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Details for Patent: 6,127,542

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Details for Patent: 6,127,542

Title: 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 cyloalkyl, 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'-mnonophosphate 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.
Inventor(s): Daugan; Alain Claude-Marie (Les Ulis, FR)
Assignee: ICOS Corporation (Bothell, WA)
Filing Date:Sep 21, 1999
Application Number:09/399,667
Claims:1. Compounds of formulae ##STR20## wherein Alk represents C.sub.1-6 alkyl; Hal represents a halogen atom;

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 cycloalkyl-C.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 ##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 and R.sup.3 together represent a 3- or 4-membered alkyl or alkenyl chain; and

R.sup.5 represents C.sub.2 -C.sub.5 alkyl, substituted at C, by a halogen atom, with the exception for compounds (III), (VI), and (VII) wherein R.sup.0 is hydrogen, R.sup.2 is phenyl, and Alk is methyl.

2. A compound of formula ##STR22## wherein Alk represents C.sub.1-6 alkyl; R.sup.0 represents hydrogen, halogen, or C.sub.1-6 alkyl;

R.sup.2 represents an optionally substituted monocyclic aromatic ring selected from thiophene, furan, and pyridine.
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