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US 5,332,750 AGranted
1,2-dihydro-2-oxopyridines
AssigneeMerck Patent GmbH
InventorsWerner Mederski, Norbert Beier, Pierre Schelling, Ingeborg Lues, Klaus-Otto Minck
Life of this patent
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Abstract
New 1,2-dihydro-2-oxopyridines of formula I ##STR1## in which R is the radical ##STR2## and R.sup.1 to R.sup.6 and X are as defined herein, and their salts, have antagonistic properties towards angiotensin II and can be used for the treatment of hypertension, aldosteronism and cardiac insufficiency.
Claims25
A 1,2-dihydro-2-oxopyridine compound of formula I ##STR10## wherein R is the radical ##STR11## R.sup.1 is H, Hal, A, OA or NO.sub.2 ;
- R.sup.2 is COOH, COOA, CN, NO.sub.2, NH.sub.2, NHCOR.sup.7, NHSO.sub.2 R.sup.7 or tetrazol-5-yl;
- R.sup.3 is CH.sub.2 NR.sup.10 R.sup.11, or tetrazol-5-yl;
- R.sup.4 is H or A;
- R.sup.5, R.sup.6 and R.sup.10 are in each case independently H, A, alkenyl having 2-6 C atoms, alkynyl having 2-6 C atoms, Ar or Ar-alkyl having 1-6 C atoms in the alkyl moiety;
- R.sup.7 is A or A monosubstituted or polysubstituted by F;
- R.sup.11 is H, A, A monosubstituted or polysubstituted by F, Ar, Ar-alkyl having 1-6 C atoms in the alkyl moiety, CO-A, CO-Ar, CO-alkyl-Ar having 1-6 C atoms in the alkyl moiety, COOA, COOAr, COO--alkyl--Ar having 1-6 C atoms in the alkyl moiety, CONR.sup.12 R.sup.13, SO.sub.2 R.sup.7 or SO.sub.2 Ar,
- NR.sup.10 R.sup.11 can also be pyrrolidino, piperidino, morpholino, succinimido or phthalimido;
- R.sup.12 and R.sup.13 are in each case independently H, A, cycloalkyl having 3-8 C atoms, alkenyl having 2-6 C atoms, alkynyl having 2-6 C atoms, or Ar;
- X is absent or is --CO--, --O--, --NH--CO--, --CO--NH--, --CH.sub.2 --O-- or --O--CH.sub.2 --;
- A is alkyl having 1-6 C atoms;
- Ar is phenyl which is unsubstituted or monosubstituted by A, OA, CF.sub.3, Hal or NO.sub.2 ;
- and
- Hal is F, Cl, Br or I;
- or
- a physiologically acceptable salt.
12 more elements
Dependencies are inferred from the claim text.