Abstract: Intermediates useful in the preparation of the antiviral agent entecavir are disclosed. A resin adsorption process for the isolation and purification of entecavir is also disclosed. Various processes useful in the preparation of entecavir are also disclosed.
Type:
Grant
Filed:
December 19, 2005
Date of Patent:
June 23, 2009
Assignee:
Bristol-Myers Squibb Company
Inventors:
Yadagiri R. Pendri, Chung-Pin H. Chen, Jing Liang, Shaopeng Wang, Milan Stojanovic, Richard P. Polniaszek, John Thottathil, Dhileepkumar Krishnamurty
Abstract: The present invention relates to tricyclic 2-pyrimidone compounds of formula (I): or stereoisomeric forms, stereoisomeric mixtures, or pharmaceutically acceptable salt forms thereof, which are useful as inhibitors of HIV reverse transcriptase, and to pharmaceutical compositions and diagnostic kits comprising the same, and methods of using the same for treating viral infection or as an assay standard or reagent.
Abstract: This disclosure provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the disclosure is concerned with new aminium salts of 1,2,3-triazoles which can be used as prodrugs to improve the solubility or pharmaceutical properties of 1,2,3-triazole containing compounds. More particularly, the present disclosure relates to compounds containing N-aminium-1,2,3-triazoles that are useful as antiviral agents and specifically for the treatment of HIV and AIDS.