Chalcogen And Acyclic Nitrogen Bonded Directly To The Same Carbon Patents (Class 546/291)
  • Patent number: 5180831
    Abstract: Quaternary pyridinium compounds, their use in inhibiting acetylcholinesterase, their roles in the prophylaxis and treatment of organophosphate poisoning, their roles in anticholinesterase therapy and their roles as agents mimicking or opposing the actions of the natural neurotransmitter acetylcholine.
    Type: Grant
    Filed: August 10, 1990
    Date of Patent: January 19, 1993
    Assignee: Georgia Tech Research Corporation
    Inventors: James C. Powers, Sheldon W. May, Maria A. Hernandez, Steve Thornton, Jan Glinski
  • Patent number: 5177089
    Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydroben or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.
    Type: Grant
    Filed: July 25, 1990
    Date of Patent: January 5, 1993
    Assignee: Eisai Co., Ltd.
    Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
  • Patent number: 5166162
    Abstract: The invention concerns a compound of formula (I) ##STR1## in which: R represents cycloalkyl, bicycloalkyl or polycycloalkyl,X represents oxygen or sulfur, andR1 represents alkyl, cycloalkyl, bicycloalkyl, or polycycloalkyl.Medicaments thereof and use of same is useful in treating a circulatory ailment related to arterial hypertension or peripheral or cerebral oedema.
    Type: Grant
    Filed: January 24, 1992
    Date of Patent: November 24, 1992
    Assignee: Adir et Compagnie
    Inventors: Bernard Masereel, Bernard Pirotte, Marc Schynts, Jacques Delarge
  • Patent number: 5157123
    Abstract: Site-specific heterobifunctional crosslinkers of the formula:X--COCH(NH.sub.2)--Y--Zwhere X is a carbonyl reactive group, Y is a variable length spacer, and Z is a thiol reactive group, are useful for the specific labelling of biomolecules or bioaffecting molecules.
    Type: Grant
    Filed: March 13, 1989
    Date of Patent: October 20, 1992
    Assignee: Georgetown University
    Inventors: Jane J. Zara, Richard D. Wood, Reinhard Bredehorst, Carl-Wilhelm Vogel
  • Patent number: 5153212
    Abstract: 2-adamantyl-4-isothiazoline-3-one has the formula ##STR1## wherein R.sub.1 and R.sub.2, each independently, represent hydrogen or halogen,or R.sub.1 and R.sub.2, taken together, form a polymethylene chain having 3-4 carbon atoms, optionally substituted by lower alkyl or halogen,or R.sub.1 and R.sub.2, taken together, form a pyridine ring with the double bond of the 4-isothiazoline-3-one ring andAda represents 1'-adamantyl, 2'-adamantyl or 1'-adamantyl methyl, and its mineral or organic acid salt.The compound is useful as an antibacteria, antialgae or antifungus agent in various industrial fields.
    Type: Grant
    Filed: June 3, 1991
    Date of Patent: October 6, 1992
    Assignee: Centre International de Recherches Dermatoglogiques (C.I.R.D.)
    Inventors: Braham Shroot, Jean Maignan, Rainer Schmidt
  • Patent number: 5151436
    Abstract: Therapeutically useful thioformamide derivatives of the formula: ##STR1## wherein R represents alkyl, Het represents pyrid-3-yl, isoquinolin-4-yl, tetrahydroquinolin-3-yl, quinolin-3-yl, pyridazin-4-yl, pyrimid-5-yl, thiazol-5-yl, thieno[2,3-b]-pyridin-5-yl, pyrazin-2-yl, indol-3-yl and thieno[3,2-b]-pyridin-6-yl, Y represents ethylene, methylene or a valency bond, and X represents carbonyl, hydroxymethylene, >C.dbd.NOR.sup.1, >C.dbd.NN(R.sup.1).sub.2 or >C.dbd.NN(R.sup.1)CON(R.sup.1).sub.2 in which R.sup.1 represents hydrogen or optionally substituted alkyl, benzyl, phenethyl, 1-naphthylmethyl, 2-naphthylmethyl or pyrid-3-ylmethyl, or two R.sup.1 substituents on the same nitrogen atom may together form an optionally substituted alkylene radical chain and salts thereof, processes for their preparation and compositions containing them are described.
    Type: Grant
    Filed: August 23, 1990
    Date of Patent: September 29, 1992
    Assignee: Rhone-Poulenc Sante
    Inventors: David C. Cook, Terance W. Hart, Iain M. Mc Lay, Malcolm N. Palfreyman, Brian W. Sharp, Roger J. A. Walsh
  • Patent number: 5149359
    Abstract: The present invention relates to derivatives of 3,4-dehydropiperidin-5-one having herbicidal activity. The derivatives have the formula ##STR1## as defined in the claims. The present invention further relates to a herbicidal composition and a method for controlling weeds which grow among agricultural crops.
    Type: Grant
    Filed: February 21, 1990
    Date of Patent: September 22, 1992
    Assignee: Agrimont S.p.A.
    Inventors: Giovanni Camaggi, Giovanni Meazza, Ciro Preziuso
  • Patent number: 5132314
    Abstract: Anthelmintically active compounds of formula I are described ##STR1## in which R.sub.1 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 thioalkyl, C.sub.1 -C.sub.2 haloalkyl, nitro, C.sub.1 -C.sub.2 alkoxy, or the group SO.sub.n R in which R is C.sub.1 -C.sub.2 alkyl or phenyl and n is 0, 1 or 2;R.sub.2 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.3 is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.4 is hydrogen or C.sub.1 -C.sub.2 alkyl;R.sub.5 is hydrogen, halogen or C.sub.1 -C.sub.5 alkyl;R.sub.6 is hydrogen, halogen or C.sub.1 -C.sub.5 alkyl;R.sub.7 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, nitro, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.8 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.sub.2 haloalkoxy or C.sub.1 -C.sub.2 alkoxy;R.sub.9 is hydrogen, halogen, C.sub.1 -C.sub.2 alkyl, C.sub.1 -C.sub.2 haloalkyl, C.sub.1 -C.
    Type: Grant
    Filed: October 25, 1991
    Date of Patent: July 21, 1992
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Maienfisch, Christof Hildenbrand, Jean-Claude Gehret
  • Patent number: 5128474
    Abstract: An aminocarbonyl-substituted pyridinesulfinic acid intermediate for production of an herbicide having formula (V): ##STR1## wherein R.sub.3 and R.sub.4 are selected from the group consisting of hydrogen and alkyl groups, or a salt thereof. The aminocarbonyl-substituted pyridinesulfinic acid or salt thereof is useful as the precursor of aminosulfonyl-substituted pyridinecarbonic acid amide, which in turn is useful as the starting material for agricultural chemicals, medicine, etc.
    Type: Grant
    Filed: July 27, 1990
    Date of Patent: July 7, 1992
    Assignee: Ishihara Sangyo Kaisha Ltd.
    Inventors: Takahiro Haga, Yasuhiro Tsujii, Tatsuo Isogai, Shigeo Murai, Hisayoshi Jonishi, Tokiya Kimura, Hiroshi Sasaki, Takao Awazu, Toshihiro Tanaka
  • Patent number: 5125956
    Abstract: Disclosed herein are herbicidal pyridine compounds substituted at the 2- or 6-position with an OR.sub.2 moiety where R.sub.2 is hydrogen, lower alkyl, halomethyl, lower cyanoalkyl, alkenyl or alkynyl, as well as herbicidal compositions and herbicidal use of these compounds.
    Type: Grant
    Filed: February 25, 1991
    Date of Patent: June 30, 1992
    Assignee: Monsanto Company
    Inventors: Donald E. Korte, Len F. Lee
  • Patent number: 5120752
    Abstract: Certain carbocyclic aryl- and heterocyclic aryl- substituted cyclopropyl N-hydroxyureas, N-hydroxy-carboxamides, and N-acyl-N-hydroxyamines inhibit 5- and/or 12-lipoxygenase and are useful in the treatment of inflammatory disease states.
    Type: Grant
    Filed: December 6, 1990
    Date of Patent: June 9, 1992
    Assignee: Abbott Laboratories
    Inventors: Dee W. Brooks, Karen E. Rodriques, Bruce W. Horrom, Hormoz Mazdiyasni
  • Patent number: 5116848
    Abstract: Certain N-2,6-dialkyl- or N-2,6-dialkoxphenyl-N'-diarylalkylurea compounds are potent inhibitors of the enzyme acyl CoA:cholesterol acyltransferase (ACAT), and are thus useful agents for the treatment of hypercholesterolemia or atherosclerosis with urea and thiourea compounds.
    Type: Grant
    Filed: March 30, 1988
    Date of Patent: May 26, 1992
    Assignee: Warner-Lambert Company
    Inventor: Bharat K. Trivedi
  • Patent number: 5112981
    Abstract: There are described compounds of the formula ##STR1## where n is 1, 2 or 3;R.sub.1 is hydrogen, formyl, loweralkylcarbonyl, arylloweralkylcarbonyl, loweralkyl, arylloweralkyl, ##STR2## R.sub.5 and R.sub.6 being independently loweralkyl or alternatively the group ##STR3## taken as a whole is ##STR4## R.sub.2 is hydrogen, loweralkyl, loweralkenyl, arylloweralkyl, --CH.sub.2 C.tbd.CH, ##STR5## R.sub.7 and R.sub.8 being independently loweralkyl or alternatively the group ##STR6## taken as a whole is ##STR7## R.sub.3 is hydrogen or loweralkyl; and R.sub.4 is hydrogen or loweralkyl;which compounds are useful as analgesic agents and also for treating various memory dysfunctions.
    Type: Grant
    Filed: June 5, 1991
    Date of Patent: May 12, 1992
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Richard C. Effland, David M. Fink
  • Patent number: 5112386
    Abstract: Acrylic acid derivatives having the formula (I): ##STR1## and stereoisomers thereof, wherein W is R.sup.1 O.sub.2 C--C.dbd.CH--ZR.sup.2, R.sup.1 and R.sup.2 are alkyl or fluoroalkyl groups, and Z is oxygen or sulphur, A, B, D and E are hydrogen, halogen, hydroxy or optionally substituted alkyl, alkoxy, aralkyl, arylalkoxy, alkenyl, alkynyl, aryl, aryloxy, arylthio, heteroaryloxy, heteroarylthio, acyloxy, amino, arylazo or acylamino, nitro, cyano, --CO.sub.2 R.sup.3, --CONR.sup.3 R.sup.4, --COR.sup.3, --CR.sup.3 .dbd.NR.sup.4, --N.dbd.CR.sup.3 R.sup.4 --S(O).sub.n R.sup.3 groups; any two of the groups, A, B, D and E, when they are in adjacent positions on the ring, optionally join to form a fused ring, n is 0, 1 or 2; and R.sup.3 and R.sup.4 are hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, alkenyl, alkynyl or optionally substituted aryl or aralkyl; and metal complexes thereof. These compounds are useful as fungicides, insecticides, nematicides or plant growth regulators.
    Type: Grant
    Filed: December 30, 1988
    Date of Patent: May 12, 1992
    Assignee: Imperial Chemical Industries PLC
    Inventors: Anthony Vivienne, John M. Clough, Paul deFraine, Christopher R. A. Godfrey, Patrick J. Crowley, Kenneth Anderton
  • Patent number: 5104883
    Abstract: Thioformamide derivatives of the formula: ##STR1## wherein: R represents alkyl; A represents an optionally substituted phenyl or heteroaromatic group; R.sup.1 represents hydrogen, alkyl, cyano, carboxyl, formyl, carbamoyl, alkoxycarbonyl or a group --(CH.sub.2).sub.n OR.sup.2, --(CH.sup.2).sub.n SR.sup.2, --(CH.sub.2).sub.n N(R.sup.2).sub.2, --CH.dbd.CHR.sup.3, --CH.dbd.NOR.sup.4, --CONHR.sup.5, or --COR.sup.6 ; R.sup.2 represents hydrogen, alkyl, alkanoyl, aryl, aryl (CH.sub.2).sub.n -- or arylCO--, or, when attached to nitrogen, two R.sup.2 groups may together represent alkylene; R.sup.3 represents hydrogen; alkyl, alkanoyl, carboxyl, carbamoyl, cyano, aryl, arylCO--, aryl(CH.sub.2).sub.n --, or aryl (CH.sub.2).sub.n CO--; R.sup.4 represents hydrogen, alkyl, aryl, aryl (CH.sub.2).sub.n -, optionally substituted alkyl, alkenyl, amino or carbamoyl N,N-disubstituted by alkylene; R.sup.5 represents alkyl, aryl, or aryl (CH.sub.2).sub.n -- or an amino acid residue; R.sup.6 represents alkyl, aryl, or aryl (CH.
    Type: Grant
    Filed: January 5, 1990
    Date of Patent: April 14, 1992
    Assignee: May & Baker Limited
    Inventors: Malcolm N. Palfreyman, Nigel Vicker, Roger J. A. Walsh
  • Patent number: 5100460
    Abstract: Herbicides of formula: ##STR1## in which: n=0,1, 2f=0,1A is chosen from the groups ##STR2## in which: Ar is chosen from the groups ##STR3## B is chosen from optionally substituted C.sub.1 -C.sub.10 alkyl and C.sub.3 -C.sub.
    Type: Grant
    Filed: July 13, 1989
    Date of Patent: March 31, 1992
    Assignee: Rhone-Poulenc Agrochimie
    Inventors: Philippe Desbordes, Michel Euvrard
  • Patent number: 5089043
    Abstract: A heterocyclic oxy-phenoxyacetic acid derivative of the formula: ##STR1## , or its salt, which is useful as a herbicide.
    Type: Grant
    Filed: November 6, 1990
    Date of Patent: February 18, 1992
    Assignee: Shionogi & Co., Ltd.
    Inventors: Yoshio Hayase, Kohei Matsumoto, Kazuo Kamei, Kinya Ide, Toshio Takahashi
  • Patent number: 5079361
    Abstract: Cross-linking reagents which are highly specific for sulphydryl groups and react with thiols at an excellent rate. The essential feature of the reagents is at least one vinyl group conjugated with an armoatic nitrogen heterocycle. Particular examples include vinyl pyridines, vinyl pyrimidines and vinyl triazines.
    Type: Grant
    Filed: September 9, 1988
    Date of Patent: January 7, 1992
    Assignee: Celltech Limited
    Inventors: Rikki P. Alexander, Michael A. W. Eaton, Thomas A. Millican, Richard C. D. Titmas
  • Patent number: 5079366
    Abstract: The invention provides novel amino acids and peptides containing them which comprise a dihydropyridine.revreaction.pyridinium salt-type redox system and which provide site-specific and sustained delivery of pharmacologically active peptides to the brain. These new amino acids contain a redox system appended directly or via an alkylene bridge to the carbon atom adjacent to the carboxyl carbon and may be incorporated into a peptide chain at a variety of positions, including non-terminal positions.
    Type: Grant
    Filed: October 4, 1989
    Date of Patent: January 7, 1992
    Assignee: University of Florida
    Inventor: Nicholas S. Bodor
  • Patent number: 5077409
    Abstract: Methods of preparing bis-aryl amide and urea compounds of the general formula: ##STR1## wherein x is a divalent amide or urea substituent and Y is a nitrogen containing heterocycle, which compounds are inhibitors of platelet activating factor.
    Type: Grant
    Filed: May 4, 1990
    Date of Patent: December 31, 1991
    Assignee: American Cyanamid Company
    Inventor: Allan Wissner
  • Patent number: 5066657
    Abstract: A crotonic acid amide derivative represented by formula (I): ##STR1## wherein X.sub.1, X.sub.2, X.sub.3, X.sub.4, and X.sub.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted lower alkyl group, a lower haloalkyl group, a lower haloalkoxy group, a nitro group, a substituted or unsubstituted lower alkanesulfonyl group, a substituted or unsubstituted alkanesulfonyloxy group, a substituted or unsubstituted benzenesulfonyl group, a substituted or unsubstituted benzenesulfonyloxy group, a substituted or unsubstituted phenoxy group, a substituted or unsubstituted benzyloxy group, a dialkylamino group, a mono- or di-lower alkanesulfonylamino group, a substituted or unsubstituted lower alkythio group, a --SO.sub.2 R.sub.1 wherein R.sub.1 represents a lower alkyl group or a lower haloalkyl group, a lower alkoxycarbonyloxy group, a substituted or unsubstituted alkoxycarbonyl group, a --CH.dbd.N--OR.sub.
    Type: Grant
    Filed: May 8, 1990
    Date of Patent: November 19, 1991
    Assignee: SDS Biotech K.K.
    Inventors: Shunji Hayashi, Satoshi Yamanaka, Sayoko Kawaguchi, Teruhiko Ishii, Toshiya Kimata, Naoaki Misu
  • Patent number: 5055582
    Abstract: This invention relates to a process for preparing useful thromboxane A.sub.2 inhibiting (.+-.)7-[3.alpha.-[1-[[(phenylamino)thioxomethyl]hydrazono]ethyl]-1.alpha. ,4.alpha.-bicyclo[2.2.1]hept-2.beta.-yl]-heptenoic acids and useful derivatives thereof from (.+-.)octahydro-1.alpha.-methyl-3a.alpha.,7a.alpha.-4.alpha.,7.alpha.-meth ano-2H-inden-2-ones.
    Type: Grant
    Filed: December 13, 1988
    Date of Patent: October 8, 1991
    Assignee: National Research Development Corporation
    Inventors: Robert B. Garland, Masateru Miyano
  • Patent number: 5047410
    Abstract: New pharmacologically active amidino and guanidino derivatives which are 5-HT.sub.3 receptor antagonists useful as antiemetic, gastric prokinetic and antimigrainic agents of the following general formula (I) ##STR1## , wherein the substituents are defined hereinbelow, which compounds are 5-HT.sub.3 receptor antagonists useful as antiemetic gastric prokinetic and antimigraine agents, inter alia.
    Type: Grant
    Filed: July 12, 1989
    Date of Patent: September 10, 1991
    Assignee: Istituto de Angeli S.p.A.
    Inventors: Arturo Donetti, Marco Turconi, Massimo Nicola, Rosamaria Micheletti
  • Patent number: 5047417
    Abstract: A butenoic or propenoic acid derivative having the following formula in which G is an aryl or a heterocyclic ring, R11 and R12 are hydrogen or an alkyl, X is sulfur or oxygen, R2 and R3 are hydrogen, an substituent such as an alkyl and J is pyridyl or phenyl having substituents and a heterocyclic ring may be formed between R2, R3 and J is provided here and is useful in the pharmacological field.
    Type: Grant
    Filed: May 19, 1989
    Date of Patent: September 10, 1991
    Assignee: Eisai Co. Ltd.
    Inventors: Norio Minami, Fumihiro Ozaki, Keiji Ishibashi, Yasuhiro Kabasawa, Megumi Ikemori, Toshiaki Ogawa, Takanori Kawamura
  • Patent number: 5047535
    Abstract: The invention relates to novel compounds which are suited for the production of multilayer films which have piezoelectric, and pyroelectric properties, and which provide second harmonic generation. The novel compounds are amphiphilic and it is possible to prepare from same polar single-layer and multi-layer films by depositing them on a substrate. When such substrate is a solid support, polar Z-type Langmuir-Blodgett films are obtained. Upon compression of films of such compounds, at an air/water interface, stable Langmuir monolayers are formed.
    Type: Grant
    Filed: August 5, 1987
    Date of Patent: September 10, 1991
    Assignee: Yeda Research and Development Company Limited
    Inventors: Meir Lahav, Leslie Leiserowitz, Jacob Sagiv, Ronit Popovitz-Biro, Karlheinz Hill, Ehud Landau
  • Patent number: 5041452
    Abstract: Novel diamides having a nitrogen-containing heterocyclic moiety such as pyridyl are disclosed that are useful for improving feed utilization efficiency of ruminants and for improving lactation of lactating ruminants.
    Type: Grant
    Filed: September 28, 1989
    Date of Patent: August 20, 1991
    Assignee: Eastman Kodak Company
    Inventor: Alan W. White
  • Patent number: 5023334
    Abstract: This invention concerns a process for killing internal parasites, especially nematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I: ##STR1## Certain of the compounds of Formula I are novel and in further embodiments of the invention provide novel compounds and compositions for use in the process of the invention. The compounds are readily prepared by conventional chemical reactions. Various pyridinyl acylhydrazones of Formula I demonstrate broad-spectrum anthelmintic activity in sheep upon oral and/or parenteral administration.
    Type: Grant
    Filed: September 1, 1989
    Date of Patent: June 11, 1991
    Assignee: The Upjohn Company
    Inventors: Douglas L. Rector, George A. Conder, Sylvester D. Folz
  • Patent number: 5021578
    Abstract: Compounds of the formula ##STR1## in which R.sup.1 denotes haloalkyl, haloalkenyl or haloalkynyl, (R.sup.2).sub.n denotes H or up to 3 halogens, A denotes N or N.fwdarw.0, R.sup.3 denotes H or alkyl, and Z denotes, inter alia, a carboxyl group or a functional derivative thereof, are valuable herbicides and growth regulators.
    Type: Grant
    Filed: February 22, 1989
    Date of Patent: June 4, 1991
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Volker Koch, Lothar Willms, Andreas Fuss, Klaus Bauer, Hermann Bieringer, Helmut Burstell
  • Patent number: 5011932
    Abstract: This invention concerns a process for killing internal parasites, especially nematodes and cestodes affecting warm blooded animals such as sheep, cattle, swine, goats, dogs, cats, horses and humans as well as poultry by administering an effective amount of a compound of the Formula I: ##STR1## Certain of the compounds of Formula I are novel and in further embodiments of the invention provide novel compounds and compositions for use in the process of the invention. The compounds are readily prepared by conventional chemical reactions. Various pyridinyl acylhydrazones of Formula I demonstrate broad-spectrum anthelmintic activity in sheep upon oral and/or parenteral administration.
    Type: Grant
    Filed: October 3, 1986
    Date of Patent: April 30, 1991
    Assignee: Upjohn Company
    Inventors: Douglas L. Rector, George A. Conder, Sylvester D. Folz
  • Patent number: 5008276
    Abstract: Fungicidal compounds of the formula (I): ##STR1## and stereoisomers thereof, wherein K is oxygen or sulphur; Z is optionally substituted aryl or optionally substituted heteroaryl; X is O, S(O).sub.n, NR.sup.4, CR.sup.1 R.sup.2, CHR.sup.5, CO, CR.sup.1 (OR.sup.2), C.dbd.CR.sup.1 R.sup.2, CHR.sup.1 CHR.sup.2, CR.sup.1 .dbd.CR.sup.2, CHR.sup.1 CR.sup.2 .dbd.CH, C.dbd.C, OCHR.sup.1, CHR.sup.1 O, OCHR.sup.1 O, S(O).sub.n CHR.sup.1, S(O).sub.n CHR.sup.1 O, CHR.sup.1 S(O).sub.n, CHR.sup.1 OSO.sub.2, NR.sup.4 CHR.sup.1, CHR.sup.1 NR.sup.4, CO.sub.2, O.sub.2 C, SO.sub.2 O, OSO.sub.2, CO.CO, COCHR.sup.1, COCHR.sup.1 O, CHR.sup.1 CO, CHOH.CHR.sup.1, CHR.sup.1.CHOH, ##STR2## CONR.sup.4, OCONR.sup.4, NR.sup.4 CO, CSNR.sup.4, OCS.NR.sup.4, SCO.NR.sup.4, NR.sup.4 CO.sub.2, NR.sup.4 CS, NR.sup.4 CSO, NR.sup.4 COS, NR.sup.4 CONR.sup.4, S(O).sub.n NR.sup.4, NR.sup.4 S(O).sub.n, CS.sub.2, S.sub.2 C, CO.S, SCO, N.dbd.N, N.dbd.CR.sup.1, CR.sup.1 .dbd.N, CHR.sup.1 CHR.sup.2 CH(OH), CHR.sup.1 OCO, CHR.sup.1 SCO, CHR.sup.1 NR.sup.
    Type: Grant
    Filed: October 17, 1988
    Date of Patent: April 16, 1991
    Assignee: Imperial Chemical Industries PLC
    Inventors: John M. Clough, Christopher R. A. Godfrey, Stephen P. Heaney, Kenneth Anderton
  • Patent number: 5008391
    Abstract: A process and intermediates for the enantioselective synthesis of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid are disclosed.
    Type: Grant
    Filed: July 7, 1989
    Date of Patent: April 16, 1991
    Assignee: Eli Lilly and Company
    Inventors: Charles J. Barnett, Thomas M. Wilson
  • Patent number: 5006658
    Abstract: A compound of Formula I or a salt thereof:Ar--Q--(CH.sub.2).sub.m --A--CH.sub.2).sub.n (CE.sup.1 .dbd.CE.sup.2).sub.a CE.sup.3 .dbd.CE.sup.4 CXNR.sup.1 R.sup.2 (1)whereAr is a 6-membered heteroaromatic ring containing, as the heteroatom or heteroatoms, one or two nitrogen atoms and is optionally substituted by one or more of halogen, cyano, C.sub.1-6 -alkyl (optionally substituted by halogen), or C.sub.1-6 -alkoxy (optionally substituted by one or more of halogen or C.sub.1-6 -alkyl), or RS(O).sub.x where x is 0, 1 or 2 and R is C.sub.1-6 -alkyl optionally substituted by one or more halogen atoms,Q is --CH.sub.2 -- or --O--,m and n are each independently 0 to 7,A is --CH.sub.2 -- or --O--,a is 0 or 1,E.sup.1 to E.sup.4 are independently hydrogen, C.sub.1-4 -alkyl or halo-C.sub.1-4 -alkyl or halogen,X is oxygen or sulphur, andR.sup.1 and R.sup.2 are independently hydrogen, C.sub.1-6 -alkyl or C.sub.3-6 -cycloalkyl, either being optionally substituted by one or more of the C.sub.1-6 -alkyl, C.sub.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: April 9, 1991
    Assignee: The Wellcome Foundation Ltd.
    Inventor: Robert J. Blade
  • Patent number: 5004743
    Abstract: Compounds having the formula: ##STR1## are leukotriene antagonists and inhibitors of leukotriene biosynthesis. These compounds are useful as anti-asthmatic, anti-allergic, anti-inflammatory, and cytoprotective agents.
    Type: Grant
    Filed: November 25, 1987
    Date of Patent: April 2, 1991
    Assignee: Merck Frosst Canada, Inc.
    Inventors: Robert N. Young, Robert Zamboni, Jacques Y. Gauthier
  • Patent number: 5001137
    Abstract: A novel pyridine compound of the formula ##STR1## wherein each symbol is as defined in the specification, or a salt thereof which exhibit inhibitory activity or prolylendopeptidase and a pharmaceutical use thereof are disclosed.
    Type: Grant
    Filed: September 14, 1989
    Date of Patent: March 19, 1991
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Takanori Oe, Yuji Ono, Kazuyuki Kawasaki, Tohru Nakajima
  • Patent number: 4996218
    Abstract: Compounds of the general formula (I) ##STR1## and physiologically acceptable salts and solvates thereof, which have .beta..sub.2 -adrenoreceptor stimulant activity. They may be used in the treatment of diseases associated with reversible airways obstruction, such as asthma and chronic bronchitis.In preferred embodiments, Q represents a chlorine atom or a trifluoromethyl group, X represents a C.sub.3-4 alkylene chain, Y a C.sub.1-5 alkylene chain, R, R.sup.1 and R.sup.2 are each preferably a hydrogen atom or a methyl group and Het represents a pyrimidinyl pyrazinyl, triazinyl, thiazolyl, quinolinyl, benzimidazolyl, benzothiazolyl, benzoxazolyl or pyridyl group.
    Type: Grant
    Filed: August 10, 1988
    Date of Patent: February 26, 1991
    Assignee: Glaxo Group Limited
    Inventor: Lawrence H. C. Lunts
  • Patent number: 4987140
    Abstract: Novel pyridines of the formula ##STR1## wherein R is selected from the group consisting of (a) phenyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen --CF.sub.3 and --NO.sub.2 and (b) a 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms, R.sub.1 and R.sub.2 are individually selected from the group consisting of (a) alkyl of 1 to 5 carbon atoms, (b) 5 to 6 member heterocyclic optionally substituted with alkyl of 1 to 5 carbon atoms and (c) phenyl and naphthyl optionally substituted with at least one member of the group consisting of hydroxy, alkyl and alkoxy of 1 to 5 carbon atoms, halogen, --NO.sub.3 and --CF.sub.3, R.sub.3 is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, --(CF.sub.2).sub.n --CF.sub.
    Type: Grant
    Filed: November 27, 1989
    Date of Patent: January 22, 1991
    Assignee: Roussel Uclaf
    Inventors: Francois Clemence, Odile Le Martret, Francoise Delevallee
  • Patent number: 4978385
    Abstract: A compound of the formual (I) ##STR1## or 1-oxide or salt thereof, whereinR.sub.1 is a C.sub.1-11 alkyl group, a lower alkenyl group, a phenyl or group which may be substituted, an aralkyl group whose nucleus may be substituted, a haloalkyl or a 5- or 6-membered heterocycle group;R.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 are, the same or different, hydrogen atom, a halogen atom, cyano group, nitro group, amino group, a lower alkyl group, a lower haloalkyl group, hydroxy group, a lower alkoxy group, an aryloxy group, carboxy group or a lower alkoxycarbonyl group;R.sub.7 is hydrogen atom, a halogen atom, a lower alkyl group, a phenyl group which may be substituted, an aralkyl group whose nucleus may be substituted, a lower alkenyl group, a lower alkynyl group, a lower alkoxy group or a haloalkyl group;R.sub.8 is a C.sub.
    Type: Grant
    Filed: May 26, 1988
    Date of Patent: December 18, 1990
    Assignee: Daicel Chemical Industries Ltd.
    Inventors: Hiroshi Yagihara, Yukihisa Goto, Kazuhisa Masamoto, Yasuo Morishima, Hirokazu Osabe
  • Patent number: 4977169
    Abstract: The invention relates to the use of N-3-(5-trifluoromethylpyridyl-2-oxy)phenyl-N'-benzoylureas of formula I ##STR1## wherein R.sub.1 is hydrogen, C.sub.1 -C.sub.2 alkoxy, C.sub.1 -C.sub.2 alkylthio, C.sub.1 -C.sub.2 alkyl or halogen,R.sub.2, R.sub.3 and R.sub.5 are independently of each other hydrogen or halogen, andR.sub.4 is hydrogen, C.sub.1 -C.sub.2 alkyl or halogen,for controlling helminths, especially nematodes and trematodes, in domestic animals and productive livestock.
    Type: Grant
    Filed: May 15, 1989
    Date of Patent: December 11, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Walter Hausermann, Max Maurer, Thomas Friedel
  • Patent number: 4975442
    Abstract: Novel fungicidal pyridyl cyclopropane carboxamidines having the general structural formula ##STR1## and tautomers thereof whereinR is selected from the group consisting of hydrogen, pyridyl, substituted pyridyl, C.sub.1 -C.sub.3 alkoxy, C.sub.1 -C.sub.6 alkyl, acyl, carbamoyl, sulfonyl and cyano;R.sub.1 is selected from the group consisting of halogen, C.sub.1 -C.sub.3 alkoxy and C.sub.1 -C.sub.3 alkenyloxy;R.sub.2 is selected from the group consisting of hydrogen and C.sub.1 -C.sub.3 alkyl;R.sub.3 is selected from the group consisting of hydrogen, alkyl, aryl or arylalkyl;and fungicidally acceptable organic and inorganic salts thereof.
    Type: Grant
    Filed: February 10, 1989
    Date of Patent: December 4, 1990
    Assignee: ICI Americas Inc.
    Inventors: Don R. Baker, Keith H. Brownell
  • Patent number: 4968341
    Abstract: Novel substituted aryloxyureas, processes for their production, and herbicides comprising them as active ingredients are provided.The substituted aryloxyureas exhibit an excellent herbicidal efficacy against weeds when applied, for example, to the weeds in a wide range of period from a preemergence stage to a growth stage.The substituted aryloxyureas of the invention have the excellent advantage of maintaining high safety on crops or crop plants in spite of their herbicidal efficacy.
    Type: Grant
    Filed: August 16, 1988
    Date of Patent: November 6, 1990
    Assignees: Kumiai Chemical Industry Co., Mitsui Petrochemical Industries, Ltd.
    Inventors: Isao Hashimoto, Tatsuyodihi Ishida, Kazutaka Tsuru, Yuji Yamada, Takeshige Miyazawa, Yasuo Nakamura, Susumu Katou, Katsuya Takahashi
  • Patent number: 4966974
    Abstract: The invention relates to 2-phenylsulphinyl-nitro-pyridines of the formula ##STR1## in which R.sub.1 denotes hydrogen, alkyl or halogen andR.sub.2, R.sub.3, R.sub.4, R.sub.5 and R.sub.6 independently of one another represent hydrogen, halogen, alkyl, haloalkyl, alkyoxy, haloalkoxy, cyano, nitro, carboxyl, alkoxycarbonyl, carboxamido, N-alkyl- or N,N-dialkylcarboxamido, acyl or primary, secondary or tertiary amino.processes for their preparation, and their use as microbicides for the protection of materials and fungicides in plant protection.
    Type: Grant
    Filed: April 3, 1989
    Date of Patent: October 30, 1990
    Assignee: Bayer Aktiengesellschaft
    Inventors: Alexander Klausener, Wilfried Paulus, Hans-Georg Schmitt, Wilhelm Brandes
  • Patent number: 4954628
    Abstract: The invention relates to a process for preparing sulphonyl-ureas of the general formula (I) ##STR1## wherein Ar.sub.1 represents a phenyl, naphthyl or thienyl group, the derivatives thereof substituted by C.sub.1-4 alkyl, C.sub.1-4 haloalkyl, (halo)alkoxycarbonyl, (halo)alkyloxy, nitro, cyano groups as well as by halogen atoms,Ar.sub.2 represents a phenyl, pyridyl, pirimidinyl or triazinyl group and the derivatives thereof substituted by C.sub.1-4 (halo)alkyl, C.sub.1-4 (halo)alkyloxy, amino, O-acyl, O-arylsulphonyl, O-(substituted carbamoyl) groups as well as by halogen atoms.
    Type: Grant
    Filed: March 2, 1989
    Date of Patent: September 4, 1990
    Assignees: Nitrokaelepek, Magyar Tudomanyos Akademia Kozponti Kemiai Kutato Intezete
    Inventors: Gabor Besenyei, Sandor Nemeth, Laszlo Simandi, Maria Belak, Maria Szabo, Jozsef Dukai, Lajos Nagy, Elemer Tomordi, Csaba Soptei, Erzsebet E. Dioszegine
  • Patent number: 4946854
    Abstract: Novel compounds of formula I ##STR1## wherein each of R.sup.1, R.sup.2, R.sup.3, R.sup.7, R.sup.8 and R.sup.9, independently of the others, is H or halogen,R.sup.4 is H, R.sup.10 CO-- or R.sup.11 NHCO-- wherein R.sup.10 is a C.sub.1 -C.sub.4 alkyl group which is unsubstituted or substituted by one to three identical or different substituents selected from the group consisting of halogen, C.sub.1 -C.sub.4 alkoxy, C.sub.1 -C.sub.4 - acyloxy and --COOG, wherein G is H, an alkali metal cation or an alkaline earth metal cation, and R.sup.11 is an unsubstituted or halo-substituted C.sub.1 -C.sub.4 alkyl or phenyl group,each of R.sup.5 and R.sup.6, independently of the other, is H, halogen, alkyl or haloalkyl andX is O, S(O)n or NH wherein n is 0, 1 or 2, the preparation of the novel compounds and their use against parasites in and on productive livestock and against insect pests, and novel starting materials and their preparation.
    Type: Grant
    Filed: December 5, 1988
    Date of Patent: August 7, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Peter Maienfisch, Jean-Claude Gehret, Bruno Frei
  • Patent number: 4946497
    Abstract: A compound of the formula (I) ##STR1## or a salt thereof, wherein R is hydrogen atom, or a group of --(CH.sub.2).sub.n --R.sub.1 wherein n is an integer from 1 to 3 and R.sub.1 is hydrogen atom, hydroxy group, a lower alkoxy group, mercapto group, a lower alkylthio group, amino group, a di-lower alkylamino group, a C.sub.3-11 alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl group, a 5- or 6-membered heterocyclic group, or a phenyl group which may be substituted by one or two substituents of a halogen, a lower alkyl or a lower alkoxy;R.sub.2 and R.sub.7 are the same, a C.sub.1-11 alkyl group, a lower alkenyl group, a lower alkynyl group, a cycloalkyl group, a lower alkoxyalkyl group, an aralkyl group whose nucleus may be substituted by one or two substituents of a halogen, a lower alkyl or a lower alkoxy, or a halalkyl group;R.sub.3, R.sub.4 and R.sub.
    Type: Grant
    Filed: November 22, 1988
    Date of Patent: August 7, 1990
    Assignee: Daicel Chemical Industries Ltd.
    Inventors: Yukihisa Goto, Kazuhisa Masamoto, Hiroshi Yagihara, Yasuo Morishima, Hirokazu Osabe
  • Patent number: 4943314
    Abstract: A compound of the formula (I) ##STR1## or a salt thereof, wherein R is hydrogen atom, phenyl group which may be substituted freely or a group of --(CH.sub.2).sub.n --R.sub.1 wherein n is an interger from 1 to 3 and R.sub.1 is hydrogen atom, hydroxy group, lower alkoxy group, mercapto group, lower alkylthio group, amino group, di-lower alkylamino group, C.sub.3-11 alkyl group, lower alkenyl group, lower alkynyl group, cycloalkyl group, 5- or 6-membered heterocyclic group, or phenyl group which may be substituted by one or two substituents of halogen, lower alkyl or lower alkoxy;R.sub.2 and R.sub.7 are different, hydrogen atom, C.sub.1-11 alkyl group, lower alkenyl group, lower alkylyl group, cycloalkyl group, lower alkoxyalkyl group, lower alkylthioalkyl group, phenyl group which may be substituted freely, aralkyl group whose nucleus may be subsituted by one or two substituents of halogen, lower alkyl or lower alkoxy or haloalkyl group or 5- or 6-membered heterocyclic group;R.sub.3, R.sub.4 and R.sub.
    Type: Grant
    Filed: March 3, 1989
    Date of Patent: July 24, 1990
    Assignee: Daicel Chemical Industries, Ltd.
    Inventors: Yukihisa Goto, Kazuhisa Masamoto, Hiroshi Yagihara, Yasuo Morishima, Hirokazu Osabe
  • Patent number: 4942242
    Abstract: Thiazolyl phenoxy derivatives are provided as well as pharmaceutical compositions containing such derivatives. The compositions are useful for lowering lipid activity in a subject and accordingly useful for reducing cholesterol and triglycerides.
    Type: Grant
    Filed: October 21, 1988
    Date of Patent: July 17, 1990
    Inventors: Tadao Kojima, Shunji Kageyama, Minoru Okada, Isao Ohata, Noboru Sato
  • Patent number: 4931448
    Abstract: Insecticidal compounds having the formula ##STR1## in which R is an optionally substituted aryl moiety; R.sub.2 is an optionally substituted alkyl, cycloalkyl or alkenyl moiety, X is sulfur, amino or C.sub.1 -C.sub.4 monoalkylamino; and R.sub.3 is: (a) an optionally substituted 3-phenoxyphenalkyl, 3-phenoxypyridylalkyl or 3-(4-pyridyloxy)phenalkyl moiety; (b) pentafluorobenzyl; or (c) 2-methyl-3-phenylbenzyl.
    Type: Grant
    Filed: November 17, 1987
    Date of Patent: June 5, 1990
    Assignee: ICI Americas Inc.
    Inventors: Michael D. Broadhurst, Thomas H. Cromartie
  • Patent number: 4931452
    Abstract: Substituted N-cyanomethyl-2-pyridinones were prepared by the reaction of alkali metal substituted-2-pyridinates with monohaloacetonitriles and found to possess insecticidal properties. The alkali metal substituted-2-pyridinates can be preformed or prepared from the corresponding 2-halopyridines or 2-pyridinols in the reaction medium. N-cyanomethyl-3-fluoro-5-(trifluoromethyl)-2-pyridinone, for example, was prepared from 2,3-difluoro-5-(trifluoromethyl)pyridine and found to control aster leafhoppers both on contact and systemically.
    Type: Grant
    Filed: August 24, 1988
    Date of Patent: June 5, 1990
    Assignee: The Dow Chemical Company
    Inventors: Sudarshan K. Malhotra, James E. Dripps, Gregory A. Bradfisch, Susan Wollowitz, Ingrid L. Knox
  • Patent number: 4927838
    Abstract: The invention relates to compounds of the formula ##STR1## wherein Y and Y' are hydrogen or taken together are O or S, *A is paraphenylene or *----(CH.sub.2).sub.n --(X).sub.s --(CH.sub.2).sub.r ----, X is O, S or --CH.dbd.CH--, n or r, independently, are integers from 0 to 3, m is an integer from 0 to 1, s is an integer from 0 to 1, provided that when s is 1, n+m must be at least 2, t is an integer from 0 to 10, R.sub.1 and R.sub.2, independently, are lower alkyl, lower alkenyl or aryl, or one of R.sub.1 or R.sub.2 is hydrogen and the other is ##STR2## wherein W is ##STR3## --CH.sub.2 --CH.sub.2 --, --CH.sub.2 --, O, S, or ##STR4## and X.sub.1 is lower alkyl, phenyl unsubstituted or mono-, di- or trisubstituted by lower alkoxy, lower alkyl or halogen, and X.sub.2, X.sub.3 and X.sub.4, independently, are hydrogen, lower alkyl, lower alkoxy or halogen, R.sub.3 is hydrogen, lower alkyl or aryl, R.sub.4 is hydrogen, lower alkyl, aryl, aryl-lower alkyl or acyl, R.sub.5 is hydrogen or lower alkyl,R.sub.
    Type: Grant
    Filed: July 5, 1988
    Date of Patent: May 22, 1990
    Assignee: Hoffman-La Roche Inc.
    Inventors: Robert W. Guthrie, Richard W. Kierstead, John G. Mullin, Jefferson W. Tilley
  • Patent number: RE33478
    Abstract: Certain novel pyridinyloxyphenoxy alkanoic acids, pyridinylthiophenoxy alkanoic acids, derivatives thereof and related compounds are described. More specifically, these novel compounds bear a fluorine substituent in the 3-position of the pyridinyl group and in the 5-position the substituent is selected from chlorine, CF.sub.3, CF.sub.2 Cl or CF.sub.2 H. These novel compounds exhibit surprising preemergent and postemergent activity in the control of grassy weeds.
    Type: Grant
    Filed: October 31, 1988
    Date of Patent: December 11, 1990
    Assignee: The Dow Chemical Company
    Inventors: Howard Johnston, Lillian H. Troxell