Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Type:
Grant
Filed:
October 13, 1998
Date of Patent:
August 15, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Jeffrey M. Bergman, Christopher J. Dinsmore, Samuel L. Graham
Abstract: A method for enhancing the mixing of materials in a roller bottle by the introduction of controlled axial and cross-sectional flow perturbations is disclosed. The effectiveness of the method is demonstrated by achieving higher efficiency in cell culturing and virus propagation in roller bottles by introducing controlled flow perturbations during the process.
Type:
Grant
Filed:
October 26, 1998
Date of Patent:
August 1, 2000
Assignees:
Merck & Co., Inc., Rutgers, The State University of New Jersey
Inventors:
Joye L. Bramble, Fernando J. Muzzio, James A. Searles
Abstract: The present invention relates to a process for treating contaminated water to precipitate metals without increasing the total dissolved solids content. In particular, the invention relates to the use of phosphoric acid and calcium hydroxide or calcium oxide to adjust the pH of chromium contaminated groundwater during the treatment process without increasing the total dissolved solids (TDS).
Type:
Grant
Filed:
October 5, 1998
Date of Patent:
August 1, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Youssef El-Shoubary, Subash C. Seth, Ned A. Speizer
Abstract: Inhibition of protein elongation factor 2 provides a target for identifying potential antifungal and antiparasitic compounds. EF2 inhibitors are useful as therapeutic agents against fungal and parasitic infections.
Type:
Grant
Filed:
June 2, 1998
Date of Patent:
August 1, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Jennifer Nielsen-Kahn, Michael C. Justice, Dennis M. Schmatz, Ming-Jo Hsu, Theresa W. Ku
Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Type:
Grant
Filed:
December 23, 1997
Date of Patent:
July 25, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Robert P. Gomez, Lekhanh O. Tran, Steven D. Young
Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods of inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Type:
Grant
Filed:
July 27, 1998
Date of Patent:
July 18, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J. Dinsmore, George D. Hartman
Abstract: Compounds represented by formula I: ##STR1## are disclosed. AR represents an aromatic group containing 6-10 atoms; and ##STR2## represents a 4 to 10 membered non-aromatic heterocycle containing at least one N atom, and optionally containing 1-2 additional N atoms and 0-1 O or S atom.A pharmaceutical composition is also included.Methods of treating cancer and cytokine mediated diseases are also included.
Type:
Grant
Filed:
January 26, 1998
Date of Patent:
July 4, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Nigel J. Liverton, Christopher F. Claiborne, David A. Claremon, Harold G. Selnick
Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Type:
Grant
Filed:
October 1, 1998
Date of Patent:
June 27, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Robert P. Gomez, Gerald E. Stokker, John S. Wai, Theresa M. Williams, Wasyl Halczenko, John H. Hutchinson, Steven D. Young, Kelly M. Solinsky
Abstract: A process of synthesizing a compound of formula I is described: ##STR1## wherein P and P' independently represent H or a protecting group, R.sub.1 represents H or C.sub.1-4 alkyl, and Hal represents a halogen characterized by reacting a compound of formula 2: ##STR2## with R.sub.2 OH, wherein R.sub.2 is C.sub.1-4 alkyl, C.sub.6-10 aryl or C.sub.5-10 heteroaryl in the presence of an acid catalyst or carbodiimide reagent to produce a compound of formula 3: ##STR3## and reacting a compound of formula 3 in the presence of a base and a haloalkylating agent to produce a compound of formula 1.
Type:
Grant
Filed:
July 27, 1998
Date of Patent:
June 27, 2000
Assignee:
Merck & Co., Inc.
Inventors:
John Y. Chung, Nobuyoshi Yasuda, Johnnie L. Leazer, Jr.
Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
Type:
Grant
Filed:
September 21, 1999
Date of Patent:
June 20, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Mark Goulet, Feroze Ujjainwalla, Thomas F. Walsh, Matthew J. Wyvratt, Jr., Jonathan R. Young, Lin Chu
Abstract: There are disclosed compounds of formula (I) ##STR1## and pharmaceutically acceptable salts thereof which are useful as antagonists of GnRH and as such may be useful for the treatment of a variety of sex-hormone related and other conditions in both men and women.
Type:
Grant
Filed:
March 25, 1999
Date of Patent:
June 20, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla
Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Abstract: The present invention relates to a package for storing, mixing, resuspending and dispensing sterile or non-sterile solutions or suspensions and comprises a sterilizable bag having fittings which provide for the introduction and exit of fluids and solids, as well as means for resuspending and stirring the fluids. Additionally, structural support means are provided for shipment, filling and dispensing. Unlike conventional stainless steel equipment, the system is disposable, does not require cleaning, provides for safe, rapid and accurate resuspension of suspended solids and can accommodate a wide range of liquid volumes.
Type:
Grant
Filed:
June 11, 1997
Date of Patent:
June 6, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Anand Ekambaram, Wendy L. Radcliff, Mark S. Rienstra, Brett L. Allred, Doyle W. Stewart
Abstract: A sterile transfer system between a bag and a enclosure suitable for use in the pharmaceutical industry, characterized on the one hand of a first part of a bag having a mouth in the form of a pocket, in which the bottom is constituted by a flexible partition separating the interior spaces of the pocket and the bag and capable of being heat-cut, on the other hand a lock chamber installed at the entrance to the sterile enclosure which includes a fixed part on which the pocket can be mounted, this part presenting a central opening receiving a mobile element constituting the door of the lock chamber, the fixed and mobile parts each being equipped with a heatable blade with closed outline overlapping and joined at their apex in airtight manner when the bag is in the closed state, vacuum outlets being provided for applying the flexible partition by means of suction against the heatable blades and effecting the cutting of it by fusion of the zones which come into contact with the blades.
Abstract: There is described antifungal combination therapy comprising the use of known antifungal agents such as the azoles or polyenes in combination with a pneumocandin derivative antifungal agent. More particularly, the invention relates to antifungal combination therapy comprising the use of azoles such as fluconazole, voriconazole, itraconazole, ketoconazole, miconazole, ER 30346, SCH 56592; polyenes such as amphotericin B, nystatin or liposomal and lipid forms thereof such as Abelcet, AmBisome and Amphocil; purine or pyrimidine nucleotide inhibitors such as flucytosine; or polyoxins such as nikkomycins, in particular nikkomycin Z or other chitin inhibitors, elongation factor inhibitors such as sordarin and analogs thereof, mannan inhibitors such as predamycin, bactericidal/permeability-inducing (BPI) protein products such as XMP.97 or XMP.127 or complex carbohydrate antifungal agents such as CAN-296 in combination with a pneumocandin derivative as described herein.
Type:
Grant
Filed:
February 24, 1999
Date of Patent:
May 30, 2000
Assignee:
Merck & Co., Inc.
Inventors:
George K. Abruzzo, Kenneth F. Bartizal, Amy M. Flattery
Abstract: The present invention relates to a process for synthesizing novel intermediates of formula III: ##STR1## wherein R.sup.1 is a halogen. The intermediate compounds described herein are useful for the preparation of carbapenem compounds.
Type:
Grant
Filed:
August 19, 1999
Date of Patent:
May 30, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Mark S. Jensen, Chunhua Yang, Nobuyoshi Yasuda, David A. Colon, Yi Xiao
Abstract: The present invention is directed to compounds which inhibit farnesyl -protein transferase (FTase) and the farnesylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting farnesyl-protein transferase and the farnesylation of the oncogene protein Ras.
Type:
Grant
Filed:
July 27, 1998
Date of Patent:
May 23, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J. Dinsmore, George D. Hartman