AR070535A1 - Compuestos inhibidores de raf y metodos para usarlos - Google Patents

Compuestos inhibidores de raf y metodos para usarlos

Info

Publication number
AR070535A1
AR070535A1 ARP090100689A ARP090100689A AR070535A1 AR 070535 A1 AR070535 A1 AR 070535A1 AR P090100689 A ARP090100689 A AR P090100689A AR P090100689 A ARP090100689 A AR P090100689A AR 070535 A1 AR070535 A1 AR 070535A1
Authority
AR
Argentina
Prior art keywords
alkyl
optionally substituted
halogen
hydrogen
cycloalkyl
Prior art date
Application number
ARP090100689A
Other languages
English (en)
Original Assignee
Array Biopharma Inc
Genentech Inc
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 Array Biopharma Inc, Genentech Inc filed Critical Array Biopharma Inc
Publication of AR070535A1 publication Critical patent/AR070535A1/es

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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
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00—Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/01—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms
    • C07C311/02—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton
    • C07C311/08—Sulfonamides having sulfur atoms of sulfonamide groups bound to acyclic carbon atoms of an acyclic saturated carbon skeleton having the nitrogen atom of at least one of the sulfonamide groups bound to a carbon atom of a six-membered aromatic ring

Landscapes

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

Abstract

Los compuestos de formula (1) son utiles para la inhibicion de las Raf quinasas. Se proporcionan métodos para usar los compuestos de formula (1) y sus estereoisomeros, tautomeros, prodrogas y sales aceptables para uso farmacéutico, para el diagnostico, la prevencion o el tratamiento in vitro, in situ, e in vivo, de trastornos en células de mamíferos, o afecciones asociadas de orden patologico. Intermediarios y proceso de preparacion. Reivindicacion 1: Un compuesto seleccionado de la formula (1), y sus estereoisomeros, tautomeros, prodrogas y sales aceptables para uso farmacéutico, en donde: R1 y R2 se seleccionan de manera independiente entre hidrogeno, halogeno, CN, alquilo C1-3 y alcoxi C1-3; R3 es hidrogeno, halogeno o alquilo C1-3; R4 es cicloalquilo C3-5, alquilo C1-6, alquenilo C2-6, o alquinilo C2-6, fenilo, un heteroarilo de 5-6 miembros, o NRnRo, en donde el cicloalquilo, alquilo, alquenilo, alquinilo, fenilo y heteroarilo están opcionalmente sustituidos con ORg, halogeno, fenilo, cicloalquilo C3-4, o alquilo C1-4 opcionalmente sustituido con halogeno; R5 es hidrogeno; halogeno; CN; NRkRI; alquilo C1-6 opcionalmente sustituido con halogeno, oxo, ORg o NRgRh; alquenilo C2-6 opcionalmente sustituido con halogeno, ORg o NRgRh; alquinilo C2-6 opcionalmente sustituido con halogeno, ORg o NRgRh; un cicloalquilo C3-6 saturado o parcialmente insaturado opcionalmente sustituido con halogeno o alquilo C1-4; un heterociclilo de 4 a 6 miembros saturado o parcialmente insaturado opcionalmente sustituido con alquilo C1-4; un heteroarilo de 5-6 miembros opcionalmente sustituido con Rc; un heterociclilo bicíclico de 9-10 miembros opcionalmente sustituido con alquilo C1-4; un heteroarilo bicíclico de 9-10 miembros opcionalmente sustituido con alquilo C1-4; o fenilo opcionalmente sustituido con Rd; R6 es hidrogeno; halogeno; CN; NRkRI; ORm; un cicloalquilo C3-6 saturado o parcialmente insaturado opcionalmente sustituido con halogeno o alquilo C1-4; un heterociclilo de 4 a 6 miembros saturado o parcialmente insaturado opcionalmente sustituido con alquilo C1-4; fenilo opcionalmente sustituido con uno a tres grupos Ra; un heteroarilo de 5-6 miembros opcionalmente sustituido con alquilo C1-4 o bencilo; alquenilo C2-6 opcionalmente sustituido con halogeno, ORg o NRgRh; alquinilo C2-6 opcionalmente sustituido con halogeno, ORg o NRgRh; o alquilo C1-6 opcionalmente sustituido con uno a tres grupos Rb; cada Ra se selecciona de manera independiente entre halogeno, CN, CF3, OH, -O-alquilo C1-4, un heterociclilo de 5-6 miembros, o alquilo C1-4 opcionalmente sustituido con NRgRh o un heterociclilo de 5-6 miembros; cada Rb se selecciona de manera independiente entre halogeno, OH, OCH3, oxo, -NReRf, fenilo opcionalmente sustituido con un halogeno, cicloalquilo C3-6, o un heterociclilo de 5-6 miembros opcionalmente sustituido con halogeno; Rc es NRhRj, alquilo C1-4, o un heterociclilo de 5-6 miembros opcionalmente sustituido con alquilo C1-4 o -(CH2)p-cicloalquilo C3-6; Rd es halogeno, CN, NRgRh, fenilo, un heterociclilo de 5-6 miembros, -O-alquilo C1-4 o alquilo C1-4, en donde el alquilo o alcoxi están opcionalmente sustituido con halogeno, OH, oxo, -O-alquilo C1-3, NRgRh, o un heterociclilo de 5-6 miembros opcionalmente sustituido con alquilo C1-3; Re y Rf se seleccionan de manera independiente entre hidrogeno, alquilo C1-4 o fenilo; cada Rg y Rh se seleccionan de manera independiente entre hidrogeno o alquilo C1-4; Rj es hidrogeno o alquilo C1-4 opcionalmente sustituido con un heterociclilo de 5-6 miembros; cada Rk y Rl se seleccionan de manera independiente de hidrogeno o alquilo C1-4; Rm se selecciona de hidrogeno o alquilo C1-4; Rn y Ro se seleccionan de manera independiente entre hidrogeno y alquilo C1-5, o Rn y Ro junto con el nitrogeno al cual están unidos forman un anillo heterocíclico de 4 a 6 miembros; y p es 0 o 1. Reivindicacion 66: Un compuesto seleccionado de la formula (2), donde R1 y R2 se seleccionan de manera independiente entre hidrogeno, halogeno, CN, alquilo C1-3 y alcoxi C1-3; R3 es hidrogeno, halogeno o alquilo C1-3; R4 es cicloalquilo C3-5, alquilo C1-6, alquenilo C2-6, o alquinilo C2-6, en donde el cicloalquilo, alquilo, alquenilo y alquinilo están opcionalmente sustituidos con ORg, halogeno o cicloalquilo C3-4; R20 es hidrogeno, alquilo C1-6, bencilo o fenilo; y Rg es hidrogeno o alquilo C1-4.
ARP090100689A 2008-02-29 2009-02-27 Compuestos inhibidores de raf y metodos para usarlos AR070535A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US3283908P 2008-02-29 2008-02-29

Publications (1)

Publication Number Publication Date
AR070535A1 true AR070535A1 (es) 2010-04-14

Family

ID=40935896

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP090100689A AR070535A1 (es) 2008-02-29 2009-02-27 Compuestos inhibidores de raf y metodos para usarlos

Country Status (16)

Country Link
US (1) US8338452B2 (es)
EP (1) EP2265608A2 (es)
JP (1) JP2011513330A (es)
KR (1) KR20100122505A (es)
CN (1) CN102015707A (es)
AR (1) AR070535A1 (es)
AU (1) AU2009222143A1 (es)
CA (1) CA2716951A1 (es)
CL (1) CL2009000447A1 (es)
EC (1) ECSP10010510A (es)
IL (1) IL207843A0 (es)
MA (1) MA32271B1 (es)
MX (1) MX2010009410A (es)
PE (1) PE20091561A1 (es)
TW (1) TW200940540A (es)
WO (1) WO2009111278A2 (es)

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US8338452B2 (en) 2012-12-25
TW200940540A (en) 2009-10-01
ECSP10010510A (es) 2010-10-30
IL207843A0 (en) 2010-12-30
MA32271B1 (fr) 2011-05-02
CA2716951A1 (en) 2009-09-11
CN102015707A (zh) 2011-04-13
PE20091561A1 (es) 2009-10-30
CL2009000447A1 (es) 2010-01-04
AU2009222143A1 (en) 2009-09-11
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MX2010009410A (es) 2010-11-30
JP2011513330A (ja) 2011-04-28

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