US 5,859,006 A · Tetracyclic derivatives; process of preparation and use

Abstract

A compound of formula (I) ##STR1## and salts and solvates thereof, in which: R.sup.0 represents hydrogen, halogen or C.sub.1-6 alkyl; R.sup.1 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, haloC.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkylC.sub.1-3 alkyl, arylC.sub.1-3 alkyl or heteroarylC.sub.1-3 alkyl; R.sup.2 represents an optionally substituted monocyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring ##STR2## attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen; and R.sup.3 represents hydrogen or C.sub.1-3 alkyl, or R.sup.1 and R.sup.3 together represent a 3- or 4-membered alkyl or alkenyl chain. A compound of formula (I) is a potent and selective inhibitor of cyclic guanosine 3', 5'-monophosphate specific phosphodiesterase (cGMP specific PDE) having a utility in a variety of therapeutic areas where such inhibition is beneficial, including the treatment of cardiovascular disorders.

Claims15

Dependent claims

A compound of formula (I) ##STR20## or salts or solvates thereof, in which:

R.sup.0 represents hydrogen, halogen or C.sub.1-6 alkyl;
R.sup.1 represents hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.2-6 alkynyl, haloC.sub.1-6 alkyl, C.sub.3-8 cycloalkyl, C.sub.3-8 cycloalkylC.sub.1-3 alkyl, arylC.sub.1-3 alkyl, wherein aryl is phenyl or phenyl substituted with one to three substituents selected from the Group consisting of halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, methylenedioxy, and mixtures thereof, or heteroarylC.sub.1-3 alkyl, wherein heteroaryl is thienyl, furyl, or pyridyl, each optionally substituted with one to three substituents selected from the group consisting of halogen, C.sub.1-6 alkyl, C.sub.1-6 alkoxy, and mixtures thereof;
R.sup.2 represents an optionally substituted mono-cyclic aromatic ring selected from benzene, thiophene, furan and pyridine or an optionally substituted bicyclic ring ##STR21## attached to the rest of the molecule via one of the benzene ring carbon atoms and wherein the fused ring A is a 5- or 6-membered ring which may be saturated or partially or fully unsaturated and comprises carbon atoms and optionally one or two heteroatoms selected from oxygen, sulphur and nitrogen;
and R.sup.3 represents hydrogen or C.sub.1-3 alkyl, or R.sup.1 or R.sup.3 together represent a 3- or 4-membered alkyl or alkenyl chain component of a 5- or 6-membered ring.

1 more element

Dependencies are inferred from the claim text.

Tetracyclic derivatives; process of preparation and use

Life of this patent

Tetracyclic derivatives; process of preparation and use

Life of this patent

Abstract

Claims15