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.
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.
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
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.
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.
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
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
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
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
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.
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.
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
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
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.
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
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.
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.