3-(piperid-4-yl)-1,2-benzisoxazole and 3-(piperazin-4-yl)-1,2-benzisoxazole compounds

• US 5,780,474 A
• Filed: 06/03/1997
• Issued: 07/14/1998
• Est. Priority Date: 06/04/1996
• Status: Expired due to Fees

• Current Assignee: Les Laboratoires Servier (Servier Sas)
• Original Assignee: Adir SA
• Inventors: Millan, Mark, Peglion, Jean-Louis, Audinot, Valerie, Brocco, Mauricette
• Primary Examiner(s): BERNHARDT, EMILY A
• Application Number:
  US08/868,116
• Time in Patent Office: 406 Days
• Field of Search: 544/368, 544/295, 544/316, 546/198, 514/254, 514/321
• US Class Current: 514/252.19
• CPC Class Codes: A61P 25/18 Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
• CPC Class Codes: A61P 25/20 Hypnotics; Sedatives
• CPC Class Codes: A61P 43/00 Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
• CPC Class Codes: C07D 413/12 linked by a chain containing hetero atoms as chain links
• CPC Class Codes: C07D 413/14 containing three or more hetero rings

Abstract

Compounds of formula: ##STR1## wherein: A, m, n, E and Y are as defined in the description, the optical isomers thereof and the physiologically-tolerable salts thereof.

These compounds, their optical isomers and their physiologically-tolerable salts, can be used as medicaments in the treatment of psychotic disorders, anxio-depressive disorders, and aggressiveness.

Claims

1. A compound selected from the group consisting of 1,2-Benzisoxazole compounds of formula I ##STR7## wherein:

A is selected the group consisting of linear and branched alkyl having from 1 to 10 carbon atoms inclusive, unsubstituted phenyl, halophenyl, hydroxyphenyl, and (lower alkoxy)phenyl,

m is selected from zero and 1,

n is selected from 1 and 2,

E is selected from the group consisting of N and CH, and

Y is selected the group consisting of hydrogen, halogen, and alkoxy having from 1 to 5 carbon atoms inclusive,

optical isomers thereof, and addition salts thereof with a pharmaceutically-acceptable acid.

2. A compound of claim 1 which is 1-{2- 4-(6-fluoro-1,2-benzisoxazol-3-yl)piperazin-1-yl!ethyl}-3-isopropylimidazolidin-2-one.

3. A compound of claim 1 selected from the group consisting of 1-{2- 4-(6-fluoro-1,2-benzisoxazol-3-yl)piperazin-1-yl!ethyl}-3-ethylimidazolidin-2-one and the hydrochloride thereof.

4. A compound of claim 1 which is 1-{2- 4-(6-fluoro-1,2-benzisoxazol-3-yl)piperid-1-yl!ethyl}-3-phenylimidazolidin-2-one.

5. A method for treating a living animal body afflicted with a condition selected from schizophrenia, anxiety, depression, and aggressiveness, comprising the step of administering to the said living animal body an amount of a compound of claim 1 which is effective for alleviation of said condition.

6. A pharmaceutical composition useful for treating schizophrenia, anxiety, depression, or aggressiveness, comprising as active ingredient a compound according to claim 1 together with one or more appropriate pharmaceutical excipients.