Abstract: The present invention relates to compounds which inhibit tyrosine kinase enzymes, compositions which contain tyrosine kinase inhibiting compounds and methods of using tyrosine kinase inhibitors to treat tyrosine kinase-dependent diseases and conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
Type:
Grant
Filed:
June 29, 1999
Date of Patent:
May 8, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, Randall W. Hungate, William F. Hoffman, William R. Huckle, Richard L. Kendall, Kenneth A. Thomas, Jr.
Abstract: 11-hydroxysordarin, biotransformation product of a fermentation with sordarin and Actinomyces spp., (Merck Culture Collection MA7235) ATCC No. 202103 is an antifungal agent. This compound may be useful in the treatment of diseases caused by fungal pathogens such as Candida albicans.
Type:
Grant
Filed:
October 26, 1999
Date of Patent:
May 8, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Michael G. Sturr, Michel M. Chartrain, Guy H. Harris, Jennifer Nielsen-Kahn, Brian Heimbuch
Abstract: There are disclosed compounds of formula (I)
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:
May 8, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Thomas F. Walsh, Mark T. Goulet, Feroze Ujjainwalla
Abstract: A device to separate rubber stoppers that have adhered together, typically as a result of sterilization. The device contains a hopper, a pair of rollers and a mechanism to turn the rollers. The rollers are hexagonal-shaped and each face has a scalloped concavity. The adhering stoppers are gravity-fed into the rollers from the hopper, where they are compressed and a shearing force is applied to separate the adherent stoppers. The separated stoppers are then collected for further processing.
Abstract: The present invention relates to novel 2-(naphthosultamyl)methyl-carbapenem antibacterial agents or pharmaceutically acceptable salts thereof in combination with other &bgr;-lactams, which are useful in treating and preventing enterococcal infections. The combinations have anti-PBP5 activity as well as activity against the critical PBPs of sensitive isolates. The antibacterial compositions of the present invention thus comprise an important contribution to therapy for treating infections caused by these difficult to control pathogens.
This combination is also useful against gram positive microorganisms, especially methicillin resistant Staphylococcus aureus (MRSA), methicillin resistant Staphylococcus epidermidis (MRSE), and methicillin resistant coagulase negative Staphylococci (MRCNS).
Type:
Grant
Filed:
August 27, 1999
Date of Patent:
April 24, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Karen L. Dorso, Jesse J. Jackson, Charles J. Gill, Joyce Kohler, Lynn L. Silver
Abstract: This application discloses a method of treating or preventing atrial arrhythmias which utilizes compounds which are blockers of the ultra-rapidly-activating delayed rectifier K+ current (IKur) of the human atrium in a use-dependent and/or rate dependent manner, and which provide the selective block preferentially at fast heart rates so that the effect is realized or maximized when required.
Type:
Grant
Filed:
April 19, 1999
Date of Patent:
April 10, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Bernard Fermini, Joseph J. Lynch, Jr., Joseph J. Salata, Richard J. Swanson
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+ current (IKur) of the human atrium.
Type:
Grant
Filed:
April 19, 1999
Date of Patent:
April 10, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Bernard Fermini, Joseph J. Lynch, Jr., Joseph J. Salata, Richard J. Swanson
Abstract: There are disclosed compounds of formula (I)
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:
October 26, 1998
Date of Patent:
April 3, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Lin Chu, Mark Goulet, Thomas F. Walsh, Matthew J. Wyvratt, Stephanie L. Witkin
Abstract: There are disclosed compounds of formula (I)
and pharmaceutically acceptable salts thereof which may be useful for the treatment of cytokine mediated diseases such as arthritis.
Type:
Grant
Filed:
July 21, 1999
Date of Patent:
March 27, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Christopher F. Claiborne, Nigel J. Liverton, David A. Claremon
Abstract: The present invention relates to tricyclic carbapenem antibacterial agents in which the carbapenem nucleus is fused to a 6 membered carbocyclic ring. The compound is further substituted with various substituent groups including at least one cationic group.
The compounds are represented by formula I:
Pharmaceutical compositions and methods of use are also included.
Abstract: We have modified PE40 toxin by removing at least two of its four cysteine amino acid residues and have formed hybrid molecules containing modified PE40 linked to a cell recognition protein that can be an antibody, a growth factor, a hormone, a lymphokine, or another polypeptide cell recognition protein for which a specific cellular receptor exists whereby the modified PE40 toxin is directed to cell types having receptors for the cell recognition protein linked to the modified PE40.
Type:
Grant
Filed:
February 10, 1997
Date of Patent:
March 27, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Allen I. Oliff, Gwynneth M. Edwards, Deborah D. Jones
Abstract: The present invention relates to a process for making propargylic alcohols by zinc-mediated catalytic, asymmetric addition of acetylenes to aldehydes.
Abstract: There are disclosed compounds of formula (I)
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:
July 14, 1998
Date of Patent:
March 13, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Mark Goulet, Wallace T. Ashton, Lin Chu, Michael H. Fisher, Peter Lin, Mitree M. Ponpipom, Matthew J. Wyvratt, Narindar N. Girotra, Jonathan Young
Abstract: Angiotensin II receptor antagonists are useful in reducing and preventing mortality and sudden cardiac death in symptomatic heart failure patients. Losartan potassium has been shown to reduce mortality and sudden cardiac death in this patient population. Additionally, losartan potassium has been shown to reduce the need for hospitalization of symptomatic heart failure patients.
Type:
Grant
Filed:
January 6, 1998
Date of Patent:
March 13, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Polly A. Beere, Paul I. Chang, Bertram Pitt, Eva J. Rucinska, Robert Segal, Divakar Sharma, Duane B. Snavely
Abstract: There are disclosed compounds of formula (I) 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:
June 1, 1998
Date of Patent:
March 6, 2001
Assignee:
Merck & Co. , Inc.
Inventors:
Mark Goulet, Wallace T. Ashton, Lin Chu, Michael H. Fisher, Matthew J. Wyvratt
Abstract: This invention relates to benzamide potassium channel inhibitors of general structural Formula I.
The compounds of this invention are useful in the treatment of autoimmune diseases, the prevention of rejection of foreign organ transplants and related afflictions, diseases and illnesses, and cardiac arrhythmias. Also within the scope of this invention are pharmaceutical formulations comprising a compound of Formula I and a pharmaceutical carrier, as well as pharmaceutical formulations comprising a compound of Formula I, one or more immunosuppressive compounds and a pharmaceutical carrier.
Type:
Grant
Filed:
October 21, 1999
Date of Patent:
February 27, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Robert K. Baker, Jianming Bao, Frank Kayser, Andrew Kotliar, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
Abstract: The invention describes an improved process for synthesizing 1-&bgr;-methyl-2-hydroxymethyl substituted carbapenems as key intermediates for the synthesis of anti-MRSA carbapenem antibiotics. The synthesis eliminates the use of BU3SnCH2OH and HMPA, which are toxic substances and not amenable to industrial scale production. The novel intermediates are also within the scope of this invention.
The invention relates to the synthesis of a compound of formula 3:
wherein R1 represents H or a suitable protecting group for an alcohol; R2 represents H or methyl; and R5 represents a carboxy protecting group as well as the compounds made therein.
Type:
Grant
Filed:
June 4, 1999
Date of Patent:
February 27, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Mark S. Jensen, Yi Xiao, Chunhua Yang, Kenneth M. Wells, Nobuyoshi Yasuda
Abstract: There are disclosed compounds of formula (I)
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.
Abstract: A stabilized carbapenem intermediate compound represented by the formula 1:
or a salt thereof is disclosed, wherein P represents a carboxyl protecting group and X represents a charge balancing group.
In addition, a process for synthesizing a compound represented by formula 2:
is disclosed wherein X+ is a charge balancing group, comprising: deprotecting a compound of the formula 1 to produce a compound 2.
Type:
Grant
Filed:
June 9, 1998
Date of Patent:
January 30, 2001
Assignee:
Merck & Co., Inc.
Inventors:
John M. Williams, Renato T. Skerlj, Karel M. J. Brands, Ulf H. Dolling, Ronald B. Jobson