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 present invention relates to benzinidazole 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/conditions such as angiogenenesis, cancer, atherosclerosis, diabetic retinopathy or autoimmune diseases, in mammals.
Type:
Grant
Filed:
March 11, 1999
Date of Patent:
December 19, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Mark T. Bilodeau, April M. Cunningham, Randall W. Hungate, Timothy J. Koester
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 famesylation of the oncogene protein Ras.
Type:
Grant
Filed:
October 5, 1998
Date of Patent:
October 3, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Byeong M. Kim, Anthony W. Shaw, Samuel L. Graham, S. Jane deSolms, Terrence M. Ciccarone
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:
October 1, 1998
Date of Patent:
June 27, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Robert P. Gomez, Gerald E. Stokker, John S. Wai, Theresa M. Williams, Wasyl Halczenko, John H. Hutchinson, Steven D. Young, Kelly M. Solinsky
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:
October 2, 1998
Date of Patent:
May 16, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Christopher J Dinsmore, Neville J. Anthony, Gerald E. Stokker, Robert P. Gomez
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: This invention relates to a key intermediate in the synthesis of an endothelin antagonist the synthesis of this key intermediate via an asymmetric conjugate addition reaction.
Type:
Grant
Filed:
July 14, 1998
Date of Patent:
February 8, 2000
Assignee:
Merck & Co., Inc.
Inventors:
Paul N. Devine, Richard D. Tillyer, Richard M. Heid, Jr., David M. Tschaen
Abstract: New substituted azetidinones of the general Formula (I) which have been found to be potent elastase inhibitors and thereby useful anti-inflammatory and antidegenerative agents are described, wherein n is
Type:
Grant
Filed:
December 12, 1996
Date of Patent:
September 14, 1999
Assignee:
Merck & Co., Inc.
Inventors:
James Doherty, Conrad Dorn, Philippe Durette, Paul Finke, Malcolm Maccoss, Sander Mills, Shrenik Shah, Soumya Sahoo, William Hagmann, Scott Polo
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:
August 17, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Neville J. Anthony, Robert P. Gomez, Kelly M. Solinsky
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 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: Losartan potassium is an angiotensin II antagonist useful in the treatment of hypertension and congestive heart failure. ##STR1## This invention relates to the process for the controlled crystallization of losartan potassium utilizing anti-solvent addition combined with massive seeding in order to obtain the desired crystal morphology and bulk physical properties necessary for successful formulation.
Type:
Grant
Filed:
October 28, 1997
Date of Patent:
January 12, 1999
Assignee:
Merck & Company, Inc.
Inventors:
Patrick Breen, Erik A. Dienemann, Albert D. Epstein, Karen A. Larson, Michael T. Kennedy, Hari Mahadevan
Abstract: This invention relates to a method for the stereoselective synthesis of a 2-aryloxycarboxylic acid using a chiral auxiliary to enhance the stereoselectivity of the alkylation of the .alpha.-halo acid with an aryloxy group.
Type:
Grant
Filed:
September 23, 1997
Date of Patent:
January 5, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Paul N. Devine, Richard M. Heid, Jr., David M. Tschaen