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AR070437A1 - Moduladores de beta - amiloide - Google Patents

Moduladores de beta - amiloide

Info

Publication number
AR070437A1
AR070437A1 ARP090100572A ARP090100572A AR070437A1 AR 070437 A1 AR070437 A1 AR 070437A1 AR P090100572 A ARP090100572 A AR P090100572A AR P090100572 A ARP090100572 A AR P090100572A AR 070437 A1 AR070437 A1 AR 070437A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
hydroxy
optionally substituted
substituted
hydrogen
Prior art date
Application number
ARP090100572A
Other languages
English (en)
Inventor
Karlheinz Baumann
Alexander Flohr
Synese Jolidon
Erwin Goetschi
Helmut Jacobsen
Thomas Luebbers
Original Assignee
Hoffmann La Roche
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 Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR070437A1 publication Critical patent/AR070437A1/es

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    • 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
    • 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
    • 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
    • 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
    • C07D401/14—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 three or more hetero rings
    • 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
    • C07D403/14—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 three or more hetero rings
    • 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
    • C07D405/14—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 three or more hetero rings
    • 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
    • C07D409/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Landscapes

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

Abstract

Se ha encontrado que los compuestos presentes de la formula (1) son moduladores de b-amiloide y por ello, pueden ser utiles para el tratamiento o la prevencion de una enfermedad asociada con la deposicion del b-amiloide en cerebro, en particular la enfermedad de Alzheimer y otras enfermedades como son la angiopatía cerebral amiloide, la hemorragia cerebral hereditaria con amiloidosis de tipo Dutch (HCHWA-D), la demencia multi-infarto, la demencia pugilística y el síndrome de Down. Reivindicacion 1: Un compuesto de formula general (1) en la que R1 es hidrogeno, alquilo inferior o alquilo inferior sustituido por hidroxi; R2 es hidrogeno, alcoxi inferior, alquilo inferior, ciano o halogeno; R3 es alquilo inferior, alquenilo inferior, alquilo inferior sustituido por fluor, (CH2)2O-alquilo inferior, (CH2)2NR82, o es 4H-benzo[1,4]oxazin-3-ona, cicloalquilo opcionalmente sustituido por hidroxi, o es heterociclo alquilo, dicho heterocicloalquilo está opcionalmente sustituido por hidroxi o S(O)2-alquilo inferior, o es (CH2)0,1-arilo o es un grupo heteroarilo de cinco o seis eslabones, dichos anillos están opcionalmente sustituidos por uno o más R' para cualquier definicion de L, o es halogeno, hidroxi, -C(O)O-alquilo inferior, OC(O)-alquilo inferior o C(O)NH2 para el caso en el que L sea un enlace, o es alcoxi inferior, hidroxi, -C(O)O-alquilo inferior, OC(O)-alquilo inferior o C(O)NH2 para el caso en el que L sea -CR6R7-, o es CH2-C(O)O-alquilo inferior para el caso en el que L sea NR8, o es alcoxi inferior, hidroxi o NR82 para el caso en el que L sea C(O); R' es halogeno, alquilo inferior, alcoxi inferior, ciano, alquilo inferior sustituido por fluor, alcoxi inferior sustituido por fluor, SF5, o es un grupo heteroarilo de cinco eslabones, que puede estar opcionalmente sustituido por alquilo inferior; Ar es un grupo heteroarilo de cinco eslabones o es piridinilo; Z es CH o N; X-Y es N-CR4=CR5, CH-CR4=N, CH-CR4=CR5 o N-NH; y en los que R4 y R5 junto con los átomos de carbono correspondientes a los que están unidos pueden formar un anillo adicional con -(CH2)3,4, y con la condicion de que si X-Y es CH-CR4=CR5 o CH-CR4=N, entonces Z sea N; R4, R5 con independencia entre sí son hidrogeno, halogeno, alquilo inferior, alcoxi inferior, C(O)O-alquilo inferior, alquilo inferior sustituido por uno o más grupos elegidos entre fluor, hidroxi, ciano o cicloalquilo, o son ciano, fenilo, bencilo o un grupo heteroarilo de cinco o seis eslabones, dichos anillos están opcionalmente sustituidos por uno o más R', o son cicloalquilo o heterocicloalquilo, que están opcionalmente sustituidos por alquilo inferior y hidroxi, y con la condicion de que R4 pueda ser hidroxi o NR82; L es un enlace, -CR6R7-, -O-, -NR8- o -C(O)-; R6, R7 con independencia entre sí son hidrogeno, alquilo inferior, cicloalquilo, fenilo o R6 y R7 junto con el átomo de carbono al que están unidos forman un grupo cicloalquilo C3-6, y con la condicion de que R6 pueda ser también hidroxi o alcoxi inferior; R8 es hidrogeno o alquilo inferior; o una sal de adicion de ácido farmacéuticamente activa del mismo.
ARP090100572A 2008-02-22 2009-02-19 Moduladores de beta - amiloide AR070437A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP08151825 2008-02-22

Publications (1)

Publication Number Publication Date
AR070437A1 true AR070437A1 (es) 2010-04-07

Family

ID=40481869

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090100572A AR070437A1 (es) 2008-02-22 2009-02-19 Moduladores de beta - amiloide

Country Status (18)

Country Link
US (2) US20090215759A1 (es)
EP (1) EP2257541B1 (es)
JP (1) JP5328816B2 (es)
KR (1) KR101247840B1 (es)
CN (1) CN101952275B (es)
AR (1) AR070437A1 (es)
AU (1) AU2009216851B2 (es)
BR (1) BRPI0907577A2 (es)
CA (1) CA2713716A1 (es)
CL (1) CL2009000380A1 (es)
ES (1) ES2428716T3 (es)
IL (1) IL206945A (es)
MX (1) MX2010008700A (es)
PE (1) PE20091472A1 (es)
RU (1) RU2010137300A (es)
TW (1) TW200938535A (es)
WO (1) WO2009103652A1 (es)
ZA (1) ZA201005399B (es)

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