Plural Nitrogens In The Six-membered Hetero Ring Patents (Class 544/66)
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Patent number: 5508278Abstract: Novel bactericidal pyrido[1,2,3-d,e,][1,3,4]benzoxadiazine derivatives of the formula (I) ##STR1## in which R.sup.1 is hydrogen or C.sub.1 -C.sub.4 -alkyl optionally substituted by hydroxyl or halogen,R.sup.2 independently of R.sup.1 is hydrogen or methyl,R.sup.3 is hydrogen or C.sub.1 -C.sub.4 -alkyl,R.sup.4 is hydrogen, C.sub.1 -C.sub.4 -alkyl optionally substituted by hydroxyl, methoxy, amino, methylamino or dimethylamino, or (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl,X.sup.Type: GrantFiled: August 26, 1994Date of Patent: April 16, 1996Assignee: Bayer AktiengesellschaftInventors: Thomas Jaetsch, Burkhard Mielke, Uwe Petersen, Thomas Philipps, Thomas Schenke, Klaus D. Bremm, Rainer Endermann, Karl G. Metzger, Martin Scheer, Michael Stegemann, Heinz-Georg Wetzstein
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Patent number: 5496943Abstract: Disclosed is a novel heterocyclic compound selected from the group consisting of the compounds [IV] to [VII], [IX] and [X]. The heterocyclic compound is useful for reactive materials in chemical industry. A process for producing the heterocyclic compound is also disclosed.Type: GrantFiled: March 13, 1992Date of Patent: March 5, 1996Assignee: Nippon Paint Co., Ltd.Inventors: Otohiko Tsuge, Taizo Hatta, Satoshi Urano, Noriyuki Tsuboniwa, Ryuzo Mizuguchi
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Patent number: 5478934Abstract: Disclosed are compounds of the formula: ##STR1## wherein: A represents arylalkyl, aryl or heteroaryl; X is nitrogen or CH; and R.sub.2, R.sub.3, R.sub.4 and R.sub.5 represent organic or inorganic substituents;and the pharmaceutically acceptable salts thereof; useful for treating disorders of the central nervous system.Type: GrantFiled: November 23, 1994Date of Patent: December 26, 1995Inventors: Jun Yuan, Jan W. F. Wasley
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Patent number: 5476934Abstract: A nitrogen-containing perfluoroalkanoyl peroxide is provided which is represented by the formula: ##STR1## wherein Rf.sub.1 and Rf.sub.2 independently stand for an alkyl group of 1 to 5 carbon atoms, provided that Rf.sub.1 and Rf.sub.2 are joined to each other in one of the three patterns of union, 1) direct union, 2) union through the medium of an oxygen atom or 3) union through the medium of a nitrogen atom to form one of the three rings, i.e. five-membered ring, six-membered ring or seven-membered ring.Type: GrantFiled: August 23, 1994Date of Patent: December 19, 1995Assignee: Agency of Industrial Science & Technology, Ministry of International Trade & IndustryInventors: Haruhiko Fukaya, Takashi Abe, Eiji Hayashi, Yoshio Hayakawa
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Patent number: 5462938Abstract: Arthropodicidal carboxanilides of Formula I and II ##STR1## wherein Q is selected from the group ##STR2## A, E, G, X, X.sup.1, Y, Z, Z.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6 and n are as defined in the text, arthropodicidal compositions containing said compounds and a method for using the compounds to control arthropods.Type: GrantFiled: June 18, 1993Date of Patent: October 31, 1995Inventors: Gary D. Annus, William E. Barnette, Stephen F. McCann, Keith D. Wing
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Patent number: 5445762Abstract: Decomposition-sensitive complex ligands can be stabilized by derivatizing them with the aid of bulky secondary or tertiary carboxylic acids or sulfonic acids. These stabilized derivatives can be added to alignment layers and liquid-crystal mixtures and increase the contrast and brightness in the FLC display.Type: GrantFiled: January 18, 1994Date of Patent: August 29, 1995Assignee: Hoechst AktiengesellschaftInventors: Javier Manero, Norbert Rosch
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Patent number: 5420099Abstract: A compound having the formula ##STR1## wherein A is CR.sub.7 ; and R.sup.1 through R.sup.7 are substituents such as hydrogen, halogen, branched and straight chain hydrocarbons, cyclic hydrocarbons, aromatics, and sulfur and nitrogen containing functional groups. Further, R.sup.5 and R.sup.6 may be taken together with the atom to which they are attached to form a group ##STR2## in which R.sup.9 and R.sup.10 are further functional groups. The compounds are useful in herbicidal compositions, particularly in combination with carriers and surfactants. A process for making this compound is also presented.Type: GrantFiled: December 21, 1992Date of Patent: May 30, 1995Assignee: Shell Research LimitedInventor: Trevor W. Newton
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Patent number: 5294611Abstract: The invention provides novel 2,3,6 substituted quinazolinones having the formula: ##STR1## wherein R.sup.6, R and X are as described in the specification, which have activity as angiotensin II (AII) antagonists.Type: GrantFiled: April 23, 1993Date of Patent: March 15, 1994Assignee: American Cyanamid CompanyInventors: Aranapakam M. Venkatesan, Jeremy I. Levin
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Patent number: 5283355Abstract: Compounds of the Formula (5) and processes for their preparation and use, particularly in the manufacture of unsymmetrical triphenodioxazine dyes: ##STR1## wherein: Y is H, alkyl, substituted alkyl, alkoxy, Cl or Br;R is a group of Formula (3) ##STR2## R.sup.1 and R.sup.2 are each independently alkyl, or R.sup.1 and R.sup.2 together with the carbon atom to which they are attached form an optionally substituted 4, 5 or 6 membered alicyclic or heterocyclic ring;R.sup.3 is H;Z is Cl, Br or A--NH; andA is H or the residue of a primary amine.Type: GrantFiled: October 22, 1991Date of Patent: February 1, 1994Assignee: Imperial Chemical Industries PLCInventor: William J. E. Norris
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Patent number: 5212301Abstract: Introduction of a fluoro substituent into an aromatic ring adjacent an electron donating group is difficult producing mixed isomers and low yields of desired products.A process for the introduction of a fluoro substituent into a substantially adjacent position to an electron-donating group into an aromatic compound in high yield is disclosed.The fluoroaromatic compounds are useful as synthetic intermediates for example in the manufacture of agrochemicals, pharmaceuticals and dyestuffs.Type: GrantFiled: May 8, 1992Date of Patent: May 18, 1993Assignee: Imperial Chemical Industries PLCInventors: John S. Moilliet, Richard D. Chambers, Michael H. Rock
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Patent number: 5208339Abstract: A nitrogen-containing perfluoroalkanoyl peroxide is provided which is represented by the formula: ##STR1## wherein Rf.sub.1 and Rf.sub.2 independently stand for an alkyl group of 1 to 5 carbon atoms, provided that Rf.sub.1 and Rf.sub.2 are joined to each other in one of the three patterns of union, 1) direct union, 2) union through the medium of an oxygen atom or 3) union through the medium of a nitrogen atom to form one of the three rings, i.e. five-membered ring, six-membered ring or seven-membered ring.Type: GrantFiled: September 8, 1992Date of Patent: May 4, 1993Assignees: Agency of Industrial Science & Technology, Ministry of International Trade & IndustryInventors: Haruhiko Fukaya, Takashi Abe, Eiji Hayashi, Yoshio Hayakawa
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Patent number: 5158959Abstract: What are disclosed are aminoacid compounds of the formula ##STR1## wherein n is 0 or 1, and salts thereof, said compounds and salts having hypotensive properties; methods for making the compounds; pharmaceutical compositions containing the compounds or salts; and use of the compounds and salts for treating hypertension.Type: GrantFiled: December 27, 1983Date of Patent: October 27, 1992Assignee: Hoechst AktiengesellschaftInventors: Rolf Geiger, Volker Teetz, Hansjorg Urbach, Bernward Scholkens, Rainer Henning
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Patent number: 5122524Abstract: New heterocyclic compounds of formula I ##STR1## in which Het means one of following groups; ##STR2## wherein R.sub.11, R.sub.13 and R.sub.14 mean independently hydrogen, hydroxymethyl or lower alkyl group, Z means S, O or NH; A means valency bond, --CH.dbd.CH--, or --CH.sub.2 --CH.sub.2 -- group; R.sub.1 and R.sub.2 independently mean nitro, cyano, halogen, amino, carboxamido, aryl, aroyl, pyridyl, alkoxycarbonyl, acyl or one of following groups; ##STR3## wherein R.sub.6 means hydrogen or lower alkyl group, R.sub.8 means lower alkyl, R.sub.7 means cyano or COOR.sub.10, wherein R.sub.10 means hydrogen or lower alkyl or R.sub.1 and R.sub.2 together form a substituted or unsubstituted 5 or 6 membered ring which may contain 1 or 2 heteroatom N; R.sub.3, R.sub.4, and R.sub.5 mean independently hydrogen, hydroxy or lower alkyl group; Y means N or CH. The compounds may be used in the treatment of congestive heart failure.Type: GrantFiled: March 15, 1991Date of Patent: June 16, 1992Assignee: Orion-yhtyma OyInventors: Heimo O. Haikala, Erkki J. Honkanen, Kari K. Lonnberg, Pentti T. Nore, Jarmo J. Pystynen, Anne M. Luiro, Aino K. Pippuri
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Patent number: 5106840Abstract: The invention relates to a method of preparing N-oxo-tetrahydro-.beta.-carbolines having formula 1. ##STR1## wherein R.sub.1 is lower alkyl or alkoxy, halogen, trifluoromethyl, lower alkylthio, hydroxy, amino, lower mono- or dialkyl- or acylamino.n has the value 0, 1 or 2,R.sub.2 is hydrogen, lower alkyl or acyl,R.sub.3 is hydrogen, lower alkyl or alkoxycarbonyl, or a phenyl group optionally substituted with a group R.sub.Type: GrantFiled: June 5, 1990Date of Patent: April 21, 1992Assignee: Duphar International Research B.V.Inventors: Peter H. H. Hermkens, Jan H. Van Maarseveen, Johan W. Scheeren, Cornelis G. Kruse
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Patent number: 5097027Abstract: Heterocyclic compounds of the formula ##STR1## are used as pigments for surface coatings and for coloring and pigmenting high molecular weight organic material.Type: GrantFiled: October 5, 1990Date of Patent: March 17, 1992Assignee: Bayer AktiengesellschaftInventor: Hans Hochstetter
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Patent number: 5086052Abstract: Pyridazinone, triazinone and oxapyridazinone compounds which are useful in inhibiting lipoxygenase enzymes, particularly 5-lipoxygenase.Type: GrantFiled: June 28, 1990Date of Patent: February 4, 1992Assignee: Abbott LaboratoriesInventors: Dee W. Brooks, George W. Carter, Anwer Basha, Bruce P. Gunn, Richard D. Dyer
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Patent number: 5082842Abstract: The compounds of the formula ##STR1## wherein Ra, Rb, Rc, Rd, Re and Rf are defined in the specification, and the pharmaceutically acceptable acid addition salts of compounds of formula A which have one or more basic substituents are described. The compounds of formula A have valuable pharmacological properties and can be used for the control or prevention of illnesses. In particular, they have muscle relaxant, sedative-hypnotic, anxiolytic and/or anticonvulsive activity and can accordingly be used in the control or prevention of muscle tensions, stress conditions, insomnia, anxiety states and/or convulsions.Type: GrantFiled: October 16, 1989Date of Patent: January 21, 1992Assignee: Hoffmann-La Roche Inc.Inventor: Ulrich Widmer
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Patent number: 5019575Abstract: New heterocyclic compounds of formula I ##STR1## in which Het means one of following groups; ##STR2## wherein R.sub.11, R.sub.13 and R.sub.14 mean independently hydrogen, hydroxymethyl or lower alkyl group, Z means S, O or NH; A means valency bond, --CH.dbd.CH--, or --CH.sub.2 --CH.sub.2 --group; R.sub.1 and R.sub.2 independently means nitro, cyano, halogen, amino, carboxamido, aryl, aroyl, pyridyl, alkoxycarbonyl, acyl or one of following groups; ##STR3## wherein R.sub.6 means hydrogen or lower alkyl group, R.sub.8 means lower alkyl, R.sub.7 means cyano or COOR.sub.10, wherein R.sub.10 means hydrogen or lower alkyl or R.sub.1 and R.sub.2 together form a substituted or unsubstituted 5 or 6 membered ring which may contain 1 or 2 heteroatom N; R.sub.3, R.sub.4, and R.sub.5 mean independently hydrogen, hydroxy or lower alkyl group; Y means N or CH. The compounds may be used in the treatment of congestive heart failure.Type: GrantFiled: February 9, 1990Date of Patent: May 28, 1991Assignee: Orion-yhtyma OyInventors: Heimo O. Haikala, Erkki J. Honkanen, Kari K. Lonnberg, Pentti T. Nore, Jarmo J. Pystynen, Anne M. Luiro, Aino K. Pippuri
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Patent number: 4952289Abstract: Methods and apparatus for electrochemical extraction of a ligand such as molecular oxygen from a first fluid environment and for release of a ligand such as molecular oxygen, as well as ligand carrier compounds therefor comprising macrocyclic amines having the general formulas: ##STR1## where: A, B, C, D, E, and F are each nitrogen, oxygen, sulfur, or phosphorous;m, n, o, p, q, and r are each typically 2, 3, 4, 5, or 6;the R substituents are each generally H or short chain (linear or branched) alkyl, although R.sub.2 may represent ketyl (.dbd.o); andM is a suitable transition metal ion.Type: GrantFiled: May 9, 1988Date of Patent: August 28, 1990Assignee: Aquanautics CorporationInventors: Joseph P. Ciccone, Emory S. DeCastro, John B. Kerr
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Patent number: 4939140Abstract: A heterocyclic oxophthalazinyl acetic acid having aldose reductast inhibitory activity of the formula ##STR1## wherein X is oxygen or sulfur; Z is a covalent bond, O, S, NH or CH.sub.2 or CHR.sub.5 Z is vinyl; R.sub.1 is hydroxy, or a prodrug group; R.sub.2 is a heterocyclic group, R.sub.3 and R.sub.4 are hydrogen or the same or a different substituent, and R.sub.5 is hydrogen, methyl or trifluoromethyl. The pharmaceutically acceptable acid addition salts of the above compounds wherein R.sub.1 is di(C.sub.1 -C.sub.4)alkylamino or (C.sub.1 -C.sub.4)alkoxy substituted by N-morpholino or di(C.sub.1 -C.sub.4)alkylamino and the pharmaceutically active base addition salts of the above compounds wherein R.sub.1 is hydroxy are also aldose reductase inhibitors.Type: GrantFiled: October 27, 1988Date of Patent: July 3, 1990Assignee: Pfizer Inc.Inventors: Eric R. Larson, Banavara L. Mylari
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Patent number: 4939251Abstract: Novel 1-azaspiro[4.4] lactams are produced by reaction of at least one hydroxy-containing primary amino compound with a 4-ketodiacid compound or a 1,6-dioxaspiro[4.4]lactone. Molar excesses of amion compound result in production of spirodilactams, while limited molar quantities of amino compound results in production of a spirolactam-lactone which reacts further with hydroxy-containing primary amino compound or with hydroxy-free primary amino compound to produce a spirodilactam. Certain of the spirolactams are useful as precursors for glycidyloxy derivatives which react with epoxy curing agents to form insoluble thermoset resins while others are useful as curing agents and yet others are converted to glycidyloxy derivatives useful as reactive diluents in epoxy resin applications.Type: GrantFiled: September 16, 1988Date of Patent: July 3, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4933336Abstract: A compound of formula (I), or a pharmaceutically acceptable salt thereof, ##STR1## in which, R.sub.1 is hydrogen, lower alkyl or CH.sub.2 OR.sub.6 ;R.sub.2 is hydrogen or lower alkyl;R.sub.3 is hydrogen or lower alkyl;each of W and Z, which are different, represents --CR.sub.4 R.sub.5 -- or --(CR.sub.x R.sub.y).sub.n --, in which,R.sub.4 is hydrogen, C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy;R.sub.5 is C.sub.1-3 alkyl, C.sub.1-3 alkylthio or C.sub.1-3 alkoxy; or together R.sub.4 and R.sub.5 form a 3 to 6 membered carbocyclic ring, or a heterocyclic ring containing one or two ring oxygen, nitrogen or sulphur atoms;or R.sub.4 and R.sub.5 together form an oxo or methylene group;each of R.sub.x and R.sub.y is hydrogen or C.sub.1-3 alkyl; n is zero or 1;R.sub.6 is hydrogen, lower alkyl, lower alkylcarbonyl, arylcarbonyl, aralkylcarbonyl, heteroarylcarbonyl, optionally substituted aminocarbonyl, lower alkoxycarbonyl and aryloxycarbonyl;R.sub.Type: GrantFiled: August 9, 1988Date of Patent: June 12, 1990Assignee: Laboratoires Sobio S.A.Inventors: Michel Martin, Guy Nadler, Richard Zimmermann
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Patent number: 4925845Abstract: Gem 3 dialkyl or spiro 4 aryl or heteroaryl 5 heterocyclic 3 H indoles and their pharmaceutically acceptable salts are prepared. They are useful for reducing blood pressure producing a positive inotropic action influencing thrombocyte aggregation and improving microcirculation. Hydrazinophenyl heterocyclic intermeidates are also disclosed.Type: GrantFiled: February 24, 1988Date of Patent: May 15, 1990Assignee: Boehringer Mannheim GmbHInventors: Alfred Mertens, Wolfgang von der Saal, Lothar Kling, Bernd Muller-Beckmann
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Patent number: 4918188Abstract: Compounds of the formula (V), ##STR1## wherein R.sup.1 is certain optionally substituted alkyl groups, R.sup.2 is hydrogen, alkyl or optionally substituted henyl and R.sup.3 and R.sup.4 are independently alkyl or optionally substituted phenyl, or together form a C.sub.4-7 cycloalkyl ring; are described as useful intermediates in the preparation of carbapenem and penem antibiotics. Processes for their preparation are described as are certain oxadiazine intermediates.Type: GrantFiled: November 10, 1988Date of Patent: April 17, 1990Assignee: Imperial Chemical Industries plcInventor: Michael B. Gravestock
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Patent number: 4895942Abstract: Novel epoxyalkoxy-containing [4.4] spirodilactams having ring nitrogen atoms in the 1- and the 6- ring positions and having a substituent on each ring nitrogen atom, at least one of which substituents contains an epoxyalkyl moiety. Such epoxy compounds are produced by reaction of a 1-halo-2,3-epoxyalkane and the corresponding hydroxy-containing spirodilactam followed by treatment with strong base.Type: GrantFiled: September 16, 1988Date of Patent: January 23, 1990Assignee: Shell Oil CompanyInventor: Pen C. Wang
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Patent number: 4864023Abstract: The invention is concerned with tricyclic compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a carboxy-protecting radical; R.sup.2 is a hydrogen atom or a lower alkyl radical which may be substituted with a halogen atom; R.sup.3 and R.sup.4 independently are a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical or a substituted or unsubstituted amino radical; X is a halogen atom; and R.sup.5 and R.sup.6 are independently a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical, a lower alkoxy radical or a substituted or unsubstituted amino radical; or R.sup.5 and R.sup.6, taken together with the adjacent nitrogen atom, may form a 5 to 7 membered heterocyclic ring which may be substituted with one or more substituents at the carbon atom(s), and the heterocyclic ring may further contain --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.7 --CO--, and also R.sup.Type: GrantFiled: August 26, 1988Date of Patent: September 5, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Kazuteru Yokose, Nobuo Shimma, Mikayo Kamata, Masahiro Aoki, Tatsuo Ohtsuka
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Patent number: 4849516Abstract: Compounds of the formula (V): ##STR1## wherein R.sup.1 is certain optionally substituted alkyl groups, R.sup.2 is hydrogen, alkyl or optionally substituted phenyl and R.sup.3 and R.sup.4 are independently alkyl or optionally substituted phenyl, or together form a C.sub.4-7 cycloalkyl ring; are described as useful intermediates in the preparation of carbapenem and penem antibiotics. Processes for their preparation are described as are certain oxadiazine intermediates.Type: GrantFiled: October 14, 1987Date of Patent: July 18, 1989Assignee: Imperial Chemical Industries PLCInventor: Michael B. Gravestock
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Patent number: 4846874Abstract: 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: December 16, 1987Date of Patent: July 11, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Robert J. Pasteris
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Patent number: 4838929Abstract: Sulfonamides such as N-[(4,6-dimethoxypyrimidin-2-aminocarbonyl]-1,3-dihydro-6-methyl-3-oxofuro [3,4-c]pyridine-4-sulfonamide are useful as herbicides and plant growth regulants.Type: GrantFiled: September 14, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Mary A. Hanagan
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Patent number: 4838925Abstract: This invention relates to novel heterocyclic carbonyl sulfonamides which are particularly useful as agricultural chemicals.Type: GrantFiled: September 25, 1987Date of Patent: June 13, 1989Assignee: E. I. Du Pont de Nemours and CompanyInventor: Chi-Ping Tseng
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Patent number: 4801584Abstract: The invention is concerned with tricyclic compounds of the formula ##STR1## wherein R.sup.1 is a hydrogen atom or a carboxy-protecting radical; R.sup.2 is a hydrogen atom or a lower alkyl radical which may be substituted with a halogen atom; R.sup.3 and R.sup.4 independently are a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical or a substituted or unsubstituted amino radical; X is a halogen atom; and R.sup.5 and R.sup.6 are independently a hydrogen atom or a lower alkyl radical which may be substituted with a hydroxy radical, a lower alkoxy radical or a substituted or unsubstituted amino radical; or R.sup.5 and R.sup.6, taken together with the adjacent nitrogen atom, may form a 5 to 7 membered heterocyclic ring which may be substituted with one or more substituents at the carbon atom(s), and the heterocyclic ring may further contain --NR.sup.7 --, --O--, --S--, --SO--, --SO.sub.2 -- or --NR.sup.7 --CO--, and also R.sup.Type: GrantFiled: September 8, 1987Date of Patent: January 31, 1989Assignee: Hoffmann-La Roche Inc.Inventors: Kazuteru Yokose, Nobuo Shimma, Miyako Kamata, Masahiro Aoki, Tatsuo Ohtsuka
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Patent number: 4775406Abstract: The salts of 1-phenylimidazole-5-carboxylic acids substituted in the phenyl ring, of the general formula (I) ##STR1## exhibit a good plant growth-regulating activity. In the general formula the symbols have the following meaning:Y is an ammonium ion substituted up to fourfold by (substituted) alkyl, (substituted) alkenyl, alkynyl, (substituted) cycloalkyl, cycloalkenyl, and (substituted) phenyl, wherein the charged N may be part of a heterocyclic radial (NH.sub.4.sup.+ is excepted); phosphonium ion substituted fourfold by alkyl, (substituted) phenyl or (substituted) benzyl; sulfonium- or sulfoxonium ion substituted threefold by alkyl, (substituted) phenyl or (substituted) benzyl; the guanidinium ion or an O-alkylisourea cation;R.sup.1, R.sup.2 independently of each other are alkyl;R.sup.3 is alkyl, alkoxy or halogen; andn is 0, 1, 2 or 3.Type: GrantFiled: November 21, 1985Date of Patent: October 4, 1988Assignee: Hoechst AktiengesellschaftInventors: Roland Schmierer, Ernst-Friedrich Schulze, Helmut Bustell, Erwin Hacker
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Patent number: 4772309Abstract: A 5-Acylamino-pyrazole derivatives of the formula ##STR1## in which R.sup.1 represents hydrogen, halogen or nitro,R.sup.2 represents hydrogen, alkyl, alkenyl, alkinyl or optionally substituted cycloalkyl,R.sup.3 represents hydrogen or alkyl,R.sup.4 represents hydrogen or alkyl,X represents oxygen or sulphur,n represents the integer 0, 1 or 2,Ar represents in each case optionally substituted phenyl or pyridyl andHet represents an optionally substituted 5- or 6- membered heterocyclic radical linked via a carbon atom,which exhibit herbicidal and plant growth regulating activity.Type: GrantFiled: March 19, 1987Date of Patent: September 20, 1988Assignee: Bayer AktiengesellschaftInventors: Jorg Stetter, Reinhold Gehring, Otto Schallner, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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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
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Patent number: 4759790Abstract: This invention relates to herbicidally active sulfonamide compounds having a heterocyclic carbonyl group ortho to the sulfonyl bridge.Type: GrantFiled: May 21, 1987Date of Patent: July 26, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Joel R. Christensen
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Patent number: 4755510Abstract: The present invention relates to novel optically active or racemic tetrahydro-1,2,4-oxadiazine-5-thione derivatives of the formula ##STR1## methods for their preparation, pharmaceutical compositions comprising the said compounds as active ingredients and a method for the anticonvulsive treatment of mammals, especially human beings.The compounds of the formula I have as good activity as diphenyl hydantoine but their toxicity is much lower.Type: GrantFiled: October 10, 1985Date of Patent: July 5, 1988Assignees: Richter Gedeon Vegyeszeti Gyar R.T., MTA Kozponti Kemiai KutatointezeteInventors: Csilla Vezert nee Solyom, Laszlo rogdi, Lajos Kisfaludy, Laszlo Otvos, Zsuzsanna Tegyey, Helga Tudos nee Feuer, Eva Palosi, Sara Ronai nee Lukacs, Eszter Cholnoky, Laszlo Szporny
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Patent number: 4741765Abstract: 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: April 3, 1987Date of Patent: May 3, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventors: Robert J. Pasteris, Ramaurthi Muthukrishnan
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Patent number: 4740231Abstract: 1-Aryl-5-alkoximinoalkylamino-pyrazoles of the formula ##STR1## in which R represents cyano or nitro, or represents an optionally substituted heterocyclic radical,R.sup.1 represents hydrogen or alkyl,R.sup.2 represents hydrogen or alkyl, or represents optionally substituted aryl,R.sup.3 represents hydrogen, alkyl or alkenyl, or represents in each case optionally substituted aralkyl or aryl andAr represents optionally substituted phenyl or pyridyl,are active as herbicides and plant growth regulants. Compounds of the formula ##STR2## in which R" has the same definition as R other than cyano, are also active and useful as intermediates as well.Type: GrantFiled: May 22, 1986Date of Patent: April 26, 1988Assignee: Bayer AktiengesellschaftInventors: Reinhold Gehring, Otto Schallner, Jorg Stetter, Hans-Joachim Santel, Robert R. Schmidt, Klaus Lurssen
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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
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Patent number: 4725305Abstract: Herbicidally active novel N,N'-bis-sulphonyl guanidines of the formula ##STR1## in which M is hydrogen, a metal or an ammonium radical, andR.sup.4, R.sup.5, R.sup.40 and R.sup.41 are various organic radicals.Type: GrantFiled: November 14, 1986Date of Patent: February 16, 1988Assignee: Bayer AktiengesellschaftInventors: Koichi Moriya, Theodor Pfister, Hans-Jochem Riebel, Ludwig Eue, Robert R. Schmidt, Klaus Lurssen, Hans-Joachim Diehr, Christa Fest, Rolf Kirsten, Joachim Kluth, Klaus-Helmut Muller, Uwe Priesnitz, Wolfgang Roy, Hans-Joachim Santel
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Patent number: 4723988Abstract: Thiophenesulfonamides such as N-[(4,6-dimethylpyrimidin-2-yl)aminocarbonyl]-3-(isoxazol-3-yl)-2-thiophen esulfonamide are useful as herbicides and plant growth regulants.Type: GrantFiled: March 27, 1987Date of Patent: February 9, 1988Assignee: E. I. Du Pont de Nemours and CompanyInventor: Rafael Shapiro
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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
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Patent number: 4713456Abstract: A process for the preparation of a 5-acylpyrimidine of the formula ##STR1## in which R is an organic radical comprising reacting a methyl ketone of the formulaR--CO--CH.sub.3in a first stage with a formylating reagent in the presence of a base to form an enolketone of the formulaR--CO--CH.dbd.CH--OR.sup.10in which R.sup.10 represents hydrogen or a base radical, thereafter reacting the enolketone in 2nd and 3rd stages with formamidine or a formamidine salt, and with an amino-formylating agent, and, in a 4th stage heating to cyclize the compound formed.The end products, some of which are new, are intermediates for making herbicides.Type: GrantFiled: August 26, 1985Date of Patent: December 15, 1987Assignee: Bayer AktiengesellschaftInventors: Hans-Ludwig Elbe, Graham Holmwood
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Patent number: 4689414Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof, wherein R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3 or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;R.sub.5 is hydrogen, alkyl, aryl, arylalkyl, cyano, nitro, ##STR2## Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl-(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl-(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR3## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR4## amino, or substituted amino; m is 0 or an integer of 1 to 6;n is an integer of 1 to 6; andp is an integer of 2 to 6.Type: GrantFiled: February 24, 1986Date of Patent: August 25, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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Patent number: 4684656Abstract: Cardiovascular activity is exhibited by compounds having the formula ##STR1## and pharmaceutically acceptable salts thereof wherein X is oxygen or sulfur;R.sub.1 is alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.2 is hydrogen, alkyl, alkenyl, alkynyl, cycloalkyl, aryl, --(CH.sub.2).sub.n --Y.sub.1, or halo substituted alkyl;R.sub.3 is hydrogen, alkyl, cycloalkyl, aryl, heterocyclo, --(CH.sub.2).sub.n --Y.sub.2, --(CH.sub.2).sub.p --Y.sub.3, or halo substituted alkyl;R.sub.4 is aryl or heterocyclo;Y.sub.1 is cycloalkyl, aryl, heterocyclo, hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.m --S--, amino, substituted amino, carbamoyl, ##STR2## Y.sub.2 is cycloalkyl, aryl, heterocyclo, carbamoyl, ##STR3## Y.sub.3 is hydroxyl, alkoxy, aryl--(CH.sub.2).sub.m --O--, mercapto, alkylthio, aryl--(CH.sub.2).sub.Type: GrantFiled: March 14, 1986Date of Patent: August 4, 1987Assignee: E. R. Squibb & Sons, Inc.Inventor: Karnail Atwal
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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
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Patent number: 4668279Abstract: Novel pyridinesulfonamide compounds containing ortho-heterocyclic substituents such as N-[(4,6-dimethoxypyrimidin-2-yl)aminocarbonyl]-2-(1H-1,2,4-triazol-1-yl)-3 -pyridinesulfonamide display utility as herbicides and plant growth regulants.Type: GrantFiled: April 22, 1985Date of Patent: May 26, 1987Assignee: E. I. Du Pont de Nemours and CompanyInventor: Morris P. Rorer
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Patent number: 4666902Abstract: Tetrahydropyridazinones of the formula I ##STR1## wherein R denotes an optionally substituted carbocyclic or heterocyclic radical, R.sup.1 denotes hydrogen; alkyl; aralkyl, which is optionally substituted in the aryl part; or acyl, and R.sup.2 denotes hydrogen; alkyl, which can optionally be substituted; or optionally substituted phenyl; and their acid addition compounds, if these can be prepared.The tetrahydropyridazinone derivatives of the formula I according to the invention and their physiologically acceptable salts exhibit useful pharmacological actions.Type: GrantFiled: June 8, 1984Date of Patent: May 19, 1987Assignee: Cassella AktiengesellschaftInventors: Gerhard Zoller, Rudi Beyerle, Melitta Just, Piero Martorana, Helmut Bohn, Rolf-Eberhard Nitz
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Patent number: 4665177Abstract: This invention relates to new tetrahydropyrimidines, to a process for their production and to their use as catalysts in the production of polyurethane plastics, including polyurethane foams.Type: GrantFiled: August 5, 1985Date of Patent: May 12, 1987Assignee: Bayer AktiengesellschaftInventors: Werner Rasshofer, Gerhard Grogler, Richard Kopp
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Patent number: 4629495Abstract: Herbicidal compounds of the formula: ##STR1## wherein A represents R.sup.1 R.sup.2 N-- (wherein R.sup.1 represents C.sub.1-8 alkyl or C.sub.2-8 alkenyl or alkynyl unsubstituted or substituted by CN, OH, C.sub.1-6 alkoxy, carboxy, C.sub.2-9 alkoxycarbonyl, aminocarbonyl optionally substituted by C.sub.1-8 alkyl or C.sub.2-8 alkenyl, C.sub.1-8 alkoxyaminocarbonyl, C.sub.1-8 alkanesulphonamidocarbonyl, --C(.dbd.O)Het, where Het represents a nitrogen-containing heterocyclic group, or one or more halogen atoms or R.sup.1 represents C.sub.3-6 cycloalkyl optionally substituted by C.sub.1-4 alkyl and R.sup.2 represents H or R.sup.1, or R.sup.1 represents C.sub.1-4 alkylthio and R.sup.2 represents H, or A represents R.sup.p (R.sup.q)--C.dbd.N-- (wherein R.sup.p represents C.sub.1-4 alkoxy or amino substituted by one or two C.sub.1-4 alkyl groups and R.sup.q represents H or C.sub.1-4 alkyl) or A represents 2-oxo-azetidin-1-yl, 2-oxo-pyrrolidin-1-yl or 2-oxo-piperidin-1-yl optionally substituted by C.sub.Type: GrantFiled: July 13, 1983Date of Patent: December 16, 1986Assignee: May & Baker LimitedInventors: Leslie R. Hatton, Edgar W. Parnell, David A. Roberts