Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1988-11-18
1990-10-23
Shah, Mukund J.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
544234, 549 32, A61K 3150, C07D49504
Patent
active
049652648
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
This invention relates to moriel thienocinnoline compounds and their pharmaceutical use.
BACKGROUND ART
Benzodiazepine (BZP) derivatives represented by diazepam have been used for a long time as an antianxiety drug or a therapeutic medicine for sleep disturbance. Recent pharmacological studies have shown that there exist receptors which exhibit a specific affinity for BZP derivatives in the central nervous system [Science, vol. 198, 849 (1977)]. In the studies and researches conducted subsequently, there have been investigated and developed not only BZP derivatives but also compounds which have structures different from BZP but exhibit a high affinity for BZP receptors and a BZP-like action (BZP agonist), compounds which exhibit a high affinity for BZP receptors but exhibit a pharmacological action reverse to BZP (BZP inverse-agonist), and compounds which exhibit a high affinity for BZP receptors but nevertheless exhibit no pharmacological activity themselves and rather show an antagonistic action against the action of the agonist or the inverseagonist (BZP antagonist) [Advance in Drug Research, vol. 14, 165 (1985)].
Since BZP derivatives which are used as an antianxiety drug have a sedative action, a muscle-relaxing action and an anticonvulsive action in addition to an antianxiety action, they often cause troubles in terms of side effects such as dizziness and sleepiness. Thus, research on non-BZP types of compounds with the object of developing selective antianxiety drugs with less side effects is thriving. Nevertheless, satisfactory compounds have not yet been found.
Also, in recent years, amnesia-inducing actions by BZP agonists were found [Nature, vol. 321, 864 (1986)], and there have been reports suggesting the possibility that BZP-antagonists exhibiting an antagonistic action against the amnesic actions induced by BZP agonists and BZP-inverse-agonists exhibiting an action reverse to the amnesic actions by BZP agonists are usable as brain-function activating drugs. [Trends in Neurosciences, vol. 11, 13 (1988)].
In the meantime, in the specification of U.S. Pat. No. 4,602,019 there are disclosed compounds such as 2,4,4a,5-tetra-hydro-7-(1H-imidazol-1-yl)-3H-indeno[1,2-c]pyridazin-3-one having a cardiac action and an antihypertensive action. The Journal of Medicinal Chemistry, vol. 24, 830 (1981) discloses compounds such as 2-(4-chlorophenyl)benzothiopyrano-[4,3-pyrazol-3-one possessing an immune-supressing action.
DISCLOSURE OF INVENTION
The present inventors have conducted intensive studies for the purpose of developing BZP-agonists, BZP-inverse-agonists or BZP-antagonists having a non-BZP-nucleus which are useful pharmaceuticals.
It has been found that the above-mentioned purpose can be attained according to the present invention described hereinafter.
That is, the first aspect of the invention is to provide thienocinnoline compounds of the general formula ##STR2## wherein R stands for hydrogen, a halogen or a lower alkyl, Ar stands for an aryl, a heteroaryl, or an aryl or a heteroaryl having as a substituent at least a halogen, a lower alkyl, a lower alkoxy, nitro, amino, hydroxy, trifluoromethyl and/or a lower alkanoylamino; and the bond between 5a-position and 6-position represents a single bond or a double bond.
The second aspect of the invention is to provide pharmaceutical compositions comprising a thienocinnoline compound of the above general formula (I).
The symbols of the general formula (I) and each of the below-mentioned general formulae are defined in detail below. The halogen represents chlorine, bromine, fluorine or the like; the lower alkyl represents an alkyl having 1 to 4 carbon atom(s) such as methyl, ethyl, propyl, isopropyl, butyl, isobutyl or tert-butyl; the lower alkoxy represents an alkoxy having 1 to 4 carbon atom(s) such as methoxy, ethoxy, propoxy, isopropoxy butoxy, isobutoxy or tertbutoxy; the lower alkanoylamino represents an alkanoylamino having 2 to 5 carbon atoms such as acetylamino, propionylamino, butyrylamino or pivaloylamino; the aryl repres
REFERENCES:
patent: 4701453 (1987-10-01), Sircar et al.
patent: 4843075 (1989-06-01), Nakao et al.
patent: 4849421 (1989-07-01), Nakao et al.
Derwent Abstract for JP 64/6278 (1/10/89).
Hisadome Masao
Morita Kenji
Nakao Toru
Takehara Shuzo
Bernhardt F.
Shah Mukund J.
Yoshitomi Pharmaceutical Industries Ltd.
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