Synthesis and use of &agr;-ketoamide derivatives and arrays
US6452050B1 · kind B1 · utility
Assignee
Inventors
Key dates
| Filing date | Mar 21, 2000 |
| Grant date | Sep 17, 2002 |
| Priority date | — |
| Expiry date | Mar 21, 2020 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07D333/60
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
The invention is based on new methods for making and using compounds and arrays of novel &agr;-ketoamides, and the arrays and compounds made by these methods. These novel compounds are potential inhibitors of proteolytic enzymes, particularly cysteine proteases such as cruzain. Application of the new methods has led to the identification of a number of new inhibitors, from amongst an array of about 38,000 &agr;-ketoamide derivatives, having specific activity against three cysteine proteases: cruzain, papain, and cathepsin B. These compounds and other compounds identified by the methods described herein can be useful, for example, in developing pharmaceutical agents for the treatment of diseases (e.g., Chagas' disease) associated with these proteases. Although the disclosed compounds have specific activity for cruzain, papain, cathepsin B, the methods described herein can also be used to identify inhibitors of other proteases.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.