Abstract: A study was done to compare the performance of a conventional V-blender to a V-blender that incorporates perturbations of the particle flow by rocking the mixing vessel during its normal rotation. Mixing was investigated using glass beads with sizes from 66.mu. to 600.mu. in vessels of approximately one liter volume. Mixture uniformity was assessed qualitatively, using two different methods. One method involved a transparent mixing vessel where it was possible to see particle flow patterns and assess the state of the mixture at its surface during the entire experiment. The second method involved disposable aluminum mixing vessels, where the mixture was solidified by infiltrating the mixture with a binder. By slicing the solidified structure, it was possible to assess the entire state of the mixture including its interior structure after the completion of each experiment. Mixture uniformity was also assessed quantitatively using image analysis of the slices.
Type:
Grant
Filed:
January 5, 1998
Date of Patent:
August 17, 1999
Assignees:
Merck & Co., Inc., Rutgers, The State University of New Jersey
Inventors:
Priscilla A. Robinson, Fernando J. Muzzio, Dean Brone, Kevin Connor, Carolyn Wightman
Abstract: Certain propanolamine compounds which have a cyclohexapeptidyl nucleus and which are found to have extremely active antibiotic activity with physical properties suitable for direct use in therapeutic compositions are described. A novel process for their preparation is also described.
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 22, 1997
Date of Patent:
August 17, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Samuel L. Graham, Lekhanh O. Tran, Ian M. Bell, S. Jane deSolms, Robert P. Gomez, Michelle Sparks Kuo, William C. Lumma, Jr., Debra S. Perlow, Anthony W. Shaw, John S. Wai, Steven D. Young
Abstract: A method of treating or preventing supraventricular tachyarrhythmias is disclosed which comprises the use of a compound which selectively blocks the ultra-rapidly-activating delayed rectifier K.sup.+ current (I.sub.Kur) of the human atrium.
Type:
Grant
Filed:
October 28, 1997
Date of Patent:
August 10, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Joseph J. Lynch, Jr., Richard J. Swanson, Joseph J. Salata, Bernard Fermini
Abstract: Protriptyline can be prepared from 5-dihydrodibenzocycloheptatriene, by deprotonation, followed by reaction at low temperatures with 1,3-bromochloropropane to give the 5-(chloropropyl)-dibenzocycloheptatriene, which is reacted with methylamine in a displacement reaction to give the protriptyline product.
Type:
Grant
Filed:
December 22, 1997
Date of Patent:
August 3, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Robert S. Hoerrner, Joseph Auerbach, John Carolan
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 invention is directed to a method useful in the treatment of preterm labor, dysmenorrhea and for the stoppage of labor preparatory to cesarean delivery.
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: A compound represented by formula I: ##STR1## is disclosed. The compounds are active primarily against gram negative organisms. Pharmaceutical compositions and methods of treatment are also disclosed.
Type:
Grant
Filed:
April 25, 1997
Date of Patent:
July 20, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Arthur A. Patchett, Ravi Nargund, Meng-Hsin Chen, H. Russell Onishi
Abstract: The present invention is directed to an improved process for preparing the phenylacetic acid side chain of the compound of the formula ##STR1## This compound exhibits utility as a Class III antiarrhythmic agent.
Type:
Grant
Filed:
August 3, 1998
Date of Patent:
July 13, 1999
Assignee:
Merck & Company, Inc.
Inventors:
Joseph E. Lynch, Yao-Jun Shi, Kenneth M. Wells
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: An efficient method for the preparation of a compound of (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl- 1,4-dihydro-2H-3, 1-benzoxazin-2-one, also known as DMP-266, a reverse transcriptase inhibitor is achieved using a cyclization reaction of the amino alcohol intermediate with an alkyl or aryl chloroformate and a base.
Type:
Grant
Filed:
February 3, 1998
Date of Patent:
July 13, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Lisa F. Frey, Richard D. Tillyer, Edward J. J. Grabowski
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:
March 25, 1997
Date of Patent:
July 6, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J. Dinsmore, Theresa M. Williams, Jeffrey Bergman
Abstract: The invention encompasses a novel process for the formation of enantiomerically enriched mixtures of compounds of Formula I, which are useful precursors in the synthesis of phosphodiestersae IV inhibitors.
Type:
Grant
Filed:
October 7, 1998
Date of Patent:
July 6, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Joseph E. Lynch, Kenneth M. Wells, Yao-Jun Shi
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:
January 29, 1998
Date of Patent:
June 22, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J. Dinsmore, George D. Hartman
Abstract: A compound having the formula ##STR1## in which R.sub.1 is an aminoalkyl group and ##STR2## is an acyl group and salts thereof having high antibiotic activity and being substantially free of lytic activity are described.
Type:
Grant
Filed:
January 15, 1993
Date of Patent:
June 22, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Frances Aileen Bouffard, James F. Dropinski
Abstract: A method is presented for isomerizing the E-isomer of 9-Deoxo-9-hydroximinoerythromycin A to its corresponding Z-isomer. The Z-isomer is useful as an antibiotic and as an intermediate for the synthesis of other macrolide antibiotics.
Abstract: Psuedomonas exotoxin 40 is modified by deleting or substituting one or more cysteine residues. Such a modified protein may be incorporated into a fusion protein with TGF.alpha.. The resulting fusion protein exhibits altered biological activities from unmodified TGF.alpha.-PE.sub.40, including decreased cell killing activity and increase receptor-binding activity.
Abstract: There is disclosed a procedure for DNA-mediated transformation of Candida albicans by electroporation utilizing lithium acetate and dithiothreitol to weaken the cell wall structure and optimize the yield of transformants.
Type:
Grant
Filed:
September 17, 1997
Date of Patent:
June 1, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Rosemarie Kelly, Elizabeth A. Register, Myra B. Kurtz, John R. Thompson