Patents Assigned to Merck & Co.
  • Process for the glycosylation of avermectin compounds
    Patent number: 5192671
    Abstract: Avermectin compounds are glycosylated the 4' and 4"-positions by adding the avermectin compounds to the fermentation medium of Saccharapolyspora erythrea. The outer oleandrose sugar group of the avermectin compound is glycosylated with a glycosyl moiety, specifically a glucose group. In addition, other changes are effected in the avermectin moiety such as selective hydroxylation, epimerization at the 2-carbon and migration of the .DELTA. 3-double bond to a .DELTA. 2-position.
    Type: Grant
    Filed: June 26, 1991
    Date of Patent: March 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Byron H. Arison, Marvin D. Schulman, Patrick J. Doherty
  • Synthesis of protease inhibitor
    Patent number: 5192668
    Abstract: A dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: February 27, 1992
    Date of Patent: March 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Laszlo R. Treiber, Lawrence F. Colwell, Jr., Byron H. Arison, Georgette Dezeny, Russell B. Lingham, Wayne J. Thompson, Suresh K. Balani
  • Method and assemblage for controlling and managing lower explosion levels
    Patent number: 5189811
    Abstract: There are disclosed a method and an assemblage for controlling and managing lower explosion levels of those products containing volatile or combustible materials which can create a potentially explosive or combustible atmosphere when such products are dried or subjected to further processing in an oven or furnace.
    Type: Grant
    Filed: March 18, 1992
    Date of Patent: March 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: James C. Rose, Thomas P. DiNardo
  • Foam-stabilized malt beverage
    Patent number: 5190778
    Abstract: A fermented malt beverage having improved foam stability and desirable lace, cling, and clarity is described. The beverage is stabilized by adding 5-400 ppm by weight of gellan gum.
    Type: Grant
    Filed: May 23, 1990
    Date of Patent: March 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Kenneth Clare, deceased, Margaret A. Lawson
  • High-glyceryl, low-acetyl gellan gum for non-brittle gels
    Patent number: 5190927
    Abstract: A partially deacylated gellan gum which forms elastic gels having low brittleness, and a process for its preparation.
    Type: Grant
    Filed: July 9, 1991
    Date of Patent: March 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Helena C. Chang, Joseph M. Kobzeff
  • Antagonists of immunosuppressive macrolides
    Patent number: 5190950
    Abstract: A method for the modification of treatment of an immuno regulatory disorder or disease with an FK-506-type immunosuppressive macrolide comprising the administration to a mammalian species in need of such modification of an effective amount of a compound of the formula I.
    Type: Grant
    Filed: September 26, 1991
    Date of Patent: March 2, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Thomas R. Beattie, Matthew J. Wyvratt, Francis J. Dumont
  • Chiral boron catalysts for reduction of ketones and process for their preparation
    Patent number: 5189177
    Abstract: The chiral catalyst of general structure 1, or its enantiomer ##STR1## is prepared by treating the corresponding N-carboxy anhydride of structure 2 ##STR2## with an aryl metal, especially a phenyl metal such as an aryl magnesium halide, aryl lithium, aryl zinc or aryl cesium, to form a 1,1-diaryl- methanol of structure 3 ##STR3## followed by treatment with a compound of structure, 4 ##STR4## The catalyst, wherein R is aromatic, is novel and in some cases superior to the catalyst wherein R is alkyl or aralkyl in directing the chirality of diborane, borane-dimethyl sulfide or borane-tetrahydrofuran reductions of ketones to secondary alcohols.
    Type: Grant
    Filed: July 15, 1991
    Date of Patent: February 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Thomas J. Blacklock, Todd K. Jones, David J. Mathre, Lyndon C. Xavier
  • Fluoromacrolides having immunosuppressive activity
    Patent number: 5189042
    Abstract: Fluoromacrolides and derivatives of the general structural Formula I: ##STR1## have been prepared from suitable precursors by oxidation and fluorination at C-20. These macrolide immunosuppressants are useful in a mammalian host for the treatment of autoimmune diseases, infectious diseases and/or the prevention of rejection of foreign organ transplants. In addition, these macrolide immunosuppressants are useful in the topical treatment of inflammatory and hyperproliferative skin diseases and cutaneous manifestations of immunologically-mediated illnesses. Also, these macrolides are useful in the treatment of reversible obstructive airways disease, particularly asthma. Furthermore, these macrolides are useful as hair revitalizing agents, especially in the treatment of male pattern alopecia or alopecia senilis.
    Type: Grant
    Filed: August 22, 1991
    Date of Patent: February 23, 1993
    Assignee: Merck & Co. Inc.
    Inventors: Mark Goulet, Thomas R. Beattie, Matthew J. Wyvratt
  • 8a-AZA-8a-homoerythromycin cyclic iminoethers
    Patent number: 5189159
    Abstract: Cyclic iminoethers of the general structural formula wherein one of the R groups is hydrogen and the other R group represents a bond between the oxygen atom at C-6 or C-12 and the imino carbon at C-9; ##STR1## These compounds are macrolides useful as antibiotics and as intermediates for the synthesis of other macrolide antibiotics.
    Type: Grant
    Filed: April 2, 1992
    Date of Patent: February 23, 1993
    Assignee: Merck & Co., Inc.
    Inventor: Robert R. Wilkening
  • Process for the glycosylation of avermectin agylcones
    Patent number: 5188944
    Abstract: Avermectin aglycones are glycosylated by fermentation in a medium of a non-producing mutant of Streptomyces avermitilis MA-6078. The glycosylation produces the monosaccharide and disaccharide derivatives while leaving the remainder of the molecule intact. The microorganism glycosylates with the .alpha.-L-oleandrose moiety.
    Type: Grant
    Filed: September 19, 1991
    Date of Patent: February 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Mary N. Omstead, Marvin D. Schulman, Noel M. Young
  • Antistasin derived anticoagulant protein
    Patent number: 5189019
    Abstract: A protein having a molecular weight of about 6,000 daltons which is biologically active in the inhibition of Factor Xa during the blood coagulation cascade, a method for producing the protein, methods for inhibiting blood coagulation using the protein, and suitable pharmaceutical compositions.
    Type: Grant
    Filed: April 23, 1990
    Date of Patent: February 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Linda O. Palladino, Melvin Silberklang, Jwu-Sheng Tung, Simon W. Law, George E. Mark
  • Methods for thrombolytic therapy
    Patent number: 5188830
    Abstract: Certain Factor XIIIa inhibitor compounds have been discovered which have been found to be useful in the lysis of blood clots and thus adaptable for administration in thrombolytic therapy either alone or together with plasminogen activator.
    Type: Grant
    Filed: April 2, 1990
    Date of Patent: February 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Joseph G. Atkinson, David A. Claremon, John J. Baldwin, Paul A. Friedman, David C. Remy, Andrew M. Stern
  • Method of preparing HIV protease inhibitors
    Patent number: 5188950
    Abstract: Novel dipeptide isosteres are the biotransformed products after incubation with rat liver slices. They inhibit HIV protease, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts (when appropriate), pharmaceutical composition ingredients, whether or not in combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: February 27, 1992
    Date of Patent: February 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Suresh K. Balani, Harri G. Ramjit, Steven M. Pitzenberger, Michael S. Schwartz, Anthony Y. H. Lu
  • Fermentation analogs of Virginiamycin M.sub.1 to treat panic and anxiety disorder
    Patent number: 5189050
    Abstract: Pharmaceutical compositions containing Virginiamycin M.sub.1 having the Formula: ##STR1## and Virginiamycin M.sub.1 analogs having the Formulae I-IV: ##STR2## are disclosed which are useful in the treatment of panic disorder or anxiety disorder.
    Type: Grant
    Filed: June 3, 1991
    Date of Patent: February 23, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Roger M. Freidinger, Mark G. Bock, Yiu-Kuen T. Lam, Raymond S. Chang, Otto D. Hensens, Cheryl D. Schwartz, Deborah L. Zink
  • Trialkylsilyl trifluoromethanesulfonate mediated .alpha.-methylenic carbon functionalization of 4-aza-5.alpha.-androstan-3-one steroids
    Patent number: 5187278
    Abstract: A novel single-pot trialkylsilyl trifluoromethanesulfonate (R.sub.3 Si-OTf) mediated process produces derivatives of 4-aza 3-keto steroids at the .alpha.-methylenic carbon through electrophilic substitution. These derivatives are useful in the preparation, through elimination of the substituent on the .alpha.-methylene carbon, of .DELTA.-1 olefin 4-aza 3-keto steroids which are potent inhibitors of 5-.alpha. reductase.
    Type: Grant
    Filed: November 1, 1991
    Date of Patent: February 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Anthony O. King, Kevin Anderson, Sandor Karady, Alan W. Douglas, Newton L. Abramson, Richard F. Shuman
  • Angiotensin II antagonists incorporating a substituted 1,3-benzodioxole or 1,3-benzodithiole
    Patent number: 5187159
    Abstract: 1,3-Benzodioxoles and 1,3-benzodithioles substituted with a 6-fused imidazole of Formula I which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: October 7, 1991
    Date of Patent: February 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: William J. Greenlee, Ralph A. Rivero
  • Method of hydroxylation with ATCC 55086
    Patent number: 5187074
    Abstract: A novel dipeptide isostere is the biotransformed product after incubation with a culture of Streptomyces. It inhibits HIV protease, and is useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as a compound, pharmaceutically acceptable salt, pharmaceutical composition ingredient, whether or not as a prodrug or as a combination with other antivirals, anti-infectives, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: February 20, 1992
    Date of Patent: February 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Laszlo R. Treiber, Russell B. Lingham, Byron H. Arison, Lawrence F. Colwell, Jr., Georgette Dezeny, Nancy E. Kohl
  • Angiotensin II antagonists incorporating a substituted imidazo [1,2-b][1,2,4]triazole
    Patent number: 5187179
    Abstract: There are disclosed substituted imidazo[1,2-b][1,2,4]triazole derivatives of Formula I which are useful as angiotensin II antagonists.
    Type: Grant
    Filed: March 22, 1991
    Date of Patent: February 16, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Wallace T. Ashton, Steven M. Hutchins, Malcolm MacCoss
  • Microbial transformation of a substituted pyridinone using actinoplanacete sp. MA 6559
    Patent number: 5185251
    Abstract: Fermentation of the microorganism Actinoplanacete sp. (MA6559), ATTC No. 53771, in the presence of the HIV reverse transcriptase inhibitor ##STR1## yields 3-[2-(benzoxazol-2-yl)ethyl]-5-(1-hydroxyethyl)-6-methyl-2(1H)-pyridinone and 3-[2-(benzoxazol-2-yl)ethyl]-5-ethyl-6-hydroxymethyl-2(1H)-pyridinone, both of which are useful in the prevention or treatment of infection by HIV and the treatment of AIDS.
    Type: Grant
    Filed: June 7, 1991
    Date of Patent: February 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: Shieh-Shung T. Chen, George Doss
  • Methods for thrombolytic therapy
    Patent number: 5185149
    Abstract: Certain Factor XIIIa inhibitor compounds have been discovered which have been found to be useful in the lysis of blood clots and thus adaptable for administration in thrombolytic therapy either alone or together with plasminogen activator.
    Type: Grant
    Filed: April 2, 1990
    Date of Patent: February 9, 1993
    Assignee: Merck & Co., Inc.
    Inventors: John J. Baldwin, Paul A. Friedman, Andrew M. Stern