Abstract: This invention relates to a process for the preparation of a key intermediate using an chiral additive to effect an asymmetric conjugate addition.
Type:
Grant
Filed:
January 5, 1998
Date of Patent:
December 7, 1999
Assignee:
Merck & Co., Inc.
Inventors:
Richard D. Tillyer, David M. Tschaen, Feng Xu
Abstract: The present invention provides novel 4-aryl-3-aminoquinolin-2-one derivatives having the general formula ##STR1## wherein R, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are as defined herein, or a non-toxic pharmaceutically acceptable salt thereof which are modulators of the large conductance calcium-activated K.sup.+ channels and are useful in the treatment of disorders which are responsive to the opening of the potassium channels.
Type:
Grant
Filed:
August 24, 1998
Date of Patent:
October 26, 1999
Assignee:
Bristol-Myers Squibb Company
Inventors:
Piyasena Hewawasam, John E. Starrett, Jr., Stephen G. Swartz
Abstract: According to the present invention, there is provided a compound, or a solvate or salt thereof of formula (I): ##STR1## Substituted hydroisoquinoline derivatives are potent and selective delta opioid agonists and antagonists and are of potential therapeutic utility as inter alia analgesics.
Abstract: Compounds of the formula I ##STR1## are suitable for the preparation of pharmaceuticals for the prophylaxis and therapy of disorders involving increased activity of matrix-degrading metalloproteinases.