Patents Represented by Attorney John S. Roberts, Jr.
  • Patent number: 4206226
    Abstract: The Pt compound may be prepared by reacting the known dichloro(1,2-diaminocyclohexane) platinum(II) (NSC 194814) with silver nitrate to replace chloro with nitro. Subsequently, benzene tricarboxylic acid is added to form an off-white precipitate (2 hrs, dark, 5.degree. C.) of the desired product which is preferably utilized as the alkali metal salt.The 4-carboxyphthalato(1,2-diaminocyclohexane)-platinum(II) and alkali metal salts thereof may be combined in multiple drug regimen with substantially improved yield cures over the parent compound. For example, the compound denoted Pt-307 may be combined in a dual regimen with cyclophosphamide (CY) and in a triple drug regimen of Pt-307 plus cyclophosphamide (CY) and either 5-fluorouracil (5-FU) or hydroxyurea (HU) as the third component.
    Type: Grant
    Filed: July 19, 1978
    Date of Patent: June 3, 1980
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventors: Glen R. Gale, Paul Schwartz
  • Patent number: 4206208
    Abstract: The Pt compound may be prepared by reacting the known dichloro(1,2-diaminocyclohexane)platinum(II) (NSC 194814) with silver nitrate to replace chloro with nitro. Subsequently, benzene tricarboxylic acid is added to form an off-white precipitate (2 hrs, dark, 5.degree. C.) of the desired product which is preferably utilized as the alkali metal salt.The 4-carboxyphthalato(1,2-diaminocyclohexane)platinum(II) and alkali metal salts thereof may be combined in multiple drug regimen with substantially improved yield cures over the parent compound. For example, the compound denoted Pt-307 may be combined in a dual regimen with cyclophosphamide (CY) and in a triple drug regimen of Pt-307 plus cyclophosphamide (CY) and either 5-fluorouracil (5-FU) or hydroxyurea (HU) as the third component.
    Type: Grant
    Filed: December 22, 1978
    Date of Patent: June 3, 1980
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventors: Glen R. Gale, Paul Schwartz
  • Patent number: 4202890
    Abstract: 4-Carboxyphthalato(1,2-diaminocyclohexane)platinum(II) (and alkali metal salts thereof) has shown antileukemic activity in mice against murine leukemia L1210. It is effective in dosages of 5-60 mg/kg of body weight and is potentiated in a treatment with cyclophosphamide (CY) (50 mg/kg of body weight) to which may be added 5-fluorouracil (5-FU) (75 mg/kg of body weight) or hydroxyurea (HU) (1000 mg/kg of body weight). Some previous platinum chelate compounds show dosage limitation due to renal impairment but the free carboxyl of the present Pt compound offers a possible route of oral administration and absorption by the stomach.The Pt compound may be prepared by reacting the known dichloro(1,2-diaminocyclohexane)platinum(II) (NSC 194814) with silver nitrate to replace chloro with nitro. Subsequently, benzene tricarboxylic acid is added to form an off-white precipitate (2 hrs, dark, 5.degree. C.) of the desired product which is preferably utilized as the alkali metal salt.
    Type: Grant
    Filed: December 22, 1978
    Date of Patent: May 13, 1980
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventors: Glen R. Gale, Paul Schwartz
  • Patent number: 4201773
    Abstract: A series of compounds showing high antileukemic activity against P388 murine leukemia and increased aqueous solubility due to substitution of --OH for the known --NH.sub.2 at the 3' position of the hexopyranose sugar, i.e., daunosamine.These compounds are coupled products of aglycon selected from daunomycinone, desmethoxy daunomycinone, adriamycinone and carminomycinone. These compounds are coupled at the 0-7 position of the aglycon with an .alpha.
    Type: Grant
    Filed: July 26, 1978
    Date of Patent: May 6, 1980
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventors: Derek Horton, Wolfgang Weckerle, Ernst F. Fuchs, Tak M. Cheung, Beat Winter, Roderick J. Sorenson
  • Patent number: 4189583
    Abstract: This invention relates to a process for the production of 4a-aryldecahydroisoquinolines where the aryl group is selected as 3-methoxy phenyl. These compounds are morphine analogs and show utility similar to the known morphine, codeine, and thebaine. In this process particular novelty is asserted for the production of a nipecotic ester ethyl 4-(3'-methoxyphenyl)-1-methyl piperidine-3-carboxylate. Furthermore, novelty is asserted for the step of conversion of the nipecotates through cyclization to cis- or trans-tert-butyl 1,6-dioxo-4a-(3'-methoxyphenyl)-2-methyldecahydroisoquinoline-7-carboxylat e, which may also be easily converted to the keto amide, trans-1,6-dioxo-4a-(3'-methoxyphenyl)-2-methyldecahydroisoquinoline.
    Type: Grant
    Filed: April 26, 1978
    Date of Patent: February 19, 1980
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventors: Henry Rapoport, Dwight D. Weller, Richard D. Gless
  • Patent number: 4188378
    Abstract: A method of utilizing 9-.beta.-D-arabinofuranosyl-2-fluoroadenine, known as 2-F-AraA (NSC 118218), in the treatment of murine leukemia and as an antiviral agent for DNA viruses, such as DNA viruses Herpes Simplex Virus Type I and Vaccinia virus grown in H.Ep-2 cells in culture. An operable dosage for utilization of 2-F-AraA is a treatment span of 1-10 days with the dosage 2-8 times per day at 8-400 mg/kg/dose. It has been further found that a single dosage on days 1, 5, and 9 based on a 10-day treatment schedule gave satisfactory results.
    Type: Grant
    Filed: January 4, 1978
    Date of Patent: February 12, 1980
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventor: John A. Montgomery
  • Patent number: 4183864
    Abstract: Steroid compounds obtained by co-oligomerization of a side chain functionalized 1,5-hexadiyne with bis(trimethylsilyl)acetylene catalyzed by cyclopentadiene cobalt dicarbonyl, CpCO(CO).sub.2, via intermediate benzocyclobutene formation followed by intramolecular cycloaddition to the sterospecific formation of the steroid nucleus. This constitutes a short steroid synthesis, five steps from commercially available acyclic precursor 1,5-hexadiyne and three steps from 2-methyl-cyclopent-2-enone.
    Type: Grant
    Filed: February 21, 1978
    Date of Patent: January 15, 1980
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventors: K. Peter C. Vollhardt, Raymond L. Funk
  • Patent number: 4178922
    Abstract: A therapeutic belt which is peculiarly adapted for the sacro-lumbar region of the body is disclosed. The belt appliance includes one or more inflatable cell structures integrally formed with the belt body as an extrusion. The inflatable structures are divided into air cell pockets by means of die cutting and heat sealing operations, and the pockets are fluidically connected to an air source by an air duct which is also integrally formed with the belt body and the inflatable cells. The pockets have different configurations and vary in size, and the extrusion is fabricated from a plastic vinyl material which exhibits a low coefficient of stretchability. The inflated configuration of the cell structure is also memorized into the material whereby substantially the same inflated configuration is always obtained. Precisely defined and located contact areas, developing predetermined amounts of counterpressure, are thus present within the appliance for application to the body portions for therapeutic purposes.
    Type: Grant
    Filed: September 23, 1977
    Date of Patent: December 18, 1979
    Inventor: James D. Curlee
  • Patent number: 4178923
    Abstract: A therapeutic corset which is peculiarly adapted for the sacro-lumbar region of the body is disclosed. The corset appliance includes one or more inflatable cell structures which are detachable from the corset and positionally adjustable therein. Different cells have differently sized and configured air pockets, and, as a result of the interchangeability of the cells as facilitated by their ready detachment from the corset, different therapeutic results may be achieved, depending upon the particular cell chosen. The cells are fabricated from a plastic vinyl material which exhibits a low coefficient of stretchability, and, in addition, the inflated configuration of the cell is memorized into the cell structure. Consequently, upon inflation of the cell, the same always assumes substantially the same configuration whereby precisely located counterpressure may be applied to particular areas of the lumbar region of the body.
    Type: Grant
    Filed: September 23, 1977
    Date of Patent: December 18, 1979
    Inventor: James D. Curlee
  • Patent number: 4178285
    Abstract: This invention relates to a method of separating the active .alpha..sub.1 -acid glycoprotein fraction, a co-factor in the lipoprotein lipase reaction, from urine of nephrotic animals and humans as follows:(a) concentrate the said urine to about 10-20% by volume;(b) precipitate undesired protein at pH 4 with ammonium sulfate; and(c) recover the .alpha..sub.1 -acid glycoprotein fraction from the supernatant, neutralize with solid NaHCO.sub.3, and purify by dialysis versus H.sub.2 O and lyophilize.This active .alpha..sub.1 -acid glycoprotein fraction is utilized in effective amounts in nephrotic animals to reverse the defect in triglyceride removal caused by the loss of plasma constituents in urine.
    Type: Grant
    Filed: December 20, 1978
    Date of Patent: December 11, 1979
    Inventors: James M. Felts, Ilona Staprans
  • Patent number: 4173582
    Abstract: The present invention relates to a method for the manufacture of an improved ureaform fertilizer. The method consists in the condensation of urea and formaldehyde carried out in a controlled system having a pH between 3.5 and 4.2 wherein the overall concentration of the reagents is in the range of 20 to 40% by weight. The ratio between the reagents is between 1.2 to 1.5 moles of urea to 1 mole of formaldehyde and the temperature of the reaction is kept between 15.degree. C. to 40.degree. C. Examples of preferred controlled systems are H.sub.3 PO.sub.4 -KH.sub.2 PO.sub.4 and H.sub.3 PO.sub.4 -NH.sub.4 H.sub.2 PO.sub.4. The method can also be performed in a continuous manner giving rise to an overall quantitative yield, and being temperature self-regulating.The ureaform obtained by the method has an activity index of over 75 and excellent physical properties.
    Type: Grant
    Filed: March 26, 1976
    Date of Patent: November 6, 1979
    Assignee: Fertilizers & Chemicals Ltd.
    Inventors: Dahlia S. Greidinger, Liuba Cohen nee Girshowitsh, Shimon Epstein
  • Patent number: 4172740
    Abstract: A system for extracting energy from the sun's rays including a bank of solar energy cells which generate electrical current when exposed to the rays of the sun, immersed in a bath of liquid formed to serve as a lens, concentrating the sun rays on the cells, and transmitting heat away from the cells. The cells are shaped so as to cause a trapping effect of radiation incident thereon. The improved solar converting unit additionally includes a method for preheating the interior thereof. The converting unit is preferably equipped with light gathering and focusing means thereby providing coherent optically output.
    Type: Grant
    Filed: March 28, 1978
    Date of Patent: October 30, 1979
    Inventor: William P. Campbell, III
  • Patent number: 4172679
    Abstract: The invention relates to a method for renewing road surfaces where in the course of one single operational step the road surface is milled away, heated and coated with new material and wherein according to a special embodiment of the invention the milling away or cutting away is performed to an amount not reaching the depth of the damages, at least part of the cut away material is distributed in the remaining recesses and is compressed, and subsequently the road surface is subjected to a heating and a subsequent aeration and is then uniformly coated with new material; and it relates also to a machine for performing the method, wherein, behind said cutting or milling device, a distribution device for distributing the milled off material in the remaining recesses of the road surface, a compression device for compressing the milled off material within the recesses, a heating device and optionally a scraper device provided for the aeration of the road surface, which are followed by a spreader device for applying
    Type: Grant
    Filed: July 5, 1978
    Date of Patent: October 30, 1979
    Inventor: Reinhard Wirtgen
  • Patent number: 4169572
    Abstract: A cable grommet with tension or strain relief for the securement of cables in the aperture of a housing comprising two tubularly shaped and coaxially telescoped clamping portions being twistable towards each other, and the inner cross section of the outer portion, which is to be inserted into the aperture of the housing, deviates from the concentric circular cross section and the inner portion being coaxially inserted into the outer portion is divided, on one of its ends, by slots extending in axial direction over part of its length to form clamping jaws which on the outer side thereof, at least partly, are provided with circumferentially extending rising or tapering projections sliding on the inner wall of said outer portion and which when the two portions are twisted towards each other press the clamping jaws against the cable guided in said inner portion.
    Type: Grant
    Filed: November 10, 1977
    Date of Patent: October 2, 1979
    Inventor: Hans Simon
  • Patent number: 4169011
    Abstract: 3'-Phosphoadenosine 5'-phosphosulfate, also known as PAPS, is useful in establishing sulfate transfer mechanisms in animals and may be produced by a chemical process yielding 68-72% product from a pure adenosine 2',3'-cyclic phosphate 5'-phosphate, which compound is initially prepared from the reaction of adenosine and pyrophosphoryl chloride. In the present procedure the pure cyclic phosphate is reacted with triethylamine-N-sulfonic acid to produce 2',3'-cyclic phosphate 5'-phosphosulfate. Subsequently, by hydrolysis with the enzyme ribonuclease-T.sub.2, the desired compound is produced. Alternatively, the 2'-phosphoadenosine 5'-phosphosulfate, known as iso-PAPS, may be produced from 2',3'-cyclic phosphate 5'-phosphosulfate by treatment with a different enzyme, PDase or spleen phosphodiesterase. This latter compound, iso-PAPS, biologically has only one-third the activity of PAPS, the natural isomer.
    Type: Grant
    Filed: October 11, 1977
    Date of Patent: September 25, 1979
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventors: Jerome P. Horwitz, John P. Neenan, Radhey S. Misra, Jurij Rozhin, Anne L. Huo, Kirsten D. Philips, deceased
  • Patent number: 4167633
    Abstract: An improved process for the production of ##STR1## FROM ##STR2## WHICH PRODUCES BUT DOES NOT ISOLATE AN INTERMEDIATE ##STR3## WHICH COMPOUND IS RETAINED IN SITU AND MINIMIZES THE COMPLEX POLYMER FORM OF A THREE-DIMENSIONAL NETWORK OF AZO LINKAGES FORMED BY THE NITROSO AND AMINO GROUPS. These groups, as they appear in the nitroso intermediate, have carcinogenic possibilities. It has been found that the nitroso compound will precipitate as a stirrable slurry if the temperature parameter is kept low at about 0.degree.-20.degree. C. A preferred route for the production of the nitroso compound from the triamino starting material utilizes as reactants 1.0-1.05 moles of sodium nitrite and 1.5 moles of HOAc in water (HCl may be substituted for HOAc). In the second state of this sequential reaction, the reduction of nitroso is carried out by a reducing agent and one preferred agent is sodium dithionite. Catalytic agents such as Raney nickel and hydrazine or nickel salts, e.g.
    Type: Grant
    Filed: July 20, 1977
    Date of Patent: September 11, 1979
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventor: Thomas J. Morrow
  • Patent number: 4159922
    Abstract: In the alkaline pulping of cellulose and particularly in the step wherein green liquor is converted to white liquor by causticizing or the addition of calcium hydroxide, it has been found that the addition of any of three specially selected organic phosphonate reagents, namely, nitrilotris(methylenephosphonic acid) (Dequest 2000); 2-phosphonobutane-1,2,4-tricarboxylic acid (Bayer PBS-AM); and hexamethylenediaminetetrakis(methylenephosphonic acid) (Nalco 7691/Dequest 2051), accelerates the speed of the reaction to the right. These acid compounds and their soluble alkali metal and ammonium salts have proved effective in increasing the acceleration rate to the right of the causticizing reaction and the production of the titratable sodium hydroxideCaO+H.sub.2 O.fwdarw.Ca(OH).sub.2ca(OH).sub.2 +Na.sub.2 CO.sub.3 .fwdarw.2NaOH+CaCO.sub.3 .dwnarw.these additives give up to a 2-4% increase in causticizing conversion to NaOH when applied at 0.
    Type: Grant
    Filed: October 12, 1978
    Date of Patent: July 3, 1979
    Assignee: Nalco Chemical Company
    Inventor: David R. Cosper
  • Patent number: 4157799
    Abstract: The invention relates to a cable grommet with a traction relief particularly for guiding a cable through the opening of an apparatus wall or the like comprising a funnel body having a thoroughfare for said cable, shoulders extending into said opening of said apparatus wall, a setscrew arranged within said funnel body under an angle relative to the axis of the thoroughfare reacting via an intermediate piece upon said cable, wherein a shoulder is provided which is connected with said funnel body and extends from the side of said setscrew into said opening and a further shoulder is provided which is connected with said funnel body and supports said cable on the other side of said opening.
    Type: Grant
    Filed: November 16, 1977
    Date of Patent: June 12, 1979
    Inventor: Hans Simon
  • Patent number: 4150236
    Abstract: Tricyclic aromatic compounds of the formula ##STR1## including those wherein: (A) R.sub.1 is H, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(b) R.sub.1 is acetyl, R.sub.2 is carbomethoxy, and R.sub.3 is methyl;(c) R.sub.1 and R.sub.3 are methyl and R.sub.2 is carbomethoxy;(d) R.sub.1, R.sub.2, and R.sub.3 are hydrogen; and(e) R.sub.1 and R.sub.3 are methyl and R.sub.2 is hydrogenAre intermediates for the total synthesis of steroids.
    Type: Grant
    Filed: July 19, 1977
    Date of Patent: April 17, 1979
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventors: Ulrich Weiss, Kenner C. Rice
  • Patent number: 4148888
    Abstract: 3-Deazaadenosine has been found to be an effective antiviral and antifocal agent in tissue culture of animals as evidenced by its activity against Rous sarcoma virus, influenza virus, vesicular stomatitis virus, Sindbis virus, and Newcastle disease virus in the range 0.03-0.3 mM. This compound has also shown use as an inhibitor of adenosylhomocysteine hydrolase from beef liver in the range of 0.001-0.008 mM (I.sub.50). The antiviral and antifocal effect is correlated with the inhibition of hydrolysis of adenosylhomocysteine in cells. This inhibition of adenosylhomocysteine hydrolase can also be demonstrated in livers of rats injected with 3-deazaadenosine.
    Type: Grant
    Filed: March 13, 1978
    Date of Patent: April 10, 1979
    Assignee: The United States of America as represented by the Department of Health, Education and Welfare
    Inventors: Giulio L. Cantoni, Peter K. Chiang, Henry H. Richards