Sulfamide and bis-sulfamide amino acid derivatives as inhibitors of proteolytic enzymes
US6495358B1 · kind B1 · utility
Assignee
Inventor
Key dates
| Filing date | Apr 19, 2000 |
| Grant date | Dec 17, 2002 |
| Priority date | — |
| Expiry date | Apr 19, 2020 |
Classification
- Technology area (CPC Y)Emerging Cross-Sectional Technologies
- CPC primaryY02P20/55
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Compounds of the general formula I are provided: and pharmaceutically acceptable salts thereof, wherein,Z is a chemical species or Ri capable of binding at a primary specificity site of a protease;Y is a chemical species reactive to a specific class of protease;each of R2, R3, R5 and R7 is independently selected from the group consisting hydrogen, alkyls, aryls, substituted aryls, alkylaryls and arylalkyls;R4 and R6 are independently selected from the group consisting of:(a) H, alkyl, aryl, arylalkyl, alkylaryl, substituted derivatives thereof, and Ri;(b) —C(O)OH and derivatives thereof, said derivatives selected from the group consisting of —C(O)OQ, —C(O)NRYRZ, —C(O)[NHCHRi(q)C(O)]qOQ, and —C(O)[NHCHRi(q)C(O)]qNRYRZ; and(c) —CHRiNH2 and derivatives thereof, said derivatives selected from the group consisting of —CHRiNHW, —CHRiNHC(O)OQ, —CHRiNHC(O)R, —CHRiNHC(O)NRYRZ, —CHRiNHC(O)[NHCHRi(q)C(O)]qOQ, —CHRiNHSO2R, and —CHRiNH[C(O)CHRi(r)NH]rW, where q and r independently are integers from 1 to 10 inclusive; J is a carboxyl protecting group; G is an amino protecting group; Q is H, R or J; W is H, R or G; each…
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.