Patent EA-002143-B1 (EA)
Title: 3,4-disubstituted phenylethanolaminotetralincarboxamide derivatives
Inventor: KITAZAWA MAKIO
IPC: C07C235/06
Filed: 1997-02-18
Abstract: 1. A 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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 a pharmaceutically acceptable salt thereof. 2. A 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative as claimed in claim 1, represented by the general formula:   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 (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration; and a pharmaceutically acceptable salt thereof. 3. The 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative as claimed in claim 2 , represented by the formula:   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; and a pharmaceutically acceptable salt thereof. 4. A pharmaceutical composition which comprises a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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; and a pharmaceutically acceptable salt thereof. 5. A pharmaceutical composition, which comprises a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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 or a pharmaceutically acceptable salt thereof. 6. A pharmaceutical composition as claimed in claim 5, which comprises a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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 (R) represents a carbon atom in R configuration; and the carbon atom marked with (S) represents a carbon atom in S configuration; or a pharmaceutically acceptable salt thereof. 7. A pharmaceutical composition as claimed in claim 6, the 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the formula:   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; or a pharmaceutically acceptable salt thereof. 8. A pharmaceutical composition as claimed in claim 6, the 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the formula:   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; or a pharmaceutically acceptable salt thereof. 9. An agent for the prevention of threatened abortion and premature labor containing, as an active ingredient, a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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; or a pharmaceutically acceptable salt thereof. 10. A bronchodilator containing, as an active ingredient, a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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; or a pharmaceutically acceptable salt thereof. 11. An agent for pain remission and stone removal in urolithiasis containing, as an active ingredient, a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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; or a pharmaceutically acceptable salt thereof. 12. An agent for the prevention of threatened abortion and premature labor or a agent for the treatment of diseases associated with bronchiostenosis and airway obstruction or an agent for pain remission and stone removal in urolithiasis as claimed in any of claims 9 to 11, containing, as an active ingredient, a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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; or a pharmaceutically acceptable salt thereof. 13. An agent for the prevention of threatened abortion and premature labor, an agent for the treatment of diseases associated with bronchiostenosis and airway obstruction or an agent for pain remission and stone removal in urolithiasis urolithiasis as claimed in any of claims 9 to 11, containing, as an active ingredient, a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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 ; or a pharmaceutically acceptable salt-thereof. 14. An agent for the prevention of threatened abortion and premature labor, an agent for for the treatment of diseases associated with bronchiostenosis and airway obstruction bronchodilator and an agent for pain remission and stone removal in urolithiasis urolithiasis as claimed in any of claims 9 to 11, containing, as an active ingredient, a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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 ; or a pharmaceutically acceptable salt-thereof. 15. 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 a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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; or a pharmaceutically acceptable salt thereof. 16. A use of a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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; 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 stone removal in urolithiasis. 17. A use of a 3,4-disubstituted phenylethanolaminotetralincarboxamide derivative represented by the general formula:   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 * represe