Ortho Fused Patents (Class 560/139)
  • Patent number: 4760174
    Abstract: Tetralin derivatives of the formula I ##STR1## where X, R.sup.1, R.sup.2 and R.sup.3 have the meanings stated in the description, and their preparation are described. The novel compounds are useful for the treatment of disorders.
    Type: Grant
    Filed: September 20, 1985
    Date of Patent: July 26, 1988
    Assignee: BASF Aktiengesellschaft
    Inventors: Fritz-Frieder Frickel, Hans-Heiner Wuest, Axel Nuerrenbach
  • Patent number: 4751240
    Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined phenolic nucleus including a phenyl-hydroxynaphthyl; hydroxyphenyl-naphthyl; phenyl-hydroxyindanyl, phenyl-hydroxybenzothienyl or mono-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages, wherein R.sup.1 is hydrogen, or alkyl, alkenyl, alkynyl, cycloalkyl, halogenoalkyl, alkoxyalkyl, halogenoalkoxyalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 --or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --(PO)R.sup.2 13 , --S--, --SO--or --SO.sub.2 --, wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene; wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro; or a salt thereof when appropriate.
    Type: Grant
    Filed: April 24, 1985
    Date of Patent: June 14, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: Jean Bowler, Graham C. Crawley, Philip N. Edwards, Alasdair T. Glen, Michael S. Large, Brian S. Tait
  • Patent number: 4745212
    Abstract: Isocyanates containing ester and/or amide groups are produced by reacting (a) an isocyanatocarboxylic acid chloride with (b) an organic compound containing a silylated alcoholic group and/or silylated phenolic hydroxyl group and/or silylated amino group which compound contains no other group which is reactive with isocyanate and chlorocarbonyl groups under the reaction conditions. The reaction of (a) with (b) is carried out at a temperature of from -20.degree. to 150.degree. C. This process makes it possible to produce the desired isocyanates with a high degree of selectivity.
    Type: Grant
    Filed: October 8, 1987
    Date of Patent: May 17, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Werner Mormann, Edith Hissmann
  • Patent number: 4739079
    Abstract: Compounds having the formula ##STR1## wherein ##STR2## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.
    Type: Grant
    Filed: March 27, 1986
    Date of Patent: April 19, 1988
    Assignee: Pfizer Inc.
    Inventors: Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4737519
    Abstract: The present invention provides certain novel substituted naphthalenes, indoles, benzofurans, and benzothiophenes of Formula I which are useful as inhibitors of leukotriene biosynthesis and as inhibitors of lipoxygenase. They are thus employed wherever it is medically necessary or desirable to inhibit these systems.
    Type: Grant
    Filed: June 25, 1986
    Date of Patent: April 12, 1988
    Assignee: The Upjohn Company
    Inventors: Ayako Yamashita, Herbert G. Johnson
  • Patent number: 4736055
    Abstract: Oxime sulfonates of formula I ##STR1## wherein Y is a polymerizable unsaturated group or epoxide group or an --OH, --NHR.sup.5, --COOH, COOR.sup.6, --COCl, --CH.sub.2 Hal, --SO.sub.2 Cl or --NCO group, Z is an (x+y)-valent connecting member, R.sup.1 and R.sup.2 are monovalent organic radicals, m is 0 or 1, x is 1 or 2 and y is 1 or 2, can be converted into polymers which can be thermally or photochemically dissociated to form free sulfonic acid groups. Said polymers can therefore be used as photoresists which can be developed with aqueous alkalis.
    Type: Grant
    Filed: April 11, 1986
    Date of Patent: April 5, 1988
    Assignee: Ciba-Geigy Corporation
    Inventors: Kurt Dietliker, Werner Rutsch, Godwin Berner, Max Hunziker, Christopher G. Demmer
  • Patent number: 4732912
    Abstract: A phenol derivative of the formulaNU--A--X--R.sup.1wherein NU is a defined bis-phenolic nucleus including a hydroxyphenyl-hydroxynaphthyl; hydroxyphenyl-hydroxyindanyl, hydroxyphenyl-hydroxybenzothienyl or di-hydroxyphenyl-ethylene or vinylene nucleus; wherein A is alkylene, alkenylene or alkynylene which may be interrupted by phenylene or other linkages,wherein R.sup.1 is hydrogen, or alkyl, alkenyl, cycloalkyl, halogenoalkyl, aryl or arylalkyl, or R.sup.1 is joined to R.sup.2, and wherein X is --CONR.sup.2 --, --CSNR.sup.2 --, --NR.sup.12 CO--, --NR.sup.12 CS--, --NR.sup.12 CONR.sup.2 --, ##STR1## --SO.sub.2 NR.sup.2 -- or --CO--, or, when R.sup.1 is not hydrogen, is --NR.sup.12 COO--, --S--, --SO-- or --SO.sub.2 --,wherein R.sup.2 is hydrogen or alkyl, or R.sup.1 and R.sup.2 together form alkylene;wherein R.sup.12 is hydrogen or alkyl, and wherein R.sup.22 is hydrogen, cyano or nitro;or a salt thereof when appropriate.
    Type: Grant
    Filed: April 27, 1984
    Date of Patent: March 22, 1988
    Assignee: Imperial Chemical Industries PLC
    Inventors: William R. Pilgrim, Derek W. Young, Brian S. Tait, Graham C. Crawley, Philip N. Edwards, George B. Hill
  • Patent number: 4707497
    Abstract: A novel phenylethanolaminotetraline having lipolytic activity of formula ##STR1## wherin X represents hydrogen, halogen, a trifluoromethyl or a lower alkyl group and R represents hydrogen, a lower alkyl group not substituted or substituted by a cycloalkyl group containing 3 to 7 carbon atoms, a hydroxy group, a lower alkoxy, carboxy or lower carbalkoxy group; a cycloalkyl group containing 3 to 7 carbon atoms; or a lower alcanoyl group; or a pharmaceutically acceptable salt thereof; a process for its preparation; and pharmaceutical compositions containing it as active ingredient, useful for the treatment of obesity.
    Type: Grant
    Filed: July 10, 1986
    Date of Patent: November 17, 1987
    Assignee: Sanofi
    Inventors: Roberto Cecchi, Robert Boigegrain, Alberto Bianchetti, Elena Poggesi, Tiziano Croci
  • Patent number: 4692463
    Abstract: The present invention describes the finding of potent antiinflammatory properties in 2,3-didemethylcolchicine and its analogs.
    Type: Grant
    Filed: November 29, 1985
    Date of Patent: September 8, 1987
    Assignee: The United States of America as represented by the Department of Health and Human Services
    Inventor: Arnold Brossi
  • Patent number: 4692546
    Abstract: Acyloxy aromatic carboxylic acids, e.g., 4-acetoxybenzoic acid, are prepared by oxidizing with oxygen an acyloxy aromatic ketone, e.g., 4-acetoxyacetophenone in the presence of manganese cations and a lower-carboxylic acid anhydride as catalyst and a co-reductant or promoter. The acyloxy aromatic ketone may be prepared by acylating a hydroxy aromatic ketone, e.g., 4-hydroxyacetophenone, which has the effect of "masking" the hydroxyl group of the ketone in a manner necessary to effect the subsequent transition-metal catalyzed oxidation of the ketone to the acyloxy aromatic carboxylic acid.
    Type: Grant
    Filed: September 25, 1985
    Date of Patent: September 8, 1987
    Assignee: Celanese Corporation
    Inventor: Kenneth G. Davenport
  • Patent number: 4689346
    Abstract: Compounds for effecting hemostatic and antifibrinolytic action, namely a 1-acylamino naphthalene-4 sulphonic acid derivative of the formula ##STR1## and compositions and method of achieving such action.
    Type: Grant
    Filed: October 28, 1985
    Date of Patent: August 25, 1987
    Assignee: Laboratorio Fides, S.A.
    Inventors: Pere P. Llobet, Elisa G. Baylina
  • Patent number: 4683241
    Abstract: Phenolic esters of the general formula I ##STR1## are useful for the prevention, management or alleviation of elastase mediated diseases or conditions.
    Type: Grant
    Filed: May 21, 1984
    Date of Patent: July 28, 1987
    Assignee: G. D. Searle & Co.
    Inventors: Masateru Miyano, James R. Deason
  • Patent number: 4642373
    Abstract: 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]-phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.
    Type: Grant
    Filed: July 6, 1984
    Date of Patent: February 10, 1987
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4632997
    Abstract: A method for preparing a cis-bicyclo[3.3.0]octylidene derivative represented by the formula: ##STR1## wherein R.sup.1 is a hydrogen atom or an alkyl group; R.sup.2 is a hydrogen atom or a protective group for hydroxyl group; and Y is ##STR2## where R.sup.3 is a hydrogen atom or a protective group for hydroxyl group; R.sup.4 is a hydrogen atom or a straight, branched or cyclic alkyl group, alkenyl group or alkynyl group; and X is a group represented by CH.dbd.CH or C.tbd.C,comprises carrying out the catalytic hydrogenation reaction of a (1-alkenyl)-cis-bicyclo[3.3.0]octene derivative represented by the formula: ##STR3## wherein R.sup.1, R.sup.2 and Y have the same meanings as defined above, in the presence of a metal carbonyl compound or its complex represented by the formula:Mw(CO)x(H)y(R)zwherein M is a metal element of the group VIB; R is a .pi. ligand or a phosphine ligand; w is 1 or 2; x is an integer of 3 to 6; y is 0 or 1; and z is 0 or an integer of 1 to 3.
    Type: Grant
    Filed: February 8, 1985
    Date of Patent: December 30, 1986
    Assignee: Sagami Chemical Research Center
    Inventors: Masakatsu Shibasaki, Mikiko Sodeoka, Yuji Ogawa
  • Patent number: 4631151
    Abstract: A fluorine-containing aromatic derivative is produced by causing a di(haloacyl)peroxide to react upon benzene, a mono-substituted benzene, naphthalene, or a mono-substituted naphthalene thereby introducing an X(CF.sub.2).sub.n -group into the benzene ring or the naphthalene ring.
    Type: Grant
    Filed: February 19, 1985
    Date of Patent: December 23, 1986
    Assignee: Nippon Oil & Fars Co., Ltd.
    Inventors: Michio Kobayashi, Masato Yoshida, Hideo Sawada, Hidehiko Hagii, Kazuyoshi Aoshima
  • Patent number: 4618701
    Abstract: 6-Hydroxy-2-naphthoic acid can be selectively acetylated to 6-acetoxy-2-naphthoic acid, in particular in the presence of admixtures of isomeric hydroxy-naphthoic acids, and thus be separated from those isomeric admixtures. The acetylation is affected in aqueous alkaline solution by reaction with acetic anhydride. By hydrolysis of the 6-acetoxy-2-naphthoic acid, a pure 6-hydroxy-2-naphthoic acid is obtained.
    Type: Grant
    Filed: February 26, 1985
    Date of Patent: October 21, 1986
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Rudolf Neeb, Wolfgang Ironich, Heinrich Volk
  • Patent number: 4599204
    Abstract: This invention concerns novel compounds useful in compositions and methods for preventing the attachment of dental plaque to the surfaces of the teeth of mammals and as inhibitors of connective tissue destruction. The compounds of this invention comprise certain [oxalylbis(iminophenylenecarbonylimino)]bis[hydroxynaphthalenesulfonic acids] and salts thereof which may be combined with pharmaceutically acceptable carriers or diluents to be administered in the form of conventional pharmaceutical compositions.
    Type: Grant
    Filed: March 11, 1985
    Date of Patent: July 8, 1986
    Assignee: American Cyanamid Company
    Inventors: John F. Poletto, Seymour Bernstein
  • Patent number: 4588833
    Abstract: Substituted succinic acid amides, in particular substituted succinic acid amides containing differing derivative groups, are prepared by reacting unsaturated carboxamides with carbon monoxide and with a nucleophilic component containing at least one mobile hydrogen atom, in the presence of cobalt compounds and, if appropriate, in the presence of one or more tertiary nitrogen bases, under an elevated pressure and at an elevated temperature.
    Type: Grant
    Filed: October 26, 1984
    Date of Patent: May 13, 1986
    Assignee: Bayer Aktiengesellschaft
    Inventors: Jurgen Kadelka, Hans-Helmut Schwarz
  • Patent number: 4576964
    Abstract: Tricyclic benzo fused compounds of the formula ##STR1## and pharmaceutically acceptable cationic and acid addition salts thereof, wherein n is zero, 1 or 2, and t is 1 or 2; M is CH or N, R.sub.1 is H or certain acyl groups; Q is CO.sub.2 R.sub.4, COR.sub.5, C(OR.sub.7)R.sub.5 R.sub.6, CN, CONR.sub.9 R.sub.10, CH.sub.2 NR.sub.9 R.sub.10, CH.sub.2 NHCOR.sub.11, CH.sub.2 NHSO.sub.2 R.sub.12, 5-tetrazolyl or when n is 1, Q and OR.sub.1 together form a lactone or certain reduced derivatives thereof; and Z is certain alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl groups, are valuable central nervous system active agents, methods for their use, pharmaceutical compositions containing them and certain intermediates therefor.
    Type: Grant
    Filed: June 7, 1984
    Date of Patent: March 18, 1986
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4570011
    Abstract: The invention is a process for the preparation of an aromatic hydrocarbon with a cyclobutene ring fused to the aromatic hydrocarbon which comprises, dissolving an ortho alkyl halomethyl aromatic hydrocarbon in an inert solvent and pyrolyzing the solution of ortho alkyl halomethyl aromatic hydrocarbon in the inert solvent under conditions such that the ortho alkyl and halomethyl substituents form a cyclobutene ring thereby forming an aromatic hydrocarbon having a fused cyclobutene ring.
    Type: Grant
    Filed: May 21, 1984
    Date of Patent: February 11, 1986
    Assignee: The Dow Chemical Company
    Inventor: Ying-Hung So
  • Patent number: 4568782
    Abstract: Disclosed is the vapor phase cyclodehydration of an aldehyde or ketone over a solid Lewis acid as catalyst to make indene or a substituted indene according to the equation: ##STR1##
    Type: Grant
    Filed: June 17, 1985
    Date of Patent: February 4, 1986
    Assignee: The Standard Oil Company
    Inventors: Marco Pagnotta, Mark C. Cesa, James D. Burrington
  • Patent number: 4568763
    Abstract: N-acyl-acyloxy aromatic amines, e.g. 4-acetoxyacetanilide (AAA), are prepared by reacting a hydroxy aromatic ketone, e.g. 4-hydroxyacetophenone, with hydroxylamine or a hydroxylamine salt and a base to obtain the ketoxime of the ketone, e.g. 4-hydroxyacetophenone oxime, and then subjecting the ketoxime to a Beckmann rearrangement and accompanying acylation by contacting the ketoxime with a carboxylic acid anhydride and a Beckmann rearrangement catalyst to form the N-acyl-acyloxy aromatic amine.
    Type: Grant
    Filed: July 3, 1984
    Date of Patent: February 4, 1986
    Assignee: Celanese Corporation
    Inventors: Kenneth G. Davenport, Charles B. Hilton
  • Patent number: 4564628
    Abstract: Novel compounds useful as dopamine receptor agonists for the treatment of various diseases of the central nervous system such as Parkinson's disease and related disorders having the structural formula ##STR1## where R.sub.2, R.sub.3 and R.sub.4 are each selected from the group consisting of H, and OA; A is H or ##STR2## R.sub.5 is selected from the group consisting of alkyl and aromatic residues; n is 2 or 3; and R.sub.1 is selected from the group consisting of 3-hydroxyphenyl, 4-hydroxyphenyl, 3-pyridyl, 4-pyridyl, ##STR3## where X is S, O or NH; and pharmaceutically acceptable salts thereof. Also disclosed is a method for inducing a dopaminergic response in a patient by adminstering a pharmacologically-effective amount of one of the foregoing compounds.
    Type: Grant
    Filed: August 13, 1984
    Date of Patent: January 14, 1986
    Assignee: Nelson Research & Development Co.
    Inventor: Alan S. Horn
  • Patent number: 4545921
    Abstract: The invention relates to a group of organic compounds of the substituted 2-hydroxyfluorene ester type, which has a smectic A mesomorphous phase. The invention also relates to the process for producing molecules of this group.The compound according to the invention is in accordance with the general chemical formula ##STR1## whereby n can be between 1 and 15 and X=Br or CN. The invention applies to the field of liquid crystals and to display means using such crystals.
    Type: Grant
    Filed: December 29, 1983
    Date of Patent: October 8, 1985
    Assignee: Thomson-CSF
    Inventors: Jean-Claude Dubois, Gilles Ravaux, Pierre Le Barny
  • Patent number: 4540806
    Abstract: Benzocycloalkane amine derivatives and their non-toxic acid addition salts as novel analgesic agents.
    Type: Grant
    Filed: December 22, 1983
    Date of Patent: September 10, 1985
    Assignee: American Home Products Corporation
    Inventors: Meier E. Freed, Magid A. Abou-Gharbia
  • Patent number: 4540811
    Abstract: A carboxylic acid esters, such as methyl propionate, is prepared by carbonylation of an olefin, such as ethylene, in the presence of an alcohol by the use of a molybdenum-nickel-alkali metal, a tungsten-nickel-alkali metal or a chromium nickel-alkali metal co-catalyst and in the presence of a halide.
    Type: Grant
    Filed: September 30, 1982
    Date of Patent: September 10, 1985
    Assignee: The Halcon SD Group, Inc.
    Inventor: Nabil Rizkalla
  • Patent number: 4512927
    Abstract: A process for the preparation of naphthyl or indene carboxylates by reaction of tetralin or indane with oxygen and a carboxylic acid in the presence of a catalyst comprising palladium is described.
    Type: Grant
    Filed: June 15, 1983
    Date of Patent: April 23, 1985
    Assignee: Ashland Oil, Inc.
    Inventor: Anil B. Goel
  • Patent number: 4499105
    Abstract: The present invention is dealing with compounds of the formula: ##STR1## and pharmaceutically acceptable salts thereof, in which n and m represent the number 1 or 2, X and Y hydrogen, alkyl (1-4 C), alkoxy (1-4 C), hydroxy, halogen, hydroxymethyl, trifluoromethyl, acyl (1-4 C), acyloxy (1-4 C) or the group NR.sub.x R.sub.y, in which R.sub.x and R.sub.y represent hydrogen, alkyl (1-4 C) or a sulphonyl group and R represents the group ##STR2## in which R.sub.1 and R.sub.2 represent hydrogen, alkyl (1-4 C), hydroxy, alkoxy (1-4 C), phenylalkoxy (7-10 C), acyloxy, amino or mono or dialkyl (1-4 C) amino, having potent platelet aggregation inhibiting properties.
    Type: Grant
    Filed: December 28, 1982
    Date of Patent: February 12, 1985
    Assignee: Akzo N.V.
    Inventor: Harm J. Panneman
  • Patent number: 4492798
    Abstract: A process for the production of an arylalkylpyruvic acid of the general formula:(R).sub.n --A--(CH.sub.2).sub.m CH.sub.2 COCOOHwherein:A represents an aromatic hydrocarbon radical containing 1 or 2 condensed benzene rings,each R, which may be the same or different, represents hydrogen or a linear or branched alkyl radical with up to 4 carbon atoms which is unsubstituted or substituted by a nitro group or by an alkoxy group containing 1 to 4 carbon atoms, or an alkoxy group containing 1 to 4 carbon atoms, or a halogeno, nitrile, nitro or alkylcarbonyloxy group,n is 0 or an integer from 1-3 when A contains one benzene ring, and n is 0 or an integer from 1-5 when A contains two condensed benzene rings and m is 1-20, which comprises carbonylating an arylalkyl halide of the general formula:(R).sub.n --A--(CH.sub.2).sub.m CH.sub.
    Type: Grant
    Filed: January 13, 1983
    Date of Patent: January 8, 1985
    Assignee: Ethyl Corporation
    Inventors: John Y. Lee, Joachim W. Wolfram
  • Patent number: 4490552
    Abstract: A novel process for the preparation of aryl esters of organic carboxylic acids in high isomer purity by decomposing a compound of the formula ##STR1## wherein Ar is an aryl radical, X is an acyloxy of an organic carboxylic acid and Y is selected from the group consisting of an acyloxy of an organic carboxylic acid and an anion of a strong organic and mineral acid in an aqueous media in the presence of a palladium salt or in the form of a two-phase reaction, wherein the aryl thallium salt is dissolved in water and the catalytic palladium salt is dissolved in a water-immiscible organic solvent and the reaction takes place with mixing.
    Type: Grant
    Filed: December 20, 1982
    Date of Patent: December 25, 1984
    Assignee: Rutgerswerke AG
    Inventor: Ulrich Knips
  • Patent number: 4477556
    Abstract: A photopolymerizable coating composition comprising(1) a nongaseous, ethylenically unsaturated, polymerizable compound,(2) a specified acidic o-nitroaromatic compound, and(3) an organic, radiation-sensitive, free-radical generating system which is useful for making a positive or negative polymeric image on a substrate.
    Type: Grant
    Filed: August 18, 1982
    Date of Patent: October 16, 1984
    Assignee: E. I. Du Pont de Nemours and Company
    Inventors: Thomas E. Dueber, William J. Nebe
  • Patent number: 4473704
    Abstract: 1,2,3,4,4a,4b,5,6,7,8,8a,12b-Dodecahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy or alkoxyalkyl)triphenylenes, 2,3,3a,3b,4,5,6,7,7a,11b-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)-1H-cyclopenta[1]phenanthrenes, 2,3,4,4a,4b,5,6,7,8,8a-decahydro-7-(oxo, hydroxy or amino)-9-hydroxy-11-(alkyl, alkoxy, alkoxyalkyl, aralkyl, aralkoxy, aryloxyalkyl or aralkoxyalkyl)-1H-pyrido[1,2-f]phenanthridines, and 1,2,3,3a,3b,4,5,6,7,7a-decahydro-6-(oxo, hydroxy or amino)-8-hydroxy-10-(alkyl, alkoxy or alkoxyalkyl)pyrrolo[1,2-f]phenanthridines and derivatives are valuable as central nervous system active agents or as intermediates to compounds having such activity.
    Type: Grant
    Filed: March 16, 1982
    Date of Patent: September 25, 1984
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4466981
    Abstract: Psoriasis in mammals is relieved by topically administering naphthalenes of the formula: ##STR1## wherein: R.sup.1 and R.sup.2 are lower alkoxy or lower alkylthio;R.sup.3 is hydrogen, lower alkyl, lower alkoxy, optionally substituted phenyl, optionally substituted phenyl lower alkyl, optionally substituted phenyl lower alkoxy, amino, lower alkylamino, lower dialkylamino, halo, cyano, or S(O).sub.n R wherein R is lower alkyl; optionally substituted phenyl; optionally substituted phenyl lower alkyl; or optionally substituted heterocyclic aryl of three to nine ring atoms containing one or two heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur, and the pharmaceutically acceptable acid addition salts thereof; and n is 0, 1 or 2; andW is alkyl of one to seven carbon atoms.
    Type: Grant
    Filed: October 27, 1982
    Date of Patent: August 21, 1984
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Gordon H. Jones, Michael C. Venuti, Young, John M.
  • Patent number: 4451664
    Abstract: An improved process for preparing diaryl esters of a monohydroxy aromatic compound with dicarboxylic acids is disclosed, in which the esterification reaction is optimized by continuously removing water and/or other by-products of the reaction from the reactor, while supplying to the reactor a make-up amount of the monohydroxy aromatic compound containing no more than about 100 ppm of water. The make-up stream may be obtained by stripping the by-product stream of water and other by-products of the reaction.
    Type: Grant
    Filed: September 24, 1982
    Date of Patent: May 29, 1984
    Assignee: Occidental Chemical Corporation
    Inventor: Gautam R. Ranade
  • Patent number: 4432885
    Abstract: Decalins of the formula ##STR1## wherein ring A is aromatic or a trans-1,4-disubstituted cyclohexane ring; R.sup.2 is methyl, --CH.sub.2 R', --OR', --CO--R', --CN, --COOH, --CO--OR', --CO--SR' or --O--CO--R'; R.sup.1 is hydrogen, methyl, --CH.sub.2 R, --OR or --CH.sub.2 OR, or when R.sup.2 is methyl, --CH.sub.2 R', --OR' or --CO--R', R.sup.1 also can be --CN, --COOH, --CO--OR, --CO--SR or --O--CO--R; R and R' each are alkyl; and R.sup.1 and R.sup.2 each have up to 12 carbon atoms and together have at most 14 carbon atoms,their racemates and optically active antipodes, are described. Liquid crystalline mixtures comprising Compound I as well as their use in electro-optical devices also are disclosed.
    Type: Grant
    Filed: December 9, 1981
    Date of Patent: February 21, 1984
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Martin Petrzilka, Kuno Schleich
  • Patent number: 4393211
    Abstract: A process for the preparation of aromatic sulfohalides by reacting an aqueous solution, containing a hydrogen halide, of an aromatic diazonium halide with sulfur dioxide, wherein(a) the aqueous solution, containing the hydrogen halide, of a diazonium salt which is derived from the corresponding aromatic amine and the halogen of the desired sulfohalide is reacted with sulfur dioxide in the presence of an inert organic solvent which is immiscible or only partially miscible with water,(b) the diazonium salt is decomposed, simultaneously or subsequently, by means of a catalyst for diazonium salt decomposition and(c) the resulting reaction mixture, or the organic phase thereof after removal of the aqueous phase, is treated with an oxidizing agent.
    Type: Grant
    Filed: November 12, 1981
    Date of Patent: July 12, 1983
    Assignee: BASF Aktiengesellschaft
    Inventors: Peter Tonne, Hagen Jaedicke
  • Patent number: 4374855
    Abstract: A broad spectrum fungicidal naphthylene diester having the formula ##STR1## wherein R, R.sup.1 and R.sup.2 are each independently a radical having not more than 4 carbon atoms selected from the group consisting of alkenyl, haloalkenyl and haloalkyl; either m or n is 1 and the remaining subscript is zero and mixtures of the above diesters and the method of applying said diesters to plants for control of fungi infestation.
    Type: Grant
    Filed: April 3, 1981
    Date of Patent: February 22, 1983
    Assignee: GAF Corporation
    Inventor: Bruce M. Resnick
  • Patent number: 4349471
    Abstract: A process for the simultaneous preparation of an aromatic sulphonic acid halide and an aromatic carboxylic acid halide or the corresponding carboxylic acid is disclosed wherein an aromatic sulphonic acid or acid anhydride is reacted with an aromatic trihalogenomethyl compound in the presence of a Bronsted acid or Lewis acid at a temperature of 20.degree. to 300.degree. C., if appropriate in the presence of a solvent. Generally, at least half an equivalent of aromatic trihalogenomethyl compound is employed per equivalent of sulphonic acid.
    Type: Grant
    Filed: January 22, 1981
    Date of Patent: September 14, 1982
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz U. Blank, Erich Wolters, Norbert Langenfeld
  • Patent number: 4341906
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrollo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) -(alk.sub.1).sub.m -X-(alk.sub.2).sub.n - wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.
    Type: Grant
    Filed: December 22, 1980
    Date of Patent: July 27, 1982
    Assignee: Pfizer Inc.
    Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4335055
    Abstract: Compounds of the formula I ##STR1## in which Z, Z.sub.1, R, m and p are as defined in patent claim 1, can be obtained in a simple and economical manner by a novel process wherein a halide of the formula II ##STR2## is reacted with a substituted or unsubstituted vinylbenzene or vinylnaphthalene derivative in the presence of a base and of certain palladium catalysts, such as palladium acetate. The compounds (I) or functional derivatives preparable therefrom are useful, for example, for the preparation of known dyes or fluorescent brighteners, or can be used directly as fluorescent brighteners or as scintillators.
    Type: Grant
    Filed: May 8, 1981
    Date of Patent: June 15, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Hans-Ulrich Blaser, Dieter Reinehr, Alwyn Spencer
  • Patent number: 4335254
    Abstract: Disclosed herein are monomeric compounds having the formula: ##STR1## wherein: R and R.sup.1 are independently hydrogen, halide or alkyl;R.sup.2 and R.sup.3 are independently hydrogen, alkyl, cycloalkyl, aryl or aralkyl;q is 0 or 1; andAr is arylene wherein no more than one of R.sup.2 and R.sup.3 is hydrogen, and a method of preparing same.These monomers can be homopolymerized or coplymerized with one or more other monomers to yield polymers having desirable solubility characteristics. In particular, copolymerizable ethylenically unsaturated monomers can comprise aldehyde-containing vinylaryl ethers to yield crosslinkable polymers useful in relief image materials or as binders in photographic layers.
    Type: Grant
    Filed: May 29, 1981
    Date of Patent: June 15, 1982
    Assignee: Eastman Kodak Company
    Inventors: John C. Wilson, Paul D. Yacobucci
  • Patent number: 4333949
    Abstract: 2,3-Dichloro-7-hydroxy-1H-inden-1-one derivatives of the formula I ##STR1## wherein R.sub.1 is hydrogen or one of the groups ##STR2## R.sub.2 and R.sub.3 independently of one another are each hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl or nitro,R.sub.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.2 -C.sub.4 -alkenyl, each of which is unsubstituted or substituted by halogen, or R.sub.4 is phenyl which is unsubstituted or is substituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogen, trifluoromethyl, cyano or nitro, or it is a C.sub.3 -C.sub.6 -cycloalkyl group, andR.sub.5 is C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl or C.sub.2 -C.sub.4 -alkenyl.These compounds exhibit a microbicidal action against in particular phytopathogenic fungi and bacteria.
    Type: Grant
    Filed: June 5, 1981
    Date of Patent: June 8, 1982
    Assignee: Ciba-Geigy Corporation
    Inventors: Elmar Sturm, Robert Nyfeler
  • Patent number: 4317910
    Abstract: Compounds having the formula ##STR1## and the pharmaceutically acceptable salts thereof, wherein n is 1 or 2; m is 2, 3 or 4; and R.sub.2 is a tertiary amino group; are intermediates useful in the preparation of compounds having hypotensive activity.
    Type: Grant
    Filed: August 14, 1978
    Date of Patent: March 2, 1982
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Frederic P. Hauck, Joyce Reid
  • Patent number: 4316045
    Abstract: A process for the catalytic preparation of aryl carboxylates is provided in which an arylmetallo carboxylate is contacted in liquid medium with an organic peracid in the presence of a catalytic amount of an aryl iodide, to form the desired aryl carboxylate.
    Type: Grant
    Filed: August 29, 1980
    Date of Patent: February 16, 1982
    Assignee: The Halcon SD Group, Inc.
    Inventor: Lawrence C. Costa
  • Patent number: 4316046
    Abstract: A process for the preparation of aryl carboxylates is provided in which an arylmetallo carboxylate is contacted with an aryliodoso carboxylate in liquid medium to form the desired aryl carboxylate. Promoters can be employed to increase the rate of reaction and improve selectivity to the aryl carboxylate.
    Type: Grant
    Filed: August 29, 1980
    Date of Patent: February 16, 1982
    Assignee: The Halcon SD Group, Inc.
    Inventor: Lawrence C. Costa
  • Patent number: 4310529
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n --wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.
    Type: Grant
    Filed: December 22, 1980
    Date of Patent: January 12, 1982
    Assignee: Pfizer Inc.
    Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4310668
    Abstract: Compounds of the formula ##STR1## wherein R.sub.1 is hydrogen, benzyl, benzoyl, alkanoyl of 1 to 5 carbon atoms or --CO--(CH.sub.2).sub.p --NR'R" wherein p is 0 or an integer from 1 to 4; each of R' and R" when taken individually is hydrogen or alkyl of 1 to 4 carbon atoms; R' and R" when taken together with the nitrogen to which they are attached form a 5- or 6-membered heterocyclic ring selected from piperidino, pyrrolo, pyrrolidino, morpholino and N-alkylpiperazino having from 1 to 4 carbon atoms in the alkyl group;R.sub.2 is selected from hydrogen, alkanoyl of 1 to 6 carbon atoms and benzoyl;R.sub.3 is selected from hydrogen, methyl and ethyl;R.sub.4 is selected from hydrogen, alkyl of 1 to 6 carbon atoms and benzyl;Z is selected from:(a) alkylene having from one to nine carbon atoms;(b) --(alk.sub.1).sub.m --X--(alk.sub.2).sub.n -- wherein each of (alk.sub.1) and (alk.sub.2) is alkylene having from 1 to 9 carbon atoms, with the proviso that the summation of carbon atoms in (alk.sub.1) plus (alk.sub.
    Type: Grant
    Filed: December 22, 1980
    Date of Patent: January 12, 1982
    Assignee: Pfizer Inc.
    Inventors: Thomas H. Althuis, Charles A. Harbert, Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4301296
    Abstract: Ester such as 3,6,9-trioxaundecane-1,11-bis(3-n-dodecylthiopropionate) when combined with conventional free amine antioxidants such as N,N'-diphenylparaphenylenediamine or with polymer bound antioxidants such as N-(4-anilinophenyl) methacrylamide produce improved antioxidant systems for SBR and NBR type polymers.
    Type: Grant
    Filed: September 29, 1980
    Date of Patent: November 17, 1981
    Assignee: The Goodyear Tire & Rubber Company
    Inventor: Joseph A. Kuczkowski
  • Patent number: 4291061
    Abstract: 2,3-Dichloro-7-hydroxy-1H-inden-1-one derivatives of the formula I ##STR1## wherein R.sub.1 is hydrogen or one of the groups ##STR2## R.sub.2 and R.sub.3 independently of one another are each hydrogen, fluorine, chlorine, bromine, C.sub.1 -C.sub.4 -alkyl, trifluoromethyl or nitro,R.sub.4 is hydrogen, C.sub.1 -C.sub.6 -alkyl or C.sub.2 -C.sub.4 -alkenyl, each of which is unsubstituted or substituted by halogen, or R.sub.4 is phenyl which is unsubstituted or is substituted by C.sub.1 -C.sub.4 -alkyl, C.sub.1 -C.sub.4 -alkoxy, halogen, trifluoromethyl, cyano or nitro, or it is a C.sub.3 -C.sub.6 -cycloalkyl group, andR.sub.5 is C.sub.1 -C.sub.6 -alkyl, C.sub.3 -C.sub.6 -cycloalkyl or C.sub.2 -C.sub.4 -alkenyl.These compounds exhibit a microbicidal action against in particular phytopathogenic fungi and bacteria.
    Type: Grant
    Filed: October 31, 1979
    Date of Patent: September 22, 1981
    Assignee: Ciba-Geigy Corporation
    Inventors: Elmar Sturm, Robert Nyfeler
  • Patent number: H83
    Abstract: This invention concerns novel compounds useful in compositions and methods for preventing the attachment of dental plaque to the surfaces of the teeth of mammals and as inhibitors of connective tissue destruction. The compounds of this invention comprise certain [ureylenebis-(phenylenesulfonylimino)]bis[hydroxynaphthalenesulfonic acids] and salts thereof which may be combined with pharmaceutically acceptable carriers or diluents to be administered in the form of conventional pharmaceutical compositions.
    Type: Grant
    Filed: March 11, 1985
    Date of Patent: July 1, 1986
    Assignee: American Cyanamid Company
    Inventors: John F. Poletto, Seymour Bernstein