Patents Examined by David E. Wheeler
  • Patent number: 3962254
    Abstract: N-substituted cyclopentano[h]-1,2,3,4-tetrahydroisoquinolines of the formula ##SPC1##Wherein R and R.sub.1 represent hydroxy, lower alkoxy, lower akanoyloxy or aryl-lower alkanoyloxy groups, R.sub.3 represents hydrogen or a lower alkyl group and R.sub.4 represents a lower alkyl, arylcarbonyl, aryl-lower alkyl, benzhydryl-lower alkyl, lower alkanoyl, aryl-lower alkanoyl, benzhydryl-lower akanoyl or benzhydrylcarbonyl group, and acid addition salts and quaternary ammonium salts thereof, and pharmaceutical compositions containing the compounds useful for lowering blood pressure in animals.
    Type: Grant
    Filed: March 28, 1974
    Date of Patent: June 8, 1976
    Assignee: Marion Laboratories, Inc.
    Inventors: Ian William Mathison, William Ebenezer Solomons, Raymond Henry Jones
  • Patent number: 3962308
    Abstract: A new method for converting certain diesters to physiologically acceptable amines which comprises reacting the diester with the desired amine in a solvent consisting essentially of water.
    Type: Grant
    Filed: August 28, 1974
    Date of Patent: June 8, 1976
    Assignee: The Upjohn Company
    Inventor: Anthony A. Sinkula
  • Patent number: 3960861
    Abstract: A series of novel 2-amino and 4-aminoquinazoline derivatives have been prepared, including their acid addition salts. These derivatives all possess a single nitrogen-containing benzo-fused heterocyclic ring moiety at either the 4- or 2- positions of the molecule, respectively, with the ring moiety being attached through the nitrogen atom to the aforesaid quinazoline nucleus. Such compounds are useful in therapy as highly potent antihypertensive agents. Methods for their preparation are described in detail, including various synthetic routes leading to the required novel intermediates.
    Type: Grant
    Filed: September 5, 1973
    Date of Patent: June 1, 1976
    Assignee: Pfizer Inc.
    Inventors: John Christopher Danilewicz, John Edward Glyn Kemp, James Robert Wright
  • Patent number: 3960868
    Abstract: wherein Ph denotes a 1,2-phenylene radical which carries cycloaliphatic radical, R.sub.x denotes a free or etherified hydroxyl group or a free or substituted amino group, R.sub.o denotes an alkyl radical, a free hydroxyl group or a hydroxyl group etherified by lower alkyl or, above all, a hydrogen atom and R.sub.1 denotes an aliphatic or cycloaliphatic hydrocarbon radical which is optionally substituted by hydroxyl, an araliphatic radical or a hydrogen atom, and their salts, which possess valuable analgesic, anti-inflammatory, anti-microbial and histamine liberation inhibiting properties.
    Type: Grant
    Filed: May 6, 1974
    Date of Patent: June 1, 1976
    Assignee: Ciba-Geigy Corporation
    Inventors: Pier Giorgio Ferrini, Georges Haas, Alberto Rossi
  • Patent number: 3959284
    Abstract: The invention relates to bis (2-benzthiazole-dithio)-N,N'-piperazines of the general formula (I) ##SPC1##a process of their production and the use as a vulcanising agent for natural or synthetic rubber as well as a process for the vulcanisation of a natural or synthetic rubber.
    Type: Grant
    Filed: March 28, 1972
    Date of Patent: May 25, 1976
    Assignee: Bayer Aktiengesellschaft
    Inventors: Rudiger Schubart, Ulrich Eholzer
  • Patent number: 3959279
    Abstract: Anti-Histaminics of the formula ##SPC1##Wherein R.sub.1 is alkyl, alkenyl or phenalkyl, R.sub.2 and R.sub.3 are hydrogen, alkyl or alkenyl and R and R' are optional are prepared by reacting a 1-substituted isatoic anhydride with a S-methyl-thiopseudourea.
    Type: Grant
    Filed: July 24, 1974
    Date of Patent: May 25, 1976
    Assignee: Sandoz, Inc.
    Inventor: Goetz E. Hardtmann
  • Patent number: 3959289
    Abstract: Novel chemical compounds of the formula: ##SPC1##WhereinR is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, phenyl, alkali metal, or an amine cation;X and Y can be the same or different and are selected from the group consisting of hydrogen, alkyl of from one to six carbon atoms, inclusive, cycloalkyl of 5 or 6 carbon atoms, inclusive, phenyl, hydroxyl, alkoxy having from one to three carbon atoms, inclusive, halogen, trifluoromethyl, cyano, carboxyamide and O C-OQ, ##EQU1## where Q is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, alkali metal, and an amine cation, with the proviso that whereR is hydrogen, alkali metal or an amine cation, then Q is the same as R, and whereR is phenyl or alkyl from one to three carbon atoms, then Q is phenyl or alkyl from one to three carbon atoms; andZ is selected from the group consisting of hydrogen, alkyl from one to three carbon atoms, inclusive, and phenyl.
    Type: Grant
    Filed: December 11, 1974
    Date of Patent: May 25, 1976
    Assignee: The Upjohn Company
    Inventors: Charles M. Hall, Herbert G. Johnson, John B. Wright
  • Patent number: 3957764
    Abstract: The invention relates to hitherto unknown derivatives of 6-aminopenicillanic acids of the formula ##SPC1##In which R.sub.1 and R.sub.2 are similar or different aliphatic, cycloaliphatic, aromatic or heterocyclic substituents linked directly or through alkyl groups to the nitrogen atom, or R.sub.1 and R.sub.2 together with the nitrogen atom form a heterocyclic ring, and R.sub.3 is a hydroxyl or substituted hydroxyl group; to pharmaceutically acceptable salts, and to methods for producing these new compounds having a strong antibacterial effect, especially on gram-negative bacteria, to pharmaceutical preparations in dosage unit forms containing the compounds of the invention solely, or in synergistic mixtures with penicillins, and to methods of treating patients with the dosage units.
    Type: Grant
    Filed: November 6, 1972
    Date of Patent: May 18, 1976
    Assignee: Lovens Kemiske Fabrik Produktionsaktieselskab
    Inventor: Frantz Johannes Lund
  • Patent number: 3956292
    Abstract: New cephalosporin antibiotics of the general formula ##SPC1##Characterized by an 7-.alpha.-furoylureido or .alpha.-thenoylureido substituent and a 3-heterocyclic thiomethyl substitutent are provided. These cephalosporins and the pharmaceutically acceptable salts and certain esters, for example the acetoxymethyl esters thereof, have a broad antibiotic spectrum against both the gram-positive and gram-negative microorganisms.
    Type: Grant
    Filed: March 3, 1975
    Date of Patent: May 11, 1976
    Assignee: Eli Lilly and Company
    Inventor: Robin D. G. Cooper
  • Patent number: 3956333
    Abstract: (1-R- or 3-trifluoromethyl)-3,4-dihydro-2(1H)-isoquinolinecarboxamidoximes where R is pentafluoroethyl or heptafluoropropyl, having antithrombotic and antibacterial activities, are prepared by reacting the corresponding (1-R- or 3-trifluoromethyl)-3,4-dihydro-2(1H)-isoquinolinecarbonitriles which are prepared from the corresponding (1-R- or 3-trifluoromethyl)-3,4-dihydroisoquinolines via the (1-R- or 3-trifluoromethyl)-1,2,3,4-tetrahydroisoquinolines. Said tetrahydroisoquinoline where R is pentafluoroethyl also has antibacterial activity.
    Type: Grant
    Filed: June 19, 1975
    Date of Patent: May 11, 1976
    Assignee: Sterling Drug Inc.
    Inventor: Denis M. Bailey
  • Patent number: 3954802
    Abstract: 6-Acylamino-penam-3-carboxylic acids and 7-acylamino-3-cephem-4-carboxylic acids in which the acyl group has the formula ##EQU1## in which R.sub.1 is hydrogen, R.sub.2 is optionally substituted phenyl, thienyl or furyl, or R.sub.1 and R.sub.2 together are optionally substituted cycloalkyl, and B is a radical which is bonded via a sulphur atom or is bonded to oxygen or sulphur with the interposition of an optionally substituted CH.sub.2 -group.
    Type: Grant
    Filed: March 22, 1973
    Date of Patent: May 4, 1976
    Assignee: Ciba-Geigy Corporation
    Inventors: Karoly Kocsis, Bruno Fechtig, Hans Bickel
  • Patent number: 3954773
    Abstract: 4-Desacetoxyvinblastine, a novel indole-dihydroindole alkaloid obtained in small quantities from Vinca rosea, intermediate for the preparation of antimitotic compounds.
    Type: Grant
    Filed: November 21, 1974
    Date of Patent: May 4, 1976
    Assignee: Eli Lilly and Company
    Inventors: Norbert Neuss, Albert J. Barnes
  • Patent number: 3954775
    Abstract: Thiazolo[5,4-f]quinoline-8-carboxylic acid derivatives having either the general formula (I): ##SPC1##wherein R.sub.1 is a lower alkyl group, a lower alkenyl group or a benzyl group; or the general formula (III-a): ##SPC2##Wherein R.sub.3 is a lower alkyl group and X is a halogen atom; and methods for the preparation thereof. The compounds of the general formula (I) are useful as antibacterial agents against gram-negative and gram-positive bacteria. The compounds of the general formula (III-a) are useful as antifungal agents against eumycetes and also as an intermediate in a preparation of the compounds of the general formula (I).
    Type: Grant
    Filed: October 17, 1974
    Date of Patent: May 4, 1976
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Hideo Agui, Toru Mitani, Mitsuo Nakashita, Eiichi Murayama, Kousaku Okamura, Takenari Nakagome, Toshiaki Komatsu, Akio Izawa, Yasuko Eda
  • Patent number: 3954774
    Abstract: N-substituted cyclopentano[f]-1,2,3,4-tetrahydroisoquinolines of the formula ##SPC1##Wherein R.sub.1 and R.sub.2 represent hydroxy, lower alkoxy, lower alkanoyloxy or aryl-lower alkanoyl groups, R.sub.3 represents hydrogen or a lower alkyl group and R.sub.4 represents a lower alkyl, arylcarbonyl, aryl-lower alkyl, benzhydryl-lower alkyl, lower alkanoyl, aryl-lower alkanoyl, benzhydryl-lower alkanoyl or benzhydrylcarbonyl group, and acid addition salts and quaternary ammonium salts thereof, and pharmaceutical compositions containing one or more of the compounds useful for lowering blood pressure in animals.
    Type: Grant
    Filed: March 28, 1974
    Date of Patent: May 4, 1976
    Assignee: Marion Laboratories, Inc.
    Inventors: Ian William Mathison, William Ebenezer Solomons, Raymond Henry Jones
  • Patent number: 3953446
    Abstract: Quinazoline derivatives which have anti-inflammatory, antiviral, uricosuric activities are prepared by reacting an indole-2-carbonylazide derivative with an oxidizing agent under mild conditions.
    Type: Grant
    Filed: August 5, 1974
    Date of Patent: April 27, 1976
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Kikuo Ishizumi, Kazuo Mori, Michihiro Yamamoto, Masao Koshiba, Shigeho Inaba, Hisao Yamamoto
  • Patent number: 3953455
    Abstract: Novel bis basic esters of 9-substituted phenanthrene and related 9-oxa and 9-aza derivatives thereof, their preparation and use for the prevention and inhibition of viral infections are disclosed.
    Type: Grant
    Filed: September 13, 1974
    Date of Patent: April 27, 1976
    Assignee: Richardson-Merrell Inc.
    Inventors: Donald R. Meyer, Arthur D. Sill
  • Patent number: 3950340
    Abstract: Dyes of the formula: ##SPC1##In whichR is unsubstituted or substituted alkyl or aralkyl;R.sup.1 to R.sup.6 is each hydrogen or a substituent;R.sup.7 is hydrogen or alkoxy;R.sup.8 is hydrogen or alkoxy;n is zero or 1;X.sup.- is an anion; andR.sup.1 and R.sup.8 may together be a radical: ##SPC2##Where R.sup.9 is hydrogen, alkyl or alkoxy; and at least one of the radicals R.sup.1 to R.sup.6 is arylmercapto.The dyes give bright colorations, particularly on polyesters and in resins.
    Type: Grant
    Filed: July 24, 1973
    Date of Patent: April 13, 1976
    Assignee: Badische Anilin- & Soda-Fabrik Aktiengesellschaft
    Inventor: Ernst Schefczik
  • Patent number: 3947451
    Abstract: New pharmacodynamically active nitrogen containing heterocyclic compounds of the general formula ##SPC1##As well as methods of preparing the same; andPharmacodynamical compositions containing the same, preferrably for treating psychiatric and psychosomatic diseases.
    Type: Grant
    Filed: September 11, 1972
    Date of Patent: March 30, 1976
    Assignee: AB Kabi
    Inventors: Nils Ake Jonsson, Lembit Mikiver, Pinchas Moses
  • Patent number: 3947453
    Abstract: Side chain modification of 24-hydroxyimino-14a-aza-D-homo-cholesta-8(9), 14(14a)-dienes provides novel azasteroids having antifungal activities.
    Type: Grant
    Filed: September 6, 1974
    Date of Patent: March 30, 1976
    Assignee: Eli Lilly and Company
    Inventor: Charles D. Jones
  • Patent number: 3947454
    Abstract: 5 OR 1'-Hydroxy-2-alkyl-7,8-cyclopentano[h]-1,2,3,4-tetrahydroisoquinolines and esters of the formulas ##SPC1##Wherein R is a lower alkyl having 1 to 6 carbon atoms, R.sub.1 is hydrogen, a lower alkyl group, an alkanoyl, benzoyl or aralkanoyl group, R.sub.2 is a lower alkyl group and R.sub.3 is hydrogen, benzoyl, an alkanoyl group or an aralkanoyl group, and acid addition salts and quaternary ammonium salts thereof. The compounds are useful in pharmaceutical compositions for lowering blood pressure in animals.Wherein R is a lower alkyl having 1 to 6 carbon atoms, R.sub.1 is hydrogen, a lower alkyl group, an alkaoyl, benzoyl or aralkanoyl group, R.sub.2 is a lower alkyl group and R.sub.3 is hydrogen, benzoyl, an alkanoyl group or an aralkanoyl group, and acid addition salts and quaternary ammonium salts thereof. The compounds are useful in pharmaceutical compositions for lowering blood pressure in animals.
    Type: Grant
    Filed: March 28, 1974
    Date of Patent: March 30, 1976
    Assignee: Marion Laboratories, Inc.
    Inventors: Ian William Mathison, William Ebenezer Solomons, Raymond Henry Jones