Benzamidoxime prodrugs as antipneumocystic agents
US5843980A · kind A · utility
Assignees
Inventors
Key dates
| Filing date | Nov 15, 1996 |
| Grant date | Dec 1, 1998 |
| Priority date | — |
| Expiry date | Nov 15, 2016 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02A50/30
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
A method of treating Pneumocystis carinii pneumonia in a subject in need of such treatment is disclosed. The method comprises orally administering to the subject a bis-benzamidoxime of Formula II ##STR1## wherein: R.sub.1 and R.sub.2 are each independently selected from the group consisting of H, loweralkyl, oxyalkyl, alkoxyalkyl, cycloalkyl, aryl, hydroxyalkyl, aminoalkyl or alkylaminoalkyl; R.sub.3 is H, loweralkyl, oxyalkyl, alkoxyalkyl, hydroxyalkyl, cycloalkyl, aryl, aminoalkyl, alkylaminoalkyl or halogen; R.sub.4 is --OY, or R.sub.1 and R.sub.4 together represent, ##STR2## wherein R.sub.5 is ##STR3## Y is H or loweralkyl; n is an integer from 0 to 2; and A is a heterocyclic aromatic group selected from the group consisting of: ##STR4## wherein R.sub.6 and R.sub.7 are each independently selected from the group consisting of H, loweralkyl, halogen, oxyalkyl, oxyaryl, or oxyarylalkyl, or a pharmaceutically acceptable salt thereof, that is reduced in the subject to produce a benzamidine having anti-P. carinii activity. The method of the present invention may alternatively comprise intravenously administering to the subject an active compound as disclosed herein. Pharmaceutical fo…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.