Patents Examined by Robert C. Whittenbaugh
  • Patent number: 4948421
    Abstract: Disclosed is a novel compound of the formula [I]: ##STR1## wherein A represents ##STR2## (wherein X is H or Cl) ##STR3## Z represents ##STR4## (wherein R.sup.1 is H or CH.sub.3, R.sup.2 is H or C.sub.1 -C.sub.4 alkyl), furylmethyl group, tetrahydrofuryl group 2-tetrahydropyranylmethyl group or tetrahydrofurfuryl group which may be substituted with methyl group. The compound has strong herbicidal effect against the weeds belonging to the Family Gramineae.
    Type: Grant
    Filed: April 20, 1988
    Date of Patent: August 14, 1990
    Assignees: Tosoh Corporation, Agro-Kanesho Co., Ltd.
    Inventors: Sinzo Someya, Seigo Koura, Mikio Ito, Yoichi Kitamura, Hiroyuki Watanabe, Kenji Tsuzuki
  • Patent number: 4948916
    Abstract: A process for producing an aminooxyacetic acid salt comprises reacting benzhydroxamic acid of formula: ##STR1## (where R.sup.1 is a hydrogen atom, an alkyl group, an alkoxy group or a halogen atom) with a halogenoacetic acid of formula:XCH.sub.2 CO.sub.2 H (III)(where X is an iodine, bromine or chlorine atom) in the presence of a metal hydroxide or a metal carbonate to form benzamidooxyacetic acid of formula (IV): ##STR2## and thereafter hydrolyzing the benzamidooxyacetic acid in the presence of a mineral acid to obtain an aminooxyacetic acid salt of formula:2H.sub.2 NOCH.sub.2 CO.sub.2 H.
    Type: Grant
    Filed: September 7, 1988
    Date of Patent: August 14, 1990
    Assignee: Dainippon Ink and Chemicals, Inc.
    Inventors: Misao Uohama, Youichirou Tani
  • Patent number: 4948896
    Abstract: Improved process for preparing pyridine-2,3-dicarboxylic acid compounds of the formula: ##STR1## wherein R.sup.1 and R.sup.3 are each H, (un)substituted alkyl, or (un)substituted phenyl; R.sup.2 is H, (un)substituted alkyl, (un)substituted phenyl, alkylthio, alkoxy, (un)substituted phenylthio, (un)substituted phenoxy, halogen, alkoxycarbonyl, aminocarbonyl which may optionally be substituted, or cyano; or both of R.sup.1 and R.sup.2 or both R.sup.2 and R.sup.3 may combined together to form a divalent alkylene; and R.sup.4 and R.sup.
    Type: Grant
    Filed: July 6, 1988
    Date of Patent: August 14, 1990
    Assignee: Daiso Co., Ltd.
    Inventor: Keishiro Nagao
  • Patent number: 4939273
    Abstract: A method for conversion of ethylidene N,N'-bis-pyrrolidone, a by-product of the vinylation of 2-pyrrolidone, into 2-pyrrolidone starting material. This method is carried out by heating the by-product at an elevated temperature for a predetermined period of time, and recovering the 2-pyrrolidone conversion product therefrom for recycle into the vinylation process.
    Type: Grant
    Filed: August 24, 1989
    Date of Patent: July 3, 1990
    Assignee: GAF Chemicals Corporation
    Inventors: Kou-Chang Liu, Paul D. Taylor
  • Patent number: 4939248
    Abstract: This invention provides compounds of the formula ##STR1## wherein Y represents an acetyl, 1-hydroxyethyl or 1-fluoroethyl group, R.sub.1 represents a hydrogen atom or an easily splittable amino-protecting group, and R.sub.2 and R.sub.3 are identical or different and each represents a hydrogen atom, a lower alkyl group, a phenyl group, a benzyl group or a diphenylmethyl group, or R.sub.2 and R.sub.3 together represent a lower alkylene group; and processes for production thereof. These compounds are useful as synthesis intermediates for production of various medicines, particulary carbapenam or carbapenem antibiotics, such as a carbapenem antibiotic of the following formula which has excellent antimicrobial activity and relatively good stability to kidney dehydropeptidase.
    Type: Grant
    Filed: August 18, 1988
    Date of Patent: July 3, 1990
    Assignee: Sanraku Incorporated
    Inventors: Takeo Yoshioka, Machiko Watanabe, Yasuo Fukagawa, Tomoyuki Ishikura
  • Patent number: 4939300
    Abstract: Aminic orthoester derivatives of the formulae ##STR1## are effective in stabilizing organic materials against oxidative, thermal and actinic degradation.
    Type: Grant
    Filed: November 16, 1987
    Date of Patent: July 3, 1990
    Assignee: Ciba-Geigy Corporation
    Inventors: Linda A. Benjamin, Joseph E. Barbiarz, Stephen D. Pastor
  • Patent number: 4937346
    Abstract: Compound of the formula ##STR1## wherein n is 1 or 2, Y is OH, R.sup.1 COO--, R.sup.2 R.sup.3 NCOO-- or R.sup.4 O whereby R.sup.1 is an alkyl group, or a possibly substituted phenyl group, R.sup.2 is an alkyl, phenethyl, or benzyl or phenyl group, R.sup.3 is H or an alkyl group and R.sup.4 is an allyl or benzyl group, and R is an alkyl, hydroxyalkyl, dimethylaminoalkyl or methylthioalkyl group or alkenyl group, processes for their preparations and methods of treatment employing such compounds. The compounds are useful for therapeutic purposes, especially for treatment of disorders in the central nervous system.
    Type: Grant
    Filed: November 30, 1987
    Date of Patent: June 26, 1990
    Assignee: Per Arvid Emil Carlsson
    Inventors: Folke L. Arvidsson, Per A. E. Carlsson, Uli A. Hacksell, John S. M. Hjorth, Per L. Lindberg, John L. G. Nilsson, Domingo Sanchez, Nils U. E. Svensson, Hakan V. Wikstrom
  • Patent number: 4935515
    Abstract: Disclosed herein are novel 1,2,3,4,5,6-hexahydro[1,3,6]triazocino[1,2-a]benzimidazole of Formulas I and II: ##STR1## wherein R.sup.1 may be phenyl, m- or p-nitrophenyl, m- or p-methylsulfonylaminophenyl, napthtyl, naphthyl mono-substituted by nitro or methylsulfonylamino, benzofurazanyl, 2-pyrimidinyl, 2- or 4-pyridinyl, 2- or 4-naphthyridinyl, pyrazinyl, isoquinolinyl, or quinolinyl;R.sup.2 may be hydrogen; C.sub.1 -C.sub.8 alkyl; phenyl(C.sub.1 -C.sub.4)alkyl or substituted-phenyl(C.sub.1 -C.sub.4)alkyl, in which phenyl may have one to three substituents selected from C.sub.1 -C.sub.4 alkyl, C.sub.1 -C.sub.4 alkoxy, fluorine, chlorine or bromine; phenyl or substituted-phenyl in which the phenyl substituents are the same as for substituted-phenyl (C.sub.1 -C.sub.4)alkyl; 2- or 4-pyrimidinyl; pyrazinyl; imidazolyl; C.sub.1 -C.sub.4 alkanoyl; halo or dihalo-(C.sub.1 -C.sub.4)alkanoyl, in which halo is fluoro or chloro; benzoyl or benzoyl substituted on the phenyl ring by one or two C.sub.1 -C.sub.
    Type: Grant
    Filed: November 6, 1989
    Date of Patent: June 19, 1990
    Assignee: American Home Products Corporation
    Inventors: Michael W. Winkley, James L. Diebold
  • Patent number: 4935443
    Abstract: Disclosed are compounds having the formula: ##STR1## wherein: R.sub.1 is hydrogen, analkyl group having 1 to 6 carbon atoms, an alkyl group having 1 to 6 carbon atoms in which one or more of the carbon atoms are substituted with a hydroxy group;R.sub.2 is an alkyl group having 1 to 6 carbon atoms in which one or more of the carbon atoms are substituted with a hydroxy group, an alkyl group having 1 to 6 carbon atoms which contains an amino group in which the amino function is substituted with hydrogen or one or two individual alkyl groups having 1 to 6 carbon atoms;or a pharmaceutically acceptable salt thereof.These compounds increase the sensitivity of hypoxic cancer cells to radiation. Methods of preparing such compounds, protocols for administering them to human patients and animals, and pharmaceutical compositions containing them are also disclosed.
    Type: Grant
    Filed: June 26, 1989
    Date of Patent: June 19, 1990
    Assignee: Merck & Co., Inc.
    Inventor: Walfred S. Saari
  • Patent number: 4935413
    Abstract: A physical property-improving reagent which comprises an alkenoylcarbamate compound of the formula: ##STR1## wherein R is a hydrogen atom or a lower alkyl group, X is an oxygen atom (--O--), a sulfur atom (--S--) or a substituted or unsubstituted imino group (--NR'--), R' being a hydrogen atom or a lower alkyl group, and Y is the residue of an active hydrogen atom-containing compound excluding --X-H therefrom dissolved in an organic solvent having a solubility parameter of not less than 8, which can impact excellent physical properties to a polymer produced with the same.
    Type: Grant
    Filed: June 5, 1987
    Date of Patent: June 19, 1990
    Assignee: Nippon Paint Co., Ltd.
    Inventors: Satoshi Urano, Ryuzo Mizuguchi, Noriyuki Tsuboniwa, Kei Aoki, Yuji Suzuki, Takeyasu Itoh
  • Patent number: 4933482
    Abstract: A process for preparing an optically active alcohol is disclosed, which comprises asymmetrically hydrogenating a .beta.-keto acid derivative in the presence of a ruthenium-optically active phosphine complex as a catalyst. The resulting alcohol has high optical purity.
    Type: Grant
    Filed: June 9, 1988
    Date of Patent: June 12, 1990
    Assignee: Takasago International Corporation
    Inventors: Noboru Sayo, Takao Saito, Hidenori Kumobayashi, Susumu Akutagawa, Ryoji Noyori, Hidemasa Takaya
  • Patent number: 4931429
    Abstract: Compounds characterized generally as .alpha.-aminoacyl .beta.-aminoactyl aminodiols are useful as renin inhibitors for the treatment of hypertension.
    Type: Grant
    Filed: October 1, 1987
    Date of Patent: June 5, 1990
    Assignee: G. D. Searle & Co.
    Inventors: Gunnar J. Hanson, John S. Baran
  • 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: 4931087
    Abstract: A picolinic acid derivative having the formula: ##STR1## wherein R is a hydrogen atom, an alkyl group, an alkenyl group, an alkynyl group, an alkali metal atom, an alkaline earth metal atom, an alkylammonium group or ##STR2## [wherein R.sup.11 is a hydrogen atom or an alkyl group, R.sup.12 is an alkoxycarbonyl group, a cyano group, a halogen atom, an acetyl group, a pivaloyl group, a benzoyl group, an alkoxy group, a phenoxy group, a halogenoacetyloxy group, a methylsulfonyloxy group, a hydroxyl group, an alkylthio group, an alkylsulfonyl group, a phenylthio group, a dialkylamino group, a naphthyl group, a pyridyl group, ##STR3## (wherein W is a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a phenoxy group, a nitro group or an alkoxycarbonyl group, and e is 1 or 2) or ##STR4## (wherein each of R.sup.3 and R.sup.4 which may be the same or different, is a hydrogen atom, an alkyl group, an alkenyl group or a phenyl group), and m is an integer of from 0 to 2], each of R.sup.1 and R.sup.
    Type: Grant
    Filed: January 12, 1989
    Date of Patent: June 5, 1990
    Assignees: Kumiai Chemical Industry Co., Ltd., Ihara Chemical Industry Co., Ltd.
    Inventors: Masahiro Shigematsu, Hideo Ohi, Shoji Kusano, Takeshige Miyazawa, Satoru Takahashi, Yasuhumi Toyokawa, Ikuo Kajiwara
  • Patent number: 4929728
    Abstract: A process for preparing 3-(1H-tetrazol-5-yl)-4(3H)-quinazolinone ammonium salts of the formula I: ##STR1## wherein: R is hydrogen, halogen, C.sub.1 -C.sub.3 alkyl or C.sub.1 -C.sub.3 alkoxy,which process comprises:reacting ethyl N-(1H-tetrazol-5-yl) formimidate in an inert solvent with substituted anthranilamide of the formula IV ##STR2## wherein R is as defined above. The process is simpler than prior processes for preparing the same compounds and thus is economically valuable.
    Type: Grant
    Filed: November 2, 1989
    Date of Patent: May 29, 1990
    Assignee: National Science Council
    Inventors: Ji-Wang Chern, Kang-Chien Liu, Chia-Yin Chen
  • Patent number: 4927449
    Abstract: Novel herbicidal tricyclic 1H-imidazole-5-carboxylic acid derivatives, compositions containing these compounds as active ingredients, and a method for controlling weeds, preferably selectively in crops of useful plants.
    Type: Grant
    Filed: December 27, 1988
    Date of Patent: May 22, 1990
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: William R. Lutz, Wim G. Verschueren, Hanspeter Fischer, Guy R. E. Van Lommen
  • Patent number: 4927842
    Abstract: Substituted 2,3,4,9-tetrahydro-1H-carbazole-1-acetic acid derivatives and methods for their preparation and use are disclosed. The compounds are useful anti-inflammatory agents.
    Type: Grant
    Filed: September 29, 1989
    Date of Patent: May 22, 1990
    Assignee: American Home Products Corporation
    Inventor: Dominick Mobilio
  • Patent number: 4925942
    Abstract: A process for the preparation of quinuclidine-3-methanol comprising reacting quinuclidine-3-one acid addition salt with an alkali metal cyanide in an aqueous media to obtain 3-cyano-3-hydroxy-quinuclidine, reacting the latter with anhydrous methanol in the presence of hydrogen chloride gas followed by treatment with aqueous alkali to obtain methyl 3-hydroxy-quinuclidine-3-carboxylate, reacting the latter with thionyl chloride to form methyl 1-azabicyclo(2,2,2)oct-2-ene-3-carboxylate, hydrogenating the latter with Raney nickel to obtain methyl 1-azabicyclo(2,2,2)octane-3-carboxylate and reducing the latter to obtain quinuclidine-3-methanol which is an intermediate for mequitazine which is useful as an antihistaminic.
    Type: Grant
    Filed: July 24, 1989
    Date of Patent: May 15, 1990
    Assignee: Rutgerswerke AG
    Inventors: Josef Gotz, Winfried Orth, Wolfgang Weiss, Bernd Rapp, Hans W. Kleffner
  • Patent number: 4925974
    Abstract: A process for the production of a blocked urea group-containing polyisocyanate from a partially blocked polyisocyanate and polyamine, comprising the steps of:(i) reacting a partially blocked polyisocyanate, said polyisocyanate being made substantially free of monomeric polyisocyanate, by vacuum thin layer evaporation with a primary polyamine, secondary polyamine, or mixtures thereof, in relative proportions such that the ratio of isocyanate groups to amino groups is in the range from about 1:1 to 1.3:1, and(ii) isolating said urea group-containing polyisocyanate by wherein the vacuum boiling point of said polyisocyanate is lower than the deblocking temperature of said urea group-containing polyisocyanate.
    Type: Grant
    Filed: September 16, 1988
    Date of Patent: May 15, 1990
    Assignee: Huels Aktiengesellschaft
    Inventor: Rainer Gras
  • Patent number: 4925855
    Abstract: New imidazole derivatives of the formula ##STR1## in which Ar denotes phenyl, biphenylyl, naphthyl or thienyl, each of which is optionally substituted by halogen, lower alkyl or lower alkoxy, R.sub.1 denotes hydrogen or lower alkyl, Alk denotes straight-chain or branched alkylene having 1 to 10 carbon atoms, Y denotes oxygen, sulfur, sulfinyl or sulfonyl, n denotes one of the numbers 0, 1 or 2, Z denotes sulfur or sulfinyl, m denotes the number 0 or 1, m being the number 0 when Y denotes sulfur, sulfinyl or sulfonyl, and m being the number 1 when Y denotes oxygen, and R.sub.2 denotes cyclohexyl, phenyl or naphthyl, each of which is optionally substituted by hydroxyl, halogen, trifluoromethyl, lower alkyl or lower alkoxy, or denotes biphenylyl or pyridyl, and processes for their preparation. The imidazole derivatives have excellent antimycotic properties for use in human and veterinary medicine.
    Type: Grant
    Filed: December 23, 1987
    Date of Patent: May 15, 1990
    Assignee: CL Pharma Aktiengesellschaft
    Inventors: Karl Schermanz, Gerald Saischek, Robert Urmann, Kurt Martetschlager