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
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
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
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
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
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
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
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.
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
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
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
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
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.
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
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
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