Thiadiazole compounds useful as inhibitors of cysteine activity dependent enzymes
US6162791A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Mar 2, 1998 |
| Grant date | Dec 19, 2000 |
| Priority date | — |
| Expiry date | Mar 2, 2018 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07K5/06043
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Novel 1,2,4-thiadiazole compounds are provided, which are effective as inhibitors of cysteine activity-dependent enzymes and in particular of cysteine proteases. The compounds are useful in treating acne by inhibition of transglutaminase, common cold by inhibition of human rhinovirus 3C protease and inflammatory joint disease by inhibition of cathepsins. The compounds of the present invention are 3,5-disubstituted 1,2,4-thiadazole of the general formula (I): ##STR1## where Z is a nitrogen containing group with recognition sequence for the enzyme and Y is a substituent that tunes the reactivity of the inhibitor towards the thiol group of the cysteine activity-dependent enzyme. The Y group may also serve in recognition.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.