Heterocycles substituted with biphenyl-3-cyclobutene-1,2-dione derivatives
AssigneeAmerican Home Products Corporation
InventorsRichard M. Soll, William A. Kinney
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AssigneeAmerican Home Products Corporation
InventorsRichard M. Soll, William A. Kinney
Estimating the term…
Biphenyl derivatives of cyclobutene-1,2-dione of formula 1 are angiotensin II antagonists and are useful for the treatment of hypertension and congestive heart failure ##STR1## wherein: Y is O, NR.sup.7, NCOR.sup.7 ; or R.sup.5 and Y taken together represent a linking chain of N.dbd.CR.sup.8 N; or R.sup.5 and Y taken together represent a linking chain of (CR.sup.9 R.sup.10).sub.n CON where n=1,2,3,4, or 5; X is N, CR.sup.7 ; Z is N, CR.sup.7 ; R.sup.1 is H, alkyl, benzyl, alkoxyalkyl, phenyl; R.sup.2 is H, alkyl, benzyl, alkoxyalkyl, phenyl, alkoxy, alkyl-OH, perfluoroalkyl, F, Cl, Br, I, NR.sup.7 R.sup.8 ; R.sup.3 is H, alkyl, benzyl, alkoxyalkyl, phenyl, alkoxy, alkyl-OH, perfluoroalkyl, F, Cl, Br, I, NR.sup.7 R.sup.8 ; R.sup.4 is H, NR.sup.7 R.sup.8, OR.sup.1, CN, F, Cl, I, Br, perfluoroalkyl, alkyl, phenyl, alkoxy, alkyl-OH, alkoxyalkyl, --(CH.sub.2).sub.n CO.sub.2 R.sup.1, --(CH.sub.2).sub.n CONR.sup.7 R.sup.8 where n=1, 2, 3, 4, or 5; R.sup.5, R.sup.6 is independently chosen from H, alkyl, benzyl, alkoxyalkyl, phenyl, F, Cl, NR.sup.7 R.sup.8 ; or R.sup.5 and R.sup.6 taken together represent a linking chain of CR.sup.9 R.sup.10 of up to 6 linking members; or R.sup.5 and R.sup.6 taken together represent a repeating linking chain of (R.sup.9 C.dbd.CR.sup.10) up to 2 repeating units; R.sup.7 is H, alkyl, phenyl, benzyl; R.sup.8 is H, alkyl, phenyl, benzyl; R.sup.9 is chosen from H, alkyl, benzyl, alkoxyalkyl, phenyl, halogen, OR.sup.1, NR.sup.7 R.sup.8 ; R.sup.10 is chosen from H, alkyl, benzyl, alkoxyalkyl, phenyl, halogen, OR.sup.1, NR.sup.7 R.sup.8 ; wherein alkyl contains 1-8 branched or straight chain carbon atoms or the pharmaceutically acceptable sets thereof.
The compounds of formula 1:
The compounds of formula 1:
The compound 3-hydroxy-4-[4'-[[[5,6,7,8-tetrahydro-2-(trifluoromethyl)-4-quinazolinyl]a mino]methyl][1,1'-biphenyl]-2-yl]-3-cyclobutene-1,2-dione or the pharmaceutically acceptable salt thereof.
Dependencies are inferred from the claim text.