Novel piperazine or homopiperazine derivates, pharmaceutical compositions containing the same and a process for their preparation

Title:

Novel piperazine or homopiperazine derivates, pharmaceutical compositions containing the same and a process for their preparation

Document Type and Number:

WIPO Patent Application WO1997044334

Kind Code:

A3

Abstract:

The invention refers to novel piperazine and homopiperazine derivatives of formula (I) being suitable for the treatment of dieseases due to pathological alterations of the central nervous system, pharmaceutical compositions containing the above derivatives, and a process for the preparation of the novel compounds. In formula (I) R<1> stands for a halo, a C1-4 alkyl group, a C1-4 alkoxy group, a trihalomethyl group, a nitro group or an amino group which latter can be substituted by a C1-4 alkyl group, and n has a value of 1 or 2, or R<1> represents a cyano group, and n has a value of 2, m is 0, 1, 2 or 3, R<2>, R<3> and R<4> mean, independently, a hydrogen, a halo, a trihalomethyl group, a C1-4 alkyl group, a C1-4 alkoxy group, a nitro group, a carboxy group, a formyl group, a hydroxy group or an amino group which latter can be substituted by a C1-4 alkyl group.

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Inventors:

RATZNE SIMONEK ILDIKO (HU)
BOZSING DANIEL (HU)
JAKOCZI IVAN (HU)
KOVANYINE LAX GYORGYI (HU)
BLASKO GABOR (HU)
SIMIG GYULA (HU)
GACSALYI ISTVAN (HU)
SCHMIDT EVA (HU)
MIKLOSNE KAVACS ANIKO (HU)
SZIRTNE KISZELLY ENIKO (HU)
SZENASI GABOR (HU)
GYERTYAN ISTVAN (HU)
EGYED ANDRAS (HU)
TIHANYI KAROLY (HU)

Application Number:

PCT/HU1997/000020

Publication Date:

March 12, 1998

Filing Date:

May 15, 1997

Export Citation:

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Assignee:

EGYT GYOGYSZERVEGYESZETI GYAR (HU)
RATZNE SIMONEK ILDIKO (HU)
BOZSING DANIEL (HU)
JAKOCZI IVAN (HU)
KOVANYINE LAX GYORGYI (HU)
BLASKO GABOR (HU)
SIMIG GYULA (HU)
GACSALYI ISTVAN (HU)
SCHMIDT EVA (HU)
MIKLOSNE KOVACS ANIKO (HU)
SZIRTNE KISZELLY ENIKO (HU)
SZENASI, GABOR (HU)
GYERTYAN, ISTVAN (HU)
EGYED, ANDRAS (HU)
TIHANYI, KAROLY (HU)

International Classes:

C07D243/08; C07D295/096; C07D295/135; C07D295/155; C07D295/185; (IPC1-7): C07D295/02; A61K31/495; C07D243/08; A61K31/55; C07D295/06; C07D295/08; C07D295/12; C07D295/14; C07D295/18

Domestic Patent References:

WO1993000313A2

1993-01-07

Foreign References:

GB2057441A	1981-04-01
EP0556889A1	1993-08-25
US4139621A	1979-02-13
EP0650964A1	1995-05-03
EP0711763A1	1996-05-15

Other References:

MOKROSZ J L ET AL: "Structure-activity relationship studies of central nervous system (CNS) agents. 5. Effect of the hydrocarbon chain on the affinity of 4-substituted 1-(3-chlorophenyl)piperazines for 5-HT1A receptor sites", J. MED. CHEM. (JMCMAR,00222623);92; VOL.35 (13); PP.2369-74, POL. ACAD. SCI.;INST. PHARMACOL.; KRAKOW; 31-343; POL. (PL), XP002041900
CHEMICAL ABSTRACTS, vol. 77, no. 7, 14 August 1972, Columbus, Ohio, US; abstract no. 48507n, HASEGAWA: "1-m-Trifluoromethylphenyl-4-arylpiperazines" XP002041903
MOKROSZ ET AL.: "Quantitative analysis of the alkyl chain effects on the 5-HT1a and 5-HT2 receptor affinities of 4-alkyl-1-arylpiperazines and their analogs", ARCH. PHARM., vol. 328, no. 2, February 1995 (1995-02-01), pages 143 - 148, XP002041901
GLENNON ET AL.: "Novel 1-phenylpiperazine and 4-phenylpiperidine derivatives as high affinity sigma ligands", J.MED.CHEM., vol. 34, 1991, pages 3360 - 3365, XP002041902

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