Patents Represented by Attorney Thomas E. Arther
  • Patent number: 4414215
    Abstract: N-Acyl derivatives of 6-(alkylamino)-5-chloro-3-nitro-pyrazinamines are disclosed to have activity in increasing the sensitivity of tumor cells to radiation. Also disclosed are methods of preparing such compounds and pharmaceutical compositions including such compounds.
    Type: Grant
    Filed: July 19, 1982
    Date of Patent: November 8, 1983
    Assignee: Merck & Co., Inc.
    Inventor: George D. Hartman
  • Patent number: 4394515
    Abstract: Novel 7- and 8-R-10,11-dihydro-11-oxodibenzo[b,f]thiepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: April 6, 1981
    Date of Patent: July 19, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Joshua Rokach, Clarence S. Rooney, Edward J. Cragoe, Jr.
  • Patent number: 4386026
    Abstract: Cell-specific ligands comprising conjugates of saccharides and amino acids or peptides are synthesized from amino acids such as ornithine, lysine, peptides such as dilysine, diornithine or oligolysine and selected saccharides having reactive functional groups protected by appropriate blocking groups. Such glycopeptides are useful as tissue specific substances, which when coupled with bioactive materials through metabolizable or hydrolyzable linkages, deliver such bioactive materials to the selected site. In this manner, antiinflammatory drugs such as dexamethasone are linked through a metabolizable or hydrolyzable linkage and on administration to an animal suffering from inflammatory disease carries the drug to the site of inflammation for intracellular release. Other examples include the macrophage ligand N.sup.2 -N.sup.2, N.sup.6 -Bis-[3-(.alpha.-D-mannopyranosylthio)propionyl]-6-lysyl-N.sup.6 -[3-(.alpha.-D-mannopyranosylthio)propionyl]-L-lysine, 5, which when coupled to .beta.
    Type: Grant
    Filed: April 20, 1981
    Date of Patent: May 31, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Mitree M. Ponpipom, Robert L. Bugianesi, James C. Robbins, Tsung-Ying Shen
  • Patent number: 4377568
    Abstract: An enteric coating medium for solid medicinal dosage units is prepared by precipitation of a pH sensitive polymer from an alcoholic solution of such a polymer and a plasticizing agent to produce a suspension of fine particles of a mixture of polymer and plasticizing agent.
    Type: Grant
    Filed: August 12, 1981
    Date of Patent: March 22, 1983
    Assignee: Merck Sharp & Dohme (I.A.) Corp.
    Inventor: Sham K. Chopra
  • Patent number: 4377515
    Abstract: Novel peptides of the formula: ##STR1## where A through G, X and Y are various amino acids and substituents; having long lasting LHRH agonist and antagonist activity; useful in promoting fertility, reducing fertility, respectively.
    Type: Grant
    Filed: October 1, 1979
    Date of Patent: March 22, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Daniel F. Veber, Roger M. Freidinger
  • Patent number: 4377584
    Abstract: 4-Aza-17.beta.-substituted-5.alpha.-androstan-3-ones and their A-homo analogs of the formula: ##STR1## where Formula (I) may also have the structure of partial Formulas (II) and/or (III);and pharmaceutically acceptable salts of the above compounds are active as testosterone 5.alpha.-reductase inhibitors, and thus useful topically for treatment of acne, seborrhea, female hirsutism, and systemically in treatment of benign prostatic hypertrophy.
    Type: Grant
    Filed: September 23, 1980
    Date of Patent: March 22, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Gary H. Rasmusson, David B. R. Johnston, Glen E. Arth, deceased
  • Patent number: 4369183
    Abstract: The invention concerns novel 2-aryl-1,2-benzisothiazolinone-1,1-dioxide compounds; methods for their preparation; pharmaceutical compositions containing them as an active ingredient; and methods of selectively inhibiting proteases, especially elastase, and of treating emphysema, rheumatoid arthritis, and various inflammatory diseases, for example, bronchial inflammation.
    Type: Grant
    Filed: February 2, 1981
    Date of Patent: January 18, 1983
    Assignee: Merck & Co., Inc.
    Inventors: Howard Jones, Robert L. Clark, Morris Zimmerman
  • Patent number: 4362621
    Abstract: An improved radial flow cell, comprising two or more sets of inlet port-groove-dam devices for improving the efficiency of radial flows and an efficient filtration device consisting of a micropore membrane and a steel screen support of low retention volume, is useful for aseptic and continuous in-line filtration of heterogeneous mixtures containing high concentrations of solids especially those resulting from fermentation processes.
    Type: Grant
    Filed: April 27, 1981
    Date of Patent: December 7, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Robert W. Dobna, B. Allen Mayles, Thomas H. Stoudt
  • Patent number: 4334077
    Abstract: The present invention relates to a process for the preparation of an enantiomer of 7 or 8-fluoro-dibenzo[b,f]thiepin-3-carboxylic acid having a negative rotation and prostaglandin antagonist activity.
    Type: Grant
    Filed: January 28, 1981
    Date of Patent: June 8, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Patrice C. Belanger, Joshua Rokach, Robert N. Young, John Scheigetz
  • Patent number: 4329363
    Abstract: The present application discloses a method of correcting an imbalance of immune homeostasis caused by cytostatic treatment or radiotherapy by administering to a patient in need of such treatment an effective amount of a novel substituted mercapto acid amide and pharmaceutical compositions containing such novel substituted mercapto acid amides.
    Type: Grant
    Filed: January 16, 1980
    Date of Patent: May 11, 1982
    Assignee: Merck & Co., Inc.
    Inventors: Conrad P. Dorn, Howard Jones
  • Patent number: 4300569
    Abstract: This invention relates to a method for efficiently labelling red blood cells , which permits the imaging of blood pools in the intact animal or human patient, accomplished by injection of a saline solution of an alkaline earth metal salt of glucoheptonic acid and a non-toxic stannous salt followed by injection with a solution of sodium pertechnetate Tc 99 m to tag the red blood cells. The invention also relates to the kit used in the method of our invention consisting of a single vial containing 25 mg. calcium glucoheptonate and 3 mg. of stannous chloride dihydrate in 2 ml. of saline solution.
    Type: Grant
    Filed: February 25, 1980
    Date of Patent: November 17, 1981
    Assignee: Merck & Co., Inc.
    Inventor: Paul-Emile Bonneau
  • Patent number: 4282365
    Abstract: Novel dibenz[b,e]oxepin derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: November 24, 1978
    Date of Patent: August 4, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Joshua Rokach, Edward J. Cragoe, Jr., Clarence S. Rooney
  • Patent number: 4276298
    Abstract: The invention concerns novel 2-aryl-1,2-benzisothiazolinone-1,1-dioxide compounds; methods for their preparation; pharmaceutical compositions containing them as an active ingredient; and methods of inhibiting proteases, especially elastase, and of treating emphysema, rheumatoid arthritis, and various inflammatory diseases, for example, bronchial inflammation.
    Type: Grant
    Filed: September 6, 1979
    Date of Patent: June 30, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Howard Jones, Robert L. Clark, Morris Zimmerman
  • Patent number: 4263207
    Abstract: Novel dibenzo[b,f][1,4]thiazepine derivatives are employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: August 1, 1978
    Date of Patent: April 21, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Joshua Rokach, Edward J. Cragoe, Jr., Clarence S. Rooney
  • Patent number: 4260771
    Abstract: This invention relates to novel interphenylene 9-thia-11-oxo-12-azaprostanoic acid compounds, salts, and derivatives thereof. These compounds have prostaglandin-like biological activity and are particularly useful as renal vasodilators, as platelet aggregation inhibitors, and for the treatment of certain autoimmune diseases.
    Type: Grant
    Filed: December 20, 1979
    Date of Patent: April 7, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Edward J. Cragoe, Jr., Ta-Jyh Lee, John B. Bicking
  • Patent number: 4257417
    Abstract: There is provided a bottle holder for a squeeze-type eyedropper bottle which includes a flat spacer member, a bottle holder attached at one end of said spacer member, and a rest piece slidably positioned at a distance intermediate the midpoint and the opposite end of said spacer member.
    Type: Grant
    Filed: July 31, 1979
    Date of Patent: March 24, 1981
    Assignee: Merck & Co., Inc.
    Inventor: Kenneth J. Gibilisco
  • Patent number: 4252818
    Abstract: 7-[3-(4-Acetyl-3-hydroxy-6-iodo-2-propylphenoxy)-2-hydroxypropoxy]-4-oxo-8- propyl-4H-1-benzopyran-2-carboxylic acid and its pharmaceutically acceptable salts are employed as antagonists of SRS-A (the slow reacting substance of anaphylaxis) in the treatment of asthma and allergic diseases.
    Type: Grant
    Filed: August 2, 1979
    Date of Patent: February 24, 1981
    Assignee: Merck & Co., Inc.
    Inventors: Joshua Rokach, Pierre A. Hamel, Ralph F. Hirschmann
  • Patent number: 4237160
    Abstract: Novel 3-hydroxymethyldibenzo[b,f]thiepin and derivatives are prepared and employed in the treatment and control of allergic conditions such as allergic asthma.
    Type: Grant
    Filed: November 27, 1979
    Date of Patent: December 2, 1980
    Assignee: Merck Sharp & Dohme (I.A.) Corp.
    Inventors: Pierre A. Hamel, Joshua Rokach
  • Patent number: 4235820
    Abstract: This invention relates to a process for the preparation of 5H-dibenzo[a,d]cycloheptene compounds and derivatives having aminoalkyl substituents at the 5-position by reducing the corresponding 5-aminoalkyl-5-hydroxy compounds with an alkali metal borohydride in trifluoroacetic acid.
    Type: Grant
    Filed: August 10, 1976
    Date of Patent: November 25, 1980
    Assignee: Merck & Co., Inc.
    Inventor: Ben E. Evans
  • Patent number: 4233457
    Abstract: This invention relates to an improved process for preparing 5-fluoro-2-methyl-1-(p-methylsulfinylbenzylidene)-3-indenyl acetic acid.
    Type: Grant
    Filed: May 17, 1979
    Date of Patent: November 11, 1980
    Assignee: Merck & Co., Inc.
    Inventors: Robert F. Czaja, Edward J. J. Grabowski