Heteroaryl amidines, methylamidines and guanidines, preparation thereof, and use thereof as protease inhibitors
US6291514A · kind A · utility
7Cited by
10References
60Claims
0Family size
Assignee
Inventors
Key dates
| Filing date | Aug 11, 1999 |
| Grant date | Sep 18, 2001 |
| Priority date | — |
| Expiry date | Aug 11, 2019 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D417/14
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention is directed to compounds of Formula I: ##STR1## wherein X is O, S or NR.sup.7 and R.sup.1 -R.sup.7, Y and Z are set forth in the specification, as well as hydrates, solvates or pharmaceutically acceptable salts thereof. Also described are methods for preparing the compounds of Formula I. The novel compounds of the present invention are potent inhibitors of proteases, especially trypsin-like serine proteases, such as chymotrypsin, trypsin, plasmin and urokinase. Certain of the compounds exhibit direct, selective inhibition of urokinase, or are intermediates useful for forming compounds having such activity.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.