Patents Examined by Joseph A. Lipovsky
  • Novel radioactive steroids
    Patent number: 4865767
    Abstract: Novel radioactive steroids labelled with tritium of the formula ##STR1## wherein .sup.3 H is tritium and R and R.sub.1 are individually selected from the group consisting of hydrogen, alkyl of 1 to 6 carbon atoms and acyl of an organic carboxylic acid of 1 to 10 carbon atoms useful for revealing receptors of glucocorticoids and in determining the number of fixation sites of glucocorticoids and novel intermediates.
    Type: Grant
    Filed: December 19, 1985
    Date of Patent: September 12, 1989
    Assignee: Roussel Uclaf
    Inventors: Alain Jouquey, Daniel Philibert, Martine Moguilewsky, Jean-Noel Veltz
  • Use of tetrahydrocortisol in glaucoma therapy
    Patent number: 4863912
    Abstract: Pharmaceutical compositions comprising tetrahydrocortisol and method of using same in the control of intraocular pressure are disclosed.
    Type: Grant
    Filed: May 19, 1986
    Date of Patent: September 5, 1989
    Assignee: New York Medical College
    Inventors: Aaron L. Southren, Bernard I. Weinstein, Gary G. Gordon
  • 17 .alpha.-(substituted-methyl)-17.beta.-hydroxy/esterified hydroxy steroids and their progestational use
    Patent number: 4861763
    Abstract: Steroids of the formula: ##STR1## which are characterized by a 17.alpha.-cyanomethyl, azidomethyl, methoxymethyl, phenylmethyl, or ethynylmethyl substituent and a 17.beta.-hydroxy/esterified hydroxy substitutent. The steroids of this invention have glucocorticoid, anti-glucocorticoid, progrestational, or anti-progestational activity, depending on the particular structure.
    Type: Grant
    Filed: July 25, 1988
    Date of Patent: August 29, 1989
    Assignee: Research Triangle Institute
    Inventors: C. Edgar Cook, C. Ray Tallent, Jerry R. Reel, Mansukh C. Wani
  • Process for the production of nourseothricine and its adsorbate
    Patent number: 4861715
    Abstract: A process is disclosed for the fermentative production of the ergotropically effective antibiotic nourseothricin, with which, using different carbohydrate sources and suitable inorganic and organic nitrogen sources as well as different mineral salts, with or without addition of stock substances of the respiratory chain or the intracellular amino acid transport, and through influencing the phosphate substance exchange and avoidance of further limitations with regulated acidity conditions, high concentrations of this antibiotic are cultivated in the culture solution. The recovery of the active substance in the culture solution follows either by chromatographic techniques in the form of salts or through addition of a physiologically compatible adsorbent as mycelium-containing nourseothricin-adsorbate, which preferably can be added to the dosaging of mixed feed agents.
    Type: Grant
    Filed: January 20, 1984
    Date of Patent: August 29, 1989
    Assignee: VEB Jenapharm
    Inventors: Friedrich Bergter, Harald Bocker, Ernst-Joachim Bormann, Wolfgang Forberg, Heinz Fricke, Udo Grafe, Hans-Helmut Grosse, Ingeborg Heller, Matthias Hilliger, Wolf Junne, Hellmut Linde, Michael Menner, Klaus-Dieter Menzel, Peter-Jurger Muller, Gunter Plonka, Hans D. Pohl, Jorg Schneider, Heinz Thrum
  • Method of treating cirrhosis
    Patent number: 4859660
    Abstract: A method of treating primary biliary cirrhosis comprising administering ursodeoxycholic acid to a patient suffering therefrom.
    Type: Grant
    Filed: November 19, 1987
    Date of Patent: August 22, 1989
    Assignee: Synthelabo
    Inventor: Raoul Poupon
  • Dermatics utilizing 17.beta.methyl-18 nor steroids and methods for their use
    Patent number: 4859659
    Abstract: Dermatics are claimed which are characterized in that they contain as the active compound one or two 17.beta.-methyl-18-nor steroids of general Formula I ##STR1## wherein is a single bond or a double bond,R.sub.1 is a hydrogen atom or a methyl group, andR.sub.2 is an alkyl group of maximally 6 carbon atoms, optionally substituted by an alkanoyloxy group containing 2-6 carbon atoms.
    Type: Grant
    Filed: December 17, 1986
    Date of Patent: August 22, 1989
    Assignee: Schering Aktiengesellschaft
    Inventors: Dieter Bittler, Henry Laurent, Klaus Nickisch, Petra Rach
  • Method for the treatment and prevention of arteriosclerosis with nitrophenyl substituted dihydropyridines
    Patent number: 4859688
    Abstract: The invention relates to a novel method for the treatment and prevention of arteriosclerosis, which comprises administering, as an active ingredient, a dihydropyridine compound of the formula: ##STR1## in which R.sup.1 is nitrophenyl and R.sup.2, R.sup.3 and R.sup.4 are each lower alkyl, or pharmaceutically acceptable salts thereof.
    Type: Grant
    Filed: March 30, 1987
    Date of Patent: August 22, 1989
    Assignee: Fujisawa Pharmaceutical Co., Ltd.
    Inventors: Isamu Yamaguchi, Jiro Hirosumi
  • Use of methyl-isoeugenol, n-dodecanol and mixtures of same as insect attractants
    Patent number: 4859463
    Abstract: Described are the uses of methyl-isoeugenol having the structure: ##STR1## n-dodecanol having the structure: ##STR2## and 1-(2-butenoyl)-2,6,6-trimethyl-1,3-cyclohexadiene having the structure: ##STR3## taken alone or taken in combination as attractants house flies (Musca domestica L. (Diptera:Muscidae)) and Stored Products Moths. The methyl-isoeugenol, n-dodecanol and 1-(2-butenoyl)-1,3-cyclohexadiene taken alone or in combination find utility primarily as bait enhancers for acute toxins and/or trapping devices.
    Type: Grant
    Filed: June 30, 1988
    Date of Patent: August 22, 1989
    Assignees: International Flavors & Fragrances Inc., The University of Florida
    Inventors: Richard A. Wilson, Jerry F. Butler, Donald Withycombe, Braja D. Mookherjee, Ira Katz, Kenneth R. Schrankel
  • Novel pharmaceutical compositions endowed with anti-progesteronic properties and a process for making the same
    Patent number: 4857519
    Abstract: This invention relates to pharmaceutical compositions endowed with anti-progesteronic properties. This invention provides pharmaceutical compositions containing a pharmacologically effective amount of a 17.beta.-OR 17.alpha.-ethynyl-5.alpha.-androst-2-ene in admixture or conjunction with an innocuous pharmaceutical carrier or vehicle. The pharmaceutical compositions according to this invention are useful to prevent nidation or gestation.
    Type: Grant
    Filed: May 5, 1987
    Date of Patent: August 15, 1989
    Inventor: Jacques Paris
  • Hydroxylated 24-homo-vitamin D derivatives and methods for preparing same
    Patent number: 4857518
    Abstract: This invention is directed to new 24-homo-vitamin D compounds, to methods for preparing the same and novel intermediate compounds.The compounds are characterized by vitamin D-like activity of the order of 1.alpha.,25-dihydroxyvitamin D.sub.3, the recognized circulating hormonal form of vitamin D, or various of its derivatives and by greater antineoplastic activity than such compounds but without their attendant calcemic activity. The compounds are useful in the treatment of disease states characterized by calcium-phosphorous imbalances and where antineoplastic activity is indicated.
    Type: Grant
    Filed: February 28, 1986
    Date of Patent: August 15, 1989
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Nobuo Ikekawa, Yoko Tanaka
  • Process for obtaining D(+)-naproxen
    Patent number: 4857462
    Abstract: A process for obtaining D-2-(6-methoxy-2-naphthyl)-propionic acid from a mixture of D- and L-2-(6-methoxy-2-naphthyl)-propionic acid lower alkyl esters is provided by asymmetric hydrolysis of the L-ester with a microbial enzyme, separation of the 2-(6-methoxy-2-naphthyl)-propionic acid from the D-2-(6-methoxy-2-naphthyl)-propionic acid lower alkyl ester and saponification of the latter, wherein the saponification is carried out enzymatically with esterase from hog liver or from Pleurotus ostreatus.
    Type: Grant
    Filed: October 27, 1986
    Date of Patent: August 15, 1989
    Assignee: Boehringer Mannheim GmbH
    Inventors: Josef Maier, Manfred Gloger, Detlef V. Hoerschelmann, Jan Strejcek, Sebastian Heimerl
  • Iodinated estradiols, intermediate products and methods of production
    Patent number: 4855125
    Abstract: A method of preparation of estradiol derivatives labeled by iodine, especially .sup.123 I, substitution at C-16 are synthesized according to the present invention. A triflate intermediate is prepared from which either 16-alpha-.sup.123 I-17-beta-estradiol or 16-beta-.sup.123 I-17-beta-estradiol are prepared by described methods. Both 16-alpha-.sup.123 I- and 16-beta-.sup.123 I-17-beta-estradiol made according to the methods described herein have a high relative specific acitvity. The methods are sufficiently rapid so that the relatively short half-life of .sup.123 I is readily accommodated without substantial radioactive decay of the label.
    Type: Grant
    Filed: September 25, 1987
    Date of Patent: August 8, 1989
    Assignee: Bio-Medical Research Laboratories
    Inventors: Richard J. Baranczuk, Jay Spicer, William P. Duncan, Gary A. Rotert
  • Compositions and methods of effecting contraception utilizing melatonin
    Patent number: 4855305
    Abstract: A method of effecting contraception in human females comprises administering an ovulation-inhibiting amount of melatonin. Optionally, the melatonin is administered in combination with a progestogen and/or an estrogen. The administration of melatonin also provides a method of preventing breast cancer in women.
    Type: Grant
    Filed: March 23, 1987
    Date of Patent: August 8, 1989
    Assignee: Applied Medical Research
    Inventor: Michael Cohen
  • Fluorine derivatives of vitamin D.sub.3 and process for producing the same
    Patent number: 4853378
    Abstract: There are disclosed novel derivatives of 26,26,26,27,27,27-hexafluorovitamin D.sub.3 having fluorine atom at the 23- and/or 24-position which have an excellent pharmacological activity and a process for production thereof. The novel compounds are represented by the general formula: ##STR1## wherein R.sub.1 ' denotes a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sub.2 denotes a hydrogen atom or a protecting group for hydroxyl group, R.sub.3 denotes a hydrogen atom, a fluorine atom, a hydroxyl group or a protected hydroxyl group and R.sub.4 and R.sub.4 ' each denotes a hydrogen atom, or one of them denotes a hydrogen atom and the other denotes a fluorine atom, hydroxyl group or a protected hydroxyl group or R.sub.4 and R.sub.4 ' are combined to denote an oxo group, with a proviso that at least one of R.sub.3, R.sub.4 and R.sub.4 ' denote a fluorine atom.
    Type: Grant
    Filed: October 14, 1987
    Date of Patent: August 1, 1989
    Assignee: Sumitomo Chemical Company, Limited
    Inventors: Noritaka Hamma, Yoshikazu Saito, Toshio Nishizawa, Takashi Katsumata
  • Method for producing monomethylformamide and dimethylformamide
    Patent number: 4853485
    Abstract: Monomethylformamide and dimethylformamide are produced by the catalytic reaction of formamide and methanol, using a quaternary ammonium compound as the catalyst.
    Type: Grant
    Filed: October 21, 1987
    Date of Patent: August 1, 1989
    Assignee: E. I. Du Pont de Nemours and Company
    Inventor: Harold E. Bellis
  • Aqueous pyrethroid insecticidal formulations in polyvinyl chloride containers, and methods of producing such formulations that are stable
    Patent number: 4851438
    Abstract: The addition of nonionic surfactants to aqueous pyrethroid insecticidal formulations increases the pyrethroid stability when the formulation is stored in a polyvinylchloride (PVC) container. The pyrethroids can be synthetic or naturally occurring pyrethroids. The nonionic surfactants are alkylphenol ethoxylates, ethoxylated primary alcohols, polyoxyethylene thioethers or mixtures thereof and have HLB values of between about 10 and about 14.
    Type: Grant
    Filed: October 20, 1986
    Date of Patent: July 25, 1989
    Assignee: S. C. Johnson & Son, Inc.
    Inventor: Stanley J. Flashinski
  • Hydroxylated 26-homo vitamin D derivatives and methods for preparing same
    Patent number: 4851400
    Abstract: This invention is directed to new 26-homo-vitamin D compounds, to methods for preparing the same and novel intermediate compounds.The compounds are characterized by vitamin D-like activity of the order of 1.alpha.,25-dihydroxyvitamin D.sub.3, the recognized circulating hormonal form of vitamin D, or various of its derivatives and by greater antineoplastic activity than such compounds but without their attendant calcemic activity. The compounds are useful in the treatment of disease states characterized by calcium-phosphorous imbalances and where antineoplastic activity is indicated.
    Type: Grant
    Filed: March 3, 1986
    Date of Patent: July 25, 1989
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Nobuo Ikekawa, Yoko Tanaka
  • Novel cyclopentano-vitamin D analogs
    Patent number: 4851401
    Abstract: This invention provides novel 1.alpha.-hydroxyvitamin D compounds, methods for their preparation, and pharmaceutical compositions of these compounds. The new compounds, which are characterized structurally by having a cyclopentane ring as part of their side chains, exhibit highly pronounced biological activity, both in terms of their effect on calcium metabolism and their effect on differentiating malignant cells to normal cells. By virtue of their biological properties, the new vitamin D analogs are effective as calcium-regulating, or differentiation-inducing agents, and thus find application as therapeutic agents in the treatment or prophylaxis of bone-related as well as neoplastic diseases.
    Type: Grant
    Filed: July 14, 1988
    Date of Patent: July 25, 1989
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Kato L. Perlman, Andrzej Kutner
  • Glycerol containing virucidal compositions
    Patent number: 4849455
    Abstract: A virucidal agent against naked vires containing at least 70% of methanol and/or ethanol and from 1 to 10% of glycerol and optionally, up of 5% of castor oil for improving the skin compatibility.
    Type: Grant
    Filed: October 21, 1986
    Date of Patent: July 18, 1989
    Assignee: Kruger GmbH & Co. KG
    Inventors: Hans J. Eggers, Gerhard Schott
  • Vitamin D related compounds and processes for their preparation
    Patent number: 4847012
    Abstract: The invention relates to a method for preparing vitamin D-related compounds and to certain intermediate compounds in such process. The intermediate compounds are characterized by an aldehyde or ester in the C-22 position in the side chain. The presence of such groups permit facile side chain additions for the preparation of vitamin D derivatives.
    Type: Grant
    Filed: April 29, 1988
    Date of Patent: July 11, 1989
    Assignee: Wisconsin Alumni Research Foundation
    Inventors: Hector F. DeLuca, Heinrich K. Schnoes, Andrzej Kutner, Kato L. Perlman, Rafal R. Sicinski, Mary E. Phelps