SI20269B - Derivati acil-piperazinil-pirimidinov, njihova priprava in uporaba kot zdravila - Google Patents

Derivati acil-piperazinil-pirimidinov, njihova priprava in uporaba kot zdravila Download PDF

Info

Publication number
SI20269B
SI20269B SI9820053A SI9820053A SI20269B SI 20269 B SI20269 B SI 20269B SI 9820053 A SI9820053 A SI 9820053A SI 9820053 A SI9820053 A SI 9820053A SI 20269 B SI20269 B SI 20269B
Authority
SI
Slovenia
Prior art keywords
piperazinyl
methoxypyrimidine
methoxy
pyrimidine
chlorohydrate
Prior art date
Application number
SI9820053A
Other languages
English (en)
Other versions
SI20269A (sl
Inventor
Arjona Jordi Corbera
Domenech David Vano
Constansa Jordi Frigola
Original Assignee
Laboratorios Del Dr. Esteve, S.A.
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, S.A. filed Critical Laboratorios Del Dr. Esteve, S.A.
Publication of SI20269A publication Critical patent/SI20269A/sl
Publication of SI20269B publication Critical patent/SI20269B/sl

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/46Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/47One nitrogen atom and one oxygen or sulfur atom, e.g. cytosine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/08Antiepileptics; Anticonvulsants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic 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
    • C07D207/30Heterocyclic 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
    • C07D207/34Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D209/00Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04Indoles; Hydrogenated indoles
    • C07D209/30Indoles; 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
    • C07D209/42Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D231/00Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
    • C07D231/02Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings not condensed with other rings
    • C07D231/10Heterocyclic 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
    • C07D231/14Heterocyclic 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
    • C07D231/16Halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24Heterocyclic 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
    • C07D239/28Heterocyclic 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
    • C07D239/32One oxygen, sulfur or nitrogen atom
    • C07D239/42One nitrogen atom
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic 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
    • C07D295/04Heterocyclic 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
    • C07D295/12Heterocyclic 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
    • C07D295/125Heterocyclic 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
    • C07D295/13Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/34Heterocyclic 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
    • C07D307/56Heterocyclic 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
    • C07D307/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/26Heterocyclic 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
    • C07D333/30Hetero atoms other than halogen
    • C07D333/32Oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04Heterocyclic 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
    • C07D333/26Heterocyclic 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
    • C07D333/38Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D333/00Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/50Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom condensed with carbocyclic rings or ring systems
    • C07D333/52Benzo[b]thiophenes; Hydrogenated benzo[b]thiophenes
    • C07D333/62Benzo[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
    • C07D333/68Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen
    • C07D333/70Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen attached in position 2
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02Heterocyclic 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
    • C07D403/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D409/00Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/12Heterocyclic 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

Landscapes

  • 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)

Claims (18)

  1. λ PATENTNI ZAHTEVKI 1. Derivat acil-piperazinil-pirimidina s splošno formulo (I)
  2. 2. Spojina po zahtevku 1, v katerem je Ri metoksi, etoksi, propoksi, izopropoksi, butoksi, sec-butoksi ali tert-butoksi.
  3. 3. Spojina po zahtevku 1, v katerem je R2 metil, etil, propil, izopropil, butil, izobutil, sec-butil, tert-butil, pentil, izopentil, neopentil ali heksil.
  4. 4. Spojina po zahtevku 1, v katerem je R2 ciklopropil, ciklobutil, ciklopentil ali cikloheksil.
  5. 5. Spojina po zahtevku 1, v katerem je R2 2-aziridinil, 2-tetrahidrofuril, 3-tetrahidrofuril, 2-tetrahidrotienil, 3-tetrahidrotienil, 2-azetidinil, 2-pirolidinil, 3-pirolidinil, 2-piperidinil, 3-piperidinil ali 4-piperidinil. 3
  6. 6. Spojina po zahtevku 1, v katerem je R2 2-fluorofenil, 3- fluorofenil, 4-fluorofenil, 2-klorofenil, 3-klorofenil, 4-klorofenil, 2- bromofenil, 3-bromofenil, 4-bromofenil, 2-aminofenil, 3-aminofenil, 4- 5 aminofenil, 2-nitrofenil, 3-nitrofenil, 4-nitrofenil. 2-acetamidofenil, 3- acetamidofenil, 4-acetamidofenil, 2-nitrofenil. 3-nitrofenil, 4-nitrofenil, 2-metilfenil, 3-metilfenil, 4-metilfenil, 2-(trifluorometil)fenil, 3-(trifluorometil)fenil, 4-(trifluorometil)fenil, 2-metoksifenil, 3-metoksifenil, 4-metoksifenil, 2,3-difluorofenil, 3,4-difluorofenil, 2,4-difluorofenil, 2,3- io dibromofenil, 3,4-dibromofenil, 2,4-dibromofenil, 2,3-dimetilfenil, 3,4- dimetilfenil, 2,4-dimetilfenil, 2,3-dimetoksifenil, 3,4-dimetoksifenil, 2,4- dimetoksifenil.
  7. 7. Spojina po zahtevku 1, v katerem je R2 fenilmetil, l-feniletil, is 2-feniletil, 3-fenilpropil, po možnosti zamenjan na aromatskem obroču.
  8. 8. Spojina po zahtevku 1, v katerem je R2 2-furil, 3-furil, 2-tienil, 3-tienil, 3-metil-2-tienil, 5-metil-2-tienil, 3-metoksi-2-tienil, 3-kloro-2-tienil, 5-kloro-2-tienil, 2-pirolil, 3-pirolil, 2-piridil, 3-piridil, 4-piridil, 2- 2o indolil, 3-indolil, 2-benzo[b]tienil, 3-benzo[b]tienil, 3-kloro-2-benzo[b]tienil, pirazolil, imidazolil, pirimidmil, piridazinil, pirazinil, benzimidazolil, kinolil, oksazolil ali tiazolil.
  9. 9. Spojina po zahtevku 1, v katerem je R2 2-tienilmetil, 2-benzo[b]tienmetil ali 3-(4-kloropirazolil)propil.
  10. 10. Spojina po zahtevku 1, ki je izbrana iz naslednje skupine: • 2-[4-(2-furilkarbonil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(2-furilkarbonil)-l-piperazinil]-4-metoksipirimidin klorohidrat, • 4-metoksi-2-[4-(2-tienilkarbonil)-l-piperazinil]pirimidin, • 4-metoksi-2-[4-(2-tienilkarbonil)-1 -piperaziniljpirimidin klorohidrat, • 2-(4-acetil-l-piperazinil)-4-metoksipirimidin, • 2-{4-[4-(4-kloropirazolil)butanoil]-1-piperazinil}-4-metoksipirimidin, • 2-{4-[4-(4-kloropirazolil)butanoil]-1 -piperazinil}-4-metoksipirimidin klorohidrat, • 2-(4-benzoil-1 -piperazinil)4-metoksipirimidin, • 2-(4-ciklopropilkarbonil-1 -piperazinilH-metoksipirimidin, • 2-[4-(2-furilkarbonil)-l-piperazinil]4-(trifluorometil)pirimidin, • 2-[4-(2-tienilkarbonil)-l-piperazinil]4-(trifluorometil)pirimidin, • 4-metoksi-2-[4-(3-tienilkarbonil)-1 -piperaziniljpirimidin, • 4-metoksi-2-[4-(3-tienilkarbonil)-l-piperazinil]pirimidinklorohidrat, • 2-[4-(5-meti!-2-tienilkarbonil)-1-piperazinil]-4-metoksipirimidin, • 2-[4-(5-metil-2-tienilkarbonil)-1 -piperazinil]-4-metoksipirimidin klorohidrat, • 4-metoksi-2-[4-(3-metoksi-2-tienilkarbonil)-1-piperazinil]pirimidin, • 4-metoksi-2-[4-(3-metoksi-2-tienilkarbonil)-1 -piperaziniljpirimidin klorohidrat, • 2-[4-(2-benzo[b]tienilkarbonil)-l-piperazinil]-4-metokšipirimidin, • 2-[4-(2-benzo[b]tienilkarbonil)-1 -piperazinil]-4-metoksipirimidin klorohidrat, • 2-[4-(2-indolilkarbonil)-1 -piperazinil]4-metoksipirimidin, • 2-[4-(3-kloro-2-benzo[b]tienilkarbonil)-l-piperazinil]-4- metoksipirimidin, • 2-[4-(3-kloro-2-benzo[b]tienilkarbonil)-l-piperazinil]-4-metoksipirimidin klorohidrat, • 4-metoksi-2-[4-(2-pirolilkarbonil)-1-piperazinil]pirimidin, • 4-metoksi-2-[4-(2-pirolilkarbonil)-1-piperazinil]pirimidin klorohidrat, • 4-metoksi-2-[4-(2-tienilacetil)-1 -piperazinil]pirimidin, • 4-metoksi-2-[4-(2-tienilacetil)-1 -piperazinil]pirimidin klorohidrat, • 2-[4-(3-metil-2-tienilkarbonil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(3-metil-2-tienilkarbonil)-l-piperazinil]-4-metoksipirimidin klorohidrat, • 2-[4-(3-kloro-2-tienilkarbonil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(3-kloro-2-tienilkarbonil)-l-piperazinil]-4-metoksipirimidin klorohidrat, • 2-[4-(3-indolilkarbonil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-{3-benzo[b]tienilacetil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(5-kloro-2-tienilkarbonil)-1-piperazinil]-4-metoksipirimidin, • 2-[4-(5-kloro-2-tienilkarbonil)-l-piperazinil]-4-metoksipirimidin klorohidrat, • 4-metoksi-2-[4-(4-klorobenzoil)-l-piperazinil]-4-metoksipirimidin, • 4-metoksi-2-[4-(4-klorobenzoil)-l-piperazinil]-4-metoksipirimidin klorohidrat, • 2-[4-(4-fluorobenzoil)-1 -piperazinil]-4-metoksipirimidin, • 2-[4-(4-fluorobenzoil)-l-piperazinil]-4-metoksipirimidin klorohidrat, • 2-[4-(4-klorobenzoil)-1 -piperazinil]-4-metoksipirimidin, • 2-[4-(4-klorobenzoil)-l-piperazinil]-4-metoksipirimidin klorohidrat, • 4-metoksi-2-[4-(3-metoksibenzoil)-l-piperazinil]pirimidin, • 4-metoksi-2-[4-(3-metoksibenzoil)-1 -piperazinil]pirimidin klorohidrat, • 2-[4-(3-fluorobenzoil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(l-fluorobenzoil)-1 -piperazinil]-4-metoksipirimidin klorohidrat, • 2-[4-(3-klorobenzoil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(3-klorobenzoil)-1-piperazinil]-4-metoksipirimidin klorohidrat, • 4-metoksi-2-[4-(2-metoksibenzoil)-1 -piperazinil]pirimidin, • 4-metoksi-2-[4-(2-metoksibenzoil)-1 -piperazinil]pirimidin klorohidrat, • 2-[4-(2-(fluorobenzoil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(2-(fluorobenzoil)-l-piperazinil]-4-metoksipirimidin klorohidrat, • 2-[4-(2-(klorobenzoil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(2-(klorobenzoil)-1 -piperazinil]-4-metoksipirimidin klorohidrat, • 4-metoksi-2-[4-(2-tetrahidrofurilkarbonil)-1-piperazinil]pirimidin, • 4-metoksi-2-(4-tiobenzoil-1 -piperazinil)pirimidin, • 4-metoksi-2-[4-(2-tetrahidrofurilkarbonil)-1 -piperazinil]pirimidin klorohidrat, • 4-metoksi-2-(4-tiobenzoil-1 -piperazinil)pirimidin klorohidrat, • 2-(4-benzoil-1-piperazinil)-4-metoksipirimidin, • 4-metoksi-2-{4-[4-(trifluorometil)benzoil]-l-piperazinil}pirimidin, • 4-metoksi-2-{4-[4-(trifluorometil)benzoil]-l-piperazinil}pirimidin klorohidrat, • 4-metoksi-2-{4-[3-(trifluorometil)benzoil]-l-piperazinil}pirimidin, • 4-metoksi-2-{4-[3-(trifluorometil)benzoil]-1 -piperaziniljpirimidin klorohidrat, • 4-metoksi-2-{4-[2-(trifluorometil)benzoil]-l-piperazinil}pirimidin, • 4-metoksi-2-{4-[2-(trifluorometil)benzoil]-l-piperazinil}pirimidin klorohidrat, • 4-metoksi-2-(4-nikotinoil-1-piperazinil)pirimidin, • 4-metoksi-2-(4-nikotinoil-1 -piperazinil)pirimidin diklorohidrat, • 2-(4-izonikotinoil-1-piperazinil)-4-metoksipirimidin, • 2-(4-izonikotinoil-1 -piperazinil)-4-metoksipirimidin diklorohidrat, • 2-[4-(1-imidazolilkarbonil)-1-piperazinil]-4-metoksipirimidin, • 2-[4-(1 -imidazolilkarbonil)-1 -piperazinil]-4-metoksipirimidin klorohidrat, • 2-(4-nikotinoil-1-piperazinil)-4-(trifluorometil)pirimidin, • 2-(4-nikotinoil-1 -piperazinil)-4-(trifIuorometil)pirimidin klorohidrat, • 4-metoksi-2-,4-(2-piridilkarbonil)-l-piperazinil]pirimidin, • 4-metoksi-2-’4-(2-piridilkarbonil)-1 -piperazinil]pirimidin diklorohidrat, • 4-etoksi-2-[4-(2-tienilkarbonil)-1 -piperazinil]pirimidin, • 4-etoksi-2-[4-(2-tienilkarbonil)-1 -piperazinil]pirimidin klorohidrat, • 2-[4-(3-kloro-2-tienilkarbonil)-l-piperazinil]-4-etoksipirimidin, • 2-[4-{3-kloro-2-tienilkarbonil)-l-piperazinil]-4-etoksipirimidin klorohidrat, • 4-etoksi-2-{4-[2-(trifluorometil)benzoil]-l-piperazinil}pirimidin, • 4-etoksi-2-{4-[2-(trifluorometil)benzoil]-l-piperazinil}pirimidin klorohidrat, • 2-[4-(2-metilbenzoil)-1-piperazinil]-4-metoksipirimidin, • 2-[4-(2-metilbenzoil)-1 -piperazinil]-4-metoksipirimidin klorohidrat, • 2-[4-(4-fluorobenzoil)-1-piperazinil]-4-izopropoksipirimidin, • 2-[4-(4-fluorobenzoil)-1 -piperazinil]-4-izopropoksipirimidin klorohidrat, • 4-izopropoksi-2-{4-[2-(trifluorometil)benzoil]-1-piperazinil]pirimidin, • 4-izopropoksi-2-{4-[2-(trifluorometil)benzoil]-l-piperazinil]pirimidin klorohidrat, • 2-[4-(3-kloro-2-tienkarbonil)-l-piperazinil]-4-izopropoksipirimidin, • 2-[4-(3-k!oro-2-tienkarbonil)-l-piperazinil]-4-izopropoksipirimidin klorohidrat, • 2-[4-(cikloheksilkarbonil)-1-piperazinil]-4-metoksipirimidin, • 2-[4-(cikloheksilkarbonil)-1 -piperazinil]-4-metoksipirimidin klorohidrat, • 4-etoksi-2[4-(4-fluorobenzoil]-1-piperazinil}pirimidin, • 4-etoksi-2[4-(4-fluorobenzoil]-1 -piperaziniljpirimidin klorohidrat, • 2-[4-(2-tiazoiilkarbonil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(2-aminobenzoil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(2-aminobenzoil)-l-piperazinit]-4-metoksipirimidin klorohidrat, • 2-[4-(3-fluoro-2-tieilkarbonil)-l-piperazinil]-4-metoksipirimidin> • 2-[4-(3-fluoro-2-tieilkarbonil)"l-piperazinil]-4-metoksipirimidin klorohidrat, • 2-[4-(4-metoksi-2-pirimidinil)-1-piperazinilkarbonil]benzoična kislina • 2-[4-(2-acetoksibenzoil)-l-piperazinil]-4-metoksipirimidin, • 2-[4-(2-hidroksibenzoil)-l-piperazinil]-4-metoksipirimidin, • natrijev 2-[4-(4-metoksi-2-pirimidinil)-l-piperazinilkarbonil]benzoat, • 2-[4-(2-hidroksibenzoil)-1 -piperazinil]-4-metoksipirimidin hidroklorat, • 4-metoksi-2-[4-(2-metoksibenzoil)-l-piperazinill-4-metoksipirimidin, in • 4-etoksi-2[4-(2-piridilkarbonil]-l-piperazinil}pirimidin.
    N
    10 kjer je X atom kisika ali žvepla; R1 alkoksi Cm ali trifluorometilni radikal; R2 alkilni radikal C^; nasičeni cikloalkil C^; heterocikloalkil vsebuje obroč s 3 do 6 atomi, v katerem je heteroatom izbran izmed is atoma kisika, žvepla ali dušika, po možnosti je N zamenjan z alkilom Ci -C6; fenil, ki je po možnosti zamenjan z 1, 2 ali 3 identičnimi ali različnimi nadomestki, izbranimi izmed fluora, klora, broma, amino, acetamido, nitro, metila, trifluorometila in metoksi; arilalkil, ki obsega alkilno skupino Cm, ki je zamenjana s fenilnim radikalom, ki je po možnosti zamenjan z 1, 2 ali 3 m identičnimi ali različnimi nadomestki, izbranimi izmed fluora, klora, broma, amino, acetamido, nitro, metila, trifluorometila in metoksi; heteroaril vsebuje obroč s 5 ali 6 heteroatomi, ki so po možnosti zamenjani, ali spojene heteroaromatske sisteme, ki so po možnosti zamenjani, 9 ali 10 1. atomov, ki vsebujejo 1 ali 2 heteroatoma, ki sta izbrana izmed kisika, žvepla in dušika, prej omenjeni nadomestki so izbrani izmed fluora, klora, broma, amino, acetamido, nitro, metila, trifluorometila in metoksi; in heteroalkil, ki vsebuje alkilno skupino iz 1 do 3 ogljikovih atomov, ki so zamenjani s heteroarilnim radikalom, ki obsega 5 ali 6 členski heteroaromatski obroč, ki je po možnosti zamenjan, ali spojeni 9 do 10 členski heteroaromatski sistemi, ki so po možnosti zamenjani z 1 ali 2 heteroatomom, ki sta izbrana izmed kisika, žvepla in dušika, prej omenjeni nadomestki so izbrani izmed fluora, klora, broma, amino, acetamido, nitro, metila, trifluorometila in metoksi; in njihove fiziološko sprejemljive soli.
  11. 11. Postopek za pripravo spojine s splošno formulo (I), v kateri X predstavlja atom kisika po zahtevku 1, ki obsega reakcijo derivata kloropirimidina s formulo (III) ^ (»O kjer ima R-j pomen, ki je definiran v zahtevku 1, z derivatom piperazina s splošno formulo (IV) X kjer ima R2 pomen, ki je definiran v zahtevku 1 in X predstavlja atom kisika.
    (V)
  12. 12. Postopek za pripravo spojine s splošno formulo (I), v kateri X predstavlja atom kisika po zahtevku 1, ki obsega reakcijo amina s formulo (V) kjer ima Ri pomen, ki je definiran v zahtevku 1, s karboksilno kislino s formulo R2COOH (VI) ali s soljo omenjene kisline, v kateri ima R2 pomen, ki je definiran v zahtevku 1.
  13. 13. Postopek za pripravo spojine s splošno formulo (I), v kateri X predstavlja atom kisika po zahtevku 1, ki obsega reakcijo amina s formulo (V) R
    (V) kjer ima Ri pomen, ki je definiran v zahtevku 1 Αϋ z derivatnim reagentom R2COY (VII), v katerem ima R2 pomen, ki je definiran v zahtevku 1 in Y predstavlja halogeni atom, azidno skupino, 1-imidazolilno skupino, skupino O-CO-R4, kjer R4 predstavlja alkilni radikal iz 1 do 6 atomov ogljika ali arilnega radikala, ki je po možnosti zamenjan z 5 enim ali večimi halogenimi atomi, ali skupino OR5, kjer R5 predstavlja aromatsko skupino ali en ali dva obroča, zamenjana z enim ali večimi halogenimi atomi ali nitro radikali, ali N-sukcinimid.
  14. 14. Postopek za pripravo spojine s splošno formulo (I), v kateri X 10 predstavlja atom žvepla po zahtevku 1, ki obsega reakcijo spojine s splošno formulo (I), v kateri X predstavlja atom kisika, z Lavvessonovim reagentom,(2,4'bis(4-metoksifenil)-1,3,2,4-ditiadifosfaetano-2,4-disulfurid), ali z fosfor pentasulfidom. is
  15. 15. Postopek za pripravo fiziološko sprejemljivih soli spojin s splošno formulo (I) po zahtevku 1, ki obsega reakcijo spojine s splošno formulo (I) z mineralno kislino ali organsko kislino v ustreznem topilu.
  16. 16. Farmacevtska zmes, ki je označena s tem, da vsebuje poleg 20 farmacevtsko sprejemljivega nosilca zdravila vsaj eno spojino s splošno formulo (I) ali eno od njenih fiziološko sprejemljivih soli po zahtevkih 1 do 10.
  17. 17. Uporaba spojine s splošno formulo (I) ali njenih farmacevtsko sprejemljivih soli po kateremkoli izmed zahtevkov 1 do 10 v izdelavi zdravila z delovanjem na centralni živčni sistem sesalcev, vključno s človekom.
  18. 18. Uporaba spojine s splošno formulo (I) ali njenih farmacevtsko sprejemljivih soli po kateremkoli izmed zahtevkov 1 do 10 v izdelavi zdravila s sedativnim, antikonvulzantnim, analgetičnim, mišično relaksantnim, antitusigenim, anksiolitičnim, antipsihotičnim, antidepresivnim, antimigrenskim in antiishemičnim (v možganih) delovanjem, v izdelavi zdravila za zdravljenje motenj spanja, nevrodegenerativnih bolezni, motenj prepoznavanja in Alzheimerjeve bolezni, uspavalnih sredstev ali sredstev za splošno anastezijo za sesalce, vključno s človekom. Za: LABORATORIOS DEL DR. ESTEVE, S.A.
SI9820053A 1997-07-21 1998-07-21 Derivati acil-piperazinil-pirimidinov, njihova priprava in uporaba kot zdravila SI20269B (sl)

Applications Claiming Priority (2)

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.
PCT/ES1998/000212 WO1999005121A1 (es) 1997-07-21 1998-07-21 Derivados de acil-piperazinil-pirimidinas, su preparacion y su aplicacion como medicamentos

Publications (2)

Publication Number Publication Date
SI20269A SI20269A (sl) 2000-12-31
SI20269B true SI20269B (sl) 2005-04-30

Family

ID=8300152

Family Applications (1)

Application Number Title Priority Date Filing Date
SI9820053A SI20269B (sl) 1997-07-21 1998-07-21 Derivati acil-piperazinil-pirimidinov, njihova priprava in uporaba kot zdravila

Country Status (34)

Country Link
US (1) US6372746B1 (sl)
EP (1) EP1006110B8 (sl)
JP (1) JP2001510831A (sl)
KR (1) KR100514148B1 (sl)
CN (1) CN1202087C (sl)
AR (1) AR017254A1 (sl)
AT (1) ATE259357T1 (sl)
AU (1) AU744633B2 (sl)
BG (1) BG64849B1 (sl)
BR (1) BR9810772A (sl)
CA (1) CA2297417C (sl)
CO (1) CO5011090A1 (sl)
DE (1) DE69821623T2 (sl)
DK (1) DK1006110T3 (sl)
EE (1) EE04151B1 (sl)
ES (2) ES2125206B1 (sl)
GE (1) GEP20033090B (sl)
HK (1) HK1032958A1 (sl)
HU (1) HUP0002517A3 (sl)
IN (1) IN183820B (sl)
IS (1) IS2076B (sl)
LT (1) LT4728B (sl)
LV (1) LV12457B (sl)
NO (1) NO314996B1 (sl)
NZ (1) NZ502400A (sl)
PL (1) PL195632B1 (sl)
PT (1) PT1006110E (sl)
RU (1) RU2205827C2 (sl)
SI (1) SI20269B (sl)
SK (1) SK284675B6 (sl)
TW (1) TW530056B (sl)
UA (1) UA59403C2 (sl)
WO (1) WO1999005121A1 (sl)
ZA (1) ZA986437B (sl)

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.
WO2002072548A2 (en) * 2001-03-09 2002-09-19 Ortho-Mcneil Pharmaceutical, Inc. Heterocyclic compounds and their use as histamine h4 ligands.
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
US7842693B2 (en) * 2002-06-12 2010-11-30 Chemocentryx, Inc. Substituted piperazines
US7589199B2 (en) * 2002-06-12 2009-09-15 Chemocentryx, Inc. Substituted piperazines
CN1867336B (zh) * 2002-06-12 2010-05-12 凯莫森特里克斯股份有限公司 1-芳基-4-取代的哌嗪衍生物及其制药用途
PL375527A1 (en) * 2002-06-29 2005-11-28 Zentaris Gmbh Arylcarbonylpiperazines and heteroarylcarbonylpiperazines and the use thereof for treating benign and malignant tumour diseases
US20040127395A1 (en) * 2002-09-06 2004-07-01 Desai Pragnya J. Use of histamine H4 receptor modulators for the treatment of allergy and asthma
EP1720545B1 (en) 2004-03-03 2014-10-29 ChemoCentryx, Inc. Bicyclic and bridged nitrogen heterocycles
US7435831B2 (en) 2004-03-03 2008-10-14 Chemocentryx, Inc. Bicyclic and bridged nitrogen heterocycles
WO2006034279A1 (en) * 2004-09-20 2006-03-30 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as therapeutic agents
BRPI0515478A (pt) * 2004-09-20 2008-07-22 Xenon Pharmaceuticals Inc derivados heterocìclicos e seu uso como mediadores de estearoil-coa-desaturase
CN101084207A (zh) * 2004-09-20 2007-12-05 泽农医药公司 杂环衍生物及其作为硬脂酰CoA去饱和酶抑制剂的用途
CN101083982A (zh) 2004-09-20 2007-12-05 泽农医药公司 用于治疗硬脂酰CoA去饱和酶介导的疾病的杂环衍生物
AU2005329423A1 (en) * 2004-09-20 2006-09-28 Xenon Pharmaceuticals Inc. Heterocyclic derivatives and their use as stearoyl-CoA desaturase inhibitors
TW200626154A (en) 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
CN101083986A (zh) * 2004-09-20 2007-12-05 泽农医药公司 双环杂环衍生物及其作为硬脂酰CoA去饱和酶(SCD)抑制剂的用途
TW200626155A (en) * 2004-09-20 2006-08-01 Xenon Pharmaceuticals Inc Heterocyclic derivatives and their use as therapeutic agents
AR051095A1 (es) * 2004-09-20 2006-12-20 Xenon Pharmaceuticals Inc Derivados heterociclicos y su uso comoinhibidores de la estearoil-coa desaturasa
BRPI0611187A2 (pt) * 2005-06-03 2010-08-24 Xenon Pharmaceuticals Inc derivados aminotiazàis como inibidores da estearoil-coa desaturase humana
WO2007014851A2 (en) * 2005-07-29 2007-02-08 F. Hoffmann-La Roche Ag Indol-3-yl-carbonyl-piperidin and piperazin derivatives
US8609672B2 (en) 2010-08-27 2013-12-17 University Of The Pacific Piperazinylpyrimidine analogues as protein kinase inhibitors
GB2497476B (en) * 2010-09-06 2018-01-10 Guangzhou Inst Biomed & Health Amide Compounds
JP2016513112A (ja) * 2013-02-18 2016-05-12 ザ スクリプス リサーチ インスティテュート 治療的潜在能力を有するバソプレッシン受容体のモジュレーター
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

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2535718A1 (fr) * 1982-11-09 1984-05-11 Sanofi Sa (piperazinyl-1)-2 pyrimidines, leurs sels, procede pour leur preparation 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
EP0257102B1 (en) * 1986-02-24 1997-11-19 Mitsui Petrochemical Industries, Ltd. Agents for treating neurophathy
FR2642759B1 (fr) * 1989-02-09 1991-05-17 Laboratorios Esteve Sa Derives de pyrimidyl-piperazinyl-alkyl azoles avec activite anxiolytique et/ou tranquillisante
FR2672052B1 (fr) * 1991-01-28 1995-05-24 Esteve Labor Dr Derives d'aryl (ou heteroaryl)-piperazinyl-alkyl-azoles, leur preparation et leur application en tant que medicaments.
GB9226610D0 (en) * 1992-12-21 1993-02-17 Smithkline Beecham Plc Compounds

Also Published As

Publication number Publication date
GEP20033090B (en) 2003-10-27
HUP0002517A3 (en) 2002-06-28
HK1032958A1 (en) 2001-08-10
IN183820B (sl) 2000-04-29
CO5011090A1 (es) 2001-02-28
ES2216297T3 (es) 2004-10-16
PT1006110E (pt) 2004-05-31
IS5353A (is) 2000-01-19
PL195632B1 (pl) 2007-10-31
CA2297417A1 (en) 1999-02-04
ES2125206B1 (es) 1999-11-16
DK1006110T3 (da) 2004-04-26
SK722000A3 (en) 2000-08-14
NZ502400A (en) 2001-06-29
CN1202087C (zh) 2005-05-18
JP2001510831A (ja) 2001-08-07
BG104100A (en) 2001-05-31
HUP0002517A2 (hu) 2001-06-28
BR9810772A (pt) 2000-08-15
SK284675B6 (sk) 2005-09-08
ATE259357T1 (de) 2004-02-15
PL338143A1 (en) 2000-09-25
NO20000294D0 (no) 2000-01-20
AR017254A1 (es) 2001-09-05
EE200000037A (et) 2000-10-16
SI20269A (sl) 2000-12-31
LT2000004A (en) 2000-07-25
US6372746B1 (en) 2002-04-16
KR20010015567A (ko) 2001-02-26
DE69821623D1 (de) 2004-03-18
EP1006110B1 (en) 2004-02-11
LT4728B (lt) 2000-11-27
LV12457A (lv) 2000-04-20
ZA986437B (en) 1999-04-07
NO20000294L (no) 2000-03-17
UA59403C2 (uk) 2003-09-15
BG64849B1 (bg) 2006-06-30
KR100514148B1 (ko) 2005-09-13
CA2297417C (en) 2008-01-29
EP1006110A1 (en) 2000-06-07
IS2076B (is) 2006-02-15
RU2205827C2 (ru) 2003-06-10
ES2125206A1 (es) 1999-02-16
CN1268124A (zh) 2000-09-27
AU8340398A (en) 1999-02-16
LV12457B (en) 2000-07-20
AU744633B2 (en) 2002-02-28
EE04151B1 (et) 2003-10-15
DE69821623T2 (de) 2005-01-05
TW530056B (en) 2003-05-01
NO314996B1 (no) 2003-06-23
EP1006110B8 (en) 2005-01-05
WO1999005121A1 (es) 1999-02-04

Similar Documents

Publication Publication Date Title
SI20269B (sl) Derivati acil-piperazinil-pirimidinov, njihova priprava in uporaba kot zdravila
RU2000104007A (ru) Производные ацилпиперазинилпиримидинов, их получение и применение в качестве лекарственных средств
JP2001510831A5 (sl)
US9873683B2 (en) P2X4 receptor antagonist
RU2386620C2 (ru) Производные пиридазин-3(2н)-она и их применение в качестве ингибиторов фдэ4
US20090004185A1 (en) Amino-substituted quinazoline derivatives as inhibitors of beta-catenin/tcf-4 pathway and cancer treatment agents
CN1823071B (zh) 用作钾通道抑制剂的噻吩并嘧啶衍生物
JP2004532806A (ja) セロトニン5ht−2レセプターのアゴニストまたはアンタゴニストとしてのピペラジニルピラジン化合物
JP2002524512A (ja) cGMPホスホジエステラーゼの縮合ピリジン阻害剤
JP2003510319A5 (sl)
WO2006062982A2 (en) Urea inhibitors of map kinases
SK9062003A3 (en) Substituted triazole diamine derivatives as kinase inhibitors
NZ601656A (en) Pyridyloxyindoles inhibitors of VEGF-R2 and use thereof for treatment of disease
KR20020072282A (ko) 벤즈아졸 유도체 및 이의 jnk 조절자로의 용도
JP2006522812A5 (sl)
RU2006111470A (ru) Тиенопиразолы
RU2005128833A (ru) Замещенные сульфамидами производные ксантина для применения в качестве ингибиторов фосфоенолпируваткарбоксикиназы (рерск)
CN102056920A (zh) 用作食欲素受体拮抗剂的四唑化合物
JP2012507525A5 (sl)
CA2396227A1 (en) 1,2-diaryl benzimidazoles for treating illnesses associated with a microglia activation
KR20090113383A (ko) 인돌 유도체
PT1173413E (pt) Utilizacao de derivados do acido 2,4-diamino-3-hidroxicarboxilicos como inibidores de proteassoma
RU2005111983A (ru) Производные 4-(фенил-пиперазинил-метил)бензамида и их применение для лечения боли или желудочно-кишечных расстройств
HRP20230793T1 (hr) Derivati indola i benzimidazola kao dvojni antagonisti 5-ht2a i 5-ht6 receptora
US7319102B1 (en) Pyrrolo[2,3-d]pyrimidine cytokine inhibitors

Legal Events

Date Code Title Description
IF Valid on the event date
OU02 Decision according to article 73(2) ipa 1992, publication of decision on partial fulfilment of the invention and change of patent claims

Effective date: 20050118

KO00 Lapse of patent

Effective date: 20080229