Patents Examined by Lenora A. Miltenberger
  • Patent number: 5075452
    Abstract: Compounds of the formula I ##STR1## in which A and X.sup.1 have the meaning given in patent claim 1 can be prepared in a simple manner, in a one-pot process and in high yields.
    Type: Grant
    Filed: December 6, 1989
    Date of Patent: December 24, 1991
    Assignee: Merck Patent Gesellschaft mit beschrankter Haftung
    Inventors: Richard Kirchlechner, Michael Casutt, Arno Basedow
  • Patent number: 5075330
    Abstract: The present invention includes N-hydroxyamide, N-hydroxyurea, N-hydroxythioamide, and N-hydroxythiourea derivatives of fenamates, indomethacin, cicloprofen, oxepinac, and indoprofen as dual inhibitors or selective ihibitors of cyclooxygenase and 5-lipoxygenase.
    Type: Grant
    Filed: October 16, 1990
    Date of Patent: December 24, 1991
    Assignee: Warner-Lambert Co.
    Inventors: Thomas R. Belliotti, Wiaczeslaw A. Cetenko, David T. Connor, Daniel L. Flynn, Catherine R. Kostlan, James B. Kramer, Jagadish C. Sircar
  • Patent number: 5066810
    Abstract: A process for the preparation of compounds of formula I ##STR1## in which X is the radical OH or Cl, by the catalytic hydrogenation of 3,5-dimethyl-4-methoxy-2-cyanopyridine, subsequent reaction of the resulting 3,5-dimethyl-4-methoxy-2-aminomethylpyridine to give 3,5-dimethyl-4-methoxy-2-hydroxymethylpyridine and, if desired, chlorination to give 3,5-dimethyl-4-methoxy-2-chloromethylpyridine, and the novel intermediate 3,5-dimethyl-4-methoxy-2-aminomethylpyridine.
    Type: Grant
    Filed: November 7, 1989
    Date of Patent: November 19, 1991
    Assignee: CL Pharma Aktiengesellschaft
    Inventor: Karl Baumann
  • Patent number: 5057533
    Abstract: An agricultural or horticultural fungicide comprising a compound of the following formula (I), as an active ingredient: ##STR1##
    Type: Grant
    Filed: July 26, 1990
    Date of Patent: October 15, 1991
    Assignee: Hodogaya Chemical Co., Ltd.
    Inventors: Kenichi Tanaka, Shinji Nishimura, Hiroshi Kawada, Katsuya Yamaguchi, Yumi Mizumura, Chieko Nomura
  • Patent number: 5049315
    Abstract: The present invention provides polycarboxylic acid imidazolines of the general formula: ##STR1## wherein X is --Cl, --OH, --O--SO.sub.3 H, --O--PO.sub.3 H.sub.2, --O--CH.sub.2 --CH.sub.2 --COOH, --NH.sub.2, --NHalk or --N(alk).sub.2, alk being an alkyl radical containing up to 6 carbon atoms, n is a whole number of from 2 to 4, R is a C.sub.8 -C.sub.18 hydrocarbon radical which is straight-chained, branched, saturated or one to three times unsaturated, m is a whole number of from 2 to 5, R' is a hydrogen atom or a carboxyl group and R" is a hydrogen atom or a methyl radical. The present invention also provides a process for the preparation of these compounds and cleaning agents containing them.
    Type: Grant
    Filed: June 8, 1990
    Date of Patent: September 17, 1991
    Assignees: Chemisches Instutut Schaefer AG, Joh. A. Benskiser GmbH
    Inventors: Hans Hitz, Rolf Schaefer, Heinrich Baust, Wolfgang Gross
  • Patent number: 5045558
    Abstract: The invention relates to N-substituted imidazoles, processes for their production as well as their use in pharmaceutical agents. The compounds according to the invention have aromatase-inhibiting properties.
    Type: Grant
    Filed: March 31, 1989
    Date of Patent: September 3, 1991
    Assignee: Schering Aktiengesellschaft
    Inventors: Peter Strehlke, Rolf Bohlmann, David Henderson, Yukishige Nishino
  • Patent number: 5043445
    Abstract: 3-7-Diheterabicylo[3.3.1]nonanes and derivatives thereof are disclosed. Their method of preparation and use as antiarrhythmic agents is given.
    Type: Grant
    Filed: November 15, 1990
    Date of Patent: August 27, 1991
    Assignee: Oklahoma State University
    Inventors: Kenneth D. Berlin, Mark D. Thompson, Benjamin J. Scherlag, Gary S. Smith
  • Patent number: 5041565
    Abstract: Novel hydrazinocarbonyloxylabdanes, intermediates and processes for the preparation thereof, and a method for treating cardiac failure utilizing compounds or compositions thereof are disclosed.
    Type: Grant
    Filed: August 30, 1989
    Date of Patent: August 20, 1991
    Assignee: Hoechst-Roussel Pharmaceuticals Inc.
    Inventors: Raymond W. Kosley, Jr., Gerard J. O'Malley
  • Patent number: 5041436
    Abstract: The invention relates to the products of formula ##STR1## in which R represents the radical ##STR2## in which R.sub.1 at any position on the benzene ring represents linear, branched or cyclic alkyl, alkenyl or alkynyl containing up to 8 carbon atoms, or the radical ##STR3## in which R.sub.2 and R.sub.3, which may be identical or different, represents hydrogen or linear alkyl, alkenyl or alkynyl containing up to 8 carbon atoms or form, together with the nitrogen atom to which they are attached, a carbonaceous heterocyclic radical optionally containing another hetero atom, or the radical OR', R' representing hydrogen, a linear, branched or cyclic alkyl containing up to 8 carbon atoms or aryl containing up to 14 carbon atoms, or the radical SR.sub.4 or S(O)R.sub.5, R.sub.4 and R.sub.5 representing linear, branched or cyclic alkyl, alkenyl, or alkynyl containing up to 8 carbon atoms, or R represents naphthyl optionally substituted with the radical R'.sub.1, R'.sub.1 being as defined above for R.sub.
    Type: Grant
    Filed: February 21, 1990
    Date of Patent: August 20, 1991
    Assignee: Roussel Uclaf
    Inventors: Emilio Toja, Fernando Barzaghi, Giulio Galliani
  • Patent number: 5030638
    Abstract: A method for providing enhanced antiviral activity with N-alkyl derivatives of 1,5-dideoxy-1,5-imino-D-glucitol is disclosed which comprises selectively increasing the alkyl chain length to at least 5 carbon atoms and up to about 10 carbon atoms to thereby improve the spectrum of enzyme inhibitory activity and the in vivo half life.
    Type: Grant
    Filed: July 19, 1990
    Date of Patent: July 9, 1991
    Assignee: G. D. Searle & Co.
    Inventors: Richard A. Partis, Richard A. Mueller
  • Patent number: 5030644
    Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: July 9, 1991
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David C. Remy, David A. Claremon
  • Patent number: 5026722
    Abstract: The invention relates to indole derivatives of the general formula (I) ##STR1## wherein Im represents an imidazolyl group of the formula: ##STR2## and R.sup.1 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-10 alkynyl, C.sub.3-7 cycloalkyl, C.sub.3-7 cycloalkylC.sub.1-4 alkyl, phenyl or phenylC.sub.1-3 alkyl;R.sup.2 represents a hydrogen atom or a group selected from C.sub.1-6 alkyl, C.sub.3-6 alkenyl, C.sub.3-7 cycloalkyl, phenyl or phenylC.sub.1-3 alkyl;X represents an oxygen atom or the group NR.sup.3 (where R.sup.3 represents a hydrogen atom or a C.sub.1-6 alkyl group);one of the groups represented by R.sup.4, R.sup.5 and R.sup.6 is a hydrogen atom or a C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl, C.sub.3-6 alkenyl, phenyl or phenylC.sub.1-3 alkyl group, and each of the other two groups, which may be the same or different, represents a hydrogen atom or a C.sub.1-6 alkyl group;Q represents a hydrogen or a halogen atom, or a hydroxy, C.sub.1-4 alkoxy, phenylC.sub.
    Type: Grant
    Filed: June 15, 1989
    Date of Patent: June 25, 1991
    Assignee: Glaxo Group Limited
    Inventors: Alexander W. Oxford, Peter C. North, David J. Cavalla
  • Patent number: 5025031
    Abstract: Herein disclosed is a method of treating convulsions with a pharmaceutical composition containing a compound of the formula:(HO).sub.p --A--[OSO.sub.2 NR.sup.1 R.sup.2 ].sub.zwhere A is an aryl, arylalkyl, or aryloxyalkyl group and is substituted on 1 or more carbon atoms with a sulfamate group (--OSO.sub.2 NR.sup.1 R.sup.2) wherein R.sup.1 and R.sup.2, same or different, are hydrogen or loweralkyl wherein p is 0 or 1 and is the number of untreated hydroxyl groups and z is 1 or 2 and is the number of --OS(O.sub.2)NR.sup.1 R.sup.2 groups. Aryl is selected from phenyl, substituted phenyl, pyridinyl, naphthyl, quinolinyl, and the like. Phenyl substituents are selected from hydrogen, halo, hydroxy, phenyl, phenoxy, benzoyl, loweralkyl, loweralkoxy, carboxy, amino, loweralkylamino, diloweralkylamino, acetamido, cyano, nitro, loweralkoxycarboyl, aminosulfonyl, imidazolyl, triazolyl, and the like. Novel compounds not previously disclosed are also described.
    Type: Grant
    Filed: November 30, 1989
    Date of Patent: June 18, 1991
    Assignee: A. H. Robins Co., Inc.
    Inventors: Young S. Lo, David A. Walsh, Ibrahim M. Uwaydah
  • Patent number: 5025025
    Abstract: Disclosed are the compounds of formula ##STR1## wherein A represents lower alkylene; B represents oxygen, sulfur, lower alkylene, lower alkylene interrupted by oxygen, sulfur, sulfinyl or sulfonyl, (oxy-, sulfinyl-, sulfonyl- or thio)-lower alkylene, lower alkenylene, phenylene or a direct bond; M represents lower alkylene, lower alkylene interrupted by oxygen, sulfur, sulfinyl or sulfonyl, (oxy-, sulfinyl, sulfonyl- or thio)-lower alkylene, lower alkenylene or a direct bond; or one of A, B and M represents lower alkylidenylene and the other two independently represent lower alkylene; R represents hydrogen unless A, B or M represents lower alkylidenylene in which case R represents the second bond to the adjacent aklylidenylene unsaturated carbon atom; Het represents 1-imidazolyl, 3-pyridyl, or 1-imidazolyl or 3-pyridyl substituted by lower alkyl; Ar represents carbocyclic or heterocyclic aryl; pharmaceutically acceptable ester and amide derivatives thereof; the N-oxides of said compounds wherein Het represent
    Type: Grant
    Filed: May 23, 1990
    Date of Patent: June 18, 1991
    Assignee: Ciba-Geigy Corporation
    Inventors: Shripad S. Bhagwat, Alan J. Main, Herman R. Rodriguez
  • Patent number: 5023337
    Abstract: The present invention is directed to the preparation of benzimidazole derivatives of the formula (I), ##STR1## wherein A=stands for S, SO or SO.sub.2,R.sup.1 =stands for C.sub.1-4 alkyl group,R.sup.2 =stands for C.sub.1-4 alkyl, C.sub.3-7 cycloalkyl or C.sub.6-10 aryl or aralkyl,comprising reacting a sulphochloride of the formula (II) ##STR2## with an alkyl aluminum compound of the formula (III).R.sub.n.sup.2 AlClhd (3-n) (III)The reaction is performed in one step.
    Type: Grant
    Filed: January 19, 1990
    Date of Patent: June 11, 1991
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Ferenc Sperber, Csaba Huszar, Attila Nemeth, Eva Somfai, Iren Pali nee Ivanics
  • Patent number: 5023269
    Abstract: The present invention provides 3-aryloxy-3-substituted propanamines capable of inhibiting the uptake of serotonin and norepinephrine.
    Type: Grant
    Filed: March 27, 1990
    Date of Patent: June 11, 1991
    Assignee: Eli Lilly and Company
    Inventors: David W. Robertson, David T. Wong, Joseph H. Krushinski, Jr.
  • Patent number: 5023256
    Abstract: Novel imidazopyridine derivatives of formula: ##STR1## wherein, R represents an alkoxyalky radical having 4-6 carbon atoms or a benzyl radical optionally substituted by a halogen atom, an alkyl or alkoxy radical having up to 3 carbon atoms,X represents hydrogen or an alkyl radical having up to 3 carbon atoms,n represents 0 or 1m represents an integer of from 2 to 5 inclusive,R.sub.1 and R.sub.2 may be the same or different and represent a saturated or unsaturated alkyl radical containing up to 4 carbon atoms or they, taken together with the adjacent nitrogen atom, may form a pyrrolidine, piperazine or homopiperazine ring which may be optionally substituted by an alkyl radical containing up to 3 carbon atoms, provided that when n is zero also m is zero and --N(R.sub.1)R.sub.2 represents the above defined piperazine or homopiperazine ring.The compounds (I) have an antihistaminic activity.
    Type: Grant
    Filed: May 7, 1990
    Date of Patent: June 11, 1991
    Assignee: Dompe Farmaceutici S.p.A.
    Inventors: Giani Roberto, Parini Ettore, Borsa Massimiliano, Lavezzo Antonio
  • Patent number: 5021440
    Abstract: Imidazole compounds including imidazoles and imidazolium salts, and their use as transglutaminase inhibitors are disclosed.
    Type: Grant
    Filed: July 31, 1989
    Date of Patent: June 4, 1991
    Assignee: Merck & Co., Inc.
    Inventors: David C. Remy, John J. Baldwin, David A. Claremon, Stella W. King
  • Patent number: 5021583
    Abstract: A Reissert compound of bisbenzimidazole can be formed by first reacting benzimidazole with an aliphatic diacid chloride to form bisbenzimidazole and then reacting the bisbenzimidazole with an aliphatic acid chloride and cyanide to form the Reissert compound thereof.
    Type: Grant
    Filed: September 21, 1990
    Date of Patent: June 4, 1991
    Assignee: Virginia Tech Intellectual Properties, Inc.
    Inventors: Harry V. Gibson, Yajnanarayana H. R. Jois
  • Patent number: 5019587
    Abstract: The present invention provides compounds of the general formula (I) which inhibit the aggregation of erythrocytes or thrombocytes ##STR1## wherein A is hydrogen or C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.2 -C.sub.6 -alkynyl, benzyl or C.sub.3 -C.sub.7 -cycloalkyl radical, B is hydrogen, R.sub.1 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl or C.sub.3 -C.sub.7 -cycloalkyl radical, R.sub.2 is a C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkenyl, C.sub.3 -C.sub.7 -cycloalkyl, C.sub.1 -C.sub.6 -alkylcarbonyl, C.sub.1 -C.sub.6 -alkoxycarbonyl, aminocarbonyl or hydrazinocarbonyl radical, or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a C.sub.3 -C.sub.7 -cycloalkyl ring, n is 0, X is a valency bond or a C.sub.1 -C.sub.6 -alkylene radical, R.sub.3 is a carbocyclic aromatic ring, which may be substituted; and the tautomers, optically-active forms and physiologically acceptable salts thereof with organic and inorganic acids.
    Type: Grant
    Filed: June 5, 1989
    Date of Patent: May 28, 1991
    Assignee: Boehringer Mannheim GmbH
    Inventors: Wolfgang V. Von Der Saal, Alfred Mertens, Erwin Boehm