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AR067759A1 - Compuestos de pirazol utiles como moduladores de la enzima raf asociada al crecimiento celular anormal - Google Patents

Compuestos de pirazol utiles como moduladores de la enzima raf asociada al crecimiento celular anormal

Info

Publication number
AR067759A1
AR067759A1 ARP080103325A ARP080103325A AR067759A1 AR 067759 A1 AR067759 A1 AR 067759A1 AR P080103325 A ARP080103325 A AR P080103325A AR P080103325 A ARP080103325 A AR P080103325A AR 067759 A1 AR067759 A1 AR 067759A1
Authority
AR
Argentina
Prior art keywords
cycloalkyl
aryl
cycloheteroalkyl
heteroaryl
optionally substituted
Prior art date
Application number
ARP080103325A
Other languages
English (en)
Original Assignee
Pfizer
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=40122511&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR067759(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Pfizer filed Critical Pfizer
Publication of AR067759A1 publication Critical patent/AR067759A1/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
    • 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
    • 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
    • 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

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)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invencion se refiere a compuestos de formula (1), y a sales farmacéuticamente aceptables de los mismos, a su síntesis y a su uso como inhibidores de Raf. Reivindicacion 1: En otra realizacion, la presente es un compuesto de formula (1) en la que: X es N o CR7; R1 es H, alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, arilo C6-14, cicloheteroalquilo C2-9 o heteroarilo C2-9, donde cada uno de dichos alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, arilo C6-14, cicloheteroalquilo C2-9 y heteroarilo C2-9 está opcionalmente sustituido con uno o más R8; R2 es cicloheteroalquilo C2-9 o heteroarilo C2-9, donde cada uno de dichos cicloheteroalquilo C2-9 y heteroarilo C5-14 está opcionalmente sustituido con uno o más R8; u opcionalmente cuando R2 es heteroarilo C2-9, los átomos de hidrogeno sobre 2 átomos adyacentes cualquiera en el anillo pueden combinarse para formar un cicloalquilo de 5-7 miembros opcionalmente sustituido con uno o más R8, un cicloheteroalquilo de 5-7 miembros opcionalmente sustituido con uno o más R8 o un heteroarilo de 5-7 miembros opcionalmente sustituido con uno o más R8; R3 es H o -NR9R10, o cuando X es CR7, R3 puede combinarse con R7 para formar un heteroarilo de 5-7 miembros opcionalmente sustituido con uno o más R8, cicloheteroalquilo de 5-7 miembros opcionalmente sustituido con uno o más R8, fenilo opcionalmente sustituido con uno o más R8 o cicloalquilo de 5-7 miembros opcionalmente sustituido con uno o más R8; cada uno de R4, R5, R6, R7 es independientemente H, -NR11R12, -CN, -C(O)R11, -C(O)OR11, -NO2, -SR11, -S(O)2R11, -OR11, alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, arilo C6-14, cicloheteroalquilo C2-9 o heteroarilo C2-9 donde cada uno de dichos alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, arilo C6-14, cicloheteroalquilo C2-9 o heteroarilo C2-9 está opcionalmente sustituido con uno o más R8; cada R8 es independientemente -OR11, fluor, cloro, bromo, oxo, ciano, -NR13R14, -C(O)N(R13R14), -C(O)R13, -C(O)OR13, -NO2, alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, arilo C6-14, cicloheteroalquilo C2-9, heteroarilo C2-9 o -(CH2)nC(O)R11, donde cada uno de dichos cicloalquilo C3-8, arilo C6-14, cicloheteroalquilo C2-9 y heteroarilo C2-9 está opcionalmente sustituido con uno o más R11; cada uno de R9 y R10 es independientemente H, -C(O)N(R13R14), -C(O)R13, -C(O)OR13, alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, arilo C6-14, cicloheteroalquilo C2-9 o heteroarilo C2-9, donde cada uno de dichos alquilo C1-6, alquenilo C2-8, alquinilo C2-8, cicloalquilo C3-8, arilo C6-14, cicloheteroalquilo C2-9 y heteroarilo C2-9 está opcionalmente sustituido con al menos un R11; o R9 y R10 tomados junto con el nitrogeno al que están unidos se combinan para formar un anillo cicloheteroalquilo de 4-7 miembros opcionalmente sustituido con uno o más R11; cada R11 y R12 es independientemente fluor, cloro, bromo, -OH, C(O)OR13, -SR13, -S(O)2R13, -OR13, -NR13R14, -C(O)N(R13R14), ciano, alquilo C1-6, heteroalquilo C1-11, cicloalquilo C3-8, -O-cicloalquilo C3-8, -S-cicloalquilo C3-8, arilo C6-14, -O-arilo C6-14, -S-arilo C6-14, cicloheteroalquilo C2-9 y heteroarilo C2-9, donde cada uno de cicloalquilo C3-8, -O-cicloalquilo C3-8, -S-cicloalquilo C3-8, arilo C6-14, -O-arilo C6-14, -S-arilo C6-14, cicloheteroalquilo C2-9 y heteroarilo C2-9 está opcionalmente sustituido con uno o más R13; cada R13 y R14 es independientemente H, oxo, alquilo C1-6, heteroalquilo C1-11, cicloalquilo C3-8, -O-cicloalquilo C3-8, -S-cicloalquilo C3-8, arilo C6-14, -O-arilo C6-14, -S-arilo C6-14, cicloheteroalquilo C2-9 y heteroarilo C2-9, donde cada uno de cicloalquilo C3-8, -O-cicloalquilo C3-8, -S-cicloalquilo C3-8, arilo C6-14, -O-arilo C6-14, -S-arilo C6-14, cicloheteroalquilo C2-9 y heteroarilo C2-9 está opcionalmente sustituido con uno o más grupos seleccionados de fluor, cloro, bromo, -OH, ciano y alquilo C1-6; n es 0, 1, 2, 3 o 4; o una sal farmacéuticamente aceptable del mismo.
ARP080103325A 2007-08-01 2008-07-31 Compuestos de pirazol utiles como moduladores de la enzima raf asociada al crecimiento celular anormal AR067759A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US95323507P 2007-08-01 2007-08-01
US8005408P 2008-07-11 2008-07-11

Publications (1)

Publication Number Publication Date
AR067759A1 true AR067759A1 (es) 2009-10-21

Family

ID=40122511

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP080103325A AR067759A1 (es) 2007-08-01 2008-07-31 Compuestos de pirazol utiles como moduladores de la enzima raf asociada al crecimiento celular anormal

Country Status (24)

Country Link
US (1) US7772246B2 (es)
EP (1) EP2183243A2 (es)
JP (1) JP4792126B2 (es)
KR (1) KR20100038119A (es)
CN (1) CN101815712A (es)
AP (1) AP2010005167A0 (es)
AR (1) AR067759A1 (es)
AU (1) AU2008281543A1 (es)
BR (1) BRPI0815042A2 (es)
CA (1) CA2695114A1 (es)
CL (1) CL2008002255A1 (es)
CO (1) CO6251265A2 (es)
CR (1) CR11241A (es)
DO (1) DOP2010000047A (es)
EA (1) EA201000113A1 (es)
EC (1) ECSP109922A (es)
MA (1) MA31574B1 (es)
PA (1) PA8791801A1 (es)
PE (1) PE20090952A1 (es)
SV (1) SV2010003472A (es)
TN (1) TN2010000052A1 (es)
TW (1) TW200911243A (es)
UY (1) UY31260A1 (es)
WO (1) WO2009016460A2 (es)

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