Abstract: Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of proteins tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.
Type:
Grant
Filed:
June 26, 2000
Date of Patent:
December 11, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Joung L. Goulet, Mark A. Holmes, Julianne A. Hunt, Sander G. Mills, William H. Parsons, Peter J. Sinclair, Dennis M. Zaller
Abstract: Pyrimidine compounds (Formula I), or their pharmaceutically acceptable salts, hydrates, solvates, crystal forms and individual diastereomers, and pharmaceutical compositions including the same, which are inhibitors of tyrosine kinase enzymes, and as such are useful in the prophylaxis and treatment of protein tyrosine kinase-associated disorders, such as immune diseases, hyperproliferative disorders and other diseases in which inappropriate protein kinase action is believed to play a role, such as cancer, angiogensis, atheroscelerosis, graft rejection, rheumatoid arthritis and psoriasis.
Type:
Grant
Filed:
June 26, 2000
Date of Patent:
November 13, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Julianne A. Hunt, Sander G. Mills, Peter J. Sinclair, Dennis M. Zaller
Abstract: Combinations of a &bgr;-adrenergic antagonist and a topical carbonic anhydrase inhibitor are particularly useful in the treatment of ocular hypertension, especially in patients insufficiently responsive to treatment with &bgr;-adrenergic antagonists.
Abstract: The present invention is directed to compounds which inhibit prenyl-protein transferase and particularly, 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 compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Type:
Grant
Filed:
February 20, 2001
Date of Patent:
November 6, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, George D. Hartman, Randall W. Hartman
Abstract: The present invention relates to carbapenem antibacterial agents in which the carbapenem nucleus is substituted at the 2 -position with a iodophenoxy linked through a group —Z—CH2—; The compound is further substituted with various substituent groups including at least one cationic group.
The compounds are represented by formula I:
wherein Z represents trans-ethenediyl or ethynediyl.
Pharmaceutical compositions and methods of use are also included.
Abstract: The present invention relates to compounds which inhibit, regulate and/or modulate tyrosine kinase signal transduction, compositions which contain these compounds, and methods of using them to treat tyrosine kinase-dependent diseases and conditions, such as angiogenesis, cancer, tumor growth, atherosclerosis, age related macular degeneration, diabetic retinopathy, inflammatory diseases, and the like in mammals.
Type:
Grant
Filed:
October 17, 2000
Date of Patent:
October 23, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Mark E. Fraley, Kenneth L. Arrington, Mark T. Bilodeau, George D. Hartman, William F. Hoffman, Yuntae Kim, Randall W. Hungate
Abstract: The present invention relates to a class of heterocyclic compounds of Formula I that are useful as potassium channel inhibitors to treat autoimmune disorders, cardiac arrhythmias, and the like.
Type:
Grant
Filed:
October 21, 1999
Date of Patent:
October 16, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Jianming Bao, Andrew Kotliar, Frank Kayser, William H. Parsons, Kathleen M. Rupprecht, Christopher F. Claiborne, David A. Claremon, Nigel Liverton, Wayne J. Thompson
Abstract: Angiotensin II receptor antagonists are useful for decreasing QT dispersion or inhibiting the progression of QT prolongation in patients. Also disclosed is a method for monitoring the reduction in die risk of experiencing an adverse cardiac event, such as sudden cardiac death, myocardial infarction or arrhythmias, using QT dispersion in patients treated with a therapeutically effective amount of an angiotensin II antagonist.
Type:
Grant
Filed:
August 10, 2000
Date of Patent:
October 9, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Robert Segal, Paul J. Robinson, Lawrence I. Deckelbaum
Abstract: The present invention relates to a novel stabilized form of carbapenem antibiotics of formula II:
compositions and methods thereof wherein the antibiotics and compositions are stabilized degradation and dimer formation. The compounds can be used in the treatment of infectious diseases, including gram positive and negative, aerobic and anaerobic bacteria. The compounds provide good stability against beta-lactamases, and a favorable duration of action.
The compounds of this invention are represented structural formula I:
or a pharmaceutically acceptable or hydrate thereof.
Type:
Grant
Filed:
April 6, 1999
Date of Patent:
October 2, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Orn Almarsson, Michael J. Kaufman, John D. Stong, John M. Williams
Abstract: The present invention is directed to compounds which inhibit a prenyl-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 a prenyl-protein transferase and the prenylation of the oncogene protein Ras.
Type:
Grant
Filed:
October 6, 1998
Date of Patent:
October 2, 2001
Assignee:
Merck & Co., Inc.
Inventors:
S. Jane deSolms, John H. Hutchinson, Anthony W. Shaw, Samuel L. Graham, Terrence M. Ciccarone
Abstract: Compounds of formula I:
as well as pharmaceutically acceptable salts therefor and compositions useful as carbapenem antibacterial agents are disclosed.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
September 25, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Timothy A. Blizzard, Robert R. Wilkening, Ronald W. Ratcliffe
Abstract: There is disclosed a method for continuously monitoring temperature at multiple locations within a controlled temperature unit (CTU) using RTDs that can be removed and reinserted. The key to the method is the collection of data using an RTD fixed in a phenolic thermowell, which in turn is inserted through a polytetrafluoroethylene-coated sleeve in the wall of the CTU. The temperature information is transmitted from a data module to an interfaced computer system where it may be presented to the operator in a graphical, tabular or text format or stored in memory. The temperature probes are easily removable so as to facilitate calibration without disruption of the contents of the CTU and can be consistently replaced in the same location within the CTU.
Type:
Grant
Filed:
October 26, 1999
Date of Patent:
September 25, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Fred J. Bailey, Mark Pinder, Carl W. Holz
Abstract: Compounds of formula I:
as well as pharmaceutically acceptable salts thereof useful as carbapenam antibacterial agents are disclosed wherein X is CR2R2, NR2, or O.
Type:
Grant
Filed:
June 23, 1999
Date of Patent:
September 18, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Timothy A. Blizzard, Robert R. Wilkening, Ronald W. Ratcliffe
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: 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.
Type:
Grant
Filed:
May 24, 1999
Date of Patent:
September 11, 2001
Assignee:
Merck & Co., Inc.
Inventors:
Frank P. Dininno, Milton L. Hammond, Kevin D. Dykstra
Abstract: The present invention is directed to azepan-2-one compounds which inhibit prenyl-protein transferase, particularly farnesyl-protein transferase (Ftase), and the prenylation of the oncogene protein Ras. The invention is further directed to chemotherapeutic compositions containing the compounds of this invention and methods for inhibiting prenyl-protein transferase and the prenylation of the oncogene protein Ras.
Type:
Grant
Filed:
December 7, 1999
Date of Patent:
September 4, 2001
Assignee:
Merck & Co., Inc.
Inventors:
S. Jane deSolms, Samuel L. Graham, Anthony W. Shaw, Terrence M. Ciccarone, Gerald E. Stokker
Abstract: The present invention relates to tricyclic carbapenem antibacterial agents wherein X is CH2, CHRa, CHRb, C═CHRa, C═CHRb, O, S, SO, SO2, CO, COO<OCO, NRa, NRb; and Z is trans-ethenediyl or ethynediyl. 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.