Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Ester doai
Patent
1999-03-08
2000-10-24
Richter, Johann
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Ester doai
514532, 514543, 514569, 514570, 514571, 560 56, 560 60, 560 61, 560 75, 562466, 562470, 562471, 562478, A61K 31215, A61K 3119, C07C 6976, C07C 6206
Patent
active
061368520
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to novel 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives which are useful as medicaments.
More particularly, the present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR2## [wherein Q represents a vinylene group or a group represented by the general formula: integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; 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, for example, compounds 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 which have gut selective sympathomimetic and anti-pollakiuria activities have been disclosed (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.
In addition, compounds represented by the general formula: ##STR4## (wherein Q.sup.1 represents an ethylene group or a vinylene group; and R.sup.a has the same meaning as defined above) or single optical isomers thereof which have antidepressant and intestine specific motility modulating activities and are useful as antidepressant and intestinal spasmolytic agents have been disclosed (cf. a published Japanese patent application (kokai) No. Hei 5-65254).
DISCLOSURE OF INVENTION
The present invention relates to 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivatives represented by the general formula: ##STR5## [wherein Q represents a vinylene group or a group represented by the general formula: integer of from 1 to 6); R represents a hydrogen atom or a lower alkyl group; 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 phenylethanolaminotetralincarboxylic acid derivative or a 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 promoting stone removal in urolithiasis which comprises as the active ingredient the above 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivative or a 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 promoting stone removal in urolithiasis which comprises administering the above 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivative or a pharmaceutically acceptable salt thereof.
The present invention relates to a use of the above 3,4-disubstituted phenylethanolaminotetralincarboxylic acid derivative or a 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 promoting stone removal in urolithiasis.
Furthermore, the pr
Kikuchi Ken
Kitazawa Makio
Kobayashi Hiroaki
Muranaka Hideyuki
Okazaki Kosuke
Keys Rosalynd
Kissei Pharmaceutical Co. Ltd.
Richter Johann
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