Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1995-04-26
1997-08-26
Grumbling, Matthew V.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
5142285, 5142328, 514267, 540575, 544 60, 544115, C07D41704, C07D41304, C07D24308, A61K 31505
Patent
active
056611471
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This is a 371 of PCT/JP94/01456, filed Sep. 2, 1994 from which priority is claimed.
The present invention relates to imidazoquinazoline derivatives or pharmacologically acceptable salts thereof which have the cyclic guanosine 3',5'-monophosphate (cGMP)-specific phosphodiesterase (PDE) inhibitory activity and are useful for treating or ameliorating cardiovascular diseases such as thrombosis, angina pectoris, hypertension, heart failure, arterial sclerosis and the like, as well as asthma and the like.
PRIOR ART
cGMP plays an important role as a second messenger in intracellular signal transduction. An inhibitor of cGMP-specific PDE, an enzyme which degrades cGMP, increases the concentration of intracellular cGMP and enhances the effects of endothelium-derived relaxing factor (EDRF), nitro vasodilator or atrial natriuretic peptide, and shows the antiplatelet activity, the anti-vasocontraction activity and the vasodilating activity and are useful for treating angina pectoris, hypertension, congestive heart failure, post-PTCA restenosis, peripheral vascular diseases, bronchitis, chronic asthma, allergic asthma, allergic gravedo, glaucoma, alimentary canal diseases such as irritable intestine syndrome and the like.
The PDE inhibitory activity and the adenosine receptor antagonistic activity of imidazo[4,5-g]quinazoline derivatives are described in J. Med. Chem., 29, 972 (1986), J. Med. Chem., 32, 2247 (1989), J. Org. Chem., 51, 616 (1986) and the references cited therein. However, these compounds are neither a particularly strong PDE inhibitor nor a selective cGMP-specific PDE inhibitor.
DISCLOSURE OF THE INVENTION
The present invention relates to imidazoquinazoline derivatives (hereinafter referred to as Compound (I); a compound having another compound number corresponds to the compound represented by the formula of the same number) represented by the formula (I): ##STR2## wherein R.sup.1 and R.sup.2 are the same or different and represent hydrogen, lower alkyl (which is optionally substituted with one to three substituents which are the same or different and are cycloalkyl, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, amino, monoalkyl-substituted amino, dialkyl-substituted amino, nitro, halogen, or alicyclic heterocycle group (which is optionally substituted with one to three substituents which are the same or different and are lower alkyl, aralkyl, aryl optionally substituted with one to three substituents which are the same or different and are lower alkoxy, or aromatic heterocycle group)), cycloalkyl, bicycloalkyl, benzocycloalkyl (which is optionally substituted with one to three substituents which are the same or different and are lower alkyl, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, amino, monoalkyl-substituted amino, dialkyl-substituted amino, nitro, sulfonamide, halogen, or trifluoromethyl), lower alkenyl, aryl (which is optionally substituted with one to three substituents which are the same or different and are lower alkyl, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, amino, monoalkyl-substituted amino, dialkyl-substituted amino, nitro, sulfonamide, halogen, or trifluoromethyl), aromatic heterocycle group-substituted alkyl (which is optionally be substituted with one to three substituents which are the same or different and are lower alkyl, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, amino, monoalkyl-substituted amino, dialkyl-substituted amino, nitro, sulfonamide, halogen or trifluoromethyl and where said alkyl part is optionally substituted with aryl), aromatic heterocycle group (which is optionally substituted with one to three substituents which are the same or different and are lower alkyl, hydroxy, lower alkoxy, carboxy, lower alkoxycarbonyl, amino, monoalkyl-substituted amino, dialkyl-substituted amino, nitro, sulfonamide, halogen, or trifluoromethyl), or aralkyl (where the aryl part of said aralkyl is optionally substituted with one to three substituents which are the same or different and are lower alkyl, lower alkoxy, dialkyl-s
REFERENCES:
patent: 4954498 (1990-09-01), Mertens et al.
patent: 5569658 (1996-10-01), Barker
J. Med. Chem., vol. 29, No. 6 (1986) 972-77.
J. Med. Chem., vol. 32, No. 10 (1989) 2247-54.
J. Org. Chem., vol. 51, No. 5 (1986) 616-20.
Ichimura Michio
Ishikawa Tomoko
Kase Hiroshi
Kinoshita Iwao
Machii Daisuke
Grumbling Matthew V.
Kyowa Hakko Kogyo Co. Ltd.
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