AR109810A1 - 1h-imidazo[4,5-b]piridin-2(3h)-onas sustituidas y uso de estas como moduladores del receptor glun2b - Google Patents

1h-imidazo[4,5-b]piridin-2(3h)-onas sustituidas y uso de estas como moduladores del receptor glun2b

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Publication number
AR109810A1
AR109810A1 ARP170102779A ARP170102779A AR109810A1 AR 109810 A1 AR109810 A1 AR 109810A1 AR P170102779 A ARP170102779 A AR P170102779A AR P170102779 A ARP170102779 A AR P170102779A AR 109810 A1 AR109810 A1 AR 109810A1
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substituted
alkyl
group
members
independently selected
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ARP170102779A
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Janssen Pharmaceutica Nv
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    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic 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
    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/12—Ketones
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
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    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/22—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
    • 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
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C—CHEMISTRY; METALLURGY
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    • C07D471/00—Heterocyclic 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
    • C07D471/02—Heterocyclic 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
    • C07D471/04—Ortho-condensed systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • 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
    • C07D207/04—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 no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—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 no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
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  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Health & Medical Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Psychology (AREA)
  • Hospice & Palliative Care (AREA)
  • Addiction (AREA)
  • Rheumatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)

Abstract

Reivindicación 1: Un compuesto, y sales farmacéuticamente aceptables, solvatos, estereoisómeros, variantes isotópicas o N-óxidos de estos, que tienen una estructura de la fórmula (1), en donde R¹ es H; CH₂F; o CH₃; R² se selecciona del grupo que consiste en fenilo; fenilo sustituido con uno, dos o tres miembros, cada uno seleccionado independientemente del grupo que consiste en halo, alquilo C₁₋₆, haloalquilo C₁₋₆, CN, O-alquilo C₁₋₆, O-haloalquilo C₁₋₆, N(CH₃)₂ y ciclopropilo; piridinilo; piridinilo sustituido con F, alquilo C₁₋₄ o haloalquilo C₁₋₄; tiazolilo; tiazolilo sustituido con alquilo C₁₋₆ o haloalquilo C₁₋₆; tienilo; y tienilo sustituido con uno o dos miembros, cada uno seleccionado independientemente del grupo que consiste en halo, alquilo C₁₋₆, haloalquilo C₁₋₆, CH₂OH, CH₂OCH₃ y ciclopropilo; R³ es H; R⁴ se seleccionada del grupo que consiste en: (a) un compuesto de fórmula (2), en donde el anillo A es un heterociclo de 4 - 6 miembros que contiene opcionalmente un heteroátomo de oxígeno adicional seleccionado del grupo que consiste en azetidinilo; azetidinilo sustituido con uno o dos miembros seleccionados independientemente del grupo que consiste en: F, OH, alquilo C₁₋₄, haloalquilo C₁₋₄, CH₂OCH₃, CN y OCH₃; pirrolidinilo; pirrolidinilo sustituido con dos miembros F; morfolinilo; piperidinilo; piperazinilo sustituido con alquilo C₁₋₆; y (2,6-diazaspiro[3.3]heptan-6-il); (b) un compuesto de fórmula (3), en donde R⁴ᵇ se selecciona del grupo que consiste en: H; alquilo C₁₋₆; CH₂CH₂OCH₃; cicloalquilo C₃₋₆; cicloalquilo C₃₋₆ sustituido con dos o tres miembros seleccionados independientemente del grupo que consiste en F o CH₃; oxetanilo; oxetanilo sustituido con CH₃; y piridinilo; (c) un compuesto de fórmula (4), en donde R⁴ᶜ se selecciona del grupo que consiste en ciclopropilo; ciclopropilo sustituido con uno o dos miembros F; CH(OH)ciclopropilo; azetidinilo; CH₂-azetidinilo; CH₂-azetidinilo sustituido con uno o dos miembros seleccionados independientemente de: F, OH, OCH₃ y CF₃; oxetanilo; oxetanilo sustituido con F o CH₃; tetrahidrofuranilo; tetrahidropiranilo; CH₂-pirrolidinilo; CH₂-pirrolidinilo sustituido con CH₃, OH u OCH₃; CH₂-piperidinilo; CH₂-piperidinilo sustituido con OH o F; morfolinilo; pirazolilo sustituido con uno o dos miembros CH₃; triazolilo sustituido con CH₃; tetrazolilo; isoxazolilo sustituido con uno o dos miembros CH₃; oxadiazolilo sustituido con CH₃ o CH₂OCH₃; tiadiazolilo; piridinilo; piridinilo sustituido con uno o dos miembros seleccionados independientemente del grupo que consiste en: Cl, F, CH₃, OCH₃ y CF₃; (2-oxo-1H-piridin-3-il); 6-oxo-1H-piridin-3-ilo; pirimidinilo; pirimidinilo sustituido con F o CH₃; pirazinilo; piridazinilo; piridazinilo sustituido con OCH₃; fenilo; fenilo sustituido con uno o dos miembros seleccionados independientemente del grupo que consiste en halo, CN, OCH₃, alquilo C₁₋₆ y CF₃; (d) un compuesto de fórmula (5), en donde R⁴ᵈ se selecciona del grupo que consiste en: OH, alquilo C₁₋₆, O-alquilo C₁₋₆, cicloalquilo C₃₋₆, tienilo y tiazolilo; y (e) alquilo C₂₋₆ sustituido con uno o dos miembros seleccionados independientemente de OH, O alquilo C₁₋₆ o ciclopropilo; CH₂CH₂NH(alquilo C₁₋₆); CH₂CH₂NH(CH₂CH₂OH); CH₂CH₂NH(cicloalquilo C₃₋₆); y difluoro(3-piridil)metilo; y R¹ᵃ y R¹ᵇ son cada uno, independientemente, H o CH₃.
ARP170102779A 2016-10-06 2017-10-05 1h-imidazo[4,5-b]piridin-2(3h)-onas sustituidas y uso de estas como moduladores del receptor glun2b AR109810A1 (es)

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US (4) US10617676B2 (es)
EP (1) EP3523311B1 (es)
JP (1) JP7001682B2 (es)
KR (1) KR20190056435A (es)
CN (2) CN114989164B (es)
AR (1) AR109810A1 (es)
AU (1) AU2017340602A1 (es)
BR (1) BR112019006691A2 (es)
CA (1) CA3038820A1 (es)
CL (1) CL2019000882A1 (es)
EA (1) EA201990848A1 (es)
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IL (1) IL265757A (es)
MA (1) MA46470A (es)
MX (1) MX2019003980A (es)
PH (1) PH12019500676A1 (es)
TW (1) TW201819376A (es)
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