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1. WO1996002525 - NOVEL ARYL PIPERAZINE-DERIVED PIPERAZIDE DERIVATIVES, METHODS FOR THEIR PREPARATION, THEIR USE AS DRUGS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME

Publication Number WO/1996/002525
Publication Date 01.02.1996
International Application No. PCT/FR1995/000975
International Filing Date 20.07.1995
Chapter 2 Demand Filed 19.02.1996
IPC
C07D 295/185 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16acylated on ring nitrogen atoms
18by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
182Radicals derived from carboxylic acids
185from aliphatic carboxylic acids
C07D 295/205 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16acylated on ring nitrogen atoms
20by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
205Radicals derived from carbonic acid
C07D 295/215 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16acylated on ring nitrogen atoms
20by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
215Radicals derived from nitrogen analogues of carbonic acid
C07D 317/66 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
317Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
08having the hetero atoms in positions 1 and 3
44ortho- or peri-condensed with carbocyclic rings or ring systems
46condensed with one six-membered ring
48Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes, unsubstituted on the hetero ring
62with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to atoms of the carbocyclic ring
66Nitrogen atoms not forming part of a nitro radical
C07D 319/18 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
319Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
101,4-Dioxanes; Hydrogenated 1,4-dioxanes
14condensed with carbocyclic rings or ring systems
16condensed with one six-membered ring
18Ethylenedioxybenzenes, not substituted on the hetero ring
CPC
C07D 295/185
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16acylated on ring nitrogen atoms
18by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
182Radicals derived from carboxylic acids
185from aliphatic carboxylic acids
C07D 295/205
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16acylated on ring nitrogen atoms
20by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
205Radicals derived from carbonic acid
C07D 295/215
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
295Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2.] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
16acylated on ring nitrogen atoms
20by radicals derived from carbonic acid, or sulfur or nitrogen analogues thereof
215Radicals derived from nitrogen analogues of carbonic acid
C07D 317/66
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
317Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
08having the hetero atoms in positions 1 and 3
44ortho- or peri-condensed with carbocyclic rings or ring systems
46condensed with one six-membered ring
48Methylenedioxybenzenes or hydrogenated methylenedioxybenzenes unsubstituted on the hetero ring
62with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to atoms of the carbocyclic ring
66Nitrogen atoms not forming part of a nitro radical
C07D 319/18
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
319Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
101,4-Dioxanes; Hydrogenated 1,4-dioxanes
14condensed with carbocyclic rings or ring systems
16condensed with one six-membered ring
18Ethylenedioxybenzenes, not substituted on the hetero ring
Applicants
  • PIERRE FABRE MEDICAMENT [FR/FR]; 45, place Abel-Gance F-92100 Boulogne, FR (AllExceptUS)
  • HALAZY, Serge [BE/FR]; FR (UsOnly)
  • JORAND, Catherine [FR/FR]; FR (UsOnly)
  • PAUWELS, Peter [BE/FR]; FR (UsOnly)
Inventors
  • HALAZY, Serge; FR
  • JORAND, Catherine; FR
  • PAUWELS, Peter; FR
Agents
  • WARCOIN, Jacques; Cabinet Regimbeau 26, avenue Kléber F-75116 Paris, FR
Priority Data
94/0898120.07.1994FR
Publication Language French (FR)
Filing Language French (FR)
Designated States
Title
(EN) NOVEL ARYL PIPERAZINE-DERIVED PIPERAZIDE DERIVATIVES, METHODS FOR THEIR PREPARATION, THEIR USE AS DRUGS AND PHARMACEUTICAL COMPOSITIONS COMPRISING SAME
(FR) NOUVELLES PIPERAZIDES DERIVEES D'ARYL PIPERAZINE, LEURS PROCEDES DE PREPARATION, LEUR UTILISATION A TITRE DE MEDICAMENT ET LES COMPOSITIONS PHARMACEUTIQUES LES COMPRENANT
Abstract
(EN)
Novel 5HT receptor antagonists of general formula (I) in which Ar1 and Ar2 are an aromatic residue, X is O, NH, CH2O or CH2NH, R1 is hydrogen, a linear or branched alkyl chain comprising 1-6 carbon atoms. The invention also concerns the salts, hydrates, solvates and physiologically acceptable bioprecursors for their therapeutic use, their geometric and optic isomers and their mixtures in all proportions and in racemic form. Also disclosed are methods for the preparation of these novel antagonists, their use as drugs and pharmaceutical compositions comprising them.
(FR)
La présente invention concerne de nouveaux antagonistes des récepteurs 5HT, répondant à la formule générale (I) dans laquelle Ar1 et Ar2 représentent un résidu aromatique, X représente O, NH, CH2O ou CH2NH, R1 représente un hydrogène, une chaîne alkyle linéaire ou ramifiée comprenant de 1 à 6 atomes de carbone, et leurs sels, hydrates, solvates et bioprécurseurs physiologiquement acceptables pour leur usage thérapeutique, leurs isomères géométriques et optiques ainsi que leurs mélanges en toutes proportions et sous forme racémique. La présente invention concerne également leurs procédés de préparation, leur utilisation à titre de médicament et les compositions pharmaceutiques les comprenant.
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