Use of 1,4-disubstituted-piperidinyl compounds in the manufacture of a medicament for the treatment of insomnia

• US 4,908,369 A
• Filed: 01/19/1989
• Issued: 03/13/1990
• Est. Priority Date: 01/21/1988
• Status: Expired due to Term

• Current Assignee: Aventis Incorporated (Sanofi )
• Original Assignee: Merrell Pharmaceuticals Incorporated (Dow, Inc.)
• Inventors: Hinze, Christian K., Schechter, Paul J., Orwin, John M.
• Primary Examiner(s): Friedman, Stanley J.
• Application Number:
  US07/299,913
• Time in Patent Office: 418 Days
• Field of Search: 514/277
• US Class Current: 514/277
• CPC Class Codes: A61K 31/445 Non condensed piperidines, e.g. piperocaine
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives

Abstract

The present invention pertains to the use of 1,4-disubstituted-piperidinyl compounds in the treatment of insomnia.

Said compounds have the following general formula: ##STR1## wherein: each of R¹, R², R³, and R⁴ is independently selected from the group consisting of hydrogen, a C_1-6 alkyl group, halogen, trifluoromethyl, hydroxy, a C_1-6 alkoxy group, or an amino group; n is 2, 3, or 4; and the pharmaceutically acceptable acid addition salts thereof.

Claims

1. A method for the treatment of insomnia comprising administering to a patient suffering from insomnia, a hypnotic quantity of a compound of the formula:

##STR3## wherein n is 2, 3, or 4, each of R¹, R², and R⁴ is independently selected from hydrogen, halogen, trifluoromethyl, C_1-6 alkyl, C_1-16 alkoxy, hydroxy or amino;

or a pharmaceutically acceptable acid addition salt thereof.

2. A method according to claim 1 wherein said compound is α

-phenyl-1-(2-phenethyl)-4-piperidine methanol.

3. A method according to claim 1 wherein said compound is α

-phenyl-1-(3-phenpropyl)-4-piperidine methanol.

4. A method according to claim 1 wherein said compound is α

-(4-methylphenyl)-1-(2-phenethyl)-4-piperidine methanol.

5. A method according to claim 1 wherein said compound is α

-(4-methoxyphenyl)-1-(2-phenethyl)-4-piperidine methanol.

6. A method according to claim 1 wherein said compound is α

-(3,5-dimethylphenyl)-1-(2-phenethyl)-4-piperidine methanol.

7. A method according to claim 1 wherein said compound is α

-(3-(trifluoromethyl)phenyl)-1-(2-phenethyl)-4-piperidine methanol.

8. A method according to claim 1 wherein said compound is α

-(2,3-dimethoxyphenyl)-1-(2-phenethyl)-4-piperidine methanol.

9. A method according to claim 1 wherein said compound is α

-(4-fluorophenyl)[1-(2-phenylethyl)-4-piperidinyl]-methanol.

10. A method according to claim 1 wherein said compound is α

-phenyl-[1-(4-phenylbutyl)-4-piperidinyl]-methanol.

11. A method according to claim 1 wherein said compound is α

-(3,4-dimethoxyphenyl-[1-(2-phenylethyl)-4-piperidinyl]-methanol.

12. A method according to claim 1 wherein said compound is α

-phenyl-[1-(4-aminophenylethyl)-4-piperidinyl]-methanol.

13. A method according to claim 1 wherein said compound is α

-phenyl-[1-(4-methoxyphenylethyl)-4-piperidinyl]-methanol.

14. A method according to claim 1 wherein said compound is α

-(4-methoxyphenyl)-[1-(4-methoxyphenylethyl)-4-piperidinyl]-methanol.

15. A method according to claim 1 wherein said compound is α

-(2,3-dimethoxyphenyl)-[1-(4-methoxyphenyl-ethyl)]-4-piperidinyl]-methanol.

16. A method according to claim 1 wherein said compound is α

-phenyl-[1-(4-methoxyphenylethyl-4-piperidinyl]-methanol.

17. A method according to claim 1 wherein said compound is α

-phenyl-[1-(4-fluorophenylethyl)-4-piperidinyl]-methanol.

18. A method according to claim 1 wherein said compound is α

-(4-hydroxyphenyl)-[1-(2-phenylethyl)-4-piperidinyl]-methanol.

19. A method according to claim 1 wherein said compound is α

-(3,4-dihydroxyphenyl)-[1-(2-phenylethyl)-4-piperidinyl]-methanol, and

20. A method according to claim 1 wherein said compound is α

-(3,4-dichlorophenyl)-1-(2-phenylethyl)-4-piperidine methanol.