Abstract: There is disclosed a novel compound having the formula ##STR1## which exhibits antifungal activity.
Type:
Grant
Filed:
January 10, 1995
Date of Patent:
November 11, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Gerald F. Bills, James E. Curotto, S. Dreikorn, Robert A. Giacobbe, Guy H. Harris, Suzanne Miller Mandala, Rosemary A. Thornton, Deborah L. Zink, Angeles Cabello Arroyo, Fernando Pelaez Perez, Teresa Diez Matas, Francisca Vicente Perez
Abstract: This invention relates to novel acyloxyisopropyl carbamates as bioreversible prodrug moieties for amino drugs and to methods of synthesizng these compounds.
Abstract: An improved process for the preparation of side chain derivatives of cyclohexapeptidyl lipopeptides represented by the formula ##STR1## wherein R.sup.1 is fully defined, is disclosed.
Type:
Grant
Filed:
February 20, 1996
Date of Patent:
November 4, 1997
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Frances A. Bouffard, James F. Dropinski, Akinlolu A. Adefarati, Jan S. Tkacz
Abstract: Compounds represented by the formula (Seq ID Nos. 1-6) ##STR1## wherein all substituents are fully defined, are disclosed. These compounds exhibit utilities as antibiotic and antifungal agents and for the treatment and prevention of Pneumocystis infections.
Type:
Grant
Filed:
March 12, 1996
Date of Patent:
September 16, 1997
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Frances A. Bouffard, Milton L. Hammond
Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## where X and Y are independently hydrogen, chloro, fluoro, bromo, iodo, or trifluoromethyl and n is 0, 1 or 2;R is hydrogen, fluoro, chloro, bromo, iodo, or trifluoromethyl, methyl, or methoxy; andthe racemates, mixtures of enantiomers, individual diastereomers or individual enantiomers with all isomeric forms and pharmaceutically acceptable salts, hydrates or crystal forms thereof, which are antiarrhythmic agents.
Type:
Grant
Filed:
August 17, 1995
Date of Patent:
August 19, 1997
Assignee:
Merck & Co., Inc.
Inventors:
David A. Claremon, Nigel Liverton, Harold G. Selnick
Abstract: An improved process for the preparation of side chain derivatives of cyclohexapeptidyl lipopeptides represented by the formula ##STR1## wherein R.sup.1 is fully defined, is disclosed.
Type:
Grant
Filed:
May 16, 1996
Date of Patent:
July 8, 1997
Inventors:
James M. Balkovec, Frances A. Bouffard, James F. Dropinski, Akinlolu A. Adefarati, Jan S. Tkacz
Abstract: A system and method for automatically feeding, inspecting and diverting tablets for continuous filling of tablet containers includes a tablet conveyor system which divides the tablets in a plurality of tablet streams for inspection by color, size and shape. Following the tablet inspection, each tablet passes through a tablet diverter which diverts the tablets to a recycle stream, reject stream or one of two bottle filling positions based upon instruction from the inspection. A bottle conveyor system is provided which feeds empty bottles into a bottle escapement mechanism which positions the empty bottles for filling. Filled bottles are moved from the bottle escapement mechanism to an exit conveyor. The entire system is computer controlled by various control mechanisms to enable the system to be fully operational without operator assistance.
Type:
Grant
Filed:
March 1, 1996
Date of Patent:
June 17, 1997
Assignee:
Merck & Co., Inc.
Inventors:
John R. Archer, David E. Cumpstey, Richard H. Gray, Stephen Owen
Abstract: This invention is concerned with novel compounds represented by structural formula I ##STR1## Z is C.sub.0-6 alkyl; and R.sup.1 is phenyl or mono or disubstituted phenyl, where the substitutents are Cl, and CF.sub.3,or pharmaceutically acceptable salts, hydrates and crystal forms thereof which are useful in the treatment of arrhythmia.
Type:
Grant
Filed:
June 7, 1995
Date of Patent:
May 20, 1997
Assignee:
Merck & Co., Inc.
Inventors:
John Butcher, David A. Claremon, Nigel Liverton, Harold G. Selnick
Abstract: There is disclosed a method of synthesizing a compound of the formula ##STR1## and novel analogs of the formula ##STR2## where R and R.sub.1 are fully defined. These compounds exhibit beneficial antiviral properties especially as inhibitors of the influenza virus.
Abstract: There are disclosed novel compounds having the formula ##STR1## which exhibit antifungal activity.
Type:
Grant
Filed:
May 9, 1995
Date of Patent:
January 28, 1997
Assignee:
Merck & Co., Inc.
Inventors:
Wendy H. Clapp, Guy H. Harris, Gerald F. Bills, James E. Curotto, Anne W. Dombrowski, Sarah J. Driekorn, Myra B. Kurtz, Maria S. Meinz, Janet C. Onishi, Jon D. Polishook, Stanley L. Streicher, John R. Thompson, Marie Williams, Deborah L. Zink
Abstract: There are disclosed novel compounds having the formula ##STR1## which exhibit antifungal activity.
Type:
Grant
Filed:
March 9, 1995
Date of Patent:
August 6, 1996
Assignee:
Merck & Co., Inc.
Inventors:
Gerald F. Bills, James E. Curotto, Sarah J. Dreikorn, Rosalind G. Jenkins, Jerrold M. Liesch, Sandra A. Morris, John R. Thompson, Deborah L. Zink, Richard K. Jansson, Angela Basilio, Teresa Diez, Fernando Pelaez, Francisca Vicente
Abstract: Compounds represented by the formula I (SEQ ID NO. 1) are disclosed: ##STR1## as well as pharmaceutically acceptable salts and hydrates thereof. R.sup.I represents C.sub.9 to C.sub.19 alkyl, C.sub.9 to C.sub.19 alkenyl, an aryl group which includes phenyl, biphenyl, naphthyl and terphenyl or a C.sub.1 to C.sub.12 alkyl, alkylamino, dialkylamino or alkoxyaryl group.R.sup.1, R.sup.2 and R.sup.4 independently represent H or --OH.R.sup.3 represents H, --OH, --O(CH.sub.2).sub.n NR.sup.V R.sup.VI, where R.sup.V and R.sup.VI independently represent H or C.sub.1-4 alkyl, or --O(CH.sub.2).sub.n NR.sup.V R.sup.VI R.sup.VII+ Y.sup.-, wherein R.sup.V and R.sup.VI are as defined above, R.sup.VII represents H or C.sub.1-4 alkyl, n is an integer of from 2-6 inclusive, and Y represents a counterion.R.sup.5 represents H, --CH.sub.3 or --OH;R.sup.6 represents H or --CH.sub.3 ;R.sup.7 represents H, --CH.sub.3, --CH.sub.2 C(.dbd.O)NH.sub.2, --(CH.sub.2).sub.2 NR.sup.V R.sup.VI or --(CH.sub.2).sub.2 NR.sup.V R.sup.VI R.sup.
Type:
Grant
Filed:
April 4, 1994
Date of Patent:
July 30, 1996
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Frances A. Bouffard, Regina M. Black
Abstract: An improved gripping and pinching device particularly useful with laboratory glassware and adaptable for use with a robot or automated system, is disclosed. The device uses flexible tubing as a gripper, eyedropper pincher and as a pinch valve which biases and releases test tubes, vials or the like upon removal and application of a vacuum or pressurizing means.
Type:
Grant
Filed:
August 1, 1994
Date of Patent:
July 16, 1996
Assignee:
Merck & Co., Inc.
Inventors:
Glenn Clarke, Gary S. Kath, Gregory W. King
Abstract: There is disclosed a method for maximizing the health of the optic nerve by application of topical .beta.-blockers to the eye. Maintaining or increasing retinal nerve fiber thickness has been found to have a link to the prevention of visual field loss and blindness.
Abstract: The present invention is directed to novel aza cyclohexapeptide compounds of the formula ##STR1## where all substituents are defined herein, which are useful as antifungal agents and for the treatment of Pneumocystis carinii infections. Compositions containing the compounds of the invention are also disclosed.
Type:
Grant
Filed:
October 31, 1994
Date of Patent:
May 14, 1996
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Frances A. Bouffard, James F. Dropinski
Abstract: There are disclosed novel semi-synthetic lipopeptides of the formula (Seq. ID Nos. 1-6) ##STR1## wherein the substituents are defined herein, which show utility as antifungal and anti-Pneumocystis agents. Pharmaceutical compositions containing said compounds are also disclosed.
Abstract: The present invention relates to aza cyclohexapeptide compounds of the formula (Seq ID Nos. 1-10) ##STR1## which may be useful as antibiotics, antifungal agents and for the treatment of Pneumocystis carinii infections.
Type:
Grant
Filed:
September 16, 1994
Date of Patent:
May 7, 1996
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Frances A. Bouffard, James F. Dropinski
Abstract: Ceretain aza cyclohexapeptide compounds have been found to have superior antibiotic properties. Novel processes for their preparation are also described.
Type:
Grant
Filed:
August 29, 1994
Date of Patent:
May 7, 1996
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Regina M. Black, Frances A. Bouffard
Abstract: A compound having the formula ##STR1## which is useful as an antifungal agent and for the treatment and control of several agricultural phytopathogens, including Phytophthora infestans, is disclosed.
Type:
Grant
Filed:
August 12, 1994
Date of Patent:
August 15, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Guy H. Harris, James E. Curotto, Robert A. Giacobbe, Suzanne M. Mandala, Richard L. Monaghan, Richard K. Jansson, Joan A. Lasota