Patents Examined by Diana G. Rivers
  • Patent number: 4474952
    Abstract: Process for the preparation of 1:1 metal complexes of azines of the formula ##STR1## in which R.sub.1 is an H atom or an alkyl or aryl group, R.sub.2 is an isocyclic or heterocyclic radical with a hydroxyl or mercapto group adjacent to the azomethine group, Y' is the radical of a methylene-active compound or of an aryl-or heteroaryl-amine and the ring A can have substituents which do not confer solubility in water, which comprises heating a hydrazone of the formula ##STR2## with an isoindolinone of the formula ##STR3## in which R.sub.1, R.sub.2, A and Y' are as defined, in the presence of a metal donor, in a polar organic solvent.
    Type: Grant
    Filed: September 13, 1982
    Date of Patent: October 2, 1984
    Assignee: Ciba-Geigy Corporation
    Inventor: Abul Iqbal
  • Patent number: 4474953
    Abstract: A process for preparing compounds of the formula ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of H, an alkyl group containing 1 to about 4 carbon atoms, an alkoxy group containing 1 to about 4 carbon atoms and halogen. The process involves reacting together a 2-aminopyridine, an alkyl tetrazol-5-ylacetate, and a trialkyl orthoformate and cyclizing the resulting intermediate.
    Type: Grant
    Filed: September 9, 1982
    Date of Patent: October 2, 1984
    Assignee: Riker Laboratories, Inc.
    Inventor: James J. Wade
  • Patent number: 4473573
    Abstract: The invention relates to N-(2-methoxyethyl)-noroxymorphone and pharmacologically acceptable acid addition salts thereof. These compounds are analgesically effective and can be used for controlling pain.
    Type: Grant
    Filed: May 17, 1983
    Date of Patent: September 25, 1984
    Assignee: Boehringer Ingelheim KG
    Inventors: Herbert Merz, Adolf Langbein, Klaus Stockhaus
  • Patent number: 4473692
    Abstract: New Camptothecin derivatives possessing high anti-tumor activity with slight toxicity, represented by the general formula: ##STR1## wherein R.sup.1 is a hydrogen atom, an alkyl group, a hydroxyl group, an alkoxy group or an acyloxy group, R.sup.2 for a hydrogen atom, an alkyl group, an aralkyl group, a hydroxymethyl group, a carboxymethyl group or an acyloxymethyl group, and R.sup.3 is the grouping --XR' (where R' is a hydrogen atom, an alkyl group or an acyl group and X is an oxygen atom or a sulfur atom), a nitro group, an amino group, an alkylamino group, an acylamino group or a halogen atom, with the proviso that when both of R.sup.1 and R.sup.2 are hydrogen atoms, R.sup.3 should not be a hydroxyl group, methoxy group or acetoxy group. These new camptothecin derivatives are prepared by treating a 5-R.sup.1 -7-R.sup.2 -camptothecin derivative with a peroxidant and then reacting the resultant 5-R.sup.1 -7-R.sup.
    Type: Grant
    Filed: September 1, 1982
    Date of Patent: September 25, 1984
    Assignee: Kabushiki Kaisha Yakult Honsha
    Inventors: Tadashi Miyasaka, Seigo Sawada, Kenichiro Nokata, Masahiko Mutai
  • Patent number: 4472401
    Abstract: A compound selected from the group consisting of pyrimido quinoxalines of the formula ##STR1## wherein R.sub.1 represents an alkoxy radical of 1 to 5 carbon atoms and R is selected from the group consisting of hydrogen, alkyl of 1 to 5 carbon atoms, --COR.sub.A, --CHO and ##STR2## R.sub.A is selected from the group consisting of alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 6 carbon atoms, alkoxy of 1 to 5 carbon atoms and phenyl optionally substituted with at least one member of the group consisting of halogen, --NO.sub.2 and alkoxy of 1 to 3 carbon atoms and their non-toxic, pharmaceutically acceptable acid addition salts having antiallergic properties.
    Type: Grant
    Filed: November 23, 1982
    Date of Patent: September 18, 1984
    Assignee: Roussel Uclaf
    Inventors: Peter D. Kennewell, David P. Kay
  • Patent number: 4472400
    Abstract: Novel triazoloquinazolones of the formula ##STR1## wherein R and R' are individually selected from the group consisting of hydrogen, halogen, nitro and alkyl and alkoxy of 1 to 3 carbon atoms, Y is selected from the group consisting of alkyl of 1 to 6 carbon atoms, alkenyl of 2 to 4 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms and aralkyl of 7 to 8 carbon atoms, B is an alkylene of 1 to 3 carbon atoms, X is selected from the group consisting of ##STR2## R.sub.1 and R.sub.2 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, aryl of 6 to 8 carbon atoms, aralkyl of 7 to 8 carbon atoms, aminoalkyl of 2 to 4 carbon atoms, mono- and dialkylaminoalkyl with each alkyl having 2 to 4 carbon atoms, piperidinoalkyl of 1 to 4 alkyl carbon atoms, morpholinoalkyl of 1 to 4 alkyl carbon atoms and piperazinylalkyl of 1 to 4 alkyl carbon atoms or R.sub.1 and R.sub.
    Type: Grant
    Filed: September 21, 1982
    Date of Patent: September 18, 1984
    Assignee: Roussel Uclaf
    Inventors: Wilfred R. Tully, Robert Westwood, David A. Rowlands, Stephen Clements-Jewery
  • Patent number: 4472389
    Abstract: An organophosphorus compound of the formula ##STR1## where R and R.sup.1 together form a 1,3-butadien-1,4-diyl group optionally substituted with a chloro group, or R and R.sup.1 together form a 1,2-ethenediylthio group wherein sulfur is attached to carbon; R.sup.2 is hydrogen, chlorine or bromine; X is O or S; R.sup.3 is C.sub.1 -C.sub.2 alkyl; and R.sup.4 is C.sub.1 or C.sub.2 alkoxy or propylthio is disclosed. The organophosphorus compounds defined above are effective in the control of insects, nematodes and acarids.
    Type: Grant
    Filed: April 18, 1983
    Date of Patent: September 18, 1984
    Assignee: Uniroyal, Inc.
    Inventors: Mark A. Dekeyser, Benjamin J. Pierce, Richard C. Moore, Winchester L. Hubbard
  • Patent number: 4472399
    Abstract: New Rutecarpine analogs are disclosed having Rutecarpine-like activity, especially diuretic activity. Also a novel process for the preparation of the Rutecarpine analogs is disclosed.
    Type: Grant
    Filed: October 2, 1981
    Date of Patent: September 18, 1984
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara Rt.
    Inventors: Jozsef Kokosi, Istvan Hermecz, Zoltan Meszaros, Sandor Virag, Lelle Vasvari, nee Debreczy, Gyorgy Szasz, Agnes Horvath, Tibor Breining, Tamas Szuts, Gyula Sebestyen
  • Patent number: 4472403
    Abstract: The invention is concerned with novel quinicine and cinchonicine derivatives having cardiovascular activities of the formula or a salt thereof, ##STR1## in which A--B is --CH.sub.2 --CH.sub.2, --CHOH--CH.sub.2 --, --CH.sub.2 --CHOH--, --C(O)--CH.sub.2 --, --CH.sub.2 --C(O)--, --C(NOR.sup.4)--CH.sub.2 -- or --CH.sub.2 --C(NOR.sup.4)--; R.sup.1 is hydrogen, hydroxy or lower alkoxy; R.sup.2 is ethyl or vinyl; R.sup.3 is C.sub.2-8 alkyl, C.sub.1-8 hydroxyalkyl, lower alkoxy-alkyl or lower alkanoyloxyalkyl, C.sub.
    Type: Grant
    Filed: October 28, 1980
    Date of Patent: September 18, 1984
    Assignee: A.C.F. Chemiefarma N.V.
    Inventors: Hans B. Trijzelaar, Ronus de Bode, Hendricus B. A. Welle
  • Patent number: 4472582
    Abstract: 3,5-Disubstituted-4'-(9-acridinylamino)-methane-sulfon-m-anisidide compounds represented by the general formula ##STR1## in which R.sup.2 and R.sup.3 represent, respectively, --CH.sub.3 and --CONHCH.sub.3, --CH.sub.3 and --CONHCH.sub.2 CONH.sub.2, --Cl and --CONHCH.sub.2 CONH.sub.2, --CONHCH.sub.3 and --CH.sub.3 ; and acid addition salts thereof have unexpectedly high antitumor activity in leukemic animals and low or no direct mutagenicity.
    Type: Grant
    Filed: June 7, 1982
    Date of Patent: September 18, 1984
    Assignee: Development Finance Corporation of New Zealand
    Inventors: Bruce F. Cain, deceased, Graham J. Atwell, Bruce C. Baguley, William A. Denny
  • Patent number: 4472577
    Abstract: A process for the production of an .alpha.-hydroxy-phosphonic acid ester of the general formula ##STR1## in which R represents an optionally substituted aryl or heteroaryl group, andR.sup.1 and R.sup.2 independently of each other represent an alkyl or phenyl group, or together represent an alkanediyl (alkylene) radical,comprising reacting .alpha.-oxo-phosphonic acid esters with hydrogen in the presence of a hydrogenation catalyst. The .alpha.-hydroxy-phosphonic acid esters of formula (I) are intermediate products for the production of pesticides.
    Type: Grant
    Filed: July 15, 1982
    Date of Patent: September 18, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventor: Reinhard Lantzsch
  • Patent number: 4471118
    Abstract: A process for the preparation of an aldehyde of the formulaR--CHO (I)in which R is an optionally substituted alkyl, alkenyl, alkinyl, cycloakyl, cycloalkenyl, aralkyl, aralkenyl, aryl or heteroaryl radical, comprising heating an .alpha.-hydroxyphosphonic acid ester of the formula ##STR1## the aldehyde of the formula (I) can be used as an intermediate in the production of pest-combating agents.
    Type: Grant
    Filed: July 15, 1982
    Date of Patent: September 11, 1984
    Assignee: Bayer Aktiengesellschaft
    Inventor: Reinhard Lantzsch
  • Patent number: 4469868
    Abstract: Alkylimidazo[1,2-c]pyrazolo[3,4-e]pyrimidines and pharmaceutically acceptable salts are described. These compounds are antipsychotic agents. Methods for their preparation, pharmaceutical compositions which contain them and methods for using said compositions are also described.
    Type: Grant
    Filed: May 24, 1982
    Date of Patent: September 4, 1984
    Assignee: Warner-Lambert Company
    Inventor: Horace A. DeWald
  • Patent number: 4468519
    Abstract: Hypotensive activity is exhibited by compounds having the formula ##STR1## and salts thereof wherein R.sub.1 is alkyl, aryl, arylalkyl, cycloalkyl, or cycloalkylalkyl;R.sub.2 is cycloalkyl, 3-cyclohexenyl or 2-alkyl-3-cyclohexenyl;R.sub.3 is alkyl, cycloalkyl, phenyl or alkoxy;R.sub.4 is hydrogen or alkyl;one of R.sub.5 and R.sub.6 is hydrogen and the other is alkyl-X-, phenyl-X-, alkoxy, phenyloxy, phenyl, cycloalkyl, alkyl, or phenylalkyl; or together R.sub.5 and R.sub.6 are --XCH.sub.2 CH.sub.2 X--;R.sub.7 is hydrogen or ##STR2## and n is 0 or 1.
    Type: Grant
    Filed: June 14, 1982
    Date of Patent: August 28, 1984
    Assignee: E. R. Squibb & Sons, Inc.
    Inventor: John Krapcho
  • Patent number: 4464534
    Abstract: The invention relates to a new process for the preparation of apovincaminic acid esters. More particularly, the invention concerns a process for preparing racemic and optionally active vincaminic acid esters of the formula (I) ##STR1## in which R.sup.1 and R.sup.2 independently stand for alkyl having from one to 6 carbon atoms, and 14-epimers thereof.According to the invention an octahydroindolo[2,3-a]quinolizine-oxime ester of the formula (II) ##STR2## in which R.sup.1 and R.sup.2 have the same meaning as defined above, is reacted with an aqueous solution of sulfurous acid or a salt thereof at a temperature of 80.degree. to 110.degree. C. and the 14-epimeric mixture obtained is epimerized or separated in a known manner and if desired, the racemic vincaminic acid esters are resolved.
    Type: Grant
    Filed: September 28, 1982
    Date of Patent: August 7, 1984
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Janos Kreidl, Andras Nemes, Maria Farkas nee Kirjak, Gyorgy Visky, Laszlo Czibula
  • Patent number: 4464535
    Abstract: The invention relates to a new process for the preparation of eburnamonine derivatives of the general Formula I ##STR1## (wherein R.sup.1 is an alkyl group having 1-6 carbon atoms) and optical and geometrical isomers thereof which comprises reacting a hydroxyimino-octahydro-indolo[2,3-a]quinolizine derivative of the general Formula II ##STR2## (wherein R.sup.1 is as stated above and R.sup.2 stands for an alkyl group having 1-6 carbon atoms being identical with or different from R.sup.1, or a hydrogen atom) or an acid addition salt thereof in an organic protic solvent or solvent mixture with an inorganic base, optionally under the addition of water or an aqueous mineral acid, at a temperature between 60.degree. C. and 200.degree. C.The compounds of the present invention are known drugs having blood pressure decreasing and cerebral vasodilatatory effect.
    Type: Grant
    Filed: November 1, 1982
    Date of Patent: August 7, 1984
    Assignee: Richter Gedeon Vegyeszeti Gyar Rt.
    Inventors: Csaba Szantay, Lajos Szabo, Gyorgy Kalaus, Janos Kreidl, Gyorgy Visky, Andras Nemes, Laszlo Czibula, Maria Farkas nee Kirjak
  • Patent number: 4463007
    Abstract: 1,2,4-Triazolo[1,5-c]-quinazolinones of the general formula I ##STR1## and their pharmaceutically tolerated salts, processes for their preparation and pharmaceutical formulations which contain these compounds and are useful drugs in the treatment of allergic disorders.
    Type: Grant
    Filed: November 15, 1982
    Date of Patent: July 31, 1984
    Assignee: BASF Aktiengesellschaft
    Inventors: Rainer Schlecker, Ludwig Friedrich, Dieter Lenke
  • Patent number: 4461769
    Abstract: Compounds of the formula I ##STR1## or pharmaceutically acceptable salts, hydrates, stereoisomers, optically active isomers, geometrical isomers or tautomeric forms thereof are disclosedwhereinR is hydrogen or lower alkylR.sup.1 is hydrogen, lower alkyl, styryl, or a carboxylic acid; orR and R.sup.1 together form a group of the formula --(CH.dbd.CH).sub.2 -- and in this case the broken line represents a further C--C bond, while in all other cases there is a single bond between positions 6 and 7;R.sup.2 is hydrogen, lower alkyl or hydroxy;R.sup.3 is hydrogen, lower alkyl, aryl, lower alkanoyl, carboxyl or a carboxyl acid derivative or a group of the formula --(CH.sub.2)m--COOH or a derivative thereof formed in the carboxylic group;n=1-3;R.sup.4 is hydrogen, lower alkyl which can be substituted by hydroxy or carboxy; trifluoromethyl, substituted or unsubstituted aryl, phenyl-lower alkyl or substituted or an unsubstituted heterocyclic group;R.sup.
    Type: Grant
    Filed: September 19, 1979
    Date of Patent: July 24, 1984
    Assignee: Chinoin Gyogyszer es Vegyeszeti Termekek Gyara R.T.
    Inventors: Istvan Hermecz, Zoltan Meszaros, Tibor Breining, Sandor Virag, Lelle Vasvari nee Debreczy, Agnes Horvath, Gabor Nagy, Attila Mandi, Tamas Szucs, Istvan Bitter, Gyula Sebestyen
  • Patent number: 4460768
    Abstract: 1:1 Nickel complexes of azines of the formula I or of a tautomer thereof ##STR1## wherein R.sub.1 is hydrogen or methyl, R.sub.2 is methyl or carbamoyl, R.sub.3 is hydrogen or chlorine, R.sub.4 is hydrogen, chlorine, methyl, trifluoromethyl or sulfamoyl, R.sub.5 is hydrogen or chlorine, R.sub.6 is hydrogen, chlorine, bromine, methyl, methoxy, trifluoromethyl, carbamoyl or alkanoylamino containing 2 to 4 carbon atoms, with the proviso that, if R.sub.2 is carbamoyl, at least two of the substituents R.sub.3 to R.sub.6 are halogen atoms and/or trifluoromethyl groups, color plastics, lacquers and printing inks in orange to red shades of outstanding fastness properties.
    Type: Grant
    Filed: December 16, 1981
    Date of Patent: July 17, 1984
    Assignee: Ciba-Geigy Corporation
    Inventors: Abul Iqbal, Paul Lienhard, Andre Pugin
  • Patent number: RE31624
    Abstract: A method of treating inflammation and inhibiting prostaglandin synthesis employing substituted 2-(arylmethoxy)phenol compounds.
    Type: Grant
    Filed: December 22, 1982
    Date of Patent: July 3, 1984
    Assignee: Forsyth Dental Infirmary for Children
    Inventor: Floyd E. Dewhirst