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Claims for Patent: 4,703,063

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Claims for Patent: 4,703,063

Title: Sulfamoyl substituted phenethylamine derivatives and process of producing them
Abstract:Novel sulfamoyl-substituted phenethylamine derivatives which exhibit .alpha.-adrenergic blocking action and are useful as an antihypertensive agent and an agent for the treatment of congestive heart failure.
Inventor(s): Imai; Kazuo (Saitama, JP), Niigata; Kunihiro (Saitama, JP), Fujikura; Takashi (Saitama, JP), Hashimoto; Shinichi (Chiba, JP), Takenaka; Toichi (Tokyo, JP)
Assignee: Yamanouchi Pharmaceutical Co., Ltd. (Tokyo, JP)
Application Number:06/756,790
Patent Claims: 1. Sulfamoyl-substituted phenethylamine derivatives represented by the general formula ##STR79## wherein R.sub.1 represents an amino group or a mono- or di-lower alkylamino group; R.sub.2 represents a hydroxyl group, a lower alkyl group, or a lower alkoxy group; R.sub.3 represents a hydrogen atom, a lower alkoxy group or a lower alkyl group; R.sub.4, R.sub.5, R.sub.6, R.sub.7, R.sub.8, and R.sub.9 each represents a hydrogen atom or a lower alkyl group; R.sub.10 represents a hydrogen atom, a lower alkyl group, or a lower alkoxy group; and Y represents an oxygen atom, and the salts thereof.

2. A pharmaceutical composition containing an effective .alpha.-adrenergic antagonistic amount of a compound of claim 1 and a pharmaceutically acceptable excipient.

3. The salts of the sulfamoyl-substituted phenethylamine derivatives as claimed in claim 1 wherein R.sub.3 is a lower alkyl group or a lower alkoxy group.

4. The compound of claim 1 wherein R.sub.3 is a hydrogen atom and the salts thereof.

5. The compound of claim 1 wherein R.sub.3 is a lower alkyl group and the salts thereof.

6. The compound of claim 1 which is a racemic compound.

7. The compound of claim 1 which is a mixture of racemic compounds.

8. The compound of claim 1 which is an optically active isomer.

9. The isomer of claim 8 which is the (+) isomer.

10. The isomer of claim 8 which is the (-) isomer.

11. The optically active isomers of the compound of claim 7.

12. The isomer of claim 11 which is the (+) isomer.

13. The isomer of claim 11 which is the (-) isomer.

14. The compound of claim 1 which is 5-{2-[2-(2-ethoxyphenoxy)ethylamino]-2-methylethyl}-2-methoxybenzenesulfon amide.

15. The compound of claim 1 which is 2-methoxy-5-{2-[2-(2-methoxyphenoxy)ethylamino]-2-methylethyl}benzenesulfo namide.

16. The compound of claim 1 which is 5-{2-[2-(2-methoxyphenoxy)ethylamino]-2-methylethyl}-2-methylbenzenesulfon amide.

17. The compound of claim 1 which is 5-{2-[2-(2-methoxyphenoxy)ethylamino]ethyl}-2-methylbenzenesulfonamide.

18. The compound of claim 1 which is 2-methoxy-5-{2-[2-(2-methoxyphenoxy)ethylamino]-2-methylethyl}-N-methylben zenesulfonamide.

19. The compound of claim 1 which is 2-methoxy-5-{2-[2-(2-methoxyphenoxy)ethylamino]-2-methylethyl}-N,N-dimethy lbenzenesulfonamide.
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