Oxygen Bonded Directly To The Diazine Ring Patents (Class 544/123)
-
Patent number: 5714438Abstract: Herbicidal 5-substituted pyrimidine compounds and derivatives thereof of the formula: ##STR1## Herbicidal compositions containing such 5-substituted pyrimidine compounds and derivatives thereof and methods of controlling undesirable vegetation using these compounds and derivatives are also disclosed. The compounds in which XR is hydroxyl are also useful as intermediates for producing the 5-substituted pyrimidine derivatives of the invention.Type: GrantFiled: December 5, 1996Date of Patent: February 3, 1998Assignee: Zeneca LimitedInventors: David B. Kanne, Michael P. Prisbylla
-
Patent number: 5684005Abstract: A class of substituted phenylpyrimidine compounds are disclosed which are potent inhibitors of the excitatory amino acid, glutamate. Such compounds are useful in the treatment or prevention of a range of CNS disorders including cerebral ischaemic damage and epilepsy.Type: GrantFiled: June 6, 1995Date of Patent: November 4, 1997Assignee: Glaxo Wellcome Inc.Inventors: Alistair Ainslie Miller, Malcolm Stuart Nobbs, Richard Martin Hyde, Michael John Leach
-
Patent number: 5668140Abstract: Substituted 4-aminopyrimidines, processes for their preparation, and their use as pesticidesThe invention relates to substituted 4-aminopyrimidines of the formula ##STR1## in which: R.sup.1 is hydrogen, halogen, alkyl or cycloalkyl,R.sup.2 is hydrogen, alkyl, halogen, trifluoromethyl, alkoxy, haloalkoxy, alkoxyalkyl, alkylthio, alkylthioalkyl, alkylamino, dialkylamino or cycloalkylamino,R.sup.3 is hydrogen, alkyl, alkoxy, haloalkoxy, alkylthio, halogen, nitro or dialkylamino,R.sup.4 is hydrogen or optionally substituted carbamoyl;R.sup.5 is hydrogen, (C.sub.1 -C.sub.8)alkyl or (C.sub.3 -C.sub.6)cycloalkyl; andQ has the meaning defined in the description, and their salts. The invention furthermore relates to processes for their preparation and to their use as pesticides.Type: GrantFiled: June 5, 1995Date of Patent: September 16, 1997Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Schaper, Gerhard Salbeck, Heinz Ehrhardt, Peter Braun, Werner Knauf, Burghard Sachse, Anna Waltersdorfer, Manfred Kern, Peter Lummen
-
Patent number: 5663334Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.Type: GrantFiled: August 21, 1996Date of Patent: September 2, 1997Assignee: SmithKline Beecham CorporationInventors: Peter William Sheldrake, Timothy Francis Gallagher, Joseph Sisko
-
Patent number: 5658854Abstract: Acylated aminophenylureas, preparation and use as herbicides and plant growth regulatorsThe compounds of the formula I or their salts ##STR1## in which G is a radical G1, G2 or G3 ##STR2## R.sup.1 is H or alkyl, R.sup.2 is COOH, CSOH or a derivative of the carboxyl or thiocarboxyl group, of 1 to 20 carbon atoms, or acyl of the type CO-R.degree. of 1-12 carbon atoms, or an imino, hydrazone or oxime derivative of the group CO-R.degree., and R.degree. , R.sup.3a, R.sup.4a, R.sup.3b, R.sup.4b, W, X, Y and Z are as defined in claim 1, are suitable as selective herbicides and plant growth regulators in crops.The preparation is carried out in analogy to known processes (see claim 5) by way of intermediates, some of which are new, from the group consisting of benzene-sulfonamides (II), benzenesulfonyl isocyanates (IV) and benzesulfonyl chlorides (VI) and heterocyclically substituted carbamates (III), amines (V) and/or (thio)-isocyanates (XIX).Type: GrantFiled: June 30, 1994Date of Patent: August 19, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Gerhard Schnabel, Lothar Willms, Klaus Bauer, Hermann Bieringer
-
Patent number: 5648315Abstract: Compounds of the formula (I) and their salts as defined below, ##STR1## in which R.sup.1 is CO--Q--R.sup.8, where R.sup.8 .dbd.H or RR.sup.2 and R.sup.3 are H or (C.sub.1 -C.sub.4)alkyl,R.sup.4 is H, R, RO, OH, RCO, RSO.sub.2, PhSO.sub.2R.sup.5 is RSO.sub.2, PhSO.sub.2, PhCO, RNHSO.sub.2, R.sub.2 NSO.sub.2, RCO, CHO, COCOR', CW--T--R.sup.9, CW--NR.sup.10 R.sup.11, CW--N(R.sup.12).sub.2 orR.sup.4 and R.sup.5 together are the chain (CH.sub.2).sub.m B or --B.sup.1 --(CH.sub.2).sub.m1 B-- where B.dbd.SO.sub.2, CO; m=3, 4; m.sup.1 =2, 3;T and W.dbd.O, S; Q.dbd.O, S, NR.sup.13 where R.sup.13 .dbd.H, R;R.sup.6 .dbd.H, R, RO, RCO, ROCO, Hal, NO.sub.2, CN;R.sup.7 .dbd.H, CH.sub.3 ; R.sup.9 .dbd.R; R.sup.10, R.sup.11 .dbd.H, R; N(R.sup.12).sub.2 =heterocycleA=pyrimidinyl and triazinyl radical or an analog thereof,where R=(substituted) aliphatic hydrocarbon radical, are suitable as selective herbicides. They are prepared by analogous processes via sulfonamides.Type: GrantFiled: October 13, 1994Date of Patent: July 15, 1997Assignee: Hoechst Schering AgrEvo GmbHInventors: Klaus Lorenz, Lothar Willms, Klaus Bauer, Hermann Bieringer
-
Patent number: 5635495Abstract: Compounds useful in the treatment of inflammation structurally represented as ##STR1## wherein X,X.sup.1 and R groups are as herein defined.Type: GrantFiled: April 6, 1995Date of Patent: June 3, 1997Assignee: The Upjohn CompanyInventors: David R. White, Edward L. Fritzen, Jr.
-
Patent number: 5633248Abstract: A compound of the formula: ##STR1## wherein Ar.sup.1 and Ar.sup.2 independently represent an optionally substituted aromatic group; P and Q independently represent a divalent aliphatic hydrocarbon group having at least 2 carbon atoms and optionally having either oxygen or sulfur in the carbon chain; R.sup.1 and R.sup.3 independently represent --CO--R, --CONH--R (R represents a hydrocarbon group or a heterocyclic group) or a hydrocarbon group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.2 and R.sup.4 independently represent hydrogen or an alkyl group; R.sup.1 and R.sup.2 or R.sup.3 and R.sup.4, taken together with the adjacent nitrogen atom, may form a nitrogen-containing heterocyclic group; and j represents 0 or 1, or a salt thereof, has excellent GnRH-receptor antagonizing activity and is useful as a prophylactic and therapeutic agent for hormone-dependent and other diseases.Type: GrantFiled: November 21, 1995Date of Patent: May 27, 1997Assignee: Takeda Chemical Industries, Ltd.Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato
-
Patent number: 5627136Abstract: Pyridine-N-oxide-substituted salicylaldehyde and salicylic acid derivatives of the general formula I ##STR1## where R is a formyl group, a CO.sub.2 H group or a radical which can be hydrolyzed to CO.sub.2 H and the other substituents have the following meanings:R.sup.2 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio;X is nitrogen or CR.sup.13, R.sup.13 being hydrogen or halogen or together with R.sup.3 forming a 3- to 4-membered alkylene or alkenylene chain in which at least one methylene group is replaced by oxygen;R.sup.3 is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy or alkylthio, or R.sup.3 is linked with R.sup.13 as indicated above to give a 5- or 6-membered ring;Y is oxygen or sulfur;R.sup.14 -R.sup.Type: GrantFiled: November 1, 1994Date of Patent: May 6, 1997Assignee: BASF AktiengesellschaftInventors: Joachim Rheinheimer, Uwe J. Vogelbacher, Ernst Baumann, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
-
Patent number: 5616537Abstract: A condensed heterocyclic derivative of the formula (I): ##STR1## (wherein R is a hydroxyl group, R.sup.3 or R.sup.4 is an alkoxy group, W is an oxygen atom, Yn is a hydrogen atom, Z is a methine group, and A is a 5- or 6-membered heterocyclic ring which may be substituted, and a herbicide, are presented. When used for paddy field treatment, upland soil treatment and foliage treatment, the condensed heterocyclic derivative of the present invention exhibits excellent herbicidal activities against gramineous and non-gramineous weeds without adversely affecting crop plants.Type: GrantFiled: March 1, 1994Date of Patent: April 1, 1997Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Sumio Yokota, Masafumi Matsuzawa, Nobuyuki Ohba, Toshihiro Nagata, Shigehiko Tachikawa, Takeshige Miyazawa, Katsutada Yanagisawa
-
Patent number: 5604181Abstract: Herbicidal compounds of formula (I) and salts thereof, where A is --N.dbd. or --CH.dbd.; X is --OH, --OR.sup.10, --SH, --SR.sup.10, --SCN, NH.sub.2, --NHacyl, --CH.sub.2 OH, --CH.sub.2 OR.sup.9 or --CN; R.sup.1 and R.sup.2, which may be the same or different, each represent alkyl, alkoxy, haloalkyl, haloalkoxy, halo, alkylamino or dialkylamino; R.sup.3 is --CN, --COOR.sup.5, --CONR.sup.6 R.sup.7, --CSNH.sub.2, --CHO, --CH.dbd.Z, --CH(Oalkyl).sub.2, --CH.sub.2 OH, --CH.sub.2 OR.sup.9, --COSR.sup.4a, --CS.sub.2 R.sup.4a, or a substituted or unsubstituted 5- or 6-membered heterocyclic group linked via a ring carbon atom which is between two ring heteroatoms; R.sup.4 and R.sup.4a, which may be the same or different, are each H, or a substituted or unsubstituted alkyl, alkenyl, alkynyl, cycloalkyl, aryl, aralkyl or heteroaryl group; R.sup.Type: GrantFiled: March 8, 1995Date of Patent: February 18, 1997Assignee: Agrevo UK LimitedInventors: Thomas L. Hough, Peter S. Gates
-
Patent number: 5599815Abstract: Compounds represented by the formula (I) and pharmacologically acceptable salts thereof: ##STR1## These compounds have little extrapyramidal effect and thus are effective as an anti-psychotic agent having few side effects.Type: GrantFiled: December 20, 1994Date of Patent: February 4, 1997Assignee: Meiji Seika Kabushiki KaishaInventors: Yoshimasa Fukuda, Toshiro Sasaki, Yuuko Nakatani, Yasuyuki Ichimaru, Taiichiro Imanishi
-
Patent number: 5593992Abstract: Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.Type: GrantFiled: June 7, 1995Date of Patent: January 14, 1997Assignee: SmithKline Beecham CorporationInventors: Jerry L. Adams, Peter W. Sheldrake, Timothy F. Gallagher, Ravishanker Garigipati
-
Patent number: 5589478Abstract: A benzenesulfonamide derivative of the formula [I]: ##STR1## wherein Ring A and Ring B are the same or different and each substituted or unsubstituted benzene ring, Q is a single bond or a group of the formula: --O--, --S--, --SO--, --SO.sub.2 -- or --CH2--, Y is a group of the formula: --O--, --S-- or --NH--, Alk is lower alkylene group or lower alkenylene group, Z is a single bond or a group of the formula: --O-- or --NH--, R is a substituted or unsubstituted aromatic heterocyclic or aryl group, R.sup.Type: GrantFiled: December 16, 1994Date of Patent: December 31, 1996Assignee: Tanabe Seiyaku Co., Ltd.Inventors: Koichiro Yamada, K osuke Yasuda, Kohei Kikkawa, Rikako Kohno
-
Patent number: 5541186Abstract: A compound of the formula ##STR1## wherein R.sup.1 to R, R.sup.a, R.sup.b X, Y, Z, m and n have the significance given in the description, can be used as medicaments, especially for the treatment and prophylaxix of conditions which are associated with endothelin activities.Type: GrantFiled: June 27, 1994Date of Patent: July 30, 1996Assignee: Hoffmann-La Roche Inc.Inventors: Volker Breu, Kaspar Burri, Jean-Marie Cassal, Martine Clozel, Georges Hirth, Bernd-Michael L offler, Marcel M uller, Werner Neidhart, Henri Ramuz
-
Patent number: 5532203Abstract: Mixtures of a herbicidally effective amount of a pyridylsulfonylurea of formula I, ##STR1## wherein R, R.sub.1, R.sub.2 and A are as defined in claim 1, and of a herbicide-antagonistically effective amount of a sulfamoylphenylurea of formula II, ##STR2## wherein R.sub.7 to R.sub.11 and A.sub.2 are as defined in claim 1, are very suitable for controlling weeds in crops of useful plants, especially maize and sugar cane.Type: GrantFiled: May 1, 1995Date of Patent: July 2, 1996Assignee: Ciba-Geigy CorporationInventors: Werner Fory, Elmar Kerber, Manfred Hudetz
-
Patent number: 5521063Abstract: The present invention describes an assay system wherein target polynucleotide molecules are captured on a support by base-specific binding to support-bound polymers, which are themselves substantially uncharged, and the target polynucleotides can be detected on the basis of their backbone charge. The assay system may also include polycationic reporter molecules which are designed to bind to the fully charged analyte backbone, but not the uncharged (or substantially uncharged) polymer backbone. In one embodiment, the reporter molecules are composed of a polycationic moiety or tail designed to bind electrostatically to a fully charged polynucleotide, under conditions where the reporter does not bind to the less charged or uncharged binding polymer carried on the diagnostic reagent.Type: GrantFiled: February 9, 1993Date of Patent: May 28, 1996Assignee: Antivirals Inc.Inventors: James E. Summerton, Dwight D. Weller
-
Patent number: 5494888Abstract: The present invention relates to 6-chloro-2-(4,6-dimethoxypyrimidin-2-yl)oxybenzoic acid iminoester derivative of the general formula I; process of their preparation and a method for their application as herbicides: ##STR1## wherein R and Q are as defined in the specification.Type: GrantFiled: January 26, 1994Date of Patent: February 27, 1996Assignee: Lucky Ltd.Inventors: Chang U. Hur, Jin H. Cho, Ho S. Lee, Sang K. Yoo, Su M. Hong, Hong W. Kim, Jae S. Rim, Yeong T. Bae, Sang H. Chae, Jeong S. Kim, Byoung B. Lee, Hun S. Oh, Woo B. Choi
-
Patent number: 5494886Abstract: R*--O--CO--NR.sup.3 A,where R.sup.3 stands for phenyl or alkyl.The compounds of formula (II) can be obtained from the corresponding sulphochlorides.Type: GrantFiled: November 10, 1994Date of Patent: February 27, 1996Assignee: Hoechst AktiengesellschaftInventors: Heinz Kehne, Lothar Willms, Oswald Ort, Klaus Bauer, Hermann Bieringer
-
Patent number: 5474996Abstract: Novel pyrimidine derivatives of the formula ##STR1## represents: either a group: ##STR2## or a group: ##STR3## having angiotensin II inhibiting activity.Type: GrantFiled: May 22, 1992Date of Patent: December 12, 1995Assignee: Roussel UclafInventors: Jean-Claude Caille, Stanislas Didierlaurent, Jean-Paul Vevert
-
Patent number: 5470975Abstract: Novel A-II receptor antagonists have the formula ##STR1## and its isomer ##STR2## wherein R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.5, R.sub.6, R.sub.7 and R.sub.8 are as defined herein.Type: GrantFiled: January 11, 1994Date of Patent: November 28, 1995Assignee: E.R. Squibb & Sons, Inc.Inventor: Karnail Atwal
-
Patent number: 5461026Abstract: The present invention relates to novel pyridinesulfonylurea derivatives, having a herbicidal activity, which is described in the following structure of general formula (I) ##STR1## wherein, Q is Q-1, Q-2, Q-3 or Q-4 as follows; ##STR2## E is single bond or CH.sub.2 R.sup.2 is C.sub.1 -C.sub.6 alkyl substituted with 1 to 3 halogens;R.sup.1, R.sup.3, W and A are defined in the claims; and these may be an agriculturally suitable salt.Type: GrantFiled: November 29, 1993Date of Patent: October 24, 1995Assignee: Korea Research Institute of Chemical TechnologyInventors: Dae-Whang Kim, Hae Sung Chang, Jae Wook Ryu, In Ho Jo
-
Patent number: 5446152Abstract: This invention refers to heterocyclic compounds of general formula ##STR1## and their pharmacologically accepted salts. The derivatives described in this invention are active in the gastro-intestinal apparatus; in particular, they have prokinetic effects, in other words they create specific stimulation on gastro-intestinal motility, facilitating the passage of the contents of the alimentary tract, and possess anti-emetic qualities, without side effects involving the central nervous system.Type: GrantFiled: April 6, 1994Date of Patent: August 29, 1995Assignee: Alfa Wassermann S.p.A.Inventors: Claudia Baldazzi, Silvano Piani, Maria Barbanti, Egidio Marchi
-
Patent number: 5441960Abstract: The present invention relates to certain novel substituted ketones which are 1-pyrimidinylacetamide derivatives of formula I, ##STR1## set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates ##STR2## useful in the synthesis of these substituted ketones processes for preparing the substituted ketones pharmaceutical compositions containing such substituted ketones and methods for their use.Type: GrantFiled: April 8, 1993Date of Patent: August 15, 1995Assignee: Zeneca LimitedInventors: Peter R. Bernstein, Philip D. Edwards, Andrew Shaw, Royston M. Thomas, Chris A. Veale, Peter Warner, Donald J. Wolanin
-
Patent number: 5439874Abstract: The invention relates to novel substituted bicyclo[3.1.0]hexanes of the formula ##STR1## in which R.sup.1 represents, e. g., hydroxyl or alkoxy,R.sup.2 to R.sup.8 represent, e. g., hydrogen or alkyl,R.sup.9 and R.sup.10 represent, e.g., methyl or methoxy,X represents, e.g., oxygen,Y represents, e.g., oxygen or sulphur andZ represents, e.g., CH or N,as well as salts of the free acid (R.sup.1 =OH) and their further functional derivatives, and furthermore to processes and novel intermediates for their preparation, and to their use as herbicides.In addition, a novel process is described for preparing certain 2-keto-bicyclo[3.1.0]hexanes, which are required as intermediates, starting from correspondingly substituted .alpha.,.beta.-unsaturated carbonyl compounds (of the methacrolein type) and .beta.-keto acid esters (of the acetoacetic acid ester type).Type: GrantFiled: July 21, 1993Date of Patent: August 8, 1995Assignee: Bayer AktiengesellschaftInventors: Mark W. Drewes, Rolf Kirsten, Hans-Joachim Santel, Klaus Lurssen, Robert R. Schmidt
-
Patent number: 5424275Abstract: Novel biphenyl derivatives represented by the formula (I) ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, X.sup.1, X.sup.2, X.sup.3 and Y are as defined hereinafter.Type: GrantFiled: October 14, 1993Date of Patent: June 13, 1995Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsunori Hiratsuka, Toru Uekawa, Naonori Hirata, Kazuo Saito, Hiroyuki Yogai
-
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
-
Patent number: 5403816Abstract: 3-Pyrimidinyloxy-substituted picolinic acid derivatives of the formula ##STR1## and their salts are useful as herbicides against annual and perennial gramineous and broadleaf weeds while exhibiting low phytotoxicity to desired crop plants.Type: GrantFiled: April 20, 1993Date of Patent: April 4, 1995Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.Inventors: Fumiaki Takabe, Yoshihiro Saito, Masatoshi Tamaru, Shigehiko Tachikawa, Ryo Hanai
-
Patent number: 5399691Abstract: The present invention provides a substituted benzoylurea derivative having the formula (I), ##STR1## (wherein Q is a --R.sub.1 N(Z.sub.2)Z.sub.3 group or a --R.sub.2 N(Z.sub.4)COR.sub.1 N(Z.sub.2)Z.sub.3 group, R.sub.1 and R.sub.2 are respectively an alkanediyl group which may be substituted with a lower alkylthio group or a phenyl group, Z.sub.1, Z.sub.2, Z.sub.3 and Z.sub.4 are respectively a hydrogen atom or a lower alkyl group, R.sub.1 and Z.sub.2 may be bonded with each other to form a heterocyclic ring with an adjacent nitrogen atom, X is a halogen atom, a lower alkyl group or a CF.sub.3 group, and Y is a halogen atom) or its salt, effective as an antitumor agent; a method for producing the same; an antitumor composition containing the same; and an intermediate product for producing the same.Type: GrantFiled: December 7, 1992Date of Patent: March 21, 1995Assignee: Ishihara Sangyo Kaisha Ltd.Inventors: Kenji Kon, Hiroshi Okada
-
Patent number: 5397781Abstract: The present invention relates to novel 5-(.omega.-substituted amino-alkanoyl amino)pyrimidine derivatives, processes for producing the derivatives, and pharmaceutical compositions containing said derivatives. The compounds in the present invention have potent effects of inhibiting ACAT activity and lowering serum cholesterol. The compounds of the present invention are extremely useful for the treatment and/or prevention of arteriosclerosis or hyperlipidemia.Type: GrantFiled: February 11, 1993Date of Patent: March 14, 1995Assignee: Mochida Pharmaceutical Company, LimitedInventors: Kazutoshi Yanagibashi, Kiyoshi Mizuguchi, Shuhei Ohnishi, Kimihiro Murakami
-
Patent number: 5393733Abstract: This invention relates to herbicidal pyridinesulfonylureas which are highly active as preemergence and postemergence herbicides.Type: GrantFiled: April 27, 1993Date of Patent: February 28, 1995Assignee: E. I. Du Pont de Nemours and CompanyInventor: Paul H. Liang
-
Patent number: 5380701Abstract: The invention relates to 3-aryluracils of formula I ##STR1## wherein W is a group of formula ##STR2## in which the linkage to the ring nitrogen atom is through the carbon atom: R.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 haloalkyl, C.sub.3 - or C.sub.4 alkenyl or C.sub.3 - or C.sub.4 alkynyl;R.sub.2 is halogen or cyano;R.sub.3 is hydrogen or fluoro;R.sub.4 is hydrogen, halogen or C.sub.1 -C.sub.4 alkyl;R.sub.5 is C.sub.1 -C.sub.4 alkyl or C.sub.1 C.sub.4 haloalkyl;R.sub.6 to R.sub.9 are each independently of one another hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.3 -C.sub.6 alkenyl, C.sub.3 -C.sub.6 alkynyl, C.sub.1 -C.sub.4 haloalkyl or phenyl; orR.sub.6 and R.sub.7 or R.sub.8 and R.sub.9, together with the linking carbon atom, form a 3-, 4-, 5- or 6-membered ring which may be substituted by one or more C.sub.1 -C.sub.4 alkyl groups; or R.sub.7 and R.sub.9, together with the linking carbon atoms, form a 3-, 4-, 5- or 6-membered ring which may be substituted by one or more C.sub.1 -C.sub.Type: GrantFiled: October 12, 1993Date of Patent: January 10, 1995Assignee: Ciba-Geigy CorporationInventors: Paul Winternitz, Martin Zeller
-
Patent number: 5378841Abstract: Alpha-morpholino subunits and polymer compositions composed of alpha-morpholino subunits are disclosed. These subunits can be linked together by uncharged linkages, one to three atoms in length, joining the morpholino nitrogen of one subunit to the 5' exocyclic carbon of an adjacent subunit. Each subunit contains a purine or pyrimidine base-pairing moiety effective to bind by hydrogen bonding to a specific base or base-pair in a target polynucleotide. The polymers of the instant invention can be used in place of standard RNA or DNA oligomers. For example, the target-specific polymers of the invention can be used in a variety of diagnostic assays for detection of RNA or DNA having a given target sequence. Further, the polymers of the invention also have potential use as therapeutic agents.Type: GrantFiled: June 8, 1993Date of Patent: January 3, 1995Assignee: Antivirals Inc.Inventors: James E. Summerton, Dwight D. Weller, Eugene P. Stirchak
-
Patent number: 5378707Abstract: Aryl-propyl-aminic compounds having the following formula ##STR1## have high activity and are useful in the agricultural field as fungicides.Type: GrantFiled: November 22, 1993Date of Patent: January 3, 1995Assignee: Minestero Dell' Universita 'e Della Ricerca Scientifica e TechnologicaInventors: Giovanni Camaggi, Lucio Filippini, Marilena Gusmeroli, Carlo Garavaglia, Luigi Mirenna
-
Patent number: 5376620Abstract: Disclosed are a sulfonamide compound represented by the following formula (I): ##STR1## wherein Y represents a lower akyl group, a lower alkenyl group, a lower alkynyl group, a halo-lower alkyl group, a cyano-lower alkyl group or --C(CH.sub.3).sub.2 (OR.sup.1) where R.sup.1 represents a lower akyl group, a lower alkenyl group, a lower alkynyl group, a halo-lower alkyl group or a cyano-lower alkyl group; Q represents a substituted or unsubstituted pyridyl group or --NR.sup.2 R.sup.3 where R.sup.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group; and R.sup.3 represents a lower alkyl group, a lower alkenyl group, a lower alkynyl group, a phenyl group or a benzyl group; or R.sup.2 and R.sup.3 may be combined to form a cycloamino group; X represents an oxygen atom or a sulfur atom; and Z represents a nitrogen atom or --CH.dbd. group;processes for preparing the same and a herbicide containing the same as an active ingredient(s).Type: GrantFiled: April 2, 1993Date of Patent: December 27, 1994Assignee: Ube Industries, Ltd.Inventors: Takaaki Abe, Yuji Akiyoshi, Hiroshi Shiraishi, Ikuo Shiraishi, Mikio Kojima, Takashi Hayama, Takaaki Kuwata
-
Patent number: 5356863Abstract: The present invention relates to an uracil derivative represented by the formula (1): ##STR1## in which R.sup.1 represents hydrogen, alkyl or haloalkyl; R.sup.2 represents haloalkyl; R.sup.3 represents hydrogen, alkyl, haloalkyl, hydroxymethyl, halogen or nitro; R.sup.4 represents hydrogen or halogen; R.sup.5 represents hydrogen, halogen, nitro or cyano; X represents oxygen or sulfur: provided that the case where both of Da and Db represent hydrogen is excluded and a herbicide containing the same. The compound can be safely applied to important crops and shows high effect against many weeds in a low amount.Type: GrantFiled: October 21, 1993Date of Patent: October 18, 1994Assignee: Nissan Chemical Industries, Ltd.Inventors: Jun Satow, Kenzou Fukuda, Kaoru Itoh, Hiroshi Kita, Yasuo Kawamura, Koichi Suzuki, Tsutomu Nawamaki, Shigeomi Watanabe, Toshiharu Endo, Kimihiro Ishikawa
-
Patent number: 5346901Abstract: Compounds of the formula: ##STR1## wherein R.sup.1 is H, C.sub.1 -C.sub.3 alkyl, C.sub.3 -C.sub.5 cycloalkyl or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.2 is H, C.sub.1 -C.sub.6 alkyl optionally substituted by OH, C.sub.1 -C.sub.3 alkoxy or C.sub.3 -C.sub.6 cycloalkyl, or C.sub.1 -C.sub.3 perfluoroalkyl; R.sup.3 is C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.6 alkynyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.1 -C.sub.6 perfluoroalkyl or (C.sub.3 -C.sub.6 cycloalky)C.sub.1 -C.sub.6 alkyl; R.sup.4 taken together with the nitrogen atom to which it is attached completes a pyrrolidinyl, piperidino, morpholino, or 4-N-(R.sup.6)-piperazinyl group; R.sup.5 is H, C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.3 alkoxy, NR.sup.7 R.sup.8, or CONR.sup.7 R.sup.8 ; R.sup.6 is H, C.sub.1 -C.sub.6 alkyl, (C.sub.1 -C.sub.3 alkoxy) C.sub.2 -C.sub.6 alkyl, hydroxy C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 N)C.sub.2 -C.sub.6 alkyl, (R.sup.7 R.sup.8 NCO)C.sub.1 -C.sub.6 alkyl, CONR.sup.7 R.sup.8, CSNR.sup.7 R.sup.Type: GrantFiled: June 29, 1993Date of Patent: September 13, 1994Assignee: Pfizer Inc.Inventors: Andrew S. Bell, David Brown, Nicholas K. Terrett
-
Patent number: 5328916Abstract: New heterocyclic compounds of the formulaX--W--CR.sup.1 R.sup.2 --CO--Y--NR.sup.3 --CHR.sup.4 --CR.sup.5 --CH.sub.2 --(CR.sup.6 R.sup.7).sub.r --Z--Het Iin which R.sup.1 to R.sup.7, W, X, Y, Z, r and Het have the meanings defined herein, and the salts thereof, inhibit the activity of human plasma renin.Type: GrantFiled: May 2, 1991Date of Patent: July 12, 1994Assignee: Merck Patent Gesellschaft mit Beschrankter HaftungInventors: Peter Raddatz, Claus J. Schmitges, Klaus-Otto Minck
-
Patent number: 5324710Abstract: Compounds of the formula I or their salts ##STR1## in which R.sup.1 to R.sup.6, W, X, a and b are as defined in claim 1 and L is a heterocyclic or isocyclic aromatic radical having 5 to 6 ring atoms, which can be condensed with an aromatic or non-aromatic 5- or 6-membered ring, where the radical can be unsubstituted or substituted, and a, b and c independently of one another are 0 or 1, are suitable as herbicides, plant growth regulators and fungicides. They can be prepared by the processes defined herein, it being possible in some cases to use novel intermediates.Type: GrantFiled: April 21, 1992Date of Patent: June 28, 1994Assignee: Hoechst AktiengesellschaftInventors: Oswald Ort, Lothar Willms, Klaus Bauer, Hermann Bieringer, Arno Schulz, Burkhard Sachse, Peter Braun
-
Patent number: 5314892Abstract: Fungicidal compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CH; and X is an optionally substituted 3- to 6-membered heterocyclic ring containing at least one trivalent nitrogen atom by which it is attached to the central pyrimidine ring.Type: GrantFiled: October 6, 1992Date of Patent: May 24, 1994Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting, David P. Bacon
-
Patent number: 5310767Abstract: The present invention relates to novel tetramethylpiperidine compounds of the formula (I) ##STR1## in which R.sub.1 is e.g. hydrogen or methyl, R.sub.2 and R.sub.3 are e.g. --(CH.sub.2).sub.2 --, R.sub.4 is e.g. --CO--, --COCO-- or --COCH.sub.2 CO--, n is e.g. 1 and R.sub.5 is e.g. hydrogen or allyl.These compounds are suitable for use as light stabilizers, heat stabilizers and oxidation stabilizers for organic materials.Type: GrantFiled: December 10, 1992Date of Patent: May 10, 1994Assignee: Ciba-Geigy CorporationInventors: Valerio Borzatta, Graziano Vignali
-
Patent number: 5300640Abstract: A novel herbicidal pyrimidine derivative represented by the formula ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.4, Y.sup.1, Y.sup.2, Y.sup.3, X and Z are as defined herein.Type: GrantFiled: December 19, 1991Date of Patent: April 5, 1994Assignee: Sumitomo Chemical Company, LimitedInventors: Mitsumori Hiratsuka, Naonori Hirata, Kazuo Saito, Hideyuki Shibata
-
Patent number: 5292740Abstract: The novel sulfonamides of formula I, ##STR1## in which the symbols R.sup.1 -R.sup.9, R.sup.a, R.sup.b, X, Y and n have the significance given in the description and salts thereof can be used for the treatment of circulatory disorders, especially hypertension, ischemia, vasopasms and angina pectoris.Type: GrantFiled: June 9, 1992Date of Patent: March 8, 1994Assignee: Hoffmann-La Roche Inc.Inventors: Kaspar Burri, Martine Clozel, Walter Fischli, Georges Hirth, Bernd-Michael Loffler, Werner Neidhart, Henri Ramuz
-
Patent number: 5290755Abstract: Salicylic acid derivatives and sulfur analogs thereof of the formula I, ##STR1## wherein the substituents are herein below defined.Type: GrantFiled: August 4, 1992Date of Patent: March 1, 1994Assignee: BASF AktiengesellschaftInventors: Uwe J. Vogelbacher, Joachim Rheinheimer, Thomas Saupe, Norbert Meyer, Matthias Gerber, Karl-Otto Westphalen, Helmut Walter
-
Patent number: 5284945Abstract: The process according to the invention for the preparation of herbicidal pyridylsulfonylureas of the formula (I) ##STR1## in which R.sup.1 to R.sup.5 and X are as defined in claim 1 comprises the reaction of the zwitterion (II) with the amino heterocycle (III) ##STR2## The novel zwitterionic 1,1,3-trioxo-1,2,4-thiadiazolo[4,5-a]pyridines can be obtained according to the invention by the reaction of phosgene with compounds IV, or the reaction of phosgene with compounds V ##STR3## in the presence of an alkyl isocyanate.Type: GrantFiled: February 26, 1993Date of Patent: February 8, 1994Assignee: Hoechst AktiengesellschaftInventor: Heinz Kehne
-
Patent number: 5280009Abstract: Pyrimidine derivatives of the Formula Ia or Ib ##STR1## where the substituents have the following meanings: R.sup.1 is hydrogen or alkyl;A is a substituted or unsubstituted bi- or tricyclic carbo- or heterocyclic radical which may contain one or several double bonds;R.sup.5 is H or alkyl;X is halogen, alkyl, haloalkyl, alkoxy, haloalkoxy, alkylthio or haloalkylthio; and addition salts thereof with organic or inorganic acids and the use of said pyrimidine derivative to control undesirable plant growth.Type: GrantFiled: July 16, 1992Date of Patent: January 18, 1994Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Klaus Ditrich, Karl-Otto Westphalen, Matthias Gerber, Helmut Walter
-
Patent number: 5276007Abstract: Substituted sulfonylureas of the general formula I ##STR1## where n and m are each 0 or 1, andR.sup.1 is hydrogen, alkyl, alkenyl or alkynyl;R.sup.2 is halogen or trifluoromethyl when m is 0, or, when m is 1, alkyl, alkenyl or alkynyl and, when X is 0 or S and m is 1, is trifluoromethyl or chlorodifluoromethyl;X is 0, S or N--R.sup.4, where R.sup.4 is hydrogen or alkyl;R.sup.3 is hydrogen, halogen, alkyl, haloalkyl or alkoxy;A is haloalkyl, halogen or ##STR2## where Z is oxygen or alkylimino N--R.sup.6 ;R.sup.5 is hydrogen, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl, alkenyl or alkynyl;R.sup.6 is hydrogen, alkyl, or together with R.sup.5 is a C.sub.4 -C.sub.6 -alkylene chain, where one methylene may be replaced by an oxygen atom or a C.sub.1 -C.sub.4 -alkylimino group, andR.sup.7 is hydrogen or halogen,and environmentally tolerated salts thereof, processes and intermediates for the manufacture of compounds I, and their use as herbicides and bioregulators.Type: GrantFiled: February 19, 1991Date of Patent: January 4, 1994Assignee: BASF AktiengesellschaftInventors: Gerhard Hamprecht, Horst Mayer, Karl-Otto Westphalen, Bruno Wuerzer, Matthias Gerber, Klaus Grossmann, Wilhelm Rademacher
-
Patent number: 5264440Abstract: Compounds having the formula (I): ##STR1## in which any two of K, L and M are nitrogen and the other is CE; X and Y are independently hydrogen, halogen, C.sub.1-4 alkyl, C.sub.3-6 cycloalkyl, C.sub.2-4 alkenyl, C.sub.2-4 alkynyl, C.sub.2-4 alkynyloxy, phenyl, benzyloxy, cyano, isocyano, isothiocyanato, nitro, NR.sup.1 R.sup.2, NR.sup.1 OR.sup.2,N.sub.3, NHCOR.sup.1, NR.sup.1 CO.sub.2 R.sup.2, NHCONR.sup.1 R.sup.2, N.dbd.CHNR.sup.1 R.sup.2, NHSO.sub.2 R.sup.1, OR.sup.1, OCOR.sup.1, OSO.sub.2 R.sup.1, SR.sup.1, SOR.sup.1, SO.sub.2 R.sup.1, SO.sub.2 OR.sup.1, SO.sub.2 NR.sup.1 R.sup.2, COR.sup.1, CR.sup.1 .dbd.NOR.sup.2, CHR.sup.1 CO.sub.2 R.sup.2, CO.sub.2 R.sup.1, CONR.sup.1 R.sup.2, CSNR.sup.1 R.sup.2, CH.sub.3 O.sub.2 C.C:CH.OCH.sub.Type: GrantFiled: July 20, 1992Date of Patent: November 23, 1993Assignee: Imperial Chemical Industries PLCInventors: John M. Clough, Christopher R. A. Godfrey, Ian T. Streeting, Rex Cheetham
-
Patent number: 5254558Abstract: The present invention relates to certain novel substituted heterocycles which are 1-pyrimidinylacetamide compounds of formula I, set out herein, which are inhibitors of human leukocyte elastase (HLE), also known as human neutrophil elastase (HNE), making them useful whenever such inhibition is desired, such as for research tools in pharmacological, diagnostic and related studies and in the treatment of diseases in mammals in which HLE is implicated. The invention also includes intermediates useful in the synthesis of these substituted heterocycles, processes for preparing the substituted heterocycles, pharmaceutical compositions containing such substituted heterocycles and methods for their use.Type: GrantFiled: August 14, 1992Date of Patent: October 19, 1993Assignee: Imperial Chemical Industries PLCInventors: Peter R. Bernstein, Philip D. Edwards, Royston M. Thomas, Chris A. Veale, Peter Warner, Donald J. Wolanin
-
Patent number: 5250530Abstract: Aminopyrimidine derivatives, their preparation, and agents containing them, and their use as fungicides comprising ##STR1## in which R.sup.1 is alkyl, alkoxyalkyl, alkylthioalkyl, cycloalkyl, alkenyl, alkynyl, cycloalkylalkyl, substituted aminoalkyl, phenyl, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl or phenoxyphenoxyalkyl, R.sup.2, R.sup.3 and R.sup.4 are H, alkyl, or phenyl, R.sup.5 is H, alkyl, cycloalkyl, cycloalkylalkyl, haloalkyl, alkoxy, alkylthio, alkoxyalkyl, R.sup.7 R.sup.8 N-,alkylthioalkyl, R.sup.7 R.sup.8 N-alkyl, halogen, alkenyl, alkynyl, phenyl, phenoxy, phenylalkyl, phenoxyalkyl, phenylmercaptoalkyl, phenylmercapto, phenylalkoxy or phenylalkylthio, R5 is H, alkyl, alkyloxy, alkenyloxy, alkynyloxy, alkylthio, halogen, or phenyl or R.sup.5 and R.sup.6 together form a chain, and R.sup.7 and R.sup.8 are H, alkyl, alkoxyalkyl, hydroxyalkyl, alkylthioalkyl, alkenyl, substituted formyl, phenyl or phenylalkyl, or R.sup.7 or R.sup.Type: GrantFiled: July 9, 1990Date of Patent: October 5, 1993Assignee: Hoechst AktiengesellschaftInventors: Wolfgang Giencke, Burkhard Sachse, Heinrich Wicke