Abstract: The invention concerns 2-oxo-1-pyrrolidine derivatives and a process for preparing them and their uses. The invention also concerns a process for preparing &agr;-ethyl-2-oxo-1-pyrrolidine acetamide derivatives from unsaturated 2-oxo-1-pyrrolidine derivatives. Particularly the invention concerns novel intermediates and their use in methods for the preparation of S-&agr;-ethyl-2-oxo-1-pyrrolidine acetamide.
Type:
Grant
Filed:
August 20, 2002
Date of Patent:
March 30, 2004
Assignee:
UCB Farchim S.A.
Inventors:
John Surtees, Violeta Marmon, Edmond Differding, Vincent Zimmermann
Abstract: Compounds of the formula:
where the formula variables are as defined in the disclosure, advantageously inhibit or block the biological activity of the picornaviral 3C protease. These compounds, as well as pharmaceutical compositions containing these compounds, are useful for treating patients or hosts infected with one or more picornaviruses, such as RVP. Intermediates and synthetic methods for preparing such compounds are also described.
Type:
Grant
Filed:
April 12, 2001
Date of Patent:
August 26, 2003
Assignee:
Agouron Pharmaceuticals, Inc.
Inventors:
Theodore O. Johnson Jr., Ye Hua, Hiep T. Luu, Peter S. Dragovich
Abstract: An improved process is provided for preparing water-soluble prodrugs of triazole antifungal compounds containing a secondary or tertiary hydroxyl group. More particularly, the improved process is directed toward preparation of water-soluble triazole antifungal compounds are provided having the general formula
wherein A is the non-hydroxy portion of a triazole antifungal compound of the type containing a secondary or tertiary hydroxyl group and R and R1 are as defined in the specification.
Type:
Grant
Filed:
October 16, 2001
Date of Patent:
September 10, 2002
Assignee:
Bristol-Myers Squibb Company
Inventors:
Chung-Pin Chen, Timothy Paul Connolly, Laxma Reddy Kolla, John D. Matiskella, Richard H. Mueller, Yadagiri Pendri, Dejah T. Petsch
Abstract: Omapatrilat (I) is a potent inhibitor of angiotensin-converting enzyme (ACE) and neutral endopeptidase (NEP) both in vitro and in vivo and is currently undergoing large scale clinical trials as an anti-hypertensive. Omapatrilat may be synthesized using the S-stereoisomer of compound (V). Compound (V) may be prepared from a novel hydantoin (III). The hydantoin may be prepared from a monoacetal (XI) or via a dinitrile (V).
Type:
Grant
Filed:
June 7, 2000
Date of Patent:
October 9, 2001
Assignee:
Dixie Chemical Company
Inventors:
Joseph C. Rongione, Robert E. Brown, Dwight E. Raff