Abstract: Certain aminoalkyl substituted amides which have a cyclohexapeptidyl group and which are found to have antibiotic activity with physical properties suitable for use in therapeutic compositions are described.
Abstract: The present invention is directed to water-soluble derivatives of antibiotic lipopeptides. The derivatives have good solubility properties in aqueous medium, rendering them more useful as therapeutic agents.
Abstract: A process for producing an antibiotic compound which is normally a minor component in the cultivation of Z. arboricola to be the major product is described.
Type:
Grant
Filed:
February 14, 1994
Date of Patent:
June 20, 1995
Assignee:
Merck & Co, Inc.
Inventors:
Jimmy M. Fountoulakis, Prakash S. Masurekar, Louis Kaplan
Abstract: This invention relates to a method for the preparation of a compound of formula I: ##STR1## a key intermediate in the synthesis of a series of Angiotensin II receptor antagonists. The invention also relates to a selective reagent for conducting the Hofmann rearrangement, particularly in the formation of a pyridinoimidazolone, which is a percursor to the formation of an imidazopyfidine of formula I. This invention also relates to a method for the preparation of imidazolutidine, a key intermediate in the synthesis of 3-(2'-(N-benzoyl)sulfonamidobiphen-4-yl)-methyl-5,7 -dimethyl-2-ethyl-3H-imidazo[4,5-b]pyridine, using pyridinoimidazolone, an unreactive urea.
Type:
Grant
Filed:
May 26, 1994
Date of Patent:
June 13, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Laura E. Fredenburgh, Robert D. Larsen, Ji Liu, Robert A. Reamer, Chris H. Senanayake, Thomas R. Verhoeven
Abstract: The present invention is directed to compounds which inhibit farnesyl-protein transferase (FPTase) 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 famesyl-protein transferase and the famesylation of the oncogene protein Ras.
Type:
Grant
Filed:
April 4, 1994
Date of Patent:
May 30, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Sheo B. Singh, Gerald F. Bills, Russell B. Lingham, Isabel Martin, Keith C. Silverman, Jack L. Smith
Abstract: This invention relates to pharmaceutical compounds of structural formulae (I) and (II): ##STR1## and compositions and methods of treatment utilizing these compounds to inhibit farnesyl protein transferase and farnesylation of the oncogene protein Ras.
Type:
Grant
Filed:
December 16, 1991
Date of Patent:
May 30, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Sheo B. Singh, Gerald F. Bills, Russell B. Lingham, Keith C. Silverman, Deborah L. Zink
Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebral and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
Type:
Grant
Filed:
March 19, 1993
Date of Patent:
May 30, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Daljit S. Dhanoa, Kenneth J. Fitch, Daniel F. Veber, Thomas F. Walsh, David L. Williams, Jr.
Abstract: There are disclosed new substituted triazolinone, triazolinethione, and triazolinimine compounds which are useful as angiotensin II antagonists. These compounds have the general formula: ##STR1## wherein G is R.sup.
Type:
Grant
Filed:
December 21, 1992
Date of Patent:
May 2, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Wallace T. Ashton, Linda L. Chang, Malcolm MacCoss, Prasun K. Chakravarty, William J. Greenlee, Arthur A. Patchett, Kelly Flanagan
Abstract: Heterocyclic compounds of structural formula: ##STR1## wherein A, B, C, and D are independently carbon atoms or nitrogen atoms are angiotensin II antagonists useful in the treatment of hypertension and congestive heart failure.
Type:
Grant
Filed:
September 2, 1992
Date of Patent:
May 2, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Prasun K. Chakravarty, William J. Greenlee, Dooseop Kim, Nathan B. Mantlo, Arthur A. Patchett, Ralph A. Rivero
Abstract: Solutions are prepared by accurately dispensing and weighing concentrated solutions of salts, acids and bases as well as water or organic solvent, and mixing to achieve homogeneity. The final solution may be stored or used directly from the system.
Type:
Grant
Filed:
November 25, 1992
Date of Patent:
April 4, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Michael D. Levin, William F. Richardson, Alan B. Todtenkopf
Abstract: Compounds of the general formula: ##STR1## or a pharmaceutically acceptable salt, hydrate or crystal form enantiomer, diastereomer or mixtures thereof are Class III antiarrhythmic agents.
Type:
Grant
Filed:
November 22, 1993
Date of Patent:
April 4, 1995
Assignee:
Merck & Co., Inc.
Inventors:
John J. Baldwin, David A. Claremon, Gerald S. Ponticello, Harold G. Selnick
Abstract: Phenoxyphenylacetic acids and derivatives of general structural formula I ##STR1## have endothelin antagonist activity and are therefore useful in treating cardiovascular disorders, such as hypertension, postischemic renal failure, vasospasm, cerebal and cardiac ischemia, myocardial infarction, inflammatory diseases, Raynaud's disease, and endotoxic shock, and asthma.
Type:
Grant
Filed:
March 19, 1993
Date of Patent:
March 28, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Scott W. Bagley, Prasun K. Chakravarty, Anna Chen, Daljit S. Dhanoa, Kenneth J. Fitch, William J. Greenlee, Elizabeth M. Naylor, James R. Tata, Thomas F. Walsh, David L. Williams, Jr.
Abstract: The present invention relates to novel potassium channel agonists which are useful in activating the calcium activated Maxi-K potassium channel in mammalian neuronal and smooth muscle tissue. The claimed compounds are of the general formula: ##STR1## In addition, a novel microbiological process for producing the claimed compounds is described.
Type:
Grant
Filed:
December 13, 1993
Date of Patent:
March 21, 1995
Assignee:
Merck & Co., Inc.
Inventors:
Maria L. Garcia, Robert A. Giacobbe, Otto D. Hensens, Gregory J. Kaczorowski, Seok H. Lee, Owen B. McManus, Deborah L. Zink