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Details for Patent: 6,025,494

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Details for Patent: 6,025,494

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 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.
Inventor(s): Daugan; Alain Claude-Marie (Les Ulis, FR)
Assignee: ICOS Corporation (Bothell, WA)
Filing Date:Aug 12, 1998
Application Number:09/133,078
Claims:1. A process of preparing a compound of formula (I) having the formula ##STR20## and salts and hydrates thereof, wherein 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, arcylC.sub.1-3 alkyl, or heterarylC.sub.1-3 alkyl;

R.sup.2 represents an optionally substituted mono-cyclic aromatic ring selected from benzene, thiophene, furan, and pyridine, or an optionally substituted bi-cyclic 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, which process comprises:

a process (A) for preparing a compound of formula (I), wherein R.sup.1 and R.sup.3 together represent a 3- or 4-membered alkyl or alkenyl chain, which process (A) comprises cyclisation of a compound of formula (VIII) ##STR22## wherein Alk represents C.sub.1-6 alkyl and R.sup.1 and R.sup.3 together represent a 3- or 4-membered chain alkyl or alkenyl; or

a process (B) for preparing a compound of formula (I) wherein R.sup.3 represents C.sub.1-3 -alkyl, which process (B) comprises cyclisation of a compound of formula (x) with a primary amine R.sup.1 NH.sub.2 ##STR23## wherein Alk represents C.sub.1-6 alkyl and R.sup.5 represents C.sub.2-5 -alkyl, substituted at C.sub.1 by a halogen atom; or

process (A) or (B) as hereinbefore described followed by

i) an interconversion step of one or more of R.sup.0, R.sup.1, R.sup.2, and R.sup.3 ; and/or either

ii) salt formation; or

iii) solvate formation.
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