3,4-disubstituted phenylethanolaminotetralincarboxamide derivati

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

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Details

514620, 544165, 546206, 548540, 564165, 564172, A61K 31165, A61K 31535, C07C23506, C07D295192

Patent

active

061332666

DESCRIPTION:

BRIEF SUMMARY
TECHNICAL FIELD

The present invention relates to novel 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives which are useful as medicaments.
More particularly, the present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives represented by the general formula: ##STR2## (wherein A represents a lower alkylene group; B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may contain an oxygen atom in the ring; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof, which have a selective .beta..sub.2 -adrenergic receptor stimulating effect with relieved burdens on the heart such as tachycardia.


BACKGROUND ART

As substituted phenylethanolaminotetralin derivatives, compounds having gut selective sympathomimetic and anti-pollakiuria activities have been disclosed, e.g., a compound represented by the general formula: ##STR3## (wherein R.sup.a represents a hydrogen atom or an ethyl group), hydrochloride or oxalate thereof, or single optical isomers thereof; and a compound represented by the formula: ##STR4## (wherein the carbon atom marked with (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration) (cf. a published Japanese patent application (kohyo) No. Hei 6-506676 and a published Japanese patent application (kohyo) No. Hei 6-506955).
However, these compounds are .beta..sub.3 -adrenergic receptor stimulating agents having a remarkable .beta..sub.3 -adrenergic receptor stimulating effect.


DISCLOSURE OF INVENTION

The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives represented by the general formula: ##STR5## (wherein A represents a lower alkylene group; B represents an amino group, a di(lower alkyl)amino group or a 3 to 7-membered alicyclic amino group which may contain an oxygen atom in the ring; n is an integer of 1 or 2; the carbon atom marked with * represents a carbon atom in R configuration, S configuration or a mixture thereof; and the carbon atom marked with (S) represents a carbon atom in S configuration) and pharmaceutically acceptable salts thereof.
The present invention relates to a pharmaceutical composition comprising the above 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative or pharmaceutically acceptable salt thereof.
The present invention relates to an agent for the prevention of threatened abortion and premature labor, a bronchodilator and an agent for pain remission and stone removal in urolithiasis which comprises as the active ingredient the above 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative or pharmaceutically acceptable salt thereof.
The present invention relates to a method for the prevention of threatened abortion and premature labor, the prevention and treatment of diseases associated with bronchiostenosis and airway obstruction, and pain remission and stone removal in urolithiasis which comprises administering the above 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative or pharmaceutically acceptable salt thereof.
The present invention relates to a use of the above 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative or pharmaceutically acceptable salt thereof for the manufacture of a pharmaceutical composition for the prevention of threatened abortion and premature labor, the prevention and treatment of diseases associated with bronchiostenosis and airway obstruction, and pain remission and stone removal in urolithiasis.
Furthermore, the present invention relates to a use of the above 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative or pharmaceutically acceptable salt thereof as an agent for the prevention of threatened abortion and premature labor, a bronchodila

REFERENCES:
Tamai et al, Chemical Abstracts, vol. 130, No. 196510, 1999.

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