Patents Examined by Diana G. Rivers
  • Patent number: 4758665
    Abstract: A process for preparing the high-hiding form of the .gamma.-crystal modification of unsubstituted linear transquinacridone having improved tinctorial strength and producing a coating of higher gloss, which comprises carrying out (a) the known cyclization of 2,5-diphenylaminoterephthalic acid in highly concentrated polyphosphoric acid or in acid polyphosphoric acid ester to the quinacridone and/or (b) the known hydrolysis of the quinacridone melt obtained in (a) and/or (c) the known aqueous alkali extraction of the quinacridone obtained in (b) and/or (d) the known finishing of the quinacridone obtained in (a) in the presence of 0.5 to 10 percent by weight, based on quinacridone, of surface-active agents.
    Type: Grant
    Filed: November 13, 1986
    Date of Patent: July 19, 1988
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Ernst Spietschka, Adolf Kroh
  • Patent number: 4758666
    Abstract: The invention relates to a new process for the preparation of 17,18-dehydro-apovincaminol-trimethoxy-benzoate of the formula (I) ##STR1## and acid addition salts thereof. According to the invention compound of the formula (I) is prepared starting from 17,18-dehydrovincamine of the formula (IIa) ##STR2## and/or 17,18-dehydro-epivincamine of formula (IIb) ##STR3## by reducing with a complex metal hydride, acylating the new hydroxy-vincaminol derivative obtained selectively with 3,4,5-trimethoxy-benzoic acid or a derivative thereof capable of acylation, optionally in the presence of a catalyst and/or an acid binding agent, and treating the corresponding acylated hydroxylderivative obtained with formic acid, in the presence of an acid chloride, and, if desired, converting the compound of formula (I) obtained into an acid addition salt thereof.
    Type: Grant
    Filed: May 9, 1986
    Date of Patent: July 19, 1988
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Janos Galambos, Tibor Keve, Bela Stefko, Gyorgy Fekete, Bela Zsadon, Anna Kassai nee Zieger, Klara Horvath nee Otta
  • Patent number: 4758565
    Abstract: This disclosure relates to a novel class of substituted quinoxaline derivatives. The disclosure further relates to pharmaceutical compositions containing such compounds and to the use of such compounds and compositions as anti-anaerobic agents.
    Type: Grant
    Filed: August 18, 1986
    Date of Patent: July 19, 1988
    Assignee: G. D. Searle & Co.
    Inventors: George J. Ellames, Kevin R. Lawson, Albert A. Jaxa-Chamiec, Roger M. Upton
  • Patent number: 4757077
    Abstract: The invention relates to novel bis-indole derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a hydrogen atom or an acetyl group;R.sub.2 stands for a hydrogen atom;R.sub.3 means an ethyl group of .alpha.-position; orR.sub.2 and R.sub.3 together represent an oxygen bridge;R.sub.4 represents an ethyl or hydroxyl group of .beta.-position; andR.sub.5 stands for a hydrogen atom or a hydroxyl group;A represents a C.sub.1-10 straight-chain or C.sub.3-10 branched-chain alkyl group, hydroxy-alkyl, acetyl-alkyl, benzyl, C.sub.3-6 alkenyl or alkynyl or C.sub.5-7 cycloalkyl group or an aromatic group or a heteroaromatic group containing one nitrogen or one oxygen atom, andX stands for oxygen or sulphur atom,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.
    Type: Grant
    Filed: June 12, 1986
    Date of Patent: July 12, 1988
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Csaba Szantay, Lajos Szabo, Katalin Honty, Tibor Keve, Tibor Acs, Sandor Eckhardt, Janos Sugar, Zsuzsa Somfai, Eva Ivan, Zsuzsa Kneffel
  • Patent number: 4753930
    Abstract: Novel insecticides and nematicides of the formula ##STR1## in which R is i-propyl or sec.-butyl, andR.sup.1 is hydrogen or halogen.
    Type: Grant
    Filed: February 12, 1987
    Date of Patent: June 28, 1988
    Assignee: Bayer Aktiengesellschaft
    Inventors: Fritz Maurer, Benedikt Becker, Bernhard Homeyer
  • Patent number: 4753948
    Abstract: The invention relates to novel furfuryl derivatives of the general formula (I), ##STR1## wherein R.sub.1 stands for a hydrogen atom or an acetyl group,R.sub.2 stands for a hydroxyl or ethyl group of.beta.-position;R.sub.3 means an ethyl group of .alpha.-position;R.sub.4 represents a hydrogen atom; orR.sub.3 and R.sub.4 together represent an oxygen bridge; andB stands for a hydroxyl of an O-acyl group, as well as their acid addition salts and pharmaceutical preparations containing these compounds. Further on, the invention relates to a process for preparing these compounds and preparations.The compounds of the general formula (I) show a cytostatic activity with less toxicity than that of the commerically available known vinblastine-type bis-indole alkaloid drugs.
    Type: Grant
    Filed: June 12, 1986
    Date of Patent: June 28, 1988
    Assignee: Richter Gedeon Vegyeszeti Gyar R.T.
    Inventors: Csaba Szantay, Lajos Szabo, Katalin Honty, Tibor Keve, Tibor Acs, Sandor Eckhardt, Janos Sugar, Zsuzsa Somjai, Eva Ivan, Zsuzsa Kneffel
  • Patent number: 4751307
    Abstract: Disclosed are improved Wittig reaction processes wherein the Wittig reaction is conducted in an anisole containing solvent.
    Type: Grant
    Filed: February 27, 1987
    Date of Patent: June 14, 1988
    Assignee: Mallinckrodt, Inc.
    Inventor: Carl R. White
  • Patent number: 4751311
    Abstract: Concentrated aqueous formulations of isothiazolin-3-ones containing 5-30% urea are stable down to -13 deg C. at pH>9.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: June 14, 1988
    Assignee: Imperial Chemical Industries
    Inventor: Bryan S. Backhouse
  • Patent number: 4749707
    Abstract: A (+) citrate salt of vinpocetine, and a procedure for preparing the salt, is disclosed. The salt is useful as a medicinal agent in cerebral-vascular disorders and in neurological treatments relating to cerebral oxygenation, especially in elderly persons.
    Type: Grant
    Filed: January 14, 1987
    Date of Patent: June 7, 1988
    Assignee: Covex, S.A.
    Inventors: Fernando Calvo, Maria T. Manresa
  • Patent number: 4749787
    Abstract: This invention relates to a chemical process of producing an antitumor alkaloid. More particularly, it relates to a method of isolation of vinblastine from Catharanthus roseus, comprising the steps of: extracting C. roseus leaves with an acidified aqueous solution; raising the pH and extracting an alkaloid mixture with an organic solvent; chromatographing a solution of the alkaloid mixture over dextran and silica gel columns to obtain vinblastine containing fractions for isolation.
    Type: Grant
    Filed: October 23, 1986
    Date of Patent: June 7, 1988
    Assignee: Harbor Branch Oceanographic Institution, Inc.
    Inventor: Sarath P. Guanasekera
  • Patent number: 4749704
    Abstract: Compounds of formula (I): ##STR1## (wherein R.sup.1 and R.sup.2 are hydroxy, alkoxy, aryloxy or acyloxy or R.sup.2 is hydrogen, R.sup.3 is hydrogen or alkyl and R.sup.4 and R.sup.5 are hydrogen or various organic substituents) have valuable antidepressant activity and may be used in the treatment of mental depression.
    Type: Grant
    Filed: March 6, 1986
    Date of Patent: June 7, 1988
    Assignees: Sankyo Company Limited, Ube Industries Limited
    Inventors: Nobuyoshi Iwata, Isao Nakayama, Kanichi Nakamura, Tomio Kimura, Takashi Kobayashi
  • Patent number: 4746665
    Abstract: The invention relates to novel nitro derivatives of the general formula (I) ##STR1## wherein R.sub.1 stands for a methyl or a formyl group;R.sub.2 stands for a hydroxy or ethyl group of .beta.-position;R.sub.3 means an ethyl group of .alpha.-position;R.sub.4 represents a hydrogen atom; orR.sub.3 and R.sub.4 together represent an oxygen bridge or a double bond;R.sub.5, R.sub.6 and R.sub.7 stand for a nitro group or hydrogen atom, with the proviso that simultaneously only one of them may stand for hydrogen atom; andY stands for --N.dbd. when R.sub.5 stands for a nitro group; whereasY stands for --NH-- when R.sub.5 stands for a hydrogen atom and a valence bond exists between the C.sub.2, and C.sub.7, atoms,as well as their acid addition salts and pharmaceutical preparations containing these compounds.Further on, the invention relates to a process for preparing these compounds and preparations.
    Type: Grant
    Filed: June 12, 1986
    Date of Patent: May 24, 1988
    Assignee: Richter Gedeon Vegyeszeti Gyar
    Inventors: Csaba Szantay, Lajos Szabo, Katalin Honty, Tibor Keve, Tibor cs, Sandor Eckhardt, Janos Sugar, Zsuzsa Somfai, Eva Ivan, Zsuzsa Kneffel
  • Patent number: 4745196
    Abstract: This invention is directed to orally active antihypertensive agents of the formula ##STR1## wherein R.sub.1 is certain alkyl or aralkyl groups.
    Type: Grant
    Filed: January 6, 1986
    Date of Patent: May 17, 1988
    Assignee: E. R. Squibb & Sons, Inc.
    Inventors: Donald S. Karanewsky, Edward W. Petrillo, Jr.
  • Patent number: 4745115
    Abstract: Compounds of the general formula I ##STR1## in which: R.sub.1 and R.sub.2 are independently hydrogen, C.sub.1-6 alkyl or together are a group X which is C.sub.3-6 polymethylene optionally in which one carbon atom is replaced by O, S or NR.sub.6 wherein R.sub.6 is hydrogen or C.sub.1-6 alkyl;R.sub.3 is a mono- or fused bi-cyclic heteroaromatic group having up to ten atoms in the aromatic ring(s), not more than four of which are selected from nitrogen, oxygen or sulphur, optionally C-substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl or cyano; or is phenyl or naphthyl, optionally substituted by one or more substituents selected from halogen, CF.sub.3, nitro, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, C.sub.1-6 alkylthio, C.sub.2-7 alkanoyl, carboxyl, C.sub.1-6 alkoxycarbonyl, cyano, CONR.sub.7 R.sub.8 wherein R.sub.7 and R.sub.8 are selected from hydrogen or C.sub.1-6 alkyl or together are a group X; NR.sub.9 R.sub.
    Type: Grant
    Filed: October 18, 1985
    Date of Patent: May 17, 1988
    Assignee: Beecham Group p.l.c.
    Inventors: Roger E. Markwell, Stephen A. Smith, David J. Hunter
  • Patent number: 4739064
    Abstract: Selective hydrogenation of the unsaturated nitrogen-containing ring in heterocyclic aromatic compounds is promoted by the use of at least one hydrogenation catalyst selected from the group consisting of nickel, cobalt, palladium, platinum, ruthenium and rhodium in the presence of reaction modifiers exemplified by carbon monoxide, carbon disulfide and hydrogen sulfide.
    Type: Grant
    Filed: December 4, 1985
    Date of Patent: April 19, 1988
    Assignee: Phillips Petroleum Company
    Inventor: James E. Shaw
  • Patent number: 4738964
    Abstract: The novel compound, 5H-thiazolo[2,3-b]quinazolin-3(2H)-one, and derivatives thereof in which a nuclear hydrogen of its benzene ring is replaced by lower alkyl, alkoxy, halogen, trifluoromethyl, NO.sub.2 or NH.sub.2 ; useful as anti-hypertensive agents and immunosuppressive agents.
    Type: Grant
    Filed: July 3, 1986
    Date of Patent: April 19, 1988
    Assignee: Pennwalt Corporation
    Inventors: Grace A. Saeva, Vassil S. Georgiev
  • Patent number: 4738710
    Abstract: The invention concerns novel compounds of the formula I ##STR1## wherein: A, B, D, E, J.sup.1, J.sup.2, U and V are chosen from hydrogen, halogen, nitro, cyano, thiocyano, amino, substituted amino, alkyl, substituted alkyl, alkenyl, cycloalkyl, alkoxy, substituted alkoxy, alkylthio, alkylsulfinyl, substituted alkylsulfinyl, alkylsulfonyl, substituted alkylsulfonyl, sulfamoyl, substituted sulfamoyl, sulfo, carboxy, alkoxycarbonyl, carbamoyl, substituted carbamoyl and optionally substituted phenyl, phenoxy and phenylthio;R.sup.1 is chosen from hydrogen, alkyl, substituted alkyl, alkenyl, alkanoyl and alkoxycarbonyl; R.sup.2 is chosen from hydrogen, alkyl, substituted alkyl and alkenyl; or R.sup.1 and R.sup.2 together form an alkylidene group;W is chosen from cyano, thiocarbamoyl, the group --CH.sub.
    Type: Grant
    Filed: September 27, 1985
    Date of Patent: April 19, 1988
    Assignee: ICI Australia Limited
    Inventors: Alexander Serban, Keith G. Watson
  • Patent number: 4739063
    Abstract: Selective hydrogenation of the unsaturated nitrogen-containing ring in heterocyclic aromatic compounds is promoted by the use of hydrogenation catalysts selected from the group consisting of iridium, iridium dioxide, rhenium, molybdenum oxide, tungsten oxide, chromium trioxide, ferric oxide, iron pentacarbonyl, cobalt oxide-molybdenum oxide and copper chromite.
    Type: Grant
    Filed: December 4, 1985
    Date of Patent: April 19, 1988
    Assignee: Phillips Petroleum Company
    Inventor: James E. Shaw
  • Patent number: 4737586
    Abstract: The present invention relates to a process for the preparation of bis-indolic compounds, and the bis-indolic compounds produced by the process.
    Type: Grant
    Filed: April 29, 1986
    Date of Patent: April 12, 1988
    Assignee: Agence Nationale de Valorisation de la Recherche
    Inventors: Pierre Potier, Nicole Langlois, Yves Langlois, Francoise Gueritte
  • Patent number: 4735946
    Abstract: The invention relates to new eburnane derivatives of the formula (I) ##STR1## wherein R.sup.1 is alkyl having from 1 to 6 carbon atoms, and acid addition salts thereof.The invention further relates to a process for the preparation of these compounds and pharmaceutical compositions containing them.Compounds of formula (I) show remarkable CNS-activity and are useful intermediates in the preparation of other, pharmaceutically active compounds.
    Type: Grant
    Filed: April 2, 1985
    Date of Patent: April 5, 1988
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Janos Kreidl, Maria Farkas nee Kirjak, Laszlo Czibula, Bela Stefko, Gyorgy Visky, Judit Meszaros nee Brill