Acetamide derivatives and protease inhibitors
US6271238A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 1, 1999 |
| Grant date | Aug 7, 2001 |
| Priority date | — |
| Expiry date | Mar 1, 2019 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The present invention relates to novel acetamide compounds having a substituted heterocyclic group and consecutive dicarbonyl structures, for example, 1-pyrimidinylacetamide compounds, and these compounds have inhibitory activity on chymotrypsin type proteases and are useful as inhibitors for said enzymes, particularly as chymase inhibitors. The novel acetamide compounds of the present invention are shown in formula (I) below: ##STR1## wherein R.sup.0 is substituted or unsubstituted phenyl; R.sup.1 is aryl or heteroaryl which may be substituted or unsubstituted; R.sup.2 is substituted or unsubstituted alkyl, arylalkyl, or heteroarylalkyl; R.sup.3 is hydrogen; acyl group; sulfonyl group; isocyanate group; thiourea; a lower alkyl or a substituted lower alkyl; aryl (1-7C) alkyl, heteroaryl (1-7C) alkyl, aryl and heteroaryl; X represents a carbon atom and Y represents a nitrogen atom; and Z is a polymethylene group wherein a hydrogen atom in the polymethylene may be replaced.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.