub.5 -haloalkyl, C.sub.1 -C.sub.5 -alkoxy, C.sub.1 -C.sub.5 -haloalkoxy, C.sub.1 -C.sub.5 -alkylthio, C.sub.2 -C.sub.10 -alkoxyalkyl or C.sub.2 -C.sub.10 -alkoxyalkoxy or is an amino group ##STR2## wherein R.sub.c is hydrogen, methyl or ethyl, andR.sub.d is hydrogen, methyl, ethyl or methoxy,A is a radical of the formula ##STR3## Y is oxygen, sulfur or ##STR4## R.sub.1 is hydrogen, halogen, nitro, trifluoromethyl, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, --COR.sub.7, --S(O).sub.m --C.sub.1 -C.sub.5 -alkyl, --SO.sub.2 R.sub.10, XR.sub.11 or --OSO.sub.2 C.sub.1 -C.sub.5 -alkyl,R.sub.2 is hydrogen, fluorine, chlorine, bromine, nitro, C.sub.1 -C.sub.5 -alkyl, C.sub.1 -C.sub.5 -alkoxy, trifluoromethyl, C.sub.1 -C.sub.5 -haloalkoxy or --COR.sub.7,R.sub.3 is hydrogen, fluorine, chlorine, bromine, nitro, methoxy or trifluoromethyl,R.sub.Type: GrantFiled: March 1, 1985Date of Patent: July 14, 1987Assignee: Ciba-Geigy CorporationInventors: Haukur Kristinsson, Werner Topfl
-
Patent number: 4678499Abstract: Benzenesulfonamide compounds such as N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl-4 -oxo-1-phenyl-indeno[1,2-C]-pyrazole-5-sulfonamide and N-[(4-methoxy-6-methyl-pyrimidin-2-yl)aminocarbonyl]-1,4-dihydro-3-methyl- 4-oxo-1-phenyl-indeno[1,2-C]pyrazole-5-sulfonamide, agricultural compositions containing them, and their herbicidal utility are disclosed.Type: GrantFiled: January 30, 1986Date of Patent: July 7, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
-
Patent number: 4678855Abstract: Benzenesulfonamides with a substituted-alkyl-S(O).sub.n -substituent are carbonic anhydrase inhibitors useful in the treatment of elevated intraocular pressure.Type: GrantFiled: October 9, 1985Date of Patent: July 7, 1987Assignee: Merck & Co., Inc.Inventor: Kenneth L. Shepard
-
Patent number: 4672065Abstract: The N-substituted phenoxyacetamides of this invention are effective fungicides. In particular, these compounds are particularly effective against Tomato Late Blight.Type: GrantFiled: May 3, 1985Date of Patent: June 9, 1987Assignee: Chevron Research CompanyInventor: David M. Spatz
-
Patent number: 4666505Abstract: The invention relates to new 1-(2-oxyaminosulphonylphenylsulphonyl)-3-heteroaryl-ureas of the general formula (I) ##STR1## in which R.sup.1 represents an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aralkyl and aryl,R.sup.2 represents hydrogen or an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl and aralkyl andR.sup.Type: GrantFiled: August 23, 1985Date of Patent: May 19, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Theodor Pfister, Uwe Priesnitz, Hans-Jochem Riebel, Wolfgang Roy, Hans-Joachim Santel, Robert R. Schmidt
-
Patent number: 4666627Abstract: Novel 4-heterocyclylvinyl-4'-styryl-biphenyls of the formula ##STR1## are described, i which A is an isoxazolyl, oxadiazolyl, pyrimidinyl or triazinyl radical which is unsubstituted or substituted by a non-chromophoric substituent, R.sub.1 is hydrogen or a non-chromophoric substituent and R.sub.2 is hydrogen, halogen, or alkyl; processes for the preparation of these compounds are also described.The novel 4-heterocyclylvinyl-4'-styryl-biphenyls can be used as fluorescent brighteners for high-molecular organic materials, in particular materials of polyamide and polyester, especially for polyester textiles.Type: GrantFiled: July 27, 1984Date of Patent: May 19, 1987Assignee: Ciba-Geigy CorporationInventor: Hans R. Meyer
-
Patent number: 4663341Abstract: This invention relates to N-aryl-3-aryl-4,5-dihydro-1H-pyrazole-1-carboxamide compounds which are useful as pesticides, compositions containing those compounds, methods of controlling pests and processes for preparing these compounds.Type: GrantFiled: January 11, 1985Date of Patent: May 5, 1987Assignee: Rohm and Haas CompanyInventor: Richard M. Jacobson
-
Patent number: 4663327Abstract: Microbicidally active novel 1-heteroaryl-4-aryl-pyrazolin-5-ones of the formula ##STR1## in which R represents hydrogen or alkyl,R.sup.1 represents halogen, hydroxyl, optionally substituted alkyl, optionally substituted alkoxy, optionally substituted phenoxy, a radical --S(O).sub.p -- alkyl which is optionally substituted in the alkyl part, nitro, optionally substituted amino or a fused-on carbocyclic or heterocyclic radical,p represents an integer 0, 1 or 2,R.sup.2 represents halogen or optionally substituted alkyl, or represents alkoxy, alkylmercapto, nitro, cyano, carboxamide or a fused-on carbocyclic radical,m represents an integer from 0 to 5,n represents an integer from 0 to 4, it being possible for the substituents to be identical or different when m and/or n represent a number greater than 1, andX, Y and Z are identical or different and represent a nitrogen atom or the radical .dbd.CH or ##STR2## wherein R.sup.Type: GrantFiled: May 10, 1985Date of Patent: May 5, 1987Assignee: Bayer AktiengesellschaftInventors: Klaus Sasse, Wilhelm Brandes, Gerd Hanssler, Paul Reinecke, Hans-Georg Schmitt, Wilfried Paulus
-
Patent number: 4661147Abstract: The invention relates to certain sulfonylurea compounds having an ester group ortho to the sulfonylurea linkage which have been found to be excellent preemergent and postemergent herbicides or plant growth regulators.Type: GrantFiled: April 29, 1985Date of Patent: April 28, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Donald J. Dumas
-
Patent number: 4658027Abstract: A process for the preparation of a 1-(2-oxyaminosulphonyl-phenylsulphonyl)-urea of the formula ##STR1## in which R.sup.1 is an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl, cycloalkyl, cycloalkylalkyl, aralkyl and aryl,R.sup.2 is hydrogen or an optionally substituted radical from the series comprising alkyl, alkenyl, alkinyl and aralkyl, andR.sup.3 is an optionally substituted and/or optionally fused six-membered aromatic heterocyclic radical containing at least one nitrogen atom,comprising reacting water with a benzodisultam of the formula ##STR2## at a temperature between 0.degree. C. and 100.degree. C. The products are herbicidally active.Type: GrantFiled: August 23, 1985Date of Patent: April 14, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Theodor Pfister, Uwe Priesnitz, Hans-Jochem Riebel, Wolfgang Roy
-
Patent number: 4657908Abstract: The invention relates to carbonyl derivatives which are histamine H-2 antagonists and which inhibit gastric acid secretion. According to the invention where is provided a guanidine derivative of the formula I: ##STR1## in which R.sup.1 and R.sup.2, same or different, are hydrogen or 1-10C alkyl, 3-8C cycloalkyl or 4-14C cycloalkylalkyl, each alkyl, cycloalkyl or cycloalkylalkyl optionally carrying one or more F, Cl or Br atoms, provided that one of R.sup.1 and R.sup.2 is halogen substituted, or R.sup.2 is hydrogen and R.sup.1 is R.sup.5 -E-W in which W is 2-6C alkylene optionally substituted by 1 or 2 1-4C alkyls, E is O, S, SO, SO.sub.2 or NR.sup.6 in which R.sup.6 is H or 1-6C alkyl, R.sup.5 is H or 1-6C alkyl optionally substituted by 1 or 2 1-4C alkyls, or R.sup.5 and R.sup.6 are joined to form a pyrrolidine, piperidine, morpholine, piperazine or N-methylpiperazine ring, or R.sup.2 is H and R.sup.Type: GrantFiled: February 12, 1985Date of Patent: April 14, 1987Assignees: ICI Americas, Inc., Imperial Chemical Industries PLCInventors: Tobias O. Yellin, David J. Gilman, Philip N. Edwards, Michael S. Large, Derrick F. Jones, Keith Oldham
-
Patent number: 4656176Abstract: 2,3-Unsaturated nitrogen-containing heterocyclic compounds with a 3-nitro group and a 2-heterocyclyl alkylamino group. The alkyl group of 2-position substituents is preferably interrupted by sulfur or oxygen. The compounds of the invention are preferably dihydropyrroles or tetrahydropyrridines or pyrimidines. The compounds of the invention are histamine H.sub.2 -receptor antagonists.Type: GrantFiled: March 21, 1985Date of Patent: April 7, 1987Assignee: SmithKline & French Laboratories LimitedInventors: Michael L. Roantree, Rodney C. Young
-
Patent number: 4647566Abstract: Compounds of the formula formula IA or IB ##STR1## wherein A represents an optionally substituted saturated divalent grouping which together with the two carbon atoms to which it is attached represents a fused 5-, 6- or 7-membered carbocyclic or heterocyclic ring selected from optionally substituted fused cyclopenteno, cyclohexeno, cyclohepteno, dihydrothieno, dihydrothiopyrano, tetrahydrothiepino, dihydrofuro, dihydropyrano, tetrahydrooxepino, dihydropyrrolo, tetrahydropyrido and tetrahydroazepino; R.sub.1 represents lower alkyl, phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R.sub.1 represents an aromatic heterocyclic radical selected from e.g. optionally substituted pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl; R.sub.2, R.sub.3, R.sub.3 ' are hydrogen or lower alkyl; and pharmaceutically acceptable salts; are useful as benzodiazepine receptor modulators for the treatment of nervous system disorders.Type: GrantFiled: January 8, 1986Date of Patent: March 3, 1987Assignee: Ciba-Geigy CorporationInventor: Naokata Yokoyama
-
Patent number: 4637829Abstract: N-(2-Heterocyclylphenylsulfonyl)-N'-pyrimidinylureas and N-(2-heterocyclylphenylsulfonyl)-N'-triazinylureas of the general formula I ##STR1## and the salts thereof with amines, alkali metal bases or alkaline earth metal bases or with quaternary ammonium bases have good pre-and postemergence selective herbicidal and growth regulating properties.In this formulaA is a substituted furyl, thienyl or pyrrole radical,E is nitrogen or the methine group --CH.dbd.,Z is oxygen or sulfur,R.sup.1 is customary phenyl substituent,R.sup.2 is hydrogen, lower alkyl or lower alkoxy,R.sup.3 and R.sup.4 are each independently hydrogen, lower alkyl, lower alkoxy, lower alkylthio, cycloalkyl, halogen, haloalkyl, haloalkoxy, haloalkylthio, alkoxyalkyl, dialkoxyalkyl, amino, diethylamino.Type: GrantFiled: April 15, 1985Date of Patent: January 20, 1987Assignee: Ciba-Geigy CorporationInventors: Rolf Schurter, Georg Pissiotas
-
Patent number: 4629496Abstract: N-(heterocycliccarbamoyl)arylsulfonamides, such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-hydroxybenzenesulfonamide , methanesulfonate are useful for plant growth retardation, brush control and weed control in crops.Type: GrantFiled: May 3, 1985Date of Patent: December 16, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: James J. Reap
-
Patent number: 4627872Abstract: New herbicidally active 2,4-diamino pyrimidines of the formula ##STR1## wherein R.sup.1 is hydrogen or halogen, R.sup.2 is an optionally halogen-substituted alkyl or is halogen or alkoxy; R.sup.3 is hydrogen or alkyl; Y is oxygen or sulfur; and Z is a branched or unbranched alkylene.Type: GrantFiled: December 5, 1985Date of Patent: December 9, 1986Assignee: Bayer AktiengesellschaftInventors: Michael Schwamborn, Engelbert Kuhle, Ludwig Eue, Robert R. Schmidt, Hans-Joachim Santel
-
Patent number: 4610824Abstract: Antibacterial activity is exhibited by novel compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof.Type: GrantFiled: October 9, 1984Date of Patent: September 9, 1986Assignee: E. R. Squibb & Sons, Inc.Inventor: Uwe D. Truner
-
Patent number: 4604465Abstract: Compounds useful for inhibiting gastric acid secretion and for the treatment of peptic ulcers caused or exacerbated by gastric acidity having the following formula (I): ##STR1## in which R.sup.1 and R.sup.2, are H, C.sub.1-10 alkyl, C.sub.3-8 cycloalkyl or cycloalkylalkyl in which the alkyl part is C.sub.1-6 and the cycloalkyl part is C.sub.3-8, each of the alkyl, cycloalkyl and cycloalkylalkyls being optionally substituted by one or more halogens selected from F, Cl and Br, provided that at least one of R.sup.1 and R.sup.2 is a halogen substituted alkyl, cycloalkyl or cycloalkylalkyl and provided that there is no halogen substituent on the carbon directly attached to the nitrogen; and X, m, Y, n and R.sup.3 are as described in the specification; and the pharmaceutically-acceptable acid-addition salts thereof.Type: GrantFiled: September 21, 1982Date of Patent: August 5, 1986Assignees: ICI Americas, Inc., Imperial Chemical Industries, LimitedInventors: Tobias O. Yellin, Philip N. Edwards, Michael S. Large
-
Patent number: 4602014Abstract: Compounds of the formula formula IA or IB ##STR1## wherein A represents an optionally substituted saturated divalent grouping which together with the two carbon atoms to which it is attached represents a fused 5-, 6- or 7-membered carbocyclic or heterocyclic ring selected from optionally substituted fused cyclopenteno, cyclohexeno, cyclohepteno, dihydrothieno, dihydrothiopyrano, tetrahydrothiepino, dihydrofuro, dihydropyrano, tetrahydrooxepino, dihydropyrrolo, tetrahydropyrido and tetrahydroazepino; R.sub.1 represents lower alkyl, phenyl, or phenyl mono- or disubstituted by lower alkyl, lower alkoxy, halogen or trifluoromethyl; or R.sub.1 represents an aromatic heterocyclic radical selected from e.g. optionally substituted pyridyl, quinolyl, isoquinolyl, pyrimidyl and thiazolyl; R.sub.2, R.sub.3, R.sub.3 ' are hydrogen or lower alkyl; and pharmaceutically acceptable salts; are useful as benzodiazepine receptor modulators for the treatment of nervous system disorders.Type: GrantFiled: June 19, 1985Date of Patent: July 22, 1986Assignee: Ciba-Geigy CorporationInventor: Naokata Yokoyama
-
Patent number: 4599103Abstract: This invention relates to ureas and isoureas which are useful as herbicides and plant growth regulants. In particular, compounds of the instant invention have demonstrated great selectivity.Type: GrantFiled: October 15, 1984Date of Patent: July 8, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: George Levitt
-
Patent number: 4592978Abstract: N-(heterocyclicaminocarbonyl)arylsulfonamides in which the aryl radical is substituted in the 2-position by a carboxy radical, ester, thioester, or amide thereof; e.g. N-[(4,6-dimethylpyrimidin-2-yl)-aminocarbonyl]-2-methoxycarbonylbenzenesul fonamide or N-[(4,6-dimethoxy-1,3,5-triazin-2-yl)aminocarbonyl]-2-methoxycarbonylbenze nesulfonamide; are useful for the regulation of plant growth and as pre-emergence and post-emergence herbicides.Type: GrantFiled: December 22, 1982Date of Patent: June 3, 1986Assignee: E. I. Du Pont de Nemours and CompanyInventor: George Levitt
-
Patent number: 4587047Abstract: Antibacterial activity is exhibited by .beta.-lactams having a ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position wherein Z is oxygen or sulfur, and R is alkyl, alkenyl, alkynyl, substituted alkyl, phenyl, substituted phenyl, a 5,6 or 7-membered heterocycle (R.sub.c), phenylalkyl, (substituted phenyl)alkyl, R.sub.c -alkyl or --NR.sub.a R.sub.b wherein R.sub.a and R.sub.b are the same or different and each is hydrogen, alkyl, substituted alkyl, phenyl, substituted phenyl, phenylalkyl, or (substituted phenyl)alkyl or one of R.sub.a and R.sub.b is hydrogen, alkyl, phenyl, substituted phenyl, phenylalkyl or (substituted phenyl)alkyl and the other is amino, alkanoylamino, arylcarbonylamino, alkoxycarbonylamino, alkylsulfonylamino, alkylamino, dialkylamino, phenylamino, (substituted phenyl)amino, hydroxy, cyano, alkoxy, phenyloxy, (substituted phenyl)oxy, phenylalkoxy, (substituted phenyl)alkoxy, R.sub.c, R.sub.c -alkyl, R.sub.Type: GrantFiled: April 1, 1982Date of Patent: May 6, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Hermann Breuer, William A. Slusarchyk, Theodor Denzel, Uwe D. Treuner
-
Patent number: 4587051Abstract: A compound having the formula ##STR1## can be prepared by heating an anion having the formula ##STR2## with a cation having the formula ##STR3## or a cation having the formula ##STR4##Type: GrantFiled: May 21, 1984Date of Patent: May 6, 1986Assignee: E. R. Squibb & Sons, Inc.Inventor: William H. Koster
-
Patent number: 4578469Abstract: Coumarin compounds of the general formula (1) ##STR1## in which A denotes an oxygen atom or a grouping >N--R in which R represents a hydrogen atom or an alkyl radical of 1 to 18 carbon atoms which may be substituted by fluorine, chlorine or bromine atoms or by alkoxy.sub.C.sbsb.1.sub.-C.sbsb.4, dialkyl.sub.C.sbsb.1.sub.-C.sbsb.4 -amino, --SO.sub.2 --N(alkyl.sub.C.sbsb.1.sub.-C.sbsb.4).sub.2 or cyano groups or a cycloaliphatic, aromatic or heterocyclic radical which may be substituted by fluorine, chlorine or bromine atoms or by alkyl.sub.C.sbsb.1.sub.-C.sbsb.4, alkoxy.sub.C.sbsb.1.sub.-C.sbsb.4, hydroxyl, cyano, sulfonamide or --SO.sub.2 --N--(alkyl.sub.C.sbsb.1.sub.-C.sbsb.4).sub.2 groups, X denotes an oxygen atom or a grouping .gtoreq.N--R' in which R' represents a hydrogen atom or an alkyl.sub.C.sbsb.1.sub.-C.sbsb.18 carbonyl, alkoxy.sub.C.sbsb.1.sub.-C.sbsb.4 carbonyl, alkyl.sub.C.sbsb.1.sub.-C.sbsb.4 carbamoyl or alkyl.sub.C.sbsb.1.sub.-C.sbsb.Type: GrantFiled: September 26, 1984Date of Patent: March 25, 1986Assignee: Hoechst AktiengesellschaftInventors: Hans-Matthias Deger, Rudiger Erckel, Horst Fruhbeis
-
Patent number: 4576749Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof).Type: GrantFiled: April 13, 1984Date of Patent: March 18, 1986Assignee: E. R. Squibb & Sons, Inc.Inventors: Robert Zahler, William H. Koster, William A. Slusarchyk
-
Patent number: 4568745Abstract: An adduct of menadione and thiamine is described having the general formula C.sub.34 H.sub.36 N.sub.4 O.sub.11 S.sub.3, molecular weight 772.84 and containing the components in a molecular ratio of 2:1 respectively.This adduct is particularly intended to be added to integrator mixtures for zootechny.Type: GrantFiled: June 22, 1983Date of Patent: February 4, 1986Assignee: Luigi Stoppani S.p.A.Inventors: Giovanni Ghelli, Alessandro Barbon, Luciano Conti, Luigi Oliari
-
Patent number: 4560508Abstract: 4-Cyano-2-azetidinone derivatives represented by the formula ##STR1## wherein R.sup.1 is an amino group which may be acylated or protected, X is a hydrogen atom or a methoxy group and W is a hydrogen atom or a sulfo group, and methods of producing the same, for example, as represented by ##STR2## wherein R.sup.2 is an acylated or protected amino group, Y is a halogen atom or a group having the formula --OCOR.sup.3, --SCOR.sup.3 or --S(O).sub.n --R.sup.3 (R.sup.3 being a hydrocarbyl group and n an integer 1 or 2), R.sup.4 is an amino group which may be acylated or protected and X is as defined above. Compounds [I] are useful as advantageous intermediates for the synthesis of optically active 4-substituted-2-azetidinone derivatives, and, when W=SO.sub.3 H, [I] are also useful as antimicrobial agents and as beta-lactamase inhibitors.Type: GrantFiled: December 20, 1982Date of Patent: December 24, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, deceased, Michihiko Ochiai, Shoji Kishimoto
-
Patent number: 4559335Abstract: Antibacterial activity is exhibited by 2-azetidinones having a 3-acylamino substituent and a 1-substituent of the formula ##STR1## (or a salt or ester thereof), wherein Z.sub.1 and Z.sub.2 are each independently oxygen or sulfur.Type: GrantFiled: October 3, 1983Date of Patent: December 17, 1985Assignee: E. R. Squibb & Sons, Inc.Inventor: Robert Zahler
-
Patent number: 4558050Abstract: Chemical compounds useful in the treatment of metabolic disorders comprising the reaction product of thiamine and a dichloroacetic acid.Type: GrantFiled: March 1, 1984Date of Patent: December 10, 1985Assignee: University of FloridaInventor: Peter W. Stacpoole
-
Patent number: 4551276Abstract: Antibiotic activity is exhibited by .beta.-lactams having an ##STR1## substituent in the 1-position and an acylamino substituent in the 3-position.Type: GrantFiled: January 23, 1984Date of Patent: November 5, 1985Assignee: E. R. Squibb & Sons, Inc.Inventors: William A. Slusarchyk, David Kronenthal
-
Patent number: 4551277Abstract: Antibacterial activity is exhibited by (3-acylamino)-2-azetidinones having in the 1-position a group of the formula ##STR1## or a salt or ester thereof wherein R.sub.5 and R.sub.6 are the same or different and each is hydrogen or alkyl.Type: GrantFiled: November 9, 1983Date of Patent: November 5, 1985Assignee: E. R. Squibb & Sons, Inc.Inventor: Uwe D. Treuner
-
Patent number: 4550105Abstract: Disclosed are compounds of the general formula: ##STR1## wherein R.sub.1 is amino, an acylated amino or a protected amino group, X is hydrogen or methoxy, and R' is hydrogen, R or R.sup.4 wherein R is an organic residue attached to the azetidine ring through a carbon atom therein and R.sub.4 is azido, a halogen, an amino group which may optionally be acylated or a group of the formula --OR.sub.5, ##STR2## or --S--S--R.sub.5 wherein R.sub.5 is an organic residue and n is 0, 1 or 2, and pharmaceutically acceptable salts and esters thereof.The compounds have antimicrobial and/or .beta.-lactamase-inhibitory activity and are of value as drugs for human beings and domesticated animals.Type: GrantFiled: December 3, 1981Date of Patent: October 29, 1985Assignee: Takeda Chemical Industries, Ltd.Inventors: Taisuke Matsuo, Shoji Kishimoto, Michihiko Ochiai
-
Patent number: 4548751Abstract: Antibacterial activity is exhibited by 3-acylamino-2-azetidinones having in the 1-position a group of the formula ##STR1## or an ester of salt thereto, wherein R.sub.5 and R.sub.6 are the same or different and each is hydrogen, alkyl, phenyl or substituted phenyl.Type: GrantFiled: August 3, 1983Date of Patent: October 22, 1985Assignee: E. R. Squibb & Sons, Inc.Inventors: Spencer D. Kimball, David Kronenthal, William H. Koster
-
Patent number: 4548747Abstract: Antibacterial activity is exhibited by .beta.lactams having a 3-acylamino substituent and in the 1-position a group of the formula ##STR1## wherein R.sub.5 and R.sub.6 are the same or different and each is hydrogen, alkyl, alkenyl, alkynyl, phenyl, substituted phenyl, cycloalkyl or R.sub.c, or R.sub.5 and R.sub.6 together with the carbon atom to which they are attached are cycloalkyl or R.sub.c, or one of R.sub.5 and R.sub.6 is hydrogen and the other is azido, halomethyl, dihalomethyl, trihalomethyl, alkoxycarbonyl, alkenyl, alkynyl, 2-phenylethenyl, 2-phenylethynyl, carboxyl, --CH.sub.2 X.sub.1, --S--X.sub.2, --O--X.sub.2, or ##STR2## and R.sub.7 is alkyl, substituted alkyl, phenyl or substituted phenyl; andR.sub.c is 4,5,6 or 7-membered heterocycle.Type: GrantFiled: May 2, 1983Date of Patent: October 22, 1985Assignee: E. R. Squibb & Sons, Inc.Inventor: Robert Zahler