AR080083A1 - Moduladores de gamma-secretasa - Google Patents

Moduladores de gamma-secretasa

Info

Publication number
AR080083A1
AR080083A1 ARP110100314A ARP110100314A AR080083A1 AR 080083 A1 AR080083 A1 AR 080083A1 AR P110100314 A ARP110100314 A AR P110100314A AR P110100314 A ARP110100314 A AR P110100314A AR 080083 A1 AR080083 A1 AR 080083A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
halogen
substituted
optionally substituted
alkyl
Prior art date
Application number
ARP110100314A
Other languages
English (en)
Inventor
Henner Knust
Luke Green
Anja Limberg
Thomas Luebbers
Andrew Thomas
Karlheinz Baumann
Erwin Goetschi
Synese Jolidons
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 AR080083A1 publication Critical patent/AR080083A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-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
    • C07D498/04—Ortho-condensed systems

Landscapes

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

Abstract

Se refiere a compuestos de la formula (1) en la que: R1/R1 con independencia entre si son hidrogeno, halogeno, alcoxi inferior o ciano; R2 es alquilo inferior, halogeno, alcoxi inferior, alquilo inferior sustituido por halogeno, alcoxi inferior sustituido por halogeno, alquilo inferior sustituido por OR, =0, -C(0)0alqui)o inferior, -C(0)NH-alquilo inferior, ciano, CH2-0-alquilo inferior, cicloalquilo, NRR' o es -O-(CH2)0-fenilo opcionalmente sustituido por halogeno, o es -(CH2)0-fenilo opcionalmente sustituido por uno, dos o tres sustituyentes elegidos entre halogeno, -(CH2)0-ciano, alquilo inferior, alquilo inferior sustituido por halogeno, alquilo inferior sustituido por hidroxi, C(O)H, -CH2-NH2-, -CH2-NH-C(O)0-alquilo inferior, -CH2-NH-C(O)-alquilo inferior, -CH2-NH-alquilo inferior, -CH2-NH-S(0)2-alquilo inferior, alcoxi inferior o por alcoxi inferior sustituido por halogeno, o es -(CH2)0-cicloalquilo, o es -(CH2)0-heterocicloalquilo que está opcionalmente sustituido por halogeno, CF3, alquilo inferior, -CH2CN, -C(O)-alquilo inferior, -C(0)0-alquilo inferior o S(O)2-alquilo inferior, o es heteroarilo elegido entre el grupo formado por furanilo, pirazinilo, piridinilo, benzooxazolilo o benzoimidazolilo, que están opcionalmente sustituidos por alquilo inferior, o es 4-metil-3,4-dihidro-2H-benzo[1 ,4]oxazina, R y R' con independencia entre si son hidrogeno o alquilo inferior, y O es el numero 0 o 1; R3 puede aparecer una o dos veces y es alquilo inferior; A es N NR a) b), c), d), Ne), h), R2 i) j) k) y R2 es hidrogeno, alquilo inferior, alquilo inferior sustituido por halogeno, C(O)-alquilo inferior, S(O)2-alquilo inferior o fenilo opcionalmente sustituido por halogeno; hetarilo es un grupo heteroarilo de 5 o 6 eslabones, que contiene N, S u O; n es el numero 0, 1, 2 o 3; si n es el numero 2 o 3, los R2 pueden ser iguales o no; o a las sales de adicion de ácido farmacéuticamente activas de los mismos. Los presentes compuestos de la formula 1 son moduladores del amiloide beta y por ello pueden ser utiles para el tratamiento o la prevencion de una enfermedad asociada con la deposicion del -amiloide en el cerebro, en particular de la enfermedad de Alzheimer, la angiopatía amiloide cerebral, la hemorragia cerebral hereditaria con amiloidosis de tipo Dutch (HCHWA-D), la demencia multiinfarto, la demencia pugilística o el síndrome de Down.
ARP110100314A 2010-02-01 2011-01-31 Moduladores de gamma-secretasa AR080083A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP10152211 2010-02-01

Publications (1)

Publication Number Publication Date
AR080083A1 true AR080083A1 (es) 2012-03-14

Family

ID=43638766

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP110100314A AR080083A1 (es) 2010-02-01 2011-01-31 Moduladores de gamma-secretasa

Country Status (11)

Country Link
US (1) US20110190269A1 (es)
EP (1) EP2531503A1 (es)
JP (1) JP2013518082A (es)
KR (1) KR20120120396A (es)
CN (1) CN102762561A (es)
AR (1) AR080083A1 (es)
CA (1) CA2780421A1 (es)
MX (1) MX2012006179A (es)
RU (1) RU2012136907A (es)
TW (1) TW201130837A (es)
WO (1) WO2011092272A1 (es)

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PT3008062T (pt) 2013-06-11 2017-06-07 Bayer Pharma AG Derivados de profármaco de triazolopiridinas substituídas
WO2017042114A1 (en) * 2015-09-09 2017-03-16 F. Hoffmann-La Roche Ag Bridged piperidine derivatives
WO2018001918A1 (en) * 2016-06-27 2018-01-04 F. Hoffmann-La Roche Ag Triazolopyridines as gamma-secretase modulators
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EP3523304B1 (en) * 2016-10-04 2021-01-27 H. Hoffnabb-La Roche Ag Bicyclic heteroaryl derivatives
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PE20211001A1 (es) 2018-02-27 2021-06-01 Incyte Corp Imidazopirimidinas y triazolopirimidinas como inhibidores de a2a / a2b
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Also Published As

Publication number Publication date
US20110190269A1 (en) 2011-08-04
KR20120120396A (ko) 2012-11-01
JP2013518082A (ja) 2013-05-20
EP2531503A1 (en) 2012-12-12
WO2011092272A1 (en) 2011-08-04
TW201130837A (en) 2011-09-16
CA2780421A1 (en) 2011-08-04
CN102762561A (zh) 2012-10-31
RU2012136907A (ru) 2014-03-10
MX2012006179A (es) 2012-06-19

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