Patents Represented by Attorney Roy D. Meredith
  • Patent number: 5858296
    Abstract: A method for preparing mimics of a wide variety of drugs and other biologlly active molecules using molecular imprinting techniques, and the mimics produced thereby, is disclosed. Specifically, the mimic is designed by: (i) polymerization of functional monomers around a known drug or biologically active molecule (the template) that exhibits a desired activity; (ii) removal of the template molecule; and then (iii) polymerization of a second class of monomers in the void left by the template, to provide a new organic molecule which exhibits one or more desired properties which are similar to that of the template.
    Type: Grant
    Filed: May 16, 1997
    Date of Patent: January 12, 1999
    Assignee: Yissum Research Development Co. of the Hebrew University of Jerusalem
    Inventor: Abraham Jacob Domb
  • Patent number: 5618830
    Abstract: Dioxobutanoic acids substituted with piperidine or similar N-substituted saturated cycloalkyls are found to inhibit the cap-dependent endonuclease of influenza virus. These compounds are useful in the prevention or treatment of infection by influenza virus and the treatment of influenza, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating influenza and methods of preventing or treating infection by influenza virus are also described.
    Type: Grant
    Filed: September 29, 1995
    Date of Patent: April 8, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Harold G. Selnick, John J. Baldwin, Gerald S. Ponticello, Joanne E. Tomassini
  • Patent number: 5605819
    Abstract: A process is disclosed that quantitatively bioconverts indene to (1S,2R)-indene oxide and (1S,2R)-indandiol, by the action of fungal haloperoxidase followed by various chemical step(s), e.g., adjusting the pH.
    Type: Grant
    Filed: May 19, 1995
    Date of Patent: February 25, 1997
    Assignee: Merck & Co., Inc.
    Inventors: Michel M. Chartrain, Neal C. Connors, George M. Garrity, Roger C. Olewinski, Jr., Thomas R. Verhoeven, Jinyou Zhang
  • Patent number: 5578597
    Abstract: The combination of the HIV protease inhibitor L-735,524 and one of ketoconazole or cimetidine is useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: July 21, 1995
    Date of Patent: November 26, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Reynold Spector, Paul J. Deutsch, Alan Nies
  • Patent number: 5559005
    Abstract: Important intermediates for preparing cephalosporin antibiotics, 7-amino-cephalosporanic acid (7-ACA) and 7-aminodeacetylcephalosporanic acid (7-ADAC), are prepared by a novel bioprocess in which a transformed Penicillium chrysogenum strain is cultured in the presence of an adipate feedstock to produce adipoyl-6-APA (6-amino penicillanic acid); followed by the in situ expression of the following genes with which the P. chrysogenum has been transformed:1) an expandase gene, e.g., from Cephalosporium acremonium, whose expression product converts the adipoyl-6-APA by ring expansion to adipoyl-7-ADCA;2) an hydroxylase gene whose expression product converts the 3-methyl side chain of adipoyl-7-ADCA to 3-hydroxymethyl, to give the first product, 7-aminodeacetylcephalosporanic acid (7-ADAC); and3) an acetyltransferase gene whose expression product converts the 3-hydroxymethyl side chain to the 3-acetyloxymethyl side chain of 7-ACA.
    Type: Grant
    Filed: May 27, 1994
    Date of Patent: September 24, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Michael J. Conder, Phyllis C. McAda, John A. Rambosek, Christopher D. Reeves
  • Patent number: 5527819
    Abstract: Novel indole compounds inhibit HIV reverse transcriptase, and are useful in the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, 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: June 7, 1995
    Date of Patent: June 18, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Theresa M. Williams, Terrence M. Ciccarone, Walfred S. Saari, John S. Wai, William J. Greenlee, Suresh K. Balani, Mark E. Goldman, Anthony D. Theoharides, deceased, Jacob M. Hoffman, Jr., William C. Lumma, Jr., Joel R. Huff, Clarence S. Rooney, Philip E. Sanderson
  • Patent number: 5527799
    Abstract: Compounds of formula ##STR1## where R.sup.1 and R.sup.2 are independently hydrogen or optionally-substituted C.sub.1-4 alkyl or aryl, or R.sup.1 and R.sup.2 are joined together to form a monocyclic or bicyclic ring system, are HIV protease inhibitors. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: March 21, 1995
    Date of Patent: June 18, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Joseph P. Vacca, Bruce D. Dorsey, James P. Guare, M. Katharine Holloway, Randall W. Hungate, Rhonda B. Levin
  • Patent number: 5519021
    Abstract: Certain benzoxazinones are useful in the inhibition of HIV reverse transcriptase (including its resistant varieties), the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: May 21, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Steven D. Young, Susan F. Britcher, Linda S. Payne, Lekhanh O. Tran, William C. Lumma, Jr.
  • Patent number: 5512560
    Abstract: HIV protease inhibitors containing hydroxypyrrolidine or hydroxypiperidine with one or more basic amines are disclosed.
    Type: Grant
    Filed: March 29, 1994
    Date of Patent: April 30, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Byeong M. Kim, Joseph P. Vacca
  • Patent number: 5508404
    Abstract: A process of reductive amination efficiently yields an HIV protease inhibitor.
    Type: Grant
    Filed: March 15, 1995
    Date of Patent: April 16, 1996
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Steven J. Cianciosi, Robert S. Hoerrner
  • Patent number: 5502053
    Abstract: Compounds of formula ##STR1## are HIV protease inhibitors, and are synthesized via a novel route. These compounds are useful in the prevention or treatment of infection by HIV and in the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: August 23, 1994
    Date of Patent: March 26, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Bruce D. Dorsey, Joel R. Huff, Susan F. Britcher
  • Patent number: 5502060
    Abstract: Oligopeptide analogs are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivitals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: October 25, 1994
    Date of Patent: March 26, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Wayne J. Thompson, Arun K. Ghosh, Joel R. Huff, Hee Y. Lee
  • Patent number: 5496948
    Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.
    Type: Grant
    Filed: June 21, 1995
    Date of Patent: March 5, 1996
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Kan K. Eng, Ralph P. Volante
  • Patent number: 5491238
    Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: February 13, 1996
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Ralph P. Volante, Kan K. Eng
  • Patent number: 5489710
    Abstract: A regioselective processes are disclosed for the synthesis of (1R,1S)-amino-(2S,2R)-alkanol, particularly (1R,1S)-amino-(2S,2R)-indanol.
    Type: Grant
    Filed: April 19, 1995
    Date of Patent: February 6, 1996
    Assignee: Merck & Co., Inc.
    Inventors: Thomas R. Verhoeven, F. Edward Roberts, Chris H. Senanayake, Kenneth M. Ryan
  • Patent number: 5489685
    Abstract: A process is disclosed for rapid synthesis of substituted furanyl pyridines.
    Type: Grant
    Filed: May 12, 1994
    Date of Patent: February 6, 1996
    Assignee: Merck & Co., Ltd.
    Inventors: Ioannis Houpis, Audrey Molina, Joseph E. Lynch, Hywyn R. O. Churchill, Ralph P. Volante, Paul J. Reider, Woo-Baeg Choi
  • Patent number: 5476874
    Abstract: Oligopeptide analogs containing sulfonamide, urea or carbamate linkages in the backbone are described. These compounds are useful in the inhibition of HIV protease, the prevention or treatment of infection by HIV and the treatment of AIDS, either as compounds, pharmaceutically acceptable salts, pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
    Type: Grant
    Filed: June 22, 1994
    Date of Patent: December 19, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Randall W. Hungate, Joseph P. Vacca
  • Patent number: 5475109
    Abstract: Dioxobutanoic acids substituted with piperidine or similar N-substituted saturated cycloalkyls are found to inhibit the cap-dependent endonuclease of influenza virus. These compounds are useful in the prevention or treatment of infection by influenza virus and the treatment of influenza, either as compound, pharmaceutically acceptable salts,. pharmaceutical composition ingredients, whether or not in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating influenza and methods of preventing or treating infection by influenza virus are also described.
    Type: Grant
    Filed: October 17, 1994
    Date of Patent: December 12, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Harold G. Selnick, Gerald S. Ponticello, John J. Baldwin, Joanne E. Tomassini
  • Patent number: 5463067
    Abstract: Intermediates of structural formula ##STR1## can be made by reacting glycidol or an activated derivative thereof with an amide. The process and intermediates are useful for synthesizing HIV protease inhibitor compounds.
    Type: Grant
    Filed: January 26, 1994
    Date of Patent: October 31, 1995
    Assignee: Merck & Co., Inc.
    Inventors: David Askin, Kan K. Eng, Ralph P. Volante
  • Patent number: 5457201
    Abstract: A chiral resolution process is described for the purification of a substituted chiral quinazoline, by salt formation with a resolving agent, followed by crystallization.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: October 10, 1995
    Assignee: Merck & Co., Inc.
    Inventors: Nobuyoshi Yasuda, Ann E. DeCamp, Edward J. J. Grabowski