Benzoheterocyclic compounds and vasopressin antagonist and oxyto

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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Details

540593, 540594, 540476, A61K 3155, C07D22316

Patent

active

056229470

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to a vasopressin antagonist and oxytocin antagonist containing a benzoheterocyclic compound as an active ingredient.


BACKGROUND ART

Some of benzoheterocyclic compounds being used as the active ingredients in the vasopressin antagonists and oxytocin antagonists which are represented by the general formula (1) containing novel compounds.
Some benzohetrocyclic compounds having chemical structural formulae similar to those of benzoheterocyclic compounds according to the present invention are disclosed in EP-A-0382185 A2 (Publication Date: Aug. 15, 1990); WO 91/05549 (Publication Date: May 2, 1991) and EP-A-0470514A1 (Publication Date: Feb. 12, 1992). Furthermore, EP-A-0514667A1 (Publication Date: Nov. 25, 1992) discloses benzoheterocyclic compounds, and is known as the junior patent application of the present invention.
The substituents bonded at 1-position in the benzoheterocyclic compounds disclosed in these prior art references are substantially different from the substituents bonded at 1-position in the benzoheterocyclic compounds according to the present invention.


DISCLOSURE OF THE INVENTION

The benzoheterocyclic compounds or a salts thereof of the present invention are prepresented by the general formula (1) as follows: ##STR2## wherein, R.sup.1 is a hydrogen atom, a halogen atom, a hydroxyl group, a lower alkanoyloxy group, an amino-lower alkoxy group which may have the substituents selected from the group consisting of lower alkyl group and lower alkanoyl group, a carboxy-substituted lower alkoxy group, a lower alkoxycarbonyl-substituted lower alkoxy group, or an aminocarbonyl-lower alkoxy group which may have lower alkyl groups as the substituents; ##STR3## (wherein R.sup.6 and R.sup.7 are the same or different, and are each a hydrogen atom, a lower alkyl group, a lower alkenyl group or a benzoyl group having halogen atoms as the substituents on the phenyl ring), group of the formula: ##STR4## (wherein A is a lower alkylene group; or a lower alkyl group; further R.sup.8 and R.sup.9 may form a 5- to 6-membered saturated or unsaturated heterocyclic group by combining with the adjacent nitrogen atom being bonded thereto, together with or without other nitrogen atom or oxygen atom, said heterocyclic group may be substituted with lower alkyl groups), residue), alkoxycarbonyl-substituted lower alkyl group, a carboxy-substituted lower alkyl group, a group of the formula: ##STR5## (wherein A is the same as defined above; atom, a lower alkyl group which may have hydroxyl groups as the substituents, a piperidinyl group which may have phenyl-lower alkyl group on the piperidine ring, a carbamoyl-substituted lower alkyl group, a pyridyl-substituted lower alkyl group, a pyridyl group, ##STR6## (wherein A is a lower alkylene group; atom or a lower alkyl group which may have hydroxyl group as the substituents; heterocyclic group, by combining with the adjacent nitrogen atom being bonded thereto, together with or without other nitrogen atom or oxygen atom, said heterocyclic group may have lower alkyl groups on the heterocyclic ring), a pyrazinyl-substituted lower alkyl group which may have, as the substituents, lower alkyl groups on the pyrazine ring, pyrrolyl-substituted lower alkyl group which may have, as the substituents, lower alkyl groups on the pyrrole ring, a pyrrolidinyl-substituted lower alkyl group which may have, as the substituents, lower alkyl groups on the pyrrolidine ring, or a phenyl group which may have halogen atoms on the phenyl ring; heterocyclic group, by combining with the adjacent nitrogen atom being bonded thereto, together with or without other nitrogen atom or oxygen atom; said heterocyclic group may be substituted with a lower alkyl group, a lower alkoxycarbonyl group, an amino group which may have the substituents selected from the group consisting of a lower alkyl group and a lower alkanoyl group, a lower alkoxycarbonyl-substituted lower alkyl group, a phenyl group which may have halogen atoms on the phenyl ring, a cyano-substituted lo

REFERENCES:
patent: 3516987 (1970-06-01), Charles et al.
patent: 3542760 (1970-11-01), Charles et al.
patent: 5258510 (1993-11-01), Ogawa et al.

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