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PE20010854A1 - USE OF SUBSTITUTED PYRIMIDINE 4 DERIVATIVES AS ANTAGONISTS OF GLUTAMATE mGluR1 RECEPTORS - Google Patents

USE OF SUBSTITUTED PYRIMIDINE 4 DERIVATIVES AS ANTAGONISTS OF GLUTAMATE mGluR1 RECEPTORS

Info

Publication number
PE20010854A1
PE20010854A1 PE2000001131A PE0011312000A PE20010854A1 PE 20010854 A1 PE20010854 A1 PE 20010854A1 PE 2000001131 A PE2000001131 A PE 2000001131A PE 0011312000 A PE0011312000 A PE 0011312000A PE 20010854 A1 PE20010854 A1 PE 20010854A1
Authority
PE
Peru
Prior art keywords
derivatives
antagonists
substituted pyrimidine
carbocyclic
alkyl
Prior art date
Application number
PE2000001131A
Other languages
Spanish (es)
Inventor
Willian Martin Owton
Kirk Willis Johnson
Samantha Jayne Ambler
Darrell Stephen Coleman
John Goldsworthy
Ann Elizabeth Kingston
Jeffrey Michael Schkeryantz
Darryle Darwin Schoepp
Stephen Richard Baker
Mohammad Sadegh Zia-Ebrahimi
Michael Scott Vannieuwenhze
Jian Eric Hong
Gunnar Erik Jagdmann Jr
Robert James Foglesong
Barry Peter Clark
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Publication of PE20010854A1 publication Critical patent/PE20010854A1/en

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    • 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
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/86Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/94Nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/95Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in positions 2 and 4
    • 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
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D491/00Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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

Abstract

SE REFIERE AL USO DE DERIVADOS DE PIRIMIDINA 4-SUSTITUIDAS DE FORMULA I, DONDE X1 ES O, NH; L ES UN ENLACE, ALQUILENO C1-C6 OPCIONALMENTE SUSTITUIDO CON F, OH, ALCOXI C1-C4, OXO; R1 ES CARBOCICLICO, HETEROCICLICO; R2 ES H, HALOGENO, CARBOXILO, CIANO, SCH2N, X2-R5; X2 ES UN ENLACE, O, S, SO, SO2, NH; R5 ES ALQUILO C1-C8, CICLOALQUILO C3-C10, HALOALQUILO C1-C6, HIDROXIALQUILO C1-C6, ENTRE OTROS; R3 Y R4 SON ALQUILO C1-C4 O JUNTO A C FORMAN UN ANILLO CARBOCICLICO, HETEROCICLICO. TAMBIEN SE REFIERE A UN PROCEDIMIENTO PARA LA PREPARACION, A COMPUESTOS INTERMEDIOS. EL COMPUESTO I ES UN ANTAGONISTA DEL RECEPTOR DE GLUTAMATO mGluR1 Y PUEDE SER UTIL PARA EL TRATAMIENTO DE DOLOR, MIGRANAREFERS TO THE USE OF 4-SUBSTITUTED PYRIMIDINE DERIVATIVES OF FORMULA I, WHERE X1 IS O, NH; L IS A BOND, C1-C6 ALKYLENE OPTIONALLY SUBSTITUTED WITH F, OH, C1-C4 ALCOXY, OXO; R1 IS CARBOCYCLIC, HETEROCYCLIC; R2 IS H, HALOGEN, CARBOXYL, CYANE, SCH2N, X2-R5; X2 IS A LINK, O, S, SO, SO2, NH; R5 IS C1-C8 ALKYL, C3-C10 CYCLOALKYL, C1-C6 HALOALKYL, C1-C6 HYDROXYALKYL, AMONG OTHERS; R3 AND R4 ARE C1-C4 ALKYL OR TOGETHER WITH C, THEY FORM A CARBOCYCLIC, HETEROCICLIC RING. IT ALSO REFERS TO A PROCEDURE FOR THE PREPARATION, TO INTERMEDIATE COMPOUNDS. COMPOUND I IS AN ANTAGONIST OF THE GLUTAMATE RECEPTOR mGluR1 AND MAY BE USEFUL FOR THE TREATMENT OF PAIN, MIGRAN

PE2000001131A 1999-11-01 2000-10-20 USE OF SUBSTITUTED PYRIMIDINE 4 DERIVATIVES AS ANTAGONISTS OF GLUTAMATE mGluR1 RECEPTORS PE20010854A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US16290099P 1999-11-01 1999-11-01

Publications (1)

Publication Number Publication Date
PE20010854A1 true PE20010854A1 (en) 2001-08-28

Family

ID=22587589

Family Applications (1)

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PE2000001131A PE20010854A1 (en) 1999-11-01 2000-10-20 USE OF SUBSTITUTED PYRIMIDINE 4 DERIVATIVES AS ANTAGONISTS OF GLUTAMATE mGluR1 RECEPTORS

Country Status (7)

Country Link
EP (1) EP1230225A2 (en)
AR (1) AR026275A1 (en)
AU (1) AU1071301A (en)
CO (1) CO5261605A1 (en)
PE (1) PE20010854A1 (en)
SV (1) SV2002000205A (en)
WO (1) WO2001032632A2 (en)

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WO2001032632A3 (en) 2001-11-08
AR026275A1 (en) 2003-02-05

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