Renal-selective biphenylalkyl 1H-substituted-1,2,4-triazole angiotensin II antagonists for treatment of hypertension
US5217985A · kind A · utility
Assignee
Inventors
Key dates
| Filing date | Aug 28, 1990 |
| Grant date | Jun 8, 1993 |
| Priority date | — |
| Expiry date | Aug 28, 2010 |
Classification
- Technology area (CPC H)Electricity
- CPC primaryH04B1/3883
- WIPO fieldOrganic fine chemistry
- WIPO sectorChemistry
Abstract
Renal-selective compounds are described which, in one embodiment, are prodrugs preferentially converted in the kidney to compounds capable of blocking angiotensin II (AII) receptors. These prodrugs are conjugates formed from two components, namely, a first component provided by an AII antagonist compound and a second component which is capable of being cleaved from the first component when both components are chemically linked within the conjugate. The two components are chemically linked by a bond which is cleaved selectively in the kidney, for example, by an enzyme. The liberated AII antagonist compound is then available to block AII receptors within the kidney. Conjugates of particular interest are glutamyl derivatives of biphenylmethyl 1H-substituted-1,2,4-triazole compounds, of which N-acetylglutamic acid, 5-[[4'-[(3,5-dibutyl-1H-1,2,4-triazol-1-yl)methyl][1,1'-biphenyl]-2-yl]]ca rbonylhydrazide, (shown below) is an example: ##STR1##
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.