Patent ID: 6043252
Filing Date: 2000-03-28
Classification: C07D

Abstract:
A combination comprising:(a) a compound of formula ##STR12## wherein R.sup.0 represents hydrogen or halogen;R.sup.1 is selected from the group consisting of:hydrogen,NO.sup.2trifluoromethyl,trifluoromethoxy,halogen,cyano,a 5- or 6-membered heterocyclic group containing at least one heteroatom selected from oxygen, nitrogen and sulphur, and is optionally substituted by --C(.dbd.O)OR.sup.a or C.sub.1-4 alkyl, C.sub.1-6 alkyl optionally substituted by --OR.sup.a, C.sub.1-3 alkoxy, C(.dbd.O) R.sup.a, O--C (.dbd.O) R.sup.a, C(.dbd.O) OR.sup.a, C.sub.1-4 alkylene-C (.dbd.O)OR.sup.a, O--C.sub.1-4 alkylene --C (.dbd.O) OR.sup.a, C.sub.1-4 alkylene--O--C.sub.1-4 alkylene-C(.dbd.O)OR.sup.a, C(.dbd.O)NR.sup.a SO.sub.2 R.sup.c, C(.dbd.O)C.sub.1-4 alkylene-Het, C.sub.1-4 alkylene-NR.sup.a R.sup.b, C.sub.2-6 alkenylene-NR.sup.a R.sup.b, C(.dbd.O)NR.sup.a R.sup.b, C(.dbd.O)NR.sup.a R.sup.c, C(.dbd.O)NR.sup.a C.sub.1-4 alkylene-OR.sup.b C(.dbd.O)NR.sup.a C.sub.1-4 alkylene-Het, OR.sup.a OC.sub.2-4 alkylene-NR.sup.a R.sup.b, OC.sub.1-4 alkylene-CH (OR.sup.a) CH.sub.2 NR.sup.a R.sup.b, O--C.sub.1-4 alkylene-Het, O--C.sub.2-4 alkylene-OR.sup.a, O--C.sub.2-4 alkylene-NRa--C(.dbd.O)--OR.sup.b, NR.sup.a R.sup.b, NR.sup.a C.sub.1-4 alkylene-NR.sup.a R.sup.b, NR.sup.a C(.dbd.O)R.sup.b, NR.sup.a C(.dbd.O)NR.sup.a R.sup.b, N(SO.sub.2 C.sub.1-4 alkyl).sub.2, NR.sup.a (SO.sub.2 C.sub.1-4 alkyl), SO.sub.2 NR.sup.a R.sup.b, and OSO.sub.2 trifluoromethyl;R.sup.2 is selected from the group consisting of:hydrogen,halogen,OR.sup.a,C.sub.1-6 alkyl,NO.sub.2, andNR.sup.a R.sup.b,or R.sup.1 and R.sup.2 are taken together to form a 3- or 4-membered alkylene or alkenylene chain component of a 5- or 6-membered ring, optionally containing at least one heteroatom selected from the group consisting of oxygen, nitrogen and suflur;R.sup.3 is selected from the group consisting of:hydrogen,halogen,NO.sub.2,trifluoromethoxy,C.sub.1-6 alkyl, andC(.dbd.O)OR.sup.a ;R.sup.4 is hydrogen,or R.sup.3 and R.sup.4 are taken together to form a 3- or 4-membered alkylene or alkenylene chain component of a 5- or 6-membered ring, optionally containing at least one heteroatom;Het represents a 5- or 6-membered heterocyclic group containing at least one heteroatom selected from the group consisting of oxygen, nitrogen, and sulfur, and is optionally substituted with C.sub.1-4 alkyl;R.sup.a and R.sup.b can be the same or different, and are independently selected from hydrogen and C.sub.1-6 alkyl;R.sup.c represents phenyl or C.sub.4-6 cycloalkyl, wherein the phenyl or C.sub.4-6 cycloalkyl can be optionally substituted by one or more halogen atoms, one or more --C(.dbd.O)OR.sup.a, or one or more --OR.sup.a ;n is an integer selected from 1, 2 and 3;m is an integer selected from 1 and 2;and pharmaceutically acceptable salts and solvates thereof; and(b) a second therapeutically active agent,for simultaneous, separate, or sequential use in the treatment of a condition where inhibition of a cGMP-specific PDE is of a therapeutic benefit.