AR054387A1 - Intermediarios utiles en la sintesis de moduladores de alquilquinolina y alquilquinazolina quinasa, y metodos de sintesis relacionados - Google Patents

Intermediarios utiles en la sintesis de moduladores de alquilquinolina y alquilquinazolina quinasa, y metodos de sintesis relacionados

Info

Publication number
AR054387A1
AR054387A1 ARP060102423A ARP060102423A AR054387A1 AR 054387 A1 AR054387 A1 AR 054387A1 AR P060102423 A ARP060102423 A AR P060102423A AR P060102423 A ARP060102423 A AR P060102423A AR 054387 A1 AR054387 A1 AR 054387A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
alkoxy
heteroaryl
halogen
Prior art date
Application number
ARP060102423A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
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 Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR054387A1 publication Critical patent/AR054387A1/es

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic 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
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/473Quinolines; Isoquinolines ortho- or peri-condensed with carbocyclic ring systems, e.g. acridines, phenanthridines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/02Heterocyclic 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
    • C07D401/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
    • C07D401/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Other In-Based Heterocyclic Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Los compuestos de la presente son utiles en la síntesis de los inhibidores de la proteína tirosinquinasa, particularmente los inhibidores de FLT3 y/o c-kit y/o TrkB. Reivindicacion 1: Un compuesto de formula (1) y N-oxidos y los isomeros estereoquímicos de éstos, donde X es N o CH; R1 y R2 están independientemente seleccionados de los restos de formulas (a-1) a (a-6) donde n es 1, 2, 3 o 4; Y es un enlace directo, O, S, NH, o N(alquilo); Ra es alcoxi, fenoxi, heteroarilo opcionalmente sustituido con R5, hidroxilo alquilamino, dialquilamino, oxazolidinonilo opcionalmente sustituido con R5, pirrolidinonilo opcionalmente sustituido con R5, piperidinonilo opcionalmente sustituido con R5, piperazinil-2-ona opcionalmente sustituido con R5, heterodionilo cíclico opcionalmente sustituido con R5, heterociclilo opcionalmente sustituido con R5, escuarilo opcionalmente sustituido con R5, -COORy, -CONRwRx, -N(Ry)CON(Rw)(Rx), -N(Rw)C(O)ORx, -N(Rw)CORy, -SRy, -SORy, -SO2Ry, - NRwSO2Ry, -NRwSO2Rx, -SO3Ry, -OSO2NRwRx, o -SO2NRwRx; Rw y Rx están independientemente seleccionados de: H, alquilo, alquenilo, aralquilo o heteroaralquilo, o Rw y Rx pueden estar tomados conjuntamente opcionalmente para formar un anillo de 5 a 7 miembros, que contiene opcionalmente una heteroporcion seleccionada de O, NH, N(alquilo), SO, SO2, o S; Ry está seleccionado de: H, alquilo, alquenilo, cicloalquilo, fenilo, aralquilo, heteroaralquilo, o heteroarilo, R5 es 1, 2 o 3 sustituyentes independientemente seleccionados de: halogeno, ciano, trifluormetilo, amino, hidroxilo, heteroarilo, alcoxi, -C(O)alquilo, -SO2alquilo, -C(O)NH(alquilo), -C(O)N(alquilo)2, -C(O)C(1-4)alquil-N(alquilo)2, alquilo, -C(1-4)alquilo-OH, -C(1-4)alquilo- OCH3, -C(O)C(1-4)alquilo-OH, -C(O)C(1-4)alquilo-OCH3, un grupo protector (donde dicho grupo protector es preferiblemente fluoren-9-il-metil-oxicarbonilo), dialquilamino, o alquilamino; con la condicion de que no esté presente el mismo sustituyente R5 más de una vez, a menos que dicho sustituyente R5 sea halogeno, hidroxilo, alcoxi, o alquilo; Rbb es H con la condicion de que ambos R1 y R2 no sean H, o Rbb es alcoxi con la condicion de que ambos R1 y R2 no sean alcoxi; o Rbb está seleccionado del grupo que consiste en: halogeno, dialquilamino, fenilo, heteroarilo, piperazinil-2-ona opcionalmente sustituido con R6, imidazolidinil-2-ona opcionalmente sustituido con R6, oxazolidinil-2-ona opcionalmente sustituido con R6, o heterociclilo opcionalmente sustituido con R6; R6 es 1, 2 o 3 sustituyentes independientemente seleccionados de: halogeno, ciano, trifluormetilo, amino, hidroxilo heteroarilo,.alcoxi, -C(O)alquilo, -SO2alquilo, -C(O)NH(alquilo), -C(O)N(alquilo)2, -C(O)C(1- 4)alquil-N(alquilo)2, alquilo, -C(1-4)alquilo-OH, -C(1-4)alquilo-OCH3, -C(O)C(1-4)alquilo-OH, -C(O)C(1-4)alquilo-OCH3, dialquilamino, o alquilamino; con la condicion de que el mismo sustituyente R6 no esté presente más de una vez, a menos que dicho sustituyente R6 sea halogeno, hidroxilo, alcoxi, o alquilo; Rc es heterociclilo opcionalmente sustituido con R7, o heteroarilo; y R7 es 1, 2 o 3 sustituyentes independientemente seleccionados de: halogeno, ciano, trifluormetilo, amino, hidroxilo, heteroarilo, alcoxi, -C(O)alquilo, -SO2alquilo, -C(O)NH(alquilo), -C(O)N(alquilo)2, -C(O)C(1-4)alquil-N(alquilo)2, alquilo, -C(1-4)alquilo-OH, -C(1-4)alquilo-OCH3, -C(O)C(1-4)alquilo-OH, -C(O)C(1-4)alquilo-OCH3, dialquilamino, o alquilamino; con la condicion de que el mismo sustituyente R7 no esté presente más de una vez, a menos que dicho sustituyente R7 sea halogeno, hidroxilo, alcoxi, o alquilo; y R99 es H, o un grupo protector.
ARP060102423A 2005-06-10 2006-06-09 Intermediarios utiles en la sintesis de moduladores de alquilquinolina y alquilquinazolina quinasa, y metodos de sintesis relacionados AR054387A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US68938405P 2005-06-10 2005-06-10
US73091905P 2005-10-27 2005-10-27
US78955106P 2006-04-05 2006-04-05

Publications (1)

Publication Number Publication Date
AR054387A1 true AR054387A1 (es) 2007-06-20

Family

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Family Applications (1)

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ARP060102423A AR054387A1 (es) 2005-06-10 2006-06-09 Intermediarios utiles en la sintesis de moduladores de alquilquinolina y alquilquinazolina quinasa, y metodos de sintesis relacionados

Country Status (20)

Country Link
US (1) US7825244B2 (es)
EP (1) EP1891040A1 (es)
JP (1) JP2008545787A (es)
KR (1) KR20080033234A (es)
AR (1) AR054387A1 (es)
AU (1) AU2006258056A1 (es)
BR (1) BRPI0612543A2 (es)
CA (1) CA2611219A1 (es)
CR (1) CR9651A (es)
EA (1) EA200800010A1 (es)
EC (1) ECSP077993A (es)
GT (1) GT200600250A (es)
IL (1) IL187688A0 (es)
MX (1) MX2007015739A (es)
NI (1) NI200700312A (es)
NO (1) NO20080160L (es)
PA (1) PA8679201A1 (es)
TW (1) TW200718694A (es)
UY (1) UY29589A1 (es)
WO (1) WO2006135646A1 (es)

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WO2016057931A1 (en) 2014-10-10 2016-04-14 The Research Foundation For The State University Of New York Trifluoromethoxylation of arenes via intramolecular trifluoromethoxy group migration

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Also Published As

Publication number Publication date
WO2006135646A1 (en) 2006-12-21
CA2611219A1 (en) 2006-12-21
IL187688A0 (en) 2008-08-07
NI200700312A (es) 2009-02-19
NO20080160L (no) 2008-01-09
US7825244B2 (en) 2010-11-02
KR20080033234A (ko) 2008-04-16
AU2006258056A1 (en) 2006-12-21
US20070021436A1 (en) 2007-01-25
EP1891040A1 (en) 2008-02-27
JP2008545787A (ja) 2008-12-18
PA8679201A1 (es) 2007-01-17
ECSP077993A (es) 2008-01-23
EA200800010A1 (ru) 2008-06-30
CR9651A (es) 2008-09-09
BRPI0612543A2 (pt) 2010-11-23
UY29589A1 (es) 2006-10-02
TW200718694A (en) 2007-05-16
MX2007015739A (es) 2008-04-29
GT200600250A (es) 2007-03-14

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