Back to results
US 5,476,857 AGranted
Imidazopyridines
AssigneeMerck Patent GmbH
InventorsWerner Mederski, Dieter Dorsch, Norbert Beier, Pierre Schelling, Ingeborg Lues, Klaus-Otto Minck, Mathias Osswald
Life of this patent
Estimating the term…
Abstract
Novel imidazopyridine derivatives of formula I: ##STR1## wherein R is ##STR2## and R.sup.1, R.sup.2, R.sup.3, R.sup.4, X and Y are as defined herein, and their salts, exhibit antagonistic properties toward angiotensin II and can be used for the treatment of hypertension, aldosteronism, cardiac insufficiency and increased intraocular pressure, and of disorders of the central nervous system.
Claims20
An imidazopyridine compound of formula I:
- ##STR12## wherein R is ##STR13## R.sup.1 is A or C.sub.3 -C.sub.7 --cycloalkyl--;
- R.sup.2 is CN or 1H-tetrazol-5-yl;
- R.sup.3 is alkenyl having 2-6 C atoms in the alkenyl moiety and which is substituted by Ar or is substituted by Ar and COOA, or is --C.sub.n H.sub.2n --R.sup.9 or --CHR.sup.10 --C.sub.k H.sub.2k --R.sup.11 ;
- R.sup.4 is H;
- R.sup.6 and R.sup.7 are each, independently, H, A, Ar or ArC.sub.n H.sub.2n --;
- R.sup.6 can also be --CH.sub.2 COOA;
- or
- R.sup.6 and R.sup.7 together can also be an alkylene chain having 2-5 C atoms, which can be monosubstituted by carbonyl oxygen, Ar, --COOA, --CO--N(A).sub.2 or --NH--CO--A or interrupted by O or by --NR.sup.16 --;
- R.sup.9 is Het.sup.1, --CO--NR.sup.6 R.sup.7, --C(.dbd.NR.sup.12)--A or --S(O).sub.m --Ar;
- R.sup.10 is COOH or COOA;
- R.sup.11 is Ar;
- R.sup.12 is OR.sup.13 ;
- R.sup.13 is A;
- R.sup.16 is Ar or SO.sub.2 --Ar;
- X is absent;
- Y is O;
- A is alkyl having 1-6 C atoms;
- Ar is an unsubstituted phenyl group or a phenyl group monosubstituted or disubstituted by A, CF.sub.3, OA, COOA or Hal;
- Het.sup.1 is 2-oxo-3-Ar-5-oxazolidinyl;
- Hal is F, Cl, Br or I;
- k is 0, 1, 2, 3 or 4;
- m is 0, 1 or 2;
- and
- n is 1, 2, 3, 4, 5 or 6;
- or a pharmaceutically acceptable salt thereof.
22 more elements
Dependencies are inferred from the claim text.