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AR065814A1 - Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. - Google Patents

Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados.

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Publication number
AR065814A1
AR065814A1 ARP080101183A ARP080101183A AR065814A1 AR 065814 A1 AR065814 A1 AR 065814A1 AR P080101183 A ARP080101183 A AR P080101183A AR P080101183 A ARP080101183 A AR P080101183A AR 065814 A1 AR065814 A1 AR 065814A1
Authority
AR
Argentina
Prior art keywords
phenyl
difluoromethoxy
amino
dihydro
methyl
Prior art date
Application number
ARP080101183A
Other languages
English (en)
Inventor
Koi M Morris
William R Solvibile
Albert Jean Robichaud
Ji-In Kim
Alexander M Porte
Michael Malas
Original Assignee
Wyeth Corp
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Filing date
Publication date
Application filed by Wyeth Corp filed Critical Wyeth Corp
Publication of AR065814A1 publication Critical patent/AR065814A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members
    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two 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
    • C07D233/70—One oxygen 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
    • 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
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links

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

Abstract

Reivindicacion 1: Un compuesto de la formula 1 caracterizado porque R1 y R2 son cada uno independientemente H o un grupo alquilo, cicloalquilo, cicloheteroalquilo, arilo o heteroarilo cada uno se sustituye opcionalmente o R1 y R2 se pueden tomarjunto con el átomo al cual ellos se adhieren para formar un anillo de 5 a 7 miembros opcionalmente sustituido que se interrumpe opcionalmente por un heteroátomo adicional seleccionado de O, N o S; R3 es H o un grupo alquilo, cicloalquilo,cicloheteroalquilo, arilo o heteroarilo cada uno se sustituye opcionalmente R4, R5 y R6 son cada uno independientemente H, halogeno, NO2, CN, COR7, NR10CO2R11, NR15COR16, OR14, NR12R13, SOnR17 o un grupo alquilo, haloalquilo, alquenilo,haloalquenilo, alquinilo, cicloalquilo, o cicloheteroalquilo cada uno se sustituye opcionalmente o cuando se adhieren a los átomos de carbono adyacentes R4 y R5 se pueden tomar junto con los átomos a los cuales ellos se adhieren para formar unanillo de 5 a 7 miembros opcionalmente sustituido que contiene opcionalmente uno o dos heteroátomos seleccionados de O, N o S; n es 0, 1 o 2; R7 y R17 son cada uno independientemente H, NR8R9, o un grupo alquilo, haloalquilo, alcoxialquilo,alquenilo, alquinilo, cicloalquilo o arilo cada uno se sustituye opcionalmente; R8 y R9 son cada uno independientemente H o un grupo alquilo, alquenilo, alquinilo o cicloalquilo cada uno se sustituye opcionalmente o R8 y R9, se pueden tomar juntocon el átomo al cual ellos se adhieren para formar un anillo de 5 a 7 miembros opcionalmente sustituido que contiene opcionalmente un heteroátomo adicional seleccionado de O, N o S; R11, R14 y R16, son cada uno independientemente H o un grupoalquilo, haloalquilo, alcoxialquilo, alquenilo, alquinilo. cicloalquilo, heteroarilo o arilo cada uno se sustituye opcionalmente; R10 y R15 son cada uno independientemente H o un grupo alquilo opcionalmente sustituido; y R12 y R13 son cada unoindependientemente H o un grupo alquilo, alquenilo, arilo o cicloalquilo cada uno se sustituye opcionalmente o R12 y R13 se pueden tomar junto con el átomo al cual ellos se adhieren para formar un anillo de 5 a 7 miembros opcionalmente sustituidoque contiene opcionalmente un heteroátomo adicional seleccionado de O, N o S; o un tautomero de éstos, un estereoisomero de estos o una sal farmacéuticamente aceptable de estos; proporciona que el compuesto no se selecciona del grupo que consistede: 2-amino-5-(4-(difluorometoxi)fenil]-3-metil-5-fenil-3,5-dihidro-4H-imidazol-4-ona; (5S)2-Amino-5-[4-(difluorometoxi)fenil]-3-metil-5-fenil-3,5-dihidro-4H-imidazol-4-ona; (5R)-2-Amino-5-[4-(difluorometoxi)-fenil]-3-metil-5-fenil-3,5-dihidro-4H-imidazol-4-ona; (5R)-2-amino-5-(3-bromofenil)-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro- 4H-imidazol-4-ona; 2-amino-5-(3-bromofenil)-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; (5R)-2-Amino-5-(3-bromo-4-fluorofenil)-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-(3-bromo-4-fIuorofenil)-5-[4-difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona, 2-Amino-5-[4-(difluorometoxi)fenil]-3-metil-5-(3-propilo fenil)-3,5-dihidro-4H-imidazol-4-ona; (5R)-2-Amino-5-[4-(difluorometoxi)fenil]-3-metil-5-(3-propilo fenil)-3,5-dihidro-4H-imidazol-4-ona; (5S)-2-Amino-5-[4-(difluorometoxi)fenil]-3-metil-5-(3-propilo fenil)-3,5-dihidro-4H-imidazol-4-ona; (5R)-2-amino-5-(3-butilfenil)-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona, (5S)-2-amino-5-(3-butilfenil)-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H- imidazol-4-ona; 2-amino-5-(3-butilfenil)-5-(4-(difluorometoxi)fenil]-3metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4(difluorometoxi)fenil]-3-metil-5-(3-pentilfenil)-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]l-3-metil-5-(3-(2-metilbutil)fenil]3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-(3-but-3-en-1-ilfenil)-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[3-(ciclopropilo metil)fenil]-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 3-(3-{2-Amino-4-[4-(difluorometoxi)fenil]-1-metil-5-oxo-4,5-dihidro-1H-imidazol-4-iI}fenil)propanonitrilo; (5R)-2-Amino-5-[4-(difluorometoxi)fenil]-3-metiI-5-(3-pent-4-en-1-ilfenil)-3,5-dihidro-4H-imidazol-4-ona; (5S)-2-Amino-5-[4-(difluorometoxi)fenil]-3-metiI-5-(3pent-4-en-1-ilfenil)-3,5- dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-3-metil-5-(3-pent-4-en-1-ilfenil)-3,5-dihidro-4H-imidazol-4-ona; N-(3-{(4R)-2-Amino-4-[4-(difluorometoxi)fenil]-1-metil-5-oxo-4,5-dihidro-1H-imidazol-4-il}fenil)-2-metoxiacetamida; N-(3-{(4S)-2-Amino-4-[4-(difluorometoxi)fenil]-1-metii-5-oxo-4,5-dihidro-1H-imidazol-4-iI}fenil)-2-metoxiacetamida; N-3-(2-Amino-4-[4-(difluorometoxi)fenil]I-1-metil-5-oxo-4,5-dihidro-1H-imidazol-4-iI}fenil)-2-metoxiacetamida; 2-Amino-5-[4-(difluorometoxi)fenil]-3-metiI-5-[3-(4,4,4-trifluorobutil)fenil]-3,5-dihidro-4H-imidazol-4-ona; 5-(3-{2-Amino-4-[4-(difluorometoxi)fenil]-1-metil-5-oxo-4,5-dihidro-1H-imidazol-4-iI}fenil)pentanonitrilo, 4-(3-{2-amino-4-[4-(difluorometoxi)fenil]-1-metil-5-oxo-4,5-dicloro-1H-imidazol-4-il}fenil)butanonitrilo; 2-Amino-5-[3-(1,4-difluorobutil)fenil]-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona, 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(3-fluorobut-3-en-1-il)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona, 2-Amino-5-[3-(4,4-difluorobut-3-en-1-il)fenil]-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona, 2-Amino-5-[3-(4,4-difluorobutil)fenil]-5-[4-(difluorometoxi)-fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(4-hidroxibut-1-in-1-il)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3(4-hidroxibutil)-fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(3-metoxiprop-1-in-1-il)-fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-{3-[(1Z)-3-metoxiprop-1-en-1-il]fenil}-3-metiI-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(3-metoxipropilo)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-8difluorometoxi)fenil]-5-3-(5-fluoropentil)-fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(4-fluorobutil)-fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(6-fluorohexil)-fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-amino-5-[4-(difluorometoxi)fenil]-5-[3-(6-fluorohexil)-fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 3-(2-Amino-4-[4-(difluorometoxi)fenil]-1-metil-5-oxo-4,5-dihidro-1H-imidazol-4-il)-N-propilo benzamida; 2-Amino-5-[4-(difluorometoxi)fenil]-5-{3-[(2-fluoroetoxi)-metil]fenil}-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-amino-5-[4-(difluorometoxi)fenil]-3-metil-5-{3[(2,2,2-trifluoroetoxi)metil]fenil}-3,5-dihidro-4H-imidazol-4-ona; 2-amino-5-[4-(difluorometoxi)fenil]-3-metil-5-{3-[(2,2,3,3-tetrafluoropropoxi)metil]fenil}-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-{3-[(1E)-6-metoxi-hex-1-en-1-il]-fenil}-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-{3-[(1E)-5-hidroxi-pent-1-en-1-il]-fenil}-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-{3-[2-(metoximetil)-ciclopropilo]fenil}-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-{3-[2-(2-metoxietil)-ciclopropilo]fenil}-3-metil-3,5-dihidro-4H-imidazol-4-ona; 5-(3-Acetilfenil)-2-amino-5-[4-(difluorometoxi)fenil]-3-metiI-3,5-dihidro-4H-imidazol-4-ona, 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(3-hidroxihex-4-in-1-il)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(3-fluoroprop-1-in-1-il)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-(3hidroxifenil)-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[-(-fluoropropox-1-il)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-(4-fluoro-3-hidroxi-fenil)-3-metil-3,5-dihidro-4H-imidazol-4-ona; (5R)-2-Amino-5-[4-(difluorometoxi)fenil]-5-[4-fluoro-3-(3-fluoropropox-1-il)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; (5S)-2-Amino-5-[4-(difluorometoxi)fenil]-5-[4-fluoro-3-(3-fluoropropox-1-il)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; (5R)-2-Amino-5-[3-(2,2-difluoroetoxi)-4-fluorofenil]-5-[4-difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; (5S)-2Aminio-5-[3-(2,2-difluoroetoxi)-4-fluorofenil]-5-[4-difluorometoxi)-fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-{3-[(4,4-difluorobut-3-en-1-il)oxi]fenil)-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-{3-[(4,4-difIuorobut-3-en-1-il)oxi]-4-fIuorofenil}-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-(4-(difluorometoxi)fenil]-5-(4-fluoro-3-pent-4-en-1-il)-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-(3-but-3-en-1-iI-4fIuorofenil)-5-[4-(difluorometoxi)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(1-hidroxibut-2-in-1-il)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-(3-(1,4-dihidroxibut-2-in-1-il)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(2,2-dimetil-3-oxociclobutil)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-3-metil-5-[3-(3-oxociclobutil)fenil]-3,5-dihidro-4H-imidazol-4-ona; 2-Amino-5-[4-(difluorometoxi)fenil]-5-[3-(3-hidroxi-ciclobutil)fenil]-3-metil-3,5-dihidro-4H-imidazol-4-ona; etil [3-(3-{2-Amino-4-[4-difluorometoxi)fenil]-1metil-5-oxo-4,5-dihidro-1H-imidazol-4-il}fenil)ciclobutilideno]acetato; metil [3-(3-{2-Amino-4-[4-difluorometoxi)fenil]-1metil-5-oxo-4,5-dihidro-1H-imidazol-4-il}fenil)ciclobutilideno]acetato; metil [3-(3-{2-Amino-4-[4-difluorometoxi)fenil]-1metil-5-oxo-4,5-dihidro-1H-imidazol-4-il}fenil)ciclobutil]acetato; 2-Amino-5-[3-(difluorometoxi)fenil]-5-[4-(difluorometoxi)-fe
ARP080101183A 2007-03-23 2008-03-19 Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados. AR065814A1 (es)

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US (2) US7723368B2 (es)
EP (1) EP2144884A2 (es)
JP (1) JP2010522237A (es)
CN (1) CN101663281A (es)
AR (1) AR065814A1 (es)
AU (1) AU2008232341A1 (es)
BR (1) BRPI0809162A2 (es)
CA (1) CA2681431A1 (es)
CL (1) CL2008000791A1 (es)
MX (1) MX2009010057A (es)
PE (1) PE20090617A1 (es)
TW (1) TW200901978A (es)
WO (1) WO2008118379A2 (es)

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AR065814A1 (es) * 2007-03-23 2009-07-01 Wyeth Corp Derivados de 5-fenilimidazolona,inhibidores de beta-secretasa,composiciones farmaceuticas que los contienen y usos para prevenir y/o tratar trastornos asociados a niveles beta-amiloides elevados.
US8450308B2 (en) 2008-08-19 2013-05-28 Vitae Pharmaceuticals, Inc. Inhibitors of beta-secretase
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