Abstract: Methods for stereoselective substitution in which a (mono or un)-&agr;-substituted unprotected &bgr;-amino ester compound or salt thereof is reacted with an aliphatic electrophile in the presence of a base selected from alkyl lithium compounds, lithium hydride, lithium amide, lithium dialkyl amides and alkali hexamethyldisilylamines.
Type:
Grant
Filed:
January 26, 2000
Date of Patent:
August 13, 2002
Assignee:
Aventis Pharmaceuticals Inc.
Inventors:
Sithamalli V. Chandramouli, Michael K. O'Brien, Tory H. Powner
Abstract: The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
Type:
Grant
Filed:
December 2, 1999
Date of Patent:
August 28, 2001
Assignee:
Aventis Pharma Deutschland GmbH
Inventors:
Yong Mi Choi-Sledeski, Heinz W. Pauls, Jeffrey N. Barton, William R. Ewing, Daniel M. Green, Michael R. Becker, Yong Gong, Julian Levell
Abstract: This invention is directed to a compound of formula I which is useful for inhibiting the activity of Factor Xa, by combining said compound with a composition containing Factor Xa. The present invention is also directed to compositions containing compounds of the formula I, methods for their preparation, their use, such as in inhibiting the formation of thrombin or for treating a patient suffering from, or subject to, a disease state associated with a physiologically detrimental excess amount of thrombin.