Patents Examined by Ethel G. Love
  • Patent number: 4594415
    Abstract: A class of novel azole dinucleotide compounds and methods for their production are provided. Compounds of the class typically have pharmacological properties and are well tolerated, being useful, for example, in treating leukemias in warm blooded animals.
    Type: Grant
    Filed: December 24, 1984
    Date of Patent: June 10, 1986
    Inventors: Roland K. Robins, Ganapathi R. Revankar
  • Patent number: 4594432
    Abstract: The invention is directed to a process and intermediates for the preparation of 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol. The end-products, 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol, are useful for the treatment of disease states which are characterized by insufficient amounts of 1,25 dihydroxycholecalciferol.
    Type: Grant
    Filed: December 27, 1983
    Date of Patent: June 10, 1986
    Assignee: Hoffman-La Roche Inc.
    Inventors: Enrico G. Baggiolini, Milan R. Uskokovic, Peter M. Wovkulich
  • Patent number: 4594339
    Abstract: Veterinarian composition for the treatment of herpes virus in animals comprising a pyrimidine nucleoside, or veterinarianically acceptable acid addition salte thereof, of the formula ##STR1## wherein A is OR.sup.3, SR.sup.3, NR.sup.3 R.sup.4 or NHacyl wherein R.sup.3 and R.sup.4 are the same or different and are hydrogen, lower alkyl of 1 to 7 carbon atoms, aralkyl, or aryl;NHacyl is alkanoyl or aroyl amide;B is oxygen or sulfur;X is halogen, alkylsulfonyl or arylsulfonyl;Y is halogen, amino, monoalkyl- or monoaralkylamino, dialkylamino, aminomethyl, hydroxymethyl, lower alkyl, aryl, aralkyl, vinyl and substituted vinyl or ethynyl and substituted ethynyl;Z is methyne or nitrogen;R.sup.1 and R.sup.2 are the same or different and are hydrogen acyl or aroyl,in a veterinarianically acceptable carrier.
    Type: Grant
    Filed: June 18, 1984
    Date of Patent: June 10, 1986
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Carlos Lopez, Kyoichi A. Watanabe, Uri Reichman, Jack J. Fox
  • Patent number: 4594350
    Abstract: Antiviral (3-ethoxypropionate) esters of (+)-cyclaradine having the formula: ##STR1## In the monoester Ry and Rz are hydrogen. In the diester Ry is the 3-ethoxypropionyl group and Rz is hydrogen. In the triester, Ry and Rz are each 3-ethoxypropionyl groups.
    Type: Grant
    Filed: July 30, 1984
    Date of Patent: June 10, 1986
    Assignee: Reagents of University of Minnesota
    Inventor: Robert Vince
  • Patent number: 4593091
    Abstract: The present invention relates to a method for preparing inner ester derivatives of gangliosides and pharmaceutical compositions containing such derivatives to be used in treating disorders of the nervous system. The pharmaceutical compositions of the present invention promote nerve regeneration by stimulating nerve sprouting.
    Type: Grant
    Filed: September 28, 1982
    Date of Patent: June 3, 1986
    Assignee: Fidia, S.p.A.
    Inventors: Francesco della Valle, Aurelio Romeo
  • Patent number: 4593019
    Abstract: N.sup.6 -Tricyclic adenosines and pharmaceutically acceptable acid addition salts having highly desirable central nervous system and cardiovascular properties, processes for their manufacture and pharmaceutical compositions and methods for using said compounds and compositions are described.
    Type: Grant
    Filed: October 26, 1984
    Date of Patent: June 3, 1986
    Assignee: Warner-Lambert Company
    Inventors: James A. Bristol, Walter Moos, Bharat K. Trivedi
  • Patent number: 4593131
    Abstract: Compounds having the formula ##STR1## wherein ##STR2## R.sub.1 is hydrogen, benzyl or alkanoyl, X is C.sub.2-4 alkylene; andZ-W is alkyl, phenylalkyl or pyridylalkyl which can have an oxygen atom as part of the alkyl chain and their use as CNS agents, antidiarrheals and antiemetics. Processes for their preparation and intermediates therefor are described.
    Type: Grant
    Filed: September 17, 1984
    Date of Patent: June 3, 1986
    Assignee: Pfizer Inc.
    Inventors: Michael R. Johnson, Lawrence S. Melvin, Jr.
  • Patent number: 4591600
    Abstract: This invention relates to quercetin or fisetin derivatives substituted on the oxygen in the 3 position by groups such as lower alkyl, cycloalkyl, methanesulfonyl or paratoluenesulfonyl.The derivatives substituted by methanesulfonyl or paratoluenesulfonyl are obtained from a 3-O-glycoside whose phenol OH groups are blocked in the form of benzoate, and from which the OH in the 3 position is released by the action of concentrated HCl; this OH is esterified by mesityl chloride or paratoluenesulfonic acid chloride, and the benzoate groups are eliminated by soda treatment. The O derivatives substituted by alkyl or cycloakyl are prepared from a suitably substituted acetonitrile or metadiphenol; the resulting derivative reacts with 3,4-dibenzyloxybenzoic acid and the resulting flavone is debenzylated by hydrogenolysis.The derivatives, object of this invention, are useful in preventive or curative therapy of ocular and nervous complications from diabetes and are also useful as hypolipidemic or hypoglycemic agents.
    Type: Grant
    Filed: March 29, 1984
    Date of Patent: May 27, 1986
    Assignee: Societe Cortial, S.A.
    Inventors: Marie-Helene Creuzet, Claude Feniou, Francoise Guichard, Gisele Prat, Jacqueline Mosser, Henri Pontagnier
  • Patent number: 4591601
    Abstract: Sulfamates of the following formula (I): ##STR1## wherein R.sup.1 and R.sup.2 are as herein defined have been found to exhibit anticonvulsant activity and are thus useful in the treatment of conditions such as epilepsy. Further, pharmaceutical compositions containing a compound of formula (I) as well as methods for their use and intermediates form part of the present invention.
    Type: Grant
    Filed: April 12, 1985
    Date of Patent: May 27, 1986
    Assignee: McNeilab, Inc.
    Inventors: Bruce E. Maryanoff, Samuel O. Nortey
  • Patent number: 4590282
    Abstract: Dioxolane and benzodioxin derivatives, intermediates therefor, synthesis thereof, and the use of the compounds for the control of pests.
    Type: Grant
    Filed: September 24, 1984
    Date of Patent: May 20, 1986
    Assignee: Sandoz Ltd.
    Inventor: Clive A. Henrick
  • Patent number: 4588824
    Abstract: Processes for preparing (S) or (R) epihalohydrin and an (S) substituted glycerol intermediate are disclosed.
    Type: Grant
    Filed: June 16, 1983
    Date of Patent: May 13, 1986
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, David E. McClure
  • Patent number: 4587351
    Abstract: The present invention pertains to a process for preparing ketones employing a silica catalyzed oxidation of a secondary alcohol with calcium hypochlorite in acetonitrile.
    Type: Grant
    Filed: April 18, 1984
    Date of Patent: May 6, 1986
    Assignee: Eli Lilly and Company
    Inventors: Randall K. Atkins, Leland O. Weigel
  • Patent number: 4585761
    Abstract: A method of combating arthropods, comprising applying to the arthropods, or to a habitat infested therewith an arthropodicidally effective amount of an antibiotic which (a) is colorless, very readily soluble in water and in pyridine but insoluble in other customary organic solvents, gives a positive reaction with ninhydrin, sodium metaperiodate/benzidine and potassium permanganate and gives a yellow coloration with iron (III) chloride, (b) has the UV and IR spectra substantially as shown in FIGS. 1 and 2, (c) on chemical degradation yields uracil, an amino-hexuronic acid and an amino-acid containing a pyridine ring, (d) on paper electrophoresis proves to be an amphoteric substance and has an isoelectric point at about pH 6 and (e) consists of the elements carbon, hydrogen, oxygen and nitrogen, or one or more active components of the antibiotic mixture, the active agent being applied alone or in admixture with a diluent or carrier.
    Type: Grant
    Filed: May 20, 1981
    Date of Patent: April 29, 1986
    Assignee: Ciba Geigy AG
    Inventors: Hans Zahner, Hartwig Holst, Gerhard Zoebelein, Adelinde Keckeisen
  • Patent number: 4584369
    Abstract: Beta-glycosyl C-nucleoside compounds showing growth inhibitory activity against leukemic cells, of the following formula, are provided: ##STR1## wherein X is NR.sub.10, S or OR.sub.10 is H or alkyl with 1 to 6 carbon atoms. ##STR2## wherein R.sub.6, R.sub.7 and R.sub.8 are independently selected from H or alkyl of 1 to 6 carbon atoms; or ##STR3## wherein R.sub.16, R.sub.11 and R.sub.12 are independently selected from H or alkyl of 1-6 carbon atoms;R.sub.3 is OH, SR.sub.13, or OR.sub.9 ;R.sub.4 is OH, SR.sub.14, or OR.sub.15 ;R.sub.9, R.sub.13, R.sub.14 and R.sub.15 are individually selected from C.sub.1 -C.sub.6 alkyl and C.sub.1 to C.sub.6 acyl;R.sub.5 is OH or H,R'.sub.5 is OH or H with the provison that at least one of R.sub.5 or R'.sub.5 is H; excluding 2-deazoxoformycin; andHCl salts thereof.
    Type: Grant
    Filed: April 2, 1984
    Date of Patent: April 22, 1986
    Assignee: Sloan-Kettering Institute for Cancer Research
    Inventors: Robert S. Klein, Muill Lim, Wuyun Ren, Joseph H. Burchenal
  • Patent number: 4582823
    Abstract: A method for treating schizophrenia without precipitating neurological side effects such as extrapyramidal syndrome and tardive dyskinesia by administering prior to or concomitantly with haloperidol a diphenylalkyladenosine or diphenylalkyl-2-amino-adenosine is described as well as pharmaceutical compositions therefor.
    Type: Grant
    Filed: August 15, 1984
    Date of Patent: April 15, 1986
    Assignee: Warner-Lambert Company
    Inventors: Thomas G. Heffner, Stephen E. Harrigan, Jerry A. Weisbach
  • Patent number: 4582919
    Abstract: There is described a novel process for producing hydroquinone derivatives of the formula ##STR1## wherein R is an ether protecting group, and their conversion into d-.alpha.-tocopherol, starting from compounds of the formula ##STR2## wherein R is an ether protecting group and R.sup.1 is hydrogen or an ether protecting group.
    Type: Grant
    Filed: June 11, 1984
    Date of Patent: April 15, 1986
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Richard Barner, Josef Hubscher
  • Patent number: 4581466
    Abstract: Benzo-fused, tetrachlorinated heterocyclic compounds are prepared by first reacting pyrocatechol or a pyrocatechol derivative with tetrachloroethylene carbonate, with the addition of a tertiary amine, and then adding phosphorus pentachloride, without intermediate isolation.
    Type: Grant
    Filed: March 25, 1985
    Date of Patent: April 8, 1986
    Assignee: Bayer Aktiengesellschaft
    Inventor: Albrecht Marhold
  • Patent number: 4579941
    Abstract: Thermally-denatured DNA MD-011 having an antitumor activity was obtained by heating the substance separated from the disrupted cells of bacteria belonging to genus Mycobacterium.
    Type: Grant
    Filed: August 13, 1982
    Date of Patent: April 1, 1986
    Assignee: Mitsuitoatsu Chemicals, Inc.
    Inventors: Yoshio Furutani, Hiroshi Yamamoto, Tamotsu Fukuda, Shizuo Shimada, Osamu Yano
  • Patent number: 4578484
    Abstract: New process for preparing the pheromone active compound lineatin (3,3,7-trimethyl-2,9-dioxatricyclo[3,3,1,0.sup.4,7 ]-nonane), by reacting a 2,2-dimethyl-3,4-pentadienal of formula 1, in which R.sub.1 and R.sub.2 is each hydrogen or lower alkyl, with .beta.-methylallyl magnesium halide; the formed 2,5,5-trimethylocta-1,6,7-trien-4-ol derivative of formula 2 is subjected to oxidation which does not attack the double bonds; the formed 2,5,5-trimethylocta-1,6,7-trien-4-one derivative of formula 3 is subjected to pyrolysis; the formed 1,4,4-trimethyl-6-methylenebicyclo[3,2,0]heptan-3-one derivative of formula 4 is subjected to oxidation; the resulting 5,5,9-trimethyl-2,6-dioxa-7-oxo-bicyclo[4,2,0]octylspiro[2,7]-decane derivative of formula 5 is subjected to oxidation; the resulting 1,5,5-trimethyl-4-oxabicyclo[4,2,0]-octan-3,7-dione of formula 6 is reduced in a per se known manner to lineatin of formula 7. Compounds 2, 3, 4 and 5 are novel.
    Type: Grant
    Filed: November 15, 1984
    Date of Patent: March 25, 1986
    Assignee: Borregaard Industries Limited
    Inventors: Lars Skattebol, Yngve Stenstrom
  • Patent number: 4578485
    Abstract: The invention concerns a method for the synthesis of 6'-ethyl spectinomycin and analogs thereof, including intermediates utilized in the method. The method comprises converting an enamine by a Grignard addition to various novel dienones not hitherto known. The dienones are then hydrogenated and deblocked to obtain 6'-ethyl spectinomycin and analogs thereof. The 6'-ethyl spectinomycin and analogs thereof prepared by the invention exhibit especially good antibacterial activity.
    Type: Grant
    Filed: February 8, 1984
    Date of Patent: March 25, 1986
    Assignee: The Upjohn Company
    Inventor: David R. White