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AR101392A1 - COMPUESTOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4(5H)-ONA Y SU USO COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE RECEPTORES mGluR2 - Google Patents

COMPUESTOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4(5H)-ONA Y SU USO COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE RECEPTORES mGluR2

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Publication number
AR101392A1
AR101392A1 ARP150102461A ARP150102461A AR101392A1 AR 101392 A1 AR101392 A1 AR 101392A1 AR P150102461 A ARP150102461 A AR P150102461A AR P150102461 A ARP150102461 A AR P150102461A AR 101392 A1 AR101392 A1 AR 101392A1
Authority
AR
Argentina
Prior art keywords
alkyl
group
monohalo
polyhalo
nrr
Prior art date
Application number
ARP150102461A
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English (en)
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Janssen Pharmaceutica Nv
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Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR101392A1 publication Critical patent/AR101392A1/es

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    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • A61K31/41621,2-Diazoles condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • 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
    • 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

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

Abstract

Reivindicación 1: Un compuesto de fórmula (1) o una forma estereoisomérica del mismo, en donde R¹ es fenilo o 2-piridinilo, cada uno opcionalmente sustituido por uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, alquilo C₁₋₄, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -alquil C₁₋₄-OH, -CN, -alquil C₁₋₄-O-alquilo C₁₋₄, cicloalquilo C₁₋₄, -O-alquilo C₁₋₄, monohalo-alquil C₁₋₄oxi, polihalo-alquil C₁₋₄oxi, SF₅, alquil C₁₋₄tio, monohalo-alquil C₁₋₄tio y polihalo-alquil C₁₋₄tio; R² se selecciona del grupo que consiste en hidrógeno; alquilo C₁₋₄; cicloalquilo C₃₋₇; Het¹; arilo; -C(O)R⁵; -C(O)Het²; Het²; y alquilo C₁₋₄ sustituido por uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, cicloalquilo C₃₋₇, arilo, Het¹ y Het²; en donde R⁵ se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₄ y cicloalquilo C₃₋₇; arilo es fenilo opcionalmente sustituido por uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, alquilo C₁₋₄, -alquil C₁₋₄-OH, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -CN, -O-alquilo C₁₋₄, -OH, alquil C₁₋₄-O-alquilo C₁₋₄, -NRR, -NHC(O)alquilo C₁₋₄, -C(O)NRR, -C(O)NH[C(O)alquil C₁₋₄], -S(O)₂NRR, -S(O)₂NH[C(O)alquil C₁₋₄] y -SO₂-alquilo C₁₋₄; Het¹ se selecciona del grupo que consiste en oxetanilo, tetrahidrofuranilo y tetrahidropiranilo; Het² es (a) un sustituyente heterociclilo aromático de 6 miembros que se selecciona del grupo que consiste en piridinilo, pirimidinilo, pirazinilo y piridazinilo, cada uno de los cuales puede sustituirse opcionalmente con uno o más sustituyentes seleccionados cada uno independientemente del grupo que consiste en halo, alquilo C₁₋₄, -alquil C₁₋₄-OH, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -CN, -O-alquilo C₁₋₄, -OH, -alquil C₁₋₄-O-alquilo C₁₋₄, -NRR, -NHC(O)alquilo C₁₋₄, -C(O)NRR, -C(O)NH[C(O)alquil C₁₋₄], -S(O)₂NRR, -S(O)₂NH[C(O)alquil C₁₋₄] y -SO₂-alquilo C₁₋₄; o (b) un heterociclilo aromático de 5 miembros que se selecciona del grupo que consiste en tiazolilo, oxazolilo, 1H-pirazolilo y 1H-imidazolilo, cada uno de los cuales puede sustituirse opcionalmente con uno o más sustituyentes seleccionados cada una independientemente del grupo que consiste en halo, alquilo C₁₋₄, -alquil C₁₋₄-OH, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -CN, -O-alquilo C₁₋₄, -OH, -alquil C₁₋₄-O-alquilo C₁₋₄, -NRR, -NHC(O)alquilo C₁₋₄, -C(O)NRR, -C(O)NH[C(O)alquil C₁₋₄], -S(O)₂NRR, -S(O)₂NH[C(O)alquil C₁₋₄] y -SO₂-alquilo C₁₋₄; cada R y R se selecciona independientemente de hidrógeno y alquilo C₁₋₄; y R³ se selecciona de hidrógeno y alquilo C₁₋₄; R⁴ se selecciona del grupo que consiste en hidrógeno, alquilo C₁₋₄, monohalo-alquilo C₁₋₄, polihalo-alquilo C₁₋₄, -alquil C₁₋₄-O-alquilo C₁₋₄ y -alquil C₁₋₄-OH; o un N-óxido, o una sal farmacéuticamente aceptable o un solvato del mismo.
ARP150102461A 2014-08-01 2015-07-31 COMPUESTOS DE 6,7-DIHIDROPIRAZOLO[1,5-A]PIRAZIN-4(5H)-ONA Y SU USO COMO MODULADORES ALOSTÉRICOS NEGATIVOS DE RECEPTORES mGluR2 AR101392A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP14179598 2014-08-01

Publications (1)

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AR101392A1 true AR101392A1 (es) 2016-12-14

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US (3) US10005786B2 (es)
EP (1) EP3177623B1 (es)
JP (1) JP6662846B2 (es)
KR (1) KR102531689B1 (es)
CN (1) CN106573936B (es)
AR (1) AR101392A1 (es)
AU (1) AU2015295298B2 (es)
BR (1) BR112017001726A2 (es)
CA (1) CA2954093C (es)
CL (1) CL2017000192A1 (es)
CY (1) CY1121649T1 (es)
DK (1) DK3177623T3 (es)
EA (1) EA031087B1 (es)
ES (1) ES2708215T3 (es)
HR (1) HRP20181997T1 (es)
HU (1) HUE042871T2 (es)
IL (1) IL250298A0 (es)
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PH (1) PH12017500161B1 (es)
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SG (1) SG11201700638YA (es)
SI (1) SI3177623T1 (es)
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JP6662846B2 (ja) 2020-03-11
SMT201900038T1 (it) 2019-02-28
EP3177623B1 (en) 2018-11-07
HUE042871T2 (hu) 2019-07-29
CA2954093A1 (en) 2016-02-04
EA201692540A1 (ru) 2017-05-31
MX376289B (es) 2025-03-07
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US20180256569A1 (en) 2018-09-13
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