Title:
ピペラジン化合物、その製造方法およびそれを含有する医薬組成物
Document Type and Number:
Japanese Patent JP4607809
Kind Code:
B2
Abstract:
Piperazine derivatives (I) and their optical isomers, and acid addition salts are new. Piperazine derivatives of formula (I) and their optical isomers, and acid addition salts are new. R 1-R 4H, halo, 1-6C alkyl, 1-6C alkoxy, phenyl or CN; X : a bond, O, -(CH 2) m-, -OCH 2- or -NR 5-; R 5H, 1-6C alkyl, COR 6 or CO 2R 6; R 61-6C alkyl; R 7H, COR 9 or 1-6C alkyl (optionally substituted 5-oxo-4,5-dihydro-1H-1,2,4-triazol-3-yl or 2,3-dihydro-1,4-benzodioxin-2-yl); R 91-6C alkyl or (hetero)aryl; R 8H or amino (optionally substituted by 1-2 groups of 1-6C alkyl); Z : N or CH; m, n : 1-2; Ak : 1-6C alkylene; Ar 1(hetero)aryl; and (MK12) Y = O, NR 7 or CHR 8. Aryl is phenyl, biphenyl or naphthyl, each of which is optionally substituted by halo, 1-6C (trihalo)alkyl, 1-6C (trihalo)alkoxy, OH or CN. Heteroaryl is 5-12 membered mono or bicyclic aromatic group, containing 1-2 O, N or S, and the heteroaryl is optionally substituted by halo, 1-6C (trihalo)alkyl, 1-6C alkoxy, OH or CN. An independent claim is included for the preparation of (I). [Image] ACTIVITY : Antidepressant; Tranquilizer; Antiaddictive; Anorectic; Eating-Disorders-Gen.; Analgesic; Antiinflammatory; Neuroleptic; Antiemetic; Gastrointestinal-Gen; Nootropic. MECHANISM OF ACTION : Serotonin receptor inhibitor; Neurokinine antagonist. The affinity of (I) for serotonin receptor was tested in frontal cortex membranes of rat. Trans-1-{2 [(3,5-dibromobenzyl)oxy]-2,3-dihydro-1H-inden-1yl}piperazine (IA) dihydrochloride exhibted a negative logarithm of inhibition constant value of 8.35.
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Inventors:
Jean-Louis Perillon
Aime desanges
Bertrand Guman
Marc Milan
Croctilde Manourie La Coeur
Aime desanges
Bertrand Guman
Marc Milan
Croctilde Manourie La Coeur
Application Number:
JP2006107151A
Publication Date:
January 05, 2011
Filing Date:
April 10, 2006
Export Citation:
Assignee:
Réra Bora Toir Servier
International Classes:
C07D211/22; A61K31/4465; A61K31/451; A61K31/453; A61K31/495; A61K31/496; A61K31/5375; A61K31/55; A61K31/551; A61P1/04; A61P1/08; A61P3/04; A61P25/00; A61P25/02; A61P25/04; A61P25/18; A61P25/22; A61P25/24; A61P25/28; A61P25/30; A61P29/00; A61P43/00; C07D213/81; C07D215/46; C07D239/02; C07D243/08; C07D249/12; C07D295/08; C07D295/14; C07D311/68; C07D313/08; C07D319/20; C07D405/04
Domestic Patent References:
| JP6179670A | ||||
| JP8325257A | ||||
| JP10279578A | ||||
| JP9502431A |
Foreign References:
| US6136824 |
Attorney, Agent or Firm:
Hajime Tsukuni
Fumio Shinoda
Fumio Shinoda