AR052258A1 - DERIVATIVES OF PHENYLPIPERAZINES WITH A COMBINED AFFINITY FOR DOPAMINE - D2 RECEPTORS AND SEROTONINE REABSORTION SITES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE AS MEDICINES FOR THE TREATMENT OF NERVIO SYSTEMS. - Google Patents

DERIVATIVES OF PHENYLPIPERAZINES WITH A COMBINED AFFINITY FOR DOPAMINE - D2 RECEPTORS AND SEROTONINE REABSORTION SITES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE AS MEDICINES FOR THE TREATMENT OF NERVIO SYSTEMS.

Info

Publication number
AR052258A1
AR052258A1 ARP050105090A ARP050105090A AR052258A1 AR 052258 A1 AR052258 A1 AR 052258A1 AR P050105090 A ARP050105090 A AR P050105090A AR P050105090 A ARP050105090 A AR P050105090A AR 052258 A1 AR052258 A1 AR 052258A1
Authority
AR
Argentina
Prior art keywords
dopamine
receptors
derivatives
unbranched
branched
Prior art date
Application number
ARP050105090A
Other languages
Spanish (es)
Inventor
Hes Roelof Van
Pieter Smid
Cornelis G Kruse
Martinus Th M Tulp
Original Assignee
Solvay Pharm Bv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Solvay Pharm Bv filed Critical Solvay Pharm Bv
Publication of AR052258A1 publication Critical patent/AR052258A1/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D319/00—Heterocyclic compounds containing six-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D319/10—1,4-Dioxanes; Hydrogenated 1,4-dioxanes
    • C07D319/14—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems
    • C07D319/16—1,4-Dioxanes; Hydrogenated 1,4-dioxanes condensed with carbocyclic rings or ring systems condensed with one six-membered ring
    • C07D319/18—Ethylenedioxybenzenes, not substituted on the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic 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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with 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 ring carbon atoms
    • C07D215/38—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • C07D263/54—Benzoxazoles; Hydrogenated benzoxazoles
    • C07D263/58—Benzoxazoles; Hydrogenated benzoxazoles with 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 in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
    • C07D265/34—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings
    • C07D265/36—1,4-Oxazines; Hydrogenated 1,4-oxazines condensed with carbocyclic rings condensed with one six-membered ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic 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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic 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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D295/00—Heterocyclic 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
    • C07D295/04—Heterocyclic 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 with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/12—Heterocyclic 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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms
    • C07D295/125—Heterocyclic 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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings
    • C07D295/13—Heterocyclic 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 with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by singly or doubly bound nitrogen atoms with the ring nitrogen atoms and the substituent nitrogen atoms attached to the same carbon chain, which is not interrupted by carbocyclic rings to an acyclic saturated chain
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/78—Benzo [b] furans; Hydrogenated benzo [b] furans
    • C07D307/82—Benzo [b] furans; Hydrogenated benzo [b] furans with 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 carbon atoms of the hetero ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/06—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2
    • C07D311/08—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring
    • C07D311/18—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring with oxygen or sulfur atoms directly attached in position 2 not hydrogenated in the hetero ring substituted otherwise than in position 3 or 7
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D321/00—Heterocyclic compounds containing rings having two oxygen atoms as the only ring hetero atoms, not provided for by groups C07D317/00 - C07D319/00
    • C07D321/02—Seven-membered rings
    • C07D321/10—Seven-membered rings condensed with carbocyclic rings or ring systems

Abstract

Derivados de fenilpiperazina con un doble modo de accion, inhibicion de la reabsorcion de la serotonina y afinidad para receptores de dopamina-D2. Uso de estos compuestos para la fabricacion de un medicamento que tiene un efecto beneficioso para el SNC. Reivindicacion 1: Compuestos de fenilpiperazina, caracterizados por la formula general (1) donde: m y n son independientemente 1, 2, 3, 4, 5, 6, 7 u 8; x es 0, 1, 2 o 3, R2 es halogeno, alquilo C1-6 ramificado o no ramificado, fenilo, bencilo, alcoxi C1-6 ramificado o no ramificado, trifluorometilo o ciano; R3 y R4 representan independientemente H, alquilo C1-6, fenilo, bencilo o acetilo; el grupo Q se selecciona entre los fragmentos estructurales A-N donde: y es 1, 2 o 3; R1 es halogeno, alquilo C1-6 ramificado o no ramificado, fenilo, bencilo, alcoxi C1-6 ramificado o no ramificado, trifluorometilo o ciano; y los tautomeros, estereoisomeros y N-oxidos de los mismos, como así también las sales, hidratos y solvatos farmacologicamente aceptables de dichos compuestos de formula (1) y sus tautomeros, estereoisomeros y N-oxidos.Phenylpiperazine derivatives with a double mode of action, inhibition of serotonin reabsorption and affinity for dopamine-D2 receptors. Use of these compounds for the manufacture of a medicament that has a beneficial effect on the CNS. Claim 1: Phenylpiperazine compounds, characterized by the general formula (1) wherein: m and n are independently 1, 2, 3, 4, 5, 6, 7 or 8; x is 0, 1, 2 or 3, R2 is halogen, branched or unbranched C1-6 alkyl, phenyl, benzyl, branched or unbranched C1-6 alkoxy, trifluoromethyl or cyano; R3 and R4 independently represent H, C1-6 alkyl, phenyl, benzyl or acetyl; group Q is selected from structural fragments A-N where: y is 1, 2 or 3; R1 is halogen, branched or unbranched C1-6 alkyl, phenyl, benzyl, branched or unbranched C1-6 alkoxy, trifluoromethyl or cyano; and the tautomers, stereoisomers and N-oxides thereof, as well as the pharmacologically acceptable salts, hydrates and solvates of said compounds of formula (1) and their tautomers, stereoisomers and N-oxides.

ARP050105090A 2004-12-07 2005-12-06 DERIVATIVES OF PHENYLPIPERAZINES WITH A COMBINED AFFINITY FOR DOPAMINE - D2 RECEPTORS AND SEROTONINE REABSORTION SITES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE AS MEDICINES FOR THE TREATMENT OF NERVIO SYSTEMS. AR052258A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP04106350 2004-12-07

Publications (1)

Publication Number Publication Date
AR052258A1 true AR052258A1 (en) 2007-03-07

Family

ID=34930004

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP050105090A AR052258A1 (en) 2004-12-07 2005-12-06 DERIVATIVES OF PHENYLPIPERAZINES WITH A COMBINED AFFINITY FOR DOPAMINE - D2 RECEPTORS AND SEROTONINE REABSORTION SITES, PHARMACEUTICAL COMPOSITIONS CONTAINING THEM AND THEIR USE AS MEDICINES FOR THE TREATMENT OF NERVIO SYSTEMS.

Country Status (14)

Country Link
EP (1) EP1828161A2 (en)
JP (1) JP2008523026A (en)
KR (1) KR20070091646A (en)
CN (1) CN101072765A (en)
AR (1) AR052258A1 (en)
AU (1) AU2005313386A1 (en)
BR (1) BRPI0518370A2 (en)
CA (1) CA2587928A1 (en)
MX (1) MX2007006756A (en)
RU (1) RU2007125636A (en)
SA (1) SA05260389B1 (en)
TW (1) TW200633987A (en)
WO (1) WO2006061372A2 (en)
ZA (1) ZA200704151B (en)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8106056B2 (en) 2006-06-16 2012-01-31 Solvay Pharmaceuticals B.V. Combination preparations comprising bifeprunox and a dopamine agonist
US8063062B2 (en) 2006-12-20 2011-11-22 Solvay Pharmaceuticals B.V. Compounds with a combination of cannabinoid-CB1 antagonism and acetylcholinesterase inhibition
US8138174B2 (en) 2007-01-10 2012-03-20 Solvay Pharmaceuticals B.V. Compounds with a combination of cannabinoid CB1 antagonism and serotonin reuptake inhibition
JP2010515704A (en) * 2007-01-10 2010-05-13 ソルベイ・フアーマシユーチカルズ・ベー・ブイ Compound exhibiting a combination of cannabinoid-CB1 antagonism and serotonin reuptake inhibition
WO2009090177A1 (en) * 2008-01-15 2009-07-23 Solvay Pharmaceuticals B.V. Bifeprunox derivatives

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2162312B1 (en) * 1971-12-10 1975-02-07 Buzas Andre
EP0189612B1 (en) * 1984-12-21 1992-11-04 Duphar International Research B.V New pharmaceutical compositions having a psychotropic activity
CN1155596C (en) * 1999-08-23 2004-06-30 索尔瓦药物有限公司 New phenylpiperazines
AR032712A1 (en) * 2001-02-21 2003-11-19 Solvay Pharm Bv A MESILATE OF PHENYLPIPERAZINE DERIVATIVES AND PHARMACEUTICAL COMPOSITIONS CONTAINING IT

Also Published As

Publication number Publication date
WO2006061372A2 (en) 2006-06-15
BRPI0518370A2 (en) 2008-11-18
JP2008523026A (en) 2008-07-03
TW200633987A (en) 2006-10-01
CA2587928A1 (en) 2006-06-15
MX2007006756A (en) 2007-11-09
WO2006061372A3 (en) 2006-11-23
KR20070091646A (en) 2007-09-11
ZA200704151B (en) 2008-08-27
RU2007125636A (en) 2009-01-20
CN101072765A (en) 2007-11-14
EP1828161A2 (en) 2007-09-05
AU2005313386A1 (en) 2006-06-15
SA05260389B1 (en) 2009-06-09

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