Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1990-08-28
1993-06-08
Higel, Floyd D.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
514383, 514252, 514326, 5482622, 548253, 5482654, 5482676, 5482668, 5482678, 548254, 5482694, 544366, 546210, C07D40310, C07D24908, A61K 3141
Patent
active
052179850
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##
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Manning Robert E.
Reitz David B.
G. D. Searle & Co.
Higel Floyd D.
Keane J. Timothy
Matukaitis Paul D.
Miltenberger Lenora A.
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