AR035260A1 - Derivados de piperidina amino sustituidas, composiciones farmaceuticas y el uso de dichos derivados para la preparacion de medicamentos como inhibidores de la gama secretasa, y para el tratamiento de la enfermedad de alzheimer - Google Patents

Derivados de piperidina amino sustituidas, composiciones farmaceuticas y el uso de dichos derivados para la preparacion de medicamentos como inhibidores de la gama secretasa, y para el tratamiento de la enfermedad de alzheimer

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Publication number
AR035260A1
AR035260A1 ARP020102925A ARP020102925A AR035260A1 AR 035260 A1 AR035260 A1 AR 035260A1 AR P020102925 A ARP020102925 A AR P020102925A AR P020102925 A ARP020102925 A AR P020102925A AR 035260 A1 AR035260 A1 AR 035260A1
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alkyl
independently selected
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different
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ARP020102925A
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Schering Corp
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    • 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
    • C07D401/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 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
    • C07D211/56—Nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 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
    • C07D211/56—Nitrogen atoms
    • C07D211/58—Nitrogen atoms attached in position 4
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
    • C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D211/06—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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
    • C07D211/36—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings 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 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
    • C07D211/60—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D211/62—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals attached in position 4
    • 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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms

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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (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)
  • Hydrogenated Pyridines (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Abstract

Derivados de piperidina amino sustituidas, que comprenden un compuesto de la fórmula (1) o las sales o solvatos farmacéuticamente aceptables del mismo, en el cual: Ar1 y Ar2 son independientemente seleccionados entre arilo y heteroarilo; Y es un enlace, o Y representa un grupo -(C(R3)2)1-3-; Cada R1 es independientemente seleccionado entre: alquilo (C1-6); arilo; arilo sustituido con uno o más sustituyentes independientemente seleccionados entre halógeno, CF3, alquilo (C1-6), alcoxi (C1-6), OCF3, NH2 o CN; heteroarilo; heteroarilo sustituido con uno o más sustituyentes independientemente seleccionados entre halógeno, CF3, alquilo (C1-6), alcoxi (C1-6), OCF3, NH2 o CN; halógeno; -CF3; -OCF3; -CN; -NO2; -NH2; -C(O)NHalquilo (C1-6); -C(O)N(alquilo (C1-6))2, donde cada grupo alquilo (C1-6) es igual o diferente de los demás; -C(O)N(alquilo (C1-6))2, donde cada grupo alquilo (C1-6) es igual o diferente de los demás y dichos grupos alquilo (C1-6) tomados junto con el nitrógeno al cual están unidos forman un anillo; -NHC(O)alquilo (C1-6), -NHC(O)Oalquilo (C1-6), -NHC(O)NHalquilo (C1-6), -NHSO2alquilo (C1-6); -OH; -OC(O)alquilo (C1-6); -Oalquilo (C1-6); -Oarilo; u -Oaralquilo (C1-6); Cada R2 es independientemente seleccionado entre: alquilo (C1-6); halógeno; -CF3; -OCF3; -CN; -NO2; -NH2; -C(O)Oalquilo (C1-6); -C(O)NHalquilo (C1-6), -N(alquilo (C1-6))2- donde cada sustituyente alquilo (C1-6) es igual o diferente de los demás; -N(alquilo (C1-6))2, donde cada sustituyente alquilo (C1-6) es igual o diferente de los demás y los sustituyentes alquilo (C1-6), junto con el átomo de nitrógeno al cual están unidos forman un anillo; -NHC(O)alquilo (C1-6); -NHC(O)Oalquilo (C1-6); -NHC(O)NHalquilo (C1-6); -NHSO2alquilo (C1-6); -OH; -OC(O)alquilo (C1-6); -Oalquilo (C1-6); -Oarilo; Oar-alquilo (C1-6); arilo; arilo sustituido con uno o más sustituyentes independientemente seleccionados entre: halógeno, CF3, alquilo (C1-6), alcoxi (C1-6), OCF3, NH2 o CN; heteroarilo; heteroarilo sustituido con uno o más sustituyentes independientemente seleccionados entre halógeno, CF3, alquilo (C1-6), alcoxi (C1-6) OCF3, NH2 o CN; -C(O)N(alquilo (C1-6))2 donde cada grupo alquilo es independientemente seleccionado; -C(O)N(alquilo (C1-6))2 donde cada grupo alquilo es independientemente seleccionado y donde los grupos alquilo, tomados junto con el átomo de nitrógeno, forman un anillo heterocicloalquilo; o un grupo seleccionado entre los restos de fórmulas (2) a (6); Cada R3 es independientemente seleccionado entre H y alquilo (C1-3); Cada R4 es independientemente seleccionado entre: alquilo (C1-3); -OH; u -Oalquilo (C1-3); R5 es seleccionado entre: hidrógeno; alquilo (C1-6); arilo; heteroarilo; -alquilen(C1-3)-Oalquilo(C1-3); -alquilen(C1-6)-S(O)0-2alquilo(C1-3); -alquilen(C1-8)-S(O)0-2NHalquilo(C1-3); -C(O)alquilo (C1-6); C(O)arilo; -C(O)aralquilo (C1-3), -C(O)heteroarilo; -C(O)heteroaralquilo (C1-3); -C(O)Oalquilo (C1-6); -C(O)NHalquilo (C1-6); -C(O)N(alquilo (C1-6))2, donde cada grupo alquilo C1-6 es igual o diferente de los demás; -C(O)N(alquilo (C1-6))2, donde cada grupo alquilo C1-6 es igual o diferente de los demás y donde los grupos alquilo C1-6, tomados junto con el nitrógeno al cual están unidos, forman un anillo de heterocicloalquilo; -C(O)alquilen(C1-3)-NHalquilo(C1-3); -C(O)alquilen(C1-3)-N(alquilo (C1-3))2; donde cada grupo alquilo es seleccionado independientemente; -SO2alquilo (C1-6); -SO2NHalquilo (C1-6); -SO2N(alquilo (C1-6))2; donde cada grupo alquilo C1-6 es igual o diferente de los demás; -SO2N(alquilo (C1-6))2, donde cada grupo alquilo C1-6 es igual o diferente de los demás y donde los grupos alquilo C1-6, tomados junto con el nitrógeno al cual están unidos, forman un anillo de heterocicloalquilo o un grupo de la fórmula (7), (8), (9) o (10); R6 es -H o alquilo (C1-6); X es seleccionado entre CH2, O, S, SO, SO2 o N-R7; R7 es seleccionado entre alquilo (C1-6), cicloalquilo (C3-6), alquilen(C1-3)-cicloalquilo(C3-6); arilo, aralquilo (C1-3), heteroarilo, heteroaralquilo (C1-3), -C(O)alquilo (C1-6), -C(O)arilo; -C(O)aralquilo (C1-3), -C(O)heteroarilo; -C(O)heteroaralquilo (C1-3), -C(O)Oalquilo (C1-6), -C(O)NHalquilo (C1-6), -C(O)N(alquilo (C1-6))2, donde cada grupo C1-6 es igual o diferente a los demás; -C(O)N(alquilo (C1-6))2, donde cada grupo alquilo C1-6 es igual o diferente a los demás y donde los grupos alquilo C1-6, tomados junto con el nitrógeno al cual están unidos, forman un anillo heterocicloalquilo; -C(O)alquilen(C1-3)-NHalquilo(C1-3), -C(O)alquilen(C1-3)-N(alquilo (C1-3))2, donde los grupos alquilo C1-3 son iguales o diferentes; o -alquilen(C1-3)-O-alquilo(C1-3); n y p son independientemente seleccionados entre 0 a 3 para formar un anillo de 4 a 7 miembros; r representa de 0 a 3; q representa de 0 a 3 y t representa de 0 a 3. También se describen composiciones farmacéuticas y el uso de dichos compuestos para la preparación de medicamentos para inhibir la gama secretasa y para el tratamiento de la enfermedad de Alzheimer.
ARP020102925A 2001-08-03 2002-08-01 Derivados de piperidina amino sustituidas, composiciones farmaceuticas y el uso de dichos derivados para la preparacion de medicamentos como inhibidores de la gama secretasa, y para el tratamiento de la enfermedad de alzheimer AR035260A1 (es)

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US (2) US7122675B2 (es)
EP (1) EP1411944A1 (es)
JP (1) JP2005504042A (es)
CN (1) CN1780621A (es)
AR (1) AR035260A1 (es)
CA (1) CA2455861A1 (es)
MX (1) MXPA04001016A (es)
WO (1) WO2003013527A1 (es)

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CA2455861A1 (en) 2003-02-20
US20030216380A1 (en) 2003-11-20
EP1411944A1 (en) 2004-04-28
US7122675B2 (en) 2006-10-17
JP2005504042A (ja) 2005-02-10
US20060009467A1 (en) 2006-01-12
WO2003013527A1 (en) 2003-02-20
CN1780621A (zh) 2006-05-31

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