Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
Type:
Grant
Filed:
August 17, 2000
Date of Patent:
February 21, 2006
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel
Abstract: Novel compounds are provided having the formula
and salt thereof, where R1 is hydrogen, an alkyl, aralkyl, hydroxymethyl, carboxymethyl acyloxymethyl or trialkylsilyl group, or a group —CH2NR3R4 where N is a linking nitrogen atom and where (a) R3 and R4 are independently selected from hydrogen and alkyl, alkenyl, hydroxyalkyl and alkoxyalkyl groups; (b) R3 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group, and R4 is —COR5 where R5 is hydrogen or an alkyl, alkenyl, hydroxyalkyl or alkoxyalkyl group; or (c) R3 and R4 taken together with the linking nitrogen atom form a saturated 3- to 7-member heterocyclic group. These compounds are useful intermediates in a process to prepare camptothecin derivatives including the anti-cancer drug irinotecan.
Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
Type:
Grant
Filed:
December 28, 2001
Date of Patent:
May 13, 2003
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
Abstract: Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.
Type:
Grant
Filed:
August 30, 2000
Date of Patent:
March 11, 2003
Assignee:
Pharmacia & Upjohn Company
Inventors:
Mikhail F. Gordeev, Gary W. Luehr, Dinesh V. Patel, Zhi-Jie Ni, Eric Gordon
Abstract: The present invention provides a compound of formula I
which is useful as antiviral agents, in particular, as agents against viruses of the herpes family.
Type:
Grant
Filed:
June 22, 2001
Date of Patent:
February 25, 2003
Assignee:
Pharmacia & Upjohn Company
Inventors:
Valerie A. Vaillancourt, Sandra Staley, Audris Huang, Richard Allen Nugent, Ke Chen, Sajiv K. Nair, James A. Nieman, Joseph Walter Strohbach
Abstract: The present invention provides for 8-hydroxy-7-substituted quinoline compounds such as formula IA
These compounds are useful as anti-viral agents. Specifically, these compounds have anti-viral activity against the herpes virus, cytomegalovirus (CMV). Many of these compounds are also active against other herpes viruses, such as the varicella zoster virus, the Epstein-Barr virus, the herpes simplex virus and the human herpes virus type 8 (HHV-8).
Type:
Grant
Filed:
October 23, 2001
Date of Patent:
December 31, 2002
Assignee:
Pharmacia & Upjohn Company
Inventors:
Valerie Ann Vaillancourt, Joseph Walter Strohbach, Olivier Bezencon, Suvit Thaisrivongs
Abstract: The present invention provides compounds of formula I useful as antimicrobial agents
wherein W, X, Y, R1, R2 and n are as defined in thereof.
Type:
Grant
Filed:
May 17, 2000
Date of Patent:
May 14, 2002
Assignee:
Pharmacia & Upjohn Co.
Inventors:
Michael J. Genin, Michael Robert Barbachyn, Jackson B. Hester, Jr., Paul D. Johnson