Phenoxypropanol connected with phenylpiperazine and phenoxyalkylamine terminal in its side chain

• US 20030055066A1
• Filed: 03/26/2002
• Published: 03/20/2003
• Est. Priority Date: 03/30/2001
• Status: Active Grant

• Current Assignee: Ing-Jun Chen, Tong-Ho Lin
• Original Assignee: Ing-Jun Chen, Tong-Ho Lin
• Inventors: Chen, Ing-Jun
• Granted Patent: US 6,846,826 B2
• Time in Patent Office: Days
• US Class Current: 514/253.13
• CPC Class Codes: C07D 213/80 in position 3

Abstract

The invention disclosed some 1,4-dihydropiridine derivative chemically have pharmacologically with adrenoceptor blocking and calcium channel blocker is now emerging.

The compound of 1,4-dihydropiridine derivative wherein has the formula I, wherein R selected from four group as follow

whetherin R present

R₁ selected from halogen(X), hydrogen(H), saturated C₁-C₆ alkyl chain, saturated C₁-C₆ alkyoxyl chain, R₂ selected from

R₃ selected from halogen(X), hydrogen(H), saturated C₁-C₆ alkyl chain, saturated C₁-C₆ alkyoxyl chain, and O—(C₁-C₃)—CF₃.

Claims

1. The 1,4-dihydropiridine derivative chemically with guaiacoxypropanolamine moiety, wherein has the formula I,

2. A 1,4-dihydropiridine derivative chemically with guaiacoxypropanolamine moiety according the claim 1, the said halogen is fluorine, chlorine, bromine and iodine.

3. A pharmaceutical compound which has competitive β

-adrenoreceptor, and using formula I as the main component, various diluents and excipients could be included when necessary.

4. A pharmaceutical compound which has β

-adrenoreceptor activity and calcium ion blocking agent, and using formula I as the main component, various diluents and excipients could be included when necessary.

5. A pharmaceutical compound which has continuously maintain hypotension activity, and using formula I as the main component, various diluents and excipients could be included when necessary.

6. A pharmaceutical compound which has vasorelaxing effect, and using formula I as the main component, various diluents and excipients could be included when necessary.

7. The manufacture method for prepared 1,4-dihydropiridine derivative compounds of formula I, by reaction vanillin or hydroxybenzaldehyde and ethanol under alkaline condition;

then epichlorohydrine is added for diffusion.

Upon reaction and pressurized reduction. The product are obtained through purification of silicone tubes. Then draw into aromatic amine groups, or halogenic phenyl piperazine at the four location aldehyde group of vanillin epoxide. As reaction with vanillin epoxide and methyl acetoacetate, come into being two hydroxyl aromatic group aldehyde at the Formula I.

8. The manufacture method for prepared 1,4-dihydropiridine derivative compounds of formula I according the claim 7, the aromatic amine groups selected from guaiacoxyethylamine, 2-(2-methylphenoxy)ethylamine,

2-(2-halophenoxy)ethylamine,

2-methylphenoxyethylamine,

(2-(2-nitrophenoxy)ethylamine, and

2-(2-trifluorophenoxy)ethylamine.

9. The manufacture method for prepared 1,4-dihydropiridine derivative compounds of formula I according the claim 7,

the aromatic amine groups selected from guaiacoxyethylamine,

2-(2-trifluoromethylphenoxy)ethylamine, (2-phenoxy)ethylamine, 2-methylphenoxyethylamine, and 2-Chlorophenoxyethylamine.