ES2125206A1 - Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos. - Google Patents

Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos.

Info

Publication number
ES2125206A1
ES2125206A1 ES09701627A ES9701627A ES2125206A1 ES 2125206 A1 ES2125206 A1 ES 2125206A1 ES 09701627 A ES09701627 A ES 09701627A ES 9701627 A ES9701627 A ES 9701627A ES 2125206 A1 ES2125206 A1 ES 2125206A1
Authority
ES
Spain
Prior art keywords
derivative
acyl
derivatives
reacting
compounds
Prior art date
Legal status (The legal status 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 status listed.)
Granted
Application number
ES09701627A
Other languages
English (en)
Other versions
ES2125206B1 (es
Inventor
Jordi Corbera-Arjona
David Vano-Domenech
Jordi Frigola-Constansa
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Esteve Pharmaceuticals SA
Original Assignee
Laboratorios del Dr Esteve SA
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 Laboratorios del Dr Esteve SA filed Critical Laboratorios del Dr Esteve SA
Priority to ES009701627A priority Critical patent/ES2125206B1/es
Priority to ARP980103475A priority patent/AR017254A1/es
Priority to CO98040807A priority patent/CO5011090A1/es
Priority to TW087111649A priority patent/TW530056B/zh
Priority to ZA986437A priority patent/ZA986437B/xx
Priority to KR10-2000-7000602A priority patent/KR100514148B1/ko
Priority to PCT/ES1998/000212 priority patent/WO1999005121A1/es
Priority to GEAP19985226A priority patent/GEP20033090B/en
Priority to EP98933660A priority patent/EP1006110B8/en
Priority to BR9810772-0A priority patent/BR9810772A/pt
Priority to IN1272CA1998 priority patent/IN183820B/en
Priority to US09/462,880 priority patent/US6372746B1/en
Priority to AU83403/98A priority patent/AU744633B2/en
Priority to DK98933660T priority patent/DK1006110T3/da
Priority to EEP200000037A priority patent/EE04151B1/xx
Priority to PT98933660T priority patent/PT1006110E/pt
Priority to HU0002517A priority patent/HUP0002517A3/hu
Priority to CNB988084589A priority patent/CN1202087C/zh
Priority to RU2000104007/04A priority patent/RU2205827C2/ru
Priority to NZ502400A priority patent/NZ502400A/en
Priority to SK72-2000A priority patent/SK284675B6/sk
Priority to SI9820053A priority patent/SI20269B/sl
Priority to PL98338143A priority patent/PL195632B1/pl
Priority to ES98933660T priority patent/ES2216297T3/es
Priority to DE69821623T priority patent/DE69821623T2/de
Priority to AT98933660T priority patent/ATE259357T1/de
Priority to CA002297417A priority patent/CA2297417C/en
Priority to JP2000504120A priority patent/JP2001510831A/ja
Priority to UA2000010370A priority patent/UA59403C2/uk
Publication of ES2125206A1 publication Critical patent/ES2125206A1/es
Application granted granted Critical
Publication of ES2125206B1 publication Critical patent/ES2125206B1/es
Priority to LT2000004A priority patent/LT4728B/lt
Priority to IS5353A priority patent/IS2076B/is
Priority to NO20000294A priority patent/NO314996B1/no
Priority to BG104100A priority patent/BG64849B1/bg
Priority to LVP-00-08A priority patent/LV12457B/en
Priority to HK01102218A priority patent/HK1032958A1/xx
Anticipated expiration legal-status Critical
Expired - Fee Related legal-status Critical Current

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47—One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/30—Indoles; Hydrogenated indoles with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
    • C07D209/42—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D231/00—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D231/14—Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D231/16—Halogen atoms or nitro radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/32—One oxygen, sulfur or nitrogen atom
    • C07D239/42—One nitrogen atom
    • 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
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D307/56—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members 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
    • C07D307/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/30—Hetero atoms other than halogen
    • C07D333/32—Oxygen atoms
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    • C07—ORGANIC CHEMISTRY
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    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur 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
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
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    • C07D333/50—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62—Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes 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
    • C07D333/68—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
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    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/14—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyridine Compounds (AREA)

Abstract

Derivados de acil-piperazinil-pirimidinas, su preparación y su aplicación como medicamentos. Los derivados de acil-piperazinil-pirimidinas (I) donde X es 0 o S; R{sub,1 es alcoxi o trifluorometilo; R{sub,2 es alquilo, cicloalquilo, heterocicloalquilo, arilo, arilalquilo, heteroarilo o heteroarilalquilo, tienen actividad sobre el sistema nervioso central. Los compuestos (I) en los que X es 0 pueden obtenerse por reacción de un derivado de pirimidina con un derivado de piperazina o por reacción de un derivado de piperazinil-pirimidina con un ácido carboxílico o una sal o derivado del mismo. Los compuestos (I) en los que X es S pueden obtenerse por reacción de (I) en los que X es 0 con el reactivo de Lawesson o con pentasulfuro de fósforo. Los compuestos (I) tienen actividad sedante, anticonvulsivante, hipnótico y anestésico general y tienen aplicación en Medicina humana y/o veterinaria.
ES009701627A 1997-07-21 1997-07-21 Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos. Expired - Fee Related ES2125206B1 (es)

Priority Applications (35)

Application Number Priority Date Filing Date Title
ES009701627A ES2125206B1 (es) 1997-07-21 1997-07-21 Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos.
ARP980103475A AR017254A1 (es) 1997-07-21 1998-07-16 UN COMPUESTO DERIVADO DE ACIL-PIPERAZINIL-PIRIMIDINA Y SUS SALES, PROCEDIMIENTO PARA SU ELABORACIoN, COMPOSICIONES FARMACÉUTICAS QUE LOS CONTIENEN Y SU EMPLEO EN LA ELABORACIoN DE MEDICAMENTOS QUE ACTUAN SOBRE EL SISTEMA NERVIOSO CENTRAL.
CO98040807A CO5011090A1 (es) 1997-07-21 1998-07-17 Derivados de acil-piperazinil-pirimidinas, procedimiento para su preparacion y composiciones farmaceuticas de los mismos
TW087111649A TW530056B (en) 1997-07-21 1998-07-17 Derivatives of acylpiperazinyl-pyrimidines, their preparation and application as medicaments with activity in the central nervous system
ZA986437A ZA986437B (en) 1997-07-21 1998-07-20 Derivatives of acyl-piperazinyl-pyrimidines their preparation and application as medicaments
PL98338143A PL195632B1 (pl) 1997-07-21 1998-07-21 Pochodne acylopiperazynylopirymidyny, sposoby ichwytwarzania, kompozycje farmaceutyczne i ich zastosowanie jako leków
GEAP19985226A GEP20033090B (en) 1997-07-21 1998-07-21 Derivatives of Acyl-Piperazinil-Pyrimidins, Preparation, Method for Their Preparation and Their Application
EP98933660A EP1006110B8 (en) 1997-07-21 1998-07-21 Derivatives of acyl-piperazinil-pyrimidins, preparation thereof and application as medicaments
BR9810772-0A BR9810772A (pt) 1997-07-21 1998-07-21 Derivados de acil-piperazinil-pirimidinas, sua preparação e aplicação como medicamentos
IN1272CA1998 IN183820B (es) 1997-07-21 1998-07-21
US09/462,880 US6372746B1 (en) 1997-07-21 1998-07-21 Derivatives of acyl-piperazinyl-pyrimidines, preparation thereof and application as medicaments
AU83403/98A AU744633B2 (en) 1997-07-21 1998-07-21 Derivatives of acyl-piperazinil-pyrimidins, preparation thereof and application as medicaments
DK98933660T DK1006110T3 (da) 1997-07-21 1998-07-21 Derivater af acylpiperazinylpyrimidiner, fremstilling deraf og anvendelse som lægemidler
EEP200000037A EE04151B1 (et) 1997-07-21 1998-07-21 Atsüülpiperasinüülpürimidiinide derivaadid, nendevalmistamine ja kasutamine ravimitena
PT98933660T PT1006110E (pt) 1997-07-21 1998-07-21 Derivados de acil-piperazinil-pirimidinas sua preparacao e aplicacao como medicamentos
HU0002517A HUP0002517A3 (en) 1997-07-21 1998-07-21 Derivatives of acyl-piperazinil-pyrimidins, preparation thereof, pharmaceutical compositions containing them and their use as medicaments
CNB988084589A CN1202087C (zh) 1997-07-21 1998-07-21 酰基－哌嗪基－嘧啶衍生物,它们的制备和作为药物的应用
RU2000104007/04A RU2205827C2 (ru) 1997-07-21 1998-07-21 Производное ацилпиперазинилпиримидина, способы его получения, фармацевтическая композиция
KR10-2000-7000602A KR100514148B1 (ko) 1997-07-21 1998-07-21 아실-피페라지닐-피리미딘 유도체 및 이의 제조방법 및약물로써의 용도
SK72-2000A SK284675B6 (sk) 1997-07-21 1998-07-21 Derivát acylpiperazinylpyrimidínu, spôsob jeho prípravy a farmaceutická kompozícia na jeho báze
SI9820053A SI20269B (sl) 1997-07-21 1998-07-21 Derivati acil-piperazinil-pirimidinov, njihova priprava in uporaba kot zdravila
PCT/ES1998/000212 WO1999005121A1 (es) 1997-07-21 1998-07-21 Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos
ES98933660T ES2216297T3 (es) 1997-07-21 1998-07-21 Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos.
DE69821623T DE69821623T2 (de) 1997-07-21 1998-07-21 Derivate von acyl-piperazinil-pyrimidinen, ihre herstellung und verwendung als medikament
AT98933660T ATE259357T1 (de) 1997-07-21 1998-07-21 Derivate von acyl-piperazinil-pyrimidinen, ihre herstellung und verwendung als medikament
CA002297417A CA2297417C (en) 1997-07-21 1998-07-21 Derivatives of acyl-piperazinyl-pyrimidines, their preparation and application as medicaments
JP2000504120A JP2001510831A (ja) 1997-07-21 1998-07-21 アシル−ピペラジニル−ピリミジン誘導体、その製法および医薬としての応用
UA2000010370A UA59403C2 (uk) 1997-07-21 1998-07-21 Похідні ацилпіперазинілпіримідинів, спосіб їх одержання (варіанти), фармацевтична композиція та активний інгредієнт для виготовлення лікарського засобу
NZ502400A NZ502400A (en) 1997-07-21 1998-07-21 Derivatives of acyl-piperazinyl-pyrimidines
LT2000004A LT4728B (lt) 1997-07-21 2000-01-18 Acilpiperazinilpirimidinų dariniai, jų gavimas ir panaudojimas vaistams
IS5353A IS2076B (is) 1997-07-21 2000-01-19 Asýl-píperasínil-pýrimídínafleiður, framleiðsla og notkun þeirra sem lyfja
NO20000294A NO314996B1 (no) 1997-07-21 2000-01-20 Derivater av acylpiperazinylpyrimidiner, farmasöytisk preparat inneholdendeslike derivater, deres fremstilling, og anvendelse tilfremstilling av legemidler
BG104100A BG64849B1 (bg) 1997-07-21 2000-01-21 Производни на ацил-пиперазинил-пиримидини, тяхното получаване и използването им като лекарствени средства
LVP-00-08A LV12457B (en) 1997-07-21 2000-01-21 ACIL-PIPERAZINIL-PYRIMIDIN DERIVATIVES, THEIR ACQUISITION AND USE OF MEDICINES \ t
HK01102218A HK1032958A1 (en) 1997-07-21 2001-03-27 Derivatives of acyl-piperazinil-pyrimidins, preparation thereof and application as medicaments.

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Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10035908A1 (de) 2000-07-21 2002-03-07 Asta Medica Ag Neue Heteroaryl-Derivate und deren Verwendung als Arzneimittel
ES2167276B1 (es) * 2000-10-20 2003-04-01 Esteve Labor Dr Nuevos derivados de cianoaril (o cianoheteroaril)-carbonil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos.
JP4544820B2 (ja) * 2001-03-09 2010-09-15 オーソ−マクニール・フアーマシユーチカル・インコーポレーテツド 複素環化合物
US7390813B1 (en) * 2001-12-21 2008-06-24 Xenon Pharmaceuticals Inc. Pyridylpiperazines and aminonicotinamides and their use as therapeutic agents
US20050119251A1 (en) * 2001-12-21 2005-06-02 Jian-Min Fu Nicotinamide derivatives and their use as therapeutic agents
KR101255356B1 (ko) * 2002-06-12 2013-04-17 케모센트릭스, 인크. 염증 및 면역 질병의 치료를 위한 ｃｃｒ１ 길항물질로서사용하기 위한 1-아릴-4-치환된 피페라진 유도체
US7842693B2 (en) * 2002-06-12 2010-11-30 Chemocentryx, Inc. Substituted piperazines
US7589199B2 (en) 2002-06-12 2009-09-15 Chemocentryx, Inc. Substituted piperazines
MXPA04012959A (es) * 2002-06-29 2005-05-16 Zentaris Gmbh Arilcarbonilpiperacinas y heteroarilcarbonilpiperacinas y su uso para tratamiento de enfermedades de tumor benigno y maligno.
US20040127395A1 (en) * 2002-09-06 2004-07-01 Desai Pragnya J. Use of histamine H4 receptor modulators for the treatment of allergy and asthma
JP4845873B2 (ja) 2004-03-03 2011-12-28 ケモセントリックス インコーポレーティッド 二環式および架橋した窒素複素環
US7435831B2 (en) 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
AR051092A1 (es) 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso como inhibidores de la estearoil-coa
JP5043668B2 (ja) * 2004-09-20 2012-10-10 ゼノン・ファーマシューティカルズ・インコーポレイテッド 複素環誘導体および治療薬としてのそれらの使用
AU2005329423A1 (en) * 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
BRPI0515500A (pt) * 2004-09-20 2008-07-29 Xenon Pharmaceuticals Inc derivados piridazina para inibição de estearoil-coa-desaturase
BRPI0515489A (pt) * 2004-09-20 2008-07-29 Xenon Pharmaceuticals Inc derivados heterocìclicos e sua utilização como inibidores de estearoil-coa desaturase
EP1799668A1 (en) * 2004-09-20 2007-06-27 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as mediators of stearoyl-coa desaturase
US7919496B2 (en) 2004-09-20 2011-04-05 Xenon Pharmaceuticals Inc. Heterocyclic derivatives for the treatment of diseases mediated by stearoyl-CoA desaturase enzymes
CA2580781A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Bicyclic heterocyclic derivatives and their use as inhibitors of stearoyl-coa-desaturase (scd)
WO2006034446A2 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Pyridine derivatives for inhibiting human stearoyl-coa-desaturase
CN101208089A (zh) * 2005-06-03 2008-06-25 泽农医药公司 氨基噻唑衍生物作为人硬酯酰-CoA去饱和酶抑制剂
KR101020351B1 (ko) * 2005-07-29 2011-03-08 에프. 호프만-라 로슈 아게 인돌-3-일-카본일-피페리딘 및 피페라진 유도체
US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
US9238643B2 (en) 2010-09-06 2016-01-19 Guangzhou Institutes Of Biomedicine And Health, Chinese Academy Of Sciences Amide compounds
CA2901577A1 (en) * 2013-02-18 2014-08-21 The Scripps Research Institute Modulators of vasopressin receptors with therapeutic potential
JP2018012645A (ja) * 2014-11-26 2018-01-25 持田製薬株式会社 新規ジアザビシクロ誘導体
KR20240063881A (ko) * 2021-07-30 2024-05-13 콘포 테라퓨틱스 엔.브이. 통증, 특히 신경병증성 통증, 및/또는 at2r 및/또는 at2r 매개 신호전달과 연관된 다른 질환 또는 장애의 치료를 위한 화합물

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0115713A1 (fr) * 1982-11-09 1984-08-15 Sanofi S.A. (Pipérazinyl-1)-2 pyrimidines, leurs sels, procédé pour leur préparation et compositions pharmaceutiques en contenant
US4547505A (en) * 1983-03-25 1985-10-15 Degussa Aktiengesellschaft N-Phenyl-N-'-cycloalkylalkanoylpiperazine useful as analgetics and process for its production
EP0382637A1 (fr) * 1989-02-09 1990-08-16 Laboratorios Del Dr. Esteve, S.A. Dérivés de pyrimidinyl-piperazinyl-alkyl azolès avec activité anxiolytique et/ou tranquillisante
EP0497659A1 (fr) * 1991-01-28 1992-08-05 Laboratorios Del Dr. Esteve, S.A. Dérivés d'aryl (ou hétéroaryl)-piperaz inyl-alkyl-azoles, leur préparation et leur application en tant que médicaments
WO1994014779A1 (en) * 1992-12-21 1994-07-07 Smithkline Beecham Plc Pyrimidinyl-piperazine derivatives and their use as medicaments

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3752141T2 (de) * 1986-02-24 1998-03-26 Mitsui Petrochemical Ind Mittel zur behandlung von neuropathie

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0115713A1 (fr) * 1982-11-09 1984-08-15 Sanofi S.A. (Pipérazinyl-1)-2 pyrimidines, leurs sels, procédé pour leur préparation et compositions pharmaceutiques en contenant
US4547505A (en) * 1983-03-25 1985-10-15 Degussa Aktiengesellschaft N-Phenyl-N-'-cycloalkylalkanoylpiperazine useful as analgetics and process for its production
EP0382637A1 (fr) * 1989-02-09 1990-08-16 Laboratorios Del Dr. Esteve, S.A. Dérivés de pyrimidinyl-piperazinyl-alkyl azolès avec activité anxiolytique et/ou tranquillisante
EP0497659A1 (fr) * 1991-01-28 1992-08-05 Laboratorios Del Dr. Esteve, S.A. Dérivés d'aryl (ou hétéroaryl)-piperaz inyl-alkyl-azoles, leur préparation et leur application en tant que médicaments
WO1994014779A1 (en) * 1992-12-21 1994-07-07 Smithkline Beecham Plc Pyrimidinyl-piperazine derivatives and their use as medicaments

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