Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1983-06-03
1987-01-27
Rizzo, Nicholas S.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514252, 544238, 544239, C07D23704, A61K 3150
Patent
active
046394516
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to new substances, namely 6-(4-acylaminophenyl)-4,5-dihydro-3(2H)-pyridazinone derivatives.
Hitherto, dihydropyridazinone compounds, for example, 6-[p-(2-chloropropionylamino)-phenyl]-5-methyl-4,5-dihydropyridazone-(3) have known as substances possessing blood pressure depressing activity and platelets aggregation inhibiting activity (Japanese Laid-open Patent Appln. No. Sho-54-9289 referred to). These substances are recognized to be useful as medicaments for the remedy of diseases of circulatory organs, such as blood pressure depressing agents and anti-thrombotic agents. Development of further pharmacological usefulness is still expected for these substances.
The new pyridazinone derivatives concerned with the present invention are also new substances possessing pharmacological effects such as myocardial-contraction reinforcing activity in addition to blood pressure depressing activity and platelet aggregation inhibiting activity, and are very useful as medicaments for ciruclatory organs, such as blood pressure depressants, anti-thrombotic agents and medicines for the remedy of heart diseases, or as intermediates for these medicaments.
DISCLOSURE OF INVENTION
The present invention provides as new chemical substances pyridazinone derivatives of the general formula: ##STR5## [wherein R.sup.1 stands for a hydrogen atom or a lower alkyl group; R.sup.2 for a hydrogen atom or a lower alkyl group; and A for (i) a ring selected from a benzene ring, a furan ring, a thiophene ring and a pyridine ring (on which ring 1-3 substituents or atoms selected from amino groups, nitro groups, lower alkanoylamino groups, hydroxyl groups, lower alkanoyloxy groups, sulfamoyl groups and halogen atoms may be present), or (ii) a grouping of the formula: ##STR6## (wherein R.sup.3 stands for a hydrogen atom, a lower alkyl group, a phenyl(lower)alkyl, a hydroxyphenyl(lower)alkyl group, a lower alkylmercapto(lower)alkyl group, a benzylmercapto(lower)alkyl group, a guanidino(lower)alkyl group, a nitroguanidino(lower)alkyl group, an indolyl(lower)alkyl group, a carbamoyl(lower)alkyl group or a carboxy(lower)alkyl group, R.sup.4 for a hydrogen atom or a lower alkyl group, R.sup.5 for a hydrogen atom, a lower alkyl group, a lower alkanoyl group, a benzoyl or a benzyloxycarbonyl group, and R.sup.3 and R.sup.4 may be combined to form a grouping ##STR7## which forms a ring) or (iii) a grouping of the formula: ##STR8## (wherein R.sup.6, R.sup.7 and R.sup.8 each stand for a hydrogen atom or a lower alkyl group, B is an oxygen atom or a sulfur atom, R.sup.9 stands for a hydrogen atom or a lower alkanoyl group, and n is 0 or 1)].
In the definitions for each notation given for the above general formula (I), the lower alkyl group means an alkyl group with 1-4 carbon atoms. Mentioned, for example, are methyl, ethyl, propyl, isopropyl, n-butyl, isobutyl, secbutyl or tert.-butyl groups. Examples of the lower alkanoyl group in the definitions for each notation given above include formyl, acetyl, propanoyl and butanoyl groups.
In compounds of the general formula (I), those in which A stands for (i) can be prepared by reacting a compound of the general formula: ##STR9## (wherein R.sup.1 stands for a hydrogen atom or a lower alkyl group with 1-4 carbon atoms and R.sup.2 for a hydrogen atom or a lower alkyl group with 1-4 carbon atoms), thiophene ring and a pyridine ring (on which ring 1-3 substituents or atoms selected from amino groups, nitro groups, lower alkanoylamino groups, hydroxyl groups, lower alkanoyloxy groups, sulfamoyl groups and halogen atoms may be present)],
Examples of the carboxylic acid of the general formula (III) include salicylic acid, acetylsalicylic acid, m-hydroxybenzoic acid, p-hydroxybenzoic acid, o-acetylaminobenzoic acid, o-aminobenzoic acid, m-aminobenzoic acid, p-aminobenzoic acid, m-acetaminobenzoic acid, p-acetaminobenzoic acid, o-nitrobenzoic acid, m-nitrobenzoic acid, p-nitrobenzoic acid, p-chlorobenzoic acid, p-bromobenzoic acid, o-chlorobenzoic acid, o-bromobenzoic acid,
REFERENCES:
patent: 3806509 (1974-04-01), Lebkuecher et al.
patent: 4544562 (1985-10-01), Rossy et al.
Fukazawa Nobuyuki
Iizuka Hajime
Kamiya Joji
Katakami Tsutomu
Nakano Takuo
Mitsui Toatsu Kagaku-Kabushiki Kaisha
Rizzo Nicholas S.
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