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US 5,401,738 AGranted
Benzimidazole compounds
AssigneeMerck Patent Gesellschaft mit beschrankter
InventorsWerner Mederski, Dieter Dorsch, Norbert Beier, Pierre Schelling, Ingeborg Lues, Klaus-Otto Minck, Mathias Osswald
Life of this patent
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Abstract
Benzimidazole compounds of the formula I ##STR1## and salts thereof, exhibit antagonistic properties toward angiotensin II and can be used for the treatment of hypertension, aldosteronism, cardiac insufficiency and an increased intraocular pressure, as well as disturbances of the central nervous system.
Claims24
A benzimidazole compound of formula I ##STR12## wherein R.sup.1 is A, C.sub.p H.sub.2p -(C.sub.3-7 -cycloalkyl), OA or SA;
- R.sup.2 and R.sup.3 are in each case, independently, ##STR13## (4) --C.sub.1-10 -alkyl, --C.sub.n H.sub.2n --COOR, --C.sub.n H.sub.2n --CN, --C.sub.m H.sub.2m --Ar, --C.sub.m H.sub.2m --Het.sup.2, --C.sub.n H.sub.2n --1H-5-tetrazolyl, --C.sub.n H.sub.2n --CH.dbd.CH--Ar, --C.sub.n H.sub.2n --CO--N(R).sub.2, --C.sub.m H.sub.2m --CO--R, --C.sub.m H.sub.2m --CO--Ar, --C.sub.n H.sub.2n --O--CON(R).sub.2 or --C.sub.n H.sub.2n --NR--CO--N(R).sub.2, or
- (5) H;
- Y is --C(R).sub.2 --C(R).sub.2 --, --CR.dbd.CR-- or --C(R).sub.2 --S--;
- R is, in each case, independently H or A;
- R.sup.4 is COOR, CN or 1H-5-tetrazolyl;
- R.sup.5 is COOR, CN, NO.sub.2, NH.sub.2 , NHCOCF.sub.3, NHSO.sub.2 CF.sub.3 or 1H-5-tetrazolyl;
- T is absent or is --NR--CO--, --CO--NR-- or --CH.dbd.CH--;
- U is --CH.dbd.C(COOR)--, --CH.dbd.C(CN)--, --CH.dbd.C(1H-5--tetrazolyl)--, --O--CH(COOR)-- or --NR--CH(COOR)--;
- m and p are each 0, 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10;
- n is 1, 2, 3, 4, 5, 6, 7, 8, 9 or 10;
- A is alkyl having 1-6 C atoms;
- Ar is a phenyl or naphthyl group which is unsubstituted or mono- or disubstituted by A, Hal, OH, OA, COOH, COOA, CN, CF.sub.3, NO.sub.2, NH.sub.2, NHA, N(A).sub.2 or combinations thereof;
- Het.sup.2 is an unsubstituted five- or six-membered heteroaromatic radical having 1 to 3 heteroatoms, said heteroatoms in each case being selected from N, O, and S atoms a substituted five- or six-membered heteroaromatic radical having 1 to 3 heteroatoms, said heteroatoms in each case being selected from N, O, and S atoms, an unsubstituted five- or six-membered heteroaromatic radical having 1 to 3 heteroatoms, said heteroatoms in each case being selected from N, O, and S atoms, wherein said radical is fused with a benzene or pyridine ring, or a substituted five- or six-membered heteroaromatic radical having 1 to 3 heteroatoms, said heteroatoms in each case being selected from N, O, and S atoms, wherein said radical is fused with a benzene or pyridine ring;
- and
- Hal is F, Cl, Br or I;
- with the provisos that
- (a) Y is only --C(R).sub.2 --C(R).sub.2 -- or --CR.dbd.CR-- if
- R.sup.1 is other than --C.sub.p H.sub.2p --(C.sub.3-7 --cycloalkyl),
- R.sup.3 is other than H, or
- R.sup.1 is other than --C.sub.p H.sub.2p --(C.sub.3-7 --cycloalkyl) and R.sup.3 is
- other than H;
- and
- (b) at least one of R.sup.2 and R.sup.3 has one of the meanings (1), (2) or (3);
- or
- a physiologically acceptable salt thereof.
22 more elements
Dependencies are inferred from the claim text.