AR114153A1 - Moduladores alostéricos positivos del receptor muscarínico de acetilcolina m₄ - Google Patents

Moduladores alostéricos positivos del receptor muscarínico de acetilcolina m₄

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Publication number
AR114153A1
AR114153A1 ARP180103545A ARP180103545A AR114153A1 AR 114153 A1 AR114153 A1 AR 114153A1 AR P180103545 A ARP180103545 A AR P180103545A AR P180103545 A ARP180103545 A AR P180103545A AR 114153 A1 AR114153 A1 AR 114153A1
Authority
AR
Argentina
Prior art keywords
cycloalkyl
hydrogen
heteroaryl
aryl
alkyl
Prior art date
Application number
ARP180103545A
Other languages
English (en)
Original Assignee
Univ Vanderbilt
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 Univ Vanderbilt filed Critical Univ Vanderbilt
Publication of AR114153A1 publication Critical patent/AR114153A1/es

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Classifications

    • 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
    • A61K31/495—Heterocyclic 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
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
    • 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
    • A61P25/28—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/12—Heterocyclic 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 three hetero rings
    • C07D495/14—Ortho-condensed systems

Landscapes

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

Abstract

En la presente se divulgan compuestos tricíclicos, incluidos compuestos de tipo tieno[2,3-d:4,5-d’]dipirimidin-4-amina y pirido[4’,3’:4,5]tieno[2,3-d]pirimidin-8-amina, que pueden ser útiles como moduladores alostéricos positivos del receptor muscarínico de acetilcolina M₄ (mAChR M₄). También se divulgan en la presente métodos de preparación de los compuestos, composiciones farmacéuticas que comprenden los compuestos y métodos de tratamiento de trastornos neurológicos y psiquiátricos asociados con el mal funcionamiento del receptor muscarínico de acetilcolina utilizando los compuestos y composiciones. Reivindicación 1: Un compuesto de fórmula (1), o una sal farmacéuticamente aceptable de estos, donde: X es N o CR⁵; R⁵ se selecciona entre hidrógeno, halo y ciano; R¹ se selecciona entre alquilo C₁₋₄, cicloalquilo C₃₋₆, hidrógeno, halo, -ORᵃ y -NRᵇRᶜ; R² y R³ se seleccionan cada uno independientemente entre hidrógeno, alquilo, alquenilo, alquinilo, arilo, heteroarilo, cicloalquilo, heteroalquilo, heterociclo y -(CRᵉRᶠ)ₙ-Y; o R² y R³ se consideran junto con el átomo de nitrógeno al que están unidos para formar un anillo heterocíclico; Y se selecciona entre halo, -OR, -SR, -C(O)R, -C(O)OR, -S(O)R, -SO₂R, -NR₂, -C(O)NR₂, -S(O)₂NR₂, arilo, heteroarilo, cicloalquilo y heterociclilo; n es 1, 2, 3, 4, 5, 6, 7 u 8; cada Rᵃ, Rᵇ y Rᶜ se seleccionan independientemente entre hidrógeno, alquilo C₁₋₄, haloalquilo C₁₋₄, arilo, heteroarilo, cicloalquilo y heterociclo; cada Rᵉ y Rᶠ se seleccionan independientemente entre hidrógeno, alquilo C₁₋₄, haloalquilo C₁₋₄ y halo; y cada R se selecciona independientemente entre hidrógeno, alquilo, arilo, arilalquilo, cicloalquilo, cicloalquilalquilo, heterociclo, heterocicloalquilo, heteroarilo, heteroarilalquilo y heteroalquilo; donde cada arilo, cicloalquilo, heterociclo y heteroarilo esta independientemente no sustituido o sustituido con 1, 2 ó 3 sustituyentes.
ARP180103545A 2017-12-05 2018-12-04 Moduladores alostéricos positivos del receptor muscarínico de acetilcolina m₄ AR114153A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US201762594849P 2017-12-05 2017-12-05

Publications (1)

Publication Number Publication Date
AR114153A1 true AR114153A1 (es) 2020-07-29

Family

ID=64902428

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP180103545A AR114153A1 (es) 2017-12-05 2018-12-04 Moduladores alostéricos positivos del receptor muscarínico de acetilcolina m₄

Country Status (8)

Country Link
US (1) US10736898B2 (es)
EP (1) EP3720860A1 (es)
JP (1) JP2021505580A (es)
CN (1) CN111433212A (es)
AR (1) AR114153A1 (es)
MA (2) MA51038A (es)
TW (1) TW201930311A (es)
WO (1) WO2019113179A1 (es)

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Also Published As

Publication number Publication date
JP2021505580A (ja) 2021-02-18
TW201930311A (zh) 2019-08-01
US10736898B2 (en) 2020-08-11
MA51038A (fr) 2020-10-14
WO2019113179A1 (en) 2019-06-13
CN111433212A (zh) 2020-07-17
US20190167688A1 (en) 2019-06-06
EP3720860A1 (en) 2020-10-14
MA51037A (fr) 2021-03-17

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