Patents Examined by Diana G. Rivers
  • N.sub.b -Quaternary derivatives of sandwicine and isosandwicine methods and intermediate products in the manufacture of their derivatives and methods of using same and pharmaceutical compositions thereof
    Patent number: 4552877
    Abstract: New N.sub.b -quaternary 10-bromosandwicine and 10-bromoisosandwicine derivatives are disclosed which exhibit antiarrhythmic properties and adrenolytic properties and which have the formula I ##STR1## wherein R represents a carbon-attached organic group containing 1 to 10 carbon atoms and A.sup..crclbar. represents an acid anion, as well as pharmaceutical formulations thereof and processes and intermediates for their preparation.
    Type: Grant
    Filed: May 31, 1984
    Date of Patent: November 12, 1985
    Assignee: Kali-Chemie Pharma GmbH
    Inventors: Wolfgang Kehrbach, Joachim Wegener, Ulrich Kuehl, Renke Budden, Gerd Buschmann
  • Pyrido[2,1-b]quinazoline derivatives useful as agents for treatment of allergic conditions and vascular disorders involving thrombosis
    Patent number: 4551460
    Abstract: Pyrido[2,1-b]quinazoline derivatives of the formulas ##STR1## wherein R.sub.1, R.sub.2 and R.sub.3 are as hereinafter set forth, are described. The compounds of formulas I and II are useful as agents for the treatment of allergic conditions as well as for the treatment of vascular disorders involving thrombosis.
    Type: Grant
    Filed: March 2, 1983
    Date of Patent: November 5, 1985
    Assignee: Hoffmann-La Roche Inc.
    Inventor: Jefferson W. Tilley
  • Eburnane derivatives, process for their preparation and pharmaceutical compositions containing them
    Patent number: 4551462
    Abstract: The invention relates to racemic or optically active eburnane derivatives of the formula (I), ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms,A stands for hydroxyl andY is hydrogen, orA and Y together form an oxo group,and the configuration of the hydrogen in the 3-position and of R is .alpha.,.alpha. and/or .beta.,.beta. or .alpha.,.beta. and/or .beta.,.alpha.,and acid addition salts thereof.The new compounds possess valuable pharmaceutical properties, thus their certain representatives show antiallergic activity, while others are potent antidepressive, gastric secretion inhibiting and anticonvulsive agents. The compounds of the formula (I) and pharmaceutically acceptable acid addition salts thereof can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the invention.
    Type: Grant
    Filed: June 27, 1983
    Date of Patent: November 5, 1985
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Janos Sapi, Eva Palosi, Bela Kiss, Elemer Ezer, Gyorgy Hajos
  • Maleimido substituted aromatic cyclotriphosphazenes
    Patent number: 4550177
    Abstract: 4-Aminophenoxy cyclotriphosphazenes are reacted with maleic anhydride to produce maleamic acids which are converted to the maleimides. The maleimides are polymerized. By selection of starting materials (e.g. hexakis amino or trisaminophenoxy-trisphenoxy-cyclotriphosphazenes), selection of molar proportions of reactants, use of mixtures of anhydrides and use of dianhydrides as bridging groups a variety of maleimides and polymers are produced. The polymers have high limiting oxygen indices, high char yields and other useful heat and fire resistant properties making them useful as, for example, impregnants of fabrics.
    Type: Grant
    Filed: April 11, 1984
    Date of Patent: October 29, 1985
    Assignee: The United States of America as represented by the Administrator of the National Aeronautics and Space Administration
    Inventors: Devendra Kumar, George M. Fohlen, John A. Parker
  • Platinum chelates of 2-hydrazino-azoles
    Patent number: 4550169
    Abstract: This disclosure describes platinum chelates of 2-hydrazino-1-aza (or 1,3-diaza,1-oxa-3-aza or 1-thia-3-aza)-1-cyclo-alkenes which possess activity as antitumor agents.
    Type: Grant
    Filed: November 21, 1983
    Date of Patent: October 29, 1985
    Assignee: American Cyanamid Company
    Inventors: Joseph J. Hlavka, Panayota Bitha, Yang-I Lin
  • Composition and methods for the treatment of chronic obstructive airway disease and cardiac disease using 3-alkylxanthines
    Patent number: 4548818
    Abstract: Compounds having activity against chronic obstructive airway disease or cardiac disease, characterized by the formula ##STR1## wherein R.sup.1 is n-propyl, n-butyl, isobutyl, n-pentyl, 2-methylbutyl, 3-methylbutyl, 2,2-dimethylpropyl, cyclopropyl, cyclobutyl, cyclopentyl or cyclohexylmethyl, and R.sup.2 is hydrogen or methyl, provided that R.sup.2 is methyl when R.sup.1 is n-propyl, n-butyl or isobutyl, or a physiologically acceptable salt thereof.
    Type: Grant
    Filed: November 23, 1981
    Date of Patent: October 22, 1985
    Inventors: Per G. Kjellin, Carl G. A. Persson
  • Eburnane oxime ethers
    Patent number: 4549020
    Abstract: The invention relates to optically active or racemic eburnane-oxime ethers of the formulae (Ia) and/or ##STR1## wherein R represents an alkyl group having 1 or 2 carbon atoms,R.sup.2 represents an alkyl group having 1 to 6 carbon atoms,and the configuration of the hydrogen in the 3-position and the R.sup.2 group is .alpha.,.alpha. and/or .beta.,.beta. or .alpha.,.beta. and/or .beta.,.alpha. and acid addition salts thereof.The new compounds show valuable pharmaceutical activities, thus are potent CNS-tranquillants, smooth muscle relaxants, sedatives and hypnotic agents, and can therefore be employed as active ingredients of pharmaceutical compositions, which are also within the scope of the present invention.
    Type: Grant
    Filed: June 27, 1983
    Date of Patent: October 22, 1985
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Janos Sapi, Maria Zajer nee Balazs, Bela Kiss, Elemer Ezer, Egon Karpati, Laszlo Szporny
  • 1,4,5,6,7,8-Hexahydro-2-methyl-5-oxo-4-(2-thiazolyl)-3-quinoline carboxylic acid 2-methyl(phenylmethyl)amino ethyl ester and pharmaceutically acceptable salts
    Patent number: 4546186
    Abstract: 1,4,5,6,7,8-Hexahydro-4-heterocyclyl-5-oxo-quinoline derivatives and corresponding acridine derivatives and pharmaceutically acceptable salts thereof are useful antihypertensive agents.
    Type: Grant
    Filed: December 14, 1983
    Date of Patent: October 8, 1985
    Assignee: American Home Products Corporation
    Inventor: Magid A. Abou-Gharbia
  • Process for preparing 2-anilinoacridone
    Patent number: 4544746
    Abstract: A process is disclosed wherein 2,5-di(phenylamino) terephthalic acid is half-cyclized by dissolving it in a mixture of polyphosphoric acid and phosphoric acid and heating at 100.degree.-120.degree. C. to form 2-(phenyl)amino-3-carboxy-9(10H)acridone (ACA). The ACA is decarboxylated to form 2-(phenyl)amino-9(10H)acridone, also known as 2-anilinoacridone, by dissolving it in tetramethylene sulfone and heating in the presence of a basic cupric carbonate catalyst.
    Type: Grant
    Filed: May 17, 1982
    Date of Patent: October 1, 1985
    Assignee: Ciba-Geigy Corporation
    Inventor: Wilfried G. Holtje
  • Schistosomicidal acridanone hydrazones
    Patent number: 4544659
    Abstract: Acridanone derivatives of the formula ##STR1## wherein the dotted line is an optional bond, R.sup.1 is hydrogen, halogen or nitro, R.sup.2 is hydrogen or lower alkyl, one of the substituents R.sup.3 and R.sup.4 is hydrogen or lower alkyl and the other together with R is an additional bond and R.sup.5 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl or lower alkyl substituted by halogen or lower alkoxy,and pharmaceutically acceptable acid addition salts thereof, processes for their preparation and pharmaceutical compositions based thereon, are described. The compounds of formula I are useful as schistosomicidal agents.
    Type: Grant
    Filed: November 15, 1983
    Date of Patent: October 1, 1985
    Assignee: Hoffman-La Roche Inc.
    Inventors: Urs Brombacher, Marc Montavon, Hermann Bretschneider, Joachim Schantl, Wolfgang Turk
  • Anti-hypertensive 9-aminomethyl-benzo[f]quinoline-3,10-dione derivatives
    Patent number: 4543354
    Abstract: Benzo[f]quinoline derivatives which are useful as antihypertensive agents and are represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl, R.sup.2 is hydrogen, lower alkyl, hydroxy-lower-alkyl or lower-alkoxy-lower-alkyl, R.sup.3 and R.sup.4 are the same or different and each is hydrogen, lower alkyl, halogen, lower alkoxy, benzyloxy or hydroxy, R.sup.5 and R.sup.6 are the same or different and each is hydrogen, straight or branched alkyl, aralkyl or cycloalkyl, or R.sup.5 and R.sup.6 together with the adjacent nitrogen atom form a heterocycle, and the dotted line in the ring is an optional bond between 1- and 2-positions, and pharmaceutically acceptable acid addition salts thereof.
    Type: Grant
    Filed: November 10, 1983
    Date of Patent: September 24, 1985
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Toru Nakao, Tsuguo Ikebe, Tetsuya Tahara, Yutaka Maruyama, Osamu Yaoka
  • (-)-10,1L Methylenedioxy-N-N-propylnoraporphine and methods employing it for inhibiting the effects of epileptic seizures and for prevention and treatment of duodenal ulcers
    Patent number: 4543256
    Abstract: A method for providing orally effective aporphine compounds, and new compounds which are orally effective in the prevention and treatment of duodenal ulcers and in the treatment of neurological and psychiatric disorders having the following formula ##STR1## wherein R.sub.1 is lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, phenyl lower alkyl, phenyl lower alkenyl and phenyl lower alkynyl, R.sub.2 and R.sub.3 are hydrogen, methyl, lower alkyl, substituted lower alkyl, cycloalkyl, substituted cycloalkyl, lower alkenyl, substituted lower alkenyl, lower alkynyl, substituted lower alkynyl, phenyl lowerThe invention described herein was made in the course of work under a grant or award from the Department of Health and Human Services.
    Type: Grant
    Filed: May 18, 1982
    Date of Patent: September 24, 1985
    Assignee: Northeastern University
    Inventor: John L. Neumeyer
  • Phenobarbital enzyme inhibitors
    Patent number: 4543412
    Abstract: Phenobarbital conjugates for use as enzyme inhibitors having the formula: ##STR1## wherein Z is a biologically compatible counter ion, n and m is an integer from 2 to 6 and R and R.sub.1 are each lower alkyl.
    Type: Grant
    Filed: November 4, 1983
    Date of Patent: September 24, 1985
    Assignee: Abbott Laboratories
    Inventors: Charles A. Flentge, Thomas R. Herrin
  • Pesticidally active pyrimidin-5-yl-(thio)phosphoric acid ester-amides
    Patent number: 4542126
    Abstract: Pyrimidin-5-yl-(thio)phosphoric acid ester-amides of the formula ##STR1## in which X is oxygen or sulphur,R is hydrogen, alkyl, aryl or cycloalkyl,R.sup.3 is alkyl, halogenoalkyl, cyanoalkyl, mono- or di-alkylamino, optionally substituted aryl, or ##STR2## R.sup.1, R.sup.2, R.sup.4, R.sup.6 and R.sup.7 each independently is alkyl, andR.sup.5 is alkyl or optionally substituted aryl which possess pesticidal activity.
    Type: Grant
    Filed: March 1, 1984
    Date of Patent: September 17, 1985
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Bernhard Homeyer, Benedikt Becker, Gerd Hanssler
  • Prodrug esters of diflunisal and related compounds
    Patent number: 4542158
    Abstract: 1-(Alkoxy or aroxy)carbonyloxyalkyl esters of diflunisal and related compounds are stable in aqueous medium and non-irritant to mucous membranes of mouth, throat, and stomach. Accordingly, they are useful Prodrugs of the analgesic and anti-inflammatory drug, diflunisal.
    Type: Grant
    Filed: October 25, 1982
    Date of Patent: September 17, 1985
    Assignee: Merck & Co., Inc.
    Inventor: Conrad P. Dorn
  • Sulfonylureas pharmaceutical formulations based on these compounds and their use for treatment of diabetes
    Patent number: 4542139
    Abstract: Sulfonylureas of the formula ##STR1## in which Y denotes alkylene having 2-3 C atoms, R denotes alkyl having 1-4 C atoms, R.sup.1 denotes hydrogen, chlorine or methyl, and R.sup.2 denotes alkyl having 3-6 C atoms, cycloalkyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkenyl, alkylcycloalkenyl or cycloalkenylalkyl, each having 5-8 C atoms, and their physiologically tolerated salts, and processes for their preparation and medicaments prepared therefrom.
    Type: Grant
    Filed: April 26, 1984
    Date of Patent: September 17, 1985
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Volker Hitzel, Rudi Weyer, Karl Giesen, Harald Ritzel
  • Topical compositions containing copper (II) complexes of 3,5-dioxo-pyrazolidine derivatives and methods of combatting inflammation with them
    Patent number: 4539206
    Abstract: Novel copper (II) coordination complexes of 3,5-dioxo-pyrazolidine derivatives with dimethylsulphoxide, dimethylformamide, and 1,4-dioxan coordination ligands are described. The complexes are potent anti-inflammatory agents and are usually applied topically in non-aqueous solution, showing good dermal penetration and systemic absorption.
    Type: Grant
    Filed: May 5, 1982
    Date of Patent: September 3, 1985
    Assignee: Alcusal Incorporated Pty. Ltd.
    Inventors: Barry Boettcher, William R. Walker
  • Process for the preparation of sulphoalkyl quaternary salts
    Patent number: 4539408
    Abstract: Quaternary sulfoalkyl or sulfoalkenyl salts of tertiary amine bases are prepared by reacting the tertiary amine bases at elevated temperatures with a hydroxy alkane sulfonic acid or a hydroxyalkene sulphonic acid.
    Type: Grant
    Filed: April 28, 1978
    Date of Patent: September 3, 1985
    Assignee: Agfa-Gevaert Aktiengesellschaft
    Inventors: Helmut Kampfer, Marie Hase, Max Glass
  • Process for making 6-desoxy-6-methylenenaloxone and 6-desoxy-6-methylenenaltrexone
    Patent number: 4535157
    Abstract: An improved Wittig reaction for making 6-desoxy-6-methylenenaloxone and 6-desoxy-6-methylenenaltrexone from naloxone and naltrexone utilizing an alkoxide base in an ethereal solvent.
    Type: Grant
    Filed: November 1, 1983
    Date of Patent: August 13, 1985
    Assignee: Key Pharmaceuticals, Inc.
    Inventors: Peter C. Meltzer, Jotham W. Coe
  • Antiallergic and antiulcer 1-oxo-1H-thiazolo[3,2-a]pyrimidine-2-carboxamides and intermediates therefor
    Patent number: 4535081
    Abstract: Antiallergy and antiulcer agents having the formula (I), ##STR1## and their pharmaceutically acceptable salts, wherein R.sub.1 and R.sub.2 taken separately are each hydrogen or lower alkyl; and R.sub.1 and R.sub.2 taken together are alkylene of 3-9 carbon atoms or phenylalkylene of 9-11 carbon atoms, with the proviso that the ring so formed is between 5- and 8-membered; acids of the formula (II), ##STR2## wherein R.sub.1 and R.sub.2 are as defined above and R.sub.3 is hydrogen, which are useful as intermediates for compounds of the formula (I), but in many instances also possess the same useful biological activity as do formula I compounds; and intermediates of the formula II wherein R.sub.1 and R.sub.2 are defined as above, and R.sub.3 is alkyl of 1 to 4 carbon atoms, carbalkoxy of 2 to 5 carbon atoms, carbophenoxy or carbobenzoxy, are also described.
    Type: Grant
    Filed: August 17, 1983
    Date of Patent: August 13, 1985
    Assignee: Pfizer Inc.
    Inventor: Saul B. Kadin