CO5650253A2 - Piperazina con grupo fenilo or-sustituido y su uso como inhibidores de glyt1 - Google Patents

Piperazina con grupo fenilo or-sustituido y su uso como inhibidores de glyt1

Info

Publication number
CO5650253A2
CO5650253A2 CO06012502A CO06012502A CO5650253A2 CO 5650253 A2 CO5650253 A2 CO 5650253A2 CO 06012502 A CO06012502 A CO 06012502A CO 06012502 A CO06012502 A CO 06012502A CO 5650253 A2 CO5650253 A2 CO 5650253A2
Authority
CO
Colombia
Prior art keywords
alkyl
substituted
halogen
alkoxy
hydroxyl
Prior art date
Application number
CO06012502A
Other languages
English (en)
Inventor
Synese Jolidon
Robert Narquizian
Matthias Heinrich Nettekoven
Roger David Norcross
Emmanuel Pinard
Henri Stalder
Original Assignee
Hoffmann La Roche
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=34130061&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=CO5650253(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of CO5650253A2 publication Critical patent/CO5650253A2/es

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Classifications

    • 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
    • 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
    • A61P25/18—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
    • A61P25/24—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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen 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
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/84—Nitriles
    • C07D213/85—Nitriles in position 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
    • C07D241/02—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings
    • C07D241/10—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D241/14—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings not condensed with other rings having 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
    • C07D241/20—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D251/00—Heterocyclic compounds containing 1,3,5-triazine rings
    • C07D251/02—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings
    • C07D251/12—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members
    • C07D251/26—Heterocyclic compounds containing 1,3,5-triazine rings not condensed with other rings having three double bonds between ring members or between ring members and non-ring members with only hetero atoms directly attached to ring carbon atoms
    • C07D251/40—Nitrogen atoms
    • C07D251/42—One nitrogen atom
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D257/00—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms
    • C07D257/02—Heterocyclic compounds containing rings having four nitrogen atoms as the only ring hetero atoms not condensed with other rings
    • C07D257/04—Five-membered rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/30—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
    • C07D263/32—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D271/00—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms
    • C07D271/02—Heterocyclic compounds containing five-membered rings having two nitrogen atoms and one oxygen atom as the only ring hetero atoms not condensed with other rings
    • C07D271/06—1,2,4-Oxadiazoles; Hydrogenated 1,2,4-oxadiazoles
    • 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
    • C07D295/16—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 acylated on ring nitrogen atoms
    • C07D295/18—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 acylated on ring nitrogen atoms by radicals derived from carboxylic acids, or sulfur or nitrogen analogues thereof
    • C07D295/182—Radicals derived from carboxylic acids
    • C07D295/192—Radicals derived from carboxylic acids from aromatic carboxylic acids
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
    • C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
    • C07D309/10—Oxygen atoms
    • C07D309/12—Oxygen atoms only hydrogen atoms and one oxygen atom directly attached to ring carbon atoms, e.g. tetrahydropyranyl ethers

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Hospice & Palliative Care (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyridine Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pyrane Compounds (AREA)

Abstract

1.- Compuestos de fórmula general en donde Ar es arilo sustituido o sin sustituir o heteroarilo de 6 miembros, que contiene uno, dos o tres átomos de nitrógeno, y en donde los grupos arilo y heteroarilo pueden estar sustituidos por uno o más sustituyentes seleccionados del grupo consistente de hidroxilo, halógeno, NO2, CN, (C1-C6)-alquilo, (C1-C6)-alquilo sustituido por halógeno, (C1-C6)-alquilo sustituido por hidroxilo, (CH2)n(C1-C6)-alcoxilo, (C1-C6) -alcoxilo sustituido por halógeno, NR7R8, C(O)R9, SO2R10, -C(CH3)=NOR7, o por un heterociclo aromático de 5 miembros, que contiene 1-4 heteroátomos, seleccionados de N y O, que está opcionalmente sustituido por (C1-C6)-alquilo;R1 es hidrógeno o (C1-C6)-alquilo;R2 es hidrógeno, (C1-C6)-alquilo, (C2-C6)-alquenilo, (C1-C6)-alquilo sustituido por halógeno, (C1-C6)-alquilo sustituido por hidroxilo, (CH2)n-(C3-C7)-cicloalquilo opcionalmente sustituido por (C1-C6)-alcoxilo o por halógeno, o es CH(CH3)-(C3-C7)-cicloalquilo, (CH2)n+1-C(O)-R9, (CH2)n+1-CN, biciclo[(2,2,1]heptilo, (CH2)n+1-O-(C1-C6)-alquilo, (CH2)n-heterocicloalquilo, (CH2)n-arilo ó heteroarilo (CH2)n de 5 ó 6 miembros que contiene uno, dos o tres heteroátomos, seleccionados del grupo consistente de oxígeno, azufre o nitrógeno en donde arilo, heterocicloalquilo y heteroarilo están sin sustituir o sustituidos por uno o más sustituyentes seleccionados del grupo consistente de hidroxilo, halógeno, (C1-C6)-alquilo o (C1-C6) -alcoxilo;R3, R4 y R6 independientemente el uno del otro son hidrógeno, hidroxilo, halógeno, (C1-C6)-alquilo, (C1-C6)- alcoxilo o O-(C3-C6)-cicloalquilo;R5 es NO2, CN, C(O)R9 o SO2R10;R7 y R8 independientemente el uno del otro son hidrógeno o (C1-C6) -alquilo;R9 es hidrógeno, (C1-C6)-alquilo, (C1-C6)-alcoxilo ó NR7R8;R10 es (C1-C6)-alquilo opcionalmente sustituido por halógeno, (CH2)n - (C3-C6)-cicloalquilo, (CH2)n-(C3-C6)-alcoxilo, (CH2)n-heterocicloalquilo o NR7R8;n es 0, 1, ó 2; y las sales farmacéuticamente aceptables de adición ácida de los mismos, ...
CO06012502A 2003-08-11 2006-02-08 Piperazina con grupo fenilo or-sustituido y su uso como inhibidores de glyt1 CO5650253A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP03017614 2003-08-11

Publications (1)

Publication Number Publication Date
CO5650253A2 true CO5650253A2 (es) 2006-06-30

Family

ID=34130061

Family Applications (1)

Application Number Title Priority Date Filing Date
CO06012502A CO5650253A2 (es) 2003-08-11 2006-02-08 Piperazina con grupo fenilo or-sustituido y su uso como inhibidores de glyt1

Country Status (37)

Country Link
US (2) US7319099B2 (es)
EP (1) EP1656361B1 (es)
JP (1) JP4252598B2 (es)
KR (1) KR100774622B1 (es)
CN (1) CN1867554B (es)
AR (1) AR045360A1 (es)
AT (1) ATE382611T1 (es)
AU (1) AU2004263306B2 (es)
BR (1) BRPI0413497B8 (es)
CA (1) CA2534675C (es)
CO (1) CO5650253A2 (es)
CR (1) CR8193A (es)
CY (1) CY1108616T1 (es)
DE (1) DE602004011076T2 (es)
DK (1) DK1656361T3 (es)
EA (1) EA009986B1 (es)
EC (1) ECSP066358A (es)
EG (1) EG26404A (es)
ES (1) ES2297458T3 (es)
HK (1) HK1098147A1 (es)
HR (1) HRP20080137T3 (es)
IL (1) IL173274A (es)
MA (1) MA27995A1 (es)
ME (1) ME00116B (es)
MX (1) MXPA06001665A (es)
MY (1) MY145356A (es)
NO (1) NO332263B1 (es)
NZ (1) NZ544820A (es)
PL (1) PL1656361T3 (es)
PT (1) PT1656361E (es)
RS (2) RS53252B (es)
SI (1) SI1656361T1 (es)
TN (1) TNSN06042A1 (es)
TW (1) TWI289556B (es)
UA (1) UA85194C2 (es)
WO (1) WO2005014563A1 (es)
ZA (1) ZA200601146B (es)

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