Upgrade to enjoy subscriber-only features like email alerts and data export. See the Plans and Pricing

Serving hundreds of leading biopharmaceutical companies globally:

Fish and Richardson
Chinese Patent Office
Mallinckrodt
Cerilliant
Argus Health
Boehringer Ingelheim
Covington
US Army
McKesson

Generated: May 26, 2018

DrugPatentWatch Database Preview

Details for Patent: 6,127,542

« Back to Dashboard

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.

For more information try a trial or see the plans and pricing

Serving hundreds of leading biopharmaceutical companies globally:

Federal Trade Commission
Daiichi Sankyo
Cipla
UBS
AstraZeneca
Queensland Health
Chinese Patent Office
US Department of Justice
Fuji

Drugs may be covered by multiple patents or regulatory protections. All trademarks and applicant names are the property of their respective owners or licensors. Although great care is taken in the proper and correct provision of this service, thinkBiotech LLC does not accept any responsibility for possible consequences of errors or omissions in the provided data. The data presented herein is for information purposes only. There is no warranty that the data contained herein is error free. thinkBiotech performs no independent verifification of facts as provided by public sources nor are attempts made to provide legal or investing advice. Any reliance on data provided herein is done solely at the discretion of the user. Users of this service are advised to seek professional advice and independent confirmation before considering acting on any of the provided information. thinkBiotech LLC reserves the right to amend, extend or withdraw any part or all of the offered service without notice.