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:
May 22, 1998
Date of Patent:
November 16, 1999
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:
November 16, 1999
Assignee:
Merck & Co., Ltd.
Inventors:
Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla, Robert L. Bugianesi
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:
May 22, 1998
Date of Patent:
November 9, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Mark Goulet, Thomas F. Walsh, Feroze Ujjainwalla, Matthew J. Wyvratt, Jr., Jonathan R. Young, Lin Chu
Abstract: Biotransformation products of a fermentation with Streptomyces sp., (Merck Culture Collection MA7165) ATCC No. 55946 are potent antifungal agents. These products may be useful in the treatment of diseases caused by fungal pathogens such as Candida sp. and Cryptococcus neoformans.
Type:
Grant
Filed:
March 24, 1998
Date of Patent:
October 26, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Ali Shafiee, Guy H. Harris, Deborah L. Zink, Janet M. Sigmund, Mark J. Rosenbach, Suzanne Miller Mandala
Abstract: The invention is a pharmaceutical composition for intravenous administration to a patient comprisinga) a pharmaceutically effective amount of a compound having the formula ##STR1## and the pharmaceutically acceptable salts thereof; b) a pharmaceutically acceptable amount of an excipient such as a bulking agent effective to form a lyophilized cake; andc) a pharmaceutically acceptable amount of acetate buffer effective to provide a pH of between about 4 and 7.
Type:
Grant
Filed:
March 28, 1997
Date of Patent:
September 14, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Maneesh J. Nerurkar, William A. Hunke, Michael J. Kaufman
Abstract: There are disclosed novel antifungal macrolides of the formula ##STR1## compositions containing said compounds, methods of using said compounds and a method for synthesizing the compounds.
Abstract: A filter tube for a reaction or other fluid vessel is disclosed which maintains the vessel under an inert gas atmosphere and maintains the integrity of the inert gas seal while performing filtered or unfiltered filling or filtered draining operations.
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: 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: 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: 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
Abstract: An access port for a reaction or other fluid vessel which maintains the vessel under an inert gas atmosphere and maintains the integrity of the inert gas seal while performing filtered filling or draining operations is presented. The port uses a deflected septum sealing technique. The invention can be used for a number of laboratory and clinical operations on a variety of size and shape vessels. The combination of the appropriate vessel with this access port is very well suited for use in lab automation systems, such as automated solid phase chemical synthesis, biological screening, combinatorial chemistry and other areas where reaction chemistry is conducted.
Type:
Grant
Filed:
June 18, 1997
Date of Patent:
March 16, 1999
Assignee:
Merck & Co., Ltd.
Inventors:
Gary S. Kath, Lihu Yang, Gregory W. King
Abstract: There is disclosed a procedure for DNA-mediated transformation of Saccharomyces cerevisiae by electroporation utilizing lithium acetate and dithiothreitol to weaken cell wall structure resulting in increased transformation efficiency.
Abstract: Novel amino acid conjugates of cyclohexa-peptidyl amines having the formula ##STR1## and having antifungal and antiparasital properties are described. The compounds exhibit less acute toxicity than the free amines.
Abstract: Compounds represented by formula I: ##STR1## are disclosed. .sup.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:
June 9, 1997
Date of Patent:
January 12, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Nigel J. Liverton, David A. Claremon, John W. Butcher, Mark T. Bilodeau
Abstract: The present invention is directed to novel carba 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.
Abstract: A compound of the formula ##STR1## is disclosed which is useful for the treatment of fungal infections and for the treatment of infections caused by Pneumocystis carinii.
Type:
Grant
Filed:
October 23, 1996
Date of Patent:
December 29, 1998
Assignee:
Merck & Co., Inc.
Inventors:
James M. Balkovec, Frances A. Bouffard, James F. Dropinski
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:
December 5, 1996
Date of Patent:
December 15, 1998
Assignee:
Merck & Co., Inc.
Inventors:
Mark Goulet, Lin Chu, Thomas F. Walsh, Michael H. Fisher, Narindar N. Girotra, Matthew J. Wyvratt, Peter Lin, Wallace T. Ashton