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AR073046A1 - Espiro compuestos inhibidores de beta - secretasa - Google Patents

Espiro compuestos inhibidores de beta - secretasa

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Publication number
AR073046A1
AR073046A1 ARP090103187A ARP090103187A AR073046A1 AR 073046 A1 AR073046 A1 AR 073046A1 AR P090103187 A ARP090103187 A AR P090103187A AR P090103187 A ARP090103187 A AR P090103187A AR 073046 A1 AR073046 A1 AR 073046A1
Authority
AR
Argentina
Prior art keywords
alkyl
alkoxy
haloalkyl
cycloalkyl
nr12r13
Prior art date
Application number
ARP090103187A
Other languages
English (en)
Original Assignee
Vitae Pharmaceuticals Inc
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 Vitae Pharmaceuticals Inc filed Critical Vitae Pharmaceuticals Inc
Publication of AR073046A1 publication Critical patent/AR073046A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/20—Spiro-condensed systems
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/06—Antiglaucoma agents or miotics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P27/00—Drugs for disorders of the senses
    • A61P27/02—Ophthalmic agents
    • A61P27/08—Mydriatics or cycloplegics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/02—Heterocyclic 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
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic 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
    • C07D491/12—Heterocyclic 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 three hetero rings
    • C07D491/20—Spiro-condensed systems
    • 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
    • C07D495/02—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 two hetero rings
    • C07D495/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D498/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
    • C07D498/16—Peri-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/10—Spiro-condensed systems

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

Abstract

Un compuesto de la formula (1). También se describen una composicion farmacéutica que comprende un compuesto representado por la formula estructural (1) y un método de uso de este compuesto para inhibir la actividad de BACE en un sujeto que necesita dicho tratamiento. Reivindicacion 1: Un compuesto representado por la formula estructural (1) o una sal farmacéuticamente aceptable del mismo, en el que R1 es H, alquilo C1-6, arilalquilo C1-6, o heteroarilalquilo C1-6; cada R2 se selecciona independientemente entre a) -H, -F, -CI, -Br y -CN, y b) alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo, heteroarilo, fenoxi o benciloxi, cada uno opcionalmente sustituido con 1 a 3 sustituyentes seleccionados entre el grupo que consiste en -F, -CI, -Br, -CN, -OR5, -NR6R7, S(O)iR5, NR11S(=O)iR5, -C(=O)OR5, -C(=O)NR12R13, -NR11C(=O)R5, -C(=S)NR12R13, -C(=O)R5, alquilo C1-6, cicloalquilo C3-6, alquenilo C2-6, haloalquilo C1-6, alquil C1-3-sulfonilaminoalquilo, hidroxialquilo C1-6, cianoalquilo C1-6, alquil C1-3-carbonilaminoalquilo C1-6 alcoxi C1-3, haloalcoxi C1-3, alcoxi C1-6-alquilo C1-3, arilo y heteroarilo; cada R3 y R4 es independientemente -H, -halogeno, -CN, -NO2, -OR5, -NR6R7, -S(O)iR5, -C(=O)OR5, -C(=O)NR12R13, -C(=O)R5, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo o heteroarilo, donde cada alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-8, arilo o heteroarilo está opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente entre el grupo que consiste en -F, Cl, Br, -CN, -OR5, -NR6R7, -S(O)iR5, -NR11S(=O)R5, -C(=O)OR5, -C(=O)NR12R13, -NR1C(=O)R5, -C(=S)NR12R13, -C(=O)R5, alquilo C1-6, alquenilo C2-6, haloalquilo C1-6, alquil C1-3-sulfonilaminoalquilo, hidroxialquilo C1-6, cianoalquilo C1-6, alquil C1-3-carbonilaminoalquilo C1-6, alcoxi C1-3, haloalcoxi C1-3, alcoxi C1-6-alquilo C1-3, un grupo arilo y un grupo heteroarilo; X es -O-, -S-, -SO-, -SO2-, -CH2O- o -OCH2-; cada Y es independientemente -C(R8R9)-; W es -N(R14)-, -S-, -O-; Z es -C(=O)-, -C(=S)-, -C(=NR15)-, -O-, -C(=O)C(R15R17)-, -C(=S)C(R16R17)-, -C(=NR15)C(R16R17)-, -N(R18)-, -(CR16R17)m- o -O-(CR16R17)-; R5 es -H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxi C1-3-alquilo C1-6, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-6, cicloheteroalquilo C3-7, arilo, heteroarilo o bencilo, cada uno de los cuales está opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente entre el grupo que consiste en -F, -Cl, -Br, -CN, alquilo C1-6, haloalquilo C1-6 y alcoxi C1-3-alquilo C1-6; cada R6 y R7 se seleccionan independientemente entre -H, alquilo C1-6, hidroxialquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8 y cicloalquil C3-8-alquilo C1-6, cada uno opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente entre el grupo que consiste en -F, -CI, -Br, -CN, alquilo C1-6, haloalquilo C1-6 y alcoxi C1-3-alquilo C1-6; cada R8 y R9 se seleccionan independientemente entre H, alquilo C1-6, hidroxialquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquilo C3-14, cicloheteroalquilo C3-13, arilo o heteroarilo, cada uno opcionalmente sustituido con 1 a 4 sustituyentes seleccionados independientemente entre el grupo que consiste en -F, -CI, -Br, -CN, -OR5, -NR6R7, -S(O)iR5, -NR11S(=O)iR5, -C(O)OR5, -C(=O)NR12R13, -NR11C(=O)R5, -C(=S)NR12R13, -C(=O)R5, alquilo C1-6, alquenilo C2-6, haloalquilo C1-6, alquil C1-3-sulfonilaminoalquilo, hidroxialquilo C1-6, cianoalquilo C1-6, alquil C1-3-carbonilaminoalquilo C1-6, alcoxi C1-3, haloalcoxi C1-3, alcoxi C1-6-alquilo C1-3, arilo, heteroarilo, cicloalquilo C3-8 y cicloheteroalquilo C3-7, o R8 y R9, junto con el carbono al que están unidos, forman el anillo A, que es un anillo monocíclico de 3-14 miembros, bicíclico de 9-14 miembros o policíclico de 9-14 miembros, donde el anillo A está opcionalmente sustituido con 1 a 4 sustituyentes seleccionados independientemente entre el grupo que consiste en -F, -CI, -Br, -CN, -OR5, -NR6R7, -S(=O)iR5, -NR11S(=O)iR5, -C(=O)OR5, -C(=O)NR12R13, -NR11C(=O)R5, -C(=S)NR12R13, -C(=O)R5, alquilo C1-6, alquenilo C2-6, haloalquilo C1-6, alquil C1-3-sulfonilaminoalquilo, hidroxialquilo C1-6, cianoalquilo C1-6, alquil C1-3-carbonilaminoalquilo C1-6, alcoxi C1-3, haloalcoxi C1-3, alcoxi C1-6-alquilo C1-3, arilo y heteroarilo; R11 es -H, alquilo C1-6 o haloalquilo C1-6; cada R12 y R13 es independientemente -H, alquilo C1-6, alcoxi C1-3-alquilo C1-6, hidroxialquilo C1-6, cianoalquilo C1-6, aminoalquilo C1-6, alquilamino C1-3-alquilo C1-6 o dialquilamino C1-3-alquilo C1-6; o R12 y R13, junto con el nitrogeno al que están unidos, forman un anillo de 3-8 miembros opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente entre el grupo que consiste en -F, -CI, -Br, -CN, -OR5, -NR6R7, -S(=O)iR5, -NR11S(=O)iR5, -C(=O)OR5, -C(=O)NR12R13, -NR11C(=O)R5, -C(=S)NR12R13, -C(=O)R5, alquilo C1-6, alquenilo C2-6, haloalquilo C1-6, alquil C1-3-sulfonilaminoalquilo, hidroxialquilo C1-6, cianoalquilo C1-6, alquil C1-3-carbonilaminoalquilo C1-6, alcoxi C1-3, haloalcoxi C1-3 y alcoxi C1-6-alquilo C1-3, donde el anillo de 3-8 miembros contiene opcionalmente de 1 a 3 heteroátomos adicionales, que se seleccionan independientemente entre O, N y S, donde, cuando el heteroátomo adicional es nitrogeno, el nitrogeno está sustituido con -H, alquilo C1-3 o haloalquilo C1-3, y cuando el heteroátomo adicional es azufre, el azufre está opcionalmente mono o di-oxigenado; R14 es -H, alquilo C1-6, haloalquilo C1-6, cicloalquilo C3-8, cicloheteroalquilalquilo C1-3, cicloalquil C3-8-alquilo C1-3, arilalquilo C1-6, heteroarilalquilo C1-6, cada uno opcionalmente sustituido con 1 a 3 sustituyentes seleccionados independientemente entre el grupo que consiste en -F, -CI, -Br, -CN, alquilo C1-6, haloalquilo C1-6 y alcoxi C1-3; R15 es -H o alquilo C1-6; cada uno de R16 y R17 es independientemente -H o alquilo C1-3; R18 es -H o alquilo C1-3; i es 0, 1 o 2; p es 1 o 2; m es 1 o 2;y n es 1 o 2.
ARP090103187A 2008-08-19 2009-08-19 Espiro compuestos inhibidores de beta - secretasa AR073046A1 (es)

Applications Claiming Priority (2)

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US18946408P 2008-08-19 2008-08-19
US21175009P 2009-04-02 2009-04-02

Publications (1)

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AR073046A1 true AR073046A1 (es) 2010-10-06

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US (2) US8450308B2 (es)
EP (1) EP2324032B1 (es)
AR (1) AR073046A1 (es)
TW (1) TW201020256A (es)
UY (1) UY32062A (es)
WO (1) WO2010021680A2 (es)

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