Carbostyril compounds and compositions containing same

Details Carbostyril compounds and compositions containing same Carbostyril compounds and compositions containing same

1982-07-12

1983-11-08

Fan, Jane T.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

424258, C07D47104

Patent

active

044143907

DESCRIPTION:

BRIEF SUMMARY
BACKGROUND ART

This invention relates to certain carbostyril compounds and to pharmaceutically acceptable salts thereof which are useful as cardiotonic agents, processes for preparing the same, and pharmaceutical compositions containing the carbostyril compounds or salts thereof.
Various carbostyril compounds are known which have hypotensive, blood platelet coagulation inhibitory or antiallergic activity as described in Japanese Patent Application (OPI) Nos. 130589/79, 135785/79, 138585/79, 141785/79, 76872/80, 49319/80, 53283/80, 53284/80 and 83781/80 (the term "OPI" as used herein refers to a "published unexamined Japanese patent application").
Further, EP-A1-7525 and EP-A1-8014 describe isoquinoline compounds which have cardiac and circulatory activities.
However, the carbostyril compounds of this invention are structurally different from the conventional carbostyril and isoquinoline compounds.


DISCLOSURE OF THE INVENTION

One object of this invention is to provide carbostyril compounds having a cardiotonic activity.
Another object of this invention is to provide a pharmaceutical composition containing the carbostyril compound in a cardiotonically effective amount.
A further object of this invention is to provide a process for preparing a carbostyril compound and its pharmaceutically acceptable salts thereof.
As a result of extensive research, this invention has been accomplished which, in one aspect, provides a carbostyril compound of the formula (I) ##STR2## wherein R.sup.1 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group, a lower alkynyl group, or a phenyl-lower alkyl group;
R.sup.2 represents a hydrogen atom, a lower alkyl group, a lower alkoxy group, a halogen atom, or a hydroxy group;
R.sup.3 represents a hydrogen atom, a lower alkyl group, a halogen atom, a nitroso group, an amino group which may be substituted with a lower alkyl group, a lower alkanoylamino group, an N,N-di-lower alkylaminomethyl group, a carbamoylmethyl group, a cyanomethyl group, or a carboxymethyl group;
R.sup.4 and R.sup.5, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group, or a nitro group;
the bonding between the 3- and 4-positions of the carbostyril nucleus is a single bond or a double bond; and
the position at which the imidazopyridyl group of the formula ##STR3## is attached to the carbostyril nucleus is the 5- or 6-position;
with the proviso that when the imidazopyridyl group is attached to the 5-position of the carbostyril nucleus, R.sup.2 should not be a hydrogen atom, a lower alkyl group, or a halogen atom; or its pharmaceutically acceptable salt.
In another aspect, this invention provides a cardiotonic composition containing a compound of the formula (I) or a pharmaceutically acceptable salt thereof in a cardiotonically effective amount.
In a further aspect, this invention provides processes for preparing the compounds of the formula (I) and pharmaceutically acceptable salts thereof.


BEST MODE FOR CARRYING OUT THE INVENTION

The compounds of the formula (I) above and pharmaceutically acceptable salts thereof have heart muscle contraction stimulating effect or positive inotropic effect and coronary blood flow increasing activity, and are useful as a cardiotonic agent for treating heart diseases such as congestive heart failure and the like. They are advantageous in that they do not or only slightly, if any, increase heart beats.
The term "lower alkyl" as used herein refers to a straight or branched chain alkyl group having 1 to 6 carbon atoms such as a methyl group, an ethyl group, a propyl group, an isopropyl group, a butyl group, a tert-butyl group, a pentyl group, a hexyl group and the like.
The term "phenyl-lower alkyl" as used herein refers to a phenyl-lower alkyl group having a straight or branched chain alkyl group having 1 to 6 carbon atoms in the alkyl moiety such as a benzyl group, a 2-phenylethyl group, a 1-phenylethyl group, a 3-phenylpropyl group, a 4-phenylbutyl group, a 1,1-dimethyl

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