Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...
Patent
1999-03-08
2000-04-04
Geist, Gary
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Heterocyclic carbon compounds containing a hetero ring...
514319, 514424, 514620, 544168, 546206, 548540, 564134, A61K 31165, A61K 31445, A61K 31535, C07C23316, C07D295185
Patent
active
060461926
DESCRIPTION:
BRIEF SUMMARY
TECHNICAL FIELD
The present invention relates to novel phenylethanolaminotetralincarboxamide derivatives which are useful as medicaments.
More particularly, the present invention relates to 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; 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; and Y represents a hydrogen atom or a chlorine atom), the 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), which have gut selective sympathomimetic and antipollakiuria activities, have been disclosed (cf., published Japanese patent application (kohyo) No. Hei 6-506676 and 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 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; 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 phenylethanolaminotetralincarboxamide 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 phenylethanolaminotetralincarboxamide 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 phenylethanolaminotetralincarboxamide derivative or a pharmaceutically acceptable salt thereof.
The present invention relates to a use of the above phenylethanolaminotetralincarboxamide 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 present invention relates to a use of the above phenylethanolaminotetralincarboxamide derivative or a pharmaceutically acceptable salt thereof as 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.
BEST M
Kikuchi Ken
Kitazawa Makio
Kobayashi Hiroaki
Muranaka Hideyuki
Okazaki Kosuke
Geist Gary
Kissei Pharmaceutical Co. Ltd.
Solola Tadfiq A.
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